Antihypertension Pharm (B4)

Front 1

aliskiren (a lis kye' ren)

Back 1

• Only currently marketed renin inhibitor
• Directly blocks renin’s enzymatic activity
• ↓ Plasma renin activity → ↓ ATI & ↓ ATII
• → ↑ plasma renin concentration
• Administration: Oral
• Adverse Effects:
o Diarrhea
o Cough
o Angioedema
o ↑ K
o Pregnancy Contraindication

Front 2

captopril (kap' toe pril)

Back 2

• ACE inhibitor
• ↓ ATII formed → ↓vasoconstriction & ↓aldosterone release → BP
• Inhibit breakdown of bradykinin (ACE catalyzes this reaction)
• Oral
• Important binding group = sulfhydryl
• Elimination: Kidney

Front 3

diazoxide (dye az ox' ide)

Back 3

• arterial vasodilator, muscle relaxation
• Mechanism – K+ channel opening
• Administration: i.v. (parenteral); Duration 4-12 hours
• Hemodynamics: ↓ PVR → ↓ BP → ↑ SNS reflexive action
• Adverse Effects:
o Excessive lowering in BP (last up to 12 hours)
o Reflexive SNS activity (angina, complicates MI or CHF)
o Fluid retention
o Hyperglycemia

Front 4

enalapril (e nal' a pril)

Back 4

• ACE inhibitor
• ↓ ATII formed → ↓vasoconstriction & ↓aldosterone release → BP
• Inhibit breakdown of bradykinin (ACE catalyzes this reaction)
• Oral or i.v.
• Prodrug – converted to enalaprilat (active metabolite; now a separate drug)
• Important binding group = carboxylic acid (not on prodrug)
• Elimination: Kidney

Front 5

fenoldopam

Back 5

• arterial vasodilator
• Parenteral drug for hypertensive emergencies
• Mechanism – stimulates dopamine receptors (D1) in blood vessels → vasodilation.
• Administration – constant i.v. infusion (rapid metabolism)
• Adverse Effects:
o Headache
o Flushing
o ↑ HR
o ↑ intraocular pressure (glaucoma contraindicated)

Front 6

Atenolol

Back 6

• B1 >>>>B2
• Beta Blocker
• Treatment of angina & HTN

Front 7

Carvedilol

Back 7

• B > a1
• Anti-HTN, also used to treat patient with CHF
• Adverse Effects:
o A1 and B-Blocker effects

Front 8

Clonidine

Back 8

• CNS acting anti-HTN drug (a2)
• Decreases sympathetic outflow
• interacts w/ imidazoline receptors - may contribute to decrease BP.
• action on peripheral alpha-receptors (initial increase in BP if given IV)
• Administration: oral, transdermal
• Adverse effects:
o CNS - sedation, depression
o dry mouth
o orthostatic hypotension
o abrupt withdrawal problems

Front 9

guanethidine

Back 9

• ↓ release of neurotransmitter at sympathetic nerve terminal
• Adverse Effects:
o Orthostatic hypotension
o interacts with tricyclic antidepressants → blocks effect

Front 10

hydralazine

Back 10

• Relaxation of arteriolar smooth muscle (NO mediated)
• Compensatory response (↑ sympathetics; salt/water retention)
• Administration: Oral, parental
• Eliminated: acetylation
• Often given w/ beta blocker + diuretic (adverse effects 1 & 2)
• Adverse effect
o Palpitation, angina (sympathetic reflex)
o Fluid retention (offsets BP ↓ effect)
o Headache (common in vasodilators)
o Drug-induced lupus (rash, joint ache, +ANA Ab – spares kidneys)
• Slow acetylators at ↑ risk of this

Front 11

labetalol

Back 11

• B > a1
• Adverse Effects:
o A1 and B-Blocker effects
o Possible hepatotoxicity

Front 12

lisinopril

Back 12

• ACE inhibitor
• ↓ ATII formed → ↓vasoconstriction & ↓aldosterone release → BP
• Inhibit breakdown of bradykinin (ACE catalyzes this reaction)
• Oral
• Important binding group = sulfhydryl
• Elimination: Kidney

