Term
|
Definition
Direct cholinomimetic
activate bowels/bladder post surg
Cholinesterase resistant |
|
|
Term
|
Definition
Direct cholinomimetic (= ACh)
Glaucoma
Cholinesterase sensitive!
(only one besides ACh) |
|
|
Term
|
Definition
Direct cholinomimetic
Glaucoma
Stimulates sweat, saliva, tears (PILE on the fluids)
Cholinesterase resistant |
|
|
Term
|
Definition
Direct cholinomimetic
Challenge test for asthma
Cholinesterase resistant |
|
|
Term
|
Definition
Anticholinesterase
Postop/neurogenic ileus, myasthenia gravis, NMJ block reversal
No CNS penetration |
|
|
Term
|
Definition
Anticholinesterase
Myasthenia gravis, long acting
No CNS penetration |
|
|
Term
|
Definition
Anticholinesterase
Myasthenia gravis Dx, very short acting |
|
|
Term
|
Definition
Acetylcholinesterase inhibitor
Glaucoma, atropine overdose CNS entry
(phys for eyes - the one with CSF entry) |
|
|
Term
|
Definition
Anticholinesterase
Glaucoma |
|
|
Term
Parathion
Mech?
Use?
Antidote? |
|
Definition
| Irreversible AChE inhibitor (organophosphate) pesticide, toxin Antidote: atropine + pralidoxime |
|
|
Term
|
Definition
Irreversible AChE inhibitor (organophosphate)
pesticide, toxin
Antidote: atropine + pralidoxime |
|
|
Term
|
Definition
Muscarinic antagonist
causes mydriasis, cycloplegia |
|
|
Term
|
Definition
Muscarinic antagonist (= atropine)
causes mydriasis, cycloplegia |
|
|
Term
|
Definition
Muscarinic antagonist (= atropine) causes mydriasis, cycloplegia
"trop"icamide, a"trop"ine |
|
|
Term
|
Definition
Muscarinic antagonist
*Parkinson's disease |
|
|
Term
|
Definition
Muscarinic antagonist
motion sickness (patch) |
|
|
Term
|
Definition
Muscarinic antagonist
Asthma, COPD |
|
|
Term
|
Definition
Muscarinic antagonist
Reduce urgency, bladder spasm |
|
|
Term
|
Definition
Muscarinic antagonist
Reduce urgency, bladder spasm |
|
|
Term
|
Definition
Muscarinic antagonist
Peptic ulcers |
|
|
Term
|
Definition
Muscarinic antagonist
peptic ulcers |
|
|
Term
|
Definition
Nicotinic antagonist
ganglionic blocker - prevents vagal reflexes
causes orthostatic hypotension, blurred vision, constipation |
|
|
Term
|
Definition
Direct sympathomimetic
a1, a2, b1, b2 - low doses ~b1 selective
anaphylaxis, open angle glaucoma, asthma, hypoTN |
|
|
Term
|
Definition
Direct sypathomimetic
a1, a2, ~b1
hypoTN
causes decreased renal perfusion (less renin effect) |
|
|
Term
|
Definition
Direct sympathomimetic
b1, b2
AV block (rarely used) |
|
|
Term
|
Definition
Direct sympathomimetic
D1, D2, > b, > a, inotropic and chronotropic
increases renal perfusion, shock, CHF |
|
|
Term
|
Definition
Direct sympathomimetic
b1 > b2, inotropic (NOT chronotropic)
CHF, cardiac stress test |
|
|
Term
|
Definition
Direct sympathomimetic
a1 > a2
pupillary dilation, vasoconstriction, nasal decongestion |
|
|
Term
|
Definition
Direct sympathomimetic
b2 selective (~b1)
Acute asthma |
|
|
Term
|
Definition
Direct sympathomimetic
b2 selective (~b1)
acute asthma |
|
|
Term
|
Definition
Direct sympathomimetic b2 selective (~b1) long-term asthma tx
MAST
metaproterenol, albuterol, salmeterol, terbutline |
|
|
Term
|
Definition
Direct sympathomimetic b2 selective (~some b1) tocolytic
("but" like al"but"erol) |
|
|
Term
|
Definition
Direct sympathomimetic b2 selective (~b1)
tocolytic
(rito-DREAM, back to sleep for baby) |
|
|
Term
|
Definition
Indirect sympathetic agonist, releases stored catecholamines
Narcolepsy, obesity, ADD |
|
|
Term
|
Definition
Indirect sympathetic agonist, releases stored catecholamines
Nasal decongestion, urinary incontinence, hypotension |
|
|
Term
|
Definition
Indirect sympathetic agonist, uptake inhibitor
Vasoconstriction & local anesthesia |
|
|
Term
|
Definition
Indirect sympathetic antagonist
a2 agonist -> low central adrenergic outflow
Hypertension, especially with renal disease (no decrease in renal blood flow) |
|
|
Term
alpha-Methyldopa
Mech?
Use? |
|
Definition
Indirect sympathetic antagonist
a2 agonist -> low central adrenergic outflow
Hypertension, especially with renal disease (no decrease in renal blood flow) |
|
|
Term
Phenoxybenzamine
Mech?
Use? |
|
Definition
non-selective alpha-blocker, irreversible
pheochromocytomas |
|
|
Term
|
Definition
non-selective alpha-blocker, reversible
pheochromocytoma |
|
|
Term
|
Definition
alpha-1 selective blocker
HTN, urinary retention in BPH |
|
|
Term
|
Definition
alpha-1 selective blocker
HTN, urinary retention in BPH |
|
|
Term
|
Definition
alpha-1 selective blocker
HTN, urinary retention in BPH |
|
|
Term
|
Definition
alpha-2 selective alpha-blocker
Depression (TCA) |
|
|
Term
"-olols"
Mech?
Use?
Toxicity |
|
Definition
Beta-blockers
HTN (reduce CO, reduce renin secretion), Angina, MI, SVT (reduce AV conduction velocity), CHF, Glaucoma
Asthma/COPD exacerbation, bardycardia/AV block, impotence, sleep effects, decreased insulin release (caution in DM) |
|
|
Term
| Propranolol, timolol, nadolol, pindolol |
|
Definition
| Non-selective beta blockers |
|
|
Term
| acebutalol, betaxolol, esmolol, atenolol, metoprolol |
|
Definition
beta-1 selective beta blockers (good for comorbid asthma/COPD)
A BEAM of beta-1 selective blockers
ace-but = 1-b |
|
|
Term
|
Definition
| non-selective alpha- and beta-blockers |
|
|
Term
|
Definition
|
|
Term
|
Definition
Selective alpha-1 blocker
HTN, urinary retention in BPH |
|
|
Term
|
Definition
inhibits alcohol dehydrogenase
methanol or ethylene glycol poisoning |
|
|
Term
|
Definition
(Antabuse)
inhibits acetaldehyde dehydrogenase, increases hangover sx |
|
|
Term
|
Definition
increase cGMP, vasodilates arteries > veins, afterload reduction
Severe HTN, CHF. With methyldopa for HTN in pregnancy. With b-blocker to prevent reflex tachycardia.
Compensatory tachycardia, fluid retention (reflex renin release), nausea, headache, angina. Drug-induced lupus. |
|
|
Term
|
Definition
Peripheral edema, flushing, dizziness, constipation
*"Nifedipine is similar to Nitrates in effect" |
|
|
Term
|
Definition
Non-dihydropyridine CCN
block voltage-dependent Ca channels on cardiac and smooth muscle
Non-DHPs: heart > vascular effect
HTN, angina, arrhythmias, Prinzmetal angina, Raynauds
Constipation, gingival hyperplasia. Cardiac depression, AV block, peripheral edema, flushing, dizziness. |
|
|
Term
|
Definition
Non-dihydropyridine CCN
block voltage-dependent Ca channels on cardiac and smooth muscle
Non-DHPs: heart > vascular effect
HTN, angina, arrhythmias, Prinzmetal angina, Raynauds
Cardiac depression, AV block, peripheral edema, flushing, dizziness, constipation |
|
|
Term
Nitroglycerin
Mech?
Use?
Tox? |
|
Definition
NO release, increase cGMP, smooth muscle dilation
Veins >> arteries, decrease preload
Angina, pulmonary edema, erection enhancer
Reflex tachycardia, hypotension, flushing, headache, "Monday disease" in industrial exposure |
|
|
Term
Isosorbide dinitrate
Mech?
Use?
Tox? |
|
Definition
NO release, increase cGMP, smooth muscle dilation
Veins >> arteries, decrease preload
Angina, pulmonary edema, erection enhancer
Reflex tachycardia, hypotension, flushing, headache, "Monday disease" in industrial exposure.
*NB: isorboside mononitrate is active metabolite, has 100% bioavail - dinitrate is hepatic glucoronidated. |
|
|
Term
Nitroprusside
Mech?
Use?
Tox?
Antidote? |
|
Definition
NO release, increase cGMP, smooth muscle dilation
Short acting, for malignant HTN
cyanide toxicity - thiosulfate to bind CN |
|
|
Term
|
Definition
D1 receptor agonist, relaxes renal smooth muscle.
Only agent that improves renal perfusion as it lowers blood pressure.
malignant hypertension |
|
|
Term
|
Definition
K+ channel opener - hyperpolarizes then relaxes smooth muscle.
Malignant hypertension.
Hyperglycemia (prevents insulin release) |
|
|
Term
|
Definition
HMG-CoA reductase inhibition, lower mavalonate. Compensatory increase in LDL uptake to make bile.
Lowers LDL, triglycerides, slight raise in HDL
Hepatotoxicity, rhabdomyolysis |
|
|
Term
|
Definition
Inhibits lipolysis in adipose tissue, reduces liver VLDL secretion
raises HDL, lowers LDL, lowers triglycerides.
*Also has vasodilatory effects
Flushing (block with ASA), hyperglycemia, hyperuricemia |
|
|
Term
Cholestyramine, Colestipol, Colesevelam
Mech?
Use?
Tox? |
|
Definition
Bile acid resins, prevent reabsorption of bile acids, liver uses cholesterol to make more.
Lowers LDL, slight HDL increase, slight triglyceride increase
Tastes bad, GI discomfort, fat-soluble vitamin def., cholesterol gallstones |
|
|
Term
|
Definition
Prevent cholesterol reabsorption at brush border
Lowers LDL
Rare hepatotoxicity |
|
|
Term
Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate
Mech?
Use?
Tox? |
|
Definition
Fibrates; upregulate LPL, increase TG clearance
large triglyceride reduction, lower LDL, raise HDL
Myositis, hepatotoxic, *cholesterol gallstones. |
|
|
Term
Digoxin
Mech?
Use?
Tox?
Antidote? |
|
Definition
Direct inhibition of Na/K ATPase, indirect increase in Ca, positive inotropy. Stimulates vagus nerve, decreases AV conductivity, SA node activity.
CHF, atrial fibrillation.
Cholinergic: N/V, diarrhea, blurry yellow vision. ECG: increased PR, decreased QT, T-wave inversion, ventricular tachyarrythmia, hyperkalemia. Worse with renal failure (excretion), hypokalemia (competes for binding), quinidine (protein binding displacement).
Slowly normalize K+, lidocaine, anti-dig Fab, Mg++ |
|
|
Term
|
Definition
Class IA antiarrhythmic: Na channel blocker.
Decrease slope of depolarization, prolong cardiac action potential duration (prolong QRS), prolong QT interval.
Atrial and ventricular arrhythmias, esp. SVT, reentrant, V-tach.
Cinchonism, thrombocytopenia, torsades de pointes. Increased toxicity with hyperkalemia. |
|
|
Term
Procainamide
Mech?
Use?
Tox? |
|
Definition
Class IA antiarrhythmic: Na channel blocker.
Decrease slope of depolarization (prolong QRS), prolong cardiac action potential duration, prolong QT interval.
Atrial and ventricular arrhythmias, esp. SVT, reentrant, V-tach.
Drug-induced lupus, thrombocytopenia, torsades de pointes. Increased toxicity with hyperkalemia. |
|
|
Term
Disopyramide
Mech?
Use?
Tox? |
|
Definition
Class IA antiarrhythmic: Na channel blocker.
Decrease slope of depolarization (prolong QRS), prolong cardiac action potential duration, prolong QT interval.
Atrial and ventricular arrhythmias, esp. SVT, reentrant, V-tach.
Thrombocytopenia, torsades de pointes. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IB antiarrhythmic: Na channel blocker
Decrease slope of depolarization (prolong QRS), shorten cardiac action potential. Preferentially affect ischemic or depolarized tissue.
Acute ventricular arrythmias (MI), digitalis-induced arrhytmias.
Local anesthetic, CNS stimlation/depression, CV depression. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IB antiarrhythmic: Na channel blocker
Decrease slope of depolarization (prolongs QRS), shorten cardiac action potential. Preferentially affect ischemic or depolarized tissue.
