- Metabolized to cysteine → Regeneration of sulphydril groups and glutathione
- acting as an alternate substrate for conjugation
- reduces disulfide bonds in mucoproteins

Reversal of MoP receptor effects such as sedation, hypotension, respiratory depression, and the dysphoric effects of partial agonists
Will precipitate acute withdrawal symptoms in opiate addicts

- Reduces hepatotoxicity
- mucolytic

- CVS: > 0.3 mg/kg → ↑MAP
- RESP: nil
- CNS: Drowsiness at high dose, Decreased pain tolerance
- OTHER: Sphincter of oddi spasm

PO: BA low

91% absorption but Oral BA 2% due to extensive first-pass metabolism

66-97%
Albumin

46%

0.5 L/kg

2 L/kg
Highly lipid soluble

Liver
Deacetylated to cysteine -> normal metabolism (Rapid)

Liver
via glucuronidation to naloxone-3-glucouronide

Unchanged: 40% urine, 3% feces

25 ml/min/kg

5.5 hrs

0.5-1.5 hrs

usually in 1st hr:
- rash around infusion site
- angiooedema
- bronchospasm
- hypo/hyper tension

Mx: stop, give antihistamine, then restart at slowest infusion rate

Rapid onset of withdrawal symptoms in opioid drug addiction
At High Doses:
- Hypertension
- Tachycardia
- Arrhythmias

Synthetic derivative of cysteine

substituted oxymorphone derivative.
pKa = 8.0

Antidote

Antidote

- paracetamol overdose
- non-paracetamol induced fulminant hepatic failure
- prevention of contrast nephropathy
- mucolytic therapy

- the reversal of respiratory depression due to opioids
- the diagnosis of suspected opioid overdose and has been used in the
treatment of.
- clonidine overdose

Level 3

Level 3

antioxidant and glutathione inducer

competitive antagonist at mu-, delta-,
kappa-, and sigma-opioid receptors

Duration: short

Onset: 1-3 mins
Peak effect: 15 mins
Duration: 30 mins
> Less than the effect site time of most opioids → requirement for repeat dosing or infusion.

IV or oral formulation
200mg/mL
compatible with 5% dextrose

clear solution for injection containing 0.02/0.4 mg/ml of naloxone hydrochloride

IV, PO, Neb (inhaled)

IV:
1st : 150mg/kg in 200ml dextrose over 15mins
2nd : 50mg/kg in 500ml over 4hrs
3rd : 100mg/kg in 1l over 16hrs

IV/IM

- Reversal of post-operative respiratory depression and coma: 20-40mcg IV PRN
- For opioid overdose reversal 0.4-2 mg IM/IV → Via infusion a 5mcg/kg/hr
- Reversal of S/Es of opioids: 1-4 mcg/kg
- Increased cardiac contractility in septic shock at doses 1mg/kg IV

effective in alleviating the pruritus, nausea,
and respiratory depression associated with the epidural or spinal administration of opioids.