Opioid Analgesics And Antagonists Block 4

Front 1

List two types of analgesics

Back 1

(1) narcotic analgesics -- opiods - have CNS effect

(2) non-narcotic analgesics -- NSAIDs - Do Not have CNS effect

Front 2

Describe two components of pain

Back 2

(1) physcial: perception, discrimination of pain

(2) psychological: reaction to pain

Front 3

How do opioids change the threshold of pain?

Back 3

Opiods raise the threshold for pain perception and alter the affective response. Opioids relieve both aspects of pain.

Front 4

List 4 sites of opiod action

Back 4

(1) thalamus
(2) limbic system
(3) brain stem
(4) spinal cord

Front 5

Describe opiod action at the spinal cord.

Back 5

Epidural opiod analgesia is segmental, rapid in onset, long lasting, produces few side effects, and no physical dependence.

Front 6

The 3 opioid receptors plus the other one.

Back 6

Mu, Kappa, Delta
Sigma - kind of is.

Front 7

Compare and contrast naloxone and naltrexone.

Back 7

Both are pure, competitive opiod antagonists.

Naloxone has a shorter duration of action (1-4h) compared to naltrexone (24h). Given for opioid overdose

Naloxone is the drug of choice in treating opiod OD.
Naltrexone is given to drug users so if they take street drugs they won't have euphoria.

Uses of pure antagonists: treatment of opioid overdose, diagnose addiction (pt will have withdrawal symptoms), treatment of compulsive use

Front 8

Morphine

Back 8

Prototype of opioids
Uses:Analgesic, treatment of cough (antitussant - suppress the cough reflex) and Antidiarrheal (causes constipation!)
-Usually given by IV

Front 9

Besides the 3 therapeutic uses of morphine, list its other effects on the body. (Essentially its side effects

Back 9

(1) mood changes - Euphoria, Mental Clouding (drowsy, lethargic, can't think)
(2) nausea & vomiting - opiods stimulate the chemoreceptor trigger zone (CTZ)
(3) respiratory depression - morphine causes decreased response of the brain stem respiratory neurons to CO2 --> decreased breathing. Also caused bronchoconstriction.
(4) miosis - constriction of pupil
(5) urinary retention - increased ADH release --> water retention
(6) dec LSH, FH release - so decreased estrogen in females and testosterone in males
(7) postural/orthostatic hypotension - due to a/v dilation due to histamine release and depressed vasomotor and adrenergic tone
8) GI effects - constipation!!
9) antitussant - inhibits cough reflex

Front 10

Describe pharmacokinetics of morphine.

-absorption
-solubility
-metabolism
-excretion

Back 10

Morphine

--variable oral absorption so administered parenterally
--low solubility so little enters brain

--glucuronide conjugation is major metabolic pathway

--excreted as glucuronide conjugate in urine

Front 11

TRUE or FALSE

All tolerance to opiods is considered a metabolic tolerance.

Back 11

FALSE

All tolerance to opiods is pharmacodynamic, meaning that there is decreased opiod receptors from down-regulation.

Front 12

Describe the onset and symptoms of opiod withdrawal.

Is it life threatening?
What drug can be used to decrease these symptoms?

Back 12

Morphine withdrawl symptoms appear 10hr after last dose and will peak between 36-72hr.
Symptoms include vomiting, diarrhea, chills, fever, tremor, and kicking of legs, increased tears (watery eyes)

It is not life threatening.
Clonidine (alpha2 agonist) can decrease symptoms.

Front 13

Opioids

Back 13

Uses: Analgesia - most can relieve all types of pain and are reserved for moderate to severe pain, Antitussive (low doses), Antidiarrheal
Sources:
-naturally occuring-from opium poppy (morphine, codeine)
-Partial synthetic (heroin, naloxone)
-Synthetic (levorphanol,merperidine, methadone)

Front 14

Codeine

Back 14

Naturally occuring opioid
-orally active but only 1/10th as analgesic as morphine.
-Used as antitussant and as analgesic in combination with aspirin or acetminophen

Front 15

Heroin (diacetylmorphine)

Back 15

Opioid
-Parenteral absorption. (IV -drug users)
-crosses BBB due to high lipid-solubility
-Not used clinically in US

Front 16

Oxycodone

Back 16

Opioid
-same effects and potency as morphine.
-But higher oral activity (can take as pills)

Front 17

Hydromorphone (Dilaudid)

Back 17

Opioid
-same effects as morphine but higher oral acitivity and 10X more potent.

Front 18

Apomorphine

Back 18

Opioid
-has little analgesic activity
-Causes respiratory depression
-Used to induce vomiting -direct action on CTZ.
-used in pts that took toxins, poisons, etc

Front 19

Dextromethorphan

Back 19

Opioid
-very little analgesic or addiction activity.
-Used as antitussant
-less drowsiness or GI effects than codeine

Front 20

Meperidine

Back 20

Synthetic Opioid
-Shorter duration of action than morphine
-used for shorter analgesia
-Orally active
-1/10th potentcy of morphine
-Used for women in labor

