Theme: “ General Pharmacology (Pharmacokinetics, Pharmacodynamics,

Basics of Pharmacotherapy).”

1. Tests of the control of knowledge.

1. What does the concept "pharmakokinetics" include?
1. Types of drug action. 2. Absorption of drugs. 3. Distribution of drugs in the organism.
4.Transformation of drugs in the organism. 5. Pharmacological effects. 6. Excretion of drugs.
2. What is the main mechanism of drug absorption in the gastrointestinal tract?
1. Filtration 2. Diffusion 3. Active transport 4. Pinocytosis
3. The following statements are correct except for one, indicate it.
1. Diffusion is the process of distribution of molecules of one substance among molecules of another
substance. 2. Diffusion is the main mechanism of absorption of drugs in the organism. 3. Diffusion occurs
along the concentration gradient. 4. Diffusion rate can be explained by Fick's Law. 5. Diffusion is the
movement of molecules of substance through the micropores of cellular membrane.
4. The following statements are correct except for one, indicate it.
1. Simplified diffusion is the transport of molecules through the membrane with the help of transport-
protein. 2. Simplified diffusion happens along the concentration gradient. 3. Ions and large water-soluble
molecules are transported with the help of simplified diffusion. 4. Simplified diffusion is carried out with
the expenditure of energy. 5. Simplified diffusion is carried out without the expenditure of energy.
5. The following statements are correct except for one, indicate it.
1. Filtration is the transport of molecules through the micropores. 2. Only small molecules (molecular
mass <1000) can be transported by filtration. 3. Small and large molecules not bound to proteins are
filtrated in renal glomeruli. 4. Any molecules can be filtrated through micropores. 5. Filtration is carried
out without the expenditure of energy.
6. What is active transport?
1. Transport of non-ionized molecules. 2. Transport of drug molecules by the dissolution in water phase.
3. Transport of drug molecules by the dissolution in lipid phase. 4. Transport of drug molecules against
concentration and electric gradient with the expenditure of energy. 5. Transport of drug molecules against
concentration and electric gradient without the expenditure of energy.
7. Indicate the main mechanism of absorption of lipid soluble molecules through cell membranes,
1. Filtration 2. Active transport 3. Pinocytosis 4. Simplified diffusion 5. Passive diffusion
8. Following factors influence the choice of route of drug introduction, except for one, indicate it.
1. Bioavailability 2. Drug forms 3. Mechanism of action 4. Stability of drug molecules to digestive juices.
5. The character of drug therapy (urgent, course, prophylactic).
9. Where are most of drugs absorbed?
1. In oral cavity. 2. In the stomach. 3. In small intestine. 4. In large intestine. 5. In rectum.
10. All values are correct, except for one, indicate it.
1. pH in stomach = 1,0-1,5. 2. pH in upper part of small intestine = 6,8-7,0. 3. pH in lower part of small
intestine = 7,4-7,6. 4. pH in stomach = 3,0-4,0. 5. pH in urine = 4,6-8,2.
11. Acidic drugs are better absorbed:
1. In stomach 2. In intestine 3. Both in stomach and in intestine
12. Alkaline drugs are better absorbed:
1. In stomach 2. In intestine 3. Both in stomach and in intestine
13. Absorption in GIT depends on:
1. Solubility in lipids 2. Solubility in water 3. Neither solubility in lipids nor solubility in water.
14. What is well-absorbed in lipids?
1. Ionized molecules 2. Non-ionized molecules 3. Both ionized and non-ionized molecules.
15. What is bioavailability of a drug?
1. Amount of drug absorbed in GIT. 2. The ratio of the amount of drug that entered the blood to the
introduced dose. 3. Amount of metabolized drug. 4. Amount of drug that reached the receptors. 5.
Amount of free fraction of drug.
16. Value of bioavailability is important for determination of:
