Rovamycin, 1.5 ml ml 16 pcs

Pharmacotherapeutic group: antibiotic, macrolide.

The ATX code is J01FA02.

Pharmacological action

Pharmacodynamics

Spiramycin belongs to the antibiotic group of macrolides.
The antibacterial spectrum of spiramycin is as follows:

• Commonly susceptible microorganisms: minimum suppressive concentration (MSC) Moderately susceptible microorganisms: the antibiotic is moderately active in vitro. Positive results may be seen at antibiotic concentrations in the inflammatory site higher than the MAC (see Pharmacokinetics). Neisseria gonorrhoea, Clostridium perfringens, Ureaplasma urealyticum.
• Resistant microorganisms (MPC > 4 mg/L): at least 50% of strains of varieties are resistant.

Methicillin – resistant Staphylococcus aureus, Enterobacteria, 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 varieties of bacteria are not listed in the spectrum. In France, 20% to 25% of pneumococci are resistant to all macrolides (cross-resistance to all macrolides).

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, with wide variability (10 to 60%).

Distribution

After oral administration of 6 million ME of spiramycin, the maximum plasma concentration is about 3.3 µg/ml.

Spiramycin does not penetrate the cerebrospinal fluid, but diffuses into breast milk. It penetrates the placental barrier (fetal blood concentration is about 50% of the concentration in maternal serum).

Concentrations in placental tissue are 5 times higher than the corresponding concentrations in blood serum.

The volume of distribution is approximately 383 liters.

The drug penetrates well into saliva and tissues (concentrations in lungs 20 to 60 µg/g, tonsils 20 to 80 µg/g, infected sinuses 75 to 110 µg/g, bones 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.

The binding to plasma proteins is low (approximately 10%).

Biotransformation

Spiramycin is metabolized in the liver with the formation of active metabolites with an unspecified chemical structure.

Excretion

It is excreted mainly with bile (concentrations 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 necessary in patients with impaired renal function.

Indications

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

– acute and chronic pharyngitis caused by beta-hemolytic 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 microorganisms most often causing this pathology, the use of Rovamycin® is indicated in case of contraindications to the use of beta-lactam antibiotics);

– acute and chronic tonsillitis caused by microorganisms sensitive to spiramycin;

– acute bronchitis caused by a bacterial infection that develops after acute viral bronchitis;

– exacerbation of chronic bronchitis;

— community-acquired pneumonia in patients without risk factors for an unfavorable 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 suspicion of it (regardless of the severity and the presence or absence of risk factors for an unfavorable outcome);

– infections of the skin and subcutaneous tissue, including impetigo, impetiginization, ecthyma, infectious dermohypodermatitis (especially erysipelas), secondary infected dermatoses, erythrasma;

— oral infections (including stomatitis, glossitis);

– non-gonococcal infections of the genital organs;

— toxoplasmosis, incl. during pregnancy;

– infections of the musculoskeletal system and connective tissue, including periodontium.

Prevention of relapses of rheumatism in patients with allergies to beta-lactam antibiotics.

Eradication of Neisseria meningitidis from the nasopharynx (if rifampicin is contraindicated) for the prevention (but not treatment) of meningococcal meningitis:

— in patients after treatment and before leaving quarantine;

– in patients who, within 10 days before hospitalization, were in contact with persons who secreted Neisseria meningitidis with saliva into the environment.

Pharmacological effect

Pharmacotherapeutic group: antibiotic, macrolide.

ATX code – J01FA02.

Pharmacological action

Pharmacodynamics

Spiramycin belongs to the macrolide group of antibiotics.
The antibacterial spectrum of spiramycin is as follows:
Generally susceptible microorganisms: minimum inhibitory concentration (MIC) Moderately sensitive microorganisms: the antibiotic is moderately active in vitro. Positive results can be observed when antibiotic concentrations at the site of inflammation are higher than the MIC (see Pharmacokinetics). Neisseria gonorrhoea, Clostridium perfringens, Ureaplasma urealyticum.
Resistant microorganisms (MIC > 4 mg/l): at least 50% of the strains of the species are resistant.
Methicillin – resistant staphylococci, Enterobacteria, Pseudomonas, Acinetobacter, Nocardia asteroides, Fusobacterium, Haemophilus, Mycoplasma hominis.
The activity of spiramycin against Toxoplasma gondii has been proven in vitro and in vivo.

