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• ﻟﺠﻨﺔ ﺗﻮﺣ-ﺪ ﻣﻨﻬﺎج ﻣﺎدة ) Pharmacology I (

  
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  اﻟﻨﺠﺎح واﻟﺘﻔﻮق ، و

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  اﻟﻤﻮﻓﻖ
• Pharmacology


  The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes
• Pharmacodynamic processes


  The actions of the drug on the body
• Pharmacokinetic processes


  The actions of the body on the drug, governing the absorption, distribution, and elimination of drugs

  
• Pharmacokinetics


  1. Absorption

  2. Distribution

  3. Metabolism

  4. Elimination

  
• Using knowledge of pharmacokinetic parameters, clinicians can design optimal drug regimens, including the route of administration, the dose, the frequency, and the duration of treatment

  
• Routes of drugs administration

  • Enteral
  • Parenteral
  • Topical
  • Others
• Enteral administration


  Administering a drug by mouth, the safest and most common, convenient, and economical method

  
• Oral

  • Easily self-administered
  • Toxicities and/or overdose may be overcome with antidotes, such as activated charcoal
• Enteric-coated preparations


  A chemical envelope that protects the drug from stomach acid, delivering it instead to the less acidic intestine
• Extended-release preparations


  Have special coatings or ingredients that control drug release, allowing for slower absorption and prolonged duration of action
• Sublingual/buccal


  Placement of drug under the tongue or between the cheek and gum, facilitating direct absorption into the bloodstream
• Sublingual and buccal routes

  • Ease of administration
  • Rapid absorption
  • Bypass of the harsh gastrointestinal environment
  • Avoidance of first-pass metabolism
• Parenteral


  Introducing drugs directly into the body by injection
• Parenteral routes


  • Highest bioavailability
  • Not subject to first-pass metabolism or the harsh GI environment
  • Provide the most control over the actual dose of drug delivered to the body
  • Irreversible and may cause pain, fear, local tissue damage, and infections

  
• Major parenteral routes


  • Intravascular (intravenous or intra-arterial)
  • Intramuscular
  • Subcutaneous
• Depot preparations


  Consist of a suspension of drug in a nonaqueous vehicle, providing a sustained dose over an extended interval
• Subcutaneous (SC)


  Injection provides absorption via simple diffusion and is slower than the IV route, minimizing the risks of hemolysis or thrombosis
• Intradermal (ID)


  Injection into the dermis, the more vascular layer of skin under the epidermis, used for diagnostic determination and desensitization
• Oral inhalation and nasal preparations

  Provide rapid delivery of drug across the large surface area of mucous membranes of the respiratory tract and pulmonary epithelium
• Intrathecal/intraventricular


  Introducing drugs directly into the cerebrospinal fluid to achieve local, rapid effects in the central nervous system
• Topical


  Application to the skin to achieve a local effect
• Transdermal


  Application to the skin to achieve systemic effects, via a transdermal patch
• Rectal


  Bypasses the portal circulation, minimizing biotransformation by the liver, useful if the drug induces vomiting or the patient is unconscious
• Absorption is the transfer of a drug from the site of administration to the bloodstream
• Mechanisms of absorption of drugs from the GI tract

  • Passive diffusion
  • Facilitated diffusion
  • Active transport
  • Endocytosis and exocytosis
• Passive diffusion


  The driving force is the concentration gradient across a membrane, does not involve a carrier, is not saturable, and shows low structural specificity
• Facilitated diffusion


  Involves specialized transmembrane carrier proteins that facilitate the passage of large molecules, does not require energy, can be saturated, and may be inhibited by competing compounds

  
• Active transport


  Energy-dependent, driven by the hydrolysis of ATP, can move drugs against a concentration gradient, is selective and may be competitively inhibited
• Endocytosis and exocytosis


  Used to transport exceptionally large drugs across the cell membrane, involving engulfment and pinching off of drug-filled vesicles

  
• Effect of pH on drug absorption


  Uncharged forms of weak acids and bases can permeate through membranes, while charged forms cannot

  
• The ratio between charged and uncharged forms is determined by the pH at the site of absorption and the ionization constant (pKa) of the drug

  
• Factors influencing absorption


  • pH at the absorption site
  • Blood flow to the absorption site
  • Total surface area available for absorption
  • Contact time at the absorption surface
• Charged form B


  Penetrates through the cell membrane
• Protonated form BH+


  Does not penetrate through the cell membrane
• The effective concentration of the permeable form of each drug at its absorption site is determined by the relative concentrations of the charged and uncharged forms

  
• The ratio between the two forms is determined by the pH at the site of absorption and by the strength of the weak acid or base, which is represented by the ionization constant, pKa