Rx Flashcards
epinephrine
Class: Adrenergics
catecholamines
A1&A2&B1&B2&B3 agonist
sympathetic stimulation = inc heart rate, contractility, BP and CO
low doses: B preferred
uses: cardiac arrest, cardiogenic shock, severe hypotension, anaphylaxis, respiratory distress, urticaria, keep anesthetic “local”
side effect: hyperglycemic effect, tachycardia, arrhythmia, MI
~adrenaline
norepinephrine
Class: Adrenergics
catecholamines
A1&A2>B1 agonist
stimulates peripheral vasoconstriction and inc BP
use: shock, severe hyoptension
side effect: MI due to increased cardiac work
isoproterenol
Class: Adrenergics catecholamines B1 & B2 agonist inc HR, contractility and cardiac output use: bradycardia, asthma, bronchitis, and emphysema. side effects: tachycardia, MI
dopamine
Class: Adrenergics catecholamines low dose: D1&D2&B1 agonist high dose: A1&A2 agonist (act as vasopressor) increase contractility and HR use: cardiogenic shock, CHF *causes renal vasodialtion side effect: arrhythmias
dobutamine
Class: Adrenergics
catecholamines
B1 agonist
uses: cardiogenic shock, congestive heart failure
(increases contractility w/o increase HR) increases cardiac output
side effect: arrhythmias, hypotension
phenylephrine
adrenergic Agonists/ sympathomimetics
direct agents
A1>A2
vasopressor
uses: rhinitis, decongestion, SVT, hypotension, shock
*big vasoconstriction= increase systemic resistance= inc BP=vagal stimulation= slows heart rate
side effect: rebound mucous swelling
midodrine
Agonists/ sympathomimetics
direct agents
A1
uses: hypotension, retinal exams (dilates pupils)
brimonidine
presynaptic anti-adrenergic
direct, Agonist A2
causes dec NE and suppresses sympathetic
uses: glaucoma (decreases aqueous humor formation)
clonidine
presynaptic anti-adrenergic direct, Agonist A2 causes dec NE and suppresses sympathetic uses: HTN, (inhibits sympathetic outflow) side effect: sedation (CNS active)
oxymetazoline (Afrin)
Agonists/ sympathomimetics
direct agents
A1 & A2
use: decongestion
albuterol/salmeterol/terbutaline (proventil/ventolin)
adrenergic Agonists/ sympathomimetics direct agents B2 causes bronchiodilation use: asthma, COPD side effects: tachycardia, tremor
fenoldopam
adrenergic Agonists/ sympathomimetics direct agents D1 use: severe HTN rapid renal and splanchnic vasodilating effects
amphetamine
adrenergic Agonists/ sympathomimetics
Indirect acting agents
mechanism: inhibits MAO, releases endogenous NE from storage vesicles= inc NE binding to adrenergic receptors
CNS excitation (can cross BBB)
stimulant: increases heart rate and blood pressure and decreases appetite
ephedrine
adrenergic Agonists/ sympathomimetics
Mixed agent
Indirect acting: inc NE release from neuron and binding to adrenergic receptor
DIRECTLY stimulates A1&B2
use: asthma, nasal decongestion, hypotension
side effect: HTN
phenoxybenzamine
adrenergic Antagonists/ adrenergic receptor blockers
A1 & A2,
noncompetitive, binds irreversibly
use: HTN
side effect: reflex tachycardia, increased insulin
phentolamine
Antagonists/ adrenergic receptor blockers
A1 & A2, competitive
causes: dilation of smooth muscle and dec BP
Uses: HTN
side effects: reflex tachycardia and arrhythmias
prazosin
Antagonists/ adrenergic receptor blockers
A1 selective
competitive
causes blood vessel vasodilation and dec BP
use: HTN (does not cause tachycardia)
side effect: hypotension and dizziness
“minipress”
tamsulosin
Antagonists/ adrenergic receptor blockers
A1a selective (GU tract)
use: benign prostatic hypertrophy and bladder obstruction
side effect: floppy iris syndrome
terazosin
Antagonists/ adrenergic receptor blockers A1a selective (GU tract) use: benign prostatic hypertrophy, HTN
pindolol
Antagonists/ adrenergic receptor blockers
B1 & B2, weak
intrinsic sympathomimetic activity (less effect on resting HR)
use: HTN
side effect: bronchoconstriction
propranolol
Antagonists/ adrenergic receptor blockers,
Antiarrhythmic: class 2
B1 & B2, strong
effect: prolongs AV conduct and refract; decreases HR and contractility
