Klindatsil

General characteristics. Structure:

Active ingredient: 150 mg of clindamycin (in the form of phosphate) in 1 ml of solution.

Excipients: benzyl alcohol, dinatrium эдетат, hydroxide sodium solution, water for injections.

Pharmacological properties:

Pharmacodynamics. Antibiotic of group of linkozamid. Possesses a broad spectrum of activity. Communicates with 50S a ribosome subunit of a microbic cell and inhibits synthesis of protein of sensitive microorganisms. Renders bacteriostatic, and concerning a number of gram-positive cocci bactericidal action. At 2-10 times surpasses lincomycin in activity.

in vitro concerning the following microorganisms is active: aerobic gram-positive cocci, including Staphylococcus aureus, Staphylococcus epidermidis, including strains developing a penicillinase (bystry development of stability to clindamycin in some strains, resistant to erythromycin is noted), Streptococcus spp. (except for Streptococcus faecalis); Pneumococcus spp.; anaerobic gram-negative bacilli, including Bacteroides spp. (including V. fragilis and V. melaninogenicus), Fusobacterium spp.; the anaerobic gram-positive bacilli which are not forming a dispute including Propionibacterium spp., Eubacterium spp., Actinomyces spp.; anaerobic and mikroaerofilny gram-positive cocci, including Peptococcus spp., Peptostreptococcus spp., Microaerophilic Streptococcus spp., Clostridia spp. Most Clostridium perfringens are sensitive to clindamycin, but S. sporogenes and S. of tertium, are often steady against effect of clindamycin therefore it is necessary to carry out sensitivity tests.

It is active concerning the majority of strains of the following microorganisms causing a bacterial vaginosis: Gardnerella vaginalis, Mobiluncus spp., Mycoplasma hominis, Bacteroides spp., Peptostreptococcus spp. In high doses it is active concerning some protozoa (Plasmodium falciparum, Toxoplasma gondii, Pneumocystis carinii).

Haemophilus influenzae, Helibacter pylori, Neisseria meningitidis, Neisseria gonorrhoeae, Ureaplasma urealyticum is clinically inefficient against Mycoplasma pneumoniae.

Has cross stability with lincomycin.

Pharmacokinetics. Absorption – high (90%). Tmax at introduction in oil in 1 h (at children) and 3 h (at adults), at in introduction – by the end of infusion. Communication with proteins of plasma – 92-94%. In therapeutic significant concentration collects in almonds, saliva, muscles, a bone tissue (on average 40% of its concentration in plasma), synovial fluid (50%), a phlegm (30-75%), bronchial tubes, lungs, a pleura, pleural liquid (50-90%), bilious channels, an appendix, fallopian pipes, trophic ulcers, wounds, purulent separated (30%), a prostate, breast milk (50-100%), fruit blood (40%), peritoneal liquid (50%), does not get through the unimpaired blood-brain barrier (at an inflammation of a meninx permeability increases). Distribution volume adults – about 0,66 l/kg, at children have 0,86 l/kg. Quickly passes through a placenta, it is found in fruit blood (40%), gets into breast milk (50–100%).

It is metabolized preferential in a liver (70-80%) with education active (N-dimetilklindamitsin and клиндамицинсульфоксид) and inactive metabolites. T½ adults have 2,4-3 h (at a heavy renal failure it is extended to 3-5 h), babies and children of more advanced age have 2,5-3,4 h, premature newborns have 6,3-8,6 h. The rest is removed during 4 days by kidneys (10%) and through intestines (3,6%) in the form of active agent, – in the form of inactive metabolites. Does not kumulirut, it is not removed by means of a hemodialysis and peritoneal dialysis.

Indications to use:

- the bacterial infections caused by sensitive microorganisms: infections of ENT organs (including tonsillitis, pharyngitis, sinusitis, average otitis);

- infections of a respiratory organs (bronchitis, pneumonia, including aspiration, abscess of lungs, pleura empyema, fibroziruyushchy alveolitis);

- infections of bones and joints (osteomyelitis, septic arthritis); purulent infections of skin and soft tissues (including acne, furuncles, phlegmon, impetigo, felon, contaminated wounds, abscesses, ugly face);

- septicaemia (first of all anaerobic), bacterial endocarditis;

- infections of pelvic bodies and intra belly infections (including peritonitis, abscesses of abdominal organs on condition of simultaneous use of means, active concerning gram-negative aerobic microbes);

- gynecologic diseases (endometritis, adnexitis, colpitis, abscesses of fallopian pipes and ovaries, salpingitis, pelviperitonitis);

- oral cavity infections (including periodontal abscess);

- toksoplazmenny encephalitis, the malaria (caused by Plasmodium falciparum) at resistance to chloroquine, the pneumonia (caused by Pneumocystis carinii), clamidiosis; scarlet fever; diphtheria.

