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Characteristics of the substance Clindamycin
Clindamycin is a semisynthetic antibiotic of the lincosamide group, formed from lincomycin by replacing the 7 (R) -hydroxyl group with 7 (S) -chlorine.
In medical practice, it is used in the form of hydrochloride, hydrochloride palmitate and phosphate.
Clindamycin hydrochloride is soluble in water, pyridine, ethanol, dimethylformamide.
Clindamycin palmitate hydrochloride is soluble in water.
Clindamycin phosphate is soluble in water.
Pharmacological action - antibacterial, antiprotozoal.
It binds to the 50S ribosomal subunit of a microbial cell and inhibits protein synthesis of sensitive microorganisms. It has a bacteriostatic effect, in high concentrations and against highly sensitive microorganisms can show a bactericidal effect. In terms of the mechanism of action and antimicrobial spectrum, it is close to lincomycin (in relation to some types of microorganisms, it is 2-10 times more active).
When taken orally, clindamycin hydrochloride is rapidly and well absorbed from the gastrointestinal tract (better than lincomycin), bioavailability - 90%, simultaneous food intake slows down absorption without changing the degree of absorption. Protein binding - 92–94%. Easily penetrates into biological fluids, organs and tissues of the body, incl. tonsils, muscle and bone tissue (approximately 40% of the concentration in the blood), bronchi, lungs, pleura, pleural fluid (50–90%), bile ducts, appendix, fallopian tubes, prostate gland, synovial fluid (50%), saliva , phlegm (30–75%), wound discharge. Poorly passes through the BBB (with inflammation of the meninges, the BBB permeability increases). The volume of distribution in adults is approximately 0.66 l / kg, in children - 0.86 l / kg. It quickly passes through the placenta, is found in the blood of the fetus (40%), penetrates into breast milk (50-100%).
Clindamycin palmitate and clindamycin phosphate are inactive; they are rapidly hydrolyzed in the body to active clindamycin.
Cmax in the blood serum after oral administration achieved through 0.75-1 hours after the / m - after 3 hours (adults) or 1 h (children) at / in infusion - the end of administration. It is metabolized in the liver to form active (N-dimethylclindamycin and clindamycin sulfoxide) and inactive metabolites. It is excreted within 4 days in the urine (10%) and through the intestines (3.6%) in the form of an active fraction, the rest in the form of inactive metabolites. T1/2 with normal renal function in adults is 2.4–3 hours, in infants and older children - 2.5–3 hours, in premature infants - 6.3–8.6 hours. In the terminal stage renal failure or severely impaired liver function, the elimination of clindamycin slows down (T1/2 in adults - 3-5 hours). Does not cumulate.
With intravaginal use of 100 mg of clindamycin phosphate in the form of 2% vaginal cream once a day for 7 days in 5 women with bacterial vaginosis, systemic absorption was approximately 5% (in the range of 2–8%) of the administered dose. The Cvaluesmax on the first day are approximately 13 ng / ml (from 3 to 34 ng / ml), on the seventh day - on average 16 ng / ml (from 7 to 26 ng / ml); Tmax - approximately 16 hours (in the range of 8-24 hours) after application. With repeated intravaginal use, systemic cumulation was absent or insignificant. T1/2 with systemic absorption - 1.5–2.6 hours.
When using clindamycin phosphate intravaginally in the form of suppositories at a dose of 100 mg 1 time per day for 3 days, approximately 30% (6–70%) of the administered dose is absorbed into systemic blood flow, while the average AUC is 3.2 μg / h / ml (0.42-11 μg / h / ml). Cmax is reached approximately 5 hours (1-10 hours) after the introduction of the vaginal suppository.
When used in the form of a gel for external use of clindamycin, phosphate is rapidly hydrolyzed by phosphatases in the ducts of the sebaceous glands to form clindamycin. The gel can be absorbed in amounts causing systemic effects.
Thesusceptible to clindamycin in vitro following microorganisms are: aerobic gram-positive cocci, including Staphylococcus aureus, Staphylococcus epidermidis, incl. strains producing and not producing penicillinase (in vitro noted the rapid development of resistance to clindamycin in some staphylococcal strains resistant to erythromycin), Streptococcus spp. (excluding Streptococcus faecalis); Pneumococcus spp .; anaerobic gram-negative bacilli, including Bacteroides spp. (including group B. fragilis and group B. melaninogenicus), Fusobacterium spp .; non-spore forming anaerobic gram-positive bacilli, including Propionibacterium spp., Eubacterium spp., Actinomyces spp .; anaerobic and microaerophilic gram-positive cocci, including Peptococcus spp., Peptostreptococcus spp., Microaerophilic Streptococcus spp., Clostridia spp. (Clostridia are more resistant to clindamycin than most other anaerobes). Most Clostridium perfringens are susceptible to clindamycin, but other species, such as C. sporogenes and C. tertium, are often resistant to clindamycin and sensitivity testing is necessary.
