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Indications

REMS

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:

Availability

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

US Brand Names

Relistor

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: laxatives

Pharmacologic Classification: opioid antagonists

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

Patient/Family Teaching

Pronunciation

me-thil-nal-TREX-one

Code

NDC Code*