LOSTAD 50 Tablet

- Hypertension

- Reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy

- Diabetic nephropathy with an elevated serum creatinine and proteinuria (urinary albumin to creatinine ratio300mg/g) in patients with type 2 diabetes and a history of hypertension. In this population, Lostad 50 reduces 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.

Dosage and Administration

Lostad 50 may be administered orally with or without food, or with other antihypertensive agents.

- Hypertension

Adult: 50mg once daily. The dose may be increased, if necessary, to 100mg daily as a single dose or in two divided doses. The maximum hypotensive effect is achieved in about 3-6 weeks after initiating treatment.

For patients with intravascular volume-depletion (e.g., those treated with high-dose diuretics), a starting dose of 25mg once daily should be considered.

No initial dosage adjustment is necessary for elderly patients or for patients with renal impairment, including patients on dialysis.

A lower dose should be considered for patients with a history of hepatic impairment.

- Hypertensive patients with left ventricular hypertrophy:

50mg once daily. A low dose of hydrochlorothiazide should be added and/or the dose of Lostad 50 should be increased to 100mg once daily based on blood pressure response.

- Renal protection in type2 diabetic patients with proteinuria and hypertension:

50mg once daily. The dose may be increased to 100mg once daily based on blood pressure response. Lostad 50 may be administered with other antihypertensive agents (e.g. diuretics, calcium-channel blockers, alpha or beta-blockers and centrally acting agents) as well as with insulin and other commonly used hypoglycemic agents (e.g. sulfonylureas, glitazones and glucosidase inhibitors).

In patients who are hypersensitive to losartan potassium or to any of its excipients.

- Adverse effects of losartan have been reported to be usually mild to transient, and include dizziness, headache, and dose-related orthostatic hypotension.

- Hypotension may occur particularly in patients with volume depletion (for example those who have received high-dose diuretics).

- Impaired renal function and, rarely, rash, urticaria, pruritus, angioedema, and raised liver enzyme values may occur.

- Hyperkalaemia, myalgia, and arthralgia have been reported.

- Losartan appears less likely than angiotensin-converting-enzyme inhibitors to cause cough.

- Other adverse effects that have been reported with angiotensin Ⅱreceptor antagonists include respiratory-tract disorders, back pain, gastrointestinal disturbances, fatigue and neutropenia.

- Rhabdomyolysis has been reported rarely.

See the package insert about the details below:

- No significant drug-drug pharmacokinetic interactions have been found in interaction studies with hydrochlorothiazide, digoxin, warfarin, cimetidine and phenobarbital.

- Rifampin,

-Fluconazole

- Potassium-sparing diuretics (e.g. spironolactone, triamterene, amiloride), potassium supplements, salt substitutes containing potassium

- NSAIDs

See the package insert about the details:

Pregnancy

When pregnancy is detected, losartan should be discontinued as soon as possible.

Lactation

A decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

- Losartan should be used with caution in patients with renal artery stenosis.

- Losartan is excreted in urine and in bile and reduced doses may therefore be required in patients with renal impairment and should be considered in patients with hepatic impairment.

- Patients with volume depletion (for example those who have received high-dose diuretic therapy) may experience hypotension; volume depletion should be corrected before starting therapy, or a low initial dose should be used.

- Since hyperkalaemia may occur, serum-potassium concentrations should be monitored, especially in the elderly and patients with renal impairment, and the concomitant use of potassium-sparing diuretic should generally be avoided.

Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensinⅡby selectively blocking the binding of angiotensinⅡto the AT, receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland).

The active metabolite is 10-40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor.

Neither losartan nor its active metabolite inhibits angiotensin-converting-enzyme (kinaseⅡ, the enzyme that converts angiotensinⅠto angiotensinⅡand degrades bradykinin): nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.