2 Pharmaceutics Exam 2 - Molecular Interactions

☆ - Dr Guo mentions "may ask this on exam"; ★ - Dr Guo says will be on exam/wants you to remember

★ Identify how many ligands there are in this image.

6

★ What is the central metal?

★ What is the ligand?

☆ How many primary valences are in the image?

3

☆ How many secondary valences are in the image?

6

☆ What is the secondary valence equal to?

the coordination number/number of ligands

What is the coordination number?

the number of bonds to the central metal ion; it is not the number of ligand

★ What is EDTA used for?

to treat poisoning of heavy metals

What is cisplatin used for?

to treat cancer

★ What are the benefits of cyclodextrin complexation?

• increase solubility

• increase bioavailability

• increase stabilization

• decrease toxicity

What is the main plasma protein?

albumin

What is human serum albumin?

most abundant protein

multifunctional protein

• contributes to osmotic pressure

• provides acid base buffering action

• transporter protein for endogenous molecules

• binding site for drug and toxins

★ How many drug binding sites do HSAs have?

two drug binding sites

What happens when there are two drugs that bind to the same HSA drug site?

they will compete for binding

What happens if the drug binds to a protein?

it won’t have therapeutic effects

What happens when a drug binds to a receptor?

it will result in a therapeutic response

What happens if the drug is free?

it will result in side effects

What is affinity?

measure of strength of interaction between the protein and drug molecule (Ka)

If the Ka increases, what happens to binding?

the binding will be stronger

Phenylbutazone has a higher Ka than Warfarin, when they are administered together, you would expect:

A. increase in protein bound warfarin
B. increase in free warfarin

increase in free warfarin

Class I drugs

dose is less than available binding sites; most drug molecules are bound to albumin and the concentration of the free drug is low

Class II drugs

dose is greater than available binding sites; most albumin molecules obtain a bound drug, and the concentration of free drug is significant

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Formula provided