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Chapter 2
Drug Action and Handling
| Term | Definition |
|---|---|
| Low Dose-Effect Curve | Measuring the response to the dose of the drug. |
| Potency | The amount of drug required to produce an effect. |
| Efficacy | Related to the maximal effect of a drug regardless of dose |
| Therapeutic action | The intended or desired results. |
| Therapeutic range | Range between the dose causing the minimum effect and the dose causing the minimum adverse effect. |
| Therapeutic index(TI) | Number that determines the safety of a drug. (the greater the TI, the safer the drug) |
| Hepatic | Liver |
| Biotransformation | Is the body's way of changing a drug so that it can be more easily excreted by the kidneys. |
| Tolerance | The need for an increasingly larger dose to obtain the same effect as the original dose. |
| Renal | Kidney |
| Duration | The length of a drugs effect. |
| Half-life | The half-life of a drug is the amount of time that passes for its concentration to fall to half(50%) of its original blood level. |
| Where is the potency of a drug shown in a drugs curve along the log-dose axis? | X-axis |
| Where is the efficacy of a drug shown in a drugs curve along the log dose axis? | Y-axis |
| What is the mechanism of action? | Refers to how the drug works at a molecular or cellular level. |
| What is an agonist? | A drug that enhances the function. |
| What is an antagonist? | A drug that inhibits the function. |
| Pharmacokinetics | The study of how the drug is processed by the body. |
| What are the 4 major steps of pharmacokinetics? | Absorption, Distribution, Metabolism, Excretion |
| What is the epression for the TI? | TI=LD |
| What are the processes a drug uses to pass through a permeable membrane? | Passive transfer and Specialized transfer |
| What is passive transfer? | Lipid-soluble substances moving across the lipoprotein membrane by a passive transfer process called simple diffusion. |
| What are the two processes of specialized transfer? | Active transport and facilitated diffusion. |
| What are the three major routes of administration? | Enternal, parental, and topical |
| The enternal route is administered... | Orally, sublingually, and rectally |
| The parental route is administered... | Intravenous, intramuscular, subcutaneous, and intradermal |
| The topical route is administered... | On the surface of the body and is slowly absorbed by the capillaries under the skin. |
| What are cell membranes composed of? | Lipids, proteins, and carbohydrates. |
| What is the function of lipids in the membrane? | Make the membrane relatively impermeable to ions and polar molecules. |
| What is the function of proteins in the membrane? | help move the molecule across the membrane. |
| What is the function of carbohydrates in the membrane? | They are combined with either proteins or lipids. |
| What physicochemical properties of chemicals influence the passage of a drug across biologic membranes? | Lipid solubility, degree of ionization, and molecular size and shape. |
| What is active transport? | When the substance is transported against a concentration gradient or electrochemical gradient. |
| What is facilitated diffusion? | The substance does not move against the concentration gradient. involves the transport of some substances into cells called pinocytosis. |
| What is absorption? | The entry of the therapeutic agent into the blood stream. |
| What are the influences of the rate of absorption? | Physiochemical factors, site of absorption, and drug solubility |
| What are the two forms that drugs occur within the blood? | Bound to plasma proteins and free |
| What are the two major barriers? | Blood-brain barrier and the placental |
| What are the factors that affect distribution? | Size of organ, blood flow to the organ, solubility of the drug, plasma membrane binding capacity, the presence of certain barriers. |
| What is metabolism? | The process where the body breaks down/converts medication into other substances. |
| Where is the primary site for drug metabolism? | The liver. |
| What is active to inactive metabolism? | An inactive drug may be formed from an active parent drug. |
| What is inactive to active metabolism? | An inactive drug may be transformed into an active compund. |
| What is active to active metabolism? | An active parent drug may be converted to a second active compound, which is then converted to an inactive product. The result is that the action of the drug is prolonged. |
| What is the first-pass effect? | When drugs are given orally, they are absorbed through the intestinal wall and then pass trhough the liver, which can inactivate some drugs. |
| What are phase 1 reactions? | Lipid soluble molecules are metabolized by three processes: Oxidation, reduction, and hydrolysis. |
| What are phase 2 reactions? | Conjugation with glucuronic acid(glucuronidation). Allows for the body to convert a lipid soluble drug to a more polar compound with the use of transferases. |
| What is the use of cytochrome p-450? | Can be used to induce or inhibit metabolism. |
| Where does drug excretion primarily occur? | kidneys. |
| What are nephrons? | Microscopic units that filter the blood and produce urine. |
| What is route 1 of extraction through the kidneys? | Glomerular filtration: Unchanged drug- filtered through glomeruli - concentrated in the renal tubular fluid. |
| What is route 2 of extraction through the kidneys? | Active tubular secretion: The drug in the bloodstream transported -across the renal tubular epithelial cells - into the renal tubular fluid. |
| What is route 3 of extraction trhough the kidneys? | Passive tubular diffusion: Favors the reabsorption of unionized, lipid-soluble compounds. The more ionized , less lipid soluble metabolites have more difficulty penetrating the cell membranes and are likely to be in tubular fluid and eliminated in unrine |
| If a drug has a short half-life, what does this mean? | It will be removed from the body faster. |