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Contents

1. Simple Choice .............................................................................................................................2 2. Multiple Choice...........................................................................................................................9 3. Associations ..............................................................................................................................16 4. Relation Analysis ......................................................................................................................25 5. Calculations...............................................................................................................................29 6. Answer key................................................................................................................................34

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1. Simple Choice

Please, choose the correct one (only one) from the answers below each question. 1. Probenecid lengthens the duration of penicillin’s effect because

A) it blocks its metabolism B) it pushes out penicillin from the silent binding sites C) capacity of tubular excretion is distributed between the two substances D) it promotes penicillin’s absorption E) it blocks penicillin’s accumulation in the peripheral compartments

2. Bioavailability is the

A) duration of drug’s therapeutic blood level B) most proper drug administration C) drug’s quantity and velocity of absorption from the preparation D) pharmacon’s effectiveness in the body E) pharmacon’s affinity to its receptor

3. In pharmacokinetics, what does “smooth tissue” mean? A) rich in water B) hardly accessible for pharmacon C) deformable mechanically D) mostly accessible for pharmacon E) bone tissue

4. Which digitaloid has the best bioavailability after per os intake? A) digitoxin B) acetyldigitoxin C) digoxin D) lanatoside C E) vinpocetine

5. Choose the right tetracycline derivative the dosage of which does not need to be decreased even in case of a reduced kidney function.

A) vancomycin B) amikacin C) gentamicin D) oxytetracycline E) doxycycline

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6. Which statement characterize the intravenous administration ?

A) microcrystal suspension can also be used B) overdose can not be corrected C) solutions that are not pH 7.4 should not be injected D) it is also suitable to produce a local effect, too E) only lesser than 10 milliliters of intake volume should be applied

7. What does “first pass effect” mean? A) the pharmacon after its absorption from the gut arrives primarily at the systemic

circuit avoiding liver B) the pharmacon after its absorption from the gut is metabolised in the liver during its

first pass C) it has the fastest effect D) the pharmacon after its absorption from the gut is excreted primarily with the bile E) pharmacons that can pass the blood-brain barrier have mainly central effect

8. Which heart glicoside binds to plasma proteins the least? A) acetyldigitoxin B) digoxin C) digitoxin D) lanatoside C E) ouabain (G-strophanthin)

9. How do you explain the quick end of the intravenous thiopental’s effect? A) it is because of the redistribution by which this substance is being stored in the

depo fat B) the substance is insignificantly lipophilic C) the substance is eliminated quickly through the lungs D) it is metabolised quickly in the skeletal muscle E) it is cleared quickly by the kidneys

10. Which substance does not typically have an enzyme inductor effect? A) androgenes B) spironolactones C) aminoglicosides D) glucocorticoids E) barbiturates

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11. What does “pharmacokinetical compartment” mean?

A) part of the body water which is located in the vascular system B) total body water (TBW) C) plasma and intracellular fluid together D) part of the body water in which the change of a particular pharmacon’s

concentration has the same kinetics E) anatomical water compartments

12. What is “lag time”? A) the duration hat is needed by the pharmacon to reach the lower level of therapeutic

blood level B) the duration that is needed by the pharmacon to reach the maximum effect after

intake C) the duration that is needed by the pharmacon to get measurable in the blood D) the duration that is needed by the pharmacological answer to take place E) the duration while the concentration reach its plateau

13. Which statement is incorrect? A) iron preparations can block the absorption of tetracyclines B) enzyme induction can provoke lethal drug intoxication C) as an effect of a long-term medicine intake the metabolism of endogenous

substances can be disturbed D) drugs that have acidic pH can block each other’s renal excretion E) only those drugs have long pharmacological effect that can bind to plasma proteins

well

14. Which statement is correct? A) enzyme induction may be neglected when calculating the right therapeutic dose B) the enzymes that are not metabolised on microsomal level can not be induced by

pharmacons C) microsomal enzyme system can not be inhibited D) metabolites of drug always have smaller pharmacological effect than the original

drugs E) therapeutic dose should always be corrected when deviation from average body

mass (70 kgs) is significant (+40 kgs)

15. The duration which is needed to reach the 95 per cent of the plateau: A) five times as long as the elimination half life B) five times as long as the absorption half life C) five times as long as the adsorption half life D) twice as long as the absorption half life E) twice as long as the elimination half life

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16. What is the meaning of "disposition"?

A) decreasing of active ingredient in the central compartment due to distribution and/or metabolism, elimination

B) liberation and distribution of active ingredient in central compartment C) distribution of active ingredient and metabolites between central and periferal

compartment D) elimination of active ingredient by distribution and excretion E) storage of active ingredient in a depot phase, and its proteine binding, respectively

17. What is the meaning of plasma clearance?

A) Percent of drug clears up from plasma in unit time. B) Volume of plasma clears up from active substance in unit time. C) Hypothetic plasma volume, which clears up from unmetabolised active substance in

unit time by any of the elimination processes. D) Volume of plasma clears up from drug in one minute passing through the liver. E) Volume of plasma clears up in unit time from drug excreted by the kidney.

18. Basic pharmacokinetic parameters (ke, t1/2) calculated from urinary data may substitute data calculated from plasma, if

A) Minimum 95 percent of drug excreted via the urine, no metabolism, no protein

binding, no storage, no enterohepatic recirculation. B) The drug excreted unchanged form 100 percent via the urine. C) Value of renal clearance is minimum 100 ml/min, no tubular reabsorption and

metabolism. D) Drug exreted minimum 90 percent via the urine, no metabolism, or known and

detectable is the metabolite, no protein binding, no storage, no tubular reabsorption. E) Drug exreted minimum 90 percent via the urine, no enterohepatic recirculation, no

protein binding, no storage, no tubular reabsorption.

