Losacar-H

Each film-coated tablet contains: Losartan potassium USP 50 mg and Hydrochlorothiazide BP 12.5 mg.

Pharmacology: Losartan antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the angiotensin II receptor (AT1 receptor) in vascular smooth muscle and the adrenal gland, producing decreased BP; hydrochlorothiazide inhibits reabsorption of sodium and chloride in ascending loop of Henle and early distal tubules.
Pharmacokinetics: It is readily absorbed from the gastro-intestinal 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(EXP-3174), which has greater pharmacological activity than losartan, and some inactive metabolites. Peak plasma concentrations of losartan & E-9174 occur 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. It is excreted in the urine and in the feces via bile, as unchanged drug metabolites.

Used in the management of hypertension not adequately controlled by individual components, losartan or hydrochlorothiazide alone.

The usual starting dose of losartan 50 mg once daily, with 25 mg recommended for patients with intravascular volume depletion (e.g. patient treated with diuretics). Losartan can be administered once or twice daily at total daily dose of 25 to 100 mg.
Hydrochlorothiazide is effective in dose of 12.5 mg to 50 mg once daily and can be given at doses of 12.5 to 25 mg as combination therapy with Losartan Potassium. To minimize the dose independent side effects, it is usually appropriate to begin combination therapy only after a patient has failed to achieve the desired effect with monotherapy; or as prescribed by the physician.

Anuria; hypersensitivity to other sulfonamide-derivatives or any component of product.

When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.
Renal Function: Use with caution.
Hepatic Function: Do not use.
Use in Children: Safety and efficacy not established.

Pregnancy: Category C (first trimester); Category D (second and third trimester).
Lactation: Undetermined (losartan); excreted in breast milk (hydrochlorothiazide).

Cardiovascular: Palpitations; orthostatic effects, angina pectoris, arrhythmias (eg, atrial fibrillation, sinus bradycardia, tachycardia, ventricular tachycardia, ventricular fibrillation), CVA, hypotension, MI, second-degree AV block (losartan); orthostatic hypotension (hydrochlorothiazide).
CNS: Dizziness; syncope, anxiety, ataxia, confusion, depression, dream abnormality, hyperesthesia, insomnia, decreased libido, memory impairment, migraine, nervousness, panic disorder, paresthesia, peripheral neuropathy, sleep disorder, sleep disorder, somnolence, tremor, vertigo (losartan); restlessness (hydrochlorothiazide).
Dermatologic: Rash; alopecia, dermatitis, dry skin, ecchymosis, erythema, flushing, photosensitivity, pruritus, sweating, urticaria (losartan); photosensitivity, urticaria, necrotizing angiitis (vasculitis and cutaneous vasculitis), erythema multiforme (eg, Stevens-Johnson syndrome), exfoliative dermatitis (eg, toxic epidermal necrolysis), purpura (hydrochlorothiazide).
EENT: Sinusitis; cough; nasal congestion, angioedema, pharyngeal discomfort, rhinitis, blurred vision, burning/stinging in the eyes, conjunctivitis, decreased visual acuity, taste perversion, tinnitus (losartan); transient blurred vision, xanthopsia (hydrochlorothiazide).
GI: Abdominal pain; anorexia, constipation, dental pain, dry mouth, dyspepsia, flatulence, gastritis, vomiting (losartan); pancreatitis, sialadenitis, cramping, gastric irritation (hydrochlorothiazide).
Genitounitary: Impotence, nocturia, urinary frequency, UTI (losartan); glucosuria, renal failure, renal dysfunction, interstitial nephritis (hydrochlorothiazide).
Hematologic: Anemia (losartan); aplastic anemia, agranulocytosis, leukopenia, hemolytic anemia, thrombocytopenia (hydrochlorothiazide).
Hepatic: Jaundice (intrahepatic cholestatic jaundice) (hydrochlorothiazide).
Metabolic: Edema; gout (losartan); hyperglycemia, hyperuricemia (hydrochlorothiazide).
Respiratory: Upper respiratory tract infection; dyspnea, epistaxis, respiratory congestion (losartan); respiratory distress (eg, pneumonitis, pulmonary edema) (hydrochlorothiazide).

Losartan Potassium: Fluconazole: Losartan plasma levels may be elevated, increasing the anti-hypertensive and adverse effects.
Lithium: Plasma levels of lithium may be elevated, increasing the pharmacologic and adverse effects.
Rifamycins (eg, rifampin): Losartan plasma levels may be reduced, decreasing the anti-hypertensive effects.
Potassium-sparing diuretics (e.g. spironolactone), potassium supplements, salt substitutes containing potassium: May lead to increased serum potassium.
Hydrochlorothiazide: Alcohol, barbiturates, narcotics: Increased risk of orthostatic hypotension.
Antidiabetic agents: Dose adjustments of antidiabetic agent may be needed.
Anti-hypertensives: Actions of other antihypertensive agents may be potentiated.
Cholestyramine, colestipol resins: Absorption of hydrochlorothiazide may be impaired.
ACTH, corticosteroids: Increased risk of electrolyte depletion (eg, hypokalemia).
Pressor amines (eg, norepinephrine): Decreased response to pressor amine.
Nondepolarizing skeletal muscle relaxants (eg, tubocurarine): Responsiveness to muscle relaxant may be increased.
Lithium: Plasma levels of lithium may be elevated, increasing the risk of toxicity.
NSAIDs: Antihypertensive, diuretic, and natriuretic effects of hydrochlorothiazide may be reduced.

Store at temperatures not exceeding 30°C.

Angiotensin II Antagonists / Diuretics

C09DA01 - losartan and diuretics ; Belongs to the class of angiotensin II receptor blockers (ARBs) in combination with diuretics. Used in the treatment of cardiovascular disease.

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