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195 Cards in this Set
- Front
- Back
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What two groups of alcaloids does opium resin contain?
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Phenanthrenes and Isoquinolines
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What is an opiate?
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A drug delivered from opium poppy
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What are opioids?
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Includes opiates, opiopeptines, synthetic, and semisynthetic drugs
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What are opiopeptines?
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Endogenous peptides meaning they are produced in the body naturally
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How much more potent are opiopeptines than morphine?
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200
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What are the four types of endogenous opioids?
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Enkephalines, dynorphins, endorphins, and endomorphins
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How many amino-acid peptides do enkephalines have?
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5. They are pentapeptides
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What are they two types of dynorphins?
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A and B
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How many amino-acid peptides do dynorphins have?
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17
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How many amino-acid peptides do endorphins have?
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31
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How many amino-acid peptides do endomorphins have?
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4
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Where are opioid receptors found?
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The limbic system, the medial and lateral thalamus, the hypothalamus, the medulla oblongata, and the spinal cord
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How many subtypes of opioid receptors are there?
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4
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What type of receptors are opioid receptors?
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G-protein family
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What is the main effect of opioid receptors on the cell membrane?
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Inhibition
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What is the process of opioid receptor inhibition?
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Phospholipase C is activated which inhibits adenylate cyclase which inhibits cAMP. This opens K channels causing repolarization and closes Ca channels causing the inhibition of neurotransmitter release.
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What are the four types of receptors?
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Mu, Kappa, Sigma, Delta
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What symptoms is Mu responsible for?
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Analgesia, supraspinal analgesia, respiratory depression, euphoria, and physical dependence
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What effects is Kappa responsible for?
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Spinal analgesia, miosis, and sedation
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What symptoms is Sigma responsible for?
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Hallucinations, respiratory stimulation, and vasomotor stimulation
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What symptoms is Delta responsible for?
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Periphery
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What is the molecular weight of Morphine?
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285
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What are the Morphine-like agonists?
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Morphine Sulphate, Hydromorphone, Oxymorphone, and Heroin
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What are the Codeine-like agonists?
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Codeine, Tramadol, Hydrocodone, and Oxycodone
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What are the synthetic opioid agonists?
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Meperidine, Fentanyl, Methadone, Levophanol
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What are the Agonists/Antagonists?
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Pentazocine (Talwin), Butorphanol (Stadol), and Nalbuphine (Nubain)
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What are the antagonists?
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Naloxone (Narcan) and Naltrexone (Deprade, ReVia)
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What are the CNS effects of Morphine?
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Dose-related analgesia, sedation and euphoria, stimulation of chemoreceptor trigger zone (CTZ), N/V, miosis, small permeability of blood brain barrier, hypothermia, and convulsions at high doses
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What are the respiratory/digestive side effects of Morphine?
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Respiratory depression, chest wall rigidity, bronchoconstriction, decreased peristalsis, stomach motility, and biliary/pancreatic secretion. Also constricts the sphincter of Oddi in pancreas
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What are the urogenital side effects of Morphine?
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Urinary bladder contraction, uterine tone reduction, and crosses the placental barrier.
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What are the skin effects of Morphine?
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Allergic skin rashes and dilation of cutaneous vessels
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Where is Morphine well absorbed?
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GI Tract
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Is first pass metabolism present when taken orally?
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Yes
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How much Morphine is protein-bound when in the body?
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30%
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Where is Morphine metabolized?
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Liver
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What is Morphine metabolized to?
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Morphine 6-glucuronide
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What are the clinical uses of Morphine?
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Analgesia, pulmonary edema, severe diarrhea, cough suppression, and anesthesia
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If Morphine is abruptly discontinued, when do withdrawal symptoms begin to occur?
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8-10 hours after last dose
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How long do withdrawal symptoms of Morphine last?
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10 days
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What are the symptoms of withdrawal?
