Drugs Containing Tylosin Active Ingredient, Indications, Drug Interactions

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Tilosin (Tylosin)

Macrolide antibiotic related to erythromycin, used primarily in cattle & swine; sometimes used orally in cats/dogs for chronic colitis; has been used anecdotally in cats as an immunomodulating agent for treating FIP.

Must be compounded for oral use in dogs and cats. Has a very unpleasant taste.

Contraindications: hypersensitivity to it or other macrolide antibiotics; probably contraindicated in horses.

Adverse Effects: Pain & local reactions after IM injection, GI upset (anorexia, & diarrhea) after PO administration. May cause severe diarrhea if administered PO to ruminants or by any route to horses. Swine: edema of rectal mucosa & mild anal protrusion with pruritus, erythema, & diarrhea.

Uses / Indications

Although the injectable form of tylosin was FDA-approved for use in dogs and cats, it is rarely used parenterally in those species. Oral tylosin is commonly recommended for the adjunctive treatment of inflammatory bowel disease (IBD; idiopathic antibiotic responsive diarrhea) in dogs, cats and some small mammals. A double-blinded prospective study, comparing tylosin to placebo in dogs with a history of chronic diarrhea that was thought to be responsive to tylosin in the past, showed that 85% of dogs receiving tylosin had perceived normal fecal consistency versus 29% of those receiving placebo (Kilpienn et al. 2009). A case-based review of the evidence for treatment of clinical signs (vomiting, diarrhea, weight loss) associated with mild lymphoplasmacytic, eosinophilic gastroenteritis, concluded that based upon current evidence, milder forms of IBD do not always require immunosuppression and can often be managed with a combination of diet change, antimicrobials (e.g., tylosin), and time (Smee et al. 2011).

Tylosin has been used has been used anecdotally in cats as an immunomodulating agent for treating FIP. In dogs, tylosin has been anecdotally used orally to treat tear staining (epiphora).

Tylosin is also used clinically in cattle and swine for infections caused by susceptible organisms but newer, approved antibiotics are generally preferred for systemic therapy.

Pharmacology / Actions

Tylosin is thought to have the same mechanism of action as erythromycin (binds to 50S ribosome and inhibits protein synthesis) and exhibits a similar spectrum of activity. It is a bacteriostatic antibiotic. Tylosin may also have immunomodulatory effects on cell-mediated immunity. Over 50% of Enterococcus faecalis canine isolates from healthy dogs were resistant to tylosin in one study. Tylosin may increase concentrations of enterococci in the jejunum, which may have probiotic effects (Suchodolski et al. 2009).

Pharmacokinetics

Tylosin tartrate is well absorbed from the GI tract, primarily from the intestine. The phosphate salt is less well absorbed after oral administration. Tylosin base injected SC or IM is reportedly rapidly absorbed.

Like erythromycin, tylosin is well distributed in the body after systemic absorption, with the exception of penetration into the CSF. The volume of distribution of tylosin is reportedly 1.7 L/kg in small animals and 1-2.3 L/kg in cattle. In lactating dairy cattle, the milk to plasma ratio is reported to be between 1-5.4.

Tylosin is eliminated in the urine and bile apparently as unchanged drug. The elimination half-life of tylosin is reportedly 54 minutes in small animals, 139 minutes in newborn calves, and 64 minutes in calves 2 months of age or older.

Contraindications / Precautions / Warnings

Tylosin is contraindicated in patients hypersensitive to it or other macrolide antibiotics (e.g., erythromycin). Most clinicians feel that tylosin is contraindicated in horses, as severe and sometimes fatal diarrheas may result from its use in that species.

Adverse Effects

Most likely adverse effects with tylosin are pain and local reactions at intramuscular injection sites, and mild GI upset (anorexia and diarrhea). Tylosin may induce severe diarrheas if administered orally to ruminants or by any route to horses. In swine, adverse effects reported include edema of rectal mucosa and mild anal protrusion with pruritus, erythema, and diarrhea.

