Absorption, Distribution and Excretion
After intravenous administration of 600 mg lincomycin, the mean peak plasma concentration (Cmax) over two hours was 15.9 μg/mL; while after intramuscular administration of the same dose, the mean Cmax was 11.6 μg/mL 60 minutes later. In healthy adult male volunteers, intramuscular administration of 600 to 1500 mg lincomycin resulted in AUC0-∞ values ranging from 92.22 to 159.91 μgh/mL. A similar study using intravenous infusion of 600 to 2400 mg lincomycin found AUC0-∞ values ranging from 72.5 to 212.8 μgh/mL. Overall, AUC increases disproportionately with dose. Following intramuscular or intravenous administration of 600 mg lincomycin, urinary excretion ranges from 1.8% to 30.3% of the administered dose. Bile is also considered an important route of excretion. Dose adjustment is necessary for patients with impaired renal or hepatic function.
Following intravenous administration of lincomycin in healthy adult males, the steady-state volumes of distribution for 600 mg, 1200 mg, and 2400 mg doses were 63.8 ± 23.8 L, 78.8 ± 17.0 L, and 105.1 ± 43.1 L, respectively.
Following intravenous administration of lincomycin in healthy adult males, the clearance rates for 600 mg, 1200 mg, and 2400 mg doses were 9.9 ± 2.5 L/h, 10.0 ± 2.0 L/h, and 11.8 ± 2.4 L/h, respectively.
Lincomycin is rapidly absorbed from the gastrointestinal tract, but the absorption rate is only 20% to 35%...After oral administration of 500 mg, the average peak plasma concentration is 2 to 5 μg/mL; its antibacterial activity against most Gram-positive microorganisms can be maintained for 6 to 8 hours, and detectable antibacterial activity can persist for 12 hours or longer. Peak plasma concentrations are reached within 30 minutes after intramuscular injection. Urinary excretion is limited and highly variable; approximately 5% of oral doses and approximately 15% of parenteral doses are excreted in urine. Bile is an important route of excretion for this antibiotic. After oral and parenteral administration, the drug is present in feces in its active form, suggesting possible excretion via bile, the intestinal wall, or both. Lincomycin is distributed in both extracellular and intracellular fluids and is detectable in most human tissues. In individuals with normal meninges, its concentration in cerebrospinal fluid is extremely low; however, in patients with meningitis, concentrations can reach approximately 40% of plasma concentrations. Lincomycin is distributed in breast milk; concentrations in human milk have been reported to be 0.5–2.4 μg/mL. For more complete data on absorption, distribution, and excretion of lincomycin (12 items in total), please visit the HSDB records page. Metabolism/Metabolites The metabolism of lincomycin is not fully understood, but the main product recovered in the body after administration is unmetabolized lincomycin. Lincomycin is partially metabolized in the liver, and the drug and its metabolites are excreted in urine, bile, and feces. Biological Half-Life After intramuscular or intravenous injection, the biological half-life of lincomycin is 5.4 ± 1.0 hours. The half-life is prolonged in patients with impaired hepatic or renal function. In patients with normal renal function, the plasma half-life of lincomycin is 4–6.4 hours. The plasma half-life in patients with impaired renal or hepatic function is proportionally prolonged to the degree of impairment. It has been reported that the plasma half-life in patients with severe renal impairment can be up to three times the normal value. The plasma half-life in patients with hepatic impairment may be twice the normal value.

Protein Binding
The serum protein binding rate of lincomycin varies considerably with dose, ranging from 28% to 86% in one study, and generally decreases with increasing serum concentration, suggesting saturation. Studies have shown that lincomycin, similar to clindamycin, primarily binds to α1-acid glycoproteins, consistent with subsequent human and animal studies. Interactions Lincomycin has been shown to have neuromuscular blocking effects and may enhance the neuromuscular blocking effects of other drugs (e.g., ether, tubocurarine, pancuronium bromide). Patients receiving this type of treatment should use lincomycin with caution. Concomitant administration of kaolin can reduce the gastrointestinal absorption of lincomycin by up to 90%, leading to a decrease in the plasma concentration of the antibiotic. If both drugs must be taken concurrently, patients should take kaolin at least 2 hours before taking lincomycin. Due to reported in vitro antagonism between lincomycin and erythromycin, these two drugs should not be used concurrently.
Anti-peristaltic drugs, such as opioids, diphenoxylate, or loperamide, may prolong or worsen pseudomembranous colitis by delaying toxin clearance.