Front 21

Fentanyl

Back 21

Synthetic Opioid
-orally active but IV in anesthesia
-80 times potency of morphine
-Short duration of action (very lipid soluble so redistribution is major means of termination of action)
-Uses: Anesthetic induction, sole anesthetic for cardiac surgeries, Neuroleptic state.
-Neuroleptic state - when combined with droperidol = Innovar --> relaxation of the muscle. Used for outpatient surgeries
-Alfentanil and Sufentanil are similar in action and potency to Fentanyl

Front 22

Methadone

Back 22

Synthetic Opioid
-orally active
-same actions/potency of morphine
-Long duration of action with half-life of 15 hours
-Uses: Chronic pain, methadone maintenance

Front 23

LAAM (L-alpha-acetyl-methadol)

Back 23

Synthetic Opioid
-long-acting twin of methadone.
-Used for maintenance treatment of heroin addiction.
-Orally active

Front 24

Propoxyphene

Back 24

Synthetic Opioid
-1/10th potency of morphine.
-used as antitussant or analgesic in combination with aspirin or acetaminophen (like Codeine)
-Orally active

Front 25

Diphenoxylate (Lomotil)

Back 25

Synthetic Opioid
-Only Oral
-Treats diarrhea
-Has abuse potential so it is combined with atropine in preparation of Lomotil.

Front 26

Loperamide (Imodium)

Back 26

Synthetic Opioid
-OTC drug for diarrhea
-As effective as Diphenoxylate in controlling chronic diarrhea but has less abuse potential.
-Poorly absorbed after oral administration and acts on intestinal musculature to inhibit motility.

Front 27

Opioid Overdose

Back 27

Classic triad of symptoms: Coma, Depressed respiration, pinpoint pupils!!!!!
Overdose Treatment:
-Restore respiration (O2 but not pure O2 - need some CO2)
-Administer Naloxone
-Watch pt because naloxone half life is much shorter than opioids

Front 28

List the specific natural or partial-synthetic opiod that fits the following..

--higher oral activity vs. morphine but same effects & potency

--higher oral activity & effects as morphine but higher potency

--higher oral activity vs. morphine but has 1/10 the potency

Back 28

(1) higher oral activity + same effects + same potency = oxycodone

(2) higher oral activity + same effects + higher potency = hydromorphone

(3) higher oral activity + 1/10 potency = codeine

Front 29

List the specific synthetic opiod that fits the following...

--used for shorter analgesia & has 1/10 potency of morphine

--same potency as morphine but has long half-life of 15h

--sole anesthetic for cardiac surgeries

--treats heroin addiction

Back 29

(1) short analgesia + 1/10 potency = meperidine

(2) same potency + halflife of 15hr = methadone

(3) cardiac surgery anesthetic = fentanyl

(4) treats heroin addiction = LAAM

Front 30

This synthetic opiod is used as an IV anesthetic and has 80x the potency of morphine.

Back 30

Fentanyl

Front 31

Name the specific drug that fits the following description..

(1) combined with droperidol to produce neuroleptic state
(2) anti-diarrheal opiod that is combined with atropine
(3) drug of choice for opiod overdose
(4) sigma agonism produces dysphoria
(5) primarily an anti-tussant
(6) 10x more potent than morphine
(7) decreases opiod withdrawal symptoms

(8) analgesic for moderate - severe pain w/ kappa antagonism

Back 31

Name the specific drug that fits the following description..

(1) combined with droperidol to produce neuroleptic state = fentanyl

(2) anti-diarrheal opiod that is combined with atropine = diphenoxylate

(3) drug of choice for opiod overdose = naloxone

(4) sigma agonism produces dysphoria = pentazocine

(5) primarily an anti-tussant = dextromethorphan

(6) 10x more potent than morphine = hydromorphone

(7) decreases opiod withdrawal symptoms = clonidine

(8) analgesic for moderate - severe pain w/ kappa antagonism = buprenorphine

Front 32

Opioid Drug Interactions

Back 32

-Additive or synergistic effects to produce CNS and/or respiratory depression - can occur with: sedative-hypnotics, ethanol, monoamine oxidase inhibitors, tricyclic antidepressants and major tranquilizers

Front 33

Pentazocine

Back 33

Opioid agonist-antagonist
-Used as analgesic for mild to moderate pain
-Weak mu antagonist - blocks morphine analgesia, induces opioid withdrawal in physically dependent. Doesn't block morphine respiratory distress.

-Agonist at kappa and sigma receptors: effective analgesia w/ limited respiratory depression, mild abstinence syndrome, Psychotomimetic effects (dysphoria, hallucinations)
-All the kappa agonist effects are blocked by naloxone

Front 34

Nalbuphine and Butorphanol

Back 34

Opioid agonist-antagonist
-analgesic for moderate to severe pain
-Mu antagonists - blocks morphine analgesia, induces opioid withdrawal in physically dependent. Doesn't block morphine respiratory distress.

-Kappa agonist: effective analgesia with limited respiratory depression, low incidence of psychomimetic effects, mild abstinence syndrome
-antagonized by naloxone

Front 35

Buprenorphine

Back 35

Opioid Agonist-Antagonist
-Analgesic for moderate to severe pain
-partial agonist at mu receptors- effects it induces are slow in onset and long lasting : analgesic, respiratory depression, euphoria, miosis, mild abstinence syndrome

-Kappa antagonist
-Antagonized by Naloxone
-Potential replacement for methadone as maintenance in opioid drug abusers.