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Medicinal Chem > Analgesics > Flashcards

Analgesics Flashcards

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1
Q

What are the different types of pain?

A
  • Cutaneous: caused by injury to the skin or superficial tissues
  • Somatic: originates from ligaments, tendons, bones, blood vessels, and nerves
  • Visceral: originates from body’s viscera or organs
  • Phantom limb: sensation of pain from a limb that has been lost
  • Neuropathic: results of injury or disease to nerve tissue
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2
Q

Conscious experience of sensory information and feeling of unpleasantness as a result of stimulation of?

A

nociceptors

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3
Q

nociceptors detect?

A

Thermal, Mechanical, and Chemical stimuli

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4
Q

morphine, oxymorphone, methadone, levorphanol, fentanyl, and oxycodone

These are all known as?

A

Stong Agonists

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5
Q

Full opioid agonists dont have a ceiling for their effectiveness but they are limited by?

A
  • AEs
    • Tolerance, Respiratory depression, constipation
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6
Q

Opioid peptide SAR

A
  • All endogenous opiod peptides have Leu or Met enkephalin as their first five AAs
  • Tyrosine at the first position is essential for activity
  • After the phenolic group and amine in tyrosine, the next essential feature is the phenyl group of Phe4.
  • Enkephalins like have different conformations
  • Replacement of L-amino acids with D-amino acids can make peptides resistant to peptidases
  • Converting terminal carboxy group into alcohol or amide protects peptide from carboxy peptidases prolonged action
  • Introduction of unnatural amino acids or bulky groups to enkephalins affects conformation
  • Restriction of conformational mobility has led to receptor selective peptides
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7
Q

Classical morphine SAR

What is absolutely essential for maximal activity?

A

OH at the 3 position

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8
Q

Heroin

Potency in relation to morphine?

A

2.5 x more potent

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9
Q

Hydromorphine

Potency in relating to morphine?

A

6 times more potent

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10
Q

Oxymorphone

Potency in relating to morphine?

A

6-10 times more potent

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11
Q

Codeine

Potency in relating to morphine?

Explain

A

1/12 x morphine

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12
Q

Dihydrocodeine

Potency in relating to morphine?

Only in combination with?

A
  • 1/12 times as potent
  • Antihistamines, caffeine, and ASA or Acetaminophen
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13
Q

Metabolism of Codeine and Morphine

This takes place in?

A

All opiate derivatives

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14
Q

Metabolism of Heroin

What can it do why is it so addictive?

Known as a?

What is the active form?

A

Crosses the BBB reason for addictiveness

Prodrug from morphine

6-Acetylmorphine

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15
Q

What are the characteristic of the Kappa receptor?

Mu?

A

Kappa

  • Analgesia, sedation, dysphoria, miosis, regulation of nociception

MU

  • Euphoria, Analgesia, Increased GI time, Emetic effects, thermo regulation
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16
Q

Meperidine

Potency in relating to morphine?

A

1/5 of morphine

No hydroxyl group

Short acting due to ester

17
Q

a-prodine and b-prodine

which one is more potent?

Not available in the US because?

A

MPP+ metabolism MPTP shit

B is more potent

18
Q

In general _____ are more potent than morphine

A

Fentanyl derivatives

19
Q

Remifentanil

Potency in relating to morphine?

What about it?

A

700-800 x more potent

Extremely short acting due to its 1 amide and 2 esters

20
Q

Sufentanil

Potency in relating to morphine?

What portion of this molecule increases its lipophilicity?

A

600-800 x more potent

Sulfur containing ring

21
Q

Methadone

Potency in relating to morphine?

What else?

A

Less dosing intervals and euphoria isnt as stong

22
Q

Tramadol

Potency in relating to morphine?

Mixed action compounds

A

1/10 morphine

Combination of reuptake blockade and opioid agonism

23
Q

Tapentadol

Potency in relating to morphine?

A

More potent than tramadol but less than morphine

24
Q

Metabolism of Methadone

What are the key features?

A
25
Q

Nalmefene

MOA

A
26
Q

Duration of action between Butorphanol and nalbuphine

A

Butorphanol is longer acting because it doesnt have the second point of conjugation

slide 66

27
Q

Buprenorphine

MOA

A

Mu partial agonists

ends up antagonizing itself somehow

28
Q

Pentazocine

MOA

A

Kappa and S

Weak Mu antagonist

29
Q

Ziconotide

MOA

What is it?

Proven to be?

With less?

Downside?

A
  • N-type valtage sensitive Ca2+ channel antagonist
  • Proven to be just at potent as morphine with less respiratory depresson and no constipation makes sense doesnt act on any of that shit.
  • Administered Intrathecally
30
Q

Methotimeprazine

MOA

WHy isnt it a Neuroleptic?

A

Not a neuroleptic b/c it has a EDG not a EWG

Nonopioid used for chronic pain

31
Q

Dextromethorphan

Type?

Why isnt it an opioid?

A

Antitussive

steriochemistry is wrong

32
Q

Loperamide

Looks like 2 things

Why can this be OTC?

A
  • Looks like anticholinergic and haloperidol
  • Antidiarrheal cant cross the BBB so its OTC
33
Q

What are the 3 ways you can isolate something to the periphery?

What are examples of these ways?

A
  1. PEG group- Naloxegol
  2. All time positive charge - Methylnaltrexone
  3. Zwitter ion - Alvimopan
34
Q

Nalfurafine

Used for?

A

Pruritis

Itching with mu agonists

potent kappa agonists blocks the itch

35
Q

Alvimopan

A

Peripherally acting mu antagonist

zwitter ion

36
Q

In general when looking for a short acting analgesic you would chose?

A

Remifentanil, Sufentanil

Remi is the shortes

37
Q

Krokodil?

A

Cheap drug of abuse prepared from Codeine

38
Q

Salvinorin A

Pure?

A

Kappa Agonist

Medicinal Chem (15 decks)

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