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JGR opioids

What is a mixed agonist-antagonist? may block or be neutral at one type of opioid receptor while activating others
what is a Central Analgesic? centrally acting opioid agonist
What is an Opioid Antagonist? Drug that competitively blocks opioid receptors
List the Phenanthrenes Morphine (MS Contin®, MSIR, etc) Hydromorphone (Dilaudid®) Levorphanol (Levo-Dromoran®) Oxymorphone (Numorphan®) Oxycodone (OxyContin®, Percocet®, etc)) Hydrocodone (Vicodin) (Vicodin®, Lortab®, etc) Codeine (Tylenon No.3®, etc)
List the Phenylpiperidines Meperidine (Demerol®) Fentanyl (Sublimaze®, Duragesic®, Actiq®) Alfentanil (Alfenta®) Sufentanil (Sufenta®) Remifentanil (Ultiva®)
List the Diphenylheptanes Methadone (Dolophine®, Methadose®)
What is an Opioid? Natural and synthetic substances that produce morphine-like effects
What is an Opiate? A term reserved for natural substances from the opium poppy
How do opioids work? They bind to the opioid receptors in CNS to mimic endogenous opiate system
What is the primary use of opioids? To relieve pain and anxiety associated with pain
Where are opioid receptors located in the body? Opioid receptors are located in the CNS, peripheral nerve terminals and in the GI tract
What is the function of the Mu receptor? Mu (μ) - Responsible primarily for most analgesic properties (Analgesia, Respiratory depression, Miosis, Reduced gastric motility, sedation, euphoria)
What is the Kappa receptor used for? Kappa (κ) Contribute to analgesic properties
What is the function of the delta receptor? Delta (δ ) Located more in the periphery and selective for enkephalins, also contributes to analgesic properties
What opioid receptor causes dysphoria? Euphoria? Kappa Mu
What opioid receptor causes GI immotility? Mu
Which opioid receptor causes less respiratory depression and miosis? Kappa
What is the MOA of opioids? MOA – Bind to opioid receptors which are G protein coupled receptors and inhibit adenylyl cyclase and control ion gating – Decreased presynaptic Ca+ influx inhibiting excitatory neurotransmiters • acetylcholine, norepinephrine, glutamate, serotonin, and
What is a rescue dose? 10-20% of total daily dose (for breakthrough pain)
What are common adverse reactions to opioids? Sedation: reduce dose by 25% or increase interval Nausea/Vomiting: give a centrally acting antiemetic Constipation*: give a stool softener & stimulant laxative Gastroparesis: give metoclopramide Respiratory Depression: reduce dose by 25% or give nalox
At what does of morphine will 70% of patients get desired analgesic effect? 10mg/70kg
What happens to the sedation side effect of opioids when given over time for chronic pain? Sedation lessens over time
What can be given to combat nausea/vomiting side effect of opioids? Antiemetic
What can be given to combat constipation side effect of opioids? Stool softener or stimulant, Reglan® if others fail
Are opioid allergies common or rare? Rare
Although rare, what type of allergic response do opioids cause? Histamine release (itching and flushing)
Does itching from opioids indicate an allergy to the drugs? No
Is there cross-sensitivity within opioid families? Yes, if allergic to one opioid you will likely be allergic to all in that family
What drug is used for opioid overdose reversal? Naloxone (Narcan®)
What do most opioid overdose patients die from? Respiratory depression
What is the MOA of Naloxone (Narcan®) in opioid overdose reversal? Opioid receptor competitive antagonist Reverses CNS and Respiratory depression
What opioids are in controlled substance category II? All phenanthrenes + methadone (Hydrocodone (Vicodin®) is III because it is always combined with Tylenol®)
What opioid is contraindicated for head injury? Why? Morphine because it causes increased IOP
What are the side effects of Morphine? Can cause orthostatic hypotension thru venous and arteriolar vessel dilation Increases ICP: Relative contraindication in severe head injury
What occurs with morphine in patients with renal impairment? Metabolite, Morphine 3 glucuronide, may accumulate contributing to side effects
What is the difference between morphine and Hydromorphine? Hydromorphine is rapid onset and 3-5 times more potent than morphine Less histamine release than morphine
Which opioid is known as “hillbilly heroin”? Oxycodone (reason for the new form that resists crushing to prevent snorting)
What dosage forms of Oxycodone are available? Immediate release and controlled release
What opioid is only available in combination with a non-opioid? Hydrocodone (Vicodin®) (always combined with Acetaminophen (Tylenol®)
What opioid is an anti-tussive? Codeine
What is the controlled substance category of Codeine? CII if lone agent
What opioid causes constipation resulting in a ceiling effect? Codeine
What opioid causes Orthostatic HOTN? What type of patients is this side effect worse in? Morphine Patients with hypovolemia
Why is Meperidine (Demerol®) a bad drug? No advantage over morphine just greater toxicity Causes euphoria and is prone to abuse
What is Meperidine (Demerol®) used for? Niche uses by old school MD’s (eye drops)
