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iPTX II > Analgesics Med Chem > Flashcards

Analgesics Med Chem Flashcards

1
Q

Analgesics inhibit the production of ___________

A

Prostaglandins

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2
Q

Aspirin is a derivative of what compound?

A

Salicylic acid

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3
Q

What is the difference in structure between aspirin and salicylic acid?

A

Aspirin has an ester group on the second carbon where salicylic acid has an alcohol group

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4
Q

Aspirin (reversibly/irreversibly) blocks COX

A

Irreversibly

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5
Q

How long does aspirin’s antiplatelet effect last?

A

8-10 days

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6
Q

Aspirin blocks
a. COX 1
b. COX 2
c. Both

A

c. Both

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7
Q

Ibuprofen is a derivative of what compound?

A

Phenylpropionic acid

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8
Q

Which is a more potent anti-inflammatory? Ibuprofen or aspirin?

A

Aspirin

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9
Q

Which is a more potent analgesic? Ibuprofen or aspirin?

A

Ibuprofen

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10
Q

NSAIDs are mostly excreted through which organ?

A

Kidneys (renally cleared)

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11
Q

Which COX is induced?

A

COX 2

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12
Q

Which COX is constitutive? (produced in the body at all times)

A

COX 1

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13
Q

Acetaminophen MOA

A

Inhibits prostaglandin synthesis via CNS inhibition of COX (not peripheral)

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14
Q

Acetaminophen is excreted through which organ?

A

Liver (hepatically cleared)

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15
Q

What are the three classes of opioid receptors?

A

– μ- receptor (MOR)
– δ- receptor (DOR)
– κ- receptor (KOR)

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16
Q

What are the targets of aspirin, ibuprofen and acetaminophen?

A

COX-1 and COX-2

17
Q

List examples of selective COX inhibitors

A

a. Celebrex – Celecoxib
b. Aleve – Naproxen

18
Q

What are the targets of morphine?

A

Opioid receptors

19
Q

Important functional groups of morphine

A

a. Phenolic -OH
b. Aromatic ring
c. N-methyl group

20
Q

What is the difference between morphine and codeine in structure?

A

Codeine is methylated (-OCH3) on carbon 3, morphine has an -OH group

21
Q

What kind of structural modifications can improve bioavailability of morphine?

A

Acetyl on carbon 3 and 6 masks polar phenyl group, making morphine able to cross BBB easier, then it is hydrolyzed in the brain to form active morphine

22
Q

What is the difference between morphine and heroine in structure?

A

Heroin has an acetyl group

23
Q

What function groups of morphine are kept in meperidine and fentanyl?

A

Nitrogen, A and D ring

24
Q

What function groups of morphine are kept in methadone or propoxyphene?

A

A ring, Nitrogen

25
Q

List two opioid receptor antagonists

A

a. Naloxone
b. Naltrexone

iPTX II (41 decks)

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