Opioids and CNS Depressants Quiz
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Questions and Answers

What is a primary use of opioids?

  • To induce sleep deprivation
  • To increase brain activity
  • To treat autoimmune diseases
  • To relieve pain (correct)
  • Which of the following is a natural opioid?

  • Fentanyl
  • Oxycodone
  • Codeine (correct)
  • Hydrocodone
  • Which type of drug is used to treat anxiety and panic attacks?

  • Antipsychotics
  • CNS depressants (correct)
  • Antidepressants
  • CNS stimulants
  • What is a potential effect of CNS depressants?

    <p>Slowed brain activity (A)</p> Signup and view all the answers

    What type of opioid is heroin classified as?

    <p>Semi-synthetic opioid (C)</p> Signup and view all the answers

    The CNS depressants category includes which of the following?

    <p>Opioids (D)</p> Signup and view all the answers

    What is a key characteristic of cyclic antidepressants (TCAs) in overdose situations?

    <p>HCO3 is used in management (B)</p> Signup and view all the answers

    Which is a common symptom of benzodiazepines toxicity?

    <p>Drowsiness and confusion (C)</p> Signup and view all the answers

    What is the most common route of opioid exposure?

    <p>Accidental exposure (C)</p> Signup and view all the answers

    Which effect is caused by opioids on gastrointestinal motility?

    <p>Increased segmental GIT motility (A)</p> Signup and view all the answers

    Which opioid receptor primarily mediates analgesia and euphoria?

    <p>Mu (m) (A)</p> Signup and view all the answers

    What respiratory sign is commonly associated with opioid toxicity?

    <p>Respiratory depression (C)</p> Signup and view all the answers

    What is opioid-induced intolerance characterized by?

    <p>Desensitization of opioid receptors (D)</p> Signup and view all the answers

    What is a common effect of opioids on the urinary system?

    <p>Urine retention (A)</p> Signup and view all the answers

    What is one of the toxicological actions of opioids?

    <p>Depressed respiratory function (C)</p> Signup and view all the answers

    Which diagnostic method is used to confirm opioid toxicity?

    <p>Toxicological screening (C)</p> Signup and view all the answers

    Which of the following symptoms is NOT associated with opioid overdose?

    <p>High metabolic activity (D)</p> Signup and view all the answers

    What complication can arise from the gastrointestinal actions of opioids?

    <p>Constipation (C)</p> Signup and view all the answers

    What sign would NOT indicate opioid toxicity in a patient?

    <p>Hypertension (C)</p> Signup and view all the answers

    What adverse effect can opioids cause related to bronchial function?

    <p>Bronchospasm (C)</p> Signup and view all the answers

    Within which system do opioids exert combined stimulation and depression effects?

    <p>Central nervous system (CNS) (D)</p> Signup and view all the answers

    What does 'drug idiosyncrasy' refer to in the context of opioid use?

    <p>Reactions occurring in a small fraction of patients (D)</p> Signup and view all the answers

    Which symptom is related to the histamine release associated with opioids?

    <p>Itching (C)</p> Signup and view all the answers

    What type of intoxication might a child experience from accidental opioid exposure?

    <p>Acute intoxication (B)</p> Signup and view all the answers

    What is a common clinical manifestation of TCA toxicity that may indicate the need for immediate intervention?

    <p>Decreased level of consciousness (C)</p> Signup and view all the answers

    Which of the following is the first drug of choice for treating cardiac arrhythmias in TCA toxicity?

    <p>Sodium bicarbonate (C)</p> Signup and view all the answers

    In the presence of CNS depression due to TCA toxicity, what is the recommended initial procedure?

    <p>Early intubation (C)</p> Signup and view all the answers

    Which of the following assessments is NOT part of the non-toxicological investigations for TCA toxicity?

    <p>Serum drug level (A)</p> Signup and view all the answers

    What complication may occur rapidly during TCA toxicity due to agitation and seizures?

    <p>Pulmonary edema (A)</p> Signup and view all the answers

    What is the primary role of naloxone in relation to opioid receptors?

    <p>It acts as a competitive antagonist at mu opioid receptors. (B)</p> Signup and view all the answers

    Which of the following is NOT an adverse effect associated with naloxone administration?

    <p>Nausea (C)</p> Signup and view all the answers

    What is the standard dose of naloxone for adults as an IV bolus?

    <p>0.4-0.8 mg (A)</p> Signup and view all the answers

    What significant effect do benzodiazepines have when administered in large oral doses?

    <p>Significant respiratory depression. (D)</p> Signup and view all the answers

    Which patient populations may experience prolonged elimination of some benzodiazepines?

