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Medicine LibreTexts

Book: Principles of Pharmacology (OCW)

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  • The object of this text is to teach students an approach to the study of pharmacologic agents. The focus is on the basic principles of biophysics, biochemistry and physiology, as related to the mechanisms of drug action, biodistribution and metabolism. The course consists of lectures and student-led case discussions. Topics covered include: mechanisms of drug action, dose-response relations, pharmacokinetics, drug delivery systems, drug metabolism, toxicity of pharmacological agents, drug interaction and substance abuse. Selected agents and classes of agents are examined in detail.

    • 1: Introduction to Pharmacology
      Pharmacology (Gr. pharmakon - a drug or poison, logos - word or discourse) is the science dealing with actions of drugs on the body (pharmacodynamics) and the fate of drugs in the body (pharmacokinetics). It overlaps with pharmacy, the science of preparation of drugs; much of it deals with therapeutics, the treatment of disease (by whatever means). Toxicology is the branch of pharmacology dealing with the "undesirable" effects of drugs on biological processes.
    • 2.1: Pharmacokinetics I
      Describe the physicochemical and physiological factors that influence the absorption of drugs from enteral and parenteral routes of administration, their distribution within the body, and their routes and mechanisms of elimination. Explain how dose, bioavailability, rate of absorption, apparent volume of distribution, total clearance, and elimination half-life affect the plasma concentrations of a drug after administration of a single dose.
    • 2.2: Pharmacokinetics II - Dosing
    • 3: Case Study - Anticholinesterase
      Reversible versus irreversible inhibition of AchE causes build up of Ach at synapse Toxicity associated with AchE inhibitors (patient case!) include global nicotinic, muscarinic, & CNS effects (DUMBBELLS) Treatment for Exposure to Irreversible Inhibitors Atropine – counteract ACh agonism 2-Pralidoxime – prevent aging
    • 5: Autonomic Pharmacology
      As you will see throughout the text, the autonomic nervous system (ANS) is a very important topic for two reasons: First, manipulation of ANS function is the basis for treating a great deal of cardiovascular, pulmonary, gastrointestinal and renal disease; second, there is hardly a drug worth mentioning without some major autonomic side effects (cf. antihistamines).
    • 6: Local Anesthetics
      Local anesthesia is the selective numbing of a particular, circumscribed region of the body by a controlled, reversible procedure. Drugs called local anesthetics (LA) are usually employed for these procedures, although directly applied pressure, cooling, or even heating will also produce numbness. The general strategy is to inhibit the propagation or generation of impulses in nerves from a defined anatomical region.
    • 7: Antiinflammatory Drugs
      Inflammation is mediated in part by prostaglandins produced by the cyclooxygenase pathway. NSAIDs inhibit this pathway and serve as combined anti-inflammatory, anti­ pyretics, and analgesics. Because NSAIDs are generally nonspecific and exert numerous side effects, there is great interest in more specific therapeutics such as selective COX-2 inhibitors and anti-cytokine agents.
    • 8.1: Vasoactive Drugs I
      Hypertensive emergencies (malignant hypertension) are defined as severe hypertension coupled with acute end-stage organ damage.
    • 8.2: Vasoactive Drugs II - Heart Failure
      Congestive heart failure simply means that the pulmonary blood volume is expanded and, therefore, the pulmonary circulation is congested with blood. The congestion arises because of elevated left ventricular end-diastolic pressure (LVEDP). An elevated LVEDP is a hallmark of uncompensated congestive heart failure. Common symptoms include shortness of breath, fatigue, orthopnea and paroxysmal nocturnal dyspnea (PND).
    • 9: Lipid Lowering Drugs - Hyperlipidemia and Atherosclerosis
      Atherosclerosis is a chronic inflammatory disease characterized by enzymatic destruction of the normal arterial skeleton (largely elastin, collagen and smooth muscle), and replacement by disorganized collagen and elastin, cholesterol, and foam cells.
    • 10: Immunosuppression for Solid Organ Transplantation
      The success of solid organ and bone marrow transplantation (BMT) has correlated with improvements in selective immunosuppression. Immunosuppression decreases both the incidence of acute and chronic organ graft and bone marrow rejection, and a potentially life threatening complication of BMT known as graft-vs-host disease (GVHD). Selective immunosuppression targets specific pathways of immune signaling and activation, and minimizes the incidence of deleterious side effects.
    • 12.1: Neuropharmacology I - Drugs for Movement Disorders
      These are a diverse group of neurologic disorders in which the normal functions of the motor system are impaired. Parkinson’s disease is by far the most common disorder of movement, affecting >3% of individuals over the age of 65.
    • 12.2: Nitric Oxide
      The objective of this lecture is to describe the effects of inhaling low levels of nitric oxide (NO) on the hemodynamic and gas exchange function of both the normal and diseased lung. Considerable attention will be paid to safety and hazards of inhaled NO therapy. Progress has been made in understanding the NO­ guanylate cyclase signal transduction system. NO was given considerable clinical investigation in pulmonary artery hypertension and adult respiratory distress syndrome (ARDS) patients.
    • 13.1: Neuropharmacology II - Anxiolytics and Antidepressants
      Depression is a frequent problem, affecting up to 5% of the population. Common presentations include low mood, loss of energy, disinterest in activities. May also include weight loss, sleep disturbance, or psychosis. Should be considered in patients with atypical dementia and chronic pain
    • 13.2: Neuropharmacology III - Anticonvulsants
      Seizures are episodes of neurologic dysfunction arising from abnormal synchronous activity of neurons. Alterations of consciousness and abnormal motor activity are the most common manifestations.  Epilepsy (recurring seizures without a clear precipitant) is common, affecting about 1% of the population.  Pharmacological treatment is very successful in the majority of cases, but requires accurate diagnosis and classification of seizures.
    • 14: Antimicrobials I and II
      Successful antimicrobial therapy occurs when an effective concentration of drug is delivered to the site of infection for a sufficient period of time. Minimum effective concentrations are those needed to inhibit growth (bacteriostatic concentration, MIC) or kill (bacteriocidal concentration,MBC) the pathogen in question.
    • 15: Chemotherapy
      Chemotherapy is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents) as part of a standardized chemotherapy regimen. Chemotherapy may be given with a curative intent (which almost always involves combinations of drugs), or it may aim to prolong life or to reduce symptoms (palliative chemotherapy). Chemotherapy is one of the major categories of the medical discipline specifically devoted to pharmacotherapy for cancer, which is called medical oncology.
    • 16: Opioid Pharmacology
      Opium – a mixture of alkaloids from Papaver somniferum. An opiate is a naturally occurring alkaloid, i.e., morphine or codeine, and an opioid is any natural or synthetic compound, which has morphine-like properties. Hundreds of opioid alkaloids and peptides have been synthesized, but all clinically available opioid analgesics are alkaloids.

    Thumbnail: Chemotherapy drugs in vials and an IV bottle. (Photo by Bill Branson. Courtesy of National Cancer Institute Visuals Online.)