Lincocin

Lincosamide Antibiotics

Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit. Lincomycin is a clear, colorless solution.

Dilution:
Dilute prior to intravenous infusion with a compatible solution, such as 5% Dextrose Injection, 10% Dextrose Injection, 5% Dextrose and 0.9% Sodium Chloride Injection, 10% Dextrose and 0.9% Sodium Chloride Injection, or Lactated Ringer's Injection, to yield a final concentration not exceeding 10 mg/mL:
600 mg/100 mL
1 g/100 mL
2 g/200 mL
3 g/300 mL
4 g/400 mL
Storage: The diluted solution is stable for 24 hours at room temperature.
 
Intravenous Infusion:
Administer by slow IV infusion at a rate no faster than 1 g/hour:
600 mg IV over 1 hour
1 g IV over 1 hour
2 g IV over 2 hours
3 g IV over 3 hours
4 g IV over 4 hours
Do not administer by intravenous bolus injection. Severe cardiopulmonary reactions have occurred when administered at greater than the recommended concentration and rate.

No dilution necessary.
Inject deeply into a large muscle mass.

Subconjunctival Administration
No dilution necessary.

toxic epidermal necrolysis / Delayed / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
serum sickness / Delayed / Incidence not known
acute generalized exanthematous pustulosis (AGEP) / Delayed / Incidence not known
exfoliative dermatitis / Delayed / Incidence not known
anaphylactic shock / Rapid / Incidence not known
erythema multiforme / Delayed / Incidence not known
angioedema / Rapid / Incidence not known
Stevens-Johnson syndrome / Delayed / Incidence not known
C. difficile-associated diarrhea / Delayed / Incidence not known
cardiac arrest / Early / Incidence not known
aplastic anemia / Delayed / Incidence not known
pancytopenia / Delayed / Incidence not known
agranulocytosis / Delayed / Incidence not known
thrombotic thrombocytopenic purpura (TTP) / Delayed / Incidence not known
oliguria / Early / Incidence not known
azotemia / Delayed / Incidence not known

bullous rash / Early / Incidence not known
stomatitis / Delayed / Incidence not known
glossitis / Early / Incidence not known
vaginitis / Delayed / Incidence not known
pseudomembranous colitis / Delayed / Incidence not known
candidiasis / Delayed / Incidence not known
superinfection / Delayed / Incidence not known
hypotension / Rapid / Incidence not known
leukopenia / Delayed / Incidence not known
neutropenia / Delayed / Incidence not known
jaundice / Delayed / Incidence not known
elevated hepatic enzymes / Delayed / Incidence not known
phlebitis / Rapid / Incidence not known

pruritus / Rapid / Incidence not known
rash / Early / Incidence not known
urticaria / Rapid / Incidence not known
diarrhea / Early / Incidence not known
nausea / Early / Incidence not known
vomiting / Early / Incidence not known
pruritus ani / Early / Incidence not known
abdominal pain / Early / Incidence not known
tinnitus / Delayed / Incidence not known
vertigo / Early / Incidence not known
injection site reaction / Rapid / Incidence not known
headache / Early / Incidence not known
dizziness / Early / Incidence not known
drowsiness / Early / Incidence not known

Consider pseudomembranous colitis in patients presenting with diarrhea after antibacterial use. Careful medical history is necessary as pseudomembranous colitis has been reported to occur over 2 months after the administration of antibacterial agents. Almost all antibacterial agents, including lincomycin, have been associated with pseudomembranous colitis or C. difficile-associated diarrhea (CDAD) which may range in severity from mild to life-threatening. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.

Lincocin

Rx

Lincosamide antibiotic
Used for serious staphylococcal, pneumococcal, and streptococcal infections in penicillin-allergic patients when other less toxic agents not appropriate
Associated with pseudomembranous colitis

600 mg IM every 24 hours. For severe infections, 600 mg IM every 12 hours or more often.

10 mg/kg (Max: 600 mg/dose) IM every 24 hours. For severe infections, 10 mg/kg IM (Max: 600 mg/dose) every 12 hours or more often.

600 to 1,000 mg IV every 8 to 12 hours. For severe infections, may increase dosage. In life-threatening infection, as much as 8 g/day IV in divided doses has been given.

10 to 20 mg/kg/day IV divided every 8 to 12 hours. Do not exceed adult doses.

