Micardis Indication:

For the treatment of hypertension.

Micardis Mechanism Of Action:

Micardis interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Micardis does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels.

Micardis Drug Interactions:

Not Available

Micardis Food Interactions:

Not Available

Micardis Generic Name:

Synonyms:

  • BIBR 277
  • BIBR 277SE

Drug Type:

Small Molecule; Approved

Absorption:

Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).

Toxicity (Overdose):

Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.

Protein Binding:

Highly bound to plasma proteins (>99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent.

Biotransformation:

Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.

Half Life:

Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.

Dosage Forms of Micardis:

Tablet Oral

Chemical IUPAC Name:

2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid

Organisms Affected:

Humans and other mammals

Micardis to general, pharmacology

General, pharmacology..
Cardiovascular