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Despiron- suspension granules

INSTRUCTIONS FOR MEDICAL USE

DESPIRON

Trade name of the drug: Despirone

Active substance (INN): Spiramycin

Form release: granules for preparation of suspension for oral administration.

Contents:

Each 5 ml of the suspension contains:

active substance: spiramycin – 1.5 million IU (333 mg).

Excipients: crosspovidone, sodium benzoate, xanthan gum, sucrose, sucralose, flavoring (vanilla multicomponent).

Description: almost white or slightly yellowish pellets with a smell of vanillin.

Pharmacotherapeutic group: Antibiotics (gr. macrolides)

ATX code: J01FA02

Pharmacological properties

It is an antibiotic of macrolide group. The mechanism of antibacterial action is caused by inhibition of protein synthesis in a microbial cell at the expense of binding to 50S-subunit of ribosome.

Sensitive microorganisms (MAC<1 mg/l): Gram-positive aerobes – Bacillus cereus, Corynebacterium diphtheriae, Enterococcus spp., Rhodococcus equi, Staphylococcus spp. (methicillin-sensitive and methicillin-resistant strains), Streptococcus B, unclassified Streptococcus, Streptococcus pneumoniae, Streptococcus pyogenes; Gram-negative aerobes – Bordetella pertussis, Branhamella catarrhalis, Campylobacter spp, Legionella spp., Moraxella spp.; anaerobes – Actinomyces spp., Bacteroides spp., Eubacterium spp., Mobiluncus spp., Peptostreptococcus spp., Porphyromonas spp., Prevotella spp, Propionibacterium acnes; different – Borrelia burgdorferi, Chlamydia spp., Coxiella spp., Leptospiria spp., Mycoplasma pneumoniae, Treponema pallidum, Toxoplasma gondii.

Moderately susceptible microorganisms (antibiotic is moderately active in vitro at antibiotic concentrations in the focus of inflammation ≥ 1 mg/L, but < 4 mg/L): Gram-negative aerobes – Neisseria gonorrhoeae; aerobes – Clostridium perfringens; various – Ureaplasma urealyticum.

Resistant microorganisms (MPC>4 mg/l; at least 50% of strains are resistant): Gram-positive aerobes – Corynebacterium jekeium, Nocardia asteroides; Gram-negative aerobes – Acinetobacter spp., Enterobacter spp., Haemophilus spp., Pseudomonas spp.; anaerobes – Fusobacterium spp.; miscellaneous – Mycoplasma hominis.

Pharmacokinetics

Absorption

Absorption of spiramycin is rapid but incomplete, with wide variability (10% to 60%). After an oral dose of 6 million IU, the Cmax of spiramycin in plasma is about 3.3 µg/ml. Absorption is not affected by food intake.

Distribution

Binding to plasma proteins is low (approximately 10%). Vd about 383 l. The drug penetrates well into saliva and tissues (concentration in lungs is 20-60 µg/g, in tonsils

  • 20-80 µg/g, in infected sinuses 75-110 µg/g, in bones 5-100 µg/g). 10 days after the end of treatment, spiramycin concentration in spleen, liver, kidney is 5-7 µg/g.

Penetrates through the placental barrier (fetal blood concentrations are approximately 50% of those in maternal serum). Concentrations in placental tissue are 5 times higher than the corresponding concentrations in blood serum. It is excreted with breast milk. Spiramycin does not penetrate the cerebrospinal fluid.

Metabolism and excretion

Spiramycin is metabolized in the liver to form active metabolites with an unspecified chemical structure.

T1/2 from plasma is about 8 hours. It is mainly excreted in the bile (concentration is 15-40 times higher than in serum). Renal excretion is about 10% of the administered dose. The amount of drug excreted in the intestine (with feces) is very low.

INDICATIONS FOR USE

Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:

  • Acute and chronic pharyngitis caused by beta-haemolytic streptococcus A (as an alternative to treatment with beta-lactam antibiotics, especially in case of contraindications to their use);
  • acute sinusitis (given the sensitivity of the most common microorganisms that cause this pathology, the use of the drug is indicated if there are contraindications to the use of beta-lactam antibiotics)
  • acute and chronic tonsillitis caused by spiramycin-sensitive microorganisms;
  • acute bronchitis caused by a bacterial infection that developed after acute viral bronchitis;
  • exacerbation of chronic bronchitis;
  • community-acquired pneumonia in patients without risk factors for adverse outcome, severe clinical symptoms, and clinical signs of pneumococcal etiology of pneumonia;
  • pneumonia caused by atypical pathogens (such as Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae, Legionella spp.) or suspected (regardless of severity and presence or absence of risk factors for adverse outcome);
  • skin and subcutaneous tissue infections, including impetigo, impetiginosis, ecthyma, infectious dermohypodermitis (especially rye), secondary infectious dermatoses, erythrasma;
  • Oral infections (including stomatitis, glossitis);
  • Non-nococcal genital infections;
  • Toxoplasmosis, including in pregnancy;
  • Infections of the musculoskeletal system and connective tissue, including periodontal. Prevention of rheumatism recurrence in patients allergic to beta-lactam antibiotics. Eradication of Neisseria meningitidis from the nasopharynx (when contraindicated to take rifampicin) for prevention (but not treatment) of meningococcal meningitis:
  • In patients after treatment and before leaving quarantine;
  • in patients who have been in contact with persons who have excreted Neisseria meningitidis with saliva into the environment for 10 days before hospitalization.

