Psychopharmacology: Chapter 1

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pharmacology
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study of the actions of drugs and their effects on living organisms
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neuropharmacology
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area of pharmacology specializing in drug-induced changes to the function of cells in the nervous system
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psychopharmacology
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area of pharmacology specializing in drug-induced changes in mood, thinking
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neuropsychopharmacology
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area of pharmacology focusing on chemical substances that interact with the nervous system to alter behavior, emotions, and cognition
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drug action
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specific molecular changes associated with a drug binding to a particular target site or receptor
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drug effects
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alterations in physiological or psychological functions associated with a specific drug
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therapeutic effect
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desired physical or behavioral change associated with a particular drug
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side effect
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undesired physical or behavioral change associated with a particular drug
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specific drug effects
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physical or behavioral changes associated with biochemical interactions of a drug with the target site
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nonspecific drug effects
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physical or behavioral changes not associated with the chemical activity of the drug-receptor interaction but with certain unique characteristics of the individual such as present mood or expectations of drug effects (based on certain unique characteristics of the individual)
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bioavailability
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concentration of drug present in the blood that is free to bind to specific target sites
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pharmacokinetic
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factors that contribute to bioavailability: the administration, absorption, distribution, binding, inactivation, and excretion of a drug
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enteral
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drug administration by oral or rectal routes (GI tract)
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parenteral
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methods of drug administration that do not use the gastrointestinal system, such as intravenous, inhalation, intramuscular, transdermal, etc
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oral administration (PO)
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method that involves administration of a drug through the mouth
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absorption
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movement of a drug from the site of administration to the circulatory system
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first pass metabolism
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phenomenon in which the liver metabolizes some of a drug before it can circulate through the body, particularly when the drug has been taken orally
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rectal administration
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drug delivery method, such as suppository, used to deliver drugs via the lower intestine.
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intravenous (IV)
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method that involves administration of a drug directly into the bloodstream by means of a vein.
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intramuscular (IM)
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method that involves administration of a drug into a muscle
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intraperitoneal (IP)
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injection technique that is the most common route of administration for small laboratory animals. The drug is injected through the abdominal wall into the peritoneal cavity – the space that surrounds the abdominal organs
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subcutaneous (SC)
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method that involves injection of a drug just below the skin.
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inhalation
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method that involves administration of a drug through the lungs
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topical
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method that involves administration of a drug through a mucous membrane such as the oral cavity, nasal mucosa, or vagina.
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intranasal administration
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topical administration of a drug into the nasal mucosa
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transdermal
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method that involves administration of a drug through the skin
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epidural
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method that involves administration of a drug into the cerebrospinal fluid surrounding the spinal cord. by-passes the blood brain barrier
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intracranial
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method that involves administration of a drug into the brain tissue
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intracerebroventricular
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method that involves administration of a drug into the brain tissue
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infusion pump
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drug delivery via an implanted pump (subcutaneous) that delivers regular, constant doses to the body or into the cerebral ventricles
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gene therapy
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application of DNA that encodes a specific protein to increase or block expression of the gene product to correct a clinical condition
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viral vectors
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use of a virus as a delivery system (called a vector) to carry a gene into the nuclei of target cells to alter protein synthesis
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psychoactive drugs
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those drugs that have an effect on thinking, mood, or behavior
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phospholipids
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lipid molecules that are major constituents of the cell membrane. they are composed of a polar head and two lipid tails
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passive diffusion
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movement of lipid-soluble materials across a biological barrier without assistance based on its concentration gradient, from higher to lower concentration.
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concentration gradient
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difference in the amount of concentration of a substance on each side of a biological barrier, such as the cell membrane
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partition coefficient
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an experimentally-derived measure of a drug’s lipid solubility used to predict its relative rate of movement across cell membranes
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ionization
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process involving the dissociation of an electrically neutral molecule into charged particles (ions)1
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cerebrospinal fluid
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fluid that surrounds the brain and spinal cord, providing cushioning that protects against trauma.
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intercellular clefts
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small gaps between adjacent cells
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fenestrations
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large pores in endothelial cells allowing rapid exchange between blood vessels and tissue
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pinocytotic vesicles
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types of vesicles that envelop and transport large molecules across the capillary wall.
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tight junctions
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connection between cells characterized by a fusing of adjoining cell memebranes
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astrocytes
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star-shaped cells of the nerve tissue that have numerous extensions and that modulate the chemical environment around neurons, metabolically assist neurons, and provide phagocytosis for cellular debris
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area postrema
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area in the medulla of the brain stem that is not isolated from chemicals in the blood. it is responsible for inducing a vomiting response when a toxic substance is present in the blood
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median eminence
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area in the hypothalamus that is not isolated from chemicals in the blood and where hypothalamic-releasing hormones are secreted for transport to the anterior pituitary gland
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xenobiotics
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chemicals that are foreign to the living organism
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teratogens
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any agent including a virus, drug, or radiation that induces abnormal fetal development, causing birth defects
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drug depots
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inactive sites where drugs accumulate. there is no biological effect from drugs binding at these sites, nor can they be metabolized
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depot binding
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type of drug interaction involving binding to an inactive site, such as to proteins in the plasma, to bone, or to fat
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first order kinetics
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term used to describe exponential elimination of drugs from the bloodstream
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half life
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time required to remove half of the drug from the blood. It is referred to as t1/2
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steady state plasma level
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the desired blood concentration of drug achieved when the absorption/distribution phase is equal to the metabolism/excretion phase
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zero order kinetics
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term used to describe a constant rate of drug removal from the body, regardless of drug concentration in the blood
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biotransformation
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inactivation of a drug through a chemical change, usually by metabolic processes in the liver
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CYP450
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class of liver enzymes, in the microsomal enzyme group, responsible for both phase 1 and phase 2 biotransformation of psychoactive drugs.
