PCL201H1 Lecture Notes - Lecture 2: Scurvy, Bioequivalence, Taxus Brevifolia

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14 Sep 2016
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PCL201
Winter 2014
Lecture 2 What is a Drug?
1. What is a drug?
2. What do drugs do?
3. The origin of drugs
Natural, semi-synthetic, synthetic, biologic
4. How are therapeutic drugs developed?
Clinical trials
Drug names
Patent protection and bioequivalence
1. What is a drug?
A chemical substance (other than those essential for normal function) that exerts a biochemical
or physiological effect in a living organism, whether therapeutic or not.
o Can be natural, semi-synthetic or synthetic
o The 3 molecules shown on slide 4 are opiates
Poisons are drugs.
o Toxins: naturally produced (e.g. Botox)
o Toxicants: not naturally produced (e.g. mustard gas analogues)
o Poisons can cause harm but may be used therapeutically at the right dose
o Toxicology: A branch of pharmacology focusing on the undesirable effects of chemically
acting substances
Dietary components, essential nutrients, and endogenous molecules can be drugs if used
outside of normal function (e.g. Vitamin C in orange juice is not classified as a drug, but IS when
used in high doses to treat scurvy)
o “Articles intended for use in the diagnosis, cure, mitigation, treatment, or prevention of
disease" and "articles (other than food) intended to affect the structure or any function
of the body of man or other animals" [FD&C Act, sec. 201(g)(1)]
o Regulated by the FDA in the US and the TBD in Canada
2. What do drugs do?
mimic (agonist) or enhance (positive allosteric modulator) the action of an endogenous
compound
o Salbutamol: β2 adrenergic receptor agonist for relief of bronchospasm in asthma and
COPD
Smooth muscle relaxation
o Diazepam (ValiumTM): Positive allosteric modulator of GABAA receptor (an inhibitory
channel that decreases neuronal activity) used for treatment of anxiety, insomnia, and
seizures
Increases frequency of channel opening when GABA binds more Cl- ions
move through channel more inhibition (CNS depressant)
block* (antagonist*) or impede (negative allosteric modulator) the action of endogenous and
other compounds
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