Naloxone Pharmacology


About Naloxone
A ?-opioid receptor competitive antagonist, Narcotic antagonist.
Mechanism of Action of Naloxone
Naloxone is a pure semisynthetic opiate antagonist. It acts as a competitive antagonist at mu, kappa and delta opiate receptors in the CNS. It reversibly and completely blocks all the opioid receptors (mu, kappa and delta).
Pharmacokinets of Naloxone
Absorption: Naloxone is rapidly inactivated after oral administration and it should be administered parenterally.
Distribution: It is widely distributed in the body tissues and fluid. Naloxone crosses the placenta.
Metabolism: Naloxone undergoes metabolism in the liver mainly by glucuronide conjugation.
Excretion: It is excreted mainly in the urine.
Onset of Action for Naloxone
1 - 2 minutes(IV), 2 - 5 minutes(IM or SC)
Duration of Action for Naloxone
Half Life of Naloxone
30-80 minutes in adults and about 3 hours in neonates
Side Effects of Naloxone
5.Cardiac arrhythmias
6.Pulmonary oedema
8.Ventricular fibrillation
Contra-indications of Naloxone
1.Hypersensitivity to Naloxone
2.Patient on Opioid therapy
3.Acute opioid withdrawal
4.Liver failure
Special Precautions while taking Naloxone
1.Hepatic impairment
2.Renal impairment
3.Opioid dependence
4.Cardiac disease
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Indications for Naloxone
1.Opioid poisoning
2.Opioid-induced respiratory depression
Interactions for Naloxone
Typical Dosage for Naloxone
Postoperative Opiate Depression: 0.1-0.2 mg IV in adults or 0.005-0.01 mg IV in children, given at 2- to 3-minute intervals until the desired response is obtained. Dose can be repeated IV or IM after 1 - 2 hour intervals depending on the response of the patient and the dosage and duration of action of the opiate administered.
Neonatal Opiate Depression: 0.01 mg/kg, administered into the umbilical vein of the neonate at 2- to 3-minute intervals until the desired response is obtained. If required doses may be repeated at 1- 2 hour intervals depending on the response of the neonate and the dosage and duration of action of the opiate administered to the mother. When the IV route cannot be used, the drug may be administered by IM or subcutaneous injection.
Opioid poisoning:
Adult: 0.4-2 mg IV, administered at 2- to 3-minute intervals if necessary.
Children: 0.01 mg/kg; if this dose does not produce the desired degree of response, a subsequent dose of 0.1 mg/kg may be administered.
Opiate addiction (oral): 200 mg to 3 g daily.
Schedule of Naloxone
Storage Requirements for Naloxone
Store at 15 - 30 degree C. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Naloxone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Naloxone
Give supportive measures and symptomatic treatment.

Home Delivery for Naloxone in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including naloxone.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for naloxone and other medicines and health products. Home delivery services for naloxone may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take naloxone only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for naloxone before they complete the sale. You can get this information while placing the order for naloxone with the pharmacy.

Naloxone is a generic medicine name and there are several brands available for it. Some of the brands for naloxone might be better known than naloxone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have naloxone in stock, you can ask for one of the branded alternatives for naloxone.