use: angina pectoris, HTN, MI, SVT, ventricular arrhythmia, tachycardia, Afib, Aflutter
side effect: bronchoconstriction, heart failure
metoprolol
Antagonists/ adrenergic receptor blockers
Antiarrhythmic: class 2
B1 selective
(-) inotropy, (-) chronotropy
use: HTN, MI, SVT, CP, tachycardias, IHD, CHF
less likely to cause bronchoconstriction
side effect: bradycardia, enters brain (CNS sedation)
labetalol
Antagonists/ adrenergic receptor blockers
causes vasodilation
Mixed: A1 & B
use: HTN, angina pectoris, CHF
side effects: hypotension, fatigue, bradycardia
carvedilol
Antagonists/ adrenergic receptor blockers
Mixed: A1 & B
use: HTN, angina pectoris, tachycardia, CHF
(inc ejection fraction)
guanethidine
Antagonists/ block adrenergic neuronal function (peripheral pre-synaptic)
decreases NE in synaptic cleft
use: severe HTN, renal HTN
side effects: hypotension, fluid retention, impaired ejaculate, diarrhea, nerve toxicity
**not used anymore
hexamethonium (C6)
nonspecific Antagonist
adrenergic and nicotinic cholinergic receptors (nAChnR)
blocks all stimulation of pre-ganglionic neurons
stops release of NE and ACh
use: HTN
side effects: severe
not used clinically
atropine
anticholinergic
nonselective muscarinic Antagonist
use: bradycardia, vagal hyperactivity, bronchospasms, over-secretions
(treats DUMBBLSS)
side effect: “hot as a hare, dry as a bone, red as a beet, blind as a bat, and mad as a hatter”
flush, blurred vision, dec secretions, hyperthermia, delirium, hallucinations
big CNS effects
cocaine
adrenergic agonist; indirect sympathomimetic
block catecholamine reuptake by membrane transporter (NET)
increases NE in synapse
use: causes vasoconstriction, local anesthesia
side effect: MI
(+) inotropic drug
increase heart contractility
(+) chronotropic drug
increase heart rate
nicotine
nicotinic agonist
nicotinic acetylcholine receptors
stimulate both para- and sympathetic postganglionic neurons
causes skeletal muscle contraction
side effect: medullary depression, inc HR/BP/RR, spasms, toxic
succinylcholine (anectine)
nicotinic agonist
binds nicotinic acetylcholine receptors (Nm subtype)
causes prolonged neuromuscular depolarization
use: paralysis for surgery
side effect: malignant hyperthermia, hypotension, arrhythmias
depolarizing blockade- cannot be overcome by cholinesterase inhibitor
pancuronium, rocuronium
antinicotinic
competetive antagonist of nicotinic acetylcholine receptors (Nm)
use: paralysis for surgery
side effect: histamine release, hypotension, increase HR, edema
nondepolarizing blockade- can be overcome by cholinesterase inhibitor
ipratropium (atrovent)
antimuscarinic
nonselective antagonist acts on parasympathetic sites
inhaled to M3 acetylcholine receptors in bronchi
cause: dec bronchoconstrictions and secretions
use: COPD
Procainamide
Antiarrhythmic: class 1A: moderate Na channel blocker binds Na in active state slows conduction/prolong refractory period reduces ectopic foci automaticity use: reentry and ectopic; SVT, VT, VF, WPW side effect: SLE, long QT
Quinidine
Antiarrhythmic: class 1A: moderate Na channel blocker binds Na in active state slows conduction/prolong refractory period reduces ectopic foci automaticity use: reentry and ectopic; SVT, VT, VF side effect: long QT, thrombocytopenia, strong anti-cholinergic effect
Lidocaine
Antiarrhythmic: class 1B: WEAK Na channel blocker binds Na in both active/inactive state increase velocity at AV; decrease AP reduces ectopic foci automaticity may shorten QT use: VT, VF, WPW, use after MI side effects: CNS toxicity and cardiac depression IV only
Flecainide
Antiarrhythmic: class 1C: STRONG Na channel blocker
reduces SA node and ectopic foci automaticity
reduces all conduction velocity
prolongs refractory period, long (QT, QRS, and PR)
use: Afib
side effects: heart block, arrhythmias
atenolol
Antiarrhythmic: class 2, B-blockers B1 selective use: HTN, CP/MI, does not cross BBB decreases HR, output, renin release little resp. effects (no B2)
labetalol
Antiarrhythmic: mixed alpha and beta blocker
