Zithrolide forte, 500mg capsules, 3pcs

Composition

One capsule contains: Active ingredient: azithromycin dihydrate-525.8 mg*(based on azithromycin) -500.0 mg;excipients: microcrystalline cellulose, lactose monohydrate, magnesium stearate, sodium lauryl sulfate; solid gelatin capsules: body: titanium dioxide E 171, gelatin; cover: titanium dioxide E 171, dye sunset yellow E 110, gelatin. * the amount is indicated based on the theoretical activity of azithromycin 95.1%

Pharmacological action

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. Binding to the 50S subunit of the ribosome, it inhibits peptidtranslase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations, it has a bactericidal effect.

It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms. Microorganisms may initially be resistant to the action of an antibiotic or may become resistant to it.

Absorption is high, acid-resistant, lipophilic. Bioavailability after a single dose of 500 mg is 37% (the effect of ”first pass” through the liver), the maximum concentration (Cmax) after oral use of 500 mg is 0.4 mg/l, the time to reach the maximum concentration (TCmax) is 2.5-2.9 hours; in tissues and cells, the concentration is 10-50 times higher than in blood serum, the volume of distribution is 31.1 l/kg. Easily passes histohematic barriers. It penetrates well into the respiratory tract, genitourinary organs and tissues, into the prostate gland, into the skin and soft tissues; it accumulates in a low pH environment, in lysosomes (which is especially important for the eradication of intracellularly located pathogens). It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages. Penetrates through cell membranes and creates high concentrations in them. The concentration in the foci of infection is significantly higher (by 24-34%) than in healthy tissues, and correlates with the severity of inflammatory edema. In the focus of inflammation, it remains in effective concentrations for 5-7 days after taking the last dose. The relationship with plasma proteins is 7-50% (inversely proportional to the concentration in the blood).

It is demethylated in the liver, and the resulting metabolites are not active. The drug is metabolized by CYP3A4, CYP3A5, and CYP3A7 isoenzymes, of which it is an inhibitor. Plasma clearance – 630 ml / min: the half-life (T1 / 2) between 8 and 24 hours after use is 14-20 hours, T1 / 2 in the range from 24 to 72 hours-41 hours. 50% is excreted unchanged in the bile,6% – by the kidneys.

Food intake significantly changes the pharmacokinetics: Cmax decreases by 52%, the area under the pharmacokinetic curve “concentration-time” (AUC) – by 43%. In elderly men (65-85 years), the pharmacokinetic parameters do not change; in women, Cmax increases (by 30-50%).

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• infections of the upper respiratory tract and ENT organs (including tonsillitis, pharyngitis, sinusitis, tonsillitis, otitis media);
• infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
• scarlet fever;
• infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatoses);
• infections of the genitourinary system (including uncomplicated urethritis and/or cervicitis);
• Lyme disease (borreliosis) – for treatment of the initial stage (erythema migrans);

Use during pregnancy and lactation

Azithromycin passes through the placenta. Use during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use azithromycin during lactation, stop breastfeeding.

Contraindications

• Severe hepatic insufficiency;
• severe renal insufficiency;
• lactation (breast-feeding);
• children under 3 years of age;
• hypersensitivity to azithromycin or other macrolides.

With caution: use the drug during pregnancy, arrhythmias (possible development of ventricular arrhythmias and prolongation of the QT interval), in children with severe liver or kidney function disorders.

Side effects

On the part of the digestive system: diarrhea, nausea, abdominal pain, flatulence, vomiting, melena, cholestatic jaundice, increased activity of ”hepatic” transaminases, constipation, anorexia, gastritis, candidiasis of the oral mucosa, dyspepsia, hyperbilirubinemia, hepatitis, pancreatitis, pseudomembranous colitis, liver dysfunction, liver failure (in rare cases with a fatal outcome, mainly on the liver). liver function disorders), liver necrosis, fulminant hepatitis.

From the cardiovascular system: palpitation, chest pain, decreased blood pressure, increased Q-T interval, pirouette-type arrhythmia, ventricular tachycardia.

