UNIT 2: INTRODUCTION TO PHARMACOLOGY

PHARMACOLOGY

The study of substances that interact with living systems

through chemical processes.

• The study of drugs or medication action.

(pharmakon) (logia)

The word pharmacology is derived from Greek

φάρμακον, (__________), “drug, poison” and -λογία, -

(_____), “study of”, “knowledge of”

Paracelsus

“All drugs are poisons; the benefit depends on the

dosage.”

(PHARMACOTHERAPEUTICS) (Medical Pharmacology)

(_______________________)

• aka (_____________)

• The science of substances used to prevent, diagnose,

and treat disease.

• Example: When a person is taking paracetamol

(TOXICOLOGY) (study of poisons)

(_____________)

• The branch of pharmacology that deals with the

undesirable effects of chemicals on living systems, from

individual cells to humans to complex ecosystems.

• The (___________) (its nature, effects and detection).

• Example: When a person is taking too much paracetamol

(DRUGS) (treatment, prevention, or

diagnosis) (10918)

(________)

refer to pharmaceutical products that pertain to

chemical compounds or biological substances, other than

food, intended for use in the (______, ______, _______) of disease in humans or animals.

• (See Pharmacy Law, R.A. (______)

(GENERIC NAME) (Common name) (General Name) (Non-proprietary name) (Official Name)

(_______________)

• (___________) or (_______)

• Assigned to a drug usually based on the chemical name

• Also known as (________________)

• Example: ibuprofen, cetirizine, amoxicillin

• Usually related to (__________) **

o Drug name that appears on the official reference [i.e.

United States Pharmacopeia (USP) – National

Formulary (NF)]

o All drugs in the world are listed down in

Pharmacopeias

(tests, procedures, and acceptance criteria) (strength, quality, and purity) (official name) (generic name)

ROLE OF USP-NF MONOGRAPH

• USP-NF monographs contain specifications (____, ______, _______) that helps ensure

the (______, _____, ______) of named items.

• Drugs available in the Philippines, generally follow

USP-NF.

• Usually the (________) found in the USP-NF is also

the (________) of the drug.

(TRADE NAME) (Brand Name) (Proprietary Name) (Counterfeit drugs) (® (registered)) (TM (Trade Mark))

(__________)

• Also known as (_______) or (__________)

• The name which pharmaceutical company adapt to their

particular drug product.

• Copyrighted by and exclusive to the company.

• (__________) – drugs made by anybody who is not

part of the company; a copycat (these people should be

sued)

• Usually have the (_________) or (______________)

symbol on drug labels.

(Montelukast) (Kastair ®) (Unilab)

Generic Name: (_______)

Brand Name: (_________)

Company: (___________)

(Metformin HCI) (N/A) (Ritemed)

Generic Name: (_______)

Brand Name: (_________)

Company: (___________)

(Phenyleprine, Chlorpheneramine Maleate, Paracetamol) (Neozep Forte) (Unilab)

Generic Name: (_______)

Brand Name: (_________)

Company: (___________)

(Unibranded generics) (Combination Drug) (Forte) (Tablet) (Capsule) ()

• (___________) → named after the corporation,

they bear only the name of their corporation or company

(eg. RiteMed, Watsons, Rhea generics, TGP generics)

• Note: There are cases of (__________) products.

Where there are 2 or more generic names.

• (_______) → drowsy; usually added to the name if a drug is

improved or something is added to it

• (_______) → takes time to dissolve in the body

• (_______) → absorbed much faster compared to tablet

(CHEMICAL NAME) (N-acetyl-para-aminophenol) (C8H9NO2)

(____________)

• The exact molecular formula of the drug.

• Complete (1) (__________) of the drug.

• Usually, a very long name and difficult to pronounce.

• Example:

o Generic Name: Paracetamol

o Brand Name: Tempra

o Chemical Name: (________________)

(APAP) [para means opposite]

o Chemical Formula: (_________)

(No difference) (No difference) (Higher in cost) (Lower in cost)

(Covered if no Generic Form Exists) (Normally always covered) (Tested and

approved by the FDA) (May Differ – but proven to be acceptable by the FDA) (No difference) (No difference) (Drugs are standard in size, color, packaging,

etc.)

(Packaging and drug itself may look different)

SIMILARITIES AND DIFFERENCES OF GENERIC

VS BRANDED DRUGS

	BRAND NAME	GENERIC DRUGS
Active Pharmaceutical Ingredient	(_________)	(________)
Price	(_________)	(________)

Insurance Coverage	(________)	(_______)
Inactive Ingredients	(________)	(_______)
Strength / Dosage	(_______)	(_______)

Appearance / Look	(_______)	(________)

CHEMICAL GROUP

• Drugs that are classified based on the chemical structure.

