Applied Pharmacology EMMS - 316

General Pharmacology I
Dr. Faisal Alamri
Assistant Professor of pharmaceutical Sciences
alamrif@ksau-hs.edu.sa
@faisalfahd0
Basic Pharmacology Block
PDNT/PMED.PMSC/PPHR -213
Credit: Dr. Wesam Saleh 1
 LECTURE OBJECTIVES

At the end of this session, the students should be able to:

1. Discuss the historical context to the development of
pharmacology
2. Introduce key physical and chemical properties of drugs
3. Discuss the complexity of drug names and classification
4. Describe how drugs are discovered
5. Define: Pharmacology, Pharmacodynamics, Pharmacokinetics,
Clinical pharmacology and therapeutics
6. Describe drug classification and drug names
 What is a drug?

• Defined by the W.H.O.

– “any substance or product that is used or intended to be

used to modify or explore physiological systems or
pathological states for the benefit of the recipient.”
• A drug may be defined as: “any substance that brings about
a change in biologic function through its chemical actions.”
• Drugs maybe synthetic chemicals, substances purified from
either plant or animal products or recombinant proteins
generated by genetic engineering.
 General Definitions
• The word Pharmacology is originally derived from the Greek:
pharmakon, meaning drug and logos, meaning knowledge.

– Pharmacology can be defined as “the study of the effects of drugs on

the function of living organisms”.

– Pharmacology deals with the actions, mechanism of action, clinical

uses, adverse effects and the fate of drugs in the body.

• Pharmacokinetics
– …

• Pharmacodynamics
– …
 Drug Development
• In vitro Studies: Isolate/synthesize a lead compound (a candidate drug);
vary and optimize

• Animal Testing: Test efficacy, toxicity, selectivity, ‘pharmacokinetics’

• Clinical testing: Test efficacy, toxicity, selectivity, ‘pharmacokinetics’
Phase 1: Limited series of healthy volunteers
Phase 2: Actual patients with the corresponding disease
Phase 3: ‘Double-blind’ studies against placebo or
reference treatment
• Approval: Review by the authorities

• Marketing: Patents expire in 15-20 years (varies with country) – after that,
generic drugs tend to take out market share
Drug Development
 Drug Names

• Chemical name:
– benzeneacetamide, 4-[2'-hydroxy-3'-[(1-
methylethyl)amino]propoxy]-.
– C14H22N2O3.

• Brand Name
– Tenormin

• Generic (nonproprietary) names

– Atenolol

 Always use GENERIC name if possible

 Drug Interactions

• Additive interaction—The sum of the effects of two drugs

given together is equal to each of them given separately but
at the same time, or 1 + 1 = 2.

• Synergistic interaction—Giving two drugs together results in a

greater effect than expected if given separately, or 1 + 1 = 3.

• Potentiation interaction—One of the drugs has no direct

effect yet increases the expected effect of the other drug, or 1
+ 0 = 3.
 Drug Administration

• Dosage size and route of administration determine the intensity of

Drug Response.
• Pharmacokinetic processes: determines how much of an
administered dose gets to its sites of action (RECEPTOR).
• Once a drug has reached its site of action, pharmacodynamic
processes determine the type and intensity of response(s).
 Drug Doses

1. The Usual Recommended Dose:

– The amount of drug given to adults that will ordinarily produce the
effect for which the drug is intended.
• Minimum Dose: the smallest dose of drug that produces the
therapeutic effect.
• The Maximum Dose: the largest dose of a drug that can be safely
administered.

2. The Toxic Dose: the amount of a drug that will produce noxious
(harmful) effects.
3. The Lethal Dose of a drug is the amount of substance (a drug) that
will cause death (
– the term "LD50" is usually associated with the lethal dose, which means that
50% of the animals given that amount of drug died.
 Drug Doses

1. The Single Dose: the amount of a drug to be E.g., Amoxicillin

taken at one time. 500 mg x 3 (tid)

2. The Daily Dose: the amount of a drug to be

taken in a 24-hour period, which is usually
divided into several individual doses. • qd = once daily
• bid = twice a day
3. The Maintenance Dose: is the amount of a
drug taken to maintain or continue a desired • tid = three times
therapeutic effect. a day
• qid = four times a
4. The Loading Dose is the initial dose(s) of a drug day
given to achieve maintenance drug levels
quickly. Loading doses are often used in
hospitals for very sick patients.
Drug Routes of Administration

Parenteral (IV, IM , SQ)

Inhaled Rectal

Oral Transdermal
Topical
 Properties of Ideal Drug

The most important characteristics of a drug are:

• Effectiveness: An effective drug is one that elicits the

responses for which it has been administered.