Front 13

Losartan

Back 13

• ATII Receptor Blocker
• ATII receptor blocker (block type I receptors)- (blood vessel, adrenal gland):
o → ↓ blood vessel constriction
o →↓ aldosterone release
o Do NOT inhibit breakdown of bradykinin
o Effects of receptor blockade:
• ↑ plasma renin activity
• lower BP → ↑ renin release
• blocks ability of ATII to feedback inhibit renin release
• ↑ plasma ATII levels
• Oral

Front 14

methyldopa

Back 14

• CNS acting anti-HTN drug (a2)
• Prodrug
• Administration: Oral, iv (no initial increase in BP)
• Adverse Effects:
o CNS- sedation, depression
o dry mouth
o orthostatic hypotension
o hepatotoxicity (^ liver labs)
o +Coomb's (hemolytic anemia)

Front 15

metoprolol

Back 15

• B1>>>B2
• Beta Blocker

Front 16

minoxidil

Back 16

• Prodrug
• Mechanism – opens K+ channels in vascular SM → relaxation
(Stabilizes membrane at RMP)
• Often given with Beta-blocker & loop diuretic
• Administration: oral
• Adverse Effects:
o Reflex ↑ SNS activity & fluid retention (=hydralazine)
o Palpitation, angina
o Headache
o Hypertrichosis - ↑ hair growth
o Pericardial effusion (serious)
o ECG changes

Front 17

Reserpine

Back 17

• antihypertensive acting at sympathetic nerve terminal → decrease NT release
• Adverse Effects:
o sedation
o depression (suicidal)

Front 18

Prazosin

Back 18

• Selective a1 receptor blocker (anti-HTN and BPH therapy)
• Administration: Oral
• Extensive metabolism
• Adverse Effects:
1st dose phenomenon (severe orthostatic hypotension)
headache

Front 19

Ramipril

Back 19

• ACE inhibitor
• ↓ ATII formed → ↓vasoconstriction & ↓aldosterone release → BP
• Inhibit breakdown of bradykinin (ACE catalyzes this reaction)
• Prodrug
• Oral
• Important binding group = sulfhydryl
• Elimination: Kidney

Front 20

Na Nirtoprusside

Back 20

• Arteriolar & venous SM relaxation
• Mechanism: activation of guanylyl cyclase → ↑ cGMP → relaxation
o Either via NO or by stimulating enzyme directly
• Administration: continuous iv infusion (rapid onset & offset of action), tirtate dose, close monitoring, protect from light (photosensitive).
• Used for hypertensive emergencies
• Elimination: → CN & SCN → urine
• Adverse Effects:
o Hypotension
o Cyanide toxicity – binds cytochrome
o thiocyanate toxicity

Front 21

Propanolol

Back 21

• Nonselective Beta-blocker B1 = B2
• Mechanism:
o ↓ HR & Contractility →↓ CO
o ↓ renal renin release (B1)
• Elimination – liver (some 1st pass effect)

Front 22

ACE inhibitor Adverse Effects:

Back 22

• Hypotension
• Cough (dry, nonproductive cough, very annoying; ↑ bradykinin)
• Angioedema (swollen lips/tongue)
• ↑ K (via ↓ aldosterone →↑K) (worse with renal insufficiency)
• ↓ Renal Function (especially is bilateral RAS)
• Fetal toxicity (birth defects)
• Rash
• ↓ Taste
• Other

Front 23

Angiotensin II Receptor Blockers Adverse Effects:

Back 23

• Hypotension
• Cough (less than ACEI)
• Angioedema (less than with ACEI)
• ↑ K (via ↓ aldosterone →↑K) (worse with renal insufficiency)
• ↓ Renal Function in bilateral RAS (BUN ↑+ creatinine ↑)
• Fetal toxicity (birth defects)
• FDA drug safety communications (↑ risk in diabetics?; ↑ risk of cancer?)