Baczartan

White to off white colored, round, biconvex, film coated tablets, plain on both sides.
Each film-coated tablet contains: Losartan Potassium USP 50 mg.

Angiotensin II Receptor Blocker.
Pharmacology: Pharmacodynamics: Losartan is orally active, non-peptide angiotensin II receptor antagonist. Losartan and its active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II selectively blocking the binding of angiotensin II to the AT, receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland).
Pharmacokinetics: 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, which has greater pharmacological activity than Losartan and some inactive metabolites. 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 feces via bile, as an unchanged drug and metabolites. Following oral dosing about 35% of the dose is excreted in the urine and about 60% in the feces. The terminal elimination half-lives of Losartan and E-3174 are about 1.5 to 2.5 hours and 3 to 9 hours respectively.

Used in the management of hypertension.

Losartan is given orally as the potassium salt. The maximum hypotensive effect is achieved in about 3 to 6 weeks after starting the treatment.
In hypertension, the usual dose of Losartan Potassium is 50 mg once daily, if necessary, increased to 100 mg daily as a single dose or in two divided doses.
An initial dose of 25 mg once daily should be given to patients with intravascular fluid depletion.
Children weighing 20-50 kg is 25 mg once daily. Children aged 6 years and over may be given an initial dose of 700 mcg/kg once daily with a maximum of 50 mg adjusted according to response.
In diabetic nephropathy, Losartan Potassium is given in an initial dose of 50 mg daily, increased to 100 mg once daily depending on the blood pressure. Or as prescribed by the physician.

Symptoms of Intoxication: Limited data are available with regard to overdose in humans. The most likely manifestation of overdose would be hypotension and tachycardia. Bradycardia could occur from parasympathetic (vagal) stimulation.
Treatment of Intoxication: If symptomatic hypotension should occur, supportive treatment should be instituted.
Measures depend on the time of medicinal product intake and the kind and severity of symptoms. Stabilization of the cardiovascular system should be given priority. After oral intake, the administration of a sufficient dose of activated charcoal is indicated. Afterward, close monitoring of the vital parameters should be performed. Vital parameters should be corrected if necessary.
Neither Losartan nor the active metabolite can be removed by hemodialysis.

Hypersensitivity to Losartan or any of the components of this product.

