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Pharm Exam I > Opiods > Flashcards

Opiods Flashcards

1
Q

Mu 1 Receptor (location, effects, drugs)

A

Supraspinal (brain) = periaqueductal or periventricular gray

  • Brady (direct central act on vagus nerve)
  • Euphoria, miosis, analgesia, hypothermia, urinary retention, psych abuse
  • ALL endogenous & exogenous agonists act on Mu1&2
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2
Q

Mu 2 Receptor (location, effects, drugs)

A

Spinal (SC) = Substantia gelatinosa & dorsal root ganglion

  • Brady (direct central act on vagus nerve)
  • Pruritis, N/V, constipation, physical dependence
  • ALL endogenous & exogenous agonists act on Mu1&2
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3
Q

Kappa Receptor (location, effects, drugs)

A

Supraspinal & Spinal

  • Dysphoria, miosis, sedation, diuresis (inhibit ADH)
  • DYNORPHINS work here & Butorphenol (agonist/ant)
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4
Q

Delta Receptor (location, effects, drugs)

A

Supraspinal & Spinal (modulator of Mu)

  • Resp depression, pruritis, constipation (mild), physical dep
  • ENKEPHALINS work here
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5
Q

Opiods: CNS Effects

A

Analgesia, euphoria, sedation, resp ctr depress, miosis, nausea CTZ (NO amnesia/anesthesia)

  • DECREASE ICP (modest) in absence of hypo vent
  • DECREASE CBF & CRMO2
  • Cerebrovascular stability
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6
Q

Opiods: CV Effects

A

No impairment of CV FUNCTION
-Dec HR (dose dependent)

Dec CO/BP (vasodilation form HISTAMINE release w/MSO4 & meperidine)

Dec CO/BP (venodilation)

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7
Q

Opiods: Resp Effects

A
  • Depression (Dose Dep), Infusion = less depression than bolus;
  • Vent depr early < 2h fent/sufent and late 6-12h MSO4
  • Hypercarbia ↓CO2 responsiveness;
  • Hypoxia
  • High airway pressures due to ↑ intrathoracic pressures
    compliance ;
    ↓RR ↑ Vt (Low Dose)
    ↓RR & Vt (High Dose)
  • Ventilatory response curve shifted Down & to the Right
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8
Q

What increases the magnitude & duration of reps depression w/opiods?

A

1) Alkalosis = ↑ % nonionized = ↑ brain penetration.

2) Secondary plasma peaks (Fentanyl & sufentanil) = reuptake into muscle, fat, lungs, & intestines

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9
Q

What factors influence the reap depressant effects of opiods?

A

Amt of pain/stimulation vs natural sleep, bolus vs continuous infusion, speed of injection, combo w/other anesthetics, age, clearance.

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10
Q

Opiods: Musculature Effects

A 
Muscle Rigidity
     Laryngeal
     Chest Wall
     Pharyngeal
     Glottic rigidity and Closure  
      have been reported
Called Wooden Chest
Tonic/Clonic (Fentanyl)
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11
Q

Opiods: Renal/GI/Liver Effects

A
  • ↑ Urine (ADH Blocked) at same time sympathetic blockade of sacral plexus cause urine retention;
  • Urine retention after epi/spine more common than IV for ♂;
  • ↓ Catecholamine release;
  • ↓ Cortisol release;
  • Oddi Spasm w/ ↑ biliary pressure (reverse w/ narcan or glucagon 0.25 – 0.5mg IV)
  • Constipation
  • ↓ Gastric Emptying
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12
Q

Opiod MOA

A

**All opioids activate inhibitory G proteins. Bind to opioid receptors & produce agonist effects (acting like an opiate)

1) Inhibit adenylyl cyclase → ↓cAMP & ↓ protein phosphorolation.
2) Opioids close voltage-gated Ca⁺⁺ channels on pre-synaptic nerve terminal to inhibit release of excitatory neurotransmitters ACh, Dopa, Norepi, (as well as glutamate & Substance P in the SC) & post-synaptic ↓ in neurotransmission.
3) promote opening of K⁺ channels → ↑K⁺ conduct. & hyperpolarization → ↓activity of post-synaptic cells. Opioids raise pain threshold by interrupting ascending pain pathways in the substantia gelatinosa in the dorsal horn of the SC & ventral caudal thalalamus & also activate descending pathways (periaquaductal gray area in midbrain, rostral ventral medulla) in CNS.
4) ↑ production of Phospholipase A2 = ↑ production of prostaglandins & leukotrienes

**Opioids also ↑ pain threshold by acting on peripheral sensory neurons. They ↓emotional reactivity to pain by acting on limbic areas of CNS.

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13
Q

Describe the various opiod potencies.

A

Sufentanil (1000x) > Remifentanil (100x) > Fentanyl (100x) > Alfentanil (10-20x) > Dilaudid (5x) > MORPHINE > Demerol (1/10th)

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14
Q

Main characteristics of Morphine

A
  • LEAST lipid soluble, low PB 30%
  • Morphine-6-glucoronide (650x more potent)
  • CI: asthma, MAOIs, RF
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15
Q

Morphine: DOA, E1/2t, Vd, Peak effects

A

Morphine:

  • DOA 3hrs
  • E1/2t 3-5hrs
  • Vd 4L/kg
  • IV peak 15-30
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16
Q

Morphine DOSE

A
  1. 5-15mg IV preop dose
  2. 01-0.02mg/kg

**Delayed resp del especially w/epidural & spinals

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17
Q

Meperidine unique MOA

A
  • Structure like atropine = antichol effects
  • Similar to LAs = bock Na channels
  • Alpha 2 agonist
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18
Q

What receptors are activated to dec shivering w/Meperidine?

