Opioids

Question 1

High efficacy agonist- prototype against which all others are compared

Answer 1

Morphine

Question 2

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

Answer 2

Meperidine (demerol)

Question 3

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

Answer 3

Methadone (Dolophine)

Question 4

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

Answer 4

Heroin

Question 5

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.

Answer 5

Fentanyl

Question 6

Medium efficacy agonist- good anti-tussive

Answer 6

Codeine

Question 7

Medium efficacy agonist- highest efficacy in this category.

Answer 7

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

Question 8

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

Answer 8

Pentazocine (schedule IV)

Question 9

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

Answer 9

Tramadol (Ultram, UltramER)

Question 10

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

Answer 10

Buprenorphine

Question 11

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.

Answer 11

Naloxone (Narcan)

Question 12

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

Answer 12

Dextromethorphan

Question 13

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

Answer 13

Loperamide

Question 14

Derived from opium

Answer 14

Opiate

Question 15

Compound with similar pharmacology to morphine

Answer 15

Opioid

Question 16

Pain relieving

Answer 16

Analgesic

Question 17

Sleep inducing

Answer 17

Narcotic

Question 18

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

Answer 18

Beta endorphins

Question 19

Endogenous opioid ligand- only in brain and spinal cord.

Answer 19

Enkephalins

Question 20

Endogenous opioid ligand- only in brain and spinal cord.

Answer 20

Dynorphins

Question 21

The major receptor for most opioid drugs

Answer 21

Mu

Question 22

Theraputic effect of opioid- Systemic

Answer 22

Analgesia and anesthesia (but not for neuropathic pain)

Question 23

Theraputic effect of opioid- Respiratory

Answer 23

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

Question 24

Theraputic effect of opioid- GI

Answer 24

Antidiarrheal (but causes constipation)

Question 25

Theraputic effect of opioid- cardiac

Answer 25

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

Question 26

Theraputic effect of opioid- psyche

Answer 26

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

Question 27

AE's of Opioids

Answer 27

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

Question 28

Triad of opioid overdose

Answer 28

Coma, respiratory depression, pinpoint pupils.

Question 29

Does tolerance to opioids affect safety?

Answer 29

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

Question 30

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

Answer 30

Hydromorphone (Dilaudid)

Question 31

Opioid C/I's

Answer 31

``` 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 ```

Question 32

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

Answer 32

Morphine

Question 33

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

Answer 33

Oxymorphone

Question 34

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

Answer 34

Fentanyl

Question 35

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

Answer 35

Fentanyl

Question 36

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

Answer 36

Methadone

Question 37

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

Answer 37

Meperidine (Demerol) | metabolized to nomeperidine

Question 38

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

Answer 38

Meperidine (Demerol)

Question 39

Medium efficacy opioid analgesic combined with aspirin

Answer 39

...dan (i.e. Percodan)

Question 40

Medium efficacy opioid analgesic combined with acetominophen

Answer 40

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

Question 41

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

Answer 41

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

Question 42

Common source of prescription drug abuse

Answer 42

medium efficacy oral opioid analgesics.

Question 43

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

Answer 43

Codeine

Question 44

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

Answer 44

Codeine

Question 45

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

Answer 45

OxyContin

Question 46

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

Answer 46

Hydrocodone (dihydrocodeinone) Vicodin and others.

Question 47

Can use to try and treat neuropathic pain.

Answer 47

Anti-depressants and Anti-convulsants.