ELADIOL 200MG TABLET

Indications

• Endometriosis
• Pelvic pain associated with endometriosis

Dosage

Adults: The recommended dosage for adults is 150 mg once daily or 200 mg twice daily, depending on the severity of symptoms and clinical response.

Mechanism of action

Elagolix binds competitively to GnRH receptors in the pituitary gland, inhibiting endogenous GnRH signaling. This leads to a dose-dependent suppression of LH and FSH, which in turn decreases the concentrations of estradiol and progesterone, the primary ovarian sex hormones that contribute to the symptoms of endometriosis.

Pharmacodynamics

Clinical studies have shown that elagolix effectively reduces estradiol levels in women with endometriosis. For instance, in a three menstrual cycle study, regimens of elagolix at doses of 150 mg once daily and 200 mg twice daily resulted in median estradiol concentrations of approximately 42 pg/mL and 12 pg/mL, respectively. Additionally, elagolix has demonstrated an ovulation rate of about 50% and 32% for the aforementioned doses. Importantly, elagolix does not exhibit clinically significant effects on the QTc interval, even at high doses.

Pharmacokinetics

Elagolix is absorbed orally, with peak plasma concentrations typically occurring within 1 to 2 hours after administration. The pharmacokinetics of elagolix demonstrate linearity across a range of doses, and it has a half-life that allows for once-daily and twice-daily dosing regimens. The drug is metabolized primarily via the liver, and its excretion occurs through urine and feces.

Adverse effects

• Hot flushes
• Headache
• Nausea
• Fatigue
• Menstrual irregularities

Precautions

• Monitor for signs of osteoporosis
• Consider risks in patients with cardiovascular disease
• Use with caution in patients with hepatic impairment

Pregnancy

Elagolix is not recommended during pregnancy due to potential risks to the fetus.

Breast-feeding

It is not known if elagolix is excreted in human milk; caution is advised.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Capsules: 150 mg
• Capsules: 200 mg

Mechanism of action

Endometriosis develops when tissue that is similar to the kind that is normally located in the uterus starts to grow outside of the uterus. Such growth leads to various symptoms like pain during periods, pelvic pain between periods, and pain during sexual intercourse. The growths themselves are referred to as lesions and frequently develop on the ovaries, fallopian tubes, and other areas around the uterus, including the bowel or bladder. The growth of these lesions is dependent upon the estrogen hormone. Elagolix is an orally-administered, nonpeptide small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of elagolix results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones, estradiol and progesterone.

Pharmacodynamics

During a three menstrual cycle study in healthy women, an elagolix 150 mg once daily regimen and a 200 mg twice daily regimen resulted in an ovulation rate of about 50% and 32%, respectively. In Phase 3 trials in women with endometriosis, elagolix caused a dose-dependent reduction in median estradiol concentrations to approximately 42 pg/mL for the 150 mg once daily regimen and 12 pg/mL for the 200 mg twice daily regimen. Furthermore, the effect of elagolix on the QTc interval was investigated in a randomized, placebo- and positive-controlled, open-label, single-dose, crossover thorough QTc study in 48 healthy adult premenopausal women. Elagolix concentrations in subjects administered a single dose of 1200 mg was seventeen times higher than the concentration in subjects given elagolix 200 mg twice daily. Nevertheless, there was no clinically relevant prolongation of the QTc interval.