Nalmefene (Selincro) Flashcards
Brand name
Selincro
Class
Opioid receptor antagonist - mu and delta receptors;
kappa receptor partial agonist
Use
Reduce alcohol consumption in patients with alcohol dependence who have a high drinking risk level
MOA
- blockade of mu opioid receptors prevents pleasurable effects of alcohol
- kappa receptor blockade reduces dysphoria
- So reduces rewarding effects of alcohol and cravings
How long until it works
Immediately, so can be used as needed
Tests
Baseline LFTs maybe
S/Es
- N/V, dizziness, insomnia, headache
- Confusion, rare hallucinations
Switch to another agent if S/Es persist
Dosing
- 18 mg/day tablet as needed (18 mg/day is max)
- after first visit, pt should keep record of alcohol use for 2 weeks- if high drinking risk, start nalmefene
- take as needed (1-2 hours before anticipated time of drinking; asap if already started drinking)
- Patient has to be OPIOID FREE for 7-10 days prior to initiating t/t
- don’t chew or crush tablet - can sensitize skin
- with or without food
Overdose symtoms
no known effects
Can use upto
1 year
Taper or not
No need
Half life
12.5 hours; metabolized by liver
Drug interactions
*Increased resp depression when takes with other CNS depressants; consider dose reduction
*UGT2B7 inhibitors (diclofenac, fluconazole, medroxyprogesterone acetate, meclofenamic acid) can increase nalmefene levels
UGT2B7 inducers (dexamethasone, phenobarbital, rifampicin, omeprazole) can decrease levels
Warning/precautions
- Pt has to be opioid free for 7-10 days
- Stop 1 week before anticipated use of opioids (eg surgery)
- Risk of resp depression with CNS depressants
C/I
- Current opioid use
- Acute opioid withdrawal
- Severe renal or hepatic impairment
- Recent history of alcohol withdrawal symptoms
- Galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption
- Allergy
