Clindacin B prolong, vaginal cream 2%+2% 20 g

Pharmacotherapeutic group: Antimicrobial and antifungal agent.

Pharmacological action

Pharmacodynamics

Butoconazole – Imidazole derivative, has fungicidal activity against Candida fungi, Trichophyton, Microsporum, Epidermaphyton and some Gram-positive bacteria. It is most effective against candidiasis. By blocking in the cell membrane formation of ergosterol from lanosterol it increases membrane permeability, which leads to lysis of the fungus cell.

Clindamycin is a bacteriostatic antibiotic of the lincosamide group, it has a broad spectrum of action, binds to 50S subunit of ribosomal membrane and inhibits protein synthesis in a microbial cell. Bactericidal action is possible against a number of Gram-positive cocci. Under in vitro conditions the following microorganisms causing bacterial vaginosis are sensitive to clindamycin: Gardnerella vaginalis, Mobiluncus spp., Mycoplasma hominis, Bacteroides spp., Peptostreptococcus spp.

The hydrophilic cream base provides a gel-like consistency of the drug at 35-40 ° C. The cream does not melt when applied intravaginally, which ensures that the active substances remain on the vaginal mucosa for 1-3 days. There is a cross-resistance between clindamycin and lincomycin.

Pharmacokinetics

Butoconazole

In intravaginal administration, approximately 1.7% of the administered dose of butoconazole. Cmax in plasma butoconazole is reached after 13 hours and is 2-18.6 ng/ml. Butoconazole is extensively metabolized, partially excreted by the kidneys and intestine.

Clindamycin

absorption

. After use of clindamycin intravaginally at a dose of 100 mg/day once (as 2% clindamycin phosphate cream) for 7 days, the Cmax of clindamycin in plasma is reached after 10 h (4-24 h) and averages 18 ng/mL (4-47 ng/mL) on day 1 and 25 ng/mL (6-61 ng/mL) on day 7, with systemic absorption of about 4% (06-11%) of the administered dose.

In women with bacterial vaginosis, approximately 4% of clindamycin undergoes systemic absorption (with a smaller variation of 2-8%) with a similar dosing regimen, Cmax is reached 14 h (4-24 h) after administration and
averages 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 are less pronounced with intravaginal administration than with oral or IV administration.

Evolution

The T1/2 is 1.5-2.6 h. Clindamycin almost does not cumulate after repeated intravaginal administration.

Pharmacokinetics in Special Patient Groups

Not enough patients aged 65 years or older have participated in clinical trials of clindamycin 2% vaginal cream to allow assessment of the difference in clinical response to therapy between this age group and younger patients. In the available reports from clinical experience, no difference in response between older and younger patients was observed.

Indications

Active ingredient

Composition

Vaginal cream from almost white to white with a grayish tint, with a specific smell.

Associates: Preservative Euxyl PE 9010 (phenoxyethanol 90%, ethylhexylglycerol 10%) – 0.5 g, which is equivalent to 0.45 g of phenoxyethanol, propylene glycol – 5 g, isopropyl myristate – 8 g, macrogoal cetostearate (macrogoal-20 cetostearyl ether) – 2 g, cetostearyl alcohol (cetyl alcohol 60%, stearyl alcohol 40%) – 6 g, hydroxypropyl diacrystalline phosphate – 8 g, sodium hydroxide – 0.26 g, purified water – up to 100 g.

How to take, the dosage

Interaction

Special Instructions

Contraindications

With caution:allergic diseases, concomitant use of muscle relaxants.

Side effects

Overdose