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PAPOM > Pharm (Comp 3) > Flashcards

Pharm (Comp 3) Flashcards

1
Q

Endogenous opioids

Examples and MOA

A

Endorphins, Enkephalins, Dynorphins

mu, delta, and kappa reptor agonists

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2
Q

Effects mediated by mu opioid receptor

A
  • Analgesia
  • euphoria
  • physical dependence
  • bradycardia
  • GI transit slowing
  • respiratory depression
  • Modulator of hormone and NT release
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3
Q

Effects mediated by kappa opioid receptor

A
  • spinal analgesia
  • miosis
  • sedation, psychomimetic effects
  • diuresis
  • slowed GI
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4
Q

Effects mediated by delta receptor

A
  • Dysphoric effects
  • Analgesia
  • Modulator of hormone and NT release
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5
Q

Strong agonist opioids

A

Morphine, methadone,

heroin, meperidine, fentanyl

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6
Q

Partial/mixed opioid agonist

A

Pentazocine, buprenorphine

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7
Q

Weak opioid agonists

A

codeine, hydrocodone

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8
Q

Morphine, Hydromorphone, Oxymorphone

MOA and action/use

A
  • Opioid receptor agonist (miu, kappa, and delta)

- Use: Alter mood/anxiolytic, sedation, depress pain reaction

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9
Q

Morphine, Hydromorphone, Oxymorphone

Toxicity

A
  • Respiratory depression, vasodilation
  • Nausea/vomiting, constipation, Biliary colic
  • Itching, hypotension, bronchoconstriction (H1)
  • Miosis
  • Increased prolactin release, inhibition of LH release
  • Tolerance, withdrawal, physical dependence, addiction
  • Increases intracranial pressure
  • Not in pregnancy. Meperidine preferred in labor.
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10
Q

Codeine, Hydrocodone

MOA and use

A

MOA: Weak opioid receptor
agonist; Metabolized to
morphine

Use: Moderate pain treatment, Anti-tussive

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11
Q

Codeine, Hydrocodone

Toxicity

A
  • Nausea, vomiting
  • drowsiness, dizziness
  • constipation
  • Combined with NSAIDs or acetaminophen
  • Codeine –> CYP2D6 metabolism. Genetic polymorphisms may increase toxic effects.
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12
Q

Methadone

MOA and Use

A
  • Opioid receptor agonist;
    antagonism on NMDA receptor
  • Use: Avoidance of
    the withdrawal reaction in opioid dependence patients
  • Long t1/2 allows a slow taper
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13
Q

Methadone

toxicity

A

Accumulates with repeated doses, which can cause respiratory depression.

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14
Q

Meperidine (Demerol)

MOA and use

A

Opioid receptor agonist; Antimuscarinic effects; Serotonin effects

Use: Like morphine, but less analgesia

  • Good in obstetrics: less neonatal respiratory
    depression. Inc contractions
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15
Q

Meperidine

Toxicity

A
  • Normeperidine (metabolite) can induce CNS stimulation esp. renal dysfunction pts
  • Serotonin syndrome with SSRIs
  • Drug interactions with monamine oxidase inhibitors (MAOIs)
  • Hyperrexia coma
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16
Q

Fentanyl, Alfentanil, Sufentanil, Remifentanil

MOA and Use

A
  • Opioid receptor agonist
  • 100x more potent than morphine
  • IV analgesic. Used for extra-anesthetic analgesia.
17
Q

Fentanyl, Alfentanil, Sufentanil, Remifentanil

Toxicity

A

Respiratory depression

Available as transdermal (patch) and transmucosal (lozenge) formulations.

18
Q

Heroin/Diacetylmorphine

MOA and Use

A
  • Opioid receptor agonist
  • Semisynthetic is
    metabolized to morphine for action.
  • Lipid soluble and crosses blood brain barrier quickly
19
Q

Heroin/Diacetylmorphine

Toxicity

A
  • Super CNS action
  • analgesia
  • Euphoria
  • dependence and addiction
  • Illicit use only
20
Q

Tramadol

MOA and Use

A
  • Mu receptor agonist. NE and 5-HT reuptake inhibitor.
  • Weak analgesic, neuropathy
    Little opioid toxicities.
  • High bioavailability, active metabolite.
21
Q

Tramadol

Toxicity

A
  • May cause hypertensive crisis with MAOI

- Often combined with acetaminophen (added liver toxicity)

22
Q

Diphenoxylate, Loperamide

MOA

A
  • Weak mu or kappa agonists

- Antidiarrheal

23
Q

Diphenoxylate, Loperamide

A
  • Diphenoxylate –> combined with atropine to reduce abuse potential
  • Loperamide –> no CNS effects, does not cross BBB (Imodium, OTC use)
24
Q

Opioid drug interactions

A

CNS depression with:

  • ethanol
  • antipsychotics
  • tricyclic antidepressants
  • sedative-hypnotics (eg. benzos)
  • antihistamines
25
Q

Opioid OD S&S, Treatment

A
  • Pupillary constriction
  • Comatose state
  • Hypotension
  • Bradycardia
  • Respiratory depression

Administer naloxone and ventilation.

26
Q

Serotonin Syndrome

  • Drugs involved
  • S&S
  • Treatment
A
  • SSRIs, TCAs, meperidine, dextromethorphan, St. John’s Wort, linezolid, “triptans” (2 of these combined together)

Symptoms: rigidity, hyperthermia, myclonus, delirium, hypertension, tachycardia, GI symptoms
- within 24 hrs of taking the two drugs

Treatment: Benzodiazepines, cyproheptadine, ventilation

27
Q

Naloxone

MOA and Use

A
  • Antagonist at all opioid receptors. IV use.

- Rapidly antagonizes all opioid effects. Precipitates withdrawal in dependent users.

28
Q

Naloxone

Toxicity

A
  • Fast onset and short duration of action

- Repeated administration needed until opioid is cleared from the body.

29
Q

Naltrexone

MOA and Use

A
  • Like Naloxone but 5x more potent; up to 72 hr duration.
  • Binds all opioid receptors. Oral use.
  • Maintenance therapy; May reduce alcohol cravings in alcoholics
30
Q

Naltrexone

Toxicity

A

Caution in hepatic impaired pts.

31
Q

Methylnaltrexone

MOA and Use

A
  • μ opioid receptor antagonist

- Treats opioid-induce constipation

32
Q

Methylnaltrexone

Toxicity

A
  • Does not cross BBB (compound is methylated)

- Targets GI tract

33
Q

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine

MOA of each

A
  • Butorphanol (κ agonist)
  • Buprenorphine (partial μ agonist, κ antagonist). Slow dissociation from μ receptor.
  • Nalbuphine and Pentazocine (κ agonist, μ antagonist)
34
Q

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine

Use

A
  • Analgesia without euphoria, less chance for dependence.
  • Buprenorphine used in some rehabilitation programs.
    Slow dissociation from the mu receptor
35
Q

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine

Toxicity

A
  • Sim to morphine
  • Administering these drugs with a pure agonist (eg. morphine) can reduce efficacy of the agonist or precipitate withdrawal.
  • Pentazocine can increase psychomimetic effects (kappa mediated)
36
Q

Opioid withdrawal symptoms

A
  • Yawning, hyperventilation
  • Lacrimation, piloerection, mydriasis
  • Fever, chills, hyperthermia
  • muscular aches, vomiting
  • anxiety and hostility

PAPOM (3 decks)

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