Module 9: Opiates & Opioids Flashcards by Kelley Jones

opium poppy

Papaver Somniferum

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Miosis

Pinpoint pupils (constricted)

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Follows 1st-pass metabolism when taken orally
Low oral bioavailability (more potent when taken other ways)
Slow to cross blood-brain barrier
Metabolite of codeine and heroin
Duration of action: 4-5 hours

Morphine

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Endogenous Opioid Peptide that bind to mu opioid receptors.

Endorphins

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Endogenous Opioid Peptide that bind to delta opioid receptors primarily.

Enkephalins

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Endogenous Opioid Peptide that bind to kappa opioid receptors primarily.

Dynorphins

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3 types of Opioid receptors

Mu, Kappa, Delta

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Peak of Opioid Abstinence Syndrome

36-72 hours

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Duration of Opioid Abstinence Syndrome

7-10 days

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Beginning of Opioid Abstinence Syndrome

6-8 hours

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Category of Opioids including morphine, codeine, hydromorphone, etc.

Phenanthrenes

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Category of Opioids including Fentanyl, sufentanil, furanryl fentanyl, etc.

Phenylpiperidines

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Opioid Classifications (mode of action)

Agonist, Antagonist, Mixed Agonist/Antagonist

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Agonist
Highest oral bioavailability
10-15% metabolized to morphine
Duration of analgesia: 3-4 hours

Codeine

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Agonist
2-3 times more potent than morphine (penetrates BBB)
poor oral biovavailbility
rapid metabolism to 6MAM (half life = 2-6 min) then to morphine

Heroin

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Agonist Derivative of Codeine
metabolized to hydromorphone and dihydrocodeine
Duration of analgesia: 3-5 hours

Hydrocodone

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Agonist
metabolite of hydrocodone and morphine (minor)
More potent than morphine
Duration of analgesia: 4-5 hours

Hydromorphone

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Agonist
Derived from thebaine
15% metabolized to oxymorphone
Duration of analgesia: 3-4 hours

Oxycodone

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Agonist
Metabolite of Oxycodone
Duration of analgesia: 3-4 hours

Oxymorphone

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Agonist
Most potent and fast-acting opioid
50-200x more potent than Morphine
Transdermal patches can give delayed concentrations for 12-24 hrs
Duration of analgesia: 1-15. hours

Fentanyl

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Agonist
Long elimination half life
Metabolizes to EDDP and EDMP
Duration of analgesia: 4-6 hours

Methadone

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Atypical opioid agonist
Metabolite (o-dm-) is 2x more potent (contributes to toxicity)
Duration of analgesia: 4-6 hours

Tramadol

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Agonist used to decrease diarrhea
Doesn’t have effects like morphine except in high doses (do to opioid receptor activities)
“poor man’s methadone”

Loperamide

Antagonist
Narcan
Rapid action (minutes)
Short duration of action (2 hours)

Naloxone

Antagonist Used to treat addition after withdrawal complete Used for chronic alcoholics

Naltrexone

Mixed Agonist/Antagonist Produces withdrawal if an opioid agonist is also taken Partial agonist at mu receptor and kappa antagonist Available in preparation w/ naloxone (Suboxone) or by itself (Buprenex) Inactive metabolite (nor-)

Buprenorphine

Location of opioid metabolism in body.

Liver Metabolized to more polar compounds

Primary mechanisms of metabolism of opioids.

N-dealkylation, conjugation of hydroxyl groups, hydrolysis

3 Opioids where the metabolites account for most of the desired effects

Codeine, Heroin, Tramadol

Isozyme largely responsible for first-pass metabolism of Opioids

CYP2D6

Morphine is primarily excreted as:

Morphine-3-glucuronide (inactive) *Morphine-6-glucuronide (more potent than morphine) **Think about how codeine is less potent and that differs from morphine at 3 group also

Opioid effects on: Pupils Eye Reaction to Light Pulse Blood Pressure Body Temperature

Pupils - constricted Eye Reaction to Light - little to none Pulse - down Blood Pressure - down Body Temperature - down

3 main signs of opioid ODs

CNS depression (respiratory depression) Coma Pinpoint Pupils

Compound present indicates ingestion of poppy seeds

Thebaine

The opioid receptor that produces central depression, analgesia, miosis, reduced gastrointestinal motility

Opioid used clinically since 1957, but recommended for removal from the U.S. drug market in 2010.

Propoxyphene

When codeine is taken as a parent drug, approximately _______ is metabolized to morphine.

10%

Semisynthetic analgesic agonist derived from codeine that is used in cough syrups:

Hydrocodone

In the hair matrix, 6-MAM has been detected in hair of heroin users at typically _______ concentrations than for morphine. The same smaller greater 6-MAM not present in hair

Greater

Opioids are _______ in nature. Basic, Neutral, or Acidic

Basic

Organic solvents are often used to extract opioids from aqueous mixtures in the pH range of:

8-10

True or False: Opiates cause pupil dilation.

False They cause constriction.

Has less potency relative to morphine: Hydrocodone, Oxycodone, Fentanyl, Codeine, Methadone

Codeine

_______ is the major metabolic route for opioids that contain available hydroxyl (OH) groups. Sulfation, Demethylation, Glucuronidation, Dealkylation, Methylation

Glucuronidation

True or False: Only the levorotatory isomer of morphine is a potent analgesic.

True

Successfully used for the treatment of respiratory depression after postsurgical opioid administration: Buprenorphine, Levorphanol, Methadone, Nalbuphine, Fentanyl

Nalbuphine

This metabolite is more potent than morphine: Morphine-6-glucuronide, Codeine, Tramadol, Morphine-3-glucuronide, Morphine

Morphine-6-glucuronide

Acidic hydrolysis of conjugated metabolites should be done with caution as this analyte may be degraded. Dihydrocodeine, Oxymorphone, Hydromorphone, 6-MAM, Codeine

6-MAM

Opioid Metabolism takes place primarily in the _______. Liver, Brain, Kidney, Urine, Spinal Fluid

Liver

This drug the longest half-life out of the listed choices. Morphine, Tramadol, Methadone, Hydrocodone, Fentanyl

Methadone

This opioid has approximately 100-200x the analgesic potency of morphine.

Fentanyl

True or False: Rapid deaths are often characterized by a higher ratio of the concentrations of free morphine to total morphine.

True Total morphine includes conjugated morphine - body has had time to process and metabolize morphine. Free morphine has not been conjugated for excretion.

Typical pKa values for Opioids are: 1.2-3.4 3.2-4.6 7.6-8.9 9.2-10.6 >10

7.6-8.9

Used to manage intestinal upset and has been used to lessen withdrawal or produce euphoric effects: Alfentanil, Loperamide, Difenoxin, Hydromorphone, Diphenoxylate

Loperamide

The presence of a low concentration of codeine relative to morphine may indicate the use of _______. Codeine only Morphine only Codeine and morphine Heroin A, C and D

A, C and D *Think: morphine does not metabolize to codeine so it can't be only morphine. Codeine metabolizes to Morphine.

True or False: All opioids are highly protein bound.

False