ellaOne® - (IR): composition and pharmaceutical form
The medicine comes as tablets for oral use. One tablet contains 30 mg of ulipristal acetate — this is the full dose for the course, and a second dose in the same cycle is not envisaged.
The tablet can be taken with food or independently of it. Its ingredients include lactose monohydrate, so the medicine is unsuitable for women with the rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome.
How ellaOne® - (IR) works
Ulipristal acetate is a synthetic selective modulator of progesterone receptors with high affinity for that receptor in humans. Its main mechanism of action is the inhibition or delay of ovulation. Pharmacodynamic data show that even when taken immediately before expected ovulation the medicine can delay the rupture of the follicle in some women.
Ulipristal also has high affinity for the glucocorticoid receptor, and its blockade was observed in animal experiments, but in humans with repeated doses of 10 mg a day no such action has been noted. Affinity for the androgen receptor is minimal, and for the oestrogen and mineralocorticoid receptors it does not exist in humans.
Indications
The medicine is used for emergency contraception within 120 hours (5 days) after unprotected intercourse or when the contraceptive method used has failed.
It is a remedy for isolated situations, not a replacement for ongoing contraception. After it is taken, the doctor always recommends choosing a reliable regular method of protection.
Method of use and dosage
One tablet is taken by mouth as early as possible and no later than 120 hours (5 days) after unprotected intercourse or the failure of the contraceptive method used. It can be taken on any day of the menstrual cycle, having first ruled out pregnancy. If vomiting begins within 3 hours of the dose, another tablet must be taken.
In impaired kidney function the dose does not need changing. Because studies are lacking, alternative doses in impaired liver function have not been established, and in severe impairment the medicine is not recommended. In girls before the onset of puberty ulipristal acetate is not used for emergency contraception. The safety and efficacy of a second dose within the same menstrual cycle have not been studied, so repeating the dose in that cycle is not recommended.
Contraindications
The medicine is not prescribed in case of hypersensitivity to ulipristal acetate or to any excipient, nor in pregnancy or suspected pregnancy.
Its use is not recommended in women with severe bronchial asthma insufficiently controlled by oral glucocorticoids, or together with emergency contraceptives containing levonorgestrel.
Special warnings and precautions
Emergency contraception does not always prevent pregnancy. There are no data on the efficacy of the medicine in women whose unprotected intercourse took place more than 120 hours before the tablet was taken. If the next period is more than 7 days late, if the bleeding at the expected time was unusual or if signs of pregnancy appear, a test should be done. With a pregnancy confirmed after the tablet, as with any other, the possibility of an ectopic pregnancy must be borne in mind — it can develop even while menstruation-like bleeding continues.
What happens to the cycle and to regular contraception
After the tablet the period may start a few days earlier or later than expected. In about 7% of women the bleeding came more than 7 days early, in 18.5% it was more than 7 days late, and in 4% the delay exceeded 20 days. Taking the tablet does not prevent continuing regular hormonal contraception, but it may weaken its contraceptive action. For that reason, after emergency contraception and until the start of the next menstrual cycle, it is recommended to use a reliable barrier method in addition during intercourse.
Drug interactions
Ulipristal acetate is metabolised by the CYP3A4 enzyme. Agents that increase its activity — rifampicin, phenytoin, phenobarbital, carbamazepine, ritonavir, St John's wort — lower the plasma concentration of ulipristal and with it the efficacy of the medicine, so such combinations are not recommended. Enzyme induction wears off slowly, and the influence persists even if the woman stopped taking such medicines in the last 2–3 weeks. Strong CYP3A4 inhibitors — ketoconazole, itraconazole, telithromycin, clarithromycin, nefazodone — may on the contrary increase exposure to ulipristal; the clinical significance of this is unknown.
Medicines that raise the pH of the stomach contents — proton pump inhibitors, antacids, H2 receptor antagonists — reduce the concentration of ulipristal and its efficacy, so taking them at the same time is not recommended. Because of its high affinity for the progesterone receptor, ulipristal may weaken the action of progestogen-containing products: both combined hormonal contraceptives and progestogen-only ones, as well as emergency contraceptives with levonorgestrel.
Pregnancy and breastfeeding
In pregnancy and suspected pregnancy the medicine is contraindicated. Data on the state of the foetus and the newborn after exposure to ulipristal acetate are very scarce: no teratogenic effect has been detected, but the results of animal studies are insufficient to assess reproductive toxicity.
Whether ulipristal acetate passes into human and animal breast milk is unknown. The substance is lipophilic and could in theory be excreted with the milk, and the risk to the child cannot be ruled out. For that reason, after taking the tablet, breastfeeding is not recommended for at least 36 hours.
Adverse effects
What women most often report are headache, nausea, abdominal pain and painful periods. The safety of ulipristal acetate was assessed in 4718 women during the clinical programme.
- common — headache, dizziness, mood changes, fatigue;
- common — nausea, abdominal pain and discomfort, vomiting;
- common — painful periods, pain in the pelvic area, increased breast tenderness;
- common — muscle and back pain;
- uncommon — emotional disturbances, restlessness, insomnia, increased activity, changes in libido, drowsiness, migraine, visual disturbances;
- uncommon — diarrhoea, dry mouth, dyspepsia, abdominal bloating, appetite disturbances, influenza;
- uncommon — heavy periods, intermenstrual bleeding, cycle disorders, vaginal discharge, vaginal inflammation, hot flushes, premenstrual syndrome, acne, skin changes, itching, chills, malaise, fever;
- rare — disorientation, tremor, disturbances of attention and taste, fainting, photophobia, urticaria, genital itching, pain during intercourse, rupture of an ovarian cyst, scanty and short periods.
After the tablet mild or moderate dizziness often occurs, drowsiness and blurred vision less often, and disturbances of attention have rarely been reported. The influence of the medicine on the ability to drive has not been specifically studied, but it may be small or moderate — worth bearing in mind before getting behind the wheel.
Overdose
Experience with ulipristal acetate overdose is limited. A small number of people received single doses of up to 200 mg, and no severe or serious adverse reactions were observed.
Even so, the recommended dose should not be exceeded: raising it does not improve the efficacy of emergency contraception.
How to get a prescription for ellaOne® - (IR) online
Ulipristal acetate is a prescription-only medicine, and time matters here: the efficacy is higher the earlier the tablet is taken after unprotected contact.
During the online consultation the doctor will clarify the timing, rule out contraindications, discuss interactions with the medicines you already take and, if there are no limitations, issue an electronic prescription — the medicine can be collected at a pharmacy with its code.