    <p>Elderly patients and those with liver disease (C)</p> Signup and view all the answers

    What is the mechanism through which benzodiazepines exert their effects?

    <p>Enhancement of the inhibitory actions of GABA (D)</p> Signup and view all the answers

    What is a common complication associated with benzodiazepine toxicity?

    <p>Aspiration pneumonia (A)</p> Signup and view all the answers

    Which of the following represents a part of the management for benzodiazepine toxicity?

    <p>Gastric lavage if in coma (B)</p> Signup and view all the answers

    What is a primary use of flumazenil?

    <p>To reverse benzodiazepine-induced sedation (B)</p> Signup and view all the answers

    Why are diuresis and dialysis not effective for TCA overdose?

    <p>TCAs are highly protein bound and have large volumes of distribution (B)</p> Signup and view all the answers

    Which of the following effects is associated with TCA action?

    <p>Inhibition of neurotransmitter reuptake (D)</p> Signup and view all the answers

    Which symptom is NOT typically associated with TCA toxicity?

    <p>Excessive salivation (C)</p> Signup and view all the answers

    Which mechanism contributes to the arrhythmogenic effect of TCAs?

    <p>Sodium channel blockade (B)</p> Signup and view all the answers

    What is a potential CNS effect of TCA toxicity?

    <p>Stimulation followed by depression (B)</p> Signup and view all the answers

    Which of the following is the result of α-adrenergic receptor antagonism by TCAs?

    <p>Orthostatic hypotension (B)</p> Signup and view all the answers

    In which scenario is flumazenil NOT recommended?

    <p>Benzodiazepine overdose due to addiction (B)</p> Signup and view all the answers

    Flashcards

    CNS depressants

    Drugs that slow down brain activity, used to treat conditions like insomnia, anxiety, pain, and seizures.

    Opioids

    A class of drugs derived from the opium poppy plant or synthetic with similar properties, primarily used for pain relief.

    Overdose

    A state of being overwhelmed by the effects of a drug, often leading to serious health problems.

    Withdrawal

    A group of symptoms that occur when a person stops using a drug they are dependent on.

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    Natural opioids

    Naturally occurring opioids, examples include morphine and codeine.

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    Semisynthetic opioids

    Opioids that are chemically modified from natural opioids, examples include heroin and apomorphine.

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    Synthetic opioids

    Opioids that are completely manufactured, examples include methadone and pethidine.

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    Opioid overdose

    A condition that occurs when someone takes too many opioids, potentially leading to respiratory depression and death.

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    Accidental Opioid Exposure

    The most common way people are exposed to opioids, often due to accidental ingestion or misuse.

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    Opioid-Induced Intolerance

    A state of decreased responsiveness to a drug, requiring higher doses to achieve the desired effect.

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    Drug Idiosyncrasy

    A rare and unpredictable reaction to a drug, not related to dose or treatment duration.

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    Mu (μ) Opioid Receptor

    The primary receptor targeted by most opioid analgesics, responsible for analgesia, euphoria, respiratory depression, and dependence.

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    Depressed Respiratory Function (Opioids)

    Opioids primarily affect respiratory function by suppressing it, leading to slowed breathing.

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    Altered Consciousness (Opioids)

    Opioids can induce a state of altered consciousness, ranging from drowsiness to deep sedation.

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    Cardiovascular Suppression (Opioids)

    Opioids can suppress cardiovascular function by impacting the vasomotor center.

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    Gastrointestinal Complications (Opioids)

    Opioids often cause constipation due to their effects on the gastrointestinal system.

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    TCA Toxicity

    A life-threatening condition characterized by decreased level of consciousness, QRS prolongation, and potentially anticholinergic symptoms, caused by overdose of Tricyclic Antidepressants (TCAs).

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    Anticholinergic Toxidrome

    A constellation of symptoms often observed in TCA overdose, including dry mouth, blurred vision, constipation, urinary retention, and dilated pupils.

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    Toxicological Assessment for TCA

    A diagnostic tool used to evaluate the severity of TCA poisoning by measuring the level of the drug in the blood.

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    Sodium Bicarbonate for TCA Toxicity

    The initial drug of choice for treating cardiac arrhythmias associated with TCA toxicity, effective in correcting acid-base imbalances caused by the overdose.

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    Decontamination in TCA Toxicity

    The process of removing the ingested drug from the gastrointestinal tract, crucial for preventing further absorption of TCAs.

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    How do opioids affect GIT?

