Pharmacodynamics and pharmacokinetics
the lincosamide antibiotic clindamycin as an active ingredient , is a local remedy used in gynecology for the treatment of gardnerellosis (vaginosis) of bacterial origin. The mechanism of action of local dosage forms of the drug (cream, suppositories) is aimed at disrupting the processes of intracellular protein synthesis in the microbial cell, which occurs at the level of the large ribosomal subunit 50S.
The spectrum of action of clindamycin is quite wide. In medium doses, the drug exhibits bacteriostatic effectiveness against many microorganisms . At higher dosages, clindamycin is characterized by a bactericidal effect aimed at destroying certain bacterial strains .
The main activity of clindamycin is observed against microorganisms leading to the formation of bacterial vaginosis , including: Mobiluncus spp. (mobiluncus), Gardnerella vaginalis (Gardnerella vaginalis), Bacteroides spp. (bacteroides), Peptostreptococcus spp. (peptostreptococci), Mycoplasma hominis (mycoplasma hominis).
Strains of Candida albicans ( thrush ) and Trichomonas vaginalis ( Trichomonas vaginalis insensitive to the effects of clindamycin .
Intravaginal (inside the vagina) single administration of clindamycin at a dose of 100 mg leads to systemic absorption of approximately 4% of the drug (about 4 mg). Plasma Cmax of clindamycin is 20 ng/ml.
Clindamycin
To avoid complications, use strictly as prescribed by your doctor!
There have been case reports of severe hypersensitivity reactions, including severe skin reactions such as drug rash with eosinophilia and systemic symptoms (DRESS syndrome), Stevens-Johnson syndrome, toxic epidermal necrolysis and acute generalized exanthematous pustulosis in patients receiving clindamycin therapy. If a hypersensitivity reaction or severe skin reaction occurs, treatment with clindamycin should be discontinued and appropriate therapy for these complications should be initiated (see sections "Contraindications" and "Side Effects").
The drug contains gasoline alcohol. There are reports that gasoline alcohol causes the development of Gasping Syndrome, which is
fatal
in children. Although therapeutic doses of the drug usually contain a dose of benzyl alcohol significantly lower than the dose at which the development of this complication was observed, the minimum amount of benzyl alcohol that has a toxic effect is unknown. The degree of toxicity of benzyl alcohol depends on the amount of drug administered and the ability of the liver and kidneys to detoxify chemical compounds. Premature and low birth weight infants are at higher risk of toxicity.
The amount of benzyl alcohol per 1 ml of drug solution is 9 mg.
Clostridium
difficile
associated diarrhea is observed with the use of almost all antibacterial drugs, including clindamycin, and manifests itself from mild forms of diarrhea to severe colitis with a fatal outcome.
Antibacterial drugs suppress the normal intestinal flora, which can contribute to increased proliferation of clostridia. Clostridium difficile
produces toxins A and B, leading to the development of
Clostridium difficile
associated diarrhea.
Hypertoxin-producing strains of Clostridium difficile
lead to increased morbidity and mortality because they may be resistant to antibiotic therapy and may require colonectomy for treatment.
All cases of diarrhea in patients during antibiotic therapy should be considered suspicious for the development of Clostridium difficile
associated diarrhea.
A thorough medical history is required if Clostridium difficile
associated diarrhea develops within 2 months after the prescription of antibacterial drugs.
Pseudomembranous colitis is manifested by diarrhea, leukocytosis, fever, abdominal pain (sometimes accompanied by the discharge of blood and mucus in the stool) and can develop both while taking clindamycin and 2-3 weeks after stopping treatment. After a diagnosis of pseudomembranous colitis is made, in mild cases it is sufficient to discontinue treatment and use ion exchange resins (colestyramine, colestipol); in moderate and severe cases, replacement of the loss of fluid, electrolytes and protein, and the prescription of an antibacterial drug effective against Clostridium difficile
, for example, vancomycin at a dose of 125-500 mg, or bacitracin at a dose of 25,000 units orally 4 times a day for 7-10 days, or metronidazole at a dose of 250-500 mg 3 times a day.
Drugs that reduce gastrointestinal motility should not be coadministered with clindamycin.
