Pharmacology

Telmisartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis. Telmisartan has much greater affinity (>3,000 fold) for the AT1 receptor than for the AT2 receptor. Because telmisartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Telmisartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Dosage & Administration

Dosage must be individualized. The usual starting dose of Telmisartan tablets is 40 mg once a day. Blood pressure response is dose-related over the range of 20 to 80 mg. Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. When additional blood pressure reduction beyond that achieved with 80 mg Telmisartan is required, may switch to the combination. No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis. Patients on dialysis may develop orthostatic hypotension; their blood pressure should be closely monitored. Telmisartan tablets may be administered with other antihypertensive agents. Telmisartan tablets may be administered with or without food. Initial therapy with Telmisartan is not recommended in patients ≥75 years old or with hepatic impairment.

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Interaction

• NSAIDS: Increased risk of renal impairment and loss of antihypertensive effect.
• Co-administration with aliskiren with Telmisartan: in patients with diabetes should be avoided.

Contraindications

Known hypersensitivity to this product or any of its components.

Side Effects

In hypertensive patients: The most common side effects of Telmisartan tablets include sinus pain and congestion (sinusitis), back pain, diarrhea etc.

For patients of cardiovascular risk reduction: The most common side effects of Telmisartan tablets in CV risk reduction include intermittent claudication and skin ulcer.

Pregnancy & Lactation

Pregnancy Category C (first trimester) and D (second and third trimester). Because of the potential for adverse effects on the nursing infant, decide whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Precautions & Warnings

• Avoid fetal or neonatal exposure.
• Hypotension.
• Monitor carefully in patients with impaired hepatic or renal function.
• Avoid concomitant use of an ACE inhibitor and angiotensin receptor blocker.

Use in Special Populations

Pediatric use: The safety and effectiveness of Telmisartan in pediatric patients have not been established.

Geriatric use: No overall differences in effectiveness and safety were observed in these patients compared to younger patients.

Hepatic impairment: Monitor carefully and up titrate slowly in patients with biliary obstructive disorders or hepatic insufficiency.

Overdose Effects

The most likely manifestation of overdosage with Telmisartan tablets would be hypotension, dizziness and tachycardia; bradycardia, increase in serum creatinine and acute renal failure could occur from parasympathetic (vagal) stimulation.

Therapeutic Class

Angiotensin-ll receptor blocker

Storage Conditions

Do not store above 30°C. Protect from light and high humidity. Keep out of the reach of children.