Administration and dosages

The drug is taken orally.

Method of suspension preparation: suspension is prepared immediately before use. Pellets are shaken in vial, boiled water cooled to room temperature is added to the mark and mixed to get a homogeneous suspension.

Adults are prescribed 6-9 million IU per day. The daily dose is divided into 2 or 3 doses. The maximum daily dose is 9 million IU.

A daily dose of only 1.5 million IU should be used in children and adolescents aged 6 to 18 years.

In children over 6 years of age the daily dose is from 150,300,000 ME per kg of body weight, which is divided into 2 or 3 doses to 6 to 9 million ME. Maximum daily dose in children is 300,000 ME per kg of body weight, but if a child weighs more than 30 kg, it should not exceed 9 million ME.

For prevention of meningococcal meningitis in adults we use 3 million ME twice a day for 5 days, in children – 75000 ME/kg of body weight twice a day for 5 days. Patients with impaired renal function due to insignificant renal excretion of spiramycin do not require dose adjustment.

Side effects

The following classification was used to indicate the incidence of adverse reactions: very common (≥10%), common (≥1%, <10); infrequent (≥0.1%, <1%); rare (≥0.01%, <0.1%), very rare, including some reports (<0.01%), the incidence is unknown (according to available data the frequency cannot be determined).

Digestive system: nausea, vomiting, diarrhea; very rare – pseudomembranous colitis (<0.01%); frequency unknown – ulcerative esophagitis, acute colitis, acute intestinal mucosal damage in patients with AIDS while using spiramycin in high doses for cryptosporidiosis (only 2 cases).

Liver and biliary tract: very rare (<0.01%) – deviation of liver function tests from normal values; cholestatic or mixed hepatitis.

Nervous system: very rare (isolated cases) – transient paresthesia.

Blood system: very rare (<0.01%) – acute hemolysis.

Cardiovascular system: very rare – prolongation of QT interval on ECG.

Immune system: skin rash, urticaria, itching, very rare (<0.01%) – angioedema, anaphylactic shock, in some cases – vasculitis, including Schoenlein-Henoch purpura.

Skin and subcutaneous tissue: very rare – acute generalized exanthematous pustulosis.

Contraindications

  • lactation period;
  • glucose-6-phosphate dehydrogenase deficiency (risk of acute hemolysis);
  • Hypersensitivity to the drug components.

Caution is exercised when bile duct obstruction and hepatic insufficiency are prescribed.

Patients with impaired renal function due to low renal excretion of spiramycin a dose change is not required.

Drug interactions

Spiramycin inhibits absorption of carbidopa with a decrease in plasma concentrations of levodopa. Clinical monitoring and dose adjustment of levodopa is required when spiramycin is concomitantly administered.

Numerous cases of increased activity of indirect anticoagulants in patients taking antibiotics have been reported. The type of infection or severity of the inflammatory reaction, age, and general condition of the patient are predisposing risk factors. In such circumstances, it is difficult to determine the extent to which the infection itself or its treatment plays a role in MHO changes. However, this effect is observed more frequently with certain groups of antibiotics, in particular with fluoroquinolones, macrolides, cyclines, sulfamethoxazole+trimethoprim combination, some cephalosporins.

Special indications

During treatment with the drug in patients with liver diseases, liver function should be periodically monitored.

If generalized erythema and pustules with high body temperature occur at the beginning of treatment, acute generalized exanthematous pustulosis should be suspected; if such a reaction occurs, treatment should be stopped, and further use of spiramycin, both in monotherapy and in combination, is contraindicated.

Effect on the ability to drive vehicles and operate machinery

There is no information about the negative effect of the drug on the ability to drive vehicles and engage in other potentially dangerous activities. However, the severity of the patient’s condition should be taken into account, which may affect attention and speed of psychomotor reactions. Therefore, the decision about the possibility of driving a car or engaging in other potentially hazardous activities in a particular patient should be made by the attending physician.

Pregnancy and lactation

The drug may be administered during pregnancy when indicated.

There is a wide experience of using the drug during pregnancy. Risk of transmitting toxoplasmosis to fetus during pregnancy is decreased from 25% to 8% if the drug is used in the first trimester, from 54% to 19% – in the second trimester, and from 65% to 44% – in the third trimester. No teratogenic or fetotoxic effects were observed.

Breast-feeding should be discontinued if the drug is administered during lactation, because penetration of spiramycin into the breast milk is possible.

Overdose

There are no known cases of spiramycin overdose.

Symptoms: nausea, vomiting, diarrhea are possible. Cases of prolongation of the QT interval, which is resolved on withdrawal of the drug, have been observed in infants receiving high doses of spiramycin or after IV administration of spiramycin in patients predisposed to QT interval prolongation.

Treatment: in case of spiramycin overdose ECG-monitoring is recommended with determination of QT interval duration, especially in the presence of risk factors (hypokalemia, congenital prolongation of the QT interval, simultaneous use of drugs that prolong the QT interval and cause development of ventricular tachycardia of “pirouette” type). There is no specific antidote. Symptomatic therapy is recommended in case of suspected spiramycin overdose.

Form of production

Granules for preparation of suspension 1.5 ml/5 ml 75 ml (vials with or without measuring spoon or cup).

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25 ° C. Period of storage of suspension after dilution at a temperature not exceeding 25 ° C for a maximum of 7 days, at 4 ° C for a maximum of 14 days.

Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription.

Azirem® Neo- capsules

INSTRUCTIONS FOR MEDICAL USE

AZIREM® NEO

Trade name of the drug: Azirem® Neo

Active substance (INN): Azithromycin

Dosage form: Capsules

Contents:

Each capsule contains:

Active ingredient: Azithromycin dihydrate (in terms of azithromycin) 250 mg and 500 mg.

Excipients: sodium starch glycolate, magnesium stearate.

Description: Solid gelatin capsules, white color, size “2” for 250 mg capsules and size “0” for 500 mg capsules, filled with powder of white or almost white color.

Pharmacotherapeutic group: Antibiotics (macrolide group).

ATX code: J01FA10.

Pharmacological properties

It is a broad-spectrum antibiotic. It is the first representative of a new subgroup of macrolide antibiotics – azalides. It has a bactericidal effect if it forms high concentrations in the inflammation focus.

Gram-positive cocci: Streptococcus pneumoniae, Stpyogenes, St.agalactiae, group C, F and G streptococci, St.viridans, Staphylococcus aureus are sensitive to the drug; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Legionella pneumophila, H. ducrei, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp. as well as Сhlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. It is inactive against erythromycin-resistant Gram-positive bacteria.

Pharmacokinetics

The drug is quickly absorbed from gastrointestinal tract, which is due to its resistance to acidic environment and lipophilicity. After 500 mg usage maximum concentration (Cmax) in plasma is reached after 2.5-2.96 hours and is 0.4 mg/ml. Bioavailability is 37%.

It penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland). High concentration in tissues (10-15 times higher than in blood plasma) and long half-life (T1/2) are caused by low binding of azithromycin with blood plasma proteins as well as its ability to penetrate into eukaryotic cells and to concentrate in low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (Vd) of 31.1 l/kg and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is particularly important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the sites of infection localization, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in the healthy tissues (on the average by 24-34%), and correlates with the degree of inflammatory edema. Despite its high concentration in phagocytes, azithromycin has no significant effect on their function. Azithromycin persists in bactericidal concentrations in the inflammatory focus for 5-7 days after the last dose, which allowed to develop short (3-day and 5-day) courses of treatment.

The drug is metabolized in the liver by demethylation.

Excretion of azithromycin from plasma is done in 2 stages: T1/2 is 14-20 hours, 8-24 hours after the last dose and 41 hours – 24-72 hours, which allows using the drug once a day.

It is eliminated mainly unchanged – 50% via the intestine, 6% – by the kidneys.

Indications for use

Infectious-inflammatory diseases caused by pathogens sensitive to the drug:

  • lower respiratory tract infections – bacterial and typical pneumonia, bronchitis;
  • infections of the upper respiratory tract and ENT organs – angina, sinusitis, tonsillitis, otitis media;
  • infections of the urogenital tract – uncomplicated urethritis, and/or cervicitis, cervicovaginitis and salpingitis;
  • skin and soft tissue infections – folliculitis, furuncles, carbuncles, acne (Acne vulgaris), impetigo, pyoderma, infected ulcers, infected dermatitis, cellulitis and rye;
  • Lyme disease (borreliosis), for treatment of the initial stage (Erythema migrans);
  • Diseases of the stomach and duodenum associated with Helicobacter pylori.

Dosage and administration method

The drug is taken 1 hour before a meal or 2 hours after a meal, once a day.

For adults with upper and lower respiratory tract infections, skin and soft tissue infections, 500 mg/day for 3 days (1.5 g course dose).

For Lyme disease (borreliosis), for treatment of initial stage (Erythema migrans) – 1 g on the 1st day and 500 mg daily from 2nd to 5th day (course dose – 3 g).

For uncomplicated urethritis and/or cervicitis 1 g is prescribed once.

For diseases of the stomach and duodenum associated with Helicobacter pylori 1 g daily for 3 days is prescribed.

For children, the drug is prescribed in doses of 10 mg/kg body weight once a day for 3 days. The course dose is 30 mg/kg of body weight.

For treatment of Erythema migrans in children, the dose is 20 mg/kg of body weight on day 1 and 10 mg/kg – on days 2 to 5.

Side effects

Digestive system disorders: nausea, vomiting, flatulence, abdominal pain, melena, cholestatic jaundice, constipation in children, gastritis, oral candidiasis, lack of appetite, transient increase of liver enzymes activity are possible.

Cardiovascular system: palpitations, chest pain.

Nervous system disorders: dizziness, headache, vertigo, somnolence, hyperkinesia, anxiety, neurosis, sleep disorders. Genitourinary system: vaginal candidomycosis, nephritis.

Allergic reactions: rash, urticaria, angioedema.

Other: hyperglycemia, arthralgia.

Contraindications

Hypersensitivity to antibiotics of macrolide group; severe hepatic and renal dysfunction; children under 12 years old and body weight less than 45 kg (for 500 mg capsules), children under 3 years old (for 250 mg capsules); pregnancy and lactation.

Drug interaction

Simultaneous use of antacids and histamine H2-receptor blockers does not change drug absorption, but decreases Cmax in blood by 30%.

Concomitant use of the drug does not affect the blood concentration of carbamazepine, didanosine, rifabutin and methylprednisolone.

Co-administration of terfenadine and macrolide class antibiotic causes arrhythmia and Q-T interval prolongation.

When concomitant use with ergot alkaloids the risk of ergotism cannot be excluded.

