Antoreb

Losartan potassium.

ANTOREB 50 mg Film-Coated Tablet: Each film-coated tablet contains: Losartan Potassium USP 50 mg.
ANTOREB 100 mg Film-Coated Tablet: Each film-coated tablet contains: Losartan Potassium USP 100 mg.

Angiotensin II Receptor Blocker (ARB).
Pharmacology: Pharmacokinetics: Losartan is an oral, specific angiotensin-II receptor (type AT1) antagonist. Angiotensin II binds to the AT1 receptor, which is present in a variety of organs (including vascular smooth muscle, the adrenal gland, the kidneys, and the heart), and causes a number of biological effects. Smooth-muscle proliferation is also stimulated by angiotensin II. It binds exclusively to the AT1 receptor according to binding and pharmacological bioassays. Losartan and its pharmacologically active carboxylic acid metabolite (E-3174), regardless of the source or mechanism of synthesis, block all physiologically significant activities of angiotensin II in vitro and in vivo.
The removal of angiotensin II negative feedback on renin secretion after losartan therapy results in enhanced plasma renin activity. Angiotensin II levels in the blood rise as plasma renin activity rises. Antihypertensive action and decrease of plasma aldosterone levels are maintained despite these increases, demonstrating effective angiotensin II receptor blockage.
Losartan binds selectively to the AT1 receptor and does not bind to or block other hormone receptors or ion channels important in cardiovascular regulation.
Furthermore, losartan does not inhibit ACE (kininase II), the enzyme that degrades bradykinin. Consequently, effects not directly related to blocking the AT1 receptor, such as the potentiation of bradykinin-mediated effects, the generation of oedema (losartan 1.7%, placebo 1.9%) or fatigue (losartan 3.8%, placebo 3.9%), are not associated with losartan.
Losartan potassium significantly lowers proteinuria, fractional excretion of albumin, and IgG in non-diabetic hypertensive patients with proteinuria. Losartan keeps the glomerular filtration rate constant while lowering the filtration fraction. Losartan induces a reduction in serum uric acid (typically less than 24 micromol) that lasts throughout the treatment.
Losartan has no influence on autonomic reflexes or plasma noradrenalin levels over time. In patients with hypertension, losartan potassium at doses up to 150 mg once daily won't produce clinically significant changes in fasting triglycerides, total cholesterol, or HDL cholesterol. Losartan at the same doses had no effect on fasting glucose levels.

Hypertension: Losartan Potassium Tablets are indicated for the treatment of hypertension.
Hypertensive patients with left ventricular hypertrophy: In hypertensive patients with left ventricular hypertrophy a reduced risk of stroke was demonstrated. The data does not support the use of Losartan Potassium Tablets for this indication in black patients.
Nephropathy in Type 2 Diabetic Patients: Indicated for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (urinary albumin to creatinine ratio ≥ 300 mg/g) in patients with type 2 diabetes and a history of hypertension.
In this population, Losartan Potassium Tablets reduce the rate of progression of nephropathy as measured by the occurrence of doubling the serum creatinine or end stage renal disease (need for dialysis or renal transplantation) or death.
Or as prescribed by the physician.

Losartan Potassium Tablets may be administered with or without food.
Losartan Potassium Tablets may be administered with other antihypertensive agents.
Hypertension: The starting and maintenance dose is 50 mg once daily for most patients. The maximal antihypertensive effect is attained 3-6 weeks after initiation of therapy. Some patients may receive an additional benefit by increasing the dose to 100 mg once daily or as prescribed by the physician.

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 the active metabolite can be removed by hemodialysis.

Losartan Potassium Tablets is contraindicated in pregnancy (see USE IN PREGNANCY & LACTATION) and in patients who are hypersensitive to any component of this product.

Hypersensitivity: Angioedema.
Hypotension and electrolyte/fluid imbalance: In patients who are intravascularly volume-depleted (e.g., those treated with high-dose diuretics), symptomatic hypotension may occur. These conditions should be corrected prior to administration of Losartan Potassium Tablets, or a lower starting dose should be used (see DOSAGE & ADMINISTRATION).
Electrolyte imbalances are common in patient with renal impairment, with or without diabetes, and should be addressed. In a clinical study conducted in type 2 diabetic patients with proteinuria, the incidence of hyperkalaemia was higher in the group treated with Losartan Potassium Tablets as compared to the placebo group; however, few patients discontinued therapy due to hyperkalaemia.
Liver Function Impairment: For patients with a history of hepatic impairment, a lower dose should be considered based on pharmacokinetic findings that show considerably elevated plasma concentrations of losartan in cirrhotic patients (see DOSAGE & ADMINISTRATION and Pharmacology: PHARMACOKINETICS under Actions).
Renal Function Impairment: Changes in renal function, including renal failure, have been recorded in susceptible individuals as a result of inhibiting the renin-angiotensin system; these changes in renal function may be reversible with discontinuation of therapy.
In patients with extraordinary renal artery stenosis or stenosis of the artery in the kidney, other medicines that impact the renin-angiotensin system may raise blood urea and serum evidence. Losartan Potassium formulation has shown similar effects.

Pregnancy: When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. When pregnancy is detected, Losartan Potassium Tablets should be discontinued as soon as possible.
Although there is no experience with the use of Losartan Potassium Tablets in pregnant women, animal studies with losartan potassium have demonstrated fetal and neonatal injury and death, the mechanism of which is believed to be pharmacologically mediated through effects on the renin-angiotensin system.
In humans, foetal renal perfusion, which is dependent upon the development of the renin-angiotensin system, begins in the second trimester; thus, risk to the fetus increases if Losartan Potassium Tablets is administered during the second or third trimesters of pregnancy.
Nursing mothers: It is not known whether losartan is excreted in human milk. Because many drugs are excreted in human milk and 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.

Hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole, and erythromycin have all been found to have no clinically significant drug interactions in clinical pharmacokinetic investigations. Rifampicin and fluconazole have been shown to lower the active metabolite levels. The clinical consequences of these interactions have not been evaluated.
Concomitant use of potassium-sparing diuretics (e.g. spironolactone, triamterene, amiloride), potassium supplements, or salt replacements containing potassium might cause an increase in serum potassium, just as other medications that block angiotensin II or its effects.
Lithium excretion may be lowered, just like other medicines that impact sodium excretion. If lithium salts are to be co-administered with angiotensin II receptor antagonists, serum lithium levels should be closely monitored.
Non-steroidal anti-inflammatory drugs (NSAIDs) including selective cyclooxygenase-2 inhibitors (COX-2 inhibitors) may reduce the effect of diuretics and other antihypertensive drugs. Therefore, the antihypertensive effect of angiotensin II receptor antagonists may be attenuated by NSAIDs including selective COX-2 inhibitors.
In some patients with compromised renal function who are being treated with non-steroidal anti-inflammatory drugs including selective cyclooxygenase-2 inhibitors, the co-administration of angiotensin II receptor antagonists may result in a further deterioration of renal function. These effects are usually reversible.

Store at temperatures not exceeding 30°C.
Keep away from direct heart and sunlight exposure.

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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