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Pharm Drugs 1 > Opioids > Flashcards

Opioids Flashcards

1
Q

synthetic opioids

A

Moriphan- agonist/antagonist types (levorphenol, butorphenol)

Diphenyls- methadone

benzomorphans- (for vasodilation) - phenazocine, pentazocine

phenylpiperidines!!!!
- miperidine, fent, alfent, sufent, remifent

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2
Q

natural/ semisynthetics

A
  • morphine is natural

- heorin, hydromorphone, codeine semisynth.

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3
Q

opioid 4 classifications

A
  • agonist
  • partial agaonist
  • mixed agonist/ antagonist
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4
Q

mu 1

A 
SUPRASPINAL, spinal analgesia
euphoria
low abuse potential
miosis
bradycardia
hypothermia
urinary retention
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5
Q

mu 2

A

crappy side effects.

spinal analgesia
depression of ventilation
physical dependence
marked constipation

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6
Q

kappa

A 
supraspinal, spinal analgesia
dysphoria
sedation
low abuse potential
miosis
DIURESIS

***only dynorphins are agonists

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7
Q

delta

A 
supraspina, spinal analgesia
depression of ventilation
physical dependence
minimal consitpation
urinary retention

***only enkephalins work here

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8
Q

opioids MOA

A

GPCR
pre and post synaptic

1- increase K conductance
2- inactivate Ca++ Ch

  • decreases NT release
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9
Q

activation of receptors

A

1- directly decrease neurotransmission

2- inhibits release of excitatory neurotransmitters (substance P)

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10
Q

supraspinal analgesia

A

receptor activation in periaqueductal/ periventricular gray matter in brain

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11
Q

Spinal analgesia

A

receptor activation in cord and dorsal root ganglion, substantia gelatinosa (inhibit substance P)

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12
Q

opioid effects on skeletal muscle

A

rigidity.

  • constrition of laryngeal/pharyngeal muscles
  • decreased chest wall compliance (diff or impossible to bag)

inhibition of GABA, increase in Dopa.

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13
Q

lipid solubility and neuraxial effects

A
  • penetration into CSF depends on LS
  • highly LS will be limited in cephalad migration by uptake into the spinal cord (fentanyl)
  • less LS will remain in CSF for transfer to cephalic region (morphine)
  • more LS = faster vascular absorption from epidural space…. quicjer peak concentrations of opioid in the blood.
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14
Q

side effects of neuraxial opioids

A

pruritis is most common
n/v
ventilatory depression (rapid with lipophilic, delayed with less lipophilic 6-12 hrs—cant go home.)

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15
Q

morphine produces….

A

analgesia, euphoria, sedation, nausea, pruritis, dry mouth, HISTAMINE, ventilatory depression

bradycardia, SA node inhibition

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16
Q

meperidine (demerol) produces…

A
  • sodium channel inhibiton (like LAs)
  • ALPHA 2 agonist effects

euphoria, sedation, analgesia

17
Q

morphine peak effects IM/IV, DOA

A

IM 45 min
IV 15-30 min

DOA 4 hrs

18
Q

meperidine DOA

A

2-4 hrs

19
Q

hydromorphone

A

5x more potent than morphine (derivative)
rapid elimination/redistribution
Q4 dosing needed!!!

20
Q

Fentanyl plasma concentration

A
  • does not decrease rapidly and is prolonged by second peak effects.
    (immobilization of sequestered drug from inactive tissue sites)
  • accumulation
  • especially affected by multiple doses or infusion*
  • large Vd
21
Q

Fentanyl uses

A
  • analgesic adjunct
  • adjuvant to blunt stimulation of incision, DL
  • as sole anesthetic in large doses d/t hemodynamic stability
22
Q

Sufentanil uses

A

adjunct for surgery and induction

infusion for outpatient surgery

23
Q

Sufentanil compared to fent/morphine

A

quicker induction
earlier emergence
earlier extubation

24
Q

Alfentanil uses

A
  • useful for blunting hemodynamic response (esp increased HR) to noxious stimuli
  • rapid effect
  • infusion for outpatient surgery (quick off)
25
Q

remifentanyl unique characteristics

A
  • ester linkage
  • metabolism by tissue/plasma esterases (not pseudocholinesterases)
  • minimal accumulation in tissues, even with infusion
26
Q

remifentanyl uses

A

blunt noxious stimuli

infusion for intermediate- long surgeries where rapid recovery is desired—- neurosurgical, O/P

27
Q

agonist/antagonist qualities

A
  • mu antagonist/partial agonist
  • kappa partial agonist

yield= analgesia with limited ventilatory depression and low probability of dependence

  • side effects similar to opioids (HD stable, skeletal muscle, urinary urgency, constipation, pruritis, N/V)
  • dysphoria at Kappa
28
Q

Nalbuphine (Nubain)

A
  • same analgesia as morphine, antagonizes respiratory effects
  • no CV effects
  • agonist at Kappa
  • reverses spasm of sphincter of oddi (intraop use)
29
Q

Butorphenol (Stadol)

A
  • agonist at kappa
  • weak antagonist/partial agonist at Mu
  • 5x more potant than morphine analgesia
  • nasal spray for migraines
30
Q

Naloxone

A
  • pure opioid antagonist
  • blocks sites, revereses respiratory depression, analgesia
  • COMPETITIVE at mu, kappa, delta
  • shorter DOA
  • titratable
  • onset 1-2 mins
  • dose-dependent reversal
31
Q

Naloxone Side Effects

A
  • tachycardia
  • HTN
  • Vent Dysrhythmias
  • severe pain
  • pulmonary edema!!!! — underlying CV disease or in healthy patients d/t catecholamine release.
32
Q

meperidine dose

A

50-100 mg IV

this drug is not always effective in patients with severe pain

33
Q

fent dose

A

1-3 mcg/kg

0.01 to 0.05 mcg/kg/min

34
Q

remifentanil dose

A

1-2 mcg/kg

0.05- 0.25 mcg/kg/min

35
Q

alfentanil dose

A

10-20 mcg/kg

0.25- 0.75 mcg/kg/min

36
Q

sufentanil dose

A

0.1-0.3 mcg/kg

.0015- 0.01 mcg/kg/min

Pharm Drugs 1 (5 decks)

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