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High yield pharmacology drugs
Source: Kaplan Review Series
323
Pharmacology
Graduate
03/27/2012

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Term
Ach
Definition
Active at muscarinic and nicotonic receptors. Short half life, no clinical use.
Term
Bethanechol
Definition
Muscarinic activity. Used to treat ileus (postop/neurogenic) and urinary retention.
Term
Methacholine
Definition
Greater muscarinic activity than nicotonic. Used to diagnose bronchial hyperreactivity (methacholine challenge test)
Term
Pilocarpine
Definition
Muscarinic activity. Used to tx. glaucoma (topical) and xerostomia as seen in Sjogren's syndrome (dry mouth).
Term
Edrophonium
Definition
Short acting acetylcholinesterase inhibitor used to diagnose myasthenia gravis. Used to differentiate myasthenia from cholinergic crisis as well.
Term
Physostigmine
Definition
acetylcholinesterase inhibitor that is a tertiary amine (can enter CNS). Used to tx. glaucoma and is useful as an antidote for atropine overdose.
Term
Neostigmine/pyridostigmine
Definition
Quaternary amine acetylcholinesterase inhibitor(no CNS entry). Used to treat ileus, urinary retention, myasthenia, and to reverse nondepolarizing NM blockers (cuarine-like drugs).
Term
Donepezil, tacrine
Definition
Lipid soluble acetylcholinesterase inhibitor. Used in the treatment of Alzheimer's disease.
Term
Organophosphate (-phate ending), echothiophate, malathion, parathion, sarin.
Definition
Lipid soluble irriversible acetylcholinesterase inhibitor. Can be used to treat glaucoma. Used as insecticides and as nerve gas.
Term
Atropine
Definition
tertiary amine (enters CNS) muscarinic blocker. prototypical. Effects in order of increasing dose include decreased secretions, mydriasis and cycloplegia, hyperthermia, tachycardia, sedation, urinary retention and constipation, and behavioral excitation and hallucinations.
Term
Tropicamide
Definition
M blocker useful in ophthalmology (topical application).
Term
Ipratropium
Definition
M blocker used in asthma and COPD (inhalational)-no CNS entry, no change in mucus viscosity.
Term
Scopolamine
Definition
M blocker used in motion sickness, causes sedation and short-term memory block.
Term
Benzotropine, trihexyphenidyl
Definition
Lipid soluble (CNS entry) used in parkinsonism and in acute extrapyramidal symptoms induced by antipsychotics.
Term
hexamethonium and mecamylamine
Definition
Ganglion blocking agent which is useful to differentiate a BP reflex from being drug induced or not.
Term
Phenylephrine
Definition
Alpha 1 receptor agonist useful as a nasal decongestand and in ophthalmologic use (mydriasis without cycloplegia).
Term
Methoxamine
Definition
Alpha 1 agonist useful in paroxysmal atrial tachycardia through the vagal reflex.
Term
Clonidine, Methyldopa
Definition
Alpha 2 receptor agonist useful in treating mild to moderate hypertension.
Term
Isoproterenol
Definition
Beta agonist (B1=B2) useful in treating bronchospasm, heart block, and bradyarrhythmias. Side effects include flushing, angina and arrhythmias.
Term
Dobutamine
Definition
Beta agonist (B1>B2) useful in congestive heart failure.
Term
albuterol, and terbutaline
Definition
Selective B2 agonists useful in the tx. of asthma.
Term
Ritodrine
Definition
Beta agonist used to prevent premature labor.
Term
Norepinephrine
Definition
Mixed acting Alpha and Beta agonist that increases pulse pressure and has a risk of causing potential reflex bradycardia. No effect on B2 receptors.
Term
Epinephrine
Definition
Mixed Alpha and Beta agonist that has 3 different patterns of activity depending on dosage.
Term
Tyramine
Definition
Indirect acting adrenergic receptor agonists that can cause hypertensive crisis (don't take with MAOa inhibitors or with red wine or cheese.
Term
Amphetamines
Definition
Indirect acting adrenergic receptor agonist that can cause extreme alpha 1 and beta 1 overreactivity. Can be used in narcolepsy and as a psychostimulant due to central release of DA, NE and serotonin.
Term
Ephedrine
Definition
Indirect acting adrenergic receptor agonists useful as an OTC cold medication.
Term
Phentolamine
Definition
Competitive Alpha inhibitor that can be used to tx. hypertension and benign prostatic hyperplasia. Gets outcompeted in pheochromocytoma.
Term
Phenoxybenzamine
Definition
Non-competitive Alpha inhibitor that can be used to tx. hypertension and benign prostatic hyperplasia. Drug of choice for pheochromocytoma. Use this before a B blocker in PCC.
Term
Prazosin, doxazosin, terazosin, tamsulosin
Definition
Selective alpha 1 blocker useful in the treatment of hypertension. Also useful to decrease urinary frequency and nocturia in those with BPH. Good on lipid profile.
Term
Acebutolol
Definition
Beta 1 selective beta blocker partial agonist (Class II antiarrhythmic). Can cause mild sedation.
Term
Atenolol
Definition
B1 selective beta blocker that is water soluble (no sedation effects). Can cause an increase of blood lipids.
Term
Metoprolol
Definition
B1 selective Beta blocker that can cause mild sedation. Can cause an increase in blood lipids.
Term
Pindolol
Definition
Beta blocker partial agonist that can cause mild sedation.
Term
Propranolol
Definition
Highly sedating beta blocker (Class II antiarrhythmic) that is useful for treating tremors, fear, etc. Can increase blood lipids.
Term
Timolol
Definition
Moderately sedative beta blocker that can increase blood lipids. Can be useful in glaucoma treatment.
Term
Labetalol and carvedilol
Definition
Combined alpha 1 and beta blocking drug useful in CHF.
Term
Sotalol
Definition
Class III antiarrhythmic beta blocker (Potassium channel blockade). Useful in life threatening ventricular arrhythmias.
Term
Quinidine
Definition
Class 1A antiarrhythmic (blocks fast Na channels in the activated state). Also causes muscarinic receptor blockade, alpha blockade, and can cause cinchonism (GI, tinnitus, ocular dysfunction, and CS excitation) and torsades.
Term
Procainamide
Definition
Class 1A antiarrhythmic (blocks fast Na channels in the activated state). Metabolized via N-acetyltransferase to form an active metabolite. Can cause SLE-like syndrome especially in slow acetylators and torsades.
Term
Lidocaine
Definition
Class 1B antiarrhythmic (blocks fast Na channels in the inactivated state). Useful antidote in digoxin toxicity and as post MI therapy due to its selectivity for hypoxia damaged cardiac muscle. Given IV to avoid first pass metabolism.
Term
Mexiletine
Definition
Class 1B antiarrhythmic (blocks fast Na channels in the inactivated state). Useful antidote in digoxin toxicity and as post MI therapy due to its selectivity for hypoxia damaged cardiac muscle. Given orally and thus can be used out patient unlike lidocaine.
Term
Flecainide
Definition
Class 1C antiarrhythmic (blocks fast Na channels in the resting state). Can lead to sudden death post MI and has limited usage.
Term
Esmolol
Definition
Class II antiarrhythmic drug (cardioselective Beta Blocker) not useful in prophylaxis post-MI but beneficial after acute SVTs.
Term
Amiodarone
Definition
Class III Potassium channel blocker. Mimics classes I, II, III an IV. Can cause pulmonary fibrosis (hapten formation via idionation), smurf skin (idonation of carbohydrates), and thyroid dysfunction.
Term
Verapamil
Definition
Class IV antiarrhythmic. Decreases SA and AV nodal activity by blocking calcium channels. Useful in SVTs and in reducing hypertension by causing smooth muscle relaxation. Can cause constipation and AV block. Additive AV block with digoxin or B blockers. Also, can displace digoxin from tissue binding sites.
Term
Diltiazem
Definition
Class IV antiarrhythmic. Decreases SA and AV nodal activity by blocking calcium channels. Useful in SVTs and in treating hypertension. Can cause AV block. Additive AV block with digoxin or B blockers.
Term
adenosine
Definition
Unclassified antiarrhythmic used to increase Gi-coupled receptor activity. DOC for paroxysmal SVT and AV nodal arrhythmias. Antagonized by theophylline and caffeine (methylxanthines)
Term
Magnesium
Definition
Unclassified antiarrhythmic used to treat torsades.
