LOSARGEN 50™ Losartan Potassium Tablets 50mg
Description, Composition, Pharmacological action, Pharmacokinetics: absorption, distribution, biotransformation, elimination, pharmacokinetics in paediatrics, Indication, Dosage and administration, Contraindications, Precaution and warnings, Pregnancy and lactation effects, Drug inetractions, Adverse effects, Overdosage and treatment, Storage, Presentation, Marketer, Licence owner and Manufacturer of Losargen Tablet Medicine for Hypertension.
Losargen is an angiotension II receptor (type AT) antagonist. It is a prodrug and requires activation in the liver to exert its pharmacological activity. It is blue coloured, STD concave, film coated tablets having break line on one side and plain on other side.
Each film coated tablet contains
Losartan Potassium 50mg
Losargen is a synthetic oral angiotensin-II receptor (type AT1) antagonist. Angiotensin II, a potent vasoconstrictor, is the primary active hormone of the renin/angiotensin system and an important determinant of the pathophysiology of hypertension. Angiotensin II binds to the AT1 receptor found in many tissues (e.g. vascular smooth muscle, adrenal gland, kidneys and the heart) and elicits several important biological actions, including vasoconstriction and the release of aldosterone. Aagiotensin II also stimulates smooth muscle cell proliferation.
Following oral administration, losargen is well absorbed and undergoes first-pass metabolism, forming an active carboxylic acid metabolite and other inactive metabolites.
Both losartan and its active metabolite are 99% bound to plasma proteins, primarily albumin. The volume of distribution of losartan is 34 litres.
About 14% of an intravenously or orally administered dose of losargen is converted to its active metabolite. In addition to the active metabolite, inactive metabolites are formed.
Plasma clearance of losargen and its active metabolite is about 600mL/min and 50mL/min, respectively. Both biliary and urinary excretion contribute to the elimination of losartan and its metabolites.
Pharmacokinetics in paediatric patients
The pharmacokinetics of losartan have been investigated in 50 hypertensive paediatric patients > 1 month to < 16 years of age following once daily oral administration of approximately 0.54 to 0.77mg/kg of losartan (mean doses).
Losargen is used alone or in combination with other classes of antihypertensive agent in management of hypertension. It is considered one of the several preferred antihypertensive drug for the initial management of hypertension in patients with chronic renal failure, diabetes mellitus and/or heart failure.
Losargen also is used in the management of diabetic nephropathy manifested by elevated serum creatinine and proteinuria (urinary albumin to creatinine ratio of 300mng/g or greater) in patient with type 2 diabetic mellitus and hypertension.
Congestive Heart Failure
Losargen can also be used in management of congestive heart failure. It is used in combination with other drugs for the management of (CHF).
DOSAGE AND ADMINISTRATION
Losargen is administered orally. Although food may decrease the rate of absorption of Losargen and peak concentration achieved, however the magnitude of effect is not clinically important.
Dosage Modification of losargen is not necessary for geriatric patients nor other adults with renal impairment including those undergoing hemodialysis.
Dosage of losargen must be individualized and adjusted according to blood pressure response. Substantial therapeutic response to losartan generally occurs within 1 week of treatment initiation, but in some studies the maximum therapeutic response occurred in 3-6 weeks. The usual initial dosage of losargen in adults is 50mg daily; lower initial dose (e.g. 25mg daily) maybe used in patients with possible depletion of intravascular volume including those receiving a diuretic or with hepatic impairment the usual maintenance dose is 25-100mg given once or in 2 divided doses daily.
For the management of diabetic nephropathy in patients with type 2 diabetic mellitus, the usual initial adult dosage of Losargen is 50mg once daily. Dosage of losargen may be increased to 100mg once daily based on blood pressure response.
Losargen tablet is contra- indicated in patients who are hypersensitive to the drug. It is also contra-indicated in 2nd and 3rd trimester of pregnancy.
Safety and efficacy of Losargen in paediatric patients younger them l8years of age have not been established.
Epidemiological evidence regarding the risk of teratogenicity following exposure to ACE inhibitors during the first trimester of pregnancy has not been conclusive; however a small increase in risk cannot be excluded. Whilst there is no controlled epidemiological data on the risk with Angiotensin II Receptor Inhibitors (AIIRAs), similar risks may exist for this class of drugs. Unless continued AIIRA therapy is considered essential, patients planning pregnancy should be changed to alternative antihypertensive treatments which have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with AIIRAs should be stopped immediately and, if appropriate, alternative therapy should be started.
Because no information is available regarding the use of losartan during breastfeeding, losartan is not recommended and alternative treatments with better established safety profiles during breast-feeding are preferable, especially while nursing a newborn or preterm infant.
Diuretics, other hypertensive potentiate the hypotensive effect of Losartan. Potassium sparing diuretics, potassium supplements, increases the risk of hyperkalemia.
NSAIDS may blunt hypotensive effect of losartan, cytochrome P450 inhibitors like ketoconazole increase the AUC of losartan by 18% but has no effect on its active metabolite. Phenobarbitone; result in 20% reduction in AUC of Losartan and its active metabolites.
Headache, dizziness, asthenia or fatigue. Rarely angioedema, first dose hypertension, transient elevation of liver transaminases and hyperkalaemia.
OVERDOSAGE AND TREATMENT
Any medication taken in excess can have serious consequences, if you suspect an overdose seek medical attention immediately. Information concerning losargen overdosage is limited. However, hypotension (low blood pressure) and abnormally rapid or slow heartbeat maybe signs of an overdose.
Store at 25oC. Keep all medicines away from reach of children.
10 blisters of 10 tablets in a carton.
NAFDAC Reg. No.: A4-1908
JB Pharmaceuticals Ltd.
408, Commercial Avenue, Sabo Yaba,
Manufactured Under License with
Celogen Pharma Pvt. Ltd., Navi Mumbai, India.
Medibios Laboratories Pvt. Ltd.,
Plot No. J-76, MIDC, Tarapur, India.