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Pharmacology Final > Opioids > Flashcards

Opioids Flashcards

1
Q

High efficacy agonist- prototype against which all others are compared

A

Morphine

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2
Q

High efficacy agonist- much less potent than morphine but faster acting.

A

Meperidine (demerol)

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3
Q

High efficacy agonist- Used to treat Heroin addicts. Has a long T1/2 and good bioavailability.

A

Methadone (Dolophine)

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4
Q

High efficacy agonist- prodrug that is rapidly converted to morphine. Metabolites are the active agents. Not legal in US (schedule 1 drug)

A

Heroin

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5
Q

High efficacy agonist- more lipophilic than morphine and 75-100X more potent. Short acting and can be given via many routes (lollipop, transdermal patch, orally, buccally, sublingual and nasal spray.

A

Fentanyl

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6
Q

Medium efficacy agonist- good anti-tussive

A

Codeine

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7
Q

Medium efficacy agonist- highest efficacy in this category.

A

Oxycodone (Percocet, percodan, Combunox) OxyContin (slow release preparation)

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8
Q

Mixed agonist/antagonist/other- Only give this orally due to severe injection site necrosis and sepsis when given IV.

A

Pentazocine (schedule IV)

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9
Q

Mixed agonist/antagonist/other- risk of seizures, avoid taking with MAOI’s (serotonin syndrome)

A

Tramadol (Ultram, UltramER)

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10
Q

Mixed agonist/antagonist/other- analgesic effects due to mu partial agonism, also kappa antagonist. SL route preferred. Widely used to treat opioid dependence.

A

Buprenorphine

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11
Q

Antagonist- competitive antagonist at ALL opioid receptors (but not at non-opioid receptors like DM). IV only. Use for treatment of opioid overdose. Short duration of 1 hr.

A

Naloxone (Narcan)

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12
Q

Non-analgesic opioids- Anti-tussive that is not active at opioid receptors but is at DM receptors.

A

Dextromethorphan

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13
Q

Non-analgesic opioids- Anti-diarrheal, little BBB penetration. Active ingredient in Imodium-AD

A

Loperamide

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14
Q

Derived from opium

A

Opiate

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15
Q

Compound with similar pharmacology to morphine

A

Opioid

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16
Q

Pain relieving

A

Analgesic

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17
Q

Sleep inducing

A

Narcotic

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18
Q

Endogenous opioid ligand released from pituitary as a hormone and also present as a neurotransmitter

A

Beta endorphins

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19
Q

Endogenous opioid ligand- only in brain and spinal cord.

A

Enkephalins

20
Q

Endogenous opioid ligand- only in brain and spinal cord.

A

Dynorphins

21
Q

The major receptor for most opioid drugs

A

Mu

22
Q

Theraputic effect of opioid- Systemic

A

Analgesia and anesthesia (but not for neuropathic pain)

23
Q

Theraputic effect of opioid- Respiratory

A

Anti-tussive (but may allow accumulation of secretions and airway compromise). Not mediated by opioid receptors, mediated by DM receptors.

24
Q

Theraputic effect of opioid- GI

A

Antidiarrheal (but causes constipation)

25
Q

Theraputic effect of opioid- cardiac

A

Relief of acute pulmonary edema, reduces preload, afterload and anxiety (but can cause respiratory depression)

26
Q

Theraputic effect of opioid- psyche

A

Mood enhancement- contributes to relief of pain and suffering (but leads to abuse liability)

27
Q

AE’s of Opioids

A 
Constipation
Nausea, vomiting (can give with Zofran (ondansetron) to alleviate)
Sedation
Miosis
Pruritis
28
Q

Triad of opioid overdose

A

Coma, respiratory depression, pinpoint pupils.

29
Q

Does tolerance to opioids affect safety?

A

NO! Even if a person has become tolerant to the drug, it is still toxic at the same doses it was before.

30
Q

More potent than morphine- associated with less pruritis, HoTN, and bronchoconstriction. Considered safer for those with renal impairment.

A

Hydromorphone (Dilaudid)

31
Q

Opioid C/I’s

A 
Head Injury
Impaired Pulmonary Function
Impaired Renal Function
Impaired Liver Function
Pregnancy
Addison's Disease or Hypothyroidism
Partial Agonists (used in combo with)
Substance Abuse History
Drug Interactions- Serotonin Syndrome w/ MAOI's
32
Q

Crushing, dissolving, or chewing this drug can cause rapid release and absorption and a potentially fatal dose.

A

Morphine

33
Q

More potent than morphine, very similar in effect to Hydromorphone. Also associated with less histamine release so less pruritis, HoTN and bronchoconstriction.

A

Oxymorphone

34
Q

Used in combo with an anesthetic for post-op or labor pain

A

Fentanyl

35
Q

Used as primary general anesthetic for cardiac surgery and patients with impaired cardiac function

A

Fentanyl

36
Q

Blocks K+ channels and can lead to long QT syndrome and potentially fatal arrhythmias.

A

Methadone

37
Q

Hepatic demethylation to toxic metabolite that can cause potentially fatal neurotoxicity, CNS hyperactivity and seizures. Cannot be reversed with Naloxone.

A

Meperidine (Demerol)

metabolized to nomeperidine

38
Q

Avoid use in combo with MAOI’s, SSRI’s, tramadol or methadone- can cause potentially fatal serotonin syndrome.

A

Meperidine (Demerol)

39
Q

Medium efficacy opioid analgesic combined with aspirin

A

…dan (i.e. Percodan)

40
Q

Medium efficacy opioid analgesic combined with acetominophen

A

…cet (i.e. percocet, Darvocet, Ultracet), also Vicodin, Tylenol with codeine #3, Lortab

41
Q

Combining medium efficacy oral opioid analgesics with aspirin, acetaminophen or ibuprofen allows for…

A

two separate mechanisms to treat pain, can use less of each.

42
Q

Common source of prescription drug abuse

A

medium efficacy oral opioid analgesics.

43
Q

“Poor metabolizers”- this drug doesn’t work for 7% of Caucasians, 3% of African Americans, 2% of Asians and 1% of Arabs.

A

Codeine

44
Q

“Ultra- metabolizers”- this drug has abnormally increased affects and toxicity in 4-5% of US population

A

Codeine

45
Q

“Hillbilly Heroin”- abuse of this drug is a significant social problem. Crushing pills disables slow release mechanism and causes a higher effective dose.

A

OxyContin

46
Q

Moderate medium efficacy oral opioid analgesic between codeine and oxycodone. Good anti-tussive. Widely prescribed (more than any other opioid.)

A

Hydrocodone (dihydrocodeinone) Vicodin and others.

47
Q

Can use to try and treat neuropathic pain.

A

Anti-depressants and Anti-convulsants.

Pharmacology Final (9 decks)

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