Zitrocin - instructions for use, dose, side effects, contraindications

Azithromycin is a broad-spectrum antibiotic from the macrolide-azalide group, which has a bacteriostatic effect. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of a microbial cell. Communicating with 50S - a subunit of the ribosome, inhibits peptidranslokase at the stage of translation and suppresses protein synthesis, slowing the growth and multiplication of bacteria. In high concentrations 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 the antibiotic or may acquire resistance to it.

In most cases, sensitive microorganisms

Gram-positive aerobes

Streptococcus viridans

Streptococcus spp. (groups C, F and G, except those resistant to erythromycin)

Staphylococcus epidermidis methicillin-sensitive

Staphylococcus aureus methicillin-sensitive

Streptococcus pneumoniae penicillin - sensitive

Streptococcus pyogenes

Gram-negative aerobes

Haemophilus influenzae

Haemophilus parainfluenzae

Legionella pneumophila

Moraxella catarrhalis Pasteurella multocida Neisseria gonorrhoeae

Anaerobes

Clostridium perfringens

Fusobacterium spp.

Prevotella spp.

Porphyriomonas spp.

Other microorganisms

Chlamydia trachomatis,

Chlamydia pneumoniae

Chlamydia psittaci

Mycoplasma pneumoniae

Mycoplasma hominis

Borrelia burgdorferi

Microorganisms that can develop resistance to azithromycin Gram-positive aerobes

Streptococcus pneumoniae penicillin-resistant

Initially, resistant microorganisms

Gram-positive aerobes

Enterococcus faecalis

Staphylococci (methicillin-resistant staphylococci with very high frequency have acquired resistance to macrolides)

Gram-positive bacteria resistant to erythromycin.

Anaerobes

Bacteroides fragilis

Pharmacokinetics:

Azithromycin is well absorbed and quickly distributed throughout the body. Absorption is high, acid-fast, lipophilic.

Bioavailability

After a single dose of 0.5 g is 37% (the effect of "first pass" through the liver), the maximum concentration in the blood plasma after oral intake of 0.5 g is 0.4 mg / l, the time to reach a maximum concentration of 2.5-2.9 hours; in tissues and cells a concentration of 10 - 50 times higher than in the plasma, the volume of distribution is 31.1 l / kg. Easily passes the histohematological barriers. It penetrates well into the respiratory tract, genito-urinary organs, the prostate, the skin and soft tissues. It is transported by phagocytes, polymorphonuclear leukocytes and macrophages. It penetrates the membranes of cells 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 the inflammatory edema.It remains in effective concentrations for 5-7 days after the last dose. Binding to blood plasma proteins - 7-50% (inversely proportional to the concentration in the blood plasma). The half-life is 35-50 hours, the half-life of the tissues is much higher. In the liver demethylated, the metabolites formed are not active. 50% of the drug is excreted in the bile in unchanged form, 6% - by the kidneys.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- infections of the upper respiratory tract and ENT organs (pharyngitis, tonsillitis, sinusitis, otitis media);

- Infections of the lower respiratory tract: acute bronchitis, exacerbation chronic bronchitis, pneumonia (including those caused by atypical pathogens);

- infections of the skin and soft tissues (acne vulgaris of moderate severity, erysipelas, impetigo, secondarily infected dermatoses);

- urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis);

- the initial stage of Lyme disease (borreliosis) - migrating erythema (erythema migrans).

Contraindications:

- hypersensitivity to antibiotics of macrolides;

- severe violations of the liver and kidneys;

- children's age till 3 years;

- lactation period;

- simultaneous administration with ergotamine and dihydroergotamine;

- lactose intolerance, insufficiency of lactase, glucose-galactose malabsorption (since the formulation includes lactose)

Carefully:

- moderate violations of the liver and kidneys;

- arrhythmias or predisposition to arrhythmias and lengthening of the interval QT;

- when co-administered with terfenadine, warfarin, digoxin.

Pregnancy and lactation:

Azithromycin is used in pregnancy only if the effect of treatment exceeds the possible risk to the fetus. During treatment with the drug, breast-feeding is suspended.

Dosing and Administration:

Tablets 125 mg

Inside, not liquid for 1 hour before meals or 2 hours after meals 1 time per day.

Children over 3 years are dosed based on the body weight:

Body mass	The amount of azithromycin (in tablets 125 mg)
18-30 kg	2 tablets (250 mg)
31-44 kg	3 tablets (375 mg)
> 45 kg	appoint doses recommended for adults

In infections of the upper and lower respiratory tract. ENT - organs, skin and soft tissues: at the rate of 10 mg / kg body weight 1 time per day for 3 days (course dose 30 mg / kg). For the convenience of dosing, it is recommended to use the above table.

In the treatment of migrating erythema (erythema migrans) the dose rate is 60 mg / kg of body weight (20 mg / kg of body weight once a day on the first day, and from 2 to 5 days at the rate of 10 mg / kg body weight once a day).