Clindamycin should be used with caution in patients with a history of gastrointestinal diseases, especially colitis. Antibiotic-associated colitis and diarrhea occur more frequently and more severely in debilitated and/or elderly patients.
When using all antibacterial agents, including clindamycin, excessive growth of microorganisms that are insensitive to this drug, especially yeast-like fungi, is possible. If superinfection develops, appropriate measures should be taken depending on the clinical situation.
Clindamycin should not be used to treat meningitis because it does not penetrate the blood-brain barrier well.
When using the drug in high doses, monitoring the concentration of clindamycin in the blood plasma is necessary. If treatment is carried out over a long period of time, liver and kidney function tests should be carried out regularly. In patients with impaired liver and kidney function, no dose adjustment of the drug is required, since clindamycin practically does not accumulate in the body if the drug is administered at intervals of 8 hours. Patients with severe hepatic and/or renal insufficiency should use the drug with caution and monitor liver function (“ liver" enzymes) and kidneys.
The drug should not be administered intravenously undiluted or simultaneously. The infusion must be carried out for at least 10-60 minutes (see section “Method of administration and dosage”).
Side effects
Some patients, when using Clindacin, experienced the development of negative side effects, including: a feeling of itching in the vagina , the formation of a maculopapular rash , the occurrence of urticaria , the development of cervicitis or colpitis (vaginitis), vulvovaginal irritation burning sensation .
In rare cases, the following were observed from the hematopoietic system: thrombocytopenia , reversible leukopenia , eosinophilia , neutropenia , agranulocytosis .
In case of significant systemic absorption of clindamycin, its inherent systemic side effects may occur, including the formation of pseudomembranous enterocolitis (very rare).
Clindacin 100 mg 3 pcs. vaginal suppositories pharmaprim
pharmachologic effect
An antibiotic from the lincosamide group, it has a wide spectrum of antimicrobial action.
The mechanism of action is due to binding to the 50 S subunit of the ribosomal membrane and suppression of protein synthesis in the microbial cell. Acts bacteriostatically. A bactericidal effect is possible against a number of gram-positive cocci. Active against Staphylococcus spp. (including Staphylococcus epidermidis, producing and non-producing penicillinase), Streptococcus spp. (excluding Enterococcus faecalis), Streptococcus pneumoniae, Corynebacterium diphtheriae, Mycoplasma spp., anaerobic and microaerophilic gram-positive cocci (including Peptococcus spp. and Peptostreptococcus spp.), Clostridium perfringens, Clostridium tetani, Bacteroides spp. (including Bacteroides fragilis and Prevotella melaninogenica), Fusobacterium spp., Propionibacterium spp., Eubacterium spp. and Actinomyces israelii.
Most strains of Clostridium perfringens are sensitive to clindamycin, but other Clostridium spp. (including Clostridium sporogenes, Clostridium tertium) are resistant to its action, and therefore for infections caused by Clostridium spp., it is recommended to determine an antibiogram.
Cross-resistance exists between clindamycin and lincomycin.
Composition and release form Clindacin 100 mg 3 pcs. vaginal suppositories pharmaprim
Vaginal suppositories - 1 sup.:
- Active substance: clindamycin (in phosphate form) - 100 mg;
- Excipients: semi-synthetic glycerides (such as “Estarinum”, “Vitepsol” or “Suppotsir”).
3 pcs. — cellular contour packaging, cardboard packs.
Description of the dosage form
Vaginal suppositories are white or white with a yellowish tint, cylindrical-conical in shape; there are no inclusions on the longitudinal section; the presence of an airy and porous rod and a funnel-shaped recess is allowed.
Directions for use and doses
Prescribe intravaginally 1 suppository 1 time/day immediately before bedtime, for 3-7 days in a row.
Before use, one suppository is released from the contour packaging, having previously cut the film along the contour of the suppository, and inserted, if possible, deep into the vagina, in a lying position.
Pharmacokinetics
After a single intravaginal administration of clindamycin at a dose of 100 mg, 4% of the administered dose is subject to systemic absorption. Cmax in plasma - 20 ng/ml.
Indications for use Clindacin 100 mg 3 pcs. vaginal suppositories pharmaprim
Bacterial vaginosis caused by microorganisms sensitive to the drug.
Contraindications
- I trimester of pregnancy;
- hypersensitivity to the components of the drug.
