Exam 2 but simplified Flashcards
Statins: Class, indications (1), MOA, AE (3), PK (3)
Class: HMG-CoA Reductase Inhibitors
Indications: High cholesterol blood lvl
MOA: Inhibits HMG CoA reductase → inc. LDL receptor proliferation → inc. LDL uptake into cell
AE: All rare, generally well tollerated
- Myopathy (rhabdomyolysis)
- Hepatotoxicity
- Renal injury
PK
- PO at night
- No grapefruit!
- Rosuvastatin is not well metabolized in Asian heritage
Colesevelam // Colestipol // Cholestyramine: Class, indications, MOA, AE
Class: Bile acid sequestrants
Indications: High cholesterol blood lvl
MOA: Nonabsorbable from GI tract → binds to bile acid → dec. reabsorption and inc. excretion of cholesterol
- Ultimately inc.s LDL receptors in the liver
AE: GI disturbance (constipation)
Ezetimibe: Indications, MOA, AE (4), PK
Indications: High cholesterol blood lvl
MOA: Act on brush border enzyme → prevents dietary cholesterol absorption and inhibits reabsorption of cholesterol secreted in the bile
AE:
- Myopathy (rhabdomyolysis)
- Hepatitis
- Pancreatitis
- Thrombocytopenia
PK: Converted to active metabolite ezetimibe glucuronide
Gemfibrozil // Fenofibrate: Class, indications, MOA, AE (4)
Class: Fibric acid derivatives (fibrates)
Indications: To lower VLDL levels
MOA: Inhibits hepatic extraction of free fatty acids → liver cannot synthesize as many triglycerides → dec. VLDL
AE: GI disturbances are most common
- Gallstones
- Myopathy
- Hepatotoxicity
Monoclonal antibody (PCSK9) inhibitor: Indications, MOA, AE (2), PK (2)
Indications: High cholesterol blood lvl
MOA: PCSK9 is a protein that binds LDL receptors in the liver
- Inhibition of PCSK9 = freed receptors = inc. LDL uptake
AE:
- Hypersensitivity
- Immunogenicity
PK: SubQ only
- Used with statins
ACL inhibitor: Indications, MOA, AE (2), PK
Indications: High cholesterol blood lvl
MOA: Inhibit ACL → dec. cholesterol synthesis → inc. LDL receptor proliferation → inc. LDL cell uptake
AE:
- Increase uric acid (gout risk)
- Increase tendon rupture risk
PK: Converted to active metabolite
Angiotensin-converting enzyme (ACE) inhibitors (-pril): Indications, MOA (5ish), AE (8), PK (3), Cont (2)
Indications: HTN
MOA: Inhibits ACE = Inhibition of ANG2 formation
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN (first dose especially)
- HyperK
- Dehydration
- Cough
- Fetal injury
- Renal failure
- Rare: Angioedema, neutropenia
PK: PO (except enalapril, which is IV)
- All prodrugs (except lisinopril) that are converted in small intestine
- Long 1/2 life
Contraindications:
- Drugs that exacerbate hypotension or K+ levels
- Pregnancy
Angiotensin II receptor blockers (ARBs) (-artan): Indications, MOA, AE (6), PK
Indications: HTN
MOA: Blocks the effects of ANG2 at the receptor
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN
- HyperK (low)
- Dehydration
- Cough (low)
- Fetal injury
- Renal failure
PK: All PO
Aliskiren: Class, indications, MOA (5ish), AE (6)
Class: Direct renin inhibitor
Indications: HTN
MOA: Inhibit release of renin = block entire RAAS
- Inc. vasodilation
- Inc. diuresis, excrete out more Na
- Dec. SNS response = dec. myocardial O2 supply
- Prevention of CV remodeling
AE:
- HypoTN
- HyperK
- Dehydration
- Cough, angioedema
- Fetal injury
- Diarrhea
Nifedipine: Class, indications (2), MOA (3), AE (5), Cont
Class: Ca channel blockers
- Dihydropyridines
Indications:
- Prinzmetal angina
- HTN
MOA: Blocks Ca2+ vascular smooth muscle
- Vasodilation of coronary arteries
- Dec. afterload
- Inc. contractility
AE:
- Peripheral edema
- Flushing
- Dizziness
- Headache
- Inc. myocardial O2 demand
Cont: No beta blockers
Verapamil // Dilitiazem: Class, indications (4), MOA, AE (6), cont (3)
Class: Ca channel blockers
- Non-dihydropyridines
Indications:
- HTN
- Angina
- Dysrhythmias
- SVT
MOA: Blocks Ca2+ @ vascular smooth muscle and the heart
- Dec. HR, contractility, AV node conduction
- Artery vasodilation → decrease afterload, coronary artery vasoconstriction
AE:
- Constipation
- Flushing, dizziness, headache
- Edema
- Bradycardia
- Heart block