Acute ventricular arrythmias (MI), digitalis-induced arrhytmias.
Local anesthetic, CNS stimlation/depression, CV depression. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IB antiarrhythmic: Na channel blocker
Decrease slope of depolarization (prolongs QRS), shorten cardiac action potential. Preferentially affect ischemic or depolarized tissue.
Acute ventricular arrythmias (MI), digitalis-induced arrhytmias.
Local anesthetic, CNS stimlation/depression, CV depression. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IC antiarrythmic: Na channel blocker.
Decrease slope of depolarization (prolongs QRS), no effect on cardiac action potential length.
V-fib, intractable SVT. Last resort. CI: structural abnormalities (post-MI)
Proarrythmic, esp. post-MI. AV node block. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IC antiarrythmic: Na channel blocker.
Decrease slope of depolarization (prolongs QRS), no effect on cardiac action potential length.
V-fib, intractable SVT. Last resort. CI: structural abnormalities (post-MI)
Proarrythmic, esp. post-MI. AV node block. Increased toxicity with hyperkalemia. |
|
|
Term
|
Definition
Class IC antiarrythmic: Na channel blocker.
Decrease slope of depolarization (prolong QRS), no effect on cardiac action potential length.
V-fib, intractable SVT. Last resort. CI: structural abnormalities (post-MI)
Proarrythmic, esp. post-MI. AV node block. Increased toxicity with hyperkalemia. |
|
|
Term
Class II anti-arrhythmics
Mech?
Use?
Tox?
Antidote? |
|
Definition
= beta-blockers
lower cAMP, lower Ca currents. Slower automaticity. Prolonged PR interval (AV node block).
V-tach, SVT, atrial fibrillation and flutter.
Asthma/COPD CI, CNS effects. Can decrease insulin release and mask effects of hypoglycemia.
Glucagon. |
|
|
Term
|
Definition
B-SAID block K!
Class III antiarrhythmics: K channel blockers
Prolong action potential duration, prolong QT interval.
Last resort!
New arrhythmias, hypotension |
|
|
Term
|
Definition
B-SAID block K!
Class III antiarrhythmics: K channel blockers
(sotalol: beta-block and K channel block)
Prolong action potential duration, prolong QT interval.
Last resort!
torsades de pointes, beta-block toxicity |
|
|
Term
|
Definition
B-SAID block K!
Class III antiarrhythmics: K channel blockers
Prolong action potential duration, prolong QT interval. Amiodarone effects lipid membrane, numerous effects.
Last resort!
**Pulmonary fibrosis, hepatotoxicity, hypo/hyperthyroidism (PFTs/LFTs/TFTs). Corneal deposits, blue/grey skin discoloration, photosensitivity, neurologic effects, constipation, CV depression. |
|
|
Term
|
Definition
B-SAID block K!
Class III antiarrhythmics: K channel blockers
Prolong action potential duration, prolong QT interval.
Last resort!
Torsades de pointes |
|
|
Term
|
Definition
B-SAID block K!
Class III antiarrhythmics: K channel blockers
Prolong action potential duration, prolong QT interval.
Last resort!
Torsades de pointes |
|
|
Term
Class IV anti-arrhythmics
Mech?
Use?
Tox? |
|
Definition
= Non-DHP CCBs: Verapamil, Diltiazem
Decrease conduction velocity, increase PR interval.
SVT, nodal arrythmias
Constipation, flushing, edema, CV depression |
|
|
Term
Adenosine
Mech?
Use?
Tox?
Antidote? |
|
Definition
Inhibit adenylyl cyclase, hyperpolarize cells.
Will abolish AV node re-entrant SVTs, use for Dx.
Flushing, hypoTN, chest pain.
Block with theophylline. |
|
|
Term
|
Definition
Adenosine deaminase inhibitor
allows for accumulation of adenosine, same effects and uses. |
|
|
Term
|
Definition
dihydropyridine CCB (-dipines)
block voltage gated Ca channels
DHPs: vascular > cardiac
HTN, Prinzmetal's angina, Raynauds. Not for typical angina, arrythmias - not cardioselective, reflex tachycardia.
Peripheral edema, flushing, dizziness, constipation. |
|
|
Term
|
Definition
Phosphodiesterase inhibitor
Increases cardiac contractility, decreases preload and afterload.
IV only, short term therapy. |
|
|
Term
Steps to lower LDL?
Steps to lower TG?
Steps to raise HDL? |
|
Definition
LDL: Diet & exercise -> Statin -> Ezetimibe.
TG: Diet & exercise -> Fibrate -> Niacin
HDL: Diet & exercise -> Niacin |
|
|
Term
|
Definition
Irreversibly bind presynaptic vesicles in adrenergic neurons. Blocks monoamine transport into vesicles, allowing them to be degraded by MAOs.
Cheap anti-hypertensive, not used in developed world anymore due to AEs.
Depression (anti-NE and 5HT effects), nasal congestion (anti-adrenergic), increased gastric acid secretion (anti-adrenergic). |
|
|
Term
Treatment for central DI?
Nephrogenic DI? |
|
Definition
Central: dDAVP (desmopressin, ADH analog)
Nephrogenic: HCTZ, indomethacin, amiloride |
|
|
Term
|
Definition
| Demeocycline, H2O restriction |
|
|
Term
|
Definition
Rapid acting insulin
Type 1DM, Type 2DM, gestational DM, hyperkalemia, stress-induced hyperglycemia
Hypoglycemia, hypersensitivity (rare), orthostatic hyptotension (rare) |
|
|
Term
|
Definition
Rapid acting insulin
Type 1DM, Type 2DM, gestational DM, hyperkalemia, stress-induced hyperglycemia
Hypoglycemia, hypersensitivity (rare), orthostatic hyptotension (rare) |
|
|
Term
|
Definition
Intermediate acting insulin
Type 1DM, Type 2DM, gestational DM, hyperkalemia, stress-induced hyperglycemia
Hypoglycemia, hypersensitivity (rare), orthostatic hyptotension (rare) |
|
|
Term
|
Definition
Long acting insulin
Type 1DM, Type 2DM, gestational DM, hyperkalemia, stress-induced hyperglycemia
Hypoglycemia, hypersensitivity (rare), orthostatic hyptotension (rare) |
|
|
Term
|
Definition
Long acting insulin
Type 1DM, Type 2DM, gestational DM, hyperkalemia, stress-induced hyperglycemia
Hypoglycemia, hypersensitivity (rare), orthostatic hyptotension (rare) |
|
|
Term
|
Definition
1st generation sulfonylurea; close K channel in beta-cell membrane, triggers insulin release
Type 2 DM only.
Disulfiram-like effects |
|
|
Term
|
Definition
1st generation sulfonylurea; close K channel in beta-cell membrane, triggers insulin release
Type 2 DM only.
Disulfiram-like effects |
|
|
Term
|
Definition
2nd generation sulfonylurea; close K channel in beta-cell membrane, triggers insulin release
Type 2 DM only.
Hypoglycemia, rare agranulocytosis |
|
|
Term
|
Definition
2nd generation sulfonylurea; close K channel in beta-cell membrane, triggers insulin release
Type 2 DM only.
Hypoglycemia, rare agranulocytosis |
|
|
Term
|
Definition
2nd generation sulfonylurea; close K channel in beta-cell membrane, triggers insulin release
Type 2 DM only.
Hypoglycemia, rare agranulocytosis |
|
|
Term
|
Definition
A biguanide; decreases gluconeogenesis (main action), also increases glycolysis, increases peripheral insulin sensitivity. Mechanism unknown.
Type 2DM, less often in type 1DM.
Lactic acidosis (CI in renal failure). |
|
|
Term
|
Definition
A thiazolidinedione. Increases insulin sensitivity in peripheral tissue by binding to PPAR-gamma nuclear TF. Increase adiponectin levels, fatty acid transport protein, insulin receptor, GLUT4.
Monotherapy for DM2, or with other agents.
Weight gain, edema. Hepatotoxic. CV toxic. |
|
|
Term
|
Definition
A thiazolidinedione. Increases insulin sensitivity in peripheral tissue by binding to PPAR-gamma nuclear TF. Increase adiponectin levels, fatty acid transport protein, insulin receptor, GLUT4.
Monotherapy for DM2, or with other agents.
Weight gain, edema. Hepatotoxic. CV toxic. |
|
|
Term
|
Definition
alpha-glucosidase inhibitor. Delays sugar hydrolysis/absorption at brush border, lowers post-prandial hyperglycemia.
Monotherapy in DM2, or combo with other agents.
Osmotic diarrhea, flatulence. |
|
|
Term
|
Definition
alpha-glucosidase inhibitor. Delays sugar hydrolysis/absorption at brush border, lowers post-prandial hyperglycemia.
Monotherapy in DM2, or combo with other agents.
Osmotic diarrhea, flatulence. |
|
|
Term
|
Definition
Amylin analog (usually released with insulin). Slows gastric emptying, promotes satiety, inhibits glucagon secretion.
DM1 and insulin-using DM2.
Hypoglycemia, nausea, diarrhea. |
|
|
Term
|
Definition
GLP-1 analog. Mechanism unknown. Enhances insulin secretion, suppresses glucagon secretion, slows gastric emptying.
DM type 2, adjunct to other oral meds.
Nausea, vomiting, pancreatitis. |
|
|
Term
Propylthiouracil
Mech
Use
Tox |
|
Definition
Inhibit thyroperoxidase; prevent organification of iodide and DIT/MIT coupling. Also inhibit peripheral conversion of T4 to T3.
Hyperthyroidism.
Skin rash, agranulocytosis, aplastic anemia. |
|
|
Term
|
Definition
Inhibit thyroperoxidase; prevent organification of iodide and DIT/MIT coupling.
Hyperthyroidism.
Skin rash, agranulocytosis, aplastic anemia, teratogen. |
|
|
Term
|
Definition
Thyroxine replacement
Hypothyroidism, myxedema
Tachycardia, heat intolerance, tremors, arrythmias |
|
|
Term
Triiodothyonine
Mech
Use
Tox |
|
Definition
Thyroxine replacement
Hypothyroidism, myxedema
Tachycardia, heat intolerance, tremors, arrythmias |
|
|
Term
|
Definition
| Adrenocorticolytic; used for adrenocortical carcinoma. |
|
|
Term
|
Definition
Inhibits 11-beta-hydroxylase, preventing cortisol synthesis.
Used to test HPA axis - if intact, should see rise in urine 11-deoxycortisol metabolites (17-hydroxy-corticosteroids). |
|
|
Term
|
Definition
Reversible blocker of H2 receptors, decreases parietal cell H+ secretion.
Peptic ulcers, gastritis, GERD.
Potent P450 inhibitor, antiandrogenic (prolactin release, gynecomastia, impotence, decreased libido). Crosses BBB (confusion, dizziness, headaches). Crosses placenta. Decreases renal excretion of creatinine, artificial "drop" in GFR. |
|
|
Term
|
Definition
Reversible blocker of H2 receptors, decreases parietal cell H+ secretion.
Peptic ulcers, gastritis, GERD.
Decreases renal excretion of creatinine, artificial "drop" in GFR. |
|
|
Term
|
Definition
Reversible blocker of H2 receptors, decreases parietal cell H+ secretion.
Peptic ulcers, gastritis, GERD.
Fewer AEs compared to other H2 blockers. |
|
|
Term
|
Definition
Reversible blocker of H2 receptors, decreases parietal cell H+ secretion.
Peptic ulcers, gastritis, GERD.
Fewer AEs compared to other H2 blockers. |
|
|
Term
|
Definition
Irreversibly inhibits H/K ATPase in stomach parietal cells, active only in acidic area.
Peptic ulcer, gastrics, Zollinger-Ellison syndrome.
Raises stomach pH, may allow bacteria into GI tract. |
|
|
Term
|
Definition
Irreversibly inhibits H/K ATPase in stomach parietal cells, active only in acidic area.
Peptic ulcer, gastrics, Zollinger-Ellison syndrome.
Raises stomach pH, may allow bacteria into GI tract. |
|
|
Term
Bismuth/sulcrafate
Mech
Use |
|
Definition
Bind to ulcer base, provide physical protection
Ulcer healing, traveler's diarrhea |
|
|
Term
|
Definition
PGE1 analog. Increases secretion of gastric mucous barrier, decreases acid production.
Prevent NSAID peptic ulcers, maintain PDA, induce labor.
CI: pregnancy (abortifacient). Diarrhea. |
|
|
Term
|
Definition
Anti-muscarinic, block M1 receptors on ECL cells, and M3 receptors on parietal cells.
Peptic ulcer (rarely used)
Tachycardia, dry mouth, accomodation loss. |
|
|
Term
|
Definition
Anti-muscarinic, block M1 receptors on ECL cells, and M3 receptors on parietal cells.
Peptic ulcer (rarely used)
Tachycardia, dry mouth, accomodation loss. |
|
|
Term
|
Definition
Somatostatin analog.
