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Provinace


COMPOSITION

Each tablet contains Perindopril erbumine 4 mg.


PHARMACODYNAMICS

Perindopril is an inhibitor of the enzyme that converts angiotensin I into angiotensin II (Angiotensin Converting Enzyme ACE). The converting enzyme, or kinase, is an exopeptidase that allows conversion of angiotensin I into the vasoconstrictor angiotensin II as well as causing the degradation of the vasodilator bradykinin into an inactive heptapeptide. Inhibition of ACE results in a reduction of angiotensin II in the plasma, which leads to increased plasma renin activity (by inhibition of the negative feedback of renin release) and reduced secretion of aldosterone. Since ACE inactivates bradykinin, inhibition of ACE also results in an increased activity of circulating and local kallikrein-kinin systems (and thus also activation of the prostaglandin system). It is possible that this mechanism contributes to the blood pressure-lowering action of ACE inhibitors and is partially responsible for certain of their side effects (e.g. cough). Perindopril acts through its active metabolite, perindoprilat. The other metabolites show no inhibition of ACE activity in vitro.


Hypertension Perindopril is active in all grades of hypertension: mild, moderate, severe; a reduction in systolic and diastolic blood pressures in both supine and standing positions is observed. Perindopril reduces peripheral vascular resistance, leading to blood pressure reduction. As a consequence, peripheral blood flow increases, with no effect on heart rate. Renal blood flow increases as a rule, while the glomerular filtration rate (GFR) is usually unchanged. The antihypertensive activity is maximal between 4 and 6 hours after a single dose and is sustained for at least 24 hours: trough effects are about 87-100 % of peak effects. The decrease in blood pressure occurs rapidly. In responding patients, normalisation is achieved within a month and persists without the occurrence of tachyphylaxis. Discontinuation of treatment does not lead to a rebound effect. Perindopril reduces left ventricular hypertrophy. In man, perindopril has been confirmed to demonstrate vasodilatory properties. It improves large artery elasticity and decreases the media: lumen ratio of small arteries. An adjunctive therapy with a thiazide diuretic produces an additive-type of synergy. The combination of an ACE inhibitor and a thiazide also decreases the risk of hypokalaemia induced by the diuretic treatment.


Heart failure Perindopril reduces cardiac work by a decrease in preload and afterload.

Studies in patients with heart failure have demonstrated :
- decreased left and right ventricular filling pressures.
- reduced total peripheral vascular resistance.
- increased cardiac output and improved cardiac index.


In comparative studies, the first administration of 2 mg of Perindopril to patients with mild to moderate heart failure was not associated with any significant reduction of blood pressure as compared to placebo.


PHARMACOKINETICS

After oral administration, the absorption of perindopril is rapid and the peak concentration complete within 1 hour. Bioavailability is 65 to 70 %. About 20 % of the total quantity of perindopril absorbed is converted into perindoprilat, the active metabolite. In addition to active perindoprilat, perindopril yields five metabolites, all inactive. The plasma half-life of perindopril is equal to 1 hour. The peak plasma concentration of perindeprilat is achieved within 3 to 4 hours. As ingestion of food decreases conversion to perindoprilat, hence bioavailability, PROVINACE should be administered orally in a single daily dose in the morning before a meal. The volume of distribution is approximately 0.2 L/kg for unbound perindoprilat. Protein binding is slight (binding of perindoprilat to angiotensin converting enzyme is less than 30 %), but is concentration-dependent. Perindoprilat is eliminated in the urine and the half-life of the unbound traction is approximately 3 to 5 hours. Dissociation of perindoprilat bound to angiotensin converting enzyme leads to an "effective" elimination half-life of 25 hours, resulting in steady-state within 4 days. After repeated administration, no accumulation of perindopril is observed. Elimination of perindoprilat is decreased in the elderly, and also in patients with heart or renal failure. Dosage adjustment in renal insufficiency is desirable depending on the degree of impairment (creatinine clearance). Dialysis clearance of perindoprilat is equal to 70ml/min. Perindopril kinetics are modified in patients with cirrhosis: hepatic clearance of the parent molecule is reduced by halt. However, the quantity of perindoprilat formed is not reduced and therefore no dosage adjustment is required (see also "Dosage and Administration" and "Warnings and Precautions").


INDICATIONS

Hypertension: Treatment of hypertension
Heart Failure: Treatment of symptomatic heart failure

RECOMMENDED DOSE

It is recommended that PROVINACE is taken once daily in the morning before a meal. The dose should be individualised according to the patient profile (see "Warnings and Precautions") and blood pressure response.


Hypertension PROVINACE may be used in monotherapy or in combination with other classes of antihypertensive therapy. The recommended starting dose is 4 mg given once daily in the morning. Patients with a strongly activated renin-angiotensin-aldosterone system ( in particular, renovascular hypertension, salt and/ or volume depletion, cardiac decompensation or severe hypertension) may experience an excessive drop in blood pressure following the initial dose. A starting dose of 2 mg is recommended in such patients and the initiation of treatment should take place under medical supervision. The dose may be increased to 8 mg once daily after one month of treatment. Symptomatic hypotension may occur following initiation of therapy with PROVINACE; this is more likely in patients who are being treated concurrently with diuretics. Caution is therefore recommended since these patients may be volume and/or salt depleted. It possible, the diuretic should be discontinued 2 to 3 days before beginning therapy with PROVINACE (see "Warnings and Precautions"). In hypertensive patients in whom the diuretic cannot be discontinued, therapy with PROVINACE should be initiated with a 2 mg dose. Renal function and serum potassium should be monitored. The subsequent dosage of PROVINACE should be adjusted according to blood pressure response. If required, diuretic therapy may be resumed. In elderly patients treatment should be initiated at a dose of 2 mg which may be progressively increased to 4 mg after one month then to 8 mg if necessary depending on renal function (see table below).


Symptomatic heart failure It is recommended that PROVINACE, generally associated with a non-potassium-sparing diuretic and/or digoxin and/or a beta blocker, be introduced under close medical supervision with a recommended starting dose of 2 mg taken in the morning. This dose may be increased by increments of 2 mg at intervals of no less than 2 weeks to 4 mg once daily it tolerated. The dose adjustment should be based on the clinical response of the individual patient. In severe heart failure and in other patients considered to be at high risk (patients with impaired renal function and a tendency to have electrolyte disturbances, patients receiving simultaneous treatment with diuretics and/or treatment with vasodilating agents), treatment should be initiated under careful supervision (see"Warnings and Precautions") . Patients at high risk of symptomatic hypotension e.g. patients with salt depletion with or without hyponatraemia, patients with hypovolaemia or patients who have been receiving vigorous diuretic therapy should have these conditions corrected, if possible, prior to therapy with PROVINACE. Blood pressure, renal function and serum potassium should be monitored closely, both before and during treatment with PROVINACE (see"Warnings and Precautions").

 

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