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Principles of Pharma
Chapter 1
| Term | Definition |
|---|---|
| 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 |
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Ciera9105
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