CNS pharmacology- Rex Flashcards

1
Q

what are the effects of CNS drugs?

A

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…)

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2
Q

the pre-cpnditions for drugs to act on the CNS are…

A
  • passage through the BBB (lipophil, active transport systems…)
  • interaction w. central structures (receptors, transporters…)
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3
Q

what is the % of GABAergic synapses in the CNS

A

30-40%

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4
Q

what is the % of glutamatergic synapses in the CNS

A

30-40%

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5
Q

what is the % of ACh synapses in the CNS

A

10%

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6
Q

what is the % of dopaminergic synapses in the CNS

A

1%

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7
Q

what is the % of noradrenergic synapses in the CNS

A

1%

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8
Q

what is the % of serotonergic synapses in the CNS

A

1%

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9
Q

on which receptor do benzodiazepines act? what does it do?

A

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

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10
Q

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

A

d. act as psychostimulants

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11
Q

what are the therapeutic uses of benzodiazepines?

A
  • sedative/hypnotic
  • anxiolytic
  • muscle relaxant
  • anticonvulsant
  • alcohol withdrawal
  • premenstrual syndrome (PMS)
  • psychosis (only supportive)
  • adjunct in mania of bipolar disorder
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12
Q

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

A

d. prescribed for long term administration

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13
Q

Discontinuation of benzodiazepine treatment causes sleep disturbances called rebound insomnia

True/False?

A

True

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14
Q

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?

A
  • 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.
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15
Q

name at least 4 adverse effects of benzodiazepines

A
  • 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
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16
Q

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

A

b, d

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17
Q

which of the following statements is/are correct?
a. benzodiazepine with short t1/2 (oxazepam, lorazepam…), directly undergo glucuronidation and have no active metabolites.

b. benzodiazepine with short t1/2 (medazepam, temazepam..), are oxidised in the liver and have no active metabolites.
c. benzodiazepine with long t1/2 (diazepam, chlordiazepam…), are metabolised in the liver and have active metabolites.
d. benzodiazepine with long t1/2, directly undergo glucuronidation and have no active metabolites.
e. all benzodiazepines are metabolised in the liver regardless of their half-life time

A

a, c

18
Q

can you name other sedative hypnotic drugs?

A
  • barbiturates (e.g. phenobarbital)
  • barb-like drugs (e.g. glutethimide)
  • azapirone (e.g. busiprone)
  • Zolpidem (e.g. ambient)
  • Sonata
19
Q

what are the 2 classes of drugs for Parkinson’s disease?

A
  1. Dopaminergic agents - promote activation od DA receptors (e.g. L-dopa)
  2. Anticholinergic drugs- prevent activation of AChR (e.g. Benztropine)
20
Q

what is the mechanism of action of dopaminergic agents in the treatment of PD?

A
  • promotion of dopamine synthesis
  • prevention of dopamine degradation
  • promotion of dopamine release
  • direct activation of dopamine receptors (e.g. D2 receptors)
21
Q

what is the mechanism of action of anticholinergic agents in the treatment of PD?

A

blockade of mAChR in the striatum –> achieving the same goal as dopaminergic drugs- balance between ACh and DA (but not as good and efficient as dopaminergic agents)

22
Q

what is the mechanism of action of L-dopa ?

A

promotes DA synthesis in the striatum and enhanced by pyroxidine to increase carboxylase activity

23
Q

which antiepileptic drug is best for treating partial, and tonic-clonic seizures? how does it work? what are the adverse effects?

A
  1. phenytoin:
    - mechanism: selective inhibition of Na+ channels
    - adverse effects: nystagmus, diplopia; sedation, cognitive impairments; ataxia
  2. carbamazepine:
    - mechanism: Na+ channel inhibition
    - adverse effects: CNS symptoms, nystagmus, ataxia; anemia, leukopenia…
    - -> also treating schizophrenia and trigeminal neuralgias
24
Q

what drugs are used to treat epilepsy?

