OPIOIDS

Question 1

Tolerance is used to describe when

Answer 1

patients require increasing dosages of opioids to have the same clinical effect.

Question 2

Dependence can be either

Answer 2

It is the presence of withdrawal symptoms when the drug is withheld. May be physical or psychological.

Question 3

Types of Opioids

Answer 3

agonists, antagonists, or mixed agonists/antagonists.

Question 4

What are the different types of Opioids receptors?

Answer 4

Mu1, Mu2, Kappa , Delta

Question 5

Principal mechanism of action of all opioids

Answer 5

Through Mu receptor agonism

Question 6

Principal mechanism of action of all opioids

Answer 6

Through Mu receptor agonism

Opiates mimics endogenous peptides such as endorphins

Question 7

Effects of opioids is based on

Answer 7

Depends on which G-COUPLED receptors to which receptor they bind to

Question 8

Metabolism of most opioids? What do you have to consider?

Answer 8

Most undergo biotransformation in the liver. Consider reducing the dose for patients with liver and kidney failure

Question 9

Metabolites opioids and kidney failure

Answer 9

May accumulate with kidney failure patients.

Question 10

Endogenous opioids

Answer 10

Peptide endorphins are the naturally occurring ligands for opioid receptors.

Question 11

Where are the opioids receptors located? the the

Answer 11

– sensory neuron of the peripheral nervous system;
– dorsal horn (layers 4 and 5 of the substantia gelatinosa) of the spinal cord, which inhibits the transmission of nociceptive information;
– brainstem medulla, which potentiates descending inhibitory pathways that modulate ascending pain signals; and the
–cortex of the brain, which decreases the perception and emotional response to pain

Question 12

Opioid receptor activation inhibits the

Answer 12

presynaptic release and postsynaptic response to excitatory neurotransmitters

Question 13

Excitatory neurotransmitters are

Answer 13

Glutamate
Acetylcholine
Substance P

Question 14

2 highly lipids soluble opioids and their implications

Answer 14

The highly lipid-soluble opiates, such as fentanyl and Sufentanil, have a rapid onset and short duration of action

Question 15

Metabolites of mophine and meperidine and their implications?

Answer 15

morphine and meperidine, have metabolites—morphine-6-glucoronide and normeperidine, respectively—that are equally active as the parent compound.

Question 16

Opiods of CBF, CMRO2, ICP

Answer 16

Opioids can reduce cerebral metabolic O2 requirements, cerebral blood flow, and intracranial pressure if alveolar ventilation is unchanged in a healthy patient;

Question 17

Opiods with patients with TBI

Answer 17

May increase ICP with patients with TBI even with controlled ventilation.

Question 18

Opioids and GI

Answer 18

an cause contraction of the sphincter of Oddi. This contraction can mimic biliary colic, but it is responsive to antagonism of the opioids or the use of glucagon.

Question 19

Opioids and Respiratory

Answer 19

decreases minute ventilation by decreasing the respiratory rate (as opposed to decreasing the tidal volume)

Question 20

Opioids and Respiratory : CO2

Answer 20

Producing a dose-dependent depression of the ventilatory response to CO2.

Question 21

Opioids and the The apnea threshold

Answer 21

The apnea threshold, defined as the highest PaCO2 without ventilatory effort, is increased with the use of opioids.

Question 22

2 Can cause histamine-induced bronchospasm

Answer 22

morphine and meperidine

Question 23

Opioids and MUSCULOSkeletAL

Answer 23

Opioids can produce generalized skeletal muscle rigidity, a phenomenon associated with the more potent opiates (e.g., fentanyl, sufentanil, carfentanil).

Question 24

Musculoskeletal changes that can occur with the administration of opioids?

Answer 24

Loss of chest wall compliance and contraction of the laryngeal and pharyngeal muscles can be severe, resulting in ventilatory difficulty, even with positive-pressure ventilation.