Application of Clindacin 100 mg 3 pcs. vaginal suppositories pharmaprim during pregnancy and breastfeeding
Intravaginal use of Clindacin during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. Clindamycin penetrates the placental barrier into the fetal circulatory system.
Clindamycin is excreted in breast milk. It is recommended to prescribe the drug with caution during lactation. Breastfeeding should be stopped during treatment.
special instructions
Vaginal suppositories are not recommended for use simultaneously with other intravaginal medications.
Influence on the ability to drive vehicles and operate machinery.
The drug does not affect the ability to concentrate and the speed of psychomotor reactions.
Overdose
Due to the low absorption of the drug, an overdose is unlikely.
Side effects Clindacin 100 mg 3 pcs. vaginal suppositories pharmaprim
From the reproductive system: cervicitis, vaginitis, vulvovaginal irritation.
From the hematopoietic organs: rarely - reversible leukopenia, neutropenia, eosinophilia, agranulocytosis, thrombocytopenia.
Allergic reactions: maculopapular rash, urticaria, itching.
Other: with systemic absorption, other systemic side effects are possible, incl. in rare cases - pseudomembranous enterocolitis.
Drug interactions
Clindacin® enhances the effect of drugs rifampicin, aminoglycosides - streptomycin, gentamicin.
Enhances muscle relaxation caused by n-cholinergic blockers.
Clindacin® is incompatible with erythromycin, ampicillin, diphenylhydantoin derivatives, barbiturates, aminophylline, calcium gluconate and magnesium sulfate.
Instructions for use of Clindacin (Method and dosage)
Clindacin cream, instructions for use
Clindacin cream is intended for intravaginal use using a special disposable applicator included in the package with the medicinal product. The recommended single daily dosage of the cream is 100 mg of clindamycin (the volume of a completely filled applicator). It is best to administer the drug in the evening (before bedtime). The duration of the treatment course, as a rule, takes from 3 to 7 days.
Using the applicator
For proper dosing and introduction of the cream into the vagina, it is recommended to use disposable applicators contained in the package with the drug and adhere to the technique for their use, namely:
- remove the protective cap from the tube of cream;
- screw a disposable plastic applicator into its place;
- squeeze the opposite end of the tube to completely fill the applicator (the applicator is considered completely filled when its independently moving piston reaches the stop);
- lying on your back, insert the applicator into the vagina as deeply as possible;
- Gently press the applicator piston until it is completely empty;
- Carefully remove the used applicator from the vagina and throw it away.
Clindacin suppositories, instructions for use
Clindacin suppositories are also used intravaginally, with a single daily administration of 1 suppository, preferably in the evening (before bedtime). The duration of the treatment course, as a rule, takes from 3 to 7 days.
For proper use of the drug, one suppository should be released from the outer contour packaging by cutting the protective film along the contours of the suppository. Then, in a lying position, insert the suppository into the vagina as deeply as possible.
Clindacin cream - according to prescription, method of application
Cream, unlike suppositories, can only be purchased with a prescription. It is inserted into the vagina using a special applicator. It is recommended to take 100 mg of cream one time. The course of treatment can vary from 3 to 7 days, depending on the severity of the disease and the severity of symptoms.
It is important not to stop treatment if all signs of the disease have disappeared after the first dose. Antibacterial therapy involves a course approach. For this category of drugs, the minimum period of use is 3 days. If therapy is interrupted, resistance of microorganisms to the active substance may develop.
Interaction
When used in combination with clindamycin, the effectiveness of aminoglycosides ( Streptomycin ), Rifampicin and Gentamicin .
Clindamycin is incompatible with Aminophylline , Erythromycin , Magnesium sulfate , Ampicillin , Calcium gluconate , diphenylhydantoin and barbiturates.
The effects of clindamycin increase muscle relaxation caused by the effects of n-cholinergic blockers .
special instructions
In case of prolonged use of the drug, the possibility of excessive growth of microorganisms insensitive to its active ingredient, especially fungal strains of Candida, is allowed.
The combined use of Clindacin with other intravaginal medications is not recommended.
Due to the minimal, but still systemic absorption of clindamycin (about 4%), against the background of its topical use, diarrhea , requiring discontinuation of the drug.
