بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية Pharmacology Tutorials Program 3rd. Years Semester2 1. Define the following term i. Drug permeation: ..................................................................................................... ii. Ion trapping phenomena: ........................................................................................ iii. Facilitated diffusion: ............................................................................................. 2. Classify the following statements as True or False with an explanation i. GIT motility doesn’t affect drug absorption. [ ii. Pharmacokinetics is the qualitative study of drug movement in, through and out of the body. [ ] iii. Water and small molecules can easily cross the membrane. [ iv. Passive diffusion according to concentration gradient require energy. [ ] v. Ionized molecules is highly absorbed than non-ionized molecules. [ ] vi. According to ion trapping effects weak acid trapped in high ph. [ ] vii. Drug with large Mwt absorbed at higher rate from drug with small Mwt. [ ] ] ] 3. Justify the following statements i. basic lipophilic molecules have higher rate of absorption from small intestine higher than other one. .............................................................................................................................. ii. Absorption rate from duodenum is higher than ileum. .............................................................................................................................. .............................................................................................................................. iii. Temperature will affect the rate of drug absorption from subcutaneous administration. ................................................................................................................................. ................................................................................................................................. iv. Intramuscular administration has higher bioavailability than subcutaneous administration. .................................................................................................................................. .................................................................................................................................. SIU.Ph.P/2018 Page 1 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية v. drug with pka 3.5 higher absorbed from basic medium. ..................................................................................................................................... ..................................................................................................................................... vi. volume of distribution is called apparent volume. ..................................................................................................................................... ..................................................................................................................................... 4. Specialized transporter system contains i-…………………………………………………………………………………… ii-…………………………………………………………………………………… iii-…………………………………………………………………………………… 5. Compare between drug permeation process ..................................................................................................................................... ..................................................................................................................................... ..................................................................................................................................... 6. Mention the two types of active transporter i-…………………………………………………………………………………… ii-…………………………………………………………………………………… 7. Mention factor affecting oral bioavailability ..................................................................................................................................... ..................................................................................................................................... ..................................................................................................................................... 8. Volume of Distribution is mainly depending on ..................................................................................................................................... ..................................................................................................................................... ..................................................................................................................................... 9. Explain the differences between endocytosis and pinocytosis ……………………………………………………………………………………… ……………………………………………………………………………………… ……………………………………………………………………………………… 10.Mention the four process in pharmacokinetic …………………..,…………………,……………………..,…………… SIU.Ph.P/2018 Page 2 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية 11.select statement from column A that match with statement in column B and put it in column C A B C A- Liver ability of molecule to pass through a membrane B- Drug permeation liquid substance C- Passive transport Is a major organ for metabolism D- Active transport Ionize form E- Pinocytosis Un ionize form F- Water soluble Need ATP an occur against Conc gradient G- Lipid soluble Water small molecules H- Ph. Kinetic Quantitative process I- Plasma alkalinization CNS distribution 12.Solve the following problems i. Mrs G.A is hypertensive patient she takes high dose of aspirin (weak acidic drug Pka 3.5) as antiplatelet. How we can manage this patient. ..................................................................................................................................... ..................................................................................................................................... ii. Mr M.F A 25-year-old suffering from asthma used theophylline tab (drug with high volume of distribution) he come to clinic suffering from severe tachycardia, diarrhea and muscle tremor, after medical examination he report that he accidentally takes large dose of his anti-asthmatic drug. How we can manage this drug toxicity case? ..................................................................................................................................... ..................................................................................................................................... SIU.Ph.P/2018 Page 3 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية MCQs: 1. All of the following are general mechanisms of drug permeation Except a) Aqueous diffusion. d) Pinocytosis or endocytosis. b) Aqueous hydrolysis. e) Special carrier transport. c) Lipid diffusion. 