From the nervous system: dizziness, headache, vertigo, drowsiness, paresthesia, impaired taste sensations, hypesthesia, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, taste sensations, myasthenia gravis; in children – headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, insomnia.

From the sensory organs: impaired clarity of visual perception, deafness, tinnitus.

From the genitourinary system: increased residual urea nitrogen, vaginal candidiasis, increased plasma creatinine, interstitial nephritis, acute renal failure. Hematopoietic disorders: leukopenia, neutropenia, thrombocytopenia, lymphopenia, eosinophilia, hemolytic anemia. Allergic reactions: rash, urticaria, pruritus of the skin, angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, hypersensitivity reaction, anaphylactic reaction.

Other: hyperglycemia, arthralgia, asthenia, photosensitivity, conjunctivitis, taste changes, weakness, peripheral edema, malaise.

Interaction

Antacids (aluminum and magnesium-containing) they do not affect bioavailability, but reduce the concentration of azithromycin in the blood by 30%, so the interval between their intake should be 1 hour before or 2 hours after taking these drugs.

When used simultaneously with derivatives of ergotamine and dihydroergotamine, it is possible to increase the toxic effect (vasospasm, dysesthesia) of the latter.

When combined with coumarin-type indirect anticoagulants (warfarin) and azithromycin (in normal doses), patients should carefully monitor prothrombin time. Caution should be exercised when using terfenadine and azithromycin together, since it has been found that simultaneous use of terfenadine and macrolides causes arrhythmia and prolongation of the Q-T interval. Based on this, the above-mentioned complications cannot be excluded when taking terfenadine and azithromycin together. When used concomitantly with cyclosporine, it is necessary to monitor the concentration of cyclosporine in the blood. When used concomitantly with digoxin, it is necessary to control the concentration of digoxin in the blood (it is possible to increase the absorption of digoxin in the intestine).

When used concomitantly with nelfinavir, it is possible to increase the frequency of azithromycin adverse reactions (hearing loss, increased activity of “hepatic” transaminases). When used concomitantly with zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or the renal excretion of it and its metabolite glucuronide, but the concentration of the active metabolite of phosphorylated zidovudine in peripheral vascular mononuclear cells increases. The clinical significance of this fact has not been determined.

Consideration should be given to the possibility of inhibition of the CYP3A4 isoenzyme azithromycin when used concomitantly with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs that are metabolized with the participation of this enzyme.

Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim/sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and methylprednisolone in the blood when used simultaneously.

How to take it, course of use and dosage

Inside,1 hour before or 2 hours after meals 1 time a day. Adults and children over 12 years of age with a body weight of more than 45 kg: – for infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues-500 mg per day for 1 reception for 3 days (course dose -1.5 g). – acne vulgaris-500 mg per day in 1 dose for 3 days, then 500 mg per day once a week for 9 weeks. The first weekly dose should be taken 7 days after the first daily dose (day 8 from the start of treatment), followed by 8 weekly doses – at intervals of 7 days. – for acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) – once 1 g. – for Lyme disease-for the treatment of stage I (erythema migrans) – 1 g on the first day and 500 mg daily from day 2 to 5 (course dose-3 g). – in the treatment of pneumonia,500 mg is prescribed daily for 7-10 days; use begins immediately after the end of the intravenous dosage form (the recommended dose for intravenous use is 500 mg once a day for at least 2 days).

Overdose

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

Treatment: discontinuation of the drug, carrying out symptomatic therapy.

Special instructions

It is necessary to observe a break of 2 hours with simultaneous use of antacids.

After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a doctor.

Form of production

500 mg capsules. 3 capsules in a contour cell package made of polyvinyl chloride film and aluminum foil printed varnished. 1 or 2 contour cell packages together with the instructions for use are placed in a pack of cardboard.

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Children over 12 years of age

Indications

Respiratory Tract Infections, Infectious diseases, Sinusitis, Bronchitis, Pneumonia, Sore Throat, Skin Infections, Pharyngitis, Tonsillitis, Urethritis, Otitis