In high doses, it acts on some protozoa (Plasmodium falciparum).
Shown is cross-resistance between clindamycin and lincomycin and antagonism between clindamycin and erythromycin.
In vitro clindamycin is active against most strains of the following microorganisms that cause bacterial vaginosis: Gardnerella vaginalis, Mobiluncus spp., Mycoplasma hominis, Bacteroides spp., Peptostreptococcus spp. Intravaginal clindamycin is ineffective for treating vulvovaginitis caused by Trichomonas vaginalis, Chlamydia trachomatis, Neisseria gonorrhoeae, Candida albicans orvirus Herpes simplex.
The anti-acne effect when applied topically is probably due to the fact that clindamycin reduces the concentration of free fatty acids on the skin and inhibits the multiplication of Propionibacterium acnes , an anaerobe found in the sebaceous glands and follicles. The sensitivity of all studiedstrainsshown P. acnes to clindamycin in vitro (MIC 0.4 μg / ml) was.
Carcinogenicity, mutagenicity, effects on fertility
Long-term studies in animals to assess the potential carcinogenicity of clindamycin have not been conducted. No mutagenic action was found in the Ames test and the micronucleus test in rats. No adverse effects on fertility and mating ability were observed in rats receiving oral clindamycin at doses up to 300 mg / kg / day (approximately 1.6 times higher than the MRA in terms of mg / m2).
Pregnancy. In a study of reproduction in animals (rats, mice) using oral doses of clindamycin up to 600 mg / kg / day (3.2 and 1.6 times higher than the MRDC in terms of mg / m2, respectively) or s / c in doses up to 250 mg / kg / day (1.3 and 0.7 times higher MRDC based on mg / m2, respectively) revealed no teratogenicity. In one experiment on mice, fetuses showed a cleft palate (this result was not confirmed in experiments on other animals and on other lines of mice).
Use of the substance Clindamycin
For systemic use: bacterial infections caused by sensitive microorganisms: infections of ENT organs (including pharyngitis, tonsillitis, sinusitis, otitis media), respiratory infections (bronchitis, pneumonia, including aspiration, abscess lungs, pleural empyema, fibrosing alveolitis), infections of bones and joints (osteomyelitis, septic arthritis), purulent infections of the skin and soft tissues (including acne, boils, phlegmon, impetigo, panaritium, infected wounds, abscesses, erysipelas), septicemia (primarily anaerobic), infections of the pelvic organs and intra-abdominal infections (including peritonitis, abscesses of the abdominal organs, subject to the simultaneous use of drugs that are active against gram-negative aerobic microorganisms), gynecological diseases (including endometritis, adnexitis , abscesses of the fallopian tubes and ovaries, salpingitis, pelvioperitonitis), oral cavity infections (including periodontal abscess), toxoplasmic encephalitis, tropical malaria ( caused by Plasmodium falciparum), resistant to chloroquine (in combination with quinine); Pneumocystis pneumonia (caused by Pneumocystis carinii), sepsis, bacterial endocarditis, scarlet fever, diphtheria.
For intravaginal use: vaginosis caused by microorganisms sensitive to clindamycin.
For external use (gel): acne.
Hypersensitivity (including to lincomycin), a history of regional enteritis, ulcerative colitis or antibiotic-associated colitis.
Restrictions on the use of
Myasthenia gravis (possibly impaired neuromuscular transmission), severe liver and / or kidney dysfunction, infancy (up to 1 month), for the gel - age up to 12 years (safety and efficacy have not been determined).
Application during pregnancy and lactation
During pregnancy, it is possible if the expected effect of therapy outweighs the potential risk to the fetus (adequate and strictly controlled studies in pregnant women have not been carried out, clindamycin passes through the placenta and can concentrate in the fetal liver, however, no complications in humans have been reported). Studies have not established whether treatment for bacterial vaginosis reduces the risk of adverse pregnancy outcomes such as premature rupture of membranes, premature onset of labor, or premature delivery.
The FDA category of action on the fetus is B.
Caution should be exercised when using during breastfeeding (it is not known whether clindamycin passes into breast milk after external and intravaginal use, but is found in breast milk after oral or parenteral administration).
Incompatible with solutions containing a complex of B vitamins, aminoglycosides, ampicillin, phenytoin, barbiturates, aminophylline, calcium gluconate and magnesium sulfate.
In vitro shows the antagonism of clindamycin with erythromycin, as well as with chloramphenicol; since this effect may be clinically significant, these drugs should not be taken simultaneously.