    Opioids can cause a decrease in the activity of the gastrointestinal (GIT) system, leading to slowed motility (movement of food through the gut), reduced gastric acid secretion, and constipation. These effects can be attributed to the influence of opioids on the muscles of the gut, slowing down the process of digestion and elimination.

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    What is the main respiratory effect of opioids?

    Opioids can cause respiratory depression by reducing the rate and depth of breathing. This is a serious side effect that can lead to life-threatening complications, especially in overdose situations.

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    How do opioids affect the urinary system?

    Opioids can cause a decrease in the tone and amplitude of ureter contractions, leading to urine retention. This can be particularly problematic for individuals at higher risk, including older males with prostatic hypertrophy.

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    How do opioids affect the respiratory system?

    Opioids can trigger bronchospasm by tightening the muscles in the airways, making it difficult to breathe. This can lead to coughing, wheezing, and shortness of breath.

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    Why can opioids cause itching?

    Opioids can lead to itching because of the release of histamine, a chemical produced by the body's immune system. Itching is a common side effect of opioid use and can be quite bothersome.

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    What are the signs and symptoms of opioid toxicity?

    A patient suspected of opioid toxicity might present with respiratory depression, low blood pressure, low body temperature, and pinpointed pupils. This is a specific set of symptoms associated with opioid poisoning, sometimes referred to as the opioid toxidrome.

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    How is opioid toxicity diagnosed?

    A confirmed diagnosis of opioid toxicity involves a combination of circumstantial evidence, history of opioid exposure, a clinical examination revealing the opioid toxidrome, and toxicological test results confirming the presence of opioids in the body.

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    What role do toxicological tests play in diagnosing opioid toxicity?

    Toxicological tests can be used to identify opioids in a patient's body fluids and tissues, providing evidence of opioid exposure. These tests can be either screening, which are quick but less specific, or confirmatory, which are highly specific but more time-consuming.

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    Activated Charcoal for Toxicity

    Activated charcoal binds to toxins in the stomach, preventing their absorption into the bloodstream.

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    Flumazenil for Benzodiazepine Reversal

    A competitive antagonist of benzodiazepine receptors, flumazenil can reverse sedation but is not recommended for overdose in addicts due to potential seizure risks.

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    Tricyclic Antidepressants (TCAs)

    Tricyclic antidepressants (TCAs) are a class of drugs used to treat depression, with a significant risk of toxicity when overdosed.

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    TCA Absorption

    TCAs are readily absorbed from the gastrointestinal tract, but their absorption is delayed due to anticholinergic effects.

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    TCA Metabolism

    TCAs are primarily metabolized in the liver, resulting in active metabolites that contribute to their toxicity.

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    TCA Mechanism of Action: Neurotransmitter Reuptake Inhibition

    TCAs block the reuptake of neurotransmitters like serotonin and norepinephrine, leading to their accumulation in the synapse.

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    TCA Effects: Sedation and Arrhythmias

    TCAs block histamine receptors leading to sedation, and sodium channels leading to heart rhythm disturbances.

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    Clinical Picture of TCA Toxicity

    TCA toxicity can lead to cardiovascular complications like hypotension and arrhythmias, as well as central nervous system effects like seizures and altered mental status.

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    What is Naloxone?

    Naloxone is an antidote for opioid overdose, effectively reversing the effects of opioid toxicity. It works by blocking opioid receptors in the brain, preventing opioids from acting on them. It does not produce its own pharmacological effects but rather acts as a competitive antagonist.

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    What is the primary target receptor of Naloxone?

    Naloxone is a derivative of oxymorphone, a synthetic opioid. It has strong affinity to the mu opioid receptor, the primary receptor responsible for opioid effects.

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    What are potential side effects of Naloxone?

    Naloxone can cause adverse effects like asystole, ventricular irritability, hypertension, pulmonary edema, and gastrointestinal issues. These effects are often triggered by a surge in catecholamines (hormones like adrenaline) or interruption of endorphin production by the body.

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    What are Benzodiazepines?

    Benzodiazepines are widely prescribed drugs that can cause serious consequences when taken in large doses. They are commonly used to manage anxiety, insomnia, and seizures.

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    How do Benzodiazepines work?

    Benzodiazepines work by enhancing the inhibitory effects of GABA, a neurotransmitter that calms the nervous system. This action explains their sedative, hypnotic, anxiolytic, and anticonvulsant effects.

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    How are benzodiazepines absorbed and distributed?

    Absorption of benzodiazepines is fast and efficient, both when taken orally and when administered intravenously. Their lipophilic nature enables them to easily cross the blood-brain barrier, quickly reaching the brain.

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    What are the main effects of Benzodiazepine overdose?

