PHA068 SAS-2.pdf

COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: ________...

COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ Lesson title: Review of Drug Delivery System and Routes of Materials: Administration; Pharmacokinetic models Pen & SAS Lesson Objectives: At the end of the lesson, you should be able to: References: 1. Explain drug delivery system Shargel, Leon. Applied 2. Describe the different routes of administration Biopharmaceutics and 3. Understand the vehicles of drug delivery systems Pharmacokinetics latest Edition, 4. Discuss the different pharmacokinetic models Boston: McGraw Hill, latest edition Rowland, M. Clinical pharmacokinetics and pharmacodynamics: concepts and applications (latest edition.). Philadelphia: Lippincott Williams & Wilkins Rosenbaum, S. Basic pharmacokinetics and pharmacodynamics: concepts and applications (latest edition). Philadelphia: Lippincott Williams & Wilkins. Productivity tip: Make your own flashcards by putting all the terms on one side of a card and the entire paragraph on the flip side. Test yourself using the flash cards. Repeat your process until every term seems completely familiar to you. A. LESSON PREVIEW 1) Introduction (10 mins) Systemic absorption of a drug depends on its physicochemical properties, the nature of the dosage form on which it is included and the anatomical and physiological characteristics of the site of absorption. These considerations are important on the biopharmaceutical production and evaluation of drugs: the design of the dosage forms requires a deep knowledge of the physiological and pathological factors that affect drug absorption for guarantying the therapeutic efficacy and to avoid possible drug-drug and drug- nutrient interactions. 2) Activity 1: What I Know Chart, part 1 (5 mins) What do you Know about the topic of the day? Answer the questions given and write your answers on the first column. Leave the third column blank for now. What I Know Questions: What I Learned (Activity 4) 1. Define Drug delivery system This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ 2. Describe enteral route of administration of drugs. 3. What are the routes of administration subject to first pass metabolism? B. MAIN LESSON Content Notes (60 mins) I. Drug delivery system  is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. For the treatment of human diseases, nasal and pulmonary routes of drug delivery are gaining increasing importance. These routes provide promising alternatives to parenteral drug delivery particularly for peptide and protein therapeutics. For this purpose, several drug delivery systems have been formulated and are being investigated for nasal and pulmonary delivery. Routes of administration 1. Enteral via gastrointestinal tract a. Oral  By far the most common route. The passage of drug from the gut into the blood is influenced by biologic and physicochemical factors, and by the dosage form. For most drugs, two- to five-fold differences in the rate or extent of gastrointestinal absorption can occur, depending on the dosage form. These two characteristics, rate and completeness of absorption, comprise bioavailability. Generally, the bioavailability of oral drugs follows the order: solution > suspension > capsule > tablet > coated tablet. o Tablets o Capsules o Syrup o Suspension o Emulsion *have first pass effect This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ b. Sublingual/ Buccal  Certain drugs are best given beneath the tongue or retained in the cheek pouch and are absorbed from these regions into the local circulation. These vascular areas are ideal for lipid-soluble drugs that would be metabolized in the gut or liver, since the blood vessels in the mouth bypass the liver (do not undergo first pass liver metabolism), and drain directly into the systemic circulation. This route is usually reserved for nitrates and certain hormones. c. Rectal  Less first pass metabolism than oral (50%)  For vomiting and unconscious patients 2. Parenteral administration- injections a. Intradermal -into the dermis of the skin b. Subcutaneous- under the skin  Some drugs, notably insulin, are routinely administered SC. Drug absorption is generally slower SC than IM, due to poorer vascularity. Absorption can be facilitated by heat, massage or vasodilators. It can be slowed by coadministration of vasoconstrictors, a practice commonly used to prolong the local action of local anesthetics. As above, arm > thigh. c. Intramuscular- into muscles  Drugs may be injected into the arm (deltoid), thigh (vastus lateralis) or buttocks (gluteus maximus). Because of differences in vascularity, the rates of absorption differ, with arm > thigh > buttocks. Drug absorption may be slow and erratic. The volume of injection, osmolality of the solution, lipid solubility and degree of ionization influence absorption. It should not be assumed that the IM route is as reliable as the IV route. d. Intravenous- into veins  Used when a rapid clinical response is necessary, e.g., an acute asthmatic episode. This route allows one to achieve relatively precise drug concentrations in the plasma, since bioavailability is not a concern. Most drugs