Azithromycin, 500 mg 3 pcs

Pharmacotherapeutic group: Azalid antibiotic

ATC code: J01FA10

Pharmacodynamics:

Azithromycin is a bacteriostatic broad spectrum antibiotic of the group of macrolides-azalids. It has a broad spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with inhibition of microbial cell protein synthesis.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

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

– lower respiratory tract infections (acute bronchitis, exacerbation of chronic bronchitis);

– community-acquired pneumonia, incl. caused by atypical pathogens (see section “Special instructions”);

– infections of the skin and soft tissues (moderate acne vulgaris, erysipelas, impetigo, secondary infected dermatoses);

– the initial stage of Lyme disease (borreliosis) – erythema migrans;

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

Pharmacological effect

Pharmacotherapeutic group: Antibiotic-azalide

ATX code: J01FA10

Pharmacodynamics:

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the macrolide-azalide group. Has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis in microbial cells.

Special instructions

If you miss one dose of Azithromycin, the missed dose should be taken as soon as possible and subsequent doses should be taken at intervals of 24 hours. The drug Azithromycin should not be used for the treatment of pneumonia in patients for whom oral therapy is impossible due to the severity of the disease and/or who have the following risk factors: cystic fibrosis, bacteremia or suspected conditions that can change the body’s response to the disease (immunodeficiency, functional asplenia, etc.) patients requiring hospitalization, elderly or debilitated patients.

Azithromycin should be used with caution in patients with mild to moderate liver dysfunction due to the possibility of developing fulminant hepatitis and severe liver failure.

If there are symptoms of impaired liver function such as rapidly increasing asthenia, jaundice, darkening of urine, tendency to bleeding, hepatic encephalopathy, therapy with Azithromycin should be stopped and a study of the functional state of the liver should be performed.

In case of mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min), therapy with Azithromycin should be carried out with caution under monitoring the state of renal function. In end-stage renal failure (creatinine clearance less than 10 ml/min), there is an increase in the concentration of azithromycin in the blood plasma by 33%.

The development of resistance of microorganisms is possible if the recommended duration of therapy courses is not observed. As with the use of other antibacterial drugs during therapy with Azithromycin, patients should be regularly examined for the presence of non-susceptible microorganisms and signs of the development of superinfections, including fungal ones.

The drug Azithromycin should not be used in longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.

It must be remembered that for the prevention of pharyngitis/tonsillitis caused by Streptococcus pyogenes as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin.

With long-term use of the drug Azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis, is possible. If diarrhea develops while taking Azithromycin, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. The use of drugs that inhibit intestinal motility is contraindicated.

Slow ventricular repolarization syndrome – QT interval prolongation syndrome – increases the risk of developing arrhythmias, including pirouette-type arrhythmias, while taking macrolides and azithromycin. Caution when using azithromycin should be observed in patients with prolongation of the QT interval receiving therapy with class IA III antiarrhythmic drugs cisapride for hypokalemia or hypomagnesemia, clinically significant bradycardia, arrhythmia or severe heart failure.

Caution should be exercised when using Azithromycin simultaneously with antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), cyclosporine, as well as in elderly patients.

The use of Azithromycin may provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Impact on the ability to drive vehicles. Wed and fur.:

If undesirable effects on the nervous system and organ of vision develop, caution should be exercised when performing actions that require increased concentration and speed of psychomotor reactions.

Active ingredient

Azithromycin

Composition

One film-coated tablet contains:

active substance:

azithromycin dihydrate (in terms of azithromycin) – 500,000 mg;

excipients:

microcrystalline cellulose – 36,000 mg;

lactose monohydrate – 33.464 mg;

povidone K-30 – 26,000 mg;

crospovidone – 26,000 mg;

sodium lauryl sulfate – 1,300 mg;

colloidal silicon dioxide – 6,600 mg;

magnesium stearate – 6,600 mg;

film coating: [hypromellose – 12,000 mg, talc – 4,000 mg, titanium dioxide – 2,200 mg, macrogol 4000 (polyethylene glycol 4000) – 1,800 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] – 20,000 mg.

Pregnancy

Azithromycin is used during pregnancy only in cases where the benefit to the mother outweighs the possible risk to the fetus. During treatment with azithromycin, breastfeeding is suspended.

Contraindications

– hypersensitivity to azithromycin, erythromycin, other macrolides, ketolides or other components of the drug;

– severe liver dysfunction;

– severe renal impairment (creatinine clearance (CC) less than 40 ml/min);

– children under 12 years of age with body weight less than 45 kg (for tablets 500 mg);

– children under 3 years of age (for tablets 125 mg);

– breastfeeding period;

– simultaneous use with ergotamine and dihydroergotamine;

– lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution:

Pregnancy; myasthenia gravis; mild to moderate liver dysfunction; mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min); elderly patients; in patients with the presence of proarrhythmic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval in patients receiving therapy with antiarrhythmic drugs class IA (quinidine procainamide) III (dofetilide amiodarone and sotalol) cisapride terfenadine antipsychotic drugs (pimozide) antidepressants (citalopram) fluoroquinolones (moxifloxacin levofloxacin) with impaired water and electrolyte balance, especially in the case of hypokalemia or hypomagnesemia with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of digoxin, varfarin, cyclosporine.

Side Effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often – at least 10%; often – not less than 1% but less than 10%; infrequently – not less than 01% but less than 1%; rarely – not less than 001% but less than 01%; very rare – less than 001% (including isolated cases).

Infectious diseases:

uncommon – candidiasis, including the mucous membrane of the oral cavity and genitals;

very rarely – pseudomembranous colitis.

