Lincocin (Lincomycin HCl Monohydrate)

LINCOCIN®

Pharmacia & Upjohn

Lincomycin HCl Monohydrate

Antibiotic

Action And Clinical Pharmacology: The mode of action of lincomycin is the inhibition of protein synthesis by the inhibition of the binding of aminoacyl sRNA to the messenger ribosome complex at the 50S ribosomal unit.

Lincomycin is absorbed rapidly after oral administration, reaching peak levels in 2 to 4 hours. Levels above the minimum inhibitory concentration for most gram-positive organisms are maintained for 6 to 8 hours. I.M. administration of lincomycin produces peak serum levels in 30 minutes with detectable levels persisting for 24 hours after a 600 mg dose.

I.V. infusions of lincomycin over a 2 hour interval yield therapeutic levels for 14 hours.

Indications And Clinical Uses: The treatment of serious infections due to sensitive gram positive organisms (staphylococci, including penicillinase-producing staphylococci, streptococci and pneumococci) when the patient is intolerant of, or the organism resistant to other appropriate antibiotics.

Also indicated in the treatment of osteomyelitis, when the causative organism has been found to be sensitive to lincomycin.

Contra-Indications: In patients previously found to be hypersensitive to the drug or patients who have previously been found hypersensitive to clindamycin.

Until further clinical experience is obtained, lincomycin is not indicated in the newborn.

Manufacturers’ Warnings In Clinical States: Use of lincomycin has been associated with severe colitis which may be fatal. The major cause of this condition is a toxin produced by C. difficile. The condition manifests as a spectrum of symptoms from watery to severe diarrhea, fever, abdominal cramps and leukocytosis. This may be accompanied by the passage of blood and mucous which may result in peritonitis, shock and toxic megacolon if the drug is not discontinued and/or the condition treated.

Positive diagnosis can be made by performing an endoscopy, culture of the stool for C. difficile and performing a selective assay for the toxin(s) produced by C. difficile.

Antibiotic associated colitis may occur 2 to 3 weeks after lincomycin administration and is more likely to be severe in elderly or debilitated patients.

Mild cases showing minimal mucosal changes may respond to drug discontinuance. More severe cases, including those showing ulceration or pseudomembrane formation, are treated with fluid, electrolyte and protein supplementation. The primary treatment for antibiotic associated colitis is vancomycin, 125 to 500 mg every 6 hours for 7 to 14 days. Where vancomycin is contraindicated, oral bacitracin 25 000 IU 4 times daily for 7 to 10 days may be used as an alternative. In critically ill patients, oral vancomycin 500 mg every 6 hours should be used.

Anticholinergics and antiperistaltic agents may worsen the condition. Other causes of colitis should be considered.

It should be noted that serious relapses have occurred up to 1 month after apparently successful treatment. A relatively prolonged period of continuing observation is therefore recommended.

Lincomycin should not be administered undiluted i.v. All i.v. doses should be given by infusion over a period of 30 to 120 minutes. Cases of cardiopulmonary arrest have been reported during the treatment of severe endocarditis when large i.v. doses (over 4 g) were given rapidly without dilution. These reactions do not occur when the drug is diluted as noted under Dosage.

This product contains benzyl alcohol. Benzyl alcohol has been reported to be associated with a fatal “Gasping Syndrome” in premature infants.

Precautions: General: Should be used with caution in those patients with a history of gastrointestinal disease, specifically colitis.

Lincomycin is not indicated for use in the treatment of meningitis as the levels within the cerebral spinal fluid do not reach an adequate concentration to combat this infection.

No serious renal or neurologic abnormalities have been reported to date. No ototoxicity has been demonstrated in any of a large number of patients treated with lincomycin.

Pregnancy: Limited experience with 322 women receiving lincomycin orally at a dosage of 500 mg 4 times/day for 7 days during pregnancy revealed no ill effect in the mother or the fetus. One hundred and ten of these patients were treated in the first trimester of pregnancy, 105 in the second trimester and 107 in the third trimester. All were suffering from cervicitis and/or vaginitis of bacterial origin in conjunction with their pregnancy. One hundred and twelve of the children, ages 6 1/2 to 7 1/2 years, from these patients have been examined and compared with a control group of 65 children born at the same time in the same hospital. Lincomycin treatment did not result in any drug related abnormalities (physical, dental or developmental) when compared with the control group.

Since safe conditions for the parenteral use of lincomycin in pregnancy have not been established, its use in such patients should involve careful consideration of expected benefits and possible risks.

