Drug reference

Naloxone

Opioid Analgesic · Antidote for Opioid Overdose

Also known as naloxone hydrochloride

Opioid AnalgesicAntidote for Opioid OverdoseATC V03AB15

CDSCO approvedSchedule HATC V03AB15

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Manufacturers advise avoid—no information

FDA category + note

Top interactionssee all 12 →

NaltrexoneContraindicatedTextbookG&G 14e · p527, p528, p529
AcetaminophenSevereTextbookHarrison 22e · p98-99
AlprazolamSevereTextbookG&G 14e
BarbituratesSevereTextbookKDT 7e · p401

Mechanism

Naloxone reverses the effects of opioid analgesics, including respiratory depression. It can be given as an antidote for loperamide overdose.

Indications

Reversal of respiratory depression caused by opioid analgesicsAntidote for loperamide overdoseopioid-induced toxicity (especially respiratory depression)neonatal respiratory depression secondary to opioids given to motherAcute treatment of opioid overdoseCombined with buprenorphine in buprenorphine maintenance therapyOpioid-induced constipation (in fixed combination with oxycodone)Opioid overdosedrug of choice for morphine poisoningreversing neonatal asphyxia due to opioid use during labourtreating overdose with other opioids and agonist-antagonists (except buprenorphine)reversing respiratory depression due to intraoperative use of opioidsadjunct to intraspinal opioid analgesia (reverses respiratory depression without abolishing pain relief)diagnosis of opioid dependencepartially reverses alcohol intoxication

Dosing

Adult: REACTIONS WITH HIGH DOSES OF LOPERAMIDE ASSOCIATED WITH ABUSE OR MISUSE (SEPTEMBER 2017) Serious cardiovascular events (such as QT prolongation, torsades de pointes, and cardiac arrest), including fatalities, have been reported in association with large overdoses of loperamide. Healthcare professionals are reminded that if symptoms of overdose occur, naloxone can be given as an antidote.…
Pediatric: 10 μg/kg intravenously, intramuscularly, or subcutaneously (for neonatal respiratory depression)

Pharmacokinetics

Onset

Acts in 2–3 min i.v.

Duration

1–3 hours

Half-life

1 h (plasma)

Bioavailability

Inactive orally because of high first pass metabolism.

Metabolism

Extensive first-pass metabolism by the liver (primarily conjugation with glucuronic acid)

Contraindications

opioid-dependent subjects (may precipitate withdrawal)

Side effects

Common

AgitationNauseaVomitingTachycardiaConstipationDiarrhea

Serious

precipitation of withdrawal syndrome (in opioid-dependent individuals)
hypertension
tachycardia
ventricular arrhythmias
pulmonary edema (due to rebound catecholamine release)
Precipitates opioid withdrawal
may include rise in BP
pulmonary edema (uncommon)

Pregnancy & lactation

Pregnancy

Manufacturers advise avoid—no information

Drug interactions

Naltrexone

Contraindicated

Textbook

Blocks the analgesic effects of opioid analgesics. Can precipitate severe withdrawal symptoms in an opioid-dependent patient.

Naltrexone is contraindicated in patients taking opioids concurrently. If opioid analgesics are needed for pain management, higher doses may be required and should be administered under strict medical supervision after considering the risks.

Source: G&G 14e · p527, p528, p529

Acetaminophen

Severe

Textbook

Acetaminophen-related hepatotoxicity, a significant cause for liver failure.

Many practitioners have moved away from opioid-acetaminophen combination analgesics to avoid the risk of excessive acetaminophen exposure.

Source: Harrison 22e · p98-99

Alprazolam

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Barbiturates

Severe

Textbook

Exaggerated CNS depression.

Source: KDT 7e · p401

Benzodiazepines

Severe

Textbook

Marked depression of respiration, cardiac contractility, and blood pressure.

Carefully monitor respiratory and cardiovascular functions when co-administering benzodiazepines with opioids due to increased risk of severe depression of vital signs.

Source: KDT 7e · p383

Chloral Hydrate

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Chlordiazepoxide Hydrochloride

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.