When concomitant use with warfarin there are described the cases of enhancing the effects of the latter.

Concomitant use of digoxin or digitoxin with azithromycin may cause a significant increase in the concentration of cardiac glycosides and risk of glycoside intoxication.

When concomitant use with cyclosporine, it is recommended to monitor the blood content of cyclosporine.

When concomitant use with lovastatin, cases of rhabdomyolysis have been described.

Concomitant use with rifabutin increases the risk of neutropenia and leukopenia.

Co-administration impairs the metabolism of cyclosporine, which increases the risk of adverse and toxic reactions caused by cyclosporine.

Special indications

If one dose of the drug is missed – the missed dose should be taken as soon as possible, and subsequent doses should be taken at 24-hour intervals.

As with any antibiotic therapy, treatment with azithromycin may lead to superinfections (including fungal).

Antacids, ethanol and food slow down and reduce absorption of azithromycin, therefore it is recommended to take a break of at least 2 hours between intake of azithromycin and the above mentioned drugs.

If it is necessary to use the drug in pregnancy, it is possible only in cases when the expected benefits to the mother increase the potential risk to the fetus.

If it is necessary to use azithromycin during lactation, discontinuation of breastfeeding should be considered.

The drug does not affect the ability to drive motor transport and other activities requiring high concentration and psychomotor reaction rate.

Overdose

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

Treatment: gastric lavage, prescription of activated charcoal, symptomatic therapy.

Form of production

Capsules, 250 mg №6 and 500 mg №3 in carton packs.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription.

Azirem ®- suspension

INSTRUCTIONS FOR MEDICAL USE

AZIREM

Trade name of the drug: Azirem®

Active substance (INN): Azithromycin

Dosage form: suspension

Contents:

5 ml of the suspension contains:

Active substance: Azithromycin – 200 mg.

Excipients: Guar gum, Trilon B (ETDA), acrylic polymer Cugop T-135, sucralose, sodium citrate, menthol, tween 80 (polysorbate-80), propylene glycol, peppermint oil, liquid sorbitol, sodium saccharine, methyl paraben (nipagin), propyl paraben (nipazole), banana flavor, orange flavor, purified water.

Description: white or almost white suspension.

Pharmacotherapeutic group: Antibiotics (macrolide group).

ATX code: J01FA10

Pharmacological properties

It is a broad-spectrum antibiotic. It is the first representative of the new generation of bacterial antibiotics – aazilogens. It has bacteriostatic properties, and in high concentrations in the inflammation focus it has bactericidal effect. The mechanism of action of azithromycin is associated with the inhibition of microbial cell protein synthesis. It binds with 50S ribosome subunit, inhibits peptide translocation stage and inhibits protein synthesis, inhibiting bacterial growth and reproduction.

Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, Staphylococcus aureus are sensitive to the drug; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp. as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.

It is inactive against erythromycin-resistant Gram-positive bacteria.

Pharmacokinetics

The drug is quickly absorbed from gastrointestinal tract, which is due to its stability in acidic environment and lipophilicity. After oral administration with a dose of 500 mg maximum concentration (Cmax) of azithromycin in blood plasma is reached after 2-3 hours and is 0.4 mg/l. Bioavailability is 37%. Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate), skin and soft tissue. Maximal concentration (in tissues and cells 10-50 times higher than in blood plasma) and long period of semiejection (T1/2) are caused by low binding of azithromycin with blood plasma proteins as well as by its ability to penetrate into eukaryotic cells and to concentrate in low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (31.1 L/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is particularly important for the elimination of intracellular pathogens It has been shown that phagocytes deliver azithromycin to the localized sites of infection, where it is released during phagocytosis. The azithromycin concentration in the foci of infection is reliably higher than in the healthy tissues (on the average by 24-34%), and correlates with the degree of the inflammatory edema. Despite its high concentration in phagocytes, azithromycin has no significant effect on their function. Azithromycin persists in bactericidal concentrations in the spectra for 5 – 7 days after the previous dose, which allowed to develop short (3-day and 5-day) courses of treatment. It is metabolized mainly in the liver to form inactive metabolites. Excretion of azithromycin from plasma is done in 2 stages: T1/2 is 14-20 hours between 8-24 hours after taking the drug, and 41 hours between 24-72 hours, which allows using the drug once a day. It is excreted mainly with bile unchanged, a small part through the kidneys.

INDICATIONS FOR USE

Infectious-inflammatory diseases caused by pathogens sensitive to the drug:

  • Infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, rhinopharyngitis, pharyngitis, tonsillitis, otitis media);
  • scarlet fever;
  • Lower respiratory tract infections (bacterial and typical pneumonia, bronchitis);
  • skin and soft tissue infections (moderate acne (Acne vulgaris), rye, impetigo, secondary infected dermatoses);
  • infections of the urogenital tract (uncomplicated urethritis and/or cervicitis);
  • Lyme disease (borreliosis), for treatment of the initial stage (erythema migrans).

Dosage and administration

Orally 1 hour before or 2 hours after the meal, once a day.

In children with upper and lower respiratory tract infections, skin and soft tissue infections, the drug is prescribed at the rate of 10 mg/kg body weight once daily for 3 days (course dose – 30 mg/kg body weight) or 5 days: first day – 10 mg/kg body weight, then 5-10 mg/kg body weight once daily for 4 days.

