Cleocin

CLEOCIN- clindamycin phosphate cream
Pharmacia and Upjohn Company LLC

FOR INTRAVAGINAL USE ONLY NOT FOR OPHTHALMIC, DERMAL, OR ORAL USE

DESCRIPTION

Clindamycin phosphate is a water soluble ester of the semi-synthetic antibiotic produced by a 7(S)-chloro-substitution of the 7(R)-hydroxyl group of the parent antibiotic lincomycin. The chemical name for clindamycin phosphate is methyl 7-chloro-6,7,8-trideoxy-6-(1-methyl-trans -4-propyl-L-2-pyrrolidinecarboxamido)-1-thio-L-threo -α–D-galacto -octopyranoside 2-(dihydrogen phosphate). It has a molecular weight of 504.96, and the molecular formula is C18 H34 ClN2 O8 PS. The structural formula is represented below:

Chemical Structure

CLEOCIN Vaginal Cream 2%, is a semi-solid, white cream, which contains 2% clindamycin phosphate, USP, at a concentration equivalent to 20 mg clindamycin per gram. The pH of the cream is between 3.0 and 6.0. The cream also contains benzyl alcohol, cetostearyl alcohol, mixed fatty acid esters, mineral oil, polysorbate 60, propylene glycol, purified water, sorbitan monostearate, and stearic acid.

Each applicatorful of 5 grams of vaginal cream contains approximately 100 mg of clindamycin phosphate.

CLINICAL PHARMACOLOGY

Mechanism of Action

Clindamycin is an antibacterial drug (See MICROBIOLOGY).

Pharmacokinetics

Following a once a day intravaginal dose of 100 mg of clindamycin phosphate vaginal cream 2%, administered to 6 healthy female volunteers for 7 days, approximately 5% (range 0.6% to 11%) of the administered dose was absorbed systemically. The peak serum clindamycin concentration observed on the first day averaged 18 ng/mL (range 4 to 47 ng/mL) and on day 7 it averaged 25 ng/mL (range 6 to 61 ng/mL). These peak concentrations were attained approximately 10 hours post-dosing (range 4–24 hours).

Following a once a day intravaginal dose of 100 mg of clindamycin phosphate vaginal cream 2%, administered for 7 consecutive days to 5 women with bacterial vaginosis, absorption was slower and less variable than that observed in healthy females. Approximately 5% (range 2% to 8%) of the dose was absorbed systemically. The peak serum clindamycin concentration observed on the first day averaged 13 ng/mL (range 6 to 34 ng/mL) and on day 7 it averaged 16 ng/mL (range 7 to 26 ng/mL). These peak concentrations were attained approximately 14 hours post-dosing (range 4–24 hours).

There was little or no systemic accumulation of clindamycin after repeated vaginal dosing of clindamycin phosphate vaginal cream 2%. The systemic half-life was 1.5 to 2.6 hours.

MICROBIOLOGY

Mechanism of Action

Clindamycin inhibits bacterial protein synthesis by binding to the 23S RNA of the 50S subunit of the ribosome. Clindamycin is predominantly bacteriostatic. Although clindamycin phosphate is inactive in vitro , rapid in vivo hydrolysis converts it to active clindamycin.

Resistance

Resistance to clindamycin is most often caused by modification of the target site on the ribosome, usually by chemical modification of RNA bases by point mutations in RNA or occasionally in proteins. Cross resistance has been demonstrated between lincosamides, macrolides and streptogramins B in some organisms. Cross resistance has been demonstrated between clindamycin and lincomycin.

Antibacterial Activity

Culture and sensitivity testing of bacteria are not routinely performed to establish the diagnosis of bacterial vaginosis (see INDICATIONS AND USAGE); standard methodology for the susceptibility testing of the potential bacterial pathogens, Gardnerella vaginalis , Mobiluncus spp., or Mycoplasma hominis , has not been defined.

The following in vitro data are available but their clinical significance is unknown. Clindamycin is active in vitro against most isolates of the following organisms reported to be associated with bacterial vaginosis:

  • Bacteroides spp.
  • Gardnerella vaginalis
  • Mobiluncus spp.
  • Mycoplasma hominis
  • Peptostreptococcus spp.

