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23 Cards in this Set
- Front
- Back
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Non-Opioid Analgesics
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(NSAIDs)
Peripheral Tissues Inhibit formation of algogenic substances anti-inflammatory/antipyuretic |
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Opioid Analgesics
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morphine/thebaine analogs
Spinal Cord/Brain Inhibit neurotransmission of pain signals Also for anesthesia |
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Adverse Side effects of opiods
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reduced blood pressure
itching (cause mast cells to release histamine), nausea and vomiting (stimulating chemoreceptor trigger zone) euphoria decreased respiration (reduce hypercapnic drive) miosis, decreased bowel motility mood disorder tolerance, physical dependence muscle rigidity |
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The Strong Opioid Agonists
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Morphine
Meperidine (Demerol) Fentanyl (Sublimaze) Sufentanil (Sulfenta) Methadone (Dolophine) Hydromorphone (Dilaudid) Oxycodone (OxyContin) |
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Methadone
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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 |
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Hydromorphone
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Hydrogenated ketone that is more potent than morphine (~8X)
overdose if used with with alcohol (fast absorption) |
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Oxycodone (OxyContin)
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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%) |
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The Moderate Opioid Agonists
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Codeine
Hydrocodone(Vicodin, Lorcet, Lortab,etc.) Propoxyphene (Darvon, Darvocet) Oxymorphone (Opana, Numorphan) |
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Codeine
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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 |
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Hydrocodone (Vicodin)
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prepatations by different companies
Vicodin, Anexsia, Dicodid, Hycodan, Hycomine, Lorcet, Lortab, Norco, Novahistex, Hydroco, Tussionex, Vicoprofen Formulated with acetominophen cannot be mixed with MAOIs |
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Propoxyphene (Darvocet, Darvon)
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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. |
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Oxymorphone (Opana, Numorphan)
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additional OH group to hydromorphone
IV, suppository, tablet administration Removed from market. High abuse “the blues” |
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Other Opioids
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Tramadol (Ultram, Ultracet) Mild pain
Loperamide (Imodium, Kaopectate, etc.) Diarrhea Diphenoxylate (Lomotil) Diarrhea Dextromethorphan (in many preparations) Cough suppression |
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tramoldol
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Tramadol
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) |
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Opioid Agonists-Antagonists [5]
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Nalorphine (no clinical use)
Pentazocine (Talwin) Nalbuphin (Nubaine) Butorphanol (Butorfanol) Buprenorphrine (Buprenex) |
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Why would we use Opioid Agonists-Antagonists?
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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
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Opioid Agonists-Antagonists s/a's?
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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. |
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Pentazocine (Talwin)
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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 |
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Butorphanol (Butorfanol)
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Kappa receptor agonist
Partial agonist/antagonist at mu receptor Supplement to anesthesia Relief of pain during labor |
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Nalbuphine (Nubain)
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Kappa receptor agonist
Partial agonist/antagonist at mu receptor Supplement to anesthesia |
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Buprenorphine (Buprenex)
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Partial mu agonist
Slow dissociation so longer activng IM, IV, oral sublingual Approved for treatment of opioid dependence Formulated with Naloxone to lower abuse |
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Naltrexone
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Opioid Antagonist
Oral and transdermal High oral bioavailability Can be used long term Also for alcohol dependence |
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Opioid Antagonists
Naloxone |
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 |
