Sumaclide - instructions for use, doses, side effects, contraindications

Azithromycin is a bacteriostatic broad-spectrum 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 protein synthesis of a microbial cell. Linking to the 50S subunit of the ribosome, Azithromycin inhibits peptidranslokase at the stage of translation, suppresses protein synthesis, slows the growth and multiplication of bacteria, has a bactericidal effect at high concentrations.

It has activity against a number of gram-positive, gram-negative anaerobes, 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

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 capable of developing resistance to azithromycin

Gram-positive aerobes: Streptococcus pneumoniae penicillin-resistant

Initially, resistant microorganisms

Gram-positive aerobes: Enterococcus faecalis, Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides), Gram-positive bacteria resistant to erythromycin.

Anaerobes: Bacteroides fragilis

Pharmacokinetics:

Absorption is high. Azithromycin resistant to acidic medium, lipophilic. Quickly absorbed in the gastrointestinal tract. Bioavailability after a single dose of 0.5 g - 37% (the effect of "first passage" through the liver), the maximum concentration of the drug in the plasma after oral intake of 0.5 g - 0.4 mg / l, the time to reach the maximum concentration of the drug in plasma - 2 , 5-2.9 h; in tissues and cells the concentration is 10-50 times higher than in serum, 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; accumulates in lysosomes (which is especially important for the eradication of intracellular pathogens). 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. Azithromycin remains in effective concentrations for 5-7 days after the last dose.The connection with plasma proteins is 7-50% (inversely proportional to the concentration in the blood).

In the liver demethylated, the metabolites formed are not active. In the metabolism of the drug, isozymes participate CYP3A4, CYP3A5, CYP3A7, of which it is an inhibitor. Plasma clearance - 630 ml / min; the half-life of the drug between 8 and 24 hours after admission is 14-20 hours, the half-life of the drug in the interval from 24 to 72 hours is 41 hours. 50% is excreted with bile in unchanged form, 6% by kidneys.

Eating significantly changes the pharmacokinetics (depending on the dosage form): capsules - the maximum plasma concentration in the plasma is reduced (by 52%) and the area under the concentration-time curve (by 43%).

In elderly men (65-85 years) the pharmacokinetic parameters do not change, the maximum concentration of the drug in plasma is increased in women (by 30-50%), in children 3-5 years of age the maximum concentration of the drug in the plasma decreases, the half-life of the drug, the area under the "concentration-time" curve.

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: pneumonia caused by atypical pathogens, acute bronchitis, exacerbation of chronic bronchitis;

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

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

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

Contraindications:

- hypersensitivity to antibiotics of the macrolide group;

- severe violations of the liver and kidneys;

- Children under 12 years of age with a body weight of less than 45 kg (for this dosage form);

- simultaneous reception with ergotamine and dihydroergotamine.

Carefully:

- mild liver and / or kidney dysfunction;

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

- with the co-administration of terfenadine, warfarin, digoxin.

Pregnancy and lactation:

In pregnancy, the drug is used only if the intended benefit to the mother exceeds the potential risk to the fetus.

During lactation during the treatment should stop breastfeeding.

Dosing and Administration:

Inside, 1 hour before or 2 hours after meals 1 time per day, adults (including the elderly) and children over 12 years of age with a body weight of more than 45 kg.

When infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 500 mg / day (2 capsules) for 1 reception for 3 days (exchange dose -1.5 g).

Acne vulgaris - 500 mg / day (2 capsules) for 1 reception for 3 days, then 500 mg / day (2 capsules) once a week for 9 weeks. The first weekly dose should be taken 7 days after the first daily dose (8 days from the start of treatment), the next 8 weekly doses - with an interval of 7 days.

In acute infections of the urogenital organs caused by Chlamydia trachomatis (uncomplicated urethritis, cervicitis) - once 1 g (4 capsules).

With migrating erythema - 1 time per day for 5 days: 1st day - 1 g (4 capsules), then from 2 to 5 days - 500 mg (2 capsules) (course dose 3 g).

The appointment of patients with impaired renal function - for patients with moderate impairment of kidney function (creatinine clearance> 40 ml / min) dose adjustment is not needed.

Side effects:

From the blood and lymphatic systems: thrombocytopenia, neutropenia.

From the side of the central nervous system: dizziness / vertigo, headache, seizures, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.

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

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

From the digestive system: Nausea, vomiting, diarrhea, abdominal pain / spasms, flatulence, digestive disorders, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in liver function tests, hepatic insufficiency, liver necrosis (possibly fatal).

Allergic reactions: itching, skin rashes, angioedema, urticaria, eosinophilia, photosensitivity, anaphylactic reaction, including Quincke's edema (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

From the musculoskeletal system: arthralgia.

From the genitourinary system: interstitial nephritis, acute renal failure.

Other: vaginitis, candidiasis.

Overdose:

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

Treatment: symptomatic.

Interaction:

- Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood by 30%, so the drug should be taken one hour before or two hours after taking these drugs and food.

- Azithromycin does not affect the concentration of carbamazepine, didanosine, rifabutin and methylprednisolone in the blood when used together.

When parenteral application azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim / sulfamethoxazole in the blood in a joint use, but do not exclude the possibility of such interactions with the administration of azithromycin for oral administration.

- Azithromycin has no effect on the pharmacokinetics of theophylline, however, when co-administered with other macrolides theophylline plasma concentrations may be increased.

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

- With the joint administration of digoxin and azithromycin, it is necessary to monitor the level of digoxin in the blood, many macrolides increase absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma.

- If it is necessary to share with warfarin, careful monitoring of prothrombin time is recommended.

- 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.

- Since it is possible to inhibit the isoenzyme CYP3A4 azithromycin in parenteral form when co-administered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism occurs with the participation of this enzyme,should take into account the possibility of such interaction in the appointment of azithromycin for oral administration.

- With the joint administration of azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or on the excretion of its and its metabolite glucuronide by the kidneys. Nevertheless, the concentration of the active metabolite - phosphorylated zidovudine - increases in mononuclear cells of peripheral vessels. The clinical significance of this fact is not clear.

- With the simultaneous administration of macrolides with ergotamine and dihydroergotamine, their toxic effect is possible.

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 following - with interruptions of 24 hours.

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

The drug should be taken at least one hour before or two hours after taking antacid preparations.

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, however, it is ineffective to prevent 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 mechanisms.

Form release / dosage:

Capsules 250 mg.

Packaging:

3 or 6 capsules in a contour cell box made of a polyvinylchloride film and aluminum foil.

6 capsules in a polymer can.

Each jar or 1 circuit cell package with instructions for use is placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005784/10

Date of registration:23.06.2010

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp19.08.2015

Illustrated instructions

Instructions

Sumaclide (Sumaklid)