Pharmacology Objectives 1. The student will be able to understand how medications are measured 2. The student will know what the FDA is and why they are necessary for safety 3. The student will know what the difference is between the Therapeutic dose and the lethal dose of a medication and some examples. 4.The student will understand the importance of knowing what drugs can be combined and where to find that information 5. The student will understand the different types of drug interactions. It’s all about Metric The metric system is used for drug dosages,measurement. Teaspoons, Tablespoons, cups,ounces to pounds are the familiar measurements milligrams, grams, kilograms are how things are measured in the medical world. Easier than you think. Everything relates by a 10th, 100th or 1000th. Examples Units of metric measurement Quantity measured Unit mass milligram Symbol mg Gram Kilogram Volume kg 1000 mg= 1 gram 1 kg= 1000 g metric ton=1000kg milliliter ml 1000 ml= 1 liter Cubic centimeter cc 1 ml= 1 cc Liter Cubic meter ** 1 tsp= 5 ml g Relationship 1 cup=250 ml l cm 1000 l= 1 cm What dose of Motrin? What dose of Motrin Overview & Uses When your child isn't feeling well, bring them relief with Children's MOTRIN®. Its safety profile is supported by one of the largest and most rigorous children's clinical studies ever conducted. And, it lasts up to 8 hours. Children's MOTRIN® will help you both feel better. Uses: Temporarily: Relieves minor aches and pains due to the common cold, flu, sore throat, headache and toothache Reduces fever Naproxen, Aleve, Naprosyn Naproxen 250 mg or 375 mg or 500 mg twice daily Naproxen sodium 275 mg (naproxen 250 mg with 25 mg sodium) twice daily 550 mg (naproxen 500 mg with 50 mg sodium) twice daily What dose of medication? What volume contains the dose you need? If you have an ampoule of 500mg in 4ml, and you need 200mg, it can appear to be a daunting calculation. The first step is to find out what volume contains 1mg (4/500) and then multiply it by how many mg you want (200). The easy way to remember this is the famous nursing equation: ‘What you want, over what you’ve got, times what it’s in’ In this instance: 200mg x 4ml / 500mg = 1.6ml The common error here is to get it upside down, and divide what you’ve got by what you want. This fortunately gives you a stupid answer, which is obviously wrong, in this case 10ml. You already know that you need a fraction of an ampoule and not two and a bit ampoules, which highlights the error. Oral vs parenteral Depends on chemical composition and how drug is metabolized. Definition Drug metabolism is the process by which the body breaks down and converts medication into active chemical substances/metabolites Precautions Drugs can interact with other drugs, foods, and beverages. Interactions can lessen or magnify the desired therapeutic effect of a drug, or may cause unwanted or unexpected side effects. There are thousands of possible drug-to-drug and drug-to-food interactions, and many medications and supplements are contraindicated (not recommended) under certain conditions or in patients with specific diseases and disorders. This is why it is imperative that patients always keep their physician fully informed about all drugs and dietary supplements (including herbal remedies) they are taking. Drug Metablolism Definitions The Liver-,The primary site of drug metabolism, the organ that plays a major role in metabolism, digestion,detoxification, and elimination of substances from the body. A solid organ located on the right in the upper abdomen. It plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body. Enzymes-organic substances (proteins) composed of amino acids that trigger and regulate chemical reactions in the body. There are over 700 identified human enzymes Metabolites- Substances produced by metabolism or by a metabolic process. They are then bound to other substances for excretion through the lungs, or bodily fluids such as saliva, sweat, breast milk, and urine, or through reabsorption by the intestines. Definitions continued the kidneys-The primary mode of excretion for drug metabolites (where urine comes from.) We have 2 located both sides of mid back Cytochrome P-450-The family of liver isoenzymes that are crucial to drug metabolism Metabolism-the sum of all the physical and chemical processes occurring in the body to organize and maintain life Catabolism- a process of metabolism that breaks down complex substances into simple ones. Cirrhosis-Liver disease characterized by the widespread disruption of the normal liver structure and function. CNS Depressant- Anything that depresses, or slows, the sympathetic impulses of the central nervous system (i.e., respiratory rate, heart rate). Drug metabolism Drugs can interact with other drugs, foods, and beverages. Interactions can lessen or magnify the desired therapeutic effect of a drug, or may cause unwanted or unexpected side effects. There are thousands of possible drug-to-drug and drug-to-food interactions, and many medications and supplements are contraindicated (not recommended) under certain conditions or in patients with specific diseases and disorders. This is why it is important that patients always keep their physician fully informed about all drugs and dietary supplements (including herbal remedies) they are taking. Drug Metabolism Physiology The primary site of drug metabolism is the liver Enzymes in the liver are responsible for chemically changing drug components into substances known as metabolites. Metabolites are then bound to other substances for excretion through the lungs, or bodily fluids such as saliva, sweat, breast milk, and urine, or through reabsorption by the intestines. The primary mode of excretion is through the kidneys. The family of liver isoenzymes known as cytochrome P-450 are crucial to drug metabolism. These enzymes (labeled CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) have a catabolic action on substances, breaking them down into metabolites. They also act to lower the concentration of medication in the bloodstream. Drug Interactions: Definition “The pharmacologic or clinical response to the administration of a drug combination