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64 Cards in this Set
- Front
- Back
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What is a Drug? |
1. Any chemical compound that can influence living processes a.Includes those that have therapeutic applications i. Small molecules ii. Biological agents
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Term Drug means? |
(A) articles recognized in the official United States Pharmacopoeia, official Homeopathic Pharmacopoeia of the United States, or official National Formulary, or any supplement to any of them; and (B) articles intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease in man or other animals; and (C) articles (other than food) intended to affect the structure or any function of the body of man or other animals; and (D) articles intended for use as a component of any article specified in clause (A), (B), or (C). A food or dietary supplement for which a claim is made is not a drug solely because the label or the labeling contains such a claim. A food, dietary ingredient, or dietary supplement for which a truthful and not misleading statement is made is not a drug under clause (C) solely because the label or the labeling contains such a statement. |
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Define Pharmacology? |
The study of drugs and their interactions with living systems 1. Sources- natural or synthetic 2. Physicochemical properties- pharmaceutics 3. Product formulation- pharmaceutics 4. Kinetic properties- Pharmacokinetics 5. Physiologic effects- pharmacodynamics |
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Clinical Pharmacology |
The study of drugs in human beings 1. Healthy volunteers 2. Acutely ill patients 3. Chronically ill patients |
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Phramcotherapy |
The use of drugs to diagnose, cure, prevent, or treat a disease or condition in humans 1. Implementing and evaluating the best therapeutic plan for the patient based on the assessment |
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Taking a Drug |
1. Name- Generic and Trade 2. Indication- Clinical use 3. Drug Disposition- how it gets to where its going 4. Drug effect- what it does when it gets there 5. Mechanism of action- how it does it 6. Comparison- Why this one is better 7. Dosing regimens- dose, route, frequency, durations 8. Monitoring- adverse events (adverse reactions, side effects, interactions) |
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The "Ideal" Drug is... |
Effective -Is useful in clinical practice Safe -Has no ability to cause injury Selective -Elicits only the anticipated responce |
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Properties of an "ideal" drug |
-Reversible action -Predictable response -Easily administered -Lack of interaction -Low cost -Chemically stable |
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Benefit vs Risk |
Medication offers a cost-effective approach to reducing human suffering from disease
Medication use in human is one of the most common causes of disease |
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What areRems |
The Food and Drug Administration Amendments Act of 2007 gave FDA the authority to require a Risk Evaluation and Mitigation Strategy from manufacturers to ensure that the benefits of a drug or biological product outweigh its risks • Recent REMS: Abstral ® to Zyprexa® |
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Benefit vs Risk |
• Adverse Drug Event – Any undesirable effect caused by the use or misuse of a drug with a patient (including “off‐target” effects) – Side effects, interactions, adverse drug reactions • Medication Error – Mishaps that occur at any point along the drug‐use process – May or may not lead to an adverse drug event – A “close call” or “near hit” is still a medication error |
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Individual Response to a Drug |
Prescribed dose -> Administered dose -> concentration at sites of action -> intensity of responses
Administration -Medication errors -Patient compliance
Pharmacokinetics -absorption -distribution -metabolism -excretion
Pharmacodynamics -Drug-receptor interaction -patient's functional state -placebo effect
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Pharmacokinetics and Pharmacodynamics |
Sources of individual variation -Physiologic variables -Pathologic variables -Genetic variables -Drug interactions |
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Dosage Forms |
Solids -Tablets -Capsules -Powders
Liquids -Solutions -Suspensions -Emulsions
Semisolids -Ointments -Creams -Gels |
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Dosage Units |
Units of Measurement -Mass -Volume -Other
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Routes of Administration |
Enteral – Oral, sublingual, buccal, enterostomy Parenteral – Intravenous, subcutaneous, intramuscular, transdermal, intra‐arterial, intra‐articular, intra‐dermal, epidural, intrathecal Topical – Skin, eye, ear, nose, lungs |
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Bioavailability |
• The extent to which the administered drug becomes available in the general circulation |
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What is Pharmacokinetics? |
• What the body does to the drug… |
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Pharmacokinetics |
• Absorption • Distribution • Metabolism • Excretion |
