update: naloxone

Naloxone is used with caution in the elderly and given to pregnant or lactating mothers only if absolutely necessary1. Observe for convulsions, excessive crying and hyperactive reflexes in neonates born to mothers with opioid dependence1. Close monitoring of the patient is required to detect when repeated doses of naloxone are required2. The duration of most opioids exceeds the half life of naloxone1. Ensure the resuscitation trolley is immediately available. Reversing opioid depression in the post operative period may induce nausea, vomiting, tachycardia, hypertension, tremors, seizures, arrhythmias or cardiac arrest1. Consequently, be cautious if your patient has a history of cardiovascular disease. Central nervous system effects include seizures and parasthesia1. Agitation, hallucination, hot flushes and tremors have been reported, especially in patients who are in pain1. Of note, dyspnoea and paradoxical respiratory depression may occur. Hypertension or hypotension may develop; however, elevated blood pressure is the more common event. ADMINISTRATION Naloxone is given predominantly in emergency situations, deeming the intravenous route appropriate in most cases1. Naloxone can be prepared as an infusion if required1. Some brands of naloxone are available in a pre-filled syringe1. Continuous surveillance of the patient is essential2. The intravenous dosage varies according to the underlying cause of opioid depression. Adults in suspected or known overdosage usually respond to 0.4mg to 2mg increments of naloxone every two to three minutes1. Conditions unresponsive to a cumulative dosage of 10mg are likely to be non opioid in origin1. Reduced dosage is used to reverse opioid depression in the post operative patient; 0.1mg to 0.2mg increments are sufficient1. Increments are titrated to effect based on respiratory recovery without the loss of analgesia. Children in known or suspected opioid overdosage are administered 0.01mg/kg of intravenous naloxone1. If no improvement is seen, an additional 0.1mg/kg dose is given. Children in postoperative opioid depression are given very small increments every two to three minutes until the desired reversal is achieved1. Neonates are administered 0.01mg/ kg increments of naloxone in IV, intramuscular or subcutaneous form1. REFERENCES

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In this clinical update you will read about the pharmacology of naloxone, a drug indicated in the reversal of opioids. GENERIC NAME Naloxone hydrochloride1. TRADE NAMES Naloxone, suboxone (sublingual tablets)1. DRUG CLASS Schedule 4 opioid antagonist1. INDICATIONS Naloxone is indicated for the reversal of opioid depression caused by natural or synthetic opioids2. Respiratory depression is the most obvious sign of narcosis. Sedation and hypotension are also reversed by naloxone1. Naloxone is diagnostic in known or suspected opioid overdosage. ACTIONS Naloxone competes for opiate receptors located in the central nervous system2. Circulating opioids cannot bind to these receptors, minimising their effect. The most rapid onset of action is achieved after intravenous administration (IV); however, intramuscular or subcutaneous routes are an alternative if IV access is unavailable1. Intravenous naloxone has a shorter half life than the same dose given intramuscularly. CONTRAINDICATIONS Naloxone is generally well tolerated. It is avoided in patients with a known hypersensitivity to the drug or its additives1. PRECAUTIONS Reversing the effects of opioids in a narcotised patient will also reverse analgesic effects and will induce acute withdrawal syndrome in patients who are physically dependent on opioids1. Therefore, the roused patient may be in pain or experiencing acute withdrawal. Box one lists the signs and symptoms of acute withdrawal from opioids.

Naloxone is ineffective in patients given non-opioid drugs

ADVERSE EFFECTS Are broadly categorised according to opioid dependence or the post operative period. Abrupt reversal of opioids in the dependent patient will likely result in acute withdrawal syndrome and the signs and symptoms listed in Box one. The possible adverse effects observed in the post operative patient (not in acute withdrawal) are; nausea, vomiting, tachycardia, hypertension, tremors, seizures, arrhythmias, heart failure, acute pulmonary oedema or cardiac arrest1.

Box 1 Signs and symptoms of acute withdrawal from opioids 1 Abdominal cramps and diarrhoea Fever Hypertension Irritability, shivering or trembling Myalgia Nausea and vomiting Piloerection Sneezing and runny nose Tachycardia

1.

Naloxone (2009). MIMS online. Retrieved 8 April 2011 from MIMS database, MIMS Australia (ANF). Eckman, M., Labus, D., & Thompson, G. (Eds.). (2009). Nursing Pharmacology Made Incredibly Easy (2nd ed.). Sydney: Lippincott, Williams and Wilkins.

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