Gruneisen, Opiods Fall 2010

Front 1

________ is the term used to describe all exogenous substances, natural and synthetic, that bind specifically to opiod receptors and produce some agonist effects.

Back 1

Opiod

Front 2

Semisynthetic opiods result from minor modification of the _______ molecule.

Back 2

Morphine

Front 3

Synthetic opiods contain the phenanthrene nucleus of morphine but are manufactured by _________ rather than chemical modification of morphine.

Back 3

synthesis

Front 4

The principal pharmacodynamic difference between opiods is potency and rate of equilibration between plasma and the site of drug efffect.
T or F

Back 4

True

Front 5

Opiods act as ______ at stereospecific opiod receptors in the CNS and outside the CNS in peripheral tissues.

Back 5

agonists

Front 6

Opiods mimic the actions of endogenous peptide opiod receptors, resulting in _______ of pain-modulating systems.

Back 6

activation

Front 7

The principal effect of opiod receptor activation is a ________ in neurotransmission, which results mostly from presynaptic inhibition of neurotransmitter release.

Back 7

decrease

Front 8

The effect of opiod receptor activation is increased _______conductance, leading to hyperpolarization of cellular membranes.

Back 8

Potassium

Front 9

Opiod receptors are classified as ____, ______, and _______ receptors.

Back 9

mu, delta, kappa

Front 10

Mu, delta and kappa receptors belong to a superfamily of _______ ________ receptors.

Back 10

G protein

Front 11

Mu or morphine-preferring receptors are principally responsible for supraspinal and spinal anesthesia.
T or F

Back 11

True

Front 12

Mu1 receptors are speculated to produce ________, whereas Mu2 receptors are responsible for __________, ________, and ___________.

Back 12

analgesia, hypoventilation, bradycardia, and physical depencence

Front 13

Opiod analgesia is _______ related and specific for visceral rather than somatic pain.

Back 13

dose

Front 14

Poorly lipid-soluble opiods, result in a ______onset of analgesia, but have a _______ duration of action than lipid-soluble opiods.

Back 14

slower, longer

Front 15

Epidural administration of morphine, fentanyl, and sufentanil produces opiod blood concentrations that are similar to those produced by _______ _______ of an equilvelant dose.

Back 15

intramuscular injection

Front 16

Coughing, straining and body position can affect opiod movement in the CSF.
T or F

Back 16

False, only coughing or straining

Front 17

What are the most common side effects after neuraxial opiods are used to treat acute postoperative pain?

Back 17

pruritus, N/V, urinary retention and depression of ventilation

Front 18

Delayed depression of ventilation typically occurs how many hours after epidural or intrathecal administration of morphine?

Back 18

6-12

Front 19

What has occurred when delayed depression of ventilation happens with epidural administration of opiods?

Back 19

cephalad migration of the opiod in the CSF and subsequent interaction with opiod receptors located in the ventral medulla.

Front 20

Despite a normal breathing rate, what might occur with neuraxial opiod administration?

Back 20

arterial hypoxemia and hypercarbia

Front 21

What reliably detects opiod-induced arterial hypoxemia, and what is the effective treatment?

Back 21

pulse oximetry, supplemental O2

Front 22

What provides early warning that opiod induced hypoventilation is occurring?

Back 22

capnography

Front 23

What is perhaps the most reliable clinical sign of depression of ventilation?

Back 23

depressed level of consciousness, possibly caused by hypercarbia

Front 24

Which drug is effective in reversing the depression of ventilation produced by neuraxial opiods?

Back 24

Naloxone

Front 25

_________ is the prototype opiod agonist with which all other opiods are compared.

Back 25

Morphine

Front 26

What effects do morphine produce?

Back 26

analgesia, euphoria, sedation and a decreased ability to concentrate

Front 27

With administration of morphine, the cause of the pain persists, but even small doses increase the threshold to pain and modify the perception of noxious stimulation such that it is no longer experienced as pain.
T or F

Back 27

True

Front 28

Morphine relieves sharp, intermittent pain best.
T or F

Back 28

False, morphine relieves continuous dull pain best

Front 29

Analgesia is most prominent when opiods are administered a few seconds after the painful stimulus occurs.
T or F

Back 29

False, analgesia is most prominent when opiods are given before the pain

Front 30

In the absence of pain, Morphine may produce dysphoria rather than euphoria.
T or F

Back 30

True

Front 31

Clearance of opiods principally occurs by ________metabolism, but large differences in _________ _________ account for pharmacokinetic differences between opiods.

