Losartan potassium, amlodipine besilate.
Each film-coated tablet contains Losartan Potassium 50 mg, Amlodipine (as besilate) 5 mg.
Pharmacokinetics: Losartan: The oral bioavailability is about 30%. The peak plasma concentration close to 800 nanograms per mL is reached within one hour after oral intake of 100 mg. The peak of the active metabolite is 2 times that of Losartan & appears between 2 and 4 hours after dosing & contributes to the late phase of the activity. The curve of plasma concentrations does not seem unaffected by food intake. The binding of Losartan and its active metabolite to plasma proteins (mainly albumin) is 99%. The plasma half life of Losartan is about 2 hours and that of its metabolites is between 6 & 9 hours. Losartan is metabolized by the liver into an active metabolite-5 carboxylic acid which is subsequently degraded. About 30 to 40% of the orally administered dose is recovered in the urine as unchanged drug & active metabolite. About 50 to 60% of orally administered dose is recovered in the feces.
Amlodipine: After oral administration of the therapeutic doses, Amlodipine is totally absorbed. The absolute bioavailability of Amlodipine ranges from 64 to 80%. The plasma peak is delayed, occurring 6 to 12 hours after dosing. The terminal elimination half life is about 35 to 50 hours & is consistent with once daily dosing. Steady state plasma levels are reached after 7 to 8 days of consecutive dosing. Amlodipine is almost entirely metabolized to inactive metabolites. 10% of the parent compound & 60% of metabolites are excreted in urine.
In vitro studies have shown that circulating Amlodipine is bound to 97.5% of plasma proteins.
For the treatment of mild to moderate hypertension in patients whose blood pressure is not adequately controlled on either monotherapy.
The recommended dosage is one tablet once a day or as directed by the physician.
Losartan and Amlodipine are contraindicated in patients with known hypersensitivity to Amlodipine and Losartan Potassium. It is also contraindicated in pregnant women (in their 2nd and 3rd trimester) and nursing mothers.
Rarely, patients with coronary arterial obstruction develop a high frequency of angina and myocardial infarction. The mechanism of this effect has not been elucidated.
Losartan and Amlodipine are well tolerated. The most commonly observed adverse effects were diarrhea, dyspepsia, myalgia, oedema, dizziness, insomnia & headache.
No significant interactions are observed when Amlodipine is co-administered with thiazide diuretics, beta blockers, ACE (angiotensin-converting enzyme) inhibitors, and nitrates, anti inflammatory drugs, antibiotics & oral hypoglycemic. Cimetidine does not alter the pharmacokinetics of Amlodipine. Amlodipine did not alter plasma levels of digoxin, phenytoin, warfarin & indometacin (INN).
Losartan Potassium: Co-administration with cimetidine may increase the serum concentration of Losartan. Co-administration with phenobarbital may reduce the serum concentration and that of its active metabolite. There is no pharmacokinetic interaction between Losartan and hydrochlorothiazide. There are no data concerning the transition in breast milk. Consequently, as a precaution, administering the drug in women who are nursing/pregnant and treatment should be discontinued if pregnancy is suspected.
Store at temperatures not exceeding 30°C.
C09DB06 - losartan and amlodipine ; Belongs to the class of angiotensin II receptor blockers (ARBs) and calcium channel blockers. Used in the treatment of cardiovascular disease.