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Chapter 10 Pharmacology Health Care Science Technology Copyright © The McGraw-Hill Companies, Inc. Objectives Describe where drugs come from. Discuss the mechanism of action of drugs. Explain how drugs are grouped into therapeutic classes. 2 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Objectives (cont.) Compare the advantages and disadvantages of different routes of drug administration. Describe the four major processes of pharmacokinetics. 3 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Objectives (cont.) Convert units within and among the metric, household, and avoirdupois systems. Calculate basic medication dosages. 4 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Introduction to Pharmacology 10-1 Sources of Drugs Pharmacotherapeutics 5 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Sources of Drugs Natural Sources – – 6 Pharmacognosy is the study of drugs made from natural sources, such as plants and animals. Plants were the main source of medicine until the early 1900s, when Sir F. G. Banting and Charles Herbert Best extracted insulin from a pancreas and tested it on diabetic dogs. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Sources of Drugs (cont.) Natural Sources (cont.) – 7 Problems associated with naturally occurring drugs: Some are broken down very quickly by the body. Some are poorly absorbed into the bloodstream. Isolating a drug from a plant or animal can be slow, expensive, and may result in harmful impurities in the drug. Naturally occurring products can be extremely scarce. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Sources of Drugs (cont.) Microscopic Organisms – 8 Penicillin, isolated by Sir Alexander Fleming in 1928, was one of the first drugs that did not come from a plant or animal. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Sources of Drugs (cont.) Synthetics and Bioengineering – – – 9 Medicinal chemistry modifies natural products by producing them synthetically or by creating new products. Aspirin, synthetically produced today, was once an extract of willow bark. Insulin was the first drug to be produced from genetically altered bacteria. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Sources of Drugs (cont.) Natural Sources (cont.) – Genetically modified E-coli used to make insulin Plasmid containing human insulin gene Bacterial Chromosome 10 Cell A Cell B Copyright © The McGraw-Hill Companies, Inc. Plasmid has been inserted into the bacterial cell Chapter 10 Pharmacotherapeutics 11 Examines the mechanism of action (MOA) of drugs. Describes the effects produced by a drug. Determines what dose of a drug is needed to produce a desired effect. Determines what dose of a drug produces toxic effects. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) 12 Mechanisms of Action (MOA) – Drugs with the same MOA are said to belong to the same therapeutic class. – Binding occurs when a drug combines with a chemical in the body. – Four common MOAs. – MOA operates on a “lock and key” principle. The drug is considered the key and the body chemical the lock. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) Mechanisms of Action (cont.) – Binding to and Stimulating a Receptor in the Body Receptors – proteins found in cells. Click for Picture 13 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) Mechanisms of Action (cont.) – Binding to and Blocking a Receptor in the Body Some drugs, called antagonists or blockers, bind to a receptor without causing a response, thus preventing the naturally occurring key from binding. Click for Picture 15 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) Mechanisms of Action (cont.) – Inhibiting an Enzyme Enzyme inhibitors increase or decrease the concentration of an enzyme. Click for Picture 17 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) Mechanisms of Action (cont.) – Decreasing the Movement of a Chemical Across a Cell Membrane Pumps and channels are used by cell membranes to control the movement of chemicals into and out of a cell. Pumps can be inhibited and channels can be blocked by this type of drug. Click for Picture 19 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) A side effect is any effect produced by a drug that is not the desired effect. – 21 Local Side Effects Occur before a drug is absorbed into the bloodstream. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacotherapeutics (cont.) – 22 Systemic Side Effects Take place after being absorbed into the bloodstream. May take the form of an allergic reaction, since drugs are not a “natural” part of our body. Most occur because the drug affects cells other than the target cells. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Section 10-1 Apply Your Knowledge Where do drugs come from? Answer: 1. Natural sources such as plants and animals. 2. Microscopic organisms such as bacteria, fungi, and molds. 3. Synthetics and bioengineering. 