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BIOPHARMACEUTICS & PHARMACOKINETICS PART 3

Total questions: 104

Worksheet time: 52mins

Name
Class
Date
1.

Accumulation is dependent upon which of the following factors

a)

Blood flow

b)

Affinity for the drug

c)

Colloidal osmotic

d)

A & B only

e)

A & C only

2.

A term defined as the combination of a drug molecule with a receptor

a)

Antagonism

b)

Intrinsic activity

c)

Affinity

d)

Efficacy

3.

The force of attraction which binds drugs to albumin

a)

Van der Waals

b)

Hydrophobic bond

c)

Hydrogen bond

d)

All of the above

4.

The prerequisites of the binding of a drug to a receptor are as follows, EXCEPT:

a)

Chemical reactivity

b)

Electronic distribution

c)

Absence of functional group

d)

None of the above

5.

A site in the biophase to which drug molecules can be bound is

a)

Fluid compartment

b)

Unit membrane

c)

Receptor

d)

None of the above

6.

Receptors are macromolecules that

a)

Are designed to attract drugs

b)

Resistant to antagonists

c)

Exist as targets for physiological neurotransmitters and hormones

d)

Only on the outer surface of cells

e)

Only inside of cells

7.

A cell or a cell component where the final interaction between drug and receptor takes place

a)

Receptor

b)

Biophase

c)

Unit membrane

d)

Ligand

e)

All

8.

A property of drug which has an affinity and generate an impulse with a receptor

a)

Antagonism

b)

Intrinsic activity

c)

Affinity

d)

Ligand binding

9.

Drugs in which the pharmacological action depends directly on the chemical structure of the drug

a)

Structure specific drugs

b)

Structure nonspecific drugs

c)

Drug agonist

d)

None of the above

10.

A theory which states that effectiveness lasts as long as the receptor is occupied

a)

Hypothesis of Paton

b)

Lock and Key hypothesis

c)

Hypothesis of Ariens and Stephenson

d)

Hypothesis of Clark

11.

A theory which states the effectiveness does not depend on the actual occupation of receptor by the drug, but upon obtaining the proper stimulus

a)

Hypothesis of Paton

b)

Hypothesis of Ariens and Stephenson

c)

Hypothesis of Clark

d)

Lock and Key hypothesis

12.

A theory which advances the idea that maximum pharmacologic effect can be obtained if all the receptors are occupied

a)

Hypothesis of Paton

b)

Hypothesis of Ariens and Stephenson

c)

Lock and Key hypothesis

d)

Hypothesis of Clark

13.

Drugs are usually released much more slowly from fat because

a)

Fat has relatively limited blood supply

b)

Drugs are fat bound than plasma bound

c)

Fat bound drugs bind to itself more

d)

All of the above

14.

Anesthetics are highly lipid soluble drugs which are stored in which body tissues?

a)

Albumin

b)

Adipose

c)

Globulin

d)

Muscle

e)

Neurons

15.

Which of the following statements concerning hydrostatic pressure and absorptive pressure is true?

a)

Represents a pressure gradient between the arterial end of the capillaries entering the tissue and the venous capillaries leaving the tissue

b)

Responsible for the penetration of relatively ionized drugs

c)

Allows small drug molecules to be filtered at the glomerulus

d)

All

16.

Maintenance of a steady state which characterized the interval environment of the healthy organism?

a)

Steady state

b)

Depot phase

c)

Homeostasis

d)

Maintenance dose

17.

The protein binding of a drug is defined by

a)

Absorption constant

b)

Affinity constant

c)

Distribution equilibrium

d)

All of the choices

18.

The extent of protein binding is determined in vitro by the following mechanisms, EXCEPT:

a)

Ultracentrifugation

b)

Dialysis

c)

Endocytosis

d)

Electrophoresis

19.

Distribution of drugs to specific tissues

a)

Independent of blood flow to the organ

b)

Independent of the solubility of the drug in that tissue

c)

Depends on the unbound drug concentration gradient between blood and the tissue

d)

Increased for drugs that are strongly bound to plasma proteins

e)

Has no effect on the half-life of the drug

20.

Loss of drug from central compartment due to transfer into other compartments and/or elimination or metabolism

a)

Dosage regimen

b)

Disposition

c)

Depot phase

d)

Creatinine clearance

e)

Circadian rhythm

21.

The sum of all body regions in which the drug concentration is in instantaneous equilibrium with that in blood or plasma

a)

Clearance

b)

Accumulation

c)

Depot phase

d)

Central compartment

22.

