Chemistry of opioids and opioid antagonists 3

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12 Terms

1
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Buprenorpine

oripavine derivative

partial MOR agonist - high affinity (t ½ = 37h)

Antagonist at KOR and DOR
analgesia, less sedation (less risk addiction)

fewer withdrawal symptoms

lower effect on respiration

<p>oripavine derivative</p><p>partial MOR agonist - high affinity (t ½ = 37h)</p><p>Antagonist at KOR and DOR<br>analgesia, less sedation (less risk addiction)</p><p>fewer withdrawal symptoms</p><p>lower effect on respiration</p>
2
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Buprenorphine metabolism

1st pass via CYP3A4 at the cyclopropylmethyl

N-dealkylation

4x less potent

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Thebaine

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Oripavine

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Suboxone

Buprenorphine + Naloxone sublingual tabs

abuse deterrent

replacement therapy for opioid dependence

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Nalbuphine

mixed agonist (KOR)/antagonist (MOR)

lower effect on respiration

can cause dysphoria

<p>mixed agonist (KOR)/antagonist (MOR)</p><p>lower effect on respiration</p><p>can cause dysphoria</p>
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Levorphanol

5x more potent than morphine

t ½ = 11-16h

LogP = 11-16h

<p>5x more potent than morphine</p><p>t ½ = 11-16h</p><p>LogP = 11-16h</p>
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Dextrorphan

result of O-demethylation on dextromethorphan

NMDA antagonist (so is PCP)

psycotropic

→ reason for abuse of dextromethorphan

<p>result of O-demethylation on dextromethorphan</p><p>NMDA antagonist (so is PCP)</p><p>psycotropic</p><p>→ reason for abuse of dextromethorphan</p>
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dextromethorphan

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Phencyclidine

“PCP”

<p>“PCP”</p>
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Butorphanol

Mixed agonist (KOR - strong)/antagonist (MOR - weak)

5-10x more potent than nalbuphine

extensive 1st pass metabolism

<p>Mixed agonist (KOR - strong)/antagonist (MOR - weak)</p><p>5-10x more potent than nalbuphine</p><p>extensive 1st pass metabolism</p>
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Pentazocine

KOR agonist

MOR antagonist

weakest mixed drug

lacks E and C ring

<p>KOR agonist</p><p>MOR antagonist</p><p>weakest mixed drug</p><p>lacks E and C ring</p>