PHARMACOLOGY 1
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PHARMACOLOGY 1 - Detalles
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| 🇬🇧 | 🇬🇧 |
| The science of substances used to prevent, diagnose and treat disease. | Medical Pharmacology |
| The science of drug preparation and the medical use of drugs -- the precursor of pharmacology | Materia Medica |
| Two General Principles (PHARMACOLOGY) | 1 All substances can under circumstances be toxic, and the chemicals in botanicals are no different from chemicals in manufactured drugs except for the proportion of impurities 2 All dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies |
| The study of the GENETIC VARIATIONS that cause differences in drug response among individuals or populations. | Pharmacogenomics (also called Pharmacogenetics) |
| The use of drugs to prevent and treat disease | Pharmacotherapeutics |
| Brand name/ Proprietary name Selected by the drug company selling the product Protected by copyright | Trade Name |
| Family Drugs that share similar characteristics Ex: Beta-adrenergic blockers | Pharmacologic Class |
| Groups drugs by therapeutic use Ex: Antihypertensives | Therapeutic Class |
| POWER PLANT: | 1 Alkaloids 2 Glycosides 3 Gums 4 Resins 5 Oils |
| Animal Magnetism Drugs obtained from animal sources | 1 hormones such as insulin 2 oils and fats (usually fixed) - cod liver oil 3 enzymes - pancreatin and pepsin 4 vaccines |
| Mineral Springs: __ | • Iron • Iodine • Epsom salt |
| Drugs produced in the laboratory | Down to DNA |
| Routes of Administration | • buccal, sublingual, translingual • gastric • intradermal • intramuscular • intravenous • oral • rectal and vaginal • respiratory • subcutaneous • topical |
| 1 activator -has affinity to the receptor and intrinsic activity 2 Inhibitor -has affinity only | 1 AGONIST 2 ANTAGONIST |
| Inhibitor has affinity only | ANTAGONIST |
| May interact directly with other drugs | Chemical Antagonists |
| The Physical Nature of Drugs | • Solid - Aspirin, Atropine • Liquid - Nicotine, Ethanol • Gaseous - Nitrous Oxide |
| Drug Size, SMALLEST and LARGEST | 1 Smallest -- Lithium ion (MW 7) 2 Largest -- Alteplase (MW 59,050) 3 Most drugs -- MW 100-1000 |
| Three major types of bonds | 1 covalent, 2 electrostatic and 3 hydrophobic |
| Implies the ability to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor | Rational Drug Design |
| Must undergo extensive animal studies | IND - Investigational New Drug |
| 1 actions of drug on the body 2 actions of the body on the drug | 1 Pharmacodynamics 2 Pharmacokinetics |
| Involves trials with people who have the disease for which the drug is thought to be effective. | Phase II |
| Exceptions to the Rule | 1 Public health threat of disease like AIDS, COVID-19 2 Sponsors of drugs that reach phase II or III clinical trials can apply for FDA approval of treatment IND status |
| 1 actions of drug on the body 2 actions of the body on the drug | 1 Pharmacodynamics 2 Pharmacokinetics |
| LADMERS | • Liberation of an active ingredient from the dosage form • Absorption into systemic circulation • Distribution • Metabolism in the body • Excretion of the drug from the body • Response |
| • directly proportional to the concentrations, surface area and permeability coefficient • inversely proportional to the thickness of the membrane | Fick's Law of Diffusion |
| Reverse of endocytosis | Exocytosis |
| Factors influencing absorption | 1 Effect of pH on drug absorption 2 Blood flow to the absorption site 3 Total surface area available for absorption 4 Contact time at the absorption surface |
| Absorbs nutrients in the small intestine | Microvilli |
| Responsible for transporting various molecules, including drugs, across cell membranes - "pumps" drugs out of the cells - associated with multi-drug resistance | Expression of P-glycoprotein |
| Bioavailability is usually measured using __ | Area Under the Curve (AUC) |
| 1) 100% Bioavailability, most rapid onset 2) 5 to <100 Bioavailability, most convenient; may have significant First Pass Effect | 1 Intravenous 2 Oral |
| Factors Influencing Bioavailability: when a drug is absorbed from the GI tract, it enters the PORTAL CIRCULATION before entering the systemic circulation | First-pass Hepatic Metabolism |
