Dalacin, vaginal cream 2% 20 g

Pharmacotherapeutic group: antibiotic – lincosamide.

ATX code: G01AA10.

Pharmacological properties

Pharmacodynamics

Clindamycin phosphate is inactive in vitro but is rapidly hydrolyzed in vivo to form clindamycin, which has antibacterial activity. Clindamycin belongs to the group of antibiotics-linkosamides, which inhibits protein synthesis in the microbial cell through interaction with the 50S ribosome subunit and affects the translation process.

Clindamycin, like most protein synthesis inhibitors, is primarily a bacteriostatic whose effectiveness is related to the duration of maintenance of the concentration of the active substance at a higher level than the MAC (Minimum Inhibitory Concentration) of the infecting organism.

Resistance to clindamycin is in most cases due to modification of ribosomal target sites usually through chemical modification of RNA nitrogen bases or point mutations of RNA or sometimes protein mutations. Under in vitro conditions, cross-resistance between lincosamides, macrolides, and Streptogramine B has been demonstrated in some organisms. There is a cross-resistance between clindamycin and lincomycin.Under in vitro conditions, the following microorganisms causing bacterial vaginosis are sensitive to clindamycin: Gardnerella vaginalis, Mobiluncus spp., Mycoplasma hominis, Bacteroides spp., Peptostreptococcus spp.Bacterial culture and sensitivity studies are not usually performed to establish the diagnosis and guide treatment for bacterial vaginosis. There is no standard methodology for evaluating the sensitivity of potential bacterial vaginosis pathogens (Gardnerella vaginalis, Mobiluncus spp.) Methods for determining the sensitivity of Bacteroides spp and Gram-positive anaerobic cocci, also Mycoplasma spp. described by the Clinical and Laboratory Standards Institute (CLSI), and borderline sensitivity values for clindamycin for Gram-negative and Gram-positive anaerobic bacteria are published by the European Committee on Antimicrobial Susceptibility Testing (EUCAST). For clinical isolates that are sensitive to clindamycin but resistant to erythromycin, clindamycin resistance should also be tested using the D-test. However, borderline values are intended to guide systemic antibiotic treatment rather than local treatment.

Pharmacokinetics

. After administration of clindamycin intravaginally at a dose of 100 mg/day once (as 2% clindamycin phosphate cream) for 7 days, serum concentrations peak about 10 h (4-24 h) after administration and average 18 ng/mL (4-47 ng/mL) on day one and 25 ng/mL (6-61 ng/mL) on day 7, with systemic absorption of about 4% (0.6-11%) of the administered dose.

In women with bacterial vaginosis, about 4% of clindamycin is absorbed with a similar dosing regimen (with a smaller variation of 2-8%), with serum concentrations peaking about 14 h (4-24 h) after administration and averaging 13 ng/mL (6-34 ng/mL) on day 1 and 16 ng/mL (7-26 ng/mL) on day 7.

The systemic effects of clindamycin when administered intravaginally are weaker than when administered orally or intravenously. After intravaginal administration of repeated doses, clindamycin almost does not accumulate in the blood. The systemic half-life is 1.5-2.6 h.

Application in older patients

In clinical trials of clindamycin 2% vaginal cream, not enough patients 65 years of age or older have participated to be able to evaluate the difference in clinical response to therapy between this age group and younger patients. In the available reports from clinical experience, there was no difference in response between older patients and younger patients.

Indications

Active ingredient

Composition

How to take, the dosage

Recommended dose: Intravaginally one full applicator (5 g cream, approximately 100 mg clindamycin) preferably before bedtime for 3 or 7 consecutive days.

Terms for Use

The 20 g package of cream contains 3 plastic applicators and the 40 g package contains 7 applicators for proper insertion of the cream into the vagina.

Interaction

Special Instructions

Before prescribing the drug, appropriate laboratory methods must rule out Trichomonas vaginalis, Chlamydia trachomatis, Neisseria gonorrhoeae, Candida albicans and Herpes simplex virus, often causing vulvovaginitis.

Intravaginal use of clindamycin can lead to increased growth of insensitive microorganisms, especially yeast-like fungi.

The use of clindamycin (like almost all antibiotics) orally or parenterally is associated with the development of severe diarrhea and in some cases pseudomembranous colitis. If severe or prolonged diarrhea develops, the drug should be discontinued and appropriate diagnostic and treatment measures should be taken if necessary.

