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WorksheetsPharmacokinetic
Total questions: 53
Worksheet time: 27mins
An 18-year-old female patient is brought to the emergency department due to drug overdose. Which of the following routes of administration is the most desirable for administering the antidote for the drug overdose?
Intramuscular
Intravenous
Oral
Subcutaneous
Transdermal
Drug A is a weakly basic drug with a pi<,. of 7.8. If administered orally, at which of the following sites of absorption will the drug be able to readily pass through the membrane?
Mouth (pH approximately 7.0)
Stomach (pH of 2.5)
Duodenum (pH approximately 6.1)
Jejunum (pH approximately 8.0)
Ileum (pH approximately 7.0)
KR2250 is an investigational cholesterol-lowering agent. KR2250 has a high molecular weight and is extensively bound to albumin. KR2250 will have a(n) ______ apparent volume of distribution (Vd)·
High
Low
Extremely high
Normal
A 40-year-old male patient (70 kg) was recently diagnosed with infection invoMng methicillin-resistant S. aureus. He received 2000 mg of vancomycin as an IV loading dose. The peak plasma concentration of vancomycin was 28.5 mg/L. The apparent volume of distribution is:
1 LJkg
7 LJkg
c. 10 LJkg
14 LJkg
70 LJkg
A 55-year-old woman is brought to the emergency department because of seizures. She has a history of renal disease and currently undergoes dialysis. She receives an intravenous infusion of antiseizure Drug X. Which of the following is likely to be observed with use of Drug X in this patient?
A
B
C
D
E
A 68-year-old woman is brought to the emergency department for treatment of a myocardial infarction. She is currently taking clopidogrel (antiplatelet agent) and aspirin daily, as well as omeprazole (potent CYP inhibitor) for heartburn. Which of the following is the most likely contributor to her myocardial infarction today?
Reduced antiplatelet activity of clopidogrel due to aspirin
Reduced antiplatelet activity of clopidogrel due to omeprazole
Hypersensitivity reaction due to clopidogrel
Increased antiplatelet activity of clopidogrel due to omeprazole
Increased antiplatelet activity of clopidogrel due to aspirin
Which of the following reactions represents Phase II of drug metabolism?
Amidation
Hydrolysis
Oxidation
Reduction
Sulfation
A pharmacokinetic study of a new antihypertensive drug is being conducted in healthy human volunteers. The half-life of the drug after administration by continuous intravenous infusion is 12 hours. Which of the following best approximates the time for the drug to reach steady state
24 hr.
48hr.
72hr
120hr
240hr
A 64-year-old female patient (60 kg) is treated with experimental Drug A for type 2 diabetes. Drug A is available as tablets with an oral bioavailability of 90%. If the vd is 2 L1kg and the desired steady-state plasma concentration is 3.0 mg/L, which of the following is the most appropriate oral loading dose of Drug A
6mg
6.66mg
108mg
360mg
400mg
A 74-year-old man was admitted to the hospital for treatment of heart failure. He received 160 meg of digoxin intravenously, and the plasma digoxin level was 0.4 ng/ mL. If the desired plasma concentration of digoxin for optimal therapeutic activity in heart failure is 1.2 nglml, and the patient has an estimated V d of 400 L, calculate the additional dose of digoxin needed for this patient to achieve the desired plasma concentration.
128 meg
160
320
480
640meg
Pharmacokinetics is
The study of biological and therapeutic effects of drugs
The study of absorption, distribution, metabolism and excretion of drugs
The study of mechanisms of drug action
The study of methods of new drug development
What does “pharmacokinetics” include
Complications of drug therapy
Drug biotransformation in the organism
Influence of drugs on metabolism processes
Influence of drugs on genes
What does “pharmacokinetics” include
Pharmacological effects of drugs
Unwanted effects of drugs
Chemical structure of a medicinal agent
Distribution of drugs in the organism
What does “pharmacokinetics” include
Localization of drug action
Mechanisms of drug action
Excretion of substances
Interaction of substances
The main mechanism of most drugs absorption in GI tract is
Active transport (carrier-mediated diffusion)
Filtration (aqueous diffusion)
Endocytosis and exocytosis
Passive diffusion (lipid diffusion)
What kind of substances can’t permeate membranes by passive diffusion
Lipid-soluble
Non-ionized substances
Hydrophobic substances
Hydrophilic substances
A hydrophilic medicinal agent has the following property
Low ability to penetrate through the cell membrane lipids
Penetrate through membranes by means of endocytosis
Easy permeation through the blood-brain barrier
High reabsorption in renal tubules
What is implied by «active transport»
Transport of drugs trough a membrane by means of diffusion
Transport without energy consumption
Engulf of drug by a cell membrane with a new vesicle formation
Transport against concentration gradient
What does the term “bioavailability” mean
Plasma protein binding degree of substance
Permeability through the brain-blood barrier
Fraction of an uncharged drug reaching the systemic circulation following any route administration
Amount of a substance in urine relative to the initial doze
The reasons determing bioavailability are
Rheological parameters of blood
Amount of a substance obtained orally and quantity of intakes
Extent of absorption and hepatic first-pass effect
Glomerular filtration rate
Pick out the appropriate alimentary route of administration when passage of drugs through liver is minimized
Oral
Transdermal
Rectal
Intraduodenal
Which route of drug administration is most likely to lead to the first-pass effect
sublingual
oral
IV
IM
What is characteristic of the oral route
