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Pharmacology
Winter Term
192
Medical
Professional
02/09/2009

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Cards

Term
Acetazolamide
Definition
Carbonic Anhydrase Inhibitor
Inhibits CA in the PCT →
↓ Na & HCO3- reabsorption
Secreted into lumen via OA trx
Inhibits 85% of PCT HCO3 reabs
Inhibits 45% of total HCO3 reabs
Metabolic acidosis, renal CaPO4 stones,
hypokalemia, CNS, allergy
Contraind: cirrhosis (encephalopathy)
CHF edema, Glaucoma
Urine alkalinization
Mountain sickness
Term
Furosemide
Definition
Loop Diuretic
Inhibits Na+/K+/2Cl- trx in TAL →
↓Na & K & 2Cl reabsorption
Secreted into lumen via OA trx
Eliminated via kidney




Hyponatremia/dehydration
Hypocalcemia
Hypokalemia
Metabolic alkalosis
Hypomagnesemia
Hyperuricemia
Ototoxicity
Allergy
Decrease luminal (+) potential
(↓ K+ pushed out) → ↓Ca2+ & Mg2+ reabs
Pulmonary edema
Edema (CH, renal, cirrhosis)
Hypercalcemia
Hyperkalemia
Term
Bumetanide
Definition
Loop Diuretic
Inhibits Na+/K+/2Cl- trx in TAL →
↓Na & K & 2Cl reabsorption
Shorter acting
50% liver elimination
(50% kidney elimination)




Hyponatremia/dehydration
Hypocalcemia
Hypokalemia
Metabolic alkalosis
Hypomagnesemia
Hyperuricemia
Ototoxicity
Allergy
40x more potent
Pulmonary edema
Edema (CH, renal, cirrhosis)
Hypercalcemia
Hyperkalemia
Term
Torsemide
Definition
Loop Diuretic
Inhibits Na+/K+/2Cl- trx in TAL →
↓Na & K & 2Cl reabsorption
Longer acting
Faster absorption
80% liver elimination




Hyponatremia/dehydration
Hypocalcemia
Hypokalemia
Metabolic alkalosis
Hypomagnesemia
Hyperuricemia
Ototoxicity
Allergy
Pulmonary edema
Edema (CH, renal, cirrhosis)
Hypercalcemia
Hyperkalemia
Term
Ethacrinic Acid
Definition
Loop Diuretic
Loop - Inhibits Na+/K+/2Cl- trx in TAL → ↓Na & K & 2Cl reabsorption
No sulfur group in its structure
Only if allergic to other loops
Worst ototoxicity
Term
Spironolactone
Definition
K+ Sparing Diuretic
Competitive aldosterone receptor in DCT &
CT → ↓ in Na+ channels & ↓
out K+ channels (Princ.)
↓ Na+ reabsorption & ↓ K+ secretion
in Principal cells
↑ H+ secretion Intercalated cells
Hyperkalemia, metabolic acidosis, gynecomastia,
impotence, ↓ libido, GI, CNS effects
Also inhibits DHT receptor →
↓ testosterone
Only diuretic not acting in lumen
Cirrhosis (ascites)
Hyperaldosteronism
Hypertension
Term
Eplerenone
Definition
K+ Sparing Diuretic
Epoxy-spironolactone derivative
Less anti-androgenic effects (less DHT &
progesterone receptor binding)
Heart failure
Term
Amiloride
Definition
K+ Sparing Diuretic
Blocks Na+ channels in Principal cells in
DT & CT →
↓ Na+ reabs & ↓ K+ secretion
Secreted unchanged into lumen via
organic base transporter
Eliminated unchanged via kidney


Hyperkalemia (NSAIDs ↑ likelihood)
Nausea, vomiting, diarrhea, leg cramps, headache,
dizziness
Edema; Hypertension
Term
Triamterene
Definition
K+ Sparing Diuretic
Blocks Na+ channels in Principal cells in
DT & CT →
↓ Na+ reabs & ↓ K+ secretion
Shorter acting
Metabolized in liver → into kidney lumen
→ INSOLUABLE & PPTS OUT
Photosensitivity 10x less potent than amiloride
Edema
Hypertension
Term
Hydrochlorothiazide
Definition
Thiazide Diuretic
Inhibits NaCl cotrx in DCT →
↓Na & Cl reabsorption
Secreted into lumen via OA trx
Absorbed orally
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
HYPERCALCEMIA
Hyperglycemia
Hyperuricemia
Allergy
Weakness
Low Na in cell sucks Na through basolatera
Na/Ca exchanger → ↑ Ca2+
reabsorption

Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
Term
Metolazone
Definition
Thiazide Diuretic
Inhibits NaCl cotrx in DCT →
↓Na & Cl reabsorption
Longer acting
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
HYPERCALCEMIA
Hyperglycemia
Hyperuricemia
Allergy
Weakness
10x more potent than HCT
Different structure from thiazides

Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
Term
Indapamide
Definition
Thiazide Diuretic
Inhibits NaCl cotrx in DCT →
↓Na & Cl reabsorption
Longer acting
Excellent oral absorption
Eliminated via liver
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
HYPERCALCEMIA
Hyperglycemia
Hyperuricemia
Allergy
Weakness
20x more potent than HCT
Different structure from thiazides

Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
Term
Chlorthalidone
Definition
Thiazide Diuretic
Inhibits NaCl cotrx in DCT →
↓Na & Cl reabsorption
Longer acting
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
HYPERCALCEMIA
Hyperglycemia
Hyperuricemia
Allergy
Weakness
Same potency as HCT
Different structure from thiazides

Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
Term
Mannitol
Definition
Osmotic Diuretic
Filtered & excreted exerting osmotic pull in
PCT & loop of henle
Must be given IV
↑ flow → ↑ urea excretion →
↓ ability to concentrate urine
Headache, nausea, vomiting,
hypernatremia/dehydration, pulmonary edema
Initial rapid expansion of plamsa volume
Intracranial pressure
Renal ADH V2 receptor antagonistexcretion of toxins
Term
Tolvaptan
Definition
ADH V2 Receptor Antagonist
ADH V2 receptor antagonist →
↑ free H2O excretion &
↓ urea & Na+ reabsorption
Heart failure
Term
Conivaptan
Definition
ADH V1a, V2 antagonist
ADH V1a antagonist →
↓ vasocx & ↓ smooth muscle growth
ADH V2 receptor antagonist →
↑ free H2O excretion &
↓ urea & Na+ reabsorption
Term
Aliskiren
Definition
Renin Inhibitor
Binds to Renin preventing the conversion of Angiotensinogen to Angiotensin I
Term
Propranolol
Definition
Class II Anti-arrhythmic
Non-selective β blocker
Na+ blocker at ↑ dose
(membrane stabilization)
↓ AV conduction velocity, prolonged PR, ↓
automaticity in ectopic foci
Myocardial depression, heart block,
bronchospasm, ↑ insulin hypoglycemia,
depression, rebound SNS if w/d
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina "golden child"
Term
Carvedilol
Definition
Class II Anti-arrhythmic
Non-selective β blocker α blocker
Antioxidant properties
Atrial Flutter; Atrial fibrillation; Ventricular arrhythmia (post-MI); Angina
Term
Nadolol
Definition
B1 B2 Blocker
Treats Hypertension/Migraine/Chest Pain
Term
Pindolol
Definition
B1 B2 Blocker with B1 ISA
Term
Labetalol
Definition
a1 B1 B2 blocker with B2 ISA
Term
Acebutolol
Definition
B1 Blocker with B1 ISA
Class II Anti-arrhythmic
LUPUS-like syndrome
Intrinsic SNS activity, but no membrane
stabilizing effects
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina
Term
Metoprolol
Definition
B1 Blocker
Class II Anti-arrhythmic
Atrial Flutter; Atrial fibrillation; Ventricular arrhythmia (post-MI); Angina
Term
Atenolol
Definition
β1 Blocker
Class II Anti-arrhythmic
Longer acting Less polar → less CNS effects
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina
Term
Esmolol
Definition
β1 Blocker
Class II Anti-arrhythmic
Used IV when immediate block is needed
Cleared quickly
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina
Term
Captopril
Definition
ACE Inhibitor
Prevent A1 → A2 conversion
Venous & arterial vasodilation →
↓ preload & afterload
(+ ↑ bradykinin)
Abrupt ↓ in BP w/first dose (vol dep)
Rash, loss of taste, cough
Heart failure
Term
Lisinopril
Definition
ACE Inhibitor
Prevent A1 → A2 conversion
Venous & arterial vasodilation →
↓ preload & afterload
(+ ↑ bradykinin)
Abrupt ↓ in BP w/first dose (vol dep)
Rash, loss of taste, cough
Heart failure
Term
Enalapril
Definition
ACE Inhibitor
Pro-drug, longer duration
Prevent A1 → A2 conversion
Venous & arterial vasodilation →
↓ preload & afterload
(+ ↑ bradykinin)
Abrupt ↓ in BP w/first dose (vol dep)
Rash, loss of taste, cough
Heart failure
Term
Benazepril
Definition
ACE Inhibitor
Pro-drug, longer duration
Prevent A1 → A2 conversion
Venous & arterial vasodilation →
↓ preload & afterload
(+ ↑ bradykinin)
Abrupt ↓ in BP w/first dose (vol dep)
Rash, loss of taste, cough, Hyperkalemia
Heart failure
Term
Losartan
Definition
ARB
Vasculature A2 receptor blocker, sim. to ACE inhib. but no cough
Term
Valsartan
Definition
ARB
Vasculature A2 receptor blocker, like ACE inhib. but no cough, less effective in Africans
Term
Nifedipine
Definition
Vasodilator
Class IV Anti-arrhythmic (dihydropyridines primarely work on VASCULATURE)
Blocks L-type Ca2+ channel →
ARTERIAL vasodiltn & ↓HR & ↓CX (less deg.)
Highly protein bound (~90%)
Liver metabolized
Worsening angina, worsening HF, heart
block (in AV dz), bradycardia,
hypotension, edema, resp, GI
Not helpful for systolic dysfx
Helpful for diastolic dysfx (cardiac filling)
Heart failure / HTN
Reentry arrhythmia
Angina (vasospastic/exer)
Term
Verapamil
Definition
Vasodilator
Class IV Anti-arrhythmic
Blocks L-type Ca2+ channels
↓ HR, ↓ CX, ↓ conduction velocity (AV),
prolongs AV refractory period
Hypotension → reflex tachy, VERY NEGATIVELY INOTROPIC (don't use w/ b block),
heart block (AV conduction dz), bradycardia
(SA conduction dz), GI
Given orally but IV is better
More active L-isomer first pass met.
SVT
(acute or chronic)
Term
Diltiazam
Definition
Vasodilator
Class IV Anti-arrhythmic
Blocks L-type Ca2+ channels
↓ HR, ↓ CX, ↓ conduction velocity (AV),
prolongs AV refractory period
Hypotension → reflex tachy, neg. inotropy,
heart block (AV conduction dz), bradycardia
(SA conduction dz), GI
Less negative inotropic effects
(less ↓ CX)
SVT (acute or chronic)
Term
Hydralazine
Definition
Vascular Smooth Muscle Dilator
↑ NO + ↑ K+ perm.
ARTERIAL vasodilation → ↓afterload, ↑CX, renal dilation → ↑renal blood flow
SE: LUPUS-LIKE SYNDROME
Term
Sodium Nitroprusside
Definition
Vascular Smooth Muscle Dilator
Metabolized to NO→AC→ ↑cGMP → vasodiltn
VENOUS & ARTERIAL vasodilation → ↓preload & afterload
Term
Nitroglycerin
Definition
Vasodilator
Metabolized to NO → VENOUS & ARTERIAL vasodiltn → ↓ preload & afterload
Flushing, headache, hypotension, reflex
tachycardia,
Fast first pass metabolism
Tolerance develops rapidly
CHF (acute & chronic)
Vasospastic Angina
(w/Ca2+ blockers)
Term
Isosorbide dinitrate
Definition
Vasodilator
Metabolized to NO → VENOUS & ARTERIAL vasodilation → ↓preload & afterload
CHF, Vasospastic Angina (w/Ca2+ blockers)
Term
Quinidine
Definition
Class 1A Na+ Blocker (Intermediate r)
Blocks V-G Na+ channels & K+ channels
Blocks α-adren & vagus
↓ automaticity, ↑ AP = prolonged QT, widened
QRS, ↑ SA & AV node conduction velocity; "1A has Added AP"
GI, hepatic granulomas, torsades, cinchonism, LUPUS-LIKE syndrome (rarely), inhibits P450; will prolong P450 drugs
Can cause PARADOXICAL ↑ IN HEART RATE in
ATRIAL FLUTTER
Chronic SVT (2nd line)
Term
Procainamide
Definition
Class 1A Na+ Blocker (Intermediate r)
Blocks V-G Na+ channels & K+ channels
(no ANS effects)
↓ automaticity
↑ refractory period
↓ conduction velocity; ↑ AP = prolonged QT "1A has Added AP"


GI, hypotension, torsades,
heart block, AGRANULOCYTOSIS, LUPUS-LIKE SYNDROME (20-50%longterm)
Converted to active metabolite NAPA →
no Na+ channel activity but blocks K+
channels
Ventricular tachycardia; SVT (2nd line if DC cardioversion doesn't work; WPW syndrome
Term
Lidocaine
Definition
Class 1B Na+ Blocker (Rapid r)
Blocks Na+ channels, ↑ gK in fast fibers during phase 3 & 4
IV use only (↑ first pass metab)
B/c of rapid r only works on ischemic or heavily-driven tissue
↓automaticity, ↓ action potential "1B has Brief AP", ↓ conduction velocity, Widened QRS but shorter QT


SEIZURES
Nystagmus, tremor, dysarthria, altered
sernsorium
Ventricular tachycardia; Ventricular fibrillation (after amiodarone)
Term
Mexiletine
Definition
Class 1B Na+ Blocker (Rapid r)
Blocks Na+ channels, ↑ gK in fast
fibers during phase 3 & 4
orally available
B/c of rapid r only works on ischemic or heavily-driven tissue; ↓automaticity, ↓ action potential, ↓ conduction velocity; Widened QRS with shortened QT
Nausea, tremor, CNS effects Orally active
Neuropathic Pain (DM pts); Ventricular Tachycardia; ventricular fibrillation (but only after amiodarone)
Term
Flecainide
Definition
Class 1C Na+ Blocker (very long r)
Blocks Na+ channels
Blocks K+ channels
Blocks Ca2+ channels
↓ conduction velocity, widened QRS,
↑ action potential "1C continuous AP", prolonged QT, prolonged PR
Proarrhythmic (after MI)
Exacerbate CHF by ↓ LV fxn (low Ca)
Heart block (in AV node dz)

Atrial arrhythmia (in NO other heart disease ie Young PPL)
Term
Propafenone
Definition
Class 1C Na+ Blocker (very long r)
Blocks Na+ channels
Blocks K+ channels
Blocks β-adrenergic
↓ conduction velocity, widened QRS, ↑
action potential "1C continuous AP",
prolonged QT, prolonged PR
Proarrhythmic (after MI)
Exacerbate CHF by ↓ LV fxn
Heart block (in AV node dz), torsades
Bradycardia & bronchospasm (β block) Metab by P450
Atrial arrhythmia "causes more arrhythmias than it's worth"
Term
Amiodarone
Definition
Class III K+ Channel Blocker
Blocks K+ channels
Blocks Na+ & Ca2+ channels
Non-competitive SNS blocker
Prolonged QT, ↓ automaticity, ↓ conduction velocity,
widened QRS, prolonged PR

Corneal deposits (100%), LIVER DZ, HYPO & HYPERTHYROIDISM, PULM FIBROSIS,
vasodilation, photosensitivity/skin color Highly lipophilic, extensive tissue distrib + LONG hl
First line agent in ACLS code
Active metabolite: desethyl-amio
Atrial tachycardia; Ventricular tachycardia; Long term stab. with ICD
Term
Sotalol
Definition
Class III - K+ Channel Blocker
Blocks K+ channels
Non-selective β blocker
↑ action potential, ↓ automaticity,
↓ conduction velocity (AV only), prolongs AV refractory period

Torsades (especially in hypokalemia)
β blocker SE's
Renal excretion of unchanged drug
β blocker w/Class III effects
Atrial arrhythmias (chronic)
Term
Ibutilide
Definition
Class III - K+ Channel Blocker
Blocks K+ channels
Non-selective β blocker
IV use only, Delays repolarization, ↑ action potential, QRS stays same


Torsades
Contraindicated in hypokalemia
IV use only
Atrial Arrhythmias (Acute)
Term
Dofetilide
Definition
Class III - K+ Channel Blocker
Blocks K+ channels (rapid delayed rectifier K+ current)↑ action potential, QRS stays same
Greater effect on atrial than ventricles
Torsades
Rx Interax: ↑ [Dofetilide]
Interfere w/cation trx in kidney, prolong QT
interval, use liver metab.
Atrial Arrhythmias (chronic)
Term
Adenosine
Definition
Anti-arrhythmic
Binds adenosine receptors → opens
ACh-sens. K+ channel (in SA/AV/atria), anti-sympathetic tone (↓Na, ↓Ca)
Shortens atrial AP, ↓ automaticity,
↑ AV refractory period,
↓ AV conduction velocity