1. Route of introduction. 2. Value of the loading dose. 3. Number of introduction. 4. Rate of excretion. 5.
Efficacy of the drug.
17. Distribution of drugs in the organism depends on:
1. Solubility in lipids. 2. Solubility in water. 3. Binding to plasma proteins. 4. Vascularization of organs.
5. Elimination.
18. Firm binding of drug to plasma proteins ensures:
1. Absorbability of drug. 2. Excretion of drug. 3. Side effects in patients with burns. 4. Side effects in
patients with liver cirrhosis. 5. Side effects in combination with other drug with high affinity to plasma
proteins.
19. The following statements are correct except for one, indicate it.
1. Hematoencephalic barrier consists of the hematocerebral and hematoliquor. 2. Both barriers are equally
penetrated by drugs. 3. Both barriers are not equally penetrated by drugs. 4. Lipid-soluble drugs penetrate
well via hematoencephalic barrier. 5. Poorly lipid-soluble drugs can't penetrate the hematoencephalic
barrier.
20. Penetration of drugs via hematoencephalic barrier in inflammatory processes and acidosis:
1 Is decreased. 2. Is increased. 3. Is not changed.
21. Following factors expressively influence on transport of drugs via placental barrier, except for one, indicate it.
1. Difference in concentration if drug in mother's blood and in placenta. 2. Molecular mass of drug. 3.
Degree of ionization and lipid-solubility of drug. 4. Placental circulation. 5. Metabolism of drug in fetus.
22. What is the acetylation of drugs?
1. Conjugation with glucuronic acid. 2. Oxidation with participation of cytochrome-450. 3. Binding to
acetic acid. 4. Binding to amino acid "glycine".
 23. What does the concept "pharmacodynamics" include?
1. Types of drug action. 2. Absorption of drugs. 3. Distribution of drugs in the organism.
4.Pharmacological effects. 5. Interaction with specific receptors.
24. What reactions can arise in repeated introductions of drugs?
1. Potentiation. 2. Cumulation. 3. Tolerance. 4. Sensibilization. 5. Tachyphylaxis
25. What phenomena can be observed in combined use of drugs?
1. Idiosyncrasy 2. Summation of the effects 3. Antagonism
26. How is the drug action which causes congenital malformations called?
1. Mutagenous action. 2. Embryotoxic action. 3. Teratogenic action.
27. Determine the types of drug synergism (the interaction of substances A and B):
1. A + B = the sum of effects. 2. A + B > of the sum of effects.
3. A + B < the sum of effects
28. How can we explain the reduction of effects of salicylates in the interaction with phenobarbital?
1. Inhibition of enzymes of the liver 2. Activation of enzymes of the liver 3. Chemical antagonism of
salicylates and phenobarbital
29. What explains the fact that in diseases of the liver the anaesthetic effect of hexobarbital (hexenalum)) is prolonged?
1. Decrease of function of microsomal enzymes of the liver. 2. Increase of function of microsomal
enzymes of the liver.
30. The breadth of therapeutic action is a range of doses:
1. From median therapeutic dose to minimum toxic dose. 2. From single dose to course dose. 3. From
minimum effective (threshold) dose to minimum toxic dose. 4. From single dose to daily dose.
31. Give the correct explanation of the term "tolerance".
1. Insuperable wish of taking of the drug. 2. Amplification of drug action in repeated introduction. 3.
Lowering of drug action in repeated introduction. 4. Increased sensibility to the drug.
32. What does the term "tachyphylaxis" mean?
1. Significant drug dependence. 2. Fast and strong effect of a drug. 3. A synonym of the term "tolerance"
4. Decrease of the effect in rapid repeated introduction of the drug (within short period of time). 5.
Increased sensibility to the drugs of definite group.
33. The cumulation of drugs is possible:
1. In decrease of reabsorption in kidneys. 2. In increase of secretion in renal tubules. 3. In lowering of the
glomerular filtration. 4. In decrease of biotransformation in the liver. 5. In activation microsomal
enzymes of the liver. 6. In impairment of binding to organ receptors.

