ROVAMICIN®
Active material: Spiramycine
When ATH: J01FA02
CCF: Macrolide antibiotics
ICD-10 codes (testimony): A39, A46, A48.1, A56.0, A56.1, A56.4, B58, B96.0, H66, J01, J03, J15, J15.7, J16.0, J32, J35.0, J42, J45, K05, L02, L03, L08.1, L30.3, M00, M05, M86, N30, N34, N41, N70, N71, N72, Z29.2
When CSF: 06.07.01
Manufacturer: AVENTIS Laboratories (France)
Pharmaceutical form, composition and packaging
Pills, coated white or white with a cream shade, round, lenticular, Engraved “RPR 107” on one side.
| 1 tab. | |
| spiramycine | 1.5 Million International Units |
Excipients: colloidal silicon dioxide, magnesium stearate, pregelatinized corn starch, hydroksypropyltsellyuloza (giproloza), sodium croscarmellose (sodium carboxymethylcellulose), microcrystalline cellulose.
The composition of the shell: Titanium dioxide, macrogol 6000, gipromelloza.
8 PC. – blisters (2) – packs cardboard.
Pills, coated White with cream shade, round, lenticular, Engraved “ROVA 3” on one side.
| 1 tab. | |
| spiramycine | 3 Million International Units |
Excipients: colloidal silicon dioxide, magnesium stearate, pregelatinized corn starch, hydroksypropyltsellyuloza (giproloza), sodium croscarmellose (sodium carboxymethylcellulose), microcrystalline cellulose.
The composition of the shell: Titanium dioxide, macrogol 6000, gipromelloza.
5 PC. – blisters (2) – packs cardboard.
| Valium for drug of a solution for / in | 1 fl. |
| spiramycine | 1.5 Million International Units |
Excipients: adipic acid.
Bottles (1) together with the solvent (amp. 4 ml) – packs cardboard.
Pharmacological action
Macrolide antibiotics. The mechanism of the antibacterial action due to inhibition of protein synthesis in the bacterial cell by binding to the 50S-ribosomal subunit.
Usually sensitive organisms (MPK≤ 1 mg / l): Streptococcus spp. (incl. Streptococcus pneumoniae), Staphylococcus spp. (methicillin-resistant and susceptible strains), Enterococcus spp., Rhodococcus equi, Bacillus cereus, Branhamella catarrhalis, Bordetella pertussis, Helicobacter pylori, Campylobacter spp., Legionella spp., Corynebacterium diphtheriae, Moraxella spp., Mycoplasma pneumoniae, Coxiella spp., Chlamydia spp., Treponema pale, Borrelia burgdorferi, Leptospira spp., Propionibacterium acnes, Actinomyces spp., Eubacterium spp., Porphyromonas spp., Mobiluncus spp., Bacteroides spp., Peptostreptococcus spp., Prevotella spp., Toxoplasma gondii (in vitro is in vivo).
Moderately susceptible microorganisms: Neisseria gonorrhoeae, Ureaplasma urealyticum, Clostridium perfringens. In respect of these antibiotic agents of moderately active in vitro, positive results may be observed at concentrations of antibiotic in the inflammation above, than the IPC.
Resistant microorganisms (IGC>4 mg / l): at least 50% strains are resistant – Enterobacter spp., Pseudomonas spp., Acinetobacter spp., Nocardia asteroids, Fusobacterium spp., Haemophilus spp., Mycoplasma hominis, Corynebacterium jekeium.
Spiramycin penetrates and accumulates in phagocytes (Neutrophils, monotsitы and peritonealynыe and alyveolyarnыe makrobiofagi). In humans, the drug concentration in phagocytes are quite high. These properties account for the effects of spiramycin on intracellular bacteria.
Pharmacokinetics
Absorption
Absorption spiramycin proishodit bystro!, but less than, with great variability (from 10% to 60%). After receiving Rovamycinum® oral dose 6 mln.ME Cmax spiramycin in plasma is about 3.3 ug / ml. After the on / in the 1.5 Million International Units spiramycin putem odnochasovoy infusions Cmax is 2.3 ug / ml. When administered 1.5 every mln.ME 8 h Css achieved by the end of the second day (Cmax about 3 ug / ml and Cmin about 0.5 ug / ml).
Distribution
Spiramycin penetrates and accumulates in phagocytes (Neutrophils, monotsitы and peritonealynыe and macrophages alyveolyarnыe). In humans, the drug concentration in phagocytes are quite high. This explains the efficacy of spiramycin against intracellular bacteria. Spiramycin does not penetrate into the cerebrospinal fluid; excreted in breast milk. It penetrates through the placental barrier (concentration in the blood of the fetus is about 50% the concentration in maternal serum). Concentrations in placental tissue 5 times higher, than corresponding concentrations in blood serum. Vd about 383 l. The drug penetrates well into the saliva and tissue (concentration in the lungs of 20-60 g / g, in the tonsils – 20-80 g / g, in infected sinuses – 75-110 g / g, bone – 5-100 g / g). After 10 days after the end of treatment spiramycin concentration in the spleen, liver, Kidney is 5-7 g / g. Plasma protein binding is low (about 10%).
Metabolism and excretion
Spiramycin is metabolized in the liver with the formation of active metabolites with unknown chemical structure.
Write mainly in the bile (concentration 15-40 times higher, than serum). Renal excretion of the active spiramycin is about 10% of the administered dose. T1/2 after administration 3 mln.ME spiramycin inside is about 8 no. T1/2 after i / v infusion of about 5 no.
Pharmacokinetics in special clinical situations
T1/2 is extended in the elderly. In patients with impaired renal function correct dosing regimen is not required.
