Lozap Plus, 50 mg+12, 5 mg 90 pcs

Lozap plus – hypotensive, diuretic.

Pharmacodynamics

A combined drug, has a hypotensive effect. It contains potassium losartan, an angiotensin II receptor antagonist (AT1 subtype), and hydrochlorothiazide, a diuretic.

Lozartan is a specific angiotensin II receptor antagonist (AT1 subtype).

It does not inhibit kinase II, an enzyme that degrades bradykinin. Reduces RPS, blood concentrations of adrenaline and aldosterone, BP, pressure in the small circle of circulation; reduces post-load, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure.

Hydrochlorothiazide is a thiazide diuretic. It reduces Na+ reabsorption, increases urinary excretion of K+, hydrogen carbonate and phosphate. Lowers BP by reducing the blood pressure, changing the reactivity of the vascular wall, reducing the pressor effect of vasoconstrictors.

Pharmacokinetics

Lozartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It has a “first pass” effect through the liver and is metabolized by carboxylation to form the active metabolite. Binding with blood plasma proteins is 99%.

The time to reach Cmaxlozartan is 1 hour, the active metabolite – 3-4 hours after oral administration. T1/2 is 1.5-2 hours, and its main metabolite – 3-4 hours respectively. About 35% of the dose is excreted with the urine, about 60% – through the intestine.

Hydrochlorothiazide is rapidly absorbed from the gastrointestinal tract. T1/2 is 5.8-14.8 hours. It is not metabolized by the liver. About 61% is excreted unchanged by the kidneys.

Indications

Arterial hypertension (in patients for whom combination therapy is optimal).

Pharmacological effect

Lozap plus – hypotensive, diuretic.

Pharmacodynamics

The combined drug has a hypotensive effect. Contains losartan potassium – an angiotensin II receptor antagonist (AT1 subtype) – and hydrochlorothiazide – a diuretic.

Losartan is a specific angiotensin II receptor antagonist (AT1 subtype).

Does not inhibit kinase II, an enzyme that destroys bradykinin. Reduces peripheral vascular resistance, blood concentrations of adrenaline and aldosterone, blood pressure, pressure in the pulmonary circulation; reduces afterload and has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure.

Hydrochlorothiazide is a thiazide diuretic. Reduces the reabsorption of Na+, increases the excretion of K+, bicarbonate and phosphates in the urine. Lowers blood pressure by reducing blood volume, changing the reactivity of the vascular wall, and reducing the pressor effect of vasoconstrictor substances.

Pharmacokinetics

Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – about 33%. It has a “first pass” effect through the liver and is metabolized by carboxylation to form an active metabolite. Plasma protein binding – 99%.

The time to reach Cmax of losartan is 1 hour, the active metabolite is 3-4 hours after oral administration. T1/2 is 1.5–2 hours, and its main metabolite is 3–4 hours, respectively. About 35% of the dose is excreted in the urine, about 60% through the intestines.

Hydrochlorothiazide is rapidly absorbed from the gastrointestinal tract. T1/2 – 5.8–14.8 hours. Not metabolized by the liver. About 61% is excreted unchanged by the kidneys.

Special instructions

Lozap plus can be prescribed together with other antihypertensive drugs.

The drug may increase plasma urea and creatinine concentrations in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney.

Hydrochlorothiazide may increase water-electrolyte imbalance (decreased blood volume, hyponatremia, hypochloremic alkalosis, hypomagnesemia, hypokalemia), impair glucose tolerance, reduce the excretion of Ca2+ in the urine and cause a transient slight increase in the concentration of Ca2+ in the blood plasma, increase the concentration of cholesterol and triglycerides, provoke the occurrence of hyperuricemia and/or gout.

