Opioid Anelgesics

Front 1

Overall opoid use

Back 1

To relieve intense pain & accompanying anxiety due to surgery, cancer, Dx. Fantastic in palliative care.

Front 2

General Method of action of Opoids

Back 2

All in this category work by binding to opioid R in CNS; all R are negatively coupled to G-proteins and decrease cAMP

Front 3

Overall PK of Opoids

Back 3

Potency proportional to affinity for Mu-R;
No plateau (Ceiling dose): think CRPS pts;
Increased dose=Increased Efficacy;
Highly lipophilic-->give orally, 1st pass effect;
In general see Liver Metab & Urinary Excretion

Front 4

MU receptor information

Back 4

Found at BOTH Pre & Post Synaptic Membranes Also on LEUKOCYTES; watch Impact on Immune response.
Major endogenous ligand is ENDORPHINS! (order End>Enk>>Dyn);
POMC is precursor to endorphin.

Front 5

Kappa Receptor Info

Back 5

Only at PREsyn;
causes mild resp depression;
Major Endogenous ligond is DYNORPHINS!

Front 6

Delta Receptor info

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Only at PREsyn;
unclear what delta does, has poor analgesia & little addiction.
Major endogenous ligand is ENKEPHALINS!

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General adverse events associated with Opoids

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sedation,
constipation,
nausea/vomiting,
urinary retention,
potential for addiction (mainly M/D),
respiratory depression; dysphoria (K),
Opioid Induced Hyperalgesia (OIH)--treatment is gen anesth Ketamine

Front 8

Why use Morphine

Back 8

good for severe and acute pain, such as metastatic cancer

Front 9

Effects of Morphine

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actions in CNS, cause sedation, drowsiness, euphoria, pupil constrict

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MOA of Morphine

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STRONG ANALGESIC, MU AGONIST

Front 11

PK of Morphine

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only 25% is left after 1st pass!

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Considerations for Morphine

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for all opioids: watch tolerance (reduced efficacy over time); chronic tolerance 1st sign is reduced analgesia

Front 13

Morphine and Hydromorphine in HIV

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Mu receptors are on leukocytes; Mu opioid agonists lead to an upregulation of HIV-1 co-receptors (effect observed in heroin addicts)

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Why use Hydromorphine

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Good for chronic pain

Front 15

MOA of Hydromorphine

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STRONG ANALGESIC, MU AGONIST

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PK of Hydromorphine

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10x more potent than morphine

Front 17

Why use Methadone

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good for chronic pain and heroin addition step-down

Front 18

MOA of Methadone

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STRONG ANALGESIC, MU AGONIST

Front 19

PK of Methadone

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long t 1/2, not as subject to first-pass effect!

Front 20

Difference of effect between Morphine and Methadone

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not as euphoric as morphine

Front 21

Why use Merperdine (Demerol)

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good choice for neonates

Front 22

MOA of Merperdine (Demerol)

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STRONG ANALGESIC, MU AGONIST

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Affect on respiratory depression of Merperdine (Demerol)

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less respiratory depression

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Merperdine (Demerol) in pregnancy

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does cross the placenta

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Severe Drug interaction with Merperdine (Demerol)

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MAOI's or SSRI's + Merperdine-->hyperpyrexia (w/seizures & coma) or serotonin syndrome, is life-threatening!

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Why use Fentanyl

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is EIGHTY times more potent than morphine! Used in SURGERY

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MOA of Fentanyl

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STRONG ANALGESIC, MU AGONIST

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Fentanyl and respiratory depression

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occasional fatalities due to respiratory depression (inc PCO2, less rxn of brainstem)

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How is Fentanyl delivered

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is given TRANSDERMALLY as a patch…"fentanyl patch", NOT GIVEN ORALLY!!

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Why use codeine

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10x less potent than morphine

Front 31

MOA of Codeine

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MODERATE ANALGESIC, MU AGONIST

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PK of Codeine

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note about 60% of codeine is left over after 1 pass and then 10 % of that is converted to morphine.

