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Neuro > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

MOA of phenytoin

A

Block voltage-gated Na+ channels

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2
Q

Cautions for phenytoin

A
  • Narrow therapeutic range
  • Teratogenic
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3
Q

MOA of carbamazepine

A

Block voltage-gated Na+ channels

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4
Q

Metabolism of carbamazepine

A
  • Liver metabolism
  • CYP inducer
  • t1/2 reduces on repeated doses
  • Promotes its own degradation
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5
Q

Cautions for carbamazepine

A

SJS / TEN

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6
Q

MOA of valproate

A
  • Block voltage-gated Na+ & Ca2+ channels
  • Inhibit GABA transaminase
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7
Q

Valproate distribution

A
  • Highly bound to plasma proteins
  • Can displace plasma protein binding of other AED –> increase toxicity
  • Demonstrates saturable protein binding even within therapeutic range
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8
Q

MOA of benzodiazepines

A
  • Allosteric regulator for GABA-A receptors on Cl- channels
  • Enhances GABA binding and Cl- influx, increasing the inhibitory effect of GABA on postsynaptic neurons
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9
Q

Absorption of diazepam

A
  • Onset: 0.5 hours
  • Half-life: 43 hours
  • Duration of action: 1-3 days
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10
Q

Absorption of lorazepam

A
  • Onset: 2 hours
  • Half life: 12 hours
  • Duration of action: 10-20 hours
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11
Q

Cautions for benzediazepines

A
  • Avoid alcohol
  • Frequent use builds tolerance
  • Gradual withdrawal needed
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12
Q

Treatment for benzodiazepine overdose

A

Flumazenil

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13
Q

MOA of barbiturates

A

Bind to a separare site from benzodiazepines and potentiate GABA-A-mediated Cl- influx

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14
Q

Barbiturates duration of action

A

Long-acting:
- 1-2 days
- anticonvulsants e.g. phenobarbital

Short-acting:
- 3-8 hours
- Sedative & hypnotics e.g. pentobarbital, amobarbitak

Ultrashort-acting:
- 20 mins
- Anesthesia e.g. thiopental

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15
Q

PK properties of levetiracetam

A
  • Linear PK
  • Route: oral or IV
  • High solubility & permeability
  • Low intra & interindividual variability
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16
Q

MOA of lamotrigine

A
  • Block voltage-gated Na+ channels
  • Inhibit glutamate release
  • Impede sustained repetitive neuronal depolarization
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17
Q

PK of lamotrigine

A
  • Linear
  • PO administration
  • Shorter half-life in children
  • Half-life decreased with carbamazepine & phenytoin, increased with valproate
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18
Q

Indication of topiramate

A
  • Monotherapy for partial & generalised seizure (including tonic-clonic)
  • Adjunct for lennox-gastaut syndrome
  • Prophylaxis of migraine in adults
19
Q

PK of topiramate

A
  • Linear
  • Oral administration
  • Long half-life
  • Primarily eliminated by renal clearance
20
Q

MOA of cafergot

A

Vasoconstriction of the external carotid network by stimulating alpha-adrenergic and 5HT receptors (1B & 1D)

21
Q

PK of cafergot

A
  • Oral / rectal administration
  • Peak concentration in 1.5-2 hours
  • High plasma protein binding
  • Low bioavailability
22
Q

DDI of cafergot

A
  • Inhibits CYP3A
  • Interacts with CYP3A inhibitors (results in ergotism: vasospasm, tissue ischemia)
23
Q

ADR of cafergot

A

Common:
- Nausea, vomiting

Rare:
- Hypersensi
- Myocardial infarct
- Ergotism

24
Q

Caution for cafergot

A

Not to be used with other vasoconstrictors e.g. ergot alkaloids, sumatriptan, 5HT1 agonists

25
Q

MOA of sumatriptan

A
  • Selective vascular 5HT1D receptor agonist
  • Selectively constricts carotid arterial circulation, but does not affect cerebral blood flow
  • Inhibits trigeminal nerve activity
26
Q

PK of sumatriptan

A
  • Oral / nasal / IV administration
  • Rapid absorption
  • Low plasma protein binding
  • Eliminated by monoamine oxidase A
27
Q

Caution for sumatriptan

A

Contraindications:
- Hypersensi
- Concurrent administration with MAO inhibitors
- History of MI

28
Q

ADR of sumatriptan

A

Common:
- Dysgeusia (unpleasant taste)
- Transient BP rise
- Flushing
- Sensation of cold
- Feeling of pressure, tightness

Rare:
- LFT derangements

29
Q

MOA of Erenumab

A
  • Inhibits binding of calcitonin gene-related peptide to CGRP receptors which acts as nocireceptive neuropeptides at trigeminal ganglion
  • Prevents CGRP from causing vasodilation and stimulating trigeminal nerves
30
Q

Indication of erenumab

A

Migraine prophylaxis in adults with at least 4 days of migraine per month

31
Q

PK of erenumab

A
  • S/C administration mostly
  • Clinical effect reached in 3 months
  • Linear PK at standard doses
32
Q

ADR of erenumab

A
  • Hypersensi
  • Injection site reactions
  • Pruritus
  • Constipation
33
Q

Drug targets for neuropharmacology

A

Agonist:
- Increase synthesis of neurotransmitters
- Reduce breakdown of neurotransmitters
- Increase release of neurotransmitters from synaptic terminal
- Inhibition of autoreceptors
- Activation of postsynaptic receptors or potentiates its activation by neurotransmitters
- Inhibit reuptake or degradation

Antagonist:
- Reduce synthesis of neurotransmitters
- Increase breakdown of neurotransmitters
- Inhibit release from presynaptic terminal
- Increase reuptake or degradation
- Inhibit postsynaptic receptor

34
Q

DDI of carbamazepine

A

1A2, 2C, 3A4, UGT inducer

35
Q

DDI of phenytoin

A

2C, 3A, UGT inducer

36
Q

DDI of phenobarbital

A

1A, 2A6, 2B, 3A, UGT inducer

37
Q

DDI of levetiracetam

A

Nil

38
Q

DDI of gabapentin

A

Nil

39
Q

DDI of pregabalin

A

Nil

40
Q

DDI of topiramate

A

Moderate 3A inducer at high dose
Weak CYP inhibitor

41
Q

DDI of perampenel

A

Weak 2B6, 3A4/5 inducer
Weak 2C8, UGT inhibitor

42
Q

DDI of rufinamide

A

Weak CYP inducer
Weak 2E1 inhibitor

43
Q

Absorption of phenytoin

A
  • Slow but complete absorption
  • Reduced absorption at doses higher than 400 mg
  • Reduced with enteral feeds (space >2 hours apart)

Neuro (5 decks)

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