Pharma-intro

Pharmacology
Lecture 1
Introduction
Definition of Pharmacology: The study of drugs and
their actions on living organisms.
Three Phases for Drug Action to Occur:
Pharmaceutic
Definition: The phase in which a drug dissolves and

becomes available for absorption in the body.
It focuses on the disintegration and dissolution of
drugs in the gastrointestinal (GI) tract.
Pharmacokinetics
Definition: The study of the process of drug movement

through the body to achieve its effect.
It includes four key processes: Absorption,
Distribution, Metabolism (Biotransformation), and
Excretion (Elimination).
Pharmacodynamics
Definition: The study of how drugs act on the body to

produce therapeutic or toxic effects.
It involves the drug’s mechanism of action, receptor
interactions, and resulting physiological effects.
Pharmacology focuses on understanding drugs and
their effects to provide safe and effective patient care.
-play a critical role in medication administration,
monitoring, and patient education,
. By understanding pharmacokinetics,
pharmacodynamics, and the therapeutic applications
of drugs, to optimize treatment outcomes while
minimizing risks.
Drug Development Stages

Drug development is a rigorous, multistep process to
ensure safety, efficacy, and quality before approval for
public use. The main stages include:
Preclinical Testing
Conducted in laboratories using animal studies to

assess toxicity, pharmacokinetics, and
pharmacodynamics.
Determines if a drug is safe for human trials.
Clinical Trials
Phase 1: Tests drug safety and dosage on a small

group of healthy volunteers (20-80 people).
Phase 2: Evaluates drug effectiveness and side effects
on a larger group of people with the condition (100-300
patients).
Phase 3: Confirms safety, efficacy, and monitoring of
adverse reactions in large groups (1,000-3,000
patients).
Phase 4: Post-marketing surveillance to detect rare or
long-term effects after the drug is released to the
public.
Regulatory Review
After clinical trials, drug manufacturers submit a New

Drug Application (NDA) or Biologics License
Application (BLA) to the FDA for approval.
Post-Marketing
Continuous monitoring ensures safety and efficacy

through surveillance of real-world usage.
Important Definitions of Terms
Adverse Drug Reaction (ADR): Unintended, harmful
reactions to a drug administered at normal doses.
Agonist: A drug that binds to a receptor and activates it

to produce a biological response.
Antagonist: A drug that binds to a receptor but inhibits
its activation, blocking a biological response.
Bioavailability: The portion of a drug that enters the

bloodstream and is available for use by the body.
First-Pass Effect: The reduction of bioavailability when

a drug is metabolized by the liver before reaching
systemic circulation (common in oral drugs).
Half-Life (t½): The time required for half the drug

concentration to be eliminated from the body.
Loading Dose: A higher initial dose given to rapidly

achieve therapeutic levels.
Maintenance Dose: Regular doses used to maintain

therapeutic drug levels.
Pharmacogenomics: The study of how genetic
variations affect an individual’s response to drugs.
Potency: The amount of drug needed to produce a

desired effect.
Therapeutic Window: The range between the minimum

effective concentration (MEC) and the minimum toxic
concentration (MTC).
Toxicity: Harmful effects of a drug when

concentrations exceed therapeutic levels.
Tolerance: A reduced response to a drug after

repeated use, requiring higher doses for the same
effect.
Pharmaceutic
Approximately 80% of drugs are taken orally, and the
pharmaceutic (dissolution) phase is the first phase of
drug action.
In the GI tract: Drugs must be in solution to be
absorbed. Solids (tablets, capsules) must disintegrate
into smaller particles and dissolve (dissolution). Liquid
drugs are already in solution.
Key Concepts:
Tablets are not 100% drug-based. Fillers, called

excipients, are used for size, shape, and dissolution of
the drug.
Additives such as potassium (K) and sodium (Na) can
enhance absorption (e.g., penicillin potassium,
penicillin sodium).
Disintegration: The breakdown of a tablet into smaller
particles.
Dissolution: The dissolving of smaller particles in GI
fluid before absorption.
Rate-Limiting Step: The time it takes the drug to
disintegrate and dissolve to become available for
absorption.
Pharmacokinetics (PK)
The process of drug movement to achieve drug action
involves four phases:
Absorption
Distribution
Metabolism (Biotransformation)
Excretion (Elimination)
Absorption
Passage of a drug from its site of administration into

the bloodstream or body fluids.
Rate depends on the route of administration: Enteral,
Parenteral, Percutaneous.
Mechanisms of absorption: Passive, active, and
pinocytosis.
Bioavailability
A subcategory of absorption. It refers to the

percentage of the administered drug dose that
reaches systemic circulation.
Oral Route: Bioavailability is always less than 100%
due to hepatic metabolism.
Intravenous (IV) Route: Bioavailability is typically
100%.
Distribution
Drugs are transported via circulating body fluids to

their sites of action.
Factors influencing distribution include blood flow,
tissue affinity, and protein-binding effects.
Protein Binding:
Bound drug = inactive.
Free drug = active and able to cause a pharmacologic
response.
Low protein levels (e.g., due to liver/kidney disease)
can lead to drug toxicity.
Metabolism
Primary site: The liver, where drugs are inactivated or

transformed for excretion.
Liver Disease: Alters metabolism, increasing toxicity
risks.
Half-Life (t½): The time it takes for half the drug to be
eliminated.
Excretion
Primary route: Urine (via kidneys).