Term
Reserpine
Definition
Antihypertensive drug that acts by destroying the vesicles of norepinephrine peripherally. Also decreases the norepinephrine, dopamine, and serotonin in the CNS. Has a serious risk of depression due to this, and can increase GI secretions by up regulation the PANS.
Term
Guanethidine
Definition
antihypertensive drug that enters sypathetic nerve terminals and bind to the vesicles of NE, inhibiting release. Antagonized by tricyclic antidepressants.
Term
Hydralazine
Definition
Antihypertensive direct acting arteriolar dilator that is useful in moderate to severe hypertension. Can cause SLE-like syndrome. Relatively safe in pregnancy.
Term
Nitroprusside
Definition
Antihypertensive that dilates both arterioles and venules via its direct action. Can cause cyanide toxicity.
Term
Minoxidil
Definition
Antihypertensive drug that acts by opening potassium channels and hyperpolarizing smooth muscle. Results in arteriolar vasodilation selectively. Often used to treat severe hypertension and has been found to be effective in treating male pattern baldness. Can cause hypertrichosis (abnormal hair growth).
Term
Diazoxide
Definition
Antihypertensive drug that acts by opening potassium channels and hyperpolarizing smooth muscle. Results in arteriolar vasodilation selectively. Used in hypertensive emergencies. Can cause hyperglycemia by reducing insulin release.
Term
Nifedipine
Definition
Dihydropyridine calcium channel blocker that can reduce TPR by relaxing smooth muscle. Also useful in treating vasospastic angina. Side effects include reflex tachycardia and gingival hyperplasia.
Term
Captopril
Definition
ACE inhibitor used in the treatment of hypertension. Can cause a dry cough, hyperkalemia, and angioedema. Contraindicated in pregnancy.
Term
Bosentan
Definition
Endothelin antagonist used to vasodilate vessels in hypertensive patients. Conraindicated in pregnancy. Used to treat pulmonary hypertension.
Term
Epoprostenol
Definition
prostacyclin (PGI2) used to cause vasodilation in hypertensive patients. Contraindicated in pregnancy. Needs slow IV infusion and inpatient care. Used to treat pulmonary hypertension. Platelet stabilizer and vasodilator
Term
Sildenafil
Definition
Type V phosphodiesterase inhibitor which causes pulmonary artery relaxation and decreases pulmonary hypertension by increasing cGMP levels. Used to treat erectile dysfunction as well.
Term
Digoxin
Definition
Inhibitor of cardiac Na/K ATPase with the goal of increasing intracellular calcium levels and increasing the contractility of a heart in heart failure. Need caution in renal impairment. Useful for CHO and SVTs (except Wolff-Parkinson-White syndrome). Do not use in hypokalemic patients (Loop and thiazide diuretic usage patients) or with quinidine or verapamil.
Term
inamrinone, milrinone
Definition
Phosphodiesterase inhibitor. Increase the cAMP levels in the heart to increase inotropy. Also, the increase in cAMP of smooth muscle helps to decrease TPR. Useful in CHF.
Term
Spironolactone
Definition
Loop diuretic used in CHF patients. Primarily treats backward failure (passive congestion). Blocks aldosterone and androgen receptors.
Term
Nesiritide
Definition
Recombinant form of human B-type naturetic peptide. Useful in treating acutely decompensated CHF. Expensive.
Term
Carvedilol
Definition
B1 selective beta blocker useful in treating non-vasospastic angina; particularly angina of effort.
Term
Isosorbide
Definition
Nitrate used to treat angina of effort by allowing for vasodilation through increased NO levels.
Term
Ranolazine
Definition
Blocker of the late inward sodium current which cause increased sodium levels (and thereby increased calcium levels) in ischemic cardiac myocytes. Used to treat angina. Results in decreased end diastolic pressure and improvement of diastolic coronary flow. Contraindicated in patients with long QT syndrome due to QT prolongation effects. Also contraindicated in patients taking drugs which already prolong the QT interval (magnesium, etc.).
Term
Mannitol
Definition
osmotic diuretic that inhibits water reabsorption throughout the tubule. Useful in IOP glaucoma, to decrease intracerebral pressure, and in oliguric states (rhabdomyolysis) as caused by some drugs (statins). Can cause acute hypovolemia.
Term
Acetazolamide, dorzolamide
Definition
Carbonic anhydrase inhibitor that results in a decreased formation of hydrogen ions inside PCT cells, decreased sodium/hydrogen antiport activity, increased sodium and HCO3 levels in the lumen of the PCT, and ultimately increased diuresis. Useful in glaucoma, acute mountain sickness, and in metabolic alkalosis. Side effects include hypokalemia, acidosis, hyperchloremia, paresthesias, renal stones and sulfonamide hypersensitivity.
Term
furosemide, ethacrynic acid, torsemide
Definition
Loop diuretic: inhibits the Na/K/2Cl transporter of the TAL and results in decreased intracellular K in TAL, decreased back diffusion of K, decreased positive potential of the cells in the TAL, decreased CA and Mg reabsorption, and increased diuresis. Used in acute pulm. edema, HF, HTN, refractory edema, ARF, and hypercalcemic states. Co-administration with NSAIDS can cancel the antihypertensive action of loop diuretics due to the inhibition of prostaglandins. Can see sulfonamide hypersensitivity and ototoxicity with this drug, especially with co-admin. of aminoglycosides.
Term
hydrochlorothiazide, indapamide, metolazone
Definition
Thiazide diuretic: blocks the Na/Cl transporter of the DCT and increased luminal Na and Cl in the lumen, leading to diuresis. Used in HTN, CHF, nephrolithiasis (calcium stones), and neprogenid ciabetes insipidus. Can see sulfonamide hypersensitivity, hypokalemia, hypercalcemia, and hpyeruricemia. Also can cause hyperglycemia and hyperlipidemia.
Term
Spironolactone, eplerenone
Definition
potassium sparing diuretic due to its anagonism of aldosterone receptors. Has antiandrogenic uses to treat female hirsutism as well as being an adjunct to K wasting diuretics in HF or HTN patients.
Term
Amiloride
Definition
potassium sparing diuretic that acts by blocking sodium channels. Adjunct to K wasting diuretics and to treat lithium induced nephrogenic diabetes insipidus.
Term
triamterene
Definition
potassium sparing diuretic that acts by blocking sodium channels. Adjunct to K wasting diuretics.
Term
lovastatin
Definition
HMG-CoA redutase inhibitor used to treat hyperlipidemia. Results in decreased liver cholesterol, increased LDL receptor expression, decreased plasma LDL, and decreased VLDL synthesis (causing decreased hypertriglycemia). Can cause myalgia, rhabdomyolysis, and hepatotoxicity. Omeprazole and grapefruit juice can increase blood levels of this drug to unsafe levels (cP450 inhibitors in general).
Term
Cholestyramine, colestipol
Definition
Bile acid sequesterant that aims to decrease the enterohepatic recirculation of bile salts, and induce the synthesis of new bile salts by the liver. This decreases liver cholesterol, increases LDL receptor expression, and decreases blood LDL. Can increase VLDL and triglycerides, so it is contraindicated in pts with hypertriglycemia.
Term
Nicotonic acid
Definition
Superdose of this vitamin causes decreased plasma VLDL, decreased LDL, and increased HDL by inhibiting VLDL synthesis. Can cause flushing.
Term
Gemfibrozil, fenofibrate
Definition
Fibrate drugs which bind PPARa and increase lipoprotein lipase expression resulting in decreased VLDL, IDL and LDL in the bloodstream. Can result in gallstones and myositis. Contraindicated in patients in patients with hypercholesterolemia; reserved for those with hypertriglycemia.
Term
Ezetimbe
Definition
Prevents intestinal absorption of cholesterol to decrease LDL. Can cause GI distress.
Term
Orlistat
Definition
Pancreatic lipase inhibitor used primarily in weight loss.
Term
Alprazolam
Definition
Benzodiazepine drug used to treat anxiety, panic and phobias.
