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Pharmocology Pt.1, Pharmokinetics - Coggle Diagram

- - - - Oral Administartion
        
        Typically lipophilic Drugs, non-polar and non-ionized
        
        all subject to FIRST PASS METABOLISM by the Liver
    - - Bypasses first pass metabolism via the liver
      - typically hydrophilic drugs (water loving), ionised and polar
      - Nb: Sublingual GTNs are taken directly to the heart via venous drianinge of the sublingual area bypassing first pass metabolism
  - - - % of total drug administered that reaches circulation (free and bound)
      - Adosoption is reduced by metabolism, elimiantion and squestration
      - Drugs bind to protein-carriers for distribution to target sites
- - - - ie hydrophilic drugs/ligands
    - - ie libpophilic drugs/ligands which are easily absorbed
  - - - Enzyme inhibition by drugs
        
        Ex. anti-microbial agents (antibiotics, antifungals and antivirals)
      - Signal transduction/transcription
        
        Intermediate steps, via second messangers and/or new proteins
        
        Ex. Antiepileptics, LA, GAs
    - - Adverse drug reactions
        
        Indirect ADRs
        
        Salivary Hypofunction (drug induced)
        
        Immunosupression = oppurtunistic oral infections
        
        Anticoagulants complicating wound healing
        
        Direct ADRs
        
        Allergic (type I-IV immune reactions)
        
        Anaphylaxis and angiodema (type I) = IgE mediated/mastcell Ex. Pencilliin allergy
        
        Pemphigous/Pemphigoid (type II) = Ab mediated
        
        Erythema multiforme (type III) = Immune complexes Ex. Antiepileptics
        
        Lichenoid reactions (Type IV) Cell mediated/delayed Ex. NSAIDs
        
        On soft tissues (Gingival hyperplasia, mucositis or motor/sensory disturbances)
        
        Ie. G. hyperplasia w/ CCBs
        
        On hard tissues (impaired bone turnover/formation)
        
        ie MRONJ w/ bisphophonates
- - - - Phase I (Oxidation-reduction)
        
        CYP-450 isoforms (liver) convert drug into more polar metabolite
        
        -OH, -NH2, -SH become water soluble, hydrophillic
      - Phase II (Conjugation/detoxifying)
        
        Further reaction of phase I metabolities to make them more hydrophillic
    - - Bind with high affinity, slowlying the breakdown of other substances (leading to high concentrations of drug within the cell)
    - - Acclerate the acitvity of CYP-450 (leading to drug inactivation)