Sumamecin (Capsules) Instructions for Use

Marketing Authorization Holder

FP Obolenskoe, JSC (Russia)

ATC Code

J01FA10 (Azithromycin)

Active Substance

Azithromycin (Rec.INN registered by WHO)

Dosage Form

Sumamecin

Capsules 250 mg: 6 or 10 pcs.

Dosage Form, Packaging, and Composition

Capsules gelatin, size No. 1, with a blue cap and a light blue body; the capsule contents are white granules.

Excipients: calcium stearate, low molecular weight medical polyvinylpyrrolidone, microcrystalline cellulose.

6 pcs. – blister packs (1) – cartons.
10 pcs. – blister packs (1) – cartons.

Clinical-Pharmacological Group

Antibiotic of the macrolide group – azalide

Pharmacotherapeutic Group

Antibiotic-azalide

Pharmacological Action

An antibiotic of the macrolide group. It is a representative of the azalide subgroup. When high concentrations are created at the site of inflammation, it has a bactericidal effect.

It has a broad spectrum of action. Active against gram-positive bacteria Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci groups CF and G, Staphylococcus aureus, Staphylococcus viridans; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

Azithromycin is not active against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics

Absorption

Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. After oral administration of 500 mg, the C_max of azithromycin in blood plasma is reached in 2.5-2.96 hours and is 0.4 mg/l. Bioavailability is 37%.

Distribution

Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland), skin and soft tissues. The high concentration in tissues (10-50 times higher than in blood plasma) and long T_1/2 are due to the low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in the low pH environment surrounding lysosomes. This, in turn, determines a large apparent V_d (31.1 l/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver Azithromycin to the sites of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, Azithromycin does not significantly affect their function. Azithromycin persists in bactericidal concentrations at the site of inflammation for 5-7 days after the last dose, which made it possible to develop short (3-day and 5-day) courses of treatment.

Metabolism and excretion

It is demethylated in the liver; the resulting metabolites are inactive.

The elimination of azithromycin from blood plasma occurs in 2 stages: T_1/2 is 14-20 hours in the interval from 8 to 24 hours after taking the drug and 41 hours – in the interval from 24 to 72 hours, which allows the drug to be used once a day.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug

• Infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, pharyngitis, otitis media);
• Scarlet fever;
• Infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
• Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
• Infections of the urogenital tract (uncomplicated urethritis and/or cervicitis);
• Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
• Diseases of the stomach and duodenum associated with Helicobacter pylori (as part of combination therapy).

ICD codes

Dosage Regimen

The drug is taken orally, 1 hour before or 2 hours after meals, once a day.

For adults with infections of the upper and lower respiratory tract, it is prescribed at a dose of 500 mg/day in one dose for 3 days (course dose – 1.5 g).

For infections of the skin and soft tissues – 1000 mg/day on the first day in one dose, then 500 mg/day daily from day 2 to day 5 (course dose – 3 g).

For acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) – a single dose of 1 g.

For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) – 1 g on the first day and 500 mg daily from day 2 to day 5 (course dose – 3 g).

For gastric and duodenal ulcers associated with Helicobacter pylori – 1 g/day for 3 days as part of combination anti-Helicobacter therapy.

For children, it is prescribed at a rate of 10 mg/kg once a day for 3 days or on the first day – 10 mg/kg, then for 4 days – 5-10 mg/kg/day for 3 days (course dose – 30 mg/kg).

For the treatment of erythema migrans in children, the drug is prescribed at a rate of 20 mg/kg on the first day and 10 mg/kg from day 2 to day 5.

Adverse Reactions

From the digestive system diarrhea (5%), nausea (3%), abdominal pain (3%), dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of liver transaminases (≤ 1%); in children – constipation, anorexia, gastritis (≤ 1%).

From the cardiovascular system palpitations, chest pain (≤ 1%).

From the central nervous system dizziness, headache, drowsiness; in children – headache (during therapy for otitis media), hyperkinesis, anxiety, neurosis, sleep disturbance (≤ 1%).

From the urinary system nephritis (≤ 1%).

From the reproductive system vaginal candidiasis.

Allergic reactions rash, angioedema; in children – itching, urticaria.

Other increased fatigue, photosensitivity; in children – conjunctivitis, itching, urticaria.

Contraindications

• Hepatic and/or renal failure;
• Lactation period;
• Children under 12 months of age;
• Hypersensitivity (including to other macrolides);

The drug should be prescribed with caution during pregnancy, in case of arrhythmias (ventricular arrhythmias and QT interval prolongation are possible), as well as to children with severe impairment of liver or kidney function.

Use in Pregnancy and Lactation

The drug can be prescribed during pregnancy only if the benefit from its use significantly outweighs the risk that always exists when using any drug during pregnancy.

If it is necessary to prescribe the drug Sumamecin during lactation, breastfeeding should be suspended during treatment.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Contraindication: children under 12 months of age.

For children, it is prescribed at a rate of 10 mg/kg once a day for 3 days or on the first day – 10 mg/kg, then for 4 days – 5-10 mg/kg/day for 3 days (course dose – 30 mg/kg).

For the treatment of erythema migrans in children, the drug is prescribed at a rate of 20 mg/kg on the first day and 10 mg/kg from day 2 to day 5.

The drug should be prescribed with caution to children with severe impairment of liver or kidney function.

Special Precautions

It is necessary to observe a 2-hour break when used simultaneously with antacids.

After discontinuation of the drug, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.

Overdose

Symptoms severe nausea, temporary hearing loss, vomiting, diarrhea.

Drug Interactions

Antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin.

When warfarin and azithromycin were co-administered (at usual doses), no change in prothrombin time was detected; however, given that the interaction of macrolides and warfarin may enhance the anticoagulant effect, patients require careful monitoring of prothrombin time.

When used concomitantly with digoxin, an increase in its plasma concentration is observed.

When used concomitantly with ergotamine and dihydroergotamine, an increase in their toxic effect (vasospasm, dysesthesia) is observed.

Against the background of simultaneous use of Sumamecin, a decrease in clearance and an increase in the pharmacological action of triazolam are noted.

Azithromycin, by inhibiting microsomal oxidation in hepatocytes, slows down the elimination and increases the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, theophylline and other xanthine derivatives).

Lincosamines weaken the effectiveness of azithromycin, tetracycline and chloramphenicol enhance it.

Sumamecin is pharmaceutically incompatible with heparin.

Storage Conditions

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

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

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.