Description

How Supplied

Enalapril tablets are presented as forms that containing 5, 10, 20 mg Enalapril(as maleate).10 tablets per blister pack, 10 blisters with a leaflet in a box

Category

Antihypertensive.

Mechanism of Action

Exact mechanism of antihypertensive action is unknown but is thought to be related to competitive inhibition of angiotensin I – converting enzyme (ACE) activity, resulting in a decreased rate of conversion of angiotensin I to angiotensin II, which is a potent vasoconstrictor. Decreased angiotensin II concentrations results in a secondary increase in plasma renin activity (PRA), that removal of the negative feedback of renin release, and a direct reduction in aldosterone secretion resulting in small increase in serum potassium, sodium and fluid loss.

Pharmacokinetics

• Absorption: Approximately 60%, not affected by the present of food.

• Protein binding: Moderate (50 to 60%).

• Half – life: 11 hours, increased in renal failure .
• Elimination: Renal-60 %; Fecal- 33 %;in dialysis-it is removable by hemodialysis,at the rate of 62 ml per minute and by peritoneal dialysis.

Pregnancy and Breast feeding

Enalapril cross the placenta ,First trimester FDA pregnancy category C. second and third trimester FDA pregnancy category D.and also distributed in breast milk.

Precautions

• Making regular visits to physician to check progress.
• Caution when driving or doing other things requiring alertness because of possible dizziness.
• Checking with physician if sever nausea, vomiting or diarrhea, extremely swelling, difficulty in swallowing or breathing and signs and symptoms of jaundice  or signs of infection occurs.
• Caution if any kind of surgery is required.
• Not taking other medication,especially nonprescription sympathomimethics,unless discussed with physician.

Drug interaction

Inform your doctor if you are taking any of the following medicines : alcohol ; diuretics; Hypotension producing medication;antacids ; nonsteroidal anti – inflammatory drugs like Indomethacin;lood from blood bank;cyclosporine;Diuretics, potassium – containing medications or supplements;salt substitutes; Allopurinol;cytosttic agents; procainamide ; systemic corticosteroids ;bone marrow depressants; Lithium ;sympathomimethics.

Dosage and Administration

Usual adult dose

• Antihypertensive: Initial-5 mg once a day, the dosage being adjusted after one or two weeks according to clinical response. Maintenance- 10 to 40 mg per day, as a single dose or in two divided doses.

• Vasodilator, Congestive heart failure: Initial- 2.5 mg once or twice a day, the dosage being adjusted after one or two weeks accordingto clinical response. Maintenance-5 to 40 mg per day , as a single dose or in two divided doses .

• Asymptomatic, Left venticular dysfunction: 2.5 mg two times a day titrated or tolerated up to a target dose of  20 mg a day in divided doses .

Note1:patients should be kept under medical supervision for at least two hours and until blood pressure has stabilized for an additional hour after the initial dose.

Note 2: in patients with hyponatremia or serum creatinine greater than 1.6 mg per deciliter,initial dose 2.5 mg once a day recommended.

    Prescribing Limit:40 mg per day.

Usual Pediatric dose

• Antihypertensive:Children 1 month to 16 years of age: initially 0.08 mg per kg of body weight per day up to 5 mg per day.(it is not administered to pediatric patients with creatinine clearance less than 30 ml per minute per 1.73m²)

Side effect

Those indicating need for medical attention : Hypotension ; skin rash with or without itching; fever;joint pain; angioedema of the extremities,face,lips,glottis and larynx , mucous membranes tongue , chest pain ; hyper kalemia ;Intestinal angioedema;neutropenia or agranulocytosis;pancreatitis.

Those indicating need for medical attention only if they continue or are bothersome : cough , dry persistent; headache ; diarrhea , dysgeusia;fatigue;nausea.

Storage

Store below  30 ^ºc (preferably between 15 ^ºc to 30 ^ºc) protect from light and moisture.keep out of reach of children.

Date of Revision: November 2012

Manufactured by Pursina pharmaceutical Co. Tehran – Iran