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28 Cards in this Set
- Front
- Back
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Heroin has a rush b/c? Similar drug oxymorphone has was attribute?
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More lipid soluble = fast acting. Oxymorphone has little antitussive activity.
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Meperidine duration and potency compared to morphine? Cough reflex? Diarrhea?
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Shorter duration and less potency. Little or no effect on cough reflex. Not used for diarrhea.
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Meperidine toxicity causes what and why?
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CNS excitation (seizures, hyperreflexia, tremors) from N-demthylated metaolite normeperidine which has no analgesic activity
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Meperidine side effects compared to morphine:
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Less b/c of antichoinergic activity -> mydriasis and tachycardia
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Drug interactions of meperidine?
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MAOI, SSRI, TCA to cause severe restlessness, excitement, fever, seizures, and delirium (serotonin syndrome)
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Fentanyl: What is 'balanced anesthesia'? What is 'neuroleptanalgesia'?
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When fentanyl or morphine is used to supplement analgesia and sedative effects of NO and halothane. Neuroleptanalgesia is fentanyl and droperidol (butyrophenone) that allows wakeful state for minor procedures
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Fentanyl: 1) duration and potency compared to morphine. 2) administration
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shorter duration but more potent. 2) IV, except for patch/lollipop forms for cancer pt
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Methadone halflife? In addition to withdrawal, list 2 other indications for pain.
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Long halflife. Cancer and neuropathic pain.
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3 indications for Codeine. What about overdose?
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1) cough. 2) diarrhea. 3) moderate pain. An overdose can cause seizures
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2 common combinations of codeine with another drug. What about a sustained oral release form of codeine?
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1) Asprin -> Percodan. 2)Acetaminophen -> Percocet. 3) Oxycodone/Oxycotin
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Codeine: Agonism? 2) bioavailability. 3) Conversion? 4) respiratory depression and dependence
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1) partial agonist. 2) good oral bioavailability. 3) 10% conversion to morphine. 4) less respiratory depression and dependence than morphine
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D-Propoxyphene is used for what, often in combo with what.
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Mild pain, only as effective as aspirin which it is often combo'd with.
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Dephenoxylate use? Note about administration?
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symptomatic Tx of diarrhea. 2) to limit iv use, only available with atropine
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Dephenoxylate solubulity and implication? 2) dependence
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1) insolubility -> limited GI absorption so most of it's action is local. 2) minimal dependence o or centrally mediated opioid effects
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Loperamide use? Distribution? Dependence?
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Used for symptomatic treatment of diarrhea, cannot cross BBB, minimal dependence
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Difenoxin use?
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symptomatic treatment of diarrhea
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Tramadol use? Enhanced risk of? Contraindications?
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1) neuropathic pain. 2) seizures. 3) epilepsy or drugs that lower seizure threshold
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Tramadol MOA? 2) Receptor activity? 3) How can it be blocked? 4) no effect on what?
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1) blocks NE and 5HT reuptake. 2) weak mu affinity. 3) blocked by 5HT3 receptor antagonist odansetron. 4) no effect on respiration
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Pentazocine use and why? Contraindication?
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Moderate pain due to ceiling in analgesic activity. Contraindicated in MI b/c it may inc BP
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Pentazocine receptor affinity? Binding causes what?
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1) Agonist at kappa -> dysphoria, hallucinations, anxiety. 2) Partial antagonist at mu -> can ppt withdrawal. 3) Binds very tight to receptors so this drug is resistant to naloxone reversal!
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4 uses for buprenorphine. Contraindication.
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1) moderate pain (analgesia ceiling effect). 2) safer than methadone for heroin detox. 3) smoking cessation. 4) depression if other Tx fail. Contraindicated for MI b/c possible inc in BP
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Buprenorphine MOA? Binding? Metabolism?
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partial agonist at mu -> can ppt withdrawal. 2) strong binding -> resistant to naloxone reversal. 3) 95% first pass metabolism -> sublingual lozenge
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Naloxone indications (2)
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1) Dx opiod dependence. 2) treat acute opioid overdose and toxicity
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Naloxone MOA
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pure competitive antagonist at opioid receptors -> ppt opioid withdrawal
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Naloxone: First pass metabolism. Duration. Reoccurrence during Tx?
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1) extensive first pass metabolism. 2) short duration. 3) Can be reoccurrence of respiratory depression and coma 1-2 hours after so might need to administer again.
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Naltrexone uses (2):
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1) opioid dependence. 2) dec craving of alcohol.
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Naltrexone MOA
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pure competitive antagonists at opioid receptors -> can ppt opioid withdrawal
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Dextromethorphan use? How? Less effect of what?
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Antitussive activity from depressing cough reflex. Less constipating effect. No analgesic activity unless taken at very high doses
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