Depending on the body weight of the child, the following dosage regimens are recommended:

Body weightAverage daily (single) dose
10-14 kg2,5 ml (100 mg)
15-24 kg5 ml (200 mg)
25-34 kg7,5 ml (300 mg)
35-44 kg10 ml (400 mg)
>45 kg12,5 ml (500 mg)

When treating Erythema migrans in children, the drug is prescribed once a day for 5 days: 20 mg/kg body weight on the first day and 10 mg/kg body weight on days 2 to 5. It is recommended to take the flacquer on the first day and 10 mg/kg of body weight on the second and fifth days. It is recommended to shake the contents of the bottle before each use.

Side effects

They occur rarely (0.7% of cases or less).

Digestive system: melena, cholestatic jaundice, nausea, vomiting, diarrhea, constipation, decreased appetite, candidomycosis of the oral mucosa, change of taste, gastritis, reversible moderate increase in liver enzymes activity.

Genitourinary system: nephritis, vaginal candidomycosis.

Cardiovascular system: palpitations, chest pain.

CNS and peripheral nervous system: dizziness, headache, somnolence, fatigue; in children – headache (in otitis media therapy), hyperkinesia, anxiety, neurosis, sleep disorders.

Allergic reactions: very rare skin rash, Quincke’s edema, skin itching, urticaria, photosensitization, conjunctivitis, Stevens-Johnson syndrome.

Laboratory parameters: in some cases – neutrophilia, eosinophilia (changed values return to normal in 2-3 weeks after discontinuation of treatment).

Other: asthenia, photosensitization.

Contraindications

  • Hypersensitivity to antibiotics of macrolide group and the drug components;
  • Severe liver or kidney function abnormalities;
  • Children under 6 months of age (efficacy and safety has not been established);
  • period of lactation.

Drug interactions

Antacids (containing aluminium, magnesium), ethanol and food considerably reduce absorption of azithromycin, therefore the drug should be taken at least 1 hour before or 2 hours after taking these drugs and food.

Unlike other macrolide antibiotics, azithromycin does not bind to cytochrome P450 isoenzymes. To date, there have been no observed interactions with te o f f l l i n g , t e r f e n d i n g , c a r ba m a z e p i n g , triazolam, digoxin. If coadministration with warfarin is necessary, careful control of prothrombin time is recommended.

Concomitant use of macrolides with ergotamine and dihydroergotamine may cause their toxic effect (vasospasm, dysesthesia). Lincosamines decrease and tetracycline and chloramphenicol increase azithromycin efficacy.

Pharmaceutically, azithromycin is incompatible with heparin. When used with bromcriptine, the blood concentration of the latter is increased.

Special indications

Caution is advised when using in patients with hepatic or renal dysfunction. It is recommended to take a break of at least 2 hours between intakes of azithromycin and antacids. If one dose of the drug is missed, the missed dose should be taken as soon as possible, and the next ones should be taken 24 hours apart.

The patient should be warned about the need to inform the doctor if any side effect occurs.

Administration of the drug in pregnancy is possible only when the proposed benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (excreted with breast milk). The drug contains sorbitol; therefore, it should not be used in patients with fructose intolerance.

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Form of production

200 mg/5 ml suspension in 15 ml vials, with or without measuring spoon or cup.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25°C. After the first opening of the original package, the suspension should be stored for 7 days at a temperature not exceeding 10 ° C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions for dispensing from pharmacies

Released by a doctor’s prescription.

Despiron – coated tablets

INSTRUCTIONS FOR MEDICAL USE

DESPIRON

Trade name of the drug: Despirone

Active substance (INN): Spiramycin

Dispensing form: coated tablets

Contents per tablet:

Active ingredient: spiramycin 1.5 million IU or 3.0 million IU.

Excipients: Aerosil (colloidal anhydrous silicone dioxide), magnesium stearate, corn starch, polyvinylpolypyrrolidone, croscarmellose sodium, microcrystalline cellulose, titanium dioxide, polyethylene glycol 4000, hypromellose.

Description: White to cream-white, biconvex, round, film-coated tablets.

Pharmacotherapeutic group: Antibiotics (gr. macrolides).

ATX code: J01FA02

Pharmacological properties

Spiramycin belongs to antibiotics of macrolide group. The antibacterial spectrum of spiramycin is as follows:

  • Generally susceptible microorganisms: minimum suppressive concentration (MPC) < 1 mg/L. More than 90% of strains are sensitive. Streptococci, methicillin-sensitive staphylococci, enterocococci, Rhodococcus equi, Branhamella catarrhalis, Bordetella pertussis, Helicobacter pylori, Campylobacter jejuni, Legionella, Corynebacterium diphtheriae, Moraxella, Mycoplasma pneumoniae, Coxiella, Chlamydia, Treponema pallidum, Borrelia burgdorferi, Leptospira, Propionibacterium acnes, Actinomyces, Eubacterium, Porphyromonas, Mobiluncus, Mycoplasma hominis, Bacteroides, Peptostreptococcus, Prevotella.
  • Moderately susceptible microorganisms: the antibiotic is moderately active in vitro. Positive results may be observed at antibiotic concentrations in the inflammation focus higher than the MAC (see Pharmacokinetics). Neisseria gonorrhoea, Clostridium perfringens, Ureaplasma urealyticum.
  • Resistant microorganisms (IPC > 4 mg/L): at least 50% of strains of varieties are resistant.
  • Methicillin – resistant staphylococci, Enterobacteriaceae, Pseudomonas, Acinetobacter, Nocardia asteroides, Fusobacterium, Haemophilus , Mycoplasma hominis.

