section name header

Pronunciation

me-thil-nal-TREX-one

Classifications

Therapeutic Classification: laxatives

Pharmacologic Classification: opioid antagonists

Indications

REMS


Action

  • Acts peripherally as mu-opioid receptor antagonist, blocking opioid effects on the GI tract.
Therapeutic effects:
  • Blocks constipating effects of opioids on the GI tract without loss of analgesia.

Pharmacokinetics

Absorption: Rapidly absorbed after SUBQ and oral administration; oral absorption delayed by high-fat meal by 2 hr.

Distribution: Moderate tissue distribution, does not cross the blood-brain barrier.

Metabolism/Excretion: Some metabolism; 85% excreted unchanged in urine.

Half-Life: 15 hr (oral).

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
SUBQrapid0.5 hr24–48 hr
POrapid1.5 hrunknown



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: sweating

GI: abdominal pain, flatulence, nausea, diarrhea

Neuro: dizziness

Misc: opioid withdrawal

Interactions

Drug-drug:

Route/Dosage

Opioid-Induced Constipation in Patients with Advanced Illness

Renal Impairment

Renal Impairment

Renal Impairment

Renal Impairment

Renal Impairment

Opioid-Induced Constipation in Patients with Non-Cancer Pain

Renal Impairment

Renal Impairment

Hepatic Impairment

Hepatic Impairment

Hepatic Impairment

Hepatic Impairment

Hepatic Impairment

Availability

Assessment

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Relistor

Code

NDC Code