My watch list
my.chemeurope.com  
Login  

Ramipril



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
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 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.


Additional recommended knowledge

Contents

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.
  • Also ramipril has been known to be abused as a downer.[citation needed]

Cautions

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

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.

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.)

Dose

  • Hypertension:

2.5mg - 10mg once daily (O/D)

  • Post MI:

2.5mg - 5mg twice daily (B/D)

(If not tolerated 1.25mg - 2.5mg BD)

  • Diabetic and non-diabetic nephropathy:

1.25mg - 10mg O/D


Patients should be started on the lowest dose and titrated up at 1 - 2 weeks at a time.

See also

  • Hypertension
  • Hypotension
  • Heart failure

[]

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Ramipril". A list of authors is available in Wikipedia.
Your browser is not current. Microsoft Internet Explorer 6.0 does not support some functions on Chemie.DE