Pharmacological properties: clindamycin - a semisynthetic antibiotic that is produced from lincomycin by replacing 7 - (R)-hydroxyl group of 7 - (S)-chloro. In vitro active against the following microorganisms:
- Aerobic Gram-positive cocci, including Staphylococcus aureus, Staphylococcus epidermidis (including strains producing and not producing penicillinase; in vitro saw a rapid development of resistance to the drug in some strains that are resistant to erythromycin); Streptococcus spp. (Except Streptococcus faecalis), Streptococcus pneumoniae;
- Anaerobic Gram-negative bacteria, including Bacteroides spp. (Including B. fragilis, B. melaninogenicus), Fusobacterium spp.;
- Anaerobic Gram-positive asporogenous bacteria, including Propionibacterium, Eubacterium, Actinomyces spp.;
- Anaerobic and microaerophilic Gram-positive cocci, including Peptococcus spp., Peptostreptococcus spp., Microaerophilic streptococci.
In in vitro studies found that the clindamycin susceptible strains of microorganisms such as Bacteroides melaninogenicus, B. disiens, B. bivius, Peptostreptococcus spp., Gardnerella vaginalis, Mobiluncus mulieris, M. curtisii, Mycoplasma hominis. Clostridium have greater resistance to clindamycin than most other anaerobes. Most Clostridium perfringens are susceptible to clindamycin, but some species (eg C. sporogenes and C. tertium) is often resistant to clindamycin. In this connection, to conduct test for sensitivity to antibiotics.
Between lincomycin and clindamycin there cross-resistance. There is antagonism between clindamycin and erythromycin.
Offer the drug in serum after prolonged use of clindamycin hydrochloride (up to 14 days) did not find the data that could indicate a cumulation of the drug or change in its metabolism. The half-life of clindamycin from the serum slightly increased in patients with significant deterioration of renal function. Hemodialysis and peritoneal dialysis is not effective in removing clindamycin from the serum. The concentration of clindamycin in the serum increased linearly with increasing doses and exceed the minimum bacteriostatic concentration for the most common microorganisms for at least 6 hours after taking the usual recommended dose. Clindamycin is widely distributed in liquids and body tissues (including bone). The average half-life of the drug is 2.4 hours Approximately 10% of the biologically active drug is excreted in the urine and 3,6% - with the feces; the remainder of the drug appears in the form of inactive metabolites. Doses up to 2 grams of clindamycin per day for 14 days were well tolerated healthy volunteers, but with increasing doses increased the percentage of adverse reactions from the digestive tract. In the CSF concentration of clindamycin does not reach a significant level even with meningitis. Pharmacokinetic parameters (clearance, half-life, volume of distribution and AUC) in different age groups (adults and elderly) after i / v administration is different, and because there is no need to change the dosage of the drug in the treatment of elderly patients with preserved function of age, respectively, liver and kidneys.
INDICATIONS: infectious-inflammatory diseases caused by microorganisms sensitive to clindamycin:
- Infection of ENT organs, including tonsillitis, pharyngitis, sinusitis, otitis media, scarlet fever;
- Respiratory infections, including bronchitis, pneumonia, lung abscess, empyema;
- Infections of skin and soft tissues, including acne, furunculosis, abscess, impetigo, abscesses, infected wounds, specific infectious processes of the skin and soft tissues (erysipelas, and paronychia / felon);
- Infections of bones and joints, including osteomyelitis and suppurative arthritis;
- Gynecological infection, including endometritis, pelviotsellyulit, infection, vaginal cuff, ovarial abscesses, salpingitis and pelvic inflammatory disease if the drug is given with an antibiotic with activity against gram-negative pathogens, infection of the cervix, caused by Chlamydia trachomatis, clindamycin monotherapy leads to eradication of the causative agent;
- Infectious processes in the abdominal cavity, including peritonitis, abscesses of the abdominal cavity (in combination with antibiotics, acting on Gram-negative aerobes);
- Septicemia and endocarditis;
- Infection of oral cavity (including periodontitis and periodontal abscess);
- Toxoplasma encephalitis in AIDS patients (in combination with pyrimethamine in patients with intolerance to standard therapy);
- Pneumocystis pneumonia in AIDS patients (in combination with primaquine);
- Malaria, including cases of multidrug-resistant Plasmodium falciparum, as monotherapy or in combination with quinine or chloroquine;
- Prevention of endocarditis in patients with allergy to penicillin (s);
- Prevention of wound infection in surgical interventions in head and neck;
- Prevention of peritonitis and intraabdominal abscesses after perforation and trauma contamination in combination with aminoglycosides (gentamicin or tobramitsinom).
