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telmisartan Micardis
Pharmacologic classification: angiotensin II receptor antagonist Therapeutic classification: antihypertensive Pregnancy risk category C (D in second and third trimesters)
Available forms Available by prescription only Tablets: 40 mg, 80 mg
Indications and dosages
Hypertension (used alone or with other antihypertensives). Adults: 40 mg P.O. once daily. Blood pressure response is dose-related over a range of 20 to 80 mg daily.
Pharmacodynamics Antihypertensive action: Inhibits vasoconstriction and aldosterone production by selectively blocking the binding of angiotensin II to its receptors.
Pharmacokinetics Absorption: Absolute bioavailability is about 42% for a 40-mg dose. Peak plasma levels are reached in 1/2 to 1 hour following oral administration.
Distribution: More than 99.5% bound to plasma proteins. Metabolism: Metabolized by glucuronide conjugation to an inactive metabolite. Excretion: Half-life is about 24 hours. Most is excreted unchanged in the feces via biliary excretion.
| Route |
Onset |
Peak |
Duration |
| P.O. |
Unknown |
1/2 hr-1 hr |
24 hr |
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Contraindications and precautions Contraindicated in pregnant women and in patients hypersensitive to drug or its components. Use cautiously in patients with biliary obstruction disorders, renal stenosis, or renal or hepatic insufficiency and in those
with an activated renin-angiotensin system, such as volume- or salt-depleted patients (such as those receiving high doses
of diuretics).
Interactions Drug-drug. Digoxin: Increases digoxin levels. Monitor digoxin levels closely. Warfarin: Decreases warfarin levels. Monitor patient closely. Drug-lifestyle. Alcohol use: Enhances hypotensive effects. Discourage alcohol use.
Adverse reactions CNS: dizziness, pain, fatigue, headache. CV: chest pain, hypertension, peripheral edema. EENT: pharyngitis, sinusitis. GI: abdominal pain, diarrhea, dyspepsia, nausea. GU: urinary tract infection. Musculoskeletal: back pain, myalgia. Respiratory: cough, upper respiratory tract infection. Other: flulike symptoms.
Effects on lab test results May increase liver enzyme levels.
Overdose and treatment Limited data exist. Most likely, symptoms include hypotension, tachycardia, dizziness, and possibly bradycardia. Treatment should involve supportive care. Telmisartan isn’t removed by hemodialysis.
Special considerations Closely monitor blood pressure. Monitor patient for hypotension following initiation of drug. Place patient in supine position if hypotension occurs and administer
I.V. normal saline solution if needed, as indicated. Blood pressure response in black patients is less than in white patients. Most of the antihypertensive effect is present within 2 weeks. Maximal blood pressure reduction usually is achieved after
4 weeks. Diuretic may be added if blood pressure isn’t controlled by drug alone. Drug isn’t removed by hemodialysis. Orthostatic hypotension may develop in patients undergoing dialysis. Pregnant patients Use of drug is contraindicated during pregnancy because of potential risk of fetal and neonatal morbidity and death. Breast-feeding patients It isn’t known whether drug appears in breast milk. Assess risks and benefits before continuing drug in breast-feeding women.
Pediatric patients Safety and efficacy in children haven’t been established. Geriatric patients No significant difference has been reported compared to younger patients.
Patient education Inform patient that drug shouldn’t be removed from blister-sealed packet until immediately before use. Inform women of childbearing age of the consequences of second- and third-trimester exposure to drug. Inform patient that transient hypotension may occur.
Reactions may be common, uncommon, life-threatening, or
COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use
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