Pharm - Opioid Analgesics And Antag

Front 1

Opioid,

Back 1

morphine like activity; reduce pain without loss of consciousness
tolerance and physical dependance

Front 2

Opiates

Back 2

morphine like activity derived from opium

Front 3

Endogenous peptides
beta-endorphins

Back 3

proopiomelanocortin (POMC)
mu receptors

Front 4

Endogenous peptides
proenkephalin

Back 4

contains met and leu-enkephalin
delta receptor

Front 5

Endogenous peptides
prodynorphin

Back 5

dynorphin A&B
kappa receptors

Front 6

Opioids
Mech - global

Back 6

interact with mu kappa and delta receptors
mimic local peptides
in CNS and periph tissues

Front 7

Opioids
secondary messengers

Back 7

inhibitory G proteins
inhibit adenylyl cyclase
dec cAMP
dec protein phosphorylation

Front 8

Opioids
Mech - channels
2

Back 8

close voltage gated Ca channels
on PREJXNAL nerve terminals to inhibit NT release (AcH, etc)
open K channels to hyperpolarize and inhibit postjxnal neurons

Front 9

Spinal cord action

Back 9

directly inhibit pain transmission
dorsal horn; thalamus

Front 10

descending CNS inhibitory pathway

Back 10

inhibiting inhibitory neurons
descending processes to spoing cord

Front 11

opioids decrese pain in

Back 11

cortex, amygdala, hippocampus
thalamus
resp center, vasomotor, CTZ, cough, GI

Front 12

Opoids
Indications
6

Back 12

Analgesia
Diarrhea
Dypnea
Cough
Anesthesia
Physical Dependance

Front 13

Opoids
Indications
Analgesia

Back 13

pre and postoperative
venodilation dec preload and relieve pain post MI
continuous pain - visceral damage

Front 14

Opoids
Indications
Diarrhea

Back 14

Codeine, diphenoxylate, loperamide
less abuse or resp depression

Front 15

Opoids
Indications
Dypnea

Back 15

acute pul edema secondary to LHF
Morphine dec. TPR; dec. respiration, relief from anxiety

Front 16

Opoids
Indications
Cough

Back 16

Codine and dextromethorphan
suppress cough reflex

Front 17

Opoids
Indications
Anesthesia

Back 17

preanesthetic mediation
fentanyl - short duration

Front 18

Opoids
Indications
Physical Dependance

Back 18

Methadone, and buprenorphine
withdrawal less severe

Front 19

Opoids
Adverse Effects
CNS

Back 19

Resp depression - direct inhib of resp center
sedation/drwosiness
nausea/vomiting - trigger CTZ

Front 20

Opoids
Contraindications

Back 20

dec resp reserve - COPD
Head injuries - inc ICP b.c of vasodilitation
preggers - neonatal resp depression

Front 21

Opoids
Tolerance

Back 21

direct neuronal effect
cross tolerance
hyperalgesia

Front 22

Physical Dependance

Back 22

abstinent withdrawal
long term opiod admin stopped
behavioral - drive to get it
physical - lacrimation/rhinorrhea, piloerection, diarrheat, flushign, muscle spasms

Front 23

Precipitated withdrawal

Back 23

administration of opioid antagonist (naloxone)

Front 24

Adverse Effects
Miosis

Back 24

Edinger west phal nucleus of oculomotor nerve constricts pupils - AcH activates
EXCEPT - Meperidine mydriasis - anti ach activity

Front 25

Adverse Effects
CV

Back 25

postural hypotension
opioids inhibit vasomoter center; periph vasodilitation

Front 26

Adverse Effects
Gi, Kidney, Gall Bladder
cause

Back 26

increase tone of SM; therefore dec. coordinated contractility

Front 27

Adverse Effects
Gi, Kidney, Gall Bladder
Constipation

Back 27

1. dec coordinated contractility of GI
2. inc anal sphincter tone
3. inattention to defication reflex

Front 28

Adverse Effects
Gi, Kidney, Gall Bladder
Urine Retention and Pain

Back 28

1. dec renal plasma flow
2. dec coordinated contractility
3. inc urethral sphinceter tone
4. inattention to urinary reflex

Front 29

Adverse Effects
Gi, Kidney, Gall Bladder
Biliary spasm - pain

Back 29

inc intrabiliary duct p by inc tone of SM of biliary tract and sphincter of Oddi
paradoxical in stones

Front 30

Adverse Effects
Puritis

Back 30

Hist release; flushing and sweating

Front 31

Opioids
Pharmaco

Back 31

absorbed in GI;
morphine sig. first pass metab
morphine 6-glucoronide has analgesic activity
morphine-3-glucoronide has neuroexcitatory activity

