Pharmacokinetics:
PRO DRUG RAMIPRIL
ACTIVE METABOLITE RAMIPRILAT
BIOAVAILABILITY 54-65%
TIME TO PEAK LEVELS PARENT DRUG
0.5-4 H
METABOLITE 1.5-3 H
A) ONSET OF ACTION 30 MIN –2 H
B) PEAK ACTION 4-8 H
C) DURATION OF ACTION ~ 24 H
HALF LIFE 13-17 H
ROUTE OF ELIMINATION 60% RENAL
40% FAECES
ACE Inhibition:
BP lowering Effect + Vasculoprotective Effect
Indications:
- Hypertension
- Myocardial Infarction
- Stroke
Dosage:
- Treatment of Congestive Heart Failure
Recommended dose is 1.25mg once daily
- Treatment of Hypertension
Recommended dose is 2.5mg once daily
- Treatment after Myocardial Infarction
Recommended dose is 5mg once daily
METABOLISM & EXCRETION:
- Ramipril is almost completely converted to Ramiprilat or inactive metabolites
(1% unchanged Ramipril is recovered in urine)
- Both Ramipril and Ramiprilat are metabolized to inactive Diketopiperazines
and Glucuronides
Route of Excretion:
60% Renally
40% Nonrenally (Hepatic)
Contraindications:
- Renal Artery Stenosis
- Pregnancy & Lactation
- Children
- Known Hypersensitivity
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