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Principles of Pharma

Chapter 1

Pharmacology Study of drugs actions and their effects on living organisms
Neuropharmacology Study of drug-induced changes in nervous system cell functioning
Psychopharmacology emphasizes drug-induced changes in mood, thinking, and behavior
Neuropsychopharmacology Identifies chemical substances that act on the nervous system to alter behavior
Neuropsychopharmacology Uses chemical agents as probes to gain an understanding of the neurobiology of behavior
Drug Action Molecular changes produced by a drug when it binds to a target site or receptor
Drug effects The molecular changes alter physiological or psychological functions
Therapeutic effects The drug-receptor interaction produces desired physical or behavioral changes
Side effects All other effect
Specific drug effects Based on physical and biochemical interactions of a drug with a target site in the living tissue
Nonspecific drug effects Based on certain unique characteristics of the individual (e.g. mood, expectations, perceptions, attitudes)
Placebo effect nonspecific effect, pharmacology inert compound, but it can have therapeutic and side effects
Explanations for Placebo effects Pavlovian conditioning, Conscious expectation of outcomes, Social learning, genetic variants
Nocebo Negative expectations may increase the level of anxiety experienced, which may influence the outcome of treatment
Placebos used to evaluate the effectiveness of new medications because they eliminate the influence of expectation
Double-blind experiement Neither patient nor observer knows which treatment the patient has received
Bioavailability Amount of drug in the blood that is free to bind at target sites
Pharmacokinetic component of drug action: the dynamic factors that contribute to bioavailability
Pharmacokinetic Routes of administration, absorption and distribution, binding, Inactivation, excretion
Enternal methods gastrointestinal (GI) tract; generally slow and procedures variable blood levels
Parenteral methods injection, pulmonary, and topical administration
Oral administration (PO) safe, self-administered, economical
Absorption Movement of the drug from site of administration to the blood circulation
First-Pass Metabolism Potentially harmful chemicals pass via the portal vein to the liver, where they are chemically altered
Rectal administration Placement of a drug-filled suppository in the rectum
Rectal administration used for infants or patients who are vomiting, unconscious, or unable to take medication orally
Intravenous (IV) injection most rapid and accurate method
Drug abuse IV injection allows drug to reach brain instantly
Intramuscular (MI) injection slower, more even absorption over a period of time
Intraperitoneal (IP) injection rarely used with humans, but common for small laboratory animals
Subcutaneous (SC) injection drug is injected just below the skin
Inhalation drug is absorbed from the lungs
Tropical drug is applied to mucous membranes
Sublingual administration drug is placed under the tongue. Avoids gastric acid, enzymes, and first-pass metabolism
Intranasal administration can cause local effects such as relieving nasal con
Intranasal absorption occurs with cocaine "snorting"
Drug effect peaks in 15 to 30 minutes
Transdermal (through the skin) administration with skin patches: controlled and sustained delivery of drug
Transdermal can be used for vaccinations
Scopolamine Motion sickness
Epidural injection Spinal anesthetics are delivered directly to the cerebrospinal fluid; bypasses blood-brain barrier
Psychoactive drugs drugs that have an effect on thinking, mood, and behavior
Drug redistribution As plasma levels fall, drug concentration in highly vascularized organs will be greater than in blood, so the drug will move from those organs back into the plasma to maintain equilibrium
Drug redistribution can terminate the action of a drug
Cerebrospinal fluid (CSF) the subarachnoid space around the brain and spinal cord, ventricles, and canals
Blood-brain barrier the separation between brain capillaries and the brain/CSF
Teratogens developmental abnormalities
Depot binding nonselective; similar drugs can compete for binding sites
Depot binding results in drugs remaining in the body for extended periods
Half-life amount of time required for removal of 50% of the drug (t1/2)
Half-life determines interval between doses
Enzyme induction Repeated use of drug increase number of enzyme molecules and speeds biotransformation
Drug tolerance & Cross drugs lose effectiveness with repeated use
Enzyme inhibition A drug may inhibit an enzyme, also reducing metabolism of other drugs. Effects are more intense or prolonged; toxicity is possible
Drug competition for an enzyme elevated levels of one drug reduces metabolism of the second, causing potentially toxic levels.
Urine the most important route for drug elimination
Therapeutic drug monitoring Multiple blood samples are taken after drug administration, and plasma levels are measured
Pharmacodynamics Study of physiological and biochemical interaction of drug molecules with cell receptors in target tissue
Receptors proteins on cell surfaces or within cells
Ligand Molecule that binds to a receptor with some selectivity
Receptor agonist has best chemical "fit" (highest affnitity)' attaches readily to the receptor, and produces significant biological effect
Receptor antagonists fit receptors but produce no cellular effect (low efficacy)
Partial agonists have intermediate efficacy
Inverse agonists initiate a biological action that is opposite to that produced by an agonist
Up-regulation number of receptors increases
down-regulation number of receptors is reduced in response to absence of ligands or chronic activation
Potency absolute amount of drug necessary to produce a specific effect
Therapeutic Index (TI) TD50/ED50
Competitive antagonists Drugs that compete with agonists to bind receptors but do not intitate intracellualr effects, reducing effect of the agonist.
Noncompetitve antagonists reduced effect by: Binding to the receptor, disturbing the cell membranes, & interfering with cell processes
Physiological antagonism two drugs interact and reduce the effectiveness of both
Potentiation The combination of two drugs produces effects greater than the sum of their individual effects
Drug Tolerance Diminished response to a drug after repeated exposure
Cross tolerance Tolerance to one drug can diminish effectiveness of a second drug
Acute tolerance develops during a single administration
Metabolic tolerance (drug disposition tolerance) repeated use of a drug reduces amount of the drug available at the target tissue
Pharmacodynamic tolerance Changes in nerve cell function compensate for continued presence of the drug
Physical dependence withdrawal or abstinence syndrome is the hallmark
Behavioral tolerance (context-specific tolerance) tolerance is not apparent or is reduced in a novel environment
Pavlovian classical conditioning
Operant Conditioning plays a part in behavioral tolerance
State-dependent learning Tasks learned in the presence of a psychoactive drug
Sensitization (reverse tolerance) Enhancement of a drug effects after repeated administration of the same dose
Pharmacogentics Study of the genetic basis for variability in drug response among individuals
Created by: Ciera9105



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