Opioid Pharm

Front 1

opiates

Back 1

agent derived from opium

Front 2

opioids

Back 2

all agents acting on morphine receptors, including antagonists

Front 3

opioid receptors

Back 3

1) mu
2) delta
3) kappa
4) sigma
5) epsilon

Front 4

opioid receptors all belong to what?

Back 4

G protein-coupled class of receptors

Front 5

What are endogenous ligands for opioid receptors?

Back 5

peptides (with varying affinities for each receptor type)

Front 6

opioid receptor activity

Back 6

1) inhibitory
2) decreasing intracellular cAMP
3) excitatory (very low doses)

Front 7

excitation of G stimulatory protein will cause what?

Back 7

1) increase activity of AC (adenylyl cyclase) and cAMP
2) increase protein kinase A
3) decrease K conductance
4) increase Ca conductance
5) increase action potential
6) increase transmitter release
7) excitatory effects

Front 8

inhibition of G(i)

Back 8

decrease the activity of adenylyl cyclase/cAMP

Front 9

inhibition of G(o)

Back 9

1) increase K conductance
2) decrease Ca conductance
3) decrease action potential
4) decrease transmitter release
5) inhibitory effects

Front 10

1) mu receptor

Back 10

1) analgesia
2) resp. depression
3) euphoria
4) miosis
5) physical dependence
6) decreased GI motility

Front 11

2) kappa receptor

Back 11

1) supraspinal analgesia
2) sedation
3) dysphoria (psychoses)

Front 12

3) delta receptor

Back 12

analgesia (spinal?)

Front 13

4) sigma receptor

Back 13

1) dysphoria
2) hallucinations

Front 14

1) mu receptor locations

Back 14

1) brainstem
2) medial thalamus
3) some in spinal cord

Front 15

2) kappa receptor locations

Back 15

1) mainly in the dorsal horn of the SC
2) some in the brainstem medullary reticular formation

Front 16

3) delta receptor locations

Back 16

mainly in the limbic system

Front 17

4) sigma receptor locations

Back 17

mainly in the hippocampus and amygdala of the limbic system

Front 18

endogenous opioids derived from what?

Back 18

precursor polypeptides

Front 19

polypeptides include:

Back 19

1) endorphines
2) dynorphines
3) enkephalins

Front 20

polypeptides deffer in chain length, but share:

Back 20

same first few AA's (61-65)

Front 21

Is endomorphine polypeptide?

Back 21

No, it is TETRApeptide
newly discovered
mu receptor selective

Front 22

endogenous opioids act as:

Back 22

1) NTM
2) neuromodulators
3) neurohormones
4) body's pain modulators

Front 23

~65% of opioid receptor homology exists among:

Back 23

1) mu
2) delta
3) kappa

Front 24

analgesia mediated via receptors located in the:

Back 24

1) dorsal horn of SC
2) periaqueductal gray matter
3) thalamus

Front 25

ventral brainstem receptors mediate effects on:

Back 25

1) coughing
2) vomiting
3) respiration
4) pupillary diameter

Front 26

hypothalamus controls what?

Back 26

neuroendocrine functions

Front 27

limbic system controls what?

Back 27

mood and behavioral effects

Front 28

peripheral mu receptors associated with:

Back 28

GI tract

Front 29

4 primary interaction of opioid ligands with opioid receptors:

Back 29

1) agonist
2) antagonist
3) partial agonist
4) mixed agonist/antagonist

Front 30

partial agonist

Back 30

binds to the receptor, but produces less than maximal response

Front 31

mixed agonist/antagonist

Back 31

binds to more than one type of opioid receptor, acting as an agonist at one, and an antagonist at others

Front 32

central opioid effects

Back 32

1) neuronal activity - <
2) analgesia
3) resp. depression
4) mood alteration
5) sedation
6) miosis
7) N/V
8) antitussive
9) endocrine (inhibits LHRH secretion)

Front 33

peripheral opioid effects

Back 33

1) histamine release
2) venous dilation
3) smooth muscle contraction
4) inhibition of Ach release

Front 34

common opioid uses:

Back 34

1) analgesia
2) pre-op sedation
3) anesthesia
4) epidural
5) diarrhea
6) cough suppression
7) opioid addiction withdrawal
8) opioid overdose (antagonist)

Front 35

major opioid SE

Back 35

1) resp. depression
2) N/V
3) hypothermia
4) constipation
5) histamine release
6) muscular rigidity

Front 36

muscular regidity is due to:

Back 36

inhibition of dopamine release in the striatum (Parkinson-like)

Front 37

ADME of the opioids

Back 37

1) most are well absorbed from GI tract
2) large 1st-pass metabolism (PO)
3) most distributes well
4) most cross placenta well

Front 38

excretion of the opioids mainly via:

Back 38

renal and biliary mechanisms of metabolized forms

Front 39

opioid agonists #1

Back 39

1) morphine (MS contin)
2) hydromorphone (Dilaudid)
3) Oxymorphone (Numorphan)
4) Codeine (Tylenol with Codeine)
5) Hydrocodone (Vicodine)
6) Oxycodone (Oxycontin)

Front 40

opioid agonists #2

Back 40

1) Heroin
2) Levorphanol (Levo-Deomoran)
3) Dextromethophan (Dimetane)
4) Meperidine (Demerol)
5) Methadone (Dolophine)
6) Propoxyphene (Darvon)

Front 41

opioid agonists #3

Back 41

1) Fentanyl (Sublimaze)
2) Sufentanil (Sufenta)
3) Alfentanil (Alfenta)

Front 42

morhine is natural alkaloid from:

