Absorption, Distribution and Excretion
A 600 mg dose of lincomycin administered over two hours intravenously results in an average Cmax of 15.9 μg/mL while the same dose given by intramuscular injection produces an average Cmax of 11.6 μg/mL after 60 minutes. Lincomycin administered intramuscularly to healthy adult male volunteers in doses between 600 and 1500 mg had an AUC0-∞ between 92.22 and 159.91 μg\*h/mL. A similar study using intravenous infusion of 600-2400 mg lincomycin found AUC0-∞ values between 72.5 and 212.8 μg\*h/mL. Overall, the AUC increases disproportionally to dose.
Following a 600 mg dose of lincomycin given either intramuscularly or intravenously, the urinary excretion ranges from 1.8-30.3% of the administered dose. Bile is also thought to be an important route of elimination. Dose adjustments are required in patients with either renal or hepatic impairment.
Lincomycin administered intravenously to healthy adult males had a steady-state volume of distribution of 63.8 ± 23.8, 78.8 ± 17.0, and 105.1 ± 43.1 L for 600, 1200, and 2400 mg doses, respectively.
Lincomycin administered intravenously to healthy adult males had a clearance of 9.9 ± 2.5, 10.0 ± 2.0, and 11.8 ± 2.4 L/h for 600, 1200, and 2400 mg doses, respectively.
Lincomycin is rapidly but only partially (20 to 35%) absorbed from gi tract ... Peak plasma concn avg 2 to 5 ug/mL after oral dose of 500 mg; values maintained ... for most gram-pos microorganisms for 6 to 8 hr, and detectable antibacterial activity persists for 12 hr or more. Im injection results in max plasma concn within 30 min.
Urinary excretion ... is limited and quite variable; about 5% of oral dose and 15% of parenteral dose appear in urine. The bile is important route of excretion of ... antibiotic. Drug appears in active form in feces after oral and parenteral admin, suggesting excretion in bile, through intestinal wall or both.
Lincomycin is distributed in both extracellular and intracellular fluids and is detectable in most human tissues. Reaches insignificant concn in cerebrospinal fluid in persons with normal meninges, and attains concn that are approx 40% of those in plasma in cases of meningitis.
Lincomycin is distributed into milk; concentrations of 0.5-2.4 ug/mL have been reported in human milk.
For more Absorption, Distribution and Excretion (Complete) data for LINCOMYCIN (12 total), please visit the HSDB record page.

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Metabolism / Metabolites
Lincomycin metabolism is poorly defined, though the primary product recovered following administration in humans is unchanged lincomycin.
Lincomycin is partially metabolized in the liver and both drug and metabolites are excreted in urine, bile, and feces.

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Biological Half-Life
Lincomycin has a biological half-life of 5.4 ± 1.0 hours following intramuscular or intravenous administration, which is prolonged in patients with impaired hepatic or renal function.
The plasma half-life of lincomycin is 4-6.4 hours in patients with normal renal function. The plasma half-life is increased in proportion to the degree of impairment in patients with reduced renal or hepatic function.100 Plasma half-lives as high as 3 times normal have been reported in patients with severe renal impairment. The half-life may be 2 times normal in patients with hepatic impairment.

Protein Binding
Lincomycin serum protein binding varies greatly depending on the dose, ranging from 28 to 86% in one study, and generally decreases with increasing serum concentration suggesting saturable binding. It has been suggested that lincomycin, like [clindamycin], is primarily bound to α1-acid glycoprotein, which is consistent with later studies in humans and animals.

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Interactions
Lincomycin has been shown to have neuromuscular blocking properties that may enhance the neuromuscular blocking action of other agents (e.g., ether, tubocurarine, pancuronium). Lincomycin should be used with caution in patients receiving such agents.
When administered concomitantly, kaolin reduces the GI absorption of lincomycin by as much as 90%, resulting in decreased plasma concentrations of the antibiotic. If administration of both drugs is necessary, patients should receive kaolin at least 2 hours before lincomycin.
Because of reported in vitro antagonism between lincomycin and erythromycin, the drugs should not be used concomitantly.
Antiperistaltic agents, such as opiates, difenoxin, diphenoxylate, or loperamide, may prolong or worsen pseudomembranous colitis by delaying toxin elimination.

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Non-Human Toxicity Values
LD50 Rat Sprague-Dawley oral 15,645 mg/kg
LD50 Rat Sprague-Dawley sc, 9778 mg/kg /Lincomycin hydrochloride/
LD50 Rat newborn 783 mg/kg /Lincomycin hydrochloride/
LD50 Rat subcutaneous 9780 mg/kg
For more Non-Human Toxicity Values (Complete) data for LINCOMYCIN (7 total), please visit the HSDB record 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
Anti-Bacterial Agents
Lincomycin is used in the treatment of serious infections caused by susceptible staphylococci, Streptococcus pneumoniae, and other streptococci. /Included in US product labeling/
MEDICATION (VET): Used im in swine for arthritis and pneumonia, particularly that caused by mycoplasma spp.
MEDICATION (VET): To help increase weight gains and feed efficiency in floor raised broilers.
For more Therapeutic Uses (Complete) data for LINCOMYCIN (9 total), please visit the HSDB record page.

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Drug Warnings
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), have occurred in patients receiving lincomycin. Treatment with anti-infectives alters normal colon flora and may permit overgrowth of C. difficile. CDAD has been reported with nearly all anti-infectives, including lincomycin, and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B, which contribute to the development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since these infections may be refractory to anti-infectives and colectomy may be required.
Overgrowth of yeasts may occur in intestinal tract.
... Other reactions recorded after oral therapy are glossitis, stomatitis, nausea, vomiting, pruritus ani, various skin rashes, urticaria, generalized pruritus, and vaginitis. Parenteral admin ... followed rarely by neutropenia, leukopenia, and thrombopenia ... which disappear when therapy is stopped.
... Other rare untoward effects ... /include/ angioedema, serum sickness, anaphylaxis, photosensitivity, and cardiopulmonary arrest (after rapid intravenous infusion).
For more Drug Warnings (Complete) data for LINCOMYCIN (20 total), please visit the HSDB record page.

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Pharmacodynamics
Lincomycin is a lincosamide antibiotic derived as a natural fermentation product from _Streptomyces lincolnensis_. Like [clindamycin], lincomycin is active against Gram-positive cocci and bacilli as well as Gram-negative cocci and some other organisms such as _Haemophilus_ spp. It is also effective against anaerobic bacteria, though in this regard [clindamycin] is generally more potent. Prescribing information highlights that the range of clinically confirmed effectiveness is largely limited to _Staphylococcus_ spp. and _Streptococcus_ spp., with additional activity noted _in vitro_. Lincomycin should be used with caution due to its association with severe cutaneous hypersensitivity reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, and acute generalized exanthematous pustulosis, and its potential to precipitate _Clostridium difficile_ associated diarrhea (CDAD), which may lead to fatal colitis. Special care should therefore be exercised when used in elderly patients, individuals with a history of gastrointestinal disease, and those with a history of asthma or significant allergies. Lincomycin for injection may contain benzyl alcohol as a preservative, which has been associated with gasping syndrome in pediatric patients. The serum half-life is extended in patients with hepatic/renal impairment and may require dose adjustments and additional monitoring. Like all antibiotics, lincomycin use may cause overgrowth of non-susceptible organisms, 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.)