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Zylovaa-H

 

COMPOSITION
Zylovaa-H Tablet 50/12.5mg:
Each film-coated tablet contains 50mg Losartan Potassium and 12.5mg Hydrochlorothiazide
Zylovaa-H Tablet 100/25mg:
Each film-coated tablet contains 100mg Losartan Potassium and 25mg Hydrochlorothiazide


PHARMACODYNAMICS
The components of losartan-hydrochlorothiazide have been shown to have an additive effect on blood-pressure reduction, reducing blood pressure to a greater degree than either component alone. This effect is thought to be a result of the complimentary actions of both components.

 

Further, as a result of its diuretic effect, hydrochlorothiazide increases plasma-renin activity, increases aldosterone secretion, decreases serum potassium, and increases the levels of angiotensin II. Administration of losartan blocks all the physiologically relevant actions of angiotensin II and through inhibition of aldosterone could tend to attenuate the potassium loss associated with the diuretic.


Losartan has been shown to have a mild and transient uricosuric effect. Hydrochlorothiazide has been shown to cause modest increases in uric acid; the combination of losartan and hydrochlorothiazide tends to attenuate the diuretic-induced hyperuricaemia.


PHARMACOKINETICS
Absorption
Losartan
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 standardised meal.


Distribution
Losartan
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
Hydrochlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.


Metabolism
Losartan
About 14% of an intravenously or orally-administered dose of losartan is converted to its active metabolite. 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.


Elimination
Losartan
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 excretions contribute to the elimination of losartan and its metabolites.


Hydrochlorothiazide
Hydrochlorothiazide is not metabolised 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% of the oral dose is eliminated unchanged within 24 hours.


Characteristics in patients
Losartan-Hydrochlorothiazide
The plasma concentrations of losartan and its active metabolite and the absorption of hydrochlorothiazide in elderly hypertensives are not significantly different from those in young hypertensives.

 

Losartan
Following oral administration in patients with mild to moderate alcoholic cirrhosis of the liver, plasma concentrations of losartan and its active metabolite were, respectively, 5-fold and 1.7-fold greater than those seen in young male volunteers. Plasma concentrations of losartan are not altered in patients with creatinine clearance above 10 ml/min.


Neither losartan nor the active metabolite can be removed by haemodialysis.


INDICATIONS
Zylovaa-H is indicated for the treatment of hypertension, for patients in whom combination therapy is appropriate.


In hypertensive patients with left ventricular hypertrophy, a reduced risk of stroke was demonstrated with losartan administered usually in combination with hydrochlorothiazide.


DOSAGE AND ADMINISTRATION
To be administered orally.
Fixed dose combination is not indicated for initial therapy.


Zylovaa-H may be administered with or without food.
Zylovaa-H may be administered with other antihypertensive agents.


Treatment of Hypertension
The usual starting and maintenance dose is 1 tablet Zylovaa-H 50/12.5mg (losartan potassium 50mg/ hydrochlorothiazide 12.5mg) once daily for most patients. For patients who do not respond adequately, the dosage may be increased to 2 tablets Zylovaa-H 50/12.5mg (losartan potassium 50mg/ hydrochlorothiazide 12.5mg) or 1 tablet Zylovaa-H 100/25mg (losartan potassium 100mg/ hydrochlorothiazide 25mg) once daily. The maximum dose is 2 tablets Zylovaa-H 50/12.5mg (Iosartan potassium 50mg/ hydrochlorothiazide 12.5mg) or 1 tablet Zylovaa-H 100/25mg (losartan potassium 100mg/ hydrochlorothiazide 25mg). In general, the antihypertensive effect is attained within three weeks after initiation of therapy.


Zylovaa-H should not be initiated in patients who are intravascularly volume-depleted (e.g. those treated with high-dose diuretics).


Zylovaa-H is not recommended for patients with severe renal impairment (creatinine clearance ≤30ml/min) or for patients with hepatic impairment.


No initial dosage adjustment of Zylovaa-H is necessary for elderly patients. Zylovaa-H Tablet 100/25mg should not be used as initial therapy in elderly patients.


Reduction in the risk of stroke in hypertensive patients with left ventricular hypertrophy
The usual starting dose is 50mg of losartan once daily. If goal blood pressure is not reached with losartan 50mg, therapy should be titrated using a combination of losartan and a low dose of hydrochlorothiazide (12.5mg) and, if needed the dose should then be increased to losartan 100mg and hydrochlorothiazide 12.5mg once daily. If necessary, the dose should be increased to losartan 100mg and hydrochlorothiazide 25mg daily. Zylovaa-H Tablet 50/12.5mg and 100/25mg are suitable alternative formulations in patients who would otherwise be treated concomitantly with losartan plus hydrochlorothiazide


CONTRAINDICATIONS
Zylovaa-H is contraindicated in:
Patients who are hypersensitive to any component of this product.
Patients with anuria.
Patients who are hypersensitive to other sulfonamide-derived drugs


WARNINGS AND PRECAUTIONS
Losartan-hydrochlorothiazide
Hypersensitivity: Angioedema (See Side Effects)


Hepatic and renal impairment: Losartan-hydrochlorothiazide is not recommended for patients with hepatic impairment or severe renal impairment (creatinine clearance ≤30ml/min). (See Dosage and Administration)


Losartan
Renal function impairment
As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function including renal failure have been reported in susceptible individuals; as with other drugs 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 or stenosis of the artery to a solitary kidney. These changes in renal function may be reversible upon discontinuation of therapy.


Hydrochlorothiazide
Hypotension and electrolyte/fluid imbalance: Symptomatic hypotension may occur in some patients. Patients should be observed for clinical signs of fluid or electrolyte imbalance, e.g. volume depletion, hyponatremia, hypochloremic alkalosis, hypomagnesemia or hypokalemia which may occur during intercurrent diarrhea or vomiting. Periodic determination of serum electrolytes should be performed at appropriate intervals in such patients.

Metabolic and endocrine effects: Thiazide therapy may impair glucose tolerance. Dosage adjustment of antidiabetic agents, including insulin, may be required. (See Drug Interactions). Thiazides may decrease urinary calcium excretion and may cause intermittent and slight elevation of serum calcium. Marked hypercalcaemia may be evidence of hidden hyperparathyroidism. Thiazides should be discontinued before carrying out tests for parathyroid function.

Increases in cholesterol and triglyceride levels may be associated with thiazide diuretic therapy.

Thiazide therapy may precipitate hyperuricaemia and/or gout in certain patients. Because losartan decreases uric acid, losartan in combination with hydrochlorothiazide attenuates the diuretic-induced hyperuricaemia.

Other: In patients receiving thiazides, hypersensitivity reactions may occur with or without a history of allergy or bronchial asthma. Exacerbation or activation of systemic lupus erythematosus has been reported with the use of thiazides.

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