Pharmacology Drug Examples

Front 1

Mechanisms of Drug action - Receptors - dosing of drugs

sufentanil

Back 1

causes respiratory arrest when used in too high an amount (1 billionth body weight)

triggers a powerful (very sensitive) receptor

Front 2

What general type of receptor does epinephrine act on to cause vasoconstriction?

Back 2

G-protein linked receptors

Front 3

Why is epinephrine given with local anesthetics?

Back 3

Causes vasoconstriction, allowing local anesthetic to stay in place for a longer time

Front 4

What type of receptor is a tyrosine kinase?

Back 4

Catalytic receptor

Front 5

Steroids generally act on what general type of cellular receptors?

Back 5

Intracellular receptors

Front 6

Aspirin exhibits what type of binding to platelets?

Back 6

Covalent binding - aspirin acetylates platelets, permanently preventing their ability to function (as the life of a platelet is roughly 8 days, affected platelets will be knocked out for 8 days)

Front 7

What general type of bonding creates the greatest specificity for a drug interaction?

Back 7

Van der Waals forces (induced dipoles) - as these forces are the weakest and act over the shortest distance, drug must match perfectly with the receptor)

Front 8

Carbonic anhydrase forms carbonic acid from CO2 and H2O, which is a primary cause of altitude sickness.

A drug that inhibits the binding of CO2 and H2O would to the catalytic site of carbonic anhydrase would be a _____ _____ drug.

(sorry, kind of fishing for an answer)

Back 8

Ligand-blocking

Front 9

Name the two types of general interactions that occur between:

1. the benzene ring of epinephrine and the phenylalanine of the beta-adrenergic receptor and

2. the hydroxyl groups on the benzene ring of epinephrine and the serine groups on the beta-adrenergic receptor

Back 9

1. Cation-pi interactions
2. Hydrogen bonding

Front 10

When epinephrine binds to its G-protein receptor, it causes a conformational change in the receptor protein, resulting in release of the intracellular subunits. This type of action is known as...

Back 10

Allosteric Inhibition - drug binds at a non-competing site, causing inhibition of the effector/active site

Front 11

When a drug binds to a non-competing site (other than the effector/active site) on a receptor, improving/enabling binding of substrate to the receptor, this is known as...

Back 11

Allosteric Activation

Front 12

When comparing two drugs that produce similar effects, the one that requires less drug to achieve the desired effect is considered to be more _____.

Back 12

Potent

Front 13

_____ refers to the maximum effect you can achieve with a certain drug.

Back 13

Efficacy

Front 14

_______ is a competitive antagonist for carbonic anhydrase. In order for it to be just 50% effective, it must bind to 99.8% of the receptors. Why?

Back 14

1. Acetylzolamide
2. Since there are many more carbonic anhydrase receptors than needed to achieve maximum effect, any competitive antagonist will have to bind almost all of the receptors to prevent activity

Front 15

Although it takes multiple days to eliminate 1/2 a dose of valium from the body, it only provides its sedative effect for about 4 hours. Why?

Back 15

It only works for about 4 hours because valium is about to leave the Vessel Rich Group (VRG) in a relatively short period of time.

Front 16

Drugs like Clorazepate that are only active after various metabolic steps have converted them into active metabolites are known collectively as...

Back 16

Pro-drugs

Front 17

This is considered to be the most important part of Phase I metabolism.

Back 17

Microsomal oxidation - uses CYP450 to essentially make the drug that is being metabolized more polar/water-soluble

Front 18

This specific cytochrome molecule metabolizes over 50% of all drugs

Back 18

CYP3A4

Front 19

This antibiotic irreversibly binds to and destroys CYP3A4, subsequently diminishing the body's ability to metabolize many drugs

Back 19

Erythromycin

Front 20

Terfenadine, a non-drowsy antihistamine, can cause someone to die when taken in conjunction with Erythromycin. Why?

Back 20

Erythromycin binds to CYP3A4 irreversibly, eventually destroying it. This being the case, terfenadine will not get properly metabolized and will remain in the body, allowing for a lethal dose to accumulate.