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Continuing
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Lincosamide antibiotics
• Lincosamides are a small group of antibiotics.
• Clindamycin and lincomycin are the most common drugs in this class.
• Clindamycin differs from lincomycin by only the addition of chlorine to the parent molecule.
• Like macrolides, these drugs are inhibitors that bind to the 50-S ribosomal subunit and interfere
with protein synthesis.
• They are traditionally considered bacteriostatic (time-dependent in action), but more recent
evidence shows that there is some bactericidal activity as well.
LINCOMYCIN
Lincomycin is available as:
• Lincomycin 1000 mg sustained release tablets
• Lincomycin 500 mg capsules
• Lincomycin 250 mg capsules
• Lincomycin 300 mg (1 ml) injection
• Lincomycin 600 mg (2 ml) injection
• Lincomycin 125 mg / 5 ml suspension
• Lincomycin 2% w/w gel for topical application
Indications and clinical uses
Lincomycin is indicated in the treatment of infections caused
by sensitive gram-positive organisms (staphylococci,
including penicillinase-producing staphylococci, streptococci,
and pneumococci) in intolerant patients or the organism
resistant to other antibiotics.
• URTI such as Laryngopharyngitis, Tonsillitis, Bacterial
Rhinosinusitis, Otitis media, etc.
• SSTI such as Boils, Furuncles, Abscess, Celulitis, etc.
• Dental infections such as Periodontitis, Gingivitis, etc.
Microbiology
ORGANISM M.I.C. (μ/mL)
Staphylococcus aureus 0.12 -2.0
Staphylococcus albus 0.8-1.5
8-Hemolytic streptococcus 0.12-2.0
Streptococcus viridans 0.12-0.5
Streptococcus pneumoniae 0.12-1.0
Clostridium tetani & perfringens 0.36-1.4
Corynebacterium diphtheriae 0.4
Minimum inhibitory concentrations (MIC)
• Lynx is a specific spectrum antibiotic exhibiting potent
activity against Gram Positive aerobic organisms.
• It also exerts a good antibacterial effect against many
anaerobic organisms.
• Lincomycin is effective against aerobic gram-positive
cocci, particularly Staphylococcus aureus, Streptococcus
pyogenes, Streptococcus viridans and Streptococcus
pneumoniae - the most common organisms causing out-
patient infections
Tissue Concentration
• Lincomycin is distributed into many body tissues and fluids including peritoneal fluid, pleural fluid, synovial
fluid, bone, bile, skin, Scar tissue and aqueous humor.
• Lynx penetrates healthy tissue, necrotic tissue and pus, and is not inhibited by bacterial enzymes.
Lynx and Host Defence
• Lynx stimulates host defense
mechanisms.
• Lynx concentrates
approximately two times the
average serum concentration in
human polymorphonuclear cells
Lynx OD: Fulfils TYPE III PK/PD antibiotic
characteristics
Lincomycin belongs to the PK/PD type III class for which efficacy is determined by a ratio of 24h-AUC / MIC.
There is an antibacterial inhibitory effect when the AUC24h / MIC is ≥ 24h.
Lincomycin is mainly effective against, and prescribed for, infections due to Gram-positive pathogenic cocci.
Minimum Inhibitory Concentrations (MIC)
 Staphylococcus (S) aureus: 0.2-3.2 mcg/mL (for most species it is: 2-2.8 mcg/mL6,7)
 Streptococcus (Strep) pneumoniae: 0.05-0.4 mcg/mL
 +Strep pyogenes: 0.04-0.8 mcg/mL
1. Rotimi VO, Olabiyi DA, Banjo TO, Okeowo PA. Randomised comparative efficacy of clindamycin, metronidazole, and lincomycin, plus gentamicin in chronic
suppurative otitis media. West African Journal of Medicine. 1990; 9(2):89-97
2. Craig W. Pharmacodynamics of antimicrobial agents as a basis for determining dosage regimens. Eur J Clin Microbiol Infect Dis 1993;12:Suppl 1:S6-8.
Lynx OD: Fulfils TYPE II PK/PD antibiotic
characteristics
LYNX OD (1000) once daily provides
blood concentrations above MIC of
susceptible pathogens for24 hours.
