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Transcript
Ch 38: Introduction to Equivalence O Many different types of equivalence O Two drugs may be equivalent in one category, but not in another © 2013-2015 Types of Equivalence O Pharmaceutical Equivalents O same active ingredients O same strength O same dosage form O same route of administration O may have different inactive ingredients O may have different release mechanisms © 2013-2015 Types of Equivalence O Pharmaceutical Equivalent Example O Procardia XL vs. Adalat CC O All the similarities required but uses a different release mechanism © 2013-2015 Types of Equivalence O Pharmaceutical Alternatives O same drug moiety O anything else may be different O different salts or esters O different strength O different dosage forms Pharmaceutical Alternatives are substitutes for treating a specific condition, but they are NOT equivalent © 2013-2015 Bioavailability O Bioavailability is a measure of the rate and extent to which the active ingredient is absorbed from a dosage form O For drugs that are not absorbed into the blood stream, bioavailability is a measurement of the rate and extent to which the active ingredient becomes available at the intended site of action © 2013-2015 Types of Equivalence O Bioequivalent Drug Products O must be Pharmaceutical Equivalents or Pharmaceutical Alternatives, AND O must have comparable bioavailability O The Rate and Extent of Absorption must have no significant differences © 2013-2015 Types of Equivalence O Therapeutic Equivalents O must be pharmaceutical equivalents, AND O must be bioequivalent O With generic drug product selection and substitution in the pharmacy we are concerned with therapeutic equivalents © 2013-2015 The Bioequivalence Study O Used to determine if a second drug is bioequivalent to a standard product O Usual study includes 24 to 36 normal healthy subjects O A single dose of the standard drug is given and blood levels are measured O Then the test is repeated using the applicant drug product © 2013-2015 The Bioequivalence Study O Two drugs are considered to be bioequivalent if the results of the two samples vary by no more than -20% /+25% O Applicant drugs that test within less than 20% of the standard to 25% over the standard are considered to be bioequivalent O For most drugs, that difference is considered to be clinically insignificant © 2013-2015 Therapeutic Equivalence Rating O In an effort to make order of bioequivalence studies, the FDA has assumed the responsibility of maintaining a reference of the results O The “Orange Book” O Approved Drug Products with Therapeutic Equivalence Evaluations O Uses a series of two letters to indicate equivalence © 2013-2015 Bioequivalence Ratings Rating AA AB AN AT Definition Drugs which are considered NOT to have potential bioavailability problems – No testing Drugs that have been shown to be bioequivalent through testing Equivalent solutions and powders for aerosolization Equivalent topical products © 2013-2015 Bioequivalence Ratings Rating BC BD BN BT Definition Non-equivalence due to PRESUMED difference in extended release dosage forms – No Testing Drugs that have been shown NOT to be bioequivalent through testing Non-Equivalent solutions and powders for aerosolization Non-Equivalent topical products © 2013-2015 DESI Drugs O Remember that effectiveness was not a requirement of drug approval until the 1962 Kefauver- Harris Amendment O The Drug Efficacy Study Implementation (DESI) looked at 3,000 drugs approved between 1938 and 1962 and tested them for effectiveness O Classified drugs according to their effectiveness © 2013-2015 DESI Drugs O When we speak of a “DESI” drug in the pharmacy, we are referring to drugs which were found to be either ineffective or less than effective under this study O Insurance plans usually refuse to reimburse for DESI drugs, for obvious reasons © 2013-2015 Ch 39: Organ System Review O Skin O Circulatory System O Gastro-Intestinal System O Respiratory System O Excretory System © 2013-2015 The Skin O Largest organ of the body O Protects us from temperature and bacteria O Composed of several layers O Epidermis O Dermis O Subcutaneous Layer © 2013-2015 The Circulatory System O Carries drugs throughout the O O O O body Heart Arteries Veins Capillaries © 2013-2015 Parts of Blood O Red Blood Cells O carry gases (O2 / CO2) O White Blood Cells O Clean up crew of the body O Platelets O Used in clotting process O Bunch together to form clots © 2013-2015 Anatomy of the Heart O Right side – not oxygenated O Left side – oxygenated © 2013-2015 Gastro-Intestinal System O Converts food O Absorbs nutrients O Replenishes water O Removes waste O Parenteral vs. Enternal © 2013-2015 Nervous System O Central Nervous System O Brain and spinal cord O Peripheral Nervous System O Outward from the spinal cord O Somatic nerves O Sensory info in O Out to skeletal muscle O Autonomic nerves O To smooth muscle © 2013-2015 Respiratory System O Structures O Mechanics O Gas Exchange © 2013-2015 