Pharmacology Basics

Introduction to Pharmacology
 Learning Objectives
At the end of this chapter the student will be able to:
1. Define various terminologies used in Pharmacology
2. Understand pharmacodynamics and
pharmacokinetics (absorption, distribution,
metabolism and excretion) of drugs
3. Understand theoretical pharmacokinetics like half-
life, order of kinetics, steady state and plasma
concentration
4. Understand drug safety and effectiveness like
factors affecting drug action and adverse drug
reactions
 Definitions
Pharmacology:
from Greek , pharmakon, "drug"; logia, "the study of“
(study of the drug)

The science that deals with effects of drugs on living

system.
• It includes the history, source, physicochemical
properties, dosage forms, methods of administration,
absorption, distribution, mechanism of action,
biotransformation, excretion, clinical uses and adverse
effects of drugs
Drug
`Any substance or product` that is used or
intended to be used to modify physiological
systems or pathological states for the benefit of
the recipient.

A substance used in the prevention, treatment or

diagnosis of disease.
• Pharmacokinetics (PK):
Study of the absorption, distribution metabolism
and excretion (ADME) of drugs (“ What the body does to a
drug ”)
• Pharmacodynamics (PD):
The study of the biological and therapeutic effects of
drugs (“What the drug do to the body”)
• Pharmacotherapeutics:
It deals with the proper selection and use of drugs for
the prevention and treatment of disease
• Toxicology:
Toxicology is the branch of pharmacology dealing
with the "undesirable" effects of drugs on biological
processes
Adverse or “Side-Effect”

• An unintended action of a drug.

• Results from a lack of specificity
of drug action.
• All drugs are capable of
producing adverse effects.
 Drug Names
Chemical name
• The drug’s chemical composition and molecular
structure
Generic name (nonproprietary name)
• Name given by the United States Adopted
Name Council
Trade name/ Brand name/Product (proprietary name)
• The drug has a registered trademark; use
of the name restricted by the drug’s owner
(usually the manufacturer)
Chemical Name Generic Name/ Brand Name/
Non- Proprietary Proprietary
Name Name

Isobutylphenylpr- Ibuprofen Trufen, Advil,

opionc acid Ultrafen
Acetaminophen Paracetamol Otamol,
Acamol,
Sedamol,
Aminobenzyl Ampicillin Ampipharm
Penicillin
Grouping of drugs:

• Pharmacologic class (or family):

– drugs that share similar characteristics
– Example: beta-adrenergic blockers are an
example of a pharmacologic class.

• Therapeutic class:
– groups drugs by therapeutic use
– Example: Antihypertensives
Principles of Prescription Writing
 Definition
A prescription is a written,
verbal, or electronic order
from a practitioner or
designated agent to a
pharmacist for a
particular medication for a
specific patient.
 The “Five Rights” of
Medication Administration
Right drug
Right dose
Right time
Right route
Right patient
 Prescription Formatting

Heading

Body

Closing
• Tablets - tab
• Capsule – cap
• Syrup – syr
• Suspension – susp
• Injection – Inj
• Metered dose inhaler – as such
• Lotion – as such
• PO: by mouth
• PR: per rectum
• IM: intramuscular
• IV: intravenous
• ID: intradermal
• IN: intranasal
• TP: topical
• SL: sublingual
• BUCC: buccal
• IP: intraperitoneal
 Controlled Substances
• Definition - a prescription drug
whose use and distribution is
tightly controlled because of its
abuse potential or risk
• Regulation is more strict
Routes of Drug Administration
ROUTES OF DRUG ADMINISTRATION
• Drug and patient related factors determine the selection of
routes for drug administration

1. Properties of the drug

 water or lipid solubility, ionization, effect of gastric pH, digestive enzymes,
first pass metabolism
2. Therapeutic objectives
 Onset of action/ duration of treatment (emergency/ routine use)
 Site of action (local / systemic).
3. Condition of the patient (unconscious, vomiting, diarrhea)
4. Age of the patient
5. Patient`s/doctor`s choice
ROUTES OF DRUG ADMINISTRATION

• Major routes of drug administration include:

A. Enteral: oral, sublingual, buccal.

B. Parenteral: Intravenous (IV), Intramuscular (IM),

Subcutaneous (SC), Intradermal (ID) .

C. Others: transdermal, nasal inhalation, oral

inhalation, topical (skin cream, eye drops, ear
drops), rectal, vaginal … etc
1. Oral:
• Most common and acceptable route
• Advantages:
• Convenient - can be self- administered, pain free, easy to
take
• Absorption - takes place along the whole length of the GI
tract
• Cheap - compared to most other parenteral routes
• Safe- low risk of infection
• Overdose and toxicities can be overcome by antidotes, such
as charcoal
1. Oral:
• Disadvantages:
• Sometimes inefficient - only part of the drug may be
absorbed
 Absorption can be affected by several factors, as gastric pH
 Destruction of drugs by gastric acid and digestive juices
 First-pass effect - drugs absorbed orally are initially transported to
the liver via the portal vein
• Irritation to gastric mucosa - nausea and vomiting
• Effect too slow for emergencies
• Unpleasant taste of some drugs
• Unable to use in unconscious patient
First-pass Effect
• The intestinal and hepatic degradation or alteration of a
drug or substance taken by mouth.