Transient: asystole, dyspnea, bronchoCX
Atrial fibrillation
Flushing
IV use only
Rx Interax: theophylline & caffeine block
adenosine receptors
Atrial tachycardia; Atial fibrillation; Produce controlled hypotension
Term
Digoxin
Definition
Anti-arrhythmic (AV Nodal Depressant)
MOA:
Direct: Blocks Na+/K+ ATPase
Indirect: vagal stimulation ↑ CX (↑ Ca2+) Vagal: ↓ atrial AP, ↓ SA automaticity & ↓ AV conduction velocity
Rx Interax: ↑ [Digoxin]
quinidine & verapamil
SVT (Acute or Chronic); CHF (↑CO)
Term
Digoxin
Definition
Digitalis Glycoside
MOA: Inhibit Na+/K+ ATPase binding
extracellularly on α subunit
Prefers E1-P form → stabilize to E2-P
form Na & Mg favor binding K favors release
MET: 25% plasma protein bound
Renal elimination, 2 day half-life
SE: Fatigue, malaise, dizziness, confusion,
delirium, anorexia, N/V, abdominal pain
color vision, halos, bradycardia, AV
block, ectopic beats, SA arrest,
ventricular arrhythmias, EKG changes
OTH: Aglycone portion = for cardiac activity; Monosaccharide chain = metab.; Eubacterium lentum in gut inactivates
USE: Heart Failure
Term
Digitoxin
Definition
Digitalis Glycoside
MOA: Inhibit Na+/K+ ATPase binding
extracellularly on α subunit
Prefers E1-P form → stabilize to E2-P
form Na & Mg favor binding K favors release
MET: >90% plasma protein bound
Hepatic elimination, 7 day half-life
SE: Fatigue, malaise, dizziness, confusion,
delirium, anorexia, N/V, abdominal pain
color vision, halos, bradycardia, AV
block, ectopic beats, SA arrest,
ventricular arrhythmias, EKG changes
OTH: Aglycone portion = for cardiac activity; Monosaccharide chain = metab.; Eubacterium lentum in gut inactivates
USE: Heart Failure
Term
Dopamine
Dobutamine
Definition
Misc. Inotropes
Stimulate β1 receptors → ↑ CX
SE: Dopamine: tachycardia, arrhymthia
Dobutamine: tolerance, vasodilation (via β2 receptors)
OTH: Dopamine vasodilates renal vasculature via D1 receptors
USE: Heart Failure (serious)
Term
Amrinone
Definition
Phosphodiesterase Inhibitor
MOA: Inhibits phosphodiesterase-III →
vasodilation & ↑ CX
MET: PDE-III selectively found in cardiac & smooth muscle
SE: Nausea, vomiting
Thrombocytopenia, liver damage Arrhythmia
OTH: Does more harm than good when used long term
USE: Heart Failure (serious)
Term
Acamprosate
Definition
Alcoholism Trx
MOA: Interacts with NMDA & GABA-A receptors
MET: Taurine derivative
OTH: Reduces hyperexcitability during withdrawal
USE: Alcoholism
Term
Disulfram
Definition
Alcoholism Trx
MOA: Irreversibly inhibit ALDH →
↑acetaldehyde
MET: Converted to active metabolites (which inhibit ALDH)
TOX: Acetaldehyde syndrome → alcohol flush reaction
USE: Alcoholism
Term
Naltrexone
Definition
Alcoholism Trx
MOA: Opiate µOR antagonist Blocks alcohol reinforcement
OTH: Reduces craving Reduces relapse rates by 50%
USE: Alcoholism
Term
Methanol
Definition
Alcoholism Trx
Methanol −ADH→ formaldehyde
−ALDH→ formic acid
TOX: Headache, vertigo, vomiting,
abd/back pain, dyspnea, met.
Acidosis, coma, resp. failure
OTH: Can cause blindness (15mL)
USE: Toxic
Term
Ethylene Glycol
Definition
Alcoholism Trx
MOA: Ethgly −ADH→ glycoaldehyde
−ALDH→ glycolic acid → glyoxylic & oxalic acid
TOX: Metabolic acidosis Renal failure (oxalate deposits)
OTH: Treat with EtOH Treat w/fomepizole: ADH inhibitor
USE: Antifreeze
Term
Fomepizole
Definition
Ethylene Glycol Trx
MOA: Alcohol Dehydrogenase Inhibitor
Term
Amphetamine
Definition
Drug of Abuse
↑ excess DA release and reverses the transport of DA, thus is more potent and longer acting than cocaine
SEL: Presynaptic DA terminal
MET: <12h; hih lasts 8-24hr
SHORT TERM USE: Euphoria rush; rapidly ↑ HR, BP; ↑ attention and decreased fatigue; ↑ activity (violent behaviors); ↓ appetite; ↑ respiration; hyperthermia
LONG TERM USE: Depletes DA in NAc (DA neve terminal damage); Dependence & psychotic symptoms; Paranoia; Hallucination; Mood disturbances; Repetitive motor activity
Term
Cocaine
Definition
Drug of Abuse
MOA: Binds to DA transporters to prevent reuptake of DA allowing an ↑ in DA-R1 effect (reward); Also ↓ VMAT2
SEL: DA transporters
USE: Local anesthetic; ↑ HR and BP; ↑ arousal and alertness; rush and euphoria; ↑ involuntary motor behaviors; stereotyped behaviors; paranoia; psychological dependence; Heart SE: cardiac arrhythmias (v fib), myocardial ischemia, cerebral vasoconstriction, seizures
Term
Heroin
Definition
Drug of Abuse
MOA: Agonst at Gi ↓ cAMP and PKA, thus ↓ Ca; K current ↑; Inhibitory response ↓ NT release; ↑ DA release in mesocorticallimbic system; Chronic use ↑ cAMP and PKA, thus activation CREB, which is inolvd in tolerance and dependance
SEL: MOR
WITHDRAWAL TRX: Methadone; Clonidine; Naltrexone; Buprenorphine
USE: euphoria, rapid tolerance to euphoria; RESP. DEPRESSION; sedation; analgesia; emetic effects; Miosis (Edinger-Westphal Stim) "Pinpoint Pupils"; Physical Dependence
Term
Lysergic Acid Diethylamide
Definition
Drugs of Abuse
MOA: thought to activate several types of 5HT receptors
MET: rapidly absorbed from oral; onset 40-60 min. peak 2-4 hrs lasting ~8hr
USE: perceptual distortions; profound hallucinations; mood changes; intense arousal; portentiousness
Term
Marijuana
Definition
Drugs of Abuse
MOA: THC binds to CBR1 receptors on GABA neurons in the NAc, inhibiting GABA release and disinhibiting DA release to ↑ DA R1 mediated signaling
SEL: CBR1's in NAc
USE: ↑ euphoria to minimize migraine; ↓ intraocular pressure (glaucoma); calm muscle spasms; restore appetite; anti-emetic
SX: lower flow to limbs; irritates lungs/airways; may lower sperm # or quality
Term
Nicotine
Definition
Drugs of Abuse
MOA: Stimulates the nAchR, on the mesoaccumbens DA system in the VTA
SEL: nAchR
TRX WITHDRAWAL: sprays, gums, patches; Buproprion (Wellbutrin); Mecamylamine nAchR antagonist
Term
Phencyclidine
Definition
Drugs of Abuse
MOA: Dissociative Anesthetic; binds Sigma receptors and NMDA-type of glutamate receptor (antagonist)
TRX WITHDRAWAL: haloperidol for psychosis
USE: emotional withdrawal; bizarre unpredictable aggressive behavior; psychosis
Term
Morphine
Definition
Strong Opoid
Potent MOR agonist
30% absorbed in gut
90% first pass metabolism
Analgesia, sedation, euphoria,
dysphoria, miosis, N/V, OH,
resp. & cough suppression
Pinpoint pupils = opioid OD
Constipation
Mod-severe pain
Myocardial infarction
Dyspnea, anxiety
Term
Methadone
Definition
Strong Opoid
Potent MOR agonist
Same potency as morphine
bioavailability than morphine
Long acting
No euphoria
Prevents W/D signs
Mod-severe pain
Opioid addiction
Term
Meperidine
Definition
Strong Opoid
Potent MOR Agonist
1/5 morphine potency
1/4 morphine duration
No cough suppression
Less constipation
No labor prolongation
OB/Surg analgesia
Mod-severe pain
Term
Fentanyl
Definition
Strong Opoid
Potent MOR Agonist
80x morphine potency Less nausea
Sufentanyl = ↑ fentanyl
Alfentanyl = ↓ fentanyl
Post-op pain
Anesthetic (w/droperidol)
Term
Codeine
Definition
Moderate Opoid Agonists
Weaker MOR agonist
Metabolized in part to morphine
Excellent bioavailability
Few SE Mild-moderate pain
Cough
Term
Oxycodone
Definition
Moderate Opoid Agonist
Weaker MOR agonist
Given w/aspirin or acetaminophen Abuse
Term
Propoxyphene
Definition
Moderate Opoid Agonist
Weaker MOR agonist
1/2 codeine potency
Given w/acetaminophen
Interax: alcohol/sedatives (fatal)
Mild-moderate pain
Term
Nalbuphine
Definition
Mixed Opoid Agon/Antag
KOR agonist
MOR antagonist
Same potency as morphine
5x pentazocine potency
Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Less psychotomimetic effects
Less MOR antagonist activity
Moderate-Severe Pain
Term
Buprenorphine
Definition
Mixed Opoid Agon/Antag
KOR agonist
MOR antagonist
25-50x morphine potency (pain)

Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Worse sedation & resp. depression
than morphine
Binds MOR w/high affinity
Mod-severe pain; Reduce Craving for Morphine
Term
Butorphanol
Definition
Mixed Opoid Agon/Antag
KOR agonist
MOR antagonist
30x pentazocine antagonism
20x pentazocine analgesia

Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Mod-severe pain
(acute)
Term
Pentazocine
Definition
Mixed Opoid Agon/Antag
KOR agonist
MOR antagonist
Given w/naloxone IV to avoid
analgesic & euphoric effects

Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Combined w/tripelennamine
("T's & blues") → heroin-like
Moderate pain
Term
Naloxone
Definition
Opoid Antagonists
Competitive opioid antagonist
(MOR) Fast onset
T-REX is bigger than an OX, and a
T-REX is more orally active!
Precipitates opioid W/D Opioid overdose
Term
Naltrexone
Definition
Opoid Antagonist
Competitive opioid antagonist
(MOR)3-5x naloxone potency
Long acting
Orally active (moreso)
Opioid addiction
(highly motivated)
Term
Tramadol
Definition
Misc. Opoids
Weak MOR agonist
Inhibits NE & 5-HT reuptake in CNS (MAR-I) stops pain trns spinal cord
1/10 codeine MOR affinity
6000x less morphine MOR affinity
Less potential for abuse &
respiratory depression
Dual mechanism of action
Dental pain
Acute Musculoskeletal pain
Cancer pain
Term
Procaine
Definition
Local Anesthetic (Ester)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
~
Quickly metabolized by PChE
SHORT ACTING
(metabolized by plasma ChE)
Given w/EPI
Aunt Ester had allergies
…but she was a peach! (PChE)
Infiltration
Nerve block
Spinal anesthesia
Term
Chloroprocaine
Definition
Local Anesthetic (Ester)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
~
Quickly metabolized by PChE
SHORT ACTING
(metabolized by plasma ChE)
Given w/EPI
Aunt Ester had allergies
…but she was a peach! (PChE)
Infiltration
Nerve block
Spinal anesthesia
Term
Tetracaine
Definition
Local Anesthetic (Ester)
More lipophilic than Pro/Coke:
Rapider onset, potenter
LONG ACTING
MOST COMMONLY USED DRUG FOR SPINAL ANESTHESIA
Topical LA
Term
Benzocaine
Definition
Local Anesthetic (Ester)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
~
Quickly metabolized by PChE
Poorly water soluble
So poorly water soluble that systemic toxicity
potential is zero.
DUSTING POWDER/OINTMENT
(burns/ulcerations)
Term
Lidocaine
Definition
Local Anesthetic (Amide)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel


Metab in Liver P450; Pts w/ Liver dx will see tox
More lipophilic than Pro/Coke:
Rapider onset, potenter
INTERMEDIATE ACTING
Drowsiness Used in ester-allergic individuals
LA
Cardiac arrhythmias
Term
Prilocaine
Definition
Local Anesthetic (Amide)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel


Metab in Liver P450; Pts w/ Liver dx will see tox
More lipophilic than Pro/Coke:
Rapider onset, potenter
INTERMEDIATE ACTING
Drowsiness Used in ester-allergic individuals
LA
Cardiac arrhythmias
Term
Mepivacaine
Definition
Local Anesthetic (Amide)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
Met. in Liver P450; Pts w/ Liver dx will see tox



More lipophilic than Pro/Coke
Rapider onset, potenter
INTERMEDIATE ACTING
LAXITY IN NEONATES; OB LA
Term
Bupivacaine
Definition
Local Anesthetic (Amide)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
Met. in Liver P450; Pts w/ Liver dx will see tox
More lipophilic than Mep/Lido:
LONG ACTING
Highly plasma protein bound
CARDIOTOXIC
Particularly long acting
(some nerve blocks last 24+ hrs!)
Analgesia + abdominal muscle control
Epidural anesthesia ;(OB)
Nerve blocks
Term
Levo-Bupivacaine
Definition
Local Anesthetic (Amide)
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
Met. in Liver P450; Pts w/ Liver dx will see tox
More lipophilic than Mep/Lido:
LONG ACTING
Highly plasma protein bound
Cardiotoxic
Particularly long acting
(some nerve blocks last 24+ hrs!)
Analgesia + abdominal muscle control
Epidural anesthesia (OB)
Nerve blocks
Term
Epinephrine
Definition
a1 a2 B1 B2 Agonist
Vasoconstrictor
All LA except Cocaine produce vasodilation → systemic absorption. LA formulated w/ Epi to ↓ system absorp. Localizes LA at desired site and lowers tox by allowing time for body to metabolize.
Term
Halothane
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Slow induction (↑ blood:gas)
Most potent (↓MAC)
HEPATOTOXICITY (free radicals)
SENSITIZES MYOCARDIUM to NE/EPI
↑cerebral blood flow
Halo = Heart
Term
Isoflurane
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Fluranes fluoride floppy
muscles


Intermediate induction
Intermediate potency
Fluranes (fluoride) can be nephrotoxic
↓minute volume
Muscle relaxation
Term
Enflurane
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Fluranes fluoride floppy
muscles


Intermediate induction
Intermediate potency
Fluranes (fluoride) can be nephrotoxic
↓minute volume
Muscle relaxation
Term
Sevoflurane
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Fast Induction (↓ blood:gas)
Low Potentcy (↑MAC)
Fluranes fluoride floppy
muscles


Fluranes (fluoride) can be nephrotoxic (sevo less)
↓minute volume
Muscle relaxation
Term
Desflurane
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Fast Induction (↓ blood:gas)
Low Potentcy (↑MAC)
Fluranes fluoride floppy
muscles


Fluranes (fluoride) can be nephrotoxic (sevo less)
↓minute volume
Muscle relaxation
Term
Nitrous Oxide
Definition
General Inhaled Anesthetic
Nonspecific interactions w/ lipid bilayer
Block K+ channels → hyperpolarization
Activate or facilitate GABA
Fast induction (↓ blood:gas)
Least potent (↑MAC)
NO potency
Term
Thiopental
Definition
General IV Anesthetics
Barbiturate
Ultra short acting
Rapid onset, short anesthesia
Diffuses out of brain
May produce "hangover"
Myocardial/Respiratory depression
↓cerebral/renal blood flow, ↓GFR
NOT Analgesic
Thio huxtable is ultra short
Term
Midazolam
Definition
General IV Anesthetic
Benzodiazepines
Slower onset
Long acting
Prolonged post-op. recovery
ANTEROGRADE AMNESIA
NOT Analgesic
Term
Fentanyl Sufentanil
Definition
General IV Anesthetic
High potency opioid Can be reversed w/naloxone Respiratory depression
Analgesic
Only anesthetic @ ↑ doses
Term
Propofol
Definition
General IV Anesthetic
Rapid onset
Rapid recovery
Anti-emetic
Respiratory depression
Hypotension
Most popular IV anesthetic Be proper, don't puke
Term
Etomidate
Definition
General IV Anesthetic
Rapid onset
Rapid recovery
Nausea & vomiting
Pain
(Minimal CV/repspiratory Depression)
Not analgesic He tummy ache
Term
Ketamine
Definition
General IV Anesthetic
Blocks NMDA receptors
CV stimulation: ↑HR, ↑BP, ↑CO
↑cerebral blood flow, ↑ICP
Disorientation, illusions, vivid dreams
Analgesic
Amnesia
Catatonia
Ketamine = catatonic
Term
Chlorpheniramine
Definition
First Generation H1 Receptor Antagonist

Block H1 receptor → ↓ histamine ax
Allergies
Motion sickness
Sedation
Antiparkinsonian effects
Anti-cholinergic effects
Anti-serotonergic effects
α receptor blocking
Local anesthetic effects
Rapidly absorbed orally
Metabolized by CYP3A4
Ineffective in bronchial asthma (mediated by
more than just ol' histamine)
Seasonal allergic rhinitis
Urticaria
Term
Diphenhydramine
Definition
First Generation H1 Receptor Antagonist

