Ulipristal acetate is a medication primarily used as an emergency contraceptive to prevent pregnancy after unprotected intercourse or contraceptive failure. It works by inhibiting ovulation and may also affect the lining of the uterus, making it less receptive to implantation. Additionally, ulipristal acetate is sometimes used to treat uterine fibroids, as it can help shrink their size before surgery.

Ulipristal acetate is a hormonal drug that inhibits ovulation, and follicular rupture, and induces apoptosis of uterine fibroids.

Ulipristal acetate Uses:

• Emergency contraception (Ella):
  • It is used as an emergency contraceptive drug for the prevention of pregnancy following unprotected sexual intercourse or following contraceptive failure.
• Uterine fibroids (Fibristal):
  • It is used to treat uterine fibroids in women who are fertile and have symptoms that range from mild to severe.

Ulipristal acetate Dose in Adults

Ulipristal acetate Dose in Emergency contraception (Ella):

• When it comes to emergency contraception like ella, you typically take one pill by mouth, which contains 30 milligrams of ulipristal acetate.
• It's best to take it as soon as possible after unprotected sex or if your birth control fails, but you can take it up to 5 days afterward and still have it be effective.

Ulipristal acetate Dose in the treatment of Uterine fibroids (Fibristal):

Premenopausal Females:

• In the treatment of uterine fibroids with Fibristal, the recommended dose for premenopausal females is 5 milligrams taken orally once a day for three months straight.
• It's important to start the first treatment course within the first week of your menstrual cycle.
• After completing one course, you can start the next one at the earliest during the first week of your second menstrual cycle following the completion of the prior treatment.
• You should take a break between courses for at least 2 menstrual cycles.
• It's been studied that you can repeat this treatment up to 4 times.

Ulipristal acetate Dose in Children

Ulipristal acetate Dose in Emergency contraception (Ella):

• Postpubertal Adolescents:
  • For children and adolescents who have not yet started menstruating (prepubertal), ulipristal, like ella, is not recommended for use before they reach menarche (the onset of menstruation).
• Children and Adolescents (prepubertal):
  • Children under the age of puberty should not take it.

Ulipristal acetate Pregnancy Risk Category: X

• If there's a known or suspected pregnancy, ulipristal shouldn't be used.
• While rare cases of birth defects have been reported when used accidentally during pregnancy, it's unclear if ulipristal is the cause.
• It's not meant to end an existing pregnancy.
• After using it for emergency contraception, expect fertility to return quickly, so it's important to start or continue regular birth control to prevent pregnancy.
• Use barrier contraception immediately after taking it and throughout the same menstrual cycle, as hormonal contraceptives might be less effective.
• Wait at least 5 days before restarting oral contraceptives after taking ulipristal.
• The CDC suggests starting any contraceptive right after using ulipristal but using a barrier method for 14 days afterward or until your period starts.
• If using ulipristal for uterine fibroids, it's best to use a non-hormonal form of birth control.

Ulipristal acetate use during breastfeeding:

• Ulipristal and its active form can be found in breast milk, with a relative infant dose of around 0.8%, which is below the generally accepted limit of 10%.
• This means breastfeeding is usually considered safe while taking ulipristal.
• The concentration of ulipristal in breast milk peaked within the first 24 hours after taking the medication and decreased significantly afterward.
• The decision to breastfeed during treatment should weigh the potential risk of exposure to the infant against the benefits of breastfeeding and treatment for the mother.
• According to CDC guidelines, ulipristal can be used for emergency contraception in breastfeeding women, but it's advised to discard breast milk for 24 hours after taking the dose.

Dose in kidney disease:

Ella:

• For ella, the manufacturer's label doesn't provide dosage adjustments because studies haven't looked into it, but it's generally not considered necessary since ulipristal is mostly eliminated through processes other than the kidneys.

Fibristal:

• Regarding Fibristal, the Canadian product, while dosage adjustment might not be needed due to minimal renal elimination of ulipristal, the manufacturer advises against using it in people with moderate to severe kidney impairment unless they are carefully monitored.

Ulipristal acetate dose in Liver disease:

Ella:

• For ella, there are no specified dosage adjustments for hepatic impairment in the manufacturer's labeling because it hasn't been studied.

