Selexipag


Generic Medicine Info
Indications and Dosage
Oral
Pulmonary arterial hypertension
Adult: Initially, 200 mcg bid, increased in increments of 200 mcg bid at weekly intervals, according to patient's tolerability. Max: 1,600 mcg bid.
Hepatic Impairment
Moderate (Child-Pugh class B): Initially, 200 mcg once daily, increased by 200 mcg once daily at wkly intervals, according to patient’s tolerability. Max: 1,600 mcg once daily.
Severe (Child-Pugh class C): Avoid use.
Administration
Film-Coated Tab: May be taken with or without food. Swallow whole, do not chew/crush/split.
Contraindications
Severe CHD or unstable angina, recent MI w/in 6 mth, decompensated cardiac failure, severe arrhythmias, TIA or recent stroke w/in 3 mth, congenital valvular defects. Concomitant use w/ strong CYP2C8 inhibitor. Severe hepatic impairment.
Special Precautions
Moderate hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Pulmonary veno-occlusive disease, hypotension, hyperthyroidism.
Nervous: Headache.
CV: Flushing.
GI: Diarrhoea, nausea, vomiting, decreased appetite, abdominal pain.
Resp: Nasopharyngitis, nasal congestion.
Endocrine: Decreased TSH, wt decrease.
Haematologic: Decreased Hb, anaemia.
Musculoskeletal: Jaw pain, limb pain, myalgia, arthralgia.
Dermatologic: Rash, urticaria, erythema.
Monitoring Parameters
Monitor LFT, thyroid function tests and for signs and symptoms of pulmonary oedema.
Overdosage
Symptoms: Mild transient nausea. Management: Supportive therapy.
Drug Interactions
Increased serum concentration w/ strong CYP2C8 inhibitor (e.g. gemfibrozil). Decreased serum concentration w/ CYP2C8 inducers (e.g. rifampicin).
Action
Description: Selexipag is a selective non prostanoid prostacyclin (IP) receptor agonist, that stimulates the release of prostacyclin, which is responsible for inducing peripheral and pulmonary vasodilation. It also inhibits platelet aggregation.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 49%. Time to peak plasma concentration: 1-3 hr (selexipag); 3-4 hr (ACT-333679).
Distribution: Volume of distribution: 11.7 L. Plasma protein binding: Approx 99%, to albumin and α1-acid glycoprotein.
Metabolism: Hydrolysed in the liver by carboxylesterase 1 into active metabolite ACT-333679, which is then metabolised by UGT1A3 and UGT2B7 via glucuronidation.  Undergoes oxidative metabolism by CYP2C8 enzyme into hydroxylated and dealkylated metabolites.
Excretion: Mainly via faeces (approx 93%); urine (12%). Terminal half-life: 0.8-2.5 hr (selexipag); 6.2-13.5 (ACT-333679).
Chemical Structure

Chemical Structure Image
Selexipag

Source: National Center for Biotechnology Information. PubChem Database. Selexipag, CID=9913767, https://pubchem.ncbi.nlm.nih.gov/compound/Selexipag (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C.
ATC Classification
B01AC27 - selexipag ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
References
Anon. Selexipag. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/12/2017.

Buckingham R (ed). Selexipag. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/12/2017.

Joint Formulary Committee. Selexipag. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/12/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Selexipag. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 12/12/2017.

Uptravi Tablet, Coated (Actellion Pharmaceuticals US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 12/12/2017.

Disclaimer: This information is independently developed by MIMS based on Selexipag from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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