difelikefalin

REMS

Moderate to severe pruritus associated with chronic kidney disease in patients undergoing hemodialysis.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

None.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of sedation in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

F and E: hyperkalemia

GI: diarrhea, nausea

Neuro: dizziness, gait disturbances, headache, mental status changes, sedation

Interactions ⬆ ⬇

Drug-drug:

Use with benzodiazepines or other CNS depressants, including other opioids, nonbenzodiazepine sedative/hypnotics, anxiolytics, antihistamines, and alcohol, may ↑ risk of sedation, dizziness, gait disturbances, and mental status changes.

Availability ⬆ ⬇

Solution for injection: 50 mcg/mL

Route/Dosage ⬆ ⬇

Dose should be based on target dry body weight.

IV (Adults ): 0.5 mcg/kg administered into the venous line of the dialysis circuit at the end of each hemodialysis treatment.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a kappa opioid agonist. Mechanism for effectiveness in pruritus unknown.

Therapeutic effects:

Reduced severity of itching.

Classifications ⬆ ⬇

Therapeutic Classification: none assigned

Pharmacologic Classification: opioid agonists

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Not metabolized by CYP450 isoenzymes. Primarily excreted in feces (59%), with 20% excreted into dialysate fluid, and 11% excreted in urine.

Half-Life: 23–31 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of difelikefalin to patient. Advise patient to read Patient Information before starting therapy and periodically during therapy in case of changes.
May cause dizziness. Driving or operating machinery not recommended until effects are understood.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