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120 Cards in this Set
- Front
- Back
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Name 3 types of Opioids receptors?
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Mu, Kappa & Delta- Opioids work mostly on Mu receptors and weakly on Kappa receptors
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How do Mu receptors respond to opioids?
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analgesia, resp depression, euphoria and sedation & related to physical dependence
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How do Kappa receptors respond to opioids?
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sedation and analgesia
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Drugs that supress the Mu receptors?
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demerol, MS, fentanyl, sufenta, and dilaudid
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What 3 types of classifications are there for opiods?
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Pure opioid agonist, agonist-antagonist and puer opioid antatgonists
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What do pure Opioid agonists do?
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activate both Mu & Kappa receptors, produce, analgesia, resp depression, euphoria, sedation, dependence and constipation
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What do agonist-Antagonist Opioids do?
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There are 4 - pentazo ine, nalbuphine, butorphanol, and buprenorphine. Act on Mu and kappa receptors, cannot give iwth pure opioid agonists
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Name a pure opioid antagonist
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Narcan
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What are the effects of Morphine?
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analgesia, resp depression, sedation, euphoria, cough supressant, & suppression of bowel motitlity
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What does Opium contain and where is it obtained?
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contains codiene, morphine and papaverine - s smooth muscle relaxant - comes from poppy plant
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What kinds of pain is MS most effective of treating?
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constant, dull pain - not as effective against sharp intermittant pain
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How does morphine & other opiates work?
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mimickes actions of endogenous opioid peptides at mu receptors
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Name adverse effects of MS
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respiratory depersision, constipation, orthostatic hypotentions, urinary retention, cough suppressant, biliay colic, emesis, elev intracranial pressure, euphoria/dysphoria, sedation, miosis, neurotoxicity
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what is most common cause of death from Opioids?
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Resp depression - tolerance to resp depression developes with long term use
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What drugs when taken with opioids can exacerbate urinary retention?
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anticholernigic (TCA's) and antihistamines
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How is MS taken?
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PO - big first pass effect - need higher oral dose, IV, IM, SQ, intrathecall, epidural
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What tolerance is developed iwth long term MS use?
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analagesia, sedation, euphoria, resp depression, no tolerance to contipation or miosis, cross tolerance to other opioids develope at same time
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How is abstinence syndrome with opiods?
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depends on half life - worse with short half life meds like MS - symptoms intense and brief, long half lives (methadone) less intense & prolonged
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Is the withdrawal from opioids dangerous?
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No takes about 10 days, very unpleasant - anorexia, irritability, tremor, gooseflesh, N/V, diarreha abd cramps, bone and muscle pain,kicking movements
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Why is prolonged use of opioids discouraged in pregnancy?
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Not tertragenic, but can cause physical dependance in newborn
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Where is MS metabolized?
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The liver - watch dosaged in pt with liver problems
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What drugs does MS interact witih?
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CNS depressants - barbituates benzoidapabines, alchohol, General anthesthesia, phenothiazines (increase resp deperssiion and sedation)
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What s/s are seen with opioid overdose?
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coma, resp depression, and pinpoint pupils
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What class of meds are opioids?
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Class II
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What opioid comes in a patch?
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Fentanyl as Duragesic, do not expose to heat like heating pad or sun can increase release of fentanyl
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What opioid comes in a transmucosal lozenge or stick?
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fentanyl for breakthrough pain with cancer also available as a buccal tablet
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Meperidine used to be the drug of choice why is it not now?
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Drug to drug interactions - interacts with MAO inhibitors causing coma and death, also interacts with TCA and SSRI
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Methadone can adversely affect the QT interval and should not be given with what other drugs?
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CNS depressants, benzodiazapines, alcohol , clarithromycin, fluvoxamine, fluconazole and nelfinavir
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What opioid drug can cause toxicity in breastfed infant?
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codiene as codiene is converted to MS and some have ultrarapid conversion of codiene to MS
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What schedule is codiene when use at an antitussive?
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Class V, Class II by itself and Class III mixed with another med
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What is the first agonist-Antagonist Opiod?
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Talwin - used for mild to moderate pain
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What drug shoudl not be prescribed with people with suicide tendencies?
