CNS pharmacology- Rex Flashcards
what are the effects of CNS drugs?
CNS drugs can be central sedative or central stimulants. –> drug types below from the most sedative to most stimulatating:
- general anaesthetics
- hypnotics
- sedative, neuroleptics
- anxiolytics
- antiepileptics/anticonvulsants
- antidepressants
- analeptics
–> some non-CNS drugs can have an effect on the CNS (antihistamines…)
the pre-cpnditions for drugs to act on the CNS are…
- passage through the BBB (lipophil, active transport systems…)
- interaction w. central structures (receptors, transporters…)
what is the % of GABAergic synapses in the CNS
30-40%
what is the % of glutamatergic synapses in the CNS
30-40%
what is the % of ACh synapses in the CNS
10%
what is the % of dopaminergic synapses in the CNS
1%
what is the % of noradrenergic synapses in the CNS
1%
what is the % of serotonergic synapses in the CNS
1%
on which receptor do benzodiazepines act? what does it do?
BDZ act on GABAa receptor complex, which is bound to Cl- channel. BDZ binds to receptor–> activates GABAa and increase the affinity of the receptor for GABA–> increases Cl- conductance & hyperpolarising the cell
–> this makes BDZ an indirect GABA agonist
Benzodiazepines do NOT…
a. have a sedative effect
b. relax skeletal muscles
c. treat alcohol withdrawal syndrome
d. act as psychostimulants
e. used to treat anxiety
d. act as psychostimulants
what are the therapeutic uses of benzodiazepines?
- sedative/hypnotic
- anxiolytic
- muscle relaxant
- anticonvulsant
- alcohol withdrawal
- premenstrual syndrome (PMS)
- psychosis (only supportive)
- adjunct in mania of bipolar disorder
Benzodiazepines are NOT…
a. used to treat anxiety
b. sedating
c. used to treat PMS
d. prescribed for long term administration
e. causing daytime drowsiness
d. prescribed for long term administration
Discontinuation of benzodiazepine treatment causes sleep disturbances called rebound insomnia
True/False?
True
a patient is suffering from severe anxiety, and is in a state of panic. What drug would you give them to relieve their symptoms? would you expect any side effects?
- benzodiazepines are good for immediate relief anxiety symptoms. In the case of this patient, long acting, low potency benzos such as clonazepam or chlordiazepam would be preferred.
- Since benzodiazepines have high addictive and abuse potential, they are best used for exacerbation of anxiety symptoms.
- common side effects of benzos are psychomotor and cognitive impairment, daytime drowsiness and sleepiness.
- alternatively, if a patient has a history of substance abuse or if sensitivity to benzos id known, one can treat anxiety with other hypnotic drugs such as barbiturates.
- for continuous treatment and prophylaxis of anxiety, SSRIs and SNRIs can be given.
name at least 4 adverse effects of benzodiazepines
- CNS depression, sedation (worse when combined with alcohol)
- behavioural disinhibition (irritability, aggression…)- rare
- psychomotor and cognitive impairment: coordination, attention, poor visual spatial ability, confusion…
- overdose - rare fatalities with benzos alone
- -> if combined with alcohol, barbiturates, narcotics or TCAs- severe CNS and respiratory depression
which of the following statements is/are correct?
a. benzodiazepines cross the BBB by binding the GABA transport system
b. benzodiazepines are lipid soluble and thus can easily cross the BBB
c. benzodiazepines persist longer in slim people
d. benzodiazepines persist longer in obese people
e. all benzodiazepines have a short half-life time
b, d