ANGELON®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ANGELON® ANGELON

Composition:

Active substance:

1 tablet contains adenosine-5'-triphosphate-histidinate-magnesium(II) tri-potassium salt octahydrate, calculated as 100 % substance, with a content of total adenine nucleotides 6.3 mg — 10 mg;

Excipients: menthol; sugar powder; lactose monohydrate; magnesium stearate; colloidal anhydrous silicon dioxide.

Pharmaceutical form. Menthol-flavored tablets.

Main physicochemical properties: round, flat tablets with beveled edges, beveled side and score line on one side, white in color.

Pharmacotherapeutic group.

Cardiological preparations. ATC code C01EB10.

Pharmacological Properties.

Pharmacodynamics.

ANGELON**®** is a medicinal product of a new class of compounds — multiligand coordination complexes with macroergic phosphates. Its molecule consists of adenosine-5'-triphosphate (ATP), the amino acid histidine, and magnesium and potassium salts, producing a characteristic pharmacological effect that cannot be attributed to any individual chemical component (ATP, histidine, K+, Mg++) alone.

ANGELON**®** affects metabolic processes in the myocardium, normalizes energy metabolism, regulates the activity of cellular membrane ion-transport systems, improves membrane lipid composition, enhances the activity of membrane-bound enzymes, strengthens the myocardial antioxidant defense system, and exerts anti-ischemic, membrane-stabilizing, and antiarrhythmic effects in supraventricular tachycardia.

The drug provides an energy-sparing effect by inhibiting the activity of the enzyme 5'-nucleotidase, which regulates the rate of hydrolysis of energy substrates. ANGELON**®** prevents structural and functional damage to cardiomyocyte plasma membranes by preserving the quantitative and qualitative lipid composition of membranes through inhibition of membrane-bound phospholipase activity. ANGELON**®** reduces the intensity of lipid peroxidation (LPO) processes, thereby decreasing the accumulation in membranes of hydrolysis and peroxidation products of phospholipid fatty acids, such as lysophospholipids, which have pronounced detergent properties and can disrupt the contractile and rhythmic functions of the heart during ischemia. In experimental myocardial ischemia, the drug enhances the activity of Na+-K+-ATPase and Ca2+, Mg2+-ATPase, as well as the membrane calcium-binding capacity. ANGELON**®** improves indices of central and peripheral hemodynamics and coronary blood flow, normalizes myocardial contractility, thereby increasing physical performance. Under ischemic conditions, the drug reduces myocardial oxygen consumption, activates cardiac functional status, increases cardiac output, thus reducing the frequency of angina attacks and dyspnea during physical exertion.

ANGELON**®** restores normal sinus rhythm in patients with paroxysmal supraventricular tachycardia associated with atrial fibrillation and flutter, and also reduces the activity of ectopic rhythm foci (atrial and ventricular extrasystoles).

ANGELON**®** normalizes tissue concentrations of potassium and magnesium and reduces uric acid concentration.

Pharmacokinetics.

After administration into the body, the medicinal product ANGELON**®** undergoes slow degradation, forming adenosine.

Clinical characteristics.

Indications.

To be used in complex therapy of:

• ischemic heart disease, stable and unstable angina pectoris, exertional angina, and angina with documented coronary spasm;
• previous myocardial infarction, post-infarction myocardial syndrome (diffuse and focal cardiosclerosis), ischemic cardiomyopathy;
• cardiac arrhythmias;
• neurocirculatory dystonia, cardiogenic neurosis;
• cardiomyopathies;
• myocarditis;
• fatigue syndrome.

Contraindications.

• Hypersensitivity to the components of the medicinal product;
• acute myocardial infarction;
• cardiogenic shock and other types of shock;
• obstructive diseases of the bronchopulmonary system;
• severe forms of bronchial asthma;
• sinoatrial block;
• second- and third-degree atrioventricular block;
• hyperkalemia, hypermagnesemia;
• hemorrhagic stroke.

Interaction with other medicinal products and other forms of interactions.

ANGELON® must not be used concomitantly with cardiac glycosides due to increased risk of developing atrioventricular block.

Concomitant use with potassium-sparing diuretics, potassium supplements, and angiotensin-converting enzyme (ACE) inhibitors may increase the risk of hyperkalemia; concomitant use with magniroute (magnesium oxide) and other magnesium-containing preparations may lead to hypermagnesemia.

Dipyridamole enhances the therapeutic effect of ANGELON®; xanthinol nicotinate, caffeine, theophylline, and aminophylline reduce it.

ANGELON® may enhance the antianginal effect of alpha- and beta-adrenoblockers, calcium channel blockers, and nitrates.

Special precautions for use.

Use with caution in pronounced arterial hypotension, concomitant use with cardiac glycosides (due to increased risk of atrioventricular block), and in patients with predisposition to bronchospasm.

During prolonged use, serum potassium and magnesium levels should be monitored.

The medicinal product contains sucrose and lactose; therefore, patients with diabetes mellitus should use it with caution. The drug is contraindicated in patients with hereditary glucose-galactose malabsorption or sucrose-isomaltase deficiency. Consumption of products containing caffeine (coffee, tea, cola drinks) should be limited.

Use during pregnancy or breastfeeding.

There are no clinical data on the safety and efficacy of the medicinal product during pregnancy; therefore, its use in pregnant women is contraindicated.

Breastfeeding should be discontinued during the treatment period.

Ability to influence reaction rate while driving or operating machinery.

If dizziness or decreased arterial pressure occurs during treatment, patients should refrain from driving or operating machinery.

Method of Administration and Dosage.

ANGELON® tablets should be taken sublingually (under the tongue) and held until completely dissolved. The single dose is 10–40 mg, 3–4 times daily, regardless of food intake.

In acute cardiac conditions (angina attack, arrhythmia), ANGELON® tablets should be taken at a dose of 10–80 mg until the patient's condition improves. The maximum daily dose is 160 mg.

The duration of treatment is determined by the physician; on average, it lasts 20–30 days. If necessary, the course may be repeated after 10–15 days.

Children.

Not to be used in children.

Overdose.

Symptoms: possible development of bradycardia, atrioventricular block, arterial hypotension, and syncope associated with sudden drop in blood pressure.
Treatment: discontinue the drug and initiate symptomatic therapy. In case of bradycardia, administer atropine sulfate.

Adverse reactions.

From the skin and subcutaneous tissue: skin rashes, itching, facial hyperemia, Quincke's edema.

From the respiratory system: bronchospasm.

From the cardiovascular system: decreased blood pressure, tachycardia, atrioventricular block, coronary artery spasm which may lead to myocardial infarction.

From the gastrointestinal tract: nausea, epigastric discomfort, increased gastrointestinal motility.

From the urinary system: increased diuresis.

From the nervous system: headache, dizziness.

From the vascular system: sensation of warmth.

From the immune system: allergic reactions, including skin rashes, itching, Quincke's edema.

Shelf life. 3 years.

The medicinal product must not be used after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding +25 °C.

Keep out of reach of children.

Packaging.

10 tablets in a blister; 3 or 4 blisters per carton box.

Category of release. Over-the-counter.

Manufacturer.

LLC Pharmaceutical Company "FARCO S".

Manufacturer's address and place of business.

360 Sviato-Pokrovska Street, settlement Hostomel, Irpin, Kyiv region, 08290, Ukraine.

Marketing Authorization Holder.

LLC Pharmaceutical Company "FARCO S".

Address of the Marketing Authorization Holder.

50-A Zodchykh Street, Kyiv, 03162, Ukraine.