Introduction to pharmacology

1. Introduction to Pharmacology

2. Pharmacology
 Origin of the name:
 Farmakon = medication, drug
 Logos = study, science
Pharmacology is the study of drugs
It studies WHAT drugs do and HOW thay
do it!
Actions Uses
Mechanisms Adverse effects

3. The History of Pharmacology
 Since the beginning people search to treat illness and cure
disease. Prehistoric people recognized the beneficial and
toxic effects of many plant and animal materials.
 Primitive people through the Egyptian period believe that evil
spirit living in the body.
 There were a lot of bizarre ideas about causes of diseases
as well as way of treatment:
◦ Diseases are caused by excesses of bile or blood in the body
◦ Wound could be healed by applying a salve to the weapon that
caused the wound
 Hipocrates (fifth century) advanced idea that disease
resulted from natural causes.
 The Arabs’ interest of in medicine, pharmacy and chemistry
was reflected in hospitals and schools

4. The History of Pharmacology

5. The History of Pharmacology
 At the end of the 17th century reliance on
observation and experimentation began
to replace theorizing in medicine.
 Materia medica (the precursor to
pharmacology)– the science of drug
preparation and the medical use of drugs
began to develop.
 The end of the18th century (Claud
Bernard) – began to develop methods of
experimental pharmacology
 2nd half of 20th century – controlled
clinical trial

6. Medication
 Any substance administered for
diagnosis, cure, treatment, mitigation
or prevention.
 Any substance that induces biologic
effects or changes in human
organism. Drugs
Medicinal
drugs
Non-
medicinal
drugs

7. Origin of the drugs / Source of
drugs

8. Origin of the drugs

10. Pharmacology
 Two sides of Pharmacology:
◦ Pharmacodynamics
◦ Pharmacon – drug
◦ Dynamics - power
 Drug action on the body
◦ Pharmacokinetics
◦ Pharmacon – drug
◦ Kinesis – movement
 Body action on tha drug

11. FK – FD relationships
FK FD

12. Acting of the drugs – the
simpliest explanation
Pharmacological effects
Molecular actions

13. Where the drugs bind?
 Drugs attache to proteins:
Enzymes
Carrier proteins (transporters),
Ion channels i
Receptors.

14. Attaching place– proteins?
 Most number of drugs act by attaching
to protein molecules.
 It was belived that general anesthetics
act by interaction with membrane
lipids. Today, it is known that general
anesthetics interact with membrane
proteins.

15. Every rule has an exception...
 Antacid
◦ Alkali + Acid  Salt + Water
 Osmotic diuretics
 Bisphosphonates
◦ Attache to calcium salts in the bones, they are
toxic to osteoclasts (similiar to rat poison).
 Some of antimicrobials and antitumor
drugs
◦ Act directly to DNA

16. How do drug find the
receptor?
 There are more molecules in the body than
molecules of the drug. So, if the the drug
walks unspecifically, without an order and an
aim, the probabilty of attaching and acting will
be very small.
 Pharmacology effect search for specific
distribution (uniformed) of drugs in body or in
the tissue. Drug molecules might be attached
to specific (correspondineg) components of
cells and tissues
 P. Ehrlich: »Corpora non agunt nisi fixata«
(the drug will not af if it is not attached.
*Paul Ehrlich (1854-1915), He got Nobel prize in phisiology and
medicines in 1908.

17. How do drug find the
receptor?
Van der Waals forces
Hydrogen bonds
Ionic bonds
Covalent bonds

18. DRUG – RECEPTOR
INTERACTION
 Attaching of drug to receptor, can lead to the activation
of receptor, but it is not obligatory. The activation is
attaching of drugs to receptor wich produces the
response of the cell, tissue, organ or organism.
 Two essential steps in creating of pharmacological
effect of an agonist:
1. Attaching of drug to receptor
2. Activation of the receptor
 Antagonist is a drug which is able to attach to the
receptor, but it is not able to activate the receptor.
Antagonist prevents attaching of agonist to the same
receptor.
 Afinity is an ability of the drug to attach to the receptor
and efficacy is abilty of the drug to activate the
receptor.

19. Drug Mechanisms and
Receptors
 Common pharmacologic action
requires drug-receptor interaction.
 Drugs may stimulate receptors
directly.
 Drugs may block receptor site for
normal chemicals of the body
 Drugs that interact with several
metabolic pathways or common
functions are likely to have greater
side effects.

20. Receptors and Drug Action

21. Why are the receptors present in
the body?
 There are endogenous substances in the
human body which are able to bind to
receptors.
 The exogenous substances can bind to
the same receptors!

22. Agonists
 Afinity
 Activity
 Endogenous
(adrenaline)
 Exogenous
(dobutamine)

23. Antagonists
 Afinity
 Without activity

24. Can antagonists be used in
therapy?
 Antihistaminics?
◦ Antagonists H1 receptoras
◦ Terapy of alergic reactions

25. Pharmacology effects– adverse
effects

26. Adverse effect or not?
It deppends on perspective?
AE: sedation!!!
AE:
sedation???

27. Terminology
 Pharmacology: is a science that studies the effect of the
drugs on the body.
 Formulary/ Register of drugs/List of approved drug
products/Drug approvals for YEAR….: are the total of
all authorized drugs available within the country in one
year. E:BNF-78-1.pdf
 Medication: is a substance administered for diagnosis,
cure, treatment, mitigation or prevention.
 Prescription: the written direction for the preparation
and the administration of the drug.

