-1-KNOWLEDGE OBJECTIVES FOR MEDICAL PHARMACOLOGY: CNS PHARMACOLOGYSPRING 2012Pharmacology of sleep1. Know the sleep stages2. Know the effects of acute and chronic alcohol use on sleep.3. Know the role of GABA A receptor complex in the hypnotic action ofbarbiturates, benzodiazepines and non-benzodiazepines.4. Know the effects on sleep of benzodiazepines, imidazopyridines, andcyclopyrrolones.Local anesthetics:Basic structural characteristics of local anesthetics.Examples of ester- and amide-linked anesthetics.Mechanism of nerve conduction.Mechanisms of local anesthetic action.Metabolism of ester- and amide-linked local anesthetics.Why are vasoconstrictors often added to the local anesthetic preparations?Toxicity and side effects of local anesthetics. Please pay attention to centralnervous system toxicity and cardiovascular toxicity.Major clinical uses of local anesthetics.General AnestheticsDefinitions: partial pressure, MAC, blood/gas partition coefficient, oil/gas partitioncoefficientWhat determines anesthetic potency?What are the 4 potential targets for the action of general anesthetics?How do blood/gas solubility, ventilation rate and cardiac output affectequilibration of anesthetics (rate of induction of anesthesia)?What is the mechanism of the “concentration effect” and the related “second gaseffect”?-2-What factors determine the rate of anesthetic equilibration into different tissues?What is the route of elimination of general anesthetics and how is recovery fromanesthesia affected by the blood/gas partition coefficient, ventilation rate andcardiac output?What are the common pharmacological effects of inhalational anesthetics?Know the major differences between the inhalational anesthetics (e.g., which ismost/least potent, induction/recovery rate, etc.- see table on handout; don'tneed to memorize numbers).What are the major uses of the various intravenous anesthetic agents discussedand their major advantages and disadvantages?Herb-Drug InteractionsDistinguish between pharmacokinetic and pharmacodynamic interactionsKnow the principle pharmacokinetic and pharmacodynamic interactions of St.John’s Wort, i.e. induction of CYP, and serotonin syndrome/photosensitivityKnow the main reasons for herb-drug interactions with Warfarin, i.e. vitamin Kactivity; decreased GI absorption, inhibition of CYP2C9, antiplatelet activity,decreased thromboxane synthesis, coumadinKnow the main reasons for caution with herbs during surgical or dentalprocedures, i.e. anticoagulant effects, sedation, or stimulus (modify anesthesia) Opioid Analgesic Drugs1. Know about mechanism of nociception (physiology)Dorsal horn of the spinal cord – gate control mechanism2. Know about classification of opioid analgesic drugsStrong agonists – morphine, meperidine, methadone, heroin, fentanylModerate agonists – propoxyphene, codeineMixed agonists-antagonists – pentazocine, nalbuphine, buprenorphineAntagonists – naloxone, naltrexone3. Know about endogenous opioid peptidesEnkepalins, endorphins, dynorphins, endomorphins4. Know about opioid receptors and the mechanism of actionMu , Kappa , Delta . All G-protein coupled receptors. Increase K+ efflux(hyperpolarization) and reduce voltage-gated Ca2+ entry.5. Know about the sites of opioid receptor expressionMu - periaqueductal gray, spinal trigeminal nucleus, cuneate and gracile nuclei,thalamus,nucleus of solitract, nucleus ambiguus, parabrachial nucleus, neurons ofthe postremaKappa- hyphothalamic region-3-Delta - dorsal horn of the spinal cord6. Know about the pharmacological actions of opioidsCNS - analgesia, sedation, euphoria, mental clouding, respiratory depression,nausea and vomiting, cough reflex, pupillary constriction (miosis)GI – constipation, biliary tract spasm7. Know about the contraindications of opioidsDecreased respiratory reserve (emphysema, severe obesity, asthma), biliarycolic, head injury, reduced blood volume, hepatic insufficiency, convulsant states8. Know about tolerance and physical dependenceTolerance develops to – analgesia, euphoria, sedation, lethal dose, nauseaTolerance does not develop to - miosis, constipation, respiratory depression(partial)Physical dependence – treat with methadone (long acting opioid)9. Know about antitussive and anesthetic usage of opioidsAntitussive – codeine, dextromethorphanAnesthetic – fentanyl, sufentanil10. Know about antagonistsNaloxone – readily reverses the coma and respiratory depression of opioidoverdoseNaltrexone – longer duration of action (up to 48 hrs)Antiseizure DrugsKnow what a seizure is, its potential causes and how it relates to epilepsy.Know the mechanisms by which neurons become hyperexcitableKnow how seizures are classified (i.e., simple partial vs. complex partial vs. tonicclonic,etc. -see table in handout)Know the general principles of antiseizure drug therapyKnow the identified mechanisms by which antiseizure drugs work.Know the drugs of choice for the various types of seizures, their mechanism ofaction and major side effects.What are the 4 major types of drug interactions seen with antiseizure drugs?Antihyperlipidemic DrugsDescribe the pathophysiology involved in the formation and progression of atheroscleroticplaques, and distinguish how HDL, LDL and TG levels are related to the risk ofatherosclerosis.-4-For each class of antilipidemic drugs, describe the mechanism of action, effect on serumlipids, salient adverse effects, drug interactions, and contraindications.Lectures 57-59 PsychopharmacotherapyAntipsychotic Drugs1. Know mechanism of action for first generation (“traditional”) and secondgeneration (“atypical”) antipsychotics, and the major classes of antidepressantsand anxiolytics.2. Know how first generation (“traditional”) and second generation (“atypical”)antipsychotics differ.3. Understand what types of side effects are associated with blockade of alpha1-adrenergic, muscarinic, and histamine receptors.4. Understand the principles of drug interactions such as CYP inhibitors andinducers, protein binding and protein saturation.Antidepressants and mood stabilizers1. Discuss key difference(s) between unipolar and bipolar mood disorders.Identify various antidepressants classified by mechanism of action(s) (e.g.,multiple receptor actions, SSRIs, MAO-Is).2. Discuss the impact of agonism or antagonism at pre-synaptic autoreceptors(i.e., short-loop negative feedback system.3. Recognize possible mechanisms by which mood stabilizers
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