T3 Komiskey - Opiates

Front 1

what are opioids?

Back 1

opioid refers to all agonists adn antagonists with morphine like activity as well as to naturally occurring and synthetic opioid peptides.

Front 2

what are the 3 classes of opioid receptors and where are they located?

Back 2

mu, kappa, and delta; throughout the CNS, including cortex, thalamus, brainstem, and spinal cord

Front 3

what are the effects of mu receptors?

Back 3

produce spinal/supraspinal analgesia, euphoria, respiratory depression, miosis, and constipation

Front 4

what receptor is responsible for producing spinal analgesia, sedation, dysphoria, and miosis?

Back 4

kappa

Front 5

waht receptor is just responsible for producing supraspinal/spinal analgesia?

Back 5

delta

Front 6

how do opioids help reduce pain?

Back 6

they cause hyperpolarization of nerve cells by activating K+ channels, and inhibit both nerve firing and presynaptic transmitter release by inhibiting voltage-operated calcium and NT release

Front 7

names some classes of analgesic agents.

Back 7

NON-OPIOIDS (NSAIDs)good for mild pain alone, good for moderate if given with low-dose opioids; OPIOIDS: choice for severe pain; ANALGESIC ADJUVANTS (muscle relaxers, antidepres, antianxiety): alone little effect, but significantly enhance the action of other pain killers

Front 8

what does opium contain?

Back 8

morphine, codeine, thebaine

Front 9

what drugs are considered strong opioid agonists?

Back 9

morphine, meperidine, methadone, fentanyl, heroin, hydromorphone

Front 10

what would a heroin user's urine reveal?

Back 10

free morphine, morphine glucuronide, free codeine, 6-monoacetylmorphine (specific for heroin use)

Front 11

what legal food can reveal a positive test for morphine and codeine?

Back 11

poppy seeds

Front 12

what receptors are activated by mechanical, thermal, and/or chemical stimuli (respond to damaging stimuli)?

Back 12

nociceptors

Front 13

where do nociceptor fibers terminate?

Back 13

in the dorsal horn of the spinal cord

Front 14

what fibers localize pain fast, which slow?

Back 14

small fibers - fast response; larger fibers - slow transfer of info, delayed response

Front 15

what are the 3 types of pain?

Back 15

nociceptive pain, inflammatory pain, and neuropathic pain

Front 16

define absence of pain sensation.

Back 16

analgesia

Front 17

deine absence of sensation.

Back 17

anesthesia

Front 18

what two tracts are involved in pain?

Back 18

anterolateral spinothalamic tract and the dorsalcolumn medial leminsical tract

Front 19

what channel do anticonvulsants and local anesthetics inhibit?

Back 19

Na+ channels

Front 20

what are the two types of afferent nociceptor pain fibers that stimulate the spinothalamic tract?

Back 20

fast-conducting, myelinated a-delta fibers and slow, visceral, unmyelinated C fibers

Front 21

give 3 examples of endogenous (naturally occuring) opioids.

Back 21

enkephalins (short interneurons associated with pain pathways, emotional behavior and motor control), endorphins (selective for mu; co-released with ACTH, stress hormone), and dynorphins (co-localized with vasopressin, may have role in fluid homeostasis)

Front 22

how does the body modulate pain with neurotransmitters?

Back 22

1. when stimulated the descending projects or the inhibitory interneuron will release various NTs: GABA, NE or endogenous opioids (ie. enkephalin); 2. bind receptors on presynapse, inhibit Ca2+ leading to reduced vesicle release; 3. bind post-synaptically, cause efflux of K+ or Cl- to hyperpolarize

Hint 22

None

Front 23

what do opioids cause?

Back 23

analgesia, eurphoria, respiratory depression, cough suppression, miosis, emesis, reduced GI motility, histamine release from mast cells, sedation

Front 24

what seems to play a role in endogenous opioid release?

Back 24

emotional stress, esp. fear/stress

Front 25

Opioids are used for therapeutic purposes, name them.

Back 25

analgesia with sedation; treatment of diarrhea; cough suppressant (dextromethorphan); opioid withdrawal (methadone); opioid overdose (naloxone); and anesthesia

Hint 25

None

Front 26

substantia gelatinosa/dorsal horn, the limbic system/thalamus, and the periaqueductal grey area(receives info from the ascending spinothalamic tract) are all areas that contain what?

Back 26

opioid receptors

Front 27

stimulation of the periaqueductal grey matter of the midbrain results in release of what?

Back 27

serotonin in the dorsal horn of the spinal cord, profound analgesia, activation of interneurons containing enkephalin, and release of norE in dorsal horn

Front 28

which opioid receptor is responsible for being the main pharmacological site?

Back 28

mu receptor; mu1: supraspinal analgesia, physical dependence, and euphoria, inhibits ACh release; mu2: spinal analgesia, respiratory depression, miosis, and decrease GI motility

Front 29

which receptor is predominately associated with endogenous opiates that produces spinal analgesia, miosis, sedation, and dysphoria?

Back 29

kappa

Front 30

name some moderate agonists of opiates.

Back 30

codeine and propoxyphene, tramadol is a synthetic codeine analog that is a weak mu agonist

Front 31

name some antagonists of opiates.

Back 31

naloxone and naltrexone

Front 32

what does the delta receptor responsible for doing?

Back 32

enhances mu agonists and reinforces supraspinal analgesia

Front 33

tolerance develops to most of morphine's effects, except with:

Back 33

miosis, constipation, and pruritis

Front 34

morphines main MOA:

Back 34

activation of mu receptors

Front 35

when is morphine indicated?