Block H1 receptor → ↓ histamine ax
Allergies
Motion sickness
Sedation
Antiparkinsonian effects
Anti-cholinergic effects
Anti-serotonergic effects
α receptor blocking
Local anesthetic effects
Strong sedation!
OTOTOXICITY
(newborns or ABX)
Allergies
Motion sickness
Sedation
(Benedryl)
Term
Promethazine
Definition
First Generation H1 Receptor Antagonist

Block H1 receptor → ↓ histamine ax
Allergies
Motion sickness
Sedation
Antiparkinsonian effects
Anti-cholinergic effects
Anti-serotonergic effects
α receptor blocking
Local anesthetic effects
STRONG SEDATION!
OTOtoxicity
(newborns or ABX)
Allergies
Motion sickness
Sedation
Term
Terfenadine
Definition
First Generation H1 Receptor Antagonist

Block H1 receptor → ↓ histamine ax
Allergies
Motion sickness
Sedation
Antiparkinsonian effects
Anti-cholinergic effects
Anti-serotonergic effects
α receptor blocking
Local anesthetic effects
Drug interax: CARDIOTOXIC w/ conazoles or
macrolides
Metabolized to fexofenadine (not cardiotoxic),
if CYP3A4 inhibited, terfenadine accumulates
Allergies
Term
Desloratadine
Definition
Second Generation H1 Receptor Antagonist
Active Metabolite of Loratadine
Long acting No significant side effects Block H1 receptor → ↓ histamine ax Allergies Little to NO sedation
(Claritin)
Term
Loratadine
Definition
Second Generation H1 Receptor Antagonist
Metabolized to Desloratadine
Long acting No significant side effects Block H1 receptor → ↓ histamine ax Allergies Little to NO sedation
(Claritin)
Term
Fexofenadine
Definition
Second Generation H1 Receptor Antagonist
Block H1 receptor → ↓ histamine ax
Little to NO Sedation
Lower risk of arrhythmia
Allergies
(Allegra)
Term
Cromolyn Sodium
Definition
Degranulation Inhibitor
Inhibit immunologically triggered mast
cell degranulation Most Effective
Ineffective after asthma attack has started
Bronchial asthma
(prophylaxis)
Term
Nedocromil
Definition
Degranulation Inhibitor
Inhibit immunologically triggered mast
cell degranulation Most Effective
Ineffective after asthma attack has started
Bronchial asthma
(prophylaxis)
Term
Magnesium Hydroxide
Definition
Antacid
Weak base neutralizes secreted HCL
Problems: Short duration of action, compliance, prevention of recurrence
Relieve pain; Promote Healing
Term
Cimetidine
Definition
H2 Receptor Antagonist
Competitive inhibitor of histamine (H2)-
stimulated gastric HCl secretion
Inhibits P450 system
Drug interax: ↑chlordiazepoxide, EtOH,
propranolol, theophylline, warfarin
Diarrhea, muscle pain
Headache, dizziness
GYNECOMASTIA, impotence

Gastric/duodenal ulcers
ZE syndrome
GERD
(Tagamet)
Term
Ranitidine
Definition
H2 Receptor Antagonist
Competitive inhibitor of histamine (H2)-
stimulated gastric HCl secretion
4-10x more effective than cimetidine
DOES NOT interfere with P450
Less side effects than cimetidine
No antiandrogenic effects
Gastric/duodenal ulcers
ZE syndrome
GERD

(Zantac)
Term
Famotidine
Definition
H2 Receptor Antagonist
Competitive inhibitor of histamine (H2)-
stimulated gastric HCl secretion
Not metabolized by P450 DON'T USE IN RENAL DISEASE
Gastric/duodenal ulcers
ZE syndrome
GERD

(Pepcid)
Term
Nizatidine
Definition
H2 Receptor Antagonist
Competitive inhibitor of histamine (H2)-
stimulated gastric HCl secretion
DON'T USE with salicylates
Gastric/duodenal ulcers
ZE syndrome
GERD
(Axid)
Term
Omeprazole
Definition
Proton Pump Inhibitor
Active form irreversibly binds & inhibits
proton pump in parietal cells
Absorbed in alkaline SI pH
Use >2 months not advisable
Diarrhea, nausea
Dizziness, headache
Heals duodenal ulcers more rapidly than H2
blockers
Gastric/duodenal ulcers
ZE syndrome
GERD
(Prilosec)
Term
Sucralfate
Definition
Mucosal Protectant
Aluminum salt of sucrose sulfate →
binds plasma proteins in crater →
protective barrier
Short acting
Drug interax: blocks tetracycline & PO4
absorption
Constipation
Nausea
Additionally: inhibits pepsin & bile aciton
Also: ↑ prostaglandin release
Duodenal ulcer
Term
Misoprostol
Definition
Misoprostol
Prostaglandin E1 analog → ↓ H+ ( ↓cAMP)
↑mucus & ↑bicarbonate secretion
Nausea, diarrhea
ABORTION IN PREGGOS
Gastric/duodenal ulcers
NSAID-induced damage
Term
Sulfasalazine
Definition
Inflammatory Bowel Disease
Bacteria split azo bond → 5-ASA (&
sulfapyridine) → ↓ inflammation
75% reaches colon
5-ASA = active metabolite
Sulfapyridine = SEs
Nausea, vomiting
Headache
Allergy
Can cause ↓ folate absorption;
Ulcerative colitis (85%)
Colonic Crohn's Dz
Term
Infliximab
Definition
Inflammatory Bowel Disease
Infliximab
Monoclonal antibody against TNF-α → ↓
inflammatory action
Single IV infusion → remission
Nausea
Serum sickness
Infections, autoimmunity, cancer;
Crohn's disease
Term
Acyclovir
Definition
Guanine nucleoside analog
Viral thymidine kinase produces analog →
binds viral DNA polymerase & inactivates
Valacyclovir −(rapidly)→ acyclovir
Nausea, vomiting, diarrhea
Headache, renal dysfx
Resistance: altered/deficient viral
thymidine kinase or
viral DNA polymerase
HSV
VZV
Term
Ganciclovir
Definition
Guanine nucleoside analog
Viral thymidine kinase produces analog →
binds viral DNA polymerase & inactivates
MYELOSUPRESSION, neutropenia vision
disturbances, carcinogenic
CNS effects
More toxic than acyclovir
CMVertables are fos
cars, cid so you ganci
the road fomi
CMV
(retinitis)
Term
Foscarnet
Definition
Inorganic pyrophosphate analog
Reversibly inhibits viral DNA & RNA polymerases
Nausea, fever, headaches, hypocalcemia,
hypomagnesemia, nephrotoxicity, anemia,
GENITAL ULCER
More toxic than gancyclovir
CMV (retinitis)
HSV
(acyclovir resist.)
Term
Zanamavir
Definition
Viral Respiratory Infections
Inhibits neuraminidase → ↓ release of virus →
↑ viral aggregates & ↓ viral spread
Orally inhaled
Used once taily to prevent flu
Nasal/throat discomfort, headache,
bronchospasm (asthmatics)
Influenza A & B If taken within ~30 hrs of SX onset →
↓ duration & respiratory complications
Term
Trifluridine
Definition
Pyrimidine analog Cornea inflammation
Tri flurting w/Kera's
tits & HSV
HSV
(Keratoconjunctivitis)
(Epithelial keratitis)
Term
Fomivirsen
Definition
Antisense oligonucleotide
Iritis, vitritis, ↑ intraocular pressure
Vision changes
Don't give to patients who have taken
cidofovir in past month

