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Ph 4 > Opiod Analgesics > Flashcards

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?

A

Morphine

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?

A

Methadone

24
Q

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?

A

Meperidine

25
Q

What STRONG AGONIST drug is offered transdermal in order to avoid GI problems?

A

Fentanyl

26
Q

What STRONG AGONIST is potent and fast acting?

A

Heroin

27
Q

What drugs are MILD/MODERATE agonist?

A
  1. Codeine
  2. Oxycodone

CO

28
Q

What mild/moderate AGONIST is used in combination with NSAIDS(aspirin, acetaminophen, etc) BUT less potent than morphine?

A

Both codeine and oxycodone

29
Q

What drug is a PARTIAL AGONIST?

A

Buprenorphine

30
Q

What PARTIAL AGONIST drug is potent, long lasting MU partial agonist, used for detox and maintenance therapy for opioid addition?

A

Buprenorphine

31
Q

What partial agonist drug is resistant to naloxone(an antagonist drug? Why?

A

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
Q

What does the ATAGONIST drugs act on?

A

MU receptors ( but can reverse Kappa and Delta w low affinity)

33
Q

Do Antagonist drugs have little effect on opioid naive patients?

A

Yes

34
Q

How long does it take to reverse the effect of morphine treated patient?

A

It takes 1-3mins which precipitates withdrawal in addicts

35
Q

What drugs are ATAGONIST drugs?

A
  1. NALoXONE

2. NALtreXONE

36
Q

What ATAGONIST has poor oral efficacy, short duration of action,must give frequently or via IV and used in acute opioids overdose?

A

NALoXONE

37
Q

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?

A

NALtreXONE

38
Q

What are some CNS effects of opioids?

A 
Analgesia
Euphoria
Sedation
Respiratory depression
Cough suppression 
Miosis (small pupil)- in ALL opioid users no matter tolerance
Nausea and vomiting
39
Q

What are some PNS effects of opioids?

A 
cardiac
GI
Biliary tract 
Renal system
Uterus
Neuroedocrine
Pruritus (rash?)
40
Q

Are opioids good for constant or intermittent pain?

A

Constant pain (it reduces sensory and emotional pain)

41
Q

When is important for this type of pain?

A

Evaluation and reevaluation

42
Q

Is fixed interval or on demand administration good for cancer pain?

A

Fixed interval dosing

43
Q

Does opioids cross placental barrier and cause infant depression?

A

Yes, also it may prolong labor, renal and biliary colic, acute pulmonary edema, cough suppression, diarrhea?, anesthesia

44
Q

Main issues of opioids are?

A

Addiction, tolerance and dependence (occurs in a few hours)

45
Q

What are 2 types of tolerance?

A
  • cellular tolerance: causes withdrawal, body gets use to drug
  • pharmkinetic tolerance: body gets rid of it faster: 20% of cases
46
Q

What are 2 types of dependence?

A
  1. Psychological dependence: lead to addiction, thinking drug is necessary which causes abuse
  2. Physical dependence: tolerance need to increase dose

*Withdrawal=death

Ph 4 (7 decks)

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