Benzodiazepines & Sedative agents Flashcards by Alex Kinsky

Q

The following effects are associated with benzodiazepine use (true or false):

Analgesia

A

False. Benzodiazepines have no direct analgesic effects.

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Q

The following effects are associated with benzodiazepine use (true or false):

Convulsions

A

False. Benzodiazepines are anticonvulsants

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Q

The following effects are associated with benzodiazepine use (true or false):

Sedation

A

True

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Q

The following effects are associated with benzodiazepine use (true or false):

Inhibition of acetylcholine at the neuromuscular junction

A

False. Benzodiazepines do not affect the neuromuscular junction.

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Q

The following effects are associated with benzodiazepine use (true or false):

Retrograde amnesia

A

False. Benzodiazepines produce anteretrograde amnesia.

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Q

The following statements describe the action of benzodiazepines (true or false):

Inhibition at the GABAA receptor

A

False. Benzodiazepines are positive allosteric modulators at the GABAA receptor.

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Q

The following statements describe the action of benzodiazepines (true or false):

Increased frequency of GABA channel opening

A

True

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Q

The following statements describe the action of benzodiazepines (true or false):

Depolarization of the postsynaptic membrane

A

False. Hyperpolarization is associated with benzodiazepine action.

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Q

The following statements describe the action of benzodiazepines (true or false):

Increased sodium entry postsynaptically

A

False. Increased chloride entry is responsible for hyperpolarization.

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Q

The following statements describe the action of benzodiazepines (true or false):

Antagonist to GABA

A

False. Benzodiazepines enhance GABA activity.

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Clonazepam is a short-acting benzodiazepine

A

False. Clonazepam is a long-acting benzodiazepine.

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Lorazepam is water-soluble

A

False. Lorazepam is solubilised is propylene glycol.

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Diazepam is metabolised to oxazepam

A

True

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Midazolam has an active metabolite

A

True. Midazolam converts into its active metabolite alpha-1 hydroxy midazolam, which contributes to 10% of drug action.

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Temazapam is conjugated by acetylation

A

False. Temazapam is glucoronidated.

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Q

The pharmacological properties of the following benzodiazepines include (true or false):

Midazolam is water soluble at PH 3

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A

True

Q

The pharmacological properties of the following benzodiazepines include (true or false):

Diazepam has an elimination half-life of 24 hours

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A

False. Diazepam has a terminal elimination half-life in excess of 36 hours.

Q

The pharmacological properties of the following benzodiazepines include (true or false):

Oxazepam is metabolised to temazepam

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A

False. Temazepam can be metabolised to oxazepam.

Q

The pharmacological properties of the following benzodiazepines include (true or false):

Diazepam is metabolised to nordiazepam and temazepam

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A

True. Diazepam undergoes N-demethylation to nordiazepam (60%) and 3-hydroxylation to temazepam (40%). Both are then further oxidated/conjugated to soluble products.

Q

The following are useful clinical actions of benzodiazepines (true or false):

Hypnosis

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A

True

Q

The following are useful clinical actions of benzodiazepines (true or false):

Muscle rigidity

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A

False. Muscle relaxation is useful.

Q

The following are useful clinical actions of benzodiazepines (true or false):

Anticonvulsant

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A

True

Q

The following are useful clinical actions of benzodiazepines (true or false):

Antiemetic

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A

False. Benzodiazepines are not useful antiemetics.

Q

The following are useful clinical actions of benzodiazepines (true or false):

Analgesia

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A

False. Benzodiazepines are not analgesic.

Regarding flumazenil (true or false): Is an imidazobenzodiazepine

True

Regarding flumazenil (true or false): Has active metabolites

False. It is metabolised in the liver to inactive metabolites via de-ethylation and conjugation.

Regarding flumazenil (true or false): May cause hypertension

True

Regarding flumazenil (true or false): Is contraindicated in QRS/QTc prolongation

True. This implies a potential mixed drug overdose and result in cardiac dysrhythmias.

Regarding flumazenil (true or false): Has an elimination half-life of 50 minutes

True. This is typically shorter than most benzodiazepines in overdose.

Regarding flumazenil (true or false): Has an initial half-life of 20 mins

False. It has a half life of 7-15 min (initial), 20-30 min (brain), 40-80 min (terminal). This is shorter than that of diazepam and midazolam such that there is a risk of patients becoming resedated.

Regarding flumazenil (true or false): Has a volume of distribution of 1 L/kg

True. Flumazenil is extensively distributed in the extravascular space and the volume of distribution at steady state is 0.9 - 1.1 l/kg

Clinical effects of benzodiazepines include (true or false): Reduced REM and slow-wave sleep

True

Clinical effects of benzodiazepines include (true or false): Anti-emesis

False

Clinical effects of benzodiazepines include (true or false): Reduced SVR

True. Benzodiazepines have minor depressant effects on SVR, preload, cardiac output and blood pressure.

Clinical effects of benzodiazepines include (true or false): Retrograde amnesia

False. Antegrade amnesia.

Clinical effects of benzodiazepines include (true or false): Reduced tidal volume

True. At non-toxic doses, this is countered by a slight increase in respiratory rate.