| Factors Influencing Bioavailability | 1 First-pass Hepatic Metabolism 2 Solubility of the drug 3 Chemical instability 4 Nature of the drug formulation |
| Show comparable bioavailability and similar times to achieve peak blood concentrations | BIOEQUIVALENCE |
| Pharmaceutically equivalent with similar chemical and safety profiles | THERAPEUTIC EQUIVALENCE |
| If the drugs have the same dosage form, contain the same active ingredient, and use the same route of administration | Pharmaceutical Equivalence |
| The process by which a drug reversibly leaves the bloodstream and enters the instertitium (extracellular fluid) and the tissues | DRUG DISTRIBUTION |
| The process by which a drug reversibly leaves the bloodstream and enters the instertitium (extracellular fluid) and the tissues. | DRUG DISTRIBUTION |
| What are the Special Barriers to Distribution? | 1 Placental (most small molecular weight drugs cross the placental barrier; fetal blood levels are usually lower than maternal) 2 Blood-brain (permeable only to lipid-soluble drugs or those of very low molecular weight) |
| • Concentration of drug at the receptor site • Commonly measured in the blood (Exception for topical agents) | EFFECTIVE DRUG CONCENTRATION |
| Plasma concentration is a function of | – the rate of input of the drug (by absorption) into the plasma – the rate of distribution – and the rate of elimination |
| Pharmacokinetics TWO BASIC PARAMETERS | 1 CLEARANCE 2 VOLUME OF DISTRIBUTION |
| The measure of the apparent space in the body available to contain the drug. | VOLUME OF DISTRIBUTION |
| The ratio of the amount of drug in the body to the drug concentration in the plasma or blood | Volume of distribution -Can be affected by liver and kidney disease |
| METABOLISM OF DRUGS Three major routes: | – Hepatic metabolism – Biliary metabolism – Urinary metabolism |
| Metabolism (Biotransformation) PHASES | 1) Phase I (Functionalization) – Redox Reactions and hydrolysis. 2) Phase II (Conjugation) – Attacks certain drugs with existing functional groups and attaches conjugate molecules |
| Metabolism (Biotransformation) May be affected by | • Drug Interactions due to inducers, inhibitors, and substrates • Genetic factors • Disease states DRUG WITH INDUCER - FASTER DRUGS WITH INHIBITOR - SLOWER |
| EXCRETION; Renal elimination of drugs: | – Glomerular filtration – Proximal tubular secretion – Distal tubular reabsorption |
| Excretion process | 1 Glomerular filtration of water and unbound drugs and metabolites 2 Active tubular secretion of acidic and basic drugs and metabolites 3 Active reabsorption of acidic and basic endogenous compounds and passive reabsorption of lipophilic drugs 4 Urinary excretion of drugs and metabolites that are filtered and or actively secreted and not reabsorbed |
| Describes the actions of a drug on the body and the influence of drug concentrations on the magnitude of the response | PHARMACODYNAMICS |
| • Their ligands are presently unknown • May prove useful targets for the development of new drugs. | ORPHAN RECEPTORS |
| • MEDIATE the actions of endogenous chemical signals such as neurotransmitters, autacoids and hormones. | REGULATORY PROTEINS |
| Membrane receptor for digitalis glycosides a TRANSPORT PROTEIN | Na+/K+ ATPase Pump |
| Ionotropic receptors associated with ligand-gated ion channels Features: LOCATION = __ EFFECT = __ | CLASS 1 LOCATION: Cell membrane EFFECT: millisecond |
| Controls Na+ channels (Ligand-gated) -- inhibited by curare and derivatives, ganglionic blockers | Nicotinic Receptor (CLASS 1) |
| Controls Cl- channels | GABAA-receptor complex (CLASS 1) |
| Metabotropic 7 transmembrane-spanning G-protein-linked Features: LOCATION = __ EFFECT= __ | Class II LOCATION: Cell membrane EFFECT: Seconds |
| G-proteins: __ | 1) Gs 2) Gi 3) Gq |
| Activates adenylyl cyclase which produces the second messenger cyclic adenosine monophosphate (cAMP) | Gs |
| Enzyme-linked receptors • Features: EFFECT = __; possesses tyrosine kinase activity as part of their structure | Class III EFFECT: minutes to hours |
| CLASS III example | • Epidermal growth factor • Atrial natriuretic peptide • Insulin |