Podcast
Questions and Answers
What is the significance of the high therapeutic index of benzodiazepines compared to barbiturates?
What is the significance of the high therapeutic index of benzodiazepines compared to barbiturates?
- It makes them less likely to cause dependence.
- It allows for a wider dosage range before toxicity occurs. (correct)
- It indicates they are more effective as first-line medications.
- It reduces the risk of overdose in chronic users.
Which benzodiazepine is classified as an ultrashort acting agent?
Which benzodiazepine is classified as an ultrashort acting agent?
- Alprazolam
- Lorazepam
- Temazepam
- Midazolam (correct)
How does lorazepam effectively address status epilepticus when IV access is difficult?
How does lorazepam effectively address status epilepticus when IV access is difficult?
- It can be administered orally for quick absorption.
- It is the only benzodiazepine with an active prodrug form.
- It is the most potent benzodiazepine available.
- It can be given intramuscularly for slower absorption. (correct)
Which term describes the process by which benzodiazepines are metabolized into inactive metabolites?
Which term describes the process by which benzodiazepines are metabolized into inactive metabolites?
What is a common consequence of chronic benzodiazepine use?
What is a common consequence of chronic benzodiazepine use?
What is the role of the GABAA receptors in the action of benzodiazepines?
What is the role of the GABAA receptors in the action of benzodiazepines?
What does the pharmacokinetic property of 'redistribution' in benzodiazepines imply?
What does the pharmacokinetic property of 'redistribution' in benzodiazepines imply?
Which of the following benzodiazepines is known to be primarily administered intravenously?
Which of the following benzodiazepines is known to be primarily administered intravenously?
What is the primary effect of benzodiazepines on GABAA receptors?
What is the primary effect of benzodiazepines on GABAA receptors?
Which of the following is NOT a common presentation of benzodiazepine overdose?
Which of the following is NOT a common presentation of benzodiazepine overdose?
In the context of benzodiazepine overdose treatment, which of the following interventions is performed FIRST?
In the context of benzodiazepine overdose treatment, which of the following interventions is performed FIRST?
Which specific antidote is used for reversing the effects of benzodiazepines?
Which specific antidote is used for reversing the effects of benzodiazepines?
What type of investigation is specifically used to measure benzodiazepine concentrations in a patient?
What type of investigation is specifically used to measure benzodiazepine concentrations in a patient?
Which method of gastrointestinal decontamination should be used if the patient is alert and has an intact gag reflex?
Which method of gastrointestinal decontamination should be used if the patient is alert and has an intact gag reflex?
What is a rare but serious complication of isolated benzodiazepine overdose?
What is a rare but serious complication of isolated benzodiazepine overdose?
Which of the following is a method that can be used for elimination of benzodiazepines from the bloodstream?
Which of the following is a method that can be used for elimination of benzodiazepines from the bloodstream?
Flashcards
BZ's Effect on GABAa Receptors
BZ's Effect on GABAa Receptors
Benzodiazepines (BZs) increase the frequency of opening at the GABAa chloride channel, leading to increased chloride ion influx.
Main Presentation of BZ Overdose
Main Presentation of BZ Overdose
Central nervous system (CNS) depression is the primary symptom of benzodiazepine overdose, leading to drowsiness, stupor, uncoordinated movements (ataxia), and potentially coma.
Typical Symptoms of BZ Overdose (Isolated)
Typical Symptoms of BZ Overdose (Isolated)
A typical presentation of BZ overdose often includes drowsiness, stupor, ataxia and mild coma. Profound coma, significant hypotension, respiratory depression, or hypothermia are unusual in isolated benzodiazepine overdoses.
Mortality from Isolated BZ Overdose
Mortality from Isolated BZ Overdose
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BZ Overdose vs Barbiturate Overdose
BZ Overdose vs Barbiturate Overdose
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Routine Investigations for BZ Overdose
Routine Investigations for BZ Overdose
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Specific Investigation for BZ Overdose
Specific Investigation for BZ Overdose
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Specific Antidote for BZ Overdose
Specific Antidote for BZ Overdose
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What are Benzodiazepines (BZ)?