A1, B1, B2 antagonist
lowers BP (A1), no reflex tachycardia (B1)
use: HTN, CHF, CP
side effect: orthostatic hypotension, heart failure
carvedilol
Antiarrhythmic: mixed alpha and beta blocker
A1, B1, B2 antagonist
lowers BP (A1), no reflex tachycardia (B1)
use: CHF, HTN, CP
side effect: orthostatic hypotension
amiodarone
Antiarrhythmic: class 3, prolong K repolarization
decrease K efflux
reduce conduction velocity
prolongs refractory and AP
use: VT, Vfib, Afib, Aflutter
side effects: long half life, long (QT, QRS, PR), eye dysfunctions
CYP3A4: affects renal/hepatic elimination (must change warfarin and digoxin levels)
sotalol
Antiarrhythmic: class 3, prolong K repolarization AND nonselective B-blocker prolong AP and refract period use: VT *less side effects than amiodarone
ibutilide
Antiarrhythmic: class 3, prolong K repolarization prolong AP slow inward Na current use: Afib, Aflutter side effect: long QT IV only
bretylium
Antiarrhythmic: class 3, prolong K repolarization
blocks the release of norepi from nerve terminals
prolongs AP
use: HTN, only affects ventricle (VT, Vfib)
verapamil
Antiarrhythmic: class 4, slow inward Ca
Non-dihydropyridine calcium channel blocker
act on heart
reduce SA/AV conduction, prolong refractory (long PR)
use: SVT, atrial tachy, atrial flutter, Afib
side effects: bradycardia, hypotension, AV block, GI effects
do not use on WPW
CYP3A4: affects renal/hepatic elimination (must change warfarin and digoxin levels)
diltiazem
Antiarrhythmic: class 4, slow inward Ca
Non-dihydropyridine calcium channel blocker
act on heart
reduce SA/AV conduction, prolong refractory (long PR)
use: SVT, CP, Afib, HTN
side effects: bradycardia, hypotension, AV block
action of B-blockers as a class
decrease HR, contractility,
decrease SA/AV automaticity, conduction velocity
decreases renin
blocks vasoconstriction and decreases peripheral vascular resistance
bronchoconstriction
hyperglycemia sx
digoxin
antiarrhythmic: cardiac glycoside
slows conduction through AV node
block Na/K-ATPase pump
decrease conduction, prolong refract (long PR)
EKG: short QT, Twave inversion
enhance vagal activity at AV node, stimulates carotid baroreceptor
decrease HR
(+) ionotroph, increased intracellular Ca
use: ventricular response of Afib, Aflutter, cardiogenic shock, CHF
side effects: digitalis toxicity, bradycardia, fatigue, hypokalemia, arrhythmias, heart block, GI: n/v/d (vagal)
do not mix with quinidine
adenosine
antiarrhythmic
prolongs refract: increase K efflux=hyperpolarization
decreases AV conduction velocity, blocks Ca entry
EKG: long PR
induces transient heart block, break re-enty
use: re-entry SVT, vasodilation
works very quickly and lasts only a short period of time
side effects: flushing, CP, arrhythmia, dyspnea, hypotension
magnesium
use: torsades de pointes, dig toxicity
potassium
use: hypokalemia and electrolyte-associated cardiac arrhythmias
side effect: VT
bethanechol
direct cholinergic agonist muscarinic: M1, M2, M3 AND nicotinic agonist increase parasym and secretions use: post-op GI and bladder motility resistant to AChE side effect: bradycardia, bronchoconstriction, parkinsonism
muscarine
cholinergic agonist
muscarinic: M1, M2, M3
not used clinically
mushroom product used to discover M receptor
pilocarpine
direct cholinergic agonist
muscarinic: M1, M2, M3
use: glaucoma (causes miosis), increase secretions (sweat/saliva)
carbachol
direct cholinergic agonist
muscarinic: M1, M2, M3
AND nicotinic agonist
increase parasym
use: glaucoma (causes miosis)
side effect: constriction
scopolamine
anticholinergic muscarinic antagonist: alkaloid receptors at eyes and glands use: motion sickness, n/v/d can enter BBB; less CNS than atropine
homatropine
anticholinergic muscarinic antagonist: alkaloid receptors at eye causes mydiasis and cycloplegia side effects: blurred vision, sensitivity, drowsiness can enter BBB
oxybutynin/darifenacin/solifenacin
anticholinergic
muscarinic antagonist: tertiary
use: bladder spasms, leakage/incontinence
can enter BBB
