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55 Cards in this Set
- Front
- Back
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Opioids CNS effects
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1. analgesia and reduced affective response to pain
2. Euphoria (or dysphoria in opiod-naive) 3. Sedation----> narcosis 4. Respiratory Depression: reduced sensitivity to CO2 5. Cough Suppression 6. Miosis (via parasympathetic pathways) 7. Nausea, vomitus: chemoreceptor trigger zone 8. Truncal Rigidity (especially Fentanyl group) 9. Addiction in non-medical setting |
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Morphine Cardiovascular Effects
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some bradycardia
orthostatic hypotension |
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Morphine GI and Genitourinary effects
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increased smooth muscle tone
increased sphincter tone antisecretory proabsorptive (constipation) increased smooth muscle tone (bladder, urether) increased tone of bladder sphincter muscle |
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Morphine Neuroendorcrine Effects
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Histamine Release
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Opiod's Use
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Analgesia
Anesthesia Acute Pulmonary Edema Cough Diarrhea |
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Opiod Routes of Admin
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Oral
Rectal Subcutaneous Intravenous Certain Derivatives:Intranasal, buccal, transmucosal, transdermal |
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Opiod Agonist: Gold Standard
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Morphine: 3-5 h
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Opiod Short Acting
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Meperidine: 2-3h
colicy pain less spasmodic effects 10x less potent than morphine |
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Opiod Ultrashort Acting (Emergency)
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Fentanyl 20-30 min (distribution)
80x more potent than morphine |
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Opiod used in Anesthesia
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Sufentanyl
Alfentanyl Remifentanyl |
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Opiod Long Acting
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Fentanyl: 9h (terminal elimination half-life)
Methadone 25hr |
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Most Abused Opiod
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Heroin
illegal in the US legal in UK |
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Opiod weak Agonist
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Codeine
10 x less potent than morphine |
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Other Opiods
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Oxycodone
Hydrocodone etc. |
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Opiod Partial Agonists: less addictive
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Tramadol: "ceiling effect: act at mu receptor
Nalbuphine Buprenorphine, buccal, ceiling effect |
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Opioid Antagonists: used for overdose
make sure to use respirator when using for addiction |
Naloxone: half life 60-100min
Naltrexone: long acting 48h Alvimopan: peripheral opiod receptors |
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Opioid Receptor Antitussive (anticough)
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Dextrometorphane
Levopropoxyphene |
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Opiod Receptor Antidiarrheals
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Loperamide
Diphenoxylate, Tintura opii |
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Apomorphine
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structural derivative of morphine but little or no binding to opiod receptors
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Apomorphine PK
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s.c., injection, injectinon pen
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Apomorphine PD
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centrally acting dopaminergic drug
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Apomorphine USE
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Adjunct treatment of parkinson's disease (off-periods)
Powerful emetic Alternative medicine, treatment of addiction |
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Fentanyl Patch
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constant flow rate into epidermis (2.5 ug/cm^2/h)
variable diffusion/perfusion into systemic circulation very useful for chronic pain treatment and cancer patients use for 3 days |
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Fentanyl Patch Bioavailability
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admin every 3 days
plasma concentration vary by factor of 5 not the case with p.o admin |
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Transdermal Fentanyl PK
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3rd order pk.
t1/2 20-30 min (ER Medic) t1/2 terminal 9h (body is saturated) t1/2 trandermal patch 17h (slow absorption from cutaneous depot Problems: apply patch to hairless skin (no soap no razor) ensure steady skin temperature apply patches to 3 different sites alternatively maximum Fe patch dose equivalent 1200 mg Mo |
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Fentanyl Patch Dose Conversion Vs. P.O. Morphine
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current recommendation 1:100
probably adequate ratio 1:70 |
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Opioid Receptors
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u (mu)
k (kappa) o (sigma) o (delta) |
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Mu
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analgesia (mostly supraspinal)
respiratory depression euphoria sedation parasympathetic stimulation (incl. miosis) |
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Kappa
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spinal analgesia
dysphoria/sedation miosis |
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Sigma
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dysphoria, hallucinations
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Delta
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various subclinical effects
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Categories of Pain
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1.Nociceptive: Traumatic, Inflammatory, Colicky, Vascular
2. Neuropathic: Deafferentiation, Sympathetically maintained |
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What does nociceptive pain respond to?
