Podcast
Questions and Answers
What are benzodiazepines commonly prescribed for?
What are benzodiazepines commonly prescribed for?
Benzodiazepines are commonly prescribed as anxiolytics and hypnotics.
What potential issue arises from the chronic use of benzodiazepines?
What potential issue arises from the chronic use of benzodiazepines?
Chronic use may lead to tolerance and dependence.
Identify two examples of benzodiazepines classified as ultrashort-acting.
Identify two examples of benzodiazepines classified as ultrashort-acting.
Triazolam and Midazolam are both classified as ultrashort-acting benzodiazepines.
Explain the primary route of excretion for benzodiazepines after metabolism.
Explain the primary route of excretion for benzodiazepines after metabolism.
Describe the distribution characteristics of benzodiazepines in the body.
Describe the distribution characteristics of benzodiazepines in the body.
What is the mechanism of action of benzodiazepines?
What is the mechanism of action of benzodiazepines?
Which benzodiazepine is often used as an IV anesthetic?
Which benzodiazepine is often used as an IV anesthetic?
How does chlorazepate differ from other benzodiazepines in terms of absorption?
How does chlorazepate differ from other benzodiazepines in terms of absorption?
What is the primary effect of benzodiazepines on GABAA receptors?
What is the primary effect of benzodiazepines on GABAA receptors?
What is the main clinical presentation of benzodiazepine overdose?
What is the main clinical presentation of benzodiazepine overdose?
How does the toxicity of benzodiazepines compare to barbiturates?
How does the toxicity of benzodiazepines compare to barbiturates?
What supportive measures should be taken for a patient with benzodiazepine overdose?
What supportive measures should be taken for a patient with benzodiazepine overdose?
Which investigation is used to determine serum benzodiazepine concentrations?
Which investigation is used to determine serum benzodiazepine concentrations?
What is the role of flumazenil in benzodiazepine overdose treatment?
What is the role of flumazenil in benzodiazepine overdose treatment?
What is one method of gastrointestinal decontamination for benzodiazepine overdose?
What is one method of gastrointestinal decontamination for benzodiazepine overdose?
What specific treatment might be considered for long-acting benzodiazepine overdoses?
What specific treatment might be considered for long-acting benzodiazepine overdoses?
Flashcards
What are benzodiazepines?
What are benzodiazepines?
Benzodiazepines are a class of psychoactive drugs commonly prescribed to alleviate anxiety and induce sleep. They are generally deemed safe, replacing more toxic options like barbiturates.
What is a potential downside of long-term benzodiazepine use?
What is a potential downside of long-term benzodiazepine use?
Benzodiazepines are known to cause tolerance and dependence with chronic use.
Name a few common benzodiazepines.
Name a few common benzodiazepines.
Diazepam (Valium), Lorazepam (Ativan), Flunitrazepam (Rohypnol), Bromazepam (Calmipam), Clonazepam (Rivotrill), and Midazolam (Dormicum) are some common examples of benzodiazepines.
How are benzodiazepines categorized?
How are benzodiazepines categorized?
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How are benzodiazepines absorbed when taken orally?
How are benzodiazepines absorbed when taken orally?
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What is a common administration method for benzodiazepines, especially for rapid effects?
What is a common administration method for benzodiazepines, especially for rapid effects?
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Where do benzodiazepines distribute within the body?
Where do benzodiazepines distribute within the body?
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What are the key metabolic processes involving benzodiazepines?
What are the key metabolic processes involving benzodiazepines?
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How do benzodiazepines affect GABA-A receptors?
How do benzodiazepines affect GABA-A receptors?
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What is the main presentation of benzodiazepine overdose?
What is the main presentation of benzodiazepine overdose?
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What is the core principle in managing benzodiazepine overdose?
What is the core principle in managing benzodiazepine overdose?
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Explain the use of gastric lavage in benzodiazepine overdose management.
Explain the use of gastric lavage in benzodiazepine overdose management.
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What is the role of activated charcoal in managing benzodiazepine overdose?
What is the role of activated charcoal in managing benzodiazepine overdose?
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What is the specific antidote used for benzodiazepine overdose and how does it work?
