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therapeutics > Pharmacology of opiates/narcotics/benzodiazepines > Flashcards

Pharmacology of opiates/narcotics/benzodiazepines Flashcards

1
Q

What are the two types of alkaloids found in opium?

A

Phenanthrenes and Benzylisoquinolines.

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2
Q

Define ‘opiates’.

A

Opiates are only those opioids that are naturally occurring.

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3
Q

What are the types of opioid receptors?

A

G protein coupled, Mu (M) * Kappa (K) * Delta (D) * Nociceptin

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4
Q

What is the role of beta-endorphins?

A

They are endogenous morphines involved in analgesia, sedation and antitussive

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5
Q

True or False: Opioid-induced side effects are mostly off-target effects.

A

False. They are mostly on-target effects.

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6
Q

What is the pharmacokinetics of morphine in terms of bioavailability?

A

Morphine has a bioavailability of 25% due to first pass metabolism and is readily absorbed

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7
Q

What are the routes of administration for opioids?

A
  • Intravenous * Intra-axial (intrathecal, epidural) * Intramuscular * Oral * Topical/transdermal
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8
Q

What is the significance of CYP2D6 in opioid management?

A

Genetic differences in CYP2D6 impact opioid metabolism and therapeutic effects. UM vs PM

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9
Q

What is the unique characteristic of fentanyl compared to morphine?

A

Fentanyl is approximately 100 times more potent than morphine and 50x more potent then heroin

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10
Q

What is the mechanism of action for opioids at the mu receptor?

A

Inhibition of neurotransmitter release via Gi signaling.

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11
Q

What is the primary use of naloxone?

A

It is used as an opioid antagonist to reverse opioid overdoses.

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12
Q

Fill in the blank: Tapentadol has _______ properties.

A

SNRI

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13
Q

What is the common consequence of chronic opioid use regarding tolerance?

A

Patients develop tolerance to analgesic effects but not to side effects like constipation.

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14
Q

What is the mechanism of action for tramadol?

A

It acts as a weak mu agonist and has SNRI properties.

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15
Q

Fill in the blank: Opioid receptor signal transduction inhibits _______ channel activity which results in a decrease in neurotransmitter release

A

calcium

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16
Q

What is the primary concern with opioid use in patients with renal impairment?

A

Increased risk of accumulation and toxicity due to decreased excretion.

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17
Q

What are the side effects of opioid withdrawal?

A
  • Pain * Anxiety * Dysphoria * Insomnia
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18
Q

What is the significance of lipophilicity in opioid pharmacokinetics?

A

Influences the onset and duration of action across the blood-brain barrier.

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19
Q

What is the primary action of the (+) isomer in Methadone?

A

NMDA antagonist

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20
Q

What is the pharmacological classification of Buprenorphine?

A

Mu opioid receptor partial agonist used in opioid replacement therapy, also has antagonist properties and abuse potential

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21
Q

What effect does Buprenorphine have on full agonists like heroin?

A

Blocks full agonist effect

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22
Q

What is the oral bioavailability of Naltrexone?

A

Decent oral bioavailability administered PO

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23
Q

What is the administration method for Naloxone?

A

I.V. or intranasal (may need to repeat every 2-5 minutes)

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24
Q

What is the onset time for Naloxone’s effects?