Clindamycin (solution)
To avoid complications, use strictly as prescribed by your doctor!
There have been case reports of severe hypersensitivity reactions, including severe skin reactions such as drug rash with eosinophilia and systemic symptoms (DRESS syndrome), Stevens-Johnson syndrome, toxic epidermal necrolysis and acute generalized exanthematous pustulosis in patients receiving clindamycin therapy. If a hypersensitivity reaction or severe skin reaction occurs, treatment with clindamycin should be discontinued and appropriate therapy for these complications should be initiated (see sections "Contraindications" and "Side Effects").
The drug contains benzyl alcohol. There are reports that benzyl alcohol causes Gasping Syndrome
- disorders of the respiratory system, manifested in the form of suffocation) with a fatal outcome in children.
Although therapeutic doses of the drug usually contain a dose of benzyl alcohol significantly lower than the dose at which the development of this complication was observed, the minimum amount of benzyl alcohol that has a toxic effect is unknown. The degree of toxicity of benzyl alcohol depends on the amount of drug administered and the ability of the liver and kidneys to detoxify chemical compounds. Premature and low birth weight infants are at higher risk of toxicity. The amount of benzyl
alcohol per 1 ml of drug solution is 9 mg.
Clostridium difficile
associated diarrhea is observed with the use of almost all antibacterial drugs, including clindamycin, and manifests itself from mild forms of diarrhea to severe colitis with a fatal outcome. Antibacterial drugs suppress the normal intestinal flora, which can contribute to increased proliferation of clostridia. Clostridium difficile produces toxins A and B, leading to the development of Clostridium difficile associated diarrhea. Hypertoxin-producing strains of Clostridium difficile lead to increased morbidity and mortality because they may be resistant to antibiotic therapy and may require colonectomy for treatment. All cases of diarrhea in patients during antibiotic therapy should be considered suspicious for the development of Clostridium difficile associated diarrhea. A thorough medical history is required if Clostridium difficile associated diarrhea develops within 2 months after the prescription of antibacterial drugs. Pseudomembranous colitis is manifested by diarrhea, leukocytosis, fever, abdominal pain (sometimes accompanied by the discharge of blood and mucus in the stool) and can develop both while taking clindamycin and 2-3 weeks after stopping treatment. After a diagnosis of pseudomembranous colitis is made, in mild cases it is sufficient to discontinue treatment and use ion exchange resins (colestyramine, colestipol); in moderate and severe cases, replacement of the loss of fluid, electrolytes and protein, and the prescription of an antibacterial drug effective against Clostridium difficile are indicated, for example, vancomycin at a dose of 125-500 mg, or bacitracin at a dose of 25,000 units orally 4 times a day for 7-10 days, or metronidazole at a dose of 250-500 mg 3 times a day.
Drugs that reduce gastrointestinal motility should not be coadministered with clindamycin.
Clindamycin should be used with caution in patients with a history of gastrointestinal diseases, especially colitis. Antibiotic-associated colitis and diarrhea occur more frequently and more severely in debilitated and/or elderly patients.
When using all antibacterial agents, including clindamycin, excessive growth of microorganisms that are insensitive to this drug, especially yeast-like fungi, is possible. If superinfection develops, appropriate measures should be taken depending on the clinical situation.
Clindamycin should not be used to treat meningitis because it does not penetrate the blood-brain barrier well.
When using the drug in high doses, monitoring the concentration of clindamycin in the blood plasma is necessary. If treatment is carried out over a long period of time, liver and kidney function tests should be carried out regularly.
In patients with impaired liver and kidney function, no dose adjustment of the drug is required, since clindamycin practically does not accumulate in the body if the drug is administered at intervals of 8 hours. Patients with severe hepatic and/or renal insufficiency should use the drug with caution and monitor liver function (“ liver" enzymes) and kidneys.
The drug should not be administered intravenously undiluted or simultaneously.
The infusion must be carried out for at least 10-60 minutes (see section “Method of administration and dosage”).
Analogs
Level 4 ATC code matches:
Ecofucin
Primafungin
Nystatin
Polygynax Virgo
Polygynax
Analogs of Clindacin are represented by local medicinal drugs used in gynecology for the treatment of similar bacterial infections: Nystatin , Polygynax , Sintomycin , Pimafucin , Natamycin , Ecofucin .
