Proligeston
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| Non-proprietary name | Proligeston | |||||||||||||||
| other names |
14 α , 17 α -propylidenedioxyprogesterone |
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| Molecular formula | C 24 H 34 O 4 | |||||||||||||||
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| Drug class |
Anti-gestation |
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| Molar mass | 386.52 g · mol -1 | |||||||||||||||
| Physical state |
firmly |
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| Melting point |
150-155 ° C |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||
Proligeston (trade name Delvosteron ® ) is a progestogen , i.e. a hormonally active drug with a gestagenic effect. It is used in veterinary medicine, especially for suppressing heat in domestic dogs or heat cycle in domestic cats used.
Chemical properties
Proligeston is a powder that is hardly soluble in water. The oral LD 50 in rats is above 2000 mg kg −1 .
Mechanism of action
Proligeston binds to progesterone receptors with high affinity . But it has only a low progesterone effect and increases the secretion of the glands in the uterus . The gonadotropin- inhibiting effect also arises from the interaction with the progesterone receptors . In addition, Proligeston also binds to glucocorticoid receptors and has a clear glucocorticotropic effect. It also stimulates the formation of growth hormone in the mammary gland .
Proligeston is slowly absorbed when administered subcutaneously . The absorbed active ingredient is broken down relatively quickly in the liver and excreted in the bile and finally in the faeces. The depot effect is based on the slow absorption into the body.
application
When used to suppress oestrus , the drug should be applied in the anestrus or metestrus , here there is an efficacy of about 98%. In contrast to other gestagens, it can also be used in the beginning proestrus, the success rate is then still 95%. A subsequent injection is indicated after three months in order to safely prevent the next cycle. Overall, however, the sexual cycle should be blocked for a maximum of two years; castration is definitely more advisable for a permanent breakdown of the sexual cycle.
It can also be used for skin diseases caused by hormonal disorders and for pseudopregnancy . According to the manufacturer, it can also be used in male animals with hypersexuality , although an anti- androgenic effect has not yet been proven.
Contraindications and side effects
The drug must not be used in diabetes mellitus (diabetes), endometritis (inflammation of the lining of the uterus ), mammary tumors , pregnancy and before sexual maturity.
The side effects are significantly lower with Proligeston than with the use of other gestagens.
Proligeston should not be used in breeding animals as there is a risk of developing glandular-cystic hypertrophy of the endometrium , endometritis or even pyometra .
Long-term treatment can result in insulin resistance and thus diabetes as well as, due to the glucocorticoid effect, atrophy of the adrenal cortex and Cushing's syndrome . Benign tumors of the breasts and acromegaly due to the effects of growth hormone may also develop.
Other side effects are local pain symptoms, possibly also permanent skin and coat changes (discoloration, hair loss ) at the injection site.
Individual evidence
- ↑ a b Entry on Proligeston at Vetpharm, accessed on August 11, 2012.
- ↑ a b Safety Data Sheet Proligestone. Biosynth Carbosynth, April 20, 2020, accessed July 18, 2020 .