Acute variceal bleeds, acromegaly, VIPoma, carcinoid tumors.
Nausea, cramps, steatorrhea. |
|
|
Term
Aluminum hydroxide
Mech
Use
Tox |
|
Definition
Antacid.
GERD, peptic ulcer.
Affect drug absorption or urinary excretion. Hypokalemia.
Constipation, hypophosphatemia, proximal muscle weakness, osteodystrophy.
Aluminum = minimum amount of poop. |
|
|
Term
Magnesium hydroxide
mech
use
tox |
|
Definition
Antacid.
GERD, peptic ulcer.
Affect drug absorption or urinary excretion. Hypokalemia.
Diarrhea, hyporeflexia, hypotension, cardiac arrest.
Mg = Must go to the bathroom. |
|
|
Term
Calcium carbonate
Mech
Use
Tox |
|
Definition
Antacid.
GERD, peptic ulcer.
Affect drug absorption, urinary excretion.
Hypercalcemia, hypokalemia, rebound acid increase, can chelate some drugs (tetracyclines, fluoroquinolones). |
|
|
Term
|
Definition
Combo of sulfapyridine (Abx) and 5-aminosalicylic acid (NSAID). Cleaved & activated by colonic bacteria for local delivery.
Ulcerative colitis, Chron's disease.
Malaise, nausea, sulfonamide toxicity, *reversible oligospermia. |
|
|
Term
|
Definition
5-HT3 antagonist.
Central-acting antiemetic. Post-op and chemo vomiting.
Headache, constipation. |
|
|
Term
|
Definition
D2 receptor antagonist. Increases GI resting tone, contractility, LES tone, motility. No change to colonic transport time.
Gastroparesis: diabetic and post-surg.
Increases Parkinsonian effects. Restlessness, drowsiness, fatigue, depression, nausea, diarrhea. Interacts with digoxin and diabetic agents. CI: small bowel obstruction (increaeses tone!) |
|
|
Term
|
Definition
Emetic - alkaloid root poison.
Used in acute poisoning cases - if poison is still in stomach/upper GI, may be possible to reduce exposure using emetic. However, rarely used today.
Lethargy, cardiotoxicity, reduces effectiveness of activated charcoal, antidotes, bowel irrigation. |
|
|
Term
|
Definition
Charcoal with high surface area (1g = 500m^2!). Highly absorptive.
Acute poisoning.
Not for acid, alkali, or petroleum poisoning. Can cause pulmonary aspiration. |
|
|
Term
|
Definition
Cofactor for ATIII. Reduces thrombin and Xa.
Immediate anticoagulation. OK during pregnancy. Monitor with aPTT.
Bleeding, HIT, osteoporosis, drug-drug interactions. Protamine sulfate for antidote. |
|
|
Term
|
Definition
| Low molecular weight heparin. Acts more on Xa, better bioavailability, 2-4 longer half-life. Less HIT risk. No laboratory monitoring needed. No antidote. |
|
|
Term
|
Definition
Hirudin derivative, directly inhibits thrombin.
Alternative to hepain, use in patients with HIT. |
|
|
Term
|
Definition
Hirudin derivative, directly inhibits thrombin.
Alternative to hepain, use in patients with HIT. |
|
|
Term
|
Definition
Interferes with gamma-carboxylation of II, VII, IX, X, C, S (vitamin K dependent factors). Long half-life, P450 metabolized, plasma protein binding. Monitor with PT.
Use for chronic anticoagulation, NOT in pregnant women (crosses placenta).
Bleeding, teratogen, skin/tissue necrosis, DDIs. Vitamin K for OD, FFP for rapid reversal. |
|
|
Term
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
tPA (alteplase)
mech
use
tox |
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
APSAC (anistreplase)
mech
use
tox |
|
Definition
= plasminogen + streptokinase
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
|
Definition
inhibits plasminogen activation
use for reversal of thrombolytics (streptokinase, tPA, urokinase, APSAC) |
|
|
Term
|
Definition
inhibits plasminogen activation
use for reversal of thrombolytics (streptokinase, tPA, urokinase, APSAC) |
|
|
Term
|
Definition
Irreversibly block ADP receptor on platelets, prevent GpIIb/IIIa expression, less fibrinogen binding.
Must be activated by P450.
Acute coronary syndrome; coronary stenting. Decreases incidence of thrombotic stoke.
Neutropenia, TTP, hemorrhage. |
|
|
Term
|
Definition
Irreversibly block ADP receptor on platelets, prevent GpIIb/IIIa expression, less fibrinogen binding.
Acute coronary syndrome; coronary stenting. Decreases incidence of thrombotic stoke.
Neutropenia, TTP, hemorrhage. |
|
|
Term
|
Definition
Antibody to GpIIb/IIIa. Prevents aggregation.
Acute coronary syndrome, percutaneous interventions.
Bleeding, thrombocytopenia. |
|
|
Term
|
Definition
Folic acid analog, inhibits DHFR.
Leukemias, lymphomas, choriocarcinoma, sarcomas. Abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis.
Myelosuppresion (leucovorin rescue). Macrovesicular liver steatosis. Mucositis. Teratogenic. |
|
|
Term
5-fluorouracil (5-FU)
mech
use
tox |
|
Definition
Pyrimidine analog. Metabolized to 5F-dUMP. Covalently complexes with folic acid, inhibits thymidylate synthase.
Colon cancer, other solid tumors, topical for basal cell carcinoma. Synergy with methotrexate.
Myelosuppresion (no leucovorin rescue! Rescue with thymidine). Photosensitivity. |
|
|
Term
6-mercaptopurine (6-MP)
mech
use
tox |
|
Definition
Purine (thiol) analog, inhibit purine synthesis.
Activated by HGPRT.
Leukemias, lymphomas.
Bone marrow, GI, liver toxicity. Metabolized by xanthine oxidase, increased toxicity with allopurinol. |
|
|
Term
6-thioguanine (6-TG)
mech
use
tox |
|
Definition
Purine analog, inhibit purine synthesis. Activated by HGPRT.
ALL
Myelosuppression, liver toxicity. Metabolized by xanthine oxidase, toxicity with allopurinol. |
|
|
Term
Cytarabine (ara-C)
mech
use
tox |
|
Definition
Pyrimidine analog (cytosine arabinoside). Inhibits DNA polymerase.
AML, ALL, NHL.
Leukopenia, thrombocytopenia, megaloblastic anemia. |
|
|
Term
|
Definition
Intercalates in DNA, generates free radicals.
Wilms tumor, Ewings sarcoma, rhabdomyosarcoma. CHILDHOOD TUMORS.
Myelosuppression. |
|
|
Term
Doxorubicin (Adriamycin)
mech
use
tox |
|
Definition
Generates free radicals. Intercalates DNA. Inhibits topoisomerase II.
Hodgkins lymphoma, myelomas, sarcomas, solid tumors.
Dilated cardiomyopathy, myelosuppression, alopecia. Extravasation hazard. |
|
|
Term
|
Definition
Free radical formation.
Testicular cancer, Hodgkin's lymphoma.
Pulmonary fibrosis, skin changes. *minimal myelosuppression. |
|
|
Term
|
Definition
Inhibits topoisomerase II.
SCLC, prostate, testicular cancer.
Myelosuppression, GI irritation, alopecia. |
|
|
Term
|
Definition
Inhibits topoisomerase I
Chemotherapy |
|
|
Term
|
Definition
Inhibits topoisomerase I
chemotherapy |
|
|
Term
Cyclophosphamide
mech
use
tox |
|
Definition
Alkylating agent. Covalent interstrand DNA crosslink. Requires liver bioactivation.
NHL, breast, ovary. Immunosuppression.
Myelosuppression. Hemorrhagic cystitis, give with MESNA tp prevent. |
|
|
Term
|
Definition
Alkylating agent. Covalent interstrand DNA crosslink. Requires liver bioactivation.
NHL, breast, ovary. Immunosuppression.
Myelosuppression. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Alkylates DNA
CML. Pre-BMT ablation.
Pulmonary fibrosis, hyperpigmentation. |
|
|
Term
|
Definition
Microtubule inhibitor. Binds tubulin, M phase cannot continue.
Hodgkins, Wilms, choriocarcinoma.
*Peripheral neurotoxicity (areflexia, peripheral neuritis, paralytic ileus). |
|
|
Term
|
Definition
Microtubule inhibitor. Binds tubulin, M phase cannot continue.
Hodgkins, Wilms, choriocarcinoma.
*Bone marrow suppression. |
|
|
Term
| Paclitaxel and other -taxols |
|
Definition
STABILIZE microtubules, block M-phase.
Ovary, breast.
Myelosuppression, hypersensitivity. |
|
|
Term
|
Definition
Cross-link DNA (C for crosslink)
Test, bladder, ovary, lung
Nephrotoxicity, acoustic nerve damage (can't pee, can't hear a high C)
Use Amifostine to protect from nephrotoxicity, (thiol-based free-radical scavenger), or chloride diuresis (IV saline). |
|
|
Term
|
Definition
Cross-link DNA (C for crosslink)
Test, bladder, ovary, lung
Nephrotoxicity, acoustic nerve damage (can't pee, can't hear a high C)
Use Amifostine to protect from nephrotoxicity, (thiol-based free-radical scavenger), or chloride diuresis (IV normal saline). |
|
|
Term
|
Definition
Inhibit ribonucleotide reductase, inhibit DNA synth
melanoma, CML, sickle cell disease (increases HbF)
Myelosuppression, GI upset |
|
|
Term
|
Definition
Selective Estrogen Receptor Modifier - antagonist in breast, agonist in bone.
Breast cancer, osteoporosis.
May increase endometrial carcinoma risk via partial agonist effects. Hot flashes. |
|
|
Term
|
Definition
Selective Estrogen Receptor Modifier - antagonist in breast, agonist in bone.
Breast cancer, osteoporosis.
Endometrial antagonist, no endometrial carcinoma risk (vs. Tamoxifen) |
|
|
Term
|
Definition
aka Herceptin
Antibody to HER-2 receptor (erb-B2 gene).
BrCa with HER-2 expression.
Cardiotoxic. |
|
|
Term
|
Definition
aka Gleevec
Inhibits bcr-abl (philadelphia chromosome tyr kinase receptor)
CML, GI stromal tumors
Fluid retention |
|
|
Term
|
Definition
aka Gleevec
Inhibits bcr-abl (philadelphia chromosome tyr kinase receptor)
CML, GI stromal tumors
Fluid retention |
|
|
Term
|
Definition
Antibody to CD20
NHL, rheumatoid arthritis (with methotrexate) |
|
|
Term
|
Definition
Selective COX-2 inhibitor
Avoids normal NSAID adverse effects of GI ulceration, and inhibited platelet aggregation - purely anti-inflammatory.
However, long-term use linked to increased thrombotic risk, which may be due to decrease production of prostacyclin. |
|
|
Term
|
Definition
Block calcium-dependent potassium channels (Gardos) on RBCs. Prevent cellular dehydration, heme polymerization.
For sickle cell anemia. |
|
|
Term
|
Definition
| Traditional NSAID; reversible non-selective COX inhibitor. |
|
|
Term
|
Definition
| Tradiational NSAID; reversibly inhibits COX, non-selective |
|
|
Term
|
Definition
| Tradiational NSAID; non-selective, reversible COX inhibition |
|
|
Term
|
Definition
AKA leucovorin
For methotrexate rescue |
|
|
Term
|
Definition
Prodrug; converted to 5-FU in tumor.
CRC, breast
Cardiotoxic, dermatitis, GI, myelosuppression, thrombocytopenia |
|
|
Term
|
Definition
deoxycytidine analog; causes DNA synthesis stop
lung, pancreas, bladder, breast
Fever, fatigue, N/V, rash, hair loss, sores |
|
|
Term
|
Definition
Purine analog
Effective for CLL
Lymphopenia, anemia, thrombocytopenia |
|
|
Term
|
Definition
Purine analog (adenosine); adenosine deaminase resistant.
Hairy cell leukemia
Fever; otherwise well tolerated |
|
|
Term
|
Definition
Methylating agent; requires hepatic activation.
Melanoma, lymphomas, sarcoma.
N/V, myelosupression, sterility |
|
|
Term
Cyclosporine
Mech?
Use?
Tox? |
|
Definition
Binds cyclophilins. Complex inhibits calcineurin, prevents IL-2 and IL-2R production, prevents Tcell differentiation/activation
Suppress organ rejection; some autoimmune dz
Viral infections, lymphoma; *nephrotoxic (mannitol diuresis) |
|
|
Term
Tacrolimus
aka?
Mech?
Use?
Tox? |
|
Definition
aka FK506
Similar to cyclosporine; binds FK-binding protein, prevents IL-2 and other cytokine secretion
Organ transplants
Significant - nephrotoxic, peripheral neuropathy, HTN, pleural effusion, hyperglycemia |
|
|
Term
Sirolimus
aka?
