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Lincomycin



Lincomycin
Systematic (IUPAC) name
 ?
Identifiers
CAS number 154-21-2
ATC code J01FF02
PubChem 9063
Chemical data
Formula C18H34N2O6S 
Mol. mass 406.538 g/mol
Pharmacokinetic data
Bioavailability 100% (IM or IV)
Metabolism  ?
Half life 5.4 ± 1.0 hours after IM or IV administration
Excretion renal and biliary
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

-only(US)

Routes IM/IV

Lincomycin is a lincosamide antibiotic that comes from the actinomyces Streptomyces lincolnensis. It has been structurally modified to its more commonly known 7-chloro-7-deoxy derivative, clindamycin.

Additional recommended knowledge

Contents

Uses

Although similar in structure, antibacterial spectrum, and in mechanism of action to macrolides they are also effective against other species as well i.e. actinomycetes, mycoplasma, and some species of Plasmodium.

However, because of its adverse effects and toxicity, it is rarely used today and reserved for patients who are either allergic to penicillin or where bacteria has developed resistance.

Clinical Pharmacology

Intramuscular administration of a single dose of 600 mg of Lincomycin produces average peak serum levels of 11.6 micrograms/ml at 60 minutes, and maintains therapeutic levels for 17 to 20 hours, for most susceptable gram-positive organisms. Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 17.3 percent).

A two hour Intravenous infusion of 600 mg of Lincomycin achieves average peak serum levels of 15.9 micrograms/ml and yields therapeutic levels for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9 to 30.3 percent (mean: 13.8 percent).

The biological half-life after IM or IV administration is 5.4 ± 1.0 hours. The serum half-life of lincomycin may be prolonged in patients with severe imparement of renal function, compared to patients with normal renal function. In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function. Hemodialysis and peritoneal dialysis are not effective in removing lincomycin from the serum.

Tissue level studies indicate that bile is an important route of excretion. Significant levels have been demonstrated in the majority of body tissues. Although lincomycin appears to diffuse in the cerebrospinal fluid (CSF), levels of lincomycin in the CSF appear inadequate for the treatment of meningitis.

How Supplied

Lincomycin, as the brand name Lincocin, is available in the following strengths and package sizes:

300mg/ml

2 ml vials and 10 ml vials

Each ml of Lincocin contains 300mg of lincomycin

Dosage and Administration

Adults

Serious infections - 600 mg (2 ml) IM every 24 hours. More severe infections - 600mg (2 ml) every 12 hours. The IV dose will be determined by the seriousness of the infection. For serious infections, doses of 600 mg to 1000 mg are given every 8 to 12 hours. Fore more severe infections, these doses may have to be increased. In life-threatening situations, daily IV administration of as much as 8000 mg have been given.

Pediatric Patients

Pediatric patients over one month of age: Serious infections - one IM injection of 10mg/kg every 24 hours. More severe infections - one IM injection of 10 mg/kg every 12 hours, or more often as indicated by susceptability testing, renal and hepatic functioning. IV dosing is 10 to 20 mg/kg/day in divided doses every 8 to 12 hours.

Subconjunctival injections

An injection of 0.75 mg, given subconjuctivally, will result in ocular fluid levels of antibiotic (lasting for at least 5 hours) with Minimum Inhibitory Concentrations sufficient for most susceptible pathogens.

Patients with diminished renal function

When therapy with lincomycin is required in individuals with severe impairment of renal function, an appropriate dose is 25 to 30 percent of that recommended for patients with normally functioning kidneys.


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Lincomycin". A list of authors is available in Wikipedia.
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