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What is Absorption |
• The passage of a drug from the site of its administration into the bloodstream |
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Absorption |
• Drug dissolution • Absorptive surface area • Blood flow at absorptive site • Membrane penetration of the drug |
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Membrane Penetration |
• Requires lipid solubility (lipophilicity) – Non‐polar molecules • Poor penetration – Polar molecules – no net charge – Ions – net electrical charge – Quaternary ammonium compounds – positive charge – Weak acids or bases – may exist in charged form • Weak acids – charged (ionized) at higher pH • Weak bases – charged (ionized) at lower pH |
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Transport Proteins |
ATP‐Binding Cassette Superfamily
Solute‐Carrier Superfamily
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Lumen |
Mucosal |
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Blood |
serosal |
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Absorption |
PO: Barriers- Epithelial & Capillary membrans Advantages- convenient, low risk, inexpensive Disadvantages- Variable, limited bioavailability, NPO patients IV Barriers- NONE Advantages- Rapid onset, dilute, controlled levels Disadvantages- costly, less convenient, irreversible, infectious fluid & embolic risk SC Barrier- Capillary Membrane Advantages- Poor soluble medication Disadvantages- Discomfort, less convenient, risks IM Barrier- Capillary Membrane Advantages- Poorly soluble & depot Meds Disadvantages- Painful, less convenient, tissue injury |
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What is Distribution?W |
• Movement of a drug (following absorption) from the blood stream to other body tissues • Determining factors related to… - Body composition -Blood flow -Tissue size & permeability • Drug lipophilicity • Plasma‐protein binding • Degree of ionization |
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Distribution |
• Permeability • Body composition • Regional blood flow • Plasma‐protein binding |
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What is Metabolism? |
• Transformation of a drug’s chemical structure by enzymatic reaction |
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Metabolism Phase I & II |
• Phase I Reactions – Usually make the drug more polar by introducing (or uncovering) a functional group (–OH, –NH2, –SH) – Hydrolysis, reduction, oxidation – (e.g.), cytochrome P450 system … CYP • Phase II Reactions – Combine an endogenous substrate (glucuronic acid, acetic acid, amino acid) with the drug’s functional group to form a more polar conjugate – Conjugation – (e.g.), UDP‐glucuronosyltransferases … UGT |
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First‐Pass Effect |
• Removal of a substantial amount of an enterally administered drug dose prior to the drug reaching the systemic circulation – Gastrointestinal metabolism – Hepatic metabolism |
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Excretion |
• The removal of a drug and it’s metabolite(s) from the body |
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Excretion Routes? |
• Several common routes of drug excretion – Renal – Biliary – Other |
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Drug half‐life (t½) |
Time for drug content to decrease by 50% |
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Steady State Drug Concentration |
Attained after approximately four half-times Time to steady state independent of dosage
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What is Pharmacodynamics |
• What the drug does to the body…and how |
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Pharmacodynamics |
• Drug Effect – physiologic, clinical – Intensity – Onset – Peak – Duration • Drug Action – cellular; mechanism of action – Receptor – Enzyme – Non‐selective – Other • Intensity of drug response – Efficacy – Potency |
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Toxic Effect |
• The unintended effect of a medication • Adverse drug events – Side effects (more predictable) A,D • Extension of pharmacologic action, or withdrawal • Includes teratogenicity, mutagenicity, and carcinogenicity – Adverse drug reactions (less predictable) B,C • Allergic • Idiosyncratic – Interactions E,F • Drug‐drug, drug‐other |
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Types of Reaction |
Type A (Augmented) Type B (Bizarre) Type C (Chronic) Type D (Delayed) Type E (End of Treatment) Type F (Failure) |
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Type A Reaction |
Occurrence -Reactions predictable from the known pharmacology often representing exaggeration of the pharmacological effect of the drug (common) Ex. Hypotension with anti-Hypertensives |
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Type B Reaction |
Unpredictable from knowledge of the basic pharmacology of the drug Show no simple dose-response relationship (uncommon) ex. Halothane Hepatitisype CT |
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Type C Reaction |
Reactions whose biological characeristics can be either predicted or rationalised in terms of chemical structure of the drug ex. Acetaminophen hepatotoxicity (uncommon) |
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Type D Reaction |
Become apparent some time after beginning use of the drug include carcinogenicity and teratogenicity (uncommon) ex Fetal hydantoin syndrome with phenytoin (uncommon) |
