Drug title

Lozol (Indapamide)

Pharmacological action

Hypotensive agent (diuretic, vasodilator). By pharmacological properties it is close to thiazide diuretics (disruption of Na reabsorption in the cortical segment of the Genle loop). Increases urinary excretion of sodium and chlorine ions and, to a lesser extent, potassium and magnesium ions. Having the ability to selectively block "slow" calcium channels, increases elasticity of arterial walls and reduces total peripheral vascular resistance. Helps reduce left ventricular hypertrophy. Does not affect plasma lipid content (TG, low-density lipoproteins, high-density lipoproteins); does not affect carbohydrate metabolism (including in patients with concomitant diabetes mellitus). Reduces the sensitivity of the vascular wall to noradrenaline and angiotensin II, stimulates the synthesis of prostaglandin E2, reduces the production of free and stable oxygen radicals. Hypotensive effect develops by the end of the first week and lasts for 24 hours against the background of single administration.

Pharmacokinetics

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract; bioavailability is high (93%). Food intake slows down absorption rate slightly, but does not affect the amount absorbed. Maximum blood plasma concentration is 12 hours after oral administration. With repeated doses, the fluctuations in plasma concentration of the drug in the interval between two doses are reduced. The equilibrium concentration is established after 7 days of regular use. T1/2 is 18 h, plasma protein binding is 79%. It also binds with elastin of smooth muscles of the vascular wall. It has high volume of distribution, passes through histohematic barriers (including placental barrier), penetrates into breast milk.

It is metabolized in the liver. About 60-80% is excreted by the kidneys as metabolites (about 5% is excreted unchanged), 20% is excreted in the intestines. Pharmacokinetics does not change in patients with renal insufficiency. It does not cumulate.

Contraindications to use

• anuria;
• hypokalemia;
• Severe hepatic (including encephalopathy) and/or renal failure;
• pregnancy;
• lactation period;
• under 18 years of age (efficacy and safety have not been established);
• concomitant use of drugs that prolong the QT interval;
• Hypersensitivity to the drug and other sulfonamide derivatives.

Caution is used if diabetes mellitus in decompensation stage, hyperuricemia (especially if accompanied with gout and urate nephrolithiasis).

Administration during pregnancy and lactation

Contraindicated in pregnancy and lactation.

Administration in patients with liver dysfunction

Contraindicated:

Severe hepatic (including encephalopathy) insufficiency.

Administration in patients with impaired renal function

Contraindicated:

Severe renal insufficiency.

Administration in children

Contraindicated:

Under 18 years of age (efficacy and safety not established).

Indications of the drug Lozol (Indapamide)

arterial hypertension.

Dosing regimen

Tablets are taken orally without chewing. The daily dose of the drug is 1 tablet. (2.5 mg) a day (in the morning). If the desired therapeutic effect is not achieved after 4 to 8 weeks of treatment, it is not recommended to increase the dose (increase in the risk of side effects without increasing the antihypertensive effect). Instead, it is recommended to include another antihypertensive drug that is not a diuretic in the drug regimen.

In cases where it is necessary to start treatment with two drugs, the dose of Indapamide remains equal to 2.5 mg in the morning once a day.