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

1 bottle contains active substance - azithromycin (in the form of azithromycin dihydrate 524.00 mg) 500 mg; Excipients: citric acid monohydrate - 110 mg, mannitol - 146 mg, sodium hydroxide - q.s.

Description:

A lyophilized powder or a white or nearly white-colored mass packed into a tablet.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Azithromycin is a macrolide antibiotic of the azalide group. Reversibly binding to the 50S subunit of ribosomes of bacterial cells, disrupts the translocation of the growing polypeptide chain from the aminoacyl region to the peptide, which leads to inhibition of protein synthesis in bacterial cells.

Sensitive: aerobic Gram-positive microorganisms - Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, aerobic gram-negative microorganisms - Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.; other - Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Moderately sensitive: Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).

Stable: aerobic Gram-positive microorganisms - Enterococcus faecalis, beta-hemolytic Streptococcus spp. groups A, Staphylococcus spp. (methicillin-resistant), including Staphylococcus aureus, resistant to erythromycin and other macrolides, lincosamides; anaerobes: Bacteroides fragilis.

Pharmacokinetics:

Azithromycin rapidly penetrates from the blood plasma into the tissue. Concentrating in phagocytes and not breaking their functions, azithromycin migrates to the focus of inflammation, accumulating directly in infected tissues. The pharmacokinetic profile of azithromycin is characterized by a low concentration in the blood plasma and a high concentration in the tissues.

In healthy volunteers, with intravenous infusion of azithromycin at a dose of 500 mg (concentration of the solution 1 mg / ml) for 3 hours, the maximum concentration of drug C_m_Oh in blood plasma was 1.1 μg / ml, with a baseline concentration of 0.18 μg / ml. Similar values were found in patients with community-acquired pneumonia who received the same therapy for 2 to 5 days (C_m_Oh 3.6 μg / ml, at a baseline concentration of 0.2 μg / ml).

The half-life of the drug is 65-72 hours.

Binding to plasma proteins decreases with an increase in the concentration of azithromycin in the blood. Azithromycin has a protein binding percentage of 51 at a concentration of 0.02 μg / ml and 7% at a concentration of 2 μg / ml.

After intravenous administration azithromycin is distributed to most tissues and body fluids. A high level of the observed volume of distribution (on average 32 l / kg) and plasma clearance (10.8 ml / min / kg) suggests that a long half-life of the drug is a consequence of the accumulation of antibiotic in tissues followed by its slow release.

Easily passes through the histohematological barriers. It penetrates well into the respiratory tract, genito-urinary organs and tissues, incl. prostate, in the skin and soft tissues; accumulates in a medium with low pH, in lysosomes (which is especially important for the eradication of intracellular pathogens). It is also 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. The body remains in effective concentrations for 5-7 days after the administration of the last dose. The main way of biotransformation is N-detylation in the liver.

It is excreted by the intestine, mostly unchanged. A small amount of the drug is excreted by the kidneys. In the first day, 11% of the kidneys are excreted, and after 5 days, 14% of the intravenously administered dose.

Indications:

- Community-acquired pneumonia of severe course caused by Chlamydia pneumoniae, Haemophilus influenzae, Legionella pneumophila, Moraxella catarrhalis, Mycoplasma pneumoniae, Staphylococcus aureus or Streptococcus pneumoniae;

- Infectious-inflammatory diseases of small pelvic organs of severe course (endometritis and salpingitis), caused by Chlamydia trachomatis, Neisseria gonorrhoeae or Mycoplasma hominis.

Contraindications:

- Hypersensitivity to antibiotics of macrolides;

- Severe violations of the liver and kidneys;

- Children up to 16 years;

- Simultaneous reception with ergotamine and dihydroergotamine.

Carefully:

With moderate violations of the liver and kidney function, patients with a disorder 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 in cases when the benefit from its use for the mother exceeds the possible risk to the fetus. During lactation, breastfeeding is suspended.

Dosing and Administration:

The drug should be used only in inpatient medical institutions! Recommended dosages for intravenous azithromycin in the treatment of adults and patients older than 16 years with the following diseases:

Community-acquired pneumonia (EP)

500 mg once a day intravenously for at least 2 days. Intravenous administration should be replaced by the subsequent oral administration of azithromycin in as a single daily dose of 500 mg until the completion of a 7-10 day general course of treatment.

Infectious-inflammatory diseases of the pelvic organs

500 mg once a day intravenously for at least 2 days. Intravenous administration should be replaced by the subsequent oral administration of azithromycin in the form of a single daily dose of 250 mg until the complete 7 day total course of treatment.

The timing of the transition to oral treatment is determined in accordance with the data of the clinical examination.

Patients with hepatic and renal insufficiency

For patients with moderate impairment of liver and kidney function (creatinine clearance> 40 ml / min) dose adjustment is not needed.

Solution for infusion is prepared in 2 stages:

Stage 1 - preparation of the reconstituted solution:

4.8 ml of sterile water for injections are added to a bottle of 500 mg of the drug and shaken carefully until the powder is completely dissolved.

In 1 ml of the resulting solution contains 100 mg of azithromycin.

The prepared solution remains stable for 24 hours at room temperature.

Stage 2 - dilution of the reconstituted solution (100 mg / ml) is carried out immediately before the introduction in accordance with the table below.

The concentration of azithromycin in the infusion solution Quantity of solvent

1.0 mg / ml 500 ml

2.0 mg / ml 250 ml

The reconstituted solution is introduced into a vial of solvent (0.9% sodium chloride solution, 5% dextrose, Ringer's solution) to obtain a final concentration of azithromycin of 1.0-2.0 mg / ml in the infusion solution.

A solution of hemomycin can not be administered intravenously by struino or intramuscular injection! It is recommended to inject the prepared solution intravenously in the form of infusion, drip (at least 1 hour).

Before injection, the solution is visually inspected. If the finished solution contains particles of the substance, then it should not be used.

The prepared solution is stable at room temperature for 24 hours.

Side effects:

From the central nervous system: dizziness / vertigo, headache, drowsiness convulsions; paresthesia, asthenia, insomnia, increased excitability, fainting, aggressiveness, anxiety, nervousness.

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

From the side of the cardiovascular system: palpitations, arrhythmias, including ventricular tachycardia, increased interval QT, bidirectional ventricular tachycardia, lowering blood pressure.

From the digestive system, nausea, vomiting, diarrhea, abdominal pain and spasms, loose stools, flatulence, digestive disorders, cholestatic jaundice, hepatitis, gastritis,change in laboratory parameters of liver function, constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, hepatic insufficiency (possibly fatal).

From the side of the circulatory and lymphatic systems: thrombocytopenia, neutropenia, leukopenia, neutrophilia.

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

From the side of the musculoskeletal system: arthralgia.

From the genitourinary system: nephritis, acute renal failure.

Local Reactions: pain and inflammation at the injection site.

Other: Candidiasis, incl. oral cavity and genital organs, fatigue, malaise, anorexia, vaginitis.

Overdose:

Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea, abdominal pain, impaired liver function.

Treatment: symptomatic.

Interaction:

Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir,midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, rifabutin and methylprednisolone in the blood in a joint application.

If it is necessary to share with cyclosporine, it is recommended to monitor the content of cyclosporine in the blood.

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

When used together with anticoagulants of indirect action (warfarin, etc. anticoagulants coumarinovogo series) it is recommended to conduct patients careful monitoring of prothrombin time.

Simultaneous use of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening QT interval. It is necessary to take into account these data in the joint use of terfenadine and azithromycin.

When combined with nelfinavir may increase the incidence of side effects from azithromycin.

The possibility of inhibiting the isoenzyme should be considered CYP3A4 azithromycin when combined with cyclosporine, terfenadine, ergot alkaloids, cisapride,pimozide, quinidine, astemizole and other drugs, the metabolism of which occurs with the participation of this enzyme.

With the joint use 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. So far, the clinical significance of this fact has not been determined.

With the joint use of azithromycin with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) is possible.

Pharmaceutically incompatible with heparin.

Special instructions:

The safety of the use and effectiveness of the injectable form of the drug Hemomycin in children under 16 years is not established.

Do not administer the drug with longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow the use of a short dosing regimen.

It is possible to attach superinfection (including fungal) in the treatment with Hemomycin (as in any antibiotic therapy).

When using the drug Hemomycin may develop diarrhea / pseudomembranous colitis caused by Clostridium difficile. In this regard, patients with diarrhea should be carefully observed.

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:

Given the likelihood of side effects from the central nervous system, it should be observed caution when driving vehicles and machinery.

Form release / dosage:

Lyophilizate for the preparation of a solution for infusions of 500 mg.

Packaging:

500 mg of the active ingredient is placed in a bottle of colorless glass 1 of the hydrolytic class, sealed with a rubber stopper and sealed with an aluminum cap with a liner in the form of a plastic disc (first opening control). 1 bottle with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature of 10 to 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000362

Date of registration:22.02.2011

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

HEMOFARM, A.D. Serbia

Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia

Information update date: & nbsp19.08.2015

Illustrated instructions

Instructions

Hemomycin (Hemomycin)