Pharmacology NCM 2310 PDF

PHARMACOLOGY NCM 2310 2nd Semester...

PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY DEFINITION OF TERMS Pharmacotherapeutics Drugs The use of drugs and the clinical indications for drugs to prevent and treat diseases Chemicals that are introduced in the body to cause Empirical therapeutics – effective, but mechanism of some sort of change action is unknown Any chemical that affects the physiologic processes of a Rational therapeutics – specific evidence has been living organism obtained for the mechanisms of drug action Medicine The application of pharmacological information together with the knowledge of the disease for its prevention, substance or preparation that is taken into or placed on mitigation or cure the body used in treating disease, control or cure a condition Posology Therapeutic Drug branch of medical science which deals with dose or Uses - cure, prevent, treat quantity of drugs which can be administered to a patient Components - effectiveness, safety, Minor side to get desired pharmacological actions. effects Pharmacogenetics NOTE: All medicines are drugs, but not all drugs are medicines. science and study of the inheritance of characteristic patterns of interaction between chemicals (drugs) and Pharmacology organisms involves identification and description of such patterns, branch of science that deals with discriminating them from non-heritable patterns, and drugs and their uses elucidation of the mechanism of inheritance biological effects of chemicals Pharmacogenetic studies illuminate many intraspecific mode of action/mechanism of action and interspecific similarities, and differences in study of drugs and their interactions with living pharmacodynamic and pharmacokinetic mechanisms systems Adverse drug reactions Chronopharmacology derived from Greek, pharmacon means drug and logos means study. relationship between the time of drug administration and Oswald Schmiedeberg - father of pharmacology the pharmacological effects produced study of how the effects of drugs vary with biological Pharmaceutics timing and endogenous periodicities goal - to improve our understanding of periodic and thus the study how various drugs form influence predictable (e.g. circadian) changes in both desired pharmacokinetic and pharmacodynamic activities effects (chronoeffectiveness) and tolerance Dosage form design affects dissolution (chronotolerance) of medication discipline of pharmacy that deals with all facets of the process of turning a new chemical entity (NCE) into a Pharmacy safe and effective medication the science of dosage form design The science of identification, compounding and deals with the formulation of a pure drug substance into dispensing of drugs a dosage form includes collection, isolation, purification, synthesis and standardization of medical substances Pharmacokinetics Toxicology The study of what the body does to the drug The process by which a drug moves thru the body and study of biologic toxins out for elimination study of poison, sources, tests, antidotes, and its Absorption, distribution, metabolism, and excretion of deleterious effects of physical and chemical agents drug(s) in the body. (including drugs) in human In Greek kinesis or movement science of poisons, their source, chemical composition, Liberation - first step in the process by which medication action, tests and antidotes enters the body and liberates the active ingredient that study of poisons and poisoning has been administered. Pharmacognosy Pharmacodynamics study of natural (plant and animal) drug sources biochemical and physical effect of drug(s) and the mechanism of drug action The study of what the drug does to the body, i.e. the mechanism of drug actions in living tissues The science and study of how drugs produce their effects PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY SOURCES OF DRUGS SYNTHETHIC SOURCES NATURAL SOURCES more potent, more stable, less toxic, safer genetically engineered Plants Chemical (Propranolol) Earliest and most common drug source (leaves, roots, Biological (Penicillin) bark, sap, seeds, bulbs, fruits, blossoms, extracts) Biotechnology (Human Insulin) Alkaloids Steroids most active component in plants arthritis and other diseases alkaline in reaction, bitter in taste Sulfonamides/chemotherapeutic agents reacts with acids to form a salt that easily kill microorganism or slow their growth dissolves in body fluids synthesized Caffeine, Nicotine, Atropine Meperidine HCI (Demerol), quinolones, Glycosides omeprazole, sulfonamides, pancuronium, digitalis from wildflower - purple foxglove, dried neostigmine leaves of plant