CHAPTER 1

Pharma/Module/RSJ/1st Sem 2020

 FUNDAMENTAL CONCEPTS OF PHARMACOLOGY

History, Definitions, Drug Information and Classifications

Pioneers of Medicine and Pharmacology:

• Hippocrates (450 B.C.)
• Francois Magendie (1783 - 1855)
• Claude Bernerd (1813 - 1878)
• Rudolf Buchheim (1820 to 1879)

1. What is Pharmacology ?
• The study of drugs and origin
• From the Greek Pharmacon (drug), logos (a discourse or treatise)
• Broadly defined as how chemical agents affect living processes:
o Hormones
o Neurotransmitters
o Growth factors
o Drugs (pharmaceuticals)
o Toxic agents in the environment
• The medicinal/organic chemists may create the candidate compound (sometimes referred to as a
new chemical entity, NCE), it is the pharmacologist who is responsible for testing it for
pharmacological activity.
• Ultimately will lead to the discovery of novel drugs for therapeutic intervention
• Pharmacology is the unique combination of several Biomedical Sciences!
o Physiology o Biochemistry
o Chemistry o Medicine
o Pharmacology

2. What is a Drug?
• French: Drogue – a dry herb
• A single active chemical entity present in a medicine that is used for diagnosis, prevention and
treatment of diseases
• WHO – in 1966 – “ Drug is any substance or product which is used or intended to be used to
modify or explore physiological systems or pathological states for the benefit of the recipient.”
• Therapeutic or diagnostic benefits
• Pharmacology studies the effects of drugs and how they exert their effects:
Example: Paracetamol can reduce body temperature in case of fever by inhibiting an enzyme
known as cyclooxygenase in CNS, which is responsible for the synthesis of a number of
inflammatory mediators.
• Penicillin cures certain bacterial infections by disrupting the synthesis of bacterial cell walls by
inhibiting a key enzyme.

Drug - refers to the type of preparation in which the drug is supplied

- Preparation depends in the most suitable for its intended route of delivery and means absorption

 Chemical name and code name

 Describe substances chemically
 For example - para - acet yl aminophen ol
• Non-proprietary Name – USAN, BAN, rINN, generic name.
• Proprietary Name (Brand Name) - Manufacturer

Example:
Chemical Name Non-proprietary Proprietary Name
N-acetyl-para-aminophenol (APAP) Paracetamol Crocin, Calpol and Decolgen,
 acetaminophen (USAN US) ……..etc
N-(4-Nitro-2-phenoxyphenyl) Nimesulide Nise, Nimulid …. etc.
methanesulfonamide

Drug Nomenclature – New drug being developed

• Chemical Name or Code name – RO 15-17288
• Non-proprietary Name: Flumazenil
• (BAN, USAN and rINN) – approved name/official name
• Proprietary name: Anexate, Lanexat, Mazicon, Romazicon

3. Sources of Drugs
• Plant sources – Morphine, digoxin, quinine, atropine, reserpine , vinca alkaloids and paclitaxel.
• Animal sources – Insulin, Thyroid extract, heparin, gonadotrophins and antitoxic sera.
• Minerals – Liquid paraffin, magnesium sulfate, magnesium trisilicate, ferrous sulfate and kaolin.
• Micro – organisms – Bacteria and fungi – Penicillin, Streptomycin
• Synthetic – Analgesics, hypnotics, anticancer drugs and antimicrobials
• Genetic Engineering – Human insulin, growth hormone genes
• Hybridoma technique – monoclonal antibodies origin

Plant Sources
• Alkaloids: Water soluble salts of water insoluble nitrogenous compounds
• Glycosides: Ether-like combination of sugar with other organic acids. Acid hydrolysis separates
sugar from non-sugr moiety
• Oils: Glycerides of oleic, palmitic or stearic acids
• Fixed oils: Peanut oil, coconut oil and castor oil
• Volatile oils: Peppermint oil, ginger, eucalyptus oil etc.
• Resins: Oxidized or polymerized volatile oils
• Oleoresins: Mixture of volatile oils and resins
• Gums: Secretory products of plants
• Opium Alkaloid Extraction

4. Drug Study
• Name (Generic and Brand Name) and classification
• Indications
• Preparation and Dosage
• Actions
• Side effects
• Contraindications
• Adverse reactions
• Cautions
• Interactions (to drug, food, sunlight)

