Indapamide-OBL (Tablets) Instructions for Use

Marketing Authorization Holder

Aliym, JSC (Russia)

ATC Code

C03BA11 (Indapamide)

Active Substance

Indapamide (Rec.INN registered by WHO)

Dosage Form

Indapamide-OBL

Film-coated tablets, 2.5 mg: 10, 15, 20, 30, 40, 45, 60 or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the core on the cross-section is white or almost white.

Excipients: lactose monohydrate, microcrystalline cellulose (Vivapur 101), magnesium stearate, sodium carboxymethyl starch (sodium starch glycolate), povidone K30.

Shell composition: hypromellose (hydroxypropyl methylcellulose), macrogol 6000 (polyethylene glycol 6000), titanium dioxide.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
15 pcs. – contour cell packs (1) – cardboard packs.
15 pcs. – contour cell packs (2) – cardboard packs.
15 pcs. – contour cell packs (3) – cardboard packs.
20 pcs. – contour cell packs (1) – cardboard packs.
20 pcs. – contour cell packs (2) – cardboard packs.
20 pcs. – contour cell packs (3) – cardboard packs.
30 pcs. – contour cell packs (1) – cardboard packs.
30 pcs. – contour cell packs (2) – cardboard packs.
30 pcs. – contour cell packs (3) – cardboard packs.

Clinical-Pharmacological Group

Diuretic. Antihypertensive drug

Pharmacotherapeutic Group

Diuretic agent

Pharmacological Action

Antihypertensive drug. Thiazide-like diuretic, a sulfonamide derivative. It causes a moderate saluretic and diuretic effect associated with the inhibition of sodium ion reabsorption in the cortical segment of the loop of Henle. It increases the excretion of sodium and chloride ions in the urine and, to a lesser extent, potassium and magnesium ions. Indapamide exerts an antihypertensive effect at doses that do not have a pronounced diuretic effect.

Having the ability to selectively block “slow” calcium channels, it increases the elasticity of arterial walls and reduces total peripheral vascular resistance. The decrease in total peripheral vascular resistance is due to several mechanisms: a decrease in the sensitivity of the vascular wall to norepinephrine and angiotensin II; an increase in the synthesis of prostaglandins with vasodilating activity; inhibition of calcium ion influx into the smooth muscle elements of the vascular wall. It helps to reduce left ventricular hypertrophy of the heart.

Indapamide-OBL exerts an antihypertensive effect, which manifests only with initially elevated blood pressure.

It does not affect the lipid content in blood plasma (triglycerides, LDL, HDL), does not affect carbohydrate metabolism (including in patients with concomitant diabetes mellitus).

The antihypertensive effect of the drug develops by the end of the first week of administration. When the drug is taken once a day, the antihypertensive effect persists for 24 hours.

Pharmacokinetics

Absorption

After oral administration, Indapamide is rapidly and completely absorbed from the gastrointestinal tract, C_max in blood plasma is reached after 1-2 hours. Bioavailability is high (93%). Taking the drug simultaneously with food somewhat slows down the rate of absorption without affecting its extent.

Distribution

With repeated doses, fluctuations in the concentration of indapamide in blood plasma in the interval between drug doses decrease, C_ss is established after 7 days of regular administration. Plasma protein binding is 79%, Indapamide also binds to the elastin of the vascular wall smooth muscle. V_d is high, it penetrates through histohematic barriers (including the placental barrier), and is excreted in breast milk.

Metabolism and excretion

It is biotransformed in the liver. 60-80% is excreted by the kidneys in the form of metabolites, about 5% unchanged, about 20% through the intestines. T_1/2 is about 18 hours.

Pharmacokinetics in special clinical cases

In case of impaired renal function, the pharmacokinetic parameters of indapamide do not change, no accumulation has been noted.

Indications

• Arterial hypertension.

ICD codes

Dosage Regimen

Take one 2.5 mg tablet once daily in the morning.

Swallow the tablet whole; do not chew or crush it.

The maximum daily dose is 2.5 mg; do not exceed this dose.

This regimen applies to both monotherapy and combination therapy with other antihypertensive agents.

Take the tablet with a glass of water, with or without food.

Regularly monitor blood pressure to assess therapeutic response.

Routinely check serum potassium and creatinine levels, especially during initial therapy and after dosage adjustments.

Monitor for signs of electrolyte imbalance, such as hypokalemia or hyponatremia.

Exercise increased caution in patients with liver cirrhosis due to the risk of metabolic alkalosis.

Use with caution in patients with a history of gout or hyperuricemia.

In patients with diabetes, monitor blood glucose levels carefully, particularly if hypokalemia develops.

Adverse Reactions

From the digestive system rarely – nausea, feeling of discomfort or pain in the epigastrium.

From the CNS rarely – weakness, fatigue, dizziness, nervousness.

