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

- unclear
- may involve establishment of concentration gradient away from primary site of action of LA

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

- energy substrate (essential fatty acids)
- managing lipophilic drug overdose by binding and facilitating clearance

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

IV only

46%

None

2 L/kg
Highly lipid soluble

Wide - distributed to fat and tissues

Liver
via glucuronidation to naloxone-3-glucouronide

Liver
Broken down to Fatty acids and glycerol

Liver and kidneys

25 ml/min/kg

0.5-1.5 hrs

not well defined

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

- Fat embolism
- Hyperlipidemia, pancreatitis
- Hepatic dysfunction
- Allergic reactions

substituted oxymorphone derivative.
pKa = 8.0

fat emulsion

Antidote

Antidote

Antidotes

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

- TPN mixtures
- Local anaesthetic toxicity with or without circulatory arrest
- Prevention of essential fatty acid deficiency syndrome

Level 3

Level 3

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

- Energy substrate
- Reverse local anaesthetic cardiotoxicity

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.

(For LA tox)
onset: minutes
peak: 15-30mins

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

white, oil-water emulsion with 20% soybean oil, egg yolk phospholipids, glycerin, sodium hydroxide and water

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

IV

For LA tox: 1.5ml/kg bolus over 1 minute →
Infusion 15 ml/kg/hr

If not stabilized, two subsequent boluses may be given 5 mins apark.
Then rate doubled to 30ml/kg/hr

Max cumulative dose 12ml/kg

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

serum amylase or lipase should be monitored for
2 days