Route of administration and doses:

Intravenously (in/in) or intramusculary (in oil): adult – 300 mg 2 times a day. At moderately severe infections – 150 - 300 mg 2 - 4 times a day, at a heavy current – 1,2 - 4,8 g/days in 2 - 4 introductions.

To children appoint 10 - 40 mg/kg/days divided into 3 - 4 introductions.

For in/in introductions part before obtaining concentration not higher than 6 mg/ml (at the rate of 1 ml of medicine in 25 ml of solvent) and enter in/in kapelno within 10-60 min. Introduction of more than 1,2 g during 1 h infusion is not recommended. Solution is stable during 24 h from the moment of preparation. 

The maximum single dose at intramuscular introduction – 600 mg, at intravenous infusion, lasting 1 h – 1200 mg.

Dose adjustment is not required to patients with a heavy renal/liver failure at use of drug with an interval not less than 8 h.

Features of use:

Pseudomembranous colitis can develop both against the background of clindamycin reception, and in 2-3 weeks after the treatment termination (3 – 15% of cases); it is shown by diarrhea, a leukocytosis, fever, abdominal pains (sometimes followed by allocation with a fecal mass of blood and slime). At emergence of these phenomena in mild cases there is enough cancellation of treatment and use of ion-exchange resins (Colestyraminum, колестипол), in hard cases compensation of loss of liquid, electrolytes and protein, purpose of Vancomycinum inside or metronidazole is shown. It is impossible to apply the medicines braking an intestines peristaltics.

Safety of use of drug for newborns is not established. Solution contains benzyl alcohol which can lead to development of a syndrome of suffocation in premature children.

At purpose of drug in high doses control of concentration of clindamycin in plasma is necessary. Patients with a heavy liver failure need to control function of a liver (blood transaminase).

It is not necessary to appoint for treatment of meningitis.

Bystry in/in introduction can lead to development of an acute left ventricular failure and a lowering of arterial pressure.

Side effects:

From the central nervous system: seldom - disturbance of neuromuscular conductivity.

From bodies of a hemopoiesis: tranzitorny neutropenia and eosinophilia, agranulocytosis, thrombocytopenia.

From cardiovascular system: at bystry in introduction – arterial hypotension, a collapse.

Allergic reactions: seldom - makulopapulezny rash, a small tortoiseshell, an itch; in some cases - exfoliative and vezikulobullezny dermatitis, a mnogoformny erythema, a toxic epidermal necrolysis, anaphylactoid reactions.

Local reactions: morbidity (in the place in oil of an injection), thrombophlebitis (in the place in/in an injection).

Others: development of superinfection, pseudomembranous colitis, azotemia, proteinuria or oligouriya.

Interaction with other medicines:

It is incompatible with the solutions containing a complex of vitamins of group B, aminoglycosides, ampicillin, Phenytoinum, barbiturates, Aminophyllinum, calcium a gluconate and magnesium sulfate.

Shows antagonism with erythromycin and chloramphenicol.

Strengthens action of muscle relaxants. At simultaneous use with opioid (narcotic) analgetics increase of respiratory depression (is possible up to an apnoea).

Appointment with the antidiarrheal medicines reducing motility of digestive tract increases risk of development of pseudomembranous colitis.

Aminoglycosides expand a range of antimicrobic action; increases antimicrobic activity of rifampicin.

Contraindications:

Hypersensitivity, ulcer colitis or enteritis, antibiotic - the associated diarrhea in the anamnesis, the neonatality period (up to 1 month).

With care. Myasthenia, heavy renal and/or liver failure, pregnancy, lactation period.

Overdose:

At overdose emergence of diarrhea, nausea and vomiting, easing of neuromuscular conductivity with development of weakness of muscles, breath difficulty, a ptosis is possible. Owing to a short elimination half-life (2,4 hours) there is no need for special measures of the help. Carry out symptomatic therapy, at disturbance of neuromuscular conductivity - неостигмин or pyridostigmine once subcutaneously. The hemodialysis and peritoneal dialysis – are not effective.

Storage conditions:

In the place protected from light, at a temperature from 15 to 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 2 ml in packaging No. 10, No. 10 x 1; in ampoules on 4 ml in packaging No. 10, No. 5 x 2.