Pharmacia & Upjohn
brand of lincomycin hydrochloride tablets
brand of lincomycin hydrochloride injection,
USP
For Use in Animals Only
For intramuscular, intravenous, and oral use
in dogs and cats.
DESCRIPTION
LINCOCIN products contain lincomycin hydrochloride, an
antibiotic produced by Streptomyces lincolnensis var.
lincolnensis, which is chemically distinct from all other clinically
available antibiotics and is isolated as a white crystalline solid. It is
stable in the dry state and in aqueous solution for at least 24 months.
Lincomycin hydrochloride is readily soluble in water at room temperature in
concentrations up to 500 mg/mL. Physical stability of aqueous solutions can
be maintained at drug concentrations up to 345 mg/mL at temperatures as low
as 4°C. The solubility in 95 percent ethanol is 80 mg/mL.
LINCOCIN products have been shown to be effective against
most of the common gram-positive pathogens. Depending on the sensitivity of
the organism and concentration of the antibiotic, it may be either
bactericidal or bacteriostatic. It has not shown cross resistance with other
available antibiotics. Microorganisms have not developed resistance to
LINCOCIN rapidly when tested by in vitro or
in vivo methods.
ACTIONS
Animal Toxicology-The acute LD50
intraperitoneally in mice is 1000 mg/kg and orally in rats is 15,645 mg/kg.
LINCOCIN was well tolerated orally in rats and dogs at doses up to 300
mg/kg/day for periods up to one year. Parenteral dosages of up to 60
mg/kg/day for 30 days subcutaneously in the rat and intramuscularly in the
dog produced no significant systemic effects or pathological findings at
necropsy.
LINCOCIN at a daily dose level of 75 mg/kg subcutaneously
was injected into mature male and female rats during a pre-breeding period
of 60 days and throughout two mating cycles (84 days). No evidence was
obtained that LINCOCIN exerted any effects on breeding performance and no
drug-induced anomalies were discovered in the young. Similarly no evidence
was obtained that LINCOCIN, when given in sustained parenteral dosage of 50
mg/kg daily to pregnant bitches, produced a teratogenic effect on the canine
embryo.
The subcutaneous LD50 value in
the newborn rat was determined to be 783 mg/kg. Newborn rats and canine pups
have tolerated multiple doses of 30-90 mg/kg/day of the drug without
evidence of ill effects.
Biological Studies-In
vitro studies indicate that the spectrum of activity includes
Staphylococcus aureus, Staphylococcus albus, ß-hemolytic
Streptococcus, Streptococcus viridans, Clostridium tetani, Erysipelothrix
insidiosa, Mycoplasma spp., and Clostridium
perfringens. The drug is not active against gram-negative organisms or
yeasts.
In vivo experimental animal studies
demonstrated the effectiveness of LINCOCIN in protecting animals infected
with Streptococcus viridans, ß-hemolytic Streptococcus,
Staphylococcus aureus, Erysipelothrix insidiosa, Mycoplasma spp., and
Leptospira pomona. It was ineffective in
Klebsiella, Pasteurella, Pseudomonas, and
Salmonella infections.
Cross resistance has not been demonstrated with penicillin,
erythromycin, triacetyloleandomycin, chloramphenicol, novobiocin,
streptomycin, or the tetracyclines. Staphylococci develop resistance to
LINCOCIN in a slow, stepwise manner based on in vitro,
serial subculture experiments. This pattern of resistance development is
unlike that shown for streptomycin.
Clinical Absorption and Excretion-Administered
intramuscularly, LINCOCIN Sterile Solution is very rapidly absorbed. In
studies with dogs, peak serum levels were reached in from ten minutes to two
hours with detectable levels for 16 to 24 hours. The concentration of
LINCOCIN in the blood serum varies with the dose administered and with the
individual animal. Levels are maintained above the in
vitro minimum inhibitory concentration for most gram-positive organisms
for six to eight hours following a therapeutic dose. Intravenous
administration also provides very rapid absorption, but should be
administered with normal saline or 5% glucose as an intravenous drip
infusion.
Administered orally to dogs, LINCOCIN was also rapidly
absorbed with serum levels present within one-half hour; peak values were
reached at two to four hours; and detectable levels persisted for 16 to 24
hours.
Tissue level studies indicate that bile is an important
route of excretion. Significant levels of LINCOCIN have been demonstrated in
the majority of body tissues. After a single oral administration of LINCOCIN
to a dog, fecal excretion amounted to 77 percent of the dose; urinary
excretion to 14 percent. After a single intramuscular injection, fecal
excretion equaled 38 percent of the dose; and urinary excretion, 49 percent.
Urinary excretion was essentially complete in less than 24 hours and fecal
excretion by 48 hours after either route of administration. LINCOCIN has
also been shown to be excreted in the milk of lactating cows, goats, rats,
and women.
