Naldemedine

SYMPROIC

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Pronunciation: nal-DEM-e-deen (sim-PROE-ik)

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

What it isPeripherally restricted mu-opioid antagonist; opioid-induced constipation.

Why this oneOral use without a food restriction distinguishes it from naloxegol while preserving central analgesia.

What limits itGI perforation is the critical risk, so avoid obstruction or structurally vulnerable bowel; CYP3A4 interactions can precipitate withdrawal.

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

Naldemedine prescription history

Animated chart of estimated U.S. prescriptions per year, Constipation meds (1900–2026). Naldemedine enters in 2017 (estimated).

FDA-approved for

opioid-induced constipation (2017)

Principal riskGI perforation in advanced illness

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityDiarrhea, dehydration and electrolyte disturbance, especially with excessive or prolonged use.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
Opioid-induced constipation (chronic non-cancer pain)	adult	0.2 mg QD

Renal Undefined

Hepatic Avoid in severe hepatic impairment

Instructions

Take with or without food
Alteration of the analgesic regimen before starting is not required
Discontinue if opioid pain medication is discontinued

Available strengths

tab 0.2 mg

Contraindications

Known or suspected GI obstruction, or increased risk of recurrent obstruction (GI perforation risk)

Cautions

Gastrointestinal perforation — monitor for severe/persistent/worsening abdominal pain
Opioid withdrawal, esp. with disrupted blood-brain barrier

Adverse reactions

Abdominal pain
Diarrhea
Nausea
Gastroenteritis
Vomiting
Opioid withdrawal symptoms

Pregnancy No human data; may precipitate opioid withdrawal in the fetus

Lactation No human data; present in rat milk — risk of opioid withdrawal in breastfed infant; may resume breastfeeding 3 days after final dose

Cost

Naldemedine (SYMPROIC)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	brand $/mo	CostPlus
0.2 mg	tab	30 qd	—	$487.68	not offered

Generic entry2033 est.

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Self-check

What food requirement distinguishes naldemedine from naloxegol?
No food restriction.
When should naldemedine be avoided because of perforation risk?
Obstruction or structurally vulnerable bowel.