75 mg by subconjunctival injection.

Dose cautiously in patients with hepatic impairment; specific recommendations are not available. Monitor serum lincomycin concentrations during high-dose therapy.

In patients with diminished renal function, reduce dose by 70% to 75%. Monitor serum lincomycin concentrations with high-dose therapy.
 
Intermittent hemodialysis
Hemodialysis is not effective in removing lincomycin from the serum.
 
Peritoneal dialysis
Peritoneal dialysis is not effective in removing lincomycin from the serum.

Atracurium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Cisatracurium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Dienogest; Estradiol valerate: (Moderate) Anti-infectives that disrupt the normal GI flora, clindamycin, lincomycin, may potentially decrease the effectiveness of estrogen-containing oral contraceptives.
Estradiol: (Moderate) Anti-infectives that disrupt the normal GI flora, clindamycin, lincomycin, may potentially decrease the effectiveness of estrogen-containing oral contraceptives. (Moderate) Anti-infectives which disrupt the normal GI flora, including lincomycin and clindamycin, may potentially decrease the effectiveness of estrogen containing oral contraceptives. Alternative or additional contraception may be advisable.
Isoflurane: (Moderate) Concurrent use of isoflurane with systemic clindamycin can result in an additive neuromuscular blockade.
Mivacurium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Neuromuscular blockers: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Oral Contraceptives: (Moderate) It would be prudent to recommend alternative or additional contraception when oral contraceptives (OCs) are used in conjunction with antibiotics. It was previously thought that antibiotics may decrease the effectiveness of OCs containing estrogens due to stimulation of metabolism or a reduction in enterohepatic circulation via changes in GI flora. One retrospective study reviewed the literature to determine the effects of oral antibiotics on the pharmacokinetics of contraceptive estrogens and progestins, and also examined clinical studies in which the incidence of pregnancy with OCs and antibiotics was reported. It was concluded that the antibiotics ampicillin, ciprofloxacin, clarithromycin, doxycycline, metronidazole, ofloxacin, roxithromycin, temafloxacin, and tetracycline did not alter plasma concentrations of OCs. Antituberculous drugs (e.g., rifampin) were the only agents associated with OC failure and pregnancy. Based on the study results, these authors recommended that back-up contraception may not be necessary if OCs are used reliably during oral antibiotic use. Another review concurred with these data, but noted that individual patients have been identified who experienced significant decreases in plasma concentrations of combined OC components and who appeared to ovulate; the agents most often associated with these changes were rifampin, tetracyclines, and penicillin derivatives. These authors concluded that because females most at risk for OC failure or noncompliance may not be easily identified and the true incidence of such events may be under-reported, and given the serious consequence of unwanted pregnancy, that recommending an additional method of contraception during short-term antibiotic use may be justified. During long-term antibiotic administration, the risk for drug interaction with OCs is less clear, but alternative or additional contraception may be advisable in selected circumstances. Data regarding progestin-only contraceptives or for newer combined contraceptive deliveries (e.g., patches, rings) are not available.
Pancuronium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Rocuronium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Sevoflurane: (Moderate) Concurrent use of sevoflurane with systemic clindamycin can result in an additive neuromuscular blockade.
Sodium picosulfate; Magnesium oxide; Anhydrous citric acid: (Major) Prior or concomitant use of antibiotics with sodium picosulfate; magnesium oxide; anhydrous citric acid may reduce efficacy of the bowel preparation as conversion of sodium picosulfate to its active metabolite bis-(p-hydroxy-phenyl)-pyridyl-2-methane (BHPM) is mediated by colonic bacteria. If possible, avoid coadministration. Certain antibiotics (i.e., tetracyclines and quinolones) may chelate with the magnesium in sodium picosulfate; magnesium oxide; anhydrous citric acid solution. Therefore, these antibiotics should be taken at least 2 hours before and not less than 6 hours after the administration of sodium picosulfate; magnesium oxide; anhydrous citric acid solution.
Succinylcholine: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Vecuronium: (Moderate) Use neuromuscular blockers and lincosamides with caution. Concomitant use of neuromuscular blockers and lincosamides may prolong neuromuscular blockade. The use of a peripheral nerve stimulator is strongly recommended to evaluate the level of neuromuscular blockade, to assess the need for additional doses of neuromuscular blocker, and to determine whether adjustments need to be made to the dose with subsequent administration.
Vitamin C: (Moderate) Monitor for decreased efficacy of lincomycin during coadministration; discontinue ascorbic acid therapy if decreased efficacy is suspected. Coadministration may result in decreased efficacy of lincomycin.
Warfarin: (Moderate) The concomitant use of warfarin with many classes of antibiotics, including aminoglycosides, may result in an increased INR thereby potentiating the risk for bleeding. Inhibition of vitamin K synthesis due to alterations in the intestinal flora may be a mechanism; however, concurrent infection is also a potential risk factor for elevated INR. Monitor patients for signs and symptoms of bleeding. Additionally, increased monitoring of the INR, especially during initiation and upon discontinuation of the antibiotic, may be necessary.