A

rapid onset 1-2 minutes rapid onset

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25
What is the half-life of Naloxone?
30-90 minutes short half life (limited oral bioavailability)
26
True or False: Naloxone and Naltrexone are interchangeable.
False
27
What symptoms may indicate Neonatal Abstinence Syndrome?
* Tremors * Yawning * Poor Feeding * Sweating
28
What are the non-pharmacological treatments for Neonatal Abstinence Syndrome?
* Swaddling * Hypercaloric Formula * Frequent Feedings * Observation * Rehydration
29
What pharmacological treatment can be used for Neonatal Abstinence Syndrome?
* Morphine Sulfate * Sublingual Buprenorphine * Methadone * Clonidine Morphine and buprenorphine linked with shorter hospital stay than methadon
30
Which endogenous peptides have the highest affinity for µ (Mu) opioid receptors?
Endorphins
31
What are the effects of κ (Kappa) opioid receptor activation?
* Analgesia * Diuresis * Sedation * Dysphoria
32
What type of actions are associated with Orphanin opioid-receptor-like subtype 1 (ORL1)?
Opposes classic µ effects, mediates pain
33
What is the significance of the opioid antagonist Naloxone in emergency situations?
May require multiple doses to avoid return of respiratory depression
34
G protein-coupled receptor
 Family A – peptide receptors  Gi/o-coupled (inhibition of cAMP production)  Open GIRK potassium channels  Close calcium channels
35
In opioid signal transduction Postsynaptic = activate GIRK channel (Gβγ) which results in _______.
Efflux of K+ => hyperpolarization (less firing)
36
OPIOID INDUCED SIDE EFFECTs
Respiratory depression Constipation Pruritus (itch)- Side effect, not allergic response Addiction Urinary retention Nausea/vomiting Miosis
37
Kappa Opioid receptor
Dynorphins natural ligand Activation is dysphoric, aversive Potential use for treatment of addiction Reduce dopamine release Counterbalance mu opioid receptor effects
38
DELTA OPIOID RECEPTOR
Enkephalins are natural ligand More dynamic expression, Intracellular and “externalized” upon chronic stimuli  Role in hypoxia/ischemia/stroke  Reduce anxiety  Reduce depression  Treat alcoholism  Relief hyperalgesia, chronic pain  Side effect: seizures!  No FDA-approved delta opioids
39
T or F : the ventral tegmental area is a greater site for opioid action then the nucleus accumbens
T
40
How do depressants cause DA release like stimulants?
1. Opioid binds mu receptor 2. Gi signaling inhibits neurotransmitter release 3. Less GABA to activate GABAA 4. Less inhibition of dopamine neuron activity 5. Increase dopamine release 6. Increased activation of dopamine receptors
41
list the drugs used for tx of constipation
senna,polyethylene glycol and dioctyl sodium sulfosuccinate/doccusate
41
Morphine is a substrate of
CYP2D6, CYP3A4
42
List the opioids that are prodrugs
heroin codeine and tramadol
43
T or F: Fentanyl and methadone do produce active metabolites
False they do not
44
Which opioid is a NMDA receptor antagonist
Methadone (non phenanthrene)  Primarily used for opioid dependence  Long duration of action/long half life  Prolonged QTc
44
T or F Dextromethorphan has limited opioid activity
T
45
METHADONE
Full mu opioid receptor agonist  ‘Slow’ acting (2-4 hours)  Slow pharmacokinetics: Accumulates with repeated dose  Racemic mixture: (+) = NMDA antagonist
46
(Fill in the blank) 3 position substitutions of ether or ester will blank
decrease potency (codeine)
47
(Fill in the blank) 6 position will increase activity with blank or blank
hydromorphone or hydrocodone
48
T OR F: 14 position OH has increased potency
T (oxycodone)
49
list the non-phenanthrenes
tramadol,merperidine, fentanyl and methadone
50
list the precursor proteins that are cleaved into more opioid subtype selective peptides include
Pro -opiomelanocortin (POMC) Preproenkephalin Prodynorphin Nociceptin/Orphanin FQ
51
Pro -opiomelanocortin (POMC) is cleaved to form
B-endorphins which target Mu opioid
52
Preproenkephalin is cleaved to form
Leu-enkephalin which targets delta opioid Met-enkephalin which target the mu and delta receptors
53
Prodynorphin is cleaved to form
dynorphins which target the Kappa opioid
54
what is the endogenous opioid of Nociceptin orphanin FQ receptor
nociceptin
55
in opioid signal transduction Presynaptic = inhibit calcium channel (Gi) which results in _______.
a decrease in neurotransmitter release
56
list the agonists of opioid receptor
sufentanil,remifentanil,alfentanil, fentanyl,hydromorphone, morphine, and hydrocodone
56
Which opioids are used for cough/antitussive purposes
Codeine and dextromethorphan
57
which opioid can be used as anti-diarrheal tx
diphenoxylate with atropine, loperamide, and eluxadoline
58
which opioids act at MOR and KOR
Pentazocine and Butorphanol Nalbuphine Buprenorphine

therapeutics (31 decks)

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