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Pharmacokinetics is:
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The study of biological and therapeutic effects of drugs
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The study of absorption, distribution, metabolism and excretion of drugs
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The study of mechanisms of drug action
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The study of methods of new drug development
Frage 2
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What does “pharmacokinetics” include?
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Complications of drug therapy
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Drug biotransformation in the organism
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Influence of drugs on metabolism processes
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Influence of drugs on genes
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What does “pharmacokinetics” include?
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Pharmacological effects of drugs
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Unwanted effects of drugs
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Chemical structure of a medicinal agent
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Distribution of drugs in the organism
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The main mechanism of most drugs absorption in GI tract is:
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Active transport (carrier-mediated diffusion)
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Filtration (aqueous diffusion)
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Endocytosis and exocytosis
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Passive diffusion (lipid diffusion)
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What kind of substances can’t permeate membranes by passive diffusion?
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Lipid-soluble
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Non-ionized substances
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Hydrophobic substances
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Hydrophilic substances
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A hydrophilic medicinal agent has the following property:
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Low ability to penetrate through the cell membrane lipids
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Penetrate through membranes by means of endocytosis
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Easy permeation through the blood-brain barrier
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High reabsorption in renal tubules
Frage 7
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What is implied by «active transport»?
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Transport of drugs trough a membrane by means of diffusion
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Transport without energy consumption
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Engulf of drug by a cell membrane with a new vesicle formation
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Transport against concentration gradient
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What does the term “bioavailability” mean?
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Plasma protein binding degree of substance
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Permeability through the brain-blood barrier
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Fraction of an uncharged drug reaching the systemic circulation following any route administration
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Amount of a substance in urine relative to the initial doze
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The reasons determining bioavailability are:
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Rheological parameters of blood
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Amount of a substance obtained orally and quantity of intakes
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Extent of absorption and hepatic first-pass effect
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Glomerular filtration rate
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Pick out the appropriate alimentary route of administration when passage of drugs through liver is minimised:
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Oral
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Transdermal
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Rectal
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Intraduodenal
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Which route of drug administration is most likely to lead to the first-pass effect?
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Sublingual
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Oral
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Intravenous
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Intramuscular
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What is characteristic of the oral route?
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Fast onset of effect
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Absorption depends on GI tract secretion and motor function
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A drug reaches the blood passing the liver
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The sterilisation of medicinal forms is obligatory
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Tick the feature of the sublingual route:
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A drug has a pretty fast absorption
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A drug is exposed to gastric secretion
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A drug is exposed more prominent liver metabolism
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A drug can be administrated in a variety of doses
Frage 14
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Pick out the parenteral route of medicinal agent administration:
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Rectal
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Oral
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Sublingual
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Inhalation
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Parenteral administration:
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Cannot be used with unconsciousness patients
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Generally results in a less accurate dosage than oral administration
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Usually produces a more rapid response than oral administration
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Is too slow for emergency use
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What is characteristic of the intramuscular route of drug administration?
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Only water solutions can be injected
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Oily solutions can be injected
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Opportunity of hypertonic solution injections
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The action develops slower, than at oral administration
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Intravenous injections are more suitable for oily solutions:
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Correct statements listing characteristics of a particular route of drug administration include all of the following EXCEPT:
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Intravenous administration provides a rapid response
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Intramuscular administration requires a sterile technique
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Inhalation provides slow access to the general circulation
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Subcutaneous administration may cause local irritation
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Most of drugs are distributed homogeneously.
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Biological barriers include all except:
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Renal tubules
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Cell membranes
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Capillary walls
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Placenta
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What is the reason of complicated penetration of some drugs through brain-blood barrier?
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High lipid solubility of a drug
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Meningitis
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Absence of pores in the brain capillary endothelium
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High endocytosis degree in a brain capillary
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The volume of distribution (Vd) relates:
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Single to a daily dose of an administrated drug
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An administrated dose to a body weight
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An uncharged drug reaching the systemic circulation
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The amount of a drug in the body to the concentration of a drug in plasma
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For the calculation of the volume of distribution (Vd) one must take into account:
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Concentration of a substance in plasma
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Concentration of substance in urine
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Therapeutical width of drug action
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A daily dose of drug
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A small amount of the volume of distribution is common for lipophylic substances easy penetrating through barriers and widely distributing in plasma, interstitial and cell fluids:
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The term “biotransformation” includes the following:
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Accumulation of substances in a fat tissue
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Binding of substances with plasma proteins
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Accumulation of substances in a tissue
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Process of physicochemical and biochemical alteration of a drug in the body
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Biotransformation of the drugs is to render them:
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Tick the drug type for which microsomal oxidation is the most prominent:
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Lipid soluble
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Water soluble
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Low molecular weight
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High molecular weight
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Pick out the right statement:
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Microsomal oxidation always results in inactivation of a compound
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Microsomal oxidation results in a decrease of compound toxicity
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Microsomal oxidation results in an increase of ionization and water solubility of a drug
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Microsomal oxidation results in an increase of lipid solubility of a drug thus its excretion from the organism is facilitated
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Stimulation of liver microsomal enzymes can:
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Require the dose increase of some drugs
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Require the dose decrease of some drugs
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Prolong the duration of the action of a drug
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Intensify the unwanted reaction of a drug
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Metabolic transformation (phase 1) is:
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Acetylation and methylation of substances
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Transformation of substances due to oxidation, reduction or hydrolysis
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Glucuronide formation
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Binding to plasma proteins
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Biotransformation of a medicinal substance results in:
Frage 32
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Process of drug reduction by special enzymes
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Process of drug oxidation by special oxidases
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Coupling of a drug with an endogenous substrate
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Solubilization in lipids
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Which of the following processes proceeds in the second phase of biotransformation?
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Acetylation
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Reduction
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Oxidation
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Hydrolysis
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Metabolic transformation and conjugation usually results in an increase of a substance biological activity:
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In case of liver disorders accompanied by a decline in microsomal enzyme activity the duration of action of some drugs is:
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Decreased
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Enlarged
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Remained unchanged
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Changed insignificantly
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Half life (t ½) is the time required to:
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Change the amount of a drug in plasma by half during elimination
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Metabolize a half of an introduced drug into the active metabolite
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Absorb a half of an introduced drug
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Bind a half of an introduced drug to plasma proteins
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Half life (t ½) doesn’t depend on:
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Elimination is expressed as follows:
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Rate of renal tubular reabsorption
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Clearance speed of some volume of blood from substance
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Time required to decrease the amount of drug in plasma by one-half
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Clearance of an organism from a xenobiotic
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The most rapid eliminated drugs are those with high glomerular filtration rate and actively secreted but aren’t passively reabsorbed:
Frage 40
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Systemic clearance (CLs) is related with:
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Only the concentration of substances in plasma
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Only the elimination rate constant
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Volume of distribution, half life and elimination rate constant
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Bioavailability and half life