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Pharmacologic PrinciplesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Pharmacologic Principles  Drug  • Any chemical that affects the processes of    a living organismCopyright © 2002, 1998, E...
Pharmacologic Principles  Pharmacology  • The study or science of drugsCopyright © 2002, 1998, Elsevier Science (USA). All...
Pharmacologic Principles: Drug Names  Chemical name  • The drug’s chemical composition and molecular    structure  Generic...
Pharmacologic Principles: Drug Names  Chemical name  • (+/-)-2-(p-isobutylphenyl) propionic acid  Generic name  • ibuprofe...
Instructors may wish to use                          EIC Image #3:           The Chemical, Generic, and Trade             ...
Pharmacologic Principles  • Pharmaceutics  • Pharmacokinetics  • Pharmacodynamics  • Pharmacotherapeutics  • Pharmacognosy...
Pharmacologic Principles  Pharmaceutics  • The study of how various drug forms influence    pharmacokinetic and pharmacody...
Pharmacologic Principles  Pharmacokinetics  • The study of what the body does to the drug:        – Absorption        – Di...
Pharmacologic Principles  Pharmacodynamics  • The study of what the drug does to the body:        – The mechanism of drug ...
Pharmacologic Principles  Pharmacotherapeutics  • The use of drugs and the clinical indications for    drugs to prevent an...
Pharmacologic Principles  Pharmacognosy  • The study of natural (plant and animal) drug sourcesCopyright © 2002, 1998, Els...
Drug Absorption of Various  Oral Preparations        Liquids, elixirs, syrups                                       Fastes...
Pharmacokinetics: Absorption   • The rate at which a drug leaves its site of     administration, and the extent to which  ...
Pharmacokinetics: Absorption  Factors That Affect Absorption  • Administration route of the drug  • Food or fluids adminis...
Pharmacokinetics: Absorption  Routes  • A drug’s route of administration affects the rate    and extent of absorption of t...
Pharmacokinetics: Absorption  Enteral Route  • Drug is absorbed into the systemic circulation    through the oral or gastr...
First-Pass Effect The metabolism of a drug and its passage  from the liver into the circulation. • A drug given via the or...
Instructors may want to use                     EIC Image #4:                                First-Pass EffectCopyright © ...
First-Pass Effect  • Routes that bypass the liver:        – Sublingual                                                   T...
Pharmacokinetics: Absorption Parenteral Route • Intravenous* • Intramuscular • Subcutaneous • Intradermal • Intrathecal • ...
Pharmacokinetics: Absorption  Topical Route  • Skin (including transdermal patches)  • Eyes  • Ears  • Nose  • Lungs (inha...
Pharmacokinetics: Distribution  The transport of a drug in the body by the   bloodstream to its site of action.  • Protein...
Pharmacokinetics: Metabolism  (also known as Biotransformation)  The biologic transformation of a drug into   an inactive ...
Pharmacokinetics: Metabolism  Factors that decrease metabolism:  • Cardiovascular dysfunction  • Renal insufficiency  • St...
Pharmacokinetics: Metabolism  Factors that increase metabolism:  • Fast acetylator  • Barbiturates  • Rifampin therapyCopy...
Pharmacokinetics: Metabolism  Delayed drug metabolism results in:  • Accumulation of drugs  • Prolonged action of the effe...
Pharmacokinetics: Excretion  The elimination of drugs from the body  • Kidneys (main organ)  • Liver  • Bowel        – Bil...
Instructors may wish to use                           EIC Image #5:                            Renal Drug ExcretionCopyrig...
Pharmacokinetics  Half-Life  • The time it takes for one half of the original amount    of a drug in the body to be remove...
Instructors may wish to use                           EIC Image #6:                                      Drug Half-LifeCop...
Pharmacodynamics  Drug actions:  • The cellular processes involved in the drug and    cell interaction  Drug effect:  • Th...
Pharmacodynamics  Onset  • The time it takes for the drug to elicit a    therapeutic response  Peak  • The time it takes f...
Pharmacodynamics:  Mechanisms of Action  The ways by which drugs can produce   therapeutic effects:  • Once the drug is at...
Pharmacodynamics:  Mechanisms of Action  • Receptor interaction  • Enzyme interaction  • Nonspecific interactionsCopyright...
Instructors may wish to insert                         EIC Image #2:                            Drugs and Receptors       ...
Pharmacotherapeutics:  Types of Therapies  • Acute therapy  • Maintenance therapy  • Supplemental therapy  • Palliative th...
Pharmacotherapeutics: Monitoring  • The effectiveness of the drug therapy must    be evaluated.  • One must be familiar wi...
Pharmacotherapeutics: Monitoring  • Therapeutic index  • Drug concentration  • Patient’s condition  • Tolerance and depend...
Pharmacotherapeutics: Monitoring  Therapeutic Index  • The ratio between a drug’s therapeutic benefits    and its toxic ef...
Pharmacotherapeutics: Monitoring  Tolerance  • A decreasing response to repetitive drug dosesCopyright © 2002, 1998, Elsev...
