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Pharm Block 4 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Receptor subtypes

A

Mu receptors: Mu1 and Mu2
Kappa receptors: Kappa1, Kappa 2, Kappa3
Delta receptors: Delta1 and Delta 2

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2
Q

Endogenous opioids

A

Pro-opiomelanocortin peptides: Beta-endorphin
Pro-enkephalin peptides: met-enkephalin peptides, leu-enkephalin
Prodynorphin peptides: Dyn-A, Dyn-B, and alpha-neo-endorphin
Endomorphins: Endomorphin-1 and Endomorphin-2
Nociceptin (orphinan F/Q)

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3
Q

Opioid receptors, endogenous ligands and function

A

Mu receptors: Mu1: Beta endorphin, endomorphin, leu-enkephalin
Mu2: Beta-endorphin, endomorphin
Kappa receptors: Kappa1: dynorphins, Beta-endorphin
Kappa2/3:dynorphins, nociceptin
Delta receptors: Delta1: enkephalins, Beta-endorphin dynorphins
Delta2:enkephalins, Beta-endorphin

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4
Q

Cloned Opioid receptors

A

MOR, DOR, KOR
7 transmembrane domains
G-protein linked (Gi or Gs) to adenyl cyclase or potassium channels (GIRKs)

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5
Q

In vivo assays

A
  1. Analgesic properties
  2. Reinforcing properties
  3. Stimulus properties
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6
Q

Analgesic assays

A

Thermal simuli
Tactile stimuli
Inflammation
Neuropathy

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7
Q

Reinforcing properties

A

Self-administration

Conditional Place Preference

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8
Q

Stimulus properties

A

Discrimination tasks

Addiction research center inventory

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9
Q

Desirable properties of morphine as an analgesic

A

Effective over a wide range of doses
Effect on mood
Sedation

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10
Q

Undesirable properties of morphine

A

Sedation, mental clouding, Dysphoria, constipation, dizziness/circulatory depression, N/V, respiratory depression, cough reflex depression, miosis, pruritis and rash, biliary tract spasms, ureter and vesical spasms, urinary retention, behavioral dependence, physical dependence, tolerance, sexual dysfunction

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11
Q

Tolerance

A

Associative or behavioral tolerance, nonassociative or pharmacologic tolerance, cross-tolerance, intrinsic efficacy, may affect development of tolerance and cross-tolerance

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12
Q

Multiple sites of action

A

Dorsal horn of the spinal cord
Activate descending inhibitory system
peripheral receptors

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13
Q

Morphine uses

A

Acute and chronic moderate to severe pain
-surgical
-postsurgical
-cancer
Often less effective for neuropathic pain

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14
Q

Morphine contraindications

A 
asthma, COPD, apnea, or other breathing disorders
liver or kidney disease
underactive thyroid
curvature of the spine with respiratory compromise
a history of head injury or brain tumor
epilepsy or other seizure disorder
low blood pressure
gallbladder disease
Addison's disease or other adrenal disorders
enlarged prostate, urination problems
mental illness
a history of drug or alcohol addiction
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15
Q

Metabolism of morphine

A

Morphine-3beta-glucuronide (inactive)
Morphine-6beta-glucuronide (active)
Accumulate in patients with renal damage

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16
Q

Heroin

A

Crosses BBB more rapidly than morphine

converted to morphine

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17
Q

Hydromorphine

A

About 8-10X potency of morphine
slightly shorter duration than morphine
available as suppository

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18
Q

Oxymorphine

A

same as hydromorphine

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19
Q

Codeine (methylmorphine)

A

About 1/10th the potency of morphine
lower efficacy than morphine
about 10% converted to morphine by CYP 2D6
67 allelic variants. 7-10% of patients are poor metabolizers
small population of northern Pacific islanders are “super metabolizers”

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20
Q

CYP2D6

A

Allelic variation in this makes a patient a poor metabolizer and the drug doesn’t work well

21
Q

Oxycodone

A

About 10 times potency of codeine
Also metabolized by CYP2D6, but has efficacy on its own
Controlled release formulation (Oxycontin)
Targin (oxycodone+naloxone)

22
Q

Hydrocodone (Dicodid and others) and dihydrocodeine

A

Same as oxycodone
Extended release formulation now also available (Zohydro)
Abuse deterrents