The Excretory System O Removes Waste Products O Regulates Fluid Retention © 2013-2015 The Kidney O Controls the amount of fluid retained in the body O Removal of waste products © 2013-2015 Ch 40: Disease States O Pathophysiology O the study of the effect of a disease on normal body functions O “Treatment” vs. “Cure” O a treatment causes the body function to normalize while the underlying disease is still present O a cure means the underlying disease is no longer present © 2013-2015 Risk Factors O Many disease states are found to be more common in individuals with certain: O O O O habits conditions genetic make-up, or traits O These are called “Risk Factors” for the disease © 2013-2015 Risk Factors O Risk Factors may be controllable or uncontrollable O What about: - weight (obesity) ? - gender ? - race ? - high cholesterol ? - age ? - smoking ? - high blood pressure ? - lack of exercise ? © 2013-2015 Chronic Disease States & Associated Risk Factors O Two-thirds of all deaths in the United States are caused by five diseases: O Heart Disease O Cancer O Stroke O Chronic Obstructive Pulmonary Disease O Diabetes © 2013-2015 Coronary Artery Disease (CAD) O Affects the arteries supplying the heart with oxygenated blood O CAD is caused by a constriction of these vessels by deposits of fat, cholesterol, and plaques O Results in a decrease in the supply of oxygen and nutrients to the muscle tissues of the heart © 2013-2015 Angina Pectoris O One of the major signs of reduced oxygen delivery O Pain that is predominantly located in the chest and/or arm O If the oxygen flow is not resumed in a short period of time, death of heart tissue can occur (aka. myocardial infarction) © 2013-2015 Stroke O Since the risk factors are essentially the same, CAD and stroke are often spoken of together O Strokes are also caused by an inadequate supply of oxygen – this time, to the brain O Can be caused by a blockage (~80%) or the rupture of a blood vessel (~20%) © 2013-2015 Risk Factors for CAD & Stroke O Major Risk Factors O High blood pressure O High blood cholesterol O Other Risk Factors O Diabetes O Tobacco use O Excess weight O Lack of exercise © 2013-2015 Chronic Obstructive Pulmonary Disease (COPD) O Covers multiple disease processes: O chronic bronchitis O chronic obstructive bronchitis O emphysema O All can cause progressive and often irreversible damage to the lungs We will concentrate on emphysema © 2013-2015 Emphysema O Irreversible destruction of the alveoli in the lungs O Causes a loss of lung efficiency and a decrease in the gas exchange O Eventually causes gasping and straining for every breathe O Leaves the patient at risk for other diseases O Asthma O Pneumonia O Bronchitis © 2013-2015 Risk Factor for Emphysema 80% is caused by Cigarette Smoking! The only hope is to quit smoking before the damage becomes too great © 2013-2015 Diabetes O Affects the proper use and storage of glucose in the body O Often develops without any tell-tale signs O There are two types of diabetes © 2013-2015 Normal Glucose Reaction O Increased blood glucose level (after a meal) O Body signals special cells in the pancreas O Insulin is released into the bloodstream O Insulin signals the cells to open special channels in the cell wall for glucose entry O Lowers blood glucose level to the normal level © 2013-2015 Type 1 Diabetes (~10%) O In Type 1 diabetes, little or no insulin is produced by the cells in the pancreas O When the body triggers insulin release, there is not enough for the desired effect O Treatment – inject additional insulin into the body © 2013-2015 Type 2 Diabetes (~90%) O With Type 2 diabetes, either there is not enough insulin produced or the receptors where the insulin works are not functioning adequately and the glucose channel in the cells do not get opened O Usual Treatment – oral medications that stimulate additional release of insulin or increase receptor sensitivity © 2013-2015 Risk Factors for Diabetes O Family History O higher if close family member has diabetes O Weight O about 80% of Type 2 are over weight O Inactivity O the less you exercise, the greater the risk O Age O after 45 y/o the risk of Type 2 increases greatly O Race O Type 1 is higher in Caucasian, Europeans O Type 2 is higher in African Americans, Hispanics, and American Indians © 2013-2015 Ch 41: Introduction to Pharmacology O In this session we will look at how drugs exert their effect on the body and some of the most common drug classes used today O While it is impossible to cover a full semester pharmacology class in this program, we will highlight the important facts on these medications O First, some definitions… © 2013-2015 “Pharmacology” O The fancy definition O the study of substances that interact with living systems through a chemical process, by binding to regulatory molecules which activate or inhibit a normal body process O The short definition O the study of the drug’s actions on the body © 2013-2015 “Toxicology” O The branch of pharmacology that deals with the undesirable