Note: due to the lack of clinical indications, some bacterial species are not listed in the spectrum. In France, 20% to 25% of pneumococci are resistant to all macrolides (cross-resistance to all macrolides).

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

Pharmacokinetics

Absorption

Absorption of spiramycin occurs quickly, but not completely, with great variability (from 10 to 60%).

Distribution

After oral administration of 6 million IU of spiramycin, the maximum plasma concentration is about 3.3 μg/ml.

Spiramycin does not penetrate into the cerebrospinal fluid, but diffuses into breast milk. Penetrates the placental barrier (the concentration in the fetal blood is approximately 50% of the concentration in the maternal blood serum).

Concentrations in placental tissue are 5 times higher than corresponding concentrations in serum.

Distribution volume – approximately 383 l.

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

Plasma protein binding is low (approximately 10%).

Biotransformation

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

Removal

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

The half-life after taking 3 million IU of spiramycin is approximately 8 hours. It may be prolonged in older patients. In patients with impaired renal function, no dose adjustment of spiramycin is required.

Special instructions

During treatment with the drug in patients with liver disease, it is necessary to periodically monitor its function.

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

Use in pediatrics

Tablets of 3 million IU are not used in children due to the difficulty of swallowing them due to the large diameter of the tablets and the risk of airway obstruction.

Impact 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 a car or engage in other potentially hazardous activities. However, the severity of the patient’s condition, which may affect attention and speed of psychomotor reactions, should be taken into account. Therefore, the decision about the possibility of driving a car or engaging in other potentially hazardous activities for a particular patient should be made by the attending physician.

Active ingredient

Spiramycin

Composition

Each film-coated tablet contains:

Active ingredients: 1.5 million IU spiramycin,

Excipients: colloidal anhydrous silicon, magnesium stearate, pregelatinized starch, hydroxypropylcellulose, croscarmellose sodium (sodium carboxymethylcellulose), microcrystalline cellulose.

Pregnancy

Rovamycin can be prescribed during pregnancy according to indications.

There is extensive experience with the use of the drug Rovamycin® during pregnancy. A decrease in the risk of transmitting toxoplasmosis to the fetus during pregnancy is observed from 25% to 8% when using the drug 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.

When prescribing Rovamycin® during lactation, breastfeeding should be stopped, since spiramycin may pass into breast milk.

Contraindications

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

The use of spiramycin is not recommended in patients with deficiency of the enzyme glucose-6-phosphate dehydrogenase, due to the possible occurrence of acute hemolysis.

The drug should be taken with caution in cases of bile duct obstruction or liver failure.

Side Effects

From the gastrointestinal tract: nausea, vomiting, diarrhea and very rare cases of pseudomembranous colitis (less than 0.01%).

Isolated cases of ulcerative esophagitis and acute colitis have been described. The possibility of developing acute damage to the intestinal mucosa in patients with AIDS when using high doses of spiramycin for cryptosporidiosis was also noted (only 2 cases).

From the peripheral and central nervous system: transient paresthesia.

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

From the hematopoietic organs: very rare cases (less than 0.01%) of acute hemolysis (see “With caution”) and thrombocytopenia.

From the cardiovascular system: possible prolongation of the QT interval on the electrocardiogram.

Hypersensitivity reactions: skin rash, urticaria, itching. Very rarely (less than 0.01%) – angioedema, anaphylactic shock.

Interaction

Inhibition of carbidopa absorption by spiramycin with a decrease in plasma levodopa concentrations. When prescribing spiramycin simultaneously, clinical monitoring and dose adjustment of levodopa is necessary.

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

Overdose

There are no known cases of spiramycin overdose.

Symptoms: possible – nausea, vomiting, diarrhea. Cases of prolongation of the QT interval that resolves when the drug is discontinued have been observed in neonates receiving high doses of spiramycin or after intravenous administration of spiramycin in patients predisposed to prolongation of the QT interval.

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

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf life

3 years.

Manufacturer

Sanofi S.p.A., Italy