Hypertension Drugs Flashcards
First Line Drug agents for Hypertension?
• ACE-inhibitors, ARBs, calcium channel blockers,
thiazide diuretics
Second line Drug agents for hypertension?
• b-blockers, aldosterone antagonists
Other Agents used to treat for hypertension aside from first and second line?
• Loop diuretics, a-blockers, direct vasodilators,
central a2-agonists, renin inhibitors
List the Ace inhibitors and their MOA?
Captopril / Enalapril / Lisinopril
MOA: • BP by peripheral vascular resistance
• INHIBIT ACE (angiotensin converting enzyme) that
cleaves angiotensin I to form angiotensin II
• DECREASE Na+ & H20 retention
• INCREASE BRADYKININ levels
• DO NOT reflexively increase cardiac output, rate or
contractility
Clinical Application of Ace inhibitors?
• Hypertension (most effective in white and/or young
patients)
+ diuretic = effectiveness similar in non-black and black
patients
• Preserve renal function in patients with either diabetic
or non-diabetic nephropathy
• Effective in treatment of chronic HF
• Standard of care for patients following MI (started 24h
after end of infarction)
ACE inhibitors AE?
• Dry hacking cough • Hyperkalemia • Hypotension • Angioedema (rare but life-threatening) • Acute renal failure (patients with bilateral renal artery stenosis) • Rash, fever, altered taste
Ace inhibitor contraindications?
• Pregnancy
During 1st trimester due to risk of congenital
malformations and during 2nd and 3rd trimesters
because of risk of fetal hypotension, anuria & renal
failure
• Patients with bilateral renal artery stenosis
• Patients with a history of angioedema related to previous
treatment with an ACEI and in patients with hereditary or
idiopathic angioedema.
Name ARBS for htn and MOA?
ARBS: Losartan / Valsartan
MOA:
• Angiotension receptor blockers (ARB’s)
• First-line agents
• Alternatives to ACEI’s (in intolerant patients)
• Block angiotensin-2 type 1 receptors
• BP by causing arteriolar & venous dilation
• Block aldosterone secretion à decrease Na+ & H20
retention
• diabetic nephrotoxicity
• DO NOT INCREASE BRADYKININ levels
ARB AE?
• Similar to those of ACE inhibitors( Hyperkalemia
• Hypotension
• Acute renal failure (patients with bilateral renal artery
stenosis)
• Rash, fever, altered taste)
• Dry cough does not occur (due to no effect on
bradykinin levels)
• Angioedema risk is significantly lower than with
ACEI’s
• Losartan reduces plasma uric acid levels by inhibiting
URAT1 transporter – can be useful in patients with
gout
ARB contraindications?
- Pregnancy
* Patients with bilateral renal artery stenosis
Renin inhibitor name, MOA and AE?
Aliskiren
MOA: • Inhibits enzyme activity of renin and prevents
conversion of angiotensinogen into angiotensin I
End result:
• Inhibits production of both angiotensin II and
aldosterone
AE:• Similar to those of ACE inhibitors
• Dry cough does not occur (due to no effect on
bradykinin levels)
• Angioedema risk is significantly lower than with
ACEI’s
Name calcium channel blockers?
Ca2+ CHANNEL CLASSES • Non-dihydropyridines • Verapamil • Diltiazem • Dihydropyridines • Nifedipine, amlodipine
Verapamil selectivity and use?
• Least selective of any Ca2+-blocker
• Significant effects in cardiac & vascular smooth muscle
• Used to treat angina, supraventricular
tachyarrhythmias, hypertension, migraine & cerebral
vasospasm
Diltiazem selectivity and use?
• Effects in both cardiac & vascular smooth muscle (less
pronounced effect on heart than verapamil)
• Good side-effect profile
• Used to treat angina, hypertension, supraventricular
tachyarrhythmias & cerebral vasospasm
Dihydropyridines selectivity and use?
Amlodipine, nifedipine
• Greater affinity for vascular Ca2+-channels than for cardiac
Ca2+-channels
• Reduce Ca2+ entry into smooth muscles to cause
coronary & peripheral vasodilatation & lower BP
• Primarily used in treating hypertension.
Calcium channel blocker clinical applications?
• Hypertension (particularly black and/or elderly
patients)
• Have intrinsic natriuretic effect (no need for diuretic)
• Useful in patients with asthma, diabetes, peripheral
vascular disease
Calcium channel blockers can and can’t be used for what clinical use?
Hypertension, angina, and cardiac arrythmias(except Dihydropyridines(amlodipine, nifedipine), these can’t be used for arrythmias).
Calcium channel PK?
• High-doses of short-acting dihydropyridine Ca2+-
channel blockers can increase risk of MI (excessive
vasodilation & reflex cardiac stimulation)
• Sustained release preparations are preferred
AE of Calcium Channel blockers
• Verapamil
Constipation (~7%), negative inotropic effects, gingival
hyperplasia
• Dihydropyridines
Hypotension, peripheral edema (esp. feet & ankles),
dizziness, headache, fatigue, gingival hyperplasia,
flushing, reflex tachycardia can occur (especially in
short-acting preparations)
• Non-dihydropyridines (verapamil & diltiazem)
Relatively contraindicated in patients taking b-blockers,
or who have 2nd or 3rd degree AV block, or severe left
ventricular systolic dysfunction
Thiazides MOA and Clinical applications with regard to hypertension?
• First-line agents (particularly black and/or elderly
patients)
MOA
• Lower BP by Na+ and H20 excretion à in extracellular
volume à in cardiac output & renal blood flow.
• Long-term treatment = normal plasma volume but
sustained decreased peripheral resistance
Thiazides
• Counteract Na+ & H20 retention caused by other
antihypertensive drugs
• Particularly useful in black & elderly (with normal renal
& cardiac function)
Thiazide AE?
- Hypokalemia
- Hyperuricemia
- Hyperglycemia
- Hypomagnesemia
- Hypercholesterolemia
- Sexual dysfunction
Loop diuretic role in Hypertension. Potassium sparing diertics role in hypertension?
Loop: • Act promptly in patients with poor renal function or heart failure
• More potent at inducing diuresis & can cause more side effects
• Used primarily in patients who do not respond to
thiazide therapy adequately
• Cause renal vascular resistance & renal blood flow
Potassium sparing:
• K+ loss in urine caused by thiazide or loop diuretics
• Used in combination with other diuretics
