pharmacology of opioids Flashcards by Deja Lenae

what are the chemical classes of opioids?

phenathrenes
phenylpiperidines
benzomorphans
dipheylheptanes

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what are the functional classes or opioids

opioid agonists

mixed agonists/antagonists

opioid antagonist

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give a classic example of opioid agonists (5)

morphine
methadone
fentanyl
codeine
hydrocodone

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give an example of a mixed opioid agonist/antagonist (2)

pentazocine
buprenorphine

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given an example of opioid antagonists (2)

naloxone and naltrexone

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opioid drugs MOA

bind to the opioid receptors in the CNS and inhibit pain pathways giving a generalized CNS depression

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onset of action of an opioid is dependent on what

patient

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duration of pain relief in opioids

immediate release
extended release
epidural/intrathecal
suppository

immediate release: 3-5 hrs

extended release: 8-24 hrs.

epidural/intrathecal- up to 24 hrs

suppository - 3 to 7 hrs

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when do we use opioid therapy

in acute/chronic pain and pain management

MI, sickle cell crisis, back pain, cancer, post operative procedures, adjunct to anesthesia, antitussive*
antidiarrheal

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opined drug side effects

CNS depression

Respiratory depression-BBW

constipation

hypotension

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what is the black box warning associated with using opioids?

respiratory depression (can be fatal) monitor closely especially during initiation or dose escalation.

*carbon dioxide retention from opioid induced respiratory depression can exacerbate the sedating effects of opioids

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acute effects of opioids

sedation, euphoria, loss of cough reflex (antitussive), slowed CNS and heart

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chronic effects of opioids

tolerance, hepatic and brain damage, dependance and addiction, loss of appetite, loss of libido

hepC from sharing needles

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how do sedatives/hypnotics interact with opioid drugs

they increase the central nervous system depression (respiratory depression)

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how to antipsychotics interact with opioids?

increase sedation and cardiovascular effects

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how do monamine oxidase inhibitors interact with opioids?

they are contraindicated because they can cause hyper pyrexic coma

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fentanyl is _ times more potent than morphine

100

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lower doses of opioids before analgesic effects are

antidiarrheal
antitussive
euphoria
nausea

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higher doses of opioids after analgesic effects are?

mitosis/vomiting
sedation
respiratory depression
coma/death

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what is the function of the mu receptor

and what is its endogenous opioid peptide affinity

supraspinal and spinal analgesia

INHIBITION OF RESPIRATION

slowed GI transit

modulation of hormone and NT release

**ENDORPHINS

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what is the function of the delta receptor

and what is the endogenous opioid peptide affinity

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supra spinal/spinal analgesia

modulation of hormone and NT release

ENKEPHALINS

what is the function of the kappa receptor

and what is the endogenous opioid peptide affinity

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supra spinal and spinal analgesia

PSYCHOMIMETIC EFFECTS

slower GI transit

DYNORPHINS

which drug is an agonist at the mu, delta, and kappa receptors

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morphine!

which drug is an agonist at the mu receptor

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methadone

what drug is a partial agonist at the mu, delta, and kappa receptor

buprenorphine

what drug is an antagonist at the mu and delta receptor

naloxone

_ is an opioid agonist that is indicated for the management of pain not reponsive to non-narcotic analgesics do not use if there is sulfa allergy, bronchial asthma, or respiratory depression

morphine

what opioid is indicated management of persistent moderate to severe chronic pain that requires continuous around the clock opioid administration for an extended period of time **pain is not controlled with non-narcotic anaglesics, combination opioids, all option exhausted

fentanyl

which opioid is most appropriate to manage abstinence symptoms and treat opioid use disorder in an outpatient rehabilitation setting (withdrawal acute and active)- full agonist

methadone (clinics) detoxification and maintence

which opioid is used for moderately to severe pain that is a semi synthetic narcotic with antitussive qualities (anti cough) very common and highly prescribed

hydrocodone

hydrocodone is frequently combined with ?

acetaminophen

what opioid is a mixed agonist/antagonist that is used in the management of severe pain that alternative treatments have failed to treat

pentazocine

pentazocine is used when? addiction?

used as a preoperative or preanaethesia medication and as a supplement does not work for addiction

concomitant use of opioids with _ or another other CNS depressants including alcohol can result in sedation, depression, coma and death

benzodiazepines

prolonged used of _ during pregnancy can result in neonatal opioid withdrawal syndrome

pentazocine

which opioid is used in the management of severe pain that was not mitigated by other option and CANNOT be mixed with a mixed agonist/antagonist analgesics because it can precipitate withdrawal symptoms

meperidine

what opioid is an analgesic, antitussive and contains the least opioid analgesic activity

codeine

which opioid exposed patients and users to the risks of opioid addiction, abuse and tissues

codeine

uses of codeine

mild pain, cough, diarrhea

when discontinuing chronic opioid therapy the dose should be

gradually tapered down

which opioid is used to treat diarrhea and decrease the amount of drainage in patients with ostomies patient with addiction can take this to minimize withdrawal effects (OTC)

loperamide

which opioid is indicated in the treatment of pain, addiction to opioids (withdrawal - acute and maintenance) it is a partial agonist and can be abused in similar ways to opioids

buprenorphine

what should you be monitoring in patients if you start them on buprenorphine

monitor for overdosing or underusing since it is a CYP3A4 inhibitor and inducers

MOA of naloxone

opioid antagonist at all sites

use of naloxone

opioid overdose (reversal of opioid reversal ) give even in opioid overdose is SUSPECTED

side effects of opioid antagonists

release of catecholamines that can cause acute withdrawal and cause pain

what is the MOA of naltrexone

opioid antagonist that is a competitive inhibitor at the mu receptors (opioid addiction - maintenance)

use of naltrexone

alcohol disorder opioid dependence

what is the concern surrounding naltrexone in opioid overdose

people treated with naltrexone may response to lower opioid doses than used before which can lead to intoxication (life threatening)

what is the concern surrounding naltrexone in opioid withdrawal

may precipitate symptoms of acute withdrawal in the opioid dependence in patients

acute withdrawal of opioids in neonates

naltrexone - shrill cry

can opioids exacerbate OTC pain relievers

yes aspirin ibuprofen bismuth naproxen diphenhydramine

pharmacology of opioids Flashcards

(52 cards)