Pharmacological properties
Pharmacodynamics. Clindamycin is an antimicrobial preparation that is effective in treating infections caused by susceptible anaerobic bacteria or susceptible strains of gram-positive aerobic bacteria. it has been shown that it exhibits antimicrobial activity in vitro against such microorganisms associated with the development of bacterial vaginosis: gardnerella vaginalis; mobiluncus spp .; bacteroides spp.; mycoplasmahominis; peptostreptococcus spp.
Pharmacokinetics. After application of 100 mg of clindamycin phosphate in the form of vaginal cream 2% in 6 healthy female volunteers for 7 days with a frequency of 1 time per day, systemic absorption of the active substance averaged 4% of the dose (range 0.6–11%). Cmax of clindamycin in blood plasma on day 1 averaged 18 ng / ml (range 4–47 ng / ml), and on day 7 averaged 25 ng / ml (range 6–61 ng / ml). These peak concentrations were recorded approximately 10 hours (range 4-24 hours) after preparation administration.
After the application of 100 mg of clindamycin phosphate in the form of vaginal cream 2% in 5 patients with bacterial vaginosis for 7 consecutive days with a frequency of 1 time per day, absorption was slower, and the variability was less compared to similar parameters for healthy women. Systemic absorption reached about 4% (range 2–8%) of the dose. Cmax of clindamycin in blood plasma on day 1 averaged 13 ng / ml (range 6–34 ng / ml), and on day 7 averaged 16 ng / ml (range 7–26 ng / ml). These peak concentrations were recorded approximately 14 hours (range 4-24 hours) after preparation administration.
Repeated (within 7 days) vaginal application of clindamycin phosphate in the form of vaginal cream 2% was not accompanied by systemic accumulation of clindamycin (or such accumulation occurred in very small amounts). Systemic T1 / 2 was 1.5-2.6 hours.
Indications
Treatment for bacterial vaginosis.
Application
Apply 1 full applicator (about 5 g) intravaginally at bedtime for 7 consecutive days.
It has been shown that in patients who are recommended a shorter course of treatment, a 3-day treatment regimen is effective.
Contraindications
Hypersensitivity to clindamycin or any of the components of the cream base. although cross-sensitization to lincomycin has not been demonstrated, dalacin cream is not recommended for use in patients with hypersensitivity to lincomycin. cream dalacin 2% is also contraindicated in persons with a history of inflammatory bowel disease or colitis associated with the use of antibiotics.
Side effects
In clinical studies, adverse reactions that were considered possibly, probably, or exactly related to intravaginal use of clindamycin phosphate cream were detected in 24% of patients. these reactions are shown below.
From the genital organs: cervicitis / vaginitis (14%); irritation of the vulva and vagina (6%).
From the side of the central nervous system: dizziness, headache, vertigo.
From the gastrointestinal tract: heartburn, nausea, vomiting, diarrhea, constipation, abdominal pain.
Dermatological reactions: rash, exanthema.
Hypersensitivity reactions: urticaria.
(Reactions for which no percentage frequency is reported occurred in less than 1% of patients.)
Also, in the course of clinical studies, the following side effects associated with the use of the preparation were identified (observed in less than 10% of patients):
urogenital - vaginal candidiasis, vulvovaginitis, vaginitis caused by Trichomonas vaginalis, vaginitis / vaginal infection, menstrual irregularities, vaginal pain, metrorrhagia, dysuria, vaginal discharge, urinary tract infections, abnormal childbirth, endometriosis, glucosuria and proteinuria;
the body as a whole - systemic candidiasis, fungal infections, generalized abdominal pain, localized abdominal pain, spastic abdominal pain, headache, pelvic pain, bacterial infections, upper respiratory tract infections, pain throughout the body, back pain, deviations in microbiological tests, allergic reactions;
Gastrointestinal tract - bad breath, diarrhea, nausea, vomiting, constipation, dyspepsia, heartburn, flatulence;
dermatological - itching (not at the injection site), rash, maculopapular rash, erythema, itching (at the injection site), skin candidiasis, urticaria;
Central nervous system - dizziness, headache;
endocrine - hyperthyroidism;
respiratory - nosebleeds;
sense organs - a change in taste.
Suspected Adverse Reactions Report. It is important to be reported on suspected adverse reactions reported after a preparation has been approved. This allows you to continue monitoring the balance of benefits and risks associated with the use of the preparation. Healthcare professionals are asked to report any suspected adverse reactions.
Special instructions
The use of clindamycin can lead to increased growth of resistant microorganisms, in particular yeast.
The use of almost all antibiotics is associated with the occurrence of diarrhea, and in some cases, pseudomembranous colitis. Thus, despite the fact that only a minimal amount of the preparation is absorbed, if severe diarrhea occurs, the preparation should be discontinued and, if necessary, appropriate diagnostic and therapeutic measures should be applied.
Dalacin cream contains carbohydrate-based components. Some of these components have been shown to weaken the rubber material of condoms and contraceptive diaphragms and reduce their effectiveness as a barrier method of contraception or protection against sexually transmitted diseases, including AIDS. During treatment with Dalacin cream, condoms and contraceptive diaphragms should not be used as a means of contraception or protection against diseases.
Use during pregnancy and lactation
Pregnancy period. Adequate and properly controlled studies with the participation of women in the first trimester of pregnancy have not been carried out, therefore, the preparation can be used in the first trimester of pregnancy only when essential. In clinical studies with the participation of pregnant women in the second trimester of pregnancy, Dalacin cream was effective in the treatment of bacterial vaginosis and its use was not associated with the occurrence of any negative effects in newborns. However, as before using any other preparation during pregnancy, before prescribing Dalacin cream, it is necessary to carefully weigh the balance of benefits and risks.
Breastfeeding period. It is not known whether clindamycin is excreted in breast milk after intravaginal administration of clindamycin phosphate. However, it has been reported about the penetration of clindamycin into breast milk after oral and parenteral administration, so it is recommended to stop breastfeeding if the preparation is used.
Children. Dalatsin cream is not recommended for use in children under the age of 12 years.
The ability to influence the reaction rate when driving or operating machinery. No data available.
Interactions
It has been shown that with the simultaneous use of clindamycin with lincomycin, as well as erythromycin with clindamycin, cross-resistance develops. antagonism between clindamycin and erythromycin has been demonstrated in vitro.
It has been shown that clindamycin has the property of blocking neuromuscular transmission and can enhance the action of other neuromuscular blockers. Therefore, it is necessary to use clindamycin with caution in patients taking these blockers.
There is no information regarding the simultaneous use with other intravaginal preparations, therefore such use is not recommended.
Patients who received clindamycin in combination with a vitamin K antagonist (eg, warfarin, acenocoumarol and fluindione) experienced an increase in coagulation test values (prothrombin time / international normalized ratio) and / or duration of bleeding. Thus, patients receiving treatment with vitamin K antagonists should frequently monitor the results of coagulation tests.
Overdose
Clindamycin phosphate vaginal cream (2%), when used intravaginally, can be absorbed in quantities sufficient to cause systemic effects. symptomatic treatment.
Storage conditions
At a temperature not exceeding 25 ° C, out of the reach of children. do not freeze!