5. Drug/Medication Classifications (
• ACE inhibitors/Receptor blockers - Vasoconstrictor; treat hypertension and CHF
• Aminoglycosides - Antibiotics, noted for potentially dangerous toxicity
• Analgesics – Relieve pain
• Antacids - Neutralize stomach acids
• Antianxiety - Relieve anxiety without marked drowsiness
• Antidiarrheals – treat diarrhea
• Antiarrhythmias - Convert any unusual heart rate or rhythm back to sinus rhythm
• Antibiotics – Treat infection
• Anticholinergics - Block the action neurotransmitters and acetycholine
• Anticoagulant - Prevent clot formation
• Anticonvulsant - Control seizures
• Antideppresant – relieve depression
• Antiemetics – prevent nausea & control vomiting
• Antifungals – relieve infection due to fungi
• Antihelminthics – treat worm infestation
 • Antihistamines – control allergic reaction
• Antihypertensives – control chronic HPN
• Antiplatelets – block platelet aggregation (MI and stokes)
• Antipsychotic – reduce psychotic symptoms
• Antipyretics – lower fever
• Antispasmodics – Decrease GI tone and motility
• Antitussives – deppress cough center in the CNS
• Antivirals – treat infection due to pathogenic virus
• Beta adrenergic bronchodilators – stimulate beta receptors to stimulate bronchodilation
• Beta blockers – treat angina, arrhythmias, HPN, glaucoma
• Bronchodilators – dilate bronchioles
• Calcium channel blockers – treat angina, HPN, tachycardia
• Cytotoxins – cause cells death; used for chemotherapy
• Decongestant – vasoconstrictor of nasal passage to relieve cold or allergies
• Digitalis – improve cardiac function by increasing force of contraction and slowing the heart rate
• Diuretics – increase urine output
• Emetics – induce vomiting
• Expectorants – liquefy mucus secretions
• Flouroquinolones – broad expectrum antibiotics
• Glucocorticoids – anti-inflammatory
• Hypnotics – promote sleep
• Hypoglycemics – lower blood glucose level
• Inotropics – strenghten heart contraction
• Insulins – insulin replacement therapy
• Laxatives – produce soft stool
• Macrolides – antibiotics: erythromycin, azythromycin
• Miotics/ Mydriatics – used to constrict the pupil
• Neuromuscular blockers – temporary paralyzing the muscle
• Nitrates – degrade nitric oxide, vasodilator to treat angina
• NSAIDs – nonsteroidal, antinflammatory
• Osmotic diuretics – promote excretion of water
• Oxytocics – stimulate uterine contraction
• Sedatives – calm an anxious person, promote drowsiness
• Thrombolytics – dissolve thrombi by promoting the digestion of fibrin
• Tricyclics - antideppresants
• Vasodilators – relax the arteriolar smooth muscle