different from that anticipated from the known effects of the two agents when given alone” Tatro DS (Ed.) Drug Interaction Facts. J.B. Lippincott Co. St. Louis 1992 Types of Drug Interactions Pharmacokinetic - What the body does with the drug - One drug alters the concentration of another by altering its absorption, distribution, metabolism, or excretion - Usually (but not always) mediated by cytochrome P450 (CYP) - Can depend on absorption (GI motility, pH) Distrubution (transport proteins) Metabolism, (CYP450). Elimination(renal Kidney function) Pharmacodynamic drug interactions Synergistic combinations Phamacologic (drug) effect is greater than the summation of the 2 drugs sometimes beneficial and sometimes harmful Beneficial: aminoglycoside +penicillin cell wall breakdown by PCN Harmful: barbituates and alcohol alcohol enhances the effects of the barbituate Antagonistic combinations Pharmacologic effect is less than the summation fo the 2 drugs Beneficial: Naloxone(Narcan) in opiate overdose Harmful zidovudine + stavudine used in treating HIV one makes the other ineffective Additivity effect equals the summation of the 2 drugs Beneficial: Asprin + acetaminophen both work together to relieve pain better Harmful: neutropenia with zidovudine + ganciclovir (HIV drugs) blood toxicity Drug interactions *Drug interactions can occur when one drug inhibits or induces a P-450 that acts on another drug. An example is nicotine, a drug contained in tobacco, and known to induce P-450s. *Individuals with liver disease (ie: cirrhosis) may have insufficient levels of P450 enzymes. As a result, the concentration of drugs metabolized by these enzymes remains high and can build up to toxic levels in the bloodstream *certain medications and foods, such as grapefruit juice, can inactivate or lessen the metabolic activity of P-450s. *The metabolic rate can vary significantly from person to person, and drug dosages that work quickly and effectively in one individual may not work well for another. Factors such as genetics, environment, nutrition, and age also influence drug metabolism; infants and elderly patients may have a reduced capacity to metabolize certain drugs, and may require adjustments in Common drug interactions What are some common drug interactions that you can think of? Are they harmful or beneficial? Example What about illegal drugs? How do you know whats really in them if they are not controlled by the FDA? How do you know the therapeutic dose or the toxic dose? Example Opiates. Legal vs illegal Suicide vs accidental overdose Tylenol (acetaminophen) Example of a common medication that when taken as prescribed is very safe for most people but if taken in higher doses or in combination with things is lethal…… Tylenol (acetaminophen) can purchase by itself or it is contained in some prescription medications and other over the counter medications. Easy to OD Why? The liver breaks down most of the drug into safe components that can be removed from the body in the urine. However, a small amount of Tylenol is expected to be metabolized into a harmful by-product called NAPQI (which stands for N-acetyl-pbenzoquinoneimine). When Tylenol is taken in recommended doses, your body can quickly remove this toxic by-product in the urine. However, when the liver needs to suddenly metabolize overdose levels of Tylenol, too much of the toxic NAPQI is made and it starts to harm the main cells of the liver Medication combinations Today, more than 600 over the counter and prescription medications contain tylenol (acetaminophen) Some examples Alka-Seltzer Plus Liquid Gels Anacin Formula 44 cough syrup Butalbital Midol Edocet Cepacol nyquil Hycotab Contac Robitussin Coricidin Sudafed Hydrocodone Dayquil Midol Fioricet Ibuprofen Advil, Motrin (ibuprofen) alternative pain, fever reducer. NSAIDS (non steroidal anti inflammatory drug) rarely affect the liver. Unlike acetaminophen (Tylenol) most NSAIDs are absorbed completely and have negligible first-pass hepatic (liver) metabolism. In other words, the way NSAIDS are metabolized makes liver toxicity (hepatotoxicity) very rare. It’s about the kidneys: NSAIDs have important adverse effects on the kidney that you should know about. Here is the science behind the problem. Ibuprofen and other NSAIDs inhibit prostaglandins, and that can cause a problem because prostaglandins dilate blood vessels leading to the kidneys. Inhibiting prostaglandins may lead to kidney ischemia (dead tissue from decreased blood flow) and thus acute kidney injury. Dr. orders in school PERMISSION TO ADMINISTER MEDICATION AT SCHOOL Student: _______________________ __________Birthdate: __ _________Grade: _____ PARENT/GUARDIAN SECTION * SECCION DE PADRE/GUARDIAN I request that the school nurse, or designated staff member, administer the medication prescribed below, in accordance with the healthcare provider instructions. I give my permission for the following medication information to be shared with school staff on a “need to know” basis. HEALTH CARE PROVIDER SECTION Diagnosis for which medication is to be given during school hours:_______________________________ Is this condition Life Threatening? Yes / No *911 will be called whenever the student’s condition deteriorates _ ________ __________ ___po_______ Beginning of school after breakfast_ Name of medication (1 per form): Dosage: Possible Method of administration: Time o side effects:____________________________________________Emergency Action:____________________________or 911 When the parent requests may we give the morning dose of the above HCP Signature medication when forgotten at home? Yes / No Date FDA Food and Drug Administration FDA is responsible for protecting the public health by assuring the safety, efficacy and security of human and veterinary drugs, biological products, medical devices, our nation's food supply, cosmetics, and products that emit radiation. FDA is also responsible for advancing the public health by helping to speed innovations that make medicines more effective, safer, and more affordable and by helping the public get the accurate, science-based information they need to use medicines and foods to maintain and improve their health.