APPLICATION: in / or / m In the case of pelvic infection in women, abdominal and other complications or severe infections in adults Dalatsin C Phosphate is usually prescribed at a daily dose of 2400-2700 mg divided by 2, 3 or 4 equal doses. To treat more lung infections caused by highly sensitive to clindamycin microorganisms can be assigned a lower daily dose - 1200-1800 mg divided into 3 or 4 of the introduction.
In severe cases, the daily dose can be increased to 4800 mg.
In most cases (except for some evidence) with the / m more than the introduction of a single dose over 600 mg is not recommended. No need for dose adjustment in the treatment of elderly patients, patients with renal or hepatic insufficiency.
Use in children older than 1 month. Daily dose Dalatsina C Phosphate is 20-40 mg / kg, divided into 3 or 4 of the introduction.
Application of newborns (children below the age of 1 month). Dose of Daqing C Phosphate is 15-20 mg / kg, divided into 3 or 4 of the introduction. In premature infants the dose may be reduced body weight, respectively.
Dosage for individual testimony
In the treatment of infections caused by β-hemolytic streptococcus, apply the above dose. Duration of treatment - not less than 10 days.
In the treatment of inflammatory diseases of the pelvic organs. Assign to 900 mg C Dalatsina phosphate / in every 8 h with a / in the introduction of an antibiotic active against gram-negative aerobes (eg gentamicin at a dose of 2.0 mg / kg with a further reduction to 1.5 mg / kg every 8 h in patients with preserved kidney function). In / in the introduction should continue for at least 4 days, and at least within 48 hours after onset of clinical effect. After parenteral administration of the drug for 6 days should continue receiving clindamycin hydrochloride inside of 450-600 mg every 6 h until the completion of 10-14-day cycle of therapy.
In the treatment of Toxoplasma encephalitis in AIDS patients. Enter in / at a dose of 600-1200 mg every 6 h for 2 weeks, followed by 300-600 mg orally every 6 hours Usually therapy is 8-10 weeks. The dose of pyrimethamine 25-75 mg orally every day for 8-10 weeks. Folinievaya acid at a dose of 10-20 mg per day should be appointed in the application of higher doses of pyrimethamine.
In the treatment of pneumonia caused by Pneumocystis carinii, in patients with AIDS. Dalatsin C Phosphate is introduced into / in to 600-900 mg every 6 hours or 900 mg every 8 hours for 21 days in combination with primaquine - by 15-30 mg orally 1 time a day.
For the prevention of surgical infection during operations in the head and neck. For intraoperative irrigation of contaminated surgical wounds in the head and neck before suturing the wounds are used 900 mg Dalatsina C phosphate, diluted in 1000 ml of isotonic p-ra sodium chloride.
Dalatsin C Phosphate should not be used in / with no dilution in the form of bolus injection. The drug should be administered by infusion over 10-60 min. Dalatsin C phosphate can be diluted in 50-100 ml of p-ra injection of dextrose 5% or sodium chloride 0.9%. The concentration of drug in the p re-infusion should not exceed 18 mg / ml, the rate of introduction - 30 mg / min . When preparing p-ra for infusion should be remembered that clindamycin phosphate is physically compatible with the p-ramie-containing sodium chloride, glucose, potassium and B vitamins in normal doses, and such antibiotics as cefalotin, kanamycin, gentamicin, penicillin or Carbenicillin. Rr Dalatsina C Phosphate is not compatible with ampicillin sodium, phenytoin sodium, barbiturates, aminophylline, calcium gluconate, magnesium sulfate, ceftriaxone sodium and ciprofloxacin.
