Lincomycin Hydrochloride

Description

DESCRIPTION LINCOCIN (lincomycin injection, USP) is a sterile solution containing lincomycin hydrochloride which is the monohydrated salt of lincomycin, a lincosamide antibacterial produced by the growth of a member of the lincolnensis group of Streptomyces lincolnensis (Fam. Streptomycetaceae ). The chemical name for lincomycin hydrochloride is Methyl 6,8-dideoxy-6-(1-methyl-trans-4-propyl-L-2-pyrolidinecarboxamido)-1-thio-D-erythro-α-D-galacto-octopyranoside monohydrochloride monohydrate. The molecular formula of lincomycin hydrochloride is C 18 H 34 N 2 O 6 S.HCl.H 2 O and the molecular weight is 461.01. The structural formula is represented below: Lincomycin hydrochloride is a white or practically white, crystalline powder and is odorless or has a faint odor. Its solutions are acid and are dextrorotatory. Lincomycin hydrochloride is freely soluble in water; soluble in dimethylformamide and very slightly soluble in acetone. LINCOCIN contains lincomycin hydrochloride in a sterile, clear, colorless solution with benzyl alcohol used as a preservative 9.45 mg/mL, and water for injection. LINCOCIN is a sterile solution for intramuscular and intravenous use. LINCOCIN is supplied in 2 mL and 10 mL multiple-dose vials containing 300 mg/mL of lincomycin (equivalent to 340 mg/mL of lincomycin hydrochloride, USP). Chemical Structure

What Is Lincomycin Hydrochloride Used For?

INDICATIONS AND USAGE LINCOCIN is indicated in the treatment of serious infections due to susceptible strains of streptococci, pneumococci, and staphylococci. Its use should be reserved for penicillin-allergic patients or other patients for whom, in the judgment of the physician, a penicillin is inappropriate. Because of the risk of CDAD, as described in the BOXED WARNING , before selecting lincomycin the physician should consider the nature of the infection and the suitability of other alternatives. Indicated surgical procedures should be performed in conjunction with antibacterial therapy. LINCOCIN may be administered concomitantly with other antimicrobial agents when indicated. LINCOCIN is not indicated in the treatment of minor bacterial infections or viral infections. To reduce the development of drug-resistant bacteria and maintain the effectiveness of LINCOCIN and other antibacterial drugs, LINCOCIN should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

Dosage and Administration

DOSAGE AND ADMINISTRATION If significant diarrhea occurs during therapy, LINCOCIN should be discontinued. (see BOXED WARNING ) INTRAMUSCULAR Adults Serious infections —600 mg (2 mL) intramuscularly every 24 hours. More severe infections —600 mg (2 mL) intramuscularly every 12 hours or more often. Pediatric patients over 1 month of age Serious infections —one intramuscular injection of 10 mg/kg (5 mg/lb) every 24 hours. More severe infections —one intramuscular injection of 10 mg/kg (5 mg/lb) every 12 hours or more often. INTRAVENOUS Adults The intravenous dose will be determined by the severity of the infection. For serious infections doses of 600 mg of lincomycin (2 mL of LINCOCIN) to 1 gram are given every 8 to 12 hours. For more severe infections these doses may have to be increased. In life-threatening situations daily intravenous doses of as much as 8 grams have been given. Intravenous doses are given on the basis of 1 gram of lincomycin diluted in not less than 100 mL of appropriate solution (see PHYSICAL COMPATIBILITIES ) and infused over a period of not less than one hour. Dose Vol. Diluent Time 600 mg 100 mL 1 hr 1 gram 100 mL 1 hr 2 grams 200 mL 2 hr 3 grams 300 mL 3 hr 4 grams 400 mL 4 hr These doses may be repeated as often as required to the limit of the maximum recommended daily dose of 8 grams of lincomycin. Pediatric patients over 1 month of age 10 to 20 mg/kg/day (5 to 10 mg/lb/day) depending on the severity of the infection may be infused in divided doses as described above for adults. NOTE: Severe cardiopulmonary reactions have occurred when LINCOCIN has been given at greater than the recommended concentration and rate (see PRECAUTIONS ). SUBCONJUNCTIVAL INJECTION 0.25 mL (75 mg) injected subconjunctivally will result in ocular fluid concentrations of antibacterial (lasting for at least 5 hours) sufficient for most susceptible pathogens. Patients with Renal Impairment When therapy with LINCOCIN is required in individuals with severe renal impairment, an appropriate dose is 25 to 30% of that recommended for patients with normally functioning kidneys (see PRECAUTIONS ). Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Side Effects (Adverse Reactions)

