Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 65mcg/1.3mL
Pruritus
Indicated for moderate-to-severe pruritus associated with chronic kidney disease in adults undergoing hemodialysis (HD)
0.5 mcg/kg IV push into venous line of dialysis circuit at the end of each HD treatment
Dosage Modifications
Hepatic impairment
- Mild-to-moderate: No dosage adjustment needed
- Severe: Pharmacokinetics not evaluated; use not recommended
Dosing Considerations
Limitation of use
- Not studied in patients on peritoneal dialysis; use not recommended
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
1-10%
Diarrhea (9%)
Dizziness (6.8%)
Nausea (6.6%)
Gait disturbances (6.6%)
Hyperkalemia (4.7%)
Headache (4.5%)
Somnolence (4.2%)
Mental status change (3.3%)
Warnings
Contraindications
None
Cautions
Dizziness, somnolence, mental status changes, and gait disturbances (eg, falls) have occurred; may subside over time with continued treatment
May impair mental or physical abilities; advise patients not to drive or operate dangerous machinery until effect on a patient’s ability to drive or operate machinery is known
Drug interaction overview
- Centrally acting depressant medications, sedating antihistamines, and opioid analgesics may increase the adverse reactions of difelikefalin; use with caution
Pregnancy & Lactation
Pregnancy
Limited human data are insufficient on use in pregnant females to evaluate drug-associated risks for major birth defects or miscarriage
Lactation
There are no data regarding drug presence in human milk, effects on breastfed infants, or effects on milk production
Studies showed difelikefalin was transferred into milk in lactating rats
When a drug is present in animal milk, it is likely that the drug will be present in human milk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Kappa opioid receptor (KOR) agonist
Relevance of KOR activation to therapeutic effectiveness is unknown
Absorption
Steady-state was reached after second dose
Mean accumulation ratio: 1.6
Distribution
Vd: 238 mL/kg
Protein bound: 23-28%
Elimination
Half-life (before dialysis): 23-31 hr
Excretion: Urine (11%); feces (59%); dialysate fluid (20%)
Administration
IV Preparation
Do not mix or dilute before administration
Visually inspect vials for particulate matter and discoloration before administering; solution should be clear and colorless; discard vials if particulate matter or discoloration is observed
Vials are for single-dose use; discard any unused product
May use the following formula to determine total injection volume on target body weight or may refer to prescribing information
Total injection volume (mL) = Patient target dry body weight (kg) x 0.01, rounded to the nearest tenth (0.1 mL)
IV Administration
Administer after blood is no longer circulating through the dialyzer; dialyzer membrane removes difelikefalin
Administer IV push into venous line of the dialysis circuit at the end of each HD session
May be given either during or after rinse back of dialysis circuit
Dose given after rinse back: Administer into venous line followed by ≥10 mL of 0.9% NaCl flush
Dose given during rinse back: No additional 0.9% NaCl is needed to flush line
Administer within 60 minutes of syringe preparation; discard any unused product
Missed regularly scheduled HD treatment: Resume at the end of next HD treatment
Storage
Unopened vials
- Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
- Do not freeze
Prepared syringe
- Store at 20-25ºC (68-77ºF); discard after 60 minutes of syringe preparation
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
