Lanatoside-OZ (Solution) Instructions for Use

Marketing Authorization Holder

Experimental Plant Of The Ssc Ls Of The Ukrmedprom Association, SC (Ukraine)

ATC Code

C01AA06 (Lanatoside C)

Active Substance

Lanatoside C

Lanatoside C (Rec.INN registered by WHO)

Dosage Form

Lanatoside-OZ

Solution for intravenous administration 200 mcg/1 ml: amp. 10 pcs.

Dosage Form, Packaging, and Composition

1 ml – ampoules (10) – carton packs.

Clinical-Pharmacological Group

Cardiac glycoside

Pharmacotherapeutic Group

Cardiotonic agent – cardiac glycoside

Pharmacological Action

A cardiac glycoside contained in Digitalis lanata. It exerts a positive inotropic effect, which is associated with an inhibitory effect on the Na⁺-K⁺-ATPase of the cardiomyocyte membrane, leading to an increase in the intracellular sodium ion content and a decrease in potassium ions.

As a result, the intracellular calcium content responsible for cardiomyocyte contractility increases, resulting in increased myocardial contractility. It enhances the work of the heart while prolonging diastole, increases stroke and minute volumes, and, along with increased myocardial tone, leads to a reduction in its size and thus to a decrease in myocardial oxygen demand.

The negative dromotropic effect is manifested by an increase in the refractoriness of the AV node. In atrial tachyarrhythmia, cardiac glycosides slow diastole, improving intracardiac and systemic hemodynamics. The negative chronotropic effect is due to direct and indirect influences on heart rhythm regulation.

In patients with chronic heart failure, it causes an indirect vasodilatory effect, reduces venous pressure, increases diuresis; reduces edema and shortness of breath.

The positive bathmotropic effect manifests itself in subtoxic and toxic doses.

Pharmacokinetics

When taken orally, absorption is 20-60%, plasma protein binding is 25-40%, T_1/2 is 28-36 hours. It is excreted by the kidneys unchanged. It is characterized by a relatively low capacity for cumulation.

Indications

As part of complex therapy for chronic heart failure of functional class II (in the presence of clinical manifestations), III and IV according to the NYHA classification; tachysystolic form of atrial fibrillation and flutter of paroxysmal and chronic course (especially in combination with chronic heart failure).

ICD codes

Dosage Regimen

Administer intravenously only. Do not administer orally or by any other route.

Determine the dosage individually based on the patient’s clinical condition, therapeutic response, and body weight.

Initiate therapy under continuous ECG monitoring in a clinical setting.

For rapid digitalization in adults, administer an initial dose of 1.6 mg, divided into 2-3 injections at 4-hour intervals.

Alternatively, administer 0.8 mg initially, followed by 0.4 mg every 4-6 hours until the desired therapeutic effect is achieved.

The total digitalizing dose typically ranges from 1.6 mg to 2.0 mg.

For maintenance therapy, administer 0.4 mg once or twice daily.

Adjust the maintenance dose based on clinical tolerance and the patient’s therapeutic response.

In patients with renal impairment, reduce the dosage. For creatinine clearance (CrCl) of 50-80 ml/min, use 50% of the standard maintenance dose.

For patients with CrCl less than 10 ml/min, use 25% of the standard maintenance dose.

For geriatric patients, use a lower dosage range and exercise increased caution due to age-related reductions in renal function.

Monitor serum electrolytes (potassium, magnesium, calcium) and renal function regularly during treatment.

Discontinue treatment immediately and consult a physician if the heart rate falls below 60 beats per minute.

Do not change the prescribed dose or administration schedule without medical supervision.

Adverse Reactions

From the digestive system decreased appetite, nausea, vomiting, diarrhea.

From the cardiovascular system arrhythmias, AV block.

From the central nervous system drowsiness, delirious psychosis, sleep disorders, headache, dizziness, confusion.

From the hematopoietic system and blood coagulation system thrombocytopenia, thrombocytopenic purpura, nosebleeds, petechiae.

Allergic reactions skin rash.

Other decreased visual acuity, gynecomastia.

Contraindications

Hypersensitivity to lanatoside C; glycoside intoxication, second-degree AV block, Wolff-Parkinson-White syndrome (WPW syndrome), intermittent complete block; pregnancy, breastfeeding period; age under 18 years.

With caution (weighing benefit/risk) bradycardia, first-degree AV block, sick sinus syndrome without an artificial pacemaker, paroxysmal ventricular tachycardia, hypertrophic obstructive cardiomyopathy, acute myocardial infarction, unstable angina, likelihood of unstable conduction through the AV node, history of Morgagni-Adams-Stokes attacks, isolated mitral stenosis with low heart rate (hypertrophic subaortic stenosis), cardiac asthma in patients with mitral stenosis (in the absence of tachysystolic form of atrial fibrillation), chronic heart failure with impaired diastolic function (restrictive cardiomyopathy, amyloidosis, constrictive pericarditis, cardiac tamponade), extrasystole, severe dilation of the heart chambers, cor pulmonale.

Water-electrolyte disturbances: hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia.

Hypothyroidism, alkalosis, myocarditis, arteriovenous shunt, hypoxia, old age, renal/hepatic failure, obesity.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding). If use during lactation is necessary, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Use with caution in patients with hepatic insufficiency.

Use in Renal Impairment

Use with caution in patients with renal insufficiency.