What are Benzodiazepines (BZ)?
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Name some common Benzodiazepines.
Name some common Benzodiazepines.
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How are Benzodiazepines classified?
How are Benzodiazepines classified?
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How are Benzodiazepines absorbed?
How are Benzodiazepines absorbed?
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Where do Benzodiazepines distribute?
Where do Benzodiazepines distribute?
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How are Benzodiazepines broken down?
How are Benzodiazepines broken down?
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How are Benzodiazepines eliminated from the body?
How are Benzodiazepines eliminated from the body?
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How do Benzodiazepines work?
How do Benzodiazepines work?
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Study Notes
Benzodiazepines (BZ)
- BZ are the most commonly prescribed psychotropic drugs
- They are often preferred to barbiturates and other toxic agents due to their higher therapeutic indices
- Chronic use of BZ can lead to tolerance and dependence
Common Benzodiazepines
- Diazepam (Valium)
- Lorazepam (Ativan)
- Flunitrazepam (Rohypnol)
- Bromazepam (Calmipam)
- Clonazepam (Rivotrill)
- Midazolam (Dormicum)
Classification by Duration of Action
- Ultrashort (<6h): Triazolam, Midazolam
- Short (12-18h): Lorazepam, Oxazepam, Temazepam
- Medium (24h): Alprazolam, Nitrazepam
- Long (24-48h): Diazepam, Clonazepam, Chlordiazepoxide, flurazepam
Pharmacokinetics - Absorption
- Oral: Well absorbed; chlorazepate is a prodrug that is converted to the active form, Nordazepam.
- IV: Midazolam is commonly used intravenously during anesthesia; Diazepam is also used in IV form for anesthesia and anticonvulsant purposes
- IM: Slow absorption; Lorazepam may be used in status epilepticus if IV access is difficult
Pharmacokinetics - Distribution
- Distributed throughout the body, crossing the blood-brain barrier and placental barrier
- Accumulate in body fat over time
- Highly bound to plasma proteins
Pharmacokinetics - Metabolism
- Most BZ are metabolized through oxidation, followed by conjugation with glucuronic acid, often producing active metabolites.
- Some BZ, like Nitrazepam and Clonazepam, directly conjugate with glucuronic acid, forming inactive metabolites
Pharmacokinetics - Excretion
- Excreted in urine after conjugation with glucuronic acid
Mechanism of Action
- BZ bind to specific BZ receptors located on the alpha subunit of GABAA receptors with high affinity
- This binding increases the frequency of opening of GABAA chloride channels
Benzodiazepines (BZ) Toxicity - Clinical Presentation
- CNS depression: The primary effect of BZ overdose. Symptoms range from drowsiness to profound coma; however, it is less severe than a barbiturate overdose
- Low grade coma
- Ataxia
- Stupor
- Profoud coma and life-threatening complications are uncommon with isolated BZ overdose
- Death from isolated BZ overdose is rare but possible
Benzodiazepines (BZ) Toxicity - Investigations
- Routine: CBC, Electrolytes, ABG, Renal function tests.
- Specific: Serum BZ concentrations using GCMS or immunoassays.
Benzodiazepines (BZ) Toxicity - Treatment
- I. Supportive: Airway management (intubation), respiration support, circulation stabilization, monitoring and maintaining vital functions
- II. GIT Decontamination: Emesis, gastric lavage (with cuffed endotracheal tube), activated charcoal (MDAC), cathartics
- III. Elimination of the poison from blood: Alkaline diuresis (for prolonged-acting agents); hemodialysis/hemoperfusion may be considered in severe or refractory cases.
Benzodiazepines (BZ) Toxicity - Antidotes
- Flumazenil (Anexatel): A competitive BZ receptor antagonist; effective in reversing the effects of BZ overdose
- Disadvantage: Should not be used for combined BZ and other drug toxicities, particularly if seizures are present.
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