CNS Pharmacology Part 1 Flashcards
What can pass the blood brain barrier?
nonpolar, lipid soluble drugs
What is the general mechanism of presynaptic inhibitive drugs?
a drug inhibits neurotransmitter release so the action potential fails
What happens when a drug blocks the synthesis of a neurotransmitter?
repletes the presynaptic terminal of neurotransmitter and therefore neuronal transmission is impaired
How do drugs that effect the storage the neurotransmitter work?
impairs the storage of the chemical transmitters in the presynaptic vesicles
How do drugs that act on the release of neurotransmitters work?
Increase the release of neurotransmitter to increase synaptic activity
Decrease the release of neurotransmitter to decrease synaptic activity
How do drugs that affect reuptake work?
blocking uptake increases activity at the synapse
it also prolongs activity at the synapse
How do degradation drugs work?
Inhibit the enzymes that are meant to break down the neurotransmitter
How do drugs that impact the CNS work (generally)?
modify synaptic transmission in some way therefore altering or preventing the job of a neurotransmitter
In order for CNS drugs to be effective they must ______________.
cross the blood brain barrier
What are three types of drugs that impact the CNS?
sedative-hypnotic medications
antianxiety medications
anti-depressant meds
What is the most common use of sedative-hypnotic meds?
promote sleep
they have general CNS depressive effects
What are the two general categories of sedative hypnotic meds?
benzodiazepines
nonbenzodiazepines (include barbiturates)
What are the pharmacokinetics of sedative-hypnotic drugs?
highly lipid soluble
metabolized in the liver
stored in non-CNS tissues
excreted via kidneys
How do benzodiazepines work?
increase the inhibitory effect at a synapse that uses the neurotransmitter GABA
temazepam
What is the mechanism of action of barbiturates?
unclear, may affect GABA
phenobarbital
What are cons of barbiturates?
addictive
prolonged use may lead to dependence
What are the benefits of the newer nonbenzodiazepines?
fewer side effects
ambien, sonata, lunesta
What are adverse effects of sedative hypnotic drugs?
tolerance
dependence-rebound insomnia, psychosis, seizures
residual effects-drowsiness, decreased motor performance, anterograde amnesia
other-GI distress, dry mouth, sore throat
What are common symptoms of anxiety?
restlessness
inability to relax
muscle aches or tension
fatigue
GI symptoms
panic attacks
What are examples of antianxiety meds?
Diazepam (Valium)
Buspirone (BuSpar)
both benzodiazepines
What is diazepam and how does it work?
benzodiazepine with minimal sedative effects
increases GABA effect
valium
What is buspirone?
acts as serotonin agonist (inreases effects of serotonin)
has fewer side effects compared to traditional benzos
What are adverse effects of antianxiety meds?
sedation
addiction
abuse
rebound anxiety
dizziness
headaches
nausea
restlessness
When do sedative hypnotics reach peak blood levels?
2-4 hours after oral administration
note benzos are associated with falls
Most antidepressant meds impact __________ and are administered ___________.
serotonin, orally
It is estimated that _________ of patients with depression do not respond adequately to medication.
1/3
What are common side effects of antidepressants?
sedation
lethargy
orthostatic hypotension
cardiac arrhythmias
seizures
