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PA 2307- Mod 8 > Opiods! > Flashcards

Opiods! Flashcards

1
Q

what is chronic pain

A

longer than 6 m

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2
Q

nociceptor vs neuropathic pain

A

nociceptor- pain from tissue injury may cause somatic pain/ visceral pain (generalized/dull)

Neuropathic- Pain that is usually described as burning/shooting/tingling/pins/needles

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3
Q

What are the mediators to fever

A

Lipopolysaccharides

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4
Q

What is released in the imflammatory process (5)

A 
Protaglandins
5-HT
Leukotriens
Histamines
Bradykinin
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5
Q

What plant is the opiote derived from

A

Papaver Somniferum

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6
Q

What are the phenanthrene alkaloids (3) and effects

A

Morpine, codeine, thebaine

Algesic, euphoric, central nervous system depressent

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7
Q

What is the benzylisoquinoline alkaloid and effects

A

Papaverine

-smooth mm relaxant causing dilation of peripheral arterioles

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8
Q

What are the 3 major receptoes for opiods

A

Mu
Kappa (more hallucinagens than mu)
Delta

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9
Q

What type of channel are the opiod receptors

A

G pro coupled

-activates pottasium currents or decreased voltage gated calcium current or inhibition of adenyly cyclase

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10
Q

Where are the opiod receptors mainly found

A

spinal cord and brain in association w neurons that modulate pain perceptopn

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11
Q

What does the mu receptor do compared to the delta and kappa

A

Mu- most of the algesia

Delta/Kappa- Contribute to analgesia at the spinal level

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12
Q

3 main effects on the cell of opiotes

A

Hyperpolarize cell to decrease firing ( open K channels)

Close Ca channels (decreased nt release)

Endorphone autoreceptors decrease release of cells nts

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13
Q

Main major effects of opiots

A 
Analgesia- better pain tolerance
Sedation
Miosis (constricted pupils)
Respiratory depresion (decreasing sensitivity of the respiratory center in medulla to CO2)
Antitissive (anti cough)
\+ neusa/vommiting
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14
Q

How does opiotes affect the GIT

A
  • billiary and bladder sphinchters contract

- depressed peristalsis–> constipation

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15
Q

What does opiotes do to histamine

A

causes release

–causes peripheral vessels to dialate, decrease blood pressure causing hypotennsion

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16
Q

What is poikilothermia and what is it associated w

A

opiote use

  • inhibit thermoregulatory mechanism in the hypothalamus ( unable to maintain a constant body temp)
  • -excessive heat loss
17
Q

What does widthdawl from opiotes cause

A 
restlessness
anxiety
vomiting
diarrhea
pupil dialation
chills
18
Q

What % of orla dose of opiods reach systemic circulation and how much larger should it be than an iv dose

A

15-30%

morphine oral dose should be 5-6x higher

19
Q

What opiotes are less susseptible to first pass metabolism

A

Codeine and oxycodone

20
Q

At plasma PH what happens to opiotes and how does it affect distribution

A

is ionized therefore limiting CNS distribution and absorption in GIT

21
Q

How quick is teh onset of opiods after IM injection

A

10-20 mins

22
Q

How is mophine metabolized in liver, half life and metabolism

A

Highly metabolized in the liver via hydroxylation + glucurondation (phase I + II)
-half life is 1.5-4 hrs

90% is excreted in urine, 10% in bile

23
Q

What is the metabolite of opium and characteristics

A

morphine 6b glucuronide- longer half life and is more potent

24
Q

What receptor does morphine work on

A

full mu antagonist ( produces both supraspinal and spinal level analgesia)

25
Q

What happens when codeine enters teh bodu

A

10-15% of codeine is converted to morphine by CYP2D6 (5-10% of ppl don’t have this and wont work)

26
Q

Heroine compared to morphine

A

Prodrug for mophine

*very lipid solube due to rapid mvmt acrss BBB

27
Q

Oxycodone bioavailability/potency vs morphine

A 
better bioavailability (no first pass effect)
twice as potent as morphine
28
Q

Meperidine vs mophine

A

less potent than morphine and shorter half life

29
Q

What is the toxic metabolite of meperidine and who should it not be given to

A

Has toxic metabolite normeperidine which is excreted renally (should not be given to those with renal probs or are taking monoamine oxidase inhibitors)

30
Q

How much more potent is fetanyl compared to morphone

A

80x

31
Q

Mathadone compared to morphine

A

similar potency to morphone but has higher bioavailability and longer half life- used for withdrawal tx

32
Q

What is hydromorphone and action timeline

A

semi synthetic derivative of morphine

-onset of action of about 15 mins duration 5 hrs

33
Q

What is tramadol a analogue of and what does it do at the synaptic cleft level

A

synthetic analoauge of codeine

produces an increased level of serotonin and noradrenaline in synaptic clefs and decreases excitability of spinal pathways

34
Q

what do combonation therapies overcome

A

ceiling effect

PA 2307- Mod 8 (8 decks)

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