Test Pharmacology UTM Test 1 - 2012 PDF

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Fall 2012: BIO200H5F: Introduction to Pharmacology (Pharmacokinetic Principles) Term Test #1: Thursday, October 4th, 2012 (5:15PM to 6:45PM) Kaneff Centre 137 Instructor: Dr. W.M. Burnham Duration: 90 Minutes Aids Allowed: Non-Programmable Calculators ***DO NOT OPEN TH E TEST BOOKLET UNTIL INSTRUCTED TO DO SO*** ***PLEASE MAKE SURE YOU HAVE ALL 11 PAGES*** 1.) Remember to fill in your NAME, STUDENT NUMBER and SIGNATURE on your Scantron Sheet. 2.) All questions are Multiple Choice. There is only ONE correct answer to each question. If two options seem possible, choose the BETTER of the two. Remember to always choose the BEST answer! 3.) All answers must be RECORDED on the Scantron Sheet in black lead pencil (HB2). Ask for a pencil if you do not have one. You WILL NOT be given additional time to transfer your answers to the Scantron sheet at the end of the test. 4.) All FIGURES appear on PAGE 11 of the test booklet. They may be torn off for easy reference. 5.) The only aids allowed are non-programmable calculators. Programmable calculators will be erased at the start of the test. 6.) There are 45 Multiple Choice Questions (1-45) each worth 1 mark, for a total of 45 Marks. You have 90 minutes for this term test. Term Test I is worth 30% of your final mark. 7.) Abbreviations: ASA = Acetylsalicylic Acid; Po/w = Partition Coefficient; Co = Initial Concentration; Vd = Apparent Volume of Distribution; L = Litres; K or kg = Kilograms; MW = Molecular Weight. 8.) Some questions ask you to find the single WRONG answer. These are indicated by “EXCEPT” or "MISMATCH". 9.) You may keep this test booklet at the end of the term test. Your T.A. will post the correct answers on Blackboard within 24 hours. If you have any questions, you make contact your T.A.

Good Luck!

Fall 2012: BIO200H5F: Term Test I

Page 1 of 11

Introduction & Drugs as Molecules: 1.) True statement: a.) A “drug” is any substance which affects an organism’s physiology. b.) The broad definition of pharmacology excludes poisons. c.) Vitamins and minerals are considered “drugs”, even if they in ingested in “physiological” amounts. d.) Any drug in excess becomes a poison. e.) Most drugs are inorganic molecules.

2.) True statement about the real world disciplines related to pharmacology. a.) Pharmaceutical chemistry deals with drug synthesis and SARs. b.) Pharmacy is also called “pharmcotherapeutics.” c.) “Forensic toxicology” is another name for “environmental toxicology.” d.) Pharmacometrics measures the atomic weight of drug molecules. e.) Pharmacoeconomics is the study of the mechanisms of action of drugs.

3.) Which reference book will discuss the melting point of a drug? a.) The CPS b.) Goodman and Gilman c.) The Merck index d.) The PDR e.) The BP

4.) According to Table 1.1 in your textbook, which of the following is a pure compound originally extracted from cinchona bark? a.) Esserine b.) Quinine c.) Ephedrine d.) Digoxin e.) Reserpine

5.) Which of the following is a semi-synthetic compound? a.) Morphine b.) Digoxin c.) Meperidine d.) Diazepam e.) Heroin

Fall 2012: BIO200H5F: Term Test I

Page 2 of 11

6.) Identify the MISMATCH (drug : type of drug name): a.) valium : a “proprietary” name b.) lanoxin : a “trade” name c.) Ro 15 1788 : a drug company code d.) propranolol : an “official” name e.) dilantin : a “non-proprietary” name

7.) What phase of drug development involves controlled marketing? a.) Preclinical testing b.) Phase 1 c.) Phase 2 d.) Phase 3 e.) Phase 4

8.) Consider Figure 1 (Page 11 of your test booklet). True statement: a.) The dose-response curve in Chart A is curvilinear because unbound receptors become rare at higher blood levels. b.) The dose-response curve in Chart B is only seen with quantal data. c.) The dose-response curve illustrated in Chart A would be seen with antacid drugs. d.) The dose-response “curve” illustrated in Chart B would be seen with both diazepam and propranolol. e.) The dose-response curve in Chart A is presented in “semi-log” form.

9.) Consider Figure 2 (Page 11 of your test booklet). True statement: a.) Drug C is the most potent drug. b.) The ED50 of Drug C is about 16. c.) The Rmax of Drug C is higher than the Rmax of Drug B. d.) The ED50 of Drug A is about 4. e.) Drug B is four times as strong as Drug A.

