Azirem® Neo- capsules

INSTRUCTIONS FOR MEDICAL USE

AZIREM® NEO

Trade name of the drug: Azirem® Neo

Active substance (INN): Azithromycin

Dosage form: Capsules

Contents:

Each capsule contains:

Active ingredient: Azithromycin dihydrate (in terms of azithromycin) 250 mg and 500 mg.

Excipients: sodium starch glycolate, magnesium stearate.

Description: Solid gelatin capsules, white color, size “2” for 250 mg capsules and size “0” for 500 mg capsules, filled with powder of white or almost white color.

Pharmacotherapeutic group: Antibiotics (macrolide group).

ATX code: J01FA10.

Pharmacological properties

It is a broad-spectrum antibiotic. It is the first representative of a new subgroup of macrolide antibiotics – azalides. It has a bactericidal effect if it forms high concentrations in the inflammation focus.

Gram-positive cocci: Streptococcus pneumoniae, Stpyogenes, St.agalactiae, group C, F and G streptococci, St.viridans, Staphylococcus aureus are sensitive to the drug; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Legionella pneumophila, H. ducrei, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp. as well as Сhlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. It is inactive against erythromycin-resistant Gram-positive bacteria.

Pharmacokinetics

The drug is quickly absorbed from gastrointestinal tract, which is due to its resistance to acidic environment and lipophilicity. After 500 mg usage maximum concentration (Cmax) in plasma is reached after 2.5-2.96 hours and is 0.4 mg/ml. Bioavailability is 37%.

It penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland). High concentration in tissues (10-15 times higher than in blood plasma) and long half-life (T1/2) are caused by low binding of azithromycin with blood plasma proteins as well as its ability to penetrate into eukaryotic cells and to concentrate in low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (Vd) of 31.1 l/kg and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is particularly important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the sites of infection localization, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in the healthy tissues (on the average by 24-34%), and correlates with the degree of inflammatory edema. Despite its high concentration in phagocytes, azithromycin has no significant effect on their function. Azithromycin persists in bactericidal concentrations in the inflammatory focus for 5-7 days after the last dose, which allowed to develop short (3-day and 5-day) courses of treatment.

The drug is metabolized in the liver by demethylation.

Excretion of azithromycin from plasma is done in 2 stages: T1/2 is 14-20 hours, 8-24 hours after the last dose and 41 hours – 24-72 hours, which allows using the drug once a day.

It is eliminated mainly unchanged – 50% via the intestine, 6% – by the kidneys.

Indications for use

Infectious-inflammatory diseases caused by pathogens sensitive to the drug:

  • lower respiratory tract infections – bacterial and typical pneumonia, bronchitis;
  • infections of the upper respiratory tract and ENT organs – angina, sinusitis, tonsillitis, otitis media;
  • infections of the urogenital tract – uncomplicated urethritis, and/or cervicitis, cervicovaginitis and salpingitis;
  • skin and soft tissue infections – folliculitis, furuncles, carbuncles, acne (Acne vulgaris), impetigo, pyoderma, infected ulcers, infected dermatitis, cellulitis and rye;
  • Lyme disease (borreliosis), for treatment of the initial stage (Erythema migrans);
  • Diseases of the stomach and duodenum associated with Helicobacter pylori.

Dosage and administration method

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

For adults with upper and lower respiratory tract infections, skin and soft tissue infections, 500 mg/day for 3 days (1.5 g course dose).

For Lyme disease (borreliosis), for treatment of initial stage (Erythema migrans) – 1 g on the 1st day and 500 mg daily from 2nd to 5th day (course dose – 3 g).

For uncomplicated urethritis and/or cervicitis 1 g is prescribed once.

For diseases of the stomach and duodenum associated with Helicobacter pylori 1 g daily for 3 days is prescribed.

For children, the drug is prescribed in doses of 10 mg/kg body weight once a day for 3 days. The course dose is 30 mg/kg of body weight.

For treatment of Erythema migrans in children, the dose is 20 mg/kg of body weight on day 1 and 10 mg/kg – on days 2 to 5.

Side effects

Digestive system disorders: nausea, vomiting, flatulence, abdominal pain, melena, cholestatic jaundice, constipation in children, gastritis, oral candidiasis, lack of appetite, transient increase of liver enzymes activity are possible.

Cardiovascular system: palpitations, chest pain.

Nervous system disorders: dizziness, headache, vertigo, somnolence, hyperkinesia, anxiety, neurosis, sleep disorders. Genitourinary system: vaginal candidomycosis, nephritis.

Allergic reactions: rash, urticaria, angioedema.

Other: hyperglycemia, arthralgia.

Contraindications

Hypersensitivity to antibiotics of macrolide group; severe hepatic and renal dysfunction; children under 12 years old and body weight less than 45 kg (for 500 mg capsules), children under 3 years old (for 250 mg capsules); pregnancy and lactation.

Drug interaction

Simultaneous use of antacids and histamine H2-receptor blockers does not change drug absorption, but decreases Cmax in blood by 30%.

Concomitant use of the drug does not affect the blood concentration of carbamazepine, didanosine, rifabutin and methylprednisolone.

Co-administration of terfenadine and macrolide class antibiotic causes arrhythmia and Q-T interval prolongation.

When concomitant use with ergot alkaloids the risk of ergotism cannot be excluded.

When concomitant use with warfarin there are described the cases of enhancing the effects of the latter.

Concomitant use of digoxin or digitoxin with azithromycin may cause a significant increase in the concentration of cardiac glycosides and risk of glycoside intoxication.

When concomitant use with cyclosporine, it is recommended to monitor the blood content of cyclosporine.

When concomitant use with lovastatin, cases of rhabdomyolysis have been described.

Concomitant use with rifabutin increases the risk of neutropenia and leukopenia.

Co-administration impairs the metabolism of cyclosporine, which increases the risk of adverse and toxic reactions caused by cyclosporine.

Special indications

If one dose of the drug is missed – the missed dose should be taken as soon as possible, and subsequent doses should be taken at 24-hour intervals.

As with any antibiotic therapy, treatment with azithromycin may lead to superinfections (including fungal).

Antacids, ethanol and food slow down and reduce absorption of azithromycin, therefore it is recommended to take a break of at least 2 hours between intake of azithromycin and the above mentioned drugs.

If it is necessary to use the drug in pregnancy, it is possible only in cases when the expected benefits to the mother increase the potential risk to the fetus.

If it is necessary to use azithromycin during lactation, discontinuation of breastfeeding should be considered.

The drug does not affect the ability to drive motor transport and other activities requiring high concentration and psychomotor reaction rate.

Overdose

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

Treatment: gastric lavage, prescription of activated charcoal, symptomatic therapy.

Form of production

Capsules, 250 mg №6 and 500 mg №3 in carton packs.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription.

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