Renicard^® (Tablets) Instructions for Use

Marketing Authorization Holder

Unichem Laboratories, Ltd. (India)

ATC Code

C09CA01 (Losartan)

Active Substance

Losartan (Rec.INN registered by WHO)

Dosage Forms

	Renicard®	Film-coated tablets, 25 mg: 30 pcs.
		Film-coated tablets, 50 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, biconvex, with a hexagon embossed on one side and a score line on the other.

Excipients: microcrystalline cellulose – 37.2 mg, lactose monohydrate – 18.5 mg, pregelatinized starch – 16 mg, magnesium stearate – 0.8 mg, talc – 2 mg, colloidal silicon dioxide – 0.5 mg.

Shell composition Opadry white (hypromellose 15 cP – 65% w/w, macrogol – 10% w/w, titanium dioxide – 20% w/w, talc – 5% w/w) – 3 mg.

10 pcs. – blisters (3) – cartons.

Film-coated tablets light pink, oblong, biconvex, with a score line on one side.

Excipients: microcrystalline cellulose – 45.6 mg, lactose monohydrate – 24.75 mg, pregelatinized starch – 20 mg, magnesium stearate – 1 mg, talc – 2.9 mg, colloidal silicon dioxide – 0.75 mg.

Shell composition Opadry pink (hypromellose 15 cP – 55% w/w, macrogol – 11% w/w, talc – 10% w/w, titanium dioxide – 23.6% w/w, iron oxide red – 0.4% w/w) – 5 mg.

10 pcs. – blisters (3) – cartons.

Clinical-Pharmacological Group

Angiotensin II receptor antagonist

Pharmacotherapeutic Group

Angiotensin II receptor antagonist

Pharmacological Action

Antihypertensive agent. It is a non-peptide blocker of angiotensin II receptors. It has high selectivity and affinity for AT₁ type receptors (through which the main effects of angiotensin II are mediated). By blocking these receptors, Losartan prevents and eliminates the vasoconstrictive action of angiotensin II, its stimulating effect on aldosterone secretion by the adrenal glands, and some other effects of angiotensin II. It is characterized by a long duration of action (24 hours or more), which is due to the formation of its active metabolite.

Pharmacokinetics

After oral administration, Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It undergoes first-pass metabolism in the liver to form a carboxyl metabolite, which has more pronounced pharmacological activity than Losartan, and a number of inactive metabolites. C_max in plasma for losartan and the active metabolite is reached after 1 hour and 3-4 hours, respectively. Plasma protein binding for losartan and the active metabolite is high – more than 98%.

T_1/2 of losartan and the active metabolite in the terminal phase is about 1.5-2.5 hours and 3-9 hours, respectively. Losartan is excreted in urine and feces (via bile) unchanged and as metabolites. About 35% is excreted in urine and about 60% in feces.

Indications

Arterial hypertension.

Reduction of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a reduction in the combined incidence of cardiovascular mortality, stroke, and myocardial infarction.

Renal protection in patients with type 2 diabetes mellitus with proteinuria – slowing the progression of renal failure, manifested by a reduction in the incidence of hypercreatininemia, the incidence of end-stage chronic renal failure requiring hemodialysis or kidney transplantation, mortality rates, as well as a reduction in proteinuria.

Chronic heart failure (as part of combination therapy, in case of intolerance or ineffectiveness of ACE inhibitor therapy).

ICD codes

Dosage Regimen

For arterial hypertension, initiate therapy with 50 mg orally once daily.

For chronic heart failure, start with a lower dose of 12.5 mg once daily.

For renal protection in type 2 diabetes with proteinuria, the usual maintenance dose is 50 mg once daily.

The therapeutic antihypertensive effect is typically attained within 3 to 6 weeks.

Adjust the dosage based on individual blood pressure response.

If the antihypertensive effect is insufficient, increase the dose to a maximum of 100 mg daily.

Administer the total daily dose of 100 mg as a single dose or as two divided doses of 50 mg each.

For volume-depleted patients, initiate therapy with 25 mg once daily.

In patients with hepatic impairment or a history of liver disease, use a lower initial dose of 25 mg daily.

For patients with intravascular volume depletion, correct this condition prior to administration or use a lower starting dose.

In elderly patients over 65 years of age, dosage adjustment is usually not necessary.

Tablets may be taken with or without food.

Swallow the tablet whole with a sufficient amount of water.

Do not crush or chew the film-coated tablets.

The 25 mg tablet is scored and can be split for dose titration.

The 50 mg tablet is also scored for easier dose adjustment.

Adverse Reactions

Cardiovascular system: dizziness, orthostatic hypotension.

Metabolism: hyperkalemia.

Allergic reactions: angioedema (including swelling of the face, lips, pharynx and/or tongue), urticaria.

Digestive system: diarrhea, increased ALT activity.

CNS: headache.

Dermatological reactions: itching.

Other: impaired renal function, myalgia.

Contraindications

Pregnancy, lactation, children and adolescents under 18 years of age, hypersensitivity to losartan.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

In patients with a history of liver disease, Losartan should be used in low doses. In liver cirrhosis, the plasma concentration of losartan increases significantly.

Use in Renal Impairment

In case of impaired renal function, a dose reduction of losartan may be required.

Pediatric Use

The safety and efficacy of losartan in children have not been established.

Geriatric Use

In elderly patients, blood potassium levels should be regularly monitored during treatment.

Special Precautions

Use with caution in arterial hypotension, reduced circulating blood volume, water-electrolyte imbalance, bilateral renal artery stenosis or stenosis of the artery of a solitary kidney, in renal/hepatic insufficiency.

In patients with fluid and/or sodium deficiency, correction of water-electrolyte imbalances should be performed before starting treatment, or a lower initial dose should be used.

In patients with dehydration (e.g., those receiving high-dose diuretic therapy), symptomatic arterial hypotension may occur at the beginning of treatment with losartan.

In case of impaired renal function, a dose reduction of losartan may be required.

In patients with a history of liver disease, Losartan should be used in low doses. In liver cirrhosis, the plasma concentration of losartan increases significantly.

Blood potassium levels should be regularly monitored during treatment, especially in elderly patients and in patients with impaired renal function.

Concomitant use of losartan with potassium-sparing diuretics should be avoided.

The safety and efficacy of losartan in children have not been established.

Drug Interactions

Concomitant use with diuretics in high doses may cause arterial hypotension.

Concomitant use with potassium preparations, potassium-sparing diuretics increases the risk of hyperkalemia.

Concomitant use with indomethacin may reduce the effectiveness of losartan.

There is a report of lithium intoxication with concomitant use with lithium carbonate.

Concomitant use with orlistat reduces the antihypertensive effect of losartan, which may lead to a significant increase in blood pressure and the development of a hypertensive crisis.

Concomitant use with rifampicin increases the clearance of losartan and reduces its effectiveness.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.