Other routes: Bile, feces, lungs, breast milk.
Urine pH and kidney function significantly impact drug
excretion.
Pharmacodynamics (PD)
Definition: The drug’s mechanism of action on the
body.
Drug Responses:
Primary Effect: Desirable.

Secondary Effect: Can be desirable or undesirable.
Key Concepts:
Onset: Time to reach the minimum effective

concentration (MEC).
Peak: Highest blood/plasma concentration.
Duration: The length of drug activity.
Receptor Theory:
Drugs interact with cell membrane receptors, which

are mostly proteins.
Four receptor families exist, and drugs can bind to
produce or block responses.
Therapeutic Index/Range:
Safety margin of a drug:
Low Index = Narrow safety margin.
High Index = Wide safety margin, less risk of toxicity.
Therapeutic Range: The range between MEC and the
minimum toxic concentration.
Side Effects/Adverse Reactions
Side Effects: Unintended effects (e.g., drowsiness).

Adverse Reactions: More severe, ranging from hives to
anaphylaxis.
Toxic Effects: Occur when drug levels exceed the
therapeutic range.
1970 – The Controlled Substance Act formed to

remedy drug abuse/dependence
- CI – Illegal drugs (highest dependency/abuse
potential)
- CII – High potential for abuse (physical &
psycological)
& dependency (Meperidine, Morphine)
- CIII – Combo drugs (Codeine preparations) High
Potential for abuse/dependency
- CIV – Medium potential for abuse/dependence
(Valium)
- CV – Limited potential for abuse (Codeine cough
syrup)
➢ Drug Approval Process

Nurse Practice Acts – Every state has its own laws
regarding drug administration by nurses. Can get a
copy.
In a civil court, the nurse can be prosecuted for giving
the wrong drug or dosage, omitting a drug, or giving the
drug by the wrong route.
➢ Drug Approval
Drug Names
Each drug may have several names
Chemical Name – Describes the drugs chemical
structure (most meaningful to the chemist)
Generic Name – Official name for the drug
- Not owned by any drug company
- Universally accepted
Brand/Trade Name – A registered trademark of a drug
company, easier to spell/pronounce
- Cardizem (brand) diltiazem HCL (generic)
➢ Drug Approval
Pregnancy
FDA developed a classification system related to the
effects of drugs on unborn child (fetus)
In drug books and literature, pregnancy category is
indicated for most drugs
- A – No risk to fetus based on studies
- B – Little to no risk based on animal studies, some
Some human studies
- C – Risk indicated based on animal studies. Risk vs.
bene.
- D – Risk to fetus proved. Risk vs. benefit to mother
- X – Risk proved. Avoid during pregnancy

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Pharmacology

Three Phases for Drug Action to Occur:

Definition: The phase in which a drug dissolves and

Definition: The study of the process of drug movement

Definition: The study of how drugs act on the body to

Drug Development Stages

Conducted in laboratories using animal studies to

Phase 1: Tests drug safety and dosage on a small

After clinical trials, drug manufacturers submit a New

Continuous monitoring ensures safety and efficacy

Agonist: A drug that binds to a receptor and activates it

Bioavailability: The portion of a drug that enters the

First-Pass Effect: The reduction of bioavailability when

Half-Life (t½): The time required for half the drug

Loading Dose: A higher initial dose given to rapidly

Maintenance Dose: Regular doses used to maintain

Potency: The amount of drug needed to produce a

Therapeutic Window: The range between the minimum

Toxicity: Harmful effects of a drug when

Tolerance: A reduced response to a drug after

Tablets are not 100% drug-based. Fillers, called

Passage of a drug from its site of administration into

A subcategory of absorption. It refers to the

Drugs are transported via circulating body fluids to

Primary site: The liver, where drugs are inactivated or

Primary route: Urine (via kidneys).

Primary Effect: Desirable.

Onset: Time to reach the minimum effective

Drugs interact with cell membrane receptors, which

Side Effects: Unintended effects (e.g., drowsiness).

1970 – The Controlled Substance Act formed to

➢ Drug Approval Process

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