ellaOne®: composition and pharmaceutical form
ellaOne® is a tablet containing 30 mg of ulipristal acetate. The pack holds a single tablet, and that reflects the essence of the medicine: it is meant for one dose in a particular situation, not for a course.
The tablet can be taken with or without food. Among its ingredients is lactose monohydrate, so women with the rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome should not take it.
How ellaOne® works
Ulipristal acetate is an oral synthetic selective progesterone receptor modulator with high affinity for that receptor in humans. Its main mechanism is the suppression or delay of ovulation. Pharmacodynamic data show that even when taken immediately before expected ovulation the medicine can, in some women, delay the rupture of the follicle.
Ulipristal also has high affinity for the glucocorticoid receptor: in animal experiments its blockade was observed, but in humans, with repeated doses of 10 mg a day, no such influence was noted. Its affinity for the androgen receptor is minimal, and for the oestrogen and mineralocorticoid receptors it is absent in humans.
Indications
ellaOne® is used for emergency contraception within 120 hours, that is 5 days, after unprotected intercourse or when the contraceptive method used has failed.
It is a remedy for isolated, rare situations. Under no circumstances does it replace a regular contraceptive method, and after its use the doctor should help choose ongoing protection.
Method of use and dosage
One tablet is taken by mouth as early as possible and no later than 120 hours after unprotected intercourse. It can be taken on any day of the menstrual cycle, but pregnancy must be ruled out beforehand. If vomiting occurs within 3 hours of the dose, another tablet is taken.
In impaired kidney function the dose does not need changing. For patients with impaired liver function alternative doses cannot be established — the relevant studies have not been carried out — and in severe hepatic impairment the medicine is not recommended. In girls before puberty it is not used for emergency contraception. A second dose within the same menstrual cycle is likewise not recommended: the safety and efficacy of such use have not been studied.
Contraindications
The list of contraindications is extremely short.
- hypersensitivity to ulipristal acetate or to any excipient;
- pregnancy, and also suspected pregnancy.
Special warnings and precautions
Emergency contraception does not always prevent pregnancy, and there are no data on the efficacy of the medicine in women whose unprotected intercourse took place more than 120 hours before the dose. If the next period is more than 7 days late, if the bleeding at the expected time looks unusual or if signs of pregnancy appear, a test should be done. With a confirmed pregnancy the possibility of an ectopic one should be borne in mind, as it can develop even alongside bleeding.
What matters after taking it
- taking the tablet does not prevent continuing regular hormonal contraception, but it may weaken its contraceptive effect;
- so until the start of the next cycle a reliable barrier method is needed during intercourse;
- simultaneous use of emergency contraceptives containing levonorgestrel is not recommended;
- repeated use within the same cycle has not been studied and is not recommended;
- in severe bronchial asthma insufficiently controlled by oral glucocorticoids the medicine is not recommended;
- the period may come earlier or later than expected: in about 7% of women it came more than 7 days early, in 18.5% it was more than 7 days late and in 4% more than 20 days late;
- after the dose mild or moderate dizziness often occurs, less often drowsiness and blurred vision and occasionally impaired attention, so the medicine may have a minor or moderate influence on the ability to drive and operate machinery.
Drug interactions
Ulipristal acetate is metabolised by the CYP3A4 enzyme, so agents that increase its activity — rifampicin, phenytoin, phenobarbital, carbamazepine, ritonavir, St John's wort — lower the plasma concentration of the medicine and its efficacy. Concomitant use is not recommended, and enzyme induction wears off slowly: the influence persists even if the woman stopped taking such agents in the last 2–3 weeks. Strong CYP3A4 inhibitors — ketoconazole, itraconazole, telithromycin, clarithromycin, nefazodone — on the contrary increase exposure, but the clinical significance of this is unknown.
Separately, medicines that raise the acidity of the stomach contents are worth remembering: proton pump inhibitors, antacids and H2 receptor antagonists lower the concentration of ulipristal and its efficacy, so they are not used at the same time. High affinity for the progesterone receptor also means the reverse influence: the medicine may disturb the action of progestogen-containing products, weakening the effect of both combined and progestogen-only hormonal contraceptives.
Pregnancy and breastfeeding
In pregnancy and where pregnancy is suspected the medicine is contraindicated. Data on the state of the foetus and the newborn after exposure to ulipristal are very scarce: no teratogenic effect has been detected, but the results of animal studies are insufficient to assess reproductive toxicity. The manufacturer maintains a pregnancy registry to follow outcomes in women who took the medicine.
Whether ulipristal acetate passes into 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 was assessed in 4718 women within the clinical development programme.
- common: headache, dizziness, nausea, abdominal pain and discomfort, vomiting;
- common in the genital sphere: painful periods, pelvic pain, breast tenderness;
- common, other: mood disturbances, muscle and back pain, fatigue;
- uncommon: emotional disturbances, restlessness, insomnia, increased activity, changes in libido, drowsiness, migraine, visual disturbances;
- uncommon in digestion and skin: diarrhoea, dry mouth, dyspepsia, abdominal bloating, acne, skin changes, itching;
- uncommon in the cycle: heavy periods, vaginal discharge, menstrual cycle disorders, intermenstrual bleeding, vaginitis, hot flushes, premenstrual syndrome;
- rare: disorientation, tremor, impaired attention and taste, fainting, urticaria, photophobia, dry throat;
- rare in the genital organs: itching of the external genitalia, pain during intercourse, rupture of an ovarian cyst, vaginal and vulvar pain, scanty and short periods.
Changes in the cycle itself — a shift in the timing of the period, its being heavier or lighter — are expected effects rather than complications. What should raise concern is a delay of more than 7 days: that is a reason to take a pregnancy test.
Overdose
Experience with ulipristal acetate overdose is limited. Single doses of up to 200 mg were given to a small number of people, and no severe or serious adverse reactions were observed.
Even so, more than one tablet should not be taken: raising the dose does not make the protection more reliable, and the safety of a second dose within one cycle has not been studied.
How to get a prescription for ellaOne® online
ellaOne® is a prescription-only medicine, and time here matters directly: the efficacy is higher the earlier the tablet is taken, and the limit is 120 hours. During the online consultation the doctor will clarify when the unprotected contact took place, rule out pregnancy and check the medicines you take that could weaken the effect of the product.
If the medicine is suitable, the doctor will issue an electronic prescription and explain what to do next: how to protect yourself until the end of the cycle and when to take a pregnancy test if the period is late.