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Propoxyphene (Darvon) - low potential for abuse
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What happens when pentazocine is given to someone physuically dependent to opioids?
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precipitate withdrawal as it is a mu receptor antagonist and should never be given to someone dependent to pure opioids
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Can buprenorphine (Buprenex) be reversed with Narcan?
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no - binds strongly to receptors - used for opioid withdrawal
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How should opioids be administered?
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on a fixed schedule to reduce risk of breakthrough pain
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When is dependence seen with opioids?
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After 20 days of high doses
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What is opioid of choice for MI?
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MS as it decrease cardiac workload, never give pentazocin or butorphanol to MI pts as they inc cardiac workload
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Which opioid antagonist is given to relieve constipation?
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RElistor (methylnaltrexone) given SQ
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Name 4 nonopioid centrally acting analgesics?
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Tramadol (ultram) clonidine (duraclon) ziconotide (Prialt) and dexmedetomidien (precedex) - no risk of dependence
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How does tramedol work?
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weak agaonist of mu recpetors, works by blocking uptake of NE and serotoniin
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What pain med is also a antihypertensive med?
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Clonidine - marketed as Duraclon for pain - adminitered by epidural infusion - approved for use with opioids for severe CA pain
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What screening tool is used for fibromyalgia?
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mVASFIQ
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What meds treat fibromyalgia?
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Pregabalin (Lyrica - relieves neuropathic pain),a duloxetine (Cymbalta) or milnaciprana (Savella a SNRI): pregabalin (25–75mg at night) if high insomnia score, duloxetine (20–30mg
in morning) if high depression score or milnacipran (12.5mg in morning) if high fatigue score |
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What other activities help fibromyalgia?
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Activity: daily stretching, both low-impact aerobic and resistance exercise alternating every other day
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How to treat fibromyalgia fatigue?
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Modafinil (provignil) (50–100mg) or
methylphenidate (5–10mg) on awakening with a second dose at lunch if necessary |
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How to treat fribromyalgia Insomnia?
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Treat insomnia with
eszopicione (Lunesta) (1–3mg), ramelteon (8mg) or a sedating anti depressant at night • Treat RLS with dopamine agonists at night• Nonrestorative sleep treated with pregablina (25–75mg) at night |
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How to treat fibromyalgia Blues?
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Antidepressant medications–
SNRI preferred, such as duloxetine (Cymbalta) (60mg once in morning), milnacipran (Savella) (50mg twice daily), venlafaxine (Effexor) (37.5mg twice daily); |
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How to treat fibromyalgia ridigity?
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Cyclobenzaprine (Flexaril) (10–50mg)
or tizanidine (Zanaflex) (4–36mg) divided over the day starting at night • Can add tramadol– acetaminophen (37.5mg/325mg) up to four times daily if needed |
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How to treat fibromyalgia pain?
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Pregabalin (Lyrica) ,a duloxetine (Cymbalta),a
or milnaciprana (Savalla) at indicated doses • Acetaminophen (1,000mg four times daily) or tramadol–acetaminophen (37.5mg/325mg up to four times daily) • Gabapentin (Neurotonin) (100–300mg each night to start, increased to 1,200–2,400mg divided three times daily) |
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What is the mechanisms of NSAIDS?
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inhibit prostaglandin (PG) formation They are analgesic, antipyretic, and anti-inflammatory
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What do prostaglandins do?
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sensitize pain receptors to bradykinin and other biochemical mediators, causing vasodilation and increased vascular permeability
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What are the physical effects of protaglandins on the body?
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inflammation Pain, heat, swelling, and redness
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What are some of the protective functions of prostaglandins?
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protect gastric mucosa by increasing mucous production and inhibiting gastric acid production, ensure renal blood flow via vasodilation actions
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What pregnancy category is ASA?
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Category D and shoudl not be given i pregnany can hurt fetus and mother
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When is ASA the chosen NSAID?
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protection against clotting disorders as a secondary preventative measure, as an anti-pyretic, for effective relief of mild-moderate pain, and as an anti-inflammatory for rheumatoid arthritis, tendinitis, and bursitis,
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What does ASA do to platlets?
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Aspirin has an irreversible effect on platelet aggregating properties, and therefore increases the risk for bleeding for the life of the platelets it finds
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Waht do members of the ibuprofen family do?
