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a chemical that affects the physiologic processes of a living organism |
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a science of that study drugs |
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describes the drugs chemical composition and molecular structure |
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what is the generic drug name |
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nonproprietary name, name given by the united states adopted name council |
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proprietary name the drug has a registered trademark ; use of the name is restricted by the drug patent owner ( usually the manufacture) |
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what are the three areas of pharmocology |
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[1] Pharmaceutics = how drug dosages affect the way in which the body metabolizes the drug [2] Pharmacokinetics= a study to determine what the body does to the drug molecules (A, D, M and E) [3] Pharmacodynamics = a study to determine to determine what the drug does to the body. |
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the study of how various drugs forms influence pharmacokinetics and pharmacodynamic activities |
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dissolution (pharmoceutics) |
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dissolving of dosage forms and their absorbtion - gel vs enteric coated |
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what are the three ways dosage is delivered |
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the study of what your body does to the drug -absorb -distribute -excrete -metabolise |
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the study what the drug does to your body - the mechanism of drug actions in living tissue |
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process of dose formulated drug |
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administration--> pharmaceutical phase I( disintegration of dosage form dissolution of drug in body)---> pharmacokinetic phase II ( absorbtion, distribution, metabolism, excretion)---> drug available for action now---> pharmacodynamics phase III ( drug receptor interaction---> effect |
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pharmacokinetics:absorbtion |
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The rate at which a drug leaves its site of administration, and the extent to which absorption occurs Bioavailability Bioequivalency |
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A measure of the amount of drug that is actually absorbed from a given dose |
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the relationship between two preparations of the same drug in the same dosage form that have a similar bioavailability. |
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factors that affect absorbtion |
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Absorption characteristics vary according to the dosage form and route -Food or fluids administered with the drug -Dosage formulation -Status of the absorptive surface -Rate of blood flow to the small intestine - Acidity of the stomach - Status of GI motility |
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ROUTES ARE IMPORTANT BECAUSE |
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A drug’s route of administration affects the rate and extent of absorption of that drug Enteral (GI tract) Parenteral Topical |
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The drug is absorbed into the systemic circulation through the oral or gastric mucosa or the small intestine Oral Sublingual Buccal Rectal (can also be topical) |
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The metabolism of a drug and its passage from the liver into the circulation A drug given via the oral route may be extensively metabolized by the liver before reaching the systemic circulation (high first-pass effect) The same drug—given IV—bypasses the liver, preventing the first-pass effect from taking place, and more drug reaches the circulation |
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-Intravenous (fastest delivery into the blood circulation) -Intramuscular -Subcutaneous -Intradermal -Intraarterial -Intrathecal - -Transdermal also can be considered parenteral |
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Introduced into or occurring in the space under the arachnoid membrane which covers the brain and spinal cord |
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pertaining to inside an artery |
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enters the dermal by a drug via ointment or patch |
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Skin (including transdermal patches) Eyes Ears Nose Lungs (inhalation) Rectum Vagina |
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The transport of a drug in the body by the bloodstream to its site of action Protein-binding Water soluble vs. fat soluble Blood-brain barrier Areas of rapid distribution: heart, liver, kidneys, brain Areas of slow distribution: muscle, skin, fat |
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areas of fast distribution |
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the heart, the liver, kidney, brain |
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areas of slow distribution |
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metabolism/biotransformation |
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The biochemical transformation of a drug into an inactive metabolite, a more soluble compound, or a more potent metabolite Liver (main organ) Skeletal muscle Kidneys Lungs Plasma Intestinal mucosa |
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Biologic transformation of a drug into: |
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An inactive metabolite A more soluble compound A more potent metabolite |
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Cytochrome P450 enzymes are essential for the metabolism of many medications. Although this class has more than 50 enzymes, six of them metabolize 90 percent of drugs, with the two most significant enzymes being CYP3A4 and CYP2D6. Genetic variability (polymorphism) in these enzymes may influence a patient's response to commonly prescribed drug classes, including beta blockers and antidepressants. |
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Metabolism or biotransformation Liver Hepatic metabolism = CYP-450 Examples of conditions and drugs that affect metabolism. |
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organs or body tissue involved in metabolism and biotransformation |
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Organs or body tissues Liver (main) Skeletal muscle Kidneys Lungs Plasma Intestinal mucosa |
