Lisinopril

Drug #423

Lisinopril is an oral angiotensin-converting enzyme (ACE) inhibitor used in the treatment of hypertension and congestive heart failure (CHF). Chemically, Lisinopril is the lysine ester of enalaprilat, the active moiety of enalapril. ACE inhibitors prevent conversion of certain enzymes in the body and prevents constriction of blood vessels and lower the blood pressure and makes the heart beat stronger. Lisinopril is active without metabolism and its (S) epimer is used clinicaly. Lisinopril is a lysine derivative of enalaprilat. Lisinopril is administered orally. It has a slower onset and a longer duration of action than either captopril or enalapril and can be dosed once daily.it was originally approved by the FDA in December 1987 for use in the treatment of hypertension. In July 1993, it was also approved for use in the treatment of CHF. Finally, in November 1995, it was approved to improve survival in hemodynamically stable patients within 24 hours post-myocardial infarction.it competes with angiotensin I for its binding site on the angiotensin-converting enzyme (ACE). As a result, the drug blocks the conversion of angiotensin I to angiotensin II. Angiotensin II is a potent vasoconstrictor and a negative feedback mediator for renin activity. Thus, when it lowers angiotensin II plasma levels, blood pressure decreases and plasma renin activity increases.

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Primary Characteristics

It is of Synthetic origin and belongs to Proline dihydrate.

It belongs to Angiotensin converting enzyme inhibitor-ACEI pharmacological group on the basis of mechanism of action and also classified in Antihypertensive Agents pharmacological group.

Molecular Weight: 441.5 · pK_a: 2.5, 4.0, 6.7, 10.1 · Solubility in Water: Soluble · Solubility in Alcohol: Insoluble · Non-proprietary name: Lisinopril.

Pharmacokinetics

Absorption: Lisinopril has an oral bioavailability is 12.5% (±12.5%).

Distribution: Lisinopril has a volume of distribution is 31-36 liter. plasma protein binding is 3-10%.

Elimination: plasma half-life is 12 hr, renal excretion is ~100% (unchanged).

Indications

Lisinopril is primarily indicated in conditions like Acute myocardial infarction, Congestive heart failure (adjunct), Diabetic nephropathy, Diabetic retinopathy, Gastric acid reduction during anaesthesia, Heart failure, Heart failure (adjunct), Hypertension, Iron deficiency anaemia.

Lisinopril is also indicated for secondary conditions like Essential and renovascular hypertension.

Contraindications

Lisinopril is contraindicated in conditions like Salt depletion, Renal artery stenosis, Hypotension, Angioneurotic edema, Renal impairment, Hypersensitivity.

Dosage

Lisinopril's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
3.75 mg	3.75 mg	Every 24h	PO	Initially for hypertension
3.75 mg	3.75 mg	Every 24h	PO	Initially for heart failure.
22.5 mg	22.5 mg	Every 24h	PO	Maintanace for hypertension
50 mg	50 mg	—	PO	Maintanance for hypertension,
Paediatric Dosage (20kg)
0 – 0	—	—		Not recommended for this age group
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown3 interactions

5 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Lisinopril in overdosage may give rise to further complications which include Angioedema , Angioedema , Airway obstruction.

Lisinopril produces potentially life-threatening effects which include Hypotension, Renal failure. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Lisinopril are Hypotension.

Lisinopril is known to cause more or less tolerable side effects which are usually transient. These include Alopecia, Asthenia , Cough , Diarrhea, Dizziness, Headache, Impotence, Nausea, Palpitation, Photosensitivity, Skin rash, Vomiting .

Warnings / Precautions

W.B.Cs counts and urinary protein estimation should be done before and after therapy. Lisinopril therapy can cause neutropenia or agranulocytosis. Patients with renal disease, patients with immunosuppression or receiving immunosuppressives, and patients with collagen vascular disease or autoimmune disease are at a greater risk for developing these complications. It should be used with caution in patients with pre-existing bone marrow depression. The dose should be adjusted in patients with renal impairment. It should be used cautiously in patients with congestive heart failure. Initial doses should be lower than in the treatment of hypertension because of a greater risk of developing hypotension. It should not be administered to patients with pre-existing renal artery stenosis. Renal function should be monitored closely during the first 2 weeks after initiating therapy. It should be discontinued if renal function worsens acutely. Other types of renal disease can actually improve during lisinopril therapy. The dose should be adjusted in patients with renal impairment. It should be used with caution in patients with hyperkalemia. It should be used during pregnancy only if clearly needed. Lisinopril is not for use in the children.

Interference in Pathology

Lisinopril may interfere in the diagnosis of Liver Function Test (LFT) , Increased in serum creatinin, Elevation in BUN.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Tabs

10 mg 20 mg 5 mg

Multi-Ingredient Combinations

Tabs

10 mg 20 mg

Storage Conditions

Lisinopril should be stored Tab.

Drug Classification

1.12.3.3 — ACE inhibitors

Manufacturers

Manufacturers of Lisinopril in Pakistan:

Alliance Atco Bosch Brookes Davis Getz GSK Harmann Hygeia ICI Medicraft Nenza Obs Obsons Pharmatec Pulse Raazee Shaheen Tabros Unison Werrick Zafa