For herpes, tri giving
acyclovir, doc (or
dox)!
CMV (retinitis)
(in HIV patients unresp)
Term
Interferon Alpha
Definition
Viral Hepatitis Infection
IFNα & IFNβ bind cellular receptors → activate JAK-
STAT → ↑ 2,5-oligoadenylate synthetase & kinase
→ ↓ protein syn
IM or SC injection
Flu-like symptoms, BONE MARROW SUPRESSION, fatigue, infections, anorexia,
diarrhea, depr, anxiety
HPV
Hepatits B & C
Kaposi's sarcoma, MS
Term
Oseltamivir
Definition
Viral Respiratory Infections
Inhibits neuraminidase → ↓ release of virus →
↑ viral aggregates & ↓ viral spread
Orally inhaled
Used once taily to prevent flu
Nausea, vomiting, headache
If taken within ~30 hrs of SX onset →
↓ duration & respiratory complications
Influenza A & B
Term
Ribavirin
Definition
Viral Hepatitis Infection
Synthetic guanosine nucleoside analog
Alters nucleotide pool → ↓ viral mRNA syn
Conjunctiva irritation, wheezing, rash
Anemia, BONE MARROW SUPRESSION
TERATOGENIC
Ribavirin blocks RNA
of virin
Hepatitis C
RSV , Influenza, HIV
Parainflu, Paramyxo
Term
Zidovudine
Definition
Nucleoside Reverse Transcriptase Inhibitor (AZT)
Converted via human thymidine kinase → AZT-TP
→ incorporated into viral DNA → terminates chain
elongation
↑ toxicity w: probenecid, tylenol,
lorazepam, indomethacin, cimetidine
Anemia, LEUKOPENIA, headaches, lactic
acidosis, hepatic steatosis, lipoatropy,
central fat, ↑lipids
Protects fetuses from infection
Resistance: mutated RT w/↓ affinity for
AZT-TP
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Term
Abacavir
Definition
Nucleoside Reverse Transcriptase Inhibitor
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
Given w/AZT or Lamivudine or
protease inhibitor
Hypersensitivity, fever, GI, malaise, rash
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Term
Didanosine
Definition
Nucleoside Reverse Transcriptase Inhibitor (ddl)
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
Orally in buffered tablets
↑ toxicity w: stavudine
PANCREATITIS (pot fatal), PAINFUL peripheral neuropathy
Resistance: mutated RT
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
(AZT resistant)
Term
Lamivudine
Definition
Nucleoside Reverse Transcriptase Inhibitor (3-TC)
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
PANCREATITIS (pediatric patients)
Resistance to AZT develops more slowly
if you add lamivudine
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Hepatitis B
Term
Zalcitabine
Definition
Nucleoside Reverse Transcriptase Inhibitor (ddC)
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
Given w/AZT or alone
(if can't tolerate AZT)
Stomatitis, peripheral neuropathy, rash
Resistance: mutated RT
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Term
Stavudine
Definition
Nucleoside Reverse Transcriptase Inhibitor (d4T)
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
Peripheral neuropathy
LACTIC ACIDOSIS (pot fatal), hepatic steatosis,
lipoatropy, central fat, ↑lipids
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Term
Efavirenz
Definition
Non-Nucleoside RT Inhibitor
Binds next to RT activation site → change
conformation → inhibit RT activity
Given w/AZT & lamivudine
Dizziness, headache, insomnia, rash
Nightmares, hallucinations
↓ [phenobarb, phenytoin, carbmzpne,
methadone, rifabutin]
Rifampin → ↓ efav
Never ever tell a nun
a lie.
HIV
Term
Nevirapine
Definition
Non-Nucleoside RT Inhibitor
Binds next to RT activation site → change
conformation → inhibit RT activity
Given w/didanosine & stavudine Rash, fever, nausea, HEPATOTOXICITY (pot fatal)
↓ [rifampin, ketoconazole, ethinyl
estradiol (BC)]
SJW → ↓ nevir

Never ever tell a nun
a lie.
HIV
Term
Tenofovir
Definition
Nucleoside Reverse Transcriptase Inhibitor
Inhibits viral reverse transcriptase → terminates
DNA chain elongation
Do not give w/didanosine, lamivudine,
abacavir
Flatulence
Renal toxicity
Zitty Zal went nuclear
& did stab a baby
lamb he tends.
HIV
Hepatitis B
Term
Lopinavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
Diarrhea, nausea, fatigue, headache,
hyperlipidemia, hyperglycemia, altered
body fat
Administered together:
Ritonavir inhibits CYP3A4 →
↑ Lopinavir
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Ritonavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
SJW lowers concentration
Diarrhea, nausea, fatigue, headache,
hyperlipidemia, hyperglycemia, altered
body fat
Administered together:
Ritonavir inhibits CYP3A4 →
↑ Lopinavir
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Indinavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
SJW lowers concentration
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Atazanavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia

Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Nelfinavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions

Diarrhea, nausea, vomiting, lipodystrophy
hyperglycemia
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Saquinavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
SJW lowers concentration
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Amprenavir
Definition
Protease Inhibitor
Interferes w/proteolysis of gag-pol viral protein
precursor → nonfunctional virions
Inhibits CYP34A (Rx toxicity)
Rifampin induces CYP3A4
Diarrhea, nausea, vomiting, lipodystrophy
hyperglycemia
Although HIV cross-resistance occurs,
most likely to still be Amprenavir
susceptible
Nel is a LIAR. She is
a professional tease
and will inhibit or slow
your fost progress
HIV
Term
Enfuvirtide
Definition
Fusion Inhibitor
Binds viral envelope glycoprotein to prevent
conformational change when binding host cell
membrane
Pain, erythema, nodules, cysts
(at injection site)
Injected twice a day Binds enfulope HIV
Term
Carbamazapine
Definition
Partial & Generalized Tonic-Clonic Seizures
Block Na+ channel
(prolong inactive state)
Enhance GABA activity
Induces liver microsomes
Produces active 10,11 epoxide metabolite
Acute: stupor, coma, convulsions, irritability
Chronic: diplopia, ataxia, GI, sedation, fluid reten
