Benzodiazepines Overview and Classification

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Questions and Answers

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?

  • Alprazolam
  • Lorazepam
  • Temazepam
  • Midazolam (correct)

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?

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

What is a common consequence of chronic benzodiazepine use?

<p>Development of tolerance and dependence. (B)</p> Signup and view all the answers

What is the role of the GABAA receptors in the action of benzodiazepines?

<p>They mediate interaction through binding at the alpha subunit. (B)</p> Signup and view all the answers

What does the pharmacokinetic property of 'redistribution' in benzodiazepines imply?

<p>They accumulate in body fat after initial distribution. (D)</p> Signup and view all the answers

Which of the following benzodiazepines is known to be primarily administered intravenously?

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

What is the primary effect of benzodiazepines on GABAA receptors?

<p>They increase the frequency of opening of the chloride channel. (B)</p> Signup and view all the answers

Which of the following is NOT a common presentation of benzodiazepine overdose?

<p>Profound coma with significant hypotension (D)</p> Signup and view all the answers

In the context of benzodiazepine overdose treatment, which of the following interventions is performed FIRST?

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

Which specific antidote is used for reversing the effects of benzodiazepines?

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

What type of investigation is specifically used to measure benzodiazepine concentrations in a patient?

<p>Serum benzodiazepine concentration via GCMS (C)</p> Signup and view all the answers

Which method of gastrointestinal decontamination should be used if the patient is alert and has an intact gag reflex?

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

What is a rare but serious complication of isolated benzodiazepine overdose?

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

Which of the following is a method that can be used for elimination of benzodiazepines from the bloodstream?

<p>Forced alkaline diuresis (D)</p> Signup and view all the answers

Flashcards

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

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)

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

Death from isolated benzodiazepine overdose is rare as long as respiratory support is given.

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BZ Overdose vs Barbiturate Overdose

Benzodiazepine (BZ) overdoses are generally safer compared to barbiturate overdoses.

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Routine Investigations for BZ Overdose

Standard investigations for BZ overdose include complete blood count (CBC), electrolyte levels, arterial blood gas (ABG), and renal function tests (RFT) to assess overall health.

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Specific Investigation for BZ Overdose

Specific investigation for BZ overdose includes measuring serum benzodiazepine concentrations using methods like gas chromatography-mass spectrometry (GCMS) or immunoassays.

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Specific Antidote for BZ Overdose

Flumazenil (Anexate) is a specific antidote for benzodiazepine overdose.

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What are Benzodiazepines (BZ)?

Benzodiazepines are the most common prescribed psychotropic drugs. They are considered safer than barbiturates and are used primarily for anxiety and insomnia. However, long-term use can lead to tolerance and dependence.

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Name some common Benzodiazepines.

These are some commonly prescribed benzodiazepines. Diazepam, lorazepam, flunitrazepam, bromazepam, clonazepam, and midazolam.

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How are Benzodiazepines classified?

Benzodiazepines are classified based on their duration of action, which refers to the time they remain effective in the body. Ultrashort-acting BZ are active for less than 6 hours, short-acting for 12-18 hours, medium-acting for 24 hours, and long-acting for 24-48 hours.

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How are Benzodiazepines absorbed?

Benzodiazepines are absorbed well when taken orally. They can also be injected intravenously (IV) or intramuscularly (IM), although IM absorption is slower.

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Where do Benzodiazepines distribute?

Benzodiazepines distribute throughout the body, including the brain (BBB) and placenta (placental barrier). They tend to accumulate in body fat and bind strongly to proteins in the blood.

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How are Benzodiazepines broken down?

Most benzodiazepines are metabolized (broken down) by the body to produce active metabolites. These metabolites are then further broken down and excreted in the urine. Some benzodiazepines are directly inactivated by conjugation with glucuronic acid.

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How are Benzodiazepines eliminated from the body?

Benzodiazepines are mainly excreted in the urine, typically after they have been conjugated with glucuronic acid.

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How do Benzodiazepines work?

Benzodiazepines work by binding to specific receptors in the brain, called GABA receptors. This interaction enhances the effects of GABA, a neurotransmitter that has calming effects. These actions lead to a sense of relaxation and sleepiness.

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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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