elagolix

Absorption: Rapidly absorbed.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A isoenzyme with some metabolism by the CYP2D6 and CYP2C8 isoenzymes as well as UGT. 90% of dose excreted in feces; <3% in urine.

Half-Life: 4–6 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Osteoporosis (may ↑ risk of bone loss);
Severe hepatic impairment;
Concurrent use of strong organic anion transporting polypeptide (OATP) 1B1 inhibitors;
OB: Pregnancy.

Use Cautiously in:

History of low-trauma fracture or other risk factors for osteoporosis;
History of suicidal thoughts/behaviors or depression;
Moderate hepatic impairment (use lower dose);
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

Endo: hot flush, night sweats

GI: nausea, ↑liver enzymes, abdominal pain, constipation, diarrhea

GU: ↓libido, menstrual irregularities

Metab: dyslipidemia, weight gain

MS: ↓bone density, arthralgia

Neuro: headache, anxiety, depression, dizziness, insomnia, mood swings, SUICIDAL THOUGHTS/BEHAVIOR

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Strong OATP1B1 inhibitors, including cyclosporine and gemfibrozil, may significantly ↑ levels and risk of toxicity; concurrent use contraindicated.
Estrogen-containing oral contraceptives may ↓ effectiveness; impact of progestin-containing oral contraceptives on effectiveness unknown; recommended to use nonhormonal contraceptives.
May ↑ estrogen exposure when used with estrogen-containing contraceptives, which may ↑ risk of thromboembolic events.
May ↓ levels and effectiveness of levonorgestrel-containing oral contraceptives.
May ↓ levels and effectiveness of CYP3A substrates, including midazolam.
May ↑ levels and risk of toxicity of CYP2C19 substrates, including omeprazole; consider ↓ omeprazole dose when using higher doses (>40 mg/day).
May ↑ levels and risk of toxicity of P-glycoprotein substrates, including digoxin; closely monitor digoxin levels.
Strong CYP3A inhibitors may ↑ levels and risk of toxicity; limit concurrent use with elagolix 200 mg twice daily to ≤1 mo; limit concurrent use with elagolix 150 mg once daily to ≤6 mo.
CYP3A inducers, including rifampin, may ↓ levels and effectiveness; concurrent use with elagolix 200 mg twice daily not recommended; limit concurrent use with elagolix 150 mg once daily to ≤6 mo.
May ↓ levels and effectiveness of rosuvastatin; consider ↑ rosuvastatin dose.

Route/Dosage ⬆ ⬇

PO (Adults ): No dyspareunia: 150 mg once daily for max duration of 24 mo; Coexisting dyspareunia: 200 mg twice daily for max duration of 6 mo.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: 150 mg once daily for max duration of 6 mo.

Availability ⬆ ⬇

Tablets: 150 mg; 200 mg
In combination with:
estradiol/norethindrone (Oriahnn). See Combination Drugs.

Assessment ⬆ ⬇

Evaluate baseline pain levels and symptomatic response to therapy.
Assess bone mineral density in patients with a history of a low-trauma fracture or other risk factors for osteoporosis or bone loss. Vitamin D and calcium supplements may be considered. Use lowest effective dose for limited duration to minimize bone loss, which may not be completely reversible after therapy discontinuation.
Monitor for signs/symptoms of hepatotoxicity (fatigue, nausea, upper abdominal pain, jaundice, scleral icterus, dark urine, clay-colored stools).
Assess for depression and mood changes during therapy. Refer patients with new or worsening depression, anxiety or other mood changes, or suicidal ideation and behavior to a mental health professional. Consider benefits and risks of continuing elagolix.

Lab Test Considerations:

Verify negative pregnancy test before starting therapy.
- Monitor liver function tests periodically during therapy. May ↑ AST and ALT. Use lowest effective dose and assess risks versus benefit of continuing therapy if ↑ transaminase occurs.
- May ↑ lipid levels during 1st 2 mo of therapy; then usually remains stable.

Implementation ⬆ ⬇

PO: Administer at the same time each day without regard to food.