Question 25

The mechanism of opioid-induced muscle rigidity is believed to be mediated by the

Answer 25

µ receptors at the supraspinal level by increasing dopamine synthesis and inhibiting γ-aminobutyric acid activity.

Question 26

How can opioids induce MUSCLE RIGIDITY?

Answer 26

decreasing the rate of opioid administration or concomitantly administering a neuromuscular blocking agent and controlling ventilation.

Question 27

Postoperative shivering can be attenuated with_______ may act through ______Receptor. Only _______Mg , administered ________

Answer 27

meperidinewhich may act through a к-receptor mechanism. Only 12.5– 25 mg meperidine, administered intravenously as a slow push, is usually needed to produce this effect in an adult.

Question 28

Opioids and CV

Answer 28

opioids can cause a dose-dependent bradycardia resulting in decreased cardiac output.

Question 29

Meperidine and CV effects

Answer 29

may also cause a decrease in myocardial contractility because it has negative inotropic effects. One exception is meperidine, which may cause tachycardia because of its structural similarities to atropine.

Question 30

2 opioids with prolongation of QTI

Answer 30

Prolongation of the QT interval has been noted with both meperidine and methadone.

Question 31

Most opioids exert their cardiovascular effects

Answer 31

both by sympatholysis via vasomotor centers in the medulla and by increased parasympathetic tone via vagal pathways.

Question 32

What are the side effects of neuraxial opioids?

Answer 32

respiratory depression, somnolence, pruritus, nausea and vomiting, and urinary retention. Generalized pruritus is the most common and least dangerous side effect seen with the use of neuraxial opioids

Question 33

How do neuraxial opioids exert their effect?

Answer 33

The site of action are the opioid receptors within the substantia gelatinosa in the dorsolateral horn of the spinal cord.

Question 34

List the commonly used opioid agonists and there relative potencies.

Answer 34

Morphine 1
Methadone 1
Meperidine 0.1
Hydromorphone 5- 8 times
Alfentanyl 20 times
Fentanyl 100 times
Sufentanyl 1000 times
Alfentanyl 20 
Remifentanyl 100 times

Question 35

Describe the pharmaco kinetics of morphine.

Peak : IM and IV

Answer 35

IM: 30 to 60 minutes
IV: 20 minutes

Question 36

Morphine excretion

Answer 36

Renal

Question 37

Morphine half life

Answer 37

2-4 hours

Question 38

What are the side effects of morphine?

Answer 38

Constipation, respiratory depression , N, V, Urinary retention

Question 39

Describe the unique pharmacokinetics of remifentanil.

Answer 39

Rapid onset of action, remifentanil has an ester linkage which undergoes rapid hydrolysis by non-specific tissue and plasma esterases.

Question 40

Which opioid antagonist is most commonly used and how is it dosed?

Answer 40

Narcan: Naloxone, 0.4mg

Question 41

Side effects of fentanyl compared to morphine

Answer 41

Delayed

Question 42

Opioids induce respiratory depression via activation of

Answer 42

μ-opioid receptors at specific sites in the central nervous system including the pre-Bötzinger complex, a respiratory rhythm generating area in the pons.

Question 43

Causes respiratory depression?

Answer 43

Fentanyl (Intrathecal)

Question 44

Side effects of Morphine MNEMONICS

Answer 44

Miosis
Orthostatic hypotension
Respiratory depression
Pruritus
Histamine release/hormonal release
Increase intracranial tension
Nausea
Euphoria
Sedation

Question 45

Effects at Mu1 receptor

Answer 45

Supraspinal analgesia
Bradycardia
Sedation
Pruritus
Nausea and vomiting

Question 46

Effects at Mu2 receptor

Answer 46

Respiratory depression
Euphoria
Physical dependence
Pruritus
Constipation

Question 47

Effects at kappa receptor

Answer 47

Spinal analgesia
Respiratory depression
Sedation
Miosis

Question 48

Effects at delta receptor

Answer 48

Spinal analgesia

Respiratory depression