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Yr 3 - Pharmacology > Drugs - Neurology > Flashcards

Drugs - Neurology Flashcards

1
Q

Give 4 types of antiepileptic drugs

A
  1. Sodium valproate
  2. Phenytoin
  3. Carbamazepine
  4. Lamotrigine
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2
Q

What is the 1st line antiepileptic indicated in generalised tonic clonic seizures

A

Sodium valproate

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3
Q

Give the 1st line antiepileptic indicated in women of childbearing age/pregnancy

A

Lamotrigine

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4
Q

What is the 1st line antiepileptic indicated in absence seizures

A

Sodium valproate

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5
Q

What is the 1st line antiepileptic indicated in focal seizures?

A

Carbamazepine

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6
Q

What is the 1st line antiepileptic indicated in myoclonic seizures?

A

Sodium valproate

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7
Q

Mechanism of sodium valproate?

A

Increases activity of GABA (principal inhibitory neurotransmitter) which has a relaxing effect on brain.

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8
Q

Which antiepileptic drug is associated with the greatest risk of foetal abnormalities?

A

Sodium valproate

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9
Q

Contraindications of sodium valproate?

A
  • Avoid where possible in women of child-bearing age, particularly around the time of contraception and first trimester of pregnancy
  • Hepatic & renal impairment
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10
Q

How does sodium valproate interact with the P450 system?

A
  • Sodium valproate is a P450 enzyme inhibitor
  • Sodium valproate itself is metabolised by P450 enzymes so is affected by enzyme inducers & inhibitors
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11
Q

How long must patients be seizure free for before they can drive?

A

12 months

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12
Q

1st line pharmacological management of trigeminal neuralgia?

A

Carbamazepine

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13
Q

Side effects of carbamazepine?

A
  • GI upset
  • Neurological effects e.g. ataxia, dizziness
  • Hypersensitivity (10%)
  • Oedema
  • Hyponatraemia due to ADH-like effect
  • Agranulocytosis (a life-threatening blood disorder where the body doesn’t make enough neutrophils)
  • Aplastic anaemia
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14
Q

Contraindications of carbamazepine?

A
  • Pregnancy → teratogenic
  • Hypersensitivity
  • Hepatic, renal or cardiac disease – increased risk of toxicity
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15
Q

How does carbamazepine interact with the P450 system?

A
  • Carbamazepine is a P450 enzyme inducer
  • Carbamazepine itself is metabolised by P450 enzymes so it affected by enzyme inducers & inhibitors
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16
Q

Side effects of phenytoin?

A
  • Folate and vitamin D deficiency:
    • Megaloblastic anaemia (folate deficiency)
    • Osteomalacia (vitamin D deficiency)
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17
Q

Give some symptoms of phenytoin toxicity

A

Nystagmus, diplopia, slurred speech, ataxia, confusion, and hyperglycaemia.

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18
Q

How does phenytoin interact with the P450 system?

A
  • P450 enzyme inducer
  • Is also metabolised by the P450 system so is affected by enzyme inducers & inhibitors
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19
Q

What severe hypersensitivity reactions can antiepileptics be associated with?

A

Increased risk for Stevens-Johnson syndrome and toxic epidermal necrolysis (SJS/TEN)

20
Q

How is lamotrigine metabolised?

A

By glucuronidation

21
Q

The interactions of lamotrigine arise from its metabolism by glucuronidation. Which drugs:

a) induce glucuronidation?
b) inhibit glucuronidation?

A

Drugs that induce glucuronidation → carbamazepine, phenytoin, oestrogens, rifampicin and protease inhibitors (these can cause lamotrigine levels to fall)

Drugs that inhibit glucuronidation → sodium valproate (can cause levels to rise and potential toxicity)

22
Q

In Parkinson’s disease, there is a deficiency of dopamine in which pathway?

A

In the nigrostriatal pathway that links the substantia nigra in the midbrain to the corpus striatum in the basal ganglia.

