Emergent Care / Stabilization:
Emergency treatment with airway stabilization, ventilatory support, and cardiovascular support are the priorities in acute opioid overdose. See naloxone administration for dosage / administration, indications, contraindications, monitoring, adverse effects, toxicity, and mechanism of action information.

Diagnosis Overview:
Opioids are found in many formulations and products, including prescription opioids for pain and cough suppression (natural and semisynthetic opioids such as codeine, oxycodone, hydrocodone), methadone, other synthetic opioids (eg, tramadol and fentanyl), and illicit drugs such as heroin and other novel nonpharmaceutical fentanyl analogs produced in clandestine laboratories. Nonopioid illicit drugs such as cocaine and methamphetamine have been adulterated with the opioid fentanyl.

Opioids act as agonists on various opioid receptors, with most of the physiological effects occurring at the μ receptor. Opioids are ingested via a variety of routes, including oral, subcutaneous, intravenous, intramuscular, inhalational, sublingual, intranasal, buccal, transmucosal, and dermal. Therapeutic and toxic doses are difficult to predict because of the development of tolerance with chronic use.

The hallmark of opioid overdose and toxicity is CNS and respiratory depression, which can lead to hypoxic cardiac arrest. Opioid toxicity is a clinical diagnosis. The opioid receptor antagonist naloxone will competitively antagonize the opioid at the level of the receptor, reversing CNS depression and stimulating respiration. Opioid overdose is characterized by a toxidrome that includes reduced consciousness / coma, miosis, and reduced respiratory rate and blood pressure.

Use of an opioid after a period of abstinence, such as occurring after incarceration, is a risk factor for CNS depression and cardiovascular embarrassment. A return to use at a previously tolerated dose constitutes an overdose for these relatively naïve individuals. Patients with hepatic or renal disease have an increased risk of toxicity from accumulation of the parent drug and/or active metabolites. Patients with decreased physiological reserve and a poor baseline respiratory function (congestive heart failure, chronic obstructive lung disease, obesity, sleep apnea) are more susceptible to opioid toxicity.

Combined ingestion of any sedative substance or respiratory depressant (ethanol, benzodiazepines, barbiturates) predisposes to increased risk of opioid toxicity.

Tianeptine is an unregulated antidepressant not approved for use in the United States that can produce adverse effects and result in dependence. Per the US Centers for Disease Control and Prevention (CDC), the clinical effects of tianeptine abuse and withdrawal can mimic opioid toxicity and withdrawal. Elixir, tablet, and powder formulations are available for purchase (online and at gas stations / convenience stores) under many brand names (eg, Stablon, Tatinol, Coaxil, Neptune's Fix, Pegasus, Zaza, Tianaa). They may be adulterated with synthetic cannabinoid receptor agonists or other drugs that can produce severe adverse effects. Be aware of potential tianeptine ingestion in patients with a history of opioid use disorder or dependence who present with altered mental status; other reported effects include tachycardia, hypotension, seizure, prolonged QT interval, prolonged QRS duration, and cardiac arrest.

Pediatric patient considerations: Pediatric patients manifest the same clinical signs and symptoms of overdose as adults. Treatment for respiratory depression is the same: airway and respiratory support and antidotal therapy with naloxone.

Resources for opioid prescribing guidelines, as well as nonopioid alternatives, can be found here.

Related topics: opioid use disorder, opioid withdrawal syndrome