10.) THOUGHT QUESTION: Consider Figure 2 (Page 11 of your test booklet). True statement: a.) The therapeutic index of Drug B is 4.0. b.) The ED1 of Drug B is about the same as the ED1 of Drug C. c.) The relative potency of Drug B to Drug C is 4.0. d.) Drugs A and C may bind to the same receptor. e.) The relative potency of Drug B to Drug A is 4.0.

Fall 2012: BIO200H5F: Term Test I

Page 3 of 11

11.) Consider Figure 3 (last pages of test). True statement: a.) The data are graded, not quantal. b.) The TI of Drug A is higher than the TI of Drug B. c.) The TD50 of Drug B is higher than the TD50 of Drug A. d.) The CSF of Drug A is higher than the CSF of Drug B. e.) CSFs are always higher than TIs.

12.) The Po/w of a drug: a.) Relates to its relative solubility in lipids and water. b.) Is above 1 if a drug is more soluble in water than in lipid. c.) Is the concentration in water divided by the concentration is lipid. d.) Is above 1 if a drug is in its “charged” (ionic) state. e.) Is never higher than 2.

13.) Addition of which of the following groups makes a drug more polar? a.) - I b.) -Cl c.) -OH d.) -CH3 e.) -Br

14.) Which of the following compounds have an intermediate polarity? a.) Quaternary amines b.) Primary amines c.) Tertiary amines d.) Aromatic hydrocarbons e.) Secondary amines

15.) Which example drug is an acid with a pKa over 7.0? a.) ASA b.) Diazepam c.) Digoxin d.) Neostigmine e.) Phenytoin

Fall 2012: BIO200H5F: Term Test I

Page 4 of 11

16.) In the Henderson-Hasselbach equation, if pH is 2 and pKa is 3, then: a.) The log of [protonated]/ [non-protonated] is -1. b.) The drug is about 90% protonated. c.) There is no statement that can be made unless you know whether the drug is an acid or a base. d.) The drug is about 1% non-protonated. e.) The drug is mostly uncharged.

17.) The Henderson-Hasselbach equation would apply to all of the following, EXCEPT: a.) ASA b.) Diazepam c.) Digoxin d.) Phenytoin e.) Propranolol

18.) The Michaelis-Menten equation: a.) Only applies to weak acids and weak bases. b.) Would apply to ASA, but not to the remaining example drugs. c.) Describes a curvilinear (not a straight line) relationship. d.) Would not apply to neostsigmine because it is a quaternary amine. e.) Is a mathematical statement of the “cut off” effect.

Absorption & Crossing Membranes: 19.) True statement: a.) The nuclear membrane restricts the passage of low Po/w molecules. b.) The plasma membrane is also called the endoplasmic reticulum. c.) The layer of unstirred water is associated with the glycocalyx. d.) Only low Po/w compounds can cross the plasma membrane. e.) Most drugs act by binding to the polar head groups of phospholipids.

20.) Where would you find fenestrated capillaries? a.) In the kidneys. b.) In the heart. c.) In the liver. d.) In the blood-brain barrier. e.) In muscle tissue.

Fall 2012: BIO200H5F: Term Test I

Page 5 of 11

21.) True statement about the blood-brain barrier: a.) It keeps most high Po/w molecules from entering the brain. b.) It exists in both the pineal and pituitary glands. c.) It is also called the “meninges”. d.) It exists in the area postrema, which also has fenestrated capillaries. e.) It is both a physical and an enzyme barrier. 22.) All of the following were mentioned in lecture as being important in the passive absorption of small, low Po/w molecules, EXCEPT: a.) Aquaporins b.) Size of molecule c.) pH d.) Concentration gradient e.) Surface area for diffusion

23.) Which of the following drugs crosses membranes by active transport? a.) Diazepam b.) Lithium c.) Propranolol d.) L-DOPA e.) Penicillin

24.) True statement about facilitated diffusion: a.) It transports molecules against the concentration gradient. b.) It is saturable. c.) It only occurs when molecules have a molecular weight over 1000 Da. d.) It only occurs with small, high Po/w molecules. e.) It requires ATP.

25.) True statement about absorption: a.) Absorption from the G.I. tract is faster if drugs are taken with food. b.) Intestinal blood flow is important for elimination but not for absorption. c.) Absorption of acidic drugs is faster if they are taken with antacids. d.) Basic drugs like diazepam cannot be absorbed from the intestine. e.) Drugs with a very high Po/w may be absorbed poorly due to the “cut off” effect.

Fall 2012: BIO200H5F: Term Test I

Page 6 of 11

26.) THOUGHT QUESTION: Which of your example drugs will be mostly charged in the stomach, mostly uncharged in the small intestine and mostly uncharged in the blood stream? a.) ASA b.) Diazepam c.) Digoxin d.) Neostigmine e.) Propranolol

27.) According to your textbook, which of the following would cross membranes by pinocytosis? a.) ASA and NSAIDs b.) Nicotine c.) Milk antigens and other proteins d.) Caffeine e.) Penicillin and L-DOPA

28.) Why are drugs made into quaternary amines? a.) To improve p.o. absorption. b.) To increase pinocytosis. c.) To keep them from crossing the blood-brain barrier. d.) To avoid the “cut off” effect. e.) To prevent active transport.

