Telmipres

• Approved Indications:
• Hypertension: For the treatment of high blood pressure to reduce the risk of cardiovascular events such as stroke and myocardial infarction.
• Cardiovascular Risk Reduction: In patients at high risk of cardiovascular events, including those with a history of myocardial infarction, stroke, or peripheral arterial disease.
• Heart Failure: Management in patients intolerant to angiotensin-converting enzyme (ACE) inhibitors.
• Diabetic Nephropathy: To delay progression of nephropathy in type 2 diabetic patients with proteinuria.
• Off-label Uses:
• Management of metabolic syndrome components.
• Adjunct therapy in resistant hypertension.

• Adults:
• Initial dose: 40 mg orally once daily.
• Maintenance dose: Adjust between 20 mg to 80 mg once daily based on response.
• Maximum dose: 80 mg daily.
• Elderly:
• Same as adults; initiate cautiously due to potential renal impairment.
• Renal Impairment:
• No initial dose adjustment required.
• Monitor renal function regularly in severe impairment.
• Hepatic Impairment:
• Use with caution in mild to moderate hepatic impairment.
• Avoid in severe hepatic impairment or cholestasis.
• Administration Route: Oral, with or without food.

Telmisartan selectively blocks the angiotensin II type 1 (AT1) receptors, preventing angiotensin II-mediated vasoconstriction and aldosterone secretion. This leads to vasodilation, reduced sodium and water retention, and decreased blood pressure. Additionally, telmisartan acts as a partial agonist of peroxisome proliferator-activated receptor gamma (PPAR-γ), which contributes to improved insulin sensitivity and beneficial metabolic effects.

• Absorption: Rapid oral absorption; peak plasma concentration within 0.5–1 hour.
• Bioavailability: Approximately 42–58%.
• Distribution: Highly bound to plasma proteins (~99.5%).
• Metabolism: Minimal hepatic metabolism via glucuronidation; not metabolized by cytochrome P450 enzymes.
• Half-life: Approximately 24 hours.
• Elimination: Primarily excreted via feces (~90%), minor renal elimination (~7%).

• Pregnancy: FDA category D. Telmisartan may cause fetal toxicity (renal impairment, oligohydramnios) especially during the second and third trimesters. Contraindicated during pregnancy.
• Lactation: Limited data available. Breastfeeding is not recommended due to potential adverse effects on the infant.

• Antihypertensive
• Angiotensin II receptor blocker (ARB)

• Known hypersensitivity to telmisartan or excipients.
• Pregnancy.
• Severe hepatic impairment or cholestasis.
• Concomitant use with aliskiren in diabetic or renal impaired patients.
• Bilateral renal artery stenosis.

• Use caution in patients with renal impairment or dehydration; monitor renal function.
• Risk of hyperkalemia, especially with potassium-sparing diuretics or supplements.
• May cause hypotension, particularly in volume- or salt-depleted patients.
• Monitor blood pressure and kidney function regularly.
• Possible angioedema; discontinue immediately if swelling occurs.
• Avoid use during pregnancy.

• Common:
• Dizziness
• Fatigue
• Back pain
• Nasopharyngitis
• Diarrhea
• Serious/Rare:
• Angioedema
• Hyperkalemia
• Renal impairment
• Hypotension
• Elevated liver enzymes

• Potassium supplements or potassium-sparing diuretics: Increased risk of hyperkalemia.
• NSAIDs: May reduce antihypertensive effects and increase risk of renal impairment.
• Aliskiren: Contraindicated in diabetic or renal impaired patients.
• No significant interaction with CYP450 enzymes as telmisartan is not metabolized by this system.

• Recommended as first-line therapy for hypertension and cardiovascular risk reduction by major guidelines including JNC 8 and ESC/ESH.
• Emphasis on avoiding use in pregnancy and monitoring renal function.
• Increasing recognition of PPAR-γ mediated metabolic benefits.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep out of reach of children.
• Do not freeze.
• No reconstitution or refrigeration required.