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Lacrimation, violent coughing/sneezing, insomnia, hypertension, tachycardia, depression, vomiting, diarrhea, and dehydration
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What segment of Morphine comprises codeine?
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3-methylether of morphine
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What is the potency of codeine?
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1/12th of morphine
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What does 30mg of codeine equal to in relation to aspirin?
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600mg
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What are the benefits of codeine over morphine?
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Less sedation, decreased respiratory depression, less GI effects, decreased rate of addiction, it is a good oral analgesic for mild pain
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What is heroin converted to in the body?
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Morphine
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What is the other name for heroin?
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Diacetylmorphine
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What is the equivalent dosage of heroin to morphine?
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3mg heroin = 10mg morphine
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What is the molecular weight of methadone?
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309.45
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Methadone is orally more effective than morphine. True or False.
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True
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What happens to methadone in the tissues?
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It gradually accumulates
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What is the danger of methadone?
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Cumulative toxicity
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What is the molecular weight of Meperidine?
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247.3
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What is the analgesic potency of meperidine?
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1/8th of morphine
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What are some significant side effects of meperidine?
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Smooth muscle spasm (bronchospasm), atropine-like activity (dry mouth, blurring of vision), hyperthermia, and convulsions with MAO
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Why is meperidine preferred to morphine during labor?
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Shorter duration of action
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What happens with large doses of Meperidine?
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CNS excitation
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What is the analgesic potency of Fentanyl?
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80/1 of morphine
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What happens when high doses of Fentanyl are given?
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Muscular rigidity
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What was the first pure opioid antagonist?
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Naloxone
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What does Naloxone do?
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It reverses respiratory depression, reverses cardiovascular effects, and precipitates withdrawal
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Naloxone is rapidly metabolized. True or False?
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True
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When is Naltrexone contraindicated?
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Anytime the liver is impaired.
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What adverse effects does Naltrexone have?
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Anxiety, cramps, and joint pain
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What are the three major classes of sedative-hypnotics?
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Barbiturates, benzodiazepines, and miscellaneous
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What is the parent compound of barbiturates?
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Barbituric acid
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Does barbituric acid depress the CNS?
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No
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What does the efficacy of barbiturates depend on?
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Lipid solubility
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What is the ultra-short barbiturate, what is its time of action, and what is it typically used for?
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Thiopental, 0-30s, adjuvant to anesthesia
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What are the short-acting barbiturates, what is their time of action, and what are they classified as?
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Hexobarbital, pentobarbital, secobarbital, 2 hours, hypnotics
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What are the intermediate barbiturates, what is their time of action, and what is their classification?
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Amobarbital, butabarbital, 3-5 hours, hypnotics
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What are the long-acting barbiturates, what is their time of action, and what is their classification?
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Barbital, phenobarbital, >6hours, hypnotics/sedatives/antiepileptics
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Where are the barbiturates absorbed?
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Stomach, small intestine, rectum, intramuscular
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What two barriers are crossed by barbiturates?
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Blood-brain barrier and placental barrier
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What receptors do barbiturates and benzodiazepines act on?
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GABA
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Both barbiturates and benzodiazepines potentiate the binding of GABA to GABA receptors. True or False?
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True
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What do barbiturates stimulate physiologically?
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Hepatic microsomal system
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What are the clinical effects of barbiturates?
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Low selectivity, narrow therapeutic index, tolerance, suppress REM sleep, high potential for dependence/abuse, oversedation, drowsiness, withdrawal (seizures, tremors, hallucinations)
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What was the first benzodiazepine?
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Valium (Diazepam)
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How do barbiturates act on GABA receptors?
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GABA binds to GABAa receptor. Barbiturates binding to receptor potentiates this binding. Chloride rushes into the cell making the membrane stable and making depolarization difficult.
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What are the therapeutic uses of Valium?
