PDA opoids

Question 1

What is analgesia?

Answer 1

a state in which no pain is felt despite the presence of normally painful stimuli

Question 2

What is teh ascending pain pathway?

Answer 2

A-delta fiber mediate sharp localized pain to dorsal horn of spinal cord
C fibers mediate dull diffuse aching pathway
activate secondary nerons that form spinothalamic tract

Question 3

What is the descending pain pathway?

Answer 3

originate in periaqueductal gray region of midbrain and nuclei of rostro-ventral medulla
descend in dorsolateral funiculus to dorsal horn
releaase norepi and serotonin

Question 4

What are the mu receptor endogenous ligands opioid?

Answer 4

Endogenous ligands: enkephalins, Beta-endorphin

Question 5

What are the endogenous ligands of kappa receptor opioid?

Answer 5

dynorphins

Question 6

What ar ehte delta recepor for opioid endogenous ligands?

Answer 6

enkephalins, beta-endorphin

Question 7

What is the mechanism of action of morphine?

Answer 7

binds receptor that is a Gi
decreases camp
opens potassium channel
decrease release of neurotransmitter
calcium entry block leads to decreased release

Question 8

What are the localization of opoids?

Answer 8

periaquaductal gray, dorsal horns of spinal cord, medulla and hypothalamus. Gi system and heart

Question 9

What receptors in limbic area for opioid receptors are responsible for drug dependence?

Answer 9

Mu and delta receptors in limbic areas may be involved in drug dependence

Question 10

What opioid receptor in limbic structure hat may be involved in dysphoric actions?

Answer 10

kappa agents and kappa receptors

Question 11

What si teh onset of action of opioids determined by?

Answer 11

lipophilicity

Question 12

What are opioids metabolized by?

Answer 12

metabolized by liver, to more polar and less active metabolites

Question 13

What is the chemical structure of heroin and what is it converted to?

Answer 13

diacetylmorphine converted to monoacetyl-morphine

Question 14

What are the effects of opioids?

Answer 14

Analgesia-full agonists
cough suppression
antidiarrheal effect
euphoria
sedation
respiratory depression
nausea
endocrine effects
pupillary constriction-miosis

Question 15

What opioid is not a full agonist for analgesia?

Answer 15

codeine and propoxyphene

Question 16

What opioids suppress cough and not necessarily by opioid receptor but by brainstem cough receptors?

Answer 16

codeine and dextromethorphan

Question 17

What are the endocrine effects of opioids?

Answer 17

Decreased LH release-Mu effect
Increased ADH secretion-mu
decrease ADH- Kappa

Question 18

What opioids effects don’t cause tolerance?

Answer 18

pupillary constriction

Constipation

Question 19

What is the structure of Heroin and basic information?

Answer 19

diacetyl morphine
more lipophilic than morphine
high abuse potential

Question 20

Codeine and Oxycodone information about structure and basic info?

Answer 20

mild to moderate paiin
morphine like efficacy not achievable at codeine
some metabolized to morphine
oxycodone is more efficacious and useful in moderate to severe pain
oxycodone is availabe as a sustaine release oral prep
major abuse problem

Question 21

What is basic infor about meperidine?

Answer 21

phenylpiperidine
shorter duration of annalgesia than morphine
forms toxic metabolite that can accumulate
interaction with MAO inhibitor

Question 22

What is basic information behind methadone and structure?

Answer 22

phenylheptylamine
mu agonist
equipotent with morphine; has good oral availability
longer duration of action
used in tx of opioid abuse and chronic pain

Question 23

What is basic structure and function fentanyl?

Answer 23

meperidine
mu agonist
100 times as potent as morphine
short acting 1 to 1.5 hours
available injectable and transdermal patches

Question 24

What type of pain is codeine for?

Answer 24

mild to moderate pain

morphine-like efficacy is not achievable at any dose

Question 25

Hydrocodone is for what type of pain?

Answer 25

moderate to moderate sever pain, usually combined with NSAID

Question 26

What type of pain is oxycodone used for?

Answer 26

moderate to severe pain-major abuse problem

Question 27

How potent is hydromorphone?

Answer 27

(dilaudid) 2-3 times as potent as morphine

Question 28

What type of agonist is nalbuphine?

Answer 28

mu antagonist and kappa agonist

Question 29

What is nalbuphine used for?

Answer 29

similar in efficacy and potency to morphine
little euphoria and low abuse potential
precipitate withdrawal in opiate dependent patients

Question 30

What is burprenorphine used for?

Answer 30

partial mu-agonist; 25 to 50times as potent as morphine
used to tx moderate to severe pain
buprenorphine+naloxone=suboxone is used to tx opioid dependence

Question 31

What is naloxone?

Answer 31

an antagonist of mu receptors, less for kappa and delta
short duration of action
used to tx opioid overdoses

Question 32

What is naltrexone used for?

Answer 32

orally active long half life; used in tx of alcoholism and opiate addiction

Question 33

What is dextromethorphan used for?

Answer 33

D-isomer of levorphanol which is a potent mu agonist; NMDA receptor antagonist. Cough suppressant

Question 34

What is tramadol used for?

Answer 34

weak mu agonist activit and also blcoks NE and serotonin uptake. Used for mild to moderate pain. Available for oral use including sustained release prep

Question 35

What are tolerances for opioids?

Answer 35

rapid-nausea and vomitting
more gradual-analgesia, euphoria, respiratoyr depression, endocrine
little-miosis and constipation