Basic Pharmacology

These are the simple concepts that are important to know and understand with medications:

Pharmacokinetics: the time of course of what the body does to the drug. Kinetics is about movement (the drugs transporting to and from the receptors) – mnemonic “ADME”

  • Absorption: the movement of a drug from the bloodstream to the tissues. Most lipid-soluble drugs are absorbed through passive diffusion (directly penetrate membrane or dissolve in lipid layer)
  • Distribution: when drugs are carried throughout the body and delivered to targets of action. Consider albumin levels: decrease protein = decrease distribution (older adults) or protein-bound drugs.
  • Metabolism: the action of enzymes to activate meds. Drugs must become more hydrophilic (water-soluble for excretion).
  • Excretion: the process of medications eliminated from the body unchanged or as metabolites.

Pharmacodynamics: What the drug does to the body -mnemonic 3D “dynamic drugdoes to the body”. The relationships between drug concentrations & responses. Drug activity at receptors:

  1. Help a process happen: agonist
  2. Block a process from happening: antagonist
  • Receptors: Drugs must bind to for effect
  • Know that: All drugs have an effect
  • A drug’s ability to cause a response is called its efficacy i.e. Morphine
  • If you give a bigger dose you will get a bigger effect up to a point, most drugs have a ceiling.

Drug’s Potency & Selectivity: a potent drug is strong, but not necessarily better (2 nickels equals one dime, i.e. same) and can cause more side effects.

  • Potency is not an important drug quality as you can give more of another drug to reach the same potency i.e. the opioid equivalent chart.
  • Selectivity: the intended effects of a drug.

Adverse Drug Reactions (ADR): Unfavorable or unintended response to a drug that is given in normal dosages. Different from side-effects (SE) which is usually an undesirable or desirable additional effect that is known. ADR may be:

  • Inherent pharmacologic effect (hypoglycemia/insulin)
  • An allergic reaction: typical immunological response
  • A local irritant effect: inflammation
    • Often r/t P450 enzyme system and biotransformation alteration
    • Interaction awareness; must be aware of and consult resources for possible interactions of new drugs with the current meds ->Report serious ADRs to FDA Medwatch Reporting Program

Properties of an Ideal Drug:

  • Effectiveness: elicits responses for which it is given – most important
  • Safety: Cannot produce harmful effects even at very high dosages and for a long time
  • Selectivity: Only elicits a response for which it is given, no side effects
  • Reversible action: most drugs should be reversible
  • Predictability: Know with certainty exactly how an individual patient will respond – impossible, must individualize
  • Ease of administration: simple, convenient route – enhances compliance and decreases errors
  • Freedom from drug interactions: few drugs are without drug interaction
  • Low cost: easy to afford; a significant factor in adherence, esp. with elderly
  • Chemical stability: drugs’ ability to be stored for a long time without loss of effectiveness – variable between drugs
  • Possession of a simple generic name: easier to remember and less confusion amongst drugs

 

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