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

Excipients: microcrystalline cellulose, povidone (polyvinylpyrrolidone low molecular weight medical), crospovidone, calcium stearate, sodium lauryl sulfate.

Hard gelatin capsules number 1: titanium dioxide, dye blue patented (patent blue V), diamond black, dye crimson Ponso 4R], azorubin, gelatin.

Description:

Capsules No. 1 with a blue lid and a casing of blue color. The contents of capsules are white granules.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

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.Contacting from 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

1. Gram-positive aerobes

Staphylococcus aureus Methicillin-sensitive;
Streptococcus pneumoniae Penicillin-sensitive;
Streptococcus pyogenes.

2. Gram-negative aerobes

Haemophilus influenzae;
Haemophilus parainfluenzae;
Legionella pneumophila;
Moraxella catarrhalis;
Pasteurella multocida;
Neisseria gonorrhoeae.

3. Anaerobes

Clostridium perfringens;
Fusobacterium spp .;
Prevotella spp.;
Porphyriomonas spp.

4. Other microorganisms

Chlamydia trachomatis;
Chlamydia pneumonia;
Chlamydia psittaci;
Mycoplasma pneumonia;
Mycoplasma hominis;
Borrelia burgdorferi.

Microorganisms capable of developing resistance to azithromycin

Gram-positive aerobes

Streptococcus pneumoniae Penicillin is sensitive.

Initially, resistant microorganisms

Gram-positive aerobes

Pnterococcus faecalis;
Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides);

Gram-positive bacteria resistant to erythromycin.

Anaerobes

Pacteroides fragilis.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. Rapidly distributed throughout the body, while in tissues are reached high concentrations of antibiotic. After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is achieved after 2.5-2.9 hours and is 0.4 mg / l. Bioavailability is 37.5%.

Azithromycin well penetrates the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), into the skin and soft tissues. High concentrations in tissues (10-50 times higher than in plasma) and a long half-life are due to low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a medium with a low pH surrounding the lysosome. This, in turn, determines the large apparent volume of distribution (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes, is especially important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin in places of infection localization, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (an average of 24-34%) and correlates with the degree of inflammatory edema. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatment courses.

In the liver demethylated, the metabolites formed are not active.

Excretion of azithromycin from the blood plasma takes place in 2 stages: the half-life period is 14-20 hours in the interval from 8 to 24 hours after the drug administration and 41 hours in the interval from 24 to 72 hours, which allows using the drug once a day.

The drug is produced mainly with bile in the unchanged form, a small part is excreted 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 of chronic bronchitis, incl. caused by atypical pathogens;

Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

The initial stage of Lyme disease (borreliosis) - migrating erythema (Erythema migrans);

Urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications:

Hypersensitivity to antibiotics of macrolides;

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);

Breast-feeding;

Simultaneous reception with ergotamine and dihydroergotamine.

Carefully:

- Moderate dysfunction of the liver and kidney;

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

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

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be turned into (it is excreted in breast milk).

Dosing and Administration:

Inside, 1 time per day, at least 1 hour before or 2 hours after eating.Adults (including the elderly) and children over 12 years of age with a body weight of over 45 kg.

With infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues

500 mg (2 capsules) once a day for 3 days (the course dose is 1.5 g).

For infections of the skin and soft tissues - 1 g / day on the first day for 1 reception, then 0.5 g / day daily from 2 to 5 days (course dose - 3 g).

With migratory erythema

1 time per day for 5 days: 1st day - 1.0 g (4 capsules), then from the 2nd to the 5th day - 500 mg (2 capsules) (course dose 3.0 g).

In cases of urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis)

Uncomplicated urethritis / cervicitis - 1 g (4 capsules) once.

Purpose for 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:

Allergic reactions: itching, skin rashes, angioedema, hives, anaphylactic reaction, including edema (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrosis.

From the blood and lymphatic systems: thrombocytopenia, neutropenia.

From the central nervous system: dizziness / vertigo, headache, cramps, 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: rarely - palpitation, arrhythmia, ventricular tachycardia, increased interval QT, bidirectional ventricular tachycardia.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain / spasms, loose stools, flatulence, digestive disorders, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory liver function parameters, liver dysfunction, liver necrosis (possibly with fatal).

From the musculoskeletal system: arthralgia.

From the genitourinary system: nephritis, acute renal failure.

Other: vaginitis, candidiasis, photosensitivity.

Overdose:

Symptoms: nausea, temporary loss of hearing, vomiting, diarrhea.Treatment: gastric lavage, symptomatic therapy.

Interaction:

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration of 30%, so the drug should be taken at least 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 It does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, blood trimethoprim / sulfamethoxazole when used together, but do not exclude the possibility of such interactions in the appointment of azithromycin for oral administration.

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

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 is no evidence of 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 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-prescribing warfarin and azithromycin, 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 that, it is impossible to exclude the above-stated complications at joint reception of terfenadine and azithromycin.

Since it is possible to inhibit the enzyme 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, the possibility of such interaction in the administration of azithromycin for oral administration should be considered.

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:

Not take with food.

In case of missing the dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.

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

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

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:

For 6 or 10 capsules in a contour cell box made of a polyvinylchloride film and aluminum foil printed lacquered.

On 1 contour acheikova packing together with the instruction on application in a pack from a 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:

3 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001542 / 01

Date of registration:31.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp22.06.2017

Illustrated instructions

Instructions

Sumamecin (Sumamecin)