should be injected over 1-2 minutes in order to prevent the occurrence of very high drug concentrations in the injected vein, possibly causing adverse effects. Some drugs, particularly those with narrow therapeutic indices or short half-lives, are best administered as a slow IV infusion or drip. e. Intra-arterial-into arteries  Used in certain special situations, notably with anticancer drugs, in an effort to deliver a high concentration of drug to a particular tissue. Typically, the injected artery leads directly to the target organ. f. Intrathecal - into the cerebrospinal fluid  The blood-brain barrier limits the entry of many drugs into cerebrospinal fluid. Under some circumstances, usually life-threatening, antibiotics, antifungals and anticancer drugs are given via lumbar puncture and injection into the subarachnoid space. g. Intraperitoneal- into the peritoneal cativity 3. Others a. Topical application  Drugs are applied to the skin, ear, nose, vagina  Usually used to provide local action This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________  No first pass metabolism  Used for lipid soluble drugs  Topical drug administration for skin disorders minimizes systemic exposure. However, systemic absorption does occur and varies with the area, site, drug, and state of the skin. b. Inhalation  Volatile anesthetics, as well as many drugs which affect pulmonary function, are administered as aerosols. Other obvious examples include nicotine and tetrahydrocannabinol (THC), which are absorbed following inhalation of tobacco or marijuana smoke. The large alveolar area and blood supply lead to rapid absorption into the blood. Drugs administered via this route are not subject to first-pass liver metabolism c. Transdermal  This route of administration achieves systemic effects by application of drugs to the skin, usually via a transdermal patch  This route is most often used for the sustained delivery of drugs, such as the antianginal drug nitroglycerin, the antiemetic scopolamine, and nicotine transdermal patches, which are used to facilitate smoking cessation.  drug enters systemic circulation by zero order kinetics – a constant amount of drug enters the circulation per unit time First pass metabolism  Drugs taken orally are first taken to the liver (via portal circulation) where they metabolized before reaching to rest of the body via general circulation  The amount reaching blood circulation is less than the amount absorbed First pass metabolism occurs in: 1. Liver 2. Gut wall 3. GIT Lumen What is the result of first pass metabolism? 1. Low bioavailability of drugs=serum level of active drug that can produce action 2. Short duration of action of drugs Factors that influence the selection of the delivery route: 1. Drug physico-chemical properties like molecular weight of the drug, half-life and chemical stability. 2. Solubility in water (hydrophobic or hydrophilic) 3. Interactions of the drug in the body like membrane permeability, bacterial degradation, enzymatic degradation 4. Dosage size This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________  Vehicles of Drug Delivery Systems Ideally, the drug delivery vehicle must be non-toxic, non-immunogenic, biocompatible and biodegradable. It must also escape recognition of the host’s defense mechanisms. The various drug delivery vehicles used are: 1. Liposomes: These are the most common vehicles used for a targeted drug delivery system. They are non-toxic, non- immunogenic and non-hemolytic. Solid lipid nanoparticles are lipid-based, ligand-coated nanocarriers that store the target drugs in a hydrophobic or hydrophilic capsule. 2. Micelles and Dendrimers: These are polymer-based delivery vehicles used to transport and deliver drugs that have poor solubility. 3. Biodegradable Particles: These particles can exactly reach the target diseased site and deliver the drug in a controlled release manner. Biodegradable particles are commonly used for drugs delivered to cardiac tissue. 4. Artificial DNA Nanostructures: Those which are artificially designed out of nucleic acids like DNA can be used. Nanostructures can sense the environment of the site of release and deliver the drug to the target site. Such a structure releases a drug only in response to a stimulus. II. Pharmacokinetic models Drugs are in a dynamic state within the body as they move between tissues and fluids, bind with plasma or cellular components, or are metabolized. The biologic nature of drug distribution and disposition is complex, and drug events often happen simultaneously. Such factors must be considered when designing drug therapy regimens. The inherent and infinite complexity of these events requires the use of mathematical models and statistics to estimate drug dosing and to predict the time course of drug efficacy for a given dose. A model is a hypothesis using mathematical terms to describe quantitative relationships concisely The predictive capability of a model lies in the proper selection and development of mathematical function(s) that parameterizes the essential factors governing the kinetic process. The key parameters in a process are commonly estimated by fitting the model