side effects: dec secretions, mydiasis and cycloplegia
tolterodine
anticholinergic muscarinic antagonist: tertiary decreases bladder tone use: overactive bladder side effects: constipation, dry mouth, headache can enter BBB
benztropine
anticholinergic
muscarinic antagonist: tertiary
central action
use: parkinsonism, tremors, rigidity, drooling, akinesia
side effects: tachycardia, hypotension, dry mouth
can enter BBB
ipratropium/tiotropium
anticholinergic muscarinic antagonist: quaternary local: respiratory inhalation tx use: bronchoconstriction, COPD, asthma
propantheline
anticholinergic muscarinic antagonist: quaternary local: GI, urinary reduces motility and delays emptying stomach use: peptic ulcers, spasms
glycopyrrolate
anticholinergic muscarinic antagonist: quaternary local: GI, urinary use: peptic ulcers also decreases secretions and cardiac relfexes in intubation
pirenzepine
muscarinic antagonist:
M1 selective
use: peptic ulcers (dec gastric acid)
trimethaphan
neural nicotinic (Nn) receptor antagonist
non-depolarizing ganglion blocker
use: HTN
causes vasodilation
triggers histamine release (inc HR, decrease contractility)
side effects: severe
not used clinically
varenicline
neural nicotinic (Nn) receptor partial agonist selective A4B2 subtype in CNS reduces nicotine stimulation use: smoking cessation side effects: psych, AMS
methyldopa
presynaptic anti-adrenergic strong Agonist A2 causes dec NE and suppresses sympathetic Use: HTN side effect: sedation
esmolol
Antagonists/ adrenergic receptor blockers
B1 selective
Use: aortic dissection, tachycardia, SVT
rapid onset, short duration
propafenone
Antiarrhythmic: class 1C: STRONG Na channel blocker
slows AV conduction, prolongs refract
use: SVT, Afib
side effects: heart failure, bradycardia, arrhythmia
do not give post MI
dofetilide
Antiarrhythmic: class 3, prolong K repolarization prolong AP increase ERP use: Afib, Aflutter side effect: long QT, dizziness
Niacin
antihyperlipidemic agent: B vitamin.
effect: - decreases the synthesis VLDL by the liver
- decrease LDL.
- decreases the synthesis of cholesterol.
- increases the level of HDL (decrease the catabolism)
- decreases Lp(a)
- lowering serum triglycerides.
use: hypertriglyceridemia; combined with an HMG CoA reductase inhibitor to treat most forms of hypercholesterolemia
side effects: flushing, hepatotoxicity
con: need large dose
Fenofibrate
antihyperlipidemic agent: fibric acid derivatives
effect: -decrease triglycerides (VLDL) (by activating protein lipase activity)
- increases HDL
use: Familial hypertriglyceridemia, Dysbetalipoproteinemia
side effects: -myopathy and rhabdo
interacts with anti-coag tx
do not use in renal failure
Colestipol
antihyperlipidemic agent: Bile acid sequestants
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.
Cholestyramine
antihyperlipidemic agent: Bile acid sequestants
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.
Colesevelam
antihyperlipidemic agent: Bile acid sequestants
**best of the group
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.
Lovastatin
antihyperlipidemic agent: HMG-CoA reductase Inhibitors
*weak
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4
Simvastatin
antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4
Pravastatin
antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Atorvastatin
antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4
Rosuvastatin
antihyperlipidemic agent: HMG-CoA reductase Inhibitors
*newest
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Asians show high levels
Ezetimibe
antihyperlipidemic agent: Cholesterol absorption inhibitor
Effects: inhibits dietary cholesterol GI absorption
- Lowers LDL
Use: lower serum cholesterol; can be combined with a statin
Side effects: minor GI
Laropiprant
Prostaglandin D2 antagonist
Use in Niacin therapy to reduce flushing
Neomycin
antihyperlipidemic agent: aminoglycoside antibiotic.
effect: inhibiting the reabsorption of cholesterol and bile salts.
effect: reduction of total body cholesterol.
