Index
- Introduction: what is it?
- Dosage: how is it used and how does it work?
- Warnings and Precautions
- Interactions and side effects
- Pregnancy and breastfeeding
- Notes (validity, storage conditions)
Questions and answers
Introduction: what is it?
EllaOne is the so-called “5 days later pill” . It is an emergency contraceptive to be taken within 120 hours (5 days) of unprotected sexual intercourse or failure of another contraceptive method.
EllaOne belongs to the pharmacotherapeutic group of sex hormones and modulators of the genital system , emergency contraceptives. EllaOne is also used for the therapy and treatment of various diseases and pathologies such as endometriosis .
The active ingredient of EllaOne is Ulipristal acetate , a synthetic selective modulator of the progesterone receptor(Selective Progesterone Receptor Modulator or SPRM) derived from orally active 19-norprogesterone, which acts by binding with great affinity to the human progesterone receptor. These SPRMs are distinguished from progesterone and progestogens in that they have a different action depending on the tissues that express the progesterone receptor. This mixed action profile causes stimulation or inhibition of the receptor in a tissue-specific manner.
EllaOne is used for emergency contraception as it can inhibit or delay ovulation by blocking the increase in luteinizing hormone levels.(LH). Even when taken immediately before ovulation is expected (when LH levels have already started to rise), Ulipristal acetate is able to postpone follicle rupture for about 5 days in 8 out of 10 women .
Ulipristal acetate also has a great affinity for the glucocorticoid receptor , without however manifesting antiglucocorticoid effects in humans, even after repeated administration at a daily dose of 10 mg. Ulipristal acetate has low affinity for the androgen receptor and no affinity for human estrogen or mineralocorticoid receptors .
EllaOne has a great effectand the results obtained from two independent clinical studies show that with Ulipristal acetate the risk of pregnancy is significantly reduced compared to levonorgestrel (one of the active ingredients of the morning after pill, also used in hormone replacement therapy in postmenopausal women. Levonorgestrel is also the active ingredient contained in Norlevo , an emergency contraceptive to be used no later than 72 hours after unprotected sexual intercourse or in case of failure of the contraceptive method used).
EllaOne is dispensed as white tablets containing 30 mg of Ulipristal acetate . EllaOne is an over-the-counter drug, butnon-over-the-counter , for patients 18 years of age and older . It is subject to a medical prescription to be renewed from time to time for patients under the age of 18.
Dosage: how is it used and how does it work?
Posology : The treatment consists of one tablet to be taken orally as soon as possible and in any case no later than 120 hours (5 days) from unprotected sexual intercourse or the failure of another contraceptive method.
The tablet can be taken before or after meals at any time during the menstrual cycle .
If vomiting occurs within 3 hours of taking the tablet, a second tablet should be taken .
Ulipristal in high doses reduces the proliferation of cells of the uterine wall, although its most important action is that of inhibiting ovulation. The antiovulatory action is probably consequent to the inhibition of the release of LH by the hypothalamus-pituitary axis and to the follicle rupture induced by LH at the level of the ovary. A 30 mg dose of ulipristal inhibits ovulation when given up to 120 hours (5 days) after intercourse by preventing follicle rupture at or shortly after LH levels peak.
Ulipristal can also inhibit implantation of the fertilized egg in the endometrium, although it has not been confirmed whether this participates in the emergency contraceptive effect.. Ulipristal in low doses, taken after fertilization of the egg but before implantation, alters the normal functioning of progesterone receptors , thus blocking the ability of the mother’s innate immune system to become immunotolerant towards the embryo and thus leaving it free of attack the embryo itself in the implantation stage.
Ulipristal is at least as effective as Levonorgestrel when given up to 72 hours after unprotected intercourse, and maintains its effect up to 120 hours after intercourse (as opposed to Levonorgestrel which loses its action beyond 72 hours from unprotected intercourse). There are no data available on the effectiveness of Ulipristal acetate taken more than 120 hours (5 days) after unprotected intercourse.
In the event of delayed menstruation or in the presence of symptoms of pregnancy , pregnancy must be ruled out prior to administration of the tablet .
Warnings and Precautions
EllaOne is intended for occasional use only . EllaOne should never replace the use of regular birth control . In any case, women should be advised to use a regular method of contraception.