Tablets 250 mg and 500 mg

Inside, not chewing 1 time per day, for 1 - 2 hours after meals. Adults and children over 12 years of age with a body weight of over 45 kg:

- at infections of the upper and lower respiratory tract. ENT - organs, skin and soft tissues: 1 tablet of 500 mg or 2 tablets of 250 mg per day for 1 reception for 3 days (exchange dose - 1.5 g)

- at the initial stage of Lyme disease (borreliosis)\ 1.0 g per day: 2 tablets of 500 mg or 4 tablets of 250 mg on the first day, from 2 to 5 days - 500 mg per day: 1 tablet of 500 mg or 2 tablets of 250 mg ( exchange rate - 3.0 g).

- with acne vulgaris of moderate severity: 1 tablet of 500 mg or 2 tablets of 250 mg once a day for 3 days, then 1 tablet of 500 mg or 2 tablets of 250 mg once a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (the 8th day from the start of treatment), the subsequent 8 weekly tablets with an interval of 7 days (course dose 6.0 g).

- with acute infections of the genito-urinary organs (including non-renonary urethritis and cervicitis, caused by chlamydia): once 1.0 g per day: 2 tablets of 500 mg or 4 tablets of 250 mg.

Side effects:

From the digestive system: nausea, vomiting, melena, abdominal pain, appetite disorder, flatulence, diarrhea or constipation, transient increase in hepatic transaminase activity, cholestatic hepatitis; In addition, children - constipation, decreased appetite, gastritis; candidymycosis of the oral mucosa.

From the central nervous system: headache, dizziness / vertigo, convulsions, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disturbances.

From the sense organs: - noise in the ears, reversible hearing loss down to deafness (when taking high doses for a long time), violation of taste sensations and perception of odor.

From the cardiovascular system: palpitation, arrhythmia, ventricular tachycardia, increased interval QT, bidirectional ventricular tachycardia.

From the side of the circulatory system: - thrombocytopenia, neutropenia.

From the genitourinary system: vaginitis, vaginal candidiasis, rarely - interstitial nephritis, acute renal failure.

From the musculoskeletal system: - arthralgia.

Allergic reactions: rash, hives, itching or skin rashes, angioedema, anaphylactic reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Other: asthenia, photosensitivity.

Overdose:

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

Treatment: symptomatic.

Interaction:

- antatsidy containing ions of aluminum and magnesium, ethanol and food slow down and reduce the absorption of azithromycin, so azithromycin should be taken 1 hour before or 2 hours after taking these drugs and food;

- azithromycin does not affect the concentration of carbamazepine, didanosine, rifabutin and methylprednisolone in the blood in a shared use;

- When parenteral application azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim / sulfamethoxazole in blood plasma in a joint use, however, the possibility of such interactions in the administration of azithromycin for oral administration should not be ruled out;

- azithromycin does not affect the pharmacokinetics of theophylline, but when combined with other macrolides, the concentration of theophylline in the blood plasma may increase;

- when it is necessary to use together with cyclosporine, it is recommended to control the content of cyclosporine in the blood plasma. Despite the fact that there are no data on the effect of azithromycin on the change in the concentration of cyclosporine in the blood plasma, other representatives of the macrolide class are able to change its level in blood plasma;

- with the joint administration of digoxin and azithromycin, it is necessary to control the level of digoxin in the blood, since many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma;

- when co-administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, however, given the possibility of enhancing the anticoagulation effect, patients need careful monitoring of prothrombin time;

- caution should be exercised in the joint administration of terfenadine and azithromycin, since it was found that the simultaneous administration of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening QT interval. Proceeding from this, it is impossible to exclude the aforementioned complications in the joint administration of terfenadine and azithromycin;

- when co-administered azithromycin with ergotamine and dihydroergotamine can manifest their toxic effect (vasospasm, dysesthesia);

- lincosamides weaken, and tetracycline and chloramphenicol increase the effectiveness of azithromycin;

- since there is the possibility of inhibiting the isoenzyme CYP3A4 azithromycin in parenteral form when coadministered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs that are metabolized with the participation of isoenzyme, should consider the possibility of such an interaction in the appointment of azithromycin for oral administration.

Special instructions:

In case of missed intake of a single dose of the drug, the missed dose should be taken as soon as possible, and the subsequent dose at an interval of 24 hours.

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

Just as with any antibiotic therapy, in the treatment of azithromycin, it is possible to attach superinfection (including fungal).

In the treatment of pharyngitis / tonsillitis caused by Streptococcus pyogenes, as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin. Azithromycin is also active against streptococcal infection in these cases, but is ineffective in preventing the development of acute rheumatic fever.

Effect on the ability to drive transp. cf. and fur:Azithromycin does not affect the ability to drive vehicles and moving machinery.

Form release / dosage:

Tablets coated with a film coating, 125 mg, 250 mg, 500 mg.

Packaging:

Tablets with a dosage of 125 mg and 250 mg: 6 tablets in the blister AL / PVC; 1 blister together with instructions for use in a cardboard box.

Tablets with a dosage of 500 mg: 3 tablets in a blister AL / PVC; 1 blister together with instructions for use in a cardboard box.

Storage conditions:

List B.

Store at a temperature of no higher than 30 C in a dry, protected from light place.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015354 / 01

Date of registration:08.10.2008

The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India

Manufacturer: & nbsp

UNIQUE PHARMACEUTICAL Laboratories India

Representation: & nbsp"UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")""UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")"India

Information update date: & nbsp24.08.2015

Illustrated instructions

Instructions

Zitrocin (Zithrocin)