Chemical formula: C₃₀H₃₇NO₄ Molecular mass: 433.592 g/mol PubChem compound: 13559281
Ulipristal interacts in the following cases:
In vivo results show that the administration of ulipristal acetate with a strong CYP3A4 inducer such as rifampicin markedly decreases Cmax and AUC of ulipristal acetate by 90% or more and decreases ulipristal acetate half-life by 2.2-fold corresponding to an approximately 10-fold decrease of ulipristal acetate exposure. Concomitant use of ulipristal with CYP3A4 inducers (e.g. barbiturates (including primidone and phenobarbital), phenytoin, fosphenytoin, carbamazepine, oxcarbazepine, herbal medicines containing Hypericum perforatum (St. John’s wort), rifampicin, rifabutin, griseofulvin, efavirenz and nevirapine) therefore reduces plasma concentrations of ulipristal acetate and may result in a decreased efficacy of ulipristal. For women who have used enzyme-inducing drugs in the past 4 weeks, ulipristal is not recommended and non-hormonal emergency contraception (i.e. a copper intrauterine device (Cu-IUD)) should be considered.
In vivo results show that administration of ulipristal acetate with a potent and a moderate CYP3A4 inhibitor increased Cmax and AUC of ulipristal acetate with a maximum of 2- and 5.9-fold, respectively. The effects of CYP3A4 inhibitors are unlikely to have any clinical consequences.
The CYP3A4 inhibitor ritonavir can also have an inducing effect on CYP3A4 when ritonavir is used for a longer period. In such cases ritonavir might reduce plasma concentrations of ulipristal acetate. Concomitant use is therefore not recommended. Enzyme induction wears off slowly and effects on the plasma concentrations of ulipristal acetate may occur even if a woman has stopped taking an enzyme inducer in the past 4 weeks.
Because ulipristal acetate binds to the progesterone receptor with high affinity, it may interfere with the action of progestogen-containing medicinal products. Contraceptive action of combined hormonal contraceptives and progestogen-only contraception may be reduced.
Administration of ulipristal acetate (10 mg) together with the proton pump inhibitor esomeprazole (20 mg daily for 6 days) resulted in approximately 65% lower mean Cmax, a delayed Tmax (from a median of 0.75 hours to 1.0 hours) and 13% higher mean AUC. The clinical relevance of this interaction for single dose administration of ulipristal acetate as emergency contraception is not known.
Concomitant use of ulipristal acetate and emergency contraception containing levonorgestrel is not recommended.
Use in women with severe asthma treated by oral glucocorticoid is not recommended.
Ulipristal acetate is not intended for use during pregnancy and should not be taken by any woman suspected or known to be pregnant.
Ulipristal acetate does not interrupt an existing pregnancy. Pregnancy may occasionally occur after ulipristal acetate intake. Although no teratogenic potential has been observed, animal data are insufficient with regard to reproduction toxicity. Limited human data regarding pregnancy exposure to ulipristal acetate do not suggest any safety concern.
Ulipristal acetate is excreted in breast milk. The effect on newborn/infants has not been studied. A risk to the breastfed child cannot be excluded. After intake of ulipristal acetate for emergency contraception, breast-feeding is not recommended for one week. During this time it is recommended to express and discard the breast milk in order to stimulate lactation.
A rapid return of fertility is likely following treatment with ulipristal acetate for emergency contraception. Women should be advised to use a reliable barrier method for all subsequent acts of intercourse until the next menstrual period.
Ulipristal acetate has minor or moderate influence on the ability to drive or use machines: mild to moderate dizziness is common after ulipristal acetate intake, somnolence and blurred vision are uncommon; disturbance in attention has been rarely reported. The patient should be informed not to drive or use machines if they are experiencing such symptoms.
The most commonly reported adverse reactions were headache, nausea, abdominal pain and dysmenorrhea.
Safety of ulipristal acetate has been evaluated in 4,718 women during the clinical development program.
The adverse reactions reported in the phase III program of 2,637 women are provided in the list below.
Adverse reactions listed below are classified according to frequency and system organ class using the following convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000) and not known (cannot be estimated from the available data).
Uncommon: Influenza
Uncommon: Appetite disorders
Common: Mood disorders
Uncommon: Emotional disorder, Anxiety, Insomnia, Hyperactivity disorder, Libido changes
Rare: Disorientation
Common: Headache, Dizziness
Uncommon: Somnolence, Migraine
Rare: Tremor, Disturbance in attention, Dysgueusia, Syncope
Uncommon: Visual disturbance
Rare: Abnormal sensation in eye, Ocular hyperaemia, Photophobia
Rare: Vertigo
Rare: Dry throat
Common: Nausea*, Abdominal pain*, Abdominal discomfort, Vomiting*
Uncommon: Diarrhoea, Dry mouth, Dyspepsia, Flatulence
Uncommon: Acne, Skin lesion, Pruritus
Rare: Urticaria
Common: Myalgia, Back pain
Common: Dysmenorrhea, Pelvic pain, Breast tenderness
Uncommon: Menorrhagia, Vaginal discharge, Menstrual disorder, Metrorrhagia, Vaginitis, Hot flush, Premenstrual syndrome
Rare: Genital pruritus, Dyspareunia, Ruptured ovarian cyst, Vulvovaginal pain, Hypomenorrhea*
Common: Fatigue
Uncommon: Chills, Malaise, Pyrexia
Rare: Thirst
* Symptom which could also be related to an undiagnosed pregnancy (or related complications)
The safety profile observed in women less than 18 years old in studies and post-marketing is similar to the safety profile in adults during the phase III program.
The adverse reactions spontaneously reported in post-marketing experience were similar in nature and frequency to the safety profile described during the phase III program.
The majority of women (74.6%) in the phase III studies had their next menstrual period at the expected time or within ± 7 days, while 6.8% experienced menses more than 7 days earlier than expected and 18.5% had a delay of more than 7 days beyond the anticipated onset of menses. The delay was greater than 20 days in 4% of the women.
A minority (8.7%) of women reported intermenstrual bleeding lasting an average of 2.4 days. In a majority of cases (88.2%), this bleeding was reported as spotting. Among the women who received ulipristal acetate in the phase III studies, only 0.4% reported heavy intermenstrual bleeding.
In the phase III studies, 82 women entered a study more than once and therefore received more than one dose of ulipristal acetate (73 women enrolled twice and 9 enrolled three times). There were no safety differences in these subjects in terms of incidence and severity of adverse reactions, change in duration or volume of menses or incidence of intermenstrual bleeding.
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