23 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Classes of Drugs and Routes of Administration 10-2 Therapeutic Classes of Drugs Routes of Administration 24 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs 25 Drugs in a therapeutic class produce their effect in the same way. Examples are listed on the following slides. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Angiotensin Converting Enzyme Inhibitors – Angiotensin is a naturally occurring protein in the body. An enzyme called angiotension converting enzyme (ACE) activates angiotensin, which, when overactive, causes high blood pressure, or hypertension. – ACE inhibitors reduce the production of angiotensin. – Representative drugs: Accupril®, Lotensin®, Prinivil®, Vasotec®, and Zestril®. – Common side effects include headache and dizziness. 26 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Beta-1 Blockers – Bind to beta-1 receptors without stimulating them, preventing epinephrine (adrenalin) and norepinephrine from binding. – Representative drugs: Lopressor®, Tenormin®, Toprol®. – Indications: hypertension, tachycardia or rapid heartbeat. – Common side effects: dizziness, drowsiness. 27 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Beta-2 Agonists – These drugs bind to beta-2 receptors on the smooth muscle cells of the bronchioles, causing dilation. Representative drugs: Ventolin®, Proventil®, Serevent®, Alupent®, Brethine®. – Indications: asthma, emphysema. – Common side effects: tremors, increased heart rate, and insomnia. 28 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Antihistamines – Antihistamines bind to histamine receptors, without stimulating them. – Representative drugs: Allegra®, Benadryl®, Claritin®, Zyrtec®. – Indications: itching, nasal congestion, seasonal allergies such as hay fever. – Common side effects: dry mouth and drowsiness. 29 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) H2 Antagonists – Bind to H2 receptors, found only in the stomach, to decrease the amount of hydrochloric acid produced. – Representative drugs: Tagamet®, Pepcid®, Zantac®. – Indications: gastroesophageal reflux disorder, gastric ulcers, duodenal ulcers. – Common side effects: diarrhea, headache. 30 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Proton Pump Inhibitors – Drugs that turn off the proton pumps in the stomach, which reduces stomach acid. – Representative drugs: Prilosec®. – Indications: gastroesophageal reflux disorder, gastric ulcers, duodenal ulcers. – Common side effects: diarrhea, headache. 31 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Narcotic Analgesics – Drugs that bind to and stimulate the endorphin receptors in the spine which inhibit nerve cells that carry pain to the brain. – Representative drugs: morphine, codeine, Demerol®, Vicodin®, Percodan®. – Indications: severe pain. – Common side effects: drowsiness, slow and shallow breathing, constipation. 32 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Nonsteroidal Anti-inflammatory Drugs – Nonsteroidal anti-inflammatory drugs (NSAIDS) inhibit the enzyme prostaglandin synthase, which makes prostaglandins. – Representative drugs: aspirin, Motrin®, Advil®, Relafen®, Naprosyn®, Aleve®. – Indications: mild to moderate pain, inflammation, fever. – Common side effects: stomach irritation. 33 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Reverse Transcriptase Inhibitors – – – – 34 Inhibit the activity of the enzyme reverse transcriptase, which is needed to convert RNA to DNA. Representative drugs: AZT, Combivir®, Sustiva®, Retrovir®. Indications: HIV infection. Common side effects: anemia, fever, rash, headache, lack of energy, nausea, vomiting, diarrhea, stomach pain, cough, shortness of breath, sore throat. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Therapeutic Classes of Drugs (cont.) Statins – Drugs that inhibit the enzyme HMG CoA reductase. – Representative drugs: Lipitor®, Pravachol®, Zocor®. – Common side effects: nausea, vomiting, diarrhea, and liver damage. 35 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Routes of Administration Routes of Administration (ROA) – the different ways used to get a drug into the tissues of the body. 36 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Routes of Administration (cont.) Oral Administration – – 37 The most common route. Client swallows a tablet, capsule, or liquid. Usually requires 30 to 60 minutes before producing an effect, or onset of action. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Routes of Administration (cont.) Parenteral Administration – all forms of administration, other than oral. – Metered-Dose Inhaler Delivers medications directly to the lungs. Rapid action. Minimal systemic side effects. 38 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Routes of Administration (cont.) – 39 Transdermal Patch – one of the most consistent and convenient dosage forms. Remove and discard old patch. Select a site for new patch. Apply the patch. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Routes of Administration (cont.) – 40 Injections – used when a rapid effect is needed. Subcutaneous (SC) injection – most frequently given in the upper arm, front of thigh, or abdomen. Intramuscular (IM) injection – normally given into relatively large muscles of the shoulder, buttocks, or outer portions of the thigh. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Section 10-2 Apply Your Knowledge What is the largest volume that can be given with an SC injection? Answer: The largest volume is 1 milliliter (mL). 41 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacokinetics and Dosages 10-3 42 Pharmacokinetics Dosages Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacokinetics Pharmacokinetics is the study of the four processes that affect the plasma concentration of drugs. 43 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacokinetics (cont.) Absorption – the process by which a drug enters the plasma. – 44 Oral medications are dissolved in the stomach. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacokinetics (cont.) Distribution – where the drug goes after entering the plasma. – 45 Some of the drug binds to the proteins in the plasma; some diffuses into other tissues. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Pharmacokinetics (cont.) 46 Transformation – chemical changes in a drug that occur after it has been absorbed into the body. Elimination – the process that removes a drug from the body. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Dosages Dosages are usually based on the weight of an individual. 47 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Dosages (cont.) Effects of Individual Differences on Maintenance Doses – 48 Age, body fat, and diseases that affect the liver and kidneys may require altering the dosage of a drug. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Section 10-3 Apply Your Knowledge List the 4 processes of pharmacokinetics. Answer: 1. Absorption 2. Distribution 3. Transformation 4. Elimination 49 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Systems of Measure 10-4 50 The Metric System Other Systems of Measure Basic Dosage Calculations Copyright © The McGraw-Hill Companies, Inc. Chapter 10 The Metric System The metric system is the most widely used measurement system in pharmacy. – – – 51 Dosage of a drug is usually measured in milligrams (mg). Liquid drugs are often measured in milliliters (mL). Client’s body weight may be measured in kilograms (kg). Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Other Systems of Measure 52 Household system – uses teaspoon and tablespoon. Avoirdupois system – uses measurements such as fluid ounce and pound. Apothecary system – seldom used, it includes terms such as minim and grain. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Other Systems of Measure (cont.) 53 Converting from one system to another with factors: – 1 kg = 2.2 lb – 1 fl oz = 30 mL – 1 tsp = 5 mL Example: 25 kg = ? lb 25 kg = 1 kg ? lb 2.2 lb 25 X 2.2 = 1 X ? Copyright © The McGraw-Hill Companies, Inc. ? = 55 lb Chapter 10 Basic Dosage Calculations A physician’s order must be obtained to administer a dose. It must include: – – – – 54 The name of the drug. The amount of drug prescribed. The frequency with which it should be administered. The route of administration. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Basic Dosage Calculations (cont.) A simple way to calculate doses is to use the following proportion: Known unit on hand Known dosage form 55 _______Dose ordered______ Unknown amount to be given Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Basic Dosage Calculations (cont.) – – – – 56 Known unit on hand – the amount of grams or milligrams in a particular drug for which the dosage is known. Known dosage form – a typical amount of medicine for which you are given the gram or milligram equivalents. Dose ordered – the amount of grams or milligrams ordered. Unknown amount to be given – what you are trying to determine; the amount of medicine to be given. Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Section 10-4 Apply Your Knowledge #1 Convert 25 grams to milligrams. Answer: 1. Add a decimal point to the measurement: 25. g 2. Add 3 zeroes so you can move the decimal point three places to the right: 25.000 g 3. Move the decimal point to the right three places: 25,000 4. Change the unit: 25,000 mg 57 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Section 10-4 Apply Your Knowledge #2 Calculate the dose to give for 500 mg Augmentin®. Answer: 20 mL 58 Copyright © The McGraw-Hill Companies, Inc. Chapter 10 Chapter 10 Credits Slide 28 Slide 30 Slide 31 Slide 32 Slide 33 Slide 38 Slide 39 Slide 58 59 Glaxo Wellcome, Inc. Glaxo Wellcome, Inc. Astra Roxane McNeil-PPC, Inc. Aaron Haupt Medical Images SmithKline Beecham Copyright © The McGraw-Hill Companies, Inc. Chapter 10