Back 42

Papaver somniferum

Front 43

morphine acts primarily at:

Back 43

mu receptors (some kappa)

Front 44

morphine develop

Back 44

rapid tolerance

Front 45

heroin

Back 45

1) diacetylmorohine
2) semisynthetic
3) easily prepared from morphine
4) twice as potent as morphine
5) enters CNS rapidly, cause euphoria
6) not approved for clinical use

Front 46

Codeine

Back 46

1) 1/10 potency of morphine
2) little risk of addiction or resp. depression
3) partially converted to morphine in the body
4) potent antitussive

Front 47

Oxycodone (Oxycontin)

Back 47

1) twice as potent as morphine
2) high euphoric liability
3) 160 mg, extended release tab. - widely abused (Hillbilly Heroin)
4) many deaths linked to chewing the extended release form

Front 48

Levorphanol (Levo-Dromoran)

Back 48

1) very potent synthetic morphine analgesic congener (5X)
2) less constipating
3) longer lasting

Front 49

Dextromethorphan (Dimetane)

Back 49

1) a dextro-rotary isomer
2) no analgesic activity
3) effective antitussive

Front 50

Meperidine (Demerol)

Back 50

1) most widely used synthetic congener
2) 1/10 as potent as MS
3) shorter duration

Front 51

Why Meperidine frequently abused?

Back 51

because it does not cause miosis, hard to detect

Front 52

Meperidine are metabolized to :

Back 52

Normeperidine
1) CNS stimulant
2) potential Sz with renal pt

Front 53

Meperidine are contraindicated with:

Back 53

MAOI therapy

Front 54

Methadone (Dolophine)

Back 54

1) same potency as MS
2) less sedation than MS
3) longer duration of action (slower elimination)
4) used to counter withdrawal symptoms

Front 55

Propoxyphene (Darvon)

Back 55

1) structurally r/t MS
2) less than 1/10 as potent as MS
3) properties similar to other opioid

Front 56

concern for Propoxyohen (Darvon)

Back 56

questions have been raised concerning it's benefit in dose strengths found in most products

Front 57

Fentanyl (Sublimaze)

Back 57

1) chemically r/t meperidine
2) ~80X as potent as MS
3) continuous epidural
4) transdermal analgesia

Front 58

advantage of Fentanyl is:

Back 58

it's short half-life of redistribution (12.5 min)

Front 59

potency of Fentanyl

Back 59

1) Sufentanil (800X)
2) Fentanyl (80X)
2) Remifentanil (80X)
4) Alfentanil (20X)

Front 60

Remifentanil (Ultiva)

Back 60

selective mu-receptor agonist
(almost 100 % at mu-receptor)

Front 61

Remifentanil differs from other Fentamyl derivatives by having:

Back 61

an ester-linkage
1) short duration due to hydrolysis by non-spe. esterases
2) rapid recovery

Front 62

opioid antagonists act by blocking:

Back 62

mu receptors mainly (some kappa blockade)

Front 63

opioid antagonists block:

Back 63

1) analgesic
2) respiratory
3) euphoric
4) miosis
5) hypotension
6) smooth muscle actions of opioids
7) endogenous beta-endorphine
8) enkephalins

Front 64

clinical use of opioid antagonists:

Back 64

to reverse opioid-induced resp. depression and in the Tx of "addicts"

Front 65

Naltrexone (Trexan)
Nalmefene (Revex)

Back 65

1) similar with Narcan
2) longer half-life
3) given orally

Front 66

Buprenorphine (Buprenex)

Back 66

1) partial opioid agonist
2) shares structural components of Codeine and Naltrexone
3) binds to mu receptors, and elicits a weaker maximal response

Front 67

use of Buprenorphine

Back 67

1) less abuse potential
2) to conteract Heroin and Morphine addiction without causeing fullblown withdrawal symptoms

Front 68

1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)

Back 68

1)mixed opioid agonist/antagonists
2) mu receptor antagonists
3) kappa receptor weak agonists

Front 69

1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)
block:

Back 69

block mu receptor mediated analgesia and euphoria

Front 70

1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)
stimulate:

Back 70

kappa induced analgesia and sedation

Front 71

large doses of Nallorphine and Levallorphan may cause:

Back 71

dysphoria and hallucinations

Front 72

Pentazocine (Talwin) and Nalbuphine (Nubain)

Back 72

have similar actions, but are stronger kappa mediated analgesics

Front 73

Tramadol (Ultram)

Back 73

1) newer analgesices
2) structural similarities to opioids and NSAIDs
3) analgesic strength similar to Codeine-Acetaminophen agents

Front 74

Tramadol (Ultram) acts to block re-uptake of:

Back 74

serotonin and NE in central synapses, which then decreases pain info transmission in the brain

Front 75

both the parent compound and an active metabolite of Tramadol have:

Back 75

weak affinity for mu receptors, but their analgesic effect is not entirely reversed by Naloxone

Front 76

Tramadol (Ultram) can cause:

Back 76

1) dizziness
2) sedation
3) Sz
4) hallucinations

Front 77

neuroleptic anesthesia: Butyrophenone

Back 77

1) Droperidol - D2 blocker with antiemetic
2) Opioid (ex. Fentanyl)
3) N2O
4) used in dental office

Front 78

New therapeutic possibilities

Back 78

1) use of peptide-type receptor agonists for pain relief (designed to target specific receptor sub-types)
2) transplantation of adrenal medullary chromaffin cells into the spinal subarachnoid space

Front 79

transplantation of adrenal medullary chromaffin cells

Back 79

1) secrete opioid peptides
2) to provide long-term pain relief to chronic pain sufferes w/o exogenous opioid SE's