- does not affect triglyceride levels.
Use: combination with niacin to lower Lp(a) levels
aliskiren
renin inhibitor
effect: blocks angiotensinogen conversion
use: HTN
side effects: hypotension, hyperkalemia, rash, GI, renal failure
CYP3A4
teratogenic
captopril, lisinopril, enalapril
“pril”
ACE inhibitor
prevents formation of angiotensin2
inc bradykinin and prostaglandins= vasodilation
use: high-renin HTN, arteriolar/venous vasodilation
post MI- enhance reperfusion
side effects: natriuresis, cough, airway irritation, angioedema, renal failure, hyperkalemia
teratogenic
losartan
“sartan”
angiotensin 2 antagonist- (ARB) blocks receptor at vascular muscle use: HTN, CHF side effects: hypotension, dizziness, renal failure, hyperkalemia teratogenic
spironolactone
aldosterone receptor antagonist
K sparing diuretic
use: edema, CHF, HTN
side effects: endocrine imbalances, hyperkalemia, gynecomastia
eplerenone
aldosterone receptor antagonist K sparing diuretic use: edema, CHF, HTN side effects: hyperkalemia **lower affinity for other steroid hormone receptors than spironolactone= less side effects
hydralazine
direct vasodilator relaxes arterioles dec BP and afterload reflex inc HR and CO directly inc renal blood flow use: HTN, pregnancy side effects: many side effects, SLE, fluid retention
minoxidil
direct vasodilator
prodrug
opens K channels=hyperpolarizes smooth muscle=relaxes arterioles
use: HTN, topical tx male pattern baldness
side effect: hirsuitism, reflex tachycardia, pulmonary damage, fluid retention
sodium nitroprusside
direct vasodilator
effect: dilates arteries and veins (dec preload and after load)
nitric oxide–>cGMP–> inactivate myosin= relax smooth muscle= vasodilation
use: IV HTN crisis
side effect: severe hypotension, cyanide toxicity, hepatotoxicity, renal toxicity
nitroglycerin
anti-anginal agent
nitric oxide–>cGMP–> inactivate myosin= relax smooth muscle= vasodilation
effect: dilates large coronary arteries= inc blood to heart
dec venous tone= dec cardiac preload
use: CP, MI
side effects: hypotension, reflex tachycardia, cerebral ischemia
do not use with: alcohol, vasodilatiors, PDE5 inhibitors (“afils”)
nifedipine
anti-HTN/anti-anginal calcium entry blocker potent peripheral vasodilator side effect= TOXIC, reflex tachy and inc CO, MI not used
nicardipine, clevidipine
anti-HTN/anti-anginal calcium entry blocker potent peripheral vasodilator use: CP, HTN emergency side effect= reflex tachy and inc CO, palpitations
isosorbide dinitrate
anti-anginal nitrate
nitric oxide–>cGMP–> inactivate myosin= relax smooth muscle= vasodilation
use: CP, CHF
do not combine with vasodilation meds
isosorbide-5-mononitrate
anti-anginal nitrate
nitric oxide–>cGMP–> inactivate myosin= relax smooth muscle= vasodilation
use: CP, CHF
do not combine with vasodilation meds
nimodipine
anti-HTN/anti-anginal calcium entry blocker effects cerebral artery vasodilation use: subarachnoid hemorrhage/CNS damage side effect: carcinogenic and teratogenic
uses for mannitol, furosemide (lasix), and hydrochlorothiazide (HCTZ)
diuretic
use: edema, CHF, HTN
works on kidney to increase Na/water excretion
aspirin
acetylsalicylic acid
anti-platelet
irreversible cyclooxygenase inhibitor
dec thromboxane A2 and prostaglandins= dec platelet aggregation
use: MI, stroke, inflammation, fever, pain
side effects: GI ulcers, bleeding, hemorrhage, asthma
recommend: low dose, not for children
PO
clopidogrel (Plavix®), prasurgel (Effient®), Ticlopidine (Ticlid)
anti-platelet: thienopyridines
irreversibly blocks ADP receptor (P2Y1 and P2Y12)
use: acute coronary syndrome, atheroclerosis, peripheral arterial disease
