- Mu receptor agonist - NMDA antagonist (good for deep nerve pain)

- sedation - vomit - constipation - resp. Depression

Opioid 2 Flashcards by Aliyah Thompson

List the agonist model drugs (5)

morphine
methadone
hydromorphone
fentanyl
tramadol

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List the 2 agonist-antagonist opioids

butorphanol
buprenorphine

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List the only full opioid antagonist

Naloxone2

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Morphine MOA

Mu receptor agonist (new agonist)

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PK of morphine

Liver metabolism & crosses placenta

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Physical effects of morphine

Analgesia (primary use), emesis, miosis, decrease GI motility

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Therapeutic Indications of Morphine

Tx acute pain, anesth. pre-med, antitussive

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Adverse effects of morphine

Hyperexcitability, hypotension, cerebral hemorrhage, edema

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What type of opioid is methdone

Synthetic

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MOA of methadone

Mu receptor agonist
NMDA antagonist (good for deep nerve pain)

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Physical effects of methadone

slower elimination rate compared to morphine
similar analgesic effect as morphine

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Therapeutic indications

pre-med
analgesia

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Adverse effect

sedation
vomit
constipation
resp. Depression

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Hydromorphone MOA

Mu receptor agonist

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Hydromorphone potency comparison to morphine

5x analgesic potency

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Therapeutic indicators for hydromorphone

Analgesia, pre-med, anesthetic

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Adverse effects of hydromorphone

Panting*, bradycard., dose-dependent excitement, cerebral hemorrhage, edema

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Why is hydromorphone being increasingly used in vet med? What is it replacing?

replacing oxymorphone
being used b/c oxymorphone is expensive & has availability issues

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T or F: Fentanyl is a synthetic opioid

True

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What are the units used in fentanyl dosing?

Mcg

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MOA of fentanyl

Mu receptor agonist

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Pharmacokinetics of fentanyl

faster onset than morphine
shorter duration of action
more potent (75-125x)

Therapeutic indications of fentanyl (3)

Continuous infusion analgesia, K9 inductor, neuropetanalgesia

Adverse effects of fentanyl

Motor response, panting, pooping, farts, bradycardia, salivation

Tramadol is a synthetic analog of…

Codeine

MOA of tramadol

Mu receptor agonist (WEAK), inhibits serotonin & NE uptake

Pharmacokinetics for tramadol

- active metabolite: desmethyltramadol - exaggerated opiate effects may be seen in cats b/c they can’t glucuronidate

Therapeutic indications

- analgesic - antitussive in small animals

Can tramadol be reversed?

Yes, only partially by nalaxone

MOA of butorphanol

- high affinity for mu receptors, but no activity - high affinity for kappa receptors, moderate agonist activity - 4-7x stronger than morphine

Is butorphanol an agonist or antagonist?

Neither, its an agonist-antagonist (Both properties)

Pharm. effects of butorphanol

Analgesia

Therapeutic indicators

Opioid reversal, analgesic, antitussive

What effect does butorphanol’s short duration of activity have on its usage?

Limits it (b/c 0.5-6 hrs)

Can butorphanol be reversed?

- yes, but it is difficult b/c of its high receptor affinity

The most generally useful anlagesic in K9 & cats is

Buprenorphine (30x stronger than morphine)

MOA of buprenorphine

- high affinity for mu receptors, but partial agonist - kappa receptor antagonist

Pharmacokinetics for butorphanol

Longer duration of action than other opioids

Therapeutic indications for buprenorphine

- analgesia for mild-mod. Pain in small animals - cats can have buccal or transmucosal admin.

Simbadol

- long acting, SQ buprenorphine - cats only - lasts 24 hrs; admin SID - for surgical pain

Zorbium

- transdermal solution - for cats - lasts for 4 days - single, in clinic dose

Opiate antagonists are…

Pure antagonists; no agonist activity

MOA naloxone

- high affinity for mu receptors (Higher doses reverse DOP and KOP)

Pharmacokinetics of naloxone

- short duration of action, so may need repeated admin

Therapeutic indications of naloxone

- Reverse opioid induced respiratory depression & shock Tx - given IV, IM, IN (if no IN response after 5 mins, repeat) - extralabel use in K9 & cats - not regulated by CSA

Adverse effects of naloxone

- CNS sedation - excitement in horses and cats - resp. Depression - bradycardia - sedation - contraindicated shock, severe cranial trauma and diseases assc. w/ resp. Compromise

Tolerance and dependence of naloxone

- aren’t used long enough in vet med to cause tolerance/depend. - if P is on opiates > 5-7 days, then withdrawal signs may be seen after stopping meds - DON’T CUT OFF COLD TURKEY, WEAN P OFF OPIOID

Schedule I drugs

No medical benefit/use

Schedule II-IV drugs

High to low abuse potential

Schedule V drugs

Lower potential for abuse compared to schedule IV

Most pure opioid agonists (i.e. morphine) are classified as

Schedule II

Buprenorphine is a Schedule….

Schedule III

Butorphanol is Schedule…