Hypersensitivity.
Angioedema: Patients with a history of angioedema (swelling of the face, lips, throat, and/or tongue) should be closely monitored.
Hypotension and Electrolyte/Fluid Imbalance: Symptomatic hypotension, especially after the first dose and after increasing the dose, may occur in patients who are volume- and/or sodium-depleted by vigorous diuretic therapy, dietary salt restriction, diarrhea, or vomiting. These conditions should be corrected prior to administration of losartan, or a lower starting dose should be used. This also applies to children 6 to 18 years of age.
Electrolyte imbalances: Electrolyte imbalances are common in patients with renal impairment, with or without diabetes, and should be addressed. In a clinical study conducted in type 2 diabetic patients with nephropathy, the incidence of diarrhea was higher in the group treated with losartan as compared to the placebo group. Therefore, the plasma concentrations of potassium as well as creatinine clearance values should be closely monitored, especially in patients with heart failure and a creatinine clearance between 30-50 mL/min should be closely monitored.
The concomitant use of potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other drugs that may increase serum potassium (e.g., trimethoprim-containing products) with losartan is not recommended.
Renal transplantation: There is no experience in patients with recent kidney transplantation.
Primary hyperaldosteronism: Patients with primary aldosteronism generally will not respond to antihypertensive medicinal products acting through inhibition of the renin-angiotensin system. Therefore, the use of losartan is not recommended.
Coronary heart disease and cerebrovascular disease: As with any antihypertensive agents, excessive blood pressure decrease in patients with ischaemic cardiovascular and cerebrovascular disease could result in a myocardial infarction or stroke.
Heart failure: In patients with heart failure, with or without renal impairment, there is - as with other medicinal products acting on the renin-angiotensin system - risk of severe arterial hypotension, and (often acute) renal impairment.
There is no sufficient therapeutic experience with losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA class IV) as well as in patients with heart failure and symptomatic life-threatening cardiac arrythmias. Therefore, losartan should be used with caution in these patient groups. The combination of losartan with a beta-blocker should be used with caution.
Aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy: As with other vasodilators, special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.
Excipients: This medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
Other warnings and precautions: As observed for angiotensin-converting enzyme inhibitors, losartan and the other angiotensin antagonists are apparently less effective in lowering blood pressure in black people than in non-blacks, possibly because of higher prevalence of low-renin states in the black hypertensive population.
Dual blockade of the renin-angiotensin-aldosterone system (RAAS): There is evidence that the concomitant use of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of hypotension, hyperkalemia, and decreased renal function (including acute renal failure). Dual blockade of RAAS through the combined use of ACE inhibitors, angiotensin II receptor blockers, or aliskiren is therefore not recommended.
If dual blockade therapy is considered absolutely necessary, this should only occur under specialist supervision and subject to frequent close monitoring of renal function, electrolytes and blood pressure.
ACE inhibitors and angiotensin II receptor blockers should not be used concomitantly in patients with diabetic nephropathy.
Losartan is contraindicated in pregnancy and in breastfeeding.
It should be used with caution in patients with renal artery stenosis.
Patients with volume depletion may experience hypotension.
Since hyperkalemia may occur, serum-potassium concentrations should be monitored, especially in the elderly and patients with renal impairment.
Hepatic Impairment: Based on pharmacokinetic data which demonstrate significantly increased plasma concentrations of losartan in cirrhotic patients, a lower dose should be considered for patients with a history of hepatic impairment. There is no therapeutic experience with losartan in patients with severe hepatic impairment. Therefore, losartan must not be administered to patients with severe hepatic impairment.
Losartan is not recommended in children with hepatic impairment.
Renal Impairment: As a consequence of inhibiting the renin-angiotensin system, changes in renal function including renal failure have been reported (in particular, in patients whose renal function is dependent on the renin-angiotensin-aldosterone system such as those with severe cardiac insufficiency or pre-existing renal dysfunction). As with other medicinal products that affect the renin-angiotensin-aldosterone system, increases in blood urea and serum creatinine have also been reported in patients with bilateral renal artery stenosis of the artery to a solitary kidney; these changes in renal function may be reversible upon discontinuation of therapy. Losartan should be used with caution in patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney.
Use in pediatric patients with renal impairment: Losartan is not recommended in children with glomerular filtration rate <30 mL/min/1.73 m² as no data are available. Renal function should be regularly monitored during treatment with losartan as it may deteriorate. This applies particularly when losartan is given in the presence of other conditions (fever, dehydration) likely to impair renal function.
Concomitant use of losartan and ACE inhibitors has been shown to impair renal function. Therefore, concomitant use is not recommended.
Use in Pregnancy: See Use in Pregnancy & Lactation for further information.

Pregnancy: Losartan should not be initiated during pregnancy. Unless continued losartan therapy is considered essential, patients planning pregnancy should be changed to alternative anti-hypertensive treatments that have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with losartan should be stopped immediately, and, if appropriate, alternative therapy should be started.
The use of losartan is not recommended during the first trimester of pregnancy. The use of losartan is contraindicated during the 2^nd and 3^rd trimester of pregnancy.
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 medicinal products. Unless continued AIIRA therapy is considered essential, patients planning pregnancy should be changed to alternative anti-hypertensive treatments that have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with losartan should be stopped immediately and, if appropriate, alternative therapy should be started.
Exposure to AIIRA therapy during the second and third trimesters is known to induce human fetotoxicity (decreased renal function, oligohydramnios, skull ossification retardation) and neonatal toxicity (renal failure, hypotension, hyperkalemia).
Should exposure to losartan have occurred from the second trimester of pregnancy, an ultrasound check of renal function and skull is recommended.
Infants whose mothers have taken losartan should be closely observed for hypotension.
Breastfeeding: 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 breastfeeding are preferable, especially while nursing a newborn or preterm infant.

Adverse drug reactions of Losartan have been reported to be usually mild and transient and include dizziness and dose-related orthostatic hypotension.
Impaired renal function and rarely rash, angioedema and raised alanine aminotransferase may occur.
Hyperkalemia, myalgia and arthralgia are also included in side effects.
Other adverse drug reactions of angiotensin II receptor antagonists include respiratory tract disorders, back pain, gastrointestinal disturbances, fatigue, neutropenia, and rhabdomyolysis.

The antihypertensive effects of Losartan may be potentiated by drugs or other agents that lower blood pressure.
NSAIDs should be used with caution in patients taking Losartan as the risk of renal impairment may be increased.
NSAIDs may also attenuate the hypotensive effect of Losartan.
Losartan and some other angiotensin II receptor antagonists are metabolized by cytochrome P450 isoenzyme and interactions may occur with drugs that affect these enzymes.

Store at temperatures not exceeding 30°C.

Angiotensin II Antagonists

C09CA01 - losartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.

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