Ramipril
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| Clinical data | |
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| Trade names | Altace |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a692027 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 28% |
| Protein binding | 73% (ramipril) 56% (ramiprilat) |
| Metabolism | Hepatic, to ramiprilat |
| Biological half-life | 2 to 4 hours |
| Excretion | Renal (60%) and fecal (40%) |
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| CAS Number | |
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| ChEMBL | |
| ECHA InfoCard | 100.170.726 |
| Chemical and physical data | |
| Formula | C23H32N2O5 |
| Molar mass | 416.511 g/mol |
| 3D model (Jmol) | |
| Melting point | 109 °C (228 °F) |
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Ramipril, sold under the brand name Altace among others, is an angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure (hypertension) and congestive heart failure. By inhibiting an enzyme, ACE inhibitors relax the muscles around small arteries (arterioles). The arterioles expand and allow blood to flow through more easily. This reduces blood pressure.
Indications for its use include:
Contraindications to its use include renovascular disease (impaired blood flow in the kidneys), severe renal impairment (especially in patients with one kidney or with bilateral renal artery stenosis), volume-depleted patients, a history of angioedema while on an ACE inhibitors, pregnancy, and hypotension.
Serious allergic reactions to this drug are unlikely, but immediate medical attention must be sought if they occur. Symptoms of a serious allergic reaction include, but are not limited to a rash or swelling of the face, mouth, tongue, or throat. In extreme cases, ramipril may lead to potentially fatal liver problems.
ACE inhibitors inhibit the actions of angiotensin converting enzyme (ACE), thereby lowering the production of angiotensin II and decreasing the breakdown of bradykinin. The decrease in angiotensin II results in relaxation of arteriole smooth muscle leading to a decrease in total peripheral resistance, reducing blood pressure as the blood is pumped through widened vessels. Its effect on bradykinin is responsible for the dry cough side effect.
Ramipril, a prodrug or precursor drug, is converted to the active metabolite ramiprilat by carboxylesterase 1. Ramiprilat is mostly excreted by the kidneys. Its half-life is variable (3–16 hours), and is prolonged by heart and liver failure, as well as kidney failure.
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Wikipedia