2. Distribution of drugs to specific tissues a) Is independent of blood flow to the organ. b) Is independent of the solubility of the drug in that tissue. c) Depends on the unbound drug concentration gradient between blood and tissue. d) Is increased for drugs that are strongly bound to plasma proteins. e) Has no effect on the half-life of the drug. 3. The following are excreted faster in basic urine (a) Weak acids. (b) Strong acids. (c) Weak Bases. (d) None of the above. 4. With regard to distribution of a drug from the blood into tissues a) Blood flow to the tissue is an important determinant. b) Solubility of the drug in the tissue is an important determinant. c) Concentration of the drug in the blood is an important determinant. d) Size (volume) of the tissue is an important determinant. e) All of the above are important determinants. 5. Active transport differs from facilitated transport in following ways, except a) Carrier is involved. c) Energy is required. b) It is against concentration d) All of the above. gradient. 6. Based on the relation between the degree of ionization and the solubility of a weak acid, the drug aspirin (pKa 3.49) will be most soluble at (a) pH 1.0. (b) pH 2.0. (c) pH 3.0. (d) pH 4.0. 7. The passage of drug molecules from a region of high drug concentration to a region of low drug concentration is known as (a) Active transport. (b) Bioavailability. (c) Biopharmaceutics. (d) Simple diffusion. (e) Pinocytosis. SIU.Ph.P/2018 Page 4 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية 8. After peroral administration, drugs generally are absorbed best from the (a) Buccal cavity. (b) Stomach. (c) Duodenum. (d) Ileum. (e) Rectum. 9. Which of the following acids has the highest degree of ionization in an aqueous solution? a) Aspirin pKa = 3.5. d) Ibuprofen pKa = 5.2. b) Indomethacin pKa = 4.5. e) Phenobarbital pKa = 7.4. c) Warfarin pKa = 5.1. 10.The excretion of a weakly acidic drug generally is more rapid in alkaline urine than in acidic urine. This process occurs because a) A weak acid in alkaline media will exist primarily in its ionized form, which cannot be reabsorbed easily. b) A weak acid in alkaline media will exist in its lipophilic form, which cannot be reabsorbed easily. c) All drugs are excreted more rapidly in an alkaline urine. 11. Alkalinization of urine hastens the reabsorption of a) Weakly basic drugs. c) Strong electrolytes. b) Weakly acidic drugs. d) Nonpolar drugs. 12.Majority of drugs cross biological membranes primarily by: a) Passive diffusion. c) Active transport. b) Facilitated diffusion. d) Pinocytosis. 13.The most important factor which governs diffusion of drugs across capillaries other than those in the brain is a) Blood flow through the capillary. b) Lipid solubility of the drug. c) pKa value of the drug. d) pH of the medium. SIU.Ph.P/2018 Page 5 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية 14.High plasma protein binding a) Increases the volume of distribution of the drug. b) decrease the therapeutic effect. c) Minimizes drug interactions. d) Generally makes the drug long acting. 15.Active transport of a substance across biological membrane has the following characteristics except a) It is specific. b) It is pH dependent. c) It is saturable. d) It requires metabolic energy. 16.Bioavailability differences among oral formulations of a drug are most likely to occur if the drug a) Is freely water soluble. b) Is completely absorbed. c) Is incompletely absorbed. d) Undergoes little first-pass metabolism. 17.A prodrug is a) The prototype member of a class of drugs. b) The oldest member of a class of drugs. c) An inactive drug that is transformed in the body to an active metabolite. d) A drug that is stored in body tissues and is then gradually released in the circulation. 18.Bioavailability of drug refers to a) Percentage of administered dose that reaches systemic circulation in the unchanged form. b) Ratio of oral to parental dose. c) Ratio of orally administered drug to that excreted in the faeces. d) Ratio of drug excreted unchanged in urine to that excreted as metabolites. 19.The most important factor governing absorption of a drug from intact skin is a) Molecular weight of the drug. b) Site of application. c) Lipid solubility of the drug. d) Nature of the base used in the formulation. SIU.Ph.P/2018 Page 6 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية 20.Weakly acidic drugs a) Have high volume of distribution. b) Are excreted faster in alkaline urine. c) Are highly ionized in the gastric juice. d) Do not cross blood—brain barrier. 21.Pharmacokinetics is a) The study of biological and therapeutic effects of drugs. b) The study of absorption, distribution, metabolism and excretion of drugs. c) The study of mechanisms of drug action. d) The study of methods of new drug development. 22.A small amount of the volume of distribution is common for lipophylic substances easy penetrating through barriers and widely distributing in plasma, interstitial and cell fluids a) True. b) False. 23.What does “pharmacokinetics” include? a) Localization of drug action. c) Excretion of substances. b) Mechanisms of drug action. d) Interaction of substances. 24.What kind of substances can’t permeate membranes by passive diffusion? a) Lipid-soluble. c) Hydrophobic substances. b) Non-ionized substances. d) Hydrophilic substances. 25.A hydrophilic medicinal agent has the following property: a) Low ability to penetrate through the cell membrane lipids. b) Penetrate through membranes by means of endocytosis. c) Easy permeation through the blood-brain barrier. d) High reabsorption in renal tubules. 26.Most of drugs are distributed homogeneously. a) True. b) False. 27.What is implied by «active transport»? a) Transport of drugs through a membrane by means of diffusion. b) Transport without energy consumption. c) Engulf of drug by a cell membrane with a new vesicle formation. d) Transport against concentration gradient. SIU.Ph.P/2018 Page 7 of 8 بسم هللا الرحمن الرحيم Sudan International University Department of Pharmacology & Pharmacy Practice جامعة السودان العالمية قسم علم األدوية والممارسة الصيدالنية 28.Tick the feature of the sublingual route a) Pretty fast absorption. b) A drug is exposed to gastric secretion. c) A drug is exposed more prominent liver metabolism. d) A drug can be administrated in a variety of doses. 29.Parenteral administration a) Cannot be used with unconsciousness patients. b) Generally; results in a less accurate dosage than oral administration. c) Usually produces a more rapid response than oral administration. d) Is too slow for emergency use. 30.Intravenous injections are more suitable for oily solutions: a) True b) False SIU.Ph.P/2018 Page 8 of 8