Drugs for Anxiety & Insomnia Flashcards
MOA of Benzodiazepenes
Potentiates GABA
- Increase FREQUENCY of opening of Cl-
channels → Cl influx
→ neuronal membrane hyperpolarization which
counteracts the depolarizing effect of
excitatory neurotransmitters
Works only in the presence of GABA
Benzodiazepene short acting specific agents
TRIAZOLAM
MIDAZOLAM
Benzodiazepene intermediate acting specific agents
OXAZEPAM
LORAZEPAM
TEMAZEPAM
ALPRAZOLAM
Benzodiazepene long acting specific agents
CLONAZEPAM
DIAZEPAM
FLURAZEPAM
PRAZEPAM
HALAZEPAM
CHLORAZEPATE
CHLORDIAZEPOXIDE
FLUNITRAZEPAM
Side & Adverse effects of BZDs
- Anterograde amnesia
→ interfere with the formation of new memory - Incoordination, dizziness, excessive drowsiness
- IV administered: respiratory depression
- Physical dependence (chronic use)
Abrupt termination
→ Withdrawal Symptoms (rebound anxiety,
insomnia, HA, irritability, muscle twitches)
→ Should be tapered gradually over a period of
several weeks.
What is Flumazenil?
BZD receptor antagonist
used to counteract adverse effects such
as respiratory depression resulting from IV
administration of BZD in cases of
accidental or intentional overdose
MOA of Barbiturates
Potentiates GABA
Increase DURATION OF TIME that Cl-
channel remains open even in the absence of GABA.
Effects of Barbiturates
CNS depression
Barbiturates are enzyme inducers.
Barbiturates do not exhibit ceiling effects.
Adverse effects of Barbiturates
Tolerance and physical dependence during continuous use, and withdrawal syndrome occurs if abruptly discontinued.
Excessive doses may lead to respiratory depression, coma, and death.
Ultra Short acting Barbiturates
THIOPENTAL
THIAMYLAL
METHOHEXITAL
Short acting Barbiturates
PENTOBARBITAL
HEXOBARBITAL
SECOBARBITAL
Intermediate acting Barbiturates
AMOBARBITAL
BUTABARBITAL
Long acting Barbiturate
PHENOBARBITAL
Indications of BZD and Barbiturates
Anxiety - sedative effect facilitates the anxiolytic effect
→ sedative is an agent that decreases CNS activity,
moderates excitement and generally calms the
individuals
→ BZD are preferred over Barbiturates
Insomnia - facilitates hypnosis
→ hypnotic agents promotes drowsiness and facilitates the
onset and maintenance of sleep
→ both BZD and Barbiturates cause day-time drowsiness
and hangover as side effects.
Anesthesia
Seizure
Muscle spasms
Advantages of BZD over Barbiturates
Has ceiling effects
Lower probability of dependency
Broad therapeutic index