Spiramycin activity against Toxoplasma gondii has been proven in vitro and in vivo. Note: Due to lack of clinical indications, some species of bacteria are not listed in the spectrum.

Spiramycin penetrates and accumulates in phagocytes (neutrophils, monocytes and peritoneal and alveolar macrobacteriophages). In humans, concentrations of the drug within phagocytes are quite high. These properties explain the effects of spiramycin on intracellular bacteria.

Pharmacokinetics

Absorption

Absorption of spiramycin is rapid but not complete. According to studies, food intake reduces absorption by 50% and prolongs the time to reach maximum plasma concentration.

Distribution

After oral administration of 6 million ME of spiramycin, the maximum plasma concentration is about 3.3 µg/ml. The plasma elimination half-life is approximately 8 hours. Spiramycin does not penetrate the cerebrospinal fluid, but diffuses into breast milk. It penetrates the placental barrier (fetal blood concentrations are about 50% of those in maternal serum). Placental tissue concentrations are 5 times higher than the corresponding concentrations in blood serum.

The volume of distribution is about 383 liters.

The drug penetrates well into saliva and tissues (concentrations in the lungs are 20 to 60 µg/g, tonsils are 20 to 80 µg/g, infected sinuses are 75 to 110 µg/g, bones are 5 to 100 µg/g). Ten days after the end of treatment, the concentration of the drug substance in the spleen, liver and kidneys is 5 to 7 µg/g.

Binding to plasma proteins is low (approximately 10%).

Biotransformation

Spiramycin is metabolized in the liver to form active metabolites with an unspecified chemical structure.

Excretion

It is excreted mainly in the bile (concentrations are 15-40 times higher than in serum). Renal excretion of active spiramycin is about 10% of the administered dose.

The elimination half-life after administration of 3 million ME of spiramycin is approximately 8 hours. It may be prolonged in elderly patients. No adjustment of the spiramycin dose is required in patients with impaired renal function.

Pregnant women: individual pharmacokinetic properties of spiramycin in pregnant women and the kinetics of maternal to fetal transfer of spiramycin have not been fully understood.

INDICATIONS FOR USE

The use of this medicine is based on the clinical studies and depending on the ranking of spiramycin among modern antibacterial agents, its antibacterial activity and pharmacokinetic properties.

The drug is recommended for the treatment of infections caused by susceptible microorganisms:

  • angina, group A beta-haemolytic streptococcus;
  • acute sinusitis;
  • acute secondary bronchial infection;
  • exacerbation of chronic bronchitis;
  • non-serious form of community-acquired pneumonia, proceeding without additional dangerous and pneumococcal symptoms. Macrolides are prescribed when community-acquired pneumonia caused by atypical pathogens is suspected, regardless of the severity of the course of the disease and the presence of additional hazards;
  • mild forms of skin infections: impetigo, infected dermatoses, ecthyma, infectious dermato-cellulitis (especially rye), erythrasma;
  • Dental infections;
  • urinary tract infections that are not gonococcal;
  • Chemoprophylaxis of recurrent acute joint rheumatism when β-lactam antibiotics are contraindicated;
  • Toxoplasmosis, also in pregnancy;
  • Prevention of meningococcal meningitis when rifampicin is contraindicated: the goal is to kill the microorganisms (Neisseria meningitides) in the nasopharynx.

Spiramycin is not used to treat meningococcal meningitis;

Methods of use and dosages:

For adults: 2-3 tablets of 3 million IU (i.e., 6-9 million IU) 2 or 3 times daily.

Maximum daily dose for adults: 9 million IU. No dose adjustment is required for elderly patients.

For children (if body weight is 20 kg or more): 150-300 thousand ME/kg/day divided into 2-3 doses. The maximum dose for children is 300,000 ME/kg/day.

Tablets of 3 million ME are not used in children.

Prevention of meningococcal meningitis: 3 million ME every 12 hours (duration 5 days).

Pregnant women infected with toxoplasmosis: 9 million IU before birth or 3 times after confirmation of the diagnosis of toxoplasmosis in the fetus. Thereafter, concomitant use of perimethamine and sulfadiazine is recommended.

Administration:

Tablets are swallowed whole with water.

Side effects

Gastro-intestinal tract: nausea, vomiting, diarrhea and very rare cases of pseudomembranous colitis (less than 0.01%). Single cases of ulcerative esophagitis and acute colitis have been described. The possibility of acute intestinal mucosal damage in patients with AIDS when using high doses of spiramycin for cryptosporidiosis is also noted (only 2 cases).

Peripheral and central nervous system: transient paresthesias.

Liver: in very rare cases (less than 0.01%) – changes in liver function tests and development of cholestatic hepatitis.

Blood organs: very rare cases (less than 0.01%) of acute hemolysis (see “Caution”) and thrombocytopenia.

Cardiovascular system: possible prolongation of the QT interval on electrocardiogram.

Hypersensitivity reactions: skin rash, urticaria, skin itching.

Very rarely (less than 0.01%) – angioedema, anaphylactic shock.

Contraindications

Hypersensitivity to spiramycin and other components of the drug, lactation period.

Spiramycin is not recommended for patients with glucose-6-phosphate dehydrogenase enzyme deficiency because of possible occurrence of acute hemolysis. The drug should be used with caution in case of bile duct obstruction or liver failure.