obtained from cell culture lanoxin, digoxin Urokinase - cultured kidney cells. Atropine - Atropa belladona produced by recombinant DNA technology Morphine - Papaver somniferum human insulin, tissue plasmogen activator Nicotine - Tobacco Hybridoma technique Reserpine (thiazide diuretic, vasodilator) - Rawolfia monoclonal antibodies sepentina Metformin - Gallega officinalis Recombinant DNA Technology or Genetic Engineering Opiates Insertion of Human or Human Modified Pro-insulin Quinine Gene into E. Coli or yeast Pilocarpine New technique for preparing drugs Physostigmine Advantages Resins mass production soluble in alcohol cost effective colonic irritant found in laxative cascara (Cascara less immunological reactions sagrada) Local irritants and caustic agents (laxatives) Oils thick greasy liquids volatile PHILIPPINE LAWS RELATED TO DRUGS peppermint, spearmint, juniper, oil of wintergreen, RA 9165 - Comprehensive Dangerous Drugs Act Of 2002 castor oil, olive oil 101 sections Animals provides for importation of Dangerous Drugs and/or Controlled Precursors and Essential Chemicals Body fluids, glands of animals establishes offences and penalty according to the Hormones – insulin different dangerous drug, regardless of the quantity and Oils & Fats – liver oils purity involved Enzymes – catalyst produced by living cells (pepsin) Vaccines – suspension of killed, modified, or RA 6675 - Generics Act of 1988 attenuated microorganism use of generic terminology Insulin, heparin, gonadotrophins and antitoxic sera ensure supply generic names the lowest possible cost Thyroid Drugs, Growth and Hormone Preparations recognition of therapeutic effectiveness promote drug safety by minimizing duplication Minerals Metallic and non-metallic minerals that provides RA 6425 - Dangerous Drugs Act of 1972 inorganic materials–from free elements, usually in Prohibited Drugs form of acids, bases or salts found in food opium Usually combined with other ingredients heroin Fe S04, Mg SO4 Restricted Drugs Dilute HCI – control/prevent indigestion barbiturates Calcium, aluminum, fluoride, iron, gold, potassium narcotics Inorganic Compounds hypnotic drugs Ferrous Sulfate Magnesium Sulfate RA 953 - Narcotics Drug Law Sodium Bicarbonate Imposition of fixed and special taxes upon all persons Aluminum Hydroxide who produce, import, manufacture, compound, deal in, Fluoride dispense, sell, distribute, or give away opium, marijuana, Iron opium poppies, or coca leaves, or any synthetic drug. Gold PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY RA 9502 - Universally Accessible Cheaper and Quality DRUG STANDARDS Medicines Act of 2008 amends: standardize the names and formulas drugs RA 8293 - Intellectual Property Code provide standards and test for the identity, purity and RA 6675 - Generics Act of 1988 quality of drugs RA 10918 - Philippine Pharmacy Law of 2016 issue as far as practical uniformity RA 10918 - The Philippine Pharmacy Law of 2016 REFERENCES ON DRUG STANDARDS regulating and modernizing the Practice of Pharmacy in the Philippines, Repealing for the Purpose Republic Act Philippine Index of Medical Specialties (PIMS) No. 5921, otherwise known as the Pharmacy Law. Medimedia Index of Medical Specialties expands the scope of the pharmacist's tasks to include (MIMS) immunization United States Pharmacopeia (USP) monographs on drug substances and dosage forms WAYS OF STANDARDIZING DRUGS approval of new drugs through The Philippine National Drug Formulary (PNDF) US FDA integral component of the Philippine Medicines Policy FDA-Philippines (formerly BFAD) which aims to make quality essential drugs available, accessible, efficacious, safe and affordable. for primary medical care contains list of drugs useful in meeting the immediate How are drugs created? therapeutic needs of the great majority of the population for commonly encountered ailments all Respect for Person over the country informed consent list of drugs’ generic name, route, administration, pharmaceutical forms, and strengths allows to Beneficence quickly find important medicine information and risk-benefit ratio practice guidelines for common health condition Justice Essential Drugs List (EDL) RESEARCH derived from PNDF, RHU use, immediate therapeutic DRUG DISCOVERY PHASE 1 (20-80 PHASE 2 (100-300 effects (ANIMALS AND TISSUE) HEALTHY ADULTS) REAL PATIENTS) initial section: rational approach to the use of medicines and physiologic & pharmacologic APPROVAL FOR SALE variables affecting response, dosage, and frequency PHASE 4 FDA APPLICATION PHASE 3 of administration (LONG-TERM) (1000+ PEOPLE) other parts: guidelines on proper prescription writing patient counseling timely