Commonly used are the rate of introduction:
Dose, mg
Volume p-ra, ml
Time of administration, min
300
50
10
600
50
20
900
50-100
30
1200
100
40
For once in / infusion does not exceed recommended dose of 1200 mg.
CONTRAINDICATIONS: Hypersensitivity to clindamycin, lincomycin or to any component of the drug.
SIDE EFFECTS: Co side of the blood system - Cases of leukopenia, neutropenia, eosinophilia, agranulocytosis and thrombocytopenia, but the true causal relationship between these changes and the drug intake was found;
by the immune system - isolated instances of anaphylactoid reactions;
from cardiovascular and respiratory systems - at too fast a / in the introduction of the drug are rare cases of cessation of breathing and heart, as well as the development of arterial hypotension;
from the digestive tract - may be abdominal pain, nausea, vomiting, diarrhea, pseudomembranous colitis, and candidiasis, esophagitis and esophageal ulcer;
of the hepatobiliary system - jaundice, changes in indicators of liver function tests;
from the skin - in some cases there were maculopapular rash, urticaria, mild to moderate generalized korepodobnaya rash, isolated cases of polymorphous erythema, pruritus, vaginitis, exfoliative, and vesicle-bullous dermatitis, toxic epidermal necrolysis, local reactions - if i / m administration the drug may experience local irritation, tenderness and abscess formation in the introduction, with a / in the conduct of - the phenomenon of thrombosis (the frequency decreases with decrease in the use of permanent in / catheters).
Cautions: Dalatsin C Phosphate Injection contains benzyl alcohol, which can cause fatal flow Gasping syndrome in infants. Treatment of clindamycin, as well as treatment of almost all other antibiotics, may be accompanied by the development of severe pseudomembranous colitis with fatal consequences. It is important to promptly suspect this diagnosis in patients who have diarrhea occurred after the application of antibacterial drugs. Antibacterial drugs suppressed vital functions of normal microflora of the colon that can cause rapid multiplication of clostridia. Our studies indicate that the toxins produced by Clostridium, especially Clostridium difficile, are a crucial and immediate cause of colitis caused by antibiotics. In establishing the diagnosis of pseudomembranous colitis should designate an appropriate treatment. In the case of mild forms of pseudomembranous colitis may be sufficient to cease treatment clindamycin. With the development of moderate and severe forms of pseudomembranous colitis should be appropriate therapy with the appointment of fluids, electrolytes, proteins and drugs effective against Clostridium difficile. Clindamycin should not be appointed for the treatment of meningitis because the drug penetrates poorly through the BBB.
If the treatment is done for a long time, it is necessary to control the function of the liver and kidneys.
Because clindamycin therapy may be enhanced by the microflora are not sensitive to this drug, especially yeast.
Clindamycin is able to penetrate through the placenta. With prolonged use of clindamycin levels in amniotic fluid is approximately 30% of the level of drug concentration in maternal blood. Clindamycin may be appointed to pregnant only if absolutely necessary.
It has been reported about the penetration of clindamycin into breast milk in concentrations from 0,7 to 3,8 mg / ml. It is recommended to stop breast-feeding during the period of Dalatsina C phosphate.
Effect of clindamycin on the ability to drive and work with potentially dangerous machinery has not been studied sufficiently.
Interactions: There is in vitro antagonism between clindamycin and erythromycin. Because such interaction may have clinical significance, these drugs should not be given simultaneously.
Clindamycin is partly a blocker of the neuromuscular conduction and may exacerbate the effects of other muscle relaxants.
OVERDOSE: under recommended doses was not observed. Hemodialysis and peritoneal dialysis are not effective.