Mech?
Use?
Tox? |
|
Definition
aka Rapamycin
Binds mTOR, inhibits T-cell prolif in response to IL-2
Immunosuppression after kidney trsplt w/ cyclosporine
Hyperlipidemia, thrombocytopenia, leukopenia |
|
|
Term
|
Definition
| Mab for IL-2 receptors on activated T-cells |
|
|
Term
Azathioprine
Mech?
Use?
Tox? |
|
Definition
Precursor of 6-mercaptopurine; toxic to proliferating lymphocytes
Kidney trsplnt, autoimmune disorders (GN, hemolytic anemia)
Bone marrow suppression. Xanthine oxidase metabolises 6-mp, so allopurinol may increase tox |
|
|
Term
Muromonab-CD3
aka?
Mech?
Use?
Tox? |
|
Definition
aka OKT3
Mab to CD3 (epsilon chain) on T cells. Blocks signal transduction.
Kidney trsplt
Cytokine release syndrome, hypersensitivity rxn |
|
|
Term
|
Definition
aka recombinant IL-2
Renal cell ca, melanoma |
|
|
Term
|
Definition
| Anemias, esp. in renal failure |
|
|
Term
|
Definition
aka recombinant G-CSF
bone marrow recovery |
|
|
Term
|
Definition
aka recombinant GM-CSF
Bone marrow recovery |
|
|
Term
|
Definition
| HBV, HCV, Kaposi's sarcoma, leukemias, melanoma |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
aka recombinant IL-11
Thrombocytopenia |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Antidote for digoxin poisoning |
|
|
Term
|
Definition
TNF-alpha mab
Chron's, RA, psoriasis, ankylosing spondylitis
Granulomatous infections - do PPD first |
|
|
Term
|
Definition
TNF-alpha mab
Chron's, RA, psoriasis
Granulomatous infxn - check PPD first |
|
|
Term
|
Definition
mab to platelet glycoprotein IIB/IIIa
Unstable angina, percutaneous coronary interventions |
|
|
Term
|
Definition
aka Herceptin
mab to erb-B2
use for HER-2 expressing breast ca |
|
|
Term
|
Definition
mab to CD20
B-cell non-Hodgkin's lymphoma |
|
|
Term
|
Definition
Synthetic retinoid; promotes cellular differentiation, immunomodulatory effects, anti-tumor effects
Psoriasis
*has 2-day halflife, but can be metabolized to Etretinate (discontinued drug) which has 120-day halflife and similar effects.
*severe teratogen - must be on contraceptives for at least 2 years! because of Etretinate halflife |
|
|
Term
|
Definition
Vitamin D analog
topical treatment of psoriasis |
|
|
Term
Antibiotics
Mechanism of action:
Block cell wall synthesis by inhibition of peptidoglycan cross-linking |
|
Definition
| Penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins |
|
|
Term
ABx
Mech
Block peptidoglycan synthesis |
|
Definition
|
|
Term
Abx
Mech
Disrupt bacterial cell membranes (detergent) |
|
Definition
|
|
Term
Abx
Mech
Block nucleotide synthesis (folate pathway) |
|
Definition
| sulfonamides (ex. sulfamethoxazole), trimethoprim |
|
|
Term
Abx
Mech
Block topoisomerases |
|
Definition
|
|
Term
Abx
Mech
block mRNA synthesis |
|
Definition
|
|
Term
Abx
Mech
block protein synthesis at 50S subunit |
|
Definition
| chloramphenicol, macrolides, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid |
|
|
Term
Abx
Mech
Block protein synth at 30S subunit |
|
Definition
| aminoglycosides, tetracyclines |
|
|
Term
| Abx Mech Free radical generation, cause DNA breaks |
|
Definition
| metronidazole, nitrofurantion |
|
|
Term
| Bacteriostatic antibiotics |
|
Definition
ECSTaTIC
Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Cloramphenicol
(generally, stop protein or DNA synth) |
|
|
Term
|
Definition
| Very Finely Proficient At Neat Cell Murder Vancomycin, Fluoroquinolones, Penicillin, Aminoglycosides, Nitrofurantoin, Cephalosporins, Metronidazole (any that damage DNA or cell wall, EXCEPT aminoglycosides - weird ones that are cidal anyway) |
|
|
Term
|
Definition
bind PBPs, block transpeptidase cross-linking of cell wall, activate autolytic enzymes
Gram-positive organisms and spirochetes.
Hypersensitivity, hemolytic anemia. |
|
|
Term
| Penicillinase-resistant penicillins Mech Uses Tox |
|
Definition
| Methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin Same as penicillin, bulkier R group gives resistance. S. aureus, except MRSA (altered target site) Hypersensitivity. Methicillin: interstitial nephritis. |
|
|
Term
Aminopenicillins
Mech
Uses
Tox |
|
Definition
Ampicillin, amoxicillin
Same as penicillin. Wide spectrum but penicillinase sensitive. Combine with beta-lactamase inhibitors.
AmOxicillin has greater Oral bioavail.
Gram-positive and some gram-negs (Hflu, Ecoli, Listeria, Proteus, Salmonella, enterococci) HELPS
Hypersensitivity, ampicillin rash, pseudomem. colitis. |
|
|
Term
Antipseudomonals
Mech
Uses
Tox |
|
Definition
Ticarcillin, carbenicillin, piperacillin (TCP: takes care of pseudomonas)
Same as penicillin, extd. spectrum. Need beta-lactamase inhibitor.
Pseudomonas spp. and other gram negs.
Hypersensitivity. |
|
|
Term
Beta-lactamase inhibitors
Mech
Uses
Tox |
|
Definition
Clavulanic acid, sulbactam, tazobactam
Inhibit beta-lactamase (penicillinase).
Use with sensitive penicillin Abx. |
|
|
Term
Cephalosporins: 1st gen
Mech
Uses
Tox |
|
Definition
Cefazolin, cephalexin
same as penicillin, b-lactamase resistant. Cidal.
gram-pos cocci, Proteus mirabilis, E. coli, Klebsiella (PEcK)
Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides. |
|
|
Term
Cephalosporins: 2nd gen
Mech
Uses
Tox |
|
Definition
Cefotoxin, Cefaclor, Cefuroxime
same as penicillin, b-lactamase resistant. Cidal.
gram pos cocci, H flu, Enterobacter, Neisseria, Proteus, Ecoli, Klebsiella, Serratia (HEN PEcKS).
Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides. Disulfram-like effect. |
|
|
Term
| Cephalosporins: 3rd gen Mech Uses Tox |
|
Definition
Ceftriaxone, Cefotaxime, Ceftazidime. Same as penicillin, b-lactamase resistant.
Better CSF distribution than previous gens.
Serious gram neg infxns.
Ceftriaxone: meningitis, gonorrhea
Ceftazidime: Pseudomonas.
Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides. |
|
|
Term
Cephalosporins: 4th gen
Mech
Uses
Tox |
|
Definition
Cefepime
Same as penicillins, b-lactamase resistant. Cidal.
IV only. Good CSF dist. More lactamase resistant.
Better activity against Pseudomonas. |
|
|
Term
|
Definition
Monobactam. Similar to penicillin. B-lactamase resistant.
Gram Neg Aerobes Only.
Less toxic. For renal failure pts. No cross-rxn with penicillins/cephalosporins. |
|
|
Term
|
Definition
A carbapenem. Same as penicillins. B-lactamase resistant.
IV only. Broad-spec, CSF penetration with inflammed meninges. Tox = last resort.
GI distress, skin rash, CNS probs/seizures. |
|
|
Term
|
Definition
A carbapenem. Same as penicillins. B-lactamase resistant.
IV only. Broad-spec, CSF penetration with inflammed meninges. Tox = last resort.
ALWAYS GIVE with Cilastatin: prevent inactivation in renal tubules by renal dihydropeptidase I.
GI distress, skin rash, CNS probs/seizures. |
|
|
Term
|
Definition
Bind D-ala D-ala portion of cell wall precursors. Resistance: change to D-ala D-lac
Gram positive only. Multidrug resistant organisms. No CSF distribution.
Nephrotoxicity, Ototoxicity, Thrombophlebitis. Flushing: "red man" - prevent with antihistamines. |
|
|
Term
Aminoglycosides
Mech
Use
Tox
Resistance |
|
Definition
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin (GNATS)
Inhibit formation of initiation complex (30S), cause mRNA misreads. Require O2. Cidal.
Gram-neg aerobes only: Pseudomoas, Enterobacter, Klebsiella. Synergy with b-lactams. Neomycin for bowel surgery. Endocarditis.
Nephrotoxicity (esp. w/ cephalosporins), Ototoxicity (esp. w/ loop diuretics). Teratogen. Acute muscle paralysis.
Enzymatic alteration of drug: acetylation, phosphorylation, adenylation. Ribosomal alteration. Biofilm formation. |
|
|
Term
|
Definition
|
|
Term
Neomycin
class?
special uses?
Tox? |
|
Definition
Aminoglycoside
Topical mostly (neosporin), not absorbed from GI tract.
Can be used to clear bowels (e.g. bowel surg prep).
Very nephro and ototoxic |
|
|
Term
Amikacin
class?
special use?
special resistance? |
|
Definition
Aminoglycoside
most broad spectrum
sterically blocks enzymatic alteration (adenylation, acetylation, phosphorylation) |
|
|
Term
Tobramycin
class?
special use? |
|
Definition
aminoglycoside
may be better against Pseudomonas |
|
|
Term
Streptomycin
Class?
Special use? |
|
Definition
Aminoglycoside
First TB drug, but monotherapy --> resistance. |
|
|
Term
|
Definition
Blocks formation of initiation complex (30S + 50S). Static.
Backup for MDROs.
Headache, hematologic toxicity, serotonergic toxicity, peripheral or optic neuropathy. |
|
|
Term
Tetracyclines
Mech
Use
Tox
Resist |
|
Definition
Tetracycline, doxycycline, demeclocycline, minocycline.
Bind 30S and precent tRNA attachment. Little CSF. Static.
Cannot take with milk, antacids, or iron: bind divalent cations and inhibit gut absorption.
Borrelia, H. pylori, Mycoplasma. Broad spec. Has intracellular penetration: Rickettsia, Chlamydia.
GI distress, discoloration of teeth, inhibition of bone growth, photosensitivity, CI for pregnancy.
Resistance by efflux. |
|
|
Term
Doxycycline
class?
special use? |
|
Definition
Tetracycline
Hepatic elimination - OK for renal failure
For Rickettsial disease |
|
|
Term
Demeclocycline
class?
special use? |
|
Definition
Tetracycline
ADH antagonist - use as diuretic in SIADH. |
|
|
Term
Macrolides
Mech Use Tox Resist |
|
Definition
Erythromycin, Azithromycin, Clarithromycin (ACE) Bind 23s rRNA of 50S subunit. Static.
STDs, URIs, Atypical pneunomia (USA!) gram+ cocci, Neisseria.
Prolonged QT interval (esp. Eryth), GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes. P450 inhibition (esp. Eryth).
Methylation of 23S rRNA binding site. |
|
|
Term
Erythromycin
class?
special use?
special toxicity?
special resistance? |
|
Definition
Macrolide
can be used as motillin analog.
Prolonged QT interval, P450 inhibition, severe GI distress.
Efflux resistance, in addition to 50S methylation. |
|
|
Term
Cloramphenicol
Mech
Use
Tox
Resist |
|
Definition
Inhibits 50S peptidyltransferase. Static.
Hepatic metabolism.
Meningitis (Hflu, Neisseria, S. pneumo). Mycoplasma, chlamydia.
Severe: anemia, aplastic anemia, "gray baby" (undeveloped UDP-glucuronyl transferase).
Plasmid encoded acetyltransferase |
|
|
Term
| Clindamycin Mech Use Tox Resist |
|
Definition
Binds 50S subunit. Static. Anaerobes (B. fragilis, C. perfringens) in aspiration pneumonia/lung abscess (anaerobes above diaphragm). No good for gram-neg anaerobes, UTIs.
Psedomem. colitis, fever, diarrhea. Neuromuscular block (Myasthenia Gravis CI).
50S methylation (like macrolides). |
|
|
Term
|
Definition
Binds membranes in calcium depd. manner, depolarizes. Sialyc acid (human) repels.
IV only. Cidal. For MDROs. No CSF entry.
GI irritation, despite IV! Elevated creatinine, muscle weakness) |
|
|
Term
| Sulfonamides Mech Use Tox Resist |
|
Definition
Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine
PABA analog, comp. inhibit dihydropteroate synthetase.
Gram+or-, Nocardia, Chlamydia. Simple UTIs.
Hypersensitivity, *hemolysis with G6PD def., nephrotoxicity, *photosensitivity, kernicterus, *displacement from albumin (e.g. Warfarin), P450 inhibition.
