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84 Cards in this Set
- Front
- Back
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2 examples of mixed opioids and non-opioids
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1) Vicodin (acetominophen and hydrocone)
2) Tylenol and codiene |
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What is morphine?
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An opioid analgesic
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What 3 forms does morphine come in?
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1) Natural
2) Semisynthetic 3) Synthetic forms |
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What is morphine most often used for?
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Moderate to severe pain
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What are 5 other uses for morphine?
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1) Cough suppression
2) Component of anesthesia 3) Decrease GI motility 4) Adjunct for pulmonary edema 5) Drug of abuse |
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What are 3 endogenous opioids released during stress?
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1) Endorphins
2) Enkephalins 3) Dymorphins |
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What is the mechanism of opioids?
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Bind to opioid receptors in CNS
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What are 3 major types of opioids?
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1) Mu
2) Kappa 3) Delta |
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Describe Mu opioid receptor effects
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Strongest analgesic effects which cause the most severe side effects (low RR, constipation, dependence)
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Describe Kappa opioid receptor effects
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Analgesic, but has less side effects than Mu (sedation, psychotic effects)
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What are 2 Kappa opioid receptor side effects?
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1) Sedation
2) Psychotic effects |
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Describe Delta opioid receptor effects
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Analgesic, but side effects are less severe than Mu and Kappa receptors
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What is a side effect of Delta opioid receptors?
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Hormonal release
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What is a mixed opioid?
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Agonist/Antagonist mixture where 1 or more of the 3 receptors (Mu, Kappa, Delta) is activated and the other sites are blocked
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What type of opioid is less likely for dependence?
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Mixed agonist/antagonist mixture
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What is an example of a mixed agonist/antagonist opioid?
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Agonist to Kappa
Antagonist to Mu |
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What is an opioid couple with at receptors in the CNS and possible PNS?
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G-proteins (Mu, Kappa, Delta)
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What do opioids inhibit?
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Afferent pain transmission in ascending pain pathways like the spinothalamics
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What 2 areas do opioids affect pain pathway synapses?
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1) Pre-synaptic
2) Post-synaptic |
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How do opioids affect pain at the presynaptic area?
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G-proteins inhibit Ca2+ entry and cAMP release causing less neurotransmitter release
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How does opioids affect pain at the post-synaptic site?
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G-proteins open K+ channels (lose K+) and hyperpolarize the membrane making it harder to excite the neuron
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What do opioids activate?
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Descending pain control pathways via disinhibition (inhibit the inhibitor to send less pain signals)
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What 2 routes are opioids usually given?
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1) oral
2) parenteral |
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If an opioid is given intravenously then how is it usually administered?
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PCA pump for safety to not overdose or become addicted
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Aside from IV, what 3 other ways can opioids like morphine be given parenteral routes?
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1) Epidural
2) Intrathecal 3) Transdermal (patches) |
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Where are opioids metabolized?
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In the liver
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What 2 things are important for effective treatment for pain in acute care?
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1) Route of admin
2) Dosing schedule |
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What must happen with the does of an opioid if given orally?
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Dose must be increase due to the first-pass effect and may not be absorbed well
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What are 4 types of opioids?
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1) Strong agonists (Mu agonists)
2) Mild-moderate agonists 3) Mixed agonists-antagonists 4) Antagonists |
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What is an example of a mild-moderate agonist?
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Codiene (3 receptors reached at a lower affinity and lower efficacy)
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What type of opioid can have hallucinogenic effects?
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Mixed- agonist-antagonists and Delta
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Opioid type used for recovery from dependence of Mu and blocks Mu from pain?
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Mixed agonist-antagonists that stimulate Kappa or Delta, but blocks or partially stimulates Mu
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What does an opioid antagonist do? When is it used?
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Binds to opioid receptor, but has no effect
Used when a pt is dependent or wants less side effects |
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What are 5 adverse effects of opioids?
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1) Sedation
2) Possible euphoria 3) Respiratory depression 4) Possible heart problems (OH) 5) GI distress/constipation (SCI, post surgery) |
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What are 4 types of problems when using opioids?
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1) Addiction
2) Tolerance 3) Physical dependence 4) Withdrawal symptoms |
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What is an addiction?
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Compulsive drug use, also with psychological dependence
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What is tolerance?
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Higher dose of drug to get the same effect (ex. enzyme induction, desensitization)
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What is physical dependence?
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Onset of withdrawal if drug is suddenly stopped
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What are 6 opioid withdrawal symptoms?
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1) Flu-like symptoms
2) Insomnia 3) Irritability 4) Tachycardia 5) Uncontrollable yawning 6) Muscle aches |
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Elimination of physical symptoms does not mean...
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the pt no longer desires the drug
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What are 2 pharmacological treatments for opioid addiction?
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1) Methadone
2) Buprenophine (Buprenex) |
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What opioid addiction treatment drug is easily tapered for a pt who is addicted?
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Methadone
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What drug is a strong opioid agonist?
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Methadone
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What drug has milder withdrawal symptoms than other opioids?
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Methadone
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What opioid addiction drug treatment is withdrawn slowly in conjunction with non-pharmacological treatment like counseling?
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Methadone
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What is a mixed agonist-antagonist opioid addiction treatment?
