Actions of Linka in details
Pharmacology: Linka is absorbed rapidly after a 500 mg oral dose, reaching peak levels in 2-4 hrs. Levels are maintained above the minimum inhibitory concentration (MIC) for most gram-positive organisms for 6-8 hrs. Urinary recovery of drug in a 24-hr period ranges from 1-31% (mean: 4) after a single oral dose of 500 mg of Linka. Tissue level studies indicate that bile is an important route of excretion. Significant levels have been demonstrated in the majority of body tissues. Although the drug is not present in significant amounts in the spinal fluid of normal volunteers, it has been demonstrated in the spinal fluid of one patient with pneumococcal meningitis.
Intramuscular administration of a single-dose of 600 mg of Linka produces a peak serum level at 30 min with defectable levels persisting for 24 hrs. Urinary excretion after this dose ranges from 1.8-24.8% (mean: 17.3).
The IV infusion over a 2-hr interval of 600 mg of Linka in 500 mL of 5% glucose in distilled water yields therapeutic levels for 14 hrs. Urinary excretion ranges from 4.9-30.3% (mean: 13.8).
The biological half-life (t½) after oral IM or IV administration is 5.4 + 1 hr.
Hemodialysis and peritoneal dialysis do not effectively remove Linka from the blood.
Microbiology: Linka has been shown to be effective against most of the common gram-positive pathogens. Depending on the sensitivity of the organism and concentration of the antibiotic, it may be either bactericidal or bacteriostatic. Cross resistance has not been demonstrated with penicillin, chloramphenicol, ampicillin, cephalosporins or the tetracyclines. Despite chemical differences, Linka exhibits antibacterial activity similar but not identical to the macrolide antibiotics (eg, erythromycin). Some cross resistance (with erythromycin) including a phenomenon known as dissociated cross resistance or macrolide effect has been reported. Microorganisms have not developed resistance to Linka rapidly when tested by in vitro or in vivo methods. Staphylococci develop resistance to Linka in a slow, stepwise manner based on in vitro, serial subculture experiments. This pattern of resistance development is unlike that shown for streptomycin.
Studies indicate that Linka does not share antigenicity with penicillin compounds.
Biological Studies: In vitro studies indicate that the spectrum or activity includes Staphylococcus aureus, Staphylococcus albus, B-hemolytic Streptococcus, Streptococcus viridans, Diplococcus pneumoniae, Clostridium tetani, Clostridium perfringens, Corynebacterium diphtheriae and Corynebacterium diphtheriae and Corynebacterium acnes.
NOTE: Linka is not active against most strains of Streptococcus faecalis, nor against Neisseria gonorrhoeae, Neisseria meningitidis, Hemophilus influenzae, or other gram‑negative organisms or yeasts.
How should I take Linka?
Linka is best taken with a full glass (8 ounces) of water on an empty stomach (either 1 hour before or 2 hours after meals), unless otherwise directed by your doctor.
To help clear up your infection completely, keep taking Linka for the full time of treatment, even if you begin to feel better after a few days. If you have a ``strep'' infection, you should keep taking Linka for at least 10 days. This is especially important in ``strep'' infections. Serious heart problems could develop later if your infection is not cleared up completely. Also, if you stop taking Linka too soon, your symptoms may return.
Linka works best when there is a constant amount in the blood. To help keep the amount constant, do not miss any doses. Also, it is best to take each dose at evenly spaced times day and night. For example, if you are to take 4 doses a day, doses should be spaced about 6 hours apart. If this interferes with your sleep or other daily activities, or if you need help in planning the best times to take your medicine, check with your health care professional.
Dosing
The dose of Linka will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Linka. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For infections caused by bacteria:
- For oral dosage form (capsules):
- Adults and teenagers—500 milligrams (mg) every six to eight hours.
- Infants up to 1 month of age—Use and dose must be determined by your doctor.
- Children 1 month of age and older—Dose is based on body weight. The usual dose is 7.5 to 15 mg per kilogram (kg) (3.4 to 6.8 mg per pound) of body weight every six hours; or 10 to 20 mg per kg (4.5 to 9.1 mg per pound) of body weight every eight hours.
