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Opiod Analgesics Flashcards

0
Q

What are receptors for endogenous opioids?

A

G-protein coupled receptors (metabotropic receptors)

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1
Q

What are the 3 families of endogenous opioids?

A

End with ‘INS’

  1. EnkephalINS
  2. EndorphINS
  3. DynorphINS

*our body makes these
DEE

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2
Q

What are the 3 classes of endogenous opioid receptors?

A
  1. Mu- Main one we will talk about
  2. Delta
  3. Kappa

MDK

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3
Q

What are the functions of MU receptor?

A
  • Supraspinal and Spinal analgesia
  • Sedation
  • inhibition of respiration
  • slowed GI
  • euphoria
  • physical dependence
  • hormone and neurotransmitter modulation
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4
Q

What is the main thing about opioids?

A

They inhibit neurotransmission

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5
Q

What receptor is on the POSTsynaptic?

A

MU

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6
Q

What receptors are on the PREsynaptic?

A

ALL: MU, KAPPA, DELTA

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7
Q

What happens if MU is located on the PREsynaptic?

A

It BLOCKS the ENTRY of CALCIUM, therefore preventing vesicle release (transmission)

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8
Q

What happens if MU is located on the POSTsynaptic?

A

It enhances K leaving the neuron causing the hyper polarization and making POSTsynaptic DIFFICULT .

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9
Q

What is pain perception perceived by?

A

Nociceptors

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10
Q

What can the body do if pain becomes too much?

A

It can inhibit it

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11
Q

What is the sedative effect?

A

It is a Supraspinal effect (stimulating descending pathway).

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12
Q

What neuron is controlling the DESCENDING pathway?

A

The GABA inhibitory neuron is controlling the decending pathway

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13
Q

What does the ascending signal pain signal cause?

A

It causes the release of opioids which stops GABA neuron leading to decending pathway signal transmission

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14
Q

What does SUPRASPINAL do?

A

It blocks inhibition of descending signal (it STOPs GABA action)

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15
Q

What does spinal do?

A

It blocks ASCENDING signal

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16
Q

What are the classes of opioids?

A
  1. Strong Agonist
  2. Mild/Moderate Agonist
  3. Opioid with mixed receptor action
  4. Antagonist (just blocks)
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17
Q

What is morphine isolated from?

A

Opium poppies

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18
Q

What drugs are semi-synthetic?

A
  • codeine
  • hydromorphone
  • oxycodone

CHO
*the rest are synthetic

19
Q

How does an agonist, partial agonist and antagonist look on a graph?

A

Agonist: same height as antagonist
Partial agonist: half the height of agonist and antagonist (has a ceiling effect)
Antagonist: as high as agonist but to the right of agonist curve

20
Q

What drugs are STRONG AGONIST ?

A
  1. Morphine
  2. Hydromorphine
  3. Methadone
  4. Meperidine
  5. Fentanyl
  6. Heroin

3M,2H, F

21
Q

What STRONG AGONIST drug has sustain release available?

22
Q

What STRONG AGOnIST is used in rotation with morphine due addiction effects/potential?

A

Hydromorphine

23
Q

What drug is a STRONG AGONIST that has bioavailability > than morphine, used for hard to treat pain, used in rotation with morphine AND hydromorphine, has a long 1/2 life (1-2 days) and used for detox and maintenance therapy for addicts?

24
What STRONG AGONIST drug has SIGNIFICANT antimuscarinic effects (seizures: caused by accumulation due to renal problems and tachycardia) BUT causes less respiratory depression than morphine?
Meperidine
25
What STRONG AGONIST drug is offered transdermal in order to avoid GI problems?
Fentanyl
26
What STRONG AGONIST is potent and fast acting?
Heroin
27
What drugs are MILD/MODERATE agonist?
1. Codeine 2. Oxycodone CO
28
What mild/moderate AGONIST is used in combination with NSAIDS(aspirin, acetaminophen, etc) BUT less potent than morphine?
Both codeine and oxycodone
29
What drug is a PARTIAL AGONIST?
Buprenorphine
30
What PARTIAL AGONIST drug is potent, long lasting MU partial agonist, used for detox and maintenance therapy for opioid addition?
Buprenorphine
31
What partial agonist drug is resistant to naloxone(an antagonist drug? Why?
Buprenorphine because it is slow to dissociate(detach) from receptors and therefore stay at the binding site longer. Also since it is partial agonist, it does NOT have a strong opioid effect.
32
What does the ATAGONIST drugs act on?
MU receptors ( but can reverse Kappa and Delta w low affinity)
33
Do Antagonist drugs have little effect on opioid naive patients?
Yes
34
How long does it take to reverse the effect of morphine treated patient?
It takes 1-3mins which precipitates withdrawal in addicts
35
What drugs are ATAGONIST drugs?
1. NALoXONE | 2. NALtreXONE
36
What ATAGONIST has poor oral efficacy, short duration of action,must give frequently or via IV and used in acute opioids overdose?
NALoXONE
37
What ATAGONIST is absorbed orally, has a rapid first pass effect, 1/2 life of 10hrs, used in maintenance therapy with addicts and and decrease alcohol cravings?
NALtreXONE
38
What are some CNS effects of opioids?
``` Analgesia Euphoria Sedation Respiratory depression Cough suppression Miosis (small pupil)- in ALL opioid users no matter tolerance Nausea and vomiting ```
39
What are some PNS effects of opioids?
``` cardiac GI Biliary tract Renal system Uterus Neuroedocrine Pruritus (rash?) ```
40
Are opioids good for constant or intermittent pain?
Constant pain (it reduces sensory and emotional pain)
41
When is important for this type of pain?
Evaluation and reevaluation
42
Is fixed interval or on demand administration good for cancer pain?
Fixed interval dosing
43
Does opioids cross placental barrier and cause infant depression?
Yes, also it may prolong labor, renal and biliary colic, acute pulmonary edema, cough suppression, diarrhea?, anesthesia
44
Main issues of opioids are?
Addiction, tolerance and dependence (occurs in a few hours)
45
What are 2 types of tolerance?
- cellular tolerance: causes withdrawal, body gets use to drug - pharmkinetic tolerance: body gets rid of it faster: 20% of cases
46
What are 2 types of dependence?
1. Psychological dependence: lead to addiction, thinking drug is necessary which causes abuse 2. Physical dependence: tolerance need to increase dose *Withdrawal=death

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