Ulipristal acetate is not intended for use in pregnancy and should not be taken by women who are actually or suspected to be pregnant . In any case, it does not interrupt an existing pregnancy.
Emergency contraception with EllaOne is not always effective in preventing pregnancy. There are no data available on the effectiveness of EllaOne in women who have had unprotected sex more than 120 hours before taking ellaOne.
Ulipristal acetate inhibits or delays ovulation. If ovulation has already occurred , it is no longer effective. As the timing of ovulation cannot be predicted, the tablet should be taken as soon as possible after unprotected intercourse.
After taking the tablet, menstruation may occur a few days earlier or later than expected. In about 7% of women, menstruation occurred more than 7 days earlier than the expected date. In 18.5% of women there was a delay of more than 7 days , while in 4% of patients the delay wasexceeded 20 days . In case of delay of more than 7 days in the onset of the next menstruation, if the bleeding of the expected menstruation is abnormal or if there are symptoms indicating pregnancy or in case of doubt, a pregnancy test should be performed, taking into consideration the possibility of an ectopic pregnancy . The presence of uterine bleeding does not exclude the possibility of an ectopic pregnancy. Women who become pregnant after taking Ulipristal acetate should contact their doctor .
Although some data seem to indicate that EllaOne may be less effective with increasing body weight or body mass index (BMI), emergency contraception should be taken as soon as possible after unprotected intercourse, regardless of weight. body or BMI .
Taking ulipristal acetate concomitantly with an emergency contraceptive containing levonorgestrel is not recommended.
EllaOne can reduce the contraceptive efficacy of a regular hormonal contraceptive . Consequently, if a patient wishes to initiate or continue the use of a hormonal contraceptive, she can do so after taking EllaOne, but the use of a barrier method is recommended.reliable until the onset of the next menstruation.
Ulipristal acetate is an emergency contraceptive which reduces the risk of pregnancy after unprotected intercourse, but does not confer contraceptive protection in subsequent intercourse , therefore women should be advised to use a method of reliable barrier (condom) until the next menstruation.
This medicine contains lactose . Patients with rare hereditary problems of galactose intolerance , the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Interactions and side effects
Before taking EllaOne together with other medicines it is advisable to ask your doctor or pharmacist to check that it is safe and not harmful to health. Interactions can occur when EllaOne is taken together with drugs that interfere with its metabolism. Ulipristal acetate is metabolised in the liver by an enzyme called cytochrome P450 3A4 (CYP3A4). Hence, molecules that influence the activity of this enzyme can alter the response to taking EllaOne.
Drugs that inhibit CYP3A4 activity (erythromycin, ritonavir) may increase the plasma concentration of Ulipristal and potentiate its activity, although the effects of CYP3A4 inhibitors are unlikely to have clinical consequences.
The in vivo results show that administration of Ulipristal acetate with a strong CYP3A4 inducer such as rifampicin reduces Ulipristal acetate levels by at least 90%, with a corresponding reduction in Ulipristal acetate exposure by approximately 10-fold.
Therefore, the concomitant use of EllaOne with CYP3A4 inducing drugs is not recommended (e.g. barbiturates(including primidone and phenobarbital), phenytoin, fosphenytoin, carbamazepine, oxcarbazepine, herbal medicines containing Hypericum perforatum ( St. John’s wort or St. John’s wort ), rifabutin, griseofulvin, efavirenz, nevirapine) due to their interaction which may cause decreased levels of Ulipristal resulting in a possible reduction in the effectiveness of EllaOne.
The CYP3A4 inhibitor ritonavir may also have an inducing effect on CYP3A4 when used for a prolonged period. In such cases, ritonavir may reduce the plasma concentrations of Ulipristal acetate. Concomitant use of ritonavir and EllaOne is therefore not recommended.
The induction of the enzyme wears off slowly and the effects on the plasma concentration of Ulipristal acetate may occur even if the woman has stopped taking an inducer of the enzyme within the last 4 weeks. For women who have used the last 4 weeks medicines that act as enzyme inducers , EllaOne not you recommended and should be considered the use of a non-hormonal emergency contraception (ie, intrauterine copper, Cu-IUD).
