Pharmacology Oral exam questions:

1. Definition of pharmacology as a science, its main aim and tasks?

Pharmacology is the science that studies the interaction of the chemical substances with live organisms, drug
administration for treatment and prophylaxis of various diseases and pathological processes

2. Sources of medical agents?

Plants: roots, bark, sap, leaves, flowers, seeds e.g. opium from poppy seeds, digitalis from fox glove, tannin used for
mouth wash

Animals: hormones for replacement in time of deficiency e.g. insulin from cattle, liver extract for anemia

Minerals: include acids, bases and salts like potassium chloride

Natural: occurring substances like proteins

Synthesis of substances i.e. synthetics

Drugs can come from organic or inorganic sources

3. Main principles and methods of medical agents testing?

Phase Comments
I Use normal volunteers
II Use patients who can benefit from the drugs, asses efficacy, pharmacokinetics
III Use larger # of patient’s asses safety and efficacy
IV Post marketing surveillance

4. Concept of pharmacokinetics of drugs?

Pharmacokinetic is the study of what we do to the drugs it involves absorption, distribution, metabolism
(biotransformation) and excretion.
Distribution (movement of blood from the blood stream to tissues and cells): the acid or base properties of a drug and
the pH of various body fluids are important considerations for drug distribution

 Weak acids drugs: tend to concentrate in compartments of high pH where they are more charged
 Weak bases: tend to concentrate in compartments of low pH where they are more charged
 most drugs are administered by mouth, this involves the portal system of the liver, some bodily compartments
have an added barrier against drugs e.g. blood-brain barrier

Metabolism of drugs: is important because it usually leads to inactivation of drug as well as making it more water
soluble which can later be excreted by the kidney unless it’s a prodrug which becomes activated by metabolism.

Types of reactions involved in drug metabolism:

 Phase I reactions: involve reactions such as oxidation, reduction and hydrolysis

 Phase II reactions: involves conjugation in which a chemical substituent is added to the drug. The most common
type of conjugation reaction is glucuronide conjugation

Most metabolism takes place in the liver, in the liver metabolism can either be:

 Microsomal- includes cytochrome P450 enzymes

 Non-microsomal

Excretion: usually occurs in he kidneys, especially for more soluble drugs, processes involved; Glomerular filtration,
active tubular secretion and reabsorption

5. Concept of pharmacodynamics of drugs?

Pharmacodynamics is the part of pharmacology that is concerned with the biochemical and physiological effects of drugs
and their mode of action, it includes the dose-effect relationship, factors modifying drug effects, dosage, drug toxicity
hence what the drug does to the organism

Drug effects includes:

Efficacy: drugs ability to produce desired change

Tolerance: drugs effects is reduced due to abuse, hence dosage must be increased

Side effects:

Local effects: drug does not go to blood stream

Systemic: effects the whole body as the drug is absorbed into the blood stream and distributed

6. Ways of delivery of drugs into an organism?

7. Ways of excretion of drugs out of an organism?

DRUG ELIMINATION

■ Zero-order elimination: Elimination of drugs in a linear constant fashion regardless of concentration. Concentration
will decrease linearly. Drug examples include alcohol, phenytoin, and aspirin (at high or toxic doses).

■ First-order elimination: Elimination of drugs in a proportional fashion to drug concentration. Concentration will
decrease exponentially with time.

8. Absorption of medical agents when different ways of delivery?

Absorption is the entry of drug with blood via the biological membrane from the site/ route of administration.

The process of drug uptake from the site of administration and transfer into the blood stream. The site of administration
will dictate the rate and efficiency of absorption. Sites of pharmacologic administration include intravenous delivery
(where absorption is total) and other sites, such as oral, intramuscular, and transmucosal/transdermal (where
absorption is only partial)

9. Mechanisms of absorption of drugs in digestive tract.

10. Factors that influence the absorption of drugs in digestive tract?

11. Penetration of medical agents through biomembranes?

The substance with higher water partition coefficient values can penetrate through natural membranes easily as
compared to those having lower value. The natural substances like amino acids, bile salts, glucose readily pass through
body membranes even if their molecules are too large.

water partition coefficient: reflects how much of the drug can get dispersed in fat instead of water

12. Modern theory of action of drugs on an organism?

13. Concept of specific receptors, agonists and antagonists?

PHARMACODYNAMICS

■ Agonist: Drugs that bind to receptors and elicit a biologic response by stabilizing the receptors in their active
conformation.

■ Full agonist: elicits a maximal response by activating all or a portion of the receptors.

■ Partial agonist: elicits a less than maximal response even if all the receptors are occupied.

■ Antagonist: Drugs that block the normal physiologic function of a receptor.

■ Competitive antagonists compete with agonist for a receptor and can be overcome by increasing the
concentration of the agonist. Shifts an agonist curve to the right.