Drug interactions

Levodopa: due to inhibition of carbidopa absorption, plasma levels of levodopa may decrease. If spiramycin is concomitantly administered, clinical monitoring and some modification of levodopa dosage is required.

Separate problems in OMN imbalance (international normalization ratios) There have been reported situations where an increase in oral anticoagulant activity has been observed in patients receiving antibiotic therapy.

Explicit infection or inflammation, the patient’s age and general condition are considered risk factors; therefore, it can be difficult to determine the effect on OMN imbalance of infection, and its treatment, antibacterial agents and some groups of antibiotics have a greater effect on OMN imbalance than others. These are mainly: fluoroquinolones, macrolides, cyclins, cotrimaxosol, and other cephalosporins.

Special Indications

It is not recommended for use in children under 6 years of age due to difficulty in swallowing the tablets.

Because of insufficient clinical information when used in patients with renal insufficiency, precautionary measures are required. Since small amounts of the drug are excreted with urine, dosage adjustment is required only for patients with renal insufficiency.

When prescribing to lactating women it is necessary to stop breastfeeding because spiramycin may penetrate into the breast milk.

Spiramycin has no teratogenic effect; therefore, pregnant women can take it without fear. Decrease of risk of toxoplasmosis transmission to fetus during pregnancy is registered from 25% to 8% if used in I trimester, from 54% to 19% – in II trimester, and from 65% to 44% – in III trimester. In patients with liver disease it is necessary to periodically monitor its function during the drug treatment.

Pregnancy and lactation

Pregnancy

If necessary, spiramycin may be prescribed during pregnancy.

According to the results of using the drug during pregnancy, the drug has no phytotoxic effect and does not cause developmental abnormalities.

Lactation period

The drug is excreted with breast milk. There is evidence of gastrointestinal tract dysfunction in newborns. Therefore, breastfeeding is not recommended.

Overdose

The toxic dose of spiramycin is unknown.

Gastrointestinal disorders (nausea, vomiting and diarrhea) may be noted after taking high doses of spiramycin.

In case of overdose it is necessary to measure the QT interval, especially in the presence of other dangerous factors (hypokalemia, congenital prolongation of the QT interval, use of drugs prolonging the QT interval and/or causing ventricular contractions).

There is no specific antidote. Symptomatic therapy is recommended in case of suspected spiramycin overdose.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription.

Reacin- injection

INSTRUCTIONS FOR MEDICAL USE

REACIN

Trade name of the drug: Reacin

Active substance (INN): Amikacin

Dosage form: Solution for injection

Contents:

2 ml of the solution (1 ampoule) contains:

Active ingredient: Amikacin (as sulfate): 100 mg and 500 mg.

Excipients: sodium citrate two aqueous, sodium metabisulfite, sulfuric acid 35%, water for injection.

Description: clear, colorless or slightly yellowish liquid.

Pharmacotherapeutic group: antibiotic of aminoglycoside group.

ATX code: J01GB06

Pharmacological properties

It is a broad-spectrum antibiotic. It actively penetrates through cell membrane and irreversibly binds with specific receptor proteins on 30S ribosome subunit. Disrupts the formation of a complex between matrix (informational) RNA and the 30S subunit of the ribosome. This results in the misreading of information from RNA and the formation of incomplete proteins. Polyribosomes disintegrate and lose the ability to synthesize protein, which leads to the death of the microbial cell.

Highly active against most gram-negative and some gram-positive microorganisms: Pseudomonas aeruginosa, including those resistant to gentamicin, tobramycin, sizomycin and netilmicin, Escherichia coli, Klebsiella spp. Serratia spp., Providencia spp., Enterobacter spp., Salmonella spp., Shigella spp., Streptococcus spp., Staphylococcus spp. including those resistant to penicillin, methicillin and some cephalosporins. It has bacteriostatic effect on Mycobacterium tuberculosis resistant to streptomycin, isoniazid, PASK and other anti-tuberculosis drugs. Anaerobic microorganisms are resistant to the drug.

Amikacin does not lose activity under the action of enzymes inactivating other aminoglycosides and may remain active against strains of Pseudomonas aeruginosa resistant to tobramycin, gentamicin and netilmicin.

Pharmacokinetics

It is practically not absorbed from the gastrointestinal tract. It is administered i / v or i/m. Cmax is reached 1 h and 0.5 h after administration of 7.5 mg/kg i / v and is 21 and 38 µg/ml, respectively. Therapeutic concentration (15-25 mcg/ml) is maintained for 10-12 hours after v/m and v/v administration. Binding to plasma proteins is 4-11%. Distribution volume is 0.2-0.4 l/kg, in newborns up to 0.68 l/kg. It easily crosses histohematic barriers, penetrates into the tissue of lungs, liver, myocardium, spleen, bone tissue, is selectively accumulated in the cortical layer of kidneys and distributed in extracellular fluid, including serum, lymph, pleural, pericardial and peritoneal exudate, synovial fluid, abscess fluid. Determined in low concentrations in bile, bronchial secretion, muscle and fatty tissue. It is not metabolized. T1/2 is 2-4 hours in adults and 5-8 hours in newborns. Renal clearance is 79-100 ml/min; in patients with impaired renal function T1/2 is increased to 70-100 hours. It is excreted mainly by kidneys (65-94%) in unchanged form by glomerular filtration, forms high concentrations in urine; a small amount is excreted with bile.