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inhibit both Cox 1 and 2 pathways and are reversible inhibitors of platelet aggregation.
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What is the difference between NSAIDS?
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primarily half lives and potenticies
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How to dose NSAIDS?
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lower dose for pain adn higher dose for antiinflammatory
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What is a COX 2 inhibitor?
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a new class of NSAIDS that do not effect COX 1 in teh stomach so safe for stomach
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Name some COX 2 inhibitors?
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Celebrex & Aleve
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When should NSAIDS not be used?
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pt with bleeding tendencies or using anticoagulants, hx of gastric bleeding, do not use with digitalis
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Why should NSAIDs not be used during the 3rd trimester
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Can cause premature closure of PDA
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What is defect that can be caused by NSAIDS when used in 1st trimester
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cardiac septal defects
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What to watch for when taking NSAIDS while breastfeeding?
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increased jaundice in newborn
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What is risk with using Tylenol
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liver damage especially when using alcohol or other liver toxic drugs
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X-rays should not be routinely ordered for low back pain T or F
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True
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What is first line drug for low back pain
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NSAIDs and acetominophen
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When shoudl xrays or MRI be ordered for low back pain?
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s/s or radiculopathy or spinal stenosis
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What are some non-pharmacologic treatment for low back pain?
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spinal manipulation; for chronic or subacute low back pain, intensive interdisciplinary rehabilitation, exercise therapy, acupuncture, massage therapy, spinal manipulation, yoga, cognitive-behavioral therapy, or progressive relaxation
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What is first line recommendations for neuro pathic pain?
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certain antidepressants (i.e., TCA & SNRI), calcium channel a2-d ligands (i.e., gabapentin (neurotin) and pregabalin (Lyrica)), and topical
lidocaine |
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What is 2nd line recommendation for neuropathic pain?
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Opioids
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What is 3rd line recommendation for neuropathic pain?
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antiepileptic and antidepressant
medications, mexiletine, N-methyl-D-aspartate receptor antagonists, and topical capsaicin |
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What is neuropathic pain
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neuropathic pain (NP) as pain ‘‘initiated
or caused by a primary lesion or dysfunction in the nervous system’ |
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Waht causes neuropathic pain?
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Many common diseases, injuries,
and interventions cause NP by producing lesions in somatosensory pathways in the peripheral or central nervous system. |
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What drugs are used for centrally acting muscle relaxants?
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diazepam, tizanidine (Zanaflex), soma, flexaril, Skelaxin, alos cause sedation
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What a muscle relaxants used for?
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epilepsy, hypocalcemia, acute & Chronic pain, and localized trauma to muscle
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What causes muscle spascity?
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MS and cerebral palsy,spinal cord injury
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What drugs are used for muscle spascity?
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BAclofen (lioresal) - works within spinal cord
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What muscle relaxant workds directly on skeletal muscle?
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Dantrolene (Dantrium), used for spascity and for Malignant hyperthermia
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What are adverse affects of COX1 & COX2 Inhibitors?
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gastric ulceration, bleeding tendencies, renal impairment resulting from COX1
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What are good affects of COX1 & COX2 Inhibitors?
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protection of MI, reduced inflammation, analgesia, reduced fever, colorectal CA prevention
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How is ASA different that other NSAIDS?
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It irreversability supressed platlet aggregation - new platlets need to be made to replace the old ones
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Is ASA protien bound?
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Yes - 80-90%
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What pain is ASA most effective against?
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joint, muslce and HA, dysmenorrhea, drug of choice for fever reduction in adults
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Why should ASA not be used in childrne with chickenpox or influenza?
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Risk of getting Reyes syndrome - Tylenol should be used in these children
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What is bad about buffered ASA solutions?
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Contain a lot of sodium so not good for someone on sodium restrictive diet
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What is the cardiac risk from long term use of NSAIDS?
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increased risk MI or stroke
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Name uses of ibuprofen?
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anti-inflammatory, anit-pyretic, alalgesic - fever, mild to mod pain, arthritic, dysmennorhea, close PDA in premature infant
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Which NSAID has a 50 hour hallf life with once a day dosing for arthritis?
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Feldene or Prioxicam
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What is acetominophen used for?