STORAGE: at room temperature (15-25 ° C).
- Aerobic Gram-positive cocci, including Staphylococcus aureus, Staphylococcus epidermidis (including strains producing and not producing penicillinase; in vitro saw a rapid development of resistance to the drug in some strains that are resistant to erythromycin); Streptococcus spp. (Except Streptococcus faecalis), Streptococcus pneumoniae;
- Anaerobic Gram-negative bacteria, including Bacteroides spp. (Including B. fragilis, B. melaninogenicus), Fusobacterium spp.;
- Anaerobic Gram-positive asporogenous bacteria, including Propionibacterium, Eubacterium, Actinomyces spp.;
- Anaerobic and microaerophilic Gram-positive cocci, including Peptococcus spp., Peptostreptococcus spp., Microaerophilic streptococci.
In in vitro studies found that the clindamycin susceptible strains of microorganisms such as Bacteroides melaninogenicus, B. disiens, B. bivius, Peptostreptococcus spp., Gardnerella vaginalis, Mobiluncus mulieris, M. curtisii, Mycoplasma hominis. Clostridium have greater resistance to clindamycin than most other anaerobes. Most Clostridium perfringens are susceptible to clindamycin, but some species (eg C. sporogenes and C. tertium) is often resistant to clindamycin. In this connection, to conduct test for sensitivity to antibiotics.
Between lincomycin and clindamycin there cross-resistance. There is antagonism between clindamycin and erythromycin.
Offer the drug in serum after prolonged use of clindamycin hydrochloride (up to 14 days) did not find the data that could indicate a cumulation of the drug or change in its metabolism. The half-life of clindamycin from the serum slightly increased in patients with significant deterioration of renal function. Hemodialysis and peritoneal dialysis is not effective in removing clindamycin from the serum. The concentration of clindamycin in the serum increased linearly with increasing doses and exceed the minimum bacteriostatic concentration for the most common microorganisms for at least 6 hours after taking the usual recommended dose. Clindamycin is widely distributed in liquids and body tissues (including bone). The average half-life of the drug is 2.4 hours Approximately 10% of the biologically active drug is excreted in the urine and 3,6% - with the feces; the remainder of the drug appears in the form of inactive metabolites. Doses up to 2 grams of clindamycin per day for 14 days were well tolerated healthy volunteers, but with increasing doses increased the percentage of adverse reactions from the digestive tract. In the CSF concentration of clindamycin does not reach a significant level even with meningitis. Pharmacokinetic parameters (clearance, half-life, volume of distribution and AUC) in different age groups (adults and elderly) after i / v administration is different, and because there is no need to change the dosage of the drug in the treatment of elderly patients with preserved function of age, respectively, liver and kidneys.
INDICATIONS: infectious-inflammatory diseases caused by microorganisms sensitive to clindamycin:
- Infection of ENT organs, including tonsillitis, pharyngitis, sinusitis, otitis media, scarlet fever;
- Respiratory infections, including bronchitis, pneumonia, lung abscess, empyema;
- Infections of skin and soft tissues, including acne, furunculosis, abscess, impetigo, abscesses, infected wounds, specific infectious processes of the skin and soft tissues (erysipelas, and paronychia / felon);
- Infections of bones and joints, including osteomyelitis and suppurative arthritis;
- Gynecological infection, including endometritis, pelviotsellyulit, infection, vaginal cuff, ovarial abscesses, salpingitis and pelvic inflammatory disease if the drug is given with an antibiotic with activity against gram-negative pathogens, infection of the cervix, caused by Chlamydia trachomatis, clindamycin monotherapy leads to eradication of the causative agent;
- Infectious processes in the abdominal cavity, including peritonitis, abscesses of the abdominal cavity (in combination with antibiotics, acting on Gram-negative aerobes);
- Septicemia and endocarditis;
- Infection of oral cavity (including periodontitis and periodontal abscess);
- Toxoplasma encephalitis in AIDS patients (in combination with pyrimethamine in patients with intolerance to standard therapy);
- Pneumocystis pneumonia in AIDS patients (in combination with primaquine);
- Malaria, including cases of multidrug-resistant Plasmodium falciparum, as monotherapy or in combination with quinine or chloroquine;
- Prevention of endocarditis in patients with allergy to penicillin (s);
- Prevention of wound infection in surgical interventions in head and neck;
- Prevention of peritonitis and intraabdominal abscesses after perforation and trauma contamination in combination with aminoglycosides (gentamicin or tobramitsinom).
