Opioid Analgesics And Antagonist

Front 1

components of pain?

Back 1

sensation and emotion

Front 2

types of analgesics and respective site of action?

Back 2

narcotic: CNS at opioid receptor;
non-narcotic (NSAIDs): at peripheral sites

Front 3

effect of opioid analgesics on pain?

Back 3

raise threshold for pain perception;
alter affective response;
(change both components of pain)

Front 4

sites of opioid action?

Back 4

thalamus
limbic system
brainstem
spinal cord

Front 5

spinal cord?

Back 5

intrathecal or epidural opioids produce analgesia that is segmental, rapid in onset, long lasting, with few side effects and no physical dependence

Front 6

precursors and products for endogenous opioids?

Back 6

proenkephalin --> enkephalins;
pro-opiomelanocortin --> endorphins;
prodynorphin --> dynorphins

Front 7

opioid receptors?

Back 7

mu
kappa
delta

Front 8

sigma?

Back 8

PCP receptor;
opioids can act on it

Front 9

cross-reactivity of opioids?

Back 9

tolerance and cross-tolerance;
can substitute or maintain physical dependence of other opioids because work on same receptors

Front 10

naloxone?

Back 10

opioid antagonist

Front 11

pharmacological effects of morphine?

Back 11

mood changes;
nausea and vomiting;
respiratory depression;
antitussive;
miosis;
urinary retention;
inhibits gonadotropin release;
cardiovascular effects;
GI effects

Front 12

mood changes seen with morphine?

Back 12

euphoria
mental clouding: drowsy, lethargic, apathetic, etc (no incoordination, slurring words)

Front 13

mechanism of nausea and vomiting with morphine?

Back 13

stimulate chemoreceptor trigger zone

Front 14

mechanism of respiratory depression with morphine?

Back 14

decreased response to CO2;
bronchoconstriction due to histamine release and direct action

Front 15

mechanism of urinary retention with morphine?

Back 15

increased ADH by central mechanism

Front 16

cardiovascular effects of morphine?

Back 16

arteriolar and venous dilation may produce postural hypotension

Front 17

GI effects of morphine?

Back 17

constipative and antidiarrheal

Front 18

morphine administration?

Back 18

parenterally

Front 19

lipid solubility of morphine and consequence?

Back 19

low lipid solubility leading to little entry to brain

Front 20

metabolism and excretion of morphine?

Back 20

glucuronide conjunction to be excreted in urine

Front 21

mechanism of tolerance to opioid?

Back 21

pharmacodynamic due to downregulation of opioid receptors and uncoupling of G protein receptor;
NOT due to an increase in metabolism

Front 22

symptoms of opioid withdrawal?

Back 22

diarrhea, vomiting, chills, fever, lacrimation, rhinorrhea, tremor, kicking movements of legs

Front 23

used to decrease opioid withdrawal symptoms?

Back 23

clonidine

Front 24

general uses of opioid analgesics?

Back 24

analgesia
antitussive
antidiarrheal

Front 25

naturally occuring opioids?

Back 25

morphine
codeine

Front 26

partial synthetic opioids?

Back 26

heroin
naloxone

Front 27

synthetic opioids?

Back 27

levorphanol
meperidine
methadone

Front 28

codeine?

Back 28

orally active but not as potent as morphine;
antitussant;
analgesic with aspirine or acetaminophen

Front 29

heroin?

Back 29

high lipid solubility;
not used clinically

Front 30

oxycodone?

Back 30

same effects and potency as morphine but higher oral activity

Front 31

hydromorphone (dilaudid)?

Back 31

same effects as morphin but higher oral activity and 10x potency

Front 32

apomorphine?

Back 32

little analgesic activity;
causes respiratory depression;
DA agonist activity;
induce vomiting

Front 33

dextromethorphan?

Back 33

antitussant;
little analgesic or addiction activity

Front 34

meperidine (demerol)?

Back 34

synthetic opioid;
shorter duration of action, orally active;
used for women in labor

Front 35

fentanyl (sublimaze)?

Back 35

synthetic opioid;
80x potency;
redistribution is major means of termination

Front 36

how is action of fentanyl terminated?

Back 36

redistribution

Front 37

fentanyl therapeutic uses?

Back 37

anesthetic induction;
sole anesthetic for cardiac surgeries;
neuroleptic state (combined with droperidol)

Front 38

similar drugs to fentanyl?

Back 38

alfentanil
sufentanil

Front 39

alfentanil?

Back 39

similar to fentanyl

Front 40

sufentanil (sufenta)?

Back 40

similar to fentanyl

Front 41

methadone (dolophine)?

Back 41

synthetic opioid;
long half life of 15 hours

Front 42

uses of methadone?

Back 42

synthetic opioid;
chronic pain;
methadone maintenance for heroin addict

Front 43

LAAM (orlaam)?

Back 43

synthetic opioid;
long-acting congener of methadone;
mused for maintenance treatment of heroin addiction

Front 44

propoxyphene (darvon)?

Back 44

synthetic opioid;
same indications and spectrum of action as codeine

Front 45

diphenoxylate (lomotil)?

Back 45

synthetic opioid;
oral administration for diarrhea;
high abuse potential (combined with atropine)

Front 46

loperamide (imodium)?

Back 46

synthetic opioid;
oral administration for diarrhea

Front 47

symptoms of opioid overdose?

Back 47

coma
depressed respiration
pinpoint pupils

Front 48

treatment for opioid overdose?

Back 48

administer naloxone
restore respiration
watch patient

Front 49

important in restoring respiration?

Back 49

not 100% O2 or remove hypoxic stimulus to breath

Front 50

opioid interactions?

Back 50

additive or synergistic with sedative-hypnotics, ethanol, MAO-Is, TCAs, tranquilizers;
neuroleptic analgesia

Front 51

pure opioid antagonists?

Back 51

naloxone
naltrexone

Front 52

naloxone (narcan)?

Back 52

pure competitive opioid antagonist;
drug of choice for opioid overdose

Front 53

naltrexone (trexan)?

Back 53

pure competitive opioid antagonist;
24 hour duration of action

Front 54

uses of pure antagonists?

Back 54

treatment of opioid overdose;
diagnose addiction;
treatment of compulsive use

Front 55

opioid agonist-antagonists?

Back 55

pentazocine
nalbuphine
butorphanol
buprenorphine

Front 56

pentazocine (talwin)?

Back 56

weak mu antagonist;
kappa agonist;
sigma agonist;
analgesic for mild to moderate pain

Front 57

consequence of pentazocine agonist activity at kappa and sigma receptors?

Back 57

spinal analgesia as effective as morphine;
limited respiratory depression;
dysphoria and hallucinations

Front 58

nalbuphine (nubain)?

Back 58

mu antagonist;
kappa agonist;
analgesic for moderate to severe pain

Front 59

butorphanol (stadol)?

Back 59

mu antagonist;
kappa agonist;
analgesic for moderate to severe pain

Front 60

consequence of nalbuphine and butorphanol kappa agonist effects?

Back 60

analgesia with limited respiratory depression;
low incidence of psychotomimetic effects

Front 61

buprenorphine (buprenex)?

Back 61

partial mu agonist;
kappa antagonist;
analgesic for moderate to severe pain

Front 62

consequence of partial mu agonist activity of buprenorphine?

Back 62

analgesic;
respiratory depression;
euphoria;
miosis;
mild morphine type abstinence syndrome;
antagonist in combo with stronger agonist activity