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Tylosin
Systematic (IUPAC) name
[(2R,3R,4E,6E,9 R,11R,12S,13S,14R) -12- {[3,6-dideoxy-4-O-(2,6-dideoxy-3-C-methyl-α- L-ribo-hexopyranosyl) -3- (dimethylamino)-β-D-glucopyranosyl]oxy}-2-ethyl-14-hydroxy-5, 9,13-trimethyl-8, 16-dioxo-11-(2-oxoethyl)oxacyclohexadeca-4,6-dien-3-yl]methyl 6-deoxy-2,3-di-O-methyl-β-D-allopyranoside
Identifiers
CAS number 1401-69-0
ATCvet code QJ01FA90 QJ51FA90
PubChem 5280440
Chemical data
Formula C 46H77NO17  
Mol. mass 916.10 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Tylosin is a macrolide-class antibiotic used in veterinary medicine. It has a broad spectrum of activity against gram positive organisms and a limited range of gram negative organisms.[1] It is found naturally as a fermentation product of Streptomyces fradiae.[2]

Tylosin is used in veterinary medicine to treat bacterial infections in a wide range of species and has a high margin of safety.[3] It has also been used as a growth promotant in some species, and as a treatment for colitis in companion animals.[2]

Contents

Mode of action

Like other macrolides, tylosin has a bacteriostatic effect on susceptible organisms, caused by inhibition of protein synthesis through binding to the 50S subunit of the bacterial ribosome.

Spectrum of activity

Tylosin has a wide spectrum of activity against gram positive bacteria including Staphylococci, Streptococci, Corynebacteria, and Erysipelothrix. It has a much narrower gram negative spectrum of activity, but has been shown to be active against Campylobacter coli, and certain spirochaetes.[4] It has also been shown to be extremely active against Mycoplasma species isolated from both mammalian and avian hosts.[3][5]

Clinical use

Tylosin has been used to treat a variety of different diseases throughout the world. Differing formulations and licensing conditions will mean that it may not be a recognized method of treatment for certain conditions in certain countries. In general, tylosin is licensed for the treatment of infections caused by organisms susceptible to the drug, but it has also been used as a treatment of colitis in small animals, as a growth promotant in food producing animals, and as a way of reducing epiphora (tear staining) around the eyes of white faced dogs.[2] It should be noted that no marketing authority exists for the use of tylosin as a tear stain remover and thus it is not legal to use it for such purposes- the exception being as a Prescription Only Medicine of last resort by vets under the Cascading Rule (UK) or the Extra Label rule (US).

Examples of bacterial infections that could potentially be treated with tylosin include respiratory infections, metritis, and acute mastitis in cattle; mastitis in sheep and goats; enteritis, pneumonia, erysipelas, and infectious arthritis in swine; and soft tissue infections in small animals.[1][2][4][5] While tylosin may be one appropriate therapeutic choice in theory for the conditions listed above, there are many other antibiotics that may be preferable for treating a specific infection, and Tylosin will not be the first choice.

It is also used as a growth promoter for a variety of terrestrial and aquatic animals grown for human consumption(Hirsch et al. 1999)

Available forms

Tylosin is available in injectable, intramammary, and oral formulations with different product ranges available in different countries.[1]

Precautions and contraindications

Administration of tylosin should be avoided in animals with a known hypersensitivity to the product, or to other macrolides.[5]

Oral administration can result in diarrhoea and gastrointestinal disturbance. This is particularly true of horses, such that it can be fatal.[6] Tylosin also has a foul taste that is difficult to disguise.

The injectable formulations of tylosin can cause pain, inflammation, and itchiness around the injection site.

Since tylosin has a relatively poor spectrum of activity against gram negative organisms, it may not be a sensible therapeutic choice in the treatment of infections caused by unknown, potentially unsusceptible organisms.

Drug interactions

Tylosin may increase digitalis blood levels and thus its toxicity,[5] and may be antagonistic to chloramphenicol or lincosamides.

Colorimetric assays of serum ALT and AST may be falsely elevated by macrolide antibiotics.

References

  1. ^ a b c Antimicrobial Therapy in Veterinary Medicine, by Steeve Giguere, P. M. Dowling, ISBN 9780813806563
  2. ^ a b c d Tylosin, marvistavet.com
  3. ^ a b Tylan 200 Injectable - Product data sheet PA9063DENZP - Elanco Animal Health
  4. ^ a b Tylosin, drugs.com
  5. ^ a b c d Tylosin-Tylan, petplace.com
  6. ^ Tylan, americanlivestock.com

Hirsch R, Ternes T, Haberer K, Kratz KL (1999). Occurrence of antibiotics in the aquatic environment. The Science of the total environment, 225:109-118.








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