19. Which situation is given on the figure from single dose administration

A) intravascular administration with significant distribution B) intracutan administration with metabolism C) extravascular administration with rapid metabolism D) intramuscular administration with excretion after metabolism E) rapid intravascular administration, when the drug excreted mainly as metabolite

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20. The following is the part of a therapeutic system.

A) loop B) coated pellets C) drug release element D) radiating energy E) phospholipide membrane

21. Definition of therapeutic systems

A) Therapeutic system is a drug containing preparation liberating the active ingredient with predicted rate and timeinterval into the systemic circulation and provide the optimal plasma level "without fluctuation".

B) Therapeutic system is a preparation with sustained release, allowing to liberate the drug according the requirements of body and prepared from bioerodible material.

C) Therapeutic system is a preparation acting systematically or locally and liberates the drug by previously programmed rate determined according to the absorption probability.

D) Therapeutic system is a preparation which liberates the active ingredient by zero order kinetic both the initial and maintaining doses through a micropore membrane.

E) Therapeutic system provides the liberation of active ingredients with short biological half life and narrow therapeutic range according to diurnal rhytm to make safe the treatment.

22. Definition of bioavailability

A) Bioavailability is that drug ratio which exert therapeutic effect after liberating from preparation at given timeinterval, absorbing and reaching the systemic circulation given different way than iv. administration.

B) Bioavailability is defined as both the relative amount of drug from an administered dosage form which enters the systemic circulation and the rate at which the drug appears in the blood stream.

C) Bioavailability is that drug amount which exert therapeutic effect after reaching systemic circulation given different way than iv. administration.

D) Bioavailability is a value of effectiveness which could be given us the amount of active ingredient in body fluids or excreted amount or as a given pharmacological effect.

E) Bioavailability is that timeinterval, when the plasma concentration is above a determined limit and processes of absorption, elimination and metabolism is of first rate.

23. Which data is needed to decide on that the drug is suitable to prepare retard preparation?

A) clearance B) area under the curve C) biological half life D) absorption rate constant E) "first-pass" effect

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24. Which method is not suitable to calculate area under the curve?

A) least square method B) weighing C) planimetry D) trapezoid rule E) integration of curve

25. Pro-pharmacon is a compound, which

A) gets active after reaching the site of action depending on the number and quality of substituents on the molecule.

B) containing the active substance in an inactivated form, in bioreversible bound, but reaching the site of action gets active according to the components.

C) contains the active substance in an inactivated form, due to reduced solubility complexes, but reaching the site of action gets active according to the components.

D) contains the active substance in an inactivated form, due to chemical alteration, changing the valance, but reaching the site of action gets active according to the components.

E) contains NH-acid groups, but reaching the site of action gets active according to the components.

26. Which are those therapeutic systems, which liberate the active ingredient through a

special hole, prepared by laser?

A) TTS patches B) IUD systems C) OCUSERT systems D) OROS systems E) flotating systems

27. Which factors has no effect on bioavailability?

A) the value of blood level us time curve (AUC○→∞) B) maximum plasma level C) therapeutic range D) time to reach maximal plasma level E) quality and quantity of food

28. What is the meaning of biological half life?

A) that time interval, during the half of the drug degrade in body B) that time interval, during the amount of drug reduced to its half C) that time interval, during only the half of the biological effect developed D) that time interval, during the half of the drug metabolised E) that time interval, during the half of the drug liberates from protein binding

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29. What is required to produce constant blood level, when the preparation contains initial

and maintenance doses

A) When the initial and maintenance doses liberate at the same time and the rate is first order.

B) When the half of the particles is uncoated in the preparation. C) When the initial and maintenance doses liberate with zero order kinetics. D) When the initial dose liberates with first order and the maintenance dose liberates

with zero order kinetics. E) When the active ingredient liberates with zero order and the maintenance dose starts

to liberate when the initial dose reaches its maximum.

30. Which are the basic conditions that provide the function of therapeutic systems?

A) Artificial materials ensure the function B) It contains the active ingredient in solid form C) Biodegradable polymer materials ensure the controlled release D) It contains a regulatory unit and produces programmed liberation E) The liberation of active ingredient is controlled by the transmission (pore size) of

the surface membrane

31. Which preparations has three dimensions?

A) prepared by spherical particles B) which can be characterized by the amount of incorporated drug in definite volume C) during their development the following three elements were evident: absorption

probability (Fabs), mean residence time (MRT), bioavailability (AUC), D) applying on skin they exert penetrating, permeating and absorbing effect E) which needs the time factor to be built into the preparation.

