Drugs Affectinf CNS Flashcards

(28 cards)

1
Q

What are the two groups of opium

A
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2
Q

What is the natural substrate for opioid receptors

A

Endorphins

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3
Q

On which receptor does the morphine mostly act

A
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4
Q

What is not a natural substrate

A

Morphine

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5
Q

List the effects of Mu-2 activation

A

Analgesia
Respiratory depression
Euphoria
Decrease GI motility
Physical dependence

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6
Q
A
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7
Q
A
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8
Q

Explain opioids and stereoselectivity

A
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9
Q

What are the opioid therapeutic challenges

A
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10
Q

What is the difference between OH at position 3 and 6 in morphine

A
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11
Q

What are the essential pharmacophoric elements of morphine

A
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12
Q

Explain codeine

A
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13
Q

Explain metabolism of codeine

A

Metabolized by o demethylation to give morphine

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14
Q

Explain codeine taken with grapefruit juice

A
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15
Q

Explain heroin

A
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16
Q

What are the 3 problems associated with analgesic narcotics

A

Tolerance
Dependence
Withdrawal symptoms

17
Q

What are the morphine derivatives antagonists

A

Naloxone and naltrexone

18
Q

Explain the activity of naltrexone

19
Q

Naloxone and naltrexone are used for what

A

To treat overdose of morphine and heroin

20
Q

What is one of the signs of morphine poisoning

A

Acute miosis ( pinpoint pupils)

21
Q

Explain the binding mode for N-phenethylmorphine

22
Q

Explain the binding modes for N-allylmorphine

23
Q

What is the influence of 14-OH group

24
Q

How to convert morphine to antagonist

A

Add allyl group
Add OH group

25
What happens when there is modification to the phenolic OH group in morphine
Decreases activity and addiction (Codeine used as antitussive)
26
What happens when there is modification to the alcoholic OH group
Increases activity and addiction because decreased polarity so more active because less polarity meaning it can penetrate the BBB more
27
Why is heterocodein less active in vitro
Because of the methods group which is a bulky group so prevent binding
28
Explain hydrocodone