Since clindamycin disrupts neuromuscular transmission and can enhance the effect of peripheral muscle relaxants, caution should be exercised and the patient should be closely monitored with simultaneous use. With simultaneous use with opioid (narcotic) analgesics, it is possible to increase respiratory depression, up to apnea. Simultaneous administration with antidiarrheal drugs that reduce gastrointestinal motility increases the risk of developing pseudomembranous colitis.
Symptoms: increased severity of side effects.
Treatment: symptomatic and supportive. Not excreted by hemodialysis and peritoneal dialysis.
Routes of administration
Inside, i / m or i / v drip, topically, intravaginally.
Precautions of the substance Clindamycin
If hypersensitivity reactions develop, treatment with clindamycin should be discontinued and (if necessary) appropriate therapy should be carried out.
Antibacterial drugs suppress the normal flora of the intestine, which can increase the proliferation of Clostridia. Cases of pseudomembranous colitis of varying severity, up to life-threatening, have been observed with the use of almost all antibacterial agents, including clindamycin.
The toxins produced by Clostridium difficile have been shown to be the main cause of antibiotic-associated colitis. Diarrhea, colitis, symptoms of pseudomembranous colitis may appear both while taking clindamycin and 2-3 weeks after stopping treatment. Pseudomembranous colitis is manifested by diarrhea, leukocytosis, fever, and abdominal pain (sometimes accompanied by fecal discharge of blood and mucus). Therefore, in all cases of diarrhea development after taking antibacterial drugs, the possibility of this diagnosis should be considered. After the diagnosis of pseudomembranous colitis in mild cases, it is sufficient to discontinue treatment and use ion exchange resins (cholestyramine, colestipol), in cases of moderate and severe cases, it is shown that the loss of fluid, electrolytes and protein is replaced, the appointment of an antibacterial drug effective against Clostridium difficile (for example, vancomycin or metronidazole).
It should be remembered that when using local dosage forms, systemic effects are possible. With external use of clindamycin in rare cases, pseudomembranous colitis developed, but with intravaginal use, it was not noted.
In patients over 60 years of age, antibiotic-associated colitis and diarrhea (caused by Clostridium difficile) are more common and may be more severe (the patient's condition and stool frequency should be closely monitored to prevent diarrhea).
When using clindamycin, excessive growth of microorganisms insensitive to it, especially yeast-like fungi, is possible. With the development of superinfection, appropriate measures should be taken depending on the clinical situation.
When administered in high doses, it is necessary to control the plasma concentration of clindamycin. If the treatment is carried out over an extended period of time, then liver and kidney function tests should be carried out regularly.
Before prescribing vaginal suppositories or vaginal cream using appropriate laboratory methods, the presence ofshould be excluded Trichomonas vaginalis, Chlamydia trachomatis, Neisseria gonorrhoeae, Candida albicans,virus Herpes simplex, often causing vulvovaginitis,.
Joint application vaginal suppositories and vaginal creams with other drugs for intravaginal administration are not recommended. During therapy, patients should not have sexual intercourse. Also, do not use intravaginal products (eg tampons). It is not recommended to use condoms or vaginal contraceptive diaphragms during therapy, as ingredients in a cream or suppository can reduce the strength of latex and rubber products.
When applied externally in the form of a gel, avoid contact of the gel on the mucous membrane of the eyes and mouth. After applying the gel to the skin, wash your hands thoroughly. In case of accidental contact with sensitive surfaces (eyes, skin abrasions, mucous membranes), rinse the area with copious amounts of cool water.
Gel for external use is not recommended to be used simultaneously with products that cause peeling and peeling of the skin (including resorcinol, salicylic acid, alcohol-containing products), with soaps or disinfectants containing abrasive substances - a cumulative irritating or drying effect and excessive skin irritation are possible ...
During treatment, care should be taken while working, drivers of vehicles and people whose profession is associated with increased concentration of attention (dizziness is possible).
From the nervous system and sensory organs: rarely - impaired neuromuscular conduction.
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): transient neutropenia (leukopenia) and eosinophilia, agranulocytosis, thrombocytopenia; with rapid intravenous administration - cardiovascular failure (collapse, cardiac arrest), arterial hypotension.
From the digestive tract: abdominal pain, pseudomembranous colitis, esophagitis, nausea, vomiting, diarrhea, dysbiosis, jaundice, liver dysfunction, hyperbilirubinemia; with intravenous administration of large doses - an unpleasant or metallic taste in the mouth.
Allergic reactions: generalized measles-like rash of mild to moderate severity, maculopapular rash, urticaria, itching; rarely - exfoliative and vesicular-bullous dermatitis, erythema multiforme, toxic epidermal necrolysis; in some cases - anaphylactoid reactions.
Others: rarely - azotemia, oliguria and / or proteinemia, polyarthritis, development of superinfection; reactions at the injection site - soreness, induration, abscess (with intramuscular injection), thrombophlebitis (with intravenous injection).