Major: APLASTIC ANEMIA, AGRANULOCYTOSIS
Accelerates metabolism: phenytoin,
primadone, ethosuximide, valproate, BC
Congener (oxcarb) less toxic, less potent
Partial seizures
Gen. tonic-clonic seizures
Trigeminal neuralgia
Bipolar Disorder
(not absence)
Term
Clonazepam
Definition
Benzodiazepine
Long Acting
Bind α1γ2 on GABA-A receptor
→ ↑ GABA binding freq.
→ ↑ Cl- conductance
→ neuron hyperpolarizaiton
→ ↓ neuron activity
~
Anxiolytic-sedative
Hypnotic
Anesthesia
Anticonvulsant
Muscle relaxation
Alcohol withdrawal
Sedation, tolerance, withdrawal
Absence seizures
Myoclonic seizures
Infantile spasms
Term
Diazepam
Definition
Benzodiazepine
Bind α1γ2 on GABA-A receptor
→ ↑ GABA binding freq.
→ ↑ Cl- conductance
→ neuron hyperpolarizaiton
→ ↓ neuron activity
~
Anxiolytic-sedative
Hypnotic
Anesthesia
Anticonvulsant
Muscle relaxation
Alcohol withdrawal
STATUS EPILEPTICUS
Term
Ethosuximide
Definition
Generalized Seizures
Block T-type Ca2+ channel (↓ threshold)
↓ rhythmic thalamic activity
Good absorption orally (stomach irritation)
75% liver metabolized
GI, lethargy, fatigue, rash, BONE MARROW SUPRESSION Phensuximide & methsuximide not as good Absence seizures
Term
Felbamate
Definition
Partial & Generalized Tonic-Clonic Seizures (in conjunction)
NMDA antagonist
Enhance GABA
APLASTIC ANEMIA
SEVERE HEPATITIS
Partial seizures
(poorly controlled)
Term
Gabapentin
Definition
Partial & Generalized Tonic-Clonic Seizures (in conjunction)
GABA analog
(↑ release of GABA)
Renal excretion of unchanged drug Somnolence, dizziness, ataxia NO LIVER INVOLVEMENT ALL RENAL!
Partial seizures
Neuropathic pain
Alcoholism
Term
Lamotrigine
Definition
Partial & Generalized Tonic-Clonic Seizures (in conjunction)
Block Na+ channel
(prolong inactive state)
May block Ca2+ channel
Headache, diplopia, rash, nausea, dizziness, ataxia Life-threatening rash in 1-2% of patients
Partial seizures
Generalized seizures
Absence seizures
Myoclonic seizures
Term
Phenobarbital
Definition
Partial & Generalized Tonic-Clonic Seizures
Block Na+ channel
(prolong inactive state)
Prolongs GABA-A channel activity
Block AMPA receptor
Sedation, ataxia, respiratory depression, rash,
nystagmus, porphyria, tolerance, withdrawal
Congeners (mephobarbital & primidone)
Partial seizures
Gen. tonic-clonic seizures
(not absence)
Term
Phenytoin
Definition
Partial & Generalized Tonic-Clonic Seizures
Block Na+ channel
(prolong inactive state)
Admin: oral / IV (status epilepticus)
90% protein bound
First order (low) → Zero order (high)
Displaced by other protein-bound Rx
Acute: nystagmus, diplopia, ataxia, GI, conf.
Chronic: GINGIVAL HYPERPLASIA, hirsutism,
osteomalacia, rash, AGRANULOCYTOSIS,
megaloblastic anemia
High IV: arrhythmia, CNS depression
Congeners (mepheny/etho-toin) more toxic
Phenacemide very toxic (refractory partial)
Fosphenytoin = more soluble (injection)
↓ BC effectiveness & birth defects
Partial seizures
Gen. tonic-clonic seizures
Status epilepticus
(not absence)
Term
Topiramate
Definition
Partial & Generalized Tonic-Clonic Seizures (in conjunction)
Block Na+ channel
(prolong inactive state)
Enhance GABA activity
Somnolence, dizziness, fatigue, cognitive slowing,
weight loss
USED FOR WEIGHT LOSS
Partial seizures
Gen. tonic-clonic seizures
Term
Valproic Acid
Definition
Generalized Seizures
Block Na+ channel
(prolong inactive state)
↑ GABA (↑ GAD) ↓GABA-T activity
Block T-type Ca2+ channel
Well absorbed
90% protein bound
Liver metabolized
Nausea, vomiting, GI, hepatotoxicity, TERATOGEN,
Sedation (w/phenobarbital)
Preferred over ethosuximide if absence +
generalized tonic-clonic seizures
Absence seizures
Myoclonic seizures
Atonic seizures
Partial seizures
Term
Echinacea
Definition
Alternative Medicines
Proposed immune stimulant
Flu-like, hepatitis, asthma, rash,
nausea, urticaria, anaphyaxis
May contain organocholine
pesticides
URI or "Colds"
Term
Ephedra
Definition
Alternative Medicines
Contains ephedrine
(sympathomimetic)
Stroke, arrhythmias, hypertension
16x risk of hemorrhagic stroke
(w/phenylpropanolamine)
Weight loss
Energy
Term
Ginger
Definition
Alternative Medicines
Effective anti-nausea
Inhibit thromboxane synthase
Contraind: anti-coagulants
(may inhibit platelet aggregation)
As effective as antihistaminics in
nausea
Motion sickness
Morning sickness
Term
Saw Palmetto
Definition
Alternative Medicines
Inhibit 5α-reductase → ↓DHT
Block α1 receptors
Headache, GI, hypertension, ↓libido Trad. > Saw palmetto > placebo BPH
Term
Kava
Definition
Alternative Medicines
Enhances GABA activty
Dry flaking skin, puffy face, red eyes,
weakness, oral tingling, GI, SOB,
EKG abnormalities
Can cause serious cirrhosis & LIVER FAILURE!
Anxiety
Insomnia
Term
Glucosamine
Definition
Alternative Medicines
Stimulate cartilage cells → GAG &
proteoglycans
Gi discomfort, nausea,
photosensitivity, systolic HTN,
proteinuria
Osteoarthritis
Wound healing
Term
Levodopa/Carbidopa
Definition
Dopamien Agonists
Dopamine agonist (→ DA)
L-DOPA −(AADC)→ DA
↑ DA in striatum
C-DOPA: ↓ peripheral AADC
L-DOPA → DA (AADC)
DA (MAO-B, DBH, COMT)
Periph: N/V, OH, arrhythmia
CNS: On-off, wear-off, dyskin
Psych: hallucin, delusion, sleep
Peak-Dose: grimace/writhe
Neuroleptic malignant syndrome
↑ SNS tone peripherally
N/V/anorexia via CTZ stimulation
Tubero-infund DA → ↓ prolactin
Parkinson's Disease
Term
Apomorphine
Definition
Potent Non-Ergot Dopamine Agonists
Dopamine agonist
Used in "frozen" cases
(Reverses "off" state)
Advanced PD on ↑ dose L-DOPA
Parkinson's Disease
Term
Bromocriptine/Pergolide
Definition
Ergot-Der. Dopamine Agonists
B: D2 agonist / D1 antagonist
P: D2 agonist / D1 agonist
B: short half-life
P: better w/L-DOPA (D1 & lipophilic)
Nausea/vomiting, somnolence, dry mouth, edema,
insomnia, postural/OH, recalled due to heart valve regurg
Peak-dose, on-off,
depr., anxiety, hallucinations
Bromo only works in pts resp. to L-Dopa; causes CARDIAC ARRHYTHMIA Pergolide
allows ↓ L-DOPA dose
Parkinson's Disease
Term
Selegiline
Definition
MOA-Inhibitor

