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Intro B Pharmacology > Drugs For Parkinson Diseases > Flashcards

Drugs For Parkinson Diseases Flashcards

1
Q

The hallmark of parkinson’s disease is …..

A

Loss of dopaminergic neuron and presence of lewy bodies in the pars compacta of the substantia nigra of the brain

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2
Q

Cardinal signs of parkinsonism disease are

A

Muscular rigidity
Bradykinesia ( Decreased movt)
Postural imbalance
Resting tremor

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3
Q

The anti-psychotics and ati-emetics are dopamine receptor antagonist which can result in parkinsonism diseases like effect examples are…..

A

Antipsychotic
Haloperidol
Thorazine

Anti emetics
Metoclopramide
Prochlorperazine

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4
Q

The rate limiting step in the synthesis of dopamine is ……..

A

Conversion of tyrosine to L DOPA
by tyrosine hydroxylase

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5
Q

Dopamine can be metabolised by which enzymes

A

Aldehyde dehydrogenase
COMT
MOA

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6
Q

The products of dopamine metabolism are

A

COMT 3MT
MAO 3,4 Ddihydroxyphenylacetic acid
ADD Homovallinic acid

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7
Q

The products of dopamine metabolism are

A

COMT 3MT
MAO 3,4 Ddihydroxyphenylacetic acid
ADD Homovallinic acid

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8
Q

The principles of drugs for treating parkinsonism disease are

A

Increase the concentration of dopamine
Work at the receptor

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9
Q

What is the single most important agent in the treatment of dopamine

A

Levodopa L-DOPA

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10
Q

Levodopa is administered………

A

Orally

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11
Q

Why is levodopa best administered on an empty stomach

A

Because its absorption is limited by the rate and extent of gastric emptying.
Hence delayed by gastric emptying

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12
Q

Dopamine is absorbed in what part of the intestine

A

Small intestine

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13
Q

L DOPA is transported across the intestine and circle of Willis by ……

A

Aromatic amino acid transporter

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14
Q

Why is CARBIDOPA administered with L DOPA

A

CARBIDOPA is a L DOPA decarboxylase inhibitor which prevents the action of L DOPA peripherally

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15
Q

CARBIDOPA cannot cross the BBB T/F

A

True

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16
Q

The half life of L DOPA is ……….

A

6-8 hours

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17
Q

Side effects of levodopa are

A

Dyskinesia
On and off effect
Hallucinations
Vomiting that can be prevented by CARBIDOPA
Confusion

18
Q

Dopamine receptor agonist used for the treatment of parkinsonism disease is divided into classes ……….. and ………..

A

Ergot classes
Non ergot classes

19
Q

The ergot derivatives used in the treatment of parkinsonism are

A

Bromocriptine
Carbegoline
Pergolide

20
Q

The non ergot dopaminergic receptor agonist are

A

Ropinirole
Pramipexole

21
Q

Ergot derivatives of DA receptor agonist undergo extensive first pass effect with ………….. %of bioavailability

A

50%

22
Q

The half lifes of ergot derivatives DA receptor agonist are

A

Pergolide 27 hours
Bromocriptine 12-14 hours

23
Q

The non ergot derivatives DA receptor agonist are metabolised in ………

A

Liver and excreted through bile and a little unchanged excreted through urine

24
Q

The two non ergot derivatives DA agonist are newer drugs, administered orally with ……… %of bioavailability

A

50-90%

25
Q

Average half life of ergot derivatives DA receptor agonist are

A

8-24 hrs

26
Q

Bromocriptine and carbegoline elicit their strong agonist effect on …….

A

D2 Receptors

27
Q

The side effects associated with ergot derivatives DA receptor agonist occurs through…….

A

Adrenergic and serotonin receptors

28
Q

Pergolide has affinity for both D1 and D2 but stronger at …..

A

D1

29
Q

Non ergot derivatives DA receptor agonists have activity on D1 D2 D3 which is the lowest and highest

A

Lowest at D1
Maximum at D2 and D3

30
Q

The peculiarity of on-off phenomenon to dopamine receptor agonist and levodopa is

A

Levodopa can result in on and off
DA agonist can be used to treat on and off phenomenon

31
Q

A side effect peculiar to pergolide is ……

A

Cardiac valvular disease

32
Q

Side effects associated with dopamine receptor agonists are

A

Nausea
Vomiting
Hypotension
Fatigue

33
Q

A side effect associated with newer non ergot derivatives dopamine receptor agonist is

A

Somnolence

34
Q

Bromocriptine inhibit the release of glutamate from glutamatergic neuron T/F

A

True

35
Q

COMT inhibitors in clinical use are

A

Entacapone
Tolcapone

36
Q

How does COMT affect the metabolism of levodopa

A

It is recruited by CARBIDOPA
It results in metabolism of L DOPA preventing its decarboxylation to Dopamine

37
Q

Differences between entacapone and tolcapone

A

Entacapone
Bioavailability is 35%
Crosses BBB less
Less hepatotoxic
2hrs half life

Tolcapone
Crosses BBB more
65% Bioavailability
More hepatotoxic
Longer half life

38
Q

Side effects of COMT inhibitors include

A

Nausea Vomiting Hypotension, confusion and Hallucinations somnolence
Hepatotoxicity

Diarrhoea
Dry mouth
Abdominal pain
Back pain
Discolouration of urine

39
Q

Which MAO enzyme is found centrally

A

MAO B

40
Q

The selective inhibition of which MOA is preffered in the treatment of PD

A

MAO B

41
Q

At what dose does selegiline act selectively on on MAOB

A

20mg/day

42
Q

Other drugs used in the treatment of parkinsonism disease are

A

Anti muscarinic agent
Artane (trihexyphenidyl)
Benztropine mesylate
Diphenyhydramine
Antiviral drug
Amantadine

Intro B Pharmacology (24 decks)

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