COMPOSITION
Each uncoated tablet contains Telmisartan 20 mg or 40 mg
Telmisartan is an angiotensin II receptor antagonist. Telmisartan keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow. Telmisartan is used to treat high blood pressure (hypertension). It is sometimes given together with other blood pressure medications.
PHARMACOLOGY
Pharmacological Actions:
Telmisartan displaces angiotensin II with very high affinity from its binding site at the AT1 receptor subtype, which is responsible for the known actions of angiotensin II.
Absorption
Following oral administration of telmisartan, absorption is rapid (tmax ranges from 0.5 to 2 hours) although the amount absorbed varies. Absolute bioavailability of telmisartan was shown to be dose dependent. The mean absolute bioavailability of 40 mg telmisartan was 40%, whereas the mean absolute bioavailability of the 160 mg dose amounted to about 60%.
Distribution
Telmisartan is highly bound to plasma protein (>99.5%), mainly albumin and alpha-1-acid glycoprotein. The mean steady state apparent volume of distribution (Vdss) is approximately 6.6 L/kg.
Metabolism
Telmisartan undergoes substantial first-pass metabolism by conjugation to the acylglucuronide. No pharmacological activity has been shown for the conjugate. Telmisartan is not metabolised by the cytochrome P450 system.
Excretion
Telmisartan is characterised by bi-exponential decay pharmacokinetics with a terminal elimination half-life of 18.3-23.0 hours.
INDICATIONS
Telmisartan is indicated for:
Treatment of hypertension
Prevention of cardiovascular morbidity and mortality in patients 55 years or older with coronary artery disease, peripheral artery disease, previous stroke, transient ischaemic attack or high risk diabetes with evidence of end organ damage.
CONTRAINDICATIONS
- Hypersensitivity to any of the components of the product
- Pregnancy
- Lactation
- Biliary obstructive disorders
- Severe hepatic impairment