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ADVANCED PHARMACOLOGY FINAL
EXAM QUESTIONS AND VERIFIED
SOLUTIONS.LATEST UPDATE 2025
Pharmacology - ✔✔✔the study of drugs (prescription, non-RX, botanicals, drugs of abuse and poison) How new drugs are developed - ✔✔✔Preclinical stage: early part of drug development
- this stage is performed on cells, tissues, and organs and in lab animals Phase I, II, & III of clinical trials and post-marketing surveillance Ideal Drug Properties - ✔✔✔• Convenient route of administration, probably taken by mouth
- Established dosage
- Immediate onset of action
- Produces a single desired biological action
- Produces no unwanted effects
- Convenient duration of action
- Dosage unaffected by loss of kidney or liver function or by disease state
- Improves quality of life
- Prolongs patient survival FDA approved drugs must be - ✔✔✔safe and effective and are screened by pharmacologists in various aspects of drug activity Clinical stage of new drug development - ✔✔✔-establish safety and effectiveness of new drugs in humans Phase 1 Clinical Trials - ✔✔✔establish biological effects, and safe doses and pharmacokinetics in a small number of healthy patients
Phase 2 Clinical trials - ✔✔✔new drugs are used to treat disease in a small number of patients and establish the potential of the drug to improve patient outcomes Phase 3 Clinical Trials - ✔✔✔compare the new medication to standard therapy in a larger number of patients studied in populations across the country. Post-marketing surveillance - ✔✔✔Monitoring safety of medications/devices AFTER they have been released on the market - important to report ADRs Clinical trials often have short follow up periods or small populations, too few participants to detect rare side effects therefore Failure to detect rare side effects in clinical trials is due to inadequate power Pharmacogenomics - ✔✔✔the study of how individual variations in drug targets or metabolism affect drug therapy Drug responses - ✔✔✔depend on the amount of drug administered. if it is an adequate dose, there will be a measurable biological response Dose-Response Curves - ✔✔✔The relationship between the dose or concentration of a drug and its biological response follows the laws of chemistry (the effect) The higher the concentration of a drug at its site of action, the more of the drug will bind to the receptor and the greater the response will be Types of Drug reponses - ✔✔✔Quantal - responses that may or may not occur (seizures or pregnancy) Graded- biological effects that can be measured (BP, diuresis)
determine the relationship between dose and effect, the selectivity of drugs, and the actions of pharmacological antagonists. Receptors provide a theoretical framework for understanding and predicting drug actions and the relationship between dose (or concentration) and effect. Also, receptors within the same "superfamily" often share properties Drug Targets - ✔✔✔enzymes, ion channel, transporters, cell surface receptors, nuclear hormone receptors, DNA Structure-activity relationship (SAR) - ✔✔✔correlation of chemical structure with pharmacological activity Ion channel receptors - ✔✔✔transmit signals across the cell membrane by increasing the flow of ions and altering the electrical potential or separation of charged ions across the membrane. Ex) nicotinic receptors responsible for muscle contraction, include receptors for ACh (nicotinic), GABA, and excitatory amino acids (glycine, aspartate, glutamate) Receptors coupled to G proteins - ✔✔✔G proteins share a similar structure in which seven regions of protein span the cell membrane to create a pocket (in which drugs can bind) and end with a receptor "tail" inside the cell. Individual G-protein receptors have the general G-protein structure but differ in their "binding site," the area that recognizes and binds to drugs, and in the intracellular portions of the G protein that control what happens after a drug is bound. Receptors are activated when specific drugs interact with the binding site, producing a conformational change, a sort of twist, in the G protein Transmembrane Receptors - ✔✔✔Consist of an extracellular hormone-binding domain and an intracellular enzyme domain that phosphorylates the amino acid tyrosine. The protein tyrosine kinase includes receptors for insulin, epidermal growth factor, and platelet- derived growth factors Intracellular Receptors Regulating Gene Expression - ✔✔✔1) Lipid soluble hormones pass thru the cell membrane and bind to intracellular receptors.