Term
Diazepam
Definition
Benzodiazepine drug used to treat anxiety, and withdrawal states. Used also as a muscle relaxant and in preop sedation. Halflife is relatively long at 8 hours for the drug, but 60 hours as its active metabolite nordiazepam. IV dosage availible.
Term
Lorazepam
Definition
Benzodiazepine drug used to treat anxiety and status epilepticus (IV dosage for this). Can also be used for preop sedation. Doesn't need liver activation.
Term
Midazolam
Definition
Benzodiazepine drug used as an anesthetic (IV) and in preop sedation. Has an extremely short halflife.
Term
Temazepam
Definition
Benzodiazepine drug used to treat sleep disorders only. Short half life and lacks metabolites.
Term
Oxazepam
Definition
Benzodiazepine drug used to treat anxiety and sleep disorders. Extremely short half life and lacks metabolites.
Term
Phenobarbital
Definition
barbituate drug used for seizures. Useful IM for febrile seizures. Can induce the P450 system and cause accelerated clearance of other drugs. Contraindicated in porphyrias.
Term
Thiopental
Definition
barbituate drug used for the induction of anesthesia. Can induce the P450 system and cause accelerated clearance of other drugs. Contraindicated in porphyrias. IV anesthetic.
Term
Zolpidem, zaleplon
Definition
Non-benzodiazepine BZ1 receptor agonists. Used in sleep disorders and have less tolerance and abuse liability when compared to benzos.
Term
Buspirone
Definition
5-HT1A receptor partial agonist; no effect on GABA receptors. Used in general anxiety disorders. Nonsedative. Takes a couple of weeks to take effect.
Term
Ethanol
Definition
Converted to glycoaldehyde, then converted to glycolic acid. Finally becomes oxalic acid and can cause metabolic acidosis.
Term
Methanol
Definition
Converted to formaldehyde and then to formic acid. Can cause ocular damage once converted to this form.
Term
Phenytoin
Definition
Anticonvulsant drug that blocks axonal sodium channels in their inactive state, preventing seizure propagation. Indicated in partial seizures (simple or complex), tonic clonic seizures, and in status epilepticus. Follows zero-order kinetics of elimination. Contraindicated in prophyrias. Can cause gingival hyperplasia and hirsutism. Also can cause osteomalacia (decreased vitamin D), megaloblastic anemia (decreased folate), and aplastic anemia. Teratogenic; causing cleft lip and palate. Induces cP450s
Term
Carbamazepine
Definition
Anticonvulsant drug that blocks axonal sodium channels in their inactive state, preventing seizure propagation. Drug of choice for trigeminal neuralgia, and can als be used in partial (simple and complex) seizures, and general tonic clonic seizures. Can be helpful to control the manic phase of bipolar disorder. Can cause an increase in ADH secretion and induce CNS edema; with the risk of causing herniation (only with high doses). Can cause gingival hyperplasia and hirsutism. Also can cause osteomalacia (decreased vitamin D), megaloblastic anemia (decreased folate), and aplastic anemia. Teratogenic; causing cleft lip, cleft palate AND spina bifida (due to folate effects). Induces cP450s.
Term
Valporic acid
Definition
Anticonvulsant drug that blocks axonal sodium channels in their inactive state, preventing seizure propagation as well as inhibiting GABA transaminase. Also blocks T-type Ca channels in the thalamus. Can be used in all seizure states (including absence seizures), bipolar disorder, and as mmigrane prophylaxis. Inhibits cytochrome P450s. Can be hepatotoxic, cause thyombocytopenia, pancreatitis, and alopecia. Can cause spina bifida.
Term
Ethosuximide
Definition
Anticonvulsant that blocks T-type Ca channels in thalamic neurons and is the DOC in absence seizures.
Term
Felbamate
Definition
Anticonvulsant which blocks Na channels and glutamate receptors. Used as an adjunct in seizure states. Can cause hepatotoxicity and aplastic anemia.
Term
Lamotrigine
Definition
Anticonvulsant which blocks Na channels and glutamate receptors. Used as an adjunct in seizure states. Can cause Stevens-Johnson syndrome.
Term
Gabapentin
Definition
Anticonvulsant drug that is often used off label for neuralgias. Increases the effects of GABA and can be used in patients with long QT syndrome. Can rarely cause aplastic anemia, but sedation is a common side effect.
Term
Nitrous oxide
Definition
Weakest of all inhaled anesthetics. Has minimal CV effects and has rapid onset and recovery. No metabolism. Can cause diffusional hypoxia and spontaneous abortions.
Term
Halothane
Definition
Strong inhaled anesthetic which can sensitize the heart to catecholamines. Has a risk of malignant hyperthermia, hepatitis, and cardiac arrhythmias.
Term
Propofol
Definition
IV anesthetic used for the induction and maintenance of anesthesia. Antiemetic (can avoid aspiration pneumonia). CNS and cardiac depressant. Milk-like appearance. No analgesic effects.
Term
fentanyl
Definition
IV opioid anesthetic and analgesic. Used to induce and maintain anesthesia. Risk of depressed respiratory function.
Term
Ketamine
Definition
Dissociative IV anesthetic useful in children. NMDA receptor antagonist. Used to induce anesthesia. Can cause emergent delirium and vivid hallucinations. Cardiovascular stimulation makes it a good choice in the elderly undergoing surgery. Can increase intracranial pressure.
Term
Procaine, benzocaine (esters)
Lidocaine, bupivacaine, mepivacaine (Amides)
Definition
Local anesthetic which blocks inactivated Na channels in peripheral nerves. Affects smaller nerve fibers sooner and lasts longer.
Term
Atracurium
Definition
nondepolarizing (competitive) D-tubocurarine like muscle relaxant drug that is safe to use in hepatic or renal impairment due to spontaneous inactivation. However, its inactivated product laudanosine can cause seizures.
Term
Mivacurium
Definition
nondepolarizing (competitive) D-tubocurarine like muscle relaxant that allows for rapid patient recovery. Metabolized by plasma cholinesterases.
Term
Succinylcholine
Definition
depolarizing (noncompetitive) muscle relaxant that first causes depolariziation, fasciculation, prolonged depolarization and paralysis followed by phase II which casues desensitization. ACHE inhibitors increase the first phase. Can cause malignant hyperthermia.
Term
Meperidine, heroin, morphine
Definition
Full opioid agonist analgesic with antimuscarinic properties (no miosis unlike others in its class). Tachycardia risk, but doesn't have the risk of GI/GU/ or gallbladder spasms. Metabolized to normeperidine by P450, an SSRI. Can cause serotonin syndrome and seizures in this way.
Term
Methadone
Definition
Full opioid agonist analgesic used in the maintenance of opioid addicts.
Term
Codeine
Definition
Full opioid partial agonist used as a cough suppressant and as a weak analgesic. Used in combination with NSAIDS typically.
Term
Buprenorphine
Definition
Partial opioid agonist that can precipitate withdrawal in an opioid addict.
Term
Nalbuphine, pentazocine
Definition
Mixed agonist-antagonist of opioid kappa receptors (agonist) and mu receptors (antagonist). Can cause analgesia but often results in dysphoria and can precipitate withdrawal.
Term
Naloxone
Definition
Opioid receptor antagonist used in the reversal of respiratory depression in an opioid OD (IV).
Term
Naltrexone
Definition
Opioid receptor antagonist given orally to decrease the craving for alcohol and used in opiate addiction.
Term
Methylnaltrexone
Definition
Opioid receptor antagonistused to treat opioid induced constipation. Won't precipitate withdrawal because it doesn't cross the BBB.
Term
Levodopa
Definition
Prodrug used in Parkinson's disease that is converted to dopamine by aromatic amino acid decarboxylase (AAAD) centrally. Always given with carbidopa (peripheral AAAD inhibitor).
Term
Tolcapone, entacapone
Definition
COMT inhibitors centrally that enhance levodopa treatment in Parkinson's disease. can be hepatotoxic.
Term
Selegiline
Definition
MAOb selective inhibitor centrally (no tyramine interactions). Initial treatment and adjunct to levodopa in Parkinson's disease.
Term
Bromocriptine, perogolide, pramipexole, ropinirole
Definition
Dopamine receptor agonist used in the treatment of Parkinson's disease. Can also be used in hyperprolactinemia and acromegaly.