• The greater the first-pass effect, the less the agent will
reach the systemic circulation when the agent is
administered orally
1. Oral:

• Wide range of oral preparations including:

A. Enteric-coated preparations
B. Extended- release preparations
A. Enteric-coated preparations:
Is a chemical envelope that resists the action of fluids and
enzymes in the stomach but dissolves readily in the upper
intestine.

• Such coat is useful for:

1. Drugs that are acid unstable (e.g. Omeprazole)
2. Stomach irritating drugs (e.g. Aspirin)
B. Extended-release Preparations (ER or XR):
• Have special coating or ingredients that control how fast the
drug is released from the pill into the body

Advantages:
• Slower adsorption and prolonged duration
• Better patient compliance
• May maintain concentrations within acceptable therapeutic
range over a long period of time
• These preparations are advantageous for drugs with short half
lives
2. Sublingual/ Buccal:
Placement under the tongue allows a drug to diffuse into the
capillary network and enter the systemic circulation directly
• The buccal route: drug is place between cheek and gum

Advantages:
– Ease of administration
– Rapid absorption
– Low risk of infection
– Bypass of the harsh GI environment
– Avoid the first-pass metabolism
2. Sublingual/ Buccal:

• Disadvantages
• Inconvenient
• Small doses
• Unpleasant taste of some drugs
II. Parenteral route:
Introduces drugs directly across the body’s barrier defenses
into systemic circulation

• Uses:
– Drugs that are poorly absorbed from GI tract (e.g.
heparin).
– Drugs that are unstable in the GI tract (e.g. insulin)
– In patients unable to take oral medication (e.g.
unconscious patients)
– Circumstances that require a rapid onset of action
• Advantages:
– Avoid first-pass metabolism or harsh GI environments.
– provides the most control over the actual dose of drug
delivered to the body.
– Good bioavailability

• Disadvantages:
– Irreversible
– Low convenience, may cause pain, fear
– local tissue damage, and infections.
1. Intravenous (IV):

• Drugs are injected directly into the blood stream through

a vein
• Drugs are administered as:
– Bolus
– Slow intravenous injection
– Intravenous infusion
 1. Intravenous (IV):

Uses and advantages:

• For drugs that are not absorbed orally
• For administering chemicals that may cause irritation when
administered via other routes
• Control over the amount of drug delivered
• Absorption phase is bypassed (100% bioavailability)
• Precise, accurate and almost immediate onset of action
• large quantities can be given, fairly pain free
1. Intravenous (IV)

Disadvantages:
• Irreversible
• May introduce infection at the site of injection
• Risk of embolism
• Risk of adverse reactions by the too-rapid delivery of
high concentrations of a drug to the plasma and tissues
2. Intramuscular (IM):

• Drugs are injected into a large muscle

• Drugs administered IM can be:
1. Very rapid absorption of drugs in aqueous
solution

2. Slow release preparations: Depot Effect

• Pain at injection sites for certain drugs

3. Subcutaneous (SC):

• This route provides absorption via simple

diffusion
• Slower than the IV route
• Advantages of SC injection:
– Minimizes the risks of hemolysis or thrombosis
associated with IV injection
– May provide constant, slow, and sustained
effects.
• SC route should not be used with drugs that
cause tissue irritation
• Absorption is limited by blood flow, affected if
circulatory problems exist
4. Intradermal (ID)

• The intradermal (ID) route involves injection into the dermis,

the more vascular layer of skin under the epidermis.
• Agents for diagnostic determination and desensitization are
usually administered by this route
III. Others

1. Oral inhalation

• Gaseous and volatile agents and aerosols

• Rapid onset of action due to rapid access to
circulation
[Link] surface area
[Link] membranes separates alveoli from
circulation
• This route is particularly effective and
convenient for patients with respiratory
complains (such as asthma)
2. Nasal inhalation:
• Administration of drugs directly into the nose.
• Local effect:
– Nasal decongestants, such as oxymetazoline
– Anti inflammatory corticosteroids, such as
mometasone furoate
• Systemic effect:
• Desmopressin for diabetes insipidus treatment
3. Intrathecal/intraventricular:

Introduce drugs directly into cerebrospinal fluid,

when:
• Drugs cannot cross the blood-brain barrier to the CNS
• Local, rapid effects are needed, it is necessary to
introduce drugs directly into the cerebrospinal fluid.
4. Topical:
• Drug is applied to the skin or mucous membrane at
various sites for local effect
• Mucosal membranes (eye, nasal, vaginal, rectal,,,,,.)
• Skin: ointment, cream,,,
4. Transdermal

• The drug is administered in the form of patch that

deliver the drug into systemic circulation (systemic
effect)
I. Stable blood levels
II. No first pass metabolism
III. Drug must be potent or patch becomes to large
IV. Variable rate of absorption
5. Rectal
Advantages
• Unconscious patients and children
• If patient is nauseous or vomiting
• Good for drugs affecting the bowel such as
laxatives
• Easy to terminate exposure

Disadvantages:
• Absorption may be variable
• Irritating drugs contraindicated
 Important
Info

The ROA is determined by the

physical characteristics of the drug,
the speed which the drug is absorbed
and/ or released, as well as the need
to bypass hepatic metabolism and
achieve high conc. at particular sites