All the following refers to the sum of all body regions to which a drug eventually distributes, but is not in instantaneous equilibrium, except

a)

Bone

b)

Small intestine

c)

Kidney

d)

Skin

e)

Adipose tissue

23.

At diffusion equilibrium, the concentrations of a drug in the various body compartments are usually not equal because

a)

All body compartments are not equal in size and weight

b)

Those compartments closed to the absorption site/s will be absorb most of the drug

c)

The CNS is a body compartment that usually does not accumulate drugs

d)

Most drugs end up in the urine

e)

The various compartments are not equally accessible to the drug nor do they have equal affinities for it.

24.

A drug can exert its pharmacologic effect only when it is

a)

Protein bound

b)

Protein unbound

c)

Free drug

d)

B and C

25.

To produce its characteristic pharmacologic effect a drug must always

a)

Reach high blood levels

b)

Be absorbed from the GIT

c)

Achieve adequate concentration at the site(s) of action

d)

Be excreted unchanged in the urine

26.

Percentage of Free, Unbound or nonprotein-bound drug depends on all the following, EXCEPT:

a)

Drug concentration

b)

Affinity for binding sites

c)

Amount of plasma proteins available for binding

d)

None

27.

Which of the ff is TRUE about free drugs?

a)

Pharmacologically inactive

b)

Unavailable for metabolism

c)

Non Diffusible

d)

Available for action

28.

If salicylates have greater affinity to plasma protein than bilirubin, what will be the consequence of taking the salicylates?

a)

Increase plasma concentration of bilirubin

b)

Salicylates will be displaced by bilirubin

c)

Increase pharmacological effects of salicylates

d)

All statements apply

29.

The equilibrium between free and bound drug acts as

a)

An equilibrium system

b)

A buffer system

c)

A transport system

d)

Way of releasing the bound drug

30.

Plasma protein binding is of significant influence on the distribution equilibrium if the drug is

a)

Polar drug

b)

Nonpolar drug

c)

Oil soluble drug

d)

Lipid soluble drug

e)

All of the above

31.

All of the following are macromolecules that participate in drug protein binding, EXCEPT

a)

Albumin

b)

Alpha 1-acid glycoprotein

c)

Lipoprotein

d)

Ceruloplasmin

e)

None

32.

The major plasma protein involved in the distribution of weak acids is

a)

Albumin

b)

Alpha acid glycoprotein

c)

Glycine

d)

VLDL

e)

LDL

33.

Alpha-1-glycoprotein binds with

a)

Acidic, highly lipophilic drugs

b)

Acidic, highly lipophobic drugs

c)

Basic, highly lipophilic drugs

d)

Basic, highly lipophobic drugs

34.

All of the following statements concerning drug plasma protein binding are true, EXCEPT

a)

Aspirin generally bind to plasma albumin

b)

Quinidine more often bind to lipoproteins and acid glycoproteins

c)

For most drugs, the ratio of bound : free drug increases as the dose increases throughout the therapeutic range

d)

Binding site on plasma proteins are nonselective and drugs compete for these limited site

35.

Which of the following is correct?

a)

Reduced binding to plasma protein by the drug molecule will decrease the therapeutic effect of the drug

b)

Saturation of binding procedures linear pharmacokinetics

c)

Bound drugs can diffuse into the tissues

d)

Only the unbound drug may be available for metabolism

36.

The displacement of drug from protein binding site causes

a)

Decrease in the intensity of pharmacologic response

b)

Decrease in the intensity of side effects

c)

Toxicity

d)

All of the above

37.

he protein binding has the following characteristics, except

a)

Selective

b)

. Pharmacologically active

c)

Reversible

d)

specific

38.

Distribution of drugs to tissues depends on all the following, EXCEPT:

a)

Depends on blood flow and size of the organ

b)

Depends on the solubility of the drug in that tissue

c)

Depends on the concentration gradient between blood and tissue

d)

Is increased for drugs that are strongly bound to plasma proteins

39.

All of the following are true concerning drug distribution except

a)

Fenestrations in brain capillaries constitute a blood-brain barrier

b)

A hydrophobic drug given IV would be distributed more rapidly to the brain than to adipose tissue

c)

A drug that is weak base will become trapped in the stomach

d)

A hydrophilic IV drug would be distributed rapidly to the kidneys

e)

Closed capillaries limit drug distribution more than open capillaries

40.