• Safety: A safe drug is defined as one that cannot produce

harmful effects.
– There is no such thing as safe drug.

• Specificity: A specific drug must act selectively on particular

cells and tissues.
– A selective drug would not produce side effects.
Additional Properties of an Ideal Drug

• 1. Reversible action
– Effects be reversible, i.e., removal/subside w/i specific time
(1/2 life is short but potent during that time)
– Example: General Anesthetic; Contraceptives

• 2. Predictability
– Know how patient will respond

• 3. Ease of Administration
– Number of doses should be low and easy to administer why?
– 1. increase compliance & 2. decrease errors
• Diabetic patient: Multiple daily injection of insulin
• Intravenous infusion
Additional Properties of an Ideal Drug

• 4. Freedom from drug interactions

– Should not increase or decrease action of other drugs or have adverse
combined effects
• Respiratory depression caused by diazepam (valium), which is
normally minimal, can greatly be intensified by alcohol.
• Antibacterial effects of Tetracycline can be greatly reduced by
taking iron or calcium supplements

• 5. Low Cost
– Easy to afford (especially with chronic illness)
• Growth hormone (somatrem) costs between $10,000 and $20,000
• Lifelong medication: hypertension, arthritis, diabetes
Additional Properties of an Ideal Drug

• 6. Chemical Stability
– No lose of effectiveness with storage

• 7. Possession of a simple generic name

– Easy to remember and pronounce
• Example: Viagra (sildenafil);
Panadol (Paracetamol)
Tylenol (acetaminophen)
 Because No Drug is Ideal …
• No drug is safe
• All drugs produce side effects
• Drug responses may be difficult to predict
• Drugs may be expensive
• Drugs may be hard to administer

All members of health care team must exercise care to promote

therapeutic effects and minimize drug induced harm
 Drug Types

• Prescription

• Complementary alternative therapies

• Non-prescription over-the-counter
• Illicit (street) drugs
 Drug classification
• Drugs May be classed either by its: Chemical group,
Therapeutic group, or Receptor action
Name Chemical group Therapeutic Group Receptor Action
Atropine tropane alkaloid Anticholenergics Muscarinic receptor
antagonist

Adrenaline Catecholamine Sympathomimetic α & β receptors

agonists
Morphine Opiate Analgesic γ, κ & μ receptor
antagonists
Midazolam Benzodiazepine Anxiolytic, Enhances GABA
anticonvulsant, and
sedative
 How Drugs Act?
• In the majority of cases, the drug molecule interacts with a
cellular receptor, causing a cellular response.
• In order to interact with its receptor, a drug must be recognized
as similar to the endogenous chemical.
– Drugs generally mimic endogenous
chemicals (e.g. Hormones or
neurotransmitters).
 Action on the receptor

AGONIST ANTAGONIST

Agents which bind to Agents which bind to the

specific receptor targets receptor but cause no
and in doing so result in response and in doing so
a biological response also block the action of
within the cell agonists
Examples of Agonists

Noradrenaline Salbutamol
Isoprenaline

  
Examples of Antagonists

Non-selective β
Prazosin blockers
Atenolol

  
Second Messenger System

Adenylate Cyclase

Inactive
Second Messenger System

Adenylate Cyclase

Activates
Second Messenger System

Adenylate Cyclase

Part of G-Protein
activates Adenylate
Cyclase
Second Messenger System

Activated
Adenylate Cyclase

ATP cAMP
 Factors that determine
Intensity of Drug Response

1. Administration- dosage size and route

• Because of errors in administration routes and dosage and
at wrong time there are many discrepancies in what patient
gets and could cause more harm than good
– Errors could be made by physicians, pharmacists or
nurses

– Should give patients complete instruction about their

medication and how to take it
 Factors that determine
Intensity of Drug Response

2. Pharmacokinetic processes
• Determines how much of an administered dose gets to its sites
of action (absorption, distribution, metabolism, excretion)

3. Pharmacodynamics
• Once a drug has reached its site of action, pharmacodynamic
processes determine the type of response and intensity

– Drug must first bind to its specific target site at (RECEPTOR)

– Followed by a sequence of events that result in response

 Factors that determine
Intensity of Drug Response

4. Sources of individual variation

• Each patient is unique in ability to respond and to how they
each respond,

– Age- very important factor

– Sex- due to hormonal differences
– Weight- less effective and longer lasting in obese
individuals (storage in fat)
– Kidney & liver functions - elimination of drug
– Genetic variables- tolerance, allergy (though not always
genetic)
 Factors that determine
Intensity of Drug Response