Term
Benztropine, trihexyphenidyl, diphenhydramine
Definition
Decrease Ach function in the treatment of Parkinson's disease. Contraindicated in patients with BPH.
Term
Amantadine
Definition
Anti-viral drug that blocks muscarinic receptors and increases dopamine release; useful in Parkinson's disease. Can cause livedo reticularis. Can also cause atropine-like side effects (The three C's; Cardiotoxicity, convulsions, and coma). Blocks the attachment, penetration, and uncoating of the influenza virus. Used prophylactically, but may decrease the duration of flu symptoms by 1-2 days. Can cause CNS effects (nervousness, insomnia and seizures in OD) and can cause the three C's of atropine like effects and livedo reticularis.
Term
Pimozide
Definition
antipsychotic drug useful for the treatment of Tourette syndrome.
Term
Chlorpromazine
Definition
Typical antipsychotic with moderate EPS, Muscarinic block, sever sedation and severe alpha block properties.
Term
Thioridazine
Definition
Typical antipsychotic with low EPS (autotreats itself), Severe muscarinic block, severe sedation, and severe alpha block properties. can cause torsades (quinidine-like) and retinal deposits.
Term
Fluphenzaine
Definition
typical antipsychotic with severe EPS, low muscarinic block, low sedation, and low alpha block properties.
Term
Halperidol
Definition
Typical antipsychotic with severe EPS, low M block, low sedation, and low alpha block properties. Can cause neuroleptic malignant syndrome and TD more commonly than other typicals.
Term
Clozapine
Definition
Atypical antipsychotic with negligible EPS, moderate M block, low sedation, and Severe alpha blocking properties. Blocks D2c and 5HT2 receptors. Can cause agranulocytosis.
Term
Olanzapine
Definition
atypical antipsychotic with negligible EPS, low M block, low sedation and moderate alpha block. Blocks 5HT2 receptors and improves negative psychotic symptoms (Amotivation, social withdrawal, flat affect, poverty of speech).
Term
Risperidone
Definition
atypical antipsychotic with low EPS, negligible M block, moderate sedation and moderate alpha block. Blocks 5HT2 receptors and improves negative psychotic symptoms (Amotivation, social withdrawal, flat affect, poverty of speech).
Term
Aripiprazole
Definition
atypical antipsychotic with low EPS, negligible M block, negligible sedation and negligible alpha block. Partial agonist of D2 receptors and blocks 5HT2 receptors.
Term
Phenelzine, tranylcypromine
Definition
MAOa and MAOb non-selective inhibitor used to treat depression. Contraindicated in patients who are on TCAs, alpha1 agonists, and levodopa. Avoid tyramine (cheeses, etc.). Can cause serotonin syndrome especially with co-administration of amphetamines and/or ephedrine.
Term
amitriptyline, imipramine, clomipramine
Definition
Tricyclic antidepressant: nonspecific blockade of 5HT and NE reuptake. Used in major depression, phobic/panic anxiety states, OCD, neurpathic pain, and enuresis. Can cause muscarinic and alpha blockade side effects. Antagonistic of alpha 2 agonists and guanethidine.
Term
Fluoxetine, paroxetine, sertaline, citalopram, fluvoxamine
Definition
SSRI drug; blocks 5HT reuptake. Used in Major depression, ODC,bulimia, anxiety disorders and premenstrual dysphoric disorder (PMDD). Can cause anxiety, agitation, bruxism, sexual dysfunction, and weight loss. Can inhibit P450 enzymes.
Term
Trazodone
Definition
Antidepressant associated with cardiac arrhythmias and priapism due to its alpha 1 blockade effects.
Term
Venlafaxine
Definition
Non-selective reuptake blocker antidepressant devoid of ANS side effects.
Term
Bupropion
Definition
Dopamine reuptake blocker antidepressant. Useful in smoking cessation programs.
Term
Murtazapine
Definition
Alpha 2 antagonist used as an antidepressant. Associated with weight gain.
Term
Lithium
Definition
DOC for bipolar disordes, bu usually requires antidepressant/antipsychotic co-administration in a full regimen. Prevents recycling of inositol (decreased PIP2) and decreases cAMP. Very narrow therapeutic index. Can cause hypothyroidism by decreasing TSH effects and can cause nephrogenic diabetes insipidus. Teratogenic (Ebstein's anomaly-malformed tricuspid valve).
Term
Methylphenidate
Definition
Amphetamine-like drug used in ADHD. Can cause agitation, restlessness, insomina, and cardiovascular toxicity.
Term
Atomoxetine
Definition
Selective NE reuptake inhibitor used in ADHD. Side effects similar to TCAs (muscarinic and alpha blockade).
Term
cocaine
Definition
Local anesthetic which blocks inactivated Na channels in peripheral nerves. Affects smaller nerve fibers sooner and lasts longer. Drug of abuse due to its effects of blocking DA, NE and 5HT reuptake centrally.
Term
Amphetamine
Definition
Blockade of reuptake of NE and Da. Release amines from mobile pool, weak MAO inhibitor. Drug of abuse.
Term
Isonazid
Definition
Antibiotic which inhibits mycolic acid synthesis. Requires conversion to its active form via catalase, therefore resistance develops due to deletions of the katG gene. Can cause hepatitis, peripheral neuritis (B6 deficiency, sideroblastic anemia (B6 deficiency), and SLE in slow acetylators
Term
Rifampin
Definition
Inhibits DNA dependent RNA polymerase as its mechanism of action. Can cause hepatitis, P450 induction, and can cause tears and other body secretions to become red-orange due to metabolite formation.
Term
Ethambutol
Definition
Inhibits the synthesis of arabingalactan (cell wall component) by blocking arabingalactan synthase. Can cause dose dependent retrobulbar neuritis leading to decreased visual accuity and decreased red-greed discrimination.
Term
Pyrazinamide
Definition
Largely unknown mechanism but seems to work by blocking an enzyme that causes the interior of the bacteria to become frankly acidic (due to product buildup), leading to cell death. Can cause hepatitis and hyperuricemia. Antituberculosis drug.
Term
Streptomycin
Definition
Protein synthesis inhibitor (aminoglycoside) used IV for TB while in the hospital. Can cause deafness, vestibular dysfunction, and nephrotoxicity.
Term
penicillin G, V, benzathine penicillin
Definition
narrow spectrum beta lactamase sensitive inhibitor of cell wall synthesis useful for treponema pallidum.
Term
nafcillin, oxacillin
Definition
beta lactamase resistant cell wall synthesis inhibitor. Narrow spectrum; useful only really for non-resistant staphylococci. Don't require renal dosing correction with renal disease.
Term
ampicillin, amoxicillin
Definition
aminopenicillin; beta-lactam sensitive and broad spectrum. Useful for gram positive cocci besides staphylococci, and a number of gram negative organisms (E. coli, B. burgdorferi, H. pylori, etc.)
Term
ticarcillin, piperacillin, azlocillin, carbenicillin
Definition
extended spectrum, antipseudomonal, beta-lactamase sensitive inhibitors of cell wall synthesis. Great for pseudomonas aeruginosa and a number of other gram negative rods. Can be combined with clavulanic acid to avoid beta lactamase.
Term
methicillin
Definition
beta lactamase resistant cell wall synthesis inhibitor. Narrow spectrum; useful only really for non-resistant staphylococci.
Term
cefazolin, cephalexin
Definition
first generation cephalosporin. Large spectrum of activity and commonly used in surgical prophylaxis.
Term
cefotetan, cefaclor
Definition
second generation cephalosporin. Wide range spectrum with increased gram negative coverage over first generation. Like first generations, doesn't enter the CNS.
Term
cefuroxime
Definition
second generation cephalosporin. Wide range spectrum with increased gram negative coverage over first generation. Enters the CNS unlike others in its generation.
Term
cefotaxime, cefdinir, cefixime
Definition
Third generation cephalosporin. Enters the CNS and is important in empiric management of meningitis and sepsis.
Term
Ceftriaxone, cefoperazone
Definition
Third generation cephalosporin. Doesn't enter CNS (TOO lipid soluble and heavily protein bound!) eliminated in bile and don't require dose adjustment in renal failure.
Term
Cefepime
Definition
Fourth generation cephalosporin. Wide spectrum and resistant to beta lactamases.
