6 - Opioid Analgesics Flashcards by G V

Opiod Agonists attach to what receptors? (3)

Kappa

Delta

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Opiod Agonists: Natural Opium Alkaloids (3)

Morphone

Codeine

Noscapine

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Opiod Agonists: Semi-synthetic Opioids (4)

Heroin

Pholcodeine

Hydromorphone

Oxymorphone

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Opiod Agonists: Synthetic Opioids (First 4)

Meperidine

Tramadol

Methadone

Dextropropoxyphene

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Opioid Agonists: Synthetic Opioids - Ultra Short Acting, Potent, and used IV (4)

Fentanil

Alfentanyl

Sufentanil

Remifentanil

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Opioid Agonists: Mixed Opiod Agonist-Antagonists (4)

Pentazocine

Buprenorphine

Nalbuphine

Butorphanol

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Opioid Agonists: Pure Opioid ANTAGONISTS (3)

Nalaxone

Naltrexone

Nalmefene

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Opioid Receptors: Mu functions (4)

Supraspinal and spinal analgesia in CNS

Sedation and euphoria

Inhibition of respiration

Slowed GI transit (periphery)

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Opioid Receptors: Kappa functions (3)

Supraspinal and spinal analgeisa

Psychotomimetic/dysphoria effects

Slowed GI transit

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Opioid Receptors: Delta functions 1)

Supraspinal and spinal analgesia

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Endogenous Opioid Peptides (3)

Endorphins

Enkephalins

Dynorphins

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Opioids Effects: CNS - Analgesia (1)

Reduce both sensory and affective components of pain

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Opioids Effects: CNS - Euphoria (1)

Pleasant floating sensation with lessened anxiety and distress

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Opioids Effects: CNS - Sedation (1)

Drowsiness and clouding of mentation

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Opioids can respond to what types of pain (3)

Dull, aching pain

Sensory (Feeling pain)

Emotional response to pain

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Opioids Effects: Respiratory depression (1)

Inhibit brain stem respiratory mechanisms (no longer respond to CO2) –> Resp rate 3-4 minutes

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Opioids Effects: Cough suppression (1)

Suppress cough reflex

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Opioids Effects: Miosis (1)

Mediated by parasympathetic pathways (M3 receptor)

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Opioids Effects: Nausea and Vomiting (1)

Activate the brainstem chemoreceptor trigger zone (CTZ) to produce nausea and vomiting AND due to delayed gastric emptying

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Opioids Effects: Cardiovascular System (1) and Morphine Actions

Peripheral arterial and venous dilation: central depression of vasomotor-stabilizing mechanisms and release of histamine

Morphine has negative ionotropic and chronotopic action on heart

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Opioids Effects: Cardiovascular System - Meperidine (2)

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Tachycardia

Anti-cholinergic (Atropine-like) action

Opioids Effects: GI Tract (1)

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Motility may decrease, but tone (persistent contraction) may INCREASE (constipation)

Opioids Effects: Biliary Tract (3)

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Contract biliary smooth muscle

The sphincter of Oddi may constrict –> reflux of bilary and pancreatic secretions –> elevated plasma amylase and lipase levels

Meperidine given for acute biliary colic (atropine like action), nitroglycerin, or atropine

Clinical Use of Opioids: Analgesia (3)

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Severe, constant pain (dull aching) with high intrinsic activity opioids (morphine, heroin, methadone)

Cancer and other terminal illnesses (trauma, gunshot wound, post-operative)

Severe pain of renal and bililary colic

Clinical Use of Opioids: Acute Pulmonary Edema from LVH - Drug (1) and Facts (3)

Morphine used Reduced cardiac preload Reduced afterload Can also give a diuretic (furosemide)

Clinical Use of Opioids: Dry Cough Drugs in Low Doses (4)

Codiene Pholcodiene Noscapine Dextromethorphan

Clinical Use of Opioids: Diarrhea Drugs (2)