Lincocin/Lincomycin/Lincomycin Hydrochloride Intramuscular Inj Sol: 1mL, 300mg
Lincocin/Lincomycin/Lincomycin Hydrochloride Intravenous Inj Sol: 1mL, 300mg

8 g/day IV. 1.2 g/day IM or more for severe infections.

8 g/day IV. 1.2 g/day IM or more for severe infections.

20 mg/kg/day IV/IM or more for severe infections. Do not exceed adult dosage limits.

20 mg/kg/day IV/IM or more for severe infections. Do not exceed adult dosage limits.

20 mg/kg/day IV/IM or more for severe infections. Do not exceed adult dosage limits.

Safety and efficacy have not been established.

Lincomycin binds to the 50 S ribosomal subunits of the bacteria and inhibits protein synthesis, eventually resulting in inhibition of bacterial cell growth or bacterial death. Antibacterial activity primarily results from inhibition of peptide bond formation. Lincomycin is either bacteriostatic or bactericidal depending on its concentration at the site of infection and the specific susceptibility of the organism being treated. Complete bacterial cross resistance has been seen with clindamycin. Resistance is most often due to methylation of specific nucleotides in the 23S RNA of the 50S ribosomal unit, which can determine cross resistance to macrolides and streptogramins B. Susceptibility testing using the D-zone test or other appropriate method is recommended for macrolide-resistant organisms to determine inducible resistance.

Lincomycin is administered via the intravenous and intramuscular routes. Lincomycin is 77% to 82% protein bound.
 
Significant lincomycin concentrations have been demonstrated in the majority of body tissues. Lincomycin appears to diffuse into cerebral spinal fluid (CSF); however, the CSF concentrations appear inadequate for the treatment of meningitis.
 
Tissue concentration studies demonstrate that bile is an important route of excretion. The biological half-life of lincomycin after intramuscular or intravenous administration is 5.4 +/- 1 hours.
 
Affected cytochrome P450 isoenzymes: none

A 2-hour intravenous infusion of lincomycin 600 mg achieves average peak serum concentrations of 15.9 mcg/mL and yields therapeutic concentrations for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9% to 30.3% (mean 13.8%).

Intramuscular administration of a single dose of 600 mg of lincomycin produces average peak serum concentrations of 11.6 mcg/mL at 60 minutes and maintains therapeutic concentrations for 17 to 20 hours for most susceptible gram-positive organisms. Urinary excretion of lincomycin after this dose ranges from 1.8% to 24.8% (mean 17.3%).

There are no adequate and well-controlled studies with lincomycin in pregnant women. Parenteral lincomycin contains benzyl alcohol, which can cross the placenta and has been associated with neonatal gasping syndrome. Use lincomycin during pregnancy only if clearly needed. Studies have shown that lincomycin crosses the placental barrier with cord serum concentrations of approximately 25% of maternal serum concentrations; no substantial accumulation occurred in the amniotic fluid. Data from 345 pregnant patients receiving lincomycin showed no adverse effects relating to pregnancy. There was no evidence of teratogenicity in rats given oral lincomycin at doses up to 6 times the maximum recommended human dose (MRHD), based on body surface area comparison, during the period of major organogenesis. There were also no adverse effects on offspring survival from birth to weaning in reproductive studies in rats given oral lincomycin at doses up to 1.2 times the MRHD based on body surface area comparison.[28493]

Lincomycin has been detected in human breast milk in concentrations of 0.5 to 2.4 mcg/mL. Because of the potential for serious adverse reactions from lincomyin in breast-fed infants, discontinue lincomycin or discontinue breast-feeding, considering the importance of the drug to the mother.