Patient/Family Teaching ⬆ ⬇

Explain the purpose and side effects of elagolix. Instruct patient to take as directed at approximately the same time each day. Take missed doses as soon as remembered if same day as missed dose; then return to regular dosing schedule; do not double doses. Advise patient to read Medication Guide before starting and with each Rx refill in case of changes.
Inform patient that elagolix may change menstrual periods (irregular bleeding or spotting, ↓ in menstrual bleeding, no bleeding at all) and make pregnancy difficult to detect. Watch for other signs of pregnancy (breast tenderness, weight gain, nausea).
May cause depression or suicide. Instruct patients and caregivers to monitor for emergence of suicidal thoughts and behaviors. Notify health care professional immediately if suicidal thoughts; new or worsening depression; anxiety; changes in behavior or mood; thoughts of suicide, dying, or hurting self; or acting on dangerous impulses occur. Instruct patient to carry wallet card and to call the National Suicide Prevention Lifeline at 1-800-273-8255 or visit www.988lifeline.org if they experience suicidal thoughts.
Advise patient and family to notify health care professional if signs/symptoms of liver problems occur.
Instruct patient to maintain adequate intake of calcium and vitamin D during therapy due to the risk of bone loss.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially birth control pills.
Rep: May result in pregnancy loss if used in early pregnancy. Advise women of reproductive potential to use effective nonhormonal contraception during therapy and for 28 days after last dose. Hormonal contraceptives may ↓ effectiveness of elagolix and may ↑ risk of thromboembolic and vascular disorders. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. . Discontinue elagolix if pregnancy occurs.

Evaluation/Desired Outcomes ⬆ ⬇

Reduction in dysmenorrhea and nonmenstrual pelvic pain.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0051- AbbVie Inc.
- 0051-0040-
  - 0051-0040-01- 15 kg in 1 DRUM (0051-0040-01)

0074- AbbVie Inc.
- 0074-0038- Orilissa
  - 0074-0038-07- 1 BLISTER PACK in 1 CARTON (0074-0038-07) / 7 TABLET, FILM COATED in 1 BLISTER PACK

0074- AbbVie Inc.
- 0074-0038- Orilissa
  - 0074-0038-28- 4 BLISTER PACK in 1 CARTON (0074-0038-28) / 7 TABLET, FILM COATED in 1 BLISTER PACK

0074- AbbVie Inc.
- 0074-0039- Orilissa
  - 0074-0039-14- 1 BLISTER PACK in 1 CARTON (0074-0039-14) / 14 TABLET, FILM COATED in 1 BLISTER PACK

0074- AbbVie Inc.
- 0074-0039- Orilissa
  - 0074-0039-56- 4 BLISTER PACK in 1 CARTON (0074-0039-56) / 14 TABLET, FILM COATED in 1 BLISTER PACK

11722- TAPI Croatia Industries Ltd.
- 11722-074-
  - 11722-074-00- 1 kg in 1 CARTON (11722-074-00)

42931- Shanghai Desano Chemical Pharmaceutical Co., Ltd.
- 42931-320-
  - 42931-320-01- 25 kg in 1 DRUM (42931-320-01)

58032- Neuland Laboratories Limited
- 58032-1028-
  58032-1028-0- 25 kg in 1 DRUM (58032-1028-0)

65129- ScinoPharm Taiwan Ltd.
- 65129-1443-
  65129-1443-0- 30 kg in 1 DRUM (65129-1443-0)

66039- Glenmark Life Sciences Limited
- 66039-958-
  66039-958-04- 65 kg in 1 DRUM (66039-958-04)

66499- Formosa Laboratories, Inc.
- 66499-0072-
  66499-0072-1- 15 kg in 1 DRUM (66499-0072-1)

68513- AbbVie Ireland NL B.V.
- 68513-0038-
  68513-0038-9- 35000 TABLET, FILM COATED in 1 BOX (68513-0038-9)

68513- AbbVie Ireland NL B.V.
- 68513-0039-
  68513-0039-9- 26000 TABLET, FILM COATED in 1 BOX (68513-0039-9)

68554- HETERO LABS LIMITED
- 68554-0131-
  68554-0131-1- 25 kg in 1 DRUM (68554-0131-1)

68554- HETERO LABS LIMITED
- 68554-0155-
  68554-0155-1- 5 kg in 1 DRUM (68554-0155-1)

69766- MSN Life Sciences Private Limited
- 69766-099-
  69766-099-01- 50 kg in 1 DRUM (69766-099-01)

71796- Dr. Reddy's Laboratories Limited
- 71796-025-
  71796-025-00- 1 kg in 1 DRUM (71796-025-00)

73435- Biophore India Pharmaceuticals Pvt. Ltd
- 73435-021-
  73435-021-11- 20 kg in 1 DRUM (73435-021-11)

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