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what are factors that decrease metabolism |
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cardiovascular dysfunction renal insufficiency starvation obstructive jaundice Slow acetylator (29% of people in parts of East Africa may have multiple copies of the gene, and will therefore not be adequately treated with standard doses of drugs such as the painkiller codeine (which is activated by the enzyme/e.g SSC story). Erythromycin( used for people allergic to penicillin) or ketoconazole (a drug used to treat a variety of fungal infections such as dandruff, jock itch, athlete's foot drug therapy) |
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what is a slow acetylator |
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A slow acetylator is a person who has an recessive single gene trait which effects the N acetylate transferase enzyme in the liver. This gene causes the enzyme to work slowly in the metabolism of certain drugs. Because of this slow pace situation the slow acetylator person will receive more of the given drug in his general circulation than a fast acetylator who is metabolizing the drug and sending it out of his body via the kidneys and urine at a quicker rate and thus leaving a smaller amount in the general circulation,i.e., bloodstream. The fast acetylator is in the optimum situation. (It is better to be fast than slow in drug metabolism.) |
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factors that increase metabolism |
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-fast acetylator -barbiturate therapy(Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia.) -rifampin therapy (is a bactericidal antibiotic drug of the rifamycin group) |
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delaying drug metabolism causes: |
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accumulation of drugs prolonged action of the drugs-->drug toxicity |
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stimulating(to heighten action, speeds up)drug metabolism |
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causes diminshed pharmacologic effects |
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the elimination of drugs from the body (excretion) is done by what three organs |
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kidney (main organ) liver bowel (biliary excretion, enterohepatic recirculation) |
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what three parts of the kidneys help in excretion |
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glomerular filtration active tubular reabsorbtion |
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-time required fpr 1/2(50%) of a given drug to be removed from the body -the time it takes for a substance (for examplemetabolite, drug, signalling molecule, radioactive nuclide, or other substance) to lose half of its pharmacologic, physiologic, or radiologic activity |
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the cellular processes involved in the drug and cell interaction |
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the physiologic reaction of the body |
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the time it takes for the drug to elicit a therapeutic responce |
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The time it takes for a drug to reach its maximum therapeutic response |
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The time a drug concentration is sufficient to elicit a therapeutic response |
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lowest blood level of drug |
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a drug cannot make a cell or tissue perform a funtion it was not designed to perform |
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Once the drug is at the site of action, it can modify the rate (increase or decrease) at which the cells or tissues function |
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pharmacodynamics mechanisms of actions |
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receptor interactions enzyme interactions nonselective interaction |
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drug binds to the receptor there is a responce |
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drug binds to the receptor, the responce is diminshed compared with that elicited by the anagonist |
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drug binds to the receptor, there is no response. drug prevents binding of agonists |
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drug competes with the agonist for the binding of the receptor. If it binds there is no responce |
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noncompetitive antagonist |
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drug combines with different parts of the receptor and inactivates it, agonist then has no effect |
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[1] Endpoint or outcome = defined and measurable. ( cure, eliminate, slow symptoms of dx process) [2] patient specific [3] time line = (e/g/antbx/7-10 days) |
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Any characteristic of the patient, especially a disease state, that makes the use of a given medication dangerous for the patient It is important to assess for contraindications! Examples please! certain congestaints are contradictions for people with high blood pressure |
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short term medical therapy |
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that is given to help keep cancer from coming back after it has disappeared following the initial therapy. |
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supplemental/replacement therapy |
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when the body has a deficiency of somthing you help replace it . for example a person with hypoxia you give them oxygen |
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(is treatment aimed at relieving symptoms -- it is not meant as a cure for the disease (cancer) |
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(fluids/fever)-Any form of treatment intended to relieve symptoms or help the patient live with them rather than attempt changes in character structure |
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guarding from or preventing the spread or occurrence of disease or infection |
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Empiric therapy (Antbx before surgery)- |
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is a medical term referring to the initiation of treatment prior to determination of a firm diagnosis |
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the effectiveness of a drug therapy must be evaluated one must be familiar with the drug's |