Fibristal:

• Regarding Fibristal, the Canadian product, no dosage adjustment is deemed necessary for mild or moderate hepatic impairment, but it hasn't been studied thoroughly.
• However, the manufacturer advises against using it in individuals with severe hepatic impairment unless they are closely monitored.

Emergency contraception (ella):

Common Side Effects of Ella (Ulipristal acetate) Include:

• Genitourinary:
  • Dysmenorrhea
• Central Nervous System:
  • Headache
• Gastrointestinal:
  • Abdominal Pain
  • Nausea
• Endocrine & Metabolic:
  • Suppressed Menstruation

Less Common Side Effects of Ella (Ulipristal acetate) Include:

• Endocrine & Metabolic:
  • Intermenstrual Bleeding
•  
• Central Nervous System:
  • Fatigue
  • Dizziness
• Genitourinary:
  • Early Menses

Common Side Effects of Fibristal (Ulipristal acetate) Include:

• Central nervous system:
  • Headache
• Endocrine & metabolic:
  • Hot flash

Less Common Side Effects of Fibristal (Ulipristal acetate) Include:

• Neuromuscular & Skeletal:
  • Back Pain
  • Arthralgia
  • Muscle Spasm
  • Limb Pain
• Cardiovascular:
  • Edema
  • Hypotension
  • Sinus Bradycardia
• Dermatologic:
  • Alopecia
  • Seborrhea
  • Night Sweats
  • Acne Vulgaris
  • Xeroderma
• Central Nervous System:
  • Aggressive Behavior
  • Drowsiness
  • Fatigue
  • Vertigo
  • Insomnia
  • Dizziness
  • Emotional Lability
  • Migraine
  • Sleep Disorder
• Endocrine & Metabolic:
  • Ovarian Hyperstimulation
  • Thyroid Disease
  • Obesity
  • Amenorrhea
  • Hypercholesterolemia
  • Hypertriglyceridemia
  • Hypothyroidism
  • Increased Gamma-Glutamyl Transferase
  • Ovarian Cyst
• Genitourinary:
  • Endometrial Hyperplasia
  • Mastalgia
  • Pelvic Pain
  • Genital Bleeding
  • Uterine Disease
  • Uterine Hemorrhage
  • Breast Swelling
  • Breast Tenderness
  • Genital Discharge
  • Vaginal Dryness
  • Vulvovaginal Candidiasis
• Infection:
  • Herpes Virus Infection
• Gastrointestinal:
  • Dyspepsia
  • Nausea
  • Constipation
  • Upper Abdominal Pain
•  
• Miscellaneous:
  • Fever
• Respiratory:
  • Epistaxis
  • Dyspnea
  • Pharyngitis

Contraindications to Ulipristal acetate Include:

• For ella, it's contraindicated in cases of known or suspected pregnancy, and according to Canadian labeling, it's also not recommended for those who are hypersensitive to ulipristal or any of its ingredients.
• As for Fibristal, the Canadian product, it's contraindicated in individuals who are hypersensitive to ulipristal or any component of the formulation. Additionally, it's not recommended for use during pregnancy or breastfeeding, and caution should be exercised if there's genital bleeding of unknown cause or for reasons other than uterine fibroids. Fibristal should not be used in individuals with breast, cervical, uterine, or ovarian cancer, or in those with current or historical hepatic disease.

Warnings and precautions

Bleeding irregularities:

• When using ulipristal, menstrual bleeding patterns may change, with cycles potentially being delayed or shortened by a few days, but typically returning to normal in following cycles.
• Spotting between periods, known as intermenstrual bleeding, can also occur.
• If menstruation is delayed by more than 7 days from the expected period, it's essential to consider the possibility of pregnancy.
• In the treatment of uterine fibroids with Fibristal, a noticeable decrease in menstrual blood loss or even the absence of periods (amenorrhea) is usually seen within 10 days of starting treatment.
• After stopping Fibristal, menstrual cycles generally return within 4 weeks.