Inhibits MAO-B → ↑ striatal DA Used when L-DOPA effects are starting to
decline or in early mono-therapy
Insomnia; Dyskinesia; Nausea; Headache; Cardiac Arrhythmia; Hypertension; Contra-indicated w/ SSRI's and Tricyclics
Parkinson's Disease
Term
Pramipexole/Ropinirole
Definition
Non-Ergot Dopamine Agonist
D2 agonist
Nausea, somnolence, dry mouth, edema,
insomnia, postural/OH
Peak-dose, on-off,
depr., anxiety, hallucinations
Reduce on-off in late PD, most effective in early-mono therapy;
Pramipexole can delay L-DOPA by 2
years
Parkinson's Disease
Term
Amantadine
Definition
Anticholinergic
Treats influenza A & hepatits C
May: alter DA release/reuptake
Block NMDA receptors
Block mACh receptors
Restlessness, agitation, insomnia,
confusion, hallucinations, OH No effect on tremor
Parkinson's Disease Bradykinesia & Rigidity or L-Dopa induced motor side-effects, no effect on Tremor
Term
Tolcapone/Entacapone
Definition
COMT-Inhibitors

Inhibits COMT → ↑ DA in cleft
Produce 2x ↑ in bioavailability & half-life
of L-DOPA Tolcapone: FATAL HEPATOTOXICITY & CNS activity
Competes w/L-DOPA → BBB Attenuates the "wearing off" time Prim in pts who have received long L-Dopa trx with motor side-effects
Parkinson's Disease Adjunctive therapy in late stage after 5/7 yrs of L-Dopa; used to amelorate "Freezing" and peak-dose dyskinesia
Term
Heparin (IV)
Definition
Anticoagulant
HMW binds Antithrombin III and catalytically accelerates (~1000-fold) interaction w/ thrombin forming inactive 1:1 ratio (also inhibits XIIa, IXa, VIIa, and Xa), LMW heparin fractions inhibit activated factor X but have much less effect on coagulation in general. Highly electronegative acidic mucopolysaccharides
1/3 of molecules in Heparin have catalytic effect
Anti-compliment
Anti-histiminic (slight)
Inhibit BOTH in vivo/in vitro clotting
Metabolism follows ZERO-ORDER KINETICS
Does NOT cross placenta/breast milk
Contraindicated in bleeding, hemophilia, GI ulcerative lesions, severe hypertension, brain, spinal cord, eye surgery, viceral carcinoma, threatened abortion. osteoporosis + fractures (long term)
Special caution renal or hepatic dysfunction.
Synergistic with oral anti-coag
Protamine sulfate neutralizes in vivo
STOPS CLOTTING
Term
Warfarin Sodium (oral)
Definition
Coumarin Anti-coagulant
Blocks gamma-carboxylation of glutamate residues in prothrombin (II) and coag factors VII, IX, and X; proteins C and S
Blocks an epoxide reductase essential in regenerating active form of Vit. K → prevents hepatic synthesis of clotting factors
8-12 hr onset; acts ONLY IN VIVO
Second-most-likely drug after Insulin to send pts to the emergency room
Very narrow therapeutic window
Variations in CYP2C9 (liv metab) and VKORC1 (Vit K) genes account for variability in pts Warfarin metabolism
Extensively bound to plamsa albumin and crosses placenta/breast milk readily → hemorrhagic event in fetus
TERATOGENIC - messes with bone formation
hydroxylated in liver, elim feces/urine
Synergistic with Pyrazolones (augment antithrombosis, peptic ulcer disease)
Barbs and Rifampin induce liver CYP enzymes, lower warfarin effect
Aspirin, hepatic disease, and hyperthyroidism augment warfarin effect
Vit. K, Chlorthalidone/Spironolactone, and hypothyroidism reduce effects of Warfarin
Term
Protamine Sulfate
Definition
Heparine Neutralizer
Term
Aspirin
Definition
*IRREVERSIBLY binding to COX *Prevents activation of thromboxane A2 (a potent stimulator of platelet aggregation) *Inhibits platelet aggregation and platelet content release *Prolongs bleeding time
*Prevention of MIs (low dose , 325mg daily)
*Excessive bleeding , GI bleeding , PUD
Term
Clopidogrel
Definition
Antiplatelet
*IRREVERSIBLE inhibition of ADP-mediated platelet aggregation *NO effect on prostaglandin metabolism
*Prevention of ischemic events
*Fewer SE than ticlopidine
*~1% LEUKOPENIA *Thrombotic thrombocytopenia purpura
Term
Urokinase
Definition
Thrombolytic
*Human enzyme produced by the kidney that converts plasminogen to plasmin *Plasmin then functions to break up the clot by dissolving fibrin
*IV for mutiple pulmonary emboli , central deep venous thrombosis *Management of acute MIs *t-PA (Altepase) is also utilized for patients with acute stroke symptoms (shown to decrease disability 1-year post CVA).
*Excessive bleeding , cerebral hemorrhage
Term
Alteplase
Definition
Thrombolytic
*Unmodified tissue plasminogen activator (t-PA) *Converts fibrin-bound plasminogen to plasmin (CLOT SELECTIVE)
*IV for mutiple pulmonary emboli , central deep venous thrombosis *Management of acute MIs *t-PA (Altepase) is also utilized for patients with acute stroke symptoms (shown to decrease disability 1-year post CVA).
*Excessive bleeding , cerebral hemorrhage
Term
Aminocaproic Acid
Definition
Fibrinolytic Inhibitor
*Inhibits fibrinolysis via inhibition of plasminogen activation
*Treatment of acute bleeding episodes in hemophilia and other bleeding disorders. *Prophylaxis for rebleeding from intracranial aneurysms
*Intravascular thrombosis , Hypotension , Myopathy , Abdominal discomfort , Diarrhea *CI: DIC , Genitourinary bleeding of the upper tract (kidneys , ureters) => potential for excessive clotting
Term
Vitamin K
Definition
Confers Biological Activity upon Prothrombin (II), VII, IX, and X
*Supplementation of naturally endogenous substance responsible for the carboxylation of coagulation factors VII , IX , X , II (prothrombin)
*Treatment of vitamin K-deficient states seen in newborns , elderly , ICU pts *Given to ALL newborns prophylacticly *Reversal of warfarin overdose
*Rapid IV infusion can cause dyspnea , chest and back pain , or death
Term
Iron Dextran
Definition
IRON
*Parenteral
*Used only for the treatment and prevention of iron deficiency anemia *Increased iron requirements-- infants , rapid growth in children, pregnancy and lactation , elderly populations , chronic kidney disease (may lose or form rbc's 2ary to hemodialysis and erythropoietin treatment) *In men and postmenopausual women presume Fe deficiency is from blood loss until proven otherwise *Inadequate iron absorbtion-- Inadequated GI absorbtion
*Inadequate GI Fe absorbtion and advanced kidney disease = parenteral iron
*Dextran hypersensitivity: urticaria , fever , phlebitis , arthralgieas , bronchospasm. Anaphylaxis and death (both rarely). *Should perform test for Iron Dextran toxicity
*CI: Pts w Fe overload , idiopathic hemchromatosis , thalassemia major , transfusion hemosiderosis.
Term
Ferrous Sulfate
Definition
IRON
*Ferrous more efficiently absorbed
*Used only for the treatment and prevention of iron deficiency anemia *Increased iron requirements-- infants , rapid growth in children, pregnancy and lactation , elderly populations , chronic kidney disease (may lose or form rbc's 2ary to hemodialysis and erythropoietin treatment) *In men and postmenopausual women presume Fe deficiency is from blood loss until proven otherwise *Inadequate iron absorbtion-- Inadequated GI absorbtion
*Normal GI absorbtion = oral preparations prefered
*SE are directly related to bioavailability *Acute oral iron toxicity in children : necrotizing gastroenteritis w/ vomitting , bloody diarrhea , lethargy and dyspnea. Followed by severe metabolic acidosis , coma , and death *Treatment of toxicity: whole bowel irrigation (eliminate unabsorbed Fe in GI Tract) ; Iron-Chelating agent , Deferoxamine sulfate (Desferal) to sequester and excrete already absorbed Fe ; Supportive therapy *As little as 400 mg Fe can cause death in children
*200-400mg Fe given daily to correct deficency rapidly (3-6 months) *50-100mg Fe can be incorporated into hemoglobin daily for Fe deficient individual. *CI: Pts w Fe overload , idiopathic hemchromatosis , thalassemia major (cooley's anemia , 2ary to numerous transfusions) , transfusion hemosiderosis.
Term
Cyanocobalamin/Hydroxocobalamin
Definition
Vitamin B12
*Vitaminer of the B12 family (somehow related to B12??)
*Pernicous anemia and malabsorbtion *Vit B12 Def (seru cobalamin levels < 200 pM/L . Macroovalocytosis and reduced hemogobin levels occur in late stages of disease)
*IM or SC
Term
Vitamin B12
Definition
*Vit B12 Def (serum cobalamin levels < 200 pM/L . Macroovalocytosis and reduced hemogobin levels occur in late stages of disease) *Normoblasts w/in 6-8 hours , Psychiatric problems relieved w/in 24 hours , Neurological damage requires more slow recovery because of need for myelin regeneration , failure of reversal after 12 - 18 months indicate that neurological damage is irreversible
*Injection (parenteral???)
*Anaphylaxis possible *Overly rapid correction of anemia can produce circulatory overload.
Term
Folic Acid
Definition
*Deficiency usually results from increased requirements : liver disease , GI abnormalities , alcoholism , drugs *Rapid response , bone marrow pathology back to normal in hours , brisk reticulocytosis in 2-5 days *Alcoholics may have impaired hepatic storage and/or increased folic acid release (even w adequate dietary intake) *Increased Folic Acid requirement during pregnancy , deficiency can cause neural tube defects , spina bifida , anencephaly
*Parenteral : critically ill , GI disorders (limiting folate absortion) *Oral : Folic acid supplements , Pregnant , Liver disease , Alcoholism , Hemodialysis
*DI: methotrexate (inhibit dihydrofolate reductase) , anti-convulsants , some anti-malarial drugs *Long term use of following drugs may increase need for folate : some oral contraceptives , steroids , analgesics , sulfsalazine *Large doses of folate can mask pernicous anemia and lead to irreversibe neurologic damage
*Present in many common foods (fruits , vegetables , meats) , Used to fortify enriched grains in America *Increased requirements or inadequate intake may lead to folate deficiency: pregnancy and lactation , children w poor diets , critical illness , severe infections , hemolytic anemia , hemodialysis , chronic diseases (eg. renal failure ,inflamation , neoplasia)
Term
Deferoxamine Sulfate
Definition
Iron Chelating Agent
Treats Iron Overdose
Term
Erythropoietin
Definition
*Erythropoietin stimulates erythroid proliferation and differentiation by interacting with specific erythropoietic receptors , member of JAK/STAT cytokine receptor superfamily , on RBC progenitor cells
*For anemia of chronic renal failure since kidneys are unable to produce enough hormone. *Can actually prevent the need for blood transfusion *ruHuEPO , Epoetin Alpha not cleared by dialysis *In selected patients , primary bone marrow disorders , aplastic anemia , secondary anemias (AIDS , chronic malignancies , chronic inflamation) *Accelerate erythropoiesis after phlebotomies to treat hemochromatosis (or maybe some other blood loss)
*SE: Rapid increase in hemoglobin-- hypertension , thrombotic complications *PTS w bone marrow disorders , nutritional and secondary anemia have high levels of endogenous erythropoietin. Positive response to this treatment is less likely *Failure to respond to this teatment can often be easily resolved by adding iron or folic acid if either of these are deficient
*Normally produced in the peritubilar interstitial cells of the kidney in response to tissue hypoxia *Increased erythropoietin reverses anemia provided there is normal bone function , sufficient iron , Vitamin B12 , Folic Acid *Normal levels : 20 IU/L , Moderately severe anemia : 100-500 IU/L , Severe anemia : 1000's of IU/L
Term
Granulocyte Colony Stimulating Factor (GCS-F) (filgrastim)
Definition
*Synthesized w recombinant DNA technology *Stimulate proliferation and differentation of their respective cell lines *React with specific receptors of various myeloid progenitor cells . Recpetors are associated wuith cytoplasmic tyrosine kinases in JAK/STAT pathway
*Neutrophil lineage *Use in autologous / allogenic (same species) hematopoietic stem cell transplantation. *Chemotherapy-induced neutropenia *Chronic neutropenia
*IV
*Bone pain *Better tolerated than GM-CSF
Term
Granulocyte Macrophage Colony Stimulating Factor (GM-CSF) (Sargramostim)
Definition
*Synthesized w recombinant DNA technology *Stimulate proliferation and differentation of their respective cell lines *React with specific receptors of various myeloid progenitor cells . Recpetors are associated wuith cytoplasmic tyrosine kinases in JAK/STAT pathway
*Multi-potential hematopoietic growth factor *Use in autologous / allogenic (same species) hematopoietic stem cell transplantation. *Chemotherapy-induced neutropenia in acute myeloid leukemia
*IV
*Fever , arthralgias , malaise
Term
Megakaryocye Growth Factor: Interleukin 11 (Oprelvekin)
Definition
*Acts through a specific cell surface cytokine receptor , stimulated the growth of multiple lymphoid and myeloid cells. *Increase number of peripheral platelets and neutrophils.
*Thrombocytopenia *Prevent thrombocytopenia in patients receiving chemotherapy for nonmyeloid cancer.
*SE: Fatigue , HA , CV effects , anemia , dyspnea (fluid retention) *Reversible upon drug discontinuation.
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