Reproductive / Nursing Safety

In a system evaluating the safety of drugs in canine and feline pregnancy (Papich 1989), this drug is categorized as in class: B (Safe for use if used cautiously. Studies in laboratory animals may have uncovered some risk, but these drugs appear to be safe in dogs and cats or these drugs are safe if they are not administered when the animal is near term.)

Overdosage / Acute Toxicity

Tylosin is relatively safe in most overdose situations. The LD50 in pigs is greater than 5 grams/kg orally, and ≈ 1 gram/kg IM. Dogs are reported to tolerate oral doses of 800 mg/kg. Long-term (2 year) oral administration of up to 400 mg/kg produced no organ toxicity in dogs. Shock and death have been reported in baby pigs overdosed with tylosin, however.

Drug Interactions

Drug interactions with tylosin have not been well documented. It has been suggested that tylosin may increase digoxin blood levels with resultant toxicity. It is suggested to refer to the erythromycin monograph for more information on potential interactions.

BENTONITE: Simultaneous administration of tylosin (in the drinking water or feed) and bentonite (mixed in the feed as a mycotoxin binder) should be avoided as it significantly reduced tylosin plasma levels and area-under-the-curve in chickens. (Devreese et al. 2012)

Laboratory Considerations

Macrolide antibiotics may cause falsely elevated values of AST(SGOT), and ALT (SGPT) when using colorimetric assays.

Fluorometric determinations of urinary catecholamines can be altered by concomitant macrolide administration.

Doses

DOGS/CATS:

Note: When using Tylan® Soluble (100 grams per bottle) powder: Using volumetric containers to measure powders is not necessarily accurate, but 1 level teaspoonful (5 mL) of powder contains ≈ 2.5-2.7 grams of tylosin; 1/8th of a teaspoonful contains ≈ 325 mg tylosin. Powder is very unpalatable.

For adjunctive treatment of inflammatory bowel disease (IBD, idiopathic antibiotic responsive diarrhea); (extra-label):

a) Dogs: 25 mg/kg PO once daily (in the study dogs were treated for 7 days, but the authors state that in dogs with tylosin-responsive diarrhea the stool remains normal as long as treatment continues, but diarrhea reappears within weeks after discontinuation). (Kilpienn et al. 2009)

b) Other anecdotal dosage recommendations range from 10 – 40 mg/kg PO q8-12h. A recent review article suggested: 20 mg/kg PO q8-12h. There is no cure but signs may be controlled (Hall 2011). Milder cases with appropriate dietary change may eventually only require once daily dosing.

For campylobacteriosis (extra-label): 11 mg/kg PO q8h. (Weese 2011)

For Clostridium perfringens-associated diarrhea (extra-label): There is little objective information guiding decisions regarding when and how to treat, but tylosin at 10 – 20 mg/kg PO q12-24h is commonly recommended (Weese 2011). Animals with chronic clostridial colitis can often be controlled with one treatment every 2-3 days. (Willard 2006).

For Cryptosporidium spp. associated diarrhea in cats (extra-label): 10 – 15 mg/kg PO q12h will sometimes resolve diarrhea. Tylosin can be a GI irritant; if the cat is responding to the first 7 days of therapy and toxicity has not been noted, continue treatment for 1 week past clinical resolution of diarrhea. Some cats with Cryptosporidium spp. infection with or without Giardia co-infection require several weeks of treatment prior to resolution of diarrhea. (Lappin 2011)

FERRETS:

For susceptible enteric infections (extra-label): 10 mg/kg PO once to twice daily. (Williams 2000)

RABBITS, RODENTS, SMALL MAMMALS:

Rabbits: 10 mg/kg SC, IM q12-24h. (Ivey et al. 2000)

Gerbils, Hamsters, Rats: 10 mg/kg SC q24h. (Adamcak et al. 2000)

CATTLE:

For susceptible infections (labeled dose; FDA-approved): 17.6 mg/kg IM once daily. Continue treatment for 24 hours after symptoms have stopped, not to exceed 5 days. Do not inject more than 10 mL per site. Use the 50 mg/mL formulation in calves weighing <200 pounds. (Package insert; Tylosin® Injection)

SWINE:

For susceptible infections (labeled dose; FDA-approved): 8.8 mg/kg IM twice daily. Continue treatment for 24 hours after symptoms have stopped, not to exceed 3 days. Do not inject more than 5 mL per site. (Package insert; Tylosin® Injection)

Monitoring

Clinical efficacy.