Patients should be warned not to have sexual intercourse or use other intravaginal devices (tampons, douches) during therapy with the drug.

The use of DALATIN cream during menstruation is not recommended. The start of therapy should be postponed until after menstruation.

The product contains ingredients that may reduce the strength of latex or rubber products, so the use of condoms, vaginal birth control diaphragms and other latex products for intravaginal use during therapy with the product and for 72 hours after use is not recommended.

Impact on driving and operating machinery

There is no reason to believe that the use of DALACIN Vaginal Cream may affect driving and operating machinery.

Synopsis

Contraindications

– hypersensitivity to clindamycin, lincomycin or any component of the drug;

– in patients with a history of antibiotic-associated colitis.

– Under 18 years of age (no safety, efficacy data available).

Side effects

The safety of clindamycin vaginal cream was evaluated in both non-pregnant patients and patients in the second and third trimesters of pregnancy.

System-organ class

Very

often

≥ 1/10

Often

From ≥1/100 to < 1/10

Infrequent

From ≥ 1/1000 to < 1/100

Rarely

≥ 1/10,000 to

< 1/1000

Very

Rarely

< 1/10,000

Frequency unknown

(impossible to estimate

based on available data)

Infectious and parasitic diseases

Fungal infections, infections caused by fungi of the genus Candida

Bacterial infections

Skin Candida

Immune system disorders

Hypersensitivity

Endocrine system disorders

Hyperthyroidism

Nervous system disorders

Headache, dizziness, dysgeusia

Hearing and vestibular disorders

Vertigo

Disorders of the respiratory system, thoracic and mediastinal organs

Infections of the upper respiratory tract

Nasal bleeding

Gastrointestinal tract disorders

Stomach pain, constipation, diarrhea, nausea, vomiting

Stomach bloating, flatulence, bad breath

Pseudomembranous colitis*, gastrointestinal distress, dyspepsia

Skin and subcutaneous tissue disorders

Skin itching, rash

Hives, erythema

Maculopapular rash

Muscle and connective tissue disorders

Back pain

Kidney and urinary tract disorders

Urinary tract infections, glucosuria, proteinuria

Dysuria

Pregnancy, postpartum and perinatal conditions

Anomalous birth

Genital and breast disorders

Vulvovaginal candidiasis

Vulvovaginitis, vulvovaginal disorders, menstrual irregularities, vulvovaginal pain, metrorrhagia, vaginal discharge

Trichomonad vulvovaginitis, vaginal infections, pelvic pain

Endometriosis

General disorders and reactions at the injection site

Inflammation, pain

Laboratory and instrumental findings

Deviation of microbiological test results from the norm

* adverse drug reactions detected in the post-registration period.

Overdose

Pregnancy use

Adequate controlled studies on the use of the drug in the first trimester of pregnancy have not been conducted; therefore, DALACIN vaginal cream may be administered to women in the first trimester of pregnancy only for absolute indications, i.e. when the potential benefit of the drug therapy for the mother exceeds the potential risk to the fetus.

In animal studies no adverse effects on the fetus were found when clindamycin was administered subcutaneously or orally, except in cases of administration of the drug in doses toxic to the mother.

When clindamycin was administered intravaginally in the second or third trimester of pregnancy, no increase in the incidence of fetal congenital abnormalities was observed. Abnormal births occurred in 1.1% of women compared to 0.5% in the placebo group if DALACIN vaginal cream was used in the second trimester for 7 days. Use of the drug in the second to third trimesters of pregnancy is possible if the potential benefit to the mother outweighs the risk to the fetus.

It is not known whether clindamycin is excreted into the breast milk after intravaginal administration. Clindamycin is detected in breast milk at a concentration of ˂0.5 to 3.8 μg/mL after systemic administration.

Clindamycin has the potential to have adverse effects on the gastrointestinal tract microflora in breastfed infants, such as diarrhea or blood in the feces, or a rash. If a nursing mother requires oral or intravenous use of clindamycin, this is not a reason to stop breastfeeding, but an alternative medication may be preferred. Consideration should be given to the developmental and health benefits of breastfeeding, the clinical necessity of maternal use of clindamycin, and any potential adverse effects associated with clindamycin or the mother’s underlying disease on the breastfed infant.

Similarities