Hupka Opioid Analgesics And Antagonists

Front 1

What are the chacteristics of opiod receptors?

Back 1

Specific binding sites associated with IINHIBITORY G PROTEIN

Front 2

What are the varients of opiod receptors?

Back 2

Mu(predominating varient),
Kappa,
and Delta

Front 3

What are the main effects for the MU receptor?

Back 3

Respiratory depression
Euphoria
Physical Dependence
and of course, analgesia

Front 4

What are the main effects for the DELTA receptor?

Back 4

Respiratory depression and
reduced GI motility
and of course, analgesia

Front 5

What are the main effects for the KAPPA receptor?

Back 5

Dysphoria
and of course, analgesia

Front 6

Of all the opiod effects, what is the most deadly?

Back 6

Respiratory depression

Front 7

Describe the first mechanisms by which opiods function?

Back 7

Opiod receptors are linked to G inhibitory proteins. Activation of Gi leads to decrerased cAMP and closure of the voltage gated Ca channels on the PRESYNAPTIC nerve, thereby decreasing neurotransmitter release.
and op

Front 8

Describe the second mechanism by which opiods function?

Back 8

Opening of K channels causing hyperpolerization (inhibition) of postsynaptic neurons.

Front 9

What is another name for opium derivates?

Back 9

phenanthrenes

Front 10

Name the opium derivates (7)

Back 10

C.H.M. H.O.H.O.
Morphine, Codine
Heroin
Hydromorphone, Oxymorphone
Hydrocodone, Oxycodone

Front 11

If a drug ends in -fentanil, what is it?

Back 11

A synthetic opiod derived from Meperidine

Front 12

What are the two synthetic opiods?

Back 12

Meperidine (demerol)
Methadone (dolophine)

Front 13

What drug is a partial agonist of the Mu receptor, but an ANTAGONIST of both the KAPPA and DELTA receptor?

Back 13

Buprenorphine

Front 14

What are the CNS effects of Morphine? 8
***O***

Back 14

Behavorial Effects (dysphoria->euphoria)
Sedation
Emetic (directly stimulate CTZ)
Antitussive (block medullary cough center)
Resp. Depression (decrease CO2 respiratory center sensitivity)
Meiosis (pin point pupils)
Muscle Rgidity and Convulsion

Front 15

Of Codine, Morphine, Meperidine, and Methadone, what has the highest antitussive effect?
***T***

Back 15

Methadone>codine>morphine>meperidine

Front 16

If a pt has resperitaory depression due to opiods, would you give them pure O2?

Back 16

NO, this will decrease their CO2 levels in an allready desinsitized respiratory CO2 center, thus you will halt their respiratory drive

Front 17

What are the peripheral effects of morphine?
***O***

Back 17

GI tract(/\tone, \/peristalsis) constipation
Biliary Tract (/\tone)
/\intercranial pressure
Histamine release->Bronchoconstriction, itching, sweating, redness of eyes
Bradycardia, urination

Front 18

What is the main mechanism of morphine metabolism?
***o***

Back 18

Glucoronide conjugation in the liver and intestines (morphine-6-glucuronide), making it water soluable, pee it out

Front 19

What is the issue with a fetus and morphine?
***O***

Back 19

Morphine corsses the placenta and crosses the underdeveloped BBB in the fetus, with a potential for addiction and harm

Front 20

What is the significance of morphine-6-glucoronide?

Back 20

It is an active analgesic metabolite that is more potent than morphine. Seen when taken via oral route or in renal failure

Front 21

What is the classic triad seen with morphine toxicity?

Back 21

COMA
PINPOINT PUPILS
RESPIRATORY DEPRESSION

Front 22

What drugs will interact negatively with morphine and enhance its CNS depressant effects?

Back 22

Phenothiazines
MAOI
Tricyclic antidepressants

Front 23

What drug may enhance the morphine effect?

Back 23

Ampthetamines

Front 24

What are the primary contraindications of opiod use? (8)

Back 24

Bronchial Asthma, Emphysemea, Liver Damage
Head Injuries, Acute Alcohol use, Previous Dependence
Convulsive Disorders, Abdominal pain of unknown origin

Front 25

What would you give to fix an opiod overdose?

Back 25

IV Naloxone (opiod antagonist)

Front 26

What is the primary casue of death in an opiod overdose?

Back 26

Respiratory supression

Front 27

How does codine become effective?

Back 27

It is METABOLIZED into morphine by CYP2d6

Front 28

Why is methadone used to treat Opiod addicts?