Indications for use

Infectious-inflammatory diseases caused by Gram-negative microorganisms (resistant to gentamicin, sisomycin and kanamycin) or by associations of Gram-positive and Gram-negative microorganisms:

  • Respiratory tract infections (bronchitis, pneumonia, pleural empyema, pulmonary abscess);
  • sepsis;
  • septic endocarditis;
  • CNS infections (including meningitis);
  • Abdominal infections (including peritonitis);
  • Infections of the urogenital tract (pyelonephritis, cystitis, urethritis);
  • purulent skin and soft tissue infections (including infected burns, infected ulcers and bedsores of various genesis);
  • biliary tract infections;
  • Bone and joint infections (including osteomyelitis);
  • wound infection;
  • postoperative infections.

Contraindications

  • neuritis of the auditory nerve;
  • Severe chronic renal failure with azotemia and uremia;
  • pregnancy;
  • Hypersensitivity to the components of the drug;
  • hypersensitivity to other aminoglycosides in anamnesis.

The drug should be used with caution in myasthenia gravis, parkinsonism, botulism (aminoglycosides may cause neuromuscular transmission failure, which leads to further weakening of skeletal muscles), dehydration, renal failure, during neonatal period, in premature children, in elderly patients, during lactation.

Side effects

Digestive system: increased liver transaminase activity, hyperbilirubinemia, nausea, vomiting.

Allergic reactions: skin rash, itching, fever, rarely – Quincke’s edema.

Blood system: anemia, leukopenia, granulocytopenia, thrombocytopenia.

CNS and peripheral nervous system: headache, somnolence, impaired neuromuscular transmission, decreased hearing, up to permanent deafness, vestibular disorders.

Urinary system: oliguria, proteinuria, microhematuria, rarely – renal failure.

Dosage and administration

I/m, i/m (by jetting for 2 min or by dropwise at a rate of 60 drops per minute). Adults and children: 5 mg/kg every 8 hours or 7.5 mg/kg every 12 hours; the maximum dose is 15 mg/kg/day, the course dose is not more than 15 g. In premature infants: the initial dose is 10 mg/kg and then 7.5 mg/kg every 18-24 hours; in newborns the initial dose is 10 mg/kg and then 7.5 mg/kg every 12 hours. The duration of treatment by intravenous injection is 3-7 days, by intravenous injection – 7-10 days. Patients with renal insufficiency need to correct the dosage regimen according to creatinine clearance.

Overdose

Symptoms: toxic reactions, neuromuscular block up to respiratory arrest, CNS depression (lethargy, coma, deep respiratory depression) in infants.

Treatment: calcium chloride IV, anticholinesterase agents (neostigmine p/k), m-choline blockers (atropine), symptomatic therapy. Hemodialysis and peritoneal dialysis are effective in impaired renal function, and exchange blood transfusion is performed in newborns.

Interaction with other drugs

Risk of nephrotoxic action increases when concomitant use of amikacin with amphotericin B, vancomycin, methoxiflurane, enflurane, NSAIDs, X-ray contrast agents, cephalothin, cyclosporine, cisplatin, polymyxins.

The risk of ototoxicity increases when concomitant use of amikacin with diuretics (furosemide, etacrynic acid), cisplatin.
When concomitant use with penicillins (in renal insufficiency) antimicrobial effect is reduced.

Concomitant use with ethyl ether and neuromuscular transmission blockers increases the risk of respiratory depression.
Amikacin is incompatible in solution with penicillins, cephalosporins, amphotericin B, chlorothiazide, erythromycin, heparin, nitrofurantoin, thiopentone as well as, depending on solution composition and concentration, with tetracyclines, B vitamins, vitamin C and potassium chloride.

Special indications

Before use, the sensitivity of the isolated pathogens is determined using disks containing 30 µg amikacin. If the diameter of the growth-free zone is 17 mm or more, the microorganism is considered sensitive, 15 to 16 mm – moderately sensitive, less than 14 mm – resistant.

Plasma concentration of amikacin should not exceed 25 µg/ml (therapeutic concentration is 15-25 µg/ml).

Kidney, auditory nerve and vestibular function should be monitored at least once a week during treatment.

The probability of nephrotoxicity is higher in patients with impaired renal function, as well as when prescribing high doses or for a long time (daily monitoring of renal function may be required in this category of patients).

In case of unsatisfactory audiometric tests, the drug dose is reduced or the treatment is discontinued.

Patients with infectious inflammatory diseases of the urinary tract are recommended to take increased amount of fluid with adequate diuresis.

In the absence of positive clinical dynamics, it should be remembered about the possibility of development of resistant microorganisms. In such cases, it is necessary to cancel the treatment and initiate appropriate therapy. Sodium disulfite contained in the drug may cause allergic complications (up to anaphylactic reactions) in patients, especially in patients with allergic history.

Administration during pregnancy and lactation

The drug is contraindicated in pregnancy.

In case of vital indications the drug may be used in lactating women. It should be kept in mind that aminoglycosides are excreted with breast milk in small amounts. They are poorly absorbed from the gastrointestinal tract, and related complications in infants have not been recorded.

Use in patients with impaired renal function

It is contraindicated in severe chronic renal failure with azotemia and uremia.

Correction of dosage regimen is required in case of impaired renal excretory function.

Administration in elderly patients

Caution should be exercised when using in elderly patients.

Form of production

Solution for injection 500 mg/2 ml and 100 mg/2 ml in 2 ml ampoules 1 ml.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription

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