side effects: GI ulcers, bleeding, thrombotic purpura
CYP450
PO, prodrug
ticagrelor (Brilinta®)
anti-platelet: thienopyridines reversible ADP receptor blocker use: reduce MI, stroke combine tx with aspirin side effect: bleeding PO
dipyridamole
anti-platelet
PDE inhibitor= inc cAMP
vasodilator (inc levels of adenosine)
use: post heart valve replacement surgery, history stroke
combine tx with warfarin or aspirin
side effect: hypotension, syncope, headache, GI
cilostazol
anti-platelet PDE 3 inhibitor= inc cAMP and PKA effect: dilates lower ext blood vessels use: intermittent claudication side effects: headache, palpitations CYP3A4, CYP2C19
abciximab
anti-platelet: glycoprotein 2b/3a inhibitor
monoclonal antibody
use: before coronary angioplasty (PCI), MI
side effect: bleeding
combine tx with heparin or aspirin
eptifibatide
anti-platelet: glycoprotein 2b/3a inhibitor
synthetic peptide, fibrinogen analog= blocks platelet crosslinking
use: acute coronary syndrome, before coronary angioplasty (PCI), MI
side effect: bleeding, renal failure
tirofiban
anti-platelet: glycoprotein 2b/3a inhibitor
reversible
use: unstable angina, before coronary angioplasty (PCI)
side effects: bleeding
heparin
Unfractionated heparin
(UFH)
anticoagulant
binds to antithrombin 3 (AT3)= more active= inactivates thrombin (factor 2) and active factor 10, 9, 11.= no fibrin
immediate action
use: DVT, PE, surgery, acute coronary syndrome
side effect: bleeding, hemorrhage, necrosis at injection site, thrombocytopenia
**highly variable anticoagulant response/effects/duration= LMWH used more
IV/injection
antidote: protamine sulfate
monitor aPTT
intrinsic pathway
Low-molecular-weight heparins, (LMWH)
enoxaparin “parin”’s
anticoagulant
smaller fragment of heparin
binds to antithrombin 3 (AT3)= more active= inactivates active factor 10
use: DVT, PE, surgery, acute coronary syndrome
side effect: bleeding, renal failure
**more controlled anticoagulant response/effects/duration= used more common
IV/injection
antidote: protamine sulfate
does not effect PT
intrinsic pathway
fondaparinux
anticoagulant inhibits factor 10a use: DVT, PE side effect: bleeding, rash does not effect PT
warfarin (coumadin)
anticoagulant inhibits enzyme epoxide reductase (VKOR)= inactive vitamin K= loss of gamma-carboxylation rxn for dependent clotting factors (2,7,9,10) uses:DVT, PE, Afib, dilated cardiomyopathy, prosthetic heart valves side effects: bleeding, necrosis, GI CYP2C9 many drug interactions NOT in pregnancy orally monitor PT/INR/vit K extrinsic pathway
lepirudin, bivalirudin
anticoagulant direct thrombin inhibitor (from hirudin) alternative to heparin (no HIT, does not use AT3) side effect: bleeding, renal failure IV
dabigatran (pradaxa),
anticoagulant prodrug, direct thrombin (factor 2a) inhibitor use: stroke, Afib, DVT, PE, post surgery *no need to monitor PT side effects: bleeding NOT in pregnancy orally
rivaroxaban, apixiban
anticoagulant prodrug, direct factor 10a inhibitor use: stroke, Afib, DVT, PE, post surgery *no need to monitor PT side effects: bleeding CYP3A4 NOT in pregnancy orally
argatroban
anticoagulant direct thrombin inhibitor (from hirudin) alternative to heparin (no HIT, does not use AT3) side effect: bleeding cleared through LIVER CYP450 IV *similar to lepirudin, bivalirudin, but better for bad renal pts
streptokinase, urokinase
thrombolytic agent
activates plasminogen= plasmin= degrades fibrin/fibrinogen
use: DVT, MI, stroke, dialysis pts with occlusion
side effect: bleeding, immune rxn
IV
tissue plasminogen activator (tPA)
thrombolytic agent activates plasminogen= plasmin= degrades fibrin and ACTIVE clot use: coronary occlusion side effects: hematoma IV