Altered enzyme, increased PABA synth, low uptake. |
|
|
Term
|
Definition
Trimethoprim (TMP)
Inhibits bacteria DHFR. Static.
Synergy with SMX. Recurrent UTIs, Shigella, Salmonella, *PCP pneumonia prophylaxis.
Megaloblastic anemia, leukopenia, granulocytopenia. Rescue with leucovorin (folinic acid). |
|
|
Term
|
Definition
SULFA? Not for FAT Pro Celeb!
Sulfonamides
sulfasalazine
sulfonylureas
furosemide
acetazolamide
thiazide diuretics
probenecid
celecoxib |
|
|
Term
|
Definition
Reduction in bacteria makes reactive metabolites, DNA damage. Cidal.
Tx or prophylaxis of UTIs.
GI disturbance, G6PD deficient --> anemia, Pulmonary rxns, hypersensitivity, headache, vertigo, neuropathies. |
|
|
Term
Fluoroquinolones
Mech
Use
Tox
Resist |
|
Definition
Ciprofloxacin, Norfloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin, nalidixic acid (a quinolone).
Inhibit DNA topoisomerase II - dsDNA breaks. Cidal.
Cannot take with mild/antacids/iron: divalent cations inhibit absorption (like tetracyclines).
Gram-and+, intracellular. Not for anaerobes. UTIs, resp. infxn, diarrhea, osteomyelitis. Pseudomonas, Neisseria.
GI upset, superinfections, skin rash, headache, dizziness. *Damage to cartilage, tendons: CI in pregnancy and children.
Mutation in DNA topoisomerase II. |
|
|
Term
Ciprofloxacin
class?
special use? |
|
Definition
fluoroquinolone
excellent lung tissue penetration -> resp. infxns. |
|
|
Term
|
Definition
Free radical toxic metabolites, damage DNA. Cidal.
*Anti-protozoal. Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes, H. pylori (GET GAP).
Disulfiram rxn with EtOH, metallic taste, headache. (Inhibits P450?) |
|
|
Term
|
Definition
Polymixin B, colistimethate (polymixin E)
Detergents, disrupt cell membrane.
Resistant gram-neg infxn.
Neurotoxicity, acute renal tubular necrosis. |
|
|
Term
M. tuberculosis
Prophylaxis?
Tx? |
|
Definition
Pro: INH
Tx: Rifampin, INH, Pyrazinamide, Ethambutol, Streptomycin (RIPES) |
|
|
Term
M. avium-intracellulare
Prophylaxis?
Tx? |
|
Definition
Pro: Azithromycin
Tx: Azithromycin, rifampin, ethambutol, streptomycin |
|
|
Term
|
Definition
| Dapsone, rifampin, clofazimine |
|
|
Term
|
Definition
Inhibit mycolic acid synthesis.
Bacterial catalase-peroxidase needed to activate.
N-acetylated: bimodal half-life.
M. tuberculosis only - Tx and prophylaxis. Neurotoxicity, hepatotoxicity, drug-induced lupus, inhibits P450.
Depletes B6 - pyridoxine (B6) can prevent neurotoxicity, lupus. |
|
|
Term
|
Definition
| Inhibits DNA-dependent RNA polymerase. M. tuberculosis with other drugs, M. leprae to delay resistance to dapsone. Meningoccocal prophylaxis, H. flu prophylaxis for contacts. Minor hepatotoxicity; induces P450; red/orange bodyfluids (4Rs: RNA polymerase inhibitor, Ramps up P450, Red/orange body fluids, Rapid resistance if used alone) |
|
|
Term
| Prophylaxis for meningococcal infection? |
|
Definition
|
|
Term
| Prophylaxis for gonorrhea? |
|
Definition
|
|
Term
| Prophylaxis for syphilis? |
|
Definition
|
|
Term
| Prophylaxis for recurrent UTIs? |
|
Definition
|
|
Term
| Prophylaxis for Pneumocystis pneumonia in AIDS? |
|
Definition
| TMP-SMX (1st choice), aerosolized pentamidine |
|
|
Term
| Prophylaxis for endocarditis with surgical/dental procedures? (controversial?) |
|
Definition
|
|
Term
| Prophylaxis for Mycobacterium avium-intracellulare? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| linezolid, streptogramins (quinupristin/dalfopristin) |
|
|
Term
|
Definition
Binds ergosterol; forms membrane pores.
Serious, systemic mycoses. Does not enter CSF; can use intrathecally for fungal meningitis.
Fever/chills, hypoTN, nephrotox (increased distal tubule permeability, increased serum K and Mg), arrythmias, anemia, IV phlebitis. Hydration to reduce nephrotoxicity. Liposomal amphotericin to reduce overall toxicity. |
|
|
Term
|
Definition
Same as amphotericin B
Topical only - too toxic! Can use for GI tract too, not absorbed. Oral candidiasis, vaginal candidiasis, diaper rash. |
|
|
Term
|
Definition
Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
Inhibit ergosterol synthesis, by inhibiting P450 enzyme: lanosterol-->ergosterol.
Systemic mycoses.
Hormone synthesis inhibition (gynecomastia), P450 inhibition, fever/chills. |
|
|
Term
|
Definition
Azole
Cryptococcal meningitis in AIDS (enters CSF), candidal infections. |
|
|
Term
Ketoconazole
Class?
Uses?
Tox? |
|
Definition
Azole
Blastomyces, Coccidiodes, Histoplasma (environmental mycoses), Candida. Also use for hypercortisolism: inhibits steroid hmn synth.
Gynecomastia is particular toxicity. |
|
|
Term
Clotrimazole and miconazole
Class?
Use? |
|
Definition
Azoles
Topical fungal infections |
|
|
Term
|
Definition
Inhibits DNA synth by conversion to 5-FU.
Systemic fungal infections along with Amphotericin B.
Nausea, vomiting, diarrhea, *bone marrow suppression. |
|
|
Term
| Caspofungin Mech? Use? Tox? |
|
Definition
Inhibits beta-glucan synthesis, a cell wall carbohydate.
Invasive aspergillosis
GI upset, flushing |
|
|
Term
|
Definition
Inhibit fungal squalene epoxidase, ultimately inhibiting ergosterol synthesis.
Use for dermatophytoses, esp. onychomycosis (finger or toenail infxn) |
|
|
Term
| Griseofulvin Mech? Use? Tox? |
|
Definition
| Interfere with microtubule formation; disrupt mitosis. Deposits in keratin containing tissue (e.g. nails). Oral drug for superficial infections; inhibits growth of dermatophytes (tinea, "ringworm"). Teratogenic, carcinogenic, confusion, headaches. P450 inducer. |
|
|
Term
| Which Abx classes *generally* have good intracellular activity? |
|
Definition
Macrolides
Fluoroquinolones
Chloramphenicol |
|
|
Term
| Which drugs/classes *generally* have good activity against anaerobes? |
|
Definition
Clindamycin
Metronidazole
Carbapenems |
|
|
Term
| Which drugs/classes are effective against aerobes only? |
|
Definition
Aminoglycosides
Aztreonam
~Fluoroquinolones (not great against anaerobes) |
|
|
Term
| Which drugs generally work against gram + only? |
|
Definition
Penicillins
Macrolides
~Clindamycin (not effective on Gram - aerobes [E. coli])
Early generation Cephalosporins |
|
|
Term
| Which drugs generally work against gram - only? |
|
Definition
|
|
Term
| Which drugs enter CSF well? |
|
Definition
Later gen. Cephalosporins
Carbapenems (when meninges inflammed)
Linezolid
Sulfonamides
Trimethoprim
Acyclovir/Ganciclovir
Anti-tuberculosis
Fluconazole
Zidovudine
Nevirapine |
|
|
Term
Pyrimethamine
Use?
Mechanism?
Tox? |
|
Definition
Anti-protozoan; best for P. falciparum, toxoplasmosis with sulfadiazine.
Inhibits plasmodial DHFR.
Not for pregnant women; give with folinic acid. |
|
|
Term
|
Definition
Antiprotozoan; no CNS entry.
Inhibits energy metabolism enzymes. |
|
|
Term
Melarsoprol
Use?
Mechanism? |
|
Definition
Antiprotozoan; +CSF entry.
Inhibits sulfhydryl groups in parasite enzymes. |
|
|
Term
| Nifurtimox Use? Mechanism? |
|
Definition
Antiprotozoan (Chagas dz)
Forms oxygen free radicals |
|
|
Term
| Sodium stibogluconate Use? Mechanism? |
|
Definition
Antiprotozoan (Leishmaniasis)
Inhibits glycolysis at PFK reaction |
|
|
Term
Chloroquine
Use?
Mechanism? |
|
Definition
Antiprotozoan; Chloroquine sensitive malaria.
Blocks plasmodium heme polymerase, accumulation of toxic hemoglobin breakdown products. |
|
|
Term
|
Definition
Antiprotozoan; kills latent malaria parasites in hepatocytes (vivax, ovale), prevents reactivation.
Same as chlorquine - use with chloroquine or quinine plus doxycycline for vivax, ovale. |
|
|
Term
Mebendazole/Albendazole
Use?
Mechanism? |
|
Definition
Antihelminthic
All intestinal helminths (trichonosis, strongyloides, nematodes, tapeworms/cestodes)
Inhibit glucose uptake and microtuble synth |
|
|
Term
Pyrantel pamoate
Use?
Mechanism? |
|
Definition
Antihelminthic; *No effect on tapeworms or flukes.
Stimulates nicotinic receptors --> contraction --> depolarization paralysis. |
|
|
Term
|
Definition
Antihelminthic; "filarial" infections: lymphatic filariasis, onchocerciasis, loa loa
Intensifies GABA neurotransmission, immobilizes. No CNS entry, no effect on humans. |
|
|
Term
Praziquantel
Use?
Mechanism? |
|
Definition
Antihelminthic; tapeworms and flukes.
Increases membrane permeability to calcium, causing contraction and paralysis. |
|
|
Term
Amantidine/Rimantidine
Mech
Use
Tox
Resist |
|
Definition
Blocks M2 ion channel; virus can not decoat in vesicle.
Amantidine: Prophylaxis and tx for Influenza A only. Parkinson's Dz (affects catechol synth). Rimantidine does not cross BBB, fewer CNS SEs.
Ataxia, dizziness, slurred speech.
Mutated M2 protein, 90% of influenza A now resistant (rarely used anymore.) |
|
|
Term
| Zanamivir, Oseltamivir, Pirimivir Mech Use Tox Resist |
|
Definition
| Inhibit neuraminidase, progeny virus can't release. Influenza A and B, prevention and shorten course. Zanam: bronchospasm, CI asthma, COPD. Oseltam: mild GI. Mutation of neuraminidase resists Oseltamivir, not Zanamivir currently. Strain dependent. |
|
|
Term
|
Definition
Guanine analog, comp. inhibits IMP dehydrogenase.
RSV, chronic HepC
No selectivity for viral enzyme! Hemolytic anemia, severe teratogen. Rarely used. |
|
|
Term
Acyclovir, Valacyclovir, Famciclovir
Mech
Use
Tox
Resist |
|
Definition
Guanosine analog. Monophosphorylated by viral thymidine kinase. Triphosphate formed by cell enzymes. Pref. inhibits viral DNA polymerase by chain termination. Valacyclovir is valine ester prodrug. Famciclovir is topical form.
HSV, VZV, EBV. HSV lesions and encephalitis. No effect on latent HSV and VZV.
Some nephrotoxicity (precipitation): hydrate!
Mutation/lack in viral thymidine kinase/DNA pol. |
|
|
Term
Ganciclovir
Mech
Use
Tox
Resist |
|
Definition
Guanosine analog. Phosphorylated by viral kinase. Less selectivity for viral DNA polymerase than acyclovir.
CMV, esp. immunocompromised pts.
Bone marrow: leukopenia, neutropenia, thrombocytopenia. Renal toxicity.
Mutated polymerase, mutated/lack kinase. |
|
|
Term
Foscarnet
Mech
Use
Tox
Resist |
|
Definition
Pyrophosphate analog. Binds viral DNA polymerase. No activation needed.
CMV retinitis in immunocomp pts when ganciclovir fails; acyclovir-resistant HSV.
Nephrotoxicity. Calcium chelation, low Ca, Mg, seizures.
Mutated DNA polymerase. |
|
|
Term
|
Definition
Nucleotide analog of cytosine monophosphate. Inhibits viral DNA polymerase. Does not require viral kinase activation.
Use Cidofovir or Foscarnet in kinase-deficient viruses (acyclovir/ganciclovir resistant) |
|
|
Term
| What constitutes a HAART regimen? |
|
Definition
3 drugs (prevent resistance):
2 NucleosideRTIs + 1 Protease inhib.
2 NucleosideRTIs + 1 Non-NucleosideRTI |
|
|
Term
Protease Inhibitors
Mechanism
Use
Toxicity |
|
Definition
"-navir": Saquinavir, Ritonavir, Indinavir, Nelfinavir, Amprenavir
Inhibit protase (pol gene), cleaves HIV proteins into functional parts.
