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Cleocin I.V.

Clinical Pharmacology
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CLINICAL PHARMACOLOGY

Biologically inactive clindamycin phosphate is rapidly converted to active clindamycin.

By the end of short-term intravenous infusion, peak serum levels of active clindamycin are reached. Biologically inactive clindamycin phosphate disappears rapidly from the serum; the average elimination half-life is 6 minutes; however, the serum elimination half-life of active clindamycin is about 3 hours in adults and 2 ½ hours in pediatric patients.

After intramuscular injection of clindamycin phosphate, peak levels of active clindamycin are reached within 3 hours in adults and 1 hour in pediatric patients. Serum level curves may be constructed from IV peak serum levels as given in Table 1 by application of elimination half-lives listed above.

Serum levels 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.

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 need not be modified in the presence of mild or moderate renal or hepatic disease.

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

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, 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 .

Serum assays for active clindamycin require an inhibitor to prevent in vitro hydrolysis of clindamycin phosphate.

 

Table 1. Average Peak and Trough Serum
Concentrations of Active Clindamycin
After Dosing With Clindamycin Phosphate
Dosage Regimen
Peak
mcg/mL
Trough
mcg/mL9
Healthy Adult Males (Post equilibrium)
  600 mg IV in 30 min q6h
10.9 2.0
  600 mg IV in 30 min q8h
10.8 1.1
  900 mg IV in 30 min q8h
14.1 1.7
  600 mg IM q12h *
9  
Pediatric Patients (first dose) *
  5-7 mg/kg IV in 1 hour
10  
  5-7 mg/kg IM
8  
  3-5 mg/kg IM
4  
* Data in this group from patients being treated for infection.

Brand Name: Cleocin I.V.
Generic Name: Clindamycin

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