effects of drugs © 2013-2015 “Drug” O Chemicals that are administered to achieve a beneficial therapeutic effect on some process within the patient, or for their toxic effect on a parasite within the patient © 2013-2015 “Receptor Site” O The spot where the drug binds to have it’s effect © 2013-2015 “Bond” O The manner in which two chemicals adhere to each other O May be very weak to very strong © 2013-2015 “Agonist” O A drug that causes a biological action to occur © 2013-2015 “Antagonist” O A drug that blocks a naturally occurring body chemical from reaching its receptor site O It stops the natural chemical from initiating a body response © 2013-2015 “Dose” O The amount of drug administered © 2013-2015 “Potency” O Concerns the amount of drug necessary to produce the desired effect O The more drug needed, the lower the potency and vice versa Relative Potency © 2013-2015 “Maximal Efficacy” O The maximum response possible from a drug O A point where giving more drug does not increase the desired effect further © 2013-2015 How Drugs Work O Physical Properties of the Drug O Bonding to Receptors O Drug Action at the Receptors O Dosage and Potency © 2013-2015 Physical Properties of the Drug In order to be biologically active, a drug must have: O the right chemical structure and size O the correct chemical bond activity O the correct shape THINK OF THE DRUG AND RECEPTOR AS A LOCK AND KEY © 2013-2015 Correct Chemical Structure & Size O The drug must have a part of itself that fits into the receptor site exactly O The rest of the drug molecule can have effects on how easily the drug can bond with the receptor © 2013-2015 Correct Bonding Properties O Must bond in the right manner O not too strong or too weak of a bond O Covalent Bonds O strong bonds O may even be irreversible O Electrostatic Bonds O can be very weak as in van der Waal’s forces O or stronger as in ionic bonds © 2013-2015 Drug Actions at the Receptor O Agonist O “turns on” the action at the receptor O causes a body action to occur O Antagonist O “turns off” the action at the receptor O stops a normal body chemical from binding to the receptor O can be “competitive” or “non-competitive” © 2013-2015 Competitive Antagonists O The effect is temporary and lasts only as long as the drug is bound to the receptor O The concentration of the drug is a major determinant of the action of the drug O A good example is the child’s game “musical chairs” © 2013-2015 Non-Competitive Antagonists O aka, Irreversible Antagonists O The drug binds permanently to the receptor O The action continues even after the blood levels of drug are insignificant O The effect will last until the cell makes a new receptor site © 2013-2015 Pharmacological Classes of Medication O Drugs can be classified by where their effects take place, by their mechanism or action, or by their chemical structure O Most times their chemical structure will give us clues as to their location and mechanism of action © 2013-2015 Ch 42: Drugs Used in Cardiac Conditions O Hypertension O Angina O Heart Failure O Hyperlipidemia O Blood Clotting Disorders © 2013-2015 Hypertension Overview O Blood pressure readings are a series of two numbers (ie, 120/80) O Systolic blood pressure O the highest pressure achieved O occurs when the heart finishes the ventricular contraction O Diastolic blood pressure O the lowest pressure O occurs right before the heart begins its contraction © 2013-2015 Hypertension Overview O Remember blood pressure is a dynamic value O You can not make decisions based on a single blood pressure reading O Blood pressure treatment should be initiated or modified in response to a series of blood pressure checks © 2013-2015 Complications of Hypertension O Stroke O Heart disease O Heart attack O Kidney damage O Other problems Symptoms often present themselves only after damage has occurred, leading to hypertension being called the “Silent Killer” © 2013-2015 How can we treat HTN? O Think in terms of plumbing O lessen the force of the “pump” O lower the amount of fluid in the system O increase the diameter of the “pipes” © 2013-2015 Diuretics O Mechanism of Action (MOA) – Decrease re- absorption of sodium and potassium causing more fluid to be eliminated by the kidneys. Initially they lower the volume of fluid in the blood vessels. Over the long term other mechanisms are involved. O Three main types: O thiazides O loop O potassium sparing O Major side effect – potassium depletion © 2013-2015 Thiazide Diuretics O Place of Action – distal tubule of the kidney O Common thiazide diuretics O hydrochlorothiazide O indapamide O metolazone O chlorthalidone © 2013-2015 Loop Diuretics O Place of Action – Loop of Henley in the kidney O Common loop diuretics O furosemide O bumetanide O torsemide LOOP SPECIFIC SIDE EFFECT – Ototoxicity at high doses © 2013-2015 Beta Adrenergic Blockers O MOA – Decrease the rate and force of the heartbeat by blocking the messages the body sends to the heart O Problem with Beta Blockers – there are beta receptors in