Ulipristal

INTRODUCTION

Indications

Prevention of pregnancy following unprotected intercourse or known/suspected contraceptive failure; not intended for routine use.

Action

Binds to progesterone receptors. Delays follicular rupture, thereby inhibiting/delaying ovulation. Changes in endometrial environment may also contribute to action. Therapeutic Effects: Prevention of pregnancy.

Adverse Reactions/Side Effects

CNS: headache, dizziness, fatigue. GI: abdominal pain, nausea. GU: altered menstrual cycle, dysmenorrhea.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Assess dizziness or fatigue that might affect gait, balance, and other functional activities (See Appendix C). Report any persistent balance problems and functional limitations to the physician, and caution the patient and family/caregivers to guard against falls and trauma.

Patient/Client-Related Instruction

• Instruct patient to report other troublesome side effects such as prolonged or severe headache, menstrual problems, or GI reactions (nausea, abdominal pain).

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: >94%.

Metabolism and Excretion: Mostly metabolized by CYP3A4 enzyme system; 1 metabolite (monodemethyl-ulipristal) pharmacologically active.

Half-life: Uliprostal—32 hr; monodemethyl-ulispristal—27 hr.

Contraindications/Precautions

Contraindicated in: Pregnancy or termination of existing pregnancy. Lactation: Not recommended during breast-feeding.

Use Cautiously in: Repeated use; regular contraception should be continued/instituted and additional method should be used during current cycle.

Interactions

Drug-Drug: Effectiveness may be ↓ by drugs that induce the CYP3A4 enzyme system, including barbiturates, bosentan, carbamazepine, oxcarbazepine, phenytoin, topiramate, felbamate, griseofulvin, and rifampin; Effects may be ↑ drugs that inhibit the CYP3A4 enzyme system, including itraconazole and ketoconazole; Efficacy of hormonal contraceptives may be ↓ during current cycle.

Drug-Natural: Effectiveness may be ↓ by St. John's wort.

Route/Dosage

PO (Adults): 1 tablet as soon as possible within 120 hr (5 days) after unprotected intercourse or known/suspected contraceptive failure. If vomiting occurs within 3 hr, dose may be repeated.

Availability

Tablet: 30 mg.