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Buprenophine (Buprenex)--partially agonist to Mu and strong antagonist to Kappa (no hallucinations, but still controls pain)
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What are 4 NSAID uses/effects?
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1) Decrease inflammation
2) Decrease mild-mod pain 3) Decrease fever 4) Anticoagulant |
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What is the mechanism of NSAIDs?
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Anti-inflammatory and analgesic effects due to inhibition of eicosanoid synthesis (inhibits PG and TX synthesis via inhibition of COX enzyme systems)
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What are eicosanoids?
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20 carbon double bonds named for their structure (PG, TX and Leukotrienes involved in mediating inflammation and other pathological responses)
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What are prostoglandins?
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Endogenous lipid-like compounds that help regulate a wide array of cell functions (pro-inflammatory)
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What are thromboxanes?
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Vasoconstricts and platelet aggregation
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What are leukotrienes?
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Pro-inflammatory; especially in airways
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What are 2 pro-inflammatory substances?
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1) Prostoglandins
2) Leukotrienes |
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What 2 eicosanoids produce inflammation, fever, clots and menstrual problems?
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1) Prostoglandins
2) Thromboxanes |
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What do PGs and TXs cause? (5)
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1) Fever
2) Pain 3) Inflammation 4) Clots 5) Menstrual problems |
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What is eicosanoid synthesis made up of?
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Phospholipids that break down into arachadonic acid
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What 2 routes can phospholipids go in breakdown of eicosanoid biosynthesis?
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1) Lipoxygenase (LOX)
2) Cycloxygenase (COX) |
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What does the COX pathway produce?
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1) Prostoglandins (PGs)
2) Thromboxanes (TXs) |
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What does LOX pathway produce?
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Leukotrienes
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What are 2 COX enzymes?
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1) COX-1
2) COX-2 |
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What is COX-1?
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Normally produced in homeostasis and protects GI lining
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What is COX-2?
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Produced in injured cells (clots) and breaks down GI lining over time
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What are aspirin (ASA) and most NSAID effects on COX pathways?
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Affect both COX-1 and COX-2 breaking down the GI lining over time
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What are 4 ASA (acetylsalicyclic acid or aspirin) uses?
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1) Treat mild to moderate pain and inflammation (esp. musculoskeletal and menstrual cramps
2) Treat fever in adults (not kids) 3) Treat vascular disorders at low doses 4) Prevents colorectal cancer (CA) |
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What are 2 adverse effects of ASA or aspirin?
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1) GI problems
2) Renal and liver problems if pre-existing disease or low body water |
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What are the 5 overdose signs and symptoms of ASA or aspirin?
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1) HA
2) Decreased hearing 3) Confusion 4) GI distress 5) Metabolic acidosis and dehydration |
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What are the adverse effects of NSAIDs (ASA)? (2)
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1) Reye syndrome in kids
2) ASA intolerance (super-sensitivity) |
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What is Reye syndrome? (4)
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1) High fever
2) Vomiting 3) Liver dysfunction 4) Leads to unresponsiveness and possibly death (usually after flu or chicken pox) |
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What are the effects of ASA on bone healing?
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Do not use after fracture or bone surgery (slows bone growth)
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What are 3 examples of NSAIDs that are ASA-like?
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1) Ibuprofen (Advil, Motrin)
2) Naproxen (Naprosyn) 3) Naproen Sodium (Aleve) |
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What are 3 main differences of NSAIDs and NSAIDs (ASA-like)?
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1) Side effects/safety
2) Cost (many are Rx only) 3) No risk of Reye syndrome |
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What are 2 adverse effects of COX-2 selective inhibitors?
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1) MI
2) CVA--shifts to favor increase platelet activity and high risk of clotting in coronary and carotid arteries in some pts |
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What are 3 key similarities/differences between acetominophen and NSAIDs?
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1) Same analgesic and antipyretic effects
2) No apparent anti-inflammatory or anticoagulant effects in oral doses 3) No GI irritation or Reye syndrome |
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What can high doses of acetominophen cause?
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Liver toxicity
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What types of pts cannot take acetominophen?
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Pts with liver problems like breaking down ethanol
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What is acetominophen often used for?
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Used first for early OA pts when they are not inflammed and those with musculoskeletal problems
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When is acetominophen appropriate to use?
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When a pt is not inflammed and when there is GI problems
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What is the mechanism of acetominophen?
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Not fully understood--inhibits COX (most likely PGs) and may preferentially inhibit CNS PGs (COX-3?)
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What is 80-90% of ASA bound to?
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Plasma proteins in the bloodstream (i.e. albumin)
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Where does ASA break down occur?
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In the bloodstream and not all in the liver (unbound drug hydrolized to active metabolite)
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Where does ASA-like substances break down in the body?
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In the bloodstream and further in liver (similar to aspirin)
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How is acetominophen absorbed?
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Rapidly--much less is bound to plasma proteins (break down mostly in liver)
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What does Tylenol or acetominophen produce in the liver?
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NAPQI (toxic metabolite) that must be conjugated for detoxification and excretion
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What 2 ways can the liver be damaged by too much acetominphen?
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1) If high NAPQI
2) If liver cannot break down NAPQI |
