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International generic name
Captopril
Drug form and composition
Tablets. One tablet contains 25 mg Captopril.
Indications
Mild, moderate and severe essential hypertension; renovascular hypertension (as
a monotherapy or in combination with diuretics); chronic congestive heart failure.
Dosage and administration
Usual dose in arterial hypertension is 12.5 - 25 mg, 2-3 times daily. If reduction
of the blood pressure is insufficient the dose may be enhanced up to 50 mg, 2-3
times daily. In renovascular and renal hypertension the dosage is 12.5 mg, 3 times
daily. In cases with renal failure daily dose depends on the creatine clearance,
and dosage intervals should be longer. In heart failure the initial dose is 6.25
or 12.5 mg, 3 times daily, which may be enhanced gradually if necessary. The initial
dose of Captopril should be consistent with used diuretics. In children Captopril
should be used with particular attention and after precise assessment. The advisable
dosage is 1-2 mg per kg body weight. Tablets should be taken 1 hour before meal.
Contraindications
Hypersensitivity to Captopril; in patients with neutropenia and thrombopenia;
Quinke’s edema; pregnancy and nursing.
Special warnings and precautions
In patients with renovascular hypertension and low sodium serum level the preparation
should be used with exceptional attention, because of enhanced hypotensive effect
of the medicine, due to high level of renin releasing. In cases with severe renal
insufficiency the treatment should be started with low doses Captopril, whereas
protein excretion in urine and serum creatine and urea level are monitored. Captopril
should be used very carefully in patients with bilateral stenosis of the renal arteries
and autoimmune diseases.
Drug interactions
Captopril may reinforce hypoglycemic effect of the insulin and oral antidiabetic
medicines. In concomitant treatment with potassium-sparing diuretics the risk of
hyperkalemia is enhanced. Enhanced risk of leucopenia exists in concomitant treatment
with immunosupressive agents. The orthostatic hypotension is more frequent in combined
therapy with neuroleptics. Captopril may elevate serum levels of digoxin and reduces
calcium channel blocker activity. Nonsteroid anti-inflammatory drugs reduce its
antihypertensive effect. Hypotensive effect of Captopril is enhanced in concomitant
treatment with vasodilators, diuretics and β-adrenoreceptor blocking agents.
Adverse reactions
Gastrointestinal disorders (mild and transitory); taste disorders; rashes; headache;
dizziness; paresthesias; hypotension. In high dosage of the preparation proteinuria,
neutropenia and leucopenia may appear. A comparatively frequent side effect is a
dry iritative cough, which resolves after discontinuation of the treatment.
Pharmacological mechanisms
Captopril belongs to ACE-inhibiting agents - blockers of the angiotensin-converting
enzyme. Renin-angiotensin system plays an important role in regulation of the blood
pressure. Activity of this pressor system is depressed in significant level by the
angiotensin-converting enzyme inhibitors, which prevent the transformation of angiotensin
I to angiotensin II. In this way ACE - inhibitors prevent formation of the most
powerful vasoconstrictive substance in the organism. ACE - inhibitors (in particular
Captopril) influence the kallikrein-kinin system also, as the angiotensin I - converting
enzyme is identical with kinase II. As the kinins (for example bradikinin) possess
powerful vasodilating effect, depressing its degradation leads to vasodilation.
Captopril, on the contrary of other vasodilators, does not cause fluid retention
and tachycardia. Combined treatment with other antihypertensive medicines is suitable.
Supplied
40 tablets of 25 mg.
Expiry
3 years.
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