    Benzodiazepine overdoses can lead to central nervous system depression, potentially causing respiratory depression and aspiration pneumonia. Other complications include skin and muscle damage due to pressure.

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    How is Benzodiazepine toxicity managed?

    Managing Benzodiazepine toxicity starts with supportive care, including airway management, breathing support, and circulation monitoring. Decontamination may involve gastric lavage, especially if the patient is in a coma.

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    Study Notes

    Acute Intoxication with CNS Depressants

    • CNS depressants are drugs that slow down brain activity, used to treat various conditions like insomnia, anxiety, stress, sleep disorders, pain, and seizures.
    • The main types of CNS depressants are sedatives, hypnotics, and tranquilizers.
    • Drugs categorized as CNS depressants include alcohol, barbiturates, benzodiazepines, and opioids.

    Opioids

    • Opioids are a class of drugs derived from opium poppy plants or synthetically produced, with similar properties.
    • Primarily used to relieve pain and induce euphoria, they act on specific opioid receptors in the brain, spinal cord, and throughout the body.
    • Opioids include natural substances like morphine and codeine, as well as semisynthetic and synthetic drugs like oxycodone, hydrocodone, fentanyl, and methadone.
      • Naturally occurring opioids: morphine and codeine.
      • Semi-synthetic opioids: heroin, apomorphine.
      • Synthetic opioids: methadone, pethidine.
    • Accidental overdose is the most common route of opioid exposure.
    • Opioid-induced intolerance is a desensitization process where opioids desensitize receptors, requiring higher doses to achieve the original pain-relieving effect.
    • "Drug idiosyncrasy" refers to reactions to drugs that occur in a small fraction of patients without an obvious relationship to dose or therapy duration.
    • Opioids act on Mu, Delta, and Kappa receptors.
      • Mu receptors are responsible for analgesia, euphoria, respiratory depression, and physiological dependence.
      • Delta and Kappa receptors are involved in spinal analgesia.
    • Opioids inhibit neuronal activity by postsynaptic hyperpolarization (increasing K+ efflux) and reducing presynaptic Ca++ influx.
    • Toxicological actions of opioids include respiratory depression, altered consciousness, cardiovascular suppression, gastrointestinal complications (constipation), and metabolic disturbances (hypoventilation and metabolic acidosis).
    • CNS actions of opioids include combined stimulation and depression; stimulation effects on the CTZ, vagus cardiac inhibitory center, third cranial nerve nucleus, and the feeling of well-being, and depressive effects on the cerebral cortex (analgesia and sedation), cough center, respiratory center, and heat regulating center (hypothermia).
    • The effects of opioids on the cardiovascular system (CVS) include suppressing the VMC and potentially causing shock.
    • Opioids can increase segmental gastrointestinal motility and decrease gastric acid secretion, leading to constipation.
    • Opioids can affect the biliary tract, aggravating biliary colic, and cause genitourinary problems, including urine retention (especially in elderly males with prostatic hypertrophy), and bronchospasm.
    • Opioids can cause itching due to histamine release.
    • Rare adverse effects include bad dreams, seizures, and hallucinations.

    Diagnosis of Opioid Toxicity

    • Circumstantial evidence includes signs of acute intoxication in addicts, accidental poisoning in children, and iatrogenic poisoning. An important factor is recent prescription or intake of opiates.
    • Clinical examination involves assessing vital signs including respiratory depression, hypotension, hypothermia, pinpoint pupils, and other indicators, which are suggestive of opioid poisoning.
    • Investigations for diagnosing opioid toxicity include toxicological tests (screening tests like immunoassays and thin-layer chromatography, and confirmatory tests like gas chromatography-mass spectrometry) and non-toxicological tests (radiographic images for cerebral bleeding, electrocardiograms to monitor bradycardia, arterial blood gas analysis, electrolyte analysis, blood glucose, and renal function tests).

    Treatment of Opioid Overdose

    • Hospitalization is mandatory.
    • Treatment focuses on maintaining a patent airway, ensuring adequate oxygenation, supporting the pulse and blood pressure, and monitoring for complications.
    • Bradycardia may necessitate atropine administration.
    • Gastric decontamination methods like syrup of ipecac, lavage, whole bowel irrigation, and activated charcoal can be considered.
    • Naloxone is the antidote of choice for opioid poisoning, which is a competitive antagonist at Mu opioid receptors.

