Ulipristal Acetate

Registered South African indications:

• Emergency contraception within 120hrs (5 days) of unprotected sexual intercourse or contraceptive failure

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Porphyria

Cautions

• Pregnancy
  - Suspected pregnancy
• Breastfeeding
• Hepatic impairment
• Regular use
• Use more than 120hrs (5 days) after unprotected intercourse
• Increased body weight or body mass index (BMI)
• Severe asthma treated by oral glucocorticoid
• Coadministration with emergency contraception containing levonorgestrel
• Coadministration with CYP3A4 inducers
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab

Emergency contraception within 120 hours (5 days) of unprotected sexual intercourse or contraceptive failure 

• Oral (tab): 30mg, immediately as a single dose, but no later than 120hrs (5 days) after unprotected intercourse or contraceptive failure

Ulipristal acetate can be taken at any time during the menstrual cycle

If vomiting occurs within 3 hours of ulipristal acetate intake, another tablet should be taken

If a woman's menstrual period is late or in case of symptoms of pregnancy, pregnancy should be excluded before ulipristal acetate is administered

Paed. forms avail. in SA and covered in this monograph: tab

Emergency contraception within 120 hours (5 days) of unprotected sexual intercourse or contraceptive failure 

Children of prepubertal age

• Not indicated for use

Adolescents

• See adult dosage

Ulipristal acetate for emergency contraception is suitable for any woman of child bearing age, including adolescents. No differences in safety or efficacy have been shown compared to adult women aged 18 and older

Pregnancy

• Not indicated for use in pregnant women
• 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. Nevertheless, it is important that any pregnancy in a woman who has taken ulipristal acetate be reported

Breastfeeding

• Caution; not recommended
• 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, breastfeeding is not recommended for one week. During this time it is recommended to express and discard the breast milk in order to stimulate lactation

Fertility

• 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

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Caution; no information available
  Mild to moderate: In the absence of specific studies, no alternate dose recommendations for ulipristal acetate can be made
  Severe: In the absence of specific studies, ulipristal acetate is not recommended

Elderly

• Not indicated for use in geriatric patients
  Use is not indicated in postmenopausal women

Porphyria Information

• Probably porphyrinogenic (PRP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Mood disorders
• Emotional disorder
• Anxiety
• Insomnia
• Hyperactivity disorder
• Libido changes
• Disorientation
• Headache
• Dizziness
• Somnolence
• Migraine
• Tremor
• Disturbance in attention
• Syncope
• Fatigue

Respiratory Disorders

• Dry throat

Gastrointestinal Disorders

• Nausea and vomiting (could also be related to an undiagnosed pregnancy or related complications)
• Abdominal pain (could also be related to an undiagnosed pregnancy or related complications)
• Abdominal discomfort
• Diarrhoea
• Dry mouth
• Dyspepsia
• Flatulence

Genitourinary Disorders

• Dysmenorrhea
• Pelvic pain
• Breast tenderness
• Menorrhagia
• Vaginal discharge
• Menstrual disorder
• Metrorrhagia
• Vaginitis
• Hot flush
• Premenstrual syndrome
• Genital pruritus
• Dyspareunia
• Ruptured ovarian cyst
• Vulvovaginal pain
• Hypomenorrhea (could also be related to an undiagnosed pregnancy or related complications)

Endocrine and Metabolic Disorders

• Appetite disorders
• Chills
• Thirst

Musculoskeletal Disorders

• Myalgia
• Back pain

Skin and Subcutaneous Tissue Disorders

• Acne
• Skin lesion
• Pruritus
• Urticaria

Immune, Blood and Lymphatic System Disorders

• Influenza
• Fever

Sensory Disorders

• Dysgeusia
• Visual disturbance
• Abnormal sensation in eye
• Ocular hyperaemia
• Photophobia
• Vertigo

• CYP3A4 inducers
• Barbiturates
• Primidone
• Phenobarbital
• Phenytoin
• Fosphenytoin
• Carbamazepine
• Oxcarbazepine
• Rifampicin
• Rifabutin
• Griseofulvin
• Efavirenz
• Nevirapine
• CYP3A4 inhibitors
• Ritonavir
• Medicinal agents affecting gastric pH
• Proton pump inhibitors
• Esomeprazole
• Hormonal contraceptives
• Progestogen-containing medicinal products
• P-glycoprotein (P-gp) substrates
• Fexofenadine

Other interactions

• Hypericum perforatum (St. John's wort)

Specific cases may require

• Pregnancy test

Additional observations

• Evaluate for pregnancy or ectopic pregnancy (if menses are delayed by more than 1 week or presence of lower abdominal pain is reported or continuous irregular bleeding occurs)

Ulipristal acetate does not prevent pregnancy in every case

• In case the next menstrual period is >7 days late, if the menstrual period is abnormal in character or if there are symptoms suggestive of pregnancy or in case of doubt, a pregnancy test should be performed
• As with any pregnancy, the possibility of an ectopic pregnancy should be considered. It is important to know that the occurrence of uterine bleeding does not rule out ectopic pregnancy. Women who become pregnant after taking ulipristal acetate should contact their doctor
• Ulipristal acetate inhibits or postpones ovulation, if ovulation has already occurred, it is no longer effective. The timing of ovulation cannot be predicted and therefore the tablet should be taken as soon as possible after unprotected intercourse
• No data are available on the efficacy of ulipristal acetate when taken more than 120 hours (5 days) after unprotected intercourse
• Limited and inconclusive data suggest that there may be reduced efficacy of ulipristal acetate with increasing body weight or body mass index (BMI)
• In all women, emergency contraception should be taken as soon as possible after unprotected intercourse, regardless of the woman's body weight or BMI
• After the tablet intake menstrual periods can sometimes occur a few days earlier or later than expected
• In approximately 7% of the women, menstrual periods occurred more than 7 days earlier than expected. In 18.5% of the women a delay of more than 7 days occurred, and in 4% the delay was greater than 20 days

Contraception after ulipristal acetate intake

• Ulipristal acetate is an emergency contraceptive that decreases pregnancy risk after unprotected intercourse but does not confer contraceptive protection for subsequent acts of intercourse. Therefore, after using emergency contraception, women should be advised to use a reliable barrier method until her next menstrual period
• Although the use of ulipristal acetate for emergency contraception does not contraindicate the continued use of regular hormonal contraception, ulipristal acetate may reduce its contraceptive action. Therefore, if a woman wishes to start or continue using hormonal contraception, she can do so after using ulipristal acetate, however, she should be advised to use a reliable barrier method until the next menstrual period

Ulipristal acetate is an orally-active synthetic selective progesterone receptor modulator which acts via high-affinity binding to the human progesterone receptor. When used for emergency contraception, the mechanism of action is inhibition or delay of ovulation via suppression of the luteinising hormone (LH) surge. Pharmacodynamic data show that even when taken immediately before ovulation is scheduled to occur (when LH has already started to rise), ulipristal acetate is able to postpone follicular rupture for at least 5 days in 78.6% of cases.

Tablet 30mg

• Ella (Actor Pharma) originator