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PR3153 > IC4 - Pharmacology > Flashcards

IC4 - Pharmacology Flashcards

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1
Q

What are the first line drugs for newly diagnosed partial and generalised tonic clonic seizures?

A

Phenytoin, carbamzepine, sodium valproate

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2
Q

What is the mechanism of action of phenytoin and carbamazepime?

A

Block voltage dependent Na+ channels

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3
Q

Phenytoin and carbamazepine are suitable for all seizures except ______.

A

Absence seizures

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4
Q

Phenytoin should be avoided in _____.

A

Pregnancy (teratogenic)

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5
Q

Why does phenytoin requires monitoring and titration?

A
  1. Narrow therapeutic range
  2. Saturation kinetics
  3. Non linear relationship between dose and plasma concentration
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6
Q

Carbamazepine is a CYP450 _____.

A

Inducer

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7
Q

Why does carbamazepine quicken elimination of other drugs?

A

It is a CYP inducer. The T1/2 of other drugs are shortened with repeated doses.

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8
Q

What is the gene that causes Carbamazepine to have effect on Asians with SJS or TEN?

A

(HLA)-B*1502 allele

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9
Q

What is the MOA of sodium valproate?

A

Block voltage dependent Na+ and Ca2+ channels and inhibits GABA transaminase to increase GABA

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10
Q

Valproate displaces other antiepileptics due to it _____ affinity with plasma proteins.

A

high

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11
Q

How does Benzodiazepines exert their effects?

A

Enhances binding of GABA by acting on GABA(A) receptors Cl- channels and increase influx of Cl- ions leading to hyperpolarization. Therefore, neurons cannot fire.

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12
Q

What is an example of benzodiazepine?

A

Diazepam

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13
Q

How is benzodiapine overdose treated?

A

Flumazenil (benzodiazepine antagonist)

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14
Q

Benzodiazepines can cause acute toxicity such as __________.

A

severe respiratory depression

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15
Q

Name one barbiturate.

A

Phenobarbital

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16
Q

How does barbiturate works?

A

Potentiate GABA(A) mediated Cl- currents at a different site

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17
Q

How is phenobarbital administered?

A

IV loading followed by IV/oral maintenance dose

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18
Q

Which population group is phenobarbital used in?

A

Pediatrics or neonatal

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19
Q

Flumazenil is _______ for barbiturate overdose.

A

not effective

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20
Q

Which group of antiepileptic has a linear dose dependent side effect for depression of CNS?

A

Barbiturates

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21
Q

Levetiracetam is a _____ derivative?

A

pyrrolidone

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22
Q

What is Levetiracetam used for?

A

Adjuctive for Partial Onset seizures, myoclonic, primary generalized tonic clonic seizures

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23
Q

How can Levetiracetam be given?

24
Q

Mr Tan has been diagnosed with Epilepsy at the A&E today due to partial onset seizures What is the drug of choice as monotherapy?

Study These Flashcards
A

Levetiracetam

25
How does lamotrigine works?
Block voltage gated sodium channels, inhibit release of glutamate and impedes sustained repetitive neuronal depolarization
26
What is the indication for lamotrigine and topiramate?
Partial seizures General seizures including tonic clonic seizures
27
Monotherapy of lamotrigine is indicated for _________ seizures.
typical absence
28
Patient A has Lennox-Gastaut syndrome. What can he be given for treatment?
Lamotrigine (adjunctive or initial) Topiramate (adjunctive)
29
Lamotrigene half life decreases if co-adminstered _______ and _______.
carbamazepine, phenytoin
30
____ when given with lamotrigine increases the half life of lamotrigine.
Valproate
31
What class of drug is topiramate?
Sulfate substituted monosacaride
32
Topiramate can be given as _____ for migrane in adults.
Prophylaxis
33
How is topiramate cleared?
Renal
34
How does cafergot works?
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)
35
What is the indication of cafergot?
Acute treatment of migraine (given at first symptom of attack)
36
How can cafergot be administered?
Oral or rectal
37
Cafergot reaches plasma concentration in ______.
1.5-2 hr
38
Cafergot has _____ plasma protein binding
high
39
Cafergot has _____ absolute bioavailability.
low ( 2 to 5%)
40
Cafergot is a _____ inhbitor.
CYP3A
41
Why should CYP3A inhibitors such as cafergot not be given together with macrolide antibitoics?
Elevated exposure to ergot toxicity (vasospasm and tissue ischaemia)
42
______ agents such as ergot alkaloids, sumatriptan and other 5HT1 agonists should not be given to patients on cafergot.
Vasoconstrictor
43
What are the side effects of cafergot?
N/V
44
What are the rare side effects of cafergot?
Hypersensitivity, myocardial infarct, ergotism (vascular ischaemia)
45
How does Sumatriptan works?
Selective vascular serotonin (5-HT1d) receptor agonist. Selectively constricts the carotid arterial circulation, but does not alter cerebral blood flow. Inhibits trigeminal nerve activity
46
What is sumatriptan indicated for?
Acute migraine with or wo aura
47
How can sumatriptan be administered?
Oral, nasal, IV
48
How is sumatriptan eliminated?
By oxidative metabolism mediated by monoamine oxidase A (MAO).
49
Sumatriptan has _____ plasma protein binding.
low
50
Who should not be given sumatriptan?
Known hypersensitivity to triptans, concurrent administration with MAO inhibitors, myocardial infarct
51
What is the undesirable effects of sumatriptan?
Dysgeusia (unpleasant taste), transient BP increase, flushing, sensation of cold, pressure, tightness
52
What are the rare side effects of sumatriptan?
Minor disturbances in liver function tests
53
How does Erenumab works?
Block CGRP receptors
54
What is the clinical indication of erenumab?
Prophylaxis of migraine in adults (at least 4 days per months)
55
How can erenumab be given?
SC , monthly
56
What are the side effects of Erenumab?
Hypersensitivity reactions, injection site reactions, constipation, puritis

PR3153 (16 decks)

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