Which of the following factors does not affect the protein binding of drugs?

a)

The availability of protein for binding

b)

The presence of competing substance for protein binding

c)

Binding affinity of protein to the drug

d)

The concentration of a drug at its receptor site

e)

None of the above

41.

The following are factors that control plasma protein concentrations, EXCEPT:

a)

Protein synthesis

b)

Distribution from interstitial to extracellular spaces

c)

Elimination from the body

d)

Diseases

e)

None

42.

The following pathological state influences the volume of distribution, EXCEPT

a)

Renal disease

b)

Hepatic disease

c)

Cardiac insufficiency

d)

Vertigo

43.

Which of the following conditions most likely increased plasma protein albumin concentration?

a)

Severe burns

b)

Cystic fibrosis

c)

Trauma

d)

Hypothyroidism

44.

When can absorption of a drug be slower than its elimination?

a)

When drugs are rapidly metabolized or excreted

b)

When drugs are poorly soluble in water

c)

When drugs are soluble in fats & oils

d)

A and B

45.

In drug metabolism, which of the following is true

a)

It is often termed detoxification or detoxification

b)

It refers solely to the chemical biotransformation of a drug by the biological environment

c)

Both

d)

None of the choices

46.

The breakdown of ingested foreign compounds to simpler structures

a)

Catabolism

b)

Anabolism

c)

Homeostasis

d)

None of the above

47.

Biotransformation of orally administered drugs occurring primarily in the liver that reduces the amount of drug finally entering the systemic circulation is often referred to as _

a)

Enterohepatic recirculation

b)

Gastric emptying

c)

Elimination

d)

First-pass effect

e)

Enzyme inductionEnzyme induction

48.

Biotransformation of a drug takes place in the liver in the presence of

a)

Energy from the body

b)

Enzymes which act as catalysts

c)

Substance destroyed in the liver

d)

A and C

49.

Patients who are poor Debrisoquine metabolizers have decreased activity of which enzyme system

a)

CYP 1A2

b)

CYP 2C9

c)

CYP 2D6

d)

CYP 2C19

e)

CYP 3A4

50.

Inactive enzymes are called

a)

Zymogens or Proenzymes

b)

HaloenzymesHaloenzymes

c)

Apoenzymes

d)

All of the choices

51.

The purpose of biotransformation reaction is

a)

Deactivate the drug

b)

Preserve the drug from destruction

c)

Promote elimination of the inactive drug

d)

A and C

52.

The metabolism of drugs generally results in

a)

Less acidic compounds

b)

More acidic compounds

c)

More polar compounds

d)

Compounds having a higher oil/water partition coefficient

53.

The metabolism of drugs generally results in

a)

less basic compounds

b)

highly protein bound drug

c)

more acidic compound

d)

highly ionized species

54.

The rate of metabolic processes depend on

a)

Absorption in gastric juice

b)

Drug concentration at a given time

c)

Presence of another drug

d)

Food interaction

55.

The principal site of drug metabolism is

a)

Kidney

b)

Muscle tissue

c)

Gut wall

d)

Liver

e)

Skin

56.

All the following are sites of drug metabolism except

a)

heart

b)

liver

c)

kidney

d)

skin

e)

Plasma

57.

Metabolites can have the following properties except

a)

Produce therapeutic activity

b)

Cannot produce toxicity

c)

Can be reactivated

d)

Can be in its inactive form

58.

Which of the following is true about metabolic pathways?

a)

transformation of an active drug into inactive form

b)

a prodrug converted into a more active form

c)

an active drug transform into a more toxic metabolite

d)

all

59.

The parent compound of morphine is

a)

phenylbutazone

b)

codeine

c)

acetyl salicylic acid

d)

amitriptyline

60.

An example of commercial drug that can be activated into a reactive metabolite upon chronic dosing is

a)

Lasix

b)

Geocillin

c)

Valium

d)

Tempra

61.

Phenylacetone is an inactive metabolite of

a)

Phenobarbital

b)

Salicylic acid

c)

Amphetamine

d)

Codeine

62.

An inactive or much less active substance which is transformed to active drug in the body is

a)

Dosage form

b)

Drug product

c)

Reactive drug

d)

Prodrug

63.

The term “prodrug” refers to

a)

Chemical substance that is part of the synthesis of another drug

b)

Compound that liberates an active drug in the body

c)

Compound which may be therapeutically active but is still under clinical trials

d)

Drug that is classified as being “probably effective”

64.

