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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
Benzodiazepine vs Barbiturate: Which has greater tendency to develop tolerance & dependence?
Barbiturate
26
Long or short acting drug is preferred to reduce risk of tolerance & dependence?
Long-acting
27
Phenobarbital as ASM is used mainly for ____
pediatric or neonatal patients (IV loading dose followed by IV or oral maintenance doses)
28
Is phenobarbital long-acting?
Yes, DOA 1-2 days
29
Use as a sedative-hypnotic has largely been replaced by_____ due to_____’ tendency to develop tolerance and dependence
benzodiazepines; barbiturates
30
Levetiracetam: dosage forms
Oral/ IV
31
Dosage form: lamotrigine
Oral route (chewable)
32
Lamotrigine: common side effects
Headache, irritability / aggression, tiredness
33
PK for lamotrigine & levetiracetam
Linear
34
Lamotrigine: adverse effects
Agranulocytosis, hallucination, movement disorders (worsens PD), SJS/TEN, hepatic failure
35
Levetiracetam: common side effects
Headache, vertigo, cough, depression, insomnia
36
Levetiracetam: adverse effects
Agranulocytosis, suicide, delirium, dyskinesia
37
Dosage for topiramate
oral
38
PK for topiramate
Linear
39
Clearance for topiramate
Predominantly renal clearance
40
Does topiramate have a long or short plasma half-life?
Long plasma half-life
41
Topiramate: common side effects
Depression, somnolence, fatigue, nausea, weight change
42
Topiramate: Adverse effects
Neutropenia, mania, tremor, transient blindness, SJS/TEN, hepatic failure
43
What is cafergot made of
A combination med containing caffeine and ergotamine
44
3 meds for moderate-severe migraine
❑ Cafergot ❑ Sumatriptan ❑ Erenumab
45
Cafergot: MOA
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
Cafergot: dosage forms
Oral, rectal
47
Cafergot: rate of absorption, ptn binding & absolute F
Rapidly absorbed (maximum plasma concentrations reached in 1.5-2 hr). High plasma protein binding, low absolute bioavailability (2-5%)
48
DDI of cafergot
Inhibits liver CYP3A. Should not be used with other CYP3A inihibitors like macrolide antibiotics→elevated exposure to ergot toxicity (vasospasm and tissue ischaemia)
49
Cafergot: side effects
Nausea and vomitting
50
Cafergot: rare effects
Hypersensitivity, myocardial infarct, ergotism (vascular ischaemia)
51
Sumatriptan: MOA
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
Sumatriptan: dosage forms
Oral, nasal, IV
53
PK for sumatriptan: ___ absorbed,___ plasma protein binding. Eliminated primarily by _____ mediated by ____
Rapidly; low; oxidative metabolism; monoamine oxidase A (MAO)
54
Sumatriptan: common effects
Dysgeusia (unpleasant taste), transient BP increase, flushing, sensation of cold, pressure, tightness
55
Sumatriptan: contraindication
- Known hypersensitivity to triptans, - concurrent administration with MAO inhibitors, - myocardial infarct
56
Sumatriptan: adverse effects
Minor disturbances in liver function tests
57
Erenumab: MOA
Blocks CGRP receptors.
58
Erenumab: dosage form
SC injection (monthly)
59
Erenumab: indication
prophylaxis of migraine in adults who have at least 4 migraine days per month
60
PK for erenumab
Linear kinetics at therapeutic doses (as CGRP receptor binding is saturated)
61
Erenumab: side effects
Hypersensitivity reactions, injection site reactions, constipation, pruritus

PR3153 (17 decks)

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