Front 32

Drug interactions

Back 32

cause resp depression - sedative hypnotics, antidepressant drugs
SSRI or MAOI - Meperidine - serotonin syndrome - hyperrexia

Front 33

Opioid Agonist
Meperidine
Features

Back 33

shorter duration than morphine
less constipation, vomiting, resp depression
obsterics
no effect on cough

Front 34

Opioid Agonist
Meperidine
Overdose

Back 34

CNS excitation (tremors), seizures
weak antiAcH activity; mydriasis

Front 35

Opioid Agonist
Meperidine
Interactions
MAO inhibitors

Back 35

restlessness, excitement, fever, seizures

Front 36

Opioid Agonist
Fetanyl
features

Back 36

more rapid onset and shorter duration
100X more potent, IV only

Front 37

Opioid Agonist
Fetanyl
Use

Back 37

preanethetic/labor

Front 38

Opioid Agonist
Fetanyl
balanced anesthesia

Back 38

supplement with NO and halothane

Front 39

Opioid Agonist
Fetanyl
Side E

Back 39

truncal rigidity; interfere with ventilation
caused by rapid admin

Front 40

Opioid Agonist
Fetanyl
transdermal patch

Back 40

breakthrough pain in cancer, etc

Front 41

Opioid Agonist
Fetanyl
CV Surgery

Back 41

minimal cardiac depression so can use

Front 42

Opioid Agonist
Methadone
Use

Back 42

oral
maintenance therapy. long duration of action; less severe withdrawal than shorter opioids

Front 43

Opioid Agonist
Hydromorphone, Heroin

Back 43

more lipid soluble

Front 44

Weak Opioid Agonist
Codine
Use

Back 44

Moderate pain
antitussive
good bioavailability - 10% converted to morphine

Front 45

Weak Opioid Agonist
Codine
Overdose

Back 45

seizures

Front 46

Weak Opioid Agonist
Codine
Combination therapy

Back 46

aspirin or acetaminophen, Vicoden
oxycodone + acetaminophen Percocet

Front 47

Weak Opioid Agonist
Codine
Oxycodone

Back 47

oral sustained release; abused

Front 48

Weak Opioid Agonist
Propoxyphene

Back 48

effective as aspirin
high doses cause resp dep; hall; seizures

Front 49

Opioid antidiarrheal agents
Diphenoxylate
Features

Back 49

limits absorption in GI tract
minimal dependance
IV
used with atropoine

Front 50

Opioid antidiarrheal agents
Loperamide
Features

Back 50

limited CNS penetration
minimal dependance
with atropine to dec abuse
IV

Front 51

Mixed Agonists-Antagonists/ Partial Agonists
Buprenorphine

Back 51

partial agonist at mu receptor

Front 52

Mixed Agonists-Antagonists/ Partial Agonists
Pentazocine

Back 52

agonist at k rec; weak antag at mu

Front 53

Mixed Agonists-Antagonists/ Partial Agonists
Pentazocine
Buprenorphine
Features

Back 53

moder at pain - ceiling to analgesic activity
less dependence

Front 54

Mixed Agonists-Antagonists/ Partial Agonists
Pentazocine
Buprenorphine
Use

Back 54

precipitate withdrawal (except for resp depression, cannot reverse
heroin detox

Front 55

Mixed Agonists-Antagonists/ Partial Agonists
Pentazocine
Buprenorphine
overdose

Back 55

bind strongly to receptors so resistant to naloxone reversal

Front 56

Mixed Agonists-Antagonists/ Partial Agonists
Pentazocine
Buprenorphine
Side E

Back 56

dysphoria, hall, depersonalization

Front 57

Tramadol
Use and Mech

Back 57

moderate pain
neuropathic pain
mu rec
weakly enhances serotonin and NE by blocking transporter for reuptake

Front 58

Tramadol
Effect

Back 58

less resp than morphine

Front 59

Tramadol
Side E

Back 59

inc risk of seizures; epilepsy
not with MAOI

Front 60

Tramadol
Contraindications

Back 60

epilepsy; not be used in MOAIs
reversed by naloxone

Front 61

Opioid Antagonists
Naloxone
Naltrexone
Methylnaltrexone
Use

Back 61

precipitate opioid withdrawal

Front 62

Opioid Antagonists
Naloxone
Use

Back 62

IV b.c poor efficacy
acute opioid overdose
short duration - can be recurrence of overdose symptoms

Front 63

Opioid Antagonists
Naltrexone

Back 63

longer duration
orally but does have large first pass metab
reduce alcohol craving

Front 64

Opioid Antagonists
Methylnaltrexone

Back 64

constipation

Front 65

non-opioid antitussive agent
Dextromethorphan

Back 65

antitussive! less constipation than codeine
no analgesic or dependence - some abuse