A drug molecule that does not possess biologic activity by itself but is converted in the body to an active metabolite is called a/an

a)

Orphan drug

b)

Prodrug

c)

Prototype drug

d)

Parent drug

e)

Metabolic drug

65.

The following are the common drug metabolic reactions, except

a)

Oxidation

b)

Carboxylation

c)

Reduction

d)

Conjugation

66.

Which of the ff is a phase II biotransformation reaction?

a)

sulfoxide formation

b)

nitro reduction

c)

ester hydrolysis

d)

sulfate conjugation

67.

“A group of iron-containing isoenzymes that activate molecular oxygen to a form capable of interacting with organic substrates.” The component of microsomal mixed-function oxidase system which this description is most closely associated

a)

Cyclooxygenase

b)

Cytochrome

c)

ATP

d)

NADPH

68.

W/c of the ff. is a synthetic reaction?

a)

O-dealkylation

b)

amide hydrolysis

c)

ketone reduction

d)

N-methylation

69.

The addition of glucuronic acid to a drug

a)

decreases its water solubility

b)

occurs at the same rate in adults and the newborn

c)

usually leads to inactivation of the drug

d)

involves CYT P-450

70.

The enzyme that catalyzes the amino acid conjugation reaction include

a)

glucuronyl transferase

b)

sulfotransferases

c)

methyltransferase

d)

coenzyme

71.

A Conjugation reaction often associated with drug toxicity include

a)

Acetylation

b)

Mercapturine acid conjugation

c)

Methylation

d)

Glucuronidation

e)

A AND B

72.

The synthetic degradation mechanism of drug in the GI tract is

a)

hydrolysisoxidation

b)

oxidation

c)

acetylation

d)

reduction

73.

All the following is true about acetylated product of sulfanilamide except

a)

delayed urinary excretion

b)

prolonged elimination half-life

c)

Less polar

d)

more hydrophilic than the parent compound

74.

Which one of the following statements is incorrect?

a)

Conjugation (phase 2) reactions involving drugs or their metabolites are not mediated by the cytochrome P-450 system in the liver

b)

Metabolism of a drug usually decreases its lipid solubility

c)

The extent to which a drug is bound to plasma proteins is not directly predictive of its rate of renal excretion

d)

For drug with first-order elimination kinetics, a constant amount of drug is lost per unit time

e)

For drugs with zero-order elimination kinetics, the relationship between drug dosage and maximally attained plasma concentration is nonlinear

75.

Substance useful for the protection of the cell against reactive electrophilic compounds

a)

sulfate

b)

glucuronic acid

c)

glutathione

d)

acetyl CoA

76.

Which of the following may lower the binding capacity of drugs during conjugation reactions?

a)

Limited amount of conjugating agent

b)

Defective process among newborn

c)

Genetic polymorphism

d)

Limited ability to synthesize the active nucleotide intermediate E. Limited amount of the conjugate transferase

e)

AOTA

77.

Chloramphenicol when given to a neonate or premature baby causes cardiovascular collapse manifesting as the so-called “gray baby syndrome”. This toxicity in such subsets of patients is due to what age-related biologic feature?

a)

Decreased protein binding

b)

Decreased urinary excretion of the metabolite

c)

Deficiency of glucuronosyl acyl transferase

d)

Increased metabolism by nitro-reduction

78.

The biological half-life of many drugs is often prolonged in newborn infants because of

a)

A higher decrease of protein binding

b)

Microsomal enzyme induction

c)

More complete absorption of drugs

d)

Incompletely developed enzyme syst

79.

An anti peptic ulcer agent causing enzyme inhibition include

a)

Benzopyrene

b)

Phenobarbital

c)

Cimetidine

d)

Thiopental

80.

Astemizole and Terfenadine have been withdrawn from the market because of their intrinsic cardiotoxicity. The risk of cardiotoxicity is increased with concomitant intake of grapefruit juice or erythromycin. The explanation for this interaction is

a)

Displacement from the protein binding

b)

Decreased urinary excretion

c)

Inhibition of the CYP3A4 enzyme

d)

Increased absorption e. Induction of metabolism

81.

Cimetidine, ketoconazole, and allopurinol share a common pharmacokinetic property that predisposes patients taking other drugs concomitantly with any of these agents to toxicity. What is this property?

a)

Inhibition of tubular secretion

b)

Increased systemic absorption

c)

Enzyme induction

d)

Enzyme inhibition

e)

Protein binding

82.