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2. Mult iple Choice More than one from the answers below each question is correct so please use this alphabet scheme to solve the test: A): only the first answer is correct B): only the third answer is correct C): only the first and fifth answers are correct D): only the second and third answers are correct E): only the second and fourth answers are correct 32. Choose the right statement. Characteristics of pharmacon’s biliary excretion are:

1. its direction is the same as drug’s concentration gradient 2. its direction can even be against drug’s concentration gradient 3. it can be saturated by increasing the plasma concentration 4. chargeless molecules influence each other’s excretion 5. ions with the same polarity stimulate each other’s excretion

33. Which parameters are redundant for the calculations of maintenance dose if the drug has Michaelis-Menten kinetics?

1. elimination half time 2. maximum velocity of pharmacon’s metabolism 3. average plasma concentration within a particular period 4. the plasma concentration by which the velocity of metabolism is half of the maximal

value 5. dosing interval

34. Which substances alkalize urine? 1. dimercaptopropanol 2. thiazide type diuretics 3. antacids 4. salicylates 5. spironolactone

35. Which statements are right if kinetic parameters of the applied drug are modified by reduced renal function?

1. dose must be decreased 2. dosing interval must be decreased 3. half life can drop significantly 4. ratio of free and bound (to plasma proteins) molecules is not changed 5. renal clearance decreases

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36. Which statements are right? They relate to the substances that take part in the entero-

hepatic cycle. 1. some have biliary elimination in form of glucuronides 2. the cycle does not change the duration of effect 3. glucuronides are absorbed in the small intestine 4. benzodiazepines do not take part in the cycle 5. temporary increase of plasma concentration can be observed in the elimination

phase

37. Which substances will have therapeutic effect after oral intake? 1. streptomycin 2. quaternary ammonium bases 3. hemisynthetic penicillin derivatives 4. insulin 5. penicillin G

38. Which substances’ kinetics can be described using the one-compartment model? 1. oxytetracycline 2. theophylline 3. caffeine 4. chloroquine 5. digitoxin

39. Which factors change drug sensitivity in newborns? 1. relatively great amount of extracellular fluid 2. increased permeability in capillaries (blood-brain, blood-liquor barrier) 3. metabolic enzyme differences between adults and newborns 4. lack or immaturity of metabolic enzymes 5. gut motility is more intense than in adults

40. What kind of information does numerically described AUCT have? 1. pharmacon’s concentration at a given point of time 2. time needed by the pharmacon to get into the systemic circulation 3. the quantity of active compound that can get into the systemic circulation from the

preparation in a given time 4. duration while the pharmacon remains measurable in the body 5. tmax and Cmax values of the blood level curve

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41. What are the consequences of being bound to plasma proteins?

1. increases the concentration of pharmacon in biophase 2. forms a depo and can prolong the duration of drug’s effect 3. it can be an origin of interactions 4. molecules bound to plasma proteins are also filtrated in glomeruli 5. pharmacon concentration of blood does not have an effect on its linkage to plasma

proteins

42. Select the right answers. Drug is metabolized 1. not only in liver. 2. only in liver. 3. only in kidneys. 4. only in liver and kidneys. 5. only in liver, kidneys and lungs.

43. Which statements are correct about lidocaine? 1. it is used in ventricular arrhythmia in most cases 2. elimination half life is 8 hours or more 3. it is used the least in ventricular arrhythmia 4. propranolol and cimetidine stimulate its metabolism 5. propranolol and cimetidine slows down its metabolism

44. Choose the right statements about procainamide. 1. its half life is 10-14 h 2. it is given orally as a prophylactic treatment 3. it can be used as a local anesthetic agent 4. its metabolite, N-acetyl-procainamide has the same antiarrhythmic effect as itself 5. it is inactivated in liver so there is no need to decrease dose in case of kidney

malfunction

45. Choose the right assertions about amphetamine. 1. it may be found unchanged in urine 2. intensity of its effect depends strongly on urine’s pH 3. urine should be acidized in acute amphetamine toxicosis 4. AUC values of the same doses are independent of the part of the day 5. metamphetamine (amphetamine derivative) has no effect

46. Which are the correct assertions about benzodiazepine? 1. very small amount is absorbed from gut so mostly intravenous intake is applied 2. binds hardly to serum proteins 3. its metabolite, N-methyl-diazepam is not as active as itself and acts as a partial

antagonist 4. average half life is 6-8 hours 5. redistribution is not characteristic to its movement in water compartments

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47. Which statements are true? Renal excretion of weak bases

1. can be decreased by the acidification of urine 2. can be sped up by the acidification of urine 3. can be stimulated by sodium bicarbonate 4. can not generally be changed by the substances that block active transport 5. can not be changed by the modification of urine’s pH

48. Which assertions are false? 1. simultaneous consumption of milk blocks the absorption of tetracyclines 2. eating slows down the absorption of digoxin 3. insulin is not absorbed from the large intestine 4. absorption of griseofulvin will be faster if it is consumed together with a fatty meal 5. insulin should be given parenterally otherwise it is digested by pepsin in stomach

49. Which statements describe the saturating dose? In case of a long-term intravenous infusion, the saturating dose

1. is used when the pharmacon has long elimination half life 2. is applied to raise the level of a planned plateau 3. has no connection with the duration of time needed to reach the plateau 4. decreases the infusion rate that maintains the planned plateau 5. has to be at least ten times as much as the maintenance dose

50. Choose the false statements. 1. using the body surface for calculations of child dose is the most proper method 2. clearance of salicylic acid is 60 per cent greater in men than in women 3. most pharmacon’s elimination half time is longer in obese (fat) people 4. body mass dependent clearance increase and decrease of elimination half life happen

at the same time 5. duration of effect and toxicity changes with the period of day

51. What does ‘A’ mean in the word LADME? 1. area under the curve 2. availability 3. absorption 4. accumulation 5. adsorption

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52. Which parameters determine the rate and extent of bioavailability?

