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PHPY 305 > Narcotics > Flashcards

Narcotics Flashcards

1
Q

Four steps of Pain

A
  1. Pain sensory fibres activated by noxious stimuli
  2. Release of pain mediators
  3. Binding of mediators to receptors
    - stimulate neurons that project to various areas of spinal cord and brain
  4. Sensation of pain
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2
Q

Pain mediators that promote pain

A

Substance P

Glutamate

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3
Q

Pain mediators that inhibit pain

A

Serotonin

Norepinephrine

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4
Q

Pain mechanism

A
  • noxious stimuli
  • propagation of action potential
  • Calcium channel opens
  • prompt release of pain mediators
  • pain mediators bind postsynaptic receptors
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5
Q

Endogenous Opioids found in the body

A

Beta-endorphin
Enkephalins
Dynorphin

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6
Q

Opioid Receptor subtypes

A

Mu, Kappa, Delta

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7
Q

Effects of Mu receptor subtype

A
  • analgesia
  • sedation and euphoria
  • inhibition of respiration
  • reduced GI peristalsis
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8
Q

Kappa and Delta subtype effects

A
  • Primarily analgesia

- most opioids are primarily Mu agonists

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9
Q

Mu agonists and analgesia

A
  • inhibition transmission of pain signals

- alter response to pain (in CNS, alter mood)

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10
Q

Opioid receptor mechanism

A
  1. Opioid binds to receptor (primarily Mu)
  2. Presynaptically inhibits Calcium channel opening
  3. Inhibits release of pain mediators
  4. Also inhibits post-synaptic response to pain mediators
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11
Q

Drug design includes (4)

A 
Full agonists (morphine)
Partial Agonists (buprenorphine)
Reuptake inhibitors (tramadol)
Antagonists (naloxone)
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12
Q

Opioid Routes of Administration

A
  • oral
  • buccal, sublingual
  • rectal
  • transdermal
  • inhaled
  • Parenteral (subcutaneous, intramuscular, intravenous)
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13
Q

Highly Potent Opioid

A

Fentanyl (100X morphine)

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14
Q

Intermediate potent Opioid

A

Morphine

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15
Q

Low potent opioid

A

Codeine (1/10th of morphine)

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16
Q

Three uses of Opioids

A 
Pain
- various forms of pain
Diarrhea 
- few are used as anti-diarrheals 
Cough
- Codeine is the opioid typically used for cough
17
Q

Opioid Pharmacokinetics

A

Some have active metabolites
- Codine -> CYP2D6 -> morphine
Are metabolized in the liver and Eli mated by kidney
Renal impairment can lead to accumulation of metabolites and toxicity

18
Q

Side Effects of Opioids

A
  • Nausea
  • Constipation
  • Sedation
  • Euphoria
  • Miosis
  • Respiratory depression
19
Q

Nausea Mechanism

A
  • Opioids stimulate the chemoreceptor trigger zone

- Anti-nauseants are used

20
Q

Constipation mechanism

A
  • stimulation of mu receptors in the gut

- slows peristalsis, reduces secretions

21
Q

Sedation Mechanism

A

Inhibits the reticular activation system in brain

22
Q

Euphoria

A

Occurs due to actions in the limbic region of the brain

23
Q

Miosis

A
  • Pinpoint pupils
  • likely parasympathetic effect
  • Can be used to confirm opioid use
24
Q

Respiratory Depression

A
  • Opioids attenuate CO2 sensors in respiratory centre
  • main cause of death with opioid toxicity
  • drug interaction with Benzodiazepines which also cause respiratory depression
25
Q

Opioid overdose treatment

A

Opioid antagonist Naloxone administered by injection

26
Q

Tolerance in Opioids (Pharmacokinetic and Pharmacodynamic)

A

Kinetic: enhanced ability to eliminate opioids
Dynamic: Reduction in the number of Mu receptors, increase the number of pain mediating receptors

27
Q

Heroin

A
  • associated with addiction
  • injected intravenously
  • highly lipophilic
  • relatively short duration of action (enhances withdrawal symptoms)
28
Q

Treatment for Opioid withdrawal

A

Methadone, administered orally and has a half life of 35 hours, causes less euphoria

29
Q

Opioid partial agonists

A

Buprenorphine

  • partial agonist at Mu receptors
  • antagonist at Kappa receptors
  • management of addiction (with naloxone)
  • moderate pain, chronic use
30
Q

Advantages of Partial over Full agonist

A
  • Safer in overdose (respiratory depression plateaus)

- Lower risk of abuse (euphoria plateaus)

31
Q

Opioid Reuptake inhibitors

A

Tramadol

  • Weak Mu agonist so less respiratory depression, constipation and less abuse potential
  • inhibits reuptake of serotonin and NE

PHPY 305 (14 decks)

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