Amlodipine besilate, losartan K.
Each tablet contains amlodipine besilate 5 mg and losartan K 50 mg.
Amlodipine + losartan contains the besilate salt of amlodipine, a dihydropyridine calcium channel blocker. Amlodipine besilate is a white to pale yellow crystalline powder, slightly soluble in water and sparingly soluble in ethanol. Amlodipine besilate's chemical name is 3-Ethyl-5-methyl(±)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate, monobenzenesulphonate.
Losartan potassium is an angiotensin II receptor (type AT1) antagonist.
Losartan potassium, a non-peptide molecule, is chemically described as 2-butyl-4-chloro-1-[p-(0-1H-tetrazol-5 ylphenyl) benzyl]imidazole-5-methanol monopotassium salt. Losartan potassium is a white to off-white free-flowing crystalline powder with a molecular weight of 461.01. It is freely soluble in water, soluble in alcohol, and slightly soluble in common organic solvents eg, acetonitrile and methyl ethyl ketone. Oxidation of the 5-hydroxymethyl group on the imidazole ring results in the active metabolite of losartan.
Pharmacology: Pharmacokinetics: Losartan is readily absorbed from the gastrointestinal tract following oral administration, with an oral bioavailability of about 33%. It
undergoes first-pass metabolism to form an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than losartan and some inactive metabolites. Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4.
Peak plasma concentrations of losartan and E-3174 occur about 1 hr and 3-4 hrs, respectively, after an oral dose. Both losartan and E-3174 are >98% bound to plasma proteins.
Losartan is excreted in the urine and in the feces via bile, as unchanged drug and metabolites. Following oral dosing about 35% of the dose if excreted in the urine and about 60% in the feces.
The terminal elimination half-lives (t½) of losartan and E-3174 are about 1.5-2.5 hrs and 3-9 hrs, respectively.
Amlodipine is well-absorbed following oral administration with peak blood concentrations occurring after 6-12 hrs. The bioavailability is about 60-65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has a prolonged terminal t½ of 35-50 hrs and steady-state plasma concentrations are not achieved until after 7-8 days of administration. Amlodipine is extensively metabolized in the liver; metabolite are mostly excreted in the urine together with <10% of a dose as unchanged drug.
Treatment of mild to moderate hypertension in case of inadequate control with monotherapy.
Usual Initial Dose: 1 tablet daily. May be increased to 2 tablets daily. Similar doses are given in the treatment of stable angina and Prinzmetal's angina.
Hypersensitivity. Patients with cardiogenic shock, recent myocardial infarction, acute unstable angina and chronic stable angina attack.
Use in pregnancy: Losartan is contraindicated in pregnancy.
Losartan should be used with caution in patients with renal artery stenosis. Reduced doses may be required in patients with renal impairment and should be considered in patients with hepatic impairment. Patients with volume depletion (eg, those who have received high-dose diuretic therapy) may experience hypotension, which may be minimized by initiating treatment with a low dose of losartan. Since hyperkalemia may occur, serum potassium concentrations should be monitored, especially in the elderly and patients with renal impairment, and the concomitant use of potassium-sparing diuretics should generally be avoided.
Amlodipine should be used with caution in patients with hypotension, in patients whose cardiac reserve is poor and in those with heart failure has been noted. It should not be used in cardiogenic shock, in patient who have recently suffered a myocardial infarction or in acute unstable angina. It should not be used to treat an angina attack in chronic stable angina. In patients with severe aortic stenosis, it may increase the risk of developing heart failure. Sudden withdrawal might be associated with an exacerbation of angina. The dose may need to be reduced in patients with hepatic impairment. It should be discontinued in patients who experience ischemic pain following its administration.
Use in lactation: Losartan should be used cautiously at all, during breastfeeding.
Use in pregnancy: Losartan is contraindicated in pregnancy.
Use in lactation: Losartan should be used cautiously at all, during breastfeeding.
Adverse effects of losartan have been reported to be usually mild and transient, and include dizziness and dose-related orthostatic hypotension. Hypotension may occur particularly in patients with volume depletion (eg, those who have received high-dose diuretics). Impaired renal function and rarely, rash, angioedema and raised liver enzyme values may occur. Hyperkalemia and myalgia have been reported. Losartan appears less likely than angiotensin-converting enzyme (ACE) inhibitors to cause cough. Other adverse effects that have been reported with angiotensin II receptor antagonists include respiratory tract disorders, back pain, gastrointestinal disturbances, fatigue and neutropenia.
The most common adverse effects are associated with its vasodilator action and often diminish on continued therapy including dizziness, flushing, headache, hypotension, peripheral edema, tachycardia and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain and mental depression have also occurred. A paradoxical increase in ischemic chest pain may occur at the start of treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischemia or transient blindness. There have been reports of rashes (including erythema multiforme), fever and
abnormalities in liver function including cholestasis, due to hyperplasia, myalgia, tremor and impotence have been reported.
May enhance antihypertensive effects of the antihypertensives eg, β-blockers, aldesleukin, antipsychotics, quinidine, carbamazepine, phenytoin, rifampicin, cimetidine and erythromycin.
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.
Amazar FC tab
30's (P17.71/film-coated tab)
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