FAR 381
Lecture 1 general principles
Pharmacology
Study of the effects of drugs on the function of organisms
• Breakdown of term
- ‘Pharmakon’ = remedy/poison (can refer to both)
- Paracelsus (all things are poison, and nothing is without poison; the dosage
alone makes it so a thing is not a poison)
- ‘-logia’ = study of
• Pharmacology includes
- Naturally-derived medicines
- Synthetic compounds
- Bio-engineered molecules
Pharmacological treatment
• Disease management aims to restore homeostasis in diseased states
- Physical therapy
- Psychotherapy
- Surgery
- Medicines (pharmacotherapy)
• Disease management often requires biological interactions
- Ensures alleviation of a disease’s specific characteristics
Drugs and medicines
• Drug
- Chemical substance of known structure, other than a nutrient or essential
ingredient, which produces a biological effect in living organisms
- E.g. we know exactly what caffeine looks like
- And it is not a nutrient or essential ingredient like vitamins
- Must be administered, not released endogenously
- E.g. insulin produced inside the body is not a drug, but insulin administered
by injection is a drug
- Medicines, research tools or recreational (illicit drugs)
,Medicine
• Chemical preparation of an agent(s) administered with the intention of producing a
therapeutic effect
• Various types to accommodate bioactivity and use
- Small molecules (e.g. adrenaline or atropine)
- Chemically synthesized or extracted from source
- Biopharmaceuticals (e.g. monoclonal antibodies)
- Large proteins produced through biotechnology
- Gases (e.g. sevoflurane or halothane)
- Volatile substances that make ideal anaesthetics
Quiz
• Which one of the following is the generic name of the drug in
the picture?
A. Nexium
B. Esomeprazole
Generic name/active compound
• Chemical name or identification of compound (e.g. paracetamol)
Trade name
• Name of medicine given by manufacturer (e.g. Panado)
Generic drugs
• DON’T confuse with a generic name!
Quiz
• Which of the following statements about generic drugs are myths?
A. Less effective than the original
B. Costs less than the original
C. More toxic than the original
D. Less research done that the original
Generic drugs
• Copies of innovator/originator drug (original), with exactly the same pharmacological
characteristics
,• Myths
- Poorly made
- A few manufacturing companies have poor GMP
- Strictly regulated and dealt with legally
- Impure chemicals used
- Results in treatment failure
- Not regulated
Different
Different Less animal/human research and
Extensive animal/human research thus less expensive (20-80%)
more expensive Different appearance (copyright)
Different nactive ingredients (e.g.
flavourings, preservatives)
Same
Active ingredient
Dosage form and strength
Route of administration
Bioequivalence (same rate and extent of absorption)
Quiz
• What needs to be proven first in the drug development pipeline?
A. Biological benefit in an animal model
B. Biological benefit in a human model
Drug discovery
• Several sources
- Natural (e.g. microorganisms, aquatic organisms, plants)
- Serendipitous discovery
- Chemical synthesis
- In silico design
- In silico fishing
, Drug development
• Pre-clinical assessment (± 4 years)
- Drugs undergo extensive in vitro and in vivo testing
- Only those that present with potential are further subjected to clinical trials
• Clinical trials (± 12 years in total, high failure rate)
- Phase I: safety in humans (10 to 20 healthy volunteers)
- Phase II: efficacy in humans (100 to 200 patients)
- Phase III: confirmation of phase I and II in larger population group (>1000 patients)
- Approval: granted based on safety and efficacy
- Phase IV: post-marketing phase
Medicinal formulations
• Various forms exist depending on route or use
- Capsules
- Tablets
- Creams/ointments/gels
- Emulsions
- Solutions (eye drops, injections)
- Powders
- Patches
- Suppositories
- Syrups
- Gases
Important terms
• Compliance
- Patient’s adherence to a recommended treatment
- Non-compliance may lead to treatment failure
- Non-compliance can also be not taking medication correctly (e.g. not taking
it with food. This can cause treatment failure and also more adverse effects)
• Contraindication
- An indication where drug usage should be avoided (illness, characteristic (e.g.
