Sedative-Hypnotics, Antianxiety, and Antidepressant Drugs Flashcards
(51 cards)
What must drugs who are targeted for the CNS be able to do?
Drugs must be able to pass through the blood-brain barrier by either diffusion or being chemically modified in order to pass through
Purpose of Neurotransmitters
Neurons release neurotransmitters in order to cause either excitation or inhibition of other neurons
Examples: AcH, amino acids, peptides
What do Sedative-Hypnotics and Antianxiety drugs do?
Produce a calming and relaxing effect by depressing the CNS on the patient, where larger doses can produce drowsiness or sleep
What are the two categories of Sedatives?
- Benzodiazepines
- Nonbenzodiazepines
Both are used to promote sleep
Why use Benzos over NonBenzos?
Benzos are mostly used for anxiety, but they also promote sleep and are considered safer than NonBenzos due to a smaller chance of lethal overdoes
Benzo Mechanism of Action
Increases the inhibition at the CNS synapses that use the neurotransmitter GABA
-GABA causes inhibition of the CNS which results in relaxation and feelings of decreased anxiety
What is the primary neurotransmitter that causes inhibition of neurons within the CNS?
GABA- so an increase in GABA results in CNS relaxation
Indications of Benzos
-sleep hypnotics
-anxiety
-decreases seizures
-general anesthesia
-muscle relaxation
Side Effects of Benzos
-drowsiness/sedation (most common)
-decreased motor response
-hang-over effect
-anterograde-amnesia
-rebound anxiety
-drug abuse/addiction
**can occur the next day
What are NonBenzos used for?
-sedation
-hypnosis
-general anesthesia
Side effects of NonBenzos
-VERY addictive
-drug abuse
-hang-over effect
What are the properties of barbiturates?
CNS depressants with potent sleep-hypnotic properties
-very small TI
-very addictive and leads to prolonged drug abuse
-NOT commonly used
Examples: Nonbenzos
NonBenzo Mechanism of Action
Binds to GABA receptors to increase inhibition of CNS- same as benzos
Benzo and NonBenzo endings
Benzo: ending in -am (flurazepam, estazolam)
NonBenzo: ending in -al (amobarbital, phenobarbital)
What are the benefits of using drugs that can act as sedatives and hypnotics but are not actually Benzos or Nonbenzos?
These drugs have been developed where they still affect GABA receptors in the brain but NOT in the same way as Benzos or NonBenzos. They have a shorter duration and shorter half-life but they do not causes a hang-over effect.
Examples: Ambien
What are the benefits of using drugs that can act as sedatives and hypnotics but are not actually Benzos or Nonbenzos?
These drugs have been developed where they still affect GABA receptors in the brain but NOT in the same way as Benzos or NonBenzos. They have a shorter duration and shorter half-life but they do not causes a hang-over effect.
Examples: Ambien
Which compounds can cause sedation-hypnosis effects?
-alcohol
-antihistamines
-antidepressants
-antipsychotics
-anticonvulsants
-opioid analgesics
Pharmacokinetics of Sedation-Hypnotic Drugs
-very lipid soluble: able to pass through BBB
-administered orally
-absorbed from GI tract
-distributed uniformly throughout body
-metabolized in liver
-excreted through kidneys
Overall Side Effects for sedative drugs
-tolerance and dependence can occur
-sleep walking
-sleep driving
-compulsive eating while sleeping
-GI discomfort
-dry mouth
-sore throat
-muscular incoordination
Drugs used to treat anxiety
-Benzos
-Buspirone
-Antidepressants
-others: beta blockers
Most common Benzo used for Anxiety
Diazepam (Valium): increases inhibition in the SC that produces skeletal muscle relaxation and contributes to one feeling relaxed and less anxious
Who should NOT use Benzos?
Benzos are not good for the elderly because of the sedation effect they can cause memory and confusion problems. Should also not be used for those who need long-term treatment due to addiction side effects.
When and when not to use Buspirone
Good for patients who need long-term treatment of anxiety, however it only has moderate efficacy and may not be effective in those with severe anxiety
Benefits and Side Effects of Buspirone
Benefits:
-less sedation and psychomotor impairments compared to Benzos
-small risk of tolerance and dependence
-low risk of abuse
Side Effects:
-HA
-dizziness
-nausea
-restlessness
-hypothermia