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enzyme induction
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increase in liver drug-metabolizing enzymes associated with repeated drug use
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enzyme inhibition
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reduction in liver enzyme activity associated with a specific drug
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drug competition
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interaction between two drugs that share a metabolic system and compete for the same metabolic enzymes. bioavailability of one or both increases
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genetic polymorphisms
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genetic variations in a population resulting in multiple forms of a particular protein
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therapeutic drug monitoring
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taking multiple blood samples to directly measure plasma levels of a drug after administration, to identify the optimum dosage for maximum therapeutic potential and minimal side effects
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pharmacodynamics
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study of physiological and biochemical interactions of a drug with the target tissue responsible for the drug’s effects
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receptor
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protein located on the surface of or within cells that bind to specific ligands to initiate biological changes within the cell
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ligand
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molecule that selectively binds to a receptor
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receptor agonists
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a neurochemical or drug that can bind to a particular receptor protein and alter the shape of the receptor to initiate a cellular response
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affinity
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attraction between a molecule and a receptor
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efficacy
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the extent to which a ligand-receptor binding initiates a biological action
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receptor antagonists
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a molecule that interacts with a receptor protein and produces no cellular effect after binding, and also prevents an “active” ligand from binding
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partial agonists
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drugs that bind to a receptor but have low efficacy, producing weaker biological effects than a full agonist. Hence they act as agonists at some receptors and antagonists at others, depending on the regional concentration of full agonist.
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inverse agonists
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substance that activates a receptor but produces the opposite effect of a typical agonists at that receptor
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up regulation
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increase in the number of receptors, which may be a consequence of denervation or of chronic antagonist treatment
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down regulation
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decrease in the number of receptors, which may be a consequence of chronic agonist treatment
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receptor subtypes
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group of receptors that respond to the same neurotransmitter but that differ from each other to varying degrees with respect to their structure, signaling mechanisms, and pharmacology
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dose response curve
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graph used to display the amount of biological change in relation to a given drug dose
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potency
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measure of the amount of drug necessary to produce a specific response
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therapeutic index
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the relationship between the drug dose that results in a toxic response compared to the dose required for the desired biological response. It is represented by the equation TI = TD50/ED50
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competitive antagonists
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drugs that bind to a receptor but has little or no efficacy. when it competes with an agonist for receptor sites, it reduces the effect of the agonist
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noncompetetive antagonist
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drug that reduces the effect of an agonist, but does not compete at the receptor site. the drug may bind to an inactive portion of the receptor, disturb the cell membrane around the receptor, or interrupt the intercellular processes initiated by the agonist-receptor association
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physiological antagonism
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drug interaction characterized by two drugs reducing each other’s effectiveness in the body
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additive effects
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drug interactions characterized by the collective sum of the two individual drug effects
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potentiation
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drug interaction characterized by an increase in effectiveness greater than the collective sum of the individual drugs
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tolerance
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decreased response to a drug as a direct result of repeated drug exposure
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cross tolerance
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tolerance to a specific drug can reduce the effectiveness of a another drug in the same class
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acute tolerance
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rapid tolerance formed during a single administration of a drug, as is the case with alcohol
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drug disposition tolerance
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metabolic tolerance. type of tolerance to a drug that is characterized by a reduces amount of drug available at the target tissue, often as a result of more-rapid drug metabolism.
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pharmacodynamic tolerance
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type of tolerance formed by changes in nerve cell functions in response to the continued presence of a drug
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behavioral tolerance
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the reduced effectiveness of a drug administered chronically that involves learning: either operant or classical conditioning
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classical conditioning
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repeated pairing of a neutral stimulus with an unconditioned stimulus. Eventually the neutral stimulus becomes a conditioned stimulus and elicits a (conditioned) response that is similar to the original unconditioned response
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operant conditioning
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type of learning in which animals learn to respond to obtain rewards and avoid punishment
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state-dependent learning
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condition characterized by better performance of a particular task that was learned in a drugged state in the same drugged state, rather than in a nondrugged state. Tasks learned in a nondrugged state are likewise performed better in a nondrugged state.
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sensitization
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enhanced response to a particular drug after repeated drug exposure
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pharmacogenetics
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the study of the genetic basis for variability in drug response among individuals
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microsomal enzymes
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enzymes in liver cells responsible for metabolizing exogenous substances such as drugs

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