If phenobarbital stimulates metabolism of warfarin, the phenomenon is called

a)

cross induction

b)

auto-induction

c)

foreign induction

d)

both a and b

83.

1. What is the effect of inducing the microsomal metabolizing enzyme system?

a)

slow metabolism

b)

reduced rate of metabolism

c)

increase rate of metabolism

d)

inhibited metabolism

84.

Enzyme inhibition results to

a)

incr metabolic rate

b)

faster elimination rate

c)

prolong pharmacologic effect

d)

decrease clinical effect

85.

Phenomenon that drug emptied via bile into the small intestine can be reabsorbed from the intestinal lumen into systemic circulation

a)

Biliary recycling

b)

Urinary recycling

c)

Systemic absorption

d)

Enterohepatic recirculation

e)

A and D only

86.

Reabsorption of drugs or its metabolites occurs in

a)

Heart

b)

Small intestines

c)

Lungs

d)

Brain

e)

Stomach

87.

Biliary recycling is influenced by the following except

a)

Rate of excretion of drug into the bile

b)

Rate of loss of drug with feces

c)

Type of food intakeType of food intake

d)

Rate of a absorption of the drug

e)

None of the above

88.

It refers to the irreversible removal of drug from the body by all routes

a)

Disposition

b)

Elimination

c)

Distribution

d)

Absorption

e)

Metabolism

89.

The final elimination from the body’s systemic circulation via the kidney into the urine, via bile, and saliva into intestines and into feces, via sweat, via skin, via milk

a)

Metabolism

b)

Distribution

c)

Absorption

d)

Excretion

90.

The termination of action of a drug is determined by

a)

Excretion of intact active molecule

b)

Excretion of inactive molecule

c)

Tissue redistribution

d)

A and C

91.

The least significant organ for excretion is the

a)

Kidneys

b)

Rectum

c)

Mammary gland

d)

Salivary gland

e)

Sebaceous gland

92.

The major pathway of excretion

a)

Via the liver

b)

Via the kidney

c)

Via the circulation system

d)

Via the large intestines

93.

Major mechanisms in determining the excretion of drugs via the kidney include all, EXCEPT

a)

Glomerular filtration

b)

Protein binding

c)

Tubular reabsorption

d)

Tubular secretion

e)

Pinocytosis

94.

A phenomenon that occurs when drugs filtered through the glomeruli are reabsorbed from the tubule into the systemic circulation

a)

Urinary recycling

b)

Biliary recycling

c)

Reabsorption

d)

A and B

95.

Renal clearance depends on

a)

Urinary pH

b)

Glomerular filtration

c)

Absorption

d)

Distribution

96.

9. Is the hypothetical volume of distribution in mL of the unmetabolized drug which is cleared per unit of time by any pathway of drug removal

a)

Diffusion layer

b)

Diurnal variation

c)

Clearance

d)

Clinical pharmacokinetics

e)

None

97.

Characterizes the clearing of the hypothetical plasma volume of a drug per unit of time or the capacity of the body to eliminate the drug after it has reached the general circulation is reflected by

a)

Hepatic clearance

b)

Renal clearance

c)

Total clearance

d)

Intrinsic clearance

e)

Genital clearance

98.

The hypothetical plasma volume in mL of the unmetabolized drug which is cleared in one minute via the kidney

a)

Volume of distribution

b)

Renal clearance

c)

Total clearanceArea under the curve

d)

Area under the curve

e)

Hepatic clearance

99.

The ratio of creatinine excreted in urine to the concentration of creatinine in plasma

a)

Creatinine concentration

b)

Creatinine excretion

c)

Creatinine clearance

d)

Renal clearance

100.

Cholekinesis is a process which involves the

a)

Formation of bile in the liver

b)

Formation of bile from the gallbladder

c)

Emptying of bile from the gallbladder

d)

Emptying of bile from the liver

101.

Reabsorption of the drugs and its metabolites occurs in the

a)

Kidney

b)

Intestines

c)

Stomach

d)

Both A and B

e)

None of the above

102.

The function of bile and bile salts is

a)

Solubilize the drug molecules after a meal

b)

Solubilize fatty/oily substances

c)

Dissolves inorganic salts

d)

A and B.

103.

The magnitude of bile production depends on

a)

Type of food

b)

The amount of bile emptied

c)

The enzyme activity

d)

All of the above

104.

Biliary excretion principle

a)

Through the bile duct into duodenum

b)

Major portion of bile is excreted

c)

As metabolite

d)

Any of the above

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