Ulipristal Acetate

Pronunciation: UE-li-PRIS-tal AS-e-tate
Class: Emergency contraceptive

Trade Names

Ella
- Tablets 30 mg

Pharmacology

Inhibition or delay of ovulation; however, alterations to the endometrium that may affect implantation may also contribute to efficacy.

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Pharmacokinetics

Absorption

C max and T max for ulipristal are approximately 176 ng/mL and 0.9 h, respectively. C max and T max for the active metabolite are 69 ng/mL and 1 h, respectively.

Distribution

Highly protein bound (more than 94%).

Metabolism

Predominantly mediated by CYP3A4. Metabolized to mono-demethylated and di-demethylated active metabolites.

Elimination

The terminal half-life is approximately 32.4 h.

Special Populations

Renal Function Impairment

No studies have been conducted.

Hepatic Function Impairment

No studies have been conducted.

Race

Exposure in South Asian patients may exceed that in white and black patients. However, no difference in efficacy and safety was observed.

Indications and Usage

Emergency contraception.

Contraindications

Known or suspected pregnancy.

Dosage and Administration

Adults and Children Who Have Undergone Menarche

PO 1 tablet as soon as possible within 120 h (5 days) after unprotected intercourse or known or suspected contraceptive failure.

General Advice

  • May be taken with or without food.
  • If vomiting occurs within 3 h after administration, consider repeating the dose.
  • Emergency contraceptive can be used at any time during the menstrual cycle.

Storage/Stability

Store between 68° and 77°F. Keep blister in outer carton to protect from light.

Drug Interactions

CYP3A4 inducers (eg, barbiturates, bosentan, carbamazepine, felbamate, griseofulvin, oxcarbazine, phenytoin, rifampin, St. John's wort, topiramate)

Ulipristal plasma concentration and pharmacologic effects may be decreased. Monitor the clinical response and adjust the ulipristal dose as needed.

CYP3A4 inhibitors (eg, itraconazole, ketoconazole)

Ulipristal plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the clinical response and adjust the ulipristal dose as needed.

Adverse Reactions

CNS

Headache (19%); fatigue (6%); dizziness (5%).

Dermatologic

Acne (postmarketing).

GI

Abdominal and upper abdominal pain (15%); nausea (13%).

Genitourinary

Dysmenorrhea (13%).

Precautions

Monitor

Evaluate patients who complain of lower abdominal pain for the possibility of ectopic pregnancy. A follow-up physical or pelvic examination is recommended if there is any doubt concerning the general health or pregnancy status of any woman after taking ulipristal.


Pregnancy

Category X . Not effective in terminating an existing pregnancy.

Lactation

Undetermined. Use is not recommended.

Children

Use before menarche is not indicated.

Elderly

Not intended for use in postmenopausal women.

Ectopic pregnancy

May occur. Consider ectopic pregnancy in women who become pregnant or complain of lower abdominal pain.

Existing pregnancy

Not indicated for termination of an existing pregnancy.

Fertility following use

A rapid return of fertility is likely following treatment; therefore, continue or initiate routine contraception as soon as possible.

Menstrual cycle effects

Menses may occur earlier or later than expected by a few days.

Repeated use

Repeated use within the same menstrual cycle is not recommended.

STDs

Does not protect against HIV (AIDS) and other STDs.

Overdosage

Symptoms

None well documented.

Patient Information

  • Instruct patients to take as soon as possible and not more than 120 h after unprotected intercourse or known or suspected contraceptive failure.
  • Advise patients that if vomiting occurs within 3 h of taking ulipristal to immediately contact their health care provider to discuss whether to take another tablet.
  • Advise patient to seek medical attention if severe lower abdominal pain occurs 3 to 5 wk after taking ulipristal in order to rule out ectopic pregnancy, or if their period is delayed more than 1 wk beyond the date expected after taking emergency contraceptives.
  • Advise patients to not take this medication if they know or suspect they are pregnant and that this medication is not indicated for termination of an existing pregnancy.
  • Inform patients that this medication is not to be used as routine contraception and not to use it repeatedly within the same menstrual cycle.
  • Inform patients that this medication may reduce the contraceptive action of regular hormonal contraceptive methods and to use a reliable barrier method of contraception for any subsequent acts of intercourse that occur during that same menstrual cycle.
  • Advise patients not to use this medication if they are breast-feeding.
  • Inform patients that this medication does not protect against HIV infection (AIDS) and other STDs.

Copyright © 2009 Wolters Kluwer Health.

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