HIV, can be part of HAART.
Inhibit P450. Hyperglycemia, GI, lipodystrophy, thrombocytopenia (indinavir). |
|
|
Term
| Nucleoside Reverse Transcriptase Inhibitors Mech Use Tox |
|
Definition
NRTIs: Zidovudine (ZDV or AZT), Didanosine (ddI), Zalcitabine (ddC), Stavudine (d4T), Lamudivine, Abacavir.
Chain termination (no 3'-OH). Need activation by host cell thymidine kinases. Selective for viral reverse transcriptase.
2 are always needed as part of HAART! ZDV for prophylaxis, during pregnancy to prevent vertical trans.
Bone marrow suppression, periph neuropathy, lactic acidosis (except abacavir), rash, megaloblastic anemia, lipoatrophy, GI intolerance (ZDV only). |
|
|
Term
Non-Nucleoside Reverse Transcriptase Inhibitors
Mech
Use
Tox |
|
Definition
Nevirapine, Efavirenz, Declaviridine (Never Ever Deliver nucleosides).
Bind reverse transcriptase, non-competitive inhibition. No kinase activation needed.
HIV, can be part of HAART.
Hypersensitivity (Stevens-Johnson), hepatotoxic, GI. Nevirapine can induce P450. |
|
|
Term
| Zidovudine Class? Special use? Special toxicity? |
|
Definition
| Nucleoside Reverse Transcriptase Inhibitor Prophylaxis: general or during pregnancy Megaloblastic anemia, GI upset |
|
|
Term
|
Definition
Fusion inhibitor. Binds gp41 subunit, prevents fusion with CD4 cells.
Used for HIV failure on HAART.
*Injection site irritation. Hypersensitivity (peptide drug). Increased bacterial pneumonia risk (mech?) |
|
|
Term
|
Definition
Non-competitive inhibitor of CCR5, prevents HIV entry.
Used for HIV failure on HAART.
*Hepatotoxicity. |
|
|
Term
|
Definition
Inhibits viral integrase, can't insert HIV DNA into genome.
Failure on HAART.
Few toxicities. |
|
|
Term
|
Definition
IFN-alpha, beta, gamma
Block replication of RNA and DNA viruses.
IFN-a: HepB, HepC, Kaposi's sarcoma (HHV8)
IFN-b: MS
IFN-g: NADPH oxidase def. (CGD)
Neutropenia. |
|
|
Term
|
Definition
IFN-alpha, beta, gamma
Block replication of RNA and DNA viruses.
IFN-a: HepB, HepC, Kaposi's sarcoma (HHV8)
IFN-b: MS
IFN-g: NADPH oxidase def. (CGD)
Neutropenia. |
|
|
Term
Antibiotics to avoid during pregnancy?
Toxicity? |
|
Definition
SAFE Moms Take Really Good Care
Sulfonamides - kernicterus
Aminoglycosides - ototoxicity
Fluoroquinolones - cartilage damage
Erythromycin - acute cholestatic hepatitis in mom
(and Clarithromycin - embryotoxic)
Metronidazole - mutagenesis
Tetracyclines - discolored teeth, bone growth inhibition
Ribavirin - teratogenic
Griseofulvin - teratogenic
Chloramphenicol - "gray baby" |
|
|
Term
| Anti-bacterials OK for pregnancy? |
|
Definition
| Penicillins, Cephalosporins, Azithromycin, Nitrofurantoin |
|
|
Term
|
Definition
Converted to pyrazinoic acid by mycobacterial enzyme pyrazinamidase, lowering pH inside bacterium
Anti-tuberculosis
hepatotoxicity |
|
|
Term
|
Definition
Inhibit arabinosyl transferase, inhibiting synthesis of mycobacterial cell wall.
Anti-TB
Red/Green colorblindness, optic neuropathy, hepatic toxicity |
|
|
Term
|
Definition
Aspirin (a salicylate)
IRREVERSIBLY inhibits COX by covalent binding. Decreased synthesis of prostaglandins and thromboxane.
Low dose for anti-platelet. Intermediate dose for antipyretic, analgesic. High dose for anti-inflammatory.
NSAID induced gastric ulcer, acute renal failure, interstitial nephritis. Reye's syndrome in children with fever (don't give under 12). Inhibits uric acid secretion (except at very high doses). |
|
|
Term
|
Definition
NSAID: reversibly inhibit COX.
Antipyretic, analgesic, anti-inflammatory.
Renal damage, fluid retention, aplastic anemia, GI upset, ulcers. |
|
|
Term
|
Definition
NSAID: reversibly inhibit COX.
Antipyretic, analgesic, anti-inflammatory.
Renal damage, fluid retention, aplastic anemia, GI upset, ulcers. |
|
|
Term
|
Definition
NSAID: reversibly inhibit COX.
Antipyretic, analgesic, anti-inflammatory. Indomethacin also for PDAs.
Renal damage, fluid retention, aplastic anemia, GI upset, ulcers. |
|
|
Term
|
Definition
NSAID: reversibly inhibit COX.
Antipyretic, analgesic, anti-inflammatory.
Renal damage, fluid retention, aplastic anemia, GI upset, ulcers. |
|
|
Term
|
Definition
COX2 inhibitor (only one left on market in US!)
Anti-inflammatory/analgesic. Patients with gastritis/ulcers, bleeding risk.
Increased thrombosis risk. Sulfa allergy. |
|
|
Term
|
Definition
aka APAP, Paracetamol, "Tylenol"
Rersible COX inhibitor, mainly in CNS. Inactivated peripherally.
Antipyretic, analgesic, NO ANTI-INFLAMMATORY action. Use to avoid Reye's syndrome in children.
Overdose causes fulminant hepatotoxicity due to glutathione depletion and toxic metabolite formation. Antidote: N-acetylcysteine, regenerates glutathione. |
|
|
Term
|
Definition
A bisphosphonate.
Inhibits osteoclast activity; reduces bone resorption, remodeling.
Malignancy associated hypercalcemia, Paget's disease, postmenopause osteoporosis.
Corrosive esophagitis (can't lie down after taking), nausea, diarrhea, rare jaw osteonecrosis. |
|
|
Term
|
Definition
A bisphosphonate.
Inhibits osteoclast activity; reduces bone resorption, remodeling.
Malignancy associated hypercalcemia, Paget's disease, postmenopause osteoporosis.
Corrosive esophagitis (can't lie down after taking), nausea, diarrhea, rare jaw osteonecrosis. |
|
|
Term
|
Definition
A bisphosphonate.
Inhibits osteoclast activity; reduces bone resorption, remodeling.
Malignancy associated hypercalcemia, Paget's disease, postmenopause osteoporosis.
Corrosive esophagitis (can't lie down after taking), nausea, diarrhea, rare jaw osteonecrosis. |
|
|
Term
|
Definition
A bisphosphonate.
Inhibits osteoclast activity; reduces bone resorption, remodeling.
Malignancy associated hypercalcemia, Paget's disease, postmenopause osteoporosis.
Corrosive esophagitis (can't lie down after taking), nausea, diarrhea, rare jaw osteonecrosis. |
|
|
Term
|
Definition
A bisphosphonate - only one IV!
Inhibits osteoclast activity; reduces bone resorption, remodeling.
Malignancy associated hypercalcemia, Paget's disease, postmenopause osteoporosis.
IV: avoids esophagitis. Nausea, diarrhea, rare jaw osteonecrosis. |
|
|
Term
|
Definition
Stabalizes tubulin, prevents microtubule polymerization, inhibits leukocyte chemotaxis and degranulation.
Acute gout (with NSAIDs)
GI side effects. |
|
|
Term
|
Definition
Inhibits uric acid reabsorption in PCT.
Chronic gout treatment.
Inhibits penicillin secretion. Sulfa allergy. |
|
|
Term
|
Definition
Inhibits xanthine oxidase, preventing formation of xanthine and uric acid.
Chronic gout treatment. Prevent tumor-lysis associated urate nephropathy.
Raises concentration of azathioprine, 6-MP. |
|
|
Term
|
Definition
Recombinant soluble TNF-alpha receptor
RA, psoriasis, ankylosing spondylitis
little toxicity
EtanerCEPT = fake reCEPTor |
|
|
Term
|
Definition
TNF-alpha mouse-human chimeric antibody
Chron's, RA, ankylosing spondylitis
Predisposes to latent TB reactivation
INFLIX pain on TNF |
|
|
Term
|
Definition
Anti-TNF fully-human synthetic antibody RA, psoriasis, ankylosing spondylitis Reactivation of latent TB risk
(Adam was first HUMAN) |
|
|
Term
Opioid analgesics
Mech
Use
Tox |
|
Definition
Morphine, Fentanyl, Codeine, Heroin, Methadone, Merperidine, Dextromethorphan
Agonists at mu opiod receptors, open K channels, close Ca channels, decrease synaptic transmission.
Pain, cough suppression, diarrhea, acute pulmonary edema, maintenance for addicts
Addiction, resp. depression, constipation, miosis, additive CNS depression, sphincter of Oddi tone - pancreatitis. Tolerance does not develop to miosis and constipation.
Treat tox. with naloxone or naltrexone (opiod receptor antagonists) |
|
|
Term
Meperidine
Class?
Special use? |
|
Definition
Opioid
Less sphincter of Oddi effect - usable in pancreatitis. |
|
|
Term
Loperamide
Class?
Special use? |
|
Definition
Opioid
Anti-diarrhea (imodium) |
|
|
Term
Diphenoxylate
Class?
Special use? |
|
Definition
|
|
Term
Dextromethorphan
Class?
Special use? |
|
Definition
|
|
Term
|
Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
|
|
Term
|
Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
|
|
Term
Buprenorphine
Mech
Use?
Tox? |
|
Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
|
|
Term
|
Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
|
|
Term
|
Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
|
|
Term
|
Definition
Very weak opioid agonist; also inhibits 5-HT and NE reuptake.
Chronic pain.
Some opioid toxicity, decreases seizure threshold. |
|
|
Term
| Drugs of choice for tonic-clonic seizures? Mechanism? |
|
Definition
Phenytoin, Carbamazepine, Valproic acid (1st)
Lamotrigine, Topiramate (2nd) Block Na channels |
|
|
Term
Drugs of choice for partial seizures?
Mechanism? |
|
Definition
Gabapentin, Tigabine, Vigabatin, Levetiracetam, Phenobarbital, Benzodiazepines
All increase GABA action by various mechanisms. |
|
|
Term
|
Definition
Na channel inactivation
Tonic-clonic seizures, *prophylaxis/prevent recurrence of status epilepticus, *class IB anti-arrythmic
Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsuitism, lymphadenopathy, megaloblastic anemia, teratogenesis. Drug induced-SLE, P450 induction. Also P450 metabolized. |
|
|
Term
|
Definition
Na channel inactivation
Tonic-clonic seizures, trigeminal neuralgia.
Diploplia, ataxia, *agranulocytosis, *aplastic anemia, liver toxicity, teratogenesis, P450 induction, SIADH, Stevens-Johnson syndrome.
NB: Oxcarbamazepine: same use, fewer AEs |
|
|
Term
|
Definition
Blockes voltage-gated Na channels
Tonic-clonic seizures
Stevens-Johnson syndrome |
|
|
Term
|
Definition
Designed as GABA analog, but mainly blocks Ca channels
Partial seizures, tonic-clonic seizures, peripheral neuropathy, bipolar disorder
Sedation, ataxia |
|
|
Term
|
Definition
Blocks Na channels, increases GABA action
Partial seizures, tonic-clonic
Sedation, mental dulling, kidney stones, weight loss |
|
|
Term
|
Definition
Phenobarbital, pentobarbital, thiopental, secobarbital
Increases GABA action by increasing duration of Cl channel opening
Partial seizures, tonic-clonic, *1st line in pregnant women, children.
Anxiety, insomnia, anesthesia induction Sedation, tolerance, dependance, induces P450. Contraindicated in porphyra (stimulate ALA synthase) |
|
|
Term
|
Definition
Inactivates NA channels, increases GABA concentration
Tonic-clonic (1st), partial, myoclonic, bipolar disorder, *also tonic-clonic + absence
GI distress,
*rare but fatal hepatotoxicity, neural tube defects (CI: preg), tremor, weight gain. |
|
|
Term
|
Definition
Blocks thalamic T-type Ca channels
Absence seizures (1st)
GI distress, fatigue, headache (EFGH), uticaria, Stevens-Johnson syndrome |
|
|
Term
|
Definition
Inhibits GABA reuptake
Partial seizures only |
|
|
Term
|
Definition
Irreversibly inhibits GABA transaminase, raising [GABA]
Partial seizures only |
|
|
Term
|
Definition
Unknown, may modulate GABA and glutamate release
Tonic clonic, partial |
|
|
Term
|
Definition
Blocks voltage gated Na channels and T-type Ca channels
Partial, Tonic-Clonic, Absence |
|
|
Term
|
Definition
Blocks glutamate at NMDA
Partial and Tonic-Clonic; less use b/c toxicity
aplastic anemia, hepatotoxicity |
|
|
Term
| Drugs acting on GABA-A receptor? |
|
Definition
Barbituates, benzodiazepines, alcohol.