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Treatment of anxiety, anesthetic premedication, sedative-hypnotic, seizures, treatment of alcohol withdrawal, treatment of night terrors, treatment of panic attacks, obstetrics during labor
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What are the pharmacodynamics of benzodiazepines?
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They potentiate the binding of inhibitory GABA to GABA receptors, benzodiazepine receptors are in the thalamus, the limbic system, and cortex; and they bind to GABAa to increase the frequency of calcium channel opening
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What is the difference between the pharmacodynamics between barbiturates and benzodiazepines?
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Cloride channels open more frequently in benzodiazepines and channel opening is prolonged in barbiturates
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What drug interactions should be avoided in benzodiazepines?
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Alcohol, opioids, anesthetics, antidepressants, and MAO inhibitors
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What is the action and 1/2 life of Midazolam?
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Short acting and 2.5 hours
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What is the action and 1/2 life of Lorazepam?
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Intermediate acting and 14 hours
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What is the action and half-life of Diazepam?
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Long-acting and 2-4 days
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What can chronic benzodiazepine use cause?
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Cognitive impairment, tolerance, and dependence
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How does Flumazenil work?
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It is a competitive antagonist for benzodiazepine site on GABAa complex
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What is the molecular weight of chloral hydrate?
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165.5
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Chloral hydrate suppresses REM. True or False?
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False
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Does chloral hydrate have an effect on RR/HR?
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No
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What does a sudden break in chloral hydrate tolerance lead to?
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Acute intoxication
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How does one determine cardiac output?
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CO = HR x SV
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What two systems control heart rate?
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Parasympathetic and Sympathetic nervous systems
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What two factors determine stroke volume?
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SNS and venous return
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What factors control the return of venous blood to the heart?
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Low pressure in right atrium, low pressure in thoracic cage, valves provide unidirectional flow, and muscle pumps
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What three factors control BP?
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Resistance, HR, volume
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What does sympathetic stimulation have upon the heart?
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Norepinephrine increases permeability of fibers to sodium and calcium. Increases heart rate. Increases contractility
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What are the parasympathetic effects on the heart?
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Acetylcholine increases permeability of fibers to potassium and increases negativity. Decreases HR. No effect on contractility
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Where is the majority of blood in CVS?
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Veins
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How much blood is in the veins?
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64%
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How much blood is in the arteries?
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13%
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How much blood is in the pulmonary circulation?
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9%
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How much blood is in the heart and arterioles/capillaries?
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7%
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What is Ohm's Law?
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Q(flow in the system) = P(pressure in the system)/R(resistance in the system)
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The sum of all resistances = total resistance in series or parallel?
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Series
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Total resistance is less than the sum of all resistances in series or parallel?
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Parallel
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What is Poiseulles Law?
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The physical law that concerns the voluminal flow of an incompressible viscous liquid through a cylindrical tube
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What are the three major factors affecting blood flow?
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Radius, viscosity, and length
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Small changes in the radius of a vessel may significantly affect the resistance to blood flow. True or False?
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True
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What is blood viscosity determined by?
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Hematocrit
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What is the viscosity of plasma?
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1.8
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What is the viscosity range of whole blood?
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3-5
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What is the viscosity of water?
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One
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What are the three factors in blood flow control?
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Local, humoral, and nervous
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What products comprise local blood flow control?
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Carbon dioxide, lactic acid, adenosine, histamine, K+ ions, H+ ions, and nitric oxide
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What products comprise humoral blood flow?
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Vasoconstrictor = epinephrine, norepinephrine, angiotensin, endothelian, and vasopressin
Vasodilatory = epinephrine, bradykinin, serotonin, histamine, prostaglandins, and nitric oxide |
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What two factors comprise nervous system blood flow control?
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Innervation of all blood vessels except capillaries and precapillaries. Vasoconstrictor and vasodilatory fibers
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Which system is the most important in blood flow control?
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Nervous
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What is solubility?
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The ability for a given solute to dissolve in a solvent. During equilibrium, dissolved gas molecules leave liquid at the same rate as other molecules that are dissolving
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What is Henry's Law?