Pharmacotherapeutics: Monitoring  Dependence  • A physiologic or psychological need for a drugCopyright © 2002, 1998, Else...
Pharmacotherapeutics: Monitoring  Interactions may occur with other drugs or food  • Drug interactions: the alteration of ...
Pharmacotherapeutics: Monitoring  Interactions  • Additive effect  • Synergistic effect  • Antagonistic effect  • Incompat...
Pharmacotherapeutics: Monitoring  Medication Misadventures  Adverse drug events  • ALL are preventable  • Medication error...
Pharmacotherapeutics: Monitoring  Some adverse drug reactions are classified as   side effects.  • Expected, well-known re...
Pharmacotherapeutics: Monitoring  Adverse Drug Reaction  An undesirable response to drug therapy  • Idiosyncratic  • Hyper...
Pharmacotherapeutics: Monitoring  Iatrogenic Responses  Unintentional adverse effects that are   treatment-induced  • Derm...
Pharmacotherapeutics: Monitoring  Other Drug-Related Effects  • Teratogenic  • Mutagenic  • CarcinogenicCopyright © 2002, ...
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Pharmacologic principles

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  1. 1. Pharmacologic PrinciplesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  2. 2. Pharmacologic Principles Drug • Any chemical that affects the processes of a living organismCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  3. 3. Pharmacologic Principles Pharmacology • The study or science of drugsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  4. 4. Pharmacologic Principles: Drug Names Chemical name • The drug’s chemical composition and molecular structure Generic name (nonproprietary name) • Name given by the United States Adopted Name Council Trade name (proprietary name) • The drug has a registered trademark; use of the name restricted by the drug’s owner (usually the manufacturer)Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  5. 5. Pharmacologic Principles: Drug Names Chemical name • (+/-)-2-(p-isobutylphenyl) propionic acid Generic name • ibuprofen Trade name • MotrinCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  6. 6. Instructors may wish to use EIC Image #3: The Chemical, Generic, and Trade Names for the Common Analgesic IbuprofenCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  7. 7. Pharmacologic Principles • Pharmaceutics • Pharmacokinetics • Pharmacodynamics • Pharmacotherapeutics • PharmacognosyCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  8. 8. Pharmacologic Principles Pharmaceutics • The study of how various drug forms influence pharmacokinetic and pharmacodynamic activitiesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  9. 9. Pharmacologic Principles Pharmacokinetics • The study of what the body does to the drug: – Absorption – Distribution – Metabolism – ExcretionCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  10. 10. Pharmacologic Principles Pharmacodynamics • The study of what the drug does to the body: – The mechanism of drug actions in living tissuesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  11. 11. Pharmacologic Principles Pharmacotherapeutics • The use of drugs and the clinical indications for drugs to prevent and treat diseasesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  12. 12. Pharmacologic Principles Pharmacognosy • The study of natural (plant and animal) drug sourcesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  13. 13. Drug Absorption of Various Oral Preparations Liquids, elixirs, syrups Fastest Suspension solutions  Powders  Capsules  Tablets  Coated tablets  Enteric-coated tablets SlowestCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  14. 14. Pharmacokinetics: Absorption • The rate at which a drug leaves its site of administration, and the extent to which absorption occurs. – Bioavailability – BioequivalentCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  15. 15. Pharmacokinetics: Absorption Factors That Affect Absorption • Administration route of the drug • Food or fluids administered with the drug • Dosage formulation • Status of the absorptive surface • Rate of blood flow to the small intestine • Acidity of the stomach • Status of GI motilityCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  16. 16. Pharmacokinetics: Absorption Routes • A drug’s route of administration affects the rate and extent of absorption of that drug. – Enteral – Parenteral – TopicalCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  17. 17. Pharmacokinetics: Absorption Enteral Route • Drug is absorbed into the systemic circulation through the oral or gastric mucosa, the small intestine, or rectum. – Oral – Sublingual – Buccal – RectalCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  18. 18. First-Pass Effect The metabolism of a drug and its passage from the liver into the circulation. • A drug given via the oral route may be extensively metabolized by the liver before reaching the systemic circulation (high first-pass effect). • The same drug—given IV—bypasses the liver, preventing the first-pass effect from taking place, and more drug reaches the circulation.Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  19. 19. Instructors may want to use EIC Image #4: First-Pass EffectCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  20. 20. First-Pass Effect • Routes that bypass the liver: – Sublingual Transdermal – Buccal Vaginal – Rectal* Intramuscular – Intravenous Subcutaneous – Intranasal Inhalation *Rectal route undergoes a higher degree of first- pass effects than the other routes listed.Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  21. 21. Pharmacokinetics: Absorption Parenteral Route • Intravenous* • Intramuscular • Subcutaneous • Intradermal • Intrathecal • Intraarticular *Fastest delivery into the blood circulationCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  22. 22. Pharmacokinetics: Absorption Topical Route • Skin (including transdermal patches) • Eyes • Ears • Nose • Lungs (inhalation) • VaginaCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  23. 23. Pharmacokinetics: Distribution The transport of a drug in the body by the bloodstream to its site of action. • Protein-binding • Water soluble vs. fat soluble • Blood-brain barrier • Areas of rapid distribution: heart, liver, kidneys, brain • Areas of slow distribution: muscle, skin, fatCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  24. 