Metabolism and nutrition: often – anorexia.

Allergic reactions:

often – skin itching, skin rash;

uncommon – hypersensitivity reactions photosensitivity reaction urticaria Stevens-Johnson syndrome angioedema;

very rarely – anaphylactic reaction, erythema multiforme, toxic epidermal necrolysis.

From the blood and lymphatic systems:

often – eosinophilia, lymphopenia;

uncommon – leukopenia, neutropenia;

very rarely – thrombocytopenia, hemolytic anemia.

From the respiratory system:

uncommon – pneumonia pharyngitis respiratory diseases rhinitis shortness of breath nosebleeds.

From the nervous system:

often – headache, dizziness, paresthesia, disturbance of taste; infrequently – hypoesthesia drowsiness insomnia nervousness;

rarely – agitation;

very rarely – anxiety aggression fainting convulsions psychomotor hyperactivity loss of smell (or anosmia) and taste myasthenia gravis anxiety;

frequency unknown – perversion of smell, delusions, hallucinations.

From the side of the organ of vision: often – blurred vision.

Hearing and labyrinth disorders:

often – deafness;

uncommon – tinnitus, hearing disorder;

rarely – vertigo.

From the cardiovascular system:

infrequently – a feeling of heartbeat, “flushes” of blood to the skin of the face;

very rarely – decreased blood pressure, increased QT interval, pirouette-type arrhythmia, ventricular tachycardia.

From the gastrointestinal tract:

very often – nausea, flatulence, abdominal pain, diarrhea;

often – dyspepsia, vomiting;

uncommon – constipation gastritis gastroenteritis dysphagia bloating dry oral mucosa belching ulcers of the oral mucosa increased secretion of the salivary glands;

very rarely – discoloration of the tongue, pancreatitis.

From the liver and biliary tract:

infrequently – increased activity of liver transaminases, increased concentration of bilirubin, hepatitis;

rarely – liver dysfunction;

very rarely – cholestatic jaundice, liver failure (in rare cases with death, mainly due to severe liver dysfunction), liver necrosis, fulminant hepatitis.

From the skin:

uncommon – dermatitis, dry skin, increased sweating.

From the musculoskeletal system and connective tissue:

often – arthralgia;

uncommon – osteoarthritis myalgia back pain neck pain.

From the genitourinary system:

infrequently – increased concentrations of urea and creatinine in the blood plasma, dysuria, pain in the kidneys, metrorrhagia, testicular dysfunction;

very rarely – interstitial nephritis, acute renal failure. Laboratory indicators:

often – a decrease in the concentration of bicarbonates in the blood plasma, an increase in the number of: basophils, monocytes, neutrophils;

uncommon – increased platelet count, increased hematocrit; increased alkaline phosphatase activity increased chlorine content increased glucose concentration in the blood plasma increased bicarbonate concentration in the blood plasma change in sodium content in the blood plasma change in potassium concentration.

Others:

often – weakness;

uncommon – chest pain, peripheral edema, asthenia, malaise, feeling of fatigue, swelling of the face, fever.

Interaction

Antacids do not affect the bioavailability of azithromycin but reduce the maximum concentration in the blood by 30%; therefore, azithromycin should be taken at least one hour before or two hours after taking these drugs or eating.

Azithromycin does not affect the plasma concentrations of carbamazepine cimetidine didanosine efavirenz fluconazole indinavir midazolam triazolam trimethoprim/sulfamethoxazole cetirizine sildenafil and methylprednisolone when used simultaneously. Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on an HMC-CoA reductase inhibition assay).

However, in the post-registration period, isolated reports of cases of rhabdomyolysis in patients receiving azithromycin and statins simultaneously were received.

The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood plasma. With simultaneous use of azithromycin and rifabutin, neutropenia was sometimes observed. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) and then cyclosporine (10 mg/kg/day once) orally for three days, a significant increase in the maximum plasma concentration and the area under the concentration-time curve of cyclosporine was detected. Caution should be exercised when using these drugs simultaneously.

If it is necessary to use these drugs simultaneously, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

When using digoxin and azithromycin simultaneously, it is necessary to monitor the concentration of digoxin in the blood plasma because many macrolides increase the absorption of digoxin in the intestine.

If simultaneous use with indirect anticoagulant agents (such as warfarin and other coumarin-type anticoagulants) is necessary, careful monitoring of prothrombin time is recommended.

It was found that the simultaneous use of terfenadine and macrolide antibiotics causes arrhythmia and prolongation of the QT interval. Based on this, the above complications cannot be excluded when taking terphenadine and azithromycin simultaneously.

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentrations of azithromycin in blood plasma. No clinically significant side effects were observed and no dose adjustment of azithromycin was required when used concomitantly with nelfinavir.

Azithromycin weakly interacts with isoenzymes of the cytochrome P450 system; It has not been revealed that azithromycin is involved in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inducer or inhibitor of isoenzymes of the cytochrome P450 system.

There was no interaction between azithromycin and theophylline.

When used concomitantly with zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or the nocturnal elimination of it and its glucuronide metabolite. Nevertheless, the concentration of the active metabolite of phosphorylated zidovudine in mononuclear cells of peripheral vessels increases. The clinical significance of this fact is not clear.

With the simultaneous use of macrolides with ergotamine and dihydroergotamine, their toxic effect may occur.

Considering the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Overdose

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

Treatment: symptomatic.

Storage conditions

Store in a place protected from light at a temperature not exceeding 25°C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after expiration date.

Manufacturer

Ozon, Russia