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Drug action
The physicochemical interaction between the drug molecule and molecules in the body that alters a physiological process in the body by one of three methods
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Endogenous molecules
produced or grown from within an organism
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Exogenous molecules
originating from outside an organism
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Three methods of drug interactions
replacement, interruption, potentation
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Replacement
exogenous drug replaces an endogenous substance; receptor agonist; Bethanechol (Urecholine) - a nonselective muscarinic receptor agonist used to treat uriniary retention
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Interruption
drug that interferes with a physiological process; receptor agonist; Cetirizine (Zyrtec) - a selective histamine 1 receptor antagonist used to treat allergic symptoms
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Potentation
drug enhances a physiological process; selective serotonin reuptake inhibitor (SSRI); Fluoxetine (Prozac) - SSRI used to treat depression
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Observable consequence example
penicillin interferes with bacterial cell wall synthesis causing death of the bacteria; Tylenol elevates the pain threshold (analgesia) and inhibits formation and release of prostaglandins in the CNS (antipyresis); action of epinephrine on blood pressure and heart rate
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Inotropy
cardiac muscle contraction
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Three phases of drug activity
pharmaceutical, pharmacokinetic and pharmacodynamic
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Pharmaceutical
occurs after drgu is given, involving disintegration/dissolution of dosage form
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Pharmacokinetic
absorption, metabolism, distribution and elimination of a drug
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Pharmacodynamic
effect of the drug on the body
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Percent of drugs administered orally
80%
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Where in GI tract most absorption occurs
small intestines
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Rate-limiting rank order
lipid soluble - water soluble - suspension solution - powder - capsules - tablets - coated tablets - enteric-coated tablets
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Four phases of pharmacokinetics
absorption, distribution, metabolism, elimination
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Three mechanisms of drugs entering bloodstream or cell
passive diffusion, active diffusion (carrier-mediated) and pinocytosis
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Passive diffusion
no energy required, how most drugs work
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Active diffusion
carrier molecule and energy required; glucose, amino acids, 5-fluorouaracil
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Pinocytosis
process of engulfing a drug and pulling it across the membrane which fuses with lysosymes in the cell taht hydrolyze or breakdown contents of the vesicle; Vitamins A, D, E & K
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Four factors affecting drug absorption
pH, solubility, routes of administration, circulation
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Bioavailability
percentage of dose that reaches the blood stream (20-40% orally)
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Nine factors affecting bioavailability
dose form, route, GI tract, food, drugs, liver metabolism, concentration, cell membrance, surface area
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Three factors affecting drug distribution
level of plasma protein, blood flow, competing drugs
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Biotransformation
drug metabolism; converted into more water-soluble form in liver which is then excreted by the kidneys
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First-pass effect
metabolism of orally administred drugs by gastrointestinal and hepatic enzymes, resulting in a significant reduction of the amount of unmetabolized drug reaching the systemic circulation
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Seven other routes by which drugs are eliminated from body
biliary and fecal (Orlistat - Alli - lipase inhibitors used in obesity), lungs (inhaled anesthetics and alcohol), breast milk (narcotics), sweat (anti-epileptics, amphetamine), saliva (penicillin, phentoin, lithium), hair (methamphetamine, methoxyphenamine), skin (benzoic acid, salicylic acid, alcohol, antipyrine, heavy metals)
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Pharmacodynamics
effect of drugs on a body
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Seven factors affecting pharmaodynamics
receptor theory, categories of drug action, therapeutic index and therapeutic range, peak and trough levels, side effects, adverse effects, contraindications
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Side effect
problem that occurs when treatment goes beyond the desired effect or occurs in addition to the desired therapeutic effect
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Fourteen different side effects
gender, environment, time of administration, pathologic state, idiosyncracy, tolerance, drug dependence, drug interaction, synergism, potentiation, placebo effect, pharmacogenetic effect, allergic reaction, toxic effect, tachyphylaxis
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Adverse effect
a harmful or abnormal result that may be caused by adminstation of a medication and may be indicated by an untoward result such as by illness or death
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Contraindication
a condition which makes a particular treatment or procedure inadvisable
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Two types of contraindications
absolute, relative
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