24. Pharmacokinetics: Metabolism (also known as Biotransformation) The biologic transformation of a drug into an inactive metabolite, a more soluble compound, or a more potent metabolite. • Liver (main organ) • Kidneys • Lungs • Plasma • Intestinal mucosaCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  25. 25. Pharmacokinetics: Metabolism Factors that decrease metabolism: • Cardiovascular dysfunction • Renal insufficiency • Starvation • Obstructive jaundice • Slow acetylator • Erythromycin or ketoconazole drug therapyCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  26. 26. Pharmacokinetics: Metabolism Factors that increase metabolism: • Fast acetylator • Barbiturates • Rifampin therapyCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  27. 27. Pharmacokinetics: Metabolism Delayed drug metabolism results in: • Accumulation of drugs • Prolonged action of the effects of the drugs Stimulating drug metabolism causes: • Diminished pharmacologic effectsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  28. 28. Pharmacokinetics: Excretion The elimination of drugs from the body • Kidneys (main organ) • Liver • Bowel – Biliary excretion – Enterohepatic circulationCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  29. 29. Instructors may wish to use EIC Image #5: Renal Drug ExcretionCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  30. 30. Pharmacokinetics Half-Life • The time it takes for one half of the original amount of a drug in the body to be removed. • A measure of the rate at which drugs are removed from the body.Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  31. 31. Instructors may wish to use EIC Image #6: Drug Half-LifeCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  32. 32. Pharmacodynamics Drug actions: • The cellular processes involved in the drug and cell interaction Drug effect: • The physiologic reaction of the body to the drugCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  33. 33. Pharmacodynamics Onset • The time it takes for the drug to elicit a therapeutic response Peak • The time it takes for a drug to reach its maximum therapeutic response Duration • The time a drug concentration is sufficient to elicit a therapeutic responseCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  34. 34. Pharmacodynamics: Mechanisms of Action The ways by which drugs can produce therapeutic effects: • Once the drug is at the site of action, it can modify the rate (increase or decrease) at which the cells or tissues function. • A drug cannot make a cell or tissue perform a function it was not designed to perform.Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  35. 35. Pharmacodynamics: Mechanisms of Action • Receptor interaction • Enzyme interaction • Nonspecific interactionsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  36. 36. Instructors may wish to insert EIC Image #2: Drugs and Receptors and possibly EIC Image #7: Drug-Receptor Interactions: DefinitionsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  37. 37. Pharmacotherapeutics: Types of Therapies • Acute therapy • Maintenance therapy • Supplemental therapy • Palliative therapy • Supportive therapy • Prophylactic therapyCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  38. 38. Pharmacotherapeutics: Monitoring • The effectiveness of the drug therapy must be evaluated. • One must be familiar with the drug’s • intended therapeutic action (beneficial) • and the drug’s unintended but potential side effects (predictable, adverse drug reactions).Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  39. 39. Pharmacotherapeutics: Monitoring • Therapeutic index • Drug concentration • Patient’s condition • Tolerance and dependence • Interactions • Side effects/adverse drug effectsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  40. 40. Pharmacotherapeutics: Monitoring Therapeutic Index • The ratio between a drug’s therapeutic benefits and its toxic effectsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  41. 41. Pharmacotherapeutics: Monitoring Tolerance • A decreasing response to repetitive drug dosesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  42. 42. Pharmacotherapeutics: Monitoring Dependence • A physiologic or psychological need for a drugCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  43. 43. Pharmacotherapeutics: Monitoring Interactions may occur with other drugs or food • Drug interactions: the alteration of action of a drug by: – Other prescribed drugs – Over-the-counter medications – Herbal therapiesCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  44. 44. Pharmacotherapeutics: Monitoring Interactions • Additive effect • Synergistic effect • Antagonistic effect • IncompatibilityCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  45. 45. Pharmacotherapeutics: Monitoring Medication Misadventures Adverse drug events • ALL are preventable • Medication errors that result in patient harm Adverse drug reactions • Inherent, not preventable event occurring in the normal therapeutic use of a drug • Any reaction that is unexpected, undesirable, and occurs at doses normally usedCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  46. 46. Pharmacotherapeutics: Monitoring Some adverse drug reactions are classified as side effects. • Expected, well-known reactions that result in little or no change in patient management • Predictable frequency • The effect’s intensity and occurrence is related to the size of the doseCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  47. 47. Pharmacotherapeutics: Monitoring Adverse Drug Reaction An undesirable response to drug therapy • Idiosyncratic • Hypersensitivity reactions • Drug interactionsCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  48. 48. Pharmacotherapeutics: Monitoring Iatrogenic Responses Unintentional adverse effects that are treatment-induced • Dermatologic • Renal damage • Blood dyscrasias • Hepatic toxicityCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  49. 49. Pharmacotherapeutics: Monitoring Other Drug-Related Effects • Teratogenic • Mutagenic • CarcinogenicCopyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
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