Monograph

B01AC21 - Treprostinil

Propably not porphyrinogenic

Rationale

Treprostinil do not inhibit or induce CYP enzymes and is therefore probably not porphyrinogenic. Side effects that can be potentially porphyrinogenic through reduction in carbohydrate intake are diarrhoea and nausea.

Chemical description

Prostacyclin analogue

Therapeutic characteristics

Treprostinil is indicated for the treatment of idiopathic or familiar pulmonary hypertension. Very common side effects that can be potentially porphyrinogenic through reduction in carbohydrate intake and that also can be confused with an acute porphyria attack are diarrhoea and nausea.

Hepatic exposure

Insignificant

Metabolism and pharmacokinetics

Treprostinil is metabolized by CYP2C8 with minor contribution by CYP2C9 (Gotzkowsky 2010). It is 91% bound to plasma proteins (Skoro-Sajer 2008). The elimination half-life is 1.3-4.6 hours. An in vitro study has shown that treprostinil does not inhibit human hepatic microsomal CYP450 isoenzymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A) (SPC). The Summary of Product Characteristics (SPC) also states that treprostinil is not an inducer of CYP1A, CYP2B and CYP3A. The data from an in vivo study showed that treprostinil had no effect on warfarin (a substrate of CYP2C8 and CYP2C9 amongst others) and this indicates that treprostinil do not induce or inhibit CYP2C8 and CYP2C9 (Wade 2003).

References

#	Citation details	PMID
*	Scientific articles
1.	Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers. Gotzkowsky SK, Dingemanse J, et al. J Clin Pharmacol. 2010 Jul;50(7):829-34.	20133511
2.	Treprostinil for the treatment of pulmonary hypertension. Skoro-Sajer N and Lang I. Expert Opin Pharmacother. 2008 Jun;9(8):1415-20.	18473715
3.	Effect of continuous subcutaneous treprostinil therapy on the pharmacodynamics and pharmacokinetics of warfarin. Wade M, Hunt TL, Lai AA. J Cardiovasc Pharmacol. 2003 Jun;41(6):908-15.
*	Summary of Product Characteristics
4.	Norwegian medicines agency. Summary of Product Characteristics (SPC). (treprostinil).

Citation details

PMID

Scientific articles

Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers.

Gotzkowsky SK, Dingemanse J, et al. J Clin Pharmacol. 2010 Jul;50(7):829-34.

20133511

Treprostinil for the treatment of pulmonary hypertension.

Skoro-Sajer N and Lang I. Expert Opin Pharmacother. 2008 Jun;9(8):1415-20.

18473715

Effect of continuous subcutaneous treprostinil therapy on the pharmacodynamics and pharmacokinetics of warfarin.

Wade M, Hunt TL, Lai AA. J Cardiovasc Pharmacol. 2003 Jun;41(6):908-15.

Summary of Product Characteristics

Norwegian medicines agency. Summary of Product Characteristics (SPC). (treprostinil).

Similar drugs

Explore alternative drugs in similar therapeutic classes B01A / B01AC or go back.

Tradenames and packages

From some sources, we get a list of packages (United Kingdom, Ireland, Estonia). Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway). What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names are the searchable terms. The gray names that follow are all mapped to the bolded term.

Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors. We strive to improve it continuously.

Netherlands

Remodulin · Remodulin 1 mg/ml, oplossing voor infusie · Remodulin 10 mg/ml, oplossing voor infusie · Remodulin 2,5 mg/ml, oplossing voor infusie · Remodulin 5 mg/ml, oplossing voor infusie · Treposuvi · Treposuvi 10 mg/ml oplossing voor infusie · Treposuvi 1mg/ml oplossing voor infusie · Treposuvi 2,5 mg/ml oplossing voor infusie · Treposuvi 5 mg/ml oplossing voor infusie · Treprostinil · Treprostinil Reddy 1 mg/ml, oplossing voor infusie · Treprostinil Reddy 10 mg/ml, oplossing voor infusie · Treprostinil Reddy 2,5 mg/ml, oplossing voor infusie · Treprostinil Reddy 5 mg/ml, oplossing voor infusie · Treprostinil Tillomed 1 mg/ml oplossing voor infusie · Treprostinil Tillomed 10 mg/ml oplossing voor infusie · Treprostinil Tillomed 2,5 mg/ml oplossing voor infusie · Treprostinil Tillomed 5 mg/ml oplossing voor infusie · Trepulmix · Trepulmix 1 mg/ml, oplossing voor infusie · Trepulmix 10 mg/ml, oplossing voor infusie · Trepulmix 2,5 mg/ml, oplossing voor infusie · Trepulmix 5 mg/ml, oplossing voor infusie

Belgium

Remodulin · Remodulin 1 mg/ml sol. perf. s.c. · Remodulin 10 mg/ml sol. perf. s.c. · Remodulin 2.5 mg/ml sol. perf. s.c. · Remodulin 5 mg/ml sol. perf. s.c. · Trepulmix · Trepulmix 1 mg/ml sol. perf. s.c. flac. · Trepulmix 10 mg/ml sol. perf. s.c. flac. · Trepulmix 2.5 mg/ml sol. perf. s.c. flac. · Trepulmix 5 mg/ml sol. perf. s.c. flac. · Tresuvi · Tresuvi 1 mg/ml sol. perf. i.v. flac. · Tresuvi 10 mg/ml sol. perf. i.v. flac. · Tresuvi 2.5 mg/ml sol. perf. i.v. flac. · Tresuvi 5 mg/ml sol. perf. i.v. flac.

United Kingdom

Treposuvi · Treposuvi 100mg/10ml solution for infusion vials · Treposuvi 10mg/10ml solution for infusion vials · Treposuvi 25mg/10ml solution for infusion vials · Treposuvi 50mg/10ml solution for infusion vials · Treprostinil · Treprostinil 100mg/20ml solution for infusion vials · Treprostinil 200mg/20ml solution for infusion vials · Treprostinil 20mg/20ml solution for infusion vials · Treprostinil 50mg/20ml solution for infusion vials · Trepulmix · Trepulmix 100mg/10ml solution for infusion vials · Trepulmix 10mg/10ml solution for infusion vials · Trepulmix 25mg/10ml solution for infusion vials · Trepulmix 50mg/10ml solution for infusion vials

Denmark