1) value of area under curve (AUC○→t) 2) value of area under curve (AUC°→°°), maximal plasma concentration (Cmax, time to

reach maximal plasma concentration (tmax) 3) value of area under curve (AUC°→°°) and value of maximal plasma concentration

(cssmax) at steady state

4) hypothetical plasma concentration at time=0 (cp0), maximal plasma concentration

(Cmax) time to reach maximal plasma concentration (tmax), elimination rate constant (kel)

5) total amount of unmetabolised active ingredient (Ae), absorption rate constant (ka), elimination rate constant (kel)

53. Which physiological factors alter the onset of biological response?

1) body weight, age, gastric emptying time 2) ratio of protein, fat, carbohydrate in food 3) body surface, height 4) energy sources in body to be mobilise 5) genetic factors, state of kidney and liver, blood flow through organs

54. The biological half life of which drugs does not alter significantly in reduced kidney function?

1) ampicilline 2) doxycycline 3) cefaclor 4) penicillin G 5) streptomycin

55. Which active ingredients have short biological half life?

1) cimetidine 2) cyclobarbitone 3) cefaclor 4) cycloserin 5) Vitamin C

56. Which in vitro models are suitable to determine the liberation of active ingredients?

1 ) rotating basket model 2) solvometer 3 ) disc model 5) paddle method

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57. What is the reference during calculation of absolute bioavailability?

1) BA of oral solution 2) BA of IV administration 3) drug product containing the active ingredient in the same dosage form and in the

same dose 4) the dose 5) drug product containing the same active ingredient, in the same dosage form and in

the same dose

58. Which analytical methods are the most sensitive ones in biopharmacy?

1) GC with flame-iorusation detector 2) GC with electroncapture detector 3) RIA 4) detection of total radioactivity 5) fluorimetry

59. The absorption of drug may be enhanced, when

1) the drug absorbs from the upper part of the colon 2) the drug absorbs from the stomach 3) the drug absorbs from the upper part of the jejunum 4) the drug absorbs from the lower part of the jejunum 5) the drug absorbs from the lower part of the colon

60. From which part of the GI tract sugars absorb?

1) jejunum 2) stomach 3) colon 4) rectum 5) oesophagus

61. Which factors has to be taken into consideration when dosage regimen is determined?

1) biological half life 2) volume of urine excreted 3) amount of metabolites excreted 4) absorbed amount of active ingredient 5) age

62. Which factors are negligible during dissolution test determined by rotating basket method?

1) rotation speed of basket 2) the humidity and temperature of surrounding air 3) the place of sampling 4) the composition of dissolution medium 5) the temperature of dissolution medium

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63. Which behaviour of the drug has determining importance from the point of view of

absorption?

1) dissolution 2) crystal habit 3) crystal water content of the polimorf 4) secondary chemical structure 5) pKa value

64. Which factors has importance in facilitated diffusion?

1) carrier molecule 2) chemical energy 3) difference in hydraulic pressure on both side of the membrane 4) concentration gradient 5) competitive inhibition

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3. Associat ions Please, answer the following questions or combine the right letters with the right numbers. 65. How many per cent of the human body’s mass is the

1. extracellular fluid? A) 76 2. interstitial fluid? B) 58 3. plasma water? C) 41 4. total body water (TBW)? D) 17 5. intracellular fluid? E) 13 F) 4

66. Choose the correct unit for each term or sign. 1. ClT A) h-1 2. AUCT B) - 3. bioavailability C) L/h 4. absorbed fraction(f) D) h.mg/L 5. ka E) % F) mg/L

67. Which is the most typical biotransformation reaction of each substance? 1. chloramphenicol A) acid-amid hydrolysis 2. cocaine B) glucuronic acid conjugation 3. sulfonamides C) nitro group reduction 4. steroids D) sulfate conjugation 5. lidocaine E) acetylation F) ester hydrolysis

68. Join the pharmacons with the tissues, organs in which they can be accumulated. 1. thiopental A) liver, nail, skin 2. tetracyclines B) fat 3. iodides C) muscles 4. chloroquine D) growing bones, teeth 5. griseofulvin E) thyroid gland F) liver, pancreas, leukocytes

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69. Which pharmacon and what kind of harm does it do?

1. petidine 2. caffeine 3. hepatotoxic substances 4. salicylates 5. antimetabolites A) serious developmental diseases, abortion B) increasing haemo- philiac liability C) cause(s) no harm D) increasing number of icterus E) depression of the CNS and hypoxia F) damage in liver, icterus

70. Combine the following symbols and their meaning!

A. cumulating factor B. loss factor C. persistency factor D. average steady-state concentration E. fluctuation

71. Combine the transport processes and the drugs (one transport process may be combined with several drugs)!

1. convective transport A. Vitamine B12 2. active transport B. kvarter ammonium

compounds 3. facilitated diffusion C. heart-glycosides 4. ion-pair formation D. ionised sulphonamides 5. pynocitosis E. Vitamine A F. Na+ G. alcohol

72. Which equation describes which transport process?

1. passive diffusion 2. convective transport 3. active transport 4. facilitated diffusion

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73. Which factors are needed for which transport process? (one transport process may be

combined with more factor)

1. passive transport 2. facilitated diffusion 3. convective transport 4. active transport 5. ion-pair formation 6.pynocitosis A. it goes according the concentration gradient B. carrier molecule C. it goes opposite to concentration gradient D. chemical energy (ATP) E. transcellular transport F. paracellular transport G. production of vacuole H. concentration differences on both sides of the memebrane I. hydrostatic pressure difference

74. Sign molecules with A, which produce autoinduction, with B produce foreign induction!

1. probenicide 2. phenobarbitone 3. alcohol 4. griseofulvine 5. phenylbutazone 6. phenytoin 7. meprobamate

