Toxicology- Lyon- Exam 1-Lecture 1 Outcomes (PART 1)

1. Herb/Nutrient/Drug interactions with pharmaceuticals can be deadly or cause nutrient depletions

2. Majority of patients will be on three of more different medications

3. Some patients need medications to survive!

Describe the rational behind having pharmacology as part of the chiropractic program

Toxicology

what is the study of adverse effects of chemical, physical or biological agents on living organism and the ecosystem?

Pharmacology

What is the study of the science of drugs...including their uses, effects and modes of action?

a substance that a person exposes themselves to in order to result in a specific outcome

a drug must interact with a molecule!!

define "drug"

TRUE

t/f: one characteristic of all drugs is they need to interact with a molecule (such as a receptor or enxyme)

NOTHING.

don't require FDA approval and are not required to determine efficacy or safety

What are the FDA requirements for supplements?

An agonist binds to the receptor/enzyme and activates activity

an antagonist binds to the receptor/enzyme to block activity

differentiate between agonist and antagonist

An agonist binds to the receptor/enzyme and activates activity

what is an agonist drug?

an antagonist binds to the receptor/enzyme to block activity

What is an antagonist drug?

Compounds that are similar to a ligand and can bind to the ligand's receptor/enzyme to activate or block activity (agonist or antagonist)

what is an anolog

pharmacodynamics

"What the drug does to the body" is referred to as...

Pharmacokinetics (what the body does to the drugs)

ADME is associated with which one...pharmacokinetics or pharmacodynamics?

pharmacokinetics

"what the body does the the drug" is referred to as...

PK- what body does to drug

PD- what drug does to body

differentiate between pharmacokinetics and pharmacodynamics

1. hormone and NT receptors

2. Enzymes

3. Membrane transport proteins

4. Membrane lipids

What are the 4 drug "targets" or "receptors" discussed in lecture

intracellular receptors are found in the cytosol or nucleus and bind lipid soluble signal molecules (steroid and amines)

whereas

cell surface receptors are only found on the surface of cells within the membrane and bind water soluble molecules (peptides and amines)

Differentiate between intracellular vs cell surface receptors

intracellular receptors

Steroid hormone receptors are what type of receptor class?

1. Ion-channel linked

2. G-protein linked

3. enzymes linked (ex: RTK and non RTK)

what are the three types of cell surface receptors mentioned in lecture?

-respond to the ligand binding

- activate rxns

-coordinate rxns

- induce ampliphication signals

what is the role of secondary messengers formed via signaling cascades

secondary messengers

cAMP and cGMP are examples of what?

response selectivity

(same effectors, different effects)

Tamoxifen acting as an antagonist on estrogen receptors expressed in breast tissue but as an agonist in bone is an example of what?

irreversible-destroys enzymes ability to interact with substrate.

reversible- substrate levels can alter inhibition of the enzyme and it's active site.

defferentiate between irreversible and reversible enzyme ingibitor

irreversible enzyme inhibitors

aspirin and penicillin are examples of what type of enzyme inhibitors?

FALSE: enzyme is cooked no matter how much substrate is present. the irreversible inhibitor is BOUND

T/F: the more substrate present near an irreversible inhibitor, the less the enzyme will be inhibited.

competitive and non-competitive inhibitors

what are the two types of reversible inhibitors?

competitive- competes with substrate for active site. once bound, blocks substrates access to active site.

non-competitive- have a separate binding site away from the substrate's active binding site. Once bound, changes the shape of the substrates active binding site.

differentiate between competitive and non competitive enzyme inhibitors.

(both reversible inhibitors)

TRUE!! substrate levels matter!

T/F: increase in substrate concentration can know the reversible inhibitors off and allow substrate to bind to the active site.

competitive (reversible) enzyme inhibitors

majority of pharmaceuticals are what type of enzyme inhibitors?

the potency

the measure of the amount of a drug necessary to produce the median effect (half of the maximum response, ED50) is what?

efficacy

think--> "biggest bang for your buck"

the measure of the magnitude of the effect of the drug (Emax) is what?

potency is least amount you can use to get the desired effect (think stevia is sweeter than sugar, therefor more potent)

whereas efficacy is the most effective affect you can get with the lowest amount (biggest bang for your buck)

what is the difference between potency and efficacy of a drug? TQ

upregulation

downregulation

When more receptors are available, this is referred to as what?

what about a loss of receptors?

strength of ligand/receptor binding and can alter efficacy of a drug

Affinity and pH can alter what?

the THERAPEUTIC INDEX

The ratio of the dose that produces toxicity in half the population to the dose that is clinically effective (ED50)

What does TD50 mean?

narrow--> effective dose is close to its toxic does. easy to OD

wide-->toxic dose isn't close to effective dose. hard to OD

A therapeutic margin with a "narrow window" vs a "wide window" means what?