Back 31

hepatic lipid solubility

Front 32

__________ is well absorbed ater IM injection, with an onset of effect in 15-30 min and a peak effect in 45-90 minutes.

Back 32

Morphine

Front 33

Absorption of morphine from the GI tract is not reliable
T or F

Back 33

True

Front 34

What is the peak effect (equilbration time between the blood and brain) after IV administration of morphine.

Back 34

15-30 min

Front 35

Reasons for poor penetration of morphine into the CNS include: (2)

Back 35

relatively poor lipid solubility and rapid metabolism with glucuronic acid

Front 36

Elimination of morphine is impaired in patients with renal failure, causing an accumulation of metabolites and unexpected ventilatory deperssant effects.
T or F

Back 36

True

Front 37

Morphine has a greater analgesic potency and slower speed of onset in men.
T or F

Back 37

False, in women

Front 38

Moprhine given to supine and normovolemic patients is unlikely to cause direct myocardial depression or hypotension.
T or F

Back 38

True

Front 39

After administration of IV morphine, the patient may exhibit _______ ________ and ________ , if changing from a supine to standing position.

Back 39

orthostatic hypotension, syncope

Front 40

Morphine induced bradycardia results from increased _________ effects

Back 40

parasympathomimetic

Front 41

The combination of opiod agonists with ______ ______ or a _________ result in decreases insystemic blood pressure that do not accompany administration of these drugs when administered alone.

Back 41

Nitrous oxide, benzodiazepine

Front 42

High doses of opiods may result in apnea, but the patient remains conscious and able to initiate a breath if asked to do so.
T or F

Back 42

True

Front 43

Clinically, depression of ventilation produced by opiod agonists manifests as a _______ frequency of breathing that is often accompanied by a compensatory________ in tidal volume.

Back 43

decrease, increase

Front 44

Why are opiods not considered true anesthetics?

Back 44

Because they do not reliably produce unconsciousness, especially in young people.

Front 45

Why must opiods be used with caution in patients with head injury?

Back 45

Because depression of ventilation and accumulation of CO2 can result in undesirable increases in ICP.

Front 46

Opiods act as cerebral vasoconstrictors to decrease cerebral blood flow and possibly ICP.
T or F

Back 46

True

Front 47

When high doses are infused rapidly, with which opiod is skeletal muscle rigidigy (ie stiff-chest syndrome) a common occurance?

Back 47

Fentanyl

Front 48

What type of drugs can be given to terminate skeletal muscle rigidity that is induced with opiod infusion? (2)

Back 48

neuromuscular blocking drug or opiod antagonist

Front 49

Opiods can be shownd to decrease MAC for volatile anesthetics in a dose-related manner until a ceiling effect is reached by what percent?

Back 49

50%

Front 50

What is the usual recommendated dose interval times for morphine to allow evaluation of its clinical effect?

Back 50

5-7 min

Front 51

Opiods can cause spasm of biliary smooth muscle, resulting in increases in intrabiliary pressure that may be associated with epigastric distress or biliary colic.
T or F

Back 51

True

Front 52

Opiods can decrease peristaltic activity and enhance the tone of pyloric shpincter, contributing to delayed gastric and intestinal tract emptying.
T or F

Back 52

True

Front 53

IM morphine produces more nausea and vominting then IV morphine.
T or F

Back 53

True

Front 54

Meperidine is a synthetic opiod that is about ____ as potent as morphine.

Back 54

1/10

Front 55

Meperidine is well absorbed from the gastrointestinal tract.
T or F

Back 55

True

Front 56

Which opiod is effective in suppressing postoperative shivering that may result in detrimental increases in metabolic O2 consumption?

Back 56

meperidine

Front 57

Meperidine causes more frequent and profound orthostatic hypotenstion than morphine.
T or F

Back 57

True

Front 58

Can meperidine at times increase or decrease HR?

Back 58

increase, has modest atropine-like effect.

Front 59

Large doses of ________ decrease myocardial contractility, an effect that is unique among the opiods.

Back 59

Meperidine

Front 60

Caution should be taken with administration of Meperidine to patients who are taking antidepressants due to the possible evoking of autonomic nervous system instability.
T or F

Back 60

True

Front 61

Fentanyl is a synthetic opiod agonist structurally related to _________.

