DRUG

Morphine

Fentanyl

Remifentanil

Nalbuphine
 MOD

Narcotic agonist-analgesic of opiate receptors; inhibits ascending pain pathways, thus altering response to pain; produces

Narcotic agonist-analgesic of opiate receptors; inhibits ascending pain pathways, thus altering response to pain; increases

Opioid agonist; inhibits ascending pain pathways, which causes alteration in response to pain; produces analgesia, respirat

Narcotic agonist-analgesic of kappa opiate receptors and partial antagonist of mu opiate receptors; inhibits ascending pain
ROUTE DISTRIBUTION DOSE/INDUCTING DOSE ONSET

Protein bound:
IV, 36%
Vd: IV, 1-4.7
PO, IV L/kg 0.15-0.2 mg/kg PO, 15-30 min; IV <5 min

Protein bound:
80-85%
IM, IV Vd: 4-6 L/kg 1-2 mcg/kg IV, immediate; IM, 7-15 min

Protein Bound:
70%
IV Vd: 100 mL/kg 0.5-1 mcg/kg 1-3 min (IV)
Protein Bound:
IM, IV 50% 0.5-1 mg/kg IM, 15 min; IV, 2-3 min
 DURATION OF ACTION SIGNIFICANT METABOLITE

4 hr (immediate release) 6-Glucuronide, 3,6-diglucuronide, 3-glucuronide

IV, 0.5-1 hr; IM, 1-2 hr Nor-fentanyl, hydroxyfentanyl, and hydroxynorfentanyl

Very-short acting Remifentanil acid

3-6 hr Glucoronide conjugates

 HALF LIFE METABOLISM

2-4 hr (immediate release) Metabolized in liver via conjugation with glucuronic acid

2-4 hr Metabolized in liver by CYP3A4

3-10 min Cleaved by non-specific plasma and tissue esterases

5 hr Metabolized in liver (glucoronidation)

 ELIMINATION REVERSAL AGENT/ANTIDOTE

Urine (2-12%), feces (7-10%) Naloxone

Total plasma clearance: 8.3

mL/min/kg

Excretion: Urine (75%), feces

(9%) Naloxone

Clearance: 40 mL/min/kg

Excretion: Urine Naloxone

Excretion: Urine, feces Naloxone