pregnancy) or interactions (e.g. with other medicines))
Lecture 1 general principles
Pharmacology
Study of the effects of drugs on the function of organisms
• Breakdown of term
- ‘Pharmakon’ = remedy/poison (can refer to both)
- Paracelsus (all things are poison, and nothing is without poison; the dosage
alone makes it so a thing is not a poison)
- ‘-logia’ = study of
• Pharmacology includes
- Naturally-derived medicines
- Synthetic compounds
- Bio-engineered molecules
Pharmacological treatment
• Disease management aims to restore homeostasis in diseased states
- Physical therapy
- Psychotherapy
- Surgery
- Medicines (pharmacotherapy)
• Disease management often requires biological interactions
- Ensures alleviation of a disease’s specific characteristics
Drugs and medicines
• Drug
- Chemical substance of known structure, other than a nutrient or essential
ingredient, which produces a biological effect in living organisms
- E.g. we know exactly what caffeine looks like
- And it is not a nutrient or essential ingredient like vitamins
- Must be administered, not released endogenously
- E.g. insulin produced inside the body is not a drug, but insulin administered
by injection is a drug
- Medicines, research tools or recreational (illicit drugs)
,Medicine
• Chemical preparation of an agent(s) administered with the intention of producing a
therapeutic effect
• Various types to accommodate bioactivity and use
- Small molecules (e.g. adrenaline or atropine)
- Chemically synthesized or extracted from source
- Biopharmaceuticals (e.g. monoclonal antibodies)
- Large proteins produced through biotechnology
- Gases (e.g. sevoflurane or halothane)
- Volatile substances that make ideal anaesthetics
Quiz
• Which one of the following is the generic name of the drug in
the picture?
A. Nexium
B. Esomeprazole
Generic name/active compound
• Chemical name or identification of compound (e.g. paracetamol)
Trade name
• Name of medicine given by manufacturer (e.g. Panado)
Generic drugs
• DON’T confuse with a generic name!
Quiz
• Which of the following statements about generic drugs are myths?
A. Less effective than the original
B. Costs less than the original
C. More toxic than the original
D. Less research done that the original
Generic drugs
• Copies of innovator/originator drug (original), with exactly the same pharmacological
characteristics
,• Myths
- Poorly made
- A few manufacturing companies have poor GMP
- Strictly regulated and dealt with legally
- Impure chemicals used
- Results in treatment failure
- Not regulated
Different
Different Less animal/human research and
Extensive animal/human research thus less expensive (20-80%)
more expensive Different appearance (copyright)
Different nactive ingredients (e.g.
flavourings, preservatives)
Same
Active ingredient
Dosage form and strength
Route of administration
Bioequivalence (same rate and extent of absorption)
Quiz
• What needs to be proven first in the drug development pipeline?
A. Biological benefit in an animal model
B. Biological benefit in a human model
Drug discovery
• Several sources
- Natural (e.g. microorganisms, aquatic organisms, plants)
- Serendipitous discovery
- Chemical synthesis
- In silico design
- In silico fishing
, Drug development
• Pre-clinical assessment (± 4 years)
- Drugs undergo extensive in vitro and in vivo testing
- Only those that present with potential are further subjected to clinical trials
• Clinical trials (± 12 years in total, high failure rate)
- Phase I: safety in humans (10 to 20 healthy volunteers)
- Phase II: efficacy in humans (100 to 200 patients)
- Phase III: confirmation of phase I and II in larger population group (>1000 patients)
- Approval: granted based on safety and efficacy
- Phase IV: post-marketing phase
Medicinal formulations
• Various forms exist depending on route or use
- Capsules
- Tablets
- Creams/ointments/gels
- Emulsions
- Solutions (eye drops, injections)
- Powders
- Patches
- Suppositories
- Syrups
- Gases
Important terms
• Compliance
- Patient’s adherence to a recommended treatment
- Non-compliance may lead to treatment failure
- Non-compliance can also be not taking medication correctly (e.g. not taking
it with food. This can cause treatment failure and also more adverse effects)
• Contraindication
- An indication where drug usage should be avoided (illness, characteristic (e.g.
pregnancy) or interactions (e.g. with other medicines))