Term
Imipenem
Definition
Cell wall synthesis inhibitor, resistant to betalactamases. Can treat everything but MRSA. Useful empiric agent in hospitals for life threatening infections. Must be administered with cilastatin to prevent renal damage via toxic metabolites. Can cause CNS effects and seizures with overdose (such as in renal dysfunction).
Term
Meropenem
Definition
Cell wall synthesis inhibitor, resistant to betalactamases. Can treat everything but MRSA. Useful empiric agent in hospitals for life threatening infections. Doesn't require any co-administrations for toxicity. Must be renally dosed.
Term
Aztreonam
Definition
Useful cell wall synthesis inhibitor (beta lactamase resistant) in that patients allergic to penicillin with a pseudomonas infection can be treated with this drug without worry of allergy.
Term
Vancomycin
Definition
Binds at the D-ala-D-ala muramyl pentapeptide to inhibit peptidoglycan chain elongation. DOC for MRSA and can be use'j[d for enteroocci and C. difficile as a backup drug. Can cause "red man syndrome" and can cause ototoxicity and neprotoxicity.
Term
gentamicin, tobramycin, amikacin
Definition
Aminoglycoside (bactericidal) uptaken via O2 dependent mechanisms (anaerobes intrinsically resistant). Not the drug of choice for yersinia pestis and tularemia. Can cause neprotoxicity and ototoxicity. May have an additive effect on muscle relaxants due to its blockade of ACh release.
Term
Streptomycin
Definition
Aminoglycoside (bactericidal) uptaken via O2 dependent mechanisms (anaerobes intrinsically resistant). Drug of choice for yersinia pestis and tularemia. an cause neprotoxicity and ototoxicity. Can have an additive effect on muscle relaxants due to its blockade of ACh release.
Term
Doxycycline
Definition
tetracycline antibiotic: blocks the attachment of aminoacyl tRNA to the acceptor site (static). Useful in prosatitis because it reaches high levels in prostatic fluid. DOC in lyme's disease (B. burgdorferi). Eliminated via the liver.
Term
Minocycline
Definition
tetracycline antibiotic: blocks the attachment of aminoacyl tRNA to the acceptor site (static). In saliva and tears in high concentrations. Used in the meningococcal carrier state and in dentistry.
Term
Demeclocycline
Definition
tetracycline antibiotic: blocks the attachment of aminoacyl tRNA to the acceptor site (static). Used in SIADH by blocking ADH receptor function in collecting ducts. Distractor on exams; not used as an antibiotic!!!
Term
tigecycline
Definition
tetracycline antibiotic: blocks the attachment of aminoacyl tRNA to the acceptor site (static). Used in complicated skin, soft tissue, and intestinal infections due to resistant gram +, gram - and anaerobic infections.
Term
Chloramphenicol
Definition
Inhibitor of the activity of peptidyl transferase in the 50S bacterial subunit. (static antibiotic). Metabolized by the liver and inhibits the P450 system. Can cause dose-dependent bone marrow suppression commonly, aplastic anemia is rare. Can cause "gray baby" syndrome in neonates.
Term
erythormycn, azithromycin, clarithromycin
Definition
Macrolide antibiotic; DOC for L. pneumophila. INhibit cP450s. Can cause reversible deafness at high doses.
Term
Telithromycin
Definition
A ketolide antibiotic active against macrolide resistant S. pneumonia (an important cause of meningitis and otitis media in young children)
Term
Clindamycin
Definition
Macrolide-like antibiotic in that it inhibits translocation of peptidyl tRNA from acceptor to donor site (static). Effective against gram positive cocci including community acquired MRSA and anaerobes such as B. fragilis as a backup drug. Gets high conc. in bone which is of value in osteomylitis. Most likely cause of pseudomembranous colitis due to C. difficile.
Term
Linezolid
Definition
Inhibits the formation of the initiation complex in bacterial translation systems by preventing the formation of the N-formylmethionyl-tRNA-ribosome-mRNA ternary complex. Treats VRSA, VRE and drug resistant pneumococci. Can cause bone marrow suppression and tends to specifically cause thrombocytopenia.
Term
Quinopristin-dalfopristin
Definition
Streptogamin hat acts by binding to sites on the 50S ribosomal subunit and prevent interaction of amino-acyl-tRNA with the acceptor site and stimulate its dissociation. Used parenterally in severe infections caused by VRSA and VRE as well as other drug resistant gram positive cocci.
Term
sulfasalazine
Definition
prodrug folic acid synthesis inhibitor used prophylactically in burns, in ulcerative colitis and rheumatoid arthritis. Inhibits dihydropteroate synthetase in the first step of folate synthesis. Can lead to Stevens-Johnson syndrome, hemolysis (with G6PD deficiency), and phototoxicity.
Term
trimethoprim-sulfamethoxazole
Definition
Folic acid synthesis inhibitor and the DOC of Nocardia infections. Can also be used to treat the fungus pneumocystis hiroveci as a backup. Alco can treat the protozoa toxoplasma gondii. Can cause kernicterus in neonates and should be avoided in pregnancy, especially in the 3rd trimester. Can lead to Stevens-Johnson syndrome, hemolysis (with G6PD deficiency), phototoxicity and leukopenia via bone marrow suppression.
Term
ciprofloxacin, levofloxacin
Definition
fluroquinolone antibiotic that inhibits topoisomerase II; bacteriocidal. Useful in UTIs, STDs, PIDs, and in bone infections due to gram negative organisms. Can cause tendonitis (achilles tendon rupture), phototoxicity, rashes, CNS effects (insomnia, dizziness, headaches, etc). Contraindicated in pregnancy and children due to the inhibition of chondrogenesis.
Term
Metronidazole
Definition
Bactericidal antibiotic that creates free radicals which destroy organisms. Also antiprotozoal (giardia, trichomonas, entamoeba). Strong against anaerobic gram negative bacteroides, clostridium, gardnerella and H. pylori. DOC in pseudomembranous colitis. Can cause a metalic like taste in the mouth and have a disulfram like effect.
Term
Amphotericin B
Definition
Polyene fungicidal drug that is the DOC for serious infections caused by aspergillus, candidia, cryptococcus, histoplasma, mucor, and sporothrix. Synergystic with flucytosine in candidiasis and cryptococcoses. Requires inpatient tx. due to the need to be slowly IV infused. Poor CNS transfusion without intrathecal administration.
Term
Nystatin
Definition
Polyene fungicidal drug that is too toxic for systemic use. Used topically for localized infections (e.g. candidiasis).
Term
Ketoconazole
Definition
Azole antifungal. Oral use in mucocutaneous candidiasis or dermatophytosis. Co-DOC for paracoccidioides and backup for blastomyces and histoplasma. Excreted via liver.
Term
Fluconazole
Definition
Azole antifungal. DOC for esophageal and invasive candidiasis and coccidioidomycoses (gargle method, unlike Amphotericin B). Can be used in prophylaxis of C meningitis. Penetrates to the CNS and can thus be used to treat meningeal infections, unlike others in its class.
Term
Clotrimazole, miconazole
Definition
Azole antifungal used topically for candidal and dermatophytic infections.
Term
Itraconazole
Definition
Azole antifungal. DOC in blastomycoses, sporotrichoses, and aspergillosis. Back up for several others. Excreted via liver.
Term
Voriconazole
Definition
Azole antifungal. DOC in blastomycoses, sporotrichoses, and aspergillosis. Back up for several others. Excreted via the kidney and needs to be renally dosed.
Term
Flucytosine
Definition
Activated via fungal cytosine deaminase to 5-FU and incorporates itself into fungal RNA, halting protein synthesis. Also forms 5-Fd-UMP which inhibits thymidylate synthase. Resistance emerges rapidly if used alone. Toxic to bone marrow. Used with amphotericin B in severe candidal and cryptococcal infections. Can enter CSF.
Term
Griseofulvin
Definition
Active only against dermatophytes (orally, not topically) by disrupting microtubule structure in fungi. Has a disulfram like effect.
Term
Terbinafine
Definition
Active against dermatophytes by inhibiting sqaline epoxidase (step before azole MOA). Can cause possible hepatotoxicity.
Term
Acyclovir
Definition
Antiviral bioactivated by thymidine kinase (TK) and host cell kinases to the triphsophate form. Acts as a chain terminator when incorporated into the viral DNA. Active againt HSV and VZV. Can cause cystalluria and nerotoxicity. NOT hematotoxic. Inactive against TK negative strains.