23
Q

Mixtures containing Codeine, hydrocodone, dihydrocodeine, or oxycodone

A

Acetaminophen or NSAIDS

Logic: additive or synergistic analgesia without concomitant increase in adverse effects

24
Q

Synthetic compounds

A 
Meperidine
Fentanyl, Sufentanyl, Alfentanyl, Remifentanyl
Methadone
L-alpha-acetyl-mathadol:LAAM
Propoxyphene
25
Q

Meperidine

A 
About 1/8th potency of morphine
Shorter duration
No miosis
biotransformed to a toxic metabolite that builds up and can cause seizures
synergistic with gila monster venom
26
Q

Fentanyl

A 
80--100X potency of morphine
fast onset, short duration
used iv for anesthesia
available as patch
available as oral slow release device
27
Q

Fentanyl derivative

A

Alfentanil, Sufentanil, Remifentanil, carfentanil, lofentanil

28
Q

Methadone

A

Potency is similar to morphine for iv administration, but 4 times more potent orally
long plasma half life
used in treatment of narcotic dependence
Duration of action increases with repeated use

29
Q

Individual differences in response to mu opioid receptor agonists

A

Pharmacokinetic differences: metabolism CYP2D6, excretion of active metabolites
Pharmacodynamic differences: Multiple MOR splice variants

30
Q

Opioid antagonists

A

Naloxone
Naltrexone
Nalmefene
Methyl naltrexone

31
Q

Signs of overdose

A 
Stuporous or in coma
Respiratory rate extremely low
pinpoint pupils
low body temperature
flacid skeletal muscles, jaw relaxed
32
Q

Naloxone

A

Short half-life

Nor effective orally

33
Q

Naltrexone

A 
Long half life
effective orally or injected
available in oral form only
used for treatment of dependence
can produce hepatotoxicity with long term use
34
Q

Nalmefene

A

Intermediate duration (8-12 hr)
orally active
no hepatotoxicity with long term use
used for treatment of alcohol dependence

35
Q

Methylnaltrexone

A

Quaternary form of drug does not cross BBB

Used to treat opioid-induced constipation

36
Q

Naloxegol

A 
PEGylated naloxol (polymer opioid antagonist); does not cross BBB
Used to treat opioid-induced constipation
37
Q

Mixed agonist-antagonist

A

Nalorphine and cyclazocine
Pentazocine: Talwin
Butorphanol
Nalbuphine

38
Q

Nalophine and Cyclazocine

A

Kappa3 receptor agaonist
Mu receptor antagonists
Produce psychotomimetic effects
produce dysphoria

39
Q

Pentazocine

A

Kappa and delta agonist
‘Ts and blues’
Talwin NX

40
Q

Butorphanol

A 
Kappa recptor agonist
Mu receptor antagonist
Available as nasal spray
5 X more efficacious in women than men
Could be due to melanocortin-1 receptor gene, regulated by LH
41
Q

Nalbuphine

A 
Kappa receptor agonist
Mu reeptor antagonist
Little dysphoria compared to nalorphine
less abuse potential than morphine
frequently used in ambulances
42
Q

Partial agonist: Buprenorphine

A 
Partial agonist at mu receptors
Partial agonist at Kappa3 receptors
Lower efficacy analgesic than morphine
Buprenophine+naloxone
Depo buprenorphine
43
Q

Tramadol

A

Opioid receptor agonist (mu and delta)
NE and 5-HT reuptake blocker (antidepressant)
alpha-2 adrenoceptor agonist
These actions are synergistic for analgesia

44
Q

Tapentadol

A

Opioid receptor agonist (mu and delta)
NE reuptake blocker (antidepressant)
These actions are synergistic for analgesia

45
Q

Dependence and WIthdrawal

A

Dependence varies from mild cravinf to compulsion to take the drug
Degree depends on dose and frequency
Withdrawal signs opposite in direction to drug effects
Will last about 72 hours for morphine and heroin
Not life threatening

46
Q

Other factors that infuence the effectiveness of opioid treatment

A

Progression of tissue-damging disease
Sensitization of CNS neurons
Collateral transmission

47
Q

Salvinorin A

A

Active ingredient in Salvia Divinorum
Very selective kappa opioid agonist
Hallucinogen

48
Q

Krokodil

A

Desomorphine
Synthesized from codeine
Heroin-like high, but rapid kinetics
chronic use produces tissue damage, phlebitis and gangrene

Pharm Block 4 (2 decks)

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