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Morphine
Opium contains ~10% morphine and it provides strong pain relief
Codeine
Opium contains ~0.5% codeine and is used in Tylenol-3
Ebers Papyrus
Ancient Egyptian medical text describing drug use and purgatives like senna
Ma Huang
Ancient Chinese drug used for coughs and fevers; ephedrine later isolated
Ephedrine
Treats asthma and works as a decongestant
Paracelsus Quote
Any substance can be a poison and dose determines remedy vs poison
Curare Poison
Used on Amazonian arrows to paralyze prey via respiratory failure
Curare Drug
Muscle relaxant used in surgery in controlled doses
Ergot Poison
Nervous effects like hallucinations and convulsions; vasoconstriction leading to limb damage; strong uterine contractions
Ergotamine
Treats migraines by constricting cranial blood vessels
Ergonovine
Stops uterine bleeding after childbirth
Peyote Contains Mescaline
Used in religious rituals and produces hallucinations
LSD Contribution
Helped show mental illness may involve endogenous brain chemicals
Sulfa Drugs
First synthetic antibacterial drugs
Penicillin
First antibiotic discovered by Alexander Fleming
Streptomycin
Antibiotic effective against tuberculosis and gram-negative infections
Basic Research
Identifies drug targets and studies molecular to whole animal effects
Lead Compound
A promising molecule selected for further safety and efficacy testing
Preclinical Pharmacology
Determines drug mechanism of action before human testing
Preclinical Toxicology
Assesses acute, chronic, reproductive, carcinogenic, and mutagenic toxicity
Phase 1 Trial
Tests safety and pharmacokinetics in 20-80 healthy volunteers
Phase 2 Trial
Tests effectiveness and safety in 100-500 patients
Phase 3 Trial
Tests safety and efficacy in 1000+ participants across multiple centres
Randomization
Assigns participants to experimental or control groups without bias
Double Blind
Neither investigator nor participant knows assigned treatment
Placebo
Inactive drug that looks identical to the real drug to control for placebo effect
Gold Standard
Best existing therapy used as control when ethical
Informed Consent
Participants must understand risks and procedures before enrolling
Compliance
How often a participant actually takes medication as intended
Phase 4
Post-market surveillance for rare or delayed adverse effects
Bioequivalence
Generic and brand drugs with same active ingredient and similar blood levels
Drug Target
Cellular molecule (often receptor) where drug produces a response
Endogenous Ligand
Native hormone or neurotransmitter that normally activates receptor
Agonist
Drug that binds and activates receptor
Antagonist
Drug that binds receptor but blocks activation
Antacid Example
Neutralizes stomach acid chemically without receptors
Cholestyramine
Binds bile acids and prevents reabsorption
Dose-Response Relationship
Effect increases with dose until maximal effect is reached
Threshold Dose
Minimum dose required before enough receptors are activated
Maximal Effect
Highest achievable response; increasing dose only adds side effects
ED50
Dose that produces 50% of maximal response or works in 50% of population
Efficacy
Maximum response a drug can produce
Potency
Amount of drug required to reach a given response
Clinical Priority
Efficacy is more important clinically than potency
ADME
Absorption distribution metabolism and excretion are the 4 pharmacokinetic processes a drug undergoes once administered
Absorption
Movement of a drug from site of administration into the blood
Distribution
Movement of a drug from blood to tissues and organs
Metabolism
Chemical conversion of a drug usually in the liver making it more water soluble for elimination
Excretion
Removal of drug from body by kidneys, lungs, GI tract, sweat, or breast milk
Bioavailability
Fraction of an administered dose that reaches systemic circulation in an active form
Thiopental Ultra-Short Action
Action ends due to redistribution from brain to muscle and fat not rapid breakdown
Route-of-Administration Importance
Different routes can change bioavailability and required dose
Sublingual
Drug placed under tongue for rapid systemic absorption
Buccal
Drug placed in the cheek for systemic absorption
Systemic
Affecting the whole body or multiple organ systems
Functional Group
Substituent responsible for characteristic molecular effects
Moiety
A part or functional group of a molecule
Drug-Drug Interaction
One drug changes the biological effect of another leading to variable response
Adverse Drug Reaction
An unwanted effect of a drug that occurs at therapeutic doses (general section content)
Therapeutic Index
Ratio describing margin between therapeutic effect and toxicity (module concept context)
Toxicity
The harmful or poisonous effect of a drug at higher doses (module concept context)
Variability in Drug Response
Patients differ due to age, genetics, sex, disease states, and other drugs (module pharmacokinetic section summary)
Drug Interactions Importance
Interactions can increase or decrease drug levels and alter safety or effectiveness (module section 05 purpose)
Other Drugs Present
Multiple drugs taken together may alter metabolism, absorption, or elimination of each other leading to changed biological effect
Central Nervous System
Brain and spinal cord
Nervous System Function
Transmits electrical impulses to coordinate body function (section purpose)
Neuron
Basic functional unit that receives and transmits nerve impulses (section visuals and summary)
Neurotransmitter
Chemical messenger released from neuron terminal to activate receptors on target cells (section visuals)
Receptor
Protein binding site receiving neurotransmitters to cause cellular response
Synapse
Junction between neurons where neurotransmitter release occurs
Normal Nerve Transmission
Electrical impulse travels along axon then chemical neurotransmitter release at terminals
How Drugs Affect CNS
Drugs can modify neurotransmitter release, receptor activation, or reuptake to alter function (section 06 purpose)
Neurotransmitter Examples
Section discusses various neurotransmitters and receptors in brain (section summary)