Losartan Potassium and Hydrochlorothiazide Tablets
Pack: Strip of 10 tablets.
COMPOSITION : Each tablet contains :-
Losartan 50 mg
HCTZ 12.5 mg
Losartan belongs to a class of medications called angiotensin II receptor antagonists. It works by blocking the action of certain natural substances that tighten the blood vessels and also by inhibiting the aldosterone secreting effect of angiotensin II, allowing the blood to flow more smoothly and the heart to pump more efficiently.
Hydrochlorothiazide belongs to class of medications called thiazide diuretics. It acts by eliminating the fluid and salts from the body. It works on the kidneys to produce more urine which removes extra water and certain salts from the body which in turn lowers blood pressure and swelling.
Following oral administration, losartan is well absorbed and undergoes first-pass metabolism, forming an active carboxylic acid metabolite and other inactive metabolites. The systemic bioavailability of losartan tablets is approximately 33%. Mean peak concentrations of losartan and its active metabolite are reached in 1 hour and in 3-4 hours, respectively. There was no clinically significant effect on the plasma concentration profile of losartan when the drug was administered with a standardized meal.
Both losartan and its active metabolite are ≥99% bound to plasma proteins, primarily albumin.The volume of distribution of losartan is 34 litres. Studies in rats indicate that losartan crosses the blood-brain barrier poorly, if at all.
Hydrochlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.
About 14% of an intravenously- or orally-administered dose of losartan is converted to its active metabolite. Following oral and intravenous administration of 14 C-labeled losartan potassium, circulating plasma radioactivity primarily is attributed to losartan and its active metabolite. Minimal conversion of losartan to its active metabolite was seen in about one percent of individuals studied. In addition to the active metabolite, inactive metabolites are formed, including two major metabolites formed by hydroxylation of the butyl side chain and a minor metabolite, an N-2 tetrazole glucuronide.
Plasma clearance of losartan and its active metabolite is about 600 mL/min and 50 mL/min, respectively. Renal clearance of losartan and its active metabolite is about 74 mL/min and 26 mL/min, respectively. When losartan is administered orally, about 4% of the dose is excreted unchanged in the urine, and about 6% of the dose is excreted in the urine as active metabolite. The pharmacokinetics of losartan and its active metabolite are linear with oral losartan
potassium doses up to 200 mg.
Following oral administration, plasma concentrations of losartan and its active metabolite decline polyexponentially with a terminal half-life of about 2 hours and 6-9 hours, respectively. During once-daily dosing with 100 mg, neither losartan nor its active metabolite accumulates significantly in plasma. Both biliary and urinary excretion contribute to the elimination of losartan and its metabolites. Following an oral dose of 14 C-labeled losartan in man, about 35% of radioactivity is recovered in the urine and 58% in the faeces.
Hydrochlorothiazide is not metabolized but is eliminated rapidly by the kidney. When plasma levels have been followed for at least 24 hours, the plasma half-life has been observed to vary between 5.6 and 14.8 hours. At least 61 percent of the oral dose is eliminated unchanged within 24 hours.
INDICATION : Hypertension, Oedema.
DOSAGE: As directed by the physician.
SIDE EFFECTS : Photosensitivity, Dry mouth, Electrolyte imbalance, Hypomagnesaemia, Gastrointestinal complaints like vomiting, Hyperuricemia, Weakness, Hyponatremia, Gout, Arrhythmias, Changes in lipid levels, Drowsiness, Seizure, Drowsiness, Muscle pain, Hypotension, Increased thirst, Hyperglycaemia, Allergic reactions e.g. rash, Lethargy, Hypokalaemia, And headache.
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