Cleocin Phosphate

CLEOCIN PHOSPHATE- clindamycin phosphate injection, solution
Medical Purchasing Solutions, LLC

To reduce the development of drug-resistant bacteria and maintain the effectiveness of CLEOCIN PHOSPHATE and other antibacterial drugs, CLEOCIN PHOSPHATE should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

Sterile Solution is for Intramuscular and Intravenous Use

CLEOCIN PHOSPHATE in the ADD-Vantage ® Vial is For Intravenous Use Only

WARNING

Clostridioides difficile- associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including CLEOCIN PHOSPHATE and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.

Because CLEOCIN PHOSPHATE therapy has been associated with severe colitis which may end fatally, it should be reserved for serious infections where less toxic antimicrobial agents are inappropriate, as described in the INDICATIONS AND USAGE section. It should not be used in patients with nonbacterial infections such as most upper respiratory tract infections.

C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile , and surgical evaluation should be instituted as clinically indicated.

DESCRIPTION

CLEOCIN PHOSPHATE Sterile Solution in vials contains clindamycin phosphate, a water soluble ester of clindamycin and phosphoric acid. Each mL contains the equivalent of 150 mg clindamycin, 0.5 mg disodium edetate and 9.45 mg benzyl alcohol added as preservative in each mL. Clindamycin is a semisynthetic antibiotic produced by a 7(S)-chloro-substitution of the 7(R)-hydroxyl group of the parent compound lincomycin.

The chemical name of clindamycin phosphate is L- threo -α-D- galacto- Octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[[(1-methyl-4-propyl-2-pyrrolidinyl)carbonyl] amino]-1-thio-, 2-(dihydrogen phosphate), (2 S-trans)-.

The molecular formula is C 18 H 34 ClN 2 O 8 PS and the molecular weight is 504.96.

The structural formula is represented below:

Chemical Structure
(click image for full-size original)

CLEOCIN PHOSPHATE in the ADD-Vantage Vial is intended for intravenous use only after further dilution with appropriate volume of ADD-Vantage diluent base solution (see Directions for Use) .

CLEOCIN PHOSPHATE IV Solution in the GALAXY plastic container for intravenous use is composed of clindamycin phosphate equivalent to 300, 600 and 900 mg of clindamycin premixed with 5% dextrose as a sterile solution. Disodium edetate has been added at a concentration of 0.04 mg/mL. The pH has been adjusted with sodium hydroxide and/or hydrochloric acid.

The plastic container is fabricated from a specially designed multilayer plastic, PL 2501. Solutions in contact with the plastic container can leach out certain of its chemical components in very small amounts within the expiration period. The suitability of the plastic has been confirmed in tests in animals according to the USP biological tests for plastic containers, as well as by tissue culture toxicity studies.

CLINICAL PHARMACOLOGY

Distribution

Biologically inactive clindamycin phosphate is converted to active clindamycin. By the end of short-term intravenous infusion, peak serum concentrations of active clindamycin are reached.

After intramuscular injection of clindamycin phosphate, peak concentrations of active clindamycin are reached within 3 hours in adults and 1 hour in pediatric patients.

Serum concentrations of clindamycin can be maintained above the in vitro minimum inhibitory concentrations for most indicated organisms by administration of clindamycin phosphate every 8 to 12 hours in adults and every 6 to 8 hours in pediatric patients, or by continuous intravenous infusion. An equilibrium state is reached by the third dose.

No significant concentrations of clindamycin are attained in the cerebrospinal fluid even in the presence of inflamed meninges.

Metabolism

In vitro studies in human liver and intestinal microsomes indicated that clindamycin is predominantly metabolized by Cytochrome P450 3A4 (CYP3A4), with minor contribution from CYP3A5, to form clindamycin sulfoxide and a minor metabolite, N-desmethylclindamycin.

Excretion

Biologically inactive clindamycin phosphate disappears from the serum with 6 minutes of the average elimination half-life; however, the average serum elimination half-life of active clindamycin is about 3 hours in adults and 2½ hours in pediatric patients.

Specific Populations

Patients with Renal/Hepatic Impairment

The elimination half-life of clindamycin is increased slightly in patients with markedly reduced renal or hepatic function. Hemodialysis and peritoneal dialysis are not effective in removing clindamycin from the serum. Dosage schedules do not need to be modified in patients with renal or hepatic disease.

Geriatric Patients

Pharmacokinetic studies in elderly volunteers (61–79 years) and younger adults (18–39 years) indicate that age alone does not alter clindamycin pharmacokinetics (clearance, elimination half-life, volume of distribution, and area under the serum concentration-time curve) after IV administration of clindamycin phosphate. After oral administration of clindamycin hydrochloride, the average elimination half-life is increased to approximately 4.0 hours (range 3.4–5.1 h) in the elderly, compared to 3.2 hours (range 2.1–4.2 h) in younger adults. The extent of absorption, however, is not different between age groups and no dosage alteration is necessary for the elderly with normal hepatic function and normal (age-adjusted) renal function 1.

Pharmacokinetics in Pediatric Patients with PMA ≤32 weeks, or >32 to ≤40 weeks

Systemic clearance (CL) in premature infants increases with increases in body weight (kg) and post-menstrual age (PMA). The dosing regimens for pediatric patients ≤32 weeks PMA (5 mg/kg) and >32 to 40 weeks PMA (7 mg/kg), both administered intravenously every 8 hours, achieve exposures comparable to therapeutic exposures in adults (weighing 70 kg) administered clindamycin 600 mg every 8 hours (Table 1).

Table 1. Predicted Drug Exposure (Mean ± SD) of Clindamycin in Adults and in Pediatric Patients with PMA ≤32 weeks, or >32 to ≤40 weeks
Age Adult (70 kg) PMA ≤32 weeks PMA>32 – ≤40 weeks
PMA: post-menstrual age; AUC ss,0–8 hour : area under the concentration-time curve during a dosing interval at steady state; C max,ss : maximum drug concentration at steady state; C min,ss : minimum or trough drug concentration at steady state.

Dose (every 8 hours)

600 mg

5 mg/kg

7 mg/kg

AUC ss,0–8 hour (mcg∙h/mL)

50.5 (30.95)

52.5 (17.0)

55.9 (23.55)

C max,ss (mcg/mL)

12.0 (3.49)

9.0 (2.02)

10.5 (2.79)

C min,ss (mcg/mL)

3.1 (3.34)

4.6 (2.00)

4.4 (2.77)

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