Glucocorticoid receptors reside in cytoplasm until it binds with a drug having glucocorticoid activity- conformation takes place and then it moves into the nucleus, where it controls the transcription of genes by binding to specific DNA sequences. Include: Corticosteroids, mineralcorticoids, sex steroids, Vitamin D, and thyroid hormones. They have more sustained response Enzymes - ✔✔✔biological molecules that encourage specific chemical reactions in the body. Drugs can act to stimulate or inhibit specific enzymes Ex) acetylcholinesterase breaks a chemical bond in ACh to terminate its action and produce acetic acid and choline Drug Action at Receptors - ✔✔✔Drugs do three basic things at receptors
- Agonists/Full agonists are drugs that produce receptor stimulation and conformational change every time they bind Full agonists DO NOT need of all of the receptors to produce a maximum response. They can produce a maximum response with 10% of the receptors. Receptors that are not needed for a response are called " spare receptors"
- Antagonists are drugs that occupy receptors without stimulating them. Antagonists occupy a receptor site and prevent other molecules, such as agonists from occupying the same site and producing a response ,therefore, the response we see is the inhibiting of the receptor stimulation by agonists Beta blockers Disease States and Receptors - ✔✔✔can selectively alter the number of receptors in various tissues throughout the body Ex) hyperthyroidism increases the number of beta-adrenoceptors, making these patients more likely to have HTN and tachycardia nonreceptor mechanisms - ✔✔✔general anethetics, sodium bicarb, and chelating agents are examples of drugs that their action is based on physiocochemical properties rather than their interaction with recpetors Pharmacokinetics - ✔✔✔the branch of pharmacology concerned with the movement of drugs within the body - absorption, distribution, metabolism, and excretion
single nucleotide polymorphism (SNP) - ✔✔✔minor mutations in proteins that can result in metabolic activity changes. explains why some groups of patients are more or less sensitive to certain drugs shown as a * - CYP2D6 --> CYP2D6* metabolism and half life - ✔✔✔metabolism is related to drug concentration so that a fixed fraction of drug is metabolized per hour. This is called first-order metabolism and is characterized by a half- life, the time period over which the drug concentration will decrease by half. Blood levels decrease by 50% in one half-life, 75% in two half-lives, and 87.5% in three half-lives. Drugs tend to be administered at intervals that are close to their half-life Prodrug - ✔✔✔Drug that is administered in an inactive form and does not become active until biotransformed by the liver. rely on metabolism to become active Drug Interactions - ✔✔✔Alterations in biotransformation are responsible for many drug-drug and drug-food interactions. There are a limited number of drug-metabolizing enzymes, and these enzymes can metabolize only one drug molecule at a time. If one drug monopolizes the enzyme, then it can block the biotransformation of other drugs, extending their time in the body and contributing to toxicity. Thus, when we look for drug interactions, we often look for drugs that are metabolized by the same CYPs Excretion - ✔✔✔removal of the drug from the body by the organs of elimination Most are eliminated by the kidneys also eliminated by: lungs, GI tract, sweat and saliva, mammary glands (breast milk) Renal Excretion - ✔✔✔theme of metabolism is to produce drug metabolites that are more water soluble and easily removed by kidneys. Glomerular filtration is the first step toward production of urine containing excreted drugs.
Tubular Reabsorption - ✔✔✔In addition to reabsorption by passive diffusion, some substances filtered at the glomerulus are reabsorbed by active transport systems located primarily in the proximal tubule of the nephron Tubular Secretion - ✔✔✔Tubular secretion often contributes to the renal elimination of drugs that have short half-lives. transports drugs from the blood into the lumen of the nephron Renal Excretion of Drugs - ✔✔✔rate at which a drug is excreted by the kidneys depends on:
- renal blood flow affects GFR
- Filtration of the glomerulus depends on the molecular size , the charge, and the degree of protein binding
- Tubular acidity will influence the degree of reabsorption *Monitor renal function Renal function is effected by: age, hydration, cardiac output Biliary Excretion - ✔✔✔In addition to metabolizing many drugs, the liver secretes about a liter of bile each day. Drugs can enter the bile and be excreted into the intestinal tract when bile is released to help digest food. Only small amounts of drug enter the bile by diffusion; instead, biliary excretion contributes to removal of some drugs Enterohepatic cycle - ✔✔✔drugs that are excreted in bile can be reabsorbed in the intestine. drug is excreted in the bile, absorbed from the intestines, and then excreted again in the bile
- Decreases the amount of drug that is actually excreted and extends the time the drug is in the body other sites of excretion - ✔✔✔pulmonary excretion: gases - nitrous oxide, ethanol
