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CNS > 15. Drugs that Target Diseases of the Brain > Flashcards

15. Drugs that Target Diseases of the Brain Flashcards

1
Q

What is the function of carbidopa?

A

Stops levodopa being broken down peripherally so more is available in the brain

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2
Q

What are the side effects of levodopa?

A

Dizziness, nausea and insomnia
Serious: disorientation, psychosis
Long term: dyskinesia, motor fluctuations

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3
Q

What drug is used as a rescue therapy for patients with motor fluctuations?

A

Apomorphine (dopamine agonist)

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4
Q

What is dopamine dysregulation syndrome?

A

Addiction to dopamine therapy

Patient craves medication, shows impulse control disorders

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5
Q

How is dopamine dysregulation syndrome treated?

A

Reduce L-dopa dose

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6
Q

When are dopamine agonists used?

A

First line in patients under 65 as fewer motor complications than L.dopa
Later in the progression of Parkinsons as nerve terminals aren’t required to convert L.dopa

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7
Q

Why are ERGOT dopamine agonists no longer used?

A

Caused fibrotic reactions in the lungs and pericardium as they were non-selective D1 and D2 agonists

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8
Q

Name 3 non-ERGOT dopamine agonists

A

Ropinirole
Apomorphine
Rotigotine as a patch

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9
Q

When are MOA-B inhibitors used?

A

Less severe, newly diagnosed Parkinsons

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10
Q

What are the side effects of MOA-B inhibitors?

A

Orthostatic hypotension, sleep disorders
Can’t have tyramine containing foods
Serotonin syndrome

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11
Q

What is the MOA of COMT inhibitors?

A

Entacopone inhibits peripheral COMT

Tolcapone inhibits central and peripheral COMT

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12
Q

What are the side effects of COMT inhibitors?

A

Urine discolouration, severe diarrhoea
Hepatic toxicity
CV risk with stalevo

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13
Q

What drugs are used in mild alzheimer’s disease?

A

Cholinesterase inhibitors

Eg. donepezil, rivastigmine, galantamine

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14
Q

What is the metabolism of donepezil and galantamine?

A

CYP450

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15
Q

What drug is used in severe Alzheimer’s disease?

A

NMDA antagonists eg. memantine

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16
Q

What anti-convulsants are sodium channel inhibitors?

A

Phenytoin
Carbamazepine
Lamotrigine

17
Q

What type of seizures is phenytoin used for?

A

Focal and secondary generalised

18
Q

What is the MOA of phenytoin?

A

Slows rate of channel recovery from inactivated state ie. prevents repetitive firing

19
Q

What are the pharmacokinetics of phenytoin?

A

Zero order kinetics

CYP450

20
Q

What is the difference between zero order and first order kinetics?

A

Zero order: same amount eliminated independent of blood conc

First order: dependent on blood conc

21
Q

What are the side effects of phenytoin?

A

Nystagmus, diplopia, ataxia
Sedation, gingival hyperplasia
Hirsutism

22
Q

What are the long term effects of phenytoin?

A

Coarse facial features

Mild peripheral neuropathy

23
Q

What type of seizures is carbamazepine useful in?

A

Generalised

24
Q

What are the pharmacokinetics of carbamazepine?

A

1st order

CYP450

25
Q

What are the side effects of carbamazepine?

A

Diplopia
Ataxia
Agranulocytosis

26
Q

What are the side effects of lamotrigine?

A

Steven-Johnson syndrome
TEN skin syndrome
Anaemia

27
Q

Which anti-convulsants are calcium channel inhibitors?

A

Ethosuximide

Sodium valproate

28
Q

What is the MOA of ethosuximide?

A

Block global T-type calcium channels

29
Q

What seizures is ethosuximide used for?

A

Absence

30
Q

What are the side effects of ethosuximide?

A 
Fatigue
GI distress
Headache
Itching
Stevens-Johnson
31
Q

What is the MOA of sodium valproate?

A

Slows rate of Na+ channel recovery
Limits T ca++ channel activity
Inhibits GABA metabolism

32
Q

What seizures is sodium valproate used for?

A

Generalised

33
Q

What are the side effects of sodium valproate?

A 
GI distress
Hepatotoxicity
Neural tube defects
Tremor
Weight gain
34
Q

Which drugs are GABA-A receptor modulators?

A

Benzodiazepines

Barbituates

35
Q

Which seizure types are benzodiazepines used for?

A

Focal
Tonic clonic
Status epilepticus

36
Q

How is a benzodiazepine overdose reversed?

A

Flumazenil

37
Q

Name 2 drugs that inhibit GABA metabolism

A

Tiagabine (competitive)

Vigabatrin (irreversible)

38
Q

Name a GABA analogue

A

Gabapentin

CNS (21 decks)

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