other areas of the body O Who should not receive beta blockers? O Asthmatics – blocks beta receptors in the lungs O Diabetics - blocks the tell-tale signs of hypoglycemia © 2013-2015 Beta Adrenergic Blockers O Non-specific O propranolol O nadolol O pindolol O Beta 1 specific O atenolol O metoprolol O bisoprolol O sotalol Note the “–olol” suffix © 2013-2015 The Renin-Angiotensin System O One of the body’s systems that constricts blood vessels when activated Angiotensin I Angiotensin II Receptor Binding Angiotensin I is not a potent vasoconstrictor O Angiotensin I is converted to angiotensin II by Angiotensin Converting Enzyme (ACE) Angiotensin II IS a potent vasoconstrictor if allowed to bind to it’s receptors © 2013-2015 ACE Iinhibitors Angiotensin IX Angiotensin II Receptor Binding O Blocks the conversion of angiotensin I angiotensin II O Major side effect – cough O Who should never receive ACE Inhibitors? O Pregnant women ACE inhibitors cause serious injury or death to the fetus © 2013-2015 ACE Inhibitors O Common ACE inhibitors O lisinopril O captopril O enalapril O ramipril O fosinopril O benazepril Note the “–pril” suffix © 2013-2015 Angiotensin Receptor Blockers X Angiotensin I Angiotensin II Receptor Binding O Block the binding of Angiotensin II to its receptor O Can be denoted both as ARB (Angiotensin Receptor Blocker) or ARA (Angiotensin Receptor Antagonist) O No side effect of cough O Same contraindication with pregnant women © 2013-2015 Common ARB’s O Common ARA’s O losartan O valsartan O candesartan O eprosartan O telmisartan O irbesartan Note the “–sartan” suffix © 2013-2015 Calcium Channel Blockers O In order for muscle fibers to contract, there must be a flow of calcium into and out of the cells O There are special “channels” where this flow occurs O Calcium channel blockers block these channels © 2013-2015 Calcium Channel Blockers O MOA #1 – Blocks the flow of calcium into vascular smooth muscle (blood vessels) O MOA #2 – Decreases the force of the heartbeat by decreasing the transmission of electrical impulses on the heart muscle Different calcium channel blockers vary in their ability to accomplish MOA #1 and #2 © 2013-2015 Calcium Channel Blockers O Common Calcium Channel Blockers O O O O O O O verapamil diltiazem nifedipine amlodipine isradipine felodipine nicardipine Note the “–dipine” suffix on several © 2013-2015 Alpha Adrenergic Blockers O MOA – Block alpha receptors on vascular smooth muscle that induce vasoconstriction O Concern with alpha blocker – Prazosin First Dose Syncope © 2013-2015 Alpha Adrenergic Blockers O Common Alpha Blockers O prazosin O terazosin O doxazosin Note the “–azosin” suffix © 2013-2015 Angina O Chest pain- “crushing feeling on the chest” caused by lack of oxygen to the heart muscle O Caused by a disruption in the blood flow of the heart O Treatment efforts directed at restoring the blood flow and accompanying oxygen O Three main classes of anti-anginal drugs O nitrates O beta blockers O calcium channel blockers © 2013-2015 Nitrates O Available in topical patches, ointment, oral tablets, and sublingual tablets O Sublingual NTG is used to treat acute chest pain O Other forms are used to prevent chest pain O Important considerations with sublingual NTG: O Should be kept in their glass bottle or an approved container – never in prescription bottles O Should be kept out of excessive heat O Dissolved under the tongue O Usual dose is 1 at onset of pain, then one every 5 minutes if pain persists. If no relief after 3 tabs © 2013-2015 GET TO ER! Heart Failure O Condition where the heart can no longer pump a sufficient amount of blood to the body O Commonly called Congestive Heart Failure (CHF) O Inotropic Medications are used in conjunction with some of the previous drug classes we have already covered O Common inotropic drugs: O digoxin O dobutamine © 2013-2015 Hyperlipidemia O Condition of abnormally high cholesterol and/or triglyceride levels in the body O Aim is to decrease the lipids in the bloodstream O Common Drugs Classes O bile acid sequestrants O niacin O fibric acid derivatives O HMG-Co A reductase inhibitors (statins) © 2013-2015 Blood Clotting Disorders O Clots may form in blood vessels throughout the body, depleting tissues of necessary oxygen and nutrients O Clots may even break off from their original location and travel to a vessel that they can no longer pass through (stroke or pulmonary embolism) O Anticoagulants work in two ways O Work in the liver to prevent the formation of clotting factors that are necessary in the formation of the clot O By directly affecting clot formation and expansion O Common Anticoagulant Drugs O heparin O warfarin O rivaroxban O apixaban O dabigatran © 2013-2015 Questions? © 2013-2015 Assignments Due Next Week O Class Eight Homework Worksheet O Study Drug Flash Cards # 141-160 NEXT WEEK IS OUR THIRD SECTION TEST! Covers Chapters 33 thru 39 NO MATH QUESTIONS © 2013-2015 Math Test Number Two 15 Questions 45 Minute Time Limit No Talking Please! © 2013-2015