INDICATIONS
LINCOCIN products are indicated in infections caused by
gram-positive organisms which are sensitive to its action, particularly
streptococci and staphylococci. The drug has proven effective in eradicating
causative organisms in most of the common upper respiratory tract
infections, in septicemia, and in infections of the skin and adjoining
tissues.
Systemic therapy with LINCOCIN has been shown to be of
benefit in many animals with pustular dermatitis. As with all antibiotics,
in vitro sensitivity studies should be performed
before LINCOCIN is utilized as sole antibiotic therapy.
LINCOCIN has been demonstrated to be effective in the
treatment of staphylococcal infections resistant to other antibiotics and
sensitive to lincomycin. The drug may be administered in combination therapy
with other antimicrobial agents when indicated.
No serious hypersensitivity reactions have been reported and
many animals have received LINCOCIN repeatedly without developing evidence
of hypersensitivity.
In dogs, LINCOCIN has demonstrated
excellent efficacy in the treatment of upper respiratory infections and of
skin diseases, particularly those caused by staphylococcus and streptococcus
organisms. LINCOCIN has demonstrated efficacy even in some chronic
conditions of long standing and in infections which have resisted treatment
with other antibacterial agents.
Infections successfully treated with LINCOCIN include
pustular dermatitis, abscesses, infected wounds (including bite and fight
wounds), tonsillitis, laryngitis, metritis, and secondary bacterial
infections associated with the canine distemper-hepatitis complex.
In cats, LINCOCIN has demonstrated
efficacy in the treatment of localized infections, such as abscesses
following fight wounds, pneumonitis, and feline rhinotracheitis.
Success in the treatment of viral diseases must be
attributed to the control of susceptible secondary bacterial invaders rather
than to any effect of LINCOCIN on the virus.
CONTRAINDICATIONS
As with all drugs, the use of LINCOCIN products is
contraindicated in animals previously found to be hypersensitive to the
drug.
LINCOCIN should not be given to animals with known
preexisting monilial infections.
The following species are sensitive to the gastrointestinal
effects of lincomycin: rabbits, hamsters, guinea pigs and horses. Therefore,
the administration of LINCOCIN should be avoided in these species.
WARNING - Not for human use.
PRECAUTIONS
The use of antibiotics occasionally results in overgrowth of
nonsusceptible organisms - particularly yeasts. Should superinfections
occur, appropriate measures should be taken.
ADVERSE REACTIONS
Loose stools occasionally have been observed in dogs and
cats on oral doses. Vomiting in cats has occasionally been reported
following oral administration.
Intramuscularly and intravenously, LINCOCIN products have
demonstrated excellent local tolerance with no reports of pain or
inflammation following injection.
DOSAGE AND ADMINISTRATION
Oral: 10 mg per pound of body weight
every 12 hours or 7 mg per pound every 8 hours.
Intramuscular: 10 mg per pound of body
weight once a day or 5 mg per pound every 12 hours.
Intravenous: 5 to 10 mg per pound of
body weight one or two times per day diluted with 5 percent glucose in water
or normal saline and given as a drip infusion.
Treatment with LINCOCIN products may be continued for
periods as long as 12 days if clinical judgment indicates.
As with any multi-dose vial, practice aseptic techniques in
withdrawing each dose. Adequately clean and disinfect the vial closure prior
to entry with a sterile needle and syringe.
HOW SUPPLIED
LINCOCIN products for veterinary use are available in the
following dosage forms and strengths:
Tablets
100 mg: Each scored tablet contains
lincomycin hydrochloride equivalent to lincomycin, 100 mg; supplied in
bottles of 500; NDC 0009-0595-05.
200 mg: Each scored tablet contains
lincomycin hydrochloride equivalent to lincomycin, 200 mg; supplied in
bottles of 250; NDC 0009-0596-02.
500 mg: Each scored tablet contains
lincomycin hydrochloride equivalent to lincomycin, 500 mg; supplied in
bottles of 100; NDC 0009-0475-01.
AQUADROPS®
Each mL containing lincomycin hydrochloride equivalent to
lincomycin, 50 mg; preserved with methylparaben 0.075%, propylparaben
0.025%, and sorbic acid 0.1%. Supplied in 20 mL bottles with graduated
dropper; NDC 0009-0570-01.
Sterile Solution
Each mL containing lincomycin hydrochloride equivalent to
lincomycin, 100 mg; also Benzyl Alcohol, 9.45 mg added as preservative.
Supplied in 20 mL vials.
Store at controlled room temperature 20° to
25° C (68° to 77° F) [see USP].
Caution: Federal (USA) law restricts
this drug to use by or on the order of a licensed veterinarian.