Composition
The active ingredient of Epsitron™ is Captopril.
Properties
Epsitron™ acts by competitively inhibiting the angiotestin converting enzyme (ACE), which converts angiotensin I to angiotensin II. Angiotensin II i snot only a potent endogenous vasoconstrictor, but it is also stimulates aldosterone secretion from the adrenal cortex. Increased aldosterone leads to sodium and water retension, increased blood volume, and thus increased blood pressure. Therefore by reducing angiotestin II, blood pressure is lowered by two mechanisms: less direct vasoconstriction and less sodium and water retention via aldosterone.
Approximately 60 to 75% of an oral dose of Epsitron™ is absorbed from the gastro-intestinal tract. It is about 30% bound to plasma proteins. It is largely excreted in the urine 40 to 50% as unchanged drug and as metabolites. The elimination half-life has been reported to be 2 to 3 hours but this is increased in renal failure.
Indications
Hypertension: Epsitron™ is used as an adjunct in treatment with a thiazide diuretic in mild to moderate hypertension and in severe hypertension resistant to other treatment.
Congestive heart failure: Epsitron™ is used as an adjunct in the treatment of severe congestive heart failure.
Dosage
The dosage of Epsitron™ must be individually titrated to clinical response in each patient.
Hypertension: In the treatment of hypertension the initial dose is 12,5mg two daily by mouth, increased gradually according to the response of the patient. In mild to moderate hypertension the usual maintenance dose is 25mg to times daily and should not exceed 50mg twice daily. n severe hypertension a dose of 50mg three times daily should not be exceeded.
Congestive heart failure: The initial dose is 6,25-12,5mg three times daily. The dose may be increased to 25mg three times daily with careful monitoring. The first dose should be given under supervision. Elderly patients should be given the first day’s treatment in hospital. Epsitron™ is not recommended in patients with renal impairment. Where it is clinically indicated in severely hypertensive patients with impaired renal function, the dose should be kept as low as possible. In this patients a loop diuretic rather than a thiazide should be used.
Side Effects
The side-effects of Epsitron™ can be broadly grouped into those caused by allergic reactions and those due to excessive pharmacological effect. The allergic reactions are most commonly manifested as urticarial rashes adn fevers. Less common but very sever effects reported thus far include pancytopenia, agranulocytosis, leukopenia, nephrotic syndrome, membranous glomerulopathy and pemphigus. The reactions caused by pharmacological effective doses include a low incidence of orthostatic hypotension, tachycardia and rarely ischaemic damage to the heart or kidneys secondary to vasopressive effects. Ageusia (loss of taste) is a common adverse effect which resolves spontaneously in some patients. Proteinuria has also been reported.