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Pharm - AntiArrhythmic/Opiods > Pharmacology of Opiod Analgesics > Flashcards

Pharmacology of Opiod Analgesics Flashcards

1
Q

Analgesia meaning

A

> to block pain neurotransmission

> antinociception

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2
Q

Anesthesia meaning

A

> to block sensory neurotransmission

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3
Q

Nociception

A

> pain sensation

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4
Q

Allodynia meaning

A

> the difference in pain sensation of a hyperalgesia and a normal pain response

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5
Q

Functions of pain

A

> pain required for survival
pain dominates other systems; demands action/attention
requires proper threshold; threshold is adaptive

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6
Q

Functions of pain in terms of tissue damage

A

> cytokines and chemical mediators
increase vascularization
sensitize somatosensory nervous system
promote recovery

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7
Q

Functions of pain in terms of spontaneous and exaggerated pain

A

> no protective or reparative role
pain becomes the pathology
maladaptive

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8
Q

Descriptive terms of pain

A

> type, temporal features, intensity, location, quality, exacerbating/alleviating factors

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9
Q

Comorbidity of chronic pain

A 
> anxiety
> depression
> insomnia/disrupted sleep
> activation of glia
> hyperalgesia/allodynia
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10
Q

Pain transmission

A

> Periphery to spinal cord DRG/Posterior columns to central

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11
Q

Pain processing centers in the brain

A

> Go to the slide in the packet…NOW

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12
Q

Supraspinal opioid circuit

A

> PAG and RVM modifying factors to suppress the sensation of pain

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13
Q

Two types of alkaloids in opium

A

> Phenanthrenes: Morphine, Codeine, Thebaine

> Benzylisoquinolines: Noscapine, Papaverine

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14
Q

Mu opioid receptor Phenanthrenes

A

> Morphine, Hydrocodone, Buprenorphine, Naloxone

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15
Q

Mu opioid receptor non-phenanthrenes

A

> Tramadol, Meperidine, Fentanyl, Methadone

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16
Q

Metabolism of Phenanthrenes

A

> Glucuronidation at 3’ and 6’ position

> Morphine-6-glucuronide still active

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17
Q

Liver metabolism of Phenanthrenes

A

> CYP2D6
alcohol co-ingestion can increase serum levels
elimination T1/2 increased with liver disease

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18
Q

Excretion of Phenanthrenes

A

> glomerular filtration

> 90% excreted in 24hr

19
Q

Opioid receptors type

A

> G protein coupled receptor - inhibition of cAMP
Mu
Kappa
Delta
Orphanin FQ receptor
Sigma receptor - not an opioid receptor

20
Q

Mu opioid receptor agonists

A

> Beta endorphins endogenous morphine: POMC
Therapeutic target: Analgesia due to cancer, peripheral, PCA
sedation
antitussive

21
Q

Side effects of mu opioid receptor agonists

A 
> respiratory depression
> constipation
> pruritis
> tolerance/dependance
> urinary retention via ADH
> nausea/vomiting
> muscle rigidity
> miosis
> contraction of biliary tract SMC
22
Q

Kappa opioid receptor agonists

A

> Dynorphins endogenous
potential use for treatment of addiction
counterbalance mu opioid receptor effects
salvia contains KOR agonist, salivinorin A

23
Q

Delta opioid receptor agonists

A

> enkephalins endogenous
dynamic expressions
role in hypoxia/ischemia/stroke/hibernation
anxiety/depression/alcoholism/hyperalgesia

24
Q

Action of opioid receptor signal transduction

A

> G-protein inhibiting Adenylyl cyclase: cAMP(D), intracellular Ca2+(D), release of NT(D)
Adenylyl cyclase activates K+ channel: hyperpolarization due to K efflux

25
Q

Synaptic action of opioid receptors

A

> presynaptic: inhibit calcium channel(Gi) decreasing in NT release
postsynaptic: activate GIRK channel increasing K efflux resulting in hyperpolarization

26
Q

Opioid agonists

A 
> sufentanil
> remifentanyl
> fentanyl
> hydromorphone(Dilaudid)
> morphine
> hydrocodone
> oxycodone
27
Q

clinical use of meperidine/demerol

A

> treat rigors

> neurotoxic: nervousness, tremors, fasciculations, seizure

28
Q

clinical use of tramadol/ultram

A

> painkiller used when stronger not preferred

> schedule IV

29
Q

clinical use of loperamide/imodium

A

> used as antidiarrheal
PgP substrate so low BBB penetration
schedule V

30
Q

clinical use of propoxyphene/darvon

A

> withdrawn due to heart rhythm abnormalities

31
Q

tramadol/ultram & tapentadol/nucynta

A

> non phenanthrene
mild opiate analgesic
SNRI properties - stimulate serotonin release
mild neuropathic pain

32
Q

meperidine/demerol

A

> normeperidine - active metabolite - accumulate and cause CNS irritability and myoclonic seizures
renally excreted; dangerous in D renal function

33
Q

methadone

A 
> non phenanthrene
> opioid dependence
> t1/2 15-60hrs and fat soluble
> NMDA antagonist
> chronic pain
34
Q

levorphanol/phenanthrene

A 
> t1/2 16hr
> analgesic half life is shorter than serum half life
> accumulate
> NMDA antagonist
> neuropathic pain
35
Q

two drugs with NMDA action

A

methadone and levorphanol

36
Q

partial mu agonists

A

> buprenorphine
partial mu ag, weak k ag, delta antag
long acting, low tolerance/dependence/addiction

37
Q

partial mu antagonist

A

naloxone and naltrexone

38
Q

Opioid for surgery

A

> fentanyl, sufentanil, remifentanil

> fast onset and short duration

39
Q

Opioid for postop, epidural

A

> hydromorphone, morphine

> potent, longer half life than fentanyl

40
Q

opioid for management

A

> oxycodone, hydrocodone, oxycontin, zohydro

> oral bioavailability, longer half life than fentanyl

41
Q

opioid for terminal cancer pain

A

> morphine

> cost, history

42
Q

opioid for intolerance

A

> meperidine

> constipation less, risk of seizure and delirium

43
Q

pharmacokinetic profile of opioids

A

> IV, SC/IM, oral increasing Plasma concentration but decreasing half life

44
Q

Time course of opioids via IV

A

> hydromorphone, methadone, meperidine, morphine, sufentanil, fentanyl, alfentanil, remifentanil

Pharm - AntiArrhythmic/Opiods (4 decks)

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