Amlodine Plus

Amlodine Plus

Manufacturer:

InnoGen Pharmaceuticals

Distributor:

InnoGen Pharmaceuticals
Full Prescribing Info
Contents
Amlodipine besilate, losartan potassium.
Description
Each film-coated tablet contains: Amlodipine (as besilate) 5 mg, Losartan (as Potassium) 50 mg and Amlodipine (as besilate) 5 mg, Losartan (as Potassium) 100 mg.
Amlodipine + Losartan contains the besilate salt of Amlodipine, a dihydropyridine calcium channel blocker (CCB). 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 3,5-methyl(4RS)-2[(2-aminoethoxy)methyl]-4-(2chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulphonate. Its empirical formula is C20H25ClN2O5.C6H6O3S and its molecular weight is 567.1.
Losartan potassium is an angiotensin II receptor (type ATI) antagonist. Losartan potassium, a non-peptide molecule, is a chemical described as 2-butyl-4-chloro-1-[p-(o-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, such as acetonitrile and methyl ethyl ketone. Oxidation of the 5-Hydroxymethyl group on the imidazole ring in the active metabolite of Losartan.
Action
Pharmacology: Pharmacokinetics: Amlodipine is well absorbed following oral administration with peak blood concentrations occurring after 6 to 12 hours. The bioavailability is about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until 7 to 8 days of administration. Amlodipine is extensively metabolized in the liver; metabolites are mostly excreted in urine together with less than 10% of dose as unchanged drug.
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 hour and 3 to 4 hours, respectively, after an oral dose. Both Losartan and E-3174 are more than 98% bound to plasma proteins. Losartan is excreted in the urine, and in the faeces 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 faeces. The terminal elimination half-lives of Losartan and E-3174 are about 1.5 to 2.5 hours and 3 to 9 hours, respectively.
Indications/Uses
Used in the treatment of mild to moderate hypertension in case of inadequate control with monotherapy.
Dosage/Direction for Use
Usual, initial dose is one (1) tablet daily. Increase if necessary to two (2) tablets daily or as prescribed by the physician.
Similar doses are given in the treatment of stable angina and Prinzmetal's angina or as prescribed by the physician.
Warnings
Hypersensitivity to any component of this product.
Special Precautions
Amlodipine should be used with caution in patients with hypotension, in patients whose cardiac reserve is poor, and in those with heart failure. It should not be used in cardiogenic shock, in patients 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 ischaemic pain following its administration.
Losartan is contraindicated in pregnancy and should be used with care, if at all, during breast feeding. It 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 (for example 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.
Use In Pregnancy & Lactation
Losartan is contraindicated in pregnancy and should be used with care, if at all, during breast feeding.
Adverse Reactions
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 (for example 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 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. They include 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 ischaemic chest pain may occur at the start of the treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia 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.
Overdose maybe associated with bradycardia and hypotension.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
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.
Presentation/Packing
5 mg/50 mg FC tab 30's. 5 mg/100 mg FC tab x 30's.
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