■ A noncompetitive antagonist inhibits by causing irreversible changes to receptors. Shifts an agonist curve
downward.

14. Concept of bioavailability of medical agents?

Bioavailability is a measure of how much drug reaches the circulatory system and is available at the site of action.
Factors influencing the bioavailability of a drug include:

■ Route of administration.

■ Degradation of drug prior to absorption.

■ Gastrointestinal (GI) absorption mechanisms (e.g., active transport vs. passive diffusion).

■ Solubility—very hydrophilic drugs unable to cross lipid-rich cell membranes and very hydrophobic drugs unable to be
absorbed due to insolubility in aqueous fluids. To be well absorbed, has to be largely hydrophobic.

■ Hepatic first pass effect.

■ Drug chemistry—presence of binders or dispersing agents, particle size, and crystal forms.

15. Distribution of drugs in an organism?

Drug Distribution: is the ability of a drug to move from the circulatory system into the interstitium and tissues. Factors
include:

■ Blood flow:

■ Protein binding: Most of the drugs are transported bound to nonspecific sites on plasma proteins, mostly to albumin
(for acidic drugs) and to α1-acid glycoprotein (for basic drugs). Binding to other proteins like ceruloplasmin and
transcortin generally occurs to a much smaller extent. The binding is usually reversible and depends on the individual
compound.

■ Permeability: ability to cross capillary barriers and specific types of capillary barriers that are largely impermeable
such as the blood brain barrier.

16. Metabolism of medical agents in an organism?

DRUG METABOLISM : occurs in the liver

■ Phase I reactions- it a functionalization reaction where they add or reveal a functional group: Convert molecules
into often still active slightly polar, water-soluble metabolites through oxidation, reduction, or hydrolysis reactions (e.g.,
cytochrome P-450 system). Hence it can be excreted more easily. E.g. hydrolysis of Procaine forms aminobenzoic acids
and diethylethanolamine hence it has lost its anesthetic ability.
■ Phase II reactions: Convert metabolites into inactive polar metabolites via acetylation, glucuronidation, or sulfation
that are then excreted by the kidneys. Some drugs undergo phase II reactions directly and some drugs undergo phase II
reactions before phase I.

Note:

 that some drugs get further activated after drug metabolism e.g. demethylation of codeine forms morphine
which is more active.
 Bioactivation: If the parent drug is inactive and the metabolite is active, it’s called a Prodrug e.g. Enalapril (non-
active) is metabolized into Enalaprilat (potent antihypertensive drug)

17. Role of cytoplasmic reticulum (microsomal enzymes) of liver in metabolism of medical agents?

18. Deposition of drugs in an organism.

19. Types of therapeutic and toxic doses.

20. Concept of width of therapeutic action of medical agents

21. Types of pharmacological effects.

22. Role of chemical structure, physical and chemical properties in the action of drugs on an organism.

23. Dependence of pharmacological effects on the dose (concentration) of medical agents.

24. Role of sex and age in the action of medical agents.

25. Peculiarities of combinative use of drugs.

26. Synergism, its types and practical significance.

27. Antagonism, its types and practical significance.

28. Main antidotes, their use for treatment of various types of toxicity.

29. Types of negative action of drugs.

30. Negative side effects of medical agents of allergic nature.

31. Negative side effects of medical agents of non-allergic nature.

32. Toxic action of medical agents.

33. Embriotoxic and fetotoxic action of drugs and poisons.

34. Teratogenic action of medical agents and poisons.

35. Individual intolerance of drugs (idiosyncrasy).

36. Significance of genetic factors in development of negative effects of medical agents.

37. Dependence of pharmacological effect from the pathologic state of an organism.

38. Function of cholinergic synapses, chemical structure and main effects of acetylcholine.

39. Concept of choline receptors, their localization, classification of medical agents that influence choline receptors?

Muscarinic Cholinergic receptors have a higher affinity to muscarine to nicotine. There are 5 different
receptor subtypes that can form G coupled protein complex:
  M1: neurons and gastric glands
 M2: Cardiac cells
 M3: Smooth muscle of eyes and lungs, GI tracts and exocrine glands
 M4 and M5

Nicotinic Cholinergic receptors have a higher affinity to Nicotine. There are 2 subtypes Nm and Nn
 Nm located in neuromuscular junction and are involved in muscle contraction
 Nn: in CNS, autonomic ganglia and are involved in transmission of cholinergic signals

Adrenergic receptors are a class of G protein coupled receptors that are targets of catecholamine’s especially
epinephrine and norepinephrine
 Alpha 1: smooth muscles
 Alpha 2: presynaptic nerves
 Beta 1: heart
 Beta 2: smooth muscles
 Beta 3: Fat tissue

Drugs that influence Cholinergic receptors:

