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RBM3800 Session 1a

Pharmacology is the study of drugs and their actions in living systems. It includes understanding why patients receive certain medications and how they work. Studying pharmacology allows one to understand important terms like bioavailability and phases of drug testing. Drugs have a long history of medical, religious, and social uses. The modern drug development process involves animal testing, clinical trials, and regulatory approval to establish safety and efficacy before marketing. Understanding drug properties, formulations, administration, and interactions with the body aids in appropriate clinical use.

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42 views24 pages

RBM3800 Session 1a

Pharmacology is the study of drugs and their actions in living systems. It includes understanding why patients receive certain medications and how they work. Studying pharmacology allows one to understand important terms like bioavailability and phases of drug testing. Drugs have a long history of medical, religious, and social uses. The modern drug development process involves animal testing, clinical trials, and regulatory approval to establish safety and efficacy before marketing. Understanding drug properties, formulations, administration, and interactions with the body aids in appropriate clinical use.

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Introduction to Pharmacology

Why Do We Study Pharmacology?

• A. It’s good for you


• B. You will be able to use fancy terms like
‘bioavailabilty’ and ‘phase 1’
• C. My lecturer likes to torture students
• D. A competent scientist must understand
why a patient is getting a medication, and
HOW IT WORKS
• E. all of the above
Pharmaceutical Industries
History of Pharmacology
Antiquity to the modern era
The ancients considered
disease a consequence of
demonic possession, or the
wrath of god. Thus, in ancient
times, the treatment of illness
with natural products was
invariably accompanied by
religious rituals deemed
essential to the healing
process.
The use of drugs
Medical/Religious/Social purposes
• Medical purposes
– aspirin, penicillin, metabolic steroids
DMT: https://www.youtube.com/watch?v=LtT6Xkk-kzk
• Pseudo-spiritual/religious purposes
– hallucinogenic drugs : ayahusca, atropine,
marajuana

• Social purposes
– alcohol, tobacco,
– ecstasy
History of Pharmacology
In 1897, Felix Hoffman, a research chemist
employed by the "Farbenfabrikin vorm. Freidr. Bayer
and Co." synthesized acetylsalicylic acid. On
February 1, 1899, Aspirin® was registered as a
trademark. On March 6th of the same year, this drug
was registered with the Imperial Patent Office in
Berlin. Aspirin quickly become popular
worldwide, and remains an important drug today.
(Interestingly, it was not until 1971 that Sir John Vane
discovered the mechanism of action of aspirin, a feat that
earned him the 1981 Nobel Prize for Medicine.)
Pharmacology
 the study of drugs, including their actions and effects in
living systems

Pharmaco
 prefix derived from the Greek work pharmakon,
meaning drug or medicine

Pharmaceutics
 the study of the ways in which various drug
formulations influence the pharmacokinetics and
pharmacodynamics of a drug

Drug formulation
 formulating drugs into different types of preparations
eg. tablet, capsule, solution, suspension, injection
Drug Dose
Administration

Disintegration
Pharmaceutical of Drug

Pharmacokinetics Absorption/distribution
metabolism/excretion

Pharmacodynamics Drug/Receptor
Interaction

Pharmacotherapeutics Drug Effect


or Response
Drug names & classifications
Before a drug is approved and marketed, it
collects three different types of names:

1. chemical name
2. approved / generic / non-proprietary name
3. proprietary / brand / trade name
Chemical name

 a precise description of the drug’s chemical


composition and molecular structure

Approved / generic name


 usually assigned by the manufacturer with the
approval of the local drug regulating authority
and becomes the official drug name
Proprietary / trade name

 when a drug company markets a particular


drug product, it selects and copyrights a
proprietary or trade name for its drug
Example of a commonly prescribed
drug

• Chemical name:
acetylsalicylic acid: acetaminophen

• Approved generic name:


Asprin : Paracetamol

• Trade names:
Aspro Clear : Panadol, Tylenol
Disprin
Steps in Drug Approval Process

• Isolation or development of new chemical


• Animal studies
• Investigational New Drug approval process
– Phase 1 - small numbers; healthy individuals
– Phase 2 - small numbers; subjects with disease
– Phase 3 - large multicenter clinical trials
• New Drug Application
• Clinical Trials
– Kidneys and liver are two most important organs

– In Phase I trials, researchers test a new drug or treatment in


a small group of people (20-80) for the first time to evaluate
its safety, determine a safe dosage range, and identify side
effects.

– In Phase II trials, the study drug or treatment is given to a


larger group of people (100-300) to see if it is effective and
to further evaluate its safety.

– In Phase III trials, the study drug or treatment is given to


large groups of people (1,000-3,000) to confirm its
effectiveness, monitor side effects, compare it to commonly
used treatments, and collect information that will allow the
drug or treatment to be used safely.

– In Phase IV trials, post marketing studies delineate


additional information including the drug's risks, benefits,
and optimal use.
Controlled Substances
High abuse potential with risk of
Schedule I severe dependence; no medical use.
High abuse potential with risk of
Schedule II severe dependence. Some medical
indications

Moderate abuse potential with risk


Schedule III of moderate to low physical
dependence and/or high
psychological dependence.

Low abuse potential with limited


Schedule IV risk of dependence.
Lowest abuse potential with limited
Schedule V dependence risks.
Pregnancy Considerations

• Increased maternal HR, CO and blood volume


– May affect absorption, distribution, effectiveness
• Drugs may cross placenta
• Drugs may cross into breast milk
• Teratogens -thalidemide
Pediatric Considerations

• ⇓ Oral absorption
• Thinner skin (⇑ topical absorption)
• ⇓ Plasma protein concentration
– ⇑ Free protein-bound drug availability
• ⇑ Extracellular fluid in neonate
• Altered metabolic rates
• ⇓ Elimination/metabolism
• BSA/weight based dosing important!
Geriatric Considerations

• ⇓ Oral absorption
• ⇓ Plasma protein concentration
• ⇓ Muscle mass, ⇑ body fat
• ⇓ Liver/renal function
• Multiple drugs
• Multiple diseases
Drug Classification

• By chemistry
– electrolytes
• By mechanism
– Beta blockers
– benzodiazepines
• By disease
– antihypertensives
– Antiemetics
Receptors
Most drugs combine (bind) with specific receptors
to produce a particular response. This association
or binding takes place by precise physicochemical
and steric interactions between specific groups of
the drug and the receptor.
1. Proteins
a. Carriers
b. Receptors
i. G protein-linked
ii. Ligand gated channels
iii. Intracellular
c. Enzymes
2. DNA
Receptor Signaling Pathways
Drug-Receptor Interactions
•Drug-receptor interactions serve as signals to trigger a
cascade of events. This cascade or signaling pathway, is a
collection of many cellular responses which serve to amplify
the signal and produce a final effect.

•Effectors are thus the molecules that translate the drug-


receptor interaction into changes in cellular activity.

•  •+        
EFFECT
DRUG DRUG + RECEPTOR DRUG + RECEPTOR EFFECTOR EFFECTOR
INTERACTION COMPLEX SYSTEM

STIMULUS BINDING ACTIVATION TRANSDUCTION AMPLIFICATION RESPONSE


SIGNALLING PATHWAY

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