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Anesthesia Basics > Pharm: Opioid Drugs > Flashcards

Pharm: Opioid Drugs Flashcards

(55 cards)

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1
Q

Meperidine (Demerol) MOA

A

Synthetic opioid
Structural similar to atropine

Metabolite = normeperidine

Causes CNS stimulation @ high risk for seizures

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2
Q

Meperdine (Demerol) dosing

A

2.5-5mg/kg

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3
Q

Meperidine (Demerol) onset and duration

A

onset: 5min
duration: 2-3hrs

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4
Q

Meperidine (Demerol) potency

A

0.1

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5
Q

Meperidine (Demerol) cautions and other uses

A

Orthostatic hypotension

Mydriasis

IV Demerol decrease postop shivering (Kappa)

Serotonin syndrome with MAO inhibitors

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6
Q

Morphine MOA

A

Opium poppy derivative

Inhibits ascending pain pathway

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7
Q

Morphine dosing

A

0.1-1mg/kg

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8
Q

Morphine onset and duration

A

onset: 20min
duration: 4-5hrs

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9
Q

Morphine potency

A

1.0

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10
Q

Morphine cautions and other uses

A

Orthostatic hypotension

Resp depression

Reduces MAC 50%

Histamine release

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11
Q

Alfentanil (Alfenta) MOA

A

Analog of fentanyl

1/5 as potent

Metabolized in liver

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12
Q

Alfentanil (Alfenta) loading and maintenance doses

A

loading: 25-100mcg/kg
maintenance: 0.5-2mcg/kg/min

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13
Q

Alfentanil (Alfenta) onset and duration

A

Onset: immediate
Duration: 15 m

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14
Q

Alfentanil (Alfenta) potency

A

10-25

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15
Q

Alfentanil (Alfenta) cautions

A

admin slowly over 1-3m

monitor for bradycardia

hypotension

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16
Q

Fentanyl (sublimaze) MOA

A

Structurally r/t meperidine

50-100 x more potent than morphine

High lipid solubility

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17
Q

Fentanyl (sublimaze) loading, maintenance and bolus dosing

A

Loading:
3-5 mcg/kg

Maintenance:
2-10 mcg/kg/hr

Bolus:
25-100 mcg

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18
Q

Fentanyl (sublimaze) onset and duration

A

Onset: 2-5 m
Duration: 30-60 m

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19
Q

Fentanyl (sublimaze) potency

A

75-125

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20
Q

Fentanyl (sublimaze) cautions

A

Stiff chest syndrome

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21
Q

Remifentanil loading, maintenance, bolus dosing

A

Loading:
1-2 mcg/kg

Maintenance:
0.1-1 mcg/kg/hr

Bolus:
0.1-1 mcg/kg

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22
Q

Remifentanil onset and duration

A

onset: 1min
duration: 5-10min

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23
Q

Remifentanil potency

24
Q

Sufentanil (sufenta) MOA

Study These Flashcards
A

Analog of fentanyl 5-10 x as potent

25
Sufentanil (Sufenta) loading, maintenance, bolus dosing
Loading: 0.25-2 mcg/kg Maintenance: 0.5-1.5 mcg/kg/hr Bolus: 2.5-10 mcg
26
Sufentanil (sufenta) onset and duration
onset 1-3min duration: dose dependent
27
Sufentanil (sufenta) potency
500-1000
28
Sufentanil (sufenta) cautions
Dose-related bradycardia HypoTN and HTN Resp dep Chest wall rigidity N/V
29
Dilaudid dosing
0.015mg/kg Q3-6hrs
30
Dilaudid onset and duration
onset 1-3 min duration 4-5hrs
31
Dilaudid cautions
Bradycardia/ tachycardia Flushing of face Agitation, dysphoria
32
MOA of opioids
: Agonist binds with stereospecific opioid receptors on the CNS (spinal & supraspinal) and periphery 🡺 Produce analgesia at CNS receptors that respond to endorphins, enkephalins, & dynorphins 🡺 Opiate-receptor activation inhibits pre-synaptic release and postsynaptic response to excitatory neurotransmitters (Ach, substance P) from nociceptive neurons
33
Classifications of pain
neuropathic somatic visceral
34
opioid receptors: Mu-1
analgesia (supraspinal, spinal), bradycardia, euphoria, hypothermia, miosis, urinary retention, low abuse - Agonist: endorphins, morphine, synthetics - Antagonist: naloxone, naltrexone, nalmefene
35
opioid receptors: Mu-2
analgesia (spinal), respiratory depression, bradycardia, euphoria, miosis, N/V, constipation, urinary retention, physical dependence - Agonist: endorphins, morphine, synthetics - Antagonist: naloxone, naltrexone, nalmefene
36
opioid receptors: Kappa
analgesia (supraspinal, spinal), possible resp depression, sedation/dysphoria, diuresis (vasopressin), low abuse - Agonist: dynorphins
37
opioid receptors: delta
analgesia (supraspinal, spinal), modulation of Mu receptors, selective of endogenous enkephalins, resp depression, urinary retention, physical dependence - Agonist: enkephalins
38
Opioid receptors: Sigma
dysphoria, hallucinations, tachycardia, mydriasis, resp stimulation - Agonist: nalorphine, pentazocine, ketamine?
39
Pain modulation: Gate Theory
large-diameter myelinated afferents (Aβ) conveying pressure and touch information have “faster” conduction speed than Aδ fibers or C fibers conveying painful information to the dorsal horn 🡺 the application of light peripheral mechanical stimuli resulting in excitation of Aβ fibers can activate the inhibitory interneurons in the dorsal horn and thus close the “gate” to the simultaneous incoming pain signals carried by Aδ and C fibers
40
Pain modulation: tolerance
over time, a drug loses its effectiveness, and a larger dose is required to produce the same physiologic response
41
Pain modulation: physical dependence
set of physiological changes that disrupts homeostasis 🡺 withdrawal = diaphoresis, insomnia, restlessness, N/V, diarrhea, abd cramps
42
Classifications of opioids: Natural Opium alkaloids
(Phenanthrene derivatives) - morphine - codeine (Benzylisoquinolone) -papaverine
43
Classifications of opioids: synthetic
(Phenylpiperidines) - alfentanil - fentanyl - sufentanil - remifentanil - meperidine - naloxone (Morphinans) - nalbupine (Phenylheptylamines) - methadone
44
Clinical effects of opioids: CNS
analgesia, sedation, and euphoria opioid induced hypercarbia
45
Clinical effects of opioids: Respiratory depression
acts on Mu and Delta receptors in the brainstem -reduce responsiveness to increasing CO2 and decreasing O2 -Shift to the right
46
Clinical effects of opioids: Cardiac
-Via medullary vagal stimulation -Dose-dependent vasodilation -Hypotension related to histamine release (morphine, codeine, and meperidine)
47
Clinical effects of opioids: Miosis
pinpoint pupils -Opioid depression of GABA interneurons leads to stimulation of Edinger-Westphal nucleus = parasympathetic signals to CN III
48
Clinical effects of opioids: GI
Decreased GI motility and intestinal propulsive activity, prolong gastric emptying time, and reduce GI secretory activity -Postoperative issues can include constipation and ileus
49
Clinical effects of opioids: PONV
emetic effect – opioids stimulate the chemoreceptor trigger zone (CTZ) in the Area Postrema of the medulla -Primary receptors in this area include serotonin type 3 (5-HT3) & dopamine type 2 (D2) -dose-dependent increase in biliary duct pressure and sphincter of Oddi tone
50
Clinical effects of opioids: Muscle Rigidity
generalized hypertonus of skeletal muscle, especially with higher dosing -Truncal rigidity, chest-wall constriction/loss of compliance, pharyngeal & laryngeal muscle constriction possible (fentanyl, sufentanil, remifentanil, alfentanil)
51
Clinical effects of opioids: Endocrine
Reduce the stress response to surgery, have immunosuppressant effect -Release vasopressin and inhibit stress-induced release of corticosteroids & gonadotropins from the pituitary
52
Clinical effects of opioids: GU & antitussive
GU: increases urinary sphincter tone Antitussive effect: cough suppression (codeine is among best suppressant)
53
Cyclooxygenase inhibitors (NSAIDS) MOA
inhibit COX *COX 1: inhibition decreases thrombosis (aspirin, irreversibly inhibits and is effective 7 days) *COX 2: produced in response to inflammation (acetaminophen, celecoxib, ketorolac)
54
Multimodal analgesia: NSAIDS
*Aspirin = salicylic acid, antiplt *Ketorolac = acetic acid derivative, can change lithium level, can promote postop bleeding, NO resp dep, need adequate renal fn *Ibuprofen = propionic acid derivative *Celecoxib: heterocyclic derivative
55
Multimodal analgesia: Tylenol (Ofirmev)
*10 mg/mL, admin 1000 mg over 15 minutes for > 50 kg *MUST DRAW UP appropriate dose from the vial and placed into a separate container for < 1000mg *<50 kg 15mg/kg q 6 (max 75mg/kg/day) *Max 4 g/day *Warnings -> hepatic injury and hypersensitivity

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