Canis ISSN: 2398-2942

Osaterone acetate

Synonym(s): 2-oxachloromadinone acetate, Ypozane

Contributor(s): Linda Horspool

Introduction

Name

  • Osaterone acetate.

Class of drug

  • Steroidal androgen antagonist.

Description

Chemical name

  • Osaterone acetate.

Molecular formula

  • 17±-acetoxy-6-chloro-2-oxa-4,6-pregnadiene-3,20-dione.

Molecular weight

  • 406.8998.

Physical properties

  • Log octanol-water partition coefficient 2.72.
  • Water solubility estimate 13.26 mg/L at 25°C.

Storage requirements

  • Shelf-life: 3 years.
  • This veterinary medicinal product does not require any special storage conditions.

Uses

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Indications

  • For the treatment of benign prostatic hypertrophy (BPH Prostate: benign hyperplasia and hypertrophy ) in male dogs.
    • BPH is an increase in size or non-malignant hypertrophy of the prostate and is the most common disease of the prostate in entire male dogs.
    • The increase in prostate size is caused by changes in the ratio of androgens, like testosterone and estrogens.
    • Many dogs are asymptomatic but clinical signs can result when there is a large degree of prostate hyperplasia.
    • Treatment aims to decrease the size of the prostate gland and thus alleviate clinical signs (such as constipation and difficulty in urinating).

Administration

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Pharmocokinetics

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Precautions

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Interactions

with other drugs

  • Osaterone is highly plasma protein bound (90% (87-92%) for the parent compound and to a lesser extent (around 80%) for the main metabolite).
  • There appear to be no interactions with other highly protein bound agents, such as diazepam Diazepam or phenylbutazone Phenylbutazone.

with diagnostic tests

  • Osaterone acetate does not have mineralocorticoid activity and has low affinity with glucocorticoid receptors, but the metabolite PB-4 (11-OH) might cause transient adrenosuppressive effects.
  • A transient decrease of plasma cortisol was noted during treatment with 0.5 mg osaterone/kg/day.
  • The response to an ACTH stimulation test ACTH stimulation test may also be suppressed for several weeks after administration of osaterone.
    o These effects can persist for a number of weeks after treatment, without clinical signs.

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references fromPubMed.
  • Albouy M, Sanquer A, Maynard L and Eun H (2008)Efficacies of osaterone and delmadinone in the treatment of benign prostatic hyperplasia in dogs.Vet Rec163, 179-183PubMed.
  • Hidenori N, Katsuhiro K, Koichi M, Sachiko S, Satoshi I, Kunio T, Shigehisa T and Masatoshi T (2000)The serum concentrations of osaterone acetate and metabolite after single and repeated oral administration of osaterone acetate tablet to dogs.Jap Pharm & Therap28(3), 213-129.
  • Minato K, Honma S, Shinohara Y and Hashimoto T (2005)Metabolism of osaterone acetate in dogs and humans.Steroids70(9), 563-572PubMed.
  • Minato K, Koizumi N, Honma S, Tsukamoto K and Iwamura S (2002)Pharmacokinetics and biliary excretion of osaterone acetate, a new steroidal antiandrogen, in dogs.Drug Metab Disp30(2), 167-172PubMed.
  • Tsutsu T, Hori T, Shimizu M, Orima H, Kawakami E, Fukuda S (2000)Regression of prostatic hypertrophy by osaterone acetate in dogs.J Vet Med Sci62(10), 1115-1119PubMed.

Other sources of information


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