to the experimental data, known as variables. A pharmacokinetic parameter is a constant for the drug that is estimated from the experimental data. For example, estimated pharmacokinetic parameters such as k depend on the method of tissue sampling, the timing of the sample, drug analysis, and the predictive model selected. A pharmacokinetic function relates an independent variable to a dependent variable, often through the use of parameters. For example, a pharmacokinetic model may predict the drug concentration in the liver 1 hour after an oral administration of a 20-mg dose. The independent variable is the time and the dependent This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ variable is the drug concentration in the liver. Based on a set of time-versus-drug concentration data, a model equation is derived to predict the liver drug concentration with respect to time. In this case, the drug concentration depends on the time after the administration of the dose, where the time–concentration relationship is defined by a pharmacokinetic parameter, k, the elimination rate constant. Such mathematical models can be devised to simulate the rate processes of drug absorption, distribution, and elimination to describe and predict drug concentrations in the body as a function of time. Pharmacokinetic models are used to: 1. Predict plasma, tissue, and urine drug levels with any dosage regimen 2. Calculate the optimum dosage regimen for each patient individually 3. Estimate the possible accumulation of drugs and/or metabolites 4. Correlate drug concentrations with pharmacologic or toxicologic activity 5. Evaluate differences in the rate or extent of availability between formulations (bioequivalence) 6. Describe how changes in physiology or disease affect the absorption, distribution, or elimination of the drug 7. Explain drug interactions A. Compartment Models  To apply mathematical principles, a model of the body must be selected. A basic type of model used in pharmacokinetics is the compartmental model. Compartmental models are categorized by the number of compartments needed to describe the drug’s behavior in the body.  The compartments do not represent a specific tissue or fluid but may represent a group of similar tissues or fluids. These models can be used to predict the time course of drug concentrations in the body Simple compartmental model  A compartment is not a real physiologic or anatomic region but is considered a tissue or group of tissues that have similar blood flow and drug affinity. Within each compartment, the drug is considered to be uniformly distributed. Mixing of the drug within a compartment is rapid and homogeneous and is considered to be “well stirred,” so that the drug concentration represents an average concentration, and each drug molecule has an equal probability of leaving the compartment. Rate constants are used to represent the overall rate processes of drug entry into and exit from the compartment. The model is an open system because drug can be eliminated from the system. This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________  To construct a compartmental model as a representation of the body, simplifications of body structures are made. Organs and tissues in which drug distribution is similar are grouped into one compartment. For example, distribution into adipose tissue differs from distribution into renal tissue for most drugs. Therefore, these tissues may be in different compartments. The highly perfused organs (e.g., heart, liver, and kidneys) often have similar drug distribution patterns, so these areas may be considered as one compartment.  The compartment that includes blood (plasma), heart, lungs, liver, and kidneys is usually referred to as the central compartment or the highly blood-perfused compartment. The other compartment that includes fat tissue, muscle tissue, and cerebrospinal fluid is the peripheral compartment, which is less well perfused than the central compartment. Typical organ groups for central and peripheral compartments Another simplification of body process concerns the expression of changes in the amount of drug in the body over time. These changes with time are known as rates. The elimination rate describes the change in the amount of drug in the body due to drug elimination over time. Most pharmacokinetic models assume that elimination does not change over time. 1. One- compartment model  The one-compartment model is the most frequently used model in clinical practice. In structuring the model, a visual representation is helpful. The compartment is represented by an enclosed square or rectangle, and rates of drug transfer are represented by straight arrows. The arrow pointing into the box simply indicates that drug is put into that compartment. And the arrow pointing out of the box indicates that drug is leaving the compartment.  This model is the simplest because there is only one compartment. The drug is both added to and eliminated from a central compartment. The central compartment is assigned to represent plasma and highly perfused tissues that rapidly equilibrate with drug. When an intravenous dose of drug is given, the drug enters directly into the central compartment. Elimination of drug occurs from the central This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ compartment because the organs involved in drug elimination, primarily kidney and liver, are well- perfused tissues. 