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Pharm > 06b: Opioids > Flashcards

06b: Opioids Flashcards

1
Q

(Opium/opiate/opioid) is naturally occurring alkaloid.

A

Opiate

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2
Q

(Opium/opiate/opioid) is mixture of alkaloids from Papaver somniferum.

A

Opium

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3
Q

(Opium/opiate/opioid) is any natural or synthetic compound with morphine-like properties.

A

Opioid

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4
Q

Morphine falls into the category of (opium/opiate/opioid).

A

Opiate

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5
Q

Morphine is opioid receptor (agonist/antagonist). Give another example in this category.

A

Agonist;

Fentanyl

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6
Q

Buprenorphine is opioid receptor (agonist/antagonist).

A

Agonist-antagonist (binds multiple receptors)

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7
Q

Naloxone is opioid receptor (agonist/antagonist).

A

Antagonist

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8
Q

Morphine is (natural/synthetic), as is (heroin/codeine/fentanyl).

A

Natural; codeine

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9
Q

Methadone is (natural/synthetic), as is (heroin/codeine/fentanyl).

A

Synthetic;

Fentanyl

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10
Q

Most clinically important opioid analgesics are (selective/non-selective) (agonists/antagonists) to (X) receptor class. Give an example.

A

Selective; agonists;
X = mu (MOP)

Sufentanil

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11
Q

T/F: All opioid receptors are RTKs.

A

False - all GPCRs

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12
Q

Opioids generally work through which second-messenger pathway?

A

Go/Gi (inhibit AC, decrease cAMP)

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13
Q

Opioid effects: (vasoconstriction/vasodilation), (brady/tachy)-cardia, (miosis/mydriasis).

A

Vasodilation, bradychardia, miosis

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14
Q

Opioid effects: smooth muscle (X) and skeletal muscle (Y).

A 
X = spasm
Y = hypertonus (stiffness)
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15
Q

Opioid (mu) receptor class impacts (pre/post)-synaptic (afferent/efferent) neuron by (increasing/decreasing) Ca (uptake/release). What does this do?

A

Pre-synaptic; (primary) afferent
Decreasing uptake;

Decrease neurotransmitter release

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16
Q

Opioids decrease release of which NT from primary afferents?

A

Substance P, ACh, NE, SA

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17
Q

Opioid (mu) receptor class impacts (pre/post)-synaptic neuron by (increasing/decreasing) K (uptake/release). What does this do?

A

Post-synaptic;
Increasing
Release (outward K current);

Hyperpolarize (IPSP)

18
Q

List the three locations in CNS where opioids play a role.

A
  1. Limbic system (impact affect to pain)
  2. PAG (descending pain modulation)
  3. Dorsal horn (primary afferent pain fibers)
19
Q

Clinical selection of an opioid is usually based on (X) considerations.

A

X = pharmacokinetic

20
Q

T/F: Pts, after opioid administration, typically report pain has vanished.

A

False - pain still present, but dulled and no longer bothers them as much

21
Q

T/F: Opioids can vary drastically in lipophilicity.

A

True - partition coeff of morphine 1.4 and fentanyl is 860

22
Q

Morphine: (slow/rapid) absorption and clearance. Relatively (hydrophobic/hydrophilic), so CNS penetration/exit are (slow/fast). This accounts for morphine’s (slow/fast) onset and (short/long) duration.

A

Rapid absorption/clearance;
Hydrophilic;
Slow;
Slow onset, long duration

23
Q

(Fentanyl/Codeine/Morphine) cleared by hepatic biotransformation.

A

All three (almost all opioids cleared by liver)

24
Q

Fentanyl: (slow/rapid) absorption and clearance. Relatively (hydrophobic/hydrophilic), so CNS penetration/exit are (slow/fast).

A

Rapid absorption/clearance;
Hydrophobic (extremely lipophilic!!)
Fast (effects rapidly parallel changes in plasma conc)

25
Q

Which property of (fentanyl/morphine) allows its administration via multiple routes?

A

Fentanyl; lipophilicity

transdermal patch, intranasal spray, buccal tablet, lollipop

26
Q

Conjugation, specifically (X), of morphine can result in (Y) product 15% of the time. This is problematic, especially in which patient population?

A 
X = glucuronidation
Y = morphine-6-glucuronide

Active metabolite, slow to clear, builds up in brain; renal failure patients

27
Q

Codeine undergoes (methylation/de-methylation) to become (X). This is a (minor/major) pathway of codeine metabolism.

A

O-Demethylation
X = morphine
Minor (10% of codeine)
BUT accounts for nearly all opioid activity

28
Q

T/F: Most codeine metabolism (80%) results in inactive metabolites.

A

True - only morphine product active

29
Q

T/F: Opioids most likely to cause problems in hepatic failure, since most cleared by liver.

A

False - renal failure because many opioids have polar active metabolites (buildup if clearance is slow)

30
Q

Opioids: polymorphisms in clearance may be good or bad, depending on which two things?

A
  1. Effect of metabolite

2. Activity of parent drug

31
Q

T/F: Analgesia from opioids is always accompanied by some respiratory depression/effect.

A

True

32
Q

Opioids: depression of ventilatory response to (high/low) (CO2/O2) levels. The extent of this resp depression is dose-(dependent/independent).

A

High CO2, low O2

Dose-dependent

33
Q

(X) is the major toxicity of opioids and nearly always cause of death from overdose. Treatment is (Y).

A 
X = respiratory depression
Y = naloxone
34
Q

T/F: Tolerant individuals requiring large amounts of opioids for analgesia are at proportionately increased risk for resp depression.

A

False

35
Q

N-Methylnaltrexone is (centrally/peripherally)-acting (agonist/antagonist) of mu opioid receptors. What’s it used for?

A

Peripherally;
Antagonist

Treats opioid-induced constipation/urinary retention without antagonizing analgesia (can’t enter CNS)

36
Q

Opioids cause nausea/vomiting via which mechanism?

A

Direct stimulation of CTZ (chemoreceptor zone) in area postrema (floor of fourth ventricle); this activates vomiting center in medulla

37
Q

Opioid-induced hives by (X) release (is/isn’t) indicative of (Y) reaction. What’s the mechanism?

A

X = His;
Isn’t (no IgE);

Y = Anaphylactoid
Competitive displacement of His from tissue mast cells

38
Q

T/F: Opioid physical dependence is the same as opioid addiction.

A

False

39
Q

Opioid withdrawal is treated with:

A

small dose of opioid

40
Q

List some symptoms of opioid withdrawal.

A
  1. Rhinorrhea
  2. Vomit/diarrhea
  3. Gooseflesh/shaking
  4. Mydriasis
  5. Sweating (diaphoresis)
41
Q

Opioid addiction: agonist maintenance utilizes which drugs? What’s the method of administration?

A

Methadone or Buprenorphine;

Orally (decrease HIV/hepatitis seroconversion)

42
Q

Methadone maintenance to treat opioid addiction has which disadvantages?

A
  1. Special license required
  2. Separate from med care
  3. Limited availability
  4. Stable/unstable pts mixed
  5. No privacy (social stigma)
  6. Can’t “graduate” from program

Pharm (16 decks)

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