Azithromycin Express, 500 mg 3 pcs

Indications

Infectious inflammatory diseases caused by microorganisms sensitive to the drug:

Active ingredient

Composition

Composition per tablet:

How to take, the dosage

Ingestion.

Take 1 hour before or 2 hours after a meal.

The dispersible tablet can be swallowed whole with water, or the dispersible tablet can be dissolved in at least 50 ml of water. The suspension should be mixed thoroughly before drinking.

Adults and children over 12 years of age with a body weight of more than 45 kg

Infections of the upper and lower respiratory tract, ENT organs, skin and soft tissue:

500 mg once daily for 3 days (course dose of 1.5 g).

In Lyme disease (initial stage of borreliosis) – erythema migrans: Once daily for 5 days: day 1 – 1000 mg, then from day 2 to day 5 – 500 mg (cumulative dose 3.0 g).

Infections of the urogenital tract caused by Chlamydia trachomatis (urethritis, cervicitis): uncomplicated urethritis/cervicitis – 1000 mg once.

Patients with renal insufficiency:In patients with a FFR of 10-80 ml/min, no dose adjustment is required. Patients with a GFR < 10 ml/min should be taken with caution.

Patients with hepatic impairment: no dose adjustment is required in patients with mild to moderate hepatic impairment.

Elderly persons:Dose adjustment is not required. Caution should be exercised in elderly patients with persistent proarrhythmogenic factors due to the high risk of arrhythmias, including pirouette-type arrhythmias.

Interaction

Antacid drugs

The antacid drugs do not affect the bioavailability of azithromycin, but decrease the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and meals.

Cetirizine

Concomitant use for 5 days in healthy volunteers of azithromycin with cetirizine (20 mg) did not result in a pharmacokinetic interaction or significant change in QT interval.

Didanosine (didezoxynosine)

The concomitant use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients showed no change in the pharmacokinetic readings of didanosine compared with the placebo group.

Digoxin and colchicine (P-glycoprotein substrates)

. Concomitant use of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates such as digoxin and colchicine results in increased serum P-glycoprotein substrate concentrations. Thus, when concomitant use of azithromycin and digoxin is necessary to consider the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The concomitant use of azithromycin (single administration of 1000 mg and multiple administration of 1200 mg or 600 mg) has little effect on pharmacokinetics, including renal excretion of zidovudine or its glucuronide metabolite. However, azithromycin administration caused an increase in the concentration of phosphorylated zidovudine, the clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

Azithromycin interacts weakly with cytochrome P450 isoenzymes. Azithromycin has not been found to be involved in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor and inducer of cytochrome P450 isoenzymes.

Sorgonum alkaloids

In view of the theoretical possibility of ergotism, concomitant use of azithromycin with derivatives of ergot alkaloids is not recommended.

Pharmacokinetic studies have been performed on the concomitant use of azithromycin and drugs metabolized by cytochrome P450 isoenzymes.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in plasma concentrations of atorvastatin (based on HMK-CoA reductase inhibition analysis). However, in the post-registration period there were isolated reports of cases of rhabdomyolysis in patients receiving azithromycin and statins simultaneously.

Carbamazepine

Pharmacokinetic studies with healthy volunteers showed no significant effect on plasma concentrations of carbamazepine and its active metabolite in patients receiving azithromycin concomitantly.

Cimetidine

In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were found, provided that cimetidine was used 2 hours before azithromycin.

Indirect-acting anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single dose of 15 mg warfarin taken by healthy volunteers. Potentiation of anticoagulant effect has been reported after concomitant use of azithromycin and indirect anticoagulants (coumarin derivatives). Despite the fact that a causal relationship has not been established, the need for frequent monitoring of prothrombin time should be considered when using azithromycin in patients receiving oral anticoagulants of indirect action (coumarin derivatives).

Cyclosporine

. In a pharmacokinetic study involving healthy volunteers who took oral azithromycin (500 mg/day once) for 3 days followed by cyclosporine (10 mg/kg/day once), there was a significant increase in maximum plasma concentration (Cmax) and the area under the concentration-time curve (AUC0-5) of cyclosporine. Caution should be exercised when concomitant use of these drugs. If concomitant use of these drugs is necessary, plasma concentrations of cyclosporine should be monitored and the dose should be adjusted accordingly.

Efavirenz

The concomitant use of azithromycin (600 mg/day once) and efavirenz
(400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole

Concomitant use of azithromycin (1200 mg once daily) did not alter the pharmacokinetics of fluconazole (800 mg once daily). Total exposure and half-life of azithromycin were not altered by concomitant use of fluconazole, but there was a decrease in Cmax of azithromycin (by 18%), which had no clinical significance.

