Description

Simple

A medication used to lower blood pressure and to reduce the risk of potentially fatal heart complications after a heart attack.

Clinical

An ACE inhibitor used for the management of hypertension and the reduction of cardiovascular mortality following myocardial infarction in hemodynamically stable patients with clinical signs of congestive heart failure.

Overview

Ramipril is a prodrug belonging to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is metabolized to ramiprilat in the liver and, to a lesser extent, kidneys. Ramiprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Ramipril may be used in the treatment of hypertension, congestive heart failure, nephropathy, and to reduce the rate of death, myocardial infarction and stroke in individuals at high risk of cardiovascular events.

Pharmacology

Indication

For the management of mild to severe hypertension. May be used to reduce cardiovascular mortality following myocardial infarction in hemodynamically stable individuals who develop clinical signs of congestive heart failure within a few days following myocardial infarction. [FDA Label] To reduce the... Read more

Pharmacodynamic

Ramipril is an ACE inhibitor similar to benazepril, fosinopril and quinapril. [5] It is an inactive prodrug that... Read more

Mechanism of action

Ramipril inhibits the RAAS system by binding to and inhibiting ACE thereby preventing the conversion of angiotensin I to angiotensin II. [ Read more

Absorption

The extent of absorption is at least 50-60%.[FDA Label]. Food decreases the rate of absorption from the GI tract without affecting the extent of absorption. The absolute bioavailabilities of ramipril and ramiprilat were 28% and 44%, respectively, when oral administration was compared to intravenous... Read more

Protein binding

Protein binding of ramipril is about 73% and that of ramiprilat about 56%.[FDA Label] Protein binding is independent of concentration over the range of 0.1μg/mL-10μg/mL

Volume of distribution

Information currently not available.

Clearance

The renal clearance of ramipril and ramiprilat was reported to be 7.2 and 77.4 mL/min/1.73m2. [ Read more

Half life

Plasma concentrations of ramiprilat decline in a triphasic manner.[FDA Label] Initial rapid decline represents distribution into tissues and has a half life of 2-4 hours. The half life of the apparent elimination phase is 9-18 hours, which is thought to represent clearance of free drug. The half-lif... Read more

Route of elimination

60% of the parent drug and its metabolites are eliminated in the urine with the remaining 40% eliminated in the feces.[FDA Label] The drug eliminated in the feces represents both absorbed drug and drug eliminated through biliary excretion although the proportion of these has not been determined. Les... Read more

Toxicity

Symptoms of overdose may include excessive peripheral vasodilation (with marked hypotension and shock), bradycardia, electrolyte disturbances, and renal failure. Cases of ACE inhibitor induced hepatotoxicity have been reported in humans and presented as acute jaundice and elevated liver enzymes.[ Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Hypotension US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 4
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abnormal kidney function US
  • Kind: experimental
    • Percent: 3
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Angina Pectoris US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Postural Hypotension US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0.5
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 0.7
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1
  • Kind: placebo
    • Percent: 0.4
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Increased sweating US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Photosensitivity US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Eosinophilia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Eosinophilic pneumonitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Arthritis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Vasculitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Elevated erythrocyte sedimentation rate US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Vision disturbances US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Positive ANA US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Neuralgia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Neuropathy US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Convulsions US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hearing Loss US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pemphigoid US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Erythema multiforme US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Toxic Epidermal Necrolysis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Diabetes
        • Drugbank Id: DBCOND0022048
    • With Drugs:
        • Name: Aliskiren
        • Drugbank Id: DB09026

    Food Interactions

    Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.

    Take with or without food. The absorption is unaffected by food.