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pain and fever - does not reduce inflammation, no GI uspet or renal impairment or does not suppress platlets
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How does acetominophen work?
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inhitbits COX in teh CNS, but not in the periphery
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What is greatest risk with acetominophen?
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liver damage d/t toxic metabolite of tylenol when overdose given
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Why is tylenol more dangerous in an alcoholic person?
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alcohol induced the P450 pathway which increase tylenols toxic metabolites, stores of glutathione (which help bind to toxic metabolite), alcohol increased liver damage
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What 2 types of pain are there?
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nociceptive (injurty to tissue - somatic: bones, joints muslce, or Visceral organs) and neuropathic (injury to peripheral nerves)
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What kinds of drugs help neuropathic pain?
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certain antidepressants (imipramine), anticonvulsnts (carbamazepine, gabapenti) and local anethetics,
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What is first step to pain ladder for cancer pain?
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Non-opioid , 2nd step adds opioids, 3rd: more powerful opioids can add adjunct at any time
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Addiction and dependence are 2 different things - describe
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Addiction is a psychologic or behavior pattern where dependence means need more drug to achieve same effect
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What type of pain med shoudl be avoided in CA patients?
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Agaonist antogonists as they prevent pure opioid agonist from working
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Name TCA's that are used for adjuctive therapy for CA or neuropathic pain?
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Amitoripyline, Desipramine, Doxepin, Imipramine, Nortriptyline
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Name other antidepressants used for CA or neuropathic pain?
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Wellbutrin, Cymbalta, and effexor
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Name anitseizure drugs used for pain?
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carbamazepien (Tegretol), Gabapentin (neurontin), Lamotrigine (Lamictal), Phenytoin (Dilatin), Pregbalin (Lyrica)
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How do CNS stimulants help with CA pain?
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inhance opioids and counteract opioid induced sedation
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How do bisphosphonates work for CA pain?
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reduce CA related bone pain
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What are symptoms of Migraines?
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unilateral (60%), bilat (40%), Throbbing pain, moderate or severe last 4 hr-3 days, activity increases pain, can have N/V, photophobia and phonophobia, onset in morning more common in females
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What are s/s of cluster HA?
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Usually unilateral behind right or left eye, Throbbing sometimes piercing, pain severe, lasts 15 min-2 hr, can have conjuctival redness, lacrimation, nasal congetsion, rhinorrhea, ptosis, miosi on same side at HA, starts at night, more common in males
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What are s/s of tension HA?
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Bilat, feels like headband, nonthrobbing, mild to mod pain, no other s/s, onset during daym, more common in females,
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What factors precipitate a migraine?
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stress, excitement, foods that contain tyramin, nitrates, chocolate, MSG, aspartame, alcohol, caffiene, estrogen, weather changes, hormone changes, lights/glare, loud noise, low sugar, change in altitude
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Patho of migraine
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dilation and inflammaiton of intracrainail bld vessesls
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What can help decrease chance of migraines?
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regular pattern of eating, sleeping and exercise. have low tolerance for ups and downs of life
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Waht ASA like drugs are used for HA?
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those combined with metoclopraminde which enhances absobption good, acetominophen not good alone, good when combined iwth ASA and caffience
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What opioids analgesic works well with migraines?
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Stadol nasal spray
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Drug to help stop a migraine
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Egrotamine - promootes vasoconstriction - addicting, Serotonin Receptor agonists (imitrex)
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Name a serotoni rectport agonist to treat migraines?
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Imitrex - constricting intracranial bld vessels and supress release of inflammatory neuropeptides
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How can imitrex be given?
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po, nasal spray or SQ
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Can imitrex be given in pregnancy?
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no tetrogenic risk cateogory C
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What drugs are used to prevent migraines?
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beta blockers (propranolol - inderal), antiepileptic drugs (depakote and topamax), TCA - amitriptyline (elavil) CA channel blockers (Verapamil & Estrogens
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What suppliments help prevent migraines?
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riboflavin, coQ10, butterbur
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What drugs help prevent cluster headaches?
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predinisone, lithium, verapamil
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What can be done to treat cluster HA once begun?
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100% O2 for 10 minutes, sublingual ergotmine, intranasal dihydroergotomine or SQ sumatripton
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