Lincomycin
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Lincomycin
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | J01 |
| PubChem | |
| 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 | |
| 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.
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[edit] 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.
[edit] 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 susceptible 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 impairment 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.
[edit] 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
[edit] 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.
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