Adverse effects.

Client Information

Most commonly used in dogs and cats to treat diarrhea and inflammation of intestines; may be used for respiratory infections in birds (including chickens) and reptiles.

Do not give to horses or ponies.

Oral doses may be given with or without food. Give with food if stomach upset or vomiting occurs.

Powder has an extremely bitter taste. Placing the dose of powder in an empty gelatin capsule may be better accepted.

When administered orally to small animals, tylosin is usually very well tolerated, but contact veterinarian if adverse effects are seen.

Chemistry / Synonyms

A macrolide antibiotic related structurally to erythromycin, tylosin is produced from Streptomyces fradiae. It occurs as an almost white to buff-colored powder with a pKa of 7.1. It is slightly soluble in water and soluble in alcohol. Tylosin is considered highly lipid soluble. The tartrate salt is soluble in water. The injectable form of the drug (as the base) is in a 50% propylene glycol solution.

Tylosin may also be known as desmycosin, tilosina, tylozin, tylosiini, tylosinum, tylozyna or Tylan®.

Storage / Stability

Unless otherwise instructed by the manufacturer, injectable tylosin should be stored in well-closed containers at room temperature. Tylosin, like erythromycin, is unstable in acidic (pH <4) media. It is not recommended to mix the parenteral injection with other drugs.

Compatibility / Compounding Considerations

Because converting volume measurements into weights is not very accurate for powders, it is recommended to actually weigh powders when using them for pharmaceutical purposes. However, if this is not possible, one (1) level teaspoon (5 mL) of commercially available tylosin tartrate (Tylan® Soluble) contains ≈ 2.5-2.7 grams of tylosin; 1/8th of a teaspoonful contains ≈ 325 mg tylosin.

Tylan tartrate powder added to food can be very unpalatable for dogs or cats. Placing the proper dose in a gelatin capsule may be preferable to mixing it into food. Another suggestion for dogs or cats that absolutely won’t eat food that has tylosin in it is to: Melt ≈ ¼ teaspoon of butter and place in one of the compartments in a mini-ice tray. Add the proper dose of tylosin powder, mix well and freeze. (Note: Stability information for this procedure has not been performed).

Dosage Forms / Regulatory Status

VETERINARY-LABELED PRODUCTS:

Note: The product Tylan® Plus Vitamins was used extensively orally in companion animals, but has been withdrawn from the market. Tylan® Soluble may be substituted, but is significantly more concentrated than Tylan® Plus Vitamins and dosage sizes (teaspoons are not equivalent) will be different.

Tylosin Injection: 50 mg/mL, 200 mg/mL; Tylan®, generic; (OTC). FDA-approved for use in nonlactating dairy cattle, beef cattle, swine, dogs, and cats. Slaughter withdrawal (at labeled doses): cattle = 21 days; swine = 14 days. Note: Although this author (Plumb) was unable to locate parenteral products FDA-approved for use in lactating dairy animals, one source (Huber 1988a) states that tylosin has a 72-hour milk withdrawal for dairy cattle, and 48 hour milk withdrawal in dairy goats and sheep. Contact FARAD for more information before using in lactating dairy animals.

Tylosin Tartrate Powder: (≈ 2.5-2.7 grams/level teaspoonful) in 100 gram bottles; Tylan® Soluble, TyloMed®-WS; (OTC). FDA-approved for use in turkeys (not layers), chickens (not layers) and swine. Slaughter withdrawal swine = 2 days; chickens = 1 day; turkeys = 5 days.

There are many FDA-approved tylosin products for addition to feed or water for use in beef cattle, swine, and poultry. Many of these products have other active ingredients included in their formulations.

HUMAN-LABELED PRODUCTS: NONE.

References / Revisions

Monograph revised/updated August 2014.

Adamcak, A. & B. Otten (2000). Rodent Therapeutics. Vet Clin NA: Exotic Anim Pract 3:1(Jan): 221-40.