APPLICATION: in / or / m In the case of pelvic infection in women, abdominal and other complications or severe infections in adults Dalatsin C Phosphate is usually prescribed at a daily dose of 2400-2700 mg divided by 2, 3 or 4 equal doses. To treat more lung infections caused by highly sensitive to clindamycin microorganisms can be assigned a lower daily dose - 1200-1800 mg divided into 3 or 4 of the introduction.
In severe cases, the daily dose can be increased to 4800 mg.
In most cases (except for some evidence) with the / m more than the introduction of a single dose over 600 mg is not recommended. No need for dose adjustment in the treatment of elderly patients, patients with renal or hepatic insufficiency.
Use in children older than 1 month. Daily dose Dalatsina C Phosphate is 20-40 mg / kg, divided into 3 or 4 of the introduction.
Application of newborns (children below the age of 1 month). Dose of Daqing C Phosphate is 15-20 mg / kg, divided into 3 or 4 of the introduction. In premature infants the dose may be reduced body weight, respectively.
Dosage for individual testimony
In the treatment of infections caused by β-hemolytic streptococcus, apply the above dose. Duration of treatment - not less than 10 days.
In the treatment of inflammatory diseases of the pelvic organs. Assign to 900 mg C Dalatsina phosphate / in every 8 h with a / in the introduction of an antibiotic active against gram-negative aerobes (eg gentamicin at a dose of 2.0 mg / kg with a further reduction to 1.5 mg / kg every 8 h in patients with preserved kidney function). In / in the introduction should continue for at least 4 days, and at least within 48 hours after onset of clinical effect. After parenteral administration of the drug for 6 days should continue receiving clindamycin hydrochloride inside of 450-600 mg every 6 h until the completion of 10-14-day cycle of therapy.
In the treatment of Toxoplasma encephalitis in AIDS patients. Enter in / at a dose of 600-1200 mg every 6 h for 2 weeks, followed by 300-600 mg orally every 6 hours Usually therapy is 8-10 weeks. The dose of pyrimethamine 25-75 mg orally every day for 8-10 weeks. Folinievaya acid at a dose of 10-20 mg per day should be appointed in the application of higher doses of pyrimethamine.
In the treatment of pneumonia caused by Pneumocystis carinii, in patients with AIDS. Dalatsin C Phosphate is introduced into / in to 600-900 mg every 6 hours or 900 mg every 8 hours for 21 days in combination with primaquine - by 15-30 mg orally 1 time a day.
For the prevention of surgical infection during operations in the head and neck. For intraoperative irrigation of contaminated surgical wounds in the head and neck before suturing the wounds are used 900 mg Dalatsina C phosphate, diluted in 1000 ml of isotonic p-ra sodium chloride.
Dalatsin C Phosphate should not be used in / with no dilution in the form of bolus injection. The drug should be administered by infusion over 10-60 min. Dalatsin C phosphate can be diluted in 50-100 ml of p-ra injection of dextrose 5% or sodium chloride 0.9%. The concentration of drug in the p re-infusion should not exceed 18 mg / ml, the rate of introduction - 30 mg / min . When preparing p-ra for infusion should be remembered that clindamycin phosphate is physically compatible with the p-ramie-containing sodium chloride, glucose, potassium and B vitamins in normal doses, and such antibiotics as cefalotin, kanamycin, gentamicin, penicillin or Carbenicillin. Rr Dalatsina C Phosphate is not compatible with ampicillin sodium, phenytoin sodium, barbiturates, aminophylline, calcium gluconate, magnesium sulfate, ceftriaxone sodium and ciprofloxacin.