• What structure is common or similar in the different drugs

• If they have the same functional groups, the activity would

be almost similar.

• β-lactam antibiotics

o Penicillins, Cephalosporins, Monobactams,

Carbapenems (all contain β-lactam ring) (Cell Wall

Synthesis Inhibitors)

• Note: The similarity on the chemical structure will equate

to the similarity of their use or their effect.

(MECHANISM OF ACTION) (specific biological target.) (site of action) (receptors) (Enzyme inducer) (activator) (inhibitor) (catalysts) (vasoconstriction) (Ion channel) (Calcium) (Calcium channel blocker (Dihydropyridine)

(___________)

Drug classes that share a common molecular mechanism

of action by modulating the activity of a (___________)

• Also known as (_________)

o For (_______), these activities include agonist

(activates the cell), antagonist (opposes the effect),

inverse agonist, or modulator.

o (________) → if an enzyme in the body is

activated by a drug

o Enzyme target mechanisms include (_______) or

(_______). Enzymes act as (________); they speed up

chemical reactions in the body.

§ Too much Angiotensin II (causes

(_______) can lead to hypertension.

o (________) modulators include opener or blocker.

o Sodium can enter through the Sodium-Potassium

pump, Calcium can enter through Calcium Ion

Channels, and so there are drugs that can open a

channel to allow entry/close an Ion channel.

o (________) – is a drug that when it enters the blood

vessels, it will lead to vasoconstriction.

o The (___________________________)

blocks the calcium so that it won’t enter thus causing

vasodilation. If calcium enters the heart, it will lead to

muscular contraction.

• -ase → enzyme; -ose → sugar

(PRIMARY EFFECT) (anatomical or functional)

(___________)

o Drug classes that are categorized by the (_____________) change the drugs induced.

o Groupings of the drug based on physiological

change

(Diuretic or Antidiuretic) (Inotrope (positive or negative) (Chronotrope (positive or negative) (Bronchodilator) (Decongestant) (Sedative)

§ (____________) – increases or

decreases the production of urine; diuresis =

urination

§ (_______________) – affects the

force of contraction of the heart by the cardiac

muscles

§ (_________________) – if the drug

increases or decreases the beat of the heart

muscle (bpm)

§ (_____________) – makes the bronchioles (air

passageways) dilate

§ (____________) – remove the clogs or

congestions in the airways

§ Antithrombotics

§ (____________) – producing sleep

THERAPEUTIC EFFECT

(__________________)

o Drug classes that are categorized by the pathology

the drugs treat.

o Grouped according to the pathology treated by the

drug

(OTC DRUGS or Over-the-counter drugs)

• (_____________________); no purchasing restrictions by

the FDA.

• These drugs can be bought without prescription.

• Can be seen in groceries or drug stores; such as

paracetamol

(PRESCRIPTION DRUGS) (Legend drugs)

(_______________)

• Also known as (___________);

• Determined unsafe for OTC purchase due to possible

adverse effects if taken without physician’s advice.

• FDA has deemed it necessary for the patient to seek a

physician first before purchasing this (1) (____________).

• Buying this drug requires (1) (_______________).

(CONTROLLED SUBSTANCES) (Drug controlled)

(______________________)

(__________________) by a special prescription requirement

because of the danger of addiction or abuse.

(PDEA) (FDA) (C-I) (C-V)

• Controlled by the (______) and the (______).

• These drugs are classified through schedule numbers (_______) to (________). As the number increases, the less prone it is for abuse and physical dependence.

PRESCRIPTION DRUGS

Products that bear the

Rx symbol in their

packaging requires

prescription.

OTC DRUGS

• Products with no Rx on

the packaging, can be

dispensed w/o

prescription.

• Pharmacy counseling

is recommended.

(C-I)

Controlled substance

• In the Philippines, there is no law regulating the use of

Marijuana. Thus, it is classified as (_____).

• As the number of the classification increases, the risk of

drug abuse and dependency is reduced.

(S-2 license)

CONTROLLED SUBSTANCES

• Have a distinct symbol on its label.

• It requires a special prescription from a physician with

valid (_______) issued by PDEA.

DRUG ACTIONS

• These are terms you usually find when searching about

drug information (i.e.: Text book, PPD, MIMS, Drug

leaflets)

• It is easier to find specific information once you

understand what is listed under each heading.

INDICATIONS

• Contains the list of medical conditions or disease for

which the drug is meant to be used.

• What the drug is used for.

