Drugs and the Human Body Overview - Basic and Ocular Pharmacology Fall 2025

drug

any chemical agent (other than food) that affects living organisms to cause a physical or emotional change in a person

-OTC (non prescription)

-prescription

What are the 2 types of pharmaceutical drugs?

-legal

-illegal

What are the 2 types of social drugs?

molecules that interact with specific molecular components (targets/receptors) of an organism to cause biochemical and physiological changes within an organism

There is a more technical definition of drugs. What is this definition?

-proteins

-lipids

-nucleic acids

-inorganic elements such as lithium, iron & heavy metals

What types of molecules are represented in pharmacology?

weak

Many organic drugs are (weak/strong) acids or bases.

yes

Can drugs be solid, liquid, or gas?

yes

Can drugs be natural OR synthetic?

small molecules

Natural/synthetic molecules are usually (small/large)?

large molecules

Biologics are usually (small/large) molecules?

more

The larger the molecules, the (more/less) complex it is?

we are better at perfecting small molecule drugs

Are we better at perfecting small or large molecule drugs?

biosimilars

Bigger drugs are __________, meaning they have a highly similar structures to other molecules of their same type.

shape

The _____ of the molecule dictates its binding to the target site

the target site (lock and key model)

The shape of the drug is complementary to what?

chiral molecules (these drugs may have different effects on the body even though they are composed of the same molecules)

mirror image molecules

pharmacology

What is the branch of medicine concerned with the uses, effects, and modes of action of drugs?

pharmacokinetics

What is the branch of medicine that is concerned with the absorption pattern, distribution pattern, metabolism, and excretion of drugs?

-chemical

-generic

-trade name

What 3 types of name can a drug have?

generic name

What is the universal common name of a drug?

indication of the class to which the drug belongs

What does the genetic name provide?

registered trademark of a company

What is the trade name of a drug?

yes

Ex: acetaminophen is marketed as Tylenol, Panadol, Aminophen, Silapap, & Nortemp

Can a single drug have multiple trade names?

yes

Ex: tablet, capsule, cream, ointment, aerosol, patches, eye drops, suspensions

Are there different dosage forms for drugs?

gets the drug to the worksite (place where you want the interaction to occur)

What is the point of having different dosage forms?

-taking drugs to change the way one feels, thinks or behaves

-psycoactive

What classifies a drug as addictive?

from plants

Ex: cocaine from coco leaf, morphine from poppy, marijuana from cannabis plant

In the past, where were many addictive drugs obtained?

Schedule 1

What type of Drug Schedule has the most potential for abuse and dependence?

NO

Do Schedule 1 drugs have medicinal qualitites?

Schedule 2

What Schedule of Drugs has a high potential for abuse and dependence BUT has some medicinal qualities?

Moderate potential for abuse and dependence BUT have acceptable medicinal qualities

What are the defining characteristics of Schedule 3 drugs?

yes -- with strict refill regulations

Do you have to have a Dr Rx to use Schedule 3 drugs?

low potential for abuse and dependence AND has acceptable medicinal qualities

What are the defining characteristics of Schedule 4 drugs?

yes -- but fewer refill regulations

Do you need Dr Rx to use Schedule 4 drugs?

least potential for abuse or dependence and have acceptable medicinal qualities

What are the defining characteristics of Schedule 5 drugs?

yes -- but have the fewest refill regulations

Do you need a Dr Rx to use Schedule 5 drugs?

-stimulants

-opioids

-sedative hypnotics

-antipsychotics

-antidepressants

-psychedelics (allucinogens)

What are some examples of addictive drug classes?

Quinine

Was was derived from Cinchona Tree Bark?

symptoms of malaria

What does quinine help alleviate?

the first artificial dye

In 1856, Perkins tried to synthesize quinine from coal tar which ended in the production of what?

Yes for both

Is drug development costly and take a long time?

true

**Sulphanilamide is an antibacterial with the side effect of lowering glucose levels in the blood and increasing diuretic activity.

**Tolbutamide is a compound that has been optimized to only lower blood sugar levels. Useful for treating Type II Diabetes. Is not not a diuretic.

**Chlorothiazide is a compound that has been optimized to only display diuretic activity. It does not lower glucose levels in the blood.

True or False:

It is possible to enhance a side effect of a drug? What is the example given of this?

yes

**Histamine receptor antagonists

**Blocking H-1 receptor with cyclicine will decrease allergic reactions. Blocking the H2 receptor with cimetidine will decrease gastric acid & ulcers

When dealing with drugs, is selectivity important?

-Safety (#1 reason)

-Efficacy

What are the 2 main reasons that drugs fail in clinical trials?

no

Does the clinical trial process ALWAYS pick up on potential problems with drugs?

-drug dosage

-amount of drug available at the target site

-other meds

-living conditions

-history of disease

-age

-drug response

-side effects

What are some factors that will influence the way a drug reacts in the body?

