Selexipag oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral formulations of selexipag.
Drugs List
Therapeutic Indications
Uses
Pulmonary arterial hypertension: functional grades II and III
Selexipag is indicated for the long term treatment of pulmonary arterial hypertension (PAH) in patients with WHO functional class (FC) II to III, either as combination therapy in patients insufficiently controlled with an endothelin receptor antagonist (ERA) and/or a phosphodiesterase type 5 (PDE-5) inhibitor or as a monotherapy in patients who are not candidates for these therapies.
Efficacy has been shown in a PAH population including idiopathic and heritable PAH, PAH associated with connective tissue disorders, and PAH associated with corrected simple congenital heart disease.
Dosage
Adults
Individualised dose titrations
Each patient should be up-titrated to the highest individually tolerated dose, which can range from 200micrograms given twice daily to 1.6mg given twice daily (individualised maintenance dose).
The recommended starting dose is 200micrograms given twice daily, approximately 12 hours apart. The dose is increased in increments of 200micrograms given twice daily, usually at weekly intervals. At the beginning of treatment and at each up-titration step it is recommended to take the first dose in the evening.
If the patient reaches a dose that cannot be tolerated, the dose should be reduced to the previous dose level.
In patients in whom up-titration was limited by reasons other than adverse reactions reflecting the mode of action of selexipag, a second attempt to continue up-titration to the highest individually tolerated dose up to a maximum dose of 1.6mg twice daily may be considered.
Individualised maintenance dose
The highest tolerated dose reached during dose titration should be maintained. If the therapy over time is less tolerated at a given dose, symptomatic treatment and/or a dose reduction to the next lower dose should be considered.
Patients with Renal Impairment
Severe renal impairment (eGFR less than 30 ml/minute/1.73 metres squared)
Dose titration should be done with caution in these patients.
Patients with Hepatic Impairment
Moderate hepatic impairment (Child-Pugh class B)
The starting dose of selexipag should be 200micrograms once daily, and increased at weekly intervals by increments of 200micrograms given once daily until adverse reactions, reflecting the mode of action of selexipag, that cannot be tolerated or medically managed are experienced.
Additional Dosage Information
Missed dose
If a dose is missed, it should be taken as soon as possible. The missed dose should not be taken if the next scheduled dose is within approximately 6 hours.
If treatment is missed for 3 days or more, selexipag should be restarted at a lower dose and then up-titrated.
Contraindications
Children under 18 years
Breastfeeding
Decompensated cardiac failure
Ischaemic heart disease
Pregnancy
Renal dialysis
Serious cardiac arrhythmias
Severe hepatic impairment
Unstable angina
Valvular defects with associated myocardial function disorder
Within 3 months of a cerebrovascular accident
Within 6 months of a myocardial infarction
Precautions and Warnings
Females of childbearing potential
Patients over 75 years
Autonomic dysfunction
Hypotension
Hypovolaemia
Left ventricular outflow obstruction
Moderate hepatic impairment
Pulmonary veno-occlusive disease
Renal impairment - eGFR below 30ml/minute/1.73m sq
Reduce dose in patients with moderate hepatic impairment
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Monitor thyroid function regularly
Consider veno-occlusive disease if pulmonary oedema occurs
Avoid abrupt withdrawal
Discontinue if pulmonary oedema occurs
Female: Ensure adequate contraception during treatment
There is limited experience with abrupt discontinuation of selexipag in patients with PAH. No evidence for acute rebound has been observed. If the decision to withdraw selexipag is taken, it should be done gradually while an alternative therapy is introduced.
Pregnancy and Lactation
Pregnancy
Selexipag is contraindicated during pregnancy.
The manufacturer does not recommend using selexipag during pregnancy. At the time of writing there is limited published information regarding the use of selexipag during pregnancy. Potential risks are unknown.
Lactation
Selexipag is contraindicated during breastfeeding.
The manufacturer does not recommend breastfeeding whilst taking selexipag. The presence of selexipag in human breast milk and the effects on exposed infants are unknown.
Side Effects
Abdominal pain
Anaemia
Arthralgia
Decreased appetite
Decreased TSH
Diarrhoea
Erythema
Extremity pain
Flushing
Haemoglobin decrease
Headache
Hyperthyroidism
Hypotension
Jaw pain
Myalgia
Nasal congestion
Nasopharyngitis
Nausea
Pain
Rash
Tachycardia
Urticaria
Vomiting
Weight loss
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: October 2019
Reference Sources
Summary of Product Characteristics: Uptravi. Actelion Pharmaceuticals UK Ltd. Revised July 2019.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 25 October 2019
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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