Back 61

meperidine

Front 62

How much stronger is fentanyl than morphine?

Back 62

75-125 times

Front 63

Fentanyl has a more rapid onset and shorter duration than morphine.
T or F

Back 63

True

Front 64

The greater potency and more rapid onset of action reflect the greater ________ _______ of fentanyl compared to morphine.

Back 64

lipid solubility

Front 65

Fentanyl might produce bradycardia and hypotenstion only if administered with other depressants or sedative drugs.
T or F

Back 65

True

Front 66

Administration of an opiod such as fentanyl before painful surgical stimulation occurs may increase the subsequent amount of opiod required in the postoperative period to provide analgesia.
T or F

Back 66

False, use of fantanyl may decrease the amount of opiod postoperatively

Front 67

Large doses of fentanyl have been used alone to produce surgical anesthesia with stable hemodynamics, however, the disadvantage to this is what?

Back 67

Opiods are not complete anesthetics and patient awareness can occur.

Front 68

__________ is an analog of fentanyl, with an analgesic potency that is 5-10 times that of fentanyl.

Back 68

Sufentanil

Front 69

Large repeated do can doses of Sufentanil can cause a cumulative effect, where as small doses are terminated quickly due to _______ ________ to inactive tissue sites.

Back 69

rapid redistribution

Front 70

After termination of sufentanil infusion, the decrease in the plasma drug concentration is accelerated by __________ and __________.

Back 70

metabolism redistribution

Front 71

_______ of ________ and ___________ may be more profound with sufentanil than with fentanyl.

Back 71

Depression of ventilation, bradycardia

Front 72

Use of large doses of potent opiods such as sufentanil may produce skeletal muscle rigidity that makes ventilation of the lungs difficult.
T or F

Back 72

True

Front 73

_________ is an analog of fentanyl with is 1/5 to 1/10 as potent and has 1/3 the duration of action.

Back 73

Alfentanil

Front 74

What is the unique advantage of alfentanil when compared with fentanyl and sufentanil?

Back 74

more rapid onset of action after IV administration (effective-site equilibrium is 1.4 min)

Front 75

Almost 90% of alfentanil exists in the lipid-soluble nonionized form at physiologic pH.
T or F

Back 75

True

Front 76

Which drug is useful when an opiod is required to blunt the response of a single brief stimulus such as tracheal intyubation or performance of a retrobulbar block?

Back 76

Alfentanil due to its rapid effect at the brain

Front 77

___________ is a selective opiod agonist with analgesic potency similar to that of fentanyl, and a blood brain equilibrium time similar to alfentanil.

Back 77

Remifentanil (effect-site equilibrium time of about 1.1 min)

Front 78

_________ is structurally unique because of its ester linkage, which renders is susceptible to hydrolysis by nonspecific plasma and tissue esterases.

Back 78

Remifentanil

Front 79

Which opiod has brevity of action, precise and rapid titration effects, rapid onset and offset, noncumulative effects and rapid recovery after discontinuation of IV infusion?

Back 79

Remifentanil

Front 80

Which opiod may be preferred whtn analgesic effect is desired transitnely and can induce anesthesia over 60-90 secs?

Back 80

Remifentanil

Front 81

The combination of Remifentanil and _________ is synergistic resulting in severe depression of ventilation.

Back 81

propofol

Front 82

Before cessation of __________ a longer-acting opiod should be administered to ensure analgesia when the patient awakens.

Back 82

Remifentanil

Front 83

Why is Remifentanil used for sedation in mechanically ventilated critically ill patients?

Back 83

the rapid onset and offset of action makes it possible to quiclky adjust the required level of sedation.

Front 84

Why might Remifentanil be associated with acute opiod tolerance?

Back 84

due to high requirements of postoperative analgesia required in patients who received relatively large doses of remifentanil intraoperatively.

Front 85

What is the action of opiod agonist-antagonists?

Back 85

the drug binds to teh mu receptor where it produces limited responses or no effect.

Front 86

What is the benefit of opiod agonist-antagonists?

Back 86

The can produce analgesia with limited depression of ventilation and a low potential to produce physical dependence.

Front 87

What drug promptly reverses opiod induced analgesia and depression of ventilation?

Back 87

Nalaxone

Front 88

What is the dose for Nalaxone?

