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).

Composition

Active substances:

losartan potassium 50 mg;

hydrochlorothiazide 12.5 mg;

Associated substances:

MCC;

Mannitol;

croscarmellose sodium;

Povidone 30;

Magnesium stearate;

hypromellose;

macrogol; talc;

dimethicone emulsion;

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

How to take, the dosage

Ingestion, regardless of meals.

The usual starting and maintenance dose is 1 tablet daily. For those patients in whom adequate BP cannot be achieved at this dosage, the dose of the drug may be increased to 2 tablets once daily.

The maximum dose is 2 tablets once daily. In general, the maximum hypotensive effect is achieved within 3 weeks after the start of treatment.

There is no need for special selection of the starting dose in elderly patients.

Interaction

Lozartan enhances the effect of other hypotensive agents. No clinically significant interaction with digoxin, indirect anticoagulants, cimetidine, phenobarbital, ketoconazole, erythromycin has been noted.

As with other drugs that block angiotensin II or its effects, simultaneous administration of potassium-saving diuretics (e.g., spironolactone, triamterene, amiloride), potassium preparations or substitute salts containing potassium may lead to hyperkalemia.

Hydrochlorothiazide. May interact with thiazide diuretics when the following drugs are prescribed concomitantly:

Barbiturates, narcotic analgesics, ethanol – potentiation of orthostatic hypotension may occur;

Hypoglycemic agents (oral agents and insulin) – correction of the dose of hypoglycemic agents may be required;

Other hypotensive agents – possible additive effect;

Colestyramine – decreased absorption of hydrochlorothiazide;

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

depolarizing myorelaxants (e.g., tubocurarin) – possible increase in myorelaxant action;

Lithium preparations – Diuretics decrease renal clearance of Li+ and increase the risk of lithium intoxication, so concomitant use is not recommended;

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

Thiazides may affect the results of parathyroid function tests due to their effect on calcium excretion.

Special Instructions

Lozap plus may be administered together with other hypotensive agents.

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

. Hydrochlorothiazide may exacerbate water-electrolyte balance disorders (decreased RBC, hyponatremia, hypochloremic alkalosis, hypomagnesemia, hypokalemia), impair glucose tolerance, decrease urinary Ca2+ excretion and cause a transient slight increase in plasma Ca2+ concentration, increase cholesterol and triglyceride concentrations, provoke the occurrence of hyperuricemia and/or gout.

Contraindications

With caution:

Side effects

Allergic reactions: Angioneurotic edema, including laryngeal and/or tongue edema leading to airway obstruction, and/or edema of the face, lips, pharynx, and/or tongue, occasionally seen with losartan.

Some of the patients with the above allergic reactions have previously had angioedema when using other drugs, including ACE inhibitors. Rarely, vasculitis, including Schoenlein-Henoch disease, has been reported with losartan.

Cardiovascular system: decreased BP.

Respiratory system: when taking losartan – cough.

Skin disorders: urticaria.

Laboratory measures: rare (5.5 mmol/l), increased liver transaminase activity.

Overdose

Symptoms: losartan – marked BP decrease, tachycardia, bradycardia (as a result of vagus stimulation);

hydrochlorothiazide – electrolyte loss (hypokalemia, hyperchloremia, hyponatremia), and dehydration resulting from excessive diuresis.

Treatment: symptomatic and supportive therapy. If the drug was taken recently, the stomach should be flushed; if necessary, correction of water-electrolyte disturbances is carried out.

Lozartan and its active metabolites are not eliminated by hemodialysis.

Pregnancy use

The administration of drugs acting directly on the renin-angiotensin system during the second and third trimesters of pregnancy may lead to fetal death. If pregnancy occurs, withdrawal of the drug is indicated.

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