What is the specific antidote used for benzodiazepine overdose and how does it work?
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What are the common investigations performed in benzodiazepine overdose?
What are the common investigations performed in benzodiazepine overdose?
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What are the elimination methods used in benzodiazepine overdose?
What are the elimination methods used in benzodiazepine overdose?
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Study Notes
Benzodiazepines (BZ)
- Benzodiazepines (BZ) are frequently prescribed psychotropic drugs.
- They are often preferred over barbiturates due to their higher therapeutic indices.
- Chronic use 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
- This classification is based on how long the drug's effects last.
- Ultrashort (<6 hours): Triazolam, Midazolam
- Short (12-18 hours): Lorazepam, Oxazepam, Temazepam
- Medium (24 hours): Alprazolam, Nitrazepam
- Long (24-48 hours): Diazepam, Clonazepam, Chlordiazepoxide, Flurazepam
Pharmacokinetics: Absorption
- Oral: Well-absorbed; chlorazepate is a prodrug that becomes Nordazepam in the stomach (active form).
- Intravenous (IV): Midazolam is commonly given intravenously for anesthesia; Diazepam is also given intravenously for anesthesia and anticonvulsant treatments.
- Intramuscular (IM): Slow absorption; lorazepam is used in status epilepticus when IV administration is difficult.
Pharmacokinetics: Distribution
- BZ distribute throughout the body, crossing the blood-brain barrier and placental barrier.
- They accumulate in body fat.
- Highly bound to plasma proteins.
Pharmacokinetics: Metabolism
- Most BZ undergo oxidation to produce active metabolites, followed by conjugation with glucuronic acid.
- Some BZ directly conjugate with glucuronic acid to form inactive metabolites (e.g., Nitrazepam, Clonazepam).
Pharmacokinetics: Excretion
- BZ and their metabolites are excreted in urine after conjugation with glucuronic acid.
Mechanism of Action
- BZ exert their effects by binding to BZ receptors located on the alpha subunit of GABAA receptors.
- This increases the frequency of GABAA chloride channel opening.
Benzodiazepines (BZ) Toxicity: Clinical Presentation
- Central Nervous System (CNS) depression: The primary sign of BZ overdose; less severe than barbiturate overdose. Symptoms include drowsiness, stupor, ataxia and low-grade coma.
- Less commonly, there is profound coma, significant hypotension, respiratory depression, or hypothermia.
- Death from isolated BZ overdose is rare.
Benzodiazepines (BZ) Toxicity: Investigations
- Routine: Complete Blood Count (CBC), Electrolytes, Arterial Blood Gas (ABG), Renal Function Tests (RFT).
- Specific: Serum BZ concentrations using gas chromatography-mass spectrometry (GCMS) or immunoassays.
Benzodiazepines (BZ) Toxicity: Treatment
- I. Supportive: Airway management (intubation), maintaining vital signs (IV fluids). Includes precautions against a "coma cocktail" (including naloxone, thiamine and glucose) and antibiotics for pneumonia, if required.
- II. Gastrointestinal (GIT) Decontamination: Emesis (if alert and gag reflex present), Gastric lavage (with endotracheal tube if compromised gag reflex), activated charcoal, multiple-dose activated charcoal (for long-acting drugs) and cathartics.
- III. Elimination: Forced alkaline diuresis (for long-acting barbiturates). Hemodialysis or hemoperfusion may be necessary to remove the drug in cases of severe hypotension, coma, or dense coma, where the kidneys or liver are unable to metabolize the drug effectively.
Benzodiazepines (BZ) Toxicity: Antidotes
- Flumazenil (Anexatel): A competitive BZ receptor antagonist that can reverse the effects of BZ.
- Advantage: Effective within minutes for isolated BZ overdose.
- Disadvantage: Not used in combined toxicity (BZs and drugs causing seizures)
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Description
This quiz covers the essential aspects of benzodiazepines, including their common types, classification based on duration of action, and pharmacokinetics. Learn about the therapeutic benefits and risks associated with these psychotropic drugs. Test your knowledge on their absorption methods and clinical uses.
