Chemistry of opioids and opioid antagonists 2

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16 Terms

1
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Hydromorphone

Dilaudid, Exalgo

4-7.5x potency of morphine

less incidence of OIP

R = H

<p>Dilaudid, Exalgo</p><p>4-7.5x potency of morphine</p><p>less incidence of OIP</p><p>R = H</p>
2
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Hydrocodone

Zohydro, Hysingla

active itself

antitussive activity

6-8x potency of morphine

R = CH3

<p>Zohydro, Hysingla</p><p>active itself</p><p>antitussive activity</p><p>6-8x potency of morphine</p><p>R = CH3</p>
3
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Oxymorphone

Opana

10x potency of morphine

R = H

<p>Opana</p><p>10x potency of morphine</p><p>R = H</p>
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Oxycodone

Roxicodone, OxyContin

1.5-2x potency of morphine

active itself

R = CH3

<p>Roxicodone, OxyContin</p><p>1.5-2x potency of morphine</p><p>active itself</p><p>R = CH3</p>
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Naloxone

pure opioid antagonist

t ½ plasma = 30-81 min

Tx opioid OD

orally ineffective (1st pass effect, glucuronidation)

Narcan, Evzio, Zimhi

nasal spray, auto-injectable, injection

<p>pure opioid antagonist</p><p>t ½ plasma = 30-81 min</p><p>Tx opioid OD</p><p>orally ineffective (1st pass effect, glucuronidation)</p><p>Narcan, Evzio, Zimhi</p><p>nasal spray, auto-injectable, injection</p>
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Naloxegol

Movantik

PAMORA - pgp substrate
Tx OIC

PEG polymer

<p>Movantik</p><p>PAMORA - pgp substrate<br>Tx OIC</p><p>PEG polymer</p>
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GI effects of opioids

inhibition of GI propulsion

increase in GI tone

inhibition of GI secretion

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OIC (opioid-induced constipation)

hard dry stool

bloating

straining

infrequent/incomplete defecation

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sequels/secondary symptoms of OIC

gastro-esophageal reflux

nausea and vomiting

anorexia

abdominal distention

abdominal cramping

interference with digestion

interference with drug absorption

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Naltrexone

antagonist - more potent than naloxone

orally active

DOA = 4h

maintenance Tx of OUD

Tx alcohol dependence

<p>antagonist - more potent than naloxone</p><p>orally active </p><p>DOA = 4h</p><p>maintenance Tx of OUD</p><p>Tx alcohol dependence</p>
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Naltrexone metabolism: AKR

forms 6 beta-naltrexol

<p>forms 6 beta-naltrexol</p>
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Bupropion

antidepressant, decreases reuptake of NE, DA

side effect - weight loss

in a combo drug with Naltrexone for Tx obesity

<p>antidepressant, decreases reuptake of NE, DA</p><p>side effect - weight loss</p><p>in a combo drug with Naltrexone for Tx obesity</p>
13
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Methylnaltrexone

Relistor

soln for injection, oral tablet

PAMORA (Tx OIC)

<p>Relistor</p><p>soln for injection, oral tablet</p><p>PAMORA (Tx OIC)</p>
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Nalmefene

soln for injection

nasal spray, auto-injector

Tx opioid OD, alcohol dependence

<p>soln for injection</p><p>nasal spray, auto-injector</p><p>Tx opioid OD, alcohol dependence</p>
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naldemedine

Symproic

Tx OIC

<p>Symproic</p><p>Tx OIC</p>
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Lybalvi

Olanzapine (antipsychotic) + Samidorphan L-malate

olanzipine - causes massive weight gain

Sami - mitigates weight gain

<p>Olanzapine (antipsychotic) + Samidorphan L-malate</p><p>olanzipine - causes massive weight gain</p><p>Sami - mitigates weight gain</p>