Indinavir

Concomitant use of azithromycin (1200 mg once) had no statistically significant effect on the pharmacokinetics of indinavir (800 mg three times daily for 5 days).

Methylprednisolone

Asithromycin has no significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times daily) causes increased equilibrium serum concentrations of azithromycin. No clinically significant adverse effects have been observed and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin
Simultaneous use of azithromycin and rifabutin has no effect on the serum concentrations of either drug. Neutropenia has sometimes been observed with concomitant use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil

When used in healthy volunteers, there was no evidence of an effect of azithromycin (500 mg/day daily for 3 days) on AUC and Cmax of sildenafil or its major circulating metabolite.

Terfenadine

In pharmacokinetic studies there has been no evidence of interaction between azithromycin and terfenadine. There have been isolated cases reported in which the possibility of such an interaction could not be completely excluded, but there has been no specific evidence that such an interaction has occurred.

The concomitant use of terfenadine and macrolides has been found to cause arrhythmias and prolongation of the QT interval.

Theophylline

No interaction between azithromycin and theophylline has been identified.

Triazolam/midazolam

There are no significant changes in pharmacokinetic parameters when azithromycin is used simultaneously with triazolam or midazolam in therapeutic doses.

Trimethoprim/sulfamethoxazole

The concomitant use of trimethoprim/sulfamethoxazole with azithromycin showed no significant effect on Cmax, total exposure, or renal excretion of trimethoprim or sulfamethoxazole. Serum azithromycin concentrations were consistent with those found in other studies.

Special Instructions

If one dose of Azithromycin EXPRESS is missed, the missed dose should be taken as soon as possible and the subsequent doses should be taken 24 hours apart.

Azithromycin EXPRESS should be taken at least one hour before or two hours after taking antacids.

The drug Azithromycin EXPRESS should be used with caution in patients with mild to moderate hepatic impairment because of the possibility of fulminant hepatitis and severe hepatic failure.

In the presence of symptoms of hepatic impairment such as: rapidly increasing asthenia, jaundice, darkened urine, bleeding tendency, hepatic encephalopathy – therapy with Azithromycin EXPRESS should be stopped and liver function tests should be performed.

In patients with renal dysfunction: in patients with GFR 10-80 ml/min the dose adjustment is not required, in patients with GFR 10 ml/min there was observed a 33% increase of systemic effect of azithromycin. Therapy with this drug should be carried out with caution under monitoring of renal function status.

As with other antibacterial agents, during therapy with Azithromycin EXPRESS, patients should be regularly monitored for the presence of non-susceptible microorganisms and signs of superinfections, including fungal infections.

The drug Azithromycin EXPRESS should not be used for longer courses than directed, since the pharmacokinetic properties of azithromycin allow a short and simple dosing regimen to be recommended.

There are no data on possible interactions between azithromycin and ergotamine and dihydroergotamine derivatives, but because of the development of ergotism when using macrolides with ergotamine and dihydroergotamine derivatives simultaneously, this combination is not recommended.

The development of pseudomembranous colitis caused by Clostridium difficile, both as mild diarrhea and severe colitis, is possible with long-term administration of Azithromycin EXPRESS. If antibiotic-associated diarrhea develops against the background of Azithromycin EXPRESS therapy, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. Drugs inhibiting intestinal peristalsis are contraindicated.

In treatment with macrolides, including azithromycin, prolongation of cardiac repolarization and QT interval have been observed, increasing the risk of cardiac arrhythmias, including pirouette arrhythmias.

Caution should be exercised when using Azithromycin EXPRESS: In patients with the presence of proarrhythmogenic factors (especially in elderly patients), including congenital or acquired QT interval prolongation; in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin) In patients with water-electrolyte balance disorders, especially in case of hypokalemia or hypomagnesemia; in patients with clinically significant bradycardia, cardiac arrhythmia, or severe heart failure.

The use of Azithromycin EXPRESS may provoke myasthenic syndrome or worsen myasthenia gravis.

As with the use of erythromycin and other macrolides, there have been isolated cases of serious allergic reactions, including angioedema and anaphylaxis (rarely fatal), dermatological reactions, including acute generalized exanthematous pustulosis (OGEP), Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS syndrome) (see side effects). Some of the reactions were recurrent and required longer follow-up and treatment.

If an allergic reaction develops, the drug should be discontinued and appropriate treatment initiated. It should be noted that after withdrawal of symptomatic therapy, symptoms of an allergic reaction may return.