Endometrial thickening

• Endometrial thickening has been noticed in individuals using Fibristal for treating uterine fibroids.
• This thickening is reversible once the treatment is stopped.
• However, if endometrial thickening persists for more than 3 months after stopping the therapy and menstrual periods have returned, further evaluation is recommended.
• These changes in the endometrial tissue, known as progesterone receptor modulator associated endometrial changes (PAEC), may resemble endometrial hyperplasia.
• It's important to inform pathologists about ulipristal therapy when submitting endometrial tissue for histologic evaluation to ensure accurate interpretation.

Asthma

• For individuals with severe uncontrolled asthma, the use of Fibristal, the Canadian product, is not recommended.
• This precaution is likely due to concerns about potential interactions or exacerbation of asthma symptoms.

Ulipristal: Drug Interaction

Monitor:

After Emergency Contraception (ella):

• Evaluate for Pregnancy: If your period is delayed by a week or more after using emergency contraception, or if you experience lower abdominal pain 3 to 5 weeks after taking it, or persistent irregular bleeding, it's important to consider the possibility of pregnancy or ectopic pregnancy.
• Pregnancy Test: If you don't experience withdrawal bleeding within 3 weeks after using emergency contraception, it's recommended to take a pregnancy test to rule out pregnancy.

Fibristal [Canadian Product] (For Treating Uterine Fibroids):

• Rule out Pregnancy: Before starting Fibristal treatment, make sure to check for pregnancy.
• Endometrial Monitoring: Periodic monitoring of the endometrium (the lining of the uterus) may be necessary during Fibristal treatment.
• Irregular Bleeding: If you experience unexpected or persistent irregular bleeding while using Fibristal.

How to administer Ulipristal acetate (Ella)?

ella (Emergency Contraception):

• Administration: You can take ella with or without food at any time during your menstrual cycle.
• Vomiting: If you vomit within 3 hours of taking ella, it might not have been fully absorbed, so you should consider taking another dose.

Fibristal (Canadian Product for Treating Uterine Fibroids):

• Administration: Take Fibristal with water, and you can do so with or without food.
• Initiation: Start taking Fibristal during the first 7 days of your menstrual cycle.

Mechanism of action of Ulipristal acetate (Ella):

Emergency Contraception (ella):

• Prevents Progestin Binding: ella works by preventing progestin, a hormone, from binding to the progesterone receptor.
• Inhibits Ovulation: When taken before ovulation, ella delays follicular rupture, which helps in inhibiting or delaying ovulation, preventing pregnancy.
• Affects Endometrium: It may also change the normal lining of the uterus (endometrium), making it less suitable for the implantation of a fertilized egg.

Treatment of Uterine Fibroids (Fibristal [Canadian Product]):

• Reduces Fibroid Size: ulipristal, in the treatment of uterine fibroids, decreases the size of these growths by inhibiting the growth of fibroid cells and causing their programmed cell death (apoptosis).

Absorption:

• Rapid: Ulipristal is absorbed quickly into the bloodstream after administration.

Protein Binding:

• High Protein Binding: Ulipristal binds extensively to plasma proteins, with over 98% bound to albumin, alpha-acid glycoprotein, high-density lipoprotein, and low-density lipoprotein.

Metabolism:

• Hepatic Metabolism: Ulipristal undergoes metabolism primarily in the liver, primarily through the CYP3A4 enzyme system.
• Active Metabolite: It forms an active metabolite called monodemethylated metabolite, along with inactive metabolites.

Half-life:

• Ulipristal: The half-life of ulipristal in elimination from the body is approximately 32 to 38 hours.
• Monodemethylated Metabolite: The half-life of the active metabolite is around 27 hours.

Time to Peak Serum Concentration:

• 1 Hour: Both ulipristal and its active metabolite reach their peak concentration in the bloodstream about 1 hour after administration.

Excretion:

• Primary Route: Feces is the primary route of elimination for ulipristal.
• Minor Route: A small portion is excreted in the urine, accounting for less than 10% of the total elimination.

International Brands of Ulipristal acetate:

• 5X
• Duella
• ella
• Ella
• ellaOne
• EllaOne
• Esmia
• Esmya
• Femelle One
• Gesprital
• Inisia
• Norpregna
• Peuli
• Post Day Plus
• Postday Plus
• Tulip
• Uliroid
• Utal
• Ella
• Fibristal

Ulipristal acetate Brand Names in Pakistan:

No Brand Available in Pakistan.