Back 88

1-4 mcg/kg IV

Front 89

The short duration of action of nalaxone might require supplemental doses to acheive the continuous desired effect of return of opiod effects.
T or F

Back 89

True

Front 90

Abrupt reversal of analgesia and sudden perception of pain might increase sympathetic nervous system symptoms in patients when nalaxone is used.
T or F

Back 90

True

Front 91

What is the most common reason for seeking medical care?

Back 91

Pain

Front 92

________ is the state in which no pain is felt, despite the presence of normally painful stinuli.

Back 92

Analgesia

Front 93

________ are compounds isolated from teh opium poppy and act at opiodreceptors, where as________ are compounds of any structural type that interact with the opiod receptors.

Back 93

Opiates, Opiods

Front 94

Opiods are unique in producing analgesia without loss of ________, _________, or __________.

Back 94

touch, proprioception, consciousness.

Front 95

__________ determines the relationship between drug dose and its concentration at receptor sites and refers to the study of plasma drug concentration versus time.

Back 95

Pharmacokinetics

Front 96

__________ relates to the concentration of the drug at its site of action and intensity of its effects.

Back 96

Pharmocodynamics

Front 97

When was morphine isolated from opium?

Back 97

1805 (some say 1803)

Front 98

When was Codeine first made?

Back 98

1832

Front 99

What are the 3 classifications of drugs that act as or against opiods?

Back 99

opiod agonists, opiod agonist-antagonists and opiod antagonists

Front 100

What are the 2 classes of opiods?

Back 100

Phenanthrenes: (morphine, codeine and thebaine)
Benzoisoquinolines (lacking opiod activity): noscapine and papavarine

Front 101

Which 3 drugs are a chemical modification of morphine?

Back 101

papaverine, thebaine(insignificant analgesic activity) and codine(substitution of a methyl group for the hydroxyl group on carbon 3)

Front 102

Which 3 drugs are synthetic opiods? These are manufactured by synthesis rather than chemical modification of Morphine.

Back 102

Levorphanol, Butorphanol and Methadone

Front 103

Which 4 drugs are semisynthetic opiods?

Back 103

Fentanyl, Sufentanil, Alfentanil and Remifentanil.

Front 104

What are the 2 actions of opiods?

Back 104

They act as stereospecific opiod receptors at pre & post synaptic sites in CNS and peripheral tissue and mimic endogenous ligands.

Front 105

What receptors are principally responsible for supraspinal and stinal analgesia?

Back 105

Mu (morphine preferring)

Front 106

What is the idea behine supraspinal and spinal analgesia?

Back 106

supraspinal- feel pain but don't care and spinal- don't feel pain

Front 107

Which drugs work at the Mu1 and Mu2 receptors?

Back 107

morphine, meperedine, fentanyl, sufentanil, alfentanil, remifentanil

Front 108

Which receptors are calcium channel-linked opiod receptors?

Back 108

kappa receptors

Front 109

What does agonist activation of kappa receptors produce?(2)

Back 109

dysphoria and diuresis

Front 110

Respiratory depression is less likely with kappa receptors than mu receptors.
T or F

Back 110

True

Front 111

What are some examples of kappa opiod receptors?

Back 111

talwin, Nubain, stadol, buprenex

Front 112

Which opiod receptors are found in vans deferens of rats?

Back 112

epsilon

Front 113

Which opiod receptors are not reversed by nalaxone?

Back 113

sigma

Front 114

Which opiod receptors serve to modulate mu receptor activity?

Back 114

delta

Front 115

All 3 receptors(mu, delta, kappa) work with G proteins to decrease neural activity by: (3)

Back 115

1. inhibit adenyl cyclase(the mechanism that makes things work inside the cell) 2. decrease conductance of voltage-gated calcium channels. 3. open inward flowing potassium channels (can't send pain message)

Front 116

The ideal opiod agonist would have what 2 characteristics?

Back 116

1) high specificity for receptors producing analgesia
2) little specificity for receptors associated with side effects(hypoventilation, nausea, physical dependence)

Front 117

During cholescystectomy, opiod-induced spasm of sphincter of oddi may be misinterperted as a a common bile duct stone or blockage in cholangiogram.
T or F

Back 117

True

Front 118

What drugs can be used to reverse morphine during a opiod-induced spasm (of sphincter of oddi)? (2)

Back 118

nalaxone or glucagon

Front 119

Where is meperidine metabolized?