    Benzodiazepines

    • Benzodiazepines are widely prescribed sedative-hypnotic drugs.
    • Benzodiazepine overdoses commonly have a relatively benign clinical course.
    • Benzodiazepines enhance the inhibitory actions of GABA.
    • Benzodiazepines are rapidly absorbed orally and parenterally, distribute readily, and penetrate the blood-brain barrier due to their lipophilic structure.
    • Benzodiazepines are highly protein-bound in plasma.
    • They are metabolized in the liver through HME, and diasaepam is metabolized to nordiazepam, an active metabolite.
    • Elderly patients or those with liver disease may experience prolonged elimination of benzodiazepines.

    Pathophysiology of Benzodiazepine Toxicity

    • Benzodiazepines enhance GABA release, leading to generalized CNS depression, sedation, and potentially hypnosis.
    • Respiratory depression, including apnea, can occur.
    • Cardiovascular effects include coronary vasodilation and decreased cardiac output with hypotension.
    • Habituation and addiction are possible.
    • Complications include aspiration pneumonia, and pressure necrosis of skin and muscles.

    Clinical Picture of Benzodiazepine Acute Toxicity

    • CNS effects include sleepiness, ataxia, impaired motor function, anterograde amnesia, slurred speech. Paradoxical effects (anxiety, delirium, hallucinations, aggression) can occur.
    • CVS effects include hypotension, bradycardia, and cardiac arrest.
    • Respiratory effects include apnea and hypoxemia.
    • Gastrointestinal effects include nausea and vomiting.
    • Allergic reactions can include urticaria and rashes.
    • Hypotonia may be observed in severe cases.
    • Large doses can lead to rapid sleep and later coma due to vasomotor and respiratory depression.

    Management of Benzodiazepine Toxicity

    • General supportive treatment, including maintaining the airway, ensuring adequate oxygenation, supporting the pulse and blood pressure, and monitoring for complications is critical.
    • Gastric lavage and activated charcoal administration may be considered.
    • Diuresis, peritoneal dialysis, and hemodialysis are not typically effective due to large volume of distribution and high plasma protein binding.
    • Flumazenil, a nonspecific benzodiazepine receptor antagonist, can be used, but isn't typically recommended for overdose patients.
    • Patients who remain asymptomatic after 4 to 6 hours of observation might be medically cleared from care. For deliberate overdose attempts, psychiatric consultation should be sought.

    Tricyclic Antidepressants (TCAs)

    • TCAs are psychoanaleptics well absorbed from the gastrointestinal tract (GIT). (anticholinergic effect) delaying absorption.
    • They are metabolized in the liver by cytochrome oxidase to active metabolites and highly plasma and tissue protein bound.
    • Little is excreted unchanged in the urine, and little gastric/biliary excretion (enterohepatic circulation).
    • TCAs inhibit the reuptake of neurotransmitters (adrenaline, noradrenaline, dopamine, serotonin) increasing their levels, inducing an antidepressant effect.
    • Other actions of TCAs include sedation, arrhythmia, and anticholinergic effects (dilated pupils, blurred vision, dry skin, tachycardia, hypertension, hyperthermia, urinary retention, ileus, dry mouth, agitation, delirium, confusion, hallucinations, slurred speech, and coma).
    • Further, they exhibit alpha-adrenergic receptor antagonism and inhibit GABA receptors.

    Clinical Picture of TCA Toxicity

    • Cardiovascular effects, including hypotension due to direct myocardial depression and peripheral vasodilation from alpha-adrenergic blockade, cardiac arrhythmias (sinus tachycardia, ventricular dysrhythmia), ECG changes (widening of QRS complex, depression of ST segment, abnormal t wave, prolonged PR and QT intervals) are observed.
    • CNS effects include stimulation (followed by depression), seizures, altered mental status (delirium, disorientation, agitation, hallucination), lethargy, and coma in severe cases.
    • Anticholinergic manifestations, hyperthermia, and acidosis might rapidly arise due to agitation and seizures, with aspiration leading to pulmonary edema.

    Investigations for TCA Toxicity

    • Toxicological tests, including serum drug level assessment, are necessary.
    • Non-toxicological investigations (acid-base status, blood gasses, ECG, X-ray chest, glucose, electrolytes, and kidney function testing) should also be conducted.

    Treatment of TCA Toxicity

    • Early intubation for patients with CNS depression and/or hemodynamic instability is recommended.

    • Monitoring of cardiac activity, and managing hypotension.

    • Sodium bicarbonate is a first-line treatment for cardiac arrhythmias.

    • Lidocaine may be used as a second-line treatment for cardiac arrhythmias.

    • Decontamination (e.g., lavage) may be considered, however, not in cases of convulsion and coma.

    • Elimination is generally not indicated, given the large volume of distribution.

    • Treat or control any convulsions or hyperthermia.

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