75. Combine numbers with capitals, where enzyminductor produces foreign induction!

1. antihistamine A. phenobarbitone 2. meprobamate B. chlortetracycline 3. phenobarbitone C. bilirubin 4. phenylbutazone D. cortisole 5. phenytoine E. aminopyrine F. chloramphenicole G. varfarine

76. Which type of metabolism functionate in which age in children?

1. cysteine conjugation A. just when born 2. glycine conjugation B. from first week 3. sulfation C. 1 month age 4. reduction, oxidization D. 2 months age 5. acetylation E. 3 months age 6. glucuronide conjugation 7. glutamine conjugation

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77. Which enzymes may be found in which juices? (One juice may consist of more

enzymes)

1. mouth A pepsine 2. oesophagus B. trypsine 3. stomach C. amylase 4. duodenum D. ptyaline 5. jejunum E. lipase 6. ileum F. chymotrypsine 7. rectum G. enterocynase H. lactose

78. Combine the numbers and capitals, if K = kl+k3!

A. k1 B. k2 C. k3 D. ka

79. Which compounds eliminated more rapid, if the pH of urine is basic (A) or acidic (B)?

1. acetazolamide 2. amphetamine 3. codeine 4. nalidixic acid 5. morphine 6. chinin 7. nitrofurantoine

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80. Combine the blood level equations with the scheme of blood level curves!

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81. Combine the compartment scheme with blood level curve!

82. Combine the elimination way with compounds! (One elimination rout may suits for

more compounds)

1. kidney A. camphor 2. bile B. ammoniumchloride 3. intestine C. salicylic acid 4. saliva D. strychnine 5. sweet E. Vitamine B1 6. lung F. erythromycine 7. milk G. doxycycline H. digoxin

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83. Combine the numbers with capitals to give the name of transport processes!

A. passive diffusion B. convective transport C. phagocytosis D. facilitated diffusion E. ion-pair mechanism F. active transport

84. What characterise the structure specific molecules (A) and non specific molecules (B)

from the point of view of drug-receptor interaction?

1. pharmacological action is independent of thermodynamic activity (low doses are needed)

2. pharmacological action is highly depend on the thermodynamic activity (high doses are needed)

3. interaction with receptors depends on chemical reactivity, the presence of characteristic functional groups, the same surface has the receptor and the molecule

4. effect highly depends on chemical structure 5. pharmacological effect is the same, inspire the chemical structure is different 6. small changes in chemical structure results in dramatical changes in

pharmacological effect 7. small changes in chemical structure does not alter the effect

85. Combine the numbers with capitals to sign the nature of interaction!

A. food B. receptor C. proteine D. enzymes E. glucuronides

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86. Combine the numbers with capitals!

A. chemical antagonism B. competitive antagonism C. partial antagonism D. no competitive antagonism E. antagonism does not produce steady state l. Drug is substituted on the receptor by another drug. The process is reversible,

amount of the drug in biophase depends on the actual concentration of antagonist. 2. Antagonist molecule has great affinity, but intrinsic activity is law. 3. The agonist and antagonist molecules bind to different receptors and produce

opposit pharmacological effect. 4. Interaction of two different molecules out of receptor results in inactive complex.

87. Combine the numbers with capitals!

A. chemical equivalence B. therapeutic equivalence C. biopharmaceutical equivalence D. pharmaceutical equivalence E. clinical equivalence 1. Dosage form containing the same dose of same active ingredient with the same

chemical structure. The quality and quantity of auxiliary materials are different. 2. The same dosage form containing the same dose of same active ingredient with the

same chemical structure. 3. Dosage form containing the same dose of same active ingredient with the same

chemical structure, which has the same bioavailability. 4. Dosage form containing the same dose of same active ingredient with the same

chemical structure, which has the same therapeutic effect.

88. How does the bioavailabilty change during the processes signed with numbers?

A. enhance B. reduced C. does not change 1. In the case of rapid gastric emptying. 2. Size reduction of particles, when it absorbes from the stomach. 3. Producing a highly water soluble complex from the active ingredient. 4. When the absorption rate constant is lower, than the disintegration and dissolution

of solid dosage form. 5. When the metabolism of the drug enhances, but the metabolite is not active.

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89. Combine the conjugation processes with the molecules, enzymes, to-factors. (One

mechanism may be combined with more factors)

1. glucuronide conjugation A. S-adenosylmethionin 2. sulphate conjugation B. acetylating enzym 3. glutamine conjugation C. Mg, Mn, Co 4. acetylation D. PAPS 5. methylation E. UDPGA 6. glycine conjugation F. coensym A G. acetyltransferase

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4. Relat ion Analysis The sentences below contain a declaration and reasoning. Please, use the letter of one of these statements by each sentence:

A): declaration and reasoning are both true and there is a connection between them B): declaration and reasoning are both true and there is no connection between them C): declaration is true, reasoning is false D): declaration is false, reasoning is true E): declaration and reasoning are both false 90. Steroid hormones are partially excreted by bile but reabsorbed since their ionic form

gets into gut. 91. Insulin is not given per os since it is not absorbed from the large intestine. 92. Acidosis increases alkalosis decreases phenobarbital caused sleeping time because the

distribution of drug is affected by pH. 93. Chloroquine is an effective antimalarial medicine since its concentration in tissues is

hundred times as much as its plasma concentration. 94. Digoxin’s apparent volume of distribution is many times as much as body mass

because a large quantity of the pharmacon accumulates in tissues. 95. Oral antidiabetics are hardly bound to plasma proteins so phenylbutazone increases the

intensity of their effect. 96. Chlorpromazine stimulates the hypnotic effect of barbiturates since it blocks the

microsomal oxydase enzymes in liver. 97. Methylxanthines are not excreted into the breast milk because they are water-soluble. 98. Anticoagulant effect of acenokumarol develops quickly because its absorption is good

from the GI tract. 99. Disulfiram is an effective drug for alcohol detoxication since it stimulates the

metabolism of alcohol in liver. 100. Theophylline’s kinetics of metabolism is first order within the therapeutic interval in

blood. At higher concentrations however, it becomes zero-order because the enzymes that participate in its metabolism are saturated.

