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504 pharm > Exam 3 > Flashcards

Exam 3 Flashcards

1
Q

K+ channel openers

A

Minoxidil, hydralazine, diazoxide

Main uses: HTN uncontrolled by other drugs, HTN emergencies, severe HTN, research

Main problems: strong inducers of the reflexes to vasodilation, can reveal myocardial ischemia

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2
Q

Calcium channel blockers

A

Several drugs approved in the U.S., all selectively inhibit L-type Ca2+ channels, these channels are present in both vascular and cardiac muscle cells, dihydropyridines are more vascular selective than other CCB’s

Uses: mild to moderate HTN, to reduce TPR, cardiac ischemia

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3
Q

Nifedipine

A

Calcium channel blocker/anti hypertensive drug
Dihydropyridines (“…dipines”)
Highly smooth muscle selective vs cardiac; evokes reflex tachycardia (because don’t bind to heart much at all)

2.5 fold increased risk of sudden death with short acting dihydropyridines. Do not use this specific class in HTN patients with ischemic heart disease

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4
Q

Diltiazem

A

Calcium channel blocker/anti hypertensive drug
Benzothiazepine
Slightly smooth muscle selective vs cardiac
Cause little to no reflex tachycardia because they block it by binding to cardiac L-type channels

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5
Q

Verapamil

A

Calcium channel blocker/anti hypertensive drug
Phenylalkylazmine
Non-selective for smooth vs cardiac
Cause little to no reflex tachycardia because they block it by binding to cardiac L-type channels

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6
Q

Sodium nitroprusside

A

Inorganic nitrate/anti hypertensive drug
Nitric oxide donor
Uses: Hypertensive emergencies, reduce bleeding during surgery (bc lower BP), cardiac ischemia (reduces pre-load and after-load and thus cardiac work)

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7
Q

Nitroglycerin

A

Organic nitrate/anti hypertensive drug
Nitric oxide donor
Uses: angina (reduces cardiac work)

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8
Q

Methyldopa (Aldomet)

A

Sympatholytic anti hypertensive drug
Centrally acting, direct alpha2-adrenergic receptor selective agonist
Inhibits sympathetic outflow from the brainstem

Uses: for HTN resistant to other treatments, decrease TPR and reduce CO

Bad side effects: nausea, withdrawal syndrome, sedation

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9
Q

Clonidine (Catapres)

A

Sympatholytic anti hypertensive drug
Centrally acting, alpha2-adrenergic receptor selective agonist (it is a prodrug)
Inhibits sympathetic outflow from the brainstem

Uses: for HTN resistant to other treatments, decrease TPR and reduce CO

Bad side effects: nausea, withdrawal syndrome, sedation

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10
Q

Trimethaphan (Arfonad)

A

Anti hypertensive drug
Peripherally acting sympatholytic ganglionic blocker
Non-depolarizing inhibitor of ganglionic nicotinic cholinergic receptor

Uses: controlled hypotension (dissecting aneurysm and reduce surgical bleeding), dampen spinal autonomic reflexes (spinal cord injury)

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11
Q

Prazosin (Minipress)

A

Alpha-1 adrenergic antagonist
Blocks the vasoconstrictor of sympathetic tone
Reduces TPR
Causes vasodilation commensurate with degree sympathetic activity is involved in vasoconstriction

Use: symptomatic prostate hypertrophy

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12
Q

Propranolol (Inderal)

A

Non-selective beta adrenergic receptor antagonist. Anti hypertensive drug
Mechanism: inhibit inotropic and chronotropic effects of asanas in the heart. Reduces cardiac output
Uses: gold standard for anti-HTN
Side effects: exercise intolerance, impotence

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13
Q

Metoprolol (Lopressor)

A

Selective Beta-1 adrenergic receptor antagonist. Anti hypertensive drug
Mechanism: inhibit inotropic and chronotropic effects of asanas in the heart. Reduces cardiac output
Uses: better for asthmatics than non selective
Side effects: exercise intolerance, impotence

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14
Q

Aliskrien (Tekturna)

A

Renin inhibitor. Anti hypertensive drug

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15
Q

Lisinopril (Prinivil)

A

ACE inhibitor. Anti hypertensive drug

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16
Q

Losartan (Cozaar)

A

AT1-Receptor antagonist. Anti hypertensive drug

17
Q

Minoxidil

A

Vasodilator drug/anti hypertension
K+ channel openers
Open K channel leads to K efflux, cell hyperpolarization; which inhibits voltage sensitive L-type Ca2+ channels, which reduces Ca2+ and causes relaxation