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At a constant temperature, the amount of a given gas dissolved in a liquid is directly proportional to the partial pressure of that gas in equilibrium with that liquid
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At higher temperatures, less gas dissolves. True or false?
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True
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Why do bubbles of air form in infusion lines passing through warming coils?
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At higher temperatures, less gas dissolves
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What is the solubility of nitrogen at temp 37 and partial pressure of 100kPa?
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0.014L
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What is the solubility of nitrous oxide at temp 37 and partial pressure of 100pKa?
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0.39
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Do gases have different solubilities?
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Yes
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At 21% O2 and 1 ATM, what is the amount of O2 in the blood?
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0.3m/O2
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Anesthetics with high solubilities are more powerful. True or false?
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True
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What is the solubility of nitrous oxide in blood at a temp 37 and partial pressure of 100kPa?
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0.47L
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What four factors determine the solubility of a gas?
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Partial pressure, temperature, gas, liquid
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What is a solubility coefficient?
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A measure of how easily gas dissolves in liquid
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What is the Bunsen Solubility Coefficient?
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The volume of gas in milliliters at standard temperature and pressure that is dissolved in one milliliter of liquid
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What is the Oswald Solubility Coefficient?
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The volume of gas which dissolves in one unit volume of liquid at a known temperature
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What is the partition coefficient?
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The ratio of a substancein one phase compared with the other. The two phases are of equal volume and are in equilibrium
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At a temp of 37, what is the nitrous oxide blood-gas partition coefficient?
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0.47
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At a temp of 37, what is the nitrous oxide gas-blood partition coefficient?
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2.1
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How much nitrous oxide dissolves in 1 L of oil?
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1.47
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How much nitrous oxide dissolves in 1 L of blood?
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0.47
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Do anesthetics have receptor sites?
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No
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Do anesthetics have pharmacologic antagonists?
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No
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What is at the foundation of anesthesia?
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Overton-Meyer correlation
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What are the principles of the Overton-Meyer correlation?
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Anesthetic potency is proportional to lipid solubility; there is a linear relationship b/t oil/gas partition coefficient and potency; olive oil is used to measure lipid solubility
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How far apart are alveoli from capillaries?
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0.1-0.5micrometers
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What is the surface area of alveoli?
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60-100m2
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What three factors affect alveolar stability?
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Alveolar interdependence, pulmonary surfactant, residual volume
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What is surfactant?
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Phospholipids that reduce surface tension of the alveoli
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What alveolar cells produce surfactant?
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Type II
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What is LaPlace's Law?
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P(collapsing pressure) = 2T(surface tension)/R(alveolar radius)
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What is the range of negative pressure in the pleural cavity?
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-4 to -9
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What is a pneumothorax?
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A life-threatening condition in which pressure within the pleural cavity is equivalent to atmospheric pressure
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What is tidal volume and what does it equal?
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The volume of air that is breathed with normal respiration. It is typically 500ml
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What is inspiratory reserve volume and what does it equal?
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IRV is the additional volume of air that can be breathed in after normal respiration. It equals 3000ml.
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What is expiratory reserve volume and what does it equal?
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ERV is the additional volume of air that can be exhaled after normal respiration. It equals 1100ml.
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What is residual volume and what does it equal?
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The volume of air that remains in the lungs after maximal exhalation. It equals 1200ml.
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What is inspiratory capacity?
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This is the volume of air that can be inhaled after normal exhalation
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What is vital capacity?
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The volume of air that can be forced out of the lungs after maximal exhalation
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What is functional residual capacity?
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The volume of air that resides in the lungs after normal exhalation
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What is total lung capacity?
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The volume of air in the lungs after maximal inhalation
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What is minute respiratory volume?
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The volume of air that can be inhaled/exhaled in one minute
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What is alveolar ventilation rate?
