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Fundamentals of Pharmacodynamics and Drug Action Study Guide

This guide covers the pharmacological management of osteoporosis and Paget's disease. It details the physiology of bone turnover, diagnostic methods like DEXA scans, and various treatment options. The content explains the mechanisms of action, administration, contraindications, and adverse effects of first-line therapies such as bisphosphonates, as well as advanced treatments including SERMs, monoclonal antibodies, and PTH analogs. It also addresses the management of Paget's disease and summariz

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Principles of Pharmacology, Drug Interactions, and Therapeutics

Drugs for Osteoporosis and Paget's Disease

Pharmacologic management of osteoporosis and Paget’s disease including the roles of vitamin D, calcitonin, growth hormone, estrogens, and dietary calcium in bone turnover.

  • Osteoporosis
  • Paget’s Disease
  • Bone turnover
  • Bone resorption
  • Bone formation
  • Bone Mineral Density (BMD)
  • Bisphosphonates
  • Calcitonin
  • Selective estrogen receptor modifiers (SERMs)
  • Monoclonal antibodies
  • Parathyroid Hormone (PTH) analogs
  • Vitamin D
  • Calcium
  • Estrogens
  • Growth hormone
  • Dual Energy X-ray Absorptiometry (DEXA)

Bisphosphonates, Calcitonin, SERMs, and Bone Formation Agents

Pharmacological treatments including bisphosphonates, calcitonin, raloxifene, conjugated estrogens with bazedoxifene, teriparatide, denosumab, and romosozumab for osteoporosis and Paget's disease.

  • Bisphosphonates mechanism of action
  • Calcitonin indications and adverse effects
  • Selective estrogen receptor modulators (SERM)
  • Teriparatide recombinant parathyroid hormone
  • RANKL inhibition
  • Romosozumab sclerostin inhibition
  • Osteoporosis treatment contraindications
  • Drug interactions and patient administration

Mechanisms of Drug Interactions

Clinical case studies exploring how enzyme induction, inhibition, and P-glycoprotein activity affect drug metabolism and therapeutic outcomes.

  • Cytochrome P450 metabolism
  • Enzyme induction
  • Enzyme inhibition
  • P-glycoprotein (PGP)
  • Autoinduction
  • Drug-drug interactions
  • Metabolite formation
  • Enterohepatic recycling
  • Genetic variation in metabolism

Principles of Therapeutics and Drug Development

This content covers the definitions of pharmacology, therapeutics, and toxicology, alongside the processes of drug nomenclature, FDA regulation, and the phases of clinical trials from drug discovery to post-marketing surveillance.

  • Pharmacology
  • Therapeutics
  • Toxicology
  • Pharmacokinetics
  • Pharmacodynamics
  • Drug Nomenclature
  • Chemical Name
  • Generic Name
  • Proprietary Name
  • Drug Discovery
  • Preclinical Testing
  • FDA Regulation
  • Investigational New Drug Application
  • New Drug Application
  • Abbreviated New Drug Application
  • Clinical Trial Phases
  • Phase I Clinical Trials
  • Phase II Clinical Trials
  • Phase III Clinical Trials
  • Phase IV Post-Marketing Studies

Drug Regulations, Preparations, and Administration Routes

This content covers regulations for brand name drugs, generic drugs, and dietary supplements, pharmaceutical preparation components including excipients, and various enteral, parenteral, and other administration routes.

  • Drug Price Competition and Patent Restoration Act of 1984
  • Dietary Supplement Health and Education Act of 1994
  • Active ingredients and excipients
  • Immediate-release formulations
  • Delayed release and enteric coated formulations
  • Sustained release and extended release formulations
  • Targeted-release formulations
  • Oral disintegrating tablets
  • Prodrugs
  • Parenteral administration routes
  • Enteral administration routes
  • Intravenous administration
  • Intramuscular administration
  • Subcutaneous administration
  • Inhalation administration
  • First-pass metabolism

Medication Labeling Terminologies and Evidence

This content covers medication labeling terminologies, mechanism of action, FDA pregnancy risk rules, and selecting drug therapy using disease oriented evidence and patient oriented evidence.

  • Boxed warning
  • Contraindication
  • Absolute contraindication
  • Relative contraindication
  • Side effects
  • Adverse Drug Effect
  • Indication
  • Off Label Indications
  • Mechanism of Action
  • Agonists
  • Antagonists
  • FDA Pregnancy Risk Categories
  • Disease Oriented Evidence
  • Patient Oriented Evidence

Drug Classifications and Prescribing Regulations

Information regarding drug scheduling, controlled substances, and federal prescribing regulations.

