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PR3153 > IC4 - Pharmacology > Flashcards

IC4 - Pharmacology Flashcards

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?

A

Oral/ IV

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?

A

Levetiracetam

25
Q

How does lamotrigine works?

A

Block voltage gated sodium channels, inhibit release of glutamate and impedes sustained repetitive neuronal depolarization

26
Q

What is the indication for lamotrigine and topiramate?

A

Partial seizures
General seizures including tonic clonic seizures

27
Q

Monotherapy of lamotrigine is indicated for _________ seizures.

A

typical absence

28
Q

Patient A has Lennox-Gastaut syndrome. What can he be given for treatment?

A

Lamotrigine (adjunctive or initial)
Topiramate (adjunctive)

29
Q

Lamotrigene half life decreases if co-adminstered _______ and _______.

A

carbamazepine, phenytoin

30
Q

____ when given with lamotrigine increases the half life of lamotrigine.

A

Valproate

31
Q

What class of drug is topiramate?

A

Sulfate substituted monosacaride

32
Q

Topiramate can be given as _____ for migrane in adults.

A

Prophylaxis

33
Q

How is topiramate cleared?

A

Renal

34
Q

How does cafergot works?

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)

35
Q

What is the indication of cafergot?

A

Acute treatment of migraine (given at first symptom of attack)

36
Q

How can cafergot be administered?

A

Oral or rectal

37
Q

Cafergot reaches plasma concentration in ______.

A

1.5-2 hr

38
Q

Cafergot has _____ plasma protein binding

A

high

39
Q

Cafergot has _____ absolute bioavailability.

A

low ( 2 to 5%)

40
Q

Cafergot is a _____ inhbitor.

A

CYP3A

41
Q

Why should CYP3A inhibitors such as cafergot not be given together with macrolide antibitoics?

A

Elevated exposure to ergot toxicity (vasospasm and tissue ischaemia)

42
Q

______ agents such as ergot alkaloids, sumatriptan and other 5HT1 agonists should not be given to patients on cafergot.

A

Vasoconstrictor

43
Q

What are the side effects of cafergot?

A

N/V

44
Q

What are the rare side effects of cafergot?

A

Hypersensitivity, myocardial infarct, ergotism (vascular ischaemia)

45
Q

How does Sumatriptan works?

A

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
Q

What is sumatriptan indicated for?

A

Acute migraine with or wo aura

47
Q

How can sumatriptan be administered?

A

Oral, nasal, IV

48
Q

How is sumatriptan eliminated?

A

By oxidative metabolism mediated by
monoamine oxidase A (MAO).

49
Q

Sumatriptan has _____ plasma protein binding.

A

low

50
Q

Who should not be given sumatriptan?

A

Known hypersensitivity to triptans,
concurrent administration with MAO inhibitors, myocardial infarct

51
Q

What is the undesirable effects of sumatriptan?

A

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

52
Q

What are the rare side effects of sumatriptan?

A

Minor disturbances in liver function
tests

53
Q

How does Erenumab works?

A

Block CGRP receptors

54
Q

What is the clinical indication of erenumab?

A

Prophylaxis of migraine in adults (at least 4 days per months)

55
Q

How can erenumab be given?

A

SC , monthly

56
Q

What are the side effects of Erenumab?

A

Hypersensitivity reactions, injection site reactions, constipation, puritis

PR3153 (16 decks)

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