INDICATIONS AND USAGE

CLEOCIN Vaginal Cream 2%, is indicated in the treatment of bacterial vaginosis (formerly referred to as Haemophilus vaginitis, Gardnerella vaginitis, nonspecific vaginitis, Corynebacterium vaginitis, or anaerobic vaginosis). CLEOCIN Vaginal Cream 2%, can be used to treat non-pregnant women and pregnant women during the second and third trimester. (See CLINICAL STUDIES.)

NOTE: For purposes of this indication, a clinical diagnosis of bacterial vaginosis is usually defined by the presence of a homogeneous vaginal discharge that (a) has a pH of greater than 4.5, (b) emits a “fishy” amine odor when mixed with a 10% KOH solution, and (c) contains clue cells on microscopic examination. Gram’s stain results consistent with a diagnosis of bacterial vaginosis include (a) markedly reduced or absent Lactobacillus morphology, (b) predominance of Gardnerella morphotype, and (c) absent or few white blood cells.

Other pathogens commonly associated with vulvovaginitis, eg, Trichomonas vaginalis, Chlamydia trachomatis, N. gonorrhoeae, Candida albicans , and Herpes simplex virus should be ruled out.

CONTRAINDICATIONS

CLEOCIN Vaginal Cream 2%, is contraindicated in individuals with a history of hypersensitivity to clindamycin, lincomycin, or any of the components of this vaginal cream. CLEOCIN Vaginal Cream 2%, is also contraindicated in individuals with a history of regional enteritis, ulcerative colitis, or a history of “antibiotic-associated” colitis.

WARNINGS

Pseudomembranous colitis has been reported with nearly all antibacterial agents, including clindamycin, and may range in severity from mild to life-threatening. Orally and parenterally administered clindamycin has been associated with severe colitis which may end fatally. Diarrhea, bloody diarrhea, and colitis (including pseudomembranous colitis) have been reported with the use of orally and parenterally administered clindamycin, as well as with topical (dermal and vaginal) formulations of clindamycin. Therefore, it is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of clindamycin, even when administered by the vaginal route, because approximately 5% of the clindamycin dose is systemically absorbed from the vagina.

Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of clostridia.Studies indicate that a toxin produced by Clostridium difficile is a primary cause of “antibiotic-associated” colitis.

After the diagnosis of pseudomembranous colitis has been established, therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to discontinuation of the drug alone. In moderate to severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation, and treatment with an antibacterial drug clinically effective against Clostridium difficile colitis.

Onset of pseudomembranous colitis symptoms may occur during or after antimicrobial treatment.

PRECAUTIONS

General

CLEOCIN Vaginal Cream 2%, contains ingredients that will cause burning and irritation of the eye. In the event of accidental contact with the eye, rinse the eye with copious amounts of cool tap water.

The use of CLEOCIN Vaginal Cream 2% may result in the overgrowth of nonsusceptible organisms in the vagina. In clinical studies involving 600 non-pregnant women who received treatment for 3 days, Candida albicans was detected, either symptomatically or by culture, in 8.8% of patients. In 9% of the patients, vaginitis was recorded. Inclinical studies involving 1325 non-pregnant women who received treatment for 7 days, Candida albicans was detected, either symptomatically or by culture, in 10.5% of patients. Vaginitis was recorded in 10.7% of the patients. In 180 pregnant women who received treatment for 7 days, Candida albicans was detected, either symptomatically or by culture, in 13.3% of patients. In 7.2% of the patients, vaginitis was recorded. Candida albicans , as reported here, includes the terms: vaginal moniliasis and moniliasis (body as a whole). Vaginitis includes the terms: vulvovaginal disorder, vulvovaginitis, vaginal discharge, trichomonal vaginitis, and vaginitis.

Information for the Patient

The patient should be instructed not to engage in vaginal intercourse, or use other vaginal products (such as tampons or douches) during treatment with this product.

The patient should also be advised that this cream contains mineral oil that may weaken latex or rubber products such as condoms or vaginal contraceptive diaphragms. Therefore, use of such products within 72 hours following treatment with CLEOCIN Vaginal Cream 2%, is not recommended.

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