  • Controlled Substances Act of 1970
  • Drug Enforcement Administration scheduling
  • Abuse potential
  • Physical and psychological dependence
  • Prescribing regulations for non-controlled and controlled substances
  • Pharmacokinetics
  • Prodrug
  • Intramuscular injection administration
  • Hard evidence in research

Pharmacology of Peripherally Acting Analgesic Drugs

This lecture covers the pharmacology of peripherally acting analgesic drugs, including the roles of prostaglandins in the inflammatory response and the mechanisms of action for acetaminophen, NSAIDs, and NaV1.8 sodium channel blockers.

  • Inflammation
  • Arachidonic acid
  • Cyclooxygenase (COX)
  • Prostaglandins
  • Eicosanoids
  • Traditional NSAIDs
  • COX-2 inhibitors
  • Acetaminophen
  • Salicylates
  • NaV1.8 sodium channel blockers
  • Suzetrigine
  • Mechanism of action
  • Adverse effects
  • Chemical mediators of inflammation

Pharmacology of Peripherally-Acting Analgesic Drugs

This topic covers the actions, therapeutic uses, adverse effects, and history of aspirin, salicylates, and acetaminophen.

  • Aspirin mechanism of action
  • COX inhibition
  • Platelet aggregation
  • Prostaglandin effects
  • Therapeutic uses of salicylates
  • Aspirin adverse effects
  • Acetaminophen metabolism
  • Hepatotoxicity
  • Glutathione detoxification

Principles and Calculations of Clinical Pharmacokinetics

Pharmacokinetics of Clearance and Steady State

This content explores steady state plasma concentration, drug clearance, and half-life during continuous and intermittent dosing.

  • Organ Clearance
  • Steady state plasma concentration (Css)
  • Half-life (t1/2)
  • First-order kinetics
  • Bioavailability
  • Half life of elimination
  • Half life of accumulation
  • Continuous dosing
  • Intermittent dosing

Pharmacokinetics Formulas and Ionization Calculations

This document provides a list of pharmacokinetic formulas and practice questions regarding bioavailability, volume of distribution, and drug ionization based on pKa and pH.

  • Bioavailability
  • Volume of distribution
  • Concentration at steady state
  • Elimination rate constant
  • Clearance
  • Extraction ratio
  • pKa
  • Ionized form
  • Unionized form
  • Plasma concentration

Fundamentals of Pharmacodynamics and Pharmacokinetics

Fundamentals of Pharmacodynamics and Drug Action

This content explores drug-receptor interactions, binding site specificity, and the mechanisms of drug action through receptors or nonreceptor-mediated processes.

  • Sites of drug action
  • Drug-receptor occupancy theory
  • Nonreceptor-mediated mechanisms
  • Drug targets
  • Transduction
  • Binding site specificity
  • Drug-receptor binding forces
  • Receptor affinity
  • Agonists and antagonists
  • Efficacy

Pharmacodynamics and Receptor Transduction Mechanisms

Receptor transduction mechanisms include intracellular receptors, transmembrane receptor-effector enzymes, gated transmembrane ion channels, and G protein-coupled receptors.

  • Intracellular receptors
  • Ligand gated ion channels
  • G protein-coupled receptors
  • Transmembrane receptor-effector enzymes
  • G protein subunits
  • Cyclic AMP (cAMP)
  • Inositol triphosphate (IP3)
  • Membrane depolarization
  • Transcription factors
  • Drug-receptor regulation

Pharmacodynamics and Dose-Response Relationships

The relationship between drug concentration and magnitude of response is quantified using graded and quantal dose-response curves.

  • Dose-response relationship
  • Graded dose-response relationship
  • Quantal dose-response relationship
  • Potency (EC50/ED50)
  • Efficacy (Emax)
  • Receptor affinity
  • Equilibrium dissociation constant (Kd)
  • Median effective dose (ED50)
  • Median toxic dose (TD50)
  • Median lethal dose (LD50)
  • Therapeutic index (TI)
  • Therapeutic window
  • Margin of safety

Pharmacodynamics of Agonists and Antagonists

This content explores the mechanisms of agonists, allosteric activators, and various types of antagonists including competitive, noncompetitive, chemical, and functional antagonists.

  • Allosteric activator
  • Competitive antagonist
  • Noncompetitive antagonist
  • Reversible inhibition
  • Irreversible inhibition
  • Chemical antagonist
  • Functional/physiological antagonist
  • Partial agonist
  • Spare receptors
  • Dose-response curve
  • Efficacy
  • Potency
  • Affinity
  • HMG-CoA reductase inhibitor
  • Cyclooxygenase inhibition

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