101. Oral antidiabetics are usually bound well to plasma proteins so they are suitable to treat

for type II of diabetes mellitus.

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102. Ammonium chloride is given in case of acute amphetamine intoxication because it

acidifies urine and increases urinary elimination of amphetamine significantly. 103. Methylxanthines are eliminated unchanged with urine so their half-life is very short (1-2

hours). 104. There is no big difference in the apparent volume of distribution (950 liters), clearance

(300 ml/min) and elimination half life of digoxin between a fat (90-110 kgs) and an average (~70 kgs) adult. Since the body mass of obese people are greater, it should be taken into consideration when calculating saturating and maintenance dose.

105. 60-80 per cent of kinidine is metabolised in liver because it binds very well to a-1-

glycoproteins. 106. Fat-soluble medicines are hardly absorbed from the surface of skin so systemic effect

can not be produced by drugs that are applied on the skin. 107. Warfarin cure should be started with 10-15 milligrams and after saturation (2-4 days) the

maintenance dose should be set based on prothrombin time since the half-life of warfarin is long.

108. Salts of weak bases are totally dissociated in the gastric juice so they are not reabsorbed

from stomach but they are from the slightly alkaline environment of gut. 109. The change of gastric motility does not influence the Cmax value of the orally given

pharmacon that is absorbed from the small intestine because increase or decrease of motility changes the pharmacon’s velocity of getting into gut.

110. Those molecules pass through the membranes with convective transport which are water

soluble and their molecular weight is between 150-400, while the diameter of pores is between 7-10 A and the viscosity of the liquid determines the rate of transport.

111. Circadian rhythm is controlled by the external biological clock, while the changes of

enzyme activity by day and night synchronises the activity of the organism. 112. Rate of drug absorption during oral administration highly depends on the disintegration

time of solid dosage form and the dissolution rate of drug, while in consecutive processes the rate limiting step is always the slowest one.

113. Drug interactions decrease absorption, while complexes are formed with reduced water

solubility. 114. Application of targeted delivery systems reduce the unwanted side effects, while smaller

amount of drug enters to the organism and it liberates only at the site of action. 115. Methylation is the most important conjugation mechanism, while it requires

methyltransferase enzyme and different to-factors are needed (Mg, Mn, Co etc.). 116. Acetylation does not functionate in new-horns, while the slow and rapid acetylation

ability develops only after 1 year old age.

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117. The dissolution and absorption rate of drugs may significantly elevated by chelate

formation and with the production of solid-solid solutions, while the drug is in a molecularly dispersed form.

118. The amorph form of penicillin G absorbs better than the crystal form, while the

dissolution of crystal molecules requires higher energy. 119. Drug preparations containing sensitive compound for gastric juice and the enterosolvent

coated preparations have to be administered with 250 ml water, while the ice water results quick emptying of stomach, therefore the drug spends shorter time there.

120. Presence of food in stomach delay the absorption of alcohol, while alcohol induce

increased acid secretion. 121. Optimised, controlled release dosage form is able to produce constant blood level during

the required time interval, while the liberation and elimination rates are equal. 122. Retard preparations with zero order liberation kinetic of initial and maintenance doses

provide constant blood level, if the maintenance dose starts to liberate, when the initial dose reaches its maximum.

123. In the oesophagus the absorption of drugs is limited by the transit time, while the

preparations must be taken with high amount of water, to prevent the instant liberation of drug.

124. Value of absorption not always corresponds with the dissociation constant as it is

required, while the anatomy of GI tract, the peristalsis, its physiologically present content serves first of all the ingestion of food and enhance the absorption of food.

125. No absorption takes place in the colon, while there is no peristalsis, and practically there

are no enzymatic processes. 126. In pulmonary absorption an important factor is the state of mucosa, while the inhalasols

provide first of all local effect. 127. The protein binding of morphine is elevated in elderly, while aging generally produced

hypoalbuminaemia. 128. The initial dose is twice as the maintenance dose, while the enhanced first dose produce

immediate effect. 129. On the base of urinary data one can calculate pharmacokinetic parameters, while the

expressed amount of drug excretes via the kidney.

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5. Calculat ions

Please, choose the right result below each exercise or question. 130. Calculate the elimination half life of penicillin if its elimination coefficient is 0.89 h-1.

A. 0.62 h B. 0.78 h C. 2.12 h D. 1.12 h E. 0.89 h

131. Determine the elimination constant of theophylline if the total body clearance is 2.96 L/h and its distribution volume is 37456 mL.

A. 7.903 h-1 B. 0.790 h-1 C. 0.079 h-1 D. 0.008 h-1 E. 1.098 h-1

132. Choose the AUCT value of lidocaine if the intaken dose is 0.2 g and the total body

clearance is 44.54 L/h. A. 4.490 h.mg/L B. 0.004 h.mg/L C. 8.908 h.mg/L D. 8908 h.mg/L E. 44.9 h.mg/L

133. Calculate how many milligrams of lidocaine should be given in infusion hourly if the plateau must be 4mg/L. The total body clearance of lidocaine is 44540 mL/h.

