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Chapter 2

Drug Action and Handling

TermDefinition
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.
Created by: C.delaRocha
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