Testimony
To ingestion (tablets)
Infectious-inflammatory diseases, caused by susceptible to malaria infections:
- Infections of upper respiratory tract (sinusitis, tonsillitis);
- Infections of the lower respiratory tract (incl. acute community-acquired pneumonia, including SARS, exacerbation of chronic bronchitis);
- Periodontal infections;
- Infections of the skin and soft tissues (mug, secondarily infected dermatitis, impetigo, ecthyma, erythrasma);
- Bone and joint infections;
- Infections of the reproductive system (not gonorrheal etiology);
- Toxoplasmosis, incl. in pregnant women.
Prevention of meningococcal meningitis cases, When rifampicin is contraindicated: eradication of Neisseria meningitidis in the nasopharynx. Spiramycin is not used for the treatment of meningococcal meningitis. The drug is recommended for prophylaxis in patients after treatment, and in individuals, had contact with the patient for 10 days before his hospitalization.
Prevention of acute rheumatism in individuals with allergic reaction to penicillin.
To / in the (infusion)
Infectious-inflammatory diseases of the upper and lower respiratory tract in adults:
- Acute pneumonia;
- Exacerbation of chronic bronchitis;
- Infectious and allergic asthma.
Dosage regimen
Adults Inside designate 2-3 tab. by 3 million. ME or 4-6 tab. by 1.5 Million International Units (ie. 6-9 Million International Units) per day for 2 or 3 admission. The maximum daily dose is 9 Million International Units.
For children weighing 20 kg or more dose of 150-300 thousand IU / kg body weight / day, divided by 2-3 admission. The maximum daily dose for children is 300 thousand IU / kg / day.
To prevention of meningococcal meningitis adult prescribers on 3 Million International Units 2 times / day (6 mln.ME / day) during 5 days, children – by 75 thousand IU / kg of body weight 2 times / day for 5 days.
Patients with impaired renal function due to the low renal excretion spiramycin dose modification is not required.
Parenteral Rovamycinum® used only Adult. Administered by i / v infusion of 1.5 IU every 8 no (4.5 mln.ME / day). If necessary, in case of severe infections, the dose may be doubled. Duration of treatment is determined individually, depending on the severity and characteristics of the course of infection. While improving the condition of the patient should continue receiving treatment by Rovamycinum® inside.
Before introducing the contents of the flask are dissolved in 4 ml water for injection. The drug is introduced into / in the drip slowly over 1 no (at least 100 ml 5% glucose solution).
After dilution the solution is stable for 12 hours when stored at room temperature.
Side effect
From the digestive system: nausea, vomiting, diarrhea; rarely (less 0.01%) – psevdomembranoznыy colitis, changes in liver function tests and cholestatic hepatitis development; in a few cases – ulcerative esophagitis and acute colitis. Noting also the possibility of acute damage to the intestinal mucosa in patients with AIDS in the application of spiramycin in high doses over cryptosporidiosis (Total 2 case).
From the central and peripheral nervous system: prehodyashtie paresthesia.
From the hematopoietic system: rarely (less 0.01%) – acute hemolysis and thrombocytopenia.
Cardio-vascular system: It may prolong the QT interval on an electrocardiogram.
Allergic reactions: skin rash, hives, itching; rarely (less 0.01%) – angioedema, anaphylactic shock.
Local reactions: rarely – moderately severe irritation of the vein, that only in exceptional cases may require discontinuation of treatment.
Other: in some cases – vasculitis, including Henoch-Schonlein purpura.
Contraindications
- Lactation;
- Deficiency of glucose-6-fosfatdegidrogenazы (the risk of acute hemolysis);
- Children's age (Pill 1.5 Million International Units – to 3 years, Pill 3 Million International Units – to 18 years);
- Hypersensitivity to spiramycin and other ingredients.
FROM caution appoint Rovamycinum® obstruction of the bile ducts or liver failure.
Pregnancy and lactation
Rovamicina® It can be administered during pregnancy on the testimony.
In appointing Rovamycinum® lactation should stop breastfeeding, since it is possible the selection of spiramycin in breast milk.
In spiramycin not vыyavleno teratogennogo actions. Reducing the risk of transmission of toxoplasmosis to the fetus during pregnancy is marked with 25% to 8% When using the drug in the I trimester, from 54% to 19% – in the II trimester, and c 65% to 44% – in the III trimester.
Cautions
In patients with impaired liver function during the use of the drug should monitor liver function tests.
In / in the introduction of the drug should be discontinued immediately in the event of any signs of an allergic reaction.
Precautions should use the drug with ergot alkaloids.
In patients with diabetes should monitor blood glucose and if necessary, adjust it in connection with, that the infusion is carried out using 5% dextrose.
Use in Pediatrics
Drug in tablet form 3 mln.ME not apply in children and adolescents under the age of 18 years.
Overdose
Symptoms: spiramycin overdose are unknown. Possible symptoms are nausea, vomiting, diarrhea.
Treatment: if necessary, symptomatic therapy. No specific antidote.
Drug Interactions
In an application with drugs, containing a combination of levodopa and carbidopa, there was a decrease in plasma levels of levodopa (and clinical monitoring is required for a change in the dose of levodopa).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
Tablets should be stored in a dry place at temperatures no higher than 25 ° C. Shelf life for tablets 1.5 Million International Units - 3 year, Pill 3 Million International Units – 4 year.
The lyophilisate should be stored in a dark place at a temperature no higher than 25 ° C. Shelf life for the freeze-dried product – 1.5 year.
After dilution the solution is stable for 12 hours when stored at room temperature.
The drug should be stored out of reach of children.