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NSAID or Opiod
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Superficial Pain
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pinch, scratch, venous puncture
easy to localize emotional quality (little or none) autonomous reponse (little or none) |
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Deep Pain
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muscle, bone, joint
difficult to localize upsetting, intimidating, horrifying, devastating mydriasis, nausea, vomiting, collapse shock |
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Visceral Pain
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Colicky pain, tumor pain
other is the same as deep |
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Acute Pain Treatment
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1. reduce pain to tolerable levels
2. quick onset of analgesia is important 3. adjust duration to clinical situation 4. sedation may be useful 5. a/e is important in case of predisposition |
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Chronic Pain Treatment
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1. ensure normal quality of life
2. onset and duration: contigous analgesia 3. sedation is unwanted 4. a/e is always relevant |
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Acute Pain Rules:
Route of application Drugs Doses Dose Interval Co-medication |
1. Intravenous
2. Standard protocols 3. standard protocols 4. ON recurrence of symptoms 5. Relevant in case of predispositon |
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Chronic Pain Rules:
Route of application Drugs Doses Dose Interval Co-medication |
1. oral, rectal, transdermal
2. according to WHO recommendations 3. always individualized 4. By the clock, at constant intervals 5. Mostly required |
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WHO Recommendations for Chronic Pain
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1. Peripheral (NSAID) analgesic
2. Weak (partial) opioid plus 1. 3. Strong opioid plus 1. Rules: by mouth, by clock, by ladder Objective: Analgesia sufficient to restore Quality of Life |
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WHO Recommendations (more specific)
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1. use sufficient dose, don't combine between NSAID and analgesics, prophylaxis: antiucler (ranitidine)
2. One partial opioid: don't combine. prophylaxis of antiucler and laxation 3. Use one strong opioid, provide rescue medication. provide prophylaxis: 1st week: antiemetic drug Metatopramide continously: laxative and antiulcer |
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GI Bleed Low Risk NSAID
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acetaminophen (paracetamol)
ibuprofen |
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GI Bleed Intermediate Risk NSAID
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aspirin
diclofenac |
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GI Bleed High Risk NSAID
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Piroxicam
Indomethacin Ketoprofen have long half lives and high dose per tablet |
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Ketorolac
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only injectable NSAID available for analgesic use in USA
slower onset than morphine but longer duration. has similar efficacy GI bleeding can still occur even with P.O admin |
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Opiod AE and solution
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constipation---> laxatives, alvimopan
urinary retention---> muscarinic drugs/alpha blockers nausea/emesis--->antiemetics (metoclopramide) pruritis---> antihistaminics dizziness euphoria,dysphoria, confusion neurlogic/psychomotor imbalances respiratory depression |
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Opiod Induced Respiratory Depression
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MOA:
1. direct depression of respiratory center neurons 2. Sedation, anesthesia Note: 1. Pain is a powerful stimulus of respiration 2. Sedation precedes any serious respiratory depression in overdose consider mechanical respiration or naloxone |
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Opioid Induced Constipation
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work on all levels:
mu and delta int he brain delta (motility) in spinal cord mu, delta, and kappa in mucosa (absorption increases and secretion decreases) mu in increasing muscle tone |
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Opioid Induced Nausea/Vomitus
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MOA: direct effect on chemoreceptor trigger zone in area postrema
Note: 1. rapid drug invasion aggravates nausea even with low dose; prefer sustained release over rapid injection 2. vagal tone plays a role 3. inform patient of partial tolerance 4. preventive: metoclopramide 5. no ondansetron (constipation) (no 5ht blockers) |
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Opiod Induced Urinary Retention
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MOA:
1. Relaxation of M. Detrusor vesicae 2. Constriciton of M. Sphincter vesicae Note: anticholinergic drugs will aggravate problem Treatment: 1. increase detrusor tone: parasympathomimetics, carbachol, betanehchol 2. relax sphincter tone: alpha1-blockers, prazosin, terazosin |
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Neuromotor skills and Psychological stability in opioid users
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intact w/ users
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Iatrogenic Opiod Addiction
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not very likely unless they have been drug user to begin with.
make sure to you give sustained release.(avoid peaks and valleys) slow and moderate development of tolerance withdrawal symptoms are inconsistent, moderate, easy to manage |
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Pain Managment
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go over example pg. 12
Female patient |
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Unusual Cases
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1. Polytoxic drug addict (heroin, methadone, benzodiazepines) needs surgery for osteomyelitis
2. Pregnant woman, heroin dependent 3. Pregnant woman, broken leg 4. Nursing mother, appendicitis 5. Baby 30 days old, underweight, tremor, seizure |