report on the problems in AMR RESEARCH AND PHARMACOLOGY Main Section: list of medicines arranged by ATC Classification Independent System Dependent Variable Intervening (Extraneous Variable) Age Sex DRUG NOMENCLATURE Weight Disease State Chemical Name Experimental first name of a drug during early stages of development Control Group (chemical structure of the drug) placebo (inert) the drug’s chemical composition and molecular structure are not capitalized Can I force my patient to participate? Ex. p-isobutylhydratropic, acid-7-chloro-2-methylamino Can a child participate? Who explains the research to the patient prior to conduct? Generic Name What happens if the patient decided not to finish the nonproprietary name or common name research midway? given before a drug becomes official (shortened chemical name) listed in US pharmacopeia-national formulary name given by the United States Adopted Name Council official accepted name of the drug not in bold letters Ex. ibuprofen PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY Trade Name Pharmacokinetics brand name or proprietary name how the body acts on the drug first letter always capitalized; followed by the symbol ® or Study of TM absorption - taken into the body Ex. Advil, Motrin, Ibuprin, Librium distribution - moved into various tissues metabolism/biotransformation - changed into a form Official Name that can be excreted name listed under US FDA (generic name frequently used) excretion - drugs removed from the body concerned with a drug’s onset of action, peak concentration level, & duration of action pharmacokinetic component - half-life of the drug Half-Life - a measure of the rate at which drugs are removed from the body Critical Concentration - sufficient/high concentration of the administered drug working at the (molecular level) reactive tissues Dosage - based on the amount that must be given to eventually reach the critical concentration Loading Dose – usually drugs that are needed to take effect quickly Ex. (Aminophylline, Lanoxin) 3 PHASES OF DRUG ACTION Dynamic Equilibrium – actual concentration that a drug reaches the body Pharmaceutics (Dissolution) Pharmacodynamics Drug goes into solution so that it can cross the biologic membrane; drug becomes solution How the drug affects the body Not found in drug administered parenterally action of drug to the body 1st phase of drug action of agents taken by mouth study of the biochemical/ physiological effects of drugs Allows drugs to take on particular size and shape (mechanism of action) Enhance drug dissolution( ex. potassium (K) - losartan K physiologic and biochemical effects of a drug on the (cozaar); sodium (Na) -cloxacillin Na (Prostaphlin-A) body 2 Phases: Primary - intended (desirable) Disintegration – breakdown into smaller parts Secondary - all other effects; desirable or undesirable Dissolution – further breakdown into smaller parts in Mechanism of action - means by which a drug produces GI tract before absorption; dissolved into liquid alteration in function of their action Rate limiting - time it takes drug to disintegrate & dissolve to become available for body to absorb it 2 MAIN MECHANISMS OF ACTION Excipients - fillers and inert substances; allow the drug to take form; additives can increase its absorbability ALTERATION IN CELLULAR ENVIRONMENT Physical changes - changes in osmotic pressures = mannitol; change in brain cells for cerebral edema FACTORS AFFECTING DISSOLUTION lubrication = sunscreen Form of drug absorption = activated charcoal liquid vs. solid conditions on the surface of the cell membrane = liquid more absorbed than solid, already in solution, stool softener docusate - has emulsifying and rapidly available for GI absorption lubricating activity that causes a lowering of the surface tension in the cells of the bowel, Gastric pH permitting water and fats to enter the stool acid vs. alkaline Chemical changes - inactivation in cellular functions acidic media (pH = 1-2) - faster disintegration and or the alteration of the chemical component of body absorption fluids = such as change in pH; antacids neutralizes gastric acid Age young vs. elderly ALTERATION IN CELLULAR FUNCTION increased pH dec absorption; low pH inc absorption Drugs alters cell functions such as increase or decrease heart rate, blood pressure, urine output Enteric coated drugs Drug actions resist disintegration in gastric acid replace/act as substitute for missing chemicals increase or stimulate certain cellular activities Disintegration occurs only in alkaline environment depress/slow cellular activities (intestine); Should not be crushed interfere with functioning of foreign cells