Diphenoxylate (small amount of atropine added to prevent misuse) Loperamide (doesn't cross BBB)

Clinical Use of Opioids: Applications in Anesthesia (Ultra Short Acting Opiods) (3)

Premedicant drugs to prep for surgery Intraoperatively as adjuncts to other anesthetic agents High doses as a primary component (e.g. fentanyl)

Alternative Routes of Administration: Rectal Suppositories (2)

Morphone Hydromorphone

Alternative Routes of Administration: Transdermal Patch (1)

Fentanyl (sustained plasma levels, all day)

Alternative Routes of Administration: Intrnasal (1)

Buturphanol (avoids first pass metabolism)

Alternative Routes of Administration: Buccal Transmucosal (1)

Fentanyl citrate lozenge or "lollipop"

Alternative Routes of Administration: Patient-Controlled Analgesia (PCA) (1)

Parenteral (usually IV) infusion device that delivers a preprogrammed dose of the desired opiod analgesic

Opioids Toxicity: Tolerance (3)

Develops 2–3 weeks of frequent exposure to ordinary therapeutic doses Marked tolerance may develop to the analgesic, sedating, and respiratory depressant effects Can give calcium channel blockers to delay tolerance

Opioids Toxicity: Physical Dependence - Withdrawal/Abstinence Syndrome (9)

Dysphoria initially Rhinorrhea Lacrimation Yawning Chills Gooseflesh Hyperventilation Hyperthermia Mydriasis

Opioids Toxicity: Psychological Dependence (1)

To derive pleasure

Opioids Agonists: Methadone Defined (4)

Extended duration of action Persistent effects with repeated administration Can also block NMDA receptors Slower duration of action so slower dependence, this less intense withdrawal

Opioids Agonists: Methadone Uses (3)

Treatment of opioid abstinence syndromes Treatment of heroin users Relief of chronic pain

Opioids With Mixed Receptor Actions: Nalbuphine (3)

Strong Kappa receptor agonist Mu receptor ANTAGONIST Will see acute withdrawal

Opioids With Mixed Receptor Actions: Buprenorphine (4)

Potent and long-acting partial receptor µ agonist. Sublingual route is preferred to avoid significant first-pass effect. Long duration of action; can be abused (similar to methadone) Detoxification and maintenance of heroin abusers.

Opioids With Mixed Receptor Actions: Suboxone is Buprenorphine and?

Naloxone

Opioids With Mixed Receptor Actions: Butorphanol (1)

Predominantly KAPPA agonist that causes dysphoria (psychotomimetic actions)

Opioids With Mixed Receptor Actions: Pentazocine (2)

Kappa AGONIST with MU ANTAGONIST or Partial agonist properties

Opioids With Mixed Receptor Actions: Tramadol (1)

Blockade of serotonin reuptake

Contraindications and Cautions: Use of pure agonists with weak PARTIAL agonists (1)

Cancel the actions of morphine --> reduced analgesia/acute withdrawal reaction

Contraindications and Cautions: Use in patients with head injuries (1)

Increases intracranial pressure from respiratory depression

Contraindications and Cautions: Use DURING pregnancy (1)

Fetus can get addicted

Contraindications and Cautions: Use in patients with impaired pulmonary function (1)

Causes respiratory depression

Contraindications and Cautions: Use in patients with impaired hepatic or renal function (1)

Opioids are metabolized in liver and excreted through kidney

Opioid Antagonists (3)

Naloxone Naltrexone Nalmefene

Opioid Antagonists: Naloxone Use (2)

Acure Opioid Overdose (Resp, Constricted pupils, and Coma) Low-dose: Treatment of adverse effects that are commonly associated with IV or epidural opioids that relieve itching, nausea and vomiting while sparing use of analgesia

Opioid Antagonists: Naltrexone Use (1)

Maintenance drug for alcohol and nicotine addicts

6 - Opioid Analgesics Flashcards

(52 cards)