PREVERSIL

 

Composition:

Each Preversil tablet contains 4 mg Perindopril Erbumine.

 

Properties:

-         Perindopril Erbumine is a pro-drug that metabolized in vivo by hydrolysis of the ester group to form perindoprilat which inhibits ACE (Angiotensin Converting Enzyme). It’s the mechanism through which this drug lowers blood pressure.

-         ACE catalyzes conversion of angiotensin I to angiotensin II. Angiotensin II is a potent peripheral vasoconstrictor which stimulates aldosterone secretion by the adrenal cortex, and provides negative feedback on renin  secretion.

-         So the inhibition of ACE results in decreased plasma angiotensin II, leading to decreased vasoconstriction, increased plasma renin activity and decreased aldosterone secretion.

-         While the principal mechanism of perindopril in blood pressure reduction is believed to be through the renin, angiotensin, aldosterone system, ACE inhibitors have some effect even in apparent low-renin hypertension.

 

Pharmacokinetics:

-         Oral administration of Preversil results in its rapid absorption with peak plasma concentrations at approximately 1 hour. The absolute bioavailability of perindopril is 75%.

• About 30-50% of systemically available perindopril is hydrolyzed to its active metabolite, perindoprilat which reachs its peak plasma concentration after 3 to 7 hours.

-         Mean total body clearance of perindopril is 219-362 ml/min, and its mean renal clearance is 23,3-28.6 ml/min.

-         Only 4-12% of the perindopril administered dose recovered unchanged in the urine.

-         Hepatic esterase appears to be responsible for the hydrolysis of perindopril.

-         The clearance of perindoprilat is almost exclusively renal.

-         Plasma concentrations of both perindopril and perindoprilat in elderly patients                    (over the age of 70) are twice those observed in younger patients.

 

Indications:

Preversil is indicated for the treatment of patients with essential hypertension, it may be used alone or given with other classes of anti-hypertensives especially thiazide diuretics. It is also recommended in the treatment of congestive heart failure.

 

Contraindications:

This drug must not be used in the following circumstances:

-         Patients with hypersensitivity to permdopril or to any other ACE inhibitors.

-         In patients with congestive heart failure.

-         pregnancy or breast feeding.

-         In children.

-         If in any doubt, ASK your physician.

 

 

 

Precautions/ Warning:

• Warn your attending physician in case of:

                  ·           Impaired renal function and hepatic insufficiency.

                  ·          Congestive heart failure.

-         Angioedema involving the face, extremities, lips, tongue and/or larynx has been reported in patients treated with ACE inhibitors.

-         It can cause symptomatic hypotension in some patients.

-         Treatment with ACE inhibitors may lead to agranulocytosis and neutropenia in rare cases.

-         Elevations of serum potassium have been observed in some patients.

 

Drug Interactions:

-         Diuretics: diuretics increase the hypotension effect of Preversil.

• Lithium: increased serum lithium and the symptoms of lithium toxicity have been reported when given with ACE inhibitors.

-         Food interactions: if Preversil is administered with food, the extent of biotransformation of perindopril to perindoprilat is reduced, so it’s administered generally in a fasting state.

 

Side Effects:

-         Gastrointestinal disorder, dizziness, cramps, localized rashes.

-         Non productive cough may sometimes occur.

-         If these problems persist, inform your physician.

  

Dosage & Administration:

-         In patients with essential hypertension the recommended initial dose is 4 mg once a day. The dosage may be titrated upward until blood pressure is controlled or to a maximum of 16 mg per day once or divided into two doses.

-         The recommended dose is 4-8 mg/day.

-         In elderly patients: the initial dosage is 4 mg daily in one or in two divided doses it may be titrated upward to a maximum of 8 mg/day.

-         In concomitant diuretics:

          ·           If treatment with Preversil alone was not adequate a diuretic can be added.

          ·           If patients currently being treated with a diuretic, symptomatic hypotension can occur following the initial dose of Preversil, that case the diuretic should be discontinued             2 to 3 days prior to Preversil therapy. If the diuretic can not be discontinued an initial dose of 2-4 mg Preversil daily in one or in two divided doses is used with careful medical supervision for several hours, then the dosage is titrated as described above.

-         In patients with impaired renal function: the initial dosage should be 2 mg/day and it should not exceed 8 mg/day.

 

Presentation:

Box contains 20 tablets of Preversil / 4 mg.

Box contains 30 tablets of Preversil / 4 mg.