Amias - General Information
Amias, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Amias competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance.
Pharmacology of Amias
Amias, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Unlike the angiotensin receptor antagonist losartan, Amias does not have an active metabolite or possess uricosuric effects.
Amias for patients
No significant drug interactions have been reported in studies of candesartan cilexetil given with other drugs such as glyburide, nifedipine, digoxin, warfarin, hydrochlorothiazide, and oral contraceptives in healthy volunteers, or given with enalapril to patients with heart failure (NYHA class II and III). Because candesartan is not significantly metabolized by the cytochrome P450 system and at therapeutic concentrations has no effects on P450 enzymes, interactions with drugs that inhibit or are metabolized by those enzymes would not be expected.
Lithiumó Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with ACE inhibitors, and with some angiotensin II receptor antagonists. An increase in serum lithium concentration has been reported during concomitant administration of lithium with ATACAND, so careful monitoring of serum lithium levels is recommended during concomitant use.
ATACAND is contraindicated in patients who are hypersensitive to any component of this product.
Additional information about Amias
Amias Indication: For the treatment of hypertension.
Mechanism Of Action: Amias competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance.
Drug Interactions: Amiloride Increased risk of hyperkaliemia
Drospirenone Increased risk of hyperkaliemia
Lithium The ARB increases serum levels of lithium
Potassium Increased risk of hyperkaliemia
Spironolactone Increased risk of hyperkaliemia
Triamterene Increased risk of hyperkaliemia
Food Interactions: Take without regard to meals.
Administer on a regular basis, at about the same time each day.
Generic Name: Candesartan
Synonyms: Candesartan cilexetil
Drug Category: Antihypertensive Agents; Angiotensin II Receptor Antagonists
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Candesartan: Atacand; Blopress; Amias; Ratacand;
Absorption: Following administration of the candesartan cilexetil prodrug, the absolute bioavailability of candesartan was estimated to be 15%. Food with a high fat content has no affect on the bioavailability of candesartan from candesartan cilexetil.
Toxicity (Overdose): No lethality was observed in acute toxicity studies in mice, rats and dogs given single oral doses of up to 2000 mg/kg of candesartan cilexetil or in rats given single oral doses of up to 2000 mg/kg of candesartan cilexetil in combination with 1000 mg/kg of hydrochlorothiazide. In mice given single oral doses of the primary metabolite, candesartan, the minimum lethal dose was greater than 1000 mg/kg but less than 2000 mg/kg.
Protein Binding: Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells.
Biotransformation: During absorption from the gastrointestinal tract, the prodrug candesartan cilexetil undergoes rapid and complete ester hydrolysis to form the active drug, candesartan. Elimination of candesartan is primarily as unchanged drug in the urine and, by the biliary route, in the feces. Minor hepatic metabolism of candesartan occurs by O -deethylation to form an inactive metabolite.
Half Life: Approximately 9 hours.
Dosage Forms of Amias: Tablet Oral
Chemical IUPAC Name: 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid
Chemical Formula: C24H20N6O3
Candesartan on Wikipedia: http://en.wikipedia.org/wiki/Candesartan
Organisms Affected: Humans and other mammals