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JGR opioids
| Question | Answer |
|---|---|
| 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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