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-intended therapeutic action ( beneficial) -unintended but potential adverse effects ( predictable, adverse reactions) |
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what else do you monitor when giving drugs |
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Therapeutic index- Drug concentration- Patient’s condition Tolerance and dependence Interactions Adverse drug effects |
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the ratio between the dosage of a drug that causes a lethal effect and the dosage that causes a therapeutic effect. Also called margin of safety |
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Ratio of a drug’s toxic level to the level that provides therapeutic benefits (digoxin question) |
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Decreasing response to repeated drug doses |
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Physiologic or psychological need for a drug |
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interaction does not occur with other drugs or food |
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A drug interaction is the alteration of a drug’s action by: |
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Other prescribed drugs Over-the-counter medications Herbal therapies |
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what are four drug interactions |
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Additive effect Synergistic effect Antagonistic effect Incompatibility |
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An effect in which two substances or actions used in combination produce a total effect the same as the sum of the individual effects. |
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is the capacity of two or more drugs acting together so that the total effect of these drugs is greater than the sum of the effects if taken independently. |
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A biologic response to exposure to multiple substances that is less than would be expected if the known effects of the individual substances were added together.drug antagonists are drugs that compete for the available receptors. They may be noncompetitive and have no pharmacological effect of their own, or competitive in that they are capable of reversing or altering an effect already achieved. |
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may be chemical, i.e. the drugs react with each other and precipitate, produce gas or similar effect, or pharmacological in that the effects of the two on tissues are opposite, or pharmaceutical, e.g. immiscibility, insolubility |
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reactions(any unintended effect on the body as a result of the use of therapeutic drugs, drugs of abuse, or the interaction of two or more pharmacologically active agents) |
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4 types of adverse drug reactions |
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Pharmacologic reactions, including adverse effects Hypersensitivity (allergic) reaction Idiosyncratic reaction(unpredictable reactions that are different for every human) Drug interaction |
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what are two adverse drug events |
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Medication errors Adverse drug reactions |
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Predictable, well-known reactions that result in little or no change in patient management Predictable frequency Occurrences are related to the size of the dose Usually resolve when the drug is discontinued |
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a drug or other substance capable of interfering with the development of a fetus, causing birth defects. |
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Mutagenic-In genetics, a mutagen (Latin, literally origin of change) is a physical or chemical agent that changes the genetic material, usually DNA, of an organism and thus increases the frequency of mutations above the natural background level |
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a cancer causing substance or agent |
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what are four main sources of drugs |
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Plants Animals Minerals Laboratory synthesis |
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The study of poisons and unwanted responses to drugs and other chemicals |
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drugs can produce actions through several ways - receptors -enzymes -nonselective interactions |
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drugs can produce actions through several ways |
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[1] receptors [2] enzymes [3] nonselective interactions |
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lock and key agonists antagonist |
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Antibiotics given before surgery ; vaccines |
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Antibiotics given prior to throat culture results |
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what monitoring do you do for prophylactic therapy and empiric therapy |
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Therapeutic /beneficial effect Adverse reactions |
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monitoring drugs what are the 5 most important things to monitor for |
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Therapeutic Index Drug concentration Patient’s condition Tolerance and Dependence Interactions Drug interactions -Additive effects -Synergistic effects -Antagonistic effects -Incompatibility |
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the study of natural ( plant and animal ) drug sources |
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system priority (A,B,C) Prevent absorption of toxic sunstance |
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desired effect is systematic ( non-local) where substance is given via the digestive tract |
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Desired effect is systemic where substance is given by routes other than the digestive tract. Parenteral administration generally has the greatest bioavailability because it avoids an absorption phase as well as possible inactivation by first-pass metabolism by the liver. It can be further divided into two subgroups: parenteral by injection or infusion and other parenteral excluding oral route of administration |
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usually for a local effect, a substance is applied directly where its action is desired. |
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