TRADE NAME

Doramycin

INTERNATIONAL NON-PATENTED NAME

Spiramycin

chemical name

The main component is (4R,5S,6S,7R,9R,10R,11E,13E,16R)-6-[[3,6-dideoxy-4-O-(2,6-dideoxy-3-C-methyl-a-L-ribo-hexopyranosyl)-3-(dimethylamino)-b-D- glucopyranosyl]oxy]-4-hydroxy-5-methoxy-9,16-dimethyl-7-(2-oxoethyl)-10-[[2,3,4,6-tetradeoxy-4-(dimethylamino)-D-erythro-hexopyranosyl]oxy]oxacyclohexadeca-11, 13-dien-2-one (Spiramycin

PHARMACEUTICAL FORM

Film coated tablets.
Description:
Doramycin 1.5 mln IU:
 Round biconvex film coated tablets with “DORA” engraved on one side and break line on the other side. Core: yellowish white.  Coat: white or almost white with milky tint.
Doramycin 3 mln IU:
Round biconvex film coated tablets with “DORA” engraved on one side.
Core: yellowish white.  Coat:  white or almost white with milky tint.

COMPOSITION:
Doramycin 1,5 mln IU
1 film coated tablet contains:
Active ingredients : spiramycin 1 500  000 IU.
Inactives ingredients: maize starch, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, talc.
Coated tablet: hydroxypropylmethylcellulose, titanium dioxide, talc, polyethylene glycol  6000, ethanol 96%.
Doramycin 3 mln IU
1 film coated tablet contains:
Active ingredients : spiramycin 3 000 000 IU.
Inactives ingredients: maize starch, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, talc.
Coated tablet: hydroxypropylmethylcellulose, titanium dioxide, talc, polyethylene glycol  4000, polyethylene glycol  6000, ethanol 96%.

ATC CODE     J01FA02

PHARMACOTHERAPEUTIC GROUP
Antimicrobial preparations.
Macrolides  group.

PHARMACOLOGICAL PROPERTIES:
PHARMACODYNAMICS
Doramycin is a macrolide antibiotic. It has a bacteriostatic action as it inhibits intracellular protein synthesis. Spiramycin is active against the following microorganisms:  streptococci, methicillin-sensitive staphylococci, enterococci, Rhodococcus equi, Branhamella catarrhalis, Bordetella pertussis, Helicobacter pylori, Campylobacter jejuni,
Legionella spp., Corynebacterium diphtheriae, Moraxella spp., Mycoplasma pneumoniae, Coxiella spp., Chlamydia spp., Treponema pallidum, Borrelia burgdorferi, Leptospira spp., Propionibacterium acnes, Actinomyces spp., Eubacterium spp., Porphyromonas spp., Mobiluncus spp., Bacteroides spp., Peptostreptococcus spp., Prevotella spp., Neisseria gonorrhoeae, Ureaplasma urealyticum, Clostridium perfringens, Toxoplasma gondii.

The following microorganisms are spiramycin-resistant: methicillin-resistant staphylococci, Enterobacter spp., Pseudomonas spp., Acinetobacter spp., Nocardia spp., Fusobacterium spp., Haemophilus spp., Mycoplasma hominis.

PHARMACOKINETICS
Absorption
The absorption of spiramycin has a high rate, but it is incomplete with wide variability (from 10% to 60%). After peroral administration in the dose of 6 000 000 IU maximum concentration of spiramycin in plasma is about 3, 3 mcg/ml.

Distribution

Spiramycin does not penetrate into cerebrospinal fluid. The drug penetrates through placental barrier (concentration in fetal blood is about 50% of concentration in maternal serum). Placental tissue concentrations of spiramycin is 5-fold higher than those of blood serum. Spiramycin is excreted with breast milk. The drug penetrates well into saliva and tissues (concentration in the lungs is 20-60 mcg/ml, in tonsils - 20-80 mcg/ml, in infected sinuses - 75-110 mcg/ml, in bones - 5-100 mcg/ml). In ten days after the end of treatment spiramycin concentration in spleen, liver, kidneys is 5-7 mcg/ml.Binding to plasma proteins is low (approximately 10%).

Metabolism and excretion

Spiramycin biotransforms in liver with the formation of active metabolites with undefined chemical structure. The drug is mainly excreted via bile (the concentration is 15-40-fold higher than that of serum). The renal excretion of spiramycin is about 10% of an administered dose. The half-life period after the drug administration in the dose of 3 000 000 IU is about 8 hours. The half-life period is longer in elder patients.