Clinical study 1 - SSTI
Study design: A clinical study
No. of subjects: 30
Duration: 14 days
Intervention: 500 mg orally twice/thrice a day
Results: A good response was seen in most
types of infections
Clinical study 2 - URTI
Study: efficacy and Safety of 3 different antibiotic
regimens for treatment of acute Pharyngitis /
Tonsilitis due to GABHS*
No. of subjects: 259
Centres: 8
Results: Lincomycin shows better microbiological
eradication rates compared to penicillin and
clarithromycin
GABHS* - Group A Beta Haemolytic Streptococci
Clinical study 3 -Dental
Study design: A clinical study
No. of subjects: 42
Duration: 5 days
Intervention: 500 mg capsules /irrigation solution
Results: All patients who were diagnosed with gingivitis, and those who underwent pre-surgical and post-
surgical periodontal procedures achieved complete relief, while 96.85% of patients diagnosed with
periodontitis achieved complete relief
Toxicity
• Lincomycin was shown to be of low acute toxicity.
• In rats and mice, the acute oral LD50 of different
pharmacopeial and premix grades of lincomycin
hydrochloride was always greater than 5000 mg/kg BW.
• Signs of toxicity observed at doses of 8000 mg/kg BW
and above included prostration, depression, diarrhea,
and convulsions.
The new technique used in the
manufacturing of LYNX OD tablet
Coating involved special grade functional polymer forming a
moisture barrier for the extended shelf life of the product
Special grade very high viscosity polymer used for manufacturing of
product ensures consistent and uniform release of the drug to
maintain a reproducible plasma level for 24 hours
Aqueous wet granulation technology involved in the manufacturing
of tablets ensures better stability of the formulation
Advantages of LYNX OD (LINCOMYCIN SR
1000 MG) tablet
Patented product (first time in India)
Improved patient compliance due to less frequent drug
administration – once daily versus 2-3 times a day frequency for
immediate release (IR) formulations
Reduction of fluctuation in steady-state drug levels (BE
compliance product)
Increased safety margin of the potent drug by reducing peaks in
drug levels following intake of each dose.
Thank You

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Lynx_OD_CME_Slides.pptx

  • 2. Lincosamide antibiotics • Lincosamides are a small group of antibiotics. • Clindamycin and lincomycin are the most common drugs in this class. • Clindamycin differs from lincomycin by only the addition of chlorine to the parent molecule. • Like macrolides, these drugs are inhibitors that bind to the 50-S ribosomal subunit and interfere with protein synthesis. • They are traditionally considered bacteriostatic (time-dependent in action), but more recent evidence shows that there is some bactericidal activity as well.
  • 3. LINCOMYCIN Lincomycin is available as: • Lincomycin 1000 mg sustained release tablets • Lincomycin 500 mg capsules • Lincomycin 250 mg capsules • Lincomycin 300 mg (1 ml) injection • Lincomycin 600 mg (2 ml) injection • Lincomycin 125 mg / 5 ml suspension • Lincomycin 2% w/w gel for topical application
  • 4. Indications and clinical uses Lincomycin is indicated in the treatment of infections caused by sensitive gram-positive organisms (staphylococci, including penicillinase-producing staphylococci, streptococci, and pneumococci) in intolerant patients or the organism resistant to other antibiotics. • URTI such as Laryngopharyngitis, Tonsillitis, Bacterial Rhinosinusitis, Otitis media, etc. • SSTI such as Boils, Furuncles, Abscess, Celulitis, etc. • Dental infections such as Periodontitis, Gingivitis, etc.
  • 5. Microbiology ORGANISM M.I.C. (μ/mL) Staphylococcus aureus 0.12 -2.0 Staphylococcus albus 0.8-1.5 8-Hemolytic streptococcus 0.12-2.0 Streptococcus viridans 0.12-0.5 Streptococcus pneumoniae 0.12-1.0 Clostridium tetani & perfringens 0.36-1.4 Corynebacterium diphtheriae 0.4 Minimum inhibitory concentrations (MIC) • Lynx is a specific spectrum antibiotic exhibiting potent activity against Gram Positive aerobic organisms. • It also exerts a good antibacterial effect against many anaerobic organisms. • Lincomycin is effective against aerobic gram-positive cocci, particularly Staphylococcus aureus, Streptococcus pyogenes, Streptococcus viridans and Streptococcus pneumoniae - the most common organisms causing out- patient infections
  • 6. Tissue Concentration • Lincomycin is distributed into many body tissues and fluids including peritoneal fluid, pleural fluid, synovial fluid, bone, bile, skin, Scar tissue and aqueous humor. • Lynx penetrates healthy tissue, necrotic tissue and pus, and is not inhibited by bacterial enzymes.