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The volume of air that reaches the alveoli per unit time
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What is anemic hypoxia?
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When total O2 in blood is low but pO2 is normal
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What is histotoxic hypoxia?
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When cells are receiving enough O2 but they cannot utilize it well because they have impaired oxidative phosphorylated enzymes
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What is circulatory hypoxia?
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When organs and tissues do not receive enough oxygen
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What is hypoxic hypoxia?
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Generalized hypoxia
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If pO2 decreases and/or pCO2 rises, what happens?
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Peripheral chemoreceptors are triggered and ventilation increases to increase pO2 or decrease pCO2
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What are the 3 categories of general anesthesia?
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Inhalation, intravenous, and balanced
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Why do we use premedications in anesthesia?
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They reduce the amount of anesthesia needed
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If you increase MAC, do you stimulate or depress the CNS?
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You stimulate the CNS
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What factors increase your MAC?
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Alcoholism, CNS stimulants, hyperthermia, young age
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What factors decrease your MAC?
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Anemia, other anesthetics, CNS depressants/sedation, Lithium, Lidocaine, opioids, hypothermia, pregnancy, very young age, and alpha 2 agonists
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What are the physiological effects of anesthesia on the CNS?
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Decreased awareness, decreased cerebral metabolism, increased cerebral blood flow, increased CSF pressure, EEG changes, seizures, shivering
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What are the physiological effects of anesthesia on the respiratory system?
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Bronchodilation, increased RR, decreased minute volume, decreased alveolar ventilation, depressed cerebral chemoreceptors, depressed response to hypoxia
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What are the physiological effects of anesthesia on the heart?
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Decreased BP, decreased myocardial oxygen consumption, decreased sympathetic response, decreased AV conduction, increased arrhythmias, increased cutaneous blood flow
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What are the physiological effects of anesthesia on the musculoskeletal system?
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Skeletal muscle relaxation, uterine tone relaxation, malignent hyperthermia
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Why was diethyl ether halted in use?
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Flammable
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What are the anesthetic properties of IV barbituates?
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Rapid induction, rapid recovery, respiratory depression, cardiac depression
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What are the anesthetic properties of benzodiazepines?
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Rapid induction, rapid recovery, minimal respiratory depression
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What are the anesthetic properties of ketamine?
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Hallucinations, trance-like state
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What are the anesthetic properties of opioids?
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Analgesia, respiratory depression, constipation, N/V, prolongs awakening, wheezing, hypotension
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How is Halothane biotransformed?
|
5% is biotransformed by P-450 by removal of bromide and chloride
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Halothane is safe for children. True or false?
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True
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What does Halothane do to metals and rubber?
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It corrodes metal and reacts with rubber
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What is the major cardiac effect of halothane?
|
It increases sensitivity to catecholamines
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What are the adverse effects of halothane?
|
Decreased liver function and malignent hyperthermia
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When does halothane hepatitis occur?
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2-5 days post-op evidenced by fever and vomiting
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What populations are susceptible to halothane hepatitis?
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Middle age, women, preexisting liver disease
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Children are susceptible to halothane hepatitis. True or false
|
False
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What anesthetic is characterized by free flouride in the system and nephrotoxicity?
|
Methoxyflurane
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Methoxyflurane is characterized by what two side effects?
|
Free flouride in the body and nephrotoxicity
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What anesthetic dissolves in rubber, stimulates salivation, and suppresses laryngeal reflexes?
|
Enflurane
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Enflurane is characterized by what side effects?
|
Stimulates salivation, dissolves in rubber, and suppresses laryngeal reflexes
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What anesthetic is used in day surgery and cannot be used in infants/children w/mask because of upper airway irritation?
|
Desflurane
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Is nitrous oxide combustible?
|
Yes
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|
What concentration of nitrous oxide maintains anesthesia?
|
75-80%
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What organ is responsible for the elimination of nitrous oxide?
|
The lungs via respiration
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