ACTIONS

• Contains the description of cellular changes occurs as a

result of the drug.

• What change the drug produces in the body to treat the

condition.

CONTRAINDICATIONS

• Contains the list of conditions for which the drug should

not be used.

CAUTIONS

• Contains the list of conditions or patient types that

demands closer observation for specific side effects

when given the drug.

(SIDE EFFECTS OR ADVERSE DRUG REACTIONS) (drowsiness)

(________________)

• Contains the list of unintended, unpleasant, or dangerous

secondary effects other than the desired effect of the

drug.

Example: Benadryl can cause (______)

INTERACTIONS

• Contains the list of other drug or specific food that may

alter the effect of the drug, generally should not be given

during the course of therapy.

• You will know what not to take together with the drug.

(PHARMACOKINETICS) absorption,

distribution, metabolism, and excretion (ADME).

(______________)

The study of the time course of drug (_____, _______, _______, ________)

• It answers the question: “what does the body do to the

drugs?”

• Describes the movement of drugs through the body.

PHARMACODYNAMICS

refers to the relationship between

drug concentration at the site of action and the

resulting effect, including the time course and intensity

of therapeutic and adverse effects.

• It answers the question: “what does the drug do to the

body?”

• Describes the body’s biological response to drugs.

PLANTS

• Considered as the primary source of drugs, where

active ingredients are extracted from bark, leaves, resin,

roots, fruits and flowers of a plant.

• Example: Lagundi for cough, Oregano leaves for cough,

Sambong for urolithiasis

(ANIMALS) (cows) (pork or pig)

(_________)

• Lacking substances in the human body can be replaced

with similar substances found in glands, organs and

tissues of animals (including humans, microorganisms).

• Drugs can also be obtained from fungi (such as

Penicillin), algae, and other living organisms.

• Example: Bovine insulin from (_______), Porcine insulin from

(___________)

MINERALS

• Substances that are found in earth and soil.

SYNTHETIC

• Drugs that are manufactured in laboratories using

advance human skills and understanding of chemistry.

SYSTEMIC EFFECT

• Drug effect that reaches widespread areas of the body.

• Usually occurs when drug reaches the blood stream.

• Example: pain relievers distributed all throughout the

body, antibiotics given in the IV.

(NATURE OF DRUGS) (“fit”)

(________________)

• To have a good (____) to only one type of receptor, a drug

molecule must be sufficiently unique in shape, charge,

and other properties to prevent its binding to other

receptors.

• It is very important for drugs to bind to our receptor.

(DRUG SIZE) (1000 g/mol) ()

(___________)

• Ave. molecular weight of drugs is between 100 and 1000

g/mol.

• To achieve such selective binding, it appears that a

molecule should in most cases be at least 100 g/mol in

size.

• The upper limit in molecular weight is determined

primarily by the requirement that drugs must be able to

move within the body (eg, from the site of administration

to the site of action).

• Note: Drugs much larger than (________) do not diffuse

readily between compartments of the body.

(DRUG REACTIVITY & DRUG-RECEPTOR BONDS)

(covalent, electrostatic, and hydrophobic bond.)

(___________________&_______________________)

• Drugs interact with receptors by means of chemical

forces or bonds.

• These are of three major types: (_______, ________, ___________)

(Covalent bonds) (covalently)

• (___________) are very strong and, in many cases, not

reversible under biologic conditions.

o If a drug binds to a receptor (_________), it is very

difficult for it to be reversed because it is strong and

irreversible.

(Electrostatic bonding)

• (_____________) is much more common bonding

in drug-receptor interactions.

o It varies from relatively strong linkages between

permanently charged ionic molecules to weaker

hydrogen bonds and very weak induced dipole

interactions such as van der Waals forces and similar

phenomena.

o A bond for charged molecules.

(Hydrophobic bonds) (“pockets.”)

(______________)

are usually quite weak and are

probably important in the interactions of highly lipid-

soluble drugs with the lipids of cell membranes and

perhaps in the interaction of drugs with the internal walls

of receptor (_________)

o For drugs that are fat-based.

(DRUG SHAPE) (chirality)

(_____________)

molecule must be such as to permit

binding to its receptor site via the bonds just described.

• is complementary to that of the receptor

site in the same way that a key is complementary to a

lock.

• The phenomenon of (_______) (stereoisomerism) is so

common in biology that more than half of all useful drugs

are chiral molecules; that is, they can exist as

enantiomeric pairs.

(enantiomer) (Active site)

o An (________) of a drug may vary in terms of

receptor selectivity, potency and intrinsic activity.

• (___________) → site where the substrate bonds