Aglepristone

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Aglepristone is a progesterone-receptor antagonist (antiorigestin) indicated for use in canine medicine for control of mesalliance (via termination of pregnancy), luteolysis of ovarian cysts[1] and induction of parturition[2].

Pharmacologically-induced luteolysis by antiprogestins in early post-implantation pregnancy in dogs results in asynchronous death and resorption of conceptuses[3].

This drug has also been safely used to minimize risks associated with early elective caesarian section[4].

Aglepristone is a synthetic steroid with anti-progesterone activity. It works by competitively binding with progesterone receptors and down-regulation of the corpus luteum[5], leading to luteolysis and cessation of pregnancy.

The use of intravaginal misoprostol[6] or dinoprost[7] facilitate pregnancy termination in resistant cases.

In vitro studies have demonstrated an affinity three times higher than that of progesterone receptor in the uterus of the bitch. In vivo studies in gestating rats demonstrate that a 10mg/kg dose by subcutaneous injection induced abortion in all treated animals. No anti-glucocorticoid effect was observed in the rat at doses ranging up to 30mg/kg over 4 days by the subcutaneous route[8].

After therapy with this drug, manual or ultrasonographic examination of the uterus should be performed to ensure uterine evacuation has occurred. In some cases, fetal retention may be an untoward complication[9]. Pregnancy termination can also be confirmed by blood measurement of progesterone (<2 ng/mL)[10].

Repeated use has been associated with development of pyometra[11].

Recommended dose rate in dogs is 10 mg/kg subcutaneously 24 hrs apart.

References

  1. Arlt SP et al (2011) Follicular cysts and prolonged oestrus in a female dog after administration of a deslorelin implant. N Z Vet J 59(2):87-91
  2. Fontbonne A et al (2009) Induction of parturition with aglepristone in various sized bitches of different breeds. Reprod Domest Anim 44(2):170-173
  3. Günzel-Apel AR et al (2009) Influence of progesterone withdrawal on pregnancy-related parameters during post-implantation early pregnancy loss. Reprod Domest Anim 44(2):174-181
  4. Levy X et al (2009) Elective caesarean operation in the bitch using aglepristone before the pre-partum decline in peripheral progesterone concentration. Reprod Domest Anim 44(2):182-184
  5. Balogh O et al (2012) Leptin and leptin receptor gene expression in the canine corpus luteum during diestrus, pregnancy and after aglepristone-induced luteolysis. Reprod Domest Anim 47(6):40-42
  6. Agaoglu AR et al (2011) The intravaginal application of misoprostol improves induction of abortion with aglepristone. Theriogenology 76(1):74-82
  7. Gogny A et al (2010) In vitro comparison of myometrial contractility induced by aglepristone-oxytocin and aglepristone-PGF2alpha combinations at different stages of the estrus cycle in the bitch. Theriogenology 74(9):1531-1538
  8. Virbac Package insert 1p0326-4
  9. Rigau T et al (2011) Partial foetal retention following aglepristone treatment in a bitch. Reprod Domest Anim 46(4):738-741
  10. Polisca A et al (2010) Aglepristone (RU534) administration to non-pregnant bitches in the mid-luteal phase induces early luteal regression. Theriogenology 74(4):672-681
  11. Pettersson CH & Tidholm A (2009) Safety and efficacy of mid-term pregnancy termination using aglepristone in dogs. J Small Anim Pract 50(3):120-123