28. Terminology Cont …..
 The therapeutic effect: is the primary effect
intended, that is the reason the drug is
prescribed, such as morphine sulfate is
analgesia.
 Side or adverse effect: secondary effect of the
drug is one that unintended, side effects are
usually predictable and may be either harmless

29. Terminology
 Drug toxicity: harmful effect of the
drug on an organism or tissue, result
from overdose or external use.
 Drug allergy: is immunological
reaction to a drug.

30. Terminology
 Drug interaction: occur when
administration of one drug before or
after alter effect of one or both drug.
 Drug misuse: Is the improper use of
common medications in way that lead to
acute and chronic toxicity.

31. Terminology
 Drug abuse: is an inappropriate intake
of substance either continually or
periodically.
 Drug dependence: is a person reliance
on or need to take drug or substance
there are two type of dependence:

32. Terminology
 Physiological dependence: is due to
biochemical changes in the body tissue
these tissue come to require substance
for normal function.
 Psychological dependence: is
emotional reliance on a drug to maintain
a since of wellbeing accompanied
feeling of need.

33. Terminology
Drug habituation: denotes a mild form of
psychological dependence.
Illicit drug: also called street drug are those
sold illegally.

34. basic concepts of Pharmacology
 Pharmacokinetics: is a bout how the body deal with
drug.
 Pharmacodynamics: is effect of drug on the body.
 Pharmacotherapeutics: is a clinical using of drug.
 Pharmacognosy: The study of natural (plant and
animal) drug sources.

35. Branches of Pharmacology
 Pharmacognosy - Origin
 Pharmacokinetics - Movement through Body
 Pharmacodynamics - Effect
 Pharmacotherapeutics - Use/Purpose
 Toxicology -Side Effects

36. The names of the drugs
 Generic name
◦ propranolol
 Brand or trade name
◦ Inderal
 Hemijsko ime
◦ (±)-1-Isopropylamino-3-(1-
naphthyloxy)propan-2-ol hydrochloride
 ATC kod
◦ C07AA05

38. Alkaloids (-endings)
 morphine (Papaver somniferum)
 quinine (Cinchona succirubra)
 atropine (Atropa belladonna)
 cocaine (Erythroxylum coca)
 colchicine (Colchicum autumnale)
 papaverine (Papaver somniferum)
 ephedrine (Ephedra sinensis)
 strychnine (Strychnos nux vomica)
 tubokurarine (Chondodendron tomentosum)

39. Alkaloids (- endings)
 nicotine (Nicotiana tabacum)
 reserpine (Rauwolfia serpentina)
 vinblastine (Cantharanthus roseus)
 physostigmine (Physostigma venenosum)
 ergonovine (Claviceps purpurea)
 pilocarpine (Pilocarpus jaborandi)
 mescaline (Lophophora williamsii)
 coffeine (Coffea arabica)
 teophylline (Camellia sinensis)

40. Medicine names
 endings...
◦ ‘…ine’ alcaloids
◦ ‘…olol’; beta-blockers
◦ ‘…opril’; ACE inhibitors
◦ ‘…dipin’; dihydropyridine Ca channel blockers
◦ ‘…cilin’; penicillins
◦ ‘…tidin’; antihistamines
◦ ‘…sartan; AT antagonists
◦ ‘…statin; HMG CoA reductase inhibitors

41. Medicine names – pharmacological
group?
 Dihydropyridines:
◦ nifedipine, nisoldipine, niludipine, nimodipine
 Local anesthetics
◦ cocaine, procaine, bupivacaine, lidocaine,
benzocaine
 ACE inhibitors
◦ captopril, enalapril, fosinopril
 Beta blockers:
◦ propranolol, metoprolol, nadolol, timolol, atenolol

42. Medicine names – pharmacological
group?
 Penicillins
◦ penicillin G, meticillin, amoxicillin, ticarcillin
 Cephalosporins
◦ cephalothin, cephaclor, cephotaxime, cephepime
 Macrolids
◦ erythromycin, clarythromycin, azithromycin
 Antimycotics
◦ ketoconazol,e itraconazol,e fluconazole,
clotrimazole

43. What to learn about drugs?
 Generic name (Brand name?)
 Mechanism of acting (molecular mechanism)

...(pharmacological effects)
 Indication i contraindications
 Adverse effects
 Important interactions
NOTE: Drug list items in the last chapter of the syllabus:
‘Simplified Table of Pharmacokinetic Values’

44. Drug Effects
Generally, drugs possess more than one effect
on the body.
 Indications :Approved for uses to treat
conditions for which the drug has been
proved to be effective
 Off-label: uses for which the drug
has shown effectiveness but is not
the approved use.
 Contraindications:
◦ Circumstances under which a drug
should not be administered

45. Repetition
1. What is a pharmacology?
2. What is a drug?
3. Where can I find the data about
approved drugs?
4. What is national formulary?
5. What does it mean ATC classification
of the drugs?
6. What is an agonist?
7. What is an antagonist?

46. Repetition cont.
8. What does it mean affinity of the
drug?
9. What does it mean efficacy of the
drug?