A

↓ shivering = Kappa & alpha 2

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19
Q

Meperidine: DOA, E1/2t, Vd

A

DOA 3hrs
E1/2t 3-5hrs
Vd 4L/kg

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20
Q

Meperidine SE

A
  • Cardiac dep, tachy (catecholamine release)
  • Normeperidine = CNS stim, conf, hallucinations, myoclonus & seizures
  • Histamine release
21
Q

Which opiod has the lowest N/V profile?

A

Meperidine

22
Q

Which drugs do you avoid w/MAOIs?

A 
Morphine = ↓ metabolism
Meperidine = Fetal serotonin syndrome
23
Q

CI to Meperidine

A

ASTHMA
Renal Dz
Seizure hx
MAOIs

24
Q

Which opiods inc ICP?

A

Fentanyl & Alfentanil

25
Q

Which opiods do you avoid in asthmatics?

A

Morphine & meperidine = histamine release

Sufentanil = resp dep, bronchospasm, apnea

26
Q

Which opiods have a secondary peak effects & wooden chest syndrome?

A

Fentanil & sufentanil

27
Q

Which opiods cause SOO spasm?

A

Alfentanil & Remifentanil

28
Q

Fentanyl: DOA, E1/2t, Vd

A

DOA 1hr
E1/2t 3-6hrs
Vd 4L/kg

29
Q

Sufentanil: DOA, E1/2t, Vd

A

DOA 30min
E1/2t 2.5hrs
Vd 3L/kg

30
Q

Alfentanil: DOA, E1/2t, Vd

A

DOA 30-60min
E1/2t 90min
Vd 0.4L/kg

31
Q

Remifentanil: DOA, E1/2t, Vd

A

DOA 10min
E1/2t 10min
Vd 0.4L/kg

32
Q

Which opiod is metabolized by plasma/tissue esterases?

A

Remifentanil

33
Q

Which opiod is MOST lipid soluble?

A

Sufentanil

34
Q

Which opiod has the highest non-ionized ratio?

A

Alfentanil (~90% nonionized = rapid onset)

35
Q

Which is the only opiod without an active metabolite?

A

Remifentanil

36
Q

Fentanyl DOSE

A
  • 25-100mcg (pre-med)
  • Titrate 25-50mcg
  • 1-3 mcg/kg (analgesia)

-0.01-0.05mcg/kg/min
Give 6mins before effect
*100x potent than morphine
>10mcg/kg = long acting – may not be able to extubated.

37
Q

Sufentanil DOSE

A
  • 0.1-0.3mcg/kg (bolus)
  • 1-2 mcg/kg minor, 2-8 mcg/kg mod, 8-50 mcg/kg sole anesth
  • 0.0015-0.01mcg/kg/min
  • 10x more potent fentanyl
  • 1000x more potent morphine
38
Q

Alfentanil DOSE

A
  • 10-20 mcg/kg 90 secs before noxious event
  • Infusion 0.25- 0.75 μg/kg/min
  • 1/5th potent of fentanyl
  • 10-20x more potent than morphine
39
Q

Remifentanil DOSE

A
  • 1-2mcg/kg over 60-90s ind infus
  • 0.05-0.25mcg/kg/min

Need additional post op pain med…should not be used alone bc will wake up in severe pain…fast wear off.
*100xmore potent than morphine

40
Q

Which opiods have the smallest Vd?

A

Alfentanil & remifentail 0.4L/kg

41
Q

Which opiod is ok to use in renal failure pts?

A

Fentanyl

42
Q

Agonist/antagonist MOA & uses

A
  • Mu antagonists & full or partial agonst @ kappa
  • Analgesia w/limited vent depression & low probability of dependence
  • SE simlar to opiods but may cause DYSPHORIA (kappa)
43
Q

What two drugs are mixed agonist/antagonists?

A

Nalbuphine (Nubain) & Butorphenol (Stadol)

44
Q

Nalbuphine (Nubain) MOA & uses

A
  • Works at kappa & sigma receptors
  • Antagonizes opiod-induced depression while maintaining anesthesia
  • Used in OB anesthesia, mild-mod pain
  • NO adverse CV problems
  • Reverses SOO spasms
45
Q

Butorphenol (Stadol) MOA & uses

A
  • Agonist @ kappa & weak antagoist or partial agonist @ Mu
  • 5x more potent than morphine for analgesia

-Used for nasal spray for migraines

46
Q

Nalaxone (Narcan) MOA & Uses

A
  • Pure, nonselective competitive opioid antagonist
  • Competitive inhibitor at Mu, Kapp, and delta
  • Blocks the receptor sites and reverses resp depression and analgesia

***Dose dep reversal of reps depression assoc w/opiod OD

47
Q

Nalaxone SE

A
  • *Can cross the placenta
  • Sympathomimetic response
  • HTN
  • Tachycardia
  • Arrhythmias
  • Rapid awakening
  • N/V
  • Severe Pain
  • Catech release = shunt all blood from periph and GI tract to central circulation – like huge fluid bolus – can give CHF and pulmonary edema
  • Seizures
48
Q

Opiod partial agonist

A

Buprenorphine

49
Q

CI to using Nalaxone

A
  • Patients with cardiac disease (CHF)/pulmonary edema
  • Opioid dependent patients
  • Pregnancy

Pharm Exam I (4 decks)

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