  • 7. Lynx and Host Defence • Lynx stimulates host defense mechanisms. • Lynx concentrates approximately two times the average serum concentration in human polymorphonuclear cells
  • 8. Lynx OD: Fulfils TYPE III PK/PD antibiotic characteristics Lincomycin belongs to the PK/PD type III class for which efficacy is determined by a ratio of 24h-AUC / MIC. There is an antibacterial inhibitory effect when the AUC24h / MIC is ≥ 24h. Lincomycin is mainly effective against, and prescribed for, infections due to Gram-positive pathogenic cocci. Minimum Inhibitory Concentrations (MIC)  Staphylococcus (S) aureus: 0.2-3.2 mcg/mL (for most species it is: 2-2.8 mcg/mL6,7)  Streptococcus (Strep) pneumoniae: 0.05-0.4 mcg/mL  +Strep pyogenes: 0.04-0.8 mcg/mL 1. Rotimi VO, Olabiyi DA, Banjo TO, Okeowo PA. Randomised comparative efficacy of clindamycin, metronidazole, and lincomycin, plus gentamicin in chronic suppurative otitis media. West African Journal of Medicine. 1990; 9(2):89-97 2. Craig W. Pharmacodynamics of antimicrobial agents as a basis for determining dosage regimens. Eur J Clin Microbiol Infect Dis 1993;12:Suppl 1:S6-8.
  • 9. Lynx OD: Fulfils TYPE II PK/PD antibiotic characteristics LYNX OD (1000) once daily provides blood concentrations above MIC of susceptible pathogens for24 hours.
  • 10. Clinical study 1 - SSTI Study design: A clinical study No. of subjects: 30 Duration: 14 days Intervention: 500 mg orally twice/thrice a day Results: A good response was seen in most types of infections
  • 11. Clinical study 2 - URTI Study: efficacy and Safety of 3 different antibiotic regimens for treatment of acute Pharyngitis / Tonsilitis due to GABHS* No. of subjects: 259 Centres: 8 Results: Lincomycin shows better microbiological eradication rates compared to penicillin and clarithromycin GABHS* - Group A Beta Haemolytic Streptococci
  • 12. Clinical study 3 -Dental Study design: A clinical study No. of subjects: 42 Duration: 5 days Intervention: 500 mg capsules /irrigation solution Results: All patients who were diagnosed with gingivitis, and those who underwent pre-surgical and post- surgical periodontal procedures achieved complete relief, while 96.85% of patients diagnosed with periodontitis achieved complete relief
  • 13. Toxicity • Lincomycin was shown to be of low acute toxicity. • In rats and mice, the acute oral LD50 of different pharmacopeial and premix grades of lincomycin hydrochloride was always greater than 5000 mg/kg BW. • Signs of toxicity observed at doses of 8000 mg/kg BW and above included prostration, depression, diarrhea, and convulsions.
  • 14. The new technique used in the manufacturing of LYNX OD tablet Coating involved special grade functional polymer forming a moisture barrier for the extended shelf life of the product Special grade very high viscosity polymer used for manufacturing of product ensures consistent and uniform release of the drug to maintain a reproducible plasma level for 24 hours Aqueous wet granulation technology involved in the manufacturing of tablets ensures better stability of the formulation
  • 15. Advantages of LYNX OD (LINCOMYCIN SR 1000 MG) tablet Patented product (first time in India) Improved patient compliance due to less frequent drug administration – once daily versus 2-3 times a day frequency for immediate release (IR) formulations Reduction of fluctuation in steady-state drug levels (BE compliance product) Increased safety margin of the potent drug by reducing peaks in drug levels following intake of each dose.
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