An ion channel, GABA increases Cl infux. |
|
|
Term
|
Definition
Baclofen (muscle relaxant)
Gi receptor. Inhibits adenylyl cyclase, K efflux, Ca influx. |
|
|
Term
|
Definition
ion channel, allows Cl influx.
No drugs active here. |
|
|
Term
Benzodiazepines
Mech
Use
Tox
Antidote |
|
Definition
"pams" and "lams": Diazepam, Lorazepam, Triazolam, Temazepam, Oxazepam, Midazolam, Alprazolam &* chlordiazepoxide.
Increase frequency of Cl channel opening at GABA-A receptor.
Anxiety, spasticity, status epilepticus, detoxification (alcohol withdrawal), night terrors (reduces REM sleep), sleepwalking, general anesthetic, hypnotic.
Dependence, additive CNS depression. Less risk of resp. depression and coma than barbituates.
Treat OD with flumazenil (competitive antagonist) |
|
|
Term
| Short acting benzodiazepines? |
|
Definition
Triazolam, Oxazepam, Midazolam (TOM thumb)
Greatest addictive potential. |
|
|
Term
Nonbenzodiazepine hypnotics
Mech
use
tox |
|
Definition
Zolpidem (ambien), zaleplon, eszopiclone
(ZZZs)
Act on benzodiazepine receptor subtype, reversed by flumazenil.
Insomina.
Ataxia, headaches, confusion. Short duration - hepatic metabolism. Less AEs and dependance than older benzodiazepines. |
|
|
Term
Inhaled anesthetics
Mech
Effects
Tox |
|
Definition
"fluranes": Halothane, Enflurane, Isoflurane, Sevoflurane, Methoxyflurane, nitrous oxide
Mechanism unknown!
Myocardial depression, resp. depression, nausea/emesis, increased cerebral blood flow, decreased cerebral metabolic demand
*Hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane), malignant hyperthermia (tx: dantrolene), expansion of trapped gas (NO2) |
|
|
Term
|
Definition
PCP analog, blocks NDMA receptor
"dissociative anesthetic". CV stimulant.
Disorientation, hallucination, bad dreams. Increased cerebral blood flow. |
|
|
Term
|
Definition
Potentiates GABA
Rapid anesthesia induction for short procedures. |
|
|
Term
|
Definition
Depolarizing neuromuscular blocker.
Cannot reverse with cholinesterase inhibitor. |
|
|
Term
Nondepolarizing neuromuscular blocking drugs
names? mech? reversal? |
|
Definition
"curarines": Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium.
Competitive for ACh receptors.
Reversable with acetylcholinesterase inhibitor |
|
|
Term
|
Definition
Blocks ryanodine receptor on muscle SR
Used in treatment of malignant hyperthermia, neuroleptic malignant syndrome |
|
|
Term
|
Definition
BALSAC
Bromocriptine: dopamine agonist
Amantidine: increase dopamine release
L-DOPA/carbidopa: dopamine precursor
Selegiline: MAO-B inhibitor, prevent dopamine breakdown.
Antimuscarinics: Benztropine, best for drug-induced Parkinsonism
COMT inhibitors: entacapone, tolcapone. Prevent L-DOPA degradation |
|
|
Term
|
Definition
NMDA receptor antagonist; prevents excitotoxicity
Alzheimer's
Dizziness, confusion, hallucination |
|
|
Term
|
Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
|
|
Term
|
Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
|
|
Term
|
Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
|
|
Term
|
Definition
5-HT-1B/1D antagonist. Vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release. Halflife < 2hrs.
Acute migraine, cluster headaches.
Coronary vasospasm, (CI: CAD, Prinzmetals) mild tingling |
|
|
Term
Dopamine agonists?
Use?
Classes? |
|
Definition
Ergot: Bromocriptine, Pergolide
Nonergot: Pramipexole, Ropinerole
Parkinson's disease, (Bromo: Prolactinoma) |
|
|
Term
Methylphenidate
Mech
Use
Tox |
|
Definition
CNS stimulant, increases catecholamines at synaptic cleft, esp. NE and dopamine
ADHD, narcolepsy, appetite control
Myosis, prolonged wakefullness, delusions, hallucinations, fever. |
|
|
Term
Dextroamphetamine
Mech
Use
Tox |
|
Definition
CNS stimulant, increases catecholamines at synaptic cleft, esp. NE and dopamine
ADHD, narcolepsy, appetite control
Myosis, prolonged wakefullness, delusions, hallucinations, fever. |
|
|
Term
Mixed amphetamine salts
Mech
Use
Tox |
|
Definition
CNS stimulant, increases catecholamines at synaptic cleft, esp. NE and dopamine
ADHD, narcolepsy, appetite control
Myosis, prolonged wakefullness, delusions, hallucinations, fever. |
|
|
Term
|
Definition
Typical antipsychotic, blocks dopamine D2 receptors (increasing cAMP).
HIGH POTENCY = greater EPS effects.
Schizophrenia (+ sx), psychosis, acute mania, Tourette's
Lipid storage, slow removal. Extrapyramidal side effects. Hyperprolactinemia. Antimuscarinic, antiadrenergic, antihistamine effects. Neuroleptic malignant syndrome (FEVER). Tardive dyskinesia. |
|
|
Term
Trifluoperazine
Mech
Use
Tox |
|
Definition
Typical antipsychotic, blocks dopamine D2 receptors (increasing cAMP).
HIGH POTENCY = greater EPS effects.
Schizophrenia (+ sx), psychosis, acute mania, Tourette's
Lipid storage, slow removal. Extrapyramidal side effects. Hyperprolactinemia. Antimuscarinic, antiadrenergic, antihistamine effects. Neuroleptic malignant syndrome (FEVER). Tardive dyskinesia. |
|
|
Term
|
Definition
Typical antipsychotic, blocks dopamine D2 receptors (increasing cAMP).
HIGH POTENCY = greater EPS effects.
Schizophrenia (+ sx), psychosis, acute mania, Tourette's
Lipid storage, slow removal. Extrapyramidal side effects. Hyperprolactinemia. Antimuscarinic, antiadrenergic, antihistamine effects. Neuroleptic malignant syndrome (FEVER). Tardive dyskinesia. |
|
|
Term
|
Definition
Typical antipsychotic, blocks dopamine D2 receptors (increasing cAMP).
LOW POTENCY = greater anti-muscarinic, -adrenergic, -histamine AEs.
Schizophrenia (+ sx), psychosis, acute mania, Tourette's
Lipid storage, slow removal. Extrapyramidal side effects. Hyperprolactinemia. Antimuscarinic, antiadrenergic, antihistamine effects. Neuroleptic malignant syndrome (FEVER). Tardive dyskinesia.
*Retinal deposits |
|
|
Term
|
Definition
Typical antipsychotic, blocks dopamine D2 receptors (increasing cAMP).
LOW POTENCY = greater anti-muscarinic, -adrenergic, -histamine AEs.
Schizophrenia (+ sx), psychosis, acute mania, Tourette's
Lipid storage, slow removal. Extrapyramidal side effects. Hyperprolactinemia. Antimuscarinic, antiadrenergic, antihistamine effects. Neuroleptic malignant syndrome (FEVER). Tardive dyskinesia.
*Corneal deposits. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Olanzapine: OCD, anxiety, depression, mania, Tourette's
Fewer EPS and anticholinergic AEs than typicals. Olanzapine: Weight gain. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Fewer EPS and anticholinergic AEs than typicals. Clozapine: AGRANULOCYTOSIS, weight gain. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Fewer EPS and anticholinergic AEs than typicals. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Fewer EPS and anticholinergic AEs than typicals. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Fewer EPS and anticholinergic AEs than typicals. |
|
|
Term
|
Definition
Atypical antipsychotic. Blocks 5-HT2, dopamine, alpha, and H1 receptors.
Schizophrenia, positive AND negative sx.
Fewer EPS and anticholinergic AEs than typicals. |
|
|
Term
|
Definition
Not established; inhibit IP3 cascade?
Bipolar disorder, SIADH
LMNOP: movement (tremor), Nephrogenic DI, hypOthyroidism, pregnancy CI (Ebstein abnormality, malformation of great vessels).
Follows Na in kidney reabsorption - any changes to that will affect Li levels. |
|
|
Term
|
Definition
5-HT1 agonist.
Generalized anxiety disorder (NOT panic disorder, social phobia, specific phobias)
Good; no sedation, addiction, tolerance. No interaction with alcohol (unlike BZD, barbituates) |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy. Imipramine: bedwetting.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Imipramine is tertiary amine, more anticholinergic AEs (avoid in elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Amitriptyline is tertiary amine, more anticholinergic effects (avoid in elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Desipramine: least sedating, but lowest seizure threshold. Secondary amine, fewer anticholinergic AEs (better for elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Nortriptylene: Secondary amine, fewer anticholinergic AEs (better for elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Clomipramine: Tertiary amine, more anticholinergic AEs (avoid in elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Doxepin: Tertiary amine, more anticholinergic AEs (avoid in elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
|
Definition
TCA. Blocks NE and 5-HT reuptake.
Depression, fibromyalgia, painful diabetic neuropathy.
Toxicity: also...
Inhibits cardiac fast Na channels: arrythmias, hypoTN.
Antimuscarinic: Hyperthermia, flushing, dilated pupils, ileus, urinary retention, sinus tachycardia.
Inhibits alpha1: vasodilation, orthostatic hypoTN.
Inhibits H1: sedation.
Amoxapine: Secondary amine, less anticholinergic AEs (better for elderly).
Severe: CCC: Convulsions, Cardiotoxicity, Coma. Treat with NaHCO3 (urine alkalinzation). |
|
|
Term
Tertiary TCAs?
Secondary TCAs?
Difference? |
|
Definition
3*: Imipramine, Amitriptyline, Clomipramine, Doxepin
2*: Desipramine, Nortriptyline, Amoxapine
3* has more anticholinergic AEs (ACID). 2* has fewer, better for elderly (DAN). |
|
|
Term
Fluoxetine
Mech
Use
Tox
Antidote |
|
Definition
SSRI. 2-4 weeks before effect.
Depression, OCD, bulemia, social phobias.
Fewer AEs than TCAs. GI distress, sexual dysfunction (anorgasmia). Serotonin syndrome with MAOis - hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures. Antidote: Cyproheptadine (5-HT antagonist). |
|
|
Term
Paroxetine
Mech
Use
Tox
Antidote |
|
Definition
SSRI. 2-4 weeks before effect.
Depression, OCD, bulemia, social phobias.
Fewer AEs than TCAs. GI distress, sexual dysfunction (anorgasmia). Serotonin syndrome with MAOis - hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures. Antidote: Cyproheptadine (5-HT antagonist). |
|
|
Term
Sertraline
Mech
Use
Tox
Antidote |
|
Definition
SSRI. 2-4 weeks before effect.
Depression, OCD, bulemia, social phobias.
Fewer AEs than TCAs. GI distress, sexual dysfunction (anorgasmia). Serotonin syndrome with MAOis - hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures. Antidote: Cyproheptadine (5-HT antagonist). |
|
|
Term
Citalopram
Mech
Use
Tox
Antidote |
|
Definition
SSRI. 2-4 weeks before effect.
Depression, OCD, bulemia, social phobias.
Fewer AEs than TCAs. GI distress, sexual dysfunction (anorgasmia). Serotonin syndrome with MAOis - hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures. Antidote: Cyproheptadine (5-HT antagonist). |
|
|
Term
|
Definition
5-HT receptor antagonist
Use for serotonin syndrome (SSRI + MAOi overdose) |
|
|
Term
|
Definition
SNRI: 5HT and NE reuptake inhibitor.
Depression. Venlaflaxine also for anxiety.
HyperTN, stimulant, sedation, nausea. |
|
|
Term
|
Definition
SNRI: 5HT and NE reuptake inhibitor (Duloxetine: greater NE effect).
Depression. Duloxetine also for diabetic peripheral neuropathy.
HyperTN, stimulant, sedation, nausea. |
|
|
Term
|
Definition
MAOi. Increases NE, 5HT, dopamine.
Atypical depression, anxiety, hypochondriasis.
Hypertensive crisis with tyramine ingestion (wine, cheese) or beta-agonists. CNS stimulation. Contraindicated with SSRIs or meperidine to prevent serotonin syndrome. |
|
|
Term
Tranylcypromine
Mech
Use
Tox |
|
Definition
MAOi. Increases NE, 5HT, dopamine.