Commonly used are the rate of introduction:
Dose, mg
Volume p-ra, ml
Time of administration, min
300
50
10
600
50
20
900
50-100
30
1200
100
40
For once in / infusion does not exceed recommended dose of 1200 mg.
CONTRAINDICATIONS: Hypersensitivity to clindamycin, lincomycin or to any component of the drug.
SIDE EFFECTS: Co side of the blood system - Cases of leukopenia, neutropenia, eosinophilia, agranulocytosis and thrombocytopenia, but the true causal relationship between these changes and the drug intake was found;
by the immune system - isolated instances of anaphylactoid reactions;
from cardiovascular and respiratory systems - at too fast a / in the introduction of the drug are rare cases of cessation of breathing and heart, as well as the development of arterial hypotension;
from the digestive tract - may be abdominal pain, nausea, vomiting, diarrhea, pseudomembranous colitis, and candidiasis, esophagitis and esophageal ulcer;
of the hepatobiliary system - jaundice, changes in indicators of liver function tests;
from the skin - in some cases there were maculopapular rash, urticaria, mild to moderate generalized korepodobnaya rash, isolated cases of polymorphous erythema, pruritus, vaginitis, exfoliative, and vesicle-bullous dermatitis, toxic epidermal necrolysis, local reactions - if i / m administration the drug may experience local irritation, tenderness and abscess formation in the introduction, with a / in the conduct of - the phenomenon of thrombosis (the frequency decreases with decrease in the use of permanent in / catheters).
Cautions: Dalatsin C Phosphate Injection contains benzyl alcohol, which can cause fatal flow Gasping syndrome in infants. Treatment of clindamycin, as well as treatment of almost all other antibiotics, may be accompanied by the development of severe pseudomembranous colitis with fatal consequences. It is important to promptly suspect this diagnosis in patients who have diarrhea occurred after the application of antibacterial drugs. Antibacterial drugs suppressed vital functions of normal microflora of the colon that can cause rapid multiplication of clostridia. Our studies indicate that the toxins produced by Clostridium, especially Clostridium difficile, are a crucial and immediate cause of colitis caused by antibiotics. In establishing the diagnosis of pseudomembranous colitis should designate an appropriate treatment. In the case of mild forms of pseudomembranous colitis may be sufficient to cease treatment clindamycin. With the development of moderate and severe forms of pseudomembranous colitis should be appropriate therapy with the appointment of fluids, electrolytes, proteins and drugs effective against Clostridium difficile. Clindamycin should not be appointed for the treatment of meningitis because the drug penetrates poorly through the BBB.
If the treatment is done for a long time, it is necessary to control the function of the liver and kidneys.
Because clindamycin therapy may be enhanced by the microflora are not sensitive to this drug, especially yeast.
Clindamycin is able to penetrate through the placenta. With prolonged use of clindamycin levels in amniotic fluid is approximately 30% of the level of drug concentration in maternal blood. Clindamycin may be appointed to pregnant only if absolutely necessary.
It has been reported about the penetration of clindamycin into breast milk in concentrations from 0,7 to 3,8 mg / ml. It is recommended to stop breast-feeding during the period of Dalatsina C phosphate.
Effect of clindamycin on the ability to drive and work with potentially dangerous machinery has not been studied sufficiently.
Interactions: There is in vitro antagonism between clindamycin and erythromycin. Because such interaction may have clinical significance, these drugs should not be given simultaneously.
Clindamycin is partly a blocker of the neuromuscular conduction and may exacerbate the effects of other muscle relaxants.
OVERDOSE: under recommended doses was not observed. Hemodialysis and peritoneal dialysis are not effective.
STORAGE: at room temperature (15-25 ° C).
No comments:
Post a Comment