A
  • phenytoin - for partial & tonic clonic seizures
  • phenobarbital - partial & generalised tonic clonic seizures
  • carbamazepine- partial & tonic clonic seizures
  • valporic acid- absence seizures, migraines, other seizures
25
Q

Drugs for aborting ongoing headaches (migraines)

A
  • aspirin
  • opioid analgesics
  • ergot alkaloids - alpha agonist vasoconstrictives
  • 5HT agonists (triptans)
26
Q

Drugs for prophylaxis (migraines)

A
  • beta blockers
  • Ca2+ channel blockers
  • TCA
27
Q

analgesic drugs…

a. cause loss of consciousness
b. relieve pain
c. are anticonvulsant drugs
d. block K+ channels

A

b

28
Q

which of the following statements about opioid receptors is/are correct?

a. u, gamma and kappa receptors reduce cAMP activity
b. ORL-1 reduces cAMP activity
c. u receptor is the pure opioid receptor
d. all opioid receptors (u, k, g, ORL-1) reduce voltage sensitive Ca2+ channel
e. all opioid receptors reduce excitation and induce hyper polarisation by enhancing K+ channel activity

A

a, c, d, e

29
Q

which of the following statements about opioid receptors is/are WRONG?

a. endorphins bind preferably to u and gamma receptors
b. nociceptin binds preferably to ORL-1
c. dynorphins and enkephalins both bind preferably to gamma receptor over u and kappa
d. enkephalin binds theoretically to u, gamma and kappa receptors, but has higher affinity to kappa
e. endogenous opioids are non selective for a specific receptor

A

c, e

30
Q

what are the adverse effects of morphine?

A
  • respiratory depression
  • constipation
  • orthostatic hypotension
  • urinary retention
  • cough suppression
  • emesis
31
Q

tolerance to morphine/opioids (characteristics)

A
  • increasing dose to obtain the same response
  • develop with analgesia, euphoria sedation, respiratory depression
  • cross-tolerance to other opioids
32
Q

what are the risks in developing high tolerance to morphine?

A
  • overdose (increasing the dose to obtain the same response–> dose may be lethal
  • physical dependence

–> after physical dependence develops - if dose is stopped abruptly –> abstinence syndrome

33
Q

which statement is correct?

a. neuropathic pain results from tissue damage
b. neuropathic pain is pain coming from visceral organs and nociceptive pain results from skin tissue damage.
c. neuropathic pain results from injury to peripheral nerve and nociceptive pain is visceral pain resulting from tissue damage.
d. neuropathic pain can be treated well with opioids

A

c

34
Q

what is the classical triad (in the context of opioid overdose) ?

A

coma - respiratory depression - pinpoint pupils

35
Q

what does ABCDE sand for in pain management?

A
A-ask and assess
B-believe
C- choose
D-deliver
E-empower and enable
36
Q

what parameters are important for pain assessment?

A
  • onset and temporal pattern
  • location
  • quality
  • intensity
  • modulating factors
  • previous treatment
  • impact
37
Q

which statement is true?

a. the WHO analgesic ladder has 3 steps with 1 being the mildest pain and 3 being the most severe pain
b. the WHO analgesic ladder has 3 steps with 3 being the mildest pain and 1 being the most severe pain

A

a

38
Q

which of the following drug classes are NOT a group of antidepressants?

a. atypical
b. amines
c. SSRI
d. azapirone
e. MAOI

A

d

39
Q

True or False- most atypical antidepressant are NA-selective

A

True

40
Q

response to antidepressant treatment…

a. takes min. 1 week
b. works only on patients with mild symptoms
c. happens immediately after beginning the treatment
d. is the same in all patients

A

a

41
Q

A patient with acute onset depression, who suffers from 5 out of 6 major symptoms of depression is willing to receive treatment. how would you start the treatment? what medications would you put them on?

A
  • antidepressant treatment should be started at a lowest effective dose and be increased gradually.
  • Since many antidepressants require long-term administration to be effective, the patient should be informed about the adverse effects, as well as the duration, and at the same time they should be monitored, to see if the treatment is generating any unwanted responses.
  • nowadays, new generation SSRIs are the most widely used antidepressants. since they are very selective, and thus have fewer side effects than others –> the more specific the treatment is the fewer side effects occur and the EC50 is lower (higer efficacy)