2. Two- compartment model  Some drugs do not distribute instantaneously to all parts of the body, however, even after intravenous bolus administration. Intravenous bolus dosing means administering a dose of drug over a very short time period. A common distribution pattern is for the drug to distribute rapidly in the bloodstream and to the highly perfused organs, such as the liver and kidneys. Then, at a slower rate, the drug distributes to other body tissues. This pattern of drug distribution may be represented by a two-compartment model. Drug moves back and forth between these compartments to maintain equilibrium  In a two-compartment model, drug can move between the central or plasma compartment to and from the tissue compartment. Although the tissue compartment does not represent a specific tissue, the mass balance accounts for the drug present in all the tissues. In this model, the total amount of drug in the body is simply the sum of drug present in the central compartment plus the drug present in the tissue compartment. Compartmental model representing transfer of drug to and from central and peripheral compartments Drug distribution in one- and two- compartment model This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ 3. Multi-compartment model  Rapid equilibration assumption not always true  Distribution may take some finite time  Body may be represented by two ‘equilibrated’ compartments with distribution between the two  Consider a highly fat-soluble drug. When given as a bolus, it distributes rapidly into all tissues including lean muscle and fat. However, lean muscle contains little fat and is therefore a poor storage reservoir for the drug. The drug is eliminated from that compartment at approximately the same rate as it is from the blood. The fat compartment however soaks up a large amount of the drug. After a while, much of the drug has been cleared from the circulating blood and lean tissue; at this stage the fat compartment begins to act as a source of the drug, topping up the serum levels as elimination takes place. a) Mammillary Model The model consists of one or more peripheral compartments connected to a central compartment Three- compartment mamillary model b) Catenary model  The catenary model consists of compartments joined to one another like the compartments of a train. In contrast, the mammillary model consists of one or more compartments around a central compartment like satellites. Because the catenary model does not apply to the way most functional organs in the body are directly connected to the plasma, it is not used as often as the mammillary model This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ B. Physiologic Pharmacokinetic Model (Flow Model) Physiologic pharmacokinetic models, also known as blood flow or perfusion models, are pharmacokinetic models based on known anatomic and physiologic data. The models describe the data kinetically, with the consideration that blood flow is responsible for distributing drug to various parts of the body. Uptake of drug into organs is determined by the binding of drug in these tissues. Because there are many tissue organs in the body, each tissue volume must be obtained and its drug concentration described. The model would potentially predict realistic tissue drug concentrations, which the two-compartment model fails to do. Clinical Correlate Drugs that do not extensively distribute into extravascular tissues, such as aminoglycosides, are generally well described by one-compartment models. Extent of distribution is partly determined by the chemistry of the agents. Aminoglycosides are polar molecules, so their distribution is limited primarily to extracellular water. Drugs extensively distributed in tissue (such as lipophilic drugs like the benzodiazepines) or that have extensive intracellular uptake may be better described by the more complex models. This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ 2. Activity 3: Skill-building Activities (20 mins+ 5 mins checking) I. Multiple choice. Write the capital letter of your answer before the number. Check your answers against the Key to Corrections found at the end of this SAS. Write your score on your paper. 