Losartan Potassium

FORMULATION :
Each film-coated tablet contains:
Losartan Potassium LISP

PHARMACOKINETICS
Losartan is readily absorbed from the gastrointestinal tract, but undergoes substantial first-pass metabolism resulting in a systemic bioavailability of about 33%. It is metabolized to an active carboxylic acid metabolite which has greater pharmacological activity than losartan; some inactive metabolites are also formed, Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and E-3174 occur about I 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 4% of the dose is excreted in urine as the active metabolite. The terminal elimination half-lives of losartan and E-3174 are about I. 5 to 2.5 hours and 3 to 9 hours, respectively.

INDICATIONS
It is used in the management of hypertension, particularly in patients who develop cough with ACE inhibitors and to reduce the risk of stroke in patients with left ventricular hypertrophy, and in the treatment of diabetic nephropathy. It is also used in heart failure and in myocardial infarction.

DOSAGE AND ADMINISTRATION
Hypertension: 50 mg to 100 mg daily as a single dose or in two divided doses. Patients with Intravascular Fluid Depletion: An initial dose of 25 mg once daily should be given. Childrens aged 6 years or overwith Hypertension : An initial dose of 700 micrograms/kg once daily, with a maximum 50 mg. Diabetic Nephropathy : 50 mg once daily, increased to 100 mg once daily depending on the bloodpressure. Or as prescribed by the physician.

CONTRAINDICATIONS
Losartan Potassium is contraindicated in pregnancy and in patients who are hypersensitive to any component of this product.

PRECAUTIONS
Losartan is contraindicated in pregnancy. It should be used with caution in patients with renal artery stenosis. Losartan is excreted in urine and in bile and reduced doses may therefore 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; volume depletion should be corrected before starting therapy, or a low initial dose should be used. 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.

Pregnancy
Losartan is contraindicated in pregnancy since it has been associated with fetal toxicity in animal studies and other drugs that act on the renin-angiotensin system, such asACE inhibitors, have been associated with fetal toxicity in humans. Oligohydramnios with subsequent fetal death occurred in a patient who received losartan during weeks 20 to 31 of pregnancy; the effect on the fetus were similar to those reported with ACE inhibitors. A number of similar cases have subsequently been reported with losartan, candesartan and valsartan.

ADVERSE EFFECTS
Adverse effects of losartan include dizziness, headache, 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, urticaria, pruritus, angioedema, and raised liver enzyme values may occur. Hyperkalemia, myalgia, and arthralgia have been reported. Losartan appears less likely than ACE inhibitors to cause cough. Other adverse effects that have been reported with angiotensin Il receptor antagonists include respiratory-tract disorders, back pain, gastrointestinal disturbances, fatigue, and neutropenia.

CAUTION
Foods, Drugs, Devices and CosmeticsAct prohibits dispensing without prescription.

STORAGE CONDITION
STORE AT TEMPERATURES NOT EXCEEDING 300C.

Keep all medicines out of children’s reach.

AVAILABILITY
Alu/AIu blister pack of I o’s (Box of 30’s).

“For suspected adverse drug reaction, report to the FDA: www.fda.gov.ph“.