Quiz 1

• PHARMACOLOGY – study of drugs
• DRUG


  Any article/agent used in the mitigation, diagnosis, prevention, treatment, and cure of diseases in man and in animals
• Main divisions of pharmacology


  • Pharmacodynamics
  • Pharmacokinetics
  • Pharmacotherapeutics
• Pharmacodynamics


  Deals with the study of biochemical and physiologic effects of drugs in biological systems and the mechanisms by which these effects were produced
• Pharmacokinetics


  Study of fate and disposition of drugs in the body
• Pharmacotherapeutics


  Study of rational drug use in the management of certain diseases
• General mechanisms by which drugs alter normal functions of cells


  • Interaction with receptors
  • Alteration of the activity of enzymes
  • Antimetabolite action
  • Non-specific chemical or physical interactions
• Receptors


  Naturally occurring target macromolecules which mediate actions of endogenous physiologic substances
• Types of drug-receptor interactions


  • Type I
  • Type II
  • Type III
  • Type IV
• Agonists are capable of binding to, and activating, a receptor
• Full agonists occupy receptors to cause maximal activation
• Partial agonists occupy receptors but cannot elicit a maximal response
• Inverse agonists produce intrinsic activity <0
• Antagonists bind to the receptor but do not initiate a response; block the action of an agonist or endogenous substance that works through the receptor
• Competitive antagonists combine with the same receptor as the agonist
• Non-competitive antagonists bind to the receptor at a site other than the agonist-binding site
• Graded-dose response curve


  Expresses an individual's response to increasing doses of a drug

  
• Efficacy


  Measure of the ability of a drug to elicit the MAXIMUM pharmacologic response
• Potency


  Relative measure of the ability of a drug to produce half of the maximum response
• Ceiling dose


  The smallest dose which produces the maximum response
• Slope


  Indicates changes in response; Steep curve implies a small change in dose produces a large change in response
• Quantal-dose response curve


  Relates the dosage of a drug to the frequency with which a designated response will occur within a population

  
• Autonomic Nervous System (ANS)


  Subdivision of the peripheral efferent nervous system; controls involuntary activity
• Divisions of the ANS


  • Parasympathetic Nervous System
  • Sympathetic Nervous System
  • Enteric Nervous System
• Synaptic transmission


  Mechanism of impulse across the synapse
• Differences between Sympathetic and Parasympathetic Nervous Systems


  • Preganglionic neuron location
  • Neurotransmitter
  • Receptor type
  • Physiological effects
• Catecholamines


  Possess a catechol nucleus and an ethylamine side chain; include Norepinephrine, Epinephrine, Dopamine
• Catecholamine biosynthesis

  1. Tyrosine

  2. DOPA

  3. Dopamine

  4. Norepinephrine

  5. Epinephrine
• Catecholamine storage and release


  • Stored in vesicles
  • Released from nerve terminals through calcium-dependent exocytosis
  • Blocked by reserpine
  • Enhanced by tyramine, ephedrine, amphetamine
  • Inhibited by guanethidine, guanadrel, bretylium
• Catecholamine termination mechanisms


  • Reuptake
  • Diffusion
  • Metabolism via COMT and MAO
• Sympathetic receptor types


  • Alpha-1
  • Alpha-2
  • Beta-1
  • Beta-2
• Sympathomimetic drug classifications


  • Direct-acting
  • Indirect-acting
  • Mixed-acting
• Sympathomimetics


  Mimic the effects of endogenous catecholamines (NE, EPI)
• Sympathomimetic drug examples


  • Epinephrine
  • Norepinephrine
  • Dopamine
  • Isoproterenol
  • Dobutamine
  • Terbutaline, Albuterol, Metaproterenol, etc.
  • Phenylephrine, Methoxamine, Metaraminol
  • Clonidine, Methyldopa, Guanabenz, Guanfacine
  • Ephedrine, Mephentermine
  • Amphetamine, Dextroamphetamine, etc.
• Sympathomimetic therapeutic uses


  • Cardiovascular
  • Respiratory
  • Eye
  • CNS
  • Other
• Sympatholytics


  Prevent or reverse the actions of endogenously released NE or EPI or exogenously administered sympathomimetic agents
• Sympatholytic drug classifications


  • Direct-acting: Alpha and Beta Blockers
  • Peripherally-acting: Adrenergic Neuronal Blockers
• Alpha blocker examples


  • Non-selective: Phenoxybenzamine, Phentolamine
  • Alpha-1 selective: Prazosin, Doxazosin, etc.
  • Alpha-2 selective: Yohimbine, Rauwolscine
• Beta blocker examples


  • Non-selective: Propranolol, Timolol
  • Cardioselective: Metoprolol, Atenolol
  • Vasodilating: Labetalol, Carvedilol
• Beta blocker therapeutic uses

  • Cardiovascular
  • Eye
  • Other