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Lincosamides are antibiotics used mainly to treat G + infections. These include lincomycin and clindamycin. Older lincomycin is no longer used in practice.

Mechanism of action[edit | edit source]

Lincosamides inhibit protein synthesis by binding to the 50S subunit of the ribosome.

Antimicrobial spectrum[edit | edit source]

It acts mainly on G + bacteria such as staphylococci and streptococci. They are also effective against anaerobes, some G− rods. Clostridium difficile, Neisseria, hemophilia and others are resistant.

Pharmacokinetics[edit | edit source]

Clindamycin after administration absorbs well. Penetrates body fluids and tissues, including bones. However, the penetration into the cerebrospinal fluid is small. It is excreted by the kidneys.

Pharmacodynamics[edit | edit source]

The effect of clindamycin is independent of concentration.

Resistance[edit | edit source]

The mechanism of resistance is the modification of ribosomes.

Indication[edit | edit source]

  • Β-lactam variant in patients with hypersensitivity to penicillin.
  • Treatment of G + and anaerobic infections. Osteomyelitis caused by S. aureus, infections of joints and tendons. Infections insensitive to other antistaphylococcal antibiotics.
  • Hospital use in patients with bone and soft tissue infections (intra-abdominal mixed aerobic anaerobic infections in combination with aminoglycosides) mainly in infections that have arisen in connection with abdominal surgery.
  • Locally in acne vulgaris.


Clindamycin[edit | edit source]

Clindamycin is one of lincosamides, which are antibiotics used as an alternative in the treatment of infections caused by gram-positive and anaerobic bacteria in patients hypersensitive to penicillins or other β-lactam antibiotics.

Mechanism of action[edit | edit source]

It consists in inhibiting proteosynthesis by binding to the 50S subunit of ribosomes of susceptible bacteria.

Spectrum[edit | edit source]

  • Anaerobic bacteria - Bacteroides fragilis, Actinomyces species, Propionibacterium acnes, Fusobacterium species, Clostridium perfringens
  • Clostridium difficile is always resistant
  • Gram-positive bacteria - Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae
  • Other microorganisms - Pneumocystis carinii, Plasmodium species

Resistance[edit | edit source]

  • The inability of a microorganism to take up an antibiotic (due to the increased ability of the drug to efflux from the cell).
  • Decreased affinity of ribosome binding sites based on genetic modification of the 50S subunit.
  • Bacterial cell esterase production.
  • These enzymes subsequently break down the antibiotic molecule and thus inactivate it.
  • There is cross-resistance between clindamycin and macrolides.

Pharmacokinetics[edit | edit source]

Absorption[edit | edit source]

  • After oral administration, it is well absorbed even in the presence of food.
  • For severe infections, it can also be given parenterally.
  • It has up to 90% bioavailability.

Distribution[edit | edit source]

  • Clindamycin has a relatively high volume of distribution - about 1.1 l / kg.
  • Up to 93% of the absorbed dose is bound to plasma proteins.
  • In sufficient concentrations, it penetrates most tissues and body fluids, including bones and abscesses.
  • Penetration into the cerebrospinal fluid is not sufficient even in inflammation (which usually increases the permeability of the blood-brain barrier).

Metabolism and excretion[edit | edit source]

  • It undergoes oxidative metabolism in the liver and metabolites are excreted by glomerular filtration.
  • The half-life of clindamycin is approximately 3 hours, but is prolonged in patients with liver or kidney disease (dose adjustment required).

Side effects[edit | edit source]

  • Rash: up to 10% of patients.
  • Pseudomembranous colitis with overgrowth of Clostridium difficile - if present, vancomycin or metronidazole are given.
  • Indigestion. Inhibition of neuromuscular transmission - increases the effect of muscle relaxants.

Dosing strategies[edit | edit source]

Clindamycin is one of the antibiotics with a concentration-independent effect. The goal of dosing is to maintain effective concentrations above the MIC (minimum inhibitory concentration) of susceptible microorganisms for at least 50% of the dosing interval, which is 6-8 hours.

Clinical indications[edit | edit source]

  • Intra-abdominal and pelvic infections with presumed involvement of anaerobic bacteria - peritonitis, abscesses, septic abortion.
  • Staphylococcal and streptococcal osteomyelitis.
  • Diabetic foot infection (in combination with antibiotics effective against aerobic gram-negative sticks).
  • Severe infections caused by Streptococcus pyogenes - necrotizing fasciitis, myositis, toxic shock. Severe streptococcal and staphylococcal cellulitis.
  • Severe orofacial inflammation, including retropharyngeal abscess.
  • Prevention of bone inflammation in dental surgery.
  • Acne vulgaris - topical administration. Aerobic vaginitis caused by streptococci, staphylococci, enterococci, E.coli - topical administration (vaginal tablet or cream)

Odkazy[edit | edit source]

Links[edit | edit source]

Související články[edit | edit source]

Reference[3][edit | edit source]

  1. LINCOVÁ, Dagmar and Hassan FARGHALI, et al. Basic and applied pharmacology. 2nd edition. Prague: Galén, 2007.  ISBN 978-80-7262-373-0 . ↑ a bSkočit nahoru k: MARTÍNKOVÁ, Jiřina, Stanislav MIČUDA and Jolana CERMANOVÁ, et al. Selected chapters from clinical pharmacology for bachelor study  [online]. © 2005. [feeling. 2010-08-14]. < >.

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