In case of impaired renal excretory function, the dose should be reduced: with a creatinine clearance (CrCl) of 50-80 ml/min, the average maintenance dose is 50% of the average maintenance dose for persons with normal renal function; with CrCl less than 10 ml/min – 25% of the usual dose.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Lanatoside C should be used with caution in elderly patients.

Special Precautions

One of the methods for monitoring the level of digitalization when prescribing cardiac glycosides is to monitor their plasma concentration.

Lanatoside C should be used with caution in patients with electrolyte disturbances (including conditions after dialysis, with diarrhea, with insufficient nutrition, prolonged vomiting, when taking diuretics), or with other drugs causing electrolyte disturbances (hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia), with hypothyroidism, alkalosis, myocarditis, obesity, in elderly patients, with hypoxia, renal/hepatic failure.

The likelihood of intoxication increases with hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia, hypothyroidism, severe dilation of the heart chambers, cor pulmonale, myocarditis.

If symptoms of overdose appear (nausea, vomiting, bradycardia, extrasystole, bigeminy, visual impairment), treatment should be discontinued for several days and then resumed at a lower dose.

In case of more pronounced signs of glycoside intoxication, the administration of potassium – 2-4 g/day in the form of potassium salts (chlorides, citrates, phosphates, and asparaginates), antiarrhythmic drugs (diphenin), and a 5% dextrose solution with vitamins (B₁, B₆, C) is recommended.

In hypertrophic obstructive cardiomyopathy, the use of lanatoside C leads to increased obstruction.

In severe mitral stenosis with normo- or bradycardia, heart failure develops due to reduced diastolic filling of the left ventricle. Lanatoside C, by increasing the contractility of the right ventricular myocardium, causes a further increase in pressure in the pulmonary artery system, which can provoke pulmonary edema or worsen left ventricular failure. In patients with mitral stenosis, cardiac glycosides are prescribed when right ventricular failure is associated or in the presence of atrial tachyarrhythmia.

In patients with second-degree AV block, the prescription of cardiac glycosides can worsen it and lead to the development of a Morgagni-Adams-Stokes attack. Prescribing cardiac glycosides for first-degree AV block requires caution, frequent ECG monitoring, and in some cases, prophylactic use of drugs that improve AV conduction. Lanatoside C, in WPW syndrome, by reducing AV conduction, promotes impulse conduction through accessory pathways bypassing the AV node and thereby provokes the development of paroxysmal tachycardia.

Lanatoside C should be used strictly in the doses and regimens recommended by the doctor, without changing the dose independently.

If the heart rate is less than 60 beats/min, you should immediately consult a doctor.

If the patient has not taken Lanatoside C for more than 2 days, this must be reported to the doctor.

Before discontinuing the use of lanatoside C, the doctor must be informed.

If side effects occur, you should immediately consult a doctor.

Before surgery or when providing emergency care, the doctor must be warned about the use of lanatoside C.

Effect on the ability to drive vehicles and mechanisms

During treatment, patients should exercise caution when driving vehicles and engaging in other activities that require high concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use with antacids, sulfasalazine, cholestyramine, the absorption of lanatoside C from the gastrointestinal tract is reduced.

Simultaneous intake of calcium preparations, catecholamines, and diuretics increases the risk of glycoside intoxication.

Corticosteroids and diuretics increase the risk of hypokalemia and hypomagnesemia; thiazides and calcium preparations (especially with intravenous administration) increase the risk of hypercalcemia; amiodarone and mercazolil increase the risk of hypothyroidism. Catecholamines, calcium preparations, and diuretics increase the risk of glycoside intoxication.

With simultaneous use with thiazide diuretics and calcium preparations (especially with intravenous administration), the risk of hypercalcemia increases.

The excretion of lanatoside C decreases and its toxicity increases when combined with diuretics (except potassium-sparing ones), insulin, amphotericin, with long-term use of dextrose, corticosteroids, antibiotics, as a result of hypokalemia and hypomagnesemia.

With simultaneous use with quinidine, verapamil, nifedipine, spironolactone (to a lesser extent), the concentration of lanatoside C in the blood plasma increases (competitive reduction of secretion by the proximal renal tubules).

Beta-blockers and verapamil enhance AV conduction disturbances.

Amiodarone and mercazolil, when used simultaneously with lanatoside C, increase the risk of hypothyroidism.

In combination with potassium permanganate, ammonia-anise drops, hydrogen peroxide, silver nitrate, raspberry syrup, alkaloid salts, sulfonamides, and tannin, Lanatoside C forms a precipitate; with acids and bases, it forms inactive products.

In combination with barbiturates (especially phenobarbital), due to the induction of liver enzymes and accelerated metabolism, the effectiveness of lanatoside C decreases.

Calcium preparations have a synergistic effect with lanatoside C.

The combination of lanatoside C with chlorpromazine promotes increased blood clotting. When lanatoside C is co-administered with heparin, the effect of heparin may be weakened due to increased blood clotting under the influence of lanatoside C.

When lanatoside C is used together with lincomycin, pseudomembranous colitis develops.

There are recommended combinations of lanatoside C with certain drugs. When lanatoside C is administered with anabolic steroids, thiamine chloride, riboflavin, pyridoxine, folic acid, orotic acid, methyluracil, methionine, phosphaden, and inosine, its inotropic effect is enhanced.

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.