- Opioid receptor agonist - Blocks release of pain neurotransmitters from nociceptive fibers - Inhibits GABA release so that dopamine fire more vigorously and can accumulate in the gap ( = pleasure)

Opioids Flashcards by Brianna Spahn

Opioid MOA, class

Opioid receptor agonist
Blocks release of pain neurotransmitters from nociceptive fibers
Inhibits GABA release so that dopamine fire more vigorously and can accumulate in the gap ( = pleasure)

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Pain neurotransmitters

Substance P
Glutamate
Calcitonin gene peptide

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Opioid receptors

Mu - brainstem and medial thalamus
Kappa - limbic, spinal cord
Delta - brain, not well studied

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Opioid receptor responsible for analgesia, respiratory depression, euphoria, sedation, decreased GI motility, addiction

Mu = Morphine Agonist

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Opioid receptor responsible for dyspnea, dependence, dysphoria

Kappa

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Full Opioid Agonists

Morphine
Fentanyl
Hydromorphone

Codeine
Oxycodone

Methadone
Heroin

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Partial Opioid Agonists

Buprenorphine

Butorphenal

Suboxone (buprenorphine + Naloxone)

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Opioid antagonists

Naloxone (Narcan)

Naltrexone

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Morphine, oxycodone, methadone, fentanyl, amphetamine - what schedule?

Schedule II

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Schedule III drugs

Moderate addiction potential

Hydrocodone, codeine, anaboilc steroids

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Schedule IV drugs

Low addiction potential

Benzodiazepine,
Meprobamate
Butorphenol
Pentazocine
Propoxyphene

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Why opioids can cause pruritus / uriticaria

Direct histamine response

Can also cause bronchospasm

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Opioid overdose triad

Miosis

Loss of consciousness

Respiratory depression

much worse w alcohol or other CNS depressants

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Antidote to opioid overdose

Naloxone

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Half life of morphine

2 hours

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Morphine drug interactions

RARE

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Which opioid crosses the BBB

Morphine

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Codeine is metabolized to

Morphine

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Potency of Codeine vs Morphine

Codeine has 50% potency of morphine

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What drugs inhibit effect of codeine and why?

2D6!

Buproprion
Cimetidine
Cocaine
Celecoxib

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Codeine warning

ULTRA METABOLIZERS

esp infants nursing from mothers who take it

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3 Kinds of oxycodone

Roxicodone
Percocet
Oxycontin

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Why is oxycodone such a high potency analgesic?

Mu AND Kappa activity

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Percocet =

Oxycodone + Acetaminophen

Most commonly used opioid

Hydrocodone

Hydrocodone metabolized to _____ by ______

HydoMORphone, by 2D6 (just like codeine)

Vicodin =

Hydrocodone + Acetaminophen aka Lorcet or Lortab

Hydromorphone ex

Dilaudid Exalgo

Hydromorphone 1/2 life

4 hours MORE POTENT THAN MORPHINE

Which is more potent - morphine of hyrdromorphone

HYDROMORPHONE (Dilaudid)

How is hydromorphone metabolized and what does that indicated?

Metabolized by Glucuronidation Indicates LIVER activity

10x more potent than Morphine No P450 interactions

OXYMORPHONE aka Opana

80x more potent than Morphine 3A4 metabolism

FENTANYL

Fentanyl administration, onset, half life

Transdermal patch 6-12 hr onset for analgesic effect clearance takes up to 24 hours

Fentanyl warnings

1. Dont heat or cut patch - dose dumping | 2. Cross reactive w codeine allergy

Opioid to avoid w elderly and with MAO-I's

Demerol Anticholinergic properties

Demerol ADR warnings

Neurologic toxicity Anxiety, tremors, seizures - NOT reversible with naloxone

Opioid that can also be used for neuropathic pain and is a SNRI

Methodone

Methodone metabolism

CYP3A4 and 2D6 Highly lipophilic

Methadone ADR warning

Cardiotoxicity - Torsades de Pointes

Used for heroin / opioid addiction. Has a "ceiling effect"

Buprenorphine Mu agonist Kappa antagonist

Naloxone / Narcan ADRs

Headache Myalgia Increased BP ---opioid withdrawal

Opioid receptor antagonist used for opioid addiction. CI in patients using opioids / alcohol

Naltrexone

Synthetic codeine analog

Tramadol

Tramadol MOA

Weak Mu receptor agonist SNRI (inhibits NE and 5HT uptake)

Tramadol indications

As effective as morphine for mild - moderate pain - labor Less effective for severe or chronic pain

Tramadol Warnings

Seizure risk at increased doses Suicide risk Serotonin syndrome risk

Serotonin syndrome

``` Agitation Confusion High BP, HR Dilated Pupils Sweating Diarrhea Muscle twitching / rigidity ```

Tramadol drug interactions

Carbamazepine Serotonergic drugs 2D5, 3A4 inhibitor

Opioid approved specifically for diabetic neuropathy

Tapentadol (Nucynta) No P450 interactions!

Tapentadol CI

EToH! Potentially fatal

Which antibiotic will increase opioid effects

Erythromycin

Which group of drugs will decrease the effects of methadone?

Rifampin Phenytoin Carbamazepine

CYD 2D6 inhibitors ``` Amitriptyline Bupropion Cimetidine Cocaine Ranitidine ```

Increase TRAMADOL levels Decrease effect of HYDROCODONE and CODEINE

CYP 3A4 Inhibitors Azoles Verapamil

Increase METHADONE levels

CYP 3A4 Inducers Phenobarb Phenytoin Carbamazepine St. John's Wort

Decrease METHADONE levels

Opioid dependence definition

3 or more of the "addiction behaviors" within a 12 month period

Chronic pain tx guidelines

Chronic Pain = lasting > 1 yr Nonopioid tx preferred Start w IR opioids, evaulate q 1-4 weeks Urine drug test before initiating