IOW, indirect inhibition of L-type Ca2+ channels

18
Q

Diuretics

A

Diuretics in HTN

Thiazide: ‘gold standard’ proven in mild HTN, reduces TPR

K+ sparing: use as adjuvants

Loop: only in refractory HTN, “big guns”

19
Q

Glyceryl trinitrate (GTN, Nitroglycerin)

A

Nitrovasodilator. Anti-anginal drug

Sublingual administration avoids the first-pass effect and produces rapid (3-5 min) onset and short duration (2-30 min). transdermal administration prolongs onset and duration of action

Mechanism: nitric oxide donor. Reduces venous return, reduction in preload reduces ventricular wall stress and myocardial oxygen demand

Adverse effects: orthostatic hypotension, reflex tachycardia, severe throbbing headache, dizziness. Cross potentiation with PDE-5 inhibitors (viagra)

20
Q

Calcium channel blockers

A

Anti-anginal drugs
Verapamil, Diltiazem, nifedipine

Block L-type “slow” calcium channels
Reduce influx of extra cellular Ca into vascular and cardiac muscle
Preferential arteriolar vasodilators vs veins
Drugs have differing selectivity for Ca channels in vascular vs cardiac tissue

21
Q

Ranolazine

A

Anti anginal drug

It inhibits the late inward sodium current in heart muscle which leads to reduction in intracellular calcium

Uses: anti-anginal effects independent of reductions in BP and/or HR. Useful as adjunct or alternative anti-anginal therapy. For chronic angina, not useful for Acute Coronary Syndrome

Adverse effects: prolongs QTc. CYP3A4 substrate

22
Q

Epinephrine, Dobutamine

A

Positive inotropic agents for acute, severe heart failure
Beta adrenergic receptor agonists: induce cAMP
Administered IV, active beta-adrenergic receptors

23
Q

Milrinone (cardiac PDE-3)

A

Positive inotropic agents for acute, severe heart failure
Phosphodiesterase inhibitors: protect cAMP
Administered IV, short term inotropic support

24
Q

Atorvastatin (Lipitor), Rosuvastatin (Crestor)

A

Treatment of hyperlipidemia
Inhibitor is cholesterol synthesis
“Statins”
HMG-CoA reductase inhibitor - reversibly competitive
First line agents in most patients with increased LDL
Movement of SCAP/SREBP complex to golgi is stimulated

25
Q

Alirocumab (Pralient), Evolucumab (Repatha)

A 
Treatment of hyperlipidemia
Inhibitor of LDL-R degradation; increased amount of LDL-R available for LDL uptake (new class, just approved)
PCSK9 inhibitor (proprotein convertase substilin kexin)
Indicated for patients who have had a stroke or heart attack. Given in combo with maximally tolerated dose of statin
26
Q

Cholestyramime

A

Treatment of hyperlipidemia
Inhibitor of bile acid absorption
Leads to a decrease of LDL in plasma
Side effect: decrease drug and fat soluble vitamin absorption

27
Q

Ezetimibe (Zetia)

A

Treatment of hyperlipidemia
Inhibitor of cholesterol absorption
Often combined with a statin to stop the compensatory increase in cholesterol production in the liver
20% decrease in serum LDL

28
Q

Niacin (Vitamin B3, nicotinic acid)

A 
Treatment of hyperlipidemia
Inhibitor of triglyceride synthesis
Lowers VLDL 45%, LDL 20%
Increases HDL 30%
Side effects: intense flushing, hyperuricemia, impaired insulin sensitivity
29
Q

Fenofibrate

A

Treatment of hyperlipidemia
Fibrate derivative
Binds to PPAR-alpha (a nuclear receptor) to cause activation and repression of genes
Decrease TG 50%, decrease LDL 15%, increase HDL 20%
Side effect: GI discomfort

30
Q

Omacor

A

Treatment of hyperlipidemia
Omega-3 polyunsaturated fatty acid (found in oily fish)
Inhibits triglyceride synthesis, stimulates fatty acid oxidation, reduces VLDL production/secretion

31
Q

Warfarin (Coumadin)

A

Anticoagulant
Warfarin completely inhibits vitamin K epoxide reductase, which decreases the reduces form of vitamin K and slows down maturation of coagulation factors
Oral administration, only active in vivo

504 pharm (2 decks)

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