Drugs List

Therapeutic Indications

Uses

Uterine fibroids

Treatment of moderate to severe symptoms caused by uterine fibroids, in adult women of childbearing age.

Contraindications

Breastfeeding
Cerebrovascular accident
Focal migraine
Galactosaemia
Hepatic neoplasm
History of severe hepatic disorder
History of venous thromboembolism
Hormone dependent neoplasm
Ischaemic heart disease
Myocardial infarction
Osteoporosis
Pregnancy
Recent arterial thromboembolic disorder
Severe hepatic disorder
Thrombophilic disorder
Undiagnosed gynaecological haemorrhage
Venous thromboembolism

Precautions and Warnings

Predisposition to thromboembolic disease
Prolonged immobilisation
Recent surgery
Recent trauma
Severe headache
Depression
Diabetes mellitus
Glucose-galactose malabsorption syndrome
Hepatic disorder
History of depression
Hypertension
Lactose intolerance
Porphyria

Assess family medical history prior to commencing treatment
Discontinue hormonal contraception before treatment initiation
Contains lactose
Exclude pregnancy prior to initiation of treatment
Monitor blood pressure before starting treatment
Perform a complete physical and gynaecological examination before therapy
Abnormal and/or irregular bleeding should be investigated
Monitor patients with a history of depression and/or suicide attempts
Patients at risk of osteoporosis should have bone density assessed
Advise patient to report any new or worsening depression/suicidal ideation
Consider discontinuing treatment if serum transaminase levels rise
Discontinue at the onset of severe depression
May cause loss of bone mineral density
May affect results of some laboratory tests
Advise patient to seek advice at first indications of pregnancy
Discontinue at first signs of jaundice
Discontinue if arterial thromboembolism develops
Discontinue if venous thromboembolism develops
Suspend treatment if hypertension cannot be controlled
Advise patient not to take St John's wort concurrently
Female: Non-hormonal contraception required for 1 month after initiation
Changes in menstrual bleeding patterns should be expected

A dual X-ray absorptiometry (DXA) is recommended before commencing therapy in patients with risk factors for osteoporosis or bone loss.

It is recommended that a DXA scan is completed after 1 year of treatment.

Consider discontinuing treatment when the patient reaches menopause, as uterine fibroids are known to regress during menopause.

Ovulation will return rapidly after discontinuing treatment in women of childbearing potential.

Before discontinuing treatment, a discussion with the patient must take place regarding contraceptive methods to be started immediately after discontinuation of treatment.

Periodic check-ups must be carried out during treatment.

Women with suspected submucosal uterine fibroids must be made aware of the possibility of uterine fibroids prolapse or expulsion during treatment. Should the patient experience severe bleeding after bleeding symptoms have improved during treatment, they must contact their physician.

Pregnancy and Lactation

Pregnancy

Relugolix with estradiol and norethisterone therapy is contraindicated during pregnancy.

Should pregnancy occur, treatment should be discontinued immediately.

Animal studies have shown teratogenic effects with exposure to relugolix in early pregnancy being associated with an increase in early miscarriage. Human data is limited and as such a potential risk cannot be ruled out.

Lactation

Relugolix with estradiol and norethisterone therapy is contraindicated during breastfeeding.

Use of relugolix with estradiol and norethisterone when breastfeeding, and for 2 weeks following discontinuation of treatment, is contraindicated by the manufacturer.

Animal data reports significant levels of relugolix in the breast milk however presence in human breast milk is unknown. Effects on exposed infants are unknown.

Side Effects

Alopecia
Breast cyst
Dyspepsia
Hot flushes
Hyperhidrosis
Irritability
Menorrhagia
Menstrual disturbances
Metrorrhagia
Night sweats
Reduced libido
Uterine haemorrhage
Uterine myoma

Presentation

Oral formulations containing relugolix, estradiol and norethisterone.

Drugs List

Therapeutic Indications

Uses

Uterine fibroids

Treatment of moderate to severe symptoms caused by uterine fibroids, in adult women of childbearing age.

Dosage

Hormonal contraceptives must be discontinued before commencing therapy with relugolix with estradiol and norethisterone.

