MICARDIS
Clinical safety rating
cautionComprehensive clinical and safety monograph for MICARDIS (MICARDIS).
Telmisartan is an angiotensin II receptor antagonist (ARB) that selectively and competitively blocks the binding of angiotensin II to the AT1 receptor, resulting in vasodilation, reduced aldosterone secretion, and decreased blood pressure.
| Metabolism | Telmisartan is metabolized by glucuronidation via UGT1A3 and UGT2B7; minimal CYP450 metabolism. |
| Excretion | Primarily biliary/fecal (approximately 60% as unchanged drug); renal elimination accounts for about 40% (mostly unchanged drug and inactive metabolites). Total recovery in feces: 60-70%; urine: 30-40%. |
| Half-life | Terminal elimination half-life is approximately 24 hours (range 20-30 hours), supporting once-daily dosing. Steady-state achieved in 5-7 days. |
| Protein binding | Highly bound (>99.5%), primarily to albumin and α1-acid glycoprotein. Binding is saturable at high concentrations but clinically not significant at therapeutic doses. |
| Volume of Distribution | Apparent volume of distribution: approximately 500 L (about 7 L/kg), indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is variable, approximately 40-60% (mean 50%) due to first-pass metabolism. Food reduces bioavailability by about 20%, but clinical effect is not significantly altered. |
| Onset of Action | Oral: Rapid absorption; antihypertensive effect begins within 2 hours, with peak effect at 4-8 hours. |
| Duration of Action | Duration of antihypertensive effect persists for 24 hours with once-daily dosing, maintaining smooth blood pressure control over the dosing interval. |
| Molecular Weight | 514.62 |
| Action Class | Angiotensin receptor blockers(ARB) |
| Brand Substitutes | Danavish Telmisartan 40mg Tablet, Telmikind 40 Tablet, Telmavas 40 Tablet, Telkonol 40mg Tablet, Lintel 40 Tablet, Ozotel 80mg Tablet, Newtel 80 Tablet, Telmikind 80 Tablet, Arbitel 80 Tablet, Tigatel 80 Tablet |
40-80 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. Not studied in GFR <30 mL/min or dialysis; use caution. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). For mild to moderate impairment (Child-Pugh A or B), maximum dose is 40 mg once daily. |
| Pediatric use | Safety and efficacy not established in pediatric patients (<18 years). |
| Geriatric use | No specific dose adjustment needed; start at lower end of dosing range (40 mg) due to possible increased sensitivity. |
| 1st trimester | Avoid. Fetal toxicity risk; limited data suggest potential teratogenic effects. |
| 2nd trimester | Contraindicated. Risk of fetal renal dysfunction, oligohydramnios, and skull ossification defects. |
| 3rd trimester | Contraindicated. Increased risk of fetal and neonatal morbidity and death. |
Clinical note
Comprehensive clinical and safety monograph for MICARDIS (MICARDIS).
| Placental transfer | Crosses placenta; detected in fetal plasma at concentrations similar to maternal. |
| Breastfeeding | Excreted in breast milk in low amounts; no known adverse effects in infants. However, due to potential for hypotension and renal effects, use with caution, especially in preterm or hypertensive infants. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Drugs acting directly on the renin-angiotensin system (RAS) can cause fetal and neonatal morbidity and death when used during the second and third trimesters. First trimester exposure does not appear to increase the risk of congenital anomalies, but should be avoided due to potential unknown risks. Oligohydramnios, fetal renal dysfunction, skull hypoplasia, hypotension, and hyperkalemia are risks associated with second and third trimester exposure. |
| Fetal Monitoring | Monitor fetal ultrasound for oligohydramnios, fetal renal function, and skull ossification during second and third trimesters. Serial ultrasound examinations should be performed to assess the intra-amniotic environment. If oligohydramnios is observed, discontinue the drug unless it is considered life-saving for the mother. Monitor neonates for hypotension, hyperkalemia, and renal function. |
| Fertility Effects | No clinical studies have assessed the effects of telmisartan on human fertility. Animal studies at high doses showed no impairment of fertility. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
Hypersensitivity to telmisartan or any excipientPregnancy (second and third trimesters)Concomitant use with aliskiren in patients with diabetes mellitus
| Precautions | Fetal toxicity: Use in pregnancy can cause injury and death to the fetus; discontinue when pregnancy is detected., Hypotension in volume- or salt-depleted patients, Renal function impairment: Monitor serum creatinine and potassium, Hyperkalemia: Risk increased with renal impairment, diabetes, or concomitant K+ supplements/sparing diuretics, Avoid coadministration with aliskiren in patients with diabetes |
| Food/Dietary | No specific food restrictions. Avoid salt substitutes containing potassium chloride. Maintain consistent dietary habits to avoid fluctuations in blood pressure. Grapefruit juice has no known interaction but other drugs may be affected; consult pharmacist for all medications. |
| Clinical Pearls | Monitor renal function and serum potassium before and during therapy, especially in patients with renal impairment or on potassium-sparing diuretics. May cause a rise in serum creatinine; usually minor and reversible. Avoid use in patients with biliary obstructive disorders or severe hepatic impairment due to primarily biliary excretion. Can be used with or without food; consistency recommended to avoid variability in absorption. Combination with aliskiren is contraindicated in diabetes. Adjust dose in patients with hepatic impairment; initial dose 40 mg once daily. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily, with or without food. Try to take it at the same time each day. · Do not stop taking this medicine without consulting your doctor, even if you feel well. High blood pressure often has no symptoms. · If you have a pregnancy potential, use effective contraception and notify your doctor immediately if you become pregnant. This drug can harm an unborn baby. · Avoid alcohol and use caution when driving or operating machinery until you know how this medicine affects you, as dizziness may occur. · Do not use salt substitutes containing potassium without your doctor's approval. This medication may increase your potassium levels. · Stay adequately hydrated, especially during exercise or in hot weather, to prevent low blood pressure. Dehydration may increase the risk of low blood pressure. · Report any signs of infection (fever, sore throat) or swelling of the face, lips, or tongue, which may indicate a serious allergic reaction. · Keep all appointments for blood pressure checks and lab work (kidney function and potassium levels). |
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