Based on mechanism of action
 Direct acting mimic the effect of acetyl choline by binding to nicotinic or muscarinic receptors
examples include:
a. Acetyl choline: Produces nonspecific cholinergic reaction and rapidly deactivated by
cholinesterase
 Indirect Acting work by binding into acetylcholinesterase enzyme to prevent the breakdown of
acetylcholine in the synaptic cleft this leads to an increase in the concentration of acetylcholine in the
synaptic cleft. The drug can be reversible or non-reversible
Based on chemistry
 Choline esters: they are hydrophilic, poorly absorbed, poorly penetrate blood brain barrier hence have
little effect on CNS eg: acetylcholine
 Alkaloids: Most alkaloids are tertiary amines that are well absorbed eg: Nicotine

40. Localization of N-choline receptors, common characteristics and classification of N-cholinergic medical agents?

41. Concept of adrenergic receptors, their localization and classification of medical agents that influence adrenergic
receptors?

Adrenergic Receptors? Are receptors that can be activated by NE, Epinephrine and adrenergic drugs. There are 2 main
types Alpha and Beta receptors

Alpha Adrenergic receptors can be divided into 2 main classes alpha 1 and alpha 2 receptors

Alpha 1 Alpha 2
Alpha 1 receptors: are gq coupled protein Alpha 2 receptors are Gi protein coupled
receptors, hence when activated they cause a receptors
 stimulatory response mediated by increase in
intracellular calcium
Locations mainly on vascular smooth muscle
throughout the whole body
Actions when activated
1. Vasoconstriction
2. Mydriases – i.e. dilation of pupil
3. Contraction of urinary sphincter and
urine retention
4. In liver, it causes glycogenolysis i.e.
glycogen to glucose
5. In kidney, it leads to inhibition of Renin
release
i.e. its activation promotes a sympathetic
response
Locations mainly on presynaptic nerve endings
and pancreatic islets
Action when activated
1. On presynaptic nerve ending its
activation causes the decrease in
production of intracellular cAMP which in
turn leads to inhibition of further release
of NE
2. Activation of alpha 2 receptors on
pancreatic islets leads to decrease in
insulin secretion

Beta Adrenergic receptors are divided into Beta1, Beta2 and Beta 3 receptors, they are all coupled with Gs protein

Beta 1 Beta 2 Beta 3

Actions when activated Actions when activated
1. In heart: when
activated they lead to
increase in heart rate,
increased cardiac
contractibility and
increase AV node
conduction
2. In kidney: they located
in juxtaglomerular cells
and when activated
they lead to increase in
Renin release which in
turn increases blood
pressure
Actions when activated
1. In Lungs: they are 1. In Adipose tissue: when
located on bronchial activated they lead to
smooth muscles and increase in lipolysis
when activated it leads 2. In urinary bladder: their
to bronchodilation activation leads to
2. Vascular smooth relaxation of bladder
muscles & arteries of and prevention of
skeletal muscle: their urination
activation leads to
vasodilation
3. In Pancreas: when
activated they lead to
increase in insulin
secretion
4. In smooth muscle of GI
tract and uterus: when
activated they lead to
decrease motility in GI
and prevention of labor

Medical agents that effect androgenic receptors

By Chemical structure: they are divided into catecholamine and non-catecholamine

Catecholamine Non-Catecholamine
Structure Organic compound with Similar in structure but without the 2
a catechol (benzene hydroxyl groups on the benzene ring
ring with 2 hydroxyl
groups) and an intermediate ethyl
chain and a terminal amine group
 Oral usability Ineffective as they are quickly Metabolized slowly by MAO hence they
metabolized by CoMT and MAO are Effective
enzymes in gut, liver, CNS and inside
the neurons
Duration of action Short as they are metabolized Long
quicky
CNS penetration Poor penetration as the hydroxyl Can penetrate the CNS as they are less
groups make the molecule polar polar

By mechanism of action:

Direct acting Non-direct acting Mixed action

These agents produce their
effect by binding to alpha or
beta receptors and mimicking
the action of epinephrine, NE
and dopamine They are non-
selective and can activate both
Alpha and Beta receptors.
They are Catecholamine’s
hence they are injected
These agents do not directly
interact with post synaptic
receptors instead they enhance
the effect of epinephrine or NE
by either:
1. Inhibition of their
reuptake
2. Inhibition of their
degradation
Examples include cocaine and
amphetamine

42. Measures that are held when acute poisonings for avoiding of absorption of the poison into blood.

43. Measures for deactivating of the poison in an organism.

44. Measures for acceleration of excretion of the poison out of an organism.

45. Pathogenic, symptomatic therapy of acute intoxication by drugs and poisons.

46. Contents and main pharmacological properties of opiates.

47. Medical and social aspects of struggle with medical dependence.

48. Medical addiction to morphine and principles of its treatment.

49. Specialties of prescription and using of narcotic drugs.