Fast onset of effect
Absorption depends on GI tract secretion and motor function
A drug reaches the blood passing the liver
The sterilization of medicinal forms is obligatory
Tick the feature of the sublingual route
Pretty fast absorption
A drug is exposed to gastric secretion
A drug is exposed more prominent liver metabolism
A drug can be administrated in a variety of doses
Pick out the parenteral route of medicinal agent administration
Rectal
Oral
Sublingual
Inhalation
Parenteral administration
Cannot be used with unconsciousness patients
Generally results in a less accurate dosage than oral administration
Usually produces a more rapid response than oral administration
Is too slow for emergency use
What is characteristic of the intramuscular route of drug administration
Only water solutions can be injected
Oily solutions can be injected
) Opportunity of hypertonic solution injections
The action develops slower, than at oral administration
Intravenous injections are more suitable for oily solutions
true
false
Correct statements listing characteristics of a particular route of drug administration include all of the followingEXCEPT
Intravenous administration provides a rapid response
Intramuscular administration requires a sterile technique
Inhalation provides slow access to the general circulation
Subcutaneous administration may cause local irritation
Most of drugs are distributed homogeneously
true
fales
Biological barriers include all except:
Renal tubules
Cell membranes
Capillary walls
Placenta
What is the reason of complicated penetration of some drugs through brain-blood barrie
High lipid solubility of a drug
Meningitis
Absence of pores in the brain capillary endothelium
High endocytosis degree in a brain capillary
The volume of distribution (Vd) relates
Single to a daily dose of an administrated drug
An administrated dose to a body weight
An uncharged drug reaching the systemic circulation
The amount of a drug in the body to the concentration of a drug in plasma
For the calculation of the volume of distribution (Vd) one must take into account
Concentration of a substance in plasma
Concentration of substance in urine
Therapeutical width of drug action
A daily dose of drug
A small amount of the volume of distribution is common for lipophylic substances easy penetrating through barriersandwidely distributing in plasma, interstitial and cell fluids
true
false
The term “biotransformation” includes the following
Accumulation of substances in a fat tissue
Binding of substances with plasma proteins
Accumulation of substances in a tissue
Process of physicochemical and biochemical alteration of a drug in the body
Biotransformation of the drugs is to render them
Less ionized
More pharmacologically active
More lipid soluble
Less lipid soluble
Tick the drug type for which microsomal oxidation is the most prominent
Lipid soluble
Water soluble
Low molecular weight
High molecular weight
Pick out the right statemen
Microsomal oxidation always results in inactivation of a compound
Microsomal oxidation results in a decrease of compound toxicity
Microsomal oxidation results in an increase of ionization and water solubility of a drug
Microsomal oxidation results in an increase of lipid solubility of a drug thus its excretion from the organismis facilitated
Stimulation of liver microsomal enzymes can
Require the dose increase of some drugs
Require the dose decrease of some drugs
Prolong the duration of the action of a drug
Intensify the unwanted reaction of a drug
Metabolic transformation (phase 1) is
Acetylation and methylation of substances
Transformation of substances due to oxidation, reduction or hydrolysis
Glucuronide formation
Binding to plasma proteins
Biotransformation of a medicinal substance results in
Faster urinary excretion
Slower urinary excretion
Easier distribution in organism
Higher binding to membranes
Conjugation is
Process of drug reduction by special enzymes
Process of drug oxidation by special oxidases
Coupling of a drug with an endogenous substrate
Solubilization in lipids
Which of the following processes proceeds in the second phase of biotransformation
Acetylation
Reduction
Oxidation
Hydrolysis
Conjugation of a drug includes the following EXCEPT
Glucoronidation
Sulfate formation
Hydrolysis
Methylation
Metabolic transformation and conjugation usually results in an increase of a substance biological activity
true
false
In case of liver disorders accompanied by a decline in microsomal enzyme activity the duration of action of somedrugsis
Decreased
Enlarged
Remained unchanged
Changed insignificantly
Half life (t ½) is the time required to
Change the amount of a drug in plasma by half during elimination
Metabolize a half of an introduced drug into the active metabolite
Absorb a half of an introduced drug
Bind a half of an introduced drug to plasma proteins
Half life (t ½) doesn’t depend on
Biotransformation
Time of drug absorption
Concentration of a drug in plasma
Rate of drug elimination
Elimination is expressed as follows
) Rate of renal tubular reabsorption
Clearance speed of some volume of blood from substance
Time required to decrease the amount of drug in plasma by one-half
Clearance of an organism from a xenobiotic
Elimination rate constant (Kelim) is defined by the following paramete
Rate of absorption
Maximal concentration of a substance in plasma
Highest single dose
Half life (t ½
Systemic clearance (CLs) is related with
Only the concentration of substances in plasma
Only the elimination rate constant
Volume of distribution, half life and elimination rate constant
Bioavailability and half life
The most rapid eliminated drugs are those with high glomerular filtration rate and actively secreted but aren’t passivelyreabsorbed:
false
true
