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Ulipristal acetate mechanism of action

Mechanism of action of ulipristal acetate.
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    1. The overview of ella ulipristal acetate
    Ella ulipristal acetate
    is a selective labelled progesterone receptor modulator. It has shown to prevent about 60% of expected pregnancies, which is comparable to the emergency contraception scheme with levonorgestrel.

    2. Ulipristal acetate Mechanism of action
    Ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. Ulipristal’s primary mechanism of action is thought to be inhibition or delay of ovulation. A single mid-follicular dose has been shown to suppress growth of lead follicles. Administration just before, or in some cases just after, the luteinising hormone surge can inhibit follicular rupture. Endometrial changes may also play a role. Early luteal administration of ulipristal results in delayed endometrial maturation and alterations in progesterone-dependent markers of implantation. A mid-luteal dose has been shown to induce early endometrial bleeding in a dose-dependent manner. It has been postulated that alterations to the endometrium may inhibit implantation by rendering the uterus less receptive to the trophoblast. However, it is not known if ulipristal has a direct endometrial effect or if the observed changes are a result of an ovarian effect.

    And someone ever done some researches about ulipristal acetate mechanism. 20 cases of women in fasting conditions were given single dose ella. The highest plasma concentration of Ulipristal acetate, active metabolites and single to methyl - ulipristal acetate were 176 and 69 ng/ml. And all of these achieved the highest in 0.9 and 1 hour. Just like the picture as follows:

    Single dose give 30 mg Ulipristal Acetate after Ulipristal Acetate and single to methyl - Ulipristal Acetate mean (plus or minus SD) plasma concentration - time graphics.

    3. Pharmacokinetics of ulipristal acetate
    Ulipristal acetate
    is metabolized in the liver, most likely by CYP3A4, and to a small extent by CYP1A2 and CYP2D6. The two main metabolites have been shown to be pharmacologically active, but less than the original drug. The main excretion route is via the faeces.

    But ulipristal acetate should not be taken by women with severe liver diseases because of its CYP mediated metabolism. And it has not been studied in women under the age of 18. So be careful if you are not more than 18 years old.

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