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
What happens when codeine enters teh bodu
10-15% of codeine is converted to morphine by CYP2D6 (5-10% of ppl don't have this and wont work)
26
Heroine compared to morphine
Prodrug for mophine *very lipid solube due to rapid mvmt acrss BBB
27
Oxycodone bioavailability/potency vs morphine
``` better bioavailability (no first pass effect) twice as potent as morphine ```
28
Meperidine vs mophine
less potent than morphine and shorter half life
29
What is the toxic metabolite of meperidine and who should it not be given to
Has toxic metabolite normeperidine which is excreted renally (should not be given to those with renal probs or are taking monoamine oxidase inhibitors)
30
How much more potent is fetanyl compared to morphone
80x
31
Mathadone compared to morphine
similar potency to morphone but has higher bioavailability and longer half life- used for withdrawal tx
32
What is hydromorphone and action timeline
semi synthetic derivative of morphine | -onset of action of about 15 mins duration 5 hrs
33
What is tramadol a analogue of and what does it do at the synaptic cleft level
synthetic analoauge of codeine produces an increased level of serotonin and noradrenaline in synaptic clefs and decreases excitability of spinal pathways
34
what do combonation therapies overcome
ceiling effect