Drugs Flashcards Preview

• Bile Acid Binding Sequestrant (gel)
• Lower LDL ~20%
• Very safe, non-systemic, but cannot be used if triglycerides >250

• Platelet aggregation inhibitor
• ADP receptor blocking agent
• Trade name: Ticlid, use is associated with increased incidence of Thrombotic Thrombocytopenic Purpura (TTP) in 1:2000-4000 patients

• IV Vasodilator 
• Primarily a venodilator

• Ib

• Binds INa+ channel in active and inactive states, but not in the resting state. So it has little effect in normal tissue, but does exert effects in sick (ischemic) tissue.

• Chronic suppression of ventricular arrhythmias (not first line, but sometimes)

• Nausea, vomiting

• Centrally acting agent
• Replaces norepinephrine in secretory vesicles in adrenergic neurons.  Acts centrally on the brain to inhibit central adrenergic outflow.
• Useful for hypertension in pregnancy, but many side effects
• Sedation, dry mouth, fatigue, depression, liver toxicity

• Platelet aggregation inhibitor
• Acetylates cyclooxygenase, irreversibly inhibiting it. Prevents production of ThromboxaneA2 (platelet activator)
• Function returns to normal after 7-10 days when new platelets appear in circulation.

• Inotrope
• Phsophodiesterase inhibitor

• Inotrope
• Complicated mechanism: direct membrane effects (mediated by blocking Na+/K+ ATPase), and indirect effects (vagomimetic). Slows conduction, mainly in the SA node, atria, and AV node.
• Control of ventricular response in atrial fibrillation/flutter (usually with a β-blocker or Ca2+ channel blocker)
• Yellow vision, anorexia, nausea, vomiting, disorientation, hallucination.  Toxicity treated with anti-digoxin antibody fragments

• III

• Blocks potassium channels, increases action potential duration and effective refractory period. Also blocks Na+ channels, β receptors, and Ca2+ channels (class I, II, and IV-like effects). Most effective, but has significant side effects.

• Suppression of ventricular tachycardia (defibrillators more effective).  Maintenance of sinus rhythm in atrial fibrillation/flutter.  Acute conversion from atrial fibrillation to sinus rhythm.

• Hyperthyroidism and hypothyroidism.  Pulmonary fibrosis, liver toxicity, photodermatitis (grayish-blue skin discoloration).  Dronedarone, a congener, has fewer side effects. 

• Beta blocker
• Blocks the B1 and B2 receptors
• Basically decrease CO.  Decreasing HR, decreased contractility, and decreased renin release.  Also causes vasoconstriction and a slight increase in PVR.  Used in patients with CAD, and for hypertension (but not as the sole agent)
• Bradycardia, hyperkalemia, fatigue, cold extremeties, bronchospasm.

• III
• K+ channel blocker
• Acute termination of atrial fibrillation and atrial flutter
• Few extracardiac effects other than GI complaints

• Loop Diuretic
• Inhibit the Na-K-2Cl symporter in the thick ascending loop of Henle
• Rapid diuresis, HTN in CKD
• Hypokalemia, hypocalcemia, hypomagnesemia, increased LDL and triglycerides, hyperglycemia

• Calcium channel blocker (Dihydropyridine)
• Block the L-type calcium channel (primarily in smooth muscle), relaxing smooth muscle
• Hypertension, decreases cardiac output and PVR.  Good in patients with diabetes, renal insufficiency, lipid problems, and asthma.
• Peripheral edema, headaches, flushing, dizziness, GERD, constipation

• Oral Vasodilator
• Block the angiotensin II receptor (AT1), decreasing sympathetic activation, relaxing smooth muscles, and causing diuresis
• Hyperkalemia, renal failure, teratogenic!

• Direct Factor Xa Inhibitor
• Small molecule inhibitor of factor Xa (free and bound)
• Anticoagulant
• Trade name: Eliquis, monitoring not required

• Calcium channel blocker (phenylalkylamine)
• Block the L-type calcium channel (mostly cardiac), relaxing smooth muscle
• Hypertension, greatly reduces PVR.  Good in patients with diabetes, renal insufficiency, lipid problems, and asthma.Constipation, dizziness, nausea, bradycardia

• Statin
• Inhibits HMG CoA Reductase, decreasing cholesterol synthesis.  Leads to increased LDL receptors
• High intensity (40/80 mg/day), moderate intensity (10 mg/day)CYP3A4

• Ib

• Binds INa+ channel in active and inactive states, but not in the resting state. So it has little effect in normal tissue, but does exert effects in sick (ischemic) tissue.