The price of analogues of suppositories of this drug varies widely, for example, 10 suppositories of the drug Sintomycin can be bought for 40-60 rubles, and 12 vaginal capsules of Polygynax for 600-650 rubles.
During pregnancy and lactation
According to the official instructions, clinical studies of the safety of Clindacin during pregnancy in the first trimester have not been conducted, and therefore its use in this period is not recommended. Treatment of women with Clindacin in the second and third trimester of pregnancy is allowed only in cases where the benefits of such therapy for the mother significantly exceed the possible negative consequences for the fetus.
Despite this, in gynecology there is a practice of prescribing Clindacin in the second and third trimester of pregnancy , since some vaginal infections undoubtedly require such treatment. Considering reviews of this drug in the form of a cream, as well as reviews of suppositories during pregnancy during these periods, it is worth noting that in the vast majority of cases, therapy with Clindacin led to relief from the infectious disease without any negative consequences for the expectant mother and fetus.
The excretion of intravaginally used clindamycin in the milk of a nursing mother has not been studied, and therefore, its administration during lactation is possible only with a positive comparison of the benefits of such treatment for the mother in comparison with the possible risks for the newborn.
Indications for use of Clindacin
Clindacin is prescribed for bacterial vaginosis, manifested by the following symptoms:
- burning of the mucous membranes and labia minora;
- swelling of the tissues of the genital organ;
- copious discharge of yellow or green color, with a characteristic unpleasant odor;
- painful intercourse;
- itching in the groin.
Vaginosis can occur for several reasons. But, regardless of the etiology, the source of the problem is always the proliferation of pathogenic bacteria. Microorganisms can enter the mucous membrane in different ways. One of the most common is sexual contact with a carrier partner. Men may not have symptoms indicating the presence of pathogenic flora, but pathogenic bacteria will be present on the mucous membrane of the penis. One unprotected sexual intercourse is enough for a woman to receive an infectious dose.
In addition, the spread of bacteria is facilitated by the lack of proper hygiene, which consists of:
- daily washing of the genitals with running water;
- mandatory daily change of underwear, and in case of heavy discharge during the period of ovulation, it is recommended to wear daily thin pads, which are changed several times during the day as they are filled;
- timely change of absorbent products during menstruation.
Every woman should remember that both daily and monthly discharge are an excellent breeding ground for the proliferation of pathogenic bacteria. Therefore, it is extremely important to regularly change linen and personal hygiene products to minimize the risk of infection.
In addition, proper washing technique reduces the incidence of diseases. The water should always be running. But despite the need to keep the intimate area clean, doctors do not recommend using soap too often. If a soap solution is used, it should have an acidic pH level. Under no circumstances should you douche without the specific recommendation of your doctor. Daily washing with warm running water from front to back is sufficient. You can use soap once every two days.
Excessive use of cleansers leads to an imbalance of beneficial flora, which creates a natural barrier to the spread of infection. With frequent use of soap and as a result of douching, local immunity is noticeably reduced.
Reviews about Clindacin
Most women who use this drug to treat bacterial vaginosis leave positive reviews about Clindacin suppositories, including patients forced to resort to this drug during pregnancy in the second and third trimester . Reviews about Clindacin cream are not so numerous, but they are also positive in terms of the effectiveness and safety of this medicinal drug. Summarizing the general impression of patients about Clindacin therapy for bacterial vaginosis , we can confidently recommend it for use according to indications, but only after consulting a specialist doctor.
Clindacin price, where to buy
In comparison with its analogues for topical use (including vaginal ointments, creams, suppositories, capsules, etc.), the cost of Clindacin is at a high level. For example, the price of Clindacin in candles No. 3 is about 650 rubles (accordingly, 6 candles can be purchased on average for 1,300 rubles). The price of Clindacin cream varies between 350-400 rubles per 20 gram tube.
- Online pharmacies in RussiaRussia
ZdravCity
- Clindacin B Prolong cream vaginal.
2%+2% tube 20gAO Akrikhin RUR 538 order - Clindacin suppositories vaginal. 100 mg 3 pcs. Pharmaprim/Akrikhin
RUR 545 order