Atypical depression, anxiety, hypochondriasis.
Hypertensive crisis with tyramine ingestion (wine, cheese) or beta-agonists. CNS stimulation. Contraindicated with SSRIs or meperidine to prevent serotonin syndrome. |
|
|
Term
|
Definition
MAOi. Increases NE, 5HT, dopamine.
Atypical depression, anxiety, hypochondriasis.
Hypertensive crisis with tyramine ingestion (wine, cheese) or beta-agonists. CNS stimulation. Contraindicated with SSRIs or meperidine to prevent serotonin syndrome. |
|
|
Term
|
Definition
Selective MAOi-B inhibitor. Increases NE, 5HT, dopamine.
Atypical depression, anxiety, hypochondriasis. Selegiline also for Parkinson's.
Hypertensive crisis with tyramine ingestion (wine, cheese) or beta-agonists. CNS stimulation. Contraindicated with SSRIs or meperidine to prevent serotonin syndrome. |
|
|
Term
|
Definition
Atypical antidepressant. Increases NE and dopamine by unknown mechanism.
Depression, smoking cessation.
Stimulant, headache, seizure in bulemic patients. No sexual side effects (vs. SSRIs) |
|
|
Term
|
Definition
Atypical antidepressant. Alpha-2 antagonist (increases NE and 5HT release), also 5HT2 and 5HT3 receptor antagonist.
Depression.
Sedation, increased appetite, weight gain, dry mouth. |
|
|
Term
|
Definition
Atypical antidepressant. Blocks NE reuptake.
Depression.
Sedation, orthostatic hypotension. |
|
|
Term
|
Definition
Atypical antidepressant. Mostly inhibits serotonin reuptake.
Insomnia - high doses needed for antidepressant effects.
Sedation, nasea, priapism (trazoBone), postural hypotension. |
|
|
Term
| Evolution of EPS side effects? |
|
Definition
4 hrs: acute dystonia (muscle spasm, stiffness, oculogyric crisis)
4 dys: akinesia (parkinsonian)
4 wks: akathisia (anxiety, restlessness)
4 mo: tardive dyskinesia (involuntary perioral movements, choreoathetoid movements, irreversible) |
|
|
Term
|
Definition
Osmotic diuretic.
Shock, drug OD, high intracranial pressure.
Pulmonary edema, dehydration. CI: anuria, CHF. |
|
|
Term
|
Definition
Carbonic anhydrase inhibitor. Self-limited NaHCO3 diuresis.
Glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness.
Hyperchloremic metabolic acidosis (normal anion gap), neuropathy, NH3 toxicity, sulfa allergy. |
|
|
Term
|
Definition
Sulfonamide loop diuretic. Inhibits Na/K/Cl cotransport on thick ascending limb. Increases calcium excretion. Also increases prostaglandins, increasing renal blood flow/GFR.
Edema, HTN, hypercalcemia.
OHDANG!: Ototoxicity, Hypokalemia, Dehydration, Allergy (sulfa), Nephritis (interstitial), Gout (hyperuricemia). Also diuretic alkalosis. |
|
|
Term
Ethacrynic acid
Mech
Use
Tox |
|
Definition
Same as furosemide, but not a sulfa drug.
Pts with sulfa allergies.
Same as furosemide except allergies. |
|
|
Term
Hydrochlorothiazide
Mech
Use
Tox |
|
Definition
Inhibit NaCl reabsorption in early DCT. Reduces Ca excretion (only one!)
HTN, CHF, hypercalciuria, nephrogenic DI.
Hypokalemia, diuretic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia. Sulfa allergy. |
|
|
Term
|
Definition
K sparing diuretic. Aldosterone competitive antagonist. Acts in cortical collecting duct.
Hyperaldosteronism, K depletion, CHF, hirsuitism.
Hyperkalemia, anti-androgen effects (gynecomastia), acidemia. |
|
|
Term
|
Definition
K sparing diuretic. Aldosterone competitive antagonist. Acts in cortical collecting duct.
Hyperaldosteronism, K depletion, CHF.
Hyperkalemia, acidemia. Like spironolactone but with less anti-androgenic effects. |
|
|
Term
|
Definition
K sparing diuretic. Blocks Na channels in cortical collecting duct - similar affect to aldosterone antagonists.
Hyperaldosteronism, K depletion, CHF.
Hyperkalemia, acidemia. |
|
|
Term
|
Definition
K sparing diuretic. Blocks Na channels in cortical collecting duct - similar affect to aldosterone antagonists.
Hyperaldosteronism, K depletion, CHF.
Hyperkalemia, acidemia. |
|
|
Term
| What is "contraction alkalosis"? |
|
Definition
| In low volume state, angiotensin II concentration increases. One effect is increased Na/H exchange in PCT, causing alkalosis. |
|
|
Term
| What is "paradoxical aciduria"? When is it seen? |
|
Definition
Seen in hypokalemic state.
In hypokalemia, Na/H exchange is favored over Na/K exchange in PCT. This causes aciduria, even if body is in alkalotic state.
One mechanism of diuretic metabolic alkalosis. |
|
|
Term
|
Definition
ACE inhibitor. Reduces ATII levels, raises bradykinin levels. Increases renin (loss of feedback inhibition).
HTN, CHF, prevention of diabetic renal disease.
CAPTOPRIL: Cough, Angioedema, Potassium increase, Taste changes, hypOtension, Pregnancy CI, Rash, Increased renin, Low ATII. Avoid with bilateral renal artery stenosis: kidneys rely on ATII mediated efferent arteriole constriction to maintain GFR. |
|
|
Term
|
Definition
ACE inhibitor. Reduces ATII levels, raises bradykinin levels. Increases renin (loss of feedback inhibition).
HTN, CHF, prevention of diabetic renal disease.
CAPTOPRIL: Cough, Angioedema, Potassium increase, Taste changes, hypOtension, Pregnancy CI, Rash, Increased renin, Low ATII. Avoid with bilateral renal artery stenosis: kidneys rely on ATII mediated efferent arteriole constriction to maintain GFR. |
|
|
Term
|
Definition
ACE inhibitor. Reduces ATII levels, raises bradykinin levels. Increases renin (loss of feedback inhibition).
HTN, CHF, prevention of diabetic renal disease.
CAPTOPRIL: Cough, Angioedema, Potassium increase, Taste changes, hypOtension, Pregnancy CI, Rash, Increased renin, Low ATII. Avoid with bilateral renal artery stenosis: kidneys rely on ATII mediated efferent arteriole constriction to maintain GFR. |
|
|
Term
|
Definition
|
|
Term
|
Definition
GnRH analog; agonist when pulsatile, antagonist when continuous.
Infertility (pulsatile use), prostate cancer (continuous use), uterine fibroids
Anti-androgen sx, nausea, vomiting. |
|
|
Term
|
Definition
Direct androgen receptor agonist
Treat hypogonadism, develop secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat ER-positive breast cancer.
Masculinization in females; reduces intratesticular testosterone in males (feedback inhibition), causing gonadal atrophy. Premature closure of epiphyseal plates. Raises LDL, lowers HDL. |
|
|
Term
|
Definition
aka Propecia
5-alpha-reductase inhibitor.
BPH, male pattern baldness. |
|
|
Term
|
Definition
Nonsteroidal competitive androgen inhibitor.
Prostate cancer. |
|
|
Term
| Ethinyl estradiol, mestrinol |
|
Definition
estrogen analogs
Hypogonadism, ovarian failure, menstrual abnormalities, hormone replacement therapy in post-menopausal women, androgen-dependent prostate cancer.
Increases endometrial carcinoma risk, bleeding in post-menopausal women, increased thrombosis risk. CI: ER positive breast cancer, history of DVTs. |
|
|
Term
|
Definition
SERM. Partial agonist at hypothalamus; prevents normal feedback inhibition, increases release of LH and FSH from pituitary, stimulates ovulation.
Infertility, PCOS.
Hot flashes, ovarian enlargement, multi-pregnancy, visual disturbances. |
|
|
Term
|
Definition
SERM. Antagonist on breast, partial agonist on uterus.
Treat ER-positive breast cancer.
Increase in endometrial cancer risk. |
|
|
Term
|
Definition
SERM. Agonist on bone; antagonist on breast AND uterus.
Osteoporosis.
No endometrial cancer risk (unlike tamoxifen) |
|
|
Term
|
Definition
Aromatase inhibitor.
Breast cancer in post-menopausal women. |
|
|
Term
|
Definition
Aromatase inhibitor.
Breast cancer in post-menopausal women. |
|
|
Term
|
Definition
aka DepoProvera
Progesterone analog. Reduce growth and increase vascularization of endometrium.
Oral contraceptive, treatment of endometrial cancer, abnormal bleeding. |
|
|
Term
|
Definition
aka RU-486
Competitive inhibitor of progesterone
Termination of pregnancy, give with misoprostol (PGE1)
Heavy bleeding, GI distress (N/V, anorexia), abdominal pain |
|
|
Term
| Synthetic estrogen/progestin combo |
|
Definition
Oral contraceptive. Prevents estrogen rise, LH surge, no ovulation.
Reliable contraception, decrease endometrial and ovarian cancer risk, decrease ectopic pregnancy risk, decrease pelvic infections, regular menses.
Must take daily, no STD protection, *increases triglycerides, *depression, weight gain, nausea, HTN, hypercoagulability.
CI: smokers > 35 years old - increase CV risk, history of thrombus, stroke, estrogen dependent tumor. |
|
|
Term
|
Definition
PGE2 analog: Causes cervical dilation, uterine contraction.
Induces labor. |
|
|
Term
|
Definition
B2-agonist, relaxes uterus.
tocolytic.
(baby "returns to dreams") |
|
|
Term
|
Definition
B2-agonist
relaxes uterus
tocolytic |
|
|
Term
|
Definition
PGE1 analog, uterine contractions
Terminate pregnancy (with mifepristone), induce labor |
|
|
Term
|
Definition
Inhibit cGMP phosphodiesterase, raise cGMP, smooth muscle relax in corpus cavernosum, erection.
Erectile dysfunction.
Headache, flushing, dyspepsia, impaired blue-green color vision. CI: nitrate use - severe hypotension (excess cGMP without PDE!)
3H: Headache, Heartburn, Hypotension |
|
|
Term
|
Definition
|
|
Term
|
Definition
| GnRH analog - see leuprolide |
|
|
Term
|
Definition
| GnRH analog - see leuprolide |
|
|
Term
|
Definition
| GnRH analog - see leuprolide |
|
|
Term
Theophylline
Mech?
Use?
Tox? |
|
Definition
Inhibits PDE, raising cAMP, causes bronchodilation.
Anti-asthma, but narrow therapeutic index.
Cardiotoxicity, neurotoxicity.
(blocks actions of adenosine) |
|
|
Term
Cromolyn Sulfate
Mech?
Use?
Tox? |
|
Definition
Prevents mast cell degranulation.
Asthma prophylaxis (not acute tx).
Rare toxicity |
|
|
Term
|
Definition
5-lipoxygenase inhibitor; blocks conversion of arachidonic acid to leukotrienes
Asthma prophylaxis |
|
|
Term
|
Definition
Block leukotriene D4 receptors
Asthma, esp. aspirin induced asthma |
|
|
Term
|
Definition
Block leukotriene D4 receptors
Asthma, esp. aspirin induced asthma |
|
|
Term
|
Definition
Removes excess sputum, does not remove cough reflex
Expectorant |
|
|
Term
N-acetylcysteine
Mech?
Use? |
|
Definition
Mucolytic
Loosen mucus plugs in CF pts
(also used in acetominophen overdose) |
|
|
Term
|
Definition
Endothelin-1 receptor antagonist
Pulmonary HTN, decreases pulm. vasc. resistance |
|
|
Term
|
Definition
Anti-IgE antibody, prevents IgE binding to mast cells.
Prophylaxis for allergen induced asthma attack. |
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Term
|
Definition
1st generation H1 blocker
Allergy, motion sickness, sleep aid
Sedation, anti-muscarinic, anti-alpha-adrenergic |
|
|
Term
|
Definition
1st generation H1 blocker
Allergy, motion sickness, sleep aid
Sedation, anti-muscarinic, anti-alpha-adrenergic |
|
|
Term
|
Definition
1st generation H1 blocker
Allergy, motion sickness, sleep aid
Sedation, anti-muscarinic, anti-alpha-adrenergic |
|
|
Term
|
Definition
2nd gen H1 blocker.
Allergy
Less CNS entry, so far less sedating than 1st gen |
|
|
Term
|
Definition
2nd gen H1 blocker.
Allergy
Less CNS entry, so far less sedating than 1st gen |
|
|
Term
|
Definition
2nd gen H1 blocker.
Allergy
Less CNS entry, so far less sedating than 1st gen |
|
|
Term
|
Definition
2nd gen H1 blocker.
Allergy
Less CNS entry, so far less sedating than 1st gen |
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