Term
Ganciclovir
Definition
antiviral drug that requires thymidine kinase for activity. Active against HSV, VZV, and CMV. Mostly used as CMV prophylaxis in AIDS patients. Dose limiting hematotoxicity and can cause seizures in OD.
Term
Foscarnet
Definition
antiviral that is not an antimetabolite. Useful against HSV, VZV and CMV and in CMV prophylaxis in AIDS patients. Dose limiting nephrotoxicity with tubular necrosis. Avoid coadministration of pentamidine IV as this can increase the nephrotoxicity.
Term
Zidovudine
Definition
Nucleoside reverse transcriptase inhibitor that comptes with natural nucleotides and can be incorporated into viral DNA to cause chain termination. Can cause severe bone marrow suppression.
Term
Didanosine
Definition
Nucleoside reverse transcriptase inhibitor that comptes with natural nucleotides and can be incorporated into viral DNA to cause chain termination. Can cause pncreatitis (major and dose limiting), peripheral neuropathy, hyperuricemia and liver dysfunction.
Term
Zalcitabine
Definition
Nucleoside reverse transcriptase inhibitor that comptes with natural nucleotides and can be incorporated into viral DNA to cause chain termination. Can cause peripheral neuropathy (major and dose limiting), GI distress, pancreatitis, neutropenia and rash.
Term
Stavudine
Definition
Nucleoside reverse transcriptase inhibitor that comptes with natural nucleotides and can be incorporated into viral DNA to cause chain termination. Would compete with AZT if given together. Can cause peripheral neuropathy (major and dose limiting) and myelosuppression (less than zidovudine).
Term
Lamivudine
Definition
Nucleoside reverse transcriptase inhibitor that comptes with natural nucleotides and can be incorporated into viral DNA to cause chain termination. Least toxic of the NRTIs, but some GI effects and neutropenia. Active in hepatitis B.
Term
Indinavir
Definition
Protease inhibitor that requires the action of aspartate protease (on the pol gene) for its action. Can cause crystalluria and needs adequate hydration.
Term
Ritonavir
Definition
Protease inhibitor that requires the action of aspartate protease (on the pol gene) for its action. Major drug interactions due to inhibition of P450s. Can cause a syndrome of disordered lipid an CHO metabolism with central adipositiy and insulin resistance.
Term
Saquinavir
Definition
Protease inhibitor that requires the action of aspartate protease (on the pol gene) for its action. One of the least toxic PIs, and has low oral bioavailibility which can predispose to resistance.
Term
Raltegravir
Definition
Integrase inhibitor used in HIV patients preventing integration of viral genome in host cell DNA.
Term
Enfuvirtide
Definition
Fusion inhibitor that binds gp41 and inhibits fusion if HIV-1 to CD4+ cells.
Term
Maraviroc
Definition
Blocks CCR5 protein on T-cell surface and prevents viral entry.
Term
Zanamivir, oseltamivir
Definition
Inhibit neuraminidases of influenza A and B and decreases the likelihood that the virus will penetrate uninfected cells.
Term
Ribavirin
Definition
Monophosphorylated form inhibits IMP dehydrogenase, while the triphosphate form inhibits viral RNA polymerase and end-capping of viral RNA. Used as a adjunct to alpha-interferons in hepatitis C and in the management of RSV in HIV pts. Used also in Lassa fever and in Hantavirus infections. Hematotoxic and teratogenic.
Term
Human interferons
Definition
used as the primary treatment of hepatitis B, C and D and can be used as an anti-tumor agent for Kaposi's sarcoma, CML, multiple myeloma, and renal carcinoma. Can also be immunoregulatory and treat MS and possibly CGD.
Term
Chloroquine
Definition
Drug of choice for P. falciparum and P. malariae and is part of a regimen with primaquine for P. vivax and P. ovale.
Term
primaquine
Definition
part of co-treatment for P. vivax and P. ovale.
Term
Mebendazole
Definition
DOC for pinworm infections. Can decrease glucose uptake in these organisms and diminish their microtubular structure.
Term
Praziquantel
Definition
Increases the calcium influx and vacuolization of cestodes (tapeworms) and trematodes (flukes). Broad spectrum.
Term
Diphenhydramine
Definition
Antihistamine with severe M block, Severe sedation, and high anti-motion sickness properties. Widely used OTC.
Term
Promethazine
Definition
Antihistamine with severe M block, Severe sedation, and moderate anti-motion sickness properties. Also has some alpha blocking properties and local anesthetic action.
Term
Chlorpheniramine
Definition
Antihistamine with moderate M block, moderate sedation, and moderate anti-motion sickness properties. Can cause CNS stimulation.
Term
Meclizine
Definition
Antihistamine with moderate M block, moderate sedation, and extremely effective anti-motion sickness properties.
Term
Cetirizine
Definition
Non-sedating antihistamine with minor M block properties, minor sedation and no antimotion effects.
Term
Loratadine, Fexofenadine
Definition
Non-sedating antihistamine with minor M block properties, no sedation and no antimotion effects. Cannot enter the CNS.
Term
Cimetidine, Ranitidine
Definition
H2 receptor blocker used to suppress secretory responses to food stimulation and nocturnal secretion of gastric acid. Useful today in GERD, Zollinger-Ellison syndrome and as a backup to PPIs in PUD.
Term
Omeprazole
Definition
Irreversible, direct inhibitor of the proton pump in the gastric parietal cell. Part of the eradication regimen for H. pylori (Clarithromycin, amoxicillin, omeprazole).
Term
Misoprostol
Definition
PGE anaog which is cytoprotective. Increases mucus and bicarbonate secretion and decreases HCl secretion in the stomach. This is the "antidote" to asprin induced ulcers.
Term
Sucralfate
Definition
Polymerizes on GI lumenal surface to protect the walls of the stomach.
Term
Bismuth Subsalicylate
Definition
Coats luminal wall of the stomach to protect ulcers. Can be combined with metronidazole and tetracycline for H. pylori
Term
Aluminum antacid
Definition
Base that neutralizes stomach acid. Can cause constipation.
Term
Magnesium antacid
Definition
Base that neutralizes stomach acid. Can ause diarrhea.
Term
Prochlorperazine, metoclopramide
Definition
DA antagonist used to treat nausea and vomiting, especially in in cancer chemotherapy.
Term
dronabinol
Definition
Cannibinoid receptor 1 (CB1) agonist used primarily to avoid nausea and vomiting.
Term
Sumatriptan
Definition
Agonist at 5HT1d receptors in cerebral vessels. Used to decrease migraine pain. Can cause asthenia, chest or throat pressure, and/or pain.
Term
Cyproheptadine
Definition
5HT2 antagonist used in carcinoid syndrome, GI tumors, and postgastrectomy. Also used for anorexia nervosa.
Term
Odansetron
Definition
Antagonist of 5HT3 receptors and prevents emesis in chemotherapy patients.
Term
Ergotamine
Definition
Partial agonist at alpha and 5HT2 receptors in the periphery and possibly in the CNS. Vasoconstrictive action causes a decrease in pulsation that may break a migrane. Used in acute migrane attacks. May cause GI distress, ischemia, gangrene, and abortion if near term.
Term
glucocorticoid
Definition
decrease phospholipase A2 activity and contributes to both antiinflammatory and immunosuppressive actions.
Term
Zileuton
Definition
inhibits lipoxygenase and decreases LTs. used in asthma treatment.
Term
Zafirlukast
Definition
LT receptor antagonist used in the treatment of asthma.
Term
Alprostadil
Definition
PGE1 agonist used to maintain the patency of the ductus arteriosis and to help with vasodilation in male impotence. Contraindicated in pregnancy unless as an abortifacient.
Term
dinoprostone
Definition
PGE2 agonist used for "cervical ripening" and as an abortifacient.
Term
Carboprost
Definition
PGF2alpha agonist used as an abortifacient.
Term
Latanoprost
Definition
PGF2alpha agonist used for the treatment of glaucoma to decrease intraocular pressure.
Term
Acetylsalicylic acid
Definition
Irreversible inhibitor of COX. Can cause hyperuricemia at low to moderate doses, and uricosuria at high doses. Reye's syndrome due to uncoupling is a risk in children.