A drug given at one dose has different concentrations in different people

Why is the dosage of drugs important?

yes

True or False:

A drug at concentration in the plasma can create different responses in different people

in the therapeutic range

What range (plasma conc) do you want a drug to be in to have the desired effect in the body?

Tyramine intake can cause hypertensive crisis in persons taking an MAO inhibitor (which increases norepinephrine release). Tyramine increases the release of NT in the body (including NorE) normally. When not broken down, NT will build up.

Tyramine (which is in cheese, red wine, beer, and other foods) can cause a hypertensive crisis. How?

Grapefruit juice will inhibit the action of CYP3A4 which is a liver enzyme that normally breaks down Amiodarone. Without it, amiodarone will build up in the body and patients risk overdose.

How can grapefruit juice interact with the medication amiodarone?

there is a decrease in drug metabolism and/or excretion. Drugs are not eliminated as well from the body and they build up. Patients with these diseases will have to take LESS amount of the drugs.

What is the problem with taking drugs & having diseases of the liver or kidneys?

No, no two individuals will react alike and behave alike under the abnormal conditions which we know as disease

Do all bodies react the same to medications?

pharmacogenomics

What is the study of how genes affect a person's response to drugs?

pharmacology (science of drugs) and genomics (study of genes and their functions) to develop effective, safe medications, and doses tailored to a person's genetic makeup

What does pharmacogenomics combine?

-identify patients and dosing to maximize efficacy of a drug

-minimize new & existing drug ADRs by identifying those at risk

-guide patient selection for smaller, cheaper, more successful clinical trials

-rescue failing clinical drugs by identifying responder subgroups

-lower dosing of drugs to prevent side effects

What are the main goals of pharmacogenomics?

SNP (single nucleotide polymorphism)

the most common type of genetic variation among individuals

a difference in a single DNA building block, called a nucleotide

**each nucleotide change can change the proteins that the gene will code for

What does each SNP represent?

true

**A SNP profile can be used to stratify patients and to try to find variants in the population.

True or False;

Different SNPs can help researchers determine the dosaging of meds that are required for individual patients?

Some DNA variations have no negative effects on protein structure and function. Other variations can lead to genetic disease or increased susceptibility to a disease

Is a SNP always bad? Are some normal?

Yes, there can be silent mutations when a gene encodes the same amino acids even after mutation. Proteins will have the same shape and function

Is it possible to have a mutation in a SNP but no change occur in the protein that is encoded?

Yes, there is vast research that supports the effects of SNPs on Drug-Metabolizing Enzymes on Plasma Conc.

Can SNPs affect drug properties (ie. metabolism)? How?

Alcohol Flush Reaction occurs when those with a ALDH2 (aldehyde dehydrogenase) deficiency drink alcohol. This is a result of not being able to break own acetaldehyde. There is a large build up and face gets flush red.

What would happen if there was a SNP that changed the metabolism of ethanol in the body?

** In this diagram, when a person takes sertraline and variants of CYP2D6 metabolize the same. This means sertraline is NOT metabolized by CYP2D6? The same drug can be given to everyone.

**Imipramine exclusively metabolized by CYP2D6. There are wild differences in the amount of drug you need to give patients. Have to give ultrametabolizers MORE of the drug and poor metabolizers LESS of the drug.

Which drug's metabolism does CYP2D6 appear to play a major role? **see pic

Yes

**For example, Arg-β1AR is more responsive to the effects of Bucinfolol, a β-blocker, than Gly-β1A. Had the clinical trial been run exclusively on patients with homozygous Arg-β1AR, the results presumably would have looked fantastic, and the drug might have become the standard measurement. Instead, bucindolol was never approved.

Can SNPs affect the drug target?

-regulates cell proliferation

-expresses few hormone receptors that would make them susceptible to Tamoxifen

15-30% of breast cancer patients have an overabundance of HER2 receptors on their tumors. What is the effect of this?

Herceptin

What drug was created to bind to the extracellular domain of the HER2 receptor on tumor of patients with breast cancer?

True

**Herceptin on breast cancer patients with HER2 receptors on tumor

True or False:

It is important to look at the combination of a drug's target and the defined subgroups of patients (with a diagnostic assay) to try to identify the right patients to use specific drugs on?

polygenic

Most disease are ____, which may require more than one target to be addressed

More RARE SNPs. These vary by geography and ethnicity.

** The ones common in one population may not be common in another

Are there more "common" SNPs or "rare" SNPs?

yes -- gender, weight, age, smoking, disease state, diet, alcohol, other remedies, patient compliance, etc.

Does the bodies response to drugs depend on other factors besides genetics?

Hospitalization rates for heart patients were reduced by 30% when genetic information was available to doctors who are prescribing drugs

What are the findings of the Mayo-Medco Warfarin Effectiveness Study?