Pharm --Lipid/HTN/CAD Flashcards
This class of antiHLD drugs is:
- -Large in size
- -Highly positively charged
- -Not absorbed, excreted in stool
- -
Bile acid sequestrants
- -positive charge lets it bind to negatively charged bile acids
- -
What are the effects of the following drug classes on HDL, LDL, and TG:
- -Niacin
- -Fibrates
- -Bile acid sequestrants
- -Statins
- -Ezetimibe
- -Niacin = lower TG, increase HDL, lower LDL
- -Fibrates = lower TG, increase HDL, variable LDL
- -Bile sequestrants = increase TG, increase HDL, lower LDL
- -Statins = lower TG, increase HDL, lower LDL
- -Ezetimibe = lower TG, increase HDL, lower LDL
Which 2 statins are lactone prodrugs that must be modified in the liver to the active hydroxy acid forms?
- -Lovastatin
- -Simvastatin
This class of antiHLDs prevent endocytosis and lysosomal degradation of LDL receptors on hepatocytes leading to higher number of LDL receptors
PCSK9 Inhibitors = more receptors –> lower LDL-C
–Alirocuma, evolucumab = human monoclonal Ab
This drug class inhibits cholesterol absorption by enterocytes in small intestines, but doesn’t affect TG absorption.
Ezetimibe
This drug class affects blood cholesterol by inhibiting cholesterogenesis in the liver
Statins –HMG-CoA reductase inhibitors
Which 2 statins have longer half-lives that can be administered once a day?
- -Atorvastatin (Lipitor)
- -Rosuvastatin (Crestor)
This drug class reduces TG synthesis in the liver, decreases lipolysis in adipose tissue, and reduces hepatic clearance of HDL-apoA-1
Nicotinic Acid (Niacin)
This drug class acts through PPARa to stimulate lipoprotein lipase(LPL) synthesis and inhibit apoC III expression. It also stimulates apoA-1 and apoA-5 expression.
Fibrates
- -LPL synthesis –> clear TG rich lipoproteins
- -apoCIII –> clear VLDL
- -apoA-1 and apoA-5 –> increase HDL
What is the best agent for increasing HDL-C?
Nicotinic Acid (Niacin)
This antiHLD drug class increases lithogenicity of bile –> risk of gallstones
Fibrates
Severe hypertriglyceridemia is a contraindication for the use of this antiHLD drug class.
Bile acid sequestrants
This antiHLD drug class binds cardiac glycosides (digoxin) and coumarin anticoagulants and interefere with their absorption.
Bile acid sequestrants
These 2 antiHLD drug classes increase hepatic LDL receptor expression
- -Statins
- -Bile acid sequestrants
This antiHLD drug class is contraindicated for pregnant or nursing women
Statins
What are the 4 major risk factors for Polygenic-environmental hyperlipidemia?
- -serum LDL cholesterol
- -age
- -HTN
- -smoking
How does myocardial ischemia affect [increase/decrease]:
- -intracellular ATP
- -Intracellular pH
- -Extracellular pH
- -Extracellular K, phosphate, fatty-acid levels
- -intracellular ATP = decrease
- -Intracellular pH = decrease (acidosis)
- -Extracellular pH = decrease (acidosis)
- -Extracellular K, phosphate, fatty-acid levels = all increase
What 3 drugs can be used in a pharmacologic stress test?
- -Dobutamine = Beta-1 stimulation sympathomimetic –> increase contractility and heart rate
- -Adenosine, dipyridamole = coronary vasodilators –> stenotic arteries don’t respond to vasodilation stimulus
Patients w/ stable angina taking his drug was associated w/ 33% reduction in risk of adverse cardiovascular events
Patients w/ unstable angina or acute MI taking this drug had reduced vascular mortality, nonfatal reinfarction, and nonfatal stroke
ASPIRIN!
This drug is a thienopyridine derivative that inhibits platelet aggregation induced by adenosine diphosphate. It also reduces blood viscosity.
Ticlopidine
What are the 3 thienopyridine class
- -Ticlopidine
- -Clopidogrel
- -Prasugrel
This drug irreversibly binds to P2Y12 receptor (GPCR for ADP).
Prasugrel – Thienopyridine class
This antiplatelet drug used in patients w/ stable angina can induce neutropenia, and in rare cases, TTP
Ticlopidine
This drug is limited to patients less than 75years old, greater than 60kg, and with no history of stroke or TIA
Prasugrel
This antiplatelet drug is a quinolone derivative that inhibits cellular phosphodiesterase which increases cAMP to inhibit platelet aggregation and vasodilation
Cilostazol
What is/causes the Bezold-Jarisch reflesx?