Back 119

Liver

Front 120

__________ is the only opiod considered adequate for surgery when given intrathecally.

Back 120

Meperidine

Front 121

What are the primary uses of Meperidine?

Back 121

analgesia in L & D; post-op pain relief; useful for post-op shivering

Front 122

Meperidiine's metabolite, normeperidine, toxicity manifests as _______ and ______ especially in renal patients using a PCA devise due to elimination half-time in a renal patient may be 35. hours

Back 122

myoclonus and zeizures.

Front 123

Normeperidine (meperidine's metabolite) has a elimination half time of __ hours and is ____ as potent as parent drug.

Back 123

15 half

Front 124

Meperidine can be seen in the urine for up to __ days.

Back 124

3

Front 125

Where are opiod receptors located in the brain?

Back 125

periaqueductal gray matter in brainstem; amygdala; corpus striatum; hypothalamus

Front 126

Where are opiod receptors located in the epidural/subarachnoid space?

Back 126

substantia gelatinosa of spinal cord

Front 127

Opiods injected in the SAS are not associated with SNS denervation, skeletal muscle weakness, or loss of proprioception as with local anesthetics and IV administration.
T or F

Back 127

True

Front 128

Epidural placement of opiods give similar effects as IV administered opiods.
T or F

Back 128

True

Front 129

Where is morphine metabolized?

Back 129

Liver

Front 130

Kidneys play a significant role in patients with impaired liver function especially in ELIMINATION of metabolites of what drug?

Back 130

morphine

Front 131

What is the metabolite of morphine?

Back 131

morphine-6-glucuronide

Front 132

Morphine-6-glucuronide has agonist properties at mu receptors and can produce ventilatory depression and analgesia.
T or F

Back 132

True

Front 133

If Morphine-6-glucuronide accumulates, what can occur?

Back 133

marked respiratory depression

Front 134

What 3 effects does morphine have on the cardiovascular system?

Back 134

decrease in systemic BP r/t drug induced bradycardia; depression of AS node and slowed conduction through AV node; and profound hypotension r/t histamine release.

Front 135

What drug will relieve both angina due to myocardial ischemia and opiod induced biliary colic pain?

Back 135

nitroglycerin; narcan only relieves biliary pain

Front 136

Fentanly is metabolized in the _______ to the metabolite _________.

Back 136

liver; norfentanyl (metabolized by N-demethylation)

Front 137

Norfentanyl is not an active metabolite.
T or F

Back 137

False

Front 138

After a single IV dose, ________can be detected in the urine for 3 days.

Back 138

Fentanyl

Front 139

Fentanyl has a large volume of distribution.
T or F

Back 139

True

Front 140

When using Fentanyl, why must you keep the patient warm?

Back 140

Because if the patient gets cold, fentanyl may be released from distributed tissue when the patient rewarms.

Front 141

Fentanyl analgesic concentrations greatly ________ effects of midazolam and _________ the required dose of propofol.

Back 141

potentiate; reduce

Front 142

Most all opiods reduce CMRO2 and CBF.
T or F

Back 142

True

Front 143

What are the 2 metabolites of Sufentanil?

Back 143

N-demethylation(inactive)
O-demethylation (active)

Front 144

A single dose of sufenta produces a longer period of analgesia and less ventilatory depression than a comparable dose of fentanyl.
T or F

Back 144

True

Front 145

Compared with large fentanyl and morphine dosages, sufenta gives: (3)

Back 145

-more rapid induction (inc lipid soluble and inc protein binding)
-earlier emergence
-earlier extubation conditions

Front 146

In giving Sufenta, one must inject slowly because...

Back 146

can cause bradycardia,and chest will rigidity(bagging may be difficult or impossible)

Front 147

Alfentanil can be used as a maintenance infusion.
T or F

Back 147

True

Front 148

Remifentanil is not metabolized by pseudocholinesterase.
T or F

Back 148

True

Front 149

Remifentanil is best administered as an infusion due to the fast on and off set.
T or F

Back 149

True

Front 150

咖啡馆

Back 150

kāfēi guǎn

Café

Front 151

Sudden complete antagonism of opiod effects may cause hypertension, tacyhcardia, ventricular cardiac arrhythmias and pulmonary edema.
T or F

Back 151

True