Back 28

Methadone has an extremely long half life, thus it is essentially weening the body off of it as it is slowly metabolized, unlike the rapidly metabolized opioids.

Front 29

What is the receptor that Methadone primarily targets?

Back 29

MU receptor

Front 30

What does tolerance of morphine effect, the Depressant or the Stimulating actions?

Back 30

Tolerance occurs to the depresant actions of morphine

Front 31

Discuss tolerance, physical dependence, and withdrawl syndrome.

Back 31

They are all directly related

Front 32

How do you estimate the level of tolerance?

Back 32

Measuring the amount of drug needed to produce drowsiness

Front 33

What three things are physical dependence related to?

Back 33

Amount, frequency, and duration of Drug use.

Front 34

For opiods, what effects will you likely never develop tolerance for?

Back 34

MIOSIS
CONSTIPATION
convulsions
antagonistic actions

Front 35

What one effect of opiods will develop only a moderate degree of tolerance?

Back 35

Bradycardia

Front 36

What receptor is primarily associated with analgesia?

Back 36

Mu, Delta, Kappa

Front 37

What receptor is primarily associated with euphoria?

Back 37

Mu

Front 38

What receptor is primarily associated with Miosis?

Back 38

Mu (and some kappa)

Front 39

What receptor is primarily associated with dysphoria?

Back 39

KAPPA

Front 40

What receptor is primarily associated with physical dependence?

Back 40

Mu

Front 41

What receptor is primarily associated with respiratory depression?

Back 41

MU

Front 42

What is the action on the Mu receptor by Morphine?

Back 42

Agonist

Front 43

What is the action on the Mu receptor by Pentazocine?

Back 43

Partial Agonist
Much less dependence then other opiods, and slightly less respiratory depression

Front 44

What is the action on the Mu receptor by Naloxone/Naltrexone?

Back 44

ANTAGONIST

Front 45

What is the difference between Naloxone/Naltrexone?

Back 45

Naloxone: Parenteral, HL 1 hour

Naltrexone: oral or injection, LONG LASTING (month if injection)

Front 46

Compare the withdrawl of mathadone vs naltrexone?

Back 46

Methadone is an agonist, and it is slow, so very mild withdrawl

Naltrexone is an ANTAGONIST, thus a SHARP and bitter withdrawl

Front 47

Which opioid analgesic is most likely to produce seratonin syndrome if administered with a MAO inhibitor?

Back 47

Meperidine (drug similiar to morphione except it also has ATROPINE LIKE TOXICITIES

Front 48

What is fentanyl?

Back 48

A merperidine congener.
Remember, merperidine is a drug similiar to morphione except it also has ATROPINE LIKE TOXICITIES

Front 49

What are the advantages of fentanyl over morphine?

Back 49

Fentanyl is 100 times more potent than morphine, and it has an extremely quick onset. Thus it should be used for breakthrough pain

Front 50

What group is Remifentanil from?
What are its advantages as a drug?

Back 50

Fentanyl group
EXTREMELY FAST halflife, must have a continuous IV.
Very useful for infusion anesthesia

Front 51

What is the main difference between opiate withdrawl and CNS depressant withdrawl?

Back 51

CNS depressant withdrawl (barbituates/alcohol) can cause DEATH!!! Opiates will not kill you

Front 52

Of morphine, meperidine, or codine, which is the least likely to cause constipation?

Back 52

Meperidine

Front 53

Of morphine, meperidine, or codine, which is the least likely to supress a cough?

Back 53

Meperidine

Front 54

What is a negative metabolite of morphine? And what can that metabolite cause?

Back 54

Morphine-3-glucuronide
It lacks analgesic effect and it can cause DYSPHORIC side effects or SEIZURES

Front 55

What is meperidine again?

Back 55

Morphine like drug, faster acting, shorter duration, and less potent than morphine, NO ANTITUSSIVE activity, LESS CONSTIPATION, LESS RESP Depression, LESS ADDICTIVE, may cause seizures, but less shivering

Front 56

What are the major negative sideeffects of meperidine again?

Back 56

ATROPINE LIKE TOXICITY
SEROTONIN SYNDROME when taking a MAO inhibitor

Front 57

What does Methylnaltrexone do and how does it work?

Back 57

Reverses opiod induced constipation but NOT analgesia because it DOES NOT enter the CNS!!!!!.
It is used for patients taking chronic opioids.

Front 58

What does Alvimopan do and how does it work?

Back 58

Used to treat post op ileus, given before and after bowel resection. (Stays in GI tract)