Please enable JavaScript.

Coggle requires JavaScript to display documents.

Pharmacology (Terms (Fig 25) (Pharmacodynamics (PD) (Effects (Irritation,…

- - - - Irritation
      - Depression
      - Stimulation
      - Cytotoxic
      - Replacement
    - - Antagonist
        
        Non-Competitive
        
        Competitve
        
        Slow down enzyme catalysed reaction rate
        
        Drug molecule that inhibits neurotransmitter effect
      - Agonist
        
        Drug molecule that mimics neurotransmitter effect
        
        Example
        
        Succinyl Choline mimics acetyl choline
        
        Does not affect enzyme catalysed reaction rate
      - Hormone/Neurotransmitter
        
        Fits into receptor
      - Purpose
        
        Drug bind to receptor => Mixture of effects
      - Effects
        
        Full
        
        Partial
        
        Direct/Competitive
        
        Indirect/Noncompetitve
        
        Inverse
    - - Dose-Response (DR) Curve
        
        Increase Dose => Increase Effect
        
        Reach EQM
      - Varies
        
        Action Site
        
        Receptor Affinity
      - Multiple
      - Therapeutic Index
        
        Relative to Safety
        
        Terms
        
        Effective Dose
        
        50% population shows response
        
        Lethal Dose
        
        50% population dies
        
        Formula
        
        LD50/ED50
        
        Higher better
        
        Safer
      - Terms
        
        Efficacy
        
        DR Curve
        
        Max Effect
        
        Peak
        
        Types
        
        Full Agonist
        
        100%
        
        Partial Agonist
        
        50%
        
        Full Antagonist
        
        0%
        
        Inverse Agonist
        
        -100%
        
        Drug ability to produce response once available receptors/binding sites occupied
        
        Potency
        
        Relative response strength for given dose
        
        DR Curve
        
        Greater potency
        
        Shift Left
        
        Inverse EC50
        
        Tolerance/Densensitization
        
        Decrease response with constant exposure for same dose
        
        More drug needed for response level
        
        DR Curve
        
        Greater response
        
        Shift Right
        
        Opposite
        
        Sensitization
        
        Cross-Tolerance
        
        Develop across drugs
        
        Mechanims
        
        PK
        
        Drug Availability changes @ action site
        
        Bioavailability decreases
        
        Absorption decreases
        
        Binding to depot sites increases
        
        PD
        
        Drug-Receptor Interaction Changes
        
        Down Regulation of Receptors
        
        G-Protein Uncoupling/Inactivation
  - - - Absorption
        
        Administration Site => Measurement Site
        
        Deliver Drug into blood stream
        
        Intravenous Delivery x
        
        Oral /
        
        Effectiveness
        
        Conc @ Action Site
        
        Hard
        
        Solution
        
        Measure in blood plasma
        
        Blood Plasma Conc ~ Therapeutic Effect
        
        1st Pass Effect (Fig 27)
        
        Drug Conc reduced significantly even before reaching systemic circulation
        (Reach whole body)
        
        Cell Membrane (Fig 28)
        
        Lipid Bilayer (Fig 29)
        
        Drug Permeability (Fig 30)
        
        Types
        
        Hydrophilic
        
        Hydrophobic
        
        Very Hydrophobic
        
        Amphiphilic
        
        Membrane Permeability of drug
        
        Epinephrine/Adrenalin
        
        Use
        
        Hormone
        
        Neurotransmitter
        
        Drug
        
        Purpose
        
        Fight-or-Flight Response
        
        Regulate Blood Pressure
        
        Modification (Fig 31)
        
        Remove hydrophilic group
        
        Enhance Uptake
      - Distribution
        
        Drug Movement around body + Drug Amount
        
        Not Even
        
        Accumulation
        
        Rate: Drug => Tissues
        
        Same principles as drug absorption
        
        Mode (Fig 32)
        
        Intravascular
        
        Volume of Distribution (Vd)
        
        High
        
        Drug stored in fat
        
        Low
        
        Drug stored in extracellular space (Interstitial)
        
        Kinetics
        
        Initial
        
        Accumulate in Liver & Brain
        
        Final
        
        Accumulate in Muscles & Fat
        
        Eqm
      - Metabolism
        
        Drug Conversion: Chem Species A => Chem Species B
        
        Purpose
        
        Degrade to soluble byproducts
        
        2 Phases
        
        Phase 1
        
        Oxidation, Hydrolysis, Reduction
        
        Occurs in liver
        
        Phase 2
        
        Conjugation: Groups add to drug
        
        Occurs in hepatocyte cytoplasm
      - Excretion
        
        Drug Loss from Measurement Site
        
        Process (Fig 33)
        
        Kidney
        
        Drug Excreting Organ
        
        Clearance
        
        Rate of removal of substance from body
        
        Elimination Kinetics
        
        0 Order
        
        Constant Amount
        
        1st Order
        
        Constant %
- - - - Therapeutic
      - Toxic