Active ingredient

Hydrochlorothiazide, Losartan

Composition

Active ingredients:

losartan potassium 50 mg;

hydrochlorothiazide 12.5 mg;

Excipients:

MCC;

mannitol;

croscarmellose sodium;

povidone 30;

magnesium stearate;

hypromellose;

macrogol; talc;

dimethicone emulsion;

dye Opaspray Yellow M-1-22801 (which contains: purified water, titanium dioxide, methyl alcohol BP, hypromellose, Quinolin Yellow (E104), Ponceau 4R (E124))

Pregnancy

Taking drugs that directly act on the renin-angiotensin system during the second and third trimesters of pregnancy can lead to fetal death. If pregnancy occurs, discontinuation of the drug is indicated.

For pregnant women, the use of diuretics is usually not recommended due to the risk of jaundice in the fetus and newborn and thrombocytopenia in the mother. Diuretic therapy does not prevent the development of pregnancy toxicosis.

Contraindications

hypersensitivity to the components of the drug;
anuria;
severe arterial hypotension;
severe dysfunction of the liver and kidneys (Cl creatinine
hypovolemia (including against the background of high doses of diuretics);
pregnancy;
lactation period;
age under 18 years (efficacy and safety have not been established).

With caution:

patients with bilateral renal stenosis or stenosis of the artery of a single kidney;
patients with diabetes mellitus, hypercalcemia, hyperuricemia and/or gout;
patients with a burdened allergic history and bronchial asthma, as well as with systemic connective tissue diseases (including systemic lupus erythematosus).

Side Effects

Allergic reactions: angioedema, including swelling of the larynx and/or tongue leading to airway obstruction, and/or swelling of the face, lips, pharynx and/or tongue, occasionally reported with losartan.

Some of the patients with the allergic reactions mentioned above previously experienced angioedema when using other drugs, incl. and ACE inhibitors. Manifestations of vasculitis, including Henoch-Schönlein disease, have been observed extremely rarely when taking losartan.

From the cardiovascular system: decreased blood pressure.

From the respiratory system: when taking losartan – cough.

From the skin: urticaria.

Laboratory indicators: rarely (5.5 mmol/l), increased activity of liver transaminases.

Interaction

Losartan enhances the effect of other antihypertensive drugs. There were no clinically significant interactions with digoxin, indirect anticoagulants, cimetidine, phenobarbital, ketoconazole, or erythromycin.

As with other drugs that block angiotensin II or its action, concomitant administration of potassium-sparing diuretics (eg, spironolactone, triamterene, amiloride), potassium supplements, or potassium-containing salt substitutes may result in hyperkalemia.

Hydrochlorothiazide. The following drugs may interact with thiazide diuretics when administered simultaneously:

barbiturates, narcotic painkillers, ethanol – potentiation of orthostatic hypotension may occur;

hypoglycemic agents (oral agents and insulin) – dosage adjustment of hypoglycemic agents may be required;

other antihypertensive drugs—an additive effect is possible;

cholestyramine – decreased absorption of hydrochlorothiazide;

corticosteroids, ACTH – increased loss of electrolytes, especially potassium;

non-depolarizing muscle relaxants (for example tubocurarine) – the effect of muscle relaxants may be enhanced;

lithium preparations – diuretics reduce the renal clearance of Li+ and increase the risk of lithium intoxication, so simultaneous use is not recommended;

NSAIDs – in some patients, the use of NSAIDs may reduce the diuretic, natriuretic and hypotensive effects of diuretics.

Due to their effect on calcium excretion, thiazides may interfere with parathyroid function tests.

Overdose

Symptoms: losartan – marked decrease in blood pressure, tachycardia, bradycardia (as a result of vagal stimulation);

hydrochlorothiazide – loss of electrolytes (hypokalemia, hyperchloremia, hyponatremia), as well as dehydration resulting from excess diuresis.

Treatment: symptomatic and supportive therapy. If the drug has been taken recently, the stomach should be rinsed; If necessary, correct water and electrolyte disturbances.

Losartan and its active metabolites are not removed by hemodialysis.

Storage conditions

In a dry place, at a temperature not exceeding 30 °C.

Shelf life

3 years

Manufacturer

Zentiva k.s., Czech Republic