Each 25 mg film coated tablet contains: Losartan potassium USP 25 mg.
Each 50 mg film coated tablet contains: Losartan potassium USP 50 mg.
Excipients/Inactive Ingredients: 25 mg: Colour: Titanium Dioxide.
50 mg: Colour: Titanium Dioxide & Red Oxide of Iron.
Pharmacology: Pharmacodynamics: Losartan is a nonpeptide angiotensin II receptor antagonist with high affinity and selectivity for the AT receptor, without binding to or blocking other hormone receptors or ion channels important in cardiovascular regulation. Angiotensin II is a potent vasoconstrictor, a primary active hormone of the renin-angiotensin system, and a major determinant of the pathophysiology of hypertension. Losartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by inhibiting the binding of angiotensin II to the AT receptor.
Pharmacokinetics: Following oral administration, bioavailability is approximately 33%. It undergoes first-pass metabolism to form an active carboxylic acid metabolite, (which has greater pharmacological activity than losartan) and some inactive metabolites. About 14% of an intravenously or orally administered dose is converted to its active metabolite. The mean peak concentrations of losartan and its active metabolite are reached in 1 hour and 3-4 hours, respectively. Both losartan and the carboxylic acid metabolite are greater than, or equal to 99% bound to plasma proteins. The distribution volume of losartan is 34 litres. The terminal half-life of losartan is 2 hours and of its active metabolite is 6-9 hours. Losartan is excreted in the urine, and in the faeces, as unchanged drug and metabolites. Following oral dosing, about 35% of the dose is excreted in the urine and about 60% in the faeces. Neither losartan nor the active metabolite can be removed by haemodialysis. Plasma concentrations of losartan are not altered in patients with impaired renal function and a creatinine clearance above 10 ml/min. Compared to patients with normal renal function, the AUC for losartan is approximately 2-fold greater in patients on haemodialysis.
LOSAPAC is indicated for the treatment of hypertension.
Hypertension: Adult Hypertensives: Dosing must be individualized. The usual starting dose of LOSAPAC is 50 mg once daily. A dose of 25 mg may be used in patients with possible depletion of intravascular volume (e.g. patients treated with diuretics) and patients with a history of hepatic impairment. LOSAPAC can be administered once or twice daily with total daily doses ranging from 25 mg to 100 mg.
If the antihypertensive effect measured at trough using once-a-day dosing is inadequate, a twice-a-day regimen at the same total daily dose or an increase in dose may give a more satisfactory response. The effect of losartan is substantially present within one week but in some studies the maximal effect occurred in 3-6 weeks.
If blood pressure is not controlled by losartan alone, a low dose of a diuretic may be added.
No initial dosage adjustment is necessary for elderly patients or for patients with renal impairment, including patients on dialysis.
Pediatric hypertensive patients 6 years or age: The usual recommended starting dose is 0.7 mg/kg once daily (up to 50 mg total). Dosage should be adjusted
according to blood pressure response. Doses above 1.4 mg/kg (or in excess of 100 mg) daily have not been studied in pediatric patients. Losartan is not recommended in pediatric patients <6 years of age or in pediatric patients with glomerular filtration rate <30mL/min/1.73m.
Hypertensive patients with left ventricular hypertrophy: The usual starting dose is 50 mg once daily. Hydrochlorothiazide 12.5 mg daily should be added and/or the dose of LOSAPAC should be increased to 100 mg once daily followed by an increase in hydrochlorothiazide to 25 mg once daily based on blood pressure response.
Nephropathy in type 2 diabetic patients: The usual starting dose is 50 mg once daily. The dose should be increased to 100 mg once daily based on blood pressure response.
The symptoms of an overdosage of LOSAPAC would be hypotension and tachycardia.
Bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted.
Neither LOSAPAC nor the active metabolite can be removed by haemodialysis.
Hypersensitivity to losartan or any of the components of this product.
Women of childbearing age should ensure adequate contraception.
LOSAPAC is contra-indicated in pregnancy and should be used with care, if at all, during breast-feeding.
LOSAPAC should be used with caution in patients with bilateral renal artery stenosis or stenosis of an artery to a single kidney, aortic valve stenosis or hypertrophic obstructive cardiomyopathy.
Symptomatic hypotension may occur after initiation of LOSAPAC. Reduced doses must be considered in patients with hepatic impairment.
Pregnancy: The use of drugs that act directly on the renin-angiotensin system during the second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death. Oligohydramnios has also been reported, presumably resulting from decreased fetal renal function; oligohydramnios in this setting has been associated with fetal limb contractures, craniofacial deformation, and hypoplastic lung development. Prematurity, intrauterine growth retardation, and patent ductus arteriosus have also been reported, although it is not clear whether these occurrences were due to exposure to the drug.
These adverse effects do not appear to have resulted from intrauterine drug exposure that has been limited to the first trimester.
Mothers whose embryos and fetuses are exposed to an angiotensin II receptor antagonist only during the first trimester should be so informed. Nonetheless, when patients become pregnant, physicians should have the patient discontinue the use of LOSAPAC as soon as possible.
LOSAPAC should be discontinued as soon as possible, when pregnancy is suspected.
LOSAPAC should not be used in pregnancy as teratogenicity has been shown in experimental animals.
Lactation: Safety has not been established.
The following side-effects may occur: Blood and lymphatic system disorders:
The following side effects have been reported and frequencies are unknown: Symptomatic anaemia, neutropenia.
Nervous system disorders: More frequent: Headache. Less frequent: Dizziness. Rare: Insomnia. The following side effect has been reported and frequencies are unknown: Migraine.
Cardiac disorders: The following side effect has been reported and frequencies are unknown: Palpitations, tachycardia.
Vascular disorders: The following side effect has been reported and frequencies are unknown: Hypotension.
Respiratory, thoracic and mediastinal disorders: Less frequent: Cough, nasal congestion, pharyngitis, upper respiratory infection. Rare: Sinus disorder.
Gastrointestinal disorder: Less frequent: Diarrhoea. The following side effect has been reported and frequencies are unknown: Dyspepsia, nausea, acute pancreatitis, abdominal pain, taste disturbances complete taste loss.
Hepato-biliary disorders: The following side effect has been reported and frequencies are unknown: Severe acute hepatotoxicity, cholestasis.
Skin and subcutaneous tissue disorders: The following side effect has been reported and frequencies are unknown: Urticaria, rash, atypical cutaneous lymphoid infiltrates. Angioedema (involving swelling of the face, lips, and/or tongue) has been reported in patients treated with LOSAPAC.
Musculoskeletal, connective tissue and bone disorders:
Less frequent: Back pain. Rare: Muscle cramps, leg pain.
The following side effect has been reported and frequencies are unknown: Myalgia.
Renal and urinary disorders: The following side effect has been reported and frequencies are unknown: Impaired renal function.
General disorders and administrative site conditions: Less frequent: Fatigue. The following side effect has been reported and frequencies are unknown: Chest pain, oedema/swelling, asthenia.
Combinations containing any of the following medications, depending on the amount present, may also interact with LOSAPAC.
Non-steroidal anti-inflammatory drugs (NSAIDs) may antagonise the antihypertensive effect of LOSAPAC.
Concurrent use with sympathomimetics may reduce the antihypertensive effects of LOSAPAC.
Potassium-sparing diuretics, potassium containing medication or potassium supplements used concurrently with LOSAPAC may result in hyperkalaemia since reduction of aldosterone production induced by LOSAPAC may lead to elevation of serum potassium.
Store in a dry place at temperature below 30°C.
C09CA01 - losartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
FC tab 25 mg x 10 x 10's. 50 mg x 10 x 10's.
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