• Ventricular arrhythmias, particular post-MI

• CNS toxicity: confusion, delirium, paresthesias, grand mal seizures

• Potassium Sparing Diuretic
• Antagonizes the mineralcorticoid (aldosterone) receptor on epithelial cells in the late distal tubule and cortical collecting duct
• Diuretic, generally an add-on therapy with another diuretic class
• Hyperkalemia, gynecomastia

Inhibit renin

• Cholesterol absorption inhibitor
• Absorbed, glucuronidated, and then localizes to the intestinal villi, preventing absorption of cholesterol
• Lower LDL ~20%
• Useful in combination with a moderate intensity statin

• Statin
• Inhibits HMG CoA Reductase, decreasing cholesterol synthesis.  Leads to increased LDL receptors
• Moderate intensity

• Vitamin B3
• Potent inhibitor of adipose tissue lipolysis by activating GPR109A (a GPCR).  This decreases flux of free fatty acids to the liver for VLDL production
• Lowers LDL and VLDL, raises HDL
• No measurable benefit when added to a statin.  Take aspirin before niacin to avoid cutaneous vasodilation and flushing.

• Disinhibit LDLR
• Dec LDL
• Myalgias, Delerium, Dementia

• Inotrope
• Beta I and B2 agonist 

• Loop Diuretic
• Inhibit the Na-K-2Cl symporter in the thick ascending loop of Henle
• Rapid diuresis, HTN in CKD
• Ototoxicity, hypokalemia, hypocalcemia, hypomagnesemia, increased LDL and triglycerides, hyperglycemia

• Unclassified
• Complicated mechanism: direct membrane effects (mediated by blocking Na+/K+ ATPase), and indirect effects (vagomimetic). Slows conduction, mainly in the SA node, atria, and AV node.
• Control of ventricular response in atrial fibrillation/flutter (usually with a β-blocker or Ca2+ channel blocker)
• Yellow vision, anorexia, nausea, vomiting, disorientation, hallucination.  Toxicity treated with anti-digoxin antibody fragments

• Act plasminogen
• Higher fibrin specificity
• Direct plasminogen activation

• Ic

• Sodium channel blocker, some β-blocking activity, negative inotropic effects

• Acute conversion of atrial fibrillation to sinus rhythm.  Maintenance of sinus rhythm in atrial fibrillation.  Suppression of premature ventricular contractions (rarely used for this, raises mortality).

• Can exacerbate bronchospasm (β-blocker...)

• Peripheral vasodilator
• Activates a potassium channel in vascular smooth muscle, causing K efflux.  This hyperpolarizes the cell and relaxes it.
• Lower blood pressure in difficult patients
• Water and sodium retention, tachycardia/angina/heart failure, hypertrichosis, effusions

• Direct Thrombin Inhibitor
• Binds both the active pocket site and fibrinogen binding exosite on thrombin.
• Anticoagulant
• Originally derived from leeches, now made with recombinant DNA technology

• IV Vasodilator
• Metabolized by blood vessels to nitric oxide, causing vasodilation.
• Lower blood pressure in difficult patients or emergencies.  Mixed venous and arterial vasodilator
• Hypotension, cyanide and thiocyanate toxicity.  IV only

• Heparin
• Lower molecular weight inhibits Xa, higher molecular weight inhibits thrombin and binds platelets. All enhance antithrombin activity.
• Anticoagulant
• Can cause heparin induced thrombocytopenia, and osteoporosis (when used chronically), can be self administered.

• Thiazide Diuretic
• Inhibit the Na-Cl symporter in the distal convoluted tubule
• First line hypertension
• Hypokalemia, hyponatremia, hypercalcemia, impotence, impaired glucose tolerance, increased cholesterol

• Ia

• Blocks INa and blocks IKr, slowing the action potential upstroke and prolonging the action potential duration. Also binds the M2 muscarinic receptor for vagolytic effects (stronger than quinidine)

• Hypertrophic obstructive cardiomyopathy (but not commonly used)

• Antimuscarinic side effects (urinary retention, constipation, blurred vision, dry mouth, closed-angle glaucoma)

• Bile Acid Binding Sequestrant (resin)
• Binds bile acids in the gut, causing depletion of hepatic cholesterol pools and increased production of LDL receptors.  Lower LDL ~20%
• Very safe, non-systemic, but cannot be used if triglycerides >250

• Platelet aggregation inhibitor
• ADP receptor blocking agent, used in patients resistant to clopidogrel
• Trade name: Brilinta