White colored, oval shaped, biconvex film-coated tablets having central break line on one side and plain on another side.
Each film-coated tablet contains: Losartan potassium, USP 100 mg.
Excipients with known effect: This product contains: Lactose: If the patient have been told by the doctor that they have an intolerance to some sugars, contact the doctor before taking this medicinal product. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Sodium benzoate (E211): This medicine contains 0.10 mg of sodium benzoate in each 100 mg tablet. Sodium benzoate may increase jaundice (yellowing of the skin and the eyes) in newborn babies (up to 4 weeks old).
Angiotensin II Receptor Blocker.
Pharmacology: Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)] is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system, and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e.g. vascular smooth muscle, adrenal gland). In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor.
Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin), nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Pharmacokinetics: Losartan is readily absorbed from the GI tract after oral doses, but undergoes substantial first-pass metabolism resulting in a systemic bioavailability of about 33%. It is metabolized to an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than losartan; some inactive metabolites are also formed. Metabolism is primarily by CYP 2C9 and CYP 3A4. Peak plasma concentrations of losartan and E-3174 occur about 1 hour and 3-4 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 feces via bile, as unchanged drug and metabolites. About 4% of an oral dose is excreted unchanged in urine and 6% is excreted in urine as the active metabolite. The terminal elimination half-lives of losartan and E-3164 are about 1.5-2.5 hours and 3-9 hours, respectively.
Used in the management of hypertension, heart failure and in myocardial infarction.
Hypertension: The usual dose is 50 mg once daily.
The maximum effect is achieved in about 3-6 weeks after initiating treatment. The dose may be increased, if necessary, to 100 mg daily in one or two divided doses. An initial dose of 25 mg once daily is suggested for the elderly over 75 years, and for patients with moderate to severe renal impairment (CrCl <20 mL/min), or intravascular fluid depletion. A reduced dose should also be considered for patients with hepatic impairment.
Significant lethality was observed in mice and rats after oral administration of 1000 mg/kg and 2000 mg/kg, respectively, about 44 and 170 times the maximum recommended human dose on a mg/m2 basis. Limited data are available in regard to overdosage in humans. The most likely manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Neither losartan nor its active metabolite can be removed by hemodialysis.
Losartan potassium is contraindicated for coadministration with aliskiren in patients with diabetes.
Fetal toxicity: Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue Losartan potassium as soon as possible.
Hypotension in volume- or salt-depleted patients: In patients with an activated renin-angiotensin system, such as volume- or salt-depleted patients (e.g. those being treated with high doses of diuretics), symptomatic hypotension may occur after initiation of treatment with Losartan potassium.
Renal function deterioration: Changes in renal function including acute renal failure can be caused by drugs that inhibit the renin-angiotensin system and by diuretics. Patients whose renal function may depend in part on the activity of the renin-angiotensin system (e.g. patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, or volume depletion) may be at particular risk of developing acute renal failure on Losartan potassium. Monitor renal function periodically in these patients. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function on Losartan potassium.
Hyperkalemia: Monitor serum potassium periodically and treat appropriately. Dosage reduction or discontinuation of Losartan potassium may be required. Concomitant use of other drugs that may increase serum potassium may lead to hyperkalemia.
Pregnancy Category D: Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue losartan as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimester of pregnancy.
It is not known whether losartan is excreted in human milk, but significant levels of losartan and its active metabolite were shown to be present in rat milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
See table.
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Agents Increasing Serum Potassium: Coadministration of losartan with other drugs that raise serum potassium levels may result in hyperkalemia. Monitor serum potassium in such patients.
Lithium: Increases in serum lithium concentrations and lithium toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists. Monitor serum lithium levels during concomitant use.
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) [Including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors)]: In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, coadministration of NSAIDs, including selective COX-2 inhibitors, with angiotensin II receptor antagonists may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving losartan and NSAID therapy. The antihypertensive effect of angiotensin II receptor antagonists may be attenuated by NSAIDs.
Dual Blockade of the Renin-Angiotensin System (RAS): Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, syncope, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. In general, avoid combined use of RAS inhibitors. Closely monitor blood pressure, renal function, and electrolytes in patients on losartan and other agents that affect the RAS. Do not co-administer aliskiren with losartan in patients with diabetes. Avoid use of aliskiren with losartan in patients with renal impairment (GFR <60 mL/min).
Store at temperatures not exceeding 30°C.
C09CA01 - losartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Cozalyn 100 FC tab 100 mg
100's
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