At treatment initiation, the first tablet must be taken within 5 days of the onset of menstrual bleeding. Irregular/heavy bleeding may occur if treatment is initiated on another day in the menstrual cycle.

Adults

Additional Dosage Information

Contraindications

Breastfeeding
Cerebrovascular accident
Focal migraine
Galactosaemia
Hepatic neoplasm
History of severe hepatic disorder
History of venous thromboembolism
Hormone dependent neoplasm
Ischaemic heart disease
Myocardial infarction
Osteoporosis
Pregnancy
Recent arterial thromboembolic disorder
Severe hepatic disorder
Thrombophilic disorder
Undiagnosed gynaecological haemorrhage
Venous thromboembolism

Precautions and Warnings

Predisposition to thromboembolic disease
Prolonged immobilisation
Recent surgery
Recent trauma
Severe headache
Depression
Diabetes mellitus
Glucose-galactose malabsorption syndrome
Hepatic disorder
History of depression
Hypertension
Lactose intolerance
Porphyria

Assess family medical history prior to commencing treatment
Discontinue hormonal contraception before treatment initiation
Contains lactose
Exclude pregnancy prior to initiation of treatment
Monitor blood pressure before starting treatment
Perform a complete physical and gynaecological examination before therapy
Abnormal and/or irregular bleeding should be investigated
Monitor patients with a history of depression and/or suicide attempts
Patients at risk of osteoporosis should have bone density assessed
Advise patient to report any new or worsening depression/suicidal ideation
Consider discontinuing treatment if serum transaminase levels rise
Discontinue at the onset of severe depression
May cause loss of bone mineral density
May affect results of some laboratory tests
Advise patient to seek advice at first indications of pregnancy
Discontinue at first signs of jaundice
Discontinue if arterial thromboembolism develops
Discontinue if venous thromboembolism develops
Suspend treatment if hypertension cannot be controlled
Advise patient not to take St John's wort concurrently
Female: Non-hormonal contraception required for 1 month after initiation
Changes in menstrual bleeding patterns should be expected

A dual X-ray absorptiometry (DXA) is recommended before commencing therapy in patients with risk factors for osteoporosis or bone loss.

It is recommended that a DXA scan is completed after 1 year of treatment.

Consider discontinuing treatment when the patient reaches menopause, as uterine fibroids are known to regress during menopause.

Ovulation will return rapidly after discontinuing treatment in women of childbearing potential.

Before discontinuing treatment, a discussion with the patient must take place regarding contraceptive methods to be started immediately after discontinuation of treatment.

Periodic check-ups must be carried out during treatment.

Women with suspected submucosal uterine fibroids must be made aware of the possibility of uterine fibroids prolapse or expulsion during treatment. Should the patient experience severe bleeding after bleeding symptoms have improved during treatment, they must contact their physician.

Pregnancy and Lactation

Pregnancy

Relugolix with estradiol and norethisterone therapy is contraindicated during pregnancy.

Should pregnancy occur, treatment should be discontinued immediately.

Animal studies have shown teratogenic effects with exposure to relugolix in early pregnancy being associated with an increase in early miscarriage. Human data is limited and as such a potential risk cannot be ruled out.

Lactation

Relugolix with estradiol and norethisterone therapy is contraindicated during breastfeeding.

Use of relugolix with estradiol and norethisterone when breastfeeding, and for 2 weeks following discontinuation of treatment, is contraindicated by the manufacturer.

Animal data reports significant levels of relugolix in the breast milk however presence in human breast milk is unknown. Effects on exposed infants are unknown.

Side Effects

Alopecia
Breast cyst
Dyspepsia
Hot flushes
Hyperhidrosis
Irritability
Menorrhagia
Menstrual disturbances
Metrorrhagia
Night sweats
Reduced libido
Uterine haemorrhage
Uterine myoma

Effects on Laboratory Tests

Estrogens and progestogens may affect the results of laboratory tests such as parameters of the liver, thyroid, adrenal and renal function, plasma protein levels, parameters indicative of carbohydrate metabolism, coagulation and fibrinolysis.

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: November 2021

Reference Sources

Summary of Product Characteristics: Ryeqo tablets. Gedeon Richter (UK) Ltd. Revised August 2021.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 16 November 2021