Term
Ibuprofen, naproxen, ketorolac
Definition
Reversible inhibitor of COX I and II with analgesic, antipyretic and antiinflammatory actions. Minimal effects on acid base balance and has no effects on uric acid elimination. Doesn't cause thrombocytopenia, agranulocytosis, CNS effects, Stevens-Johnson syndrome, or hematotoxicity.
Term
indomethacin
Definition
Reversible inhibitor of COX I and II with analgesic, antipyretic and antiinflammatory actions. Minimal effects on acid base balance and has no effects on uric acid elimination. Can cause thrombocytopenia, agranulocytosis, and CNS effects.
Term
Sulindac
Definition
Reversible inhibitor of COX I and II with analgesic, antipyretic and antiinflammatory actions. Minimal effects on acid base balance and has no effects on uric acid elimination. Can cause Stevens-Johnson syndrome, or hematotoxicity.
Term
Celecoxib
Definition
Selective COX II inhibitor. Cross sensitivity with sulfonamides.
Term
Acetaminophen
Definition
Does not inhibit COX in peripheral tissues and lax significant anti-inflammatory effects. Equivalent analgesic and antipyretic activity to ASA due to inhibition of cyclooxygenases in the CNS. Not implicated in Reye syndrome and has no effect on uric acid. Not bronchospastic. Can be hepatotoxic and can be managed with N-acetylcysteine.
Term
Hydroxychloroquine
Definition
Stabilizes lysosomes and decreases chemotaxis of WBCs in order to treat rheumatoid arthritis. Can cause GI distress and visual dysfunction (cinchonism) and hemolysis in G6PD.
Term
Methotrexate
Definition
Cytotoxic drug to lymphocytes used to treat rheumatoid arthritis. Can be hematotoxic.
Term
Sulfasalazine
Definition
Decreases B-cell functions and possibly inhibits COX. Used to treat RA. Can cause Hemolysis in G6PD
Term
Penicillamine
Definition
Suppresses T cells and circulating rheumatoid factor to treat RA. Can also chelate copper and treat Wilson's disease. Can cause proteinurea, hematotoxicity and autoimmune disease.
Term
Etanercept
Definition
Binds TNF as a recombinant form of TNF receptor. Predisposes to infection. Used to tx. RA.
Term
Infliximab
Definition
Monoclonal antibody to TNF; used to tx. RA.
Term
Colchicine
Definition
Binds to tubulin to decrease microtubular polymerization and decrease LTB4. This decreases leukocyte and granulocyte migration. Used historically to tx. gout. Can cause diarrhea and GI pain. With chronic use, this can cause hematuria, alopecia, myelosuppression, gastritis and peripheral neuropathy.
Term
Allopurinol
Definition
Prodrug that acts as a suicide substrate for xanthine oxidase (forms alloxanthine). Decreased purine metabolism thus leads to decreased uric acid in gout patients.
Term
Probenecid
Definition
Inhibits proximal tubular reabsorption of urate, but ineffective of GFR less than 50mL/min. Also inhibits secretion of many acidic drugs (cephalasporins, flurorquinolones). ASA may decrease its effects.
Term
Cortisol, Prednisone, Triamcinolone, Betamethasone, Dexamethasone
Definition
Glucocorticoid. Can cause cortical arophy, malaise, myalgia, arthralgia, and fever. May cause shock with abrupt withdrawal. Can also cause iatrogenic cushingoid syndrome with long term use. Other effects include hyperglycemia, osteoporosis, and increased GI acid and pepsin release.
Term
Salmeterol
Definition
Selective B2 agonists useful in the tx. of asthma. Useful in decreasing nighttime attacks (prophylaxis only) due to its long time of action.
Term
Theophylline
Definition
Inhibitor of PDE and antagonises adenosine causing bronchodilation. Used in asthma. Increased toxicity by erythromycin, cimetidine and fluoroquinolones. Can be useful in status asthmaticus especially in pts. with a loss of beta agonist sensitivity.
Term
Cromolyn and nedocromil
Definition
Prevent degranulation of pulmonary mast cells and decrease the release of histamine, PAF, and LTC4 from inflammatory cells.
Term
Zafirlukast, montelukast
Definition
Antagonists at LTD4 receptors with slow onset of activity used prophylactically for many asthma forms.
Term
Zileuton
Definition
Selective inhibitor of lipoxygenases. Decreases the formation of all leukotrinenes. Rapid onset and is adjunctive to steroids.
Term
Heparin
Definition
Large polysaccharide given parenterally and elimiated hepatically and via the reticuloendothelial route. Half life of about 2 hours. Catalyzes the binding of antithrombin III to factors IIa, IXa, Xa XIa, and XIIa, resulting in their rapid inactivation. Monitored via PTT. Antagonized by protamine sulfate. Used in rapid anticoagulation.
Term
Warfarin
Definition
Small molecule that is lipid soluble. 98% lipid bound once absorbed. Halflife reflects this; 30+ hours. Decreased synthesis of K-Dependent factors II, VII, IX, X, protein C and protein S. No effect on factors already present (works in vivo only because of this!). Measured via PT/INR. Antagonized by K megadose. Used for longer term anticoagulation. Can cause skin necrosis with low protein C. Teratogenic (bone dysmorphogenesis).
Term
argatroban
Definition
substitute for a patient suffering from HIT. Direct thrombin inhibitor.
Term
Dabigatran
Definition
Oral anticoagulant that does not require monitoring of PT or INR. Used in A. fib as an alternative to warfarin.
Term
Bivalirudin
Definition
Used with asprin in unstable angina when undergoing PTCA.
Term
Streptokinase
Definition
Acts on both bound and free plasminogen depleting circulating plasminogen and factors V and VIII. Antigenic and may cause a problem.
Term
Alteplase (tPa)
Definition
CLot specific, acting mainly on fibrin-bound plasminogen, the natural activator, so no allergy problems.
Term
Ticlopidine, clopidogrel
Definition
Block ADP receptors on platelets decreasing their activation.
Term
Abciximab, eptifibatide, tirofiban
Definition
Antagonists tat bind to glycoprotein IIb/IIIa receptors to decrease platelet aggregation by preventing the cross-linking reaction. Used mainly in acute coronary syndromes and postangioplasty.
Term
Lispro insulin
Definition
Fast onset and short duration insulin used in diabetics.
Term
Regular insulin
Definition
Intermediate onset insulin with moderate duration used in diabetics.
Term
Glargine
Definition
Regular onset peakless LONG acting insulin used in diabetics. Used as background insulin.
Term
Acetohexamide
Definition
Active metabolite first generation sulfonylurea; decrease the dose in renal dysfunction.
Term
Tolbutamide
Definition
first generation sulfonylurea appropriate in renal dysfunction. Side effects include hypoglycemia, weight gain, and drug interactions (more so with first generation) with cimetidine, insulin, salicylates and sulfonamides.
Term
Chlorpropamide
Definition
first generation sulfonylurea that is long acting. Can caue SIADH and has disulfiram like effects. Side effects include hypoglycemia, weight gain, and drug interactions (more so with first generation) with cimetidine, insulin, salicylates and sulfonamides.
Term
Glipizide
Definition
Second generation sulfonylurea. decrease dosage in hepatic dysfunction. Side effects include hypoglycemia, weight gain, and drug interactions (more so with first generation) with cimetidine, insulin, salicylates and sulfonamides.
Term
Glyburide
Definition
Second generation sulfonylurea. Decrease dose in renal dysfunction. Side effects include hypoglycemia, weight gain, and drug interactions (more so with first generation) with cimetidine, insulin, salicylates and sulfonamides.
Term
Metformin
Definition
Euglycemic; doesn't cause hypoglycemia! Increased tissue sensitivity to insulin and decreased liver gluconeogenesis. Can cause lactic acidosis and GI distress (Commonly a culprit in a patient who has metabolic acidosis, diabetes and a large anion gap).
Term
Acarbose, miglitol
Definition
No hypoglycemia; inhibits alpha glucosidase in brush boarders and inhibit carb absorption. This can cause GI discomfort and flatulence; not to mention diarrhea.
