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Pharmacology term 3 > Opioid analgesics 3 > Flashcards

Opioid analgesics 3 Flashcards

1
Q

what is opium

A

Opium is an extract of the juice of the poppy (papawer somniferum) that contains morphine

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2
Q

opium is used for what?

A

Used for social and medicinal purposes for thousands of years produce euphoria, analgesia and sleep and to prevent diarrhoea

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3
Q

when opium was introduced what was the RoA and name

A

Orally as tincture of laudanum

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4
Q

List the types of opioid receptors

A
  1. Mu
  2. Delta
  3. Kappa
  4. NOP (originally referred to as opioid receptor like receptor 1 or ORL 1)
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5
Q

List 4 types of opium alkaloids

A
  1. Morphine
  2. Fentanyl
  3. Pethidine
  4. Tramadol
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6
Q

which opium alkaloids that produce the atypical agonist effect on opioid receptors

A

Tramadol

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7
Q

Explain the mechanism of action of opioids in the spinal cord

A
  1. Morphine and other opioid agonist activates presynaptic mu, gamma or k opioid receptors on primary afferent neurons.
  2. Thesereceptors are coupled negatively to adenylate cyclase (AC) via G proteins (G ai).
  3. Inhibition of cyclic adenosine monophosphate (cAMP) formation leads to opening of potassium channels and closing of calcium channels.
  4. G By subunits may also participate in the modulation of ion channels
  5. Potassium efflux causes membrane hyperpolarization
  6. The closing of calcium channels inhibits the release of neurotransmitters, such as substance P.
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8
Q

List the pharmacological effects of opioids

A
  1. Central nervous system effects
  2. Cardiovascular effects
  3. Gastrointestinal and biliary effects
  4. Genitourinary effects
  5. Neuroendocrine system effects
  6. Immune system effects
  7. Dermal effects
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9
Q

List the central nervous system effects of opioids

A

Analgesia
Dysphoria or euphoria
Inhibition of cough reflex
Miosis
Physical dependence
Respiratory depression
Sedation

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10
Q

Effect on midbrain dopaminergic, serotonergic and noradrenergic nuclei can causes what?

A

Sedation and euphoria, and many patient experience dysphoria after administration of opioids.

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11
Q

explain how miosis occur?

A

Miosis (constricted pupils) is produced by the direct stimulation of the Edinger-Westphal nucleus of the oculomotor nerve (cranial nerve III), which activates parasympathetic stimulation of the iris sphincter muscle. Because little or no tolerance develops to miosis, this sign can be diagnostic of an opioid overdose.

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12
Q

Cpdeine and other opioids (dextromethorphan) inhibits what?

A

Cough reflex at sites in the medulla where this reflex intergated.

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13
Q

list the cardiovascular effects of opioids

A
  • Decreased myocardial oxygen demand
  • Vasodilation and hypotension
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14
Q

explain the most prominent cardiovascular effects

A

The most prominent cardiovascular effect: vasodilation, which is partly caused by histamine release from mast cells in peripheral tissues.
Cause orthostatic hypotension from decreased peripheral resistance and a reduction in baroreceptor reflex activity.
In patients with coronary artery disease, the decreased peripheral resistance leads to a reduction of cardiac work and myocardial oxygen demand.

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15
Q

List the gastrointestinal, biliary, genitourinary effects

A
  • Nausea and vomiting (via central nervous system action)
  • Constipation (increased intestinal smooth muscle tone)
  • Increased biliary sphincter tone and pressure
  • Increased bladder sphincter tone: Urinary retention
  • Prolongation of labour
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16
Q

List the neuroendocrine system effects

A

Neuroendocrine System Effects
* Inhibition of release of luteinizing hormone
* Stimulation of release of antidiuretic hormone and prolactin

17
Q

List the immune system effects

A

Immune System Effects
* Suppression of function of natural killer cells

18
Q

List the dermal effects

A

Dermal Effects
* Flushing
* Pruritus
* Urticaria (hives) or other rash

19
Q

List the major adverse effects of opioids

A
  • Major adverse effect: respiratory depression, usually the cause of death in severe overdoses. Increase in cerebral blood flow leading to increased intracranial pressure, opioids should not be used in the case of a closed-head injury. Rapidly reversed by the intravenous
    administration of an opioid antagonist such as naloxone.
  • Nausea and vomiting (stimulating the CTZ in the medulla and increase the sensitivity of the vestibular organ of the inner ear)
  • Histamine release = itching and flushing reaction (redness and a feeling of warmth over the upper torso)
  • Allergic reactions uncommon. Substitute with opioid from a different chemical class
20
Q

RoA for morphine

A

Oral or parenteral

Pharmacology term 3 (6 decks)

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