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Pharmacology > Analgesic Drugs > Flashcards

Analgesic Drugs Flashcards

1
Q

Nociception

A

“Detection of noxious stimuli or stimuli that are capable of damaging tissue”

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2
Q

4 pain processes

A

Transduction: damage has happened, to primary afferent nociceptor
Transmission: primary afferent nociceptor to spinal cord
Modulation: can interrupt the pain pathway and cause less pain
Perception: brain receives stimulus and makes you consciously aware of the pain

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3
Q

Nociceptive stimulus causes what type of pain?

A

Acute pain

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4
Q

Neuropathic Pain

A
  • “pain induced by injury to or disease of the somatosensory system”
  • develops slowly, outlasts healing of original injury
  • allodynia, hyperalgesia, causalgia (burning)
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5
Q

Analgesic Drugs

A

Selectively blocks the sensation of pain without blocking other symptoms or loss of consciousness

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6
Q

Anesthetic

A
  • Local anaesthetic blocks nerve conduction and all local sensations (including pain)
  • General anaesthetics cause loss of sensations and unconsciousness
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7
Q

Opioids

A
  1. Higher centres of CNS
    - Pain can still be felt but produces less suffering
    - During perception
  2. Reduces neurotransmitter released from terminals pain fibres in dorsal horn of spinal cord
    - During modulation

Bind to opioid receptors
All opioid analgesics are full agonists or partial agonists at receptors

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8
Q

Opiate

A

Any drug derived from opium

  • Morphine
  • Codeine
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9
Q

Opioid Receptors

A

mu receptors
- Analgesia

kappa receptors

  • Analgesia
  • Dysphoria and hallucinations
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10
Q

Pharmacological Properties of Opioids

A
  1. Analgesia (u and k)
  2. Sedation and Mental clouding
  3. Euphoria and Tranquility (u and k)
  4. Antitussive
  5. Depression of Respiratory Centre (u)
  6. Nausea, vomiting
  7. Miosis - pin-point pupil (u and k)
  8. tolerance and serious dependence (u)
  9. Constipation (u and S)
  10. Postural hypotension
  11. Dilation of cutaneous bv (warm skin)
  12. Urinary urgency but difficulty in urination
  13. Biliary colic and epigastric distress
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11
Q

Examples of Opioids

A 
Heroin (diamorphine)
Morphine
Methadone (longer action than morphine)
Fentanyl
Codeine
Oxycodone
Loperamide (Imodium – no CNS action)
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12
Q

Opioid Analgesics - Indications

A

Main - To alleviate mild to moderate to severe pain
- Often given with adjuvant analgesic agents to assist with pain relief

Also used for

  • cough suppression (codeine)
  • treatment of diarrhea (loperamide)
  • balance anaesthesia (fentanyl)
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13
Q

Morphine

A

*Morphine sulfate

  • Acute and chronic pain - less effective in neuropathic pain
  • “The standard” for drugs
  • Primarily affects mu opoiid receptor
  • t 1/2 = 2-4 hours

Extensive liver metabolism

  • Inactivation
  • First pass metabolism
  • IV is 3-4x more effective than po

Pregnancy/breast feeding

  • Risk for physical dependence
  • Crosses placenta
  • Enters breast milk
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14
Q

Analgesics and Cancer Pain

A

Chronic pain

  • requires fixed schedule around-the-clock treatment
  • opioids, NSAIDs, adjuvants
  • eg. morphine sulphate (MS) Contin

Breakthrough pain

  • transient episodes of pain while chronic pain is controlled
  • access to rescue medication
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15
Q

WHO Pain Management Ladder

A
  1. Non-opioid + Adjuvant
  2. Opioid for mild to moderate pain + non-opioid + adjuvant
  3. Opioid for moderate to severe pain + non-opioid + adjuvant
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16
Q

NSAID’s and Adjuvant - Cancer Pain

A

NSAID
- the most common non-narcotic analgesic

Adjuvants

  • antidepressants eg. amitriptyline (Elavil)
  • antiseizure drugs eg. carbamazepine
  • glucocorticoids
17
Q

Morphine - Contraindicaitons

A
  • Known drug allergy, hepatic dysfunction
  • Severe asthma or other respiratory insufficiency
  • Respiratory depression
  • Elevated intracranial pressure (ICP)
  • Pregnancy
18
Q

Opioid Analgesics - Adverse

A 
Main
- Respiratory Depression
- CNS depression with possible coma
- Nausea and vomiting (1-3 days)
- Constipation - no tolerance development 
\_\_
- Hypotension
- Histamine release
- Urinary retention
- Diaphoresis and flushing
- Pupil constriction (miosis)
19
Q

Opioid Analgesics - Interactions

A

CNS depressants have cumulative effects

  • eg. antipsycotics, sedatives, (benzodiazepines, barbiturates)
  • ethanol
20
Q

Codeine

A

Moderate Opioid Analgesics

  • Less analgesia and respiratory depression
  • Less metabolism to morphine (~10% of oral dose)
  • Antitussive
  • Often combined acetaminophen in T1, T2, T3
  • Acetylsalicylic acid in 222’s or 292
21
Q

Oxycodone

A 
Moderate Opioid Agonists 
 Oxycontin or Percodan
- metabolism required for activation
- similar to codeine effect
- abuse potential
- widely used with acetaminophen (Percocet)
22
Q

Naloxone

A

Opioid Antagonists
Narcan, naltrexone
Antagonistic

Used for complete or partial reversal of opioid-induced respiratory depression

Shorter half life than other opioids (1-2 hours)

23
Q

Opioid Analgesic - Implications

A

Oral forms should be taken with food to lessen gastric upset
- Withhold dose if respiratory rate is less than 12 breaths/minute

Constipation:

  • Should take with adequate fluid and fibre intake
  • Usually stool softener (docusate) used daily when started on codeine

Orthostatic Hypotension

Pharmacology (29 decks)

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