Telmisartan is a nonpeptide AT1 angiotensin II receptor antagonist. Exerts antihypertensive activity by preventing angiotensin II from binding to AT1 receptors thus inhibiting the vasoconstriction and aldosterone-secreting effects of angiotensin II.

Absorption
Rapidly absorbed. Dose dependent bioavailability 42% (after 40 mg dose); 58% (after 160-mg dose). Peak plasma concentrations: 0.5-1 hours.

Distribution
Protien binding: 99%.

Metabolism
Undergoes conjugation with glucuronic acid to form inactive metabolites.

Excretion
Excreted almost entirely as unchanged drug in faeces via bile. <1% excreted via urine. Terminal elimination half-life: 24 hours.

Information Not Available

URTI, dizziness, back pain, sinusitis, pharyngitis and diarrhoea. Slight elevations in liver enzymes.

Potentially Fatal: Rarely angioedema, rash, pruritus and urticaria.

Warnings
Pregnancy
When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.

Overdosage
Hypotension, dizziness, tachycardia or bradycardia. Supportive treatment to be instituted. Not removed by haemodialysis.

Hepatic insufficiency, biliary obstruction, renal impairment, renaly artery stenosis. Correct volume depletion before initiating treatment. Monitor serum potassium levels regularly, especially in elderly and renally-impaired patients.

Concurrent use increases digoxin concentration; increases risk of lithium toxicity; increases risk of hyperkalaemia with potassium sparing diuretics, heparin.

Food Interaction
Food slightly reduces the bioavailability

Oral
Hypertension
Adult: Initially, 40 mg once daily. Max: 80 mg/day.
Renal impairment: Severe impairment/ Haemodialysis: Initial dose 20 mg/day.
Hepatic impairment: Mild to moderate: Max 40 mg/day. Severe: Contra-indicated

May be taken with or without food

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

In 2nd & 3rd trimesters.

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Contraindicated in lactation

Safety and efficacy not established

Information Not Available

Severe hepatic impairment, biliary obstructive disorders. Pregnancy. Lactation.

Oral
Store at 15-30°C

Information Not Available