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Cardiovascular
Pharmacology
Dr. Hiwa K. Saaed
PhD Pharmacology & Toxicology
2015-16
Reference: Lippincott illustrated Reviews of Pharmacology 6th ed.
Hypertension
Hypertension (BP >140/90 mm Hg)
is defined as either a sustained SBP of > 140 mm Hg or a
sustained DBP of > 90 mm Hg.)
Optimal healthy blood pressure is (<120/<80).
I. NON-PHARMACOLOGICAL
– Quitting cigarette smoking,
– regular exercise,
– restricting dietary intake of: salt, saturated fats, and
calories
will improve peripheral circulation, prevent increases in blood
volume, reduce plasma cholesterol levels and total body
weight.
ANTIHYPERTENSIVE DRUGS
• Thiazide diuretics: (bendroflumethiazide)
• β-adrenoreceptor antagonists: (propranolol, atenolol,
metoprolol)
• Calcium channel antagonists: (nifedipine, amlodipine)
• Angiotensin converting enzyme (ACE) inhibitors: (captopril,
enalapril)
• Angiotensin II subtype I (AT1) receptor antagonists (losartan,
valsartan)
• Renin synthesis inhibitor: (Aliskiren)
• α1 adrenoreceptor antagonists: (prazosin, terazosin)
• Vasodilator drugs e.g. K+ channel activators: minoxidil
• Centrally-acting drugs e.g. α2 adrenoreceptor agonists:
(clonidine, methyldopa)
TREATMENT STRATEGIES
• For most patients, the blood pressure goal when treating
hypertension is a SBP<140 mm Hg and a DBP< 90 mm Hg.
• Mild hypertension can sometimes be controlled with
monotherapy, but most patients require more than one drug to
achieve blood pressure control.
• Current recommendations are:
– to initiate therapy with a thiazide diuretic, ACE inhibitor, angiotensin
receptor blocker (ARB), or calcium channel blocker (CCB).
– if blood pressure is inadequately controlled, a second drug should be
added.
A. Individualized care
Therapeutic uses
Calcium channel blockers have an intrinsic natriuretic effect and, therefore,
do not usually require the addition of a diuretic.
These agents are useful in the treatment of hypertensive patients who also
have asthma, diabetes, angina, and/or peripheral vascular disease.
Black hypertensives respond well to calcium channel blockers.
• Most of these agents have short half-lives (3-8 hours). Treatment is
required three times a day to maintain good control of hypertension.
Therapeutic Indications of CCBs
Adverse effects of CCBs
Dihydrpyridines:
Dizziness, headache, and a feeling of fatigue
caused by a decrease in blood pressure.
Peripheral edema is another commonly
reported side effect of this class.
Nifedipine and other dihydropyridines may
cause gingival hyperplasia.
Verapamil and diltiazem
Constipation and AV block, should be avoided
in patients with heart failure or with AV block.
Alpha(α )-Adrenoceptor-blocking Agents
A. Sodium nitroprusside
• is administered IV, is metabolized rapidly (half life of minutes) and
requires continuous infusion to maintain its hypotensive action.
• It is capable of reducing blood pressure in all patients regardless of
the cause of hypertension,
• acting equally on arterial and venous smooth muscle. It can reduce
cardiac preload.
• Adverse effects: hypotension caused by overdose. Nitroprusside
metabolism results in cyanide ion production.
• Although cyanide toxicity is rare, it can be effectively treated with an
infusion of sodium thiosulfate to produce thiocyanate, which is less
toxic and is eliminated by the kidneys.
[Note: Nitroprusside is poisonous if given orally because of its
hydrolysis to cyanide.]
HTN Emergency
B. Labetalol
• is both an (alpha- and a beta-blocker and is given as an IV bolus or
infusion.
• NO reflex tachycardia.
• The major limitation is a longer half-life, which precludes rapid titration.
• carries the contraindications of a nonselective beta- blocker.
C. Fenoldopam
• Fenoldopam is a peripheral dopamine-1 receptor agonist that is given as an
IV infusion.
• Unlike other parenteral antihypertensive agents, fenoldopam maintains or
increases renal perfusion while it lowers blood pressure, beneficial in
patients with renal insufficiency.
D. Nicardipine
• Nicardipine, a calcium channel blocker, can be given as an IV infusion.
• limitation is a long half-life
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