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Telmisartan

MICARDIS

What it isAngiotensin II receptor blocker with partial PPAR-gamma activity; hypertension and cardiovascular risk reduction.

Why this oneThe longest half-life of the ARBs, so it forgives a late dose, and it has outcome data in high-risk patients.

What limits itHyperkalemia and the hemodynamic creatinine rise. Contraindicated in pregnancy.

FDA-approved for

FDA label

BOXED WARNING Fetal toxicity — discontinue as soon as pregnancy is detected.
FDA dosingPopulationStartTargetMax
HypertensionAdults40 mg QD40–80 mg QD80 mg QD
Cardiovascular risk reductionAdults unable to take ACE inhibitors80 mg QD80 mg QD80 mg QD

Titration Most antihypertensive effect within 2 wk; maximal by 4 wk

Renal No initial dosage adjustment (including hemodialysis); monitor for orthostatic hypotension on dialysis

Hepatic Biliary obstruction or hepatic insufficiency: initiate at low dose, titrate slowly

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Can cause fetal harm (2nd/3rd trimester RAS effects) — discontinue when pregnancy detected

Lactation Do not breastfeed during treatment (risk of hypotension, hyperkalemia, renal impairment in infant)

⚠ BOXED WARNING

Principal riskHyperkalemia and acute kidney injury

Cost, est. cash$5–$150/month

Generic entry2014

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk4 / 4

Legacy pregnancy categoryD

Defining liabilityHyperkalemia, kidney injury, fetal toxicity and increased lithium exposure.

Mechanism of action: Telmisartan ballicule

Telmisartan ballicule: receptor binding, kinetics and half-life diagram

Open Telmisartan in the interactive console ↗

Memory aids: mascots and interaction avatars

Telmisartan MICARDIS mascot mnemonic cartoon
“Tell me Sartan (what) My card is”
Telmisartan OATP substrate avatar
OATP substrate
Telmisartan Box: minimal PK interactions avatar
Box: minimal PK interactions

Open Telmisartan in the interactive console ↗