- For injection dosage form:
- Adults and teenagers—600 mg to 1 gram injected into a vein over at least one hour, every eight to twelve hours; or 600 mg injected into a muscle every twelve to twenty-four hours.
- Infants up to 1 month of age—Use and dose must be determined by your doctor.
- Children 1 month of age and older—Dose is based on body weight. The usual dose is 10 mg per kg (4.5 mg per pound) of body weight injected into a muscle every twelve to twenty-four hours; or 3.3 to 6.7 mg per kg (1.5 to 3 mg per pound) of body weight injected into a vein every eight hours; or 5 to 10 mg per kg (2.3 to 4.5 mg per pound) of body weight injected into a vein every twelve hours.
- For oral dosage form (capsules):
Missed Dose
If you miss a dose of Linka, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Linka administration
Linka is given as an injection into a muscle, or through a needle placed into a vein. Your doctor, nurse, or other healthcare provider will give you this injection. You may be given instructions on how to inject your medicine at home. Do not use this medicine at home if you do not fully understand how to give the injection and properly dispose of needles and other items used in giving the medicine.
Linka is usually given every 12 to 24 hours. Follow your doctor's instructions.
Use each disposable needle only one time. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.
Use this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Linka will not treat a viral infection such as the common cold or flu.
To be sure this medication is not causing harmful effects, your blood may need to be tested on a regular basis. Your kidney or liver function may also need to be tested.
If you store this medication at home, keep at room temperature away from moisture and heat.
Linka pharmacology
Intramuscular administration of a single dose of 600 mg of Linka produces average peak serum levels of 11.6 μg/mL at 60 minutes and maintains therapeutic levels for 17 to 20 hours for most susceptible gram-positive organisms. Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 17.3 percent).
A two hour intravenous infusion of 600 mg of Linka achieves average peak serum levels of 15.9 μg/mL and yields therapeutic levels for 14 hours for most susceptible gram-positive organisms. Urinary excretion ranges from 4.9 to 30.3 percent (mean: 13.8 percent).
The biological half-life after intramuscular or intravenous administration is 5.4 ± 1.0 hours. The serum half-life of Linka may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function. In patients with abnormal hepatic function, serum half-life may be twofold longer than in patients with normal hepatic function. Hemodialysis and peritoneal dialysis are not effective in removing Linka from the serum.
Tissue level studies indicate that bile is an important route of excretion. Significant levels have been demonstrated in the majority of body tissues. Although Linka appears to diffuse into cerebrospinal fluid (CSF), levels of Linka in the CSF appear inadequate for the treatment of meningitis.
Microbiology
Linka has been shown to be active against most strains of the following organisms both in vitro and in clinical infections:.
Staphylococcus aureus
Streptococcus pneumoniae
The following in vitro data are available; but their clinical significance is unknown.
Linka has been shown to be active in vitro against the following microorganisms; however, the safety and efficacy of Linka in treating clinical infections due to these organisms have not been established in adequate and well controlled trials.
Gram-positive Bacteria
Corynebacterium diphtheriae
Streptococcus pyogenes
Viridans group streptococci
Anaerobic Bacteria
Clostridium tetani
Clostridium perfringens
Cross resistance has been demonstrated between clindamycin and Linka. Resistance is most often due to methylation of specific nucleotides in the 23S RNA of the 50S ribosomal subunit, which can determine cross resistance to macrolides and streptogramins B (MLSB phenotype). Macrolide-resistant isolates of these organisms should be tested for inducible resistance to Linka/clindamycin using the D-zone test or other appropriate method.
There are currently no antimicrobial susceptibility testing (AST) interpretive criteria for Linka
Animal Pharmacology
In vivo experimental animal studies demonstrated the effectiveness of Linka preparations (Linka) in protecting animals infected with Streptococcus viridans, β-hemolytic Streptococcus, Staphylococcus aureus, Diplococcus pneumoniae and Leptospira pomona. It was ineffective in Klebsiella, Pasteurella, Pseudomonas, Salmonella and Shigella infections.
Clinical Studies
Experience with 345 obstetrical patients receiving this drug revealed no ill effects related to pregnancy.
References
- NCIt. "Lincomycin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Lincomycin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