A. 1782 mg/h B. 11.14 mg/h C. 111.4 mg/h D. 178.2 mg/h E. 17.8 mg/h

134. Determine the physiological availability of per os given 20 milligrams of oxoprenolol if AUC

T is 503.6 h.µg/L. Its intravenous value is 618.6 h.µg/L.

A. 81.41 % B. 0.81 % C. 31.15 % D. 68.85 % E. 100.0 %

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135. Calculate the bioavailability of theophylline tablet. 250 milligrams of theophylline

injection’s AUCT is 84.46 h.mg/L. 300 milligrams of theophylline tablet’s AUC

T is

101.35 h.mg/L. A. 83.83% B. 100.0% C. 10.0% D. 90.0% E. 66.6%

136. Calculate the relative bioavailability of chloroquine suppository. AUCT of a 350 mg

tablet is 23.88 h.mg/L and the AUCT of the suppository that has 1050 milligrams of

active compound is 34.08 h.mg/L. A. 33.33% B. 70.07% C. 21.02% D. 47.57% E. 52.43%

137. Determine the renal clearance of gentamicin if the amount of hourly-secreted pharmacon is 12.94 milligrams in urinE) The average plasma concentration in the observed period is 3070 µg/L.

A. 23.7 L/h B. 0.24 L/h C. 4.21 L/h D. 39.27 L/h E. 44.21 L/h

138. Calculate the total body clearance of 0.5 grams of paracetamol’s per os dosage if its AUC

T value is 21.59 h.mg/L and the patient’s factor of liver function is 0.7.

A. 16.21 L/h B. 23.15 L/h C. 262.72 L/h D. 33.16 L/h E. 23.70 L/h

139. Determine the maintenance dose of paracetamol that provides 9 mg/L balanced plasma concentration in case of a per os intake repeated in every 6 hours. The total body clearance of the patient (suffering from liver disease) is 6.945 L/h.

A. 1250 mg B. 540 mg C. 54 mg D. 375 mg E. 7.77 mg

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140. Calculate the excretion rate of meperidine in the kidneys if half-life of the active

compound is 3.2 h in the plasma and 20 per cent is eliminated unmodified with urine. A. 0.032 h-1 B. 0.043 h-1 C. 0.054 h-1 D. 0.065 h-1 E. 0.076 h-1

141. Determine the total body clearance of theophylline where the pharmacon has a 9.6 hour long elimination half time and its distribution volume is 23.85 L.

A. 1.13 L/h B. 1.22 L/h C. 1.49 L/h D. 1.60 L/h E. 1.72 L/h

142. Determine the total body clearance of metoprolol if the pharmacon’s t1/2 value is 3.2 h and its distribution volume is 4.2 L/kg. The patient is 50 kilograms heavy.

A. 65.6 h-1 B. 45.5 L/h C. 3.0 L/kg/h D. 45.5 L/kg/h E. 65.6 L/h

143. A 70-kg heavy person had a phenobarbital overdose. At the first time his blood level had been 90 µg/ml and 5 hours later, it decreased to 63 µg/ml. Calculate the zero order elimination rate if the distribution volume of drug is 1 L/kg.

A. 70 mg/h B. 378 µg/h C. 378 mg/h D. 378 mg/L/h E. 5.4 µg/h

144. Calculate the total body clearance of a pharmacon that was measured in a 52.7-kg heavy patient. The elimination half life based on the plasma concentration change was 0.5744 h. Its distribution volume was 1 L/kg.

A. 63.6 L/kg/h B. 1.27 L/kg/h C. 0.287 L/kg/h D. 14.36 L/h E. 41.4 L/kg/h

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145. Fate of drug in organism when l00 mg dose is administered may be characterised by

open one compartment model. Volume of distribution is 17 litre, biological half life is 1.5 hours. What is the value of AUC0→°°?

a. 1.278 µg/ml·hour b. 4.835 µg/ml·hour c. 12.78 µg/ml·hour

146. What is the clearance value of that drug, which is administered in 250 mg dose,

it distributes immediately in 14.71 litre volume and its elimination rate constant is 0.48 hour-1?

a. 1190 ml/hour b. 119 ml/hour c. 101.9 ml/hour

147. What is the value of biological half life, if cop =88.87 mg/ml and the value of

plasmaconcentration at time t=6 hours is 36.81 mg/ml?

a. 4.7 hours b. 5.3 hours c. 14.7 hours

148. Fate of drug in organism may be characterised by open two compartment model and B=529 mg/ml, α=0.118, cop=2721mg/ml, biological half life is 10.5 hours. What is the value of summarised elimination rate constant (k13)?

a. 1.023 hours-1 b. 10.23 hours-1 c. 0.1023 hours-1

149. Which is the value of time to reach maximal plasma level (tmax) in a patient with

reduced liver function, when the value of biological half life (t1/2) is doubled as the normal (1.5 hours) and the absorption rate constant (ka) is unchanged (2.1 hour-1)?

a. t max (normal) = 9.2 hours t max (reduced) = 11.8 hours b. t max (normal) = 0.92 hours t max (reduced) = 1.18 hours c. t max (normal) = 9.02 hours t max (reduced) = 10.18 hours

150. A patient with renal failure is treated by normal dose (D=200 mg).

The volume of distribution (Vd ) in a normal patient is 1.7 litre, in patient with renal failure is 0.93 litre. The elimination rate constant (kel) of normal patient is 0.086 hour-1. What is the value of kel in patient with reduced function, when its AUC value is five fold that of normal patient?