Back 35

acute pain (do not use in chronic non-malignant pain); dyspnea and pulmonary edema, pre-anesthetic medication, open heart surgery, decrease fear in dying

Front 36

is morphine equally effective orally vs parentally?

Back 36

no, only 25% for oral

Front 37

what does morphine do to respiration? does it make people nauseated?

Back 37

decreases rate, volume and tidal exchange: respiratory depression is dose related; morphine stimulates CTZ and may cause nausea and vomiting

Front 38

what are the cardiovascular effects of morphine?

Back 38

vasodilation, thus a decrease in blood pressure (histamine causes vasodilation and morphine suppresses the reflex vasoconstriction)

Front 39

what are the GI effects of morphine?

Back 39

increased tone and decreased mobility - constipation

Front 40

name the drug that is 10 times more potent than morphine, more expensive, lasts longer, and has less tendency to induce N/V, less effect on respiratory center and doesn't cause histamine release.

Back 40

oxymorphone - to prevent severe bradycardia, an anticholinergic should be given

Front 41

name the opioid that produces less sedation, shorter duration of action, and less vomiting occurs; it is the only opioid that will directly depress the myocardium.

Back 41

meperidine (Demerol) activates mu receptors; only 1/3 potency of morphine,(not recommended for alleviated post-op pain b/c its short duration of action)

Front 42

name some meperidine analogues used to treat diarrhea.

Back 42

loperamide (imodium) and diphenoxylate

Front 43

codeine gets turned into what in the liver?

Back 43

morphine

Front 44

what opioid drug is 75-125 times more potent than morphine, be active for only 45-60min, with MINIMAL CARDIO effects except for bradyarrhythmias, however, more severe respiratory depression.

Back 44

fentanyl

Front 45

Name some fentanyl congeners.

Back 45

sufentanyl (1000xs more potent than morphine); alfentanil and remifentail (rapid onset of analgesia)

Front 46

what two piperidines are used for short, painful procedures that need intense analgesia and suppressing stress response?

Back 46

alfentanil and remifentanil

Front 47

explain the pharmacokinetics of opiates.

Back 47

ABSORPTION: RAPIDLY ABSORBED in GI, high rate of 1st metabolism, highly lipophilic can be absorbed transdermally; DISTRIBUTION: all bind to plasma proteins; will rapidly leave the blood to go into other tissues; METABOLISM: first pass effect; most are converted to more polar metabolites in the liver, turned into glucuronides or N-demethylated; 6-glucuronide is more potent; 3-glucuronide is inactive and found in urine; EXCRETION: kidneys

Front 48

what signifies acute morphine poisoning?

Back 48

Triad of Coma, miosis, cyanosis (decreased respirations); respiratory failure

Front 49

what would be a good way to painlessly administer an analgesic to a child for a surgical procedure. it takes effect within 15-20min and lasts 1-2hrs?

Back 49

intrabuccal fentanyl (Oralet and Actiq-used for CA pts with breakthrough pain)

Front 50

what is a good way to manage chronic malignant pain, duration of action of 72hrs

Back 50

transdermal fentanyl

Front 51

what drug is commonly abused by crushing the extended release opioid?

Back 51

oxycontin

Front 52

describe codeine's effects and indications.

Back 52

10% gets converted to morphine, has a higher oral efficiency and slower development of tolerance than morphine, less respiratory depression, less dependence, less euphoria; INDICATIONS: moderate pain and as an antitussive

Front 53

name a codeine analog that is for mild to mod pain and is excreted renally;and describe its MOA.

Back 53

tramadol (Ultram); blocks reuptake of NorE and 5-HT

Front 54

name the most prescribed drug that is highly abused and more potent than codeine.

Back 54

hydrocodone

Front 55

what type of drugs may be used to reverse depressant effects of opioid while preserving it's analgesic qualities?

Back 55

any non-pure mu agoinst: ie. partial mu agonist, poor mu antagonist, and kappa agonist

Front 56

name the drug that is 1/3 as potent as morphine wiht faster onset and shorter duration; and is a kappa agonist, mu and delta antagonist

Back 56

pentazocine

Front 57

name a long acting, potent opioid , mu and kappa partial agonist, delta antagonist

Back 57

buprenorphine - PARTIAL AGONIST 20-50x potency of morphine; used to in tx of opiate addicts; available worldwide(less physical depend. ceiling effect on respiratory depression)

Front 58

high doses of this drug can cause CNS stimulation with convulsions, respiratory depression, haluucinations, confusion, and coma (chemically related to methadone with <1/2 the analgesic potency of codeine.

Back 58

D-propoxyphene

Front 59

name the drug that antagonizes most opioid receptors agonists (almost pure antagonist) that is used to reverse opiod overdose.

Back 59

naloxone (Narcan) - short half-life; observe for recurrent signs of opiate intoxication (given IV)

Front 60

name the longer acting derivative of the opiate antagonist naloxone?

Back 60

naltrexone (clinically used to tx opiate addicts - it reduces pleasure from opiates)

Front 61

what is the purpose of combining a low dose opioid antagonist with an opiate agonist?

Back 61

pain relief is more easily achieved, enhances the analgesic effect

Front 62

name 4 drugs that are used to treat opiate dependence.

Back 62

methadone (full agonist at the mu receptor; its long half-life helps prevent withdrawal), buprenorphine (suppresses withdrawal, blocks subsequent opiate use), LAAM, and naltrexone

Front 63

name some common OTC meds that contain dextromethorphan.

Back 63

vicks 44 cough relief; Robitussin DM, Coricidin cough & cold

Front 64

how would someone present clinically with a dextromethorphan overdose?

Back 64

slurred speech, restlessness, poor coordination, difficulty breathing, seizures