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Common use of Codeine

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often formulated w/aspirin and acetaminophen as a cough suppressant in cold medicines

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Why use Propoxyphene

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Similar to methadone but less potent

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MOA of Propoxyphene

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MODERATE ANALGESIC, MU AGONIST

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How does the abuse potential of propoxyphene compare to that of codeine

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equal

Front 37

Why use Pentazocine

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preop analgesia/sedative in obstetrics; rheumatoid arthritis

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MOA of Pentazocine

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Low dose KAPPA AGONIST, High Dose KAPPA AGONIST & MU PARTIAL AGONIST/MU ANTAGONIST; effects similar to morphine overall

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PK of Pentazocine

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dose effect-->at lo is K agonist, at hi dose is dysphoric K agonist and M agonist/antag

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Why was Pentazocine created

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this drug class is an attempt to reduce mechanisms of abuse

Front 41

How does abuse of Buprenorpine
compare to morphine

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Buprenorpine
is less

Front 42

Drug interactions of Buprenorpine

Back 42

taking buprenorpine increases resistance to naloxone

Front 43

MOA of Butorphanol

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MU PARTIAL AGONIST, KAPPA AGONIST

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MOA of Nalbuphine

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MU PARTIAL AGONIST, KAPPA AGONIST

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Why use Naloxone

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treating opioid overdose in EMERGENCIES; get patient breathing!

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Affect of Naloxone

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fast reversal of Mu agonists in 1-2 minutes; reverses respiratory depression

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MOA of Naloxone

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NARCOTIC ANTAGONIST (do NOT activate opioid-R)

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Why use Buprenorpine

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Good for acute or chronic pain.

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MOA of Buprenorpine

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Potent Mu PARTIAL AGONIST; note SLOW dissociation from Mu receptor--> long duration of action.

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How is Buprenorpine delivered

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given sublingually (under tongue)

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How does abuse of Buprenorpine
compare to morphine

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Buprenorpine
is less

Front 52

Drug interactions of Buprenorpine

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taking buprenorpine increases resistance to naloxone

Front 53

MOA of Butorphanol

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MU PARTIAL AGONIST, KAPPA AGONIST

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MOA of Nalbuphine

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MU PARTIAL AGONIST, KAPPA AGONIST

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Why use Naloxone

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treating opioid overdose in EMERGENCIES; get patient breathing!

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Affect of Naloxone

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fast reversal of Mu agonists in 1-2 minutes; reverses respiratory depression

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MOA of Naloxone

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NARCOTIC ANTAGONIST (do NOT activate opioid-R)

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PK of Naloxone

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FAST acting, crosses BBB to reverse respiratory depression

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How does Naloxone interact with acupuncture

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EFFECT of low frequency/high intensity acupuncture "as much as patient can take" is BLOCKED by Naloxone (acupuncture causes release of Endorphin & Enkephalin but Mu-R are antagonized by the drug)
note that high frequency/low intensity acupuncture "patient can barely feel it" is NOT AFFECTED by these drugs!

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What happens to someone on Buprenorpine when given Naloxone

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pts who take buprenorpine may be resistant to treatment!

Front 61

What is the difference between naloxone methylbromide (quaternary Naloxone) and Naloxone

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quaternary Naloxone doesn't cross the BBB

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Why use Naltrexone

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treating overdose long term

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MOA of Naltrexone

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NARCOTIC ANTAGONIST (do NOT activate opioid-R)

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PK of Naltrexone

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orally active, longer duration of action

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Triad of narcotic OD

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triad of narcotic OD: pinpoint pupils, respiratory depression, coma

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Mu receptor location

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Presynaptic (Periaqueductal Grey (PAG) around CA in midbrain & Dorsal horn of spinal cord; Postsynaptic=olfactory bulb, nucleus accumbens (ventral striatum, basal gang), limbic cortex and amydala

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What is the first choice of kappa receptors

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dynorphins