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Type E Reaction |
Occur soon after drug withdrawal ex. Withdrawal seizures on stopping phenytoin (uncommon) |
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Type F Reaction |
Unexpected failure of therapy. Often dose-related and caused by drug interactions ex. Inadequate oral contraceptive dosage, particularly when used with specific enzymes inducers (common) |
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Pharmacodynamics |
• Drug Effect – physiologic, clinical – Intensity – Onset – Peak – Duration • Drug Action – cellular; mechanism of action – Receptor – Enzyme – Non‐selective – Other |
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Mechanism of Action |
• Receptor – Reactive site to the drug’s chemical structure and degree of affinity produce an effect – Agonist – Antagonist (competitive or non‐competitive) – Partial agonist • Enzyme – Drug acts as a substrate to alter activity • Non‐selective – Physico‐chemical interference with metabolic process(es) |
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Drug‐Receptor Interaction |
• Drug affinity for the receptor – Higher affinity, strong attraction, requires less drug – Potency • Intrinsic activity of the drug – Degree of receptor activation following drug binding – Maximum efficacy |
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Drug‐Receptor Interaction |
• Agonists – Drug that activates receptor; mimics physiologic actions – Good affinity and high intrinsic activity • Antagonists – Drug that blocks receptor and physiologic actions – Good affinity but no intrinsic activity • Partial agonists – Mimic physiologic actions to a lesser degree – Affinity but only moderate intrinsic activity – “Agonist‐antagonist” |
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Pharmacotherapeutics |
• Implementing and evaluating the best therapeutic plan involving medication for the patient based on the assessment • Goal of therapy – General approach – Patient specific – SMART (Specific, Measurable, Attainable, Realistic, Trackable) |
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Pharmacotherapeutics |
• Assessment – Integrate data on the patient and their meds to identify any real or potential drug‐related problems • Etiology, severity, consequence if not addressed • Therapeutic options – Acute, maintenance, supplement/repletion, palliative, supportive, prophylactic, empiric • Goals of therapy – Sustain function/life, prevent progression, maintain normal function, patient comfort, maintain/improve integrity of body function, prevent disease, limit specific disease or disorder |
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Pharmacotherapeutics |
• Plan – Specific order … – Counsel / educate … – Implement and evaluate … |
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Pharmacotherapeutics |
• SPECIFIC ORDER –Drug regimen: Drug name, dose, route, interval or frequency, duration – Monitoring regimen: • Health care provider • Patient or caregiver |
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Pharmacotherapeutics |
• Counsel / educate – Patient‐centered – Individualized – Requirements • Assess patient’s motivation, readiness to learn, comprehension of directions, and support system –Use all available resources |
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Pharmacotherapeutics |
• Implement and evaluate – Prescribe or administer – Monitoring parameters – Re‐assess patient |
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Pharmacotherapeutics |
• Sources of Patient Variability – Life Stage – Disease State – Nutritional State – Genetics – Circadian – Other |
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Genetics |
• Pharmacogenomics – Study of the application of gene technology in drug development and characterization • Pharmacogenetics – Study of the genetic variability between individuals that determine differences in drug response – Variant alleles • Single nucleotide polymorphisms (SNPs) – Synonymous vs non‐synonymous • Structure variations – Insertions, deletions, duplication, translocation, … |
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Variant Alleles |
• Including genes that code for drug: – Transporters • OATP – Metabolizing enzymes • CYP2D6 • UGT1A1 – Therapeutic targets • VKORC1 |
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Therapeutics |
• Definitions • Modalities |
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Therapeutics or Therapy
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– Management of disease by one or more methods • Behaviour therapy • Drug therapy • Electroshock therapy • Hyperbaric oxygen therapy • Occupational therapy • Physical therapy • Psychoanalytic therapy • Radiation therapy • Surgical therapy |
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Prevention |
• Prophylactic therapy – Primary the risk factors – Secondary • Status‐post injury or illness • Measures to prevent further disease progression, morbidity, and mortality |
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Treatment |
• Traditional medical or surgical management for a diagnosed condition or disease |
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Therapeutic Modulations |
• Medication maintenance • Nutrition |
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Nutrition |
Preventative – Dietary Guidelines ... – Food Guides ... – Dietary Supplements ... Treatment – Diet Therapy – Nutrition Support Therapy |
