Opioid and Opioid Tolerance

Question 1

Agonist

Answer 1

† Strong agonist: morphine, hydromorphone, oxymorphone,

methadone, meperidine, fentanyl, levorphanol

Question 2

† Partial agonist

Answer 2

codeine, oxycodone, hydrocodone,

propoxyphrene

Question 3

Antagonist

Answer 3

† Nalorphine, naloxone, naltrexone

Question 4

Mixed agonist-antagonist

Answer 4

† Nalbuphine,burenorphine, butophenol, pentazocine

Question 5

… Short-acting

Answer 5

† All medication released at once
† Peaks and valleys effect
† Acute or break through pain

Question 6

… Long-acting examples

Answer 6

† MS Contin, Oxycontin, Kadian

Question 7

long acting do not

Answer 7

crush you will get a bolus and overdose

Question 8

long acting remember

Answer 8

† Small amounts released over time, providing more stable
blood level
† Good for chronic pain management

Question 9

new recommendations are calling for

Answer 9

short acting

Question 10

… Clinical Indications for opioids

Answer 10

† Acute and chronic pain, Acute pulmonary edema

Question 11

Route and Onset

Answer 11

† Parenteral 5-15 min
† Neuraxial 5 min
† Transdermal 16-24h
† Transmucosal (Oral and nasal) rapid-15min
† IM 60 min (erratic)
† PO 40-60min
† Intrathecal/epidural 5-15min

Question 12

Opioid MOA

Answer 12

Bind to receptors in CNS (Mu, Kappa, Delta)

Question 13

… Supraspinal (medulla and midbrain) - MOA

Answer 13

† Activation of post-synaptic neurons
† Inhibition of neurons involved in pain transmission by
increased influx of K+

Question 14

Spinal MOA/Activity

Answer 14

† Activation of presynaptic receptors
† Increased Ca++ influx and decreased release of
nociceptive neurotransmitters

Question 15

Absorption/Distribution/ Metabolism/Elmination

Answer 15

… Absorption
† First pass effect
… Distribution
† Lungs liver kidney spleen slow penetration of blood Lungs, liver, kidney, spleen, slow penetration of bloodbrain barrier; storage in fat, skeletal muscle
… Metabolism
… Elimination: renal

Question 16

MU 1

Answer 16

… Mu1: Supraspinal analgesia, euphoria, miosis, bradycardia,

urinary retention

Question 17

MU 2

Answer 17

Mu2: Spinal analgesia, respiratory depression, decreased GI

Question 18

KAPPA

Answer 18

Kappa: Supraspinal/spinal analgesia, sedation, miosis,

diuresis, hallucinations, respiratory depression

Question 19

DELTA

Answer 19

Delta: supraspinal analgesia, respiratory depression, urinary
retention

Question 20

Opioid Other effects

Answer 20

Other Effects: constipation, biliary colic, orthostatic

hypotension

Question 21

opioid tolerance is dependent on

Answer 21

Dependent on dose, dosing frequency, duration and

consistency of use

Question 22

opioid tolerance charcitresitics

Answer 22

† Shorter duration of pain relief
† Decrease in peak analgesic effect
† Increasing amount needed to achieve relief

Question 23

opioid tolerance managment

Answer 23

† Lengthen time between doses

† Increase dose to avoid shorter dosing interval

Question 24

no more than ___ MME for acute pain

Answer 24

700

Question 25

Opioid Dependence

3 or more of the following:

Answer 25

… Drug tolerance
… Withdrawal symptoms
… Use of the drug in larger
amounts or for longer
i d th i d f
… Significant time spent
obtaining the substance or
recovering from its effects
… Foregoing of important
activities or willingness to periods than required for
medical necessity
… Repeated unsuccessful
attempts to decrease or
discontinue use
… Drug use to avoid
withdrawal
activities, or willingness to
accept severe physical,
social, or professional
negative consequences, due
to drug use

Question 26

Physical Dependence

Answer 26

Repeated opioid use leads to physical adaptation

of body to drug and physical need for opioids

Question 27

… Withdrawal symptoms experienced when off

opioids for

Answer 27

36-72 h

Question 28

duration of withdrawal

Answer 28

2 to 5 weeks

Question 29

physical dependence resutls in

Answer 29

continued use of drug despite negative consequences

Question 30

Psychological Dependence

Answer 30

Continued drug use for reasons other than tolerance
and withdrawal, such as the experience from a
drug’s pleasurable effects or to block out or to
escape from reality

Question 31

Addiction

Answer 31

Addiction is a primary, chronic, neurobiologic disease,
with genetic, psychosocial, and environmental factors
influencing its development and manifestations. It is
characterized by behaviors that include one or more
of the following: impaired control over drug use,
compulsive use, continued use despite harm, and
craving.
… American Pain Society

Question 32

Opioid Addiction

Answer 32

… Most severe form of dependence
… Patient has uncontrollable cravings for the drug
… Is willing to risk any adverse consequences to obtain
it
… Requires ever-higher doses in order to ward off
withdrawal and/or to obtain the pleasurable
narcotic high associated with the drug

Question 33

Drug interactions

Answer 33

… CNS depressants
† Sedative- hypnotics, alcohol, anesthetics, barbiturates
… GI/GU effects (constipation, urinary retention)
† Anticholinerg , ,p ics, TCAs, phenothiazines
… MAOIs (coma, HTN)
… Cimetidine enhances opioid effects
… Diuretics (orthostatic hypotension)
… Nicotine decreases effects of opioids

Question 34

Contraindications and Precautions

Answer 34

… Use in patient with
head injuries
… Pregnancy
… Impaired pulmonary
… Hypersensitivity
… Abdominal pain
… Labor and Delivery
… Impaired pulmonary … ETOH
function
… Impaired hepatic or
renal function
… ETOH
… Prostate disease
… Urinary strictures