Lactation: Lincomycin has been reported in breast milk at concentrations of 0.5 to 2.4 µg/mL.

Patients with Special Diseases and Conditions: The serum half-life of lincomycin is increased in those patients with impaired renal or hepatic function. Therefore, consideration should be given to reducing the frequency of administration in these patients.

Since adequate data are not yet available in patients with pre-existing endocrine or metabolic diseases, its use in such patients is not recommended at this time unless special clinical circumstances so indicate. Efficacy of lincomycin in the prophylactic treatment of rheumatic fever has not been established.

Drug Interactions: In vitro studies have shown antagonistic activity between lincomycin and erythromycin; therefore, these agents should not be used concurrently.

Because lincomycin has been shown to have neuromuscular blocking properties which may enhance the action of other neuromuscular blocking agents, it should be used with caution in patients receiving such agents.

Laboratory Tests: The use of antibiotics occasionally results in overgrowth of non-susceptible organisms – particularly yeasts. Should superinfections occur, appropriate measures should be taken. No direct relationship of the drug to liver disease has been established. However, it is recommended that all patients receiving treatment for longer than 1 or 2 weeks have liver function tests performed. If abnormal tests appear, the drug should be discontinued unless, in the opinion of the physician, the drug should be continued for the treatment of a serious infection.

During clinical studies of lincomycin in the therapy of infectious disease, a few cases of neutropenia and/or leukopenia were reported. No cases of irreversible toxicity to the hematopoietic system have been reported; however, it is recommended that blood counts be obtained early and repeated periodically during the course of lincomycin therapy.

Adverse Reactions: The following adverse reactions have been reported with the use of lincomycin:

Gastrointestinal: nausea, vomiting, abdominal distress and persistent diarrhea (see Warnings) and, with oral preparations, esophagitis.

Hematopoietic: neutropenia, leukopenia, agranulocytosis, and thrombocytopenic purpura have been reported. There have been rare reports of aplastic anemia and pancytopenia in which lincomycin could not be ruled out as the causative agent.

Hypersensitivity Reactions: Hypersensitivity reactions such as angioneurotic edema, serum sickness and anaphylaxis have been reported, some of these in patients sensitive to penicillin. Rare instances of erythema multiforme, some resembling Stevens-Johnson syndrome, have been associated with lincomycin administration.

Skin and Mucous Membranes: Pruritus, skin rashes, urticaria, vaginitis, and rare instances of exfoliative and vesiculobullous dermatitis have been reported.

Liver: Jaundice and abnormal liver function tests (particularly elevation of serum transaminase) have been observed during lincomycin therapy.

Cardiovascular: Instances of hypotension following parenteral administration have been reported, particularly after too rapid administration. Rare instances of cardiopulmonary arrest have been reported after too rapid i.v. administration (see Dosage).

Local Reactions: Local irritation, pain, induration, and sterile abscess formation have been seen with i.m. injection. Thrombophlebitis has been reported with i.v. injection. These reactions can be minimized by deep i.m. injection and avoidance of indwelling i.v. catheters.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: No cases of large overdosage have been reported. It would be expected however that should overdosage occur, gastrointestinal side effects, including abdominal pain, nausea, vomiting and diarrhea, might be seen.

Overdosage should be treated with simple gastric lavage. No specific antidote is known.

In B-hemolytic streptococcal infections, continue treatment for at least 10 days to diminish the likelihood of subsequent rheumatic fever or glomerulonephritis.

Reconstituted Solutions: Lincocin (600 mg/2 mL and 1 800 mg/6 mL) was found to be compatible with 500 mL of the following solutions for a period of 24 hours at room temperature: 5% Dextrose in Water, 5% Dextrose in Saline, 10% Dextrose in Water, 10% Dextrose in Saline, Invert sugar 10%, Polysal M with 5% dextrose, Ringer’s Solution, Sodium lactate 1/6 molar.

Compatibility was determined by a study which indicated no appreciable change in the pH of the resultant mixture and no loss of potency of the lincomycin when diluted as indicated above.

Availability And Storage: Capsules: Each No. 0, hard gelatin capsule with light blue, opaque body and dark blue, opaque cap branded with Lincocin 500 on both parts contains: lincomycin HCl monohydrate equivalent to lincomycin base 500 mg.
Sterile Solution: Each mL of sterile solution contains: lincomycin HCl monohydrate equivalent to lincomycin base 300 mg. Also contains benzyl alcohol. Vials of 2 and 10 mL.

LINCOCIN® Pharmacia & Upjohn Lincomycin HCl Monohydrate Antibiotic

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