- Hypotension
Contraindications:
- BB and Digoxin
- HF
Hydralazine: Class, indications, MOA, AE (5)
Class: Vasodilator
Indications: HTN
Actions: Dec. afterload
MOA: Unknown
- Direct arteriole vasodilation
AE:
- Fluid retention with long-term use
- Headache
- Dizziness
- Hypotension
- Reflex tachycardia
Sodium nitroprusside: Class, indications, MOA, AE, PK
Class: Vasodilator
Actions: Dec. preload
Indications:
- Prinzmetal angina
- HTN
MOA: Vasodilate veins via NO
AE: Tolerance can develop rapidly
PK: PO has insane first pass effect
Nitroglycerin: Class, indications, MOA, AE, Cont (4)
Class: Organic nitrates
Indications: HTN
- Angina
MOA: Converted to NO = NO activated guan = guan catalyzes cGMP = cGMP inhibits light chain = relax, vasodilation
AE: Tolerance
Contraindications:
Other hypotensive drugs + nitrates (ex: PDE5 inhibitors)
BB, CBB, diuretics
Digoxin: Class, indications, MOA, AE (5), Cont (4)
Class: Cardiac glycoside
Indications: HTN
MOA: Selectively inhibits Na/K/ATPase pump
- Build up of Ca2+ intracellularly = inc. actin/myosin interactions
AE: Heart dysrhythmia
GI: Anorexia + N/V (she’s so mean she causes bulimia)
CNS: Fatigue + visual disturbances
Contraindications:
Heart block
Bradycardia
Renal impairment
Electrolyte disturbances
Furosemide: Class, indications, MOA, AE (5), Cont (2)
Class: Loop Diuretics
Indications: HTN
MOA: Blocks Na/Cl/K cotransporter in ascending LoH → excrete Na+/K+/2Cl- in urine followed by water
AE:
- HypoK
- HypoNa+
- HypoCl-
- Ototoxicity
- Dehydration/hypotension
Contraindications:
Other ototoxic drugs (aminoglycoside antibiotics)
Digoxin
Hydrochlorothiazide (HCTZ): Class, indications, MOA, AE (6)
Class: Thiazide Diuretics
MOA: Block Na/Cl/K reabsorb @early distal convoluted tubule → these are excreted in urine followed by water
AE:
- HypoK
- HypoNa+
- HypoCl-
- Dehydration/hypotension
- Increase uric acid lvl (gout risk)
- Ineffective in kidney disease
Spironolactone: Class, indications, MOA, AE (3)
Class: K+ Sparing Diuretics
MOA: Blocks aldosterone
- Decrease prod of Na/K exchange protein transporter
- K+ retention, Na+/H2O excretion @late distal convol tubule
- Dec. remodeling of CV system
AE:
- HyperK
- Endocrine: Menstrual irregularities, gynecomastia
Mannitol: Class, indications, MOA, AE (2)
Class: Osmotic Diuretics
MOA: Freely filtered in GFR, stays in filtrate → draw water out to be excreted in urine
AE: Fluid overload/edema
- HF
Heparin // LMWH: Class, indications (5), MOA, AE
Class: Antithrombin activator
Indications:
- DVT/PE
- Open heart surgery
- Dialysis
- Disseminated intravascular coagulation (DIC)
- Acute MI
MOA: Activate antithrombin → inhibit coagulation factors to prevent
AE: Hemorrhage/bleeding
Warfarin: Class, indications (3), MOA, AE, PK (3)
Class: Vitamin K inhibitor
Indications:
- DVT/PE
- Thromboembolism in prosthetic heart valves
- MI/stroke risk
MOA: Inhibits enzyme that activates vitamin K → prevents synthesis of factors 2, 7, 9, 10 → dec. fibrin formation
AE: Hemorrhage/bleeding
PK:
- 99% protein bound
- Free drug crosses membranes (placenta, breastmilk)
- CYP450 hepatic metabolism
Dabigatran // Bivalirudin // Desirudin // Argatroban: Class, indications (2), MOA, AE (2), PK (2)
Class: Direct thrombin inhibitors
Indications: Prevent thrombosis
- DVT/PE
MOA: Inhibit thrombin → dec. conversion of fibrinogen to fibrin and activation of factor XIII → prevents fibrin mesh formation
AE: GI upset
- Hemorrhage/bleeding
PK:
- Food affects absorption rate
- Low protein binding
Rivaroxaban: Class, indications (3) , MOA, AE, cont
Class: Direct factor Xa inhibitors
Indications:
- DVT/PE
- Prevent thrombosis
- CVA
MOA: Inhibit factor 10a → prevent fibrin mesh formation
AE: Hemorrhage/bleeding
Cont: Pregnancy
Asprin: Class, indications (5), MOA, AE, PK
Class: COX inhibitor (irreversible)
Indications:
- Acute MI
- CVA
- TIA
- Chronic stable angina
- Stents
MOA: Inhibit COX → dec. platelet activation/aggregation, dec. TXA2 mediated vasoconstriction → inhibit platelet plug
AE: Hemorrhage/bleeding
PK: Effects last the lifetime of platelet