1. What is the route of administration of Fentanyl lozenge? A. Oral B. Buccal C. Sublingual D. None of the choices 2. One drug commonly administered transdermally is: A. Nitrogylcerin B. Aspirin C. Epinephrine D. Salbutamol inhaler 3. The administration route for a drug injected just beneath the top layer of the skin is called: A. Intradermal B. Subcutaneous C. Intramuscular D. Intraperitoneal 4. Common route of administration of Insulin A. Intradermal B. Subcutaneous C. Intramuscular D. Intraperitoneal 5. Drugs administered via this route are not subject to first pass metabolism, except: A. Rectal B. Transdermal C. Nasal Inhalation D. Topical 6. First pass metabolism occurs in: A. Liver B. Gut wall C. All of the choices D. None of the choices 7. Liposomal Amphotericin B used for the treatment of refractory Cryptococcus neoformans encephalitis is administered via this route A. Subcutenous B. Intravenous C. Intra-arterial D. Intrathecal 8. What is the result of first pass metabolism? A. Low bioavailability of drugs B. short duration of action of drugs C. All of the choices D. None of the choices 9. This route allows one to achieve relatively precise drug concentrations in the plasma This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ A. Subcutenous B. Intravenous C. Intra-arterial D. Intrathecal 10. Scopolamine used to treat motion sickness is commonly administered via this route A. Rectal B. Transdermal C. Nasal Inhalation D. Topical 11. The main advantage of oral administration of drugs, compared to intravenous is: A. Better absorption of the drug B. Better distribution of the drug C. Prevention of first pass metabolism D. Relatively cheaper and safer 12. What is the route of administration of Dulcolax suppository used to treat constipation? A. Rectal B. Transdermal C. Nasal Inhalation D. Topical 13. This route allows the medication to be rapidly absorbed through the mucous membranes of the mouth and blood vessels of the tongue A. Oral B. Buccal C. Sublingual D. None of the choices 14. What are the factors that influence the selection of the delivery route of drugs? A. Dosage size B. Physico chemical properties of drugs C. All of the choices D. None of the choices 15. Which of the ff. can sense the environment of the site of release and deliver the drug to the target site? A. Liposomes B. Micelles C. Biodegradable particles D. Artificial DNA nanostructures II. Modified True or False. Write TRUE if the statement is correct, but if it is FALSE change the underlined word or group of words to make the whole statement true. ____________1. TRUE The compartments do not represent a specific tissue or fluid but may represent a group of similar tissues or fluids. ____________2. Open A compartment model is a closed system. ____________3. TRUE Adipose tissue is considered a peripheral compartment ____________4. Two- compartment In one- compartment model, the drug moves back and forth between the central and peripheral compartment to maintain equilibrium This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ ____________5. Catenary The mammillary model consists of compartments joined to one another like compartments of a train ____________6. TRUE In one- compartment model, the drug is both added to and eliminated from a central compartment ____________7.The TRUE one-compartment model is the most frequently used model in clinical practice. ____________8. Mammillary The catenary model consists of one or more compartments around a central compartment like satellites. ____________9. TRUE When an intravenous dose of drug is given, the drug enters directly into the central compartment. ____________10. Central In one-compartment model, the peripheral compartment is assigned to represent plasma and highly perfused tissues that rapidly equilibrate with drug. ____________11. TRUE The central compartment is a highly blood-perfused compartment. ____________12. TRUE Physiologic pharmacokinetic models are also known as blood flow or perfusion models. ____________13. TRUE The elimination rate describes the change in the amount of drug in the body due to drug elimination over time. ____________14. TRUE In a two- compartment model, the total amount of drug in the body is simply the sum of drug present in the central compartment plus the drug present in the tissue compartment. ____________15. Central Elimination of drug occurs from the peripheral compartment because the organs involved in drug elimination, primarily kidney and liver, are well-perfused tissues. 3. Activity 4: What I Know Chart, part 2 (5 mins) This serves as a review and summary of what you have learned from the session. Monitor how your knowledge has changed by reviewing the questions in the What I Know Chart from Activity 1 and write your answers to the questions based on what you now know in the third column of the chart. 4. Activity 5: Check for Understanding (10 mins). Multiple Choice. Write the capital letter of your answer before the number. Answers will be provided and discussed by your instructor. 1. The route of administration which will by-pass the GIT degradation and hepatic metabolism is: a.Intravenous injection b.Sublingual c. Buccal d.All the above 2. It is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. a.Dosage form b.Drug Delivery system c. Biopharmaceutics d.Pharmacokinetics 3. What is the route of Administration of Clonidine 75mcg tablet? a.Oral b.Intravenous c. Sublingual d.Buccal This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ 4. Which of the following Route of Administration that has 100% bioavailability? a.Oral b.Buccal c. Topical d.Intravenous 5. A rectal suppository is used to treat a fever. This would represent what type of drug delivery? a.Parenteral and local b.Parenteral and systemic c. Enteral and local d.Enteral and systemic 6. Which one of the following does not rely on topical drug delivery? a.Nasal spray b.Anti-dandruff