 
THERAPEUTIC INDICATIONS
Infectious-inflammatory diseases caused by sensitive to the preparation microorganisms:
Infections of lower respiratory tract::

 - acute non-hospital pneumonia, including atypical form (caused by Legionella pneumophila, Mycoplasma pneumoniae, Chlamydia spp.);

- exacerbation of chronic bronchitis, acute bronchitis.

Diseases of ENT-organs:

- sinusitis, tonsillitis, otitis.

Osteomyelites and arthritises.

Infections of skin:

- erysipelas;

- secondary infected dermatoses;

- abscesses and phlegmons, including stomatology.

Non-gonococcal infections of the genital and urinary tracts:

- prostatitis;

- urethritis.

Diseases which are genital tract transmissible:

- genital and extragenital clamidiosis;

- syphilis, gonorrhea (in case of allergy to penicillin preparations)

Toxoplasmosis (including toxoplasmosis in pregnant women).

Preventive measures for meningococcosis meningitis in people, who had contact with the patient not more than 10 days before the establishment of the diagnosis.

Preventive measures for acute articulate rheumatism.

contra indications
Doramicin is contraindicated upon:
- hypersensitivity to spiramycin and other preparation components
- evident hepatic dysfunction.

UNDESIRABLE EFFECTS
Sometimes there is a possibility of nausea, vomiting, diarrhea, allergic skin reactions.

POSOLOGY AND METHOD OF ADMINISTRATION
For adults: the daily dose of Doramycin is 6 - 9 mln IU divided into 2 or 3 doses.
With acute bronchopulmonary disease:  1.5 mln IU every 8 hours (the daily dose is 4,5 mln IU), for severe cases the 2-fold increase of the dose is possible.
For meningococcosis meningitis prevention: adults are prescribed the dose of 3 mln IU every 12 hours during 5 days, children with body weight below 20 kg are prescribed 0,75 mln
IU per 1 kg every 12 hours during 5 days.
For patients with  compromised renal function the dosage adjustment is not required due to poor renal excretion.
For children:  with body weight below 10kg Doramycin is administered in the dose of 3, 75 mln

                         IU daily;

                         with body weight below 10-20 kg the daily dose of  Doramycin is 1,5 - 3 mln IU

                         divided into  2-4 doses;

                         with body weight below 20 kg Doramycin is administered in the daily dose of

                         1,5 mln IU per 10 kg of body weight divided into 2 or 3 doses.

 
OVERDOSE
Toxic dose of spiramycin is not determined.
A specific antidote does not exist. Symptomatic therapy is carried out.

INTERACTION WITH OTHER MEDICAMENTS
Simultaneous application of spiramycin with medicines causing ventricular flutter and fibrillation as  antiarrhythmic drugs (chinidin, hydrochinidin, disopyramide, amiodarone, sotalol, dofetilide, ibutilide), sultopride (neuroleptic of the benzamide group) and other medicines (bepridil, cisapride, diphemanil, mizolastine, vincamine, erythromycin) is contraindicated.

During simultaneous administration with medicines containing the combination of levodopa and carbidopa the decrease of levodopa plasma level was observed.

PARTICULAR INDICATION
It is necessary to monitor hepatic function for patients with compromised liver function.

THE INFLUENCE ON THE ABILITY FOR DRIVIING VEHICLES AND OPERATING OF

MECHANISMS:
The drug doesn’t cause changes in psychophysical state of patient and doesn’t influence on the ability for driving vehicles and operating of mechanisms.

APPLICATION DURING PREGNANCY AND BREAST-FEEDIN
Application of  Doramycin is possible in pregnancy under indications.
If the drug is administered during lactation period breast-feeding should be stopped as spiramycin penetrates into breast milk.

PresentATIon
Doramycin 1.5 mln IU
Film-coated tablets in a blister. 8 tablets in a blister.  2  blisters in a carton box together with instruction.
Doramycin 3 mln IU
Film-coated tablets in a blister. 5 tablets in a blister.  2  blisters in a carton box together with instruction.

STORAGE CONDITIONS

Store in a dry place at temperature not above 25°С.

Keep out of the reach of children.

SHELF LIFE
3 years from the date of manufacture.
Do not apply after the expiry date.

CONDITIONS OF SALES IN DRUGSTORES
Sold under the doctor's prescription.