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Non-human toxicity values
Sprague-Dawley rat oral LD50: 15,645 mg/kg
Sprague-Dawley rat subcutaneous LD50: 9778 mg/kg (lincomycin hydrochloride)
Neonatal rat LD50: 783 mg/kg (lincomycin hydrochloride)
Rat subcutaneous LD50: 9780 mg/kg
For more information on the non-human toxicity values (complete) for LINCOMYCIN (7 in total), please visit the HSDB records page.

[1]. Sasaki E, e al. Construction of the octose 8-phosphate intermediate in lincomycin A biosynthesis: characterization of the reactions catalyzed by LmbR and LmbN. J Am Chem Soc. 2012;134(42):17432-17435.

Therapeutic Uses

Antimicrobial Agents
Lincomycin is used to treat serious infections caused by susceptible Staphylococcus, Streptococcus pneumoniae, and other streptococci. /US Product Label Includes/
Veterinary Drug: For arthritis and pneumonia in pigs, especially mycoplasma-induced pneumonia.
Veterinary Drug: To help improve weight gain and feed conversion ratio in free-range broilers.
For more complete data on the therapeutic uses of lincomycin (9 in total), please visit the HSDB record page.

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Drug Warnings
Patients treated with lincomycin have experienced nonspecific colitis and diarrhea, as well as potentially fatal Clostridium difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis). Anti-infective drug treatment can alter the normal colonic flora and may lead to Clostridium difficile overgrowth. Almost all anti-infective drugs, including lincomycin, have been reported to cause Clostridium difficile-associated diarrhea (CDAD), ranging in severity from mild diarrhea to fatal colitis. Clostridium difficile produces toxins A and B, which are important factors in the development and progression of CDAD; highly toxin-producing Clostridium difficile strains are associated with higher morbidity and mortality because these infections may be unresponsive to anti-infective drugs and may even require colectomy. Yeast overgrowth may occur in the gut. Other adverse reactions recorded after oral treatment include glossitis, stomatitis, nausea, vomiting, anal pruritus, various rashes, urticaria, generalized pruritus, and vaginitis. Parenteral administration…rarely, neutropenia, leukopenia, and thrombocytopenia may occur…these symptoms usually resolve upon discontinuation of the drug. Other rare adverse reactions…including angioedema, serum sickness, anaphylactic reactions, photosensitivity, and cardiopulmonary arrest (after rapid intravenous infusion). For more complete data on drug warnings for lincomycin (20 in total), please visit the HSDB record page.

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Pharmacodynamics
Lincomycin is a lincosamide antibiotic derived from the natural fermentation product of Streptomyces lincolnensis. Similar to clindamycin, lincomycin is effective against Gram-positive cocci and bacilli, as well as Gram-negative cocci and some other microorganisms (such as Haemophilus spp.). Lincomycin is also effective against anaerobic bacteria, but clindamycin is generally more potent in this regard. Prescribing information emphasizes that its clinically proven efficacy is primarily limited to Staphylococcus and Streptococcus spp., although other activities have been observed in vitro. Lincomycin should be used with caution because it is associated with severe skin hypersensitivity reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, and acute generalized pustulosis) and may induce Clostridium difficile-associated diarrhea (CDAD), potentially leading to fatal colitis. Special caution should be exercised in elderly patients, patients with a history of gastrointestinal disease, and patients with a history of asthma or severe allergies. Injectable lincomycin may contain benzyl alcohol as a preservative, and benzyl alcohol has been associated with wheezing syndrome in pediatric patients. Patients with hepatic or renal impairment may have a prolonged serum half-life, potentially requiring dose adjustment and additional monitoring. As with other antibiotics, lincomycin use may lead to overgrowth of non-susceptible bacteria, which should be considered.

C18H34N2O6S

406.538

406.213

154-21-2

Lincomycin-d3;Lincomycin hydrochloride monohydrate;7179-49-9

3000540

Amorphous solid

1.16

771.9±70.0 °C

261-263°C

345ºC

1.6510 (estimate)

0.273

5

8

7

27

499

9

CCC[C@@H]1C[C@H](N(C1)C)C(N[C@@H]([C@@H]2[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O2)[C@H](O)C)=O

OJMMVQQUTAEWLP-KIDUDLJLSA-N

InChI=1S/C18H34N2O6S/c1-5-6-10-7-11(20(3)8-10)17(25)19-12(9(2)21)16-14(23)13(22)15(24)18(26-16)27-4/h9-16,18,21-24H,5-8H2,1-4H3,(H,19,25)/t9-,10-,11+,12-,13+,14-,15-,16-,18-/m1/s1

(2S,4R)-N-[(1R,2R)-2-hydroxy-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-1-methyl-4-propylpyrrolidine-2-carboxamide

U 10149; U-10149; Lincomycin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)