Influence on driving and operating ability

In case of adverse effects on the nervous system and visual system, caution should be exercised when performing activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Contraindications

Hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides or other drug components; severe hepatic impairment; phenylketonuria; children under 12 years of age with body weight less than 45 kg; simultaneous use with ergotamine and dihydroergotamine.

With caution

Myasthenia; mild to moderate hepatic impairment; terminal renal failure with GFR (glomerular filtration rate) less than 10 ml/min; in patients with proarrhythmogenic factors (especially in older patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with electrolyte balance disorders, especially in case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; concomitant use of digoxin, warfarin, cyclosporine.

Side effects

The following classification is used to determine the frequency of side effects of the drug: very often (≥ 1/10); often (≥ 1/100 and < 1/10); infrequently
(≥ 1/1000 and < 1/100); rarely (≥ 1/10000 and < 1/1000); very rarely (< 1/10000); frequency is unknown (cannot be determined based on available data).

Infectious and parasitic diseases: infrequent – candidiasis, including oral mucosa, vaginal infection, pneumonia, fungal infection, bacterial infection, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; unknown frequency – pseudomembranous colitis.

Blood and lymphatic system disorders: frequently – leukopenia, neutropenia, eosinophilia; very rarely – thrombocytopenia, hemolytic anemia.

From the immune system: infrequent – angioedema, hypersensitivity reaction; unknown frequency – anaphylactic reaction.

Metabolism and nutrition: infrequently – anorexia.

From the nervous system: frequent – headache; infrequent – dizziness, taste disturbance, paresthesias, somnolence, insomnia, nervousness; frequent – agitation; unknown frequency – hypoesthesia, anxiety, aggression, fainting, seizures, psychomotor hyperactivity, loss of smell, perversion of sense of smell, loss of taste, myasthenia, delirium, hallucinations.

Visual organ: not infrequently – visual impairment.

Hearing and labyrinth organ side: infrequent – hearing disorder, vertigo; unknown frequency – hearing disorder, including deafness and/or tinnitus.

Cardiac side: infrequent – palpitations, unknown frequency -increase of QT interval on electrocardiogram, “pirouette” type arrhythmia, ventricular tachycardia.

vascular side: infrequent – “rushes” of blood to the face; unknown frequency – lowering of blood pressure.

Respiratory system, chest and mediastinal organs:infrequent – shortness of breath, nasal bleeding.

From the gastrointestinal tract: very often – diarrhea; often – nausea, vomiting, abdominal pain; infrequently – flatulence, dyspepsia, constipation, gastritis, dysphagia, abdominal bloating, dry oral mucosa, belching, oral mucosa ulcers, increased salivary gland secretion; very rarely – color change of tongue, pancreatitis.

From the liver and biliary tract: frequently – hepatitis; frequently – impaired liver function, cholestatic jaundice; unknown frequency – liver failure (rarely fatal, mostly in the background of severe liver dysfunction); hepatic necrosis, fulminant hepatitis.

Skin and subcutaneous tissue: frequent – skin rash, pruritus, urticaria, dermatitis, dry skin, sweating; seldom – photosensitization reaction; acute generalized exanthematous pustulosis (OGEP); unknown frequency – Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS syndrome).

Skeletal and muscular system disorders: infrequent – osteoarthritis, myalgia, back pain, neck pain; unknown frequency – arthralgia.

Kidney and urinary tract side: infrequent – dysuria, renal pain; unknown frequency – interstitial nephritis, acute renal failure.

Reproductive organs and mammary glands: infrequent – metrorrhagia, impaired testicular function.

Others: infrequent – edema, asthenia, malaise, feeling of fatigue, facial edema, chest pain, fever, peripheral edema.

Laboratory and instrumental findings: frequently – decreased lymphocyte count, increased eosinophil count, increased basophil count, increased monocyte count, increased neutrophil count, decreased plasma bicarbonate concentration; infrequently – increased aspartate aminotransferase activity, alanine aminotransferase activity, increased plasma bilirubin concentration, increased plasma urea concentration, increased plasma creatinine concentration, changes in plasma potassium content, increased plasma alkaline phosphatase activity, increased plasma chloride concentration, increased blood glucose concentration, increased platelet count, decreased hematocrit, increased plasma bicarbonate concentration, change in plasma sodium concentration.

Overdose

Symptoms:Nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: symptomatic.

Pregnancy use

Pregnancy

In pregnancy, use only if the expected benefit to the mother exceeds the potential risk to the fetus.

The WHO recommends azithromycin as the drug of choice in the treatment of chlamydial infection in pregnant women.

Breastfeeding

Breastfeeding is used only if the expected benefit to the mother exceeds the potential risk to the baby. If it is necessary to use the drug during breastfeeding it is recommended to stop breastfeeding.

Similarities