Treprostinil

REMODULIN

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Pronunciation: tre-PROS-ti-nil

Treprostinil ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Treprostinil ballicule

What it isProstacyclin analog; pulmonary arterial hypertension.

Why this oneIt can be given subcutaneously, intravenously, by inhalation or orally, the widest route range of the prostacyclins.

What limits itInfusion-site pain is often severe with the subcutaneous route. Headache, jaw pain and diarrhea; abrupt interruption causes rebound.

Treprostinil molecular structure (skeletal formula) — Molecular structure: Treprostinil

FDA-approved for

pulmonary arterial hypertension (2002)

FDA label

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FDA dosing	Population	Start	Target	Max
PAH (WHO Group 1, NYHA II–IV) — new to prostacyclin infusion	Adults	1.25 ng/kg/min continuous SC (or IV) infusion	Titrate to clinical response	Undefined
PAH — transition from epoprostenol	Adults	10% of current epoprostenol dose, raised as epoprostenol is reduced	~110% of starting epoprostenol dose (+5–10% increments as needed)	Undefined

Titration Weekly: +1.25 ng/kg/min per week for first 4 weeks, then +2.5 ng/kg/min per week (more often if tolerated)

Renal No dose adjustment; not cleared by dialysis

Hepatic Mild–moderate: start 0.625 ng/kg/min (ideal body weight), titrate slowly; severe: not studied

If 1.25 ng/kg/min not tolerated, reduce to 0.625 ng/kg/min. Pediatric safety and effectiveness not established.

Instructions

Continuous SC infusion preferred; central IV line if SC not tolerated (site pain/reaction)
Undiluted rate (mL/h) = dose (ng/kg/min) × weight (kg) × 0.00006 ÷ vial strength (mg/mL)
May dilute with high-pH glycine diluent, Sterile Water, or 0.9% NaCl; IV sets need in-line 0.22- or 0.2-micron filter
Avoid abrupt cessation; restart within a few hours at the same rate, longer interruptions may need re-titration
Keep backup pump and infusion sets immediately available
Epoprostenol transition in hospital with constant observation

Available strengths

inj 0.4, 1, 2.5, 5, 10 mg/mL
cap 26.5, 53, 79.5, 106 mcg
ER tab 0.125, 0.25, 1, 2.5, 5 mg
powder 0.016, 0.0265, 0.032, 0.048, 0.053, 0.064, 0.0795, 0.08, 0.106 mg/inh
sol 0.6 mg/mL
inhaler 16, 32, 48, 64, 80 mcg
inhaler 1.74 mg/2.9 mL

Cautions

Catheter-related bloodstream infection/sepsis (IV)
Worsening PAH on abrupt withdrawal or large dose reduction
Hepatic insufficiency — titrate slowly
Symptomatic hypotension
Bleeding risk (inhibits platelet aggregation)

Adverse reactions

Infusion site pain (85%)
Infusion site reaction (83%)
Headache
Diarrhea
Nausea
Rash
Jaw pain
Vasodilatation
Edema
Hypotension

Pregnancy Limited case reports insufficient to inform risk; PAH increases maternal/fetal mortality; rabbit malformations at ~5–7× human exposure.

Lactation No data on presence in human milk or effects on breastfed infant or milk production.

Cost

Treprostinil (REMODULIN)

Strength		#/mo	CostPlus
0.4 mg/mL	inj	per unit	not offered
1 mg/mL	inj	per unit	not offered
2.5 mg/mL	inj	per unit	not offered
5 mg/mL	inj	per unit	not offered
10 mg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Treprostinil is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2017

NO BOXED WARNINGS

Principal riskSevere infusion-site pain subcutaneously

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

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