ADVERSE REACTIONS The following adverse reactions have been reported with the use of lincomycin. Gastrointestinal disorders Diarrhea, nausea, vomiting, glossitis, stomatitis, abdominal pain, abdominal discomfort Event has been reported with intravenous injection. , anal pruritus Skin and subcutaneous tissue disorders Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, dermatitis bullous, dermatitis exfoliative, erythema multiforme (see WARNINGS ), rash, urticaria, pruritus Infections and infestations Vaginal infection, pseudomembranous colitis, Clostridioides difficile colitis (see WARNINGS ) Blood and lymphatic system disorders Pancytopenia, agranulocytosis, aplastic anemia, leukopenia, neutropenia, thrombocytopenic purpura Immune system disorders Anaphylactic reaction (see WARNINGS ), angioedema, serum sickness Hepatobiliary disorders Jaundice, liver function test abnormal, transaminases increased Renal and urinary disorders Renal impairment, oliguria, proteinuria, azotemia Cardiac disorders Cardio-respiratory arrest (see DOSAGE AND ADMINISTRATION ) Vascular disorders Hypotension (see DOSAGE AND ADMINISTRATION ), thrombophlebitis Ear and labyrinth disorders Vertigo, tinnitus Neurologic disorders Headache, dizziness, somnolence General disorders and administration site conditions Injection site abscess sterile Reported with intramuscular injection. , injection site induration , injection site pain , injection site irritation

Drug Interactions

Drug Interactions Lincomycin has been shown to have neuromuscular blocking properties that may enhance the action of other neuromuscular blocking agents; therefore, it should be used with caution in patients receiving such agents.

Contraindications

CONTRAINDICATIONS LINCOCIN is contraindicated in patients previously found to be hypersensitive to lincomycin or clindamycin.

Pregnancy and Breastfeeding

Pregnancy There are no adequate and well-controlled studies in pregnant women. LINCOCIN Sterile Solution contains benzyl alcohol as a preservative. Benzyl alcohol can cross the placenta. See WARNINGS . LINCOCIN should be used during pregnancy only if clearly needed. Teratogenic Effects In a study with 60 pregnant women, cord serum concentrations were approximately 25% of the maternal serum concentrations, indicating that lincomycin crosses the placenta, and no substantial accumulation occurred in the amniotic fluid. Experience with 345 obstetrical patients receiving LINCOCIN revealed no ill effects related to pregnancy. There was no evidence of teratogenicity when lincomycin was administered in diet to pregnant Sprague Dawley rats during the period of major organogenesis at doses up to 5000 mg/kg (approximately 6 times the maximum recommended human dose [MRHD], respectively, based on body surface area comparison). Nonteratogenic Effects Reproduction studies performed in rats administered oral lincomycin in diet for 2 weeks prior to mating, throughout pregnancy and lactation, revealed no adverse effects on survival of offspring from birth to weaning at doses up to 1000 mg/kg (1.2 times the MRHD based on body surface area comparison) up to 2 generations.

Nursing Mothers Lincomycin has been reported to appear in human milk in concentrations of 0.5 to 2.4 mcg/mL. Because of the potential for serious adverse reactions in nursing infants from LINCOCIN, a decision should be made whether to discontinue nursing, or to discontinue the drug, taking into account the importance of the drug to the mother.

Overdosage

OVERDOSAGE Serum concentrations of lincomycin are not appreciably affected by hemodialysis and peritoneal dialysis.

How Supplied

HOW SUPPLIED LINCOCIN (lincomycin injection, USP) is available as a sterile, clear, and colorless solution in the following strength and package sizes: Unit of Sale Concentration NDC 0009-0555-01 or NDC 0009-0104-04 600 mg/2 mL 2 mL multiple-dose vial (300 mg/mL) NDC 0009-0107-04 3,000 mg/10 mL 10 mL multiple-dose vial (300 mg/mL) Each mL of LINCOCIN contains 300 mg lincomycin (equivalent to 340 mg lincomycin hydrochloride, USP); also benzyl alcohol, 9.45 mg added as preservative. Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP].