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Anesthesia Basics > Pharm: Opioid Drugs > Flashcards

Pharm: Opioid Drugs Flashcards

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

A

250

24
Q

Sufentanil (sufenta) MOA

A

Analog of fentanyl 5-10 x as potent

25
Q

Sufentanil (Sufenta) loading, maintenance, bolus dosing

A

Loading:
0.25-2 mcg/kg

Maintenance:
0.5-1.5 mcg/kg/hr

Bolus:
2.5-10 mcg

26
Q

Sufentanil (sufenta) onset and duration

A

onset 1-3min
duration: dose dependent

27
Q

Sufentanil (sufenta) potency

A

500-1000

28
Q

Sufentanil (sufenta) cautions

A

Dose-related bradycardia

HypoTN and HTN

Resp dep

Chest wall rigidity

N/V

29
Q

Dilaudid dosing

A

0.015mg/kg
Q3-6hrs

30
Q

Dilaudid onset and duration

A

onset 1-3 min
duration 4-5hrs

31
Q

Dilaudid cautions

A

Bradycardia/
tachycardia

Flushing of face

Agitation, dysphoria

32
Q

MOA of opioids

A

: 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
Q

Classifications of pain

A

neuropathic
somatic
visceral

34
Q

opioid receptors: Mu-1

A

analgesia (supraspinal, spinal), bradycardia, euphoria, hypothermia, miosis, urinary retention, low abuse
- Agonist: endorphins, morphine, synthetics
- Antagonist: naloxone, naltrexone, nalmefene

35
Q

opioid receptors: Mu-2

A

analgesia (spinal), respiratory depression, bradycardia, euphoria, miosis, N/V, constipation, urinary retention, physical dependence
- Agonist: endorphins, morphine, synthetics
- Antagonist: naloxone, naltrexone, nalmefene

36
Q

opioid receptors: Kappa

A

analgesia (supraspinal, spinal), possible resp depression, sedation/dysphoria, diuresis (vasopressin), low abuse
- Agonist: dynorphins

37
Q

opioid receptors: delta

A

analgesia (supraspinal, spinal), modulation of Mu receptors, selective of endogenous enkephalins, resp depression, urinary retention, physical dependence
- Agonist: enkephalins

38
Q

Opioid receptors: Sigma

A

dysphoria, hallucinations, tachycardia, mydriasis, resp stimulation
- Agonist: nalorphine, pentazocine, ketamine?

39
Q

Pain modulation: Gate Theory

A

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
Q

Pain modulation: tolerance

A

over time, a drug loses its effectiveness, and a larger dose is required to produce the same physiologic response

41
Q

Pain modulation: physical dependence

A

set of physiological changes that disrupts homeostasis
🡺 withdrawal = diaphoresis, insomnia, restlessness, N/V, diarrhea, abd cramps

42
Q

Classifications of opioids: Natural Opium alkaloids

A

(Phenanthrene derivatives)
- morphine
- codeine
(Benzylisoquinolone)
-papaverine

43
Q

Classifications of opioids: synthetic

A

(Phenylpiperidines)
- alfentanil
- fentanyl
- sufentanil
- remifentanil
- meperidine
- naloxone
(Morphinans)
- nalbupine
(Phenylheptylamines)
- methadone

44
Q

Clinical effects of opioids: CNS

A

analgesia, sedation, and euphoria

opioid induced hypercarbia

45
Q

Clinical effects of opioids: Respiratory depression

A

acts on Mu and Delta receptors in the brainstem
-reduce responsiveness to increasing CO2 and decreasing O2
-Shift to the right

46
Q

Clinical effects of opioids: Cardiac

A

-Via medullary vagal stimulation
-Dose-dependent vasodilation
-Hypotension related to histamine release (morphine, codeine, and meperidine)

47
Q

Clinical effects of opioids: Miosis

A

pinpoint pupils
-Opioid depression of GABA interneurons leads to stimulation of Edinger-Westphal nucleus = parasympathetic signals to CN III

48
Q

Clinical effects of opioids: GI

A

Decreased GI motility and intestinal propulsive activity, prolong gastric emptying time, and reduce GI secretory activity
-Postoperative issues can include constipation and ileus

49
Q

Clinical effects of opioids: PONV

A

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
Q

Clinical effects of opioids: Muscle Rigidity

A

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
Q

Clinical effects of opioids: Endocrine

A

Reduce the stress response to surgery, have immunosuppressant effect
-Release vasopressin and inhibit stress-induced release of corticosteroids & gonadotropins from the pituitary

52
Q

Clinical effects of opioids: GU & antitussive

A

GU: increases urinary sphincter tone

Antitussive effect: cough suppression (codeine is among best suppressant)

53
Q

Cyclooxygenase inhibitors (NSAIDS) MOA

A

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
Q

Multimodal analgesia: NSAIDS

A

*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
Q

Multimodal analgesia: Tylenol (Ofirmev)

A

*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

Anesthesia Basics (7 decks)

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