Linzagolix

Drugs affecting Gonadotrophin · Gonadotrophin-releasing hormone antagonist

Indications

Treatment of moderate to severe symptoms of uterine fibroids. Symptomatic treatment of endometriosis in women with a history of previous medical or surgical treatment for their endometriosis.

Dosage

Adults: Uterine fibroids: 100 mg, or if needed 200 mg once daily with concomitant hormonal add-back therapy (ABT, oestradiol 1 mg and norethisterone acetate 0.5 mg tab once daily). 100 mg once daily for women in whom ABT is not recommended or who prefer to avoid hormonal therapy. 200 mg once daily for short-term use (<6 months), when reduction of uterine and fibroid volume is desired. Endometriosis: 200 mg once daily with concomitant hormonal add-back therapy. Children: Not recommended.

Adverse Effects

Headache, nausea/vomiting, constipation, hot flush, upper abdominal pain, decreased libido, elevated liver enzymes, hyperhidrosis, night sweats, arthralgia, decreased BMD, vaginal hemorrhage, pelvic pain, change in menstrual bleeding pattern, vulvovaginal dryness, asthenia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Severe hepatic impairment (Child-Pugh C). Moderate or severe renal impairment. End-stage renal disease. Osteoporosis. Genital bleeding of unknown aetiology. Contra-indications related to ABT. Hormonal contraception. Galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. Precautions: DXA scan is recommended prior to starting treatment in patients with risk factor for osteoporosis or bone loss. Mild renal impairment. Cardiovascular diseases, family history of QT prolongation or hypokalaemia. Known abnormal hepatic history. Pre-existing elevated lipid profiles. History of depression/suicidal ideation.

Interactions

Strong CYP3A4 inhibitors/inducers, narrow therapeutic index CYP2C8 substrates (e.g. almotriptan, aminophenazone, amiodarone, amitriptyline, amodiaquine). Avoid paclitaxel, repaglinide, sorafenib and hormonal contraceptives.

Advice to Patient

Treatment should be started in the 1st week of the menstrual cycle and should be taken continuously once daily. Take tab with or without meals. Females of reproductive potential must use effective non-hormonal contraception during treatment. Report signs or symptoms that treatment if jaundice develops.

Pharmacokinetics

Absorption: Rapid. Metabolism: Hepatic. Half-life elimination: Approx. 15 hrs. Time to peak, plasma: 2-4 hrs. Excretion: Urine (mainly). Faeces (1/3rd of the dose).

Compiled by Healify Pharmacy from published drug references. How we compile it →

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