2.Solve the pharmacological problems

PROBLEM 1. What does the choice of the route of drug introduction depend on?
1. The drug form. 2. The mechanism of drug action. 3. Stability of the drug to digestive juices. 4. Action
of factors of external environment. 5. Biological rhythms of the organism. 6. Bioavailability of the drug.
7.Pharmacological effects of the drug. 8. Type of drug therapy (etiotropic, pathogenetic, symptomatic). 9.
Character of drug therapy (urgent, course, preventive).
PROBLEM 2. Determine the mechanisms of drug absorption.
A - the liposoluble substances are absorbed through the cellular membrane owing to gradient of
concentration of the substances. B - the substances are absorbed by invagination in the cellular membrane
with the subsequent formation of a vesicle. This is the way of absorption of some proteins and the
complex of cyanocobalamin (vitamin B12) with gastromucoprotein. C - The absorption depends on
hydrostatic pressure. Water, small water-soluble molecules are absorbed through pores by this way. D -
the absorption is carried out with participation of transport systems of cellular membranes, it can go on
against gradient of concentration with expenditure of energy. Water-soluble polar molecules of sugars,
amino acids are absorbed by this mechanism.

PROBLEM 3. What drugs can easily penetrate through the capillary wall?
1. The ones binding to proteins.
2. Water-soluble substances:
a) Through lipoprotein membranes; b) through pores in the capillary wall;
3. Liposoluble substances:
a) Through the cellular membranes; b) through pores in the capillary wall.
PROBLEM 4. What drugs can penetrate through the hematoencephalic and placental barriers.
1. Polar water-soluble molecules.
2. Neutral liposoluble molecules.
PROBLEM 5. What drug fraction determines the action of the drug? Why?
1. The fraction connected with proteins of plasma (bound fraction).
2. The non-connected (free) fraction.
PROBLEM 6. Determine the type of transformation of drugs in the organism.
The transformation of substances is carried out mainly owing to oxidation, reduction and hydrolysis with
participation of corresponding enzymes.
PROBLEM 7. Determine the type of drug transformation in the organism.
The transformation of substances is carried out by biosynthetic way which is accompanied by connection
of drug or its metabolites with a number of chemical groups or biogenic substances.
PROBLEM 8. What substances undergo the reverse absorption (reabsorption) in renal tubules?
1. Liposoluble non-polar substances.
2. Water-soluble polar substances.
PROBLEM 9. How does the change of the pH of the urine exert influence upon the excretion of polar substances (weak
acids and weak bases).
1. The alkaline urine increases the excretion of
2. The acidic urine increases the excretion of
 PROBLEM 10. Choose the direct, indirect, main and side effects of cardiac glycosides.
1. Increase of contractile activity of myocardium. 2. Increase of diuresis and disappearance of edemas.
3. Increase of a stroke and minute volume of the heart, improvement of blood circulation. 4. Appearance
of extrasystoles.
direct - ; indirect - ; main - ; side -
PROBLEM 11. What types of drug action determine the following effects?
1. Hyperemia, feeling of a burning in the place of contact with the drug. 2. Improvement of functions of
the organs which do not contact with the drug. 3. Rise of pharmacological effects after absorption of a
drug into the blood.
local - ; general - ; direct - ; indirect -
PROBLEM 12. Determine the type of interaction of medicinal substances (A and B).
1. Increase of the effect:
a) A + B = the sum of the effects; b) A + B > the sum of effects.
2. Decrease of the effect (A + B < the sum of the effects):
a) on the level of biomolecules; b) on the level of molecules of drugs; c) on the level of physical
processes.
3. Decrease of the effect on the level of biomolecules:
a) in the action upon the same biomolecule; b) in the action upon different biomolecules; c) drug A
eliminates the action of drug B and on the contrary; d) drug A eliminates the action of drug B, but not on
the contrary.