Term
Pioglitazone, rosiglitazone
Definition
Thiazolidinediones; bind to PPAR gamma effectively "skippin" insulin receptors. Decrease hepatic gluconeogenesis and triglyceride synthesis. Also increases insulin receptor numbers. Less hypoglycemia than sulfonylureas, but weight gain and edema seen.
Term
Exenatide
Definition
Long acting GLP-1 receptor full agonist; used in combo with other drugs. Augments glucose dependent insulin secretion. Can cause hypoglycemia and nausea when combined with oral sulfonylureas.
Term
Sitagliptin
Definition
Inhibits dipeptidyl peptidase (DPP-4) thereby inhibiting the inactivation of GLP-1. Causes augmentation of glucose dependent insulin secretion.
Term
dexamethasone
Definition
extremely potent cortisol analog used to diagnose Cushing's syndrome or disease.
Term
Anastrozole
Definition
Aromatase inhibitor used to decrease estrogen snthesis. Used in the tx. of estrogen dependent, post-menopausal breast cancer.
Term
Clomiphene
Definition
Fertility pill. Decreases feedback inhibition of FSH and LH to increase ovulation and encourage pregnancy. Multiparity is common.
Term
Tamoxifen
Definition
Estrogen receptor agonist at bone, partial agonist at endometrium, and antagonist at the breast. Used to treat estrogen dependent breast cancer.
Term
Raloxifene
Definition
Estrogen receptor agonist in the bone, antagionis in the breast and uterus. No increased cancer risk in menopause. Prophlylaxis for postmenopausal osteoporosis.
Term
Medorxyprogesterone, norethindrone
Definition
Increases the feedback inhibiton of gonadotropins by acting as progesterone. Used in contraception and in HRT.
Term
Desogestrel
Definition
Increases the feedback inhibiton of gonadotropins by acting as progesterone. Used in contraception and in HRT. Devoid of androgenic and antiestrogenic activities common to other derivative.
Term
Flutamide
Definition
androgen receptor blocker, used for androgen receptor positive prostate cancer.
Term
Leuprolide
Definition
GnRH analog, repository form used for androgen receptive prostate cancer.
Term
Finasteride
Definition
5-alpha reductase inhibitor preventing DHT production. Used to prevent hair loss and prostate enlargement. Teratogenic (sleeping next to a man using this product on their head can expose a fetus!)
Term
propylthiouracil
Definition
Blocks the synthesis of hyroxine. Can cross the placental barrier, but safer in pregnancy due to highly protein bound.
Term
methimazole
Definition
Inhibits the iodination of thyroglobulin. Not safe in pregnancy; easily crosses the placental barrier and isn't extensively protein bound.
Term
Lugol's solution
Definition
Potassium iodide plus iodine used in thyrotoxicosis as negative feedback pre-operatively. No long term use due to thyroid escape.
Term
Somatrem, somatropin
Definition
GH analog; used in pituitary dwarfism and osteoporosis.
Term
Octreotide
Definition
Somatostatin analog used in acromegaly, carcinoid, and secretory GI tumors.
Term
Cosyntropin
Definition
ACTH analog used in infantile spasms caused by hypoglycemia. Induces gluconeogenesis.
Term
Leuprolide, nafarelin
Definition
GnRH analog. Used in endometriosis and prostate carcinoma.
Term
Urofollitropin, Placental HCG, menotropins
Definition
FSH and LH analog, used in hypogonadal states.
Term
Bromocriptine, perogolide
Definition
PIH (DA) analog; used in hyperprolactinemia
Term
Oxytocin
Definition
Used in labor induction.
Term
Desmopressin (V2 selective)
Definition
Vasopressin analog with use in pituitary diabetes insipidus, hemophilia A (Increased factor VIII), von WIllebrand's disease (increased VW factor from endothelium weibel palade bodies), and in primary nocturnal enuresis.
Term
Bisphosphonates (-nate)-Etidronate, pamidronate, alendronate
Definition
Stabilizes hydroxyapatite and induces osteoblasts. Established use in Paget disease and in postmenopausal osteoporosis. Can cause bone mineralization defects, GI distress and esophageal ulcers.
Term
Teriparatide
Definition
Recombinant DNA PTH analog used to stimulate osteoblasts and cause new bone formation. May increase the risk of osteosarcoma if used for less than 2 years. Can't use continuously or osteoclasts become stimulated.
Term
Cyclophosphamide
Definition
Alkylating agent, attacks guanine N7 dysfunctional DNA. Used in Non-Hodgekin lymphoma, ovarian cancer, breast cancer, and neuroblastoma. Use mesna to avoid hemorrhagic cystitis.
Term
Cisplatin
Definition
Alkylating agent used in testicular, ovarian, bladder and lung cancer. Use amifostine to avoid neprotoxicity. Can also cause neurotoxicity (irriversible deafness)
Term
Procarbazine
Definition
Alkylating agent used in Hodgekin's disease. Can cause BMS and is leukemogenic.
Term
Doxorubicin
Definition
Intercalator, forms free radicals, and inhibits topoisomerase. Used in Hodgekins, breast cancer, endometrial cancer, lung cancer and ovarian cancers. Use dexrazoxane to avoid BMS (prevents free radical formation; not a free radical trapper).
Term
Methotrexate (CCS)
Definition
Antimetabolite, inhibits DHF reductase (S phase). Used in Leukemias, lymphomas, breast cancer, rheumatoid arthritis and in psoriasis. Use leucovorin as a folinic acid rescue for this drug.
Term
5-Fluorouracil (CCS), Capecitabine
Definition
Pyrimidine antimetabolite (S phase) bioactivated to inhibit thymidylate synthase. Used to treat breast, ovarian, head and neck cancer. Topically used for basal cell cancer and keratoses. Used also for colorectal cancer. Can cause BMS
Term
Bleomycin
Definition
Complexes with Fe and O2 to cause DNA stran scission (G2 phase). Used in Hodgekin's lymphoma, testicular cancer, head and neck cancer, and skin cancer. Can cause pneumonitis and pulmonary fibrosis.
Term
vinblastine, vincristine
Definition
Decrease microtubular polymerization and spindle poisons (M phase). Used for Hodgekins, testicular cancer, Kaposi's sarcoma,, Hodgekin, leukemias, and Wilm's tumors. Can cause BMS and neurotoxicity.
Term
All-trans retinoic acid (ATRA)
Definition
Differentiating agent, promots differentiation of promyelocytes. Used to treat AML and M3 cancers. Can cause "differentiation syndrome" with respiratory distress, pleural and pericardial effusions, and CNS symptoms.
Term
Aldesleukin (IL-2)
Definition
Clinically used cytokine used to incrase lymphcyte differentiation and increase NKs. Used in renal cell cancer and metastatic melanoma.
Term
IL-11
Definition
Increased platelet formation, used in thrombocytopenia.
Term
Filgastim (G-CSF)
Definition
Increased granulocytes, used for marrow recovery.
Term
Sargramostim (GM-CSF)
Definition
Increased granulocytes and macrophages, used for marrow recovery.
Term
Trombopoietin
Definition
Used for thrombocytopenia
Term
Cyclosporine
Definition
binds to cyclophilin and decreases calcineurin to decrease T cell activation of transcription factors for IL-2, 3, and interferon gamma. DOC for organ or tissue transplantation. Risk of neprotoxicity, peripheral neuropathy and gingival oergrowth.
Term
tacrolimus
Definition
binds to FK-binding protein and decreases calcineurine to decrease T cell activation of transcription factors for IL-2, 3, and interferon gamma. Used alternatively to other agents for renal or liver transplants. Risk of neprotoxicity and peripheral neuropathy.
Term
Mcophenolate
Definition
Inhibitor of de novo synthesis of purines used as an adjunctive immunosuppressant, permitting dose reductions of cyclosporine to reduce toxicity.
Term
Azathioprine
Definition
Prodrug converted to 6-mercaptopurine. Can cause bone marrow suppression.
Term
Rhogam
Definition
Anti D immunoglobulin used to prevent hemolytic disease of the newborn in subsequent pregnancies of an Rh negative mother.
Term
Abciximab
Definition
Antiplatelet antibody; antagonist of IIb/IIIa receptors.
Term
Trastuzumab
Definition
Breast cancer antagonist to ERB-B2 antibody (GF receptor)
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