What is the contraindication for Meperidine (Demerol®)? Elderly and pts. With renal impairment because it produces a toxic metabolite normeperidine that is renally cleared. Toxin causes CNS excitability such as tremor, muscle twitches and seizures
What are the DDI for Meperidine? MAOIs
What opioid has a DDI for MAOIs? Meperidine (Demerol®)
What is the difference between Meperidine (Demerol®) and Fentanyl Fentanyl is more potent, more lipophilic, shorter acting than meperidine
Which opioid is not used for acute pain due to taking too long to titrate dose? Fentanyl patch (Duragesic® )(Works up to 72hours but takes 12-24h for full onset & 6days to reach steady state)
Why should Fentanyl patch (Duragesic®) not be used in a hospital? Patch form lends itself to patient misuse
What is a good opioid for breakthrough cancer pain? Fentanyl transbuccal route (Actiq® Lollipop)
Which opioid has unpredictable half-life? Methadone (use with caution when transitioning from morphine)
What are the uses of Methadone? Analgesia and heroine withdrawal
What unique actions of Methadone make it useful for neuropathic and chronic pain? Agonist at mu, kappa, and delta receptors Antagonist at NMDA receptor Blocks serotonin and norepinephrine reuptake
What opioid was withdrawn from the market due to severe cardiovascular toxicity? Propoxyphene (Darvon®)
What is the MOA of mixed agonist-antagonists? Agonist or partial agonist at one opioid receptors and antagonist at 2 others
Why were mixed agonist-antagonists developed? Developed to stimulate the analgesic portion of the opioid receptor while blocking the toxicity portion
What is the problem with mixed agonist-antagonists? They don’t work well. Used as 2nd or 3rd line analgesic, Naloxone (Narcan®)does not fully resolve
What are the adverse effects of mixed agonist-antagonists? Same opioid AE plus psychotomimetic effects (delirium), precipitate opioid withdrawal when transitioning from other opioid
What causes the ceiling affect in mixed agonist-antagonists? Respiratory depression
What receptors do Pentazocine act on? Agonist on kappa receptor (causes dysphoria) weak antagonist at mu and delta
What are the contraindications for Pentazocine? Why? Angina because it increases mean aortic pressure and pulmonary arterial pressure, increasing the work of the heart
What receptor does Buprenophrine act on? Only a partial agonist on Mu
What are the uses of Buprenophrine? Opioid detox (lublingual form) Analgesia (parenteral form)
What receptors does Butorphanol (Stadol®) act on? Agonist on kappa receptor (causes dysphoria) weak antagonist at mu and delta
What is butorphanol (Stadol®) uses for? Migraine headaches
What is the only non-controlled mixed agonist-antagonist? Nalbuphin (Nubain®)
What receptors does Nalbuphin (Nubain®) act on? Kappa receptor agonists and a mu receptor antagonist
What is a primary use of Nalbuphin (Nubain®)? Labor and Delivery
How is Tramadol (Ultram®) different from other opioids? It is a mu receptor agonist and inhibits serotonin and norepinephrine reuptake
What is the controlled substance category of Tramadol (Ultram®)? Not controlled
What is the primary use of Tramadol (Ultram®)? Moderate to moderately severe acute pain, potentially useful for chronic pain
What are the adverse reactions of Tramadol (Ultram®? Similar to opioids, increase risk of seizures*, anaphylactoid response
What are the drug to drug interactions of Tramadol (Ultram®)? SSRIs, TCAs, MAOIs, neuroleptics, or other drugs that lower the sz threshold
What are adjuvant agents? Non-analgesic drugs that work as monoagents or in combination with analgesics to stop pain
What are the adjuvants that are useful in neuropathic and chronic pain? Tricyclic antidepressants : Amitriptyline (Elavil®) Anticonvulsants decrease neuronal excitability Gabapentin(Neurontin®) – PHN Duloxetine (Cymbalta®) – DPN Pregabalin (Lyrica®) – DPN & PHN Local anesthetics: Lidocaine 5% patch – PHN Counterirrit
How does the adjuvant Capsaicin work? Depletes substance P
How do Tricyclic antidepressants work? Block reuptake of NE and 5HT
What is Tolerance? Neuroadaptation by the body causing diminution of drug effect over time due to exposure • Requires dose increase, does not lead to addiction • With stable disease, opioid use often stabilizes
What is Physical Dependence? Occurrence of an abstinence syndrome following administration of an antagonist or abrupt dose reduction/discontinuation • Likely with long-term use • Requires a taper to prevent withdrawal syndrome
What is Addiction? Behavioral pattern characterized by a loss of control over drug use, compulsive drug use, and continued use despite harm • Low occurrence with rational therapy in low risk patients (genetic, social and psych factors)
What is Pseudoaddiction? Under-treatment of chronic pain leads to behaviors resembling addiction
What is the most common mistake made in pain management? Under-dosing
How does physical dependence differ from addiction? It is a physiological response from using the drug as indicated
Created by: joannasan



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