Competitive opioid antagonists bind to the opioid receptors with higher affinity than agonists, but do not activate the receptors.
Displacing the agonist, attenuated or reverses the agonist effects.
A synthetic congener of oxymorphone.
Available as an intravenous, intramuscularly,subcutaneous administered drug forms, and intranasal forms.
Indicated for complete or partial reversal of opioid depression, including respiratory depression.
Indicated for diagnosis of suspected or known acute opioid overdosage.
May be useful as an adjunct to increase blood pressure in septic shock.
Most rapid onset of action occurs when the drug is administered intravenously.
Usual dose of .04 mg to 2 mg is administered intravenously,/ intramuscularly and the dose may be repeated at two to three minute intervals.
The elimination half-life of naloxone can be shorter than that of the opioid itself, so repeat dosing or continuous infusion may be required.
If no response is noted after 10 mg of the drug has been administered the diagnosis of opioid toxicity should be questioned.
Crosses the blood brain barrier as a mu-receptor antagonist.
Overdoses results from opioid’s agonist effects at the mu-opioid receptor, located on the brain stem neurons that control breathing.
The mu-opioid receptor antagonist naloxone can reverse an overdose, if it administered shortly after the overdose occurs.
Utilized, in small doses, for partial reversal of opioid respiratory depression associated with analgesics with surgery.
Too rapid of opioid reversal may be associated with nausea, vomiting, sweating and circulatory stress.
Side effects with the use of this agent postoperatively include hypotension, hypertension, ventricular tachycardia, ventricular fibrillation, dyspnea, pulmonary edema and cardiac arrest.
Abrupt reversal of opioid effects in patients physically dependent on opioid may precipitate acute withdrawal syndrome, body aches, fever, sweating, runny nose, sneezing, piloerection, yawning, shivering weakness nervousness, restlessness, irritability, nausea, vomiting, diarrhea, abdominal cramps, hypertension, tachycardia.
Patients with an opioid overdose require restoration of ventilation and oxygenation through artificial means, or reversal of opioid-induced respiratory depression with naloxone.
Time we administration of naloxone is often sufficient to count the life-threatening respiratory depression.
Neonates may experience opioid withdrawal with convulsions, irritability, excessive crying and hyperactive reflexes.
Large doses are required to antagonize buprenorphine.
In opioid addicts methohexital (Brevital), a barbiturate, can block the acute onset of withdrawal symptoms.
Coprescribing naloxone with long-term opioids significantly reduced opioid-related emergency department (ED) visits by 63% at 1 year.
Available intravenously and as a nasal spray.
The US Food and Drug Administration (FDA) has approved for generic naloxone hydrochloride nasal spray that can stop or reverse the effects of an opioid overdose.
Naloxone nasal spray is the first for use in the community setting by individuals who have no medical training.
Intranasal naloxone at a dose of 4 mg offers effective and ease of administration for patients receiving long-term opioid therapy.
It delivers a consistent, measured dose when used as directed., for both adults and children.
The drug is sprayed into one nostril while the patient is lying on his or her back.
Higher dose intranasal naloxone formulation for emergencytreatment of opioid overdose has been approved.
A single spray of new formulation delivers 8 mg.