23
Q

How does a lack of dopamine generate features of Parkinson’s e.g. bradycardia, rigidity?

A

Via direct and indirect circuits, this causes the basal ganglia to exert greater inhibitory effects on the thalamus which, in turn, reduces excitatory input to the motor cortex

24
Q

In the treatment of Parkinson’s, why is it not possible to give dopamine itself? Why is levodopa given instead?

A

As is does not cross the BBB

By contrast, levodopa is a precursor of dopamine that can enter the brain via a membrane transporter

25
Q

What is levodopa always given alongside?

A

Peripheral decarboxylase inhibitors (e.g. carbidopa, benserazide)

26
Q

Why is levodopa always given alongside peripheral decarboxylase inhibitors?

A

These drugs stop levodopa being broken down in the body before it gets the chance to enter the brain.

27
Q

Give 2 peripheral decarboxylase inhibitors given alongside levodopa

A
  • Carbidopa (co-careldopa = levodopa + carbidopa)
  • Benserazide (co-benyldopa = levodopa + benserazide)
28
Q

Indications for levodopa?

A

Parkinson’s disease

  • Levodopa is the most effective treatment for symptoms but becomes less effective over time
  • It is often reserved for when other treatments are not managing to control symptoms (e.g. ropinirole, pramipexol)
29
Q

Pharmacological management of status epilepticus?

A

1st line → benzodiazepines e.g. IV lorazepam (repeated once after 10−20 minutes if the seizure continues)

2nd line → phenytoin infusion

30
Q

Side effects of levodopa?

A
  • Dyskinesias (often occurs when dose is too high)
  • Postural hypotension
  • Wearing off effect – symptoms worsen towards end of the dosage interval (seems to get worse as duration of therapy increases)
  • GI upset
31
Q

What is dyskinesia?

A

Dyskinesia is uncontrolled, involuntary movement that may occur with long-term levodopa use

32
Q

How can peripheral side effects of levodopa be reduced?

A

Peripheral side effects can be reduced by the co-administration of a peripheral dopa decarboxylase inhibitor e.g. carbidopa.

33
Q

What can be given to manage postural hypotension?

A

Fludrocortisone

34
Q

Why is levodopa is always given with a peripheral doxa-decarboxylase inhibitor?

A

To reduce its conversion to dopamine outside the brain → this desirable interaction reduces nausea and lowers the dose needed for therapeutic effect

35
Q

Why should dopaminergic agents should not usually be combined with antipsychotics or metoclopramide?

A

due to opposing effects on dopamine receptors

36
Q

What agents are preferred in early, non-severe Parkinson’s?

A

Dopamine agonists e.g. Ropinirole, Pramipexol

37
Q

When is levodopa indicated in Parkinson’s?

A

Levodopa is the more effective option when symptoms are disabling

38
Q

What unique side effect can dopamine agonists E.g. Ropinirole, Pramipexol lead to?

A

Can lead to impulsivity e.g. pathological gambling, hypersexuality

39
Q

What does the nigrostriatal pathway connect?

A

The substantia nigra with the corpus striatum of the basal ganglia

40
Q

Give 2 other classes of drugs indicated in Parkinson’s disease

A

COMT Inhibitors

Monoamine Oxidase-B Inhibitors

41
Q

What is the 1st line pharmacological agent used to ease the symptoms of a migraine attack or cluster headache?

A

Triptans (e.g. Sumatriptan, Almotriptan)

42
Q

What class of drug are triptans?

A

5HT receptor agonist (serotonin receptor agonist)

43
Q

2 main indications for triptans?

A
  • Migraine attack
  • Cluster headache
44
Q

Which 2 anticholinergics may be indicated in Parkinso’s?

A

Procyclidine,

45
Q

Purpose of anticholinergics in Parkinson’s?

A

Antispasmodic drugs used to treat stiffness, tremors, spasms and poor muscle control.

Yr 3 - Pharmacology (18 decks)

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