Benzodiazepines & Sedative agents Flashcards
The following effects are associated with benzodiazepine use (true or false):
Analgesia
False. Benzodiazepines have no direct analgesic effects.
The following effects are associated with benzodiazepine use (true or false):
Convulsions
False. Benzodiazepines are anticonvulsants
The following effects are associated with benzodiazepine use (true or false):
Sedation
True
The following effects are associated with benzodiazepine use (true or false):
Inhibition of acetylcholine at the neuromuscular junction
False. Benzodiazepines do not affect the neuromuscular junction.
The following effects are associated with benzodiazepine use (true or false):
Retrograde amnesia
False. Benzodiazepines produce anteretrograde amnesia.
The following statements describe the action of benzodiazepines (true or false):
Inhibition at the GABAA receptor
False. Benzodiazepines are positive allosteric modulators at the GABAA receptor.
The following statements describe the action of benzodiazepines (true or false):
Increased frequency of GABA channel opening
True
The following statements describe the action of benzodiazepines (true or false):
Depolarization of the postsynaptic membrane
False. Hyperpolarization is associated with benzodiazepine action.
The following statements describe the action of benzodiazepines (true or false):
Increased sodium entry postsynaptically
False. Increased chloride entry is responsible for hyperpolarization.
The following statements describe the action of benzodiazepines (true or false):
Antagonist to GABA
False. Benzodiazepines enhance GABA activity.
The pharmacological properties of the following benzodiazepines include (true or false):
Clonazepam is a short-acting benzodiazepine
False. Clonazepam is a long-acting benzodiazepine.
The pharmacological properties of the following benzodiazepines include (true or false):
Lorazepam is water-soluble
False. Lorazepam is solubilised is propylene glycol.
The pharmacological properties of the following benzodiazepines include (true or false):
Diazepam is metabolised to oxazepam
True
The pharmacological properties of the following benzodiazepines include (true or false):
Midazolam has an active metabolite
True. Midazolam converts into its active metabolite alpha-1 hydroxy midazolam, which contributes to 10% of drug action.
The pharmacological properties of the following benzodiazepines include (true or false):
Temazapam is conjugated by acetylation
False. Temazapam is glucoronidated.
The pharmacological properties of the following benzodiazepines include (true or false):
Midazolam is water soluble at PH 3
True
The pharmacological properties of the following benzodiazepines include (true or false):
Diazepam has an elimination half-life of 24 hours
False. Diazepam has a terminal elimination half-life in excess of 36 hours.
The pharmacological properties of the following benzodiazepines include (true or false):
Oxazepam is metabolised to temazepam
False. Temazepam can be metabolised to oxazepam.
The pharmacological properties of the following benzodiazepines include (true or false):
Diazepam is metabolised to nordiazepam and temazepam
True. Diazepam undergoes N-demethylation to nordiazepam (60%) and 3-hydroxylation to temazepam (40%). Both are then further oxidated/conjugated to soluble products.
The following are useful clinical actions of benzodiazepines (true or false):
Hypnosis
True
The following are useful clinical actions of benzodiazepines (true or false):
Muscle rigidity
False. Muscle relaxation is useful.
The following are useful clinical actions of benzodiazepines (true or false):
Anticonvulsant
True
The following are useful clinical actions of benzodiazepines (true or false):
Antiemetic
False. Benzodiazepines are not useful antiemetics.
The following are useful clinical actions of benzodiazepines (true or false):
Analgesia
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.