Presence of food – interferes with dissolution & invading microorganisms/neoplasms) absorption, enhance absorption of other drugs, may be chemotherapeutic agents protectants of gastric mucosa. PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY PHARMACOKINETIC PROCESSES ADMINISTRATION AND ABSORPTION Absorption ORAL what happens to a drug from the time it is introduced to most common, non-invasive, practical & viable the body until it reaches the circulating fluids and tissues Easily broken down by the gastric juices or the process by which medication enters the blood Affected by presence or absence of food in the stream stomach occurs after dissolution of a solid form of the drug of Ideal timing for administration after administration of liquid or parenteral drug first step in the passage of a drug through the body INTRAVENOUS unless IV drugs that cannot survive in enough quantity when Rate at which a drug leaves its site of administration, given orally and the extent to which absorption occurs Reaches their full strength at the time of injection Bioavailability - a measure of the extent of drug More likely to cause toxic effect (↑ margin for error) absorption in the body (0% to 100%) Bioequivalent - 2 drugs have the same bioavailability INTRAMUSCULAR and same concentration of active ingredients absorbed directly in the capillaries in the muscles & Areas of Absorption: sent into circulation (1 - 5cc) (site of giving?) GI, Orally, Rectally, Skin, Mucous Membranes, Takes effect faster in men than in women Lungs, Muscles, Subcutaneous Site of absorption - small intestine SUBCUTANEOUS small amount (0.5 - 1mL) usually in the upper arm, 3 PROCESSES OF ABSORPTION abdomen, thigh drugs move rapidly in vessels than in oral Passive Absorption (Diffusion) major process of absorption RECTAL/VAGINAL movement from higher concentration to lower absorbed by the perfusion of local blood flow in the concentration rectum/vagina ↑ concentration in one side, drug molecules moves treatment of local irritation or infection towards the area of ↓ concentration Movement towards the other side is faster if RESPIRATORY molecules are smaller, water-soluble and lipid available in all forms that targets the lungs Effortless process, passive process mostly in gas or inhalation form or mist no energy required occurs when smaller molecules diffuse across BUCCAL/SUBLINGUAL & TRANSLINGUAL membrane common route for certain cases of emergency drugs prevent destruction/transformation in the GI Active Transport uses energy to actively move a molecule across a cell TOPICAL membrane superficial or external use only requires a carrier (enzyme or protein) used for dermatologic, ophthalmic, otic and nasal carrier molecule actively moves the drug across preparation the membrane Energy is required SPECIAL AREAS/INFUSIONS from lower concentration to higher concentration given to a specific area of the body moves from an area of ↓ concentration to area of ↑ Epidural – injected in epidural space concentration (usually electrolytes) Intrapleural – injected in the pleural cavity Used to absorb electrolytes (i.e. sodium, potassium) Intraperitoneal – injected in the peritoneal cavity and some drugs (levodopa) Intraosseous – injected in the rich vascular bone network (long bone) Pinocytosis Intra-articular – injected into a joint engulfs the drug to carry it across the membrane used to transport drugs of exceptionally large size across the cell membrane involves engulfment of a drug by the cell membrane FACTORS AFFECTING DRUG ABSORPTION and transport into the cell by pinching off the drug Route of Drug Administration filled vesicle. Blood Flow through the tissue at the point of drug Transport fat-soluble vitamins (vit. A, D, E, K) administration Drug Solubility lipid soluble and nonionized: absorbed faster first pass effect or hepatic first pass or first-pass metabolism Lidocaine and NTG PHARMACOLOGY NCM 2310 2nd Semester A.Y. 2022-2023 Lecture | Level 2 | CPU CON Batch 2025 Neri, H.A.G. | BSN 2E UNIT 1: INTRODUCTION TO PHARMACOLOGY OTHER FACTORS AFFECTING DRUG ABSORPTION FACTORS THAT AFFECT BIOAVAILABILITY Drug solubility lipid soluble drugs pass readily through GI membrane Drug form water – soluble drugs need an enzyme or protein Route of administration fat-soluble and ionized (easily crosses cell GI mucosa & motility membrane, can cross BBB CNS) or H²O soluble Food & other drugs ↑ food pord of gastric acid, ↑ drug absorption Local condition at site of absorption (i.e. “azole”) weak acids less ionized in stomach - readily pass Changes in liver metabolism through the SMALL INTESTINE ↓ liver function, ↑ bioavailability Low protein-bound drugs -