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23 Cards in this Set

  • Front
  • Back
Non-Opioid Analgesics
Peripheral Tissues Inhibit formation of algogenic substances
Opioid Analgesics
morphine/thebaine analogs

Spinal Cord/Brain
Inhibit neurotransmission of pain signals

Also for anesthesia
Adverse Side effects of opiods
reduced blood pressure
itching (cause mast cells to release histamine),
nausea and vomiting (stimulating chemoreceptor trigger zone)
decreased respiration (reduce hypercapnic drive)
miosis, decreased bowel motility
mood disorder
tolerance, physical dependence
muscle rigidity
The Strong Opioid Agonists
Meperidine (Demerol)
Fentanyl (Sublimaze)
Sufentanil (Sulfenta)
Methadone (Dolophine)
Hydromorphone (Dilaudid)
Oxycodone (OxyContin)
for addiction although can be used for analgesia.
slow metabolism, high lipid solubility, t1/2 24-36 hours
has still addictive properties
Same side effects
Hydrogenated ketone that is more potent than morphine (~8X)
overdose if used with with alcohol (fast absorption)
Oxycodone (OxyContin)
Several formulations
percocet with aspirin
percodan/Tylox etc. with acetaminophen
OxyContin which is sustained release
other versions which are “instant release”
Administration orally, intranasally, via IV/IM/subcu injection, or rectally oral high bioavailability (up to 90%)
The Moderate Opioid Agonists
Hydrocodone(Vicodin, Lorcet, Lortab,etc.)
Propoxyphene (Darvon, Darvocet)
Oxymorphone (Opana, Numorphan)
Prodrug of morpine
In Tylenol 3 for mild/moderate pain

Metabolized by CYP2D6 which in some patients is low.

methyl group is removed to give morphine but since only about ~10% then low effect
Said to have more bioavailability than morphine because less first pass metabolism since no glucoronidation at that site.

Allergic reaction is release of histamine from mast cells
Hydrocodone (Vicodin)
prepatations by different companies
Vicodin, Anexsia, Dicodid, Hycodan, Hycomine, Lorcet, Lortab, Norco, Novahistex, Hydroco, Tussionex, Vicoprofen
Formulated with acetominophen
cannot be mixed with MAOIs
Propoxyphene (Darvocet, Darvon)
racemic mixture of levopropoxyphene and dextropropoxyphene
Darvocet is the Dextro- isomer with acetaminophen
Used for mild to moderate pain
Can be used for withdrawal from other opioids
Can be addictive
efficacy AND Therapeutic index is low
Extensive first pass metabolism with toxic by-products
can be used as local anesthetic
not Opioid receptor
Mild to moderate when an NSAID not enough and codeine not tolerated
we know it is not opioid receptor property because not inhibited by nalaxone.
Oxymorphone (Opana, Numorphan)
additional OH group to hydromorphone
IV, suppository, tablet administration
Removed from market.
High abuse “the blues”
Other Opioids
Tramadol (Ultram, Ultracet) Mild pain
Loperamide (Imodium, Kaopectate, etc.) Diarrhea
Diphenoxylate (Lomotil) Diarrhea
Dextromethorphan (in many preparations) Cough suppression
racemic mixture
with acetominophen is ultracet
not related in structure to other opioids and is only moderate mu weak delta and kappa agonist, 10 times less potent than morphine

metabolized extensively p450 (CYP 2D6)
low abuse potential but some dependence is observed
used for patients that respond poorly to NSAIDS
can interact with coumadin and can cause seizures
Should not be taken with SSRIs (potentiate and also inhibit metabolism)
Opioid Agonists-Antagonists [5]
Nalorphine (no clinical use)
Pentazocine (Talwin)
Nalbuphin (Nubaine)
Butorphanol (Butorfanol)
Buprenorphrine (Buprenex)
Why would we use Opioid Agonists-Antagonists?
Lack complete agonist effect at mu receptors so less respiratory depression and lower chance fro drug dependence than the complete opioid agonists. Also less constipation
Opioid Agonists-Antagonists s/a's?
Side effects are anxiety, nightmares, psychotomimetic effects such as hallucinations because of kappa agonist activity.

If patient is on a full agonist, can cause withdrawal.
Pentazocine (Talwin)
Kappa and sigma receptor agonist
Supplement to anesthesia
Oral formulations for pain
Formulated with naloxone
Formulated with aspirin or acetaminophen
Paraenteral use can cause severe condiopulmonary reactions
Butorphanol (Butorfanol)
Kappa receptor agonist
Partial agonist/antagonist at mu receptor

Supplement to anesthesia
Relief of pain during labor
Nalbuphine (Nubain)
Kappa receptor agonist
Partial agonist/antagonist at mu receptor

Supplement to anesthesia
Buprenorphine (Buprenex)
Partial mu agonist

Slow dissociation so longer activng
IM, IV, oral sublingual
Approved for treatment of opioid dependence
Formulated with Naloxone to lower abuse
Opioid Antagonist

Oral and transdermal
High oral bioavailability
Can be used long term
Also for alcohol dependence
Opioid Antagonists

Opioid Antagonists
IV for rapid termination of opioid respiratory depression (poor oral bioavailability
Short half-life
May need repeated dosing
Also in other opioid medications – not to block if used oral but if crushed and used IV