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PR3153 > IC4 > Flashcards

IC4 Flashcards

1
Q

Example of postsynaptic receptors

A

GCRP, ion channels

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2
Q

Signal termination is performed by ______

A

catalytic enzymes and / or reuptake transporters

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3
Q

Major transmitter in excitatory synapses

A

Glutamate

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4
Q

Glutamate is implicated in ____

A

learning and memory

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5
Q

Major transmitter in inhibitory synapses

A

GABA

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6
Q

Acetylcholine is involved in ____

A

learning, arousal and reward

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7
Q

Dopamine is Involved in _____

A

motor system, reward

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8
Q

Does activation of autoreceptor inhibit/ excite neurotransmitter release?

A

Inhibit

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9
Q

At BBB, Na+–K+ ATPase in the barrier cells pumps____ into the CSF and pumps____ out of the CSF into the blood.

A

sodium; potassium

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10
Q

What happens when lipid solubility is too high

A

→ sequestered in capillary bed
→uptake by peripheral tissues

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11
Q

Is Transmembrane diffusion saturable?

A

No, it is non-saturable

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12
Q

At BBB, transporter systems are regulated by ____

A

cerebral blood flow, co-factors, hormones / peptide modulators

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13
Q

MOA for phenytoin

A

Blocks voltage-gated Na+ channel

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14
Q

Indication for phenytoin

A

Suitable for all types of seizures except absence seizures

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15
Q

Can phenytoin be used in pregnancy?

A

No, teratogenic

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16
Q

Carbamazepine: MOA

A

Blocks voltage-gated Na+ channel

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17
Q

MOA for valproate

A
  • Blockade of voltage-dependent Na+ and Ca2+ channels
  • Also inhibits GABA transaminase -> increased GABA
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18
Q

Benzodiazepines: MOA

A

Enhances binding of GABA to Cl- channel, leading to influx of Cl- ions → hyperpolarization of cell → neurons not firing

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19
Q

Benzodiazepines: what happens in acute toxicity/ overdose

A

Can cause severe respiratory depression, especially used concurrently with alcohol

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20
Q

Benzodiazepines: side effects

A

– Drowsiness, confusion, amnesia.
– Impaired muscle co-ordination (impairs manual skills).

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21
Q

Benzodiazepines: tolerance and dependence depends on ____

A

frequency of use

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22
Q

Barbiturates: MOA

A

potentiate GABA(A) mediated Cl- currents, but at a site distinct from benzodiazepines

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23
Q

An example of drug under barbiturate class

A

Phenobarbital

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24
Q

How to treat benzodiazepine overdose? Can the same be used for barbiturate?

A

Flumazenil; No

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25
Q

Benzodiazepine vs Barbiturate: Which has greater tendency to develop tolerance & dependence?

A

Barbiturate

26
Q

Long or short acting drug is preferred to reduce risk of tolerance & dependence?

A

Long-acting

27
Q

Phenobarbital as ASM is used mainly for ____

A

pediatric or neonatal patients (IV loading dose followed by IV or oral maintenance doses)

28
Q

Is phenobarbital long-acting?

A

Yes, DOA 1-2 days

29
Q

Use as a sedative-hypnotic has largely been replaced by_____ due to_____’ tendency to develop tolerance and dependence

A

benzodiazepines; barbiturates

30
Q

Levetiracetam: dosage forms

A

Oral/ IV

31
Q

Dosage form: lamotrigine

A

Oral route (chewable)

32
Q

Lamotrigine: common side effects

A

Headache, irritability / aggression, tiredness

33
Q

PK for lamotrigine & levetiracetam

A

Linear

34
Q

Lamotrigine: adverse effects

A

Agranulocytosis, hallucination, movement disorders (worsens PD), SJS/TEN, hepatic failure

35
Q

Levetiracetam: common side effects

A

Headache, vertigo, cough, depression, insomnia

36
Q

Levetiracetam: adverse effects

A

Agranulocytosis, suicide, delirium, dyskinesia

37
Q

Dosage for topiramate

A

oral

38
Q

PK for topiramate

A

Linear

39
Q

Clearance for topiramate

A

Predominantly renal clearance

40
Q

Does topiramate have a long or short plasma half-life?

A

Long plasma half-life

41
Q

Topiramate: common side effects

A

Depression, somnolence, fatigue, nausea, weight change

42
Q

Topiramate: Adverse effects

A

Neutropenia, mania, tremor, transient blindness, SJS/TEN, hepatic failure

43
Q

What is cafergot made of

A

A combination med containing caffeine and ergotamine

44
Q

3 meds for moderate-severe migraine

A

❑ Cafergot
❑ Sumatriptan
❑ Erenumab

45
Q

Cafergot: MOA

A

Tonic action on vascular smooth muscles in the external carotid network.
Leads to vasoconstriction by stimulating alpha-adrenergic and 5- HT receptors (especially 5-HT1B and 5-HT1D receptors)

46
Q

Cafergot: dosage forms

A

Oral, rectal

47
Q

Cafergot: rate of absorption, ptn binding & absolute F

A

Rapidly absorbed (maximum plasma concentrations reached in 1.5-2 hr). High plasma protein binding, low absolute bioavailability (2-5%)

48
Q

DDI of cafergot

A

Inhibits liver CYP3A. Should not be used with other CYP3A inihibitors like macrolide antibiotics→elevated exposure to ergot toxicity (vasospasm and tissue ischaemia)

49
Q

Cafergot: side effects

A

Nausea and vomitting

50
Q

Cafergot: rare effects

A

Hypersensitivity, myocardial infarct, ergotism (vascular ischaemia)

51
Q

Sumatriptan: MOA

A

Selective vascular serotonin (5-HT1b &1d) receptor agonist.
Selectively constricts the carotid arterial circulation, but does not alter cerebral blood flow.
Inhibits trigeminal nerve activity

52
Q

Sumatriptan: dosage forms

A

Oral, nasal, IV

53
Q

PK for sumatriptan: ___ absorbed,___ plasma protein binding.
Eliminated primarily by _____ mediated by ____

A

Rapidly; low; oxidative metabolism; monoamine oxidase A (MAO)

54
Q

Sumatriptan: common effects

A

Dysgeusia (unpleasant taste), transient BP increase, flushing, sensation of cold, pressure, tightness

55
Q

Sumatriptan: contraindication

A
  • Known hypersensitivity to triptans,
  • concurrent administration with MAO inhibitors,
  • myocardial infarct
56
Q

Sumatriptan: adverse effects

A

Minor disturbances in liver function tests

57
Q

Erenumab: MOA

A

Blocks CGRP receptors.

58
Q

Erenumab: dosage form

A

SC injection (monthly)

59
Q

Erenumab: indication

A

prophylaxis of migraine in adults who have at least 4 migraine days per month

60
Q

PK for erenumab

A

Linear kinetics at therapeutic doses (as CGRP receptor binding is saturated)

61
Q

Erenumab: side effects

A

Hypersensitivity reactions, injection site reactions, constipation, pruritus

PR3153 (17 decks)

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