29.) True statement: a.) Propranolol is mostly uncharged in the blood. b.) ASA is mostly charged in the stomach. c.) Phenytoin is mostly uncharged in the blood. d.) Digoxin is mostly charged in the stomach. e.) Neostigmine is mostly uncharged in the intestine.

30.) Which transporter is involved in multi-drug resistance (MDR)? a.) P-glycoprotein. b.) Alpha 1 acid glycoprotein c.) The sodium-potassium ATPase pump d.) Glucose 6 phosphate e.) The 5-HTT

Fall 2012: BIO200H5F: Term Test I

Page 7 of 11

Distribution: 31.) True statement about the apparent volume of distribution (Vd): a.) It is calculated using the formula: Vd = D X Co b.) It is always 42 litres for a 70kg man. c.) It is calculated using the formula: Vd = Ca - Cv d.) It may be larger than the whole body. e.) It is 20% of the body weight.

32.) You have given 100 mg of Drug X, and obtained a concentration of 2 mg/L in the plasma. What is the apparent Vd of Drug X? a.) 2.8 L b.) 42 L c.) 50 L d.) 100 L e.) Cannot be calculated without knowing the pKa of the drug

33.) What compound could you use to calculate the volume of the total body water? a.) Diazepam b.) Sulfanilamide c.) Mannitol d.) Neostigmine e.) Inulin

34.) THOUGHT QUESTION: What real aqueous compartment of the body has a volume of about 40% of the body weight? a.) Intravascular water b.) Intracellular water c.) Extracellular water d.) CSF e.) Total body water

35.) Which reservoir decreases a drug’s apparent volume of distribution? a.) Muscle proteins b.) Body fat c.) Cytoplasmic proteins d.) CSF e.) Alpha-1-acid glycoproteins

Fall 2012: BIO200H5F: Term Test I

Page 8 of 11

36.) Which of the following compounds would concentrate in body fat? a.) Inulin b.) A drug with a Po/w of 10 c.) Neostigmine d.) A drug with a Po/w of 0.01 e.) Evans blue dye

37.) All of your example drugs bind to plasma proteins, EXCEPT: a.) ASA b.) Diazepam c.) Digoxin d.) Neostigmine e.) Phenytoin

38.) Forty minutes after i.v. administration of a drug: a.) The blood concentration will equal Co. b.) Changes in blood concentration will relate to elimination. c.) Blood concentrations are stable, and do not decline farther. d.) Changes in blood concentration will relate to distribution. e.) Binding to plasma proteins has not yet occurred. 39.) “Redistribution”: a.) Only occurs with low Po/w drugs. b.) Occurs because drugs bind to plasma proteins. c.) Is seen with short-acting anaesthetics. d.) Only occurs when drugs bind covalently. e.) Is predicted by the Henderson-Hasselbach equation.

40.) According to you textbook, enterohepatic circulation increases the half-life of some drugs because: a.) Entry into body fat always increases the half-life. b.) It is an intravascular reservoir. c.) Conjugated molecules are de-conjugated in the intestine and re-absorbed. d.) The heart is part of the VPG. e.) It blocks the sodium pump.

Fall 2012: BIO200H5F: Term Test I

Page 9 of 11

Routes of Administration: 41.) Which route of administration is faster when hyaluronidase is co-administered with the drug? a.) percutaneous b.) i.v. c.) i.m. d.) s.c. e.) p.o.

42.) Which route of drug administration typically shows a hepatic first pass effect? a.) topical b.) i.v. c.) i.m d.) s.c. e.) p.o.

Example Drugs: 43.) Which of your example drugs enhances GABAergic inhibition? a.) ASA b.) Diazepam c.) Digoxin d.) Neostigmine e.) Phenytoin

44.) Which of your example drugs is a benzodiazepine? a.) Astrin b.) Valium c.) Lanoxin d.) Prostigmin e.) Dilantin

45.) Which of your example drugs binds irreversibly to an enzyme? a.) ASA b.) Diazepam c.) Neostigmine d.) Phenytoin e.) Propranolol

Fall 2012: BIO200H5F: Term Test I

Page 10 of 11

Figures:

Figure 1:

Chart A

Chart B

Figure 2: Drugs are designated “A”, “B” and “C” A

B

100

Response

80

C 60 40 20 0 2

4

8

16

32

64

128

256

Dose (mg/kg)

Figure 3: Therapeutic

Toxic

PROBIT

8 7 6 5 4 3 2

A

B

A

ED50

TD50

2 mg/kg

4 mg/kg

Fall 2012: BIO200H5F: Term Test I

B

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