From the cardiovascular system rarely – orthostatic hypotension.

Allergic reactions possible – skin manifestations.

From the electrolyte balance and metabolism hypokalemia, hyponatremia, hyperuricemia, hyperglycemia, hypochloremia are possible.

Contraindications

• Acute cerebrovascular accident;
• Severe renal impairment;
• Severe hepatic impairment;
• Severe forms of diabetes mellitus;
• Severe forms of gout;
• Hypersensitivity to indapamide.

Use in Pregnancy and Lactation

The drug is not recommended for use during pregnancy and lactation.

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment. The drug should be prescribed with caution and under close supervision to patients with liver cirrhosis (risk of developing metabolic alkalosis, enhanced by manifestations of hepatic encephalopathy).

Use in Renal Impairment

Contraindicated in severe renal impairment.

Special Precautions

Indapamide-OBL should be prescribed with caution to patients with decompensated diabetes mellitus, with hyperuricemia (especially accompanied by gout and urate nephrolithiasis).

In patients with diabetes mellitus, while taking Indapamide-OBL, it is important to control glucose levels, especially against the background of hypokalemia.

During the administration of Indapamide-OBL, the development of hypokalemia is possible. Potassium and creatinine levels in the blood should be monitored, especially in patients receiving cardiac glycosides, laxatives, against the background of hyperaldosteronism, as well as in elderly patients.

The drug should be prescribed with caution and under close supervision to patients with liver cirrhosis (risk of developing metabolic alkalosis, enhanced by manifestations of hepatic encephalopathy). The high-risk group also includes patients with an increased QT interval on the ECG (congenital or developed against the background of any pathological process).

Hypercalcemia while taking the drug may be a consequence of previously undiagnosed hyperparathyroidism.

As is known, sulfonamide derivatives can exacerbate the course of systemic lupus erythematosus, which should be taken into account when treating with Indapamide-OBL.

The drug can be used as monotherapy or in combination with other antihypertensive drugs (beta-blockers, calcium channel blockers, ACE inhibitors).

Use in pediatrics

Studies of the safety and efficacy of Indapamide-OBL in children have not been conducted.

Overdose

Indapamide, even in very high doses (up to 40 mg, i.e., 27 times the therapeutic dose), does not have a toxic effect.

Symptoms: disturbances of water-electrolyte balance, arterial hypotension, nausea, vomiting, convulsions, dizziness, confusion, polyuria or oliguria, ending in anuria (due to hypovolemia); respiratory depression.

Treatment: gastric lavage, correction of water-electrolyte balance, symptomatic therapy. There is no specific antidote.

Drug Interactions

With the simultaneous use of indapamide with drugs that can cause hypokalemia (including saluretics, glucocorticoids and mineralocorticoids (with systemic use), tetracosactide, amphotericin B (intravenously), laxatives), the risk of developing hypokalemia increases, in connection with which control of blood potassium levels and, if necessary, correction is required.

With the simultaneous use of indapamide with cardiac glycosides, the risk of digitalis intoxication increases; with calcium preparations – hypercalcemia.

With the simultaneous use of indapamide with metformin, lactic acidosis may be aggravated.

With the simultaneous use of indapamide with astemizole, erythromycin (intravenously), pentamidine, sultopride, terfenadine, vincamine, class I antiarrhythmic drugs (quinidine, disopyramide) and class III antiarrhythmic drugs (amiodarone, bretylium, sotalol), the likelihood of cardiac arrhythmias of the “torsades de pointes” type increases.

With the simultaneous use of indapamide with NSAIDs, corticosteroids, tetracosactide, sympathomimetics, a decrease in the antihypertensive effect of indapamide is possible; with baclofen – an increase.

The combination of indapamide with potassium-sparing diuretics may be effective in some categories of patients, however, the possibility of developing hypo- or hyperkalemia is not completely excluded, especially in patients with diabetes mellitus and renal failure.

With the simultaneous use of indapamide with ACE inhibitors, in case of hyponatremia development, the risk of arterial hypotension and/or acute renal failure increases (especially with existing renal artery stenosis).

When using iodine-containing contrast agents in high doses while taking Indapamide-OBL, the risk of impaired renal function increases. Before using iodine-containing contrast agents, patients need to restore blood volume.

Tricyclic antidepressants (such as imipramine) with simultaneous use enhance the antihypertensive effect of indapamide and increase the risk of orthostatic hypotension.

With the combined use of indapamide with cyclosporine, an increase in plasma creatinine levels is possible.

With the simultaneous use of indapamide with lithium preparations, an increase in the concentration of lithium in blood plasma is possible due to a decrease in its excretion.

Storage Conditions

List B. The drug should be stored in a dry, light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Pharmacy supply terms

The drug is dispensed by prescription.

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.