a. 0.215 hour-1 b. 0.031 hour-1 c. 0.31 hour-1

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151. What is the value of biological half life (t1/2), when A = 26.8 µg/ml, B = 31.5 µg/ml,

maximal plasma concentration (cmax) is 12 µg/ml, time to reach maximal plasma concentration (tmax) is 2.1 hours? The fate of drug may be characterised by open one compartment model.

a. 1.51 hours b. 2.51 hours c. 3.51 hours

152. What is the optimal liberation rate constant in the case of a preparation with zero order dissolution process, when the optimal blood level is 400 mg and the biological half life is 6 hours?

a. 0.464 mg/hour b. 0.146 mg/min c. 46.4 mg/hour

153. Tablet is produced from spairingly soluble material using polyvinil alcohol. The blood level values after administration are as follows:

Time (hour)

1 2 3 5 7 10

Form Plasma levels (µg/ml)

L 0.25 0.37 0.52 0.83 0.52 0.45 Calculate the value of area under blood level us time curve (AUC0→t)using the trapezoid rule, and calculate the value of (AUC0→∞), when cop = 1.77 mg/ml and t1/2 = 3 hours.

a. (AUC0→10)= 50.35 µg/ml·hour (AUC10→∞) =26.30 µg/ml·hour b. (AUC0→10)= 5.035 µg/ml·hour (AUC10→∞) =2.630 µg/ml·hour c. (AUC0→10)= 0.5035 µg/ml·hour (AUC10→∞) =0.263 µg/ml·hour

154. The patient is treated in every 8 hour with 80 mg dose. T volume of distribution is 1.997 litre, biological half life is 2.8 hours. Which doses are needed to reach the same average plasma level, when the same dose is given in every 12 hours (F=0.98)?

a. 100 mg b. 120 mg c. 115 mg

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6. Answer key 1. C 2. C 3. D 4. A 5. E 6. B 7. B 8. E 9. A 10. C 11. D 12. C 13. E 14. B 15. A 16. A 17. C 18. D 19. E 20. C 21. A 22. B 23. C 24. A 25. B 26. D 27. C 28. B 29. E 30. D 31. E 32. D 33. A 34. D 35. C 36. C 37. B 38. A 39. E 40. B 41. D 42. A 43. C 44. E 45. D 46. B 47. E 48. B 49. A 50. A 51. B 52. E 53. C 54. D 55. B

56. C 57. E 58. E 59. D 60. A 61. C 62. D 63. C 64. D 65. 1.D 65. 2.E 65. 3.F 65. 4.B 65. 5.C 66. 1.C 66. 2.D 66. 3.E 66. 4.B 66. 5.A 67. 1.C 67. 2.F 67. 3.D 67. 4.B 67. 5.A 68. 1.B 68. 2.D 68. 3.E 68. 4.F 68. 5.A 69. 1.E 69. 2.D 69. 3.F 69. 4.B 69. 5.A 70. 1.C 70. 2.B 70. 3.A 70. 4.E 71. 1.D 71. 2.C, F 71. 3.A 71. 4.B 71. 5.E 72. 1.B 72. 2.A 72. 3.D 72. 4.D 73. 1.A, E, H 73. 2.A, B, E, H 73. 3.A, F, I 73. 4.B, C, E, D 73. 5.A, E, F 73. 6.E, G 74. 1.A 74. 2.A

74. 3.B 74. 4.B 74. 5.A 74. 6.B 74. 7.A 75. 1.A 75. 2.G 75. 3.C, F 75. 4.E 75. 5.D 76. 1.E 76. 2.E 76. 3.A 76. 4.B 76. 5.C 76. 6.D 76. 7.E 77. 1.D 77. 3.A, E 77. 4.B, C, F, E 77. 5.C 77. 6.E, G 78. 1.D 78. 2.A 78. 3.B 78. 4.C 79. 1.A 79. 2.B 79. 3.B 79. 4.A 79. 5.B 79. 6.B 79. 7.A 80. 1.B 80. 2.A 80. 3.C 80. 4.D 81. 1.B 81. 2.C 81. 3.D 81. 4.A 82. 1.C 82. 2.D 82. 3.G 82. 4.H 82. 5.E 82. 6.A, B 82. 7.F 83. 1.A 83. 2.D 83. 3.B 83. 5.C 83. 6.F 84. 1.A 84. 2.B

84. 3.A 84. 4.A 84. 5.B 84. 6.A 84. 7.B 85. 1.A 85. 2.C 85. 3.D 85. 4.E 85. 5.B 86. 1.B 86. 2.C 86. 3.D 86. 4.A 87. 1.D 87. 2.A 87. 3.C 87. 4.B 88. 1.B 88. 2.A 88. 3.A 88. 4.C 88. 5.B 89. 1.E 89. 2.D 89. 3.B 89. 4.G 89. 5.A, C 89. 6.F 90. C 91. C 92. A 93. B 94. A 95. D 96. C 97. E 98. D 99. C 100. A 101. B 102. A 103. E 104. C 105. B 106. E 107. A 108. A 109. D 110. B 111. C 112. A 113. E 114. A 115. D

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116. C 117. A 118. D 119. A 120. B 121. C 122. A 123. E 124. B 125. E

126. B 127. D 128. D 129. B 130. B 131. C 132. A 133. D 134. A 135. B

136. D 137. C 138. A 139. D 140. B 141. E 142. B 143. C 144. A 145. C

146. B 147. A 148. C 149. B 150. B 151. A 152. C 153. B 154. B