PROBLEM 13. How to explain that in diseases of the liver the anaesthetic effect of thiopental sodium may be
significantly prolonged?

PROBLEM 14. How to explain that in simultaneous administration of phenobarbital or griseofulvine or rifampicine
(each drug influences function of the liver) with other drug the action of the other one may be weakened?

PROBLEM 15. Determine the types of drug therapy:

A - the therapy is directed on prevention of diseases; B - the therapy is directed on elimination of the
reason of the disease; C - the therapy is directed on elimination of undesirable signs; D - the therapy is
directed on elimination of deficit of natural biogenic substances.

3. Solve the situational problems.

PROBLEM 1. A morphine addict woman (morphinist) took the narcotic drugs during pregnancy. The
baby was born at time with normal body weight. But soon after the labor the baby became anxious, he
twitched in convulsions, constantly cried, declined breast-feeding; the mucous membranes were cyanotic,
the body temperature was increased. A physician determined this condition as "the syndrome of morphine
abstinence".
Questions: explain the reason of abstinence in the newborn. Enumerate the main complications in foetus and newborn
caused by taking of drugs during pregnancy.

PROBLEM 2. A woman during breast-feeding took a course of anticoagulant therapy for treatment of
thrombophlebitis. During the course of treatment by ethyl biscoumacetate (neodicumarinum) the woman
didn't discontinue the breast-feeding. Soon she found out that the baby's urine became red and he had
hemorrhages in the nasal mucosa and in skin. With these complaints she addressed to a doctor.
Questions: explain the reason of arisen complication in the baby. Give recommendations to the woman in this situation.

PROBLEM 3. A patient with cirrhosis of the liver complicated by chronic hepatic insufficiency was
delivered to the traumatology department in relation with dislocation of the humeral joint. In the setting
of bones the short-acting anaesthesia was used (thiopental sodium intravenously). But instead of usual
duration of the drug action (20-30 min.) the anaesthesia was maintained for an hour.
Questions: explain the reason of the described condition.

PROBLEM 4. A patient with inoperable cancer of the stomach complained on pain. To relieve the pain a
physician administered to this patient regular subcutaneous injections of trimeperidine (promedolum). But
soon the analgesic effect of the drug began to decrease. The patient waited for the next injection with
impatience, because pain was strengthened not only in the area of the tumor, but in the whole body. The
patient complained of nausea and was haunted by thoughts of suicide. The introduction of trimeperidine
(promedolum) in the administered dose eliminated these signs only for a short period of time.
Questions: explain the reason of the described pathological state.
PROBLEM 5. A patient took digitoxin (elimination rate constant is about 7%) in relation with chronic
heart failure. In several days the effect was reached, but treatment had to be continued. The patient
continued to take the drug in the same dose, but in a week the signs of intoxication were arisen.
Questions: explain the reason of appearence of intoxication.

PROBLEM 6. A patient took promethazine (diprazinum) in relation with the allergic reaction. On his
friend's birthday, disregarding the doctor's advice, the patient took significant (but ordinary for himself)
amount of alcohol. Instead of an expected improvement of mood the alcoholic coma developed.
Questions: Determine the character of the described interaction of drugs and alcohol.

PROBLEM 7. A patient took PO half a glass of organophosphorous compound (strong inhibitor of the
enzyme acetylcholine esterase) with the aim of suicide. Besides the gastric lavage, cleansing enema,
infusion therapy the injection of atropine (it blocks m-cholinoceptors) was made. As a result of this the
signs of the intoxication completely disappeared.
Questions: Determine the type of interaction between atropine and organophosphorous compound.

PROBLEM 8. A patient took the long-lasting course of antibioticotherapy in relation with regard to
chronic infectious disease. During treatment he began to complain of skin rash, itch, rhinitis. After the
next injection of the antibiotic asphyxia, edema of lips, increase of body temperature were observed. The
doctor abolished the antibioticotherapy and indicated necessary drugs.
Questions: Determine the type of arisen pathological condition.