shampoo c. Insulin pen d.Ophthalmic ointment 7. This route is most often used for the sustained delivery of drugs a. Inhalation b. Transdermal c. Rectal d. Oral 8. What is the ff. Oral drugs has the lowest bioavailability? a. Solutions b. Capsule c. Film-coated tablet d. Suspension 9. This route is used when a rapid clinical response is necessary? a. Intramuscular b. Subcutaneous c. Intravenous d. Intradermal 10. The ff. is/are the advantage/s of sublingual administration, except: a. No occurrence of gastrointestinal degradation b. Used to provide local action of the drug c. No first pass metabolism d. A&C 11. Which organ comprises the peripheral compartment in a two compartment model? a. Liver b. Lungs c. Kidneys d. Muscles 12. Which organs comprise the central compartment in a two compartment model? a. Muscles b. Skin c. Adipose d. Liver This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ 13. In pharmacokinetics, the term rate refers to a change in which of the following measurements over time. a. Drug dose b. Drug elimination c. Concentration of drug in plasma d. None of the choices 14. Highly perfused organs and blood comprise what is usually known as the peripheral compartment. a. True b. False 15. The most commonly used model in clinical pharmacokinetic situations is the: a. One- compartment model b. Two- compartment model c. Multicompartment model 16. Instantaneous distribution to most body tissues and fluids is assumed in which of the following models? a. One- compartment model b. Two- compartment model c. Multicompartment model 17. Is the simplest way to describe the process of drug distribution and elimination in the body. a. One compartment model b. Two compartment model c. Three compartment model 18. This model would potentially predict realistic tissue drug concentrations a. Mammillary Model b. Catenary model c. Flow model 19. This model consists of one or more compartments around a central compartment like satellites a. Mammillary model b. Catenary model c. Flow model 20. This model consists of compartments joined to one another like the compartments of a train a. Mammillary model b. Catenary model c. Flow model C. LESSON WRAP-UP 1) Activity 6: Thinking about Learning (5 mins) A. Work Tracker You are done with this session! Let’s track your progress. Shade the session number you just completed. 1 2 3 4 5 6 7 8 9 10 This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ B. Think about your Learning Which part of the topic was easy for you? Which part of the topic was difficult to understand? How did you study and comprehend hard topics of this module? Frequently Asked Questions (FAQs) What are the advantages of oral route of administration of drugs? The oral administration route is preferred over the various other administration routes of drug delivery due to the many advantages it exhibits. These advantages include safety, good patient compliance, ease of ingestion, pain avoidance, and versatility to accommodate various types of drugs (Sastry et al., 2000). Which route of administration is not by mouth? Parenteral route Parenteral administration refers to any non-oral means of medicine administration, but is generally interpreted as relating to injecting directly into the body, bypassing the skin and mucous membranes What are the reasons to use a multi- compartment model instead of a physiologic model? Physiologic models are complex and require more information for accurate prediction compared to compartment models. Missing information in the physiologic model will lead to bias or error in the model. Compartment models are more simplistic in that they assume that both arterial and venous drug concentrations are similar. The compartment model accounts for a rapid distribution phase and a slower elimination phase. Physiologic clearance models postulate that arterial blood drug levels are higher than venous blood drug levels. In practice, only venous blood samples are usually sampled. Organ drug clearance is useful in the treatment of cancers and in the diagnosis of certain diseases involving arterial perfusion. Physiologic models are difficult to use for general application. What is the purpose of pharmacokinetic models? The purpose of pharmacokinetic models is to relate the time course of the drug in the body to its pharmacodynamic and/or toxic effects. The pharmacokinetic model also provides a basis for drug product design, the design of dosage regimens, and a better understanding of the action of the body on the drug This document is the property of PHINMA EDUCATION  COURSE CODE:PHA068 (BIOPHARMACEUTICS AND PHARMACOKINETICS) STUDENT ACTIVITY SHEET MODULE #2 Name: _________________________________________________________ Class number: _______ Section: ____________ Schedule: __________________________________ Date: ______________ Key to corrections Activity 3: Skill Building Activities I. Multiple choice 1. B 11. D 2. A 12. A 3. A 13. C 4. B 14. C 5. A 15. D 6. C 7. D 8. C 9. B 10. B II. Modified True or False. 1. T 2. Open 3. T 4. Two- compartment 5. Catenary 6. T 7. T 8. Mammillary 9. T 10. Central 11. T 12. T 13. T 14. T 15. Central This document is the property of PHINMA EDUCATION