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CNS Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Mechanism of action of opioids

A

Act on mu, kappa & delta which are Gi protien-couples receptors in CNS & periphery
Act at afferent pain-conducting fibers (peripheral analgesia), spinal cord (spinal analgesia), brain (suoraspinal analgesia). Limbic system (euphoria & dec emotional response to pain)
At cellular level, inhibit Ca++ influx & release of excitatory NT presynaptically while stimulating K+ influx postsynaptically causing hyperpolarization.

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2
Q

The opioid partial agonist is ….., while the weak opioid analgesic is ……

A

Buorenorphine
Propoxyphene

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3
Q

…&…. are metabolized into morphine

A

Heroin,codeine

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4
Q

Mention uses of opioids

A

Analgesic
Anesthetic
Acute pulmonary edema in LVF following MI
Antitussive
Antidiarrheal

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5
Q

Mention analgesic uses of morphine

A

Chronic visceral pain
Postoperative/cancer pain
Acute trauma
MI

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6
Q

Mention the main effects of morphine

A

Analgesia, euphoria, sedation

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7
Q

Mention the inhibitory effects of morphine

A

Inhbits:
VMC, VD
Respiratory center, inc CO2 causing cerebral VD & inc intracranial tension
Cough center
Uterine tone
Thermoregulatory center

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8
Q

Enumerate stimulatory effects of morphine

A

Stimulate:
Occulomotor nucleus (miosis)
CTZ
Urinary & GIT walls, inc tone of sphincters (spasmogenic) & dec walls peristalsis
Histamine release

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9
Q

Mention the antitussive & antidiarrheal opioids

A

T: codeine, dextrimethorphan
D: loperamide, diphenoxylate

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10
Q

Mention the contraindications of morphine

A

Acute undiagnosed abdominal pain
Normal labour pain
Closed head injury
Biliary colic & enlarged prostate
Asthma
Extremes if age, hypothyroidism, liver dysfunction
Peptic ulcer

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11
Q

GR: Morphine is CI in normal labour pain

A

Because it causes uterine relaxation and can delay normal labour
Also can cross the placenta and cause respiratory center depression of the fetus keading to Asphyxia Neonatorum

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12
Q

GR: Morphine is CI in closed head injury

A

Because morphine may increase intracranial pressure and increase brain damage.

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13
Q

Mention uses of methadone

A
  1. Treatment of opioid addicts
  2. Analgesic in severe chronic pain
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14
Q

GR: methadone is used in Treatment of opioid addicts

A

Because it is orally active & long acting thus used to replace morphine/heroin. Its gradual withdrawal is associated with less severe & smoother withdrawal symptoms

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15
Q

Mention a sode effect specific to methadone

A

Prolong QT interval, inc risk of torsades de pointes

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16
Q

Enumerate differences between pethidine & morphine

A

Pethidine is:
1. Less constipating (short acting)
2. Less respiratory depression in newborn & does not delay labour
3. Atropine-like actions
4. Inc risk of convulsions in higher doses due to accumulation of toxic metabolite norpethidine (not used for more than 48 hrs)

17
Q

Mention a side effect specific to fentanyl

A

Chest wall rigidity, dec thoracic compliance & dec ventiallation with higher doses

18
Q

Uses of fentanyl

A

Analgesic in severe pain
Anaesthesia (preanesthetic medication & in CV surgery)
Conscious sedation, neurolepanalgesia, neurolepanaesthesia

19
Q

…..is more potent than fentanyl, while …..is ultra-short acting

A

Sufentanil
Remifentanil

20
Q

Mention the advantages & disadvtanges of tramadol

A

Adv: less constipation, respiratory depression & addiction
Dis: inc risk of convulsions

21
Q

Mention advantages of buprenorphine

A

Less addiction
Respiratory depression is not dose dependent due to ceiling effect but if it occurs more difficult to reverse due to higher receptor affinity

22
Q

Mention uses of partial agonists

A

Analgesic in severe pain
Alternative to methadone for treatment of opioid addict

23
Q

Discuss drug interactions of opioids

A
  1. Opioids + other CNS depressants = additive CNS depression
  2. Pethidine + MAOI = serotonin syndrome
  3. Pure + partial agonist = withdrawal symotoms & dec analgesic effect
24
Q

Treatment of acute morphine toxicity & signs of improvement

A

Support respiration
Naloxone (opioid antagonist)
Increase in respiratory rate & pupillary dilation

25
Q

Uses of naloxone & naltrexone

A
  1. Acute opioid toxicity, Asphyxia neonatorum
  2. Opioid & alcohola abuse
26
Q

When should naltrexone be given to addicts & why?

A

After full detoxification
To avoid precipitation of withdrawal syndrome

27
Q

List steps of treatment of addiction

A
  1. Symptomatic treatment (NSAIDs for pain, antiemetic)
  2. Sympatholytic e.g. clonidine
  3. Detoxification replace with methadone or buprenorphine then gradual withdrawal
  4. Maintenance with Naltrexone (block euphoria of opioids)

CNS Pharmacology (11 decks)

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