Devreese, M., et al. (2012). Interaction between tylosin and bentonite clay from a pharmacokinetic perspective. Veterinary Journal 194(3): 437-9.

Hall, E. J. (2011). Antibiotic-Responsive Diarrhea in Small Animals. Veterinary Clinics of North America-Small Animal Practice 41(2): 273-+.

Ivey, E. & J. Morrisey (2000). Therapeutics for Rabbits. Vet Clin NA: Exotic Anim Pract 3:1(Jan): 183-216.

Kilpienn, S., et al. (2009). Effect of Tylosin on Dogs with Diarrhea: A Placebo-Controlled, Randomized, Double-Blinded, Prospective Clinical Trial. Proceedings: ECVIM. Accessed via Veterinary Information Network; vin.com

Lappin, M. R. (2011). Diagnosis and Treatment of Cryptosporidium and Isospora in Cats. Proceedings: World Small Animal; Veterinary Association World Congress. Accessed via Veterinary Information Network; vin.com

Papich, M. (1989). Effects of drugs on pregnancy. Current Veterinary Therapy X: Small Animal Practice. R. Kirk. Philadelphia, Saunders: 1291-9.

Smee, N. M. & T. L. Towell (2011). What Is the Evidence? Journal of the American Veterinary Medical Association 238(9): 1111-3.

Suchodolski, J. S., et al. (2009). The Effect of Tylosin on Small Intestinal Microbiota in Healthy Dogs. Proceedings: ECVIM. Accessed via Veterinary Information Network; vin.com

Weese, J. S. (2011). Bacterial Enteritis in Dogs and Cats: Diagnosis, Therapy, and Zoonotic Potential. Veterinary Clinics of North America-Small Animal Practice 41(2): 287-+.

Willard, M. (2006). Chronic Diarrhea: Part 2. Proceedings: ACVC. Accessed via Veterinary Information Network; vin.com

Williams, B. (2000). Therapeutics in Ferrets. Vet Clin NA: Exotic Anim Pract 3:1(Jan): 131-53.

İlaçlar (36)

Medicines containing Tylosin active ingredient

AVİLOSİNE

Tilosin (Tylosin)

AVİTAYLO %30

Tilosin (Tylosin)

BİO-TYLOS

Tilosin (Tylosin)

EKOTAY 200

Tilosin (Tylosin)

HİPRATYL

Tilosin (Tylosin)

MEDİCATAY

Tilosin (Tylosin)

MYCOSİD

Tilosin (Tylosin)

PHARMACİN

Tilosin (Tylosin)

PHARMASIN %100

Tilosin (Tylosin)

PHARMASIN %25/VİP

Tilosin (Tylosin)

PHARMASİN 200

Tilosin (Tylosin)

TAVİLİN

Tilosin (Tylosin)

TAVİLİN 200

Tilosin (Tylosin)

TAYLOMİSİN

Tilosin (Tylosin)

TAYLOMİSİN 200

Tilosin (Tylosin)

TAYLOSOL

Tilosin (Tylosin)

TAYLOVİM

Tilosin (Tylosin)

TAYLOVİM %30

Tilosin (Tylosin)

TAYMAVET-200

Tilosin (Tylosin)

TAYMAVET-50

Tilosin (Tylosin)

TEKNOTİL

Tilosin (Tylosin)

TEKNOTİL 200

Tilosin (Tylosin)

TİLOSEPTİN

Tilosin (Tylosin)

TİLOSİNA 200 GANADEXİL

Tilosin (Tylosin)

TYFORCE

Tilosin (Tylosin)

TYLARON 200

Tilosin (Tylosin)

TYLOCEL 200

Tilosin (Tylosin)

TYLOCURE

Tilosin (Tylosin)

TYLOMİS 200

Tilosin (Tylosin)

TYLONET %30

Tilosin (Tylosin)

VET-TYLO

Tilosin (Tylosin)

VITAYLOZIN

Tilosin (Tylosin)

TAY-MAX

Tilosin (Tylosin)

TYLOFARM

Tilosin (Tylosin)

TİLOTARMED %20

Tilosin (Tylosin)

TYLOFARM TOZ

Tilosin (Tylosin)

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