6. Other Definition of Terms

 Pharmacoepidemiology: Study of effect of Drugs on populations
 Pharmacoeconomics: Study of cost effectiveness of drug treatment; the cost of medications is of
worldwide concern, particularly among certain groups such as elderly and AIDS patients
 Chemotherapy: It is the branch of therapeutics which is concerned with the effects of drugs upon
microorganisms and parasites, living or multiplying in a living organism. It also includes the drugs
used in malignancy
 Pharmacognosy: is the science of identification of drugs
 Toxicology: is the science of poisons which includes detection and measurement of poisons as well as
treatment of poisoning. Poisons are the substances causing harmful, dangerous or fatal symptoms in
man and animals.
 National Formulary: It is the book published as product information on drugs available to prescribers
in respective countries
o Examples – National formulary – BNF by BMA and PSGB
 Essential Medicines
o WHO defines – “Essential Medicines are those that satisfy the priority healthcare needs of the
population. Essential medicines are intended to be available within the context of functioning
health systems at all times and in adequate amounts, in appropriate dosage forms, with assured
quality and adequate information, and at a price the individual and the community can afford.”
 Orphan Drugs
 o These are the drugs or biological products for diagnosis, prevention and treatment of a rare disease
or a more common disease (endemic only in poor countries) for which there is no reasonable
expectation that the cost of developing and marketing will be recovered from the sale of these
medicines.
 Examples: Rifabutin, Succimer, Fomepizole and liposomal amphotericin B etc .
 Bioavailability - defined as both the relative amount of drug from an administered dosage form which
enters the systemic circulation and the rate at which the drug appears in the blood stream.
 Blood flow rate - is the speed of blood perfusion in an organ, usually expressed in ml/100 g organ
weight/min. Blood flow rates, or immobilization, and exercise.
 Blood, Plasma or Serum Levels - demonstrate the concentration in blood, plasma or serum upon
administration of a dosage form by various routes of administration. Blood, plasma, or serum level
curves are plots of drug concentration versus time on numeric or semi log graft paper . Blood plasma
or serum levels are obtain from blood samples by venipuncture by in certain time intervals after
administration of the drug product and chemical and microbiological analysis of the drug in the
biloogical fluid.
 Dosage Regimen or Dose Rate is the systematized dosage schedule for therapy, eg, the proper dose
sizes and the proper dosing intervals required to produces clinical effectiveness or to maintain a
therapeutic concentration in the body.
 Dose Dependency refers to a change of one or more of the pharmacokinetic processes of absorption,
distribution, metabolism and excretion with increasing dose size.
 Drug dependence is now referred to as substance use disorder. If an individual with drug dependence
stops taking that drug suddenly, that person will experience predictable and measurable symptoms,
known as a withdrawal syndrome.
 Dose Size is the amount of drug in gg(=mcg), mg, units or other dimensions to be administered.
 Dosing Interval is the time period between administrations of maintenance doses.
 Drug Release or Liberation is the delivery of active ingredient from a dosage form into solution. The
Dissolution medium is either a biological fluid or an artificial test fluid ( in vitro). Drug release is
characterized by the speed. Liberation rate is constant and the amount of drug appearing in solution.
 Drug Tolerance is a person's diminished response to a drug, which occurs when the drug is used
repeatedly and the body adapts to the continued presence of the drug.
 Drug Resistance refers to the ability of microorganisms or cancer cells to withstand the effects of a
drug usually effective against them.
 A drug Product or Dosage Form is the gross pharmaceutical form containing the active ingredient(s)
(drug)s and vehicle substances necessary in formulating a medicament of desired dosage, desired
volume and desired application form, ready for administration.
 Drug Receptor Interaction is the combining of drug molecule with the receptor for which it has
affinity, and the initiation of a pharmacologic response by its intrinsic activity.
 Elimination Half life of a drug is the time in hours necessary to deduce the drug concentration in the
blood, plasma or serum to self half after equilibrium is reached. The elimination half-life may be
influenced by: dose size, variation in urinary excretion (pH) , intersubject variation age, protein
binding, other drugs and diseases (especially renal and liver diseases). Loss of drug from the body, as
described by the elimination half life, means the elimination of the administered parent drug molecule
(not its metabolites) by urinary excretion, metabolism or other pathways of elimination (lung, skin,
etc.)
 Excretion of drug is the final elimination from the body's systemic circulation via kidney into urine,
via bile and saliva into intestines and into feces, sweat, via skin and via milk.
 Extravascular Administration refers to all routes of administration except those where the drug is
directly introduces into the blood stream. Extravascular routes are IM, SC, PO, Oral, Rectal, IP,
Topical, etc.
 Homeostasis is the maintenance of a steady state which characterizes the internal environment of the
healthy organism. An important function of homeostasis is the regulation of the fluid medium and
volume of the cell.
 Intravascular Administration refers to all routes of administration where the drug is directly introduces
into the blood stream i.e, IV, Intra arterial and intracardiac: bioavailability = 100 percent f= 1.
 I.V. Bolus is a physiologic nonsense and poor use (misuse) of language. A bolus (greek bolos) is a
bite, something solid which is swallowed and is then absorbed from the intestines. The correct term
would be I.V Push.
 Therapeutic range is the range of drug concentration in the blood, which gives the desired effect
without causing serious side effects or toxicity.

Disclaimer: List of terminologist provided are not complete, more can be learned through further reading and future topic,

____Surname, First Name_________________

BSN 2-_____

ACTIVITY 1:
I. Fill in the blank. Finish each of the following statements using the correct term.

1. Therapeutic drugs, often called _____________________, are those drugs used in the prevention or
treatment of diseases.
2. Before a drug becomes official, it is given a ___________________ name or common name. This
name may be used in any country and by any manufacturer.
3. __________________ drugs, sometimes referred to as recreational drugs, are drugs or chemincal
substances used for nontherapeutic purposes.
4. The study of drugs and the actions thay have in the human body is _______________________.
5. The actual substance that causes the response in a living organism is a(n) ____________________.

II. Definition of terms.

1. What is drug?
2. What is medicine?
3. Drug name used by the state listed in the FDA Formulary?
4. Official name of a drug?

III. Determine the pharmacologic terminologies applied to the following

____________ 5. Drug addict
____________ 6. A client taking medication for long time who develops adaptation
____________ 7. A client taking medication which is not anymore effective

IV. Determine the source of drug stated below. Write the corresponding letter of the sources of drugs on
then space provided.
A. Plants C. Animals
B. Minerals D Synthetic
.

____ 1. Auranofin ____ 8. Digitalis

____ 2. Lomotil ____ 9. Bactrim
____ 3. Codeine ____ 10. Morphine
___ 4. Milk of Magnesia ____ 11. Insulin: regular NPH
____ 5. Thyroid ____ 12. Pepsin
____ 6. Demerol ____ 13. Septra
____ 7. Zinc Oxide ointment ____ 14. Quinidine

IV. Determine the classification of the following drugs.

___________________ 15. Paracetamol ___________________ 18. Amoxicillin
___________________ 16. Zantac ___________________ 19. Toradol
___________________ 17. Humulin R ___________________ 20. Clopidogril