Pharmacology and Drug Policy Lecture Notes

Flashcards covering pharmacology notes including drug policies, FDA trial phases, neurotransmitter systems, receptor dynamics, and pharmacokinetics.

Pure Food & Drug Act (1906)

1906 federal law that established the FDA drug approval process.

Preclinical Animal Studies

First phase of the FDA approval process, taking approximately 5 to 10 years to complete.

Phase 1 Clinical Trial

FDA trial phase focused on safety, involving 20 to 100 healthy volunteers.

Phase 2 Clinical Trial

FDA trial phase focused on efficacy, testing 100 to 500 volunteer individuals who have the target condition.

Phase 3 Clinical Trial

FDA trial phase evaluating safety and efficacy in 1000+ normal people, weighing overall risk versus potential benefit.

Post-Market Surveillance

Phase 4 of FDA approval, monitoring a drug for side effects and outcomes after market release.

Drug Patent

Legal protection granting exclusive rights to a drug for 20 years before generic versions can be produced.

Harrison Narcotics Act (1914)

1914 act regulating drugs based on their addictive potential.

Marihuana Tax Act (1937)

1937 act outlawing marihuana by requiring an unobtainable license, targeting Black and Mexican populations.

Controlled Substances Act (1970)

1970 act establishing the 5-tier drug scheduling system based on medicinal uses and addictive potential.

Schedule 1 Drugs

Drug classification reserved for substances with high addictive potential and no recognized medicinal use, such as Heroin, hallucinogens, MDMA, and weed.

Schedule 2 Drugs

Drug classification for substances with high abuse potential like PCP, Meth, and cocaine.

Schedule 5 Drugs

Drug classification with little or no addictive potential and many medicinal effects, such as cough syrup and Lyrica.

Anti-Drug Abuse Act (1986)

1986 law introducing emergency drug scheduling, civil forfeiture, mandatory minimum sentences, and international trade reduction.

Anti-Drug Abuse Act of 1988

1988 legislation moving legal BAC from $0.10$ to $0.08$, establishing death penalty, and stripping federal aid, licenses, and voting rights for drug offenses.

Harm Reduction

Approach emphasizing help over punishment, using strategies like needle exchange programs, Narcan, safe rides, methadone clinics, and safe injection sites.

Electrical Communication

Intraneuronal communication occurring within a single neuron via ions.

Chemical Communication

Interneuronal communication occurring between neurons using neurotransmitters.

Resting Membrane Potential

Electrical potential of a neuron at rest preparing for a signal, equal to $-70\text{ mV}$.

Excitatory Postsynaptic Potential (EPSP)

Signal causing depolarization (more positive potential) that makes a neuron more likely to fire.

Inhibitory Postsynaptic Potential (IPSP)

Signal causing hyperpolarization (more negative potential) that makes a neuron less likely to fire.

Action Potential Threshold

The required voltage level of $-55\text{ mV}$ that a neuron must reach to fire an all-or-nothing action potential.

Vesicles

Membrane-bound sacs in axon terminals that dock, bind, and release neurotransmitters into the synapse upon an action potential.

Synapse

The physical space between neurons where neurotransmitters are released to bind to receptors.

Acetylcholine (ACH)

Neurotransmitter linked to movement, attention, and memory; increased ACH enhances movement, while Botox decreases ACH.

Dopamine (DA)

Monoamine neurotransmitter linked to reward, attention, movement, and prediction, acting on subtypes D1 through D5.

Serotonin (5HT)

Monoamine neurotransmitter linked to mood, appetite, and sexual behavior, with subtypes 5HT1 through 5HT7.

Norepinephrine (NOR)

Monoamine neurotransmitter (noradrenaline) linked to arousal and stimulation, acting on alpha and beta receptors.

Histamines

Monoamine neurotransmitters linked to arousal, alertness, and itching, with receptor subtypes H1 and H2.

GABA

Primary inhibitory amino acid neurotransmitter in the brain, with receptor subtypes A and B.

Glutamate (GLU)

Primary excitatory amino acid neurotransmitter, with NMDA, AMPA, and Kainate receptor subtypes.

Glycine

Inhibitory amino acid neurotransmitter active primarily in the spinal cord.

Endorphins

Opioid neuropeptides responsible for pain relief, acting on mu and kappa receptor subtypes.

Substance P

Neuropeptide involved in transmitting pain signals.

Anandamide

Endocannabinoid neurotransmitter involved in regulating hunger and sleep.

Synaptic Cleft Structure

Illustration depicting nerve cell structures, vesicles releasing neurotransmitters across the synaptic cleft to receptors, and clearance mechanisms (reuptake, diffusion, degradation).

Ligand

Any molecule that binds to a receptor with some degree of selectivity.

Receptor

Specific site or cellular location where a ligand binds.

Ionotropic Receptor

Receptor type where ligand binding directly opens an ion channel, producing faster and shorter-lasting effects.

Metabotropic Receptor

Receptor type where ligand binding activates a G-protein to open an ion channel, producing slower and longer-lasting effects.

Affinity

Refers to how well a ligand binds to a specific receptor.

Efficacy

Refers to the degree of effect a ligand produces after binding to initiate an action.

Agonist

Drug that binds to a receptor and produces a full effect by activating the receptor.

Antagonist

Drug that binds to a receptor with no efficacy, preventing an effect from occurring.

Competitive Antagonist

Antagonist that binds to and blocks the same receptor site as the primary ligand (e.g., Narcan).

Non-Competitive Antagonist

Antagonist that binds to a different site on the receptor to prevent its activation.

Partial Agonist

Drug possessing partial efficacy that activates a receptor to a lesser maximum degree than a full agonist.

Inverse Agonist

Drug that binds to a receptor and produces a full effect directly opposite to what normally occurs.

Allosteric Modulators

Substances (positive or negative) that bind to a secondary site to change a receptor's overall response.

Potency

The amount of drug necessary to produce a given effect; a rightward curve shift indicates less potency.

$$\text{ED}_{50}$$

Effective dose that produces 50% of the maximum effect in 50% of the test population.

$$\text{LD}_{50}$$

Lethal dose (toxic dose) required to cause death in 50% of the test population.

Therapeutic Index

Safety ratio comparing lethal dose to effective dose ($\text{LD}_{50}:\text{ED}_{50}$).

Physiological Antagonism

Interaction where two drugs produce opposing physical effects by acting through entirely different organ systems.

Potentiated Effect

Interaction where two combined drugs produce an effect GREATER than the simple sum of their individual effects (e.g., cocaethylene).

Pharmacodynamics

Study of what a drug does to the body, distinguishing between specific drug actions and broader drug effects.

Pharmacokinetics

Study of what the body does to a drug, summarized by Absorption, Distribution, Metabolism, and Excretion (ADME).

Bioavailability

The fraction or amount of unchanged drug free in the bloodstream available to bind to receptors.

Upregulation

An increase in the total number of cell receptors, typically occurring in response to reduced neurotransmitter activity or receptor blockade.

Downregulation

A decrease in the total number of cell receptors, typically occurring in response to repeated agonist stimulation.