Ramipril

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Ramipril
Systematic (IUPAC) name
(1S,5S,7S)-8-[(2S)-2-[[(1S)-1-ethoxycarbonyl-3-phenyl- propyl]amino]propanoyl]-8-azabicyclo[3.3.0]octane-7- carboxylic acid
Identifiers
CAS number	87333-19-5
ATC code	C09AA05
PubChem	5362129
DrugBank	APRD00009
Chemical data
Formula	C23H32N2O5
Mol. mass	416.511 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	28%
Protein binding	73% (ramipril) 56% (ramiprilat)
Metabolism	Hepatic, to ramiprilat
Half life	2 to 4 hours
Excretion	Renal (60%) and fecal (40%)
Therapeutic considerations
Pregnancy cat.	D
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Ramipril (marketed as Tritace/Ramace or Altace) is an angiotensin-converting enzyme (ACE) inhibitor, used to treat hypertension and congestive heart failure. ACE inhibitors lower the production of angiotensin II, therefore relaxing arterial muscles while at the same time enlarging the arteries, allowing the heart to pump blood more easily, and increasing blood flow due to more blood being pumped into and through larger passageways.

Ramipril is a prodrug and is converted to the active metabolite ramiprilat by liver esterase enzymes. Ramiprilat is mostly excreted by the kidneys. The half-life of ramiprilat is variable (3-16 hours), and is prolonged by heart and liver failure, as well as kidney failure.

It is marketed by King Pharmaceuticals under the brand name Altace and was protected by the U.S. Patent No. 5,061,722 (was scheduled to expire on 29^th Oct, 2008) assigned to Aventis. On September 11, 2007 in an appeal by Lupin Pharmaceuticals the United States Court of Appeals for the Federal Circuit reversed a district court trial verdict, finding that Aventis's patent on Altace was invalid for obviousness - opening the gate of this medicine to generic manufacturers.

Contents 1 Indications 2 Cautions 3 Contraindications 4 Side-effects 5 Dose 6 See also 7 External links

[edit] Indications

Indications for its use include:

• Hypertension;
• Congestive heart failure;
• Following myocardial infarction in patients with clinical evidence of heart failure;
• Susceptible patients over 55 years: prevention of myocardial infarction, stroke, cardiovascular death or need of revascularization procedures.

[edit] Cautions

• Do not take potassium supplements without seeking medical advice.
• Do not take during pregnancy

[edit] Contraindications

Renovascular disease, severe renal impairment (especially in patients with one kidney or with bilateral renal artery stenosis), volume-depleted patients, history of angioedema while on an ACE inhibitor, pregnancy, hypotension.

[edit] Side-effects

• may cause swelling of the mouth, tongue, or throat
• low blood sugar in patients taking other medicine for diabetes which shows as sweating or shakiness
• Dry cough may develop, dizziness, and light-headedness due to low blood pressure. (It is recommended to start treatment with the lowest dose.)

[edit] Dose

Patients are started on the lowest dose and titrated up every 1 - 2 weeks as required.

[edit] See also

• Hypertension
• Hypotension
• Heart failure
• Chest Pains

[edit] External links

• Altace (ramipril), a registered trademark of King Pharmaceuticals, Inc.

v • d • e Agents acting on the renin-angiotensin system (C09) ACE inhibitors Benazepril • Captopril • Cilazapril • Delapril • Enalapril • Fosinopril • Imidapril • Lisinopril • Moexipril • Perindopril • Quinapril • Ramipril • Spirapril • Temocapril • Trandolapril • Zofenopril Angiotensin II receptor antagonists (AIIRA) Azilsartan • Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan Renin inhibitors Aliskiren • Remikiren

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