Medicines affecting gastric pH. Concomitant administration of Ulipristal acetate with the proton pump inhibitor esomeprazole (20 mg daily for 6 days) resulted in a mean reduction in peak peak concentration of approximately 65%, a delay in absorption but with a slight increase in amount absorbed. The clinical relevance of this interaction for the administration of a single dose of ulipristal acetate as emergency contraception is unknown.
The use of EllaOne in women with severe asthma being treated with oral glucocorticoids is not recommended .
Since Ulipristal acetate binds with great affinity to the progesterone receptor, it may interfere with the action of progestogen-containing medicines. Contraceptive action of combined hormonal contraceptives and contraceptive based only progestin may be reduced.
The concomitant use of Ulipristal acetate and an emergency contraceptive method containing Levonorgestrel is not recommended.
Available data indicate that administration of Ulipristal acetate at clinically relevant concentrations does not alter the elimination of drugs metabolised by cytochromes CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4 and does not cause clinical consequences when administered with drugs that are substrates of P -glycoprotein (P-gp).
The most frequently reported adverse reactions were headache , nausea , abdominal pain and dysmenorrhea .
Ulipristal acetate has little effect on the ability to drive or use machines: dizziness is common after taking EllaOnemild to moderate; drowsiness and blurred vision are uncommon episodes; disturbances in attention have rarely been reported. The patient should be advised that she should not drive or operate machinery if she experiences such symptoms .
Experience of overdose with Ulipristal acetate is poor. Single doses of the drug up to 200 mg have been administered to women without safety concerns.
It is important to report the suspected adverse reactionsthat can occur after the marketing authorization of the drug, as this allows continuous monitoring of the benefit / risk ratio of the drug itself. Healthcare professionals, but also patients, are asked to report any suspected adverse reactions via the national reporting system at https://www.vigifarmaco.it/ .
Pregnancy and breastfeeding
Pregnancy
EllaOne is not intended for use during pregnancy and should not be taken by women who are actually or suspected to be pregnant.
Ulipristal acetate does not terminate an existing pregnancy .
After taking Ulipristal acetate may occasionally establishment a pregnancy . Although no teratogenic potential was found, the results obtained in animal species are insufficient for a clear assessment of reproductive toxicity. Limited data on human pregnancy exposure to EllaOne do not suggest safety concerns, but it is important that any pregnancies of women who have taken EllaOne are reported.on the drug manufacturer’s website www.hra-pregnancy-registry.com . The purpose of this web log is to collect safety information from women who have taken ellaOne during pregnancy or who have become pregnant after taking EllaOne. All collected patient data will remain anonymous .
Feeding time
Ulipristal acetate is excreted in breast milk . The effect on newborns / infants has not been studied. A risk to the breast-fed infant cannot be excluded. After taking Ulipristal acetate for emergency contraception, the ‘ feeding with breast milk does not it recommended for a week . During this period, the mother is recommended to take milk from the breast and discard it to keep milk production active.
Fertility
A rapid return to fertility is expected after treatment with Ulipristal acetate as an emergency contraceptive . Therefore, women should be advised to use a reliable barrier method for all subsequent sexual intercourse up to the next menstruation.
Notes (validity, storage conditions)
EllaOne tablets are valid for 3 years and should be stored below 25 ° C in their original packaging to protect the medicine from moisture and light.
Questions and answers
CAN I BLEED AFTER TAKING ELLAONE?
A minority (about one in ten) of women reported intermenstrual bleeding for an average of 2-3 days. In the majority of cases (9 out of 10) the bleeding was described as spotting.
CAN IT ALSO BE TAKEN TWICE A DAY?
The day pill is a means of remedying emergency situations and should not be considered a contraceptive of continuous use. The assumption of two doses at short intervals is however possible in particular cases, without a specific concern about possible side effects. The influence on the next menstrual cycle may be null or cause some small delay or advance, depending on the biochemical-hormonal characteristics of each woman.
IN WHICH CASES SHOULD I USE ELLAONE INSTEAD OF THE PROGESTOGEN PILL?
EllaOne is at least as effective as levonorgestrel (a progestin) when given up to 72 hours after unprotected intercourse, and maintains its effect for up to 120 hours after intercourse (as opposed to progestogen which loses its action beyond 72 hours from an unprotected relationship). Therefore, ellaOne should be used if unprotected intercourse has occurred for more than 72 hours (3 days), but within 120 hours (5 days).