Nitrates – stimulation of cardiac sensory receptors –> vagal efferent discharge –> bradycardia
In the setting of unstable angina/non-ST elevated MI, what anticoagulant therapy should be initiated?
Heparin
Classification of HTN:
- -Stage 1
- -Stage 2
- -Stage 1 = 140-159 systolic, 90-99 diastolic
- -Stage 2 = systolic over 160 OR diastolic over 100
Risk of end organ disease from HTN increased in these 2 populations:
- -African American
- -Premenopausal women
Angiotensin blockers [increase/decrease] TPR:
–Decrease – inhibit production/action of Angiotensin II –> less vasoconstriction –> lower TPR
In a patient w/ severe HTN, in the setting of CHF or cirrhosis, and with renal insufficiency (GRF less than 30-40), what diuretic class is used?
Loop diuretics
Diuretics [increase/decrease] cardiac output
–Decrease – Diuresis –> volume depletion –> low preload –> low CO –> low BP
–CO returns to normal over time
Angiotensin Receptor Blockers (ARBs) are [competitive/non-competitive] antagonists at the vascular endothelium
Competititve
2 Mechanisms of ACE Inhibitors
- -Block endothelial ACE (converts Angiotensin I –> Angiotensin II)
- -Inhibit breakdown of bradykinin (vasodilator)
Bradykinin is a potent vaso (dilator/constrictor)
Vasodilator
What do you use when you want a short acting ACEI
Captopril
What ACEI is a prodrug that has a more active metabolite?
Enalapril –> enalaprilat (more active)
What are the ARBs?
- -Losartan
- -Valsartan
- -Irbesartan
What causes cough side effect of ACEI?
–Bradykinin
Ca Channel blockers:
- -2 Dihydropyridines:
- -2 Non-dihydropyridines:
- -2 Dihydropyridines: amlodipine, nifedipine
- -2 Non-dihydropyridines: verapamil, diltiazem
Ca Channel blockers (dihydropyridines vs non-dihydropiridines):
- -Which raises heart rate?
- -Which can cause Raynauds sydrome?
- -Which decreases oxygen demand?
- -Which raises heart rate? = Dihydropyridine–> reflex tachy
- -Which can cause Raynauds sydrome? = both
- -Which decreases oxygen demand? = non-dihyropyridines
What HTN drug has the following characteristics:
- primary antiHTN mechanism = reduce CO
- -can mask symptoms of hypoglycemia in diabetics
- -can cause depression
- -worsens symptoms of peripheral vascular disease
Propranolol – non-selective B blocker
Unique B blockers (Labetolol, Carvedilol, Esmolol):
- -Used in hypertensive urgency
- -Used for ACS or CHF
- -Used IV for AV nodal blocking b/c it’s unique short T1/2
- -HTN emergency = labetolol
- -ACS, CHF = Carvedilol
- -IV, short half life = Esmolol
This drug relaxes smooth muscle of peripheral arterioles. Is used for refractory HTN and hair loss.
Minoxidil
This drug relaxes smooth muscle of peripheral arterioles. Is used IV for acute HTN urgency or chronic CHF
Hydralazine
Sympathoplegic drugs stimluate a2 to reduce vasomotor tone
- -Which is routinely?
- -Which is used in pregnancy?
- -The other one?
Routinely = Clonidine
Pregnancy = a-methyl dopa
Other one = Guanabenz
2 Ganglion blockers used for HTN?
–Guanethidine = block NE release
–Reserpine = depletes NE –> decreases CO and TPR
Antiplatelets: which are reversible and irreversible
- -Aspirin
- -Ticlopidine
- -Clopidogrel
- -Prasugrel
- -Ticagrelor
- -Aspirin = irreversible COX inhibitor
- -Ticlopidine = reversible ADP receptor inhibitor
- -Clopidogrel = irreversible ADP receptor inhibitor
- -Prasugrel = irreversible ADP (P2Y12) receptor inhibitor
- -Ticagrelor = allosteric ADP receptor blockade
In the kidney, Angiotensin causes more constriction in the [afferent/efferent] arterioles of the glomerulus
–Efferent – more blood in glomerulus –> increased glomerular pressure
Bradykinin is associated with what 2 clinical symptoms?
- -Cough
- -Angioedema (swelling of skin around mouth, mucosa of mouth, tongue)
2 Mechanisms of nitrates relieving angina:
- -Dilate coronary arteries –> increases oxygen delivery
- -Venous dilation –> reduce ventricular preload –> reduce myocardial oxygen demand
If you use phosphodiesterase inhibitors for erectile dysfunction, what antianginal drug can’t you give?
Nitrates = PDE inhibitors inhibit cGMP –> “may cause an unsafe drop in blood pressure ;)”
