Term
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Definition
| Complexation is the interaction between two or more compounds to form a complex. |
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Term
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Definition
| A central atom or ion (usually metallic) bound to surrounding molecules or ions known as ligand. |
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Term
| What is the term for the atom within the ligand bound with the central atom/ion? |
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Definition
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Term
| What is the term for the central atom/ion in a complex? |
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Definition
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Term
| Define coordination number |
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Definition
| The maximum number of bonds the substrate (central) atom can form |
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Term
| What are some qualities that complexation can effect? |
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Definition
-Enhance aqueous solubility
-Enhance drug stability
-Drug delivery
-Receptors at the site of action |
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Term
| Give an example of when complexation is harmful in drug delivery |
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Definition
| Tetracyclines should not be consumed with dairy because of complexation with calcium, lowering solubility |
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Term
| Define inorganic metal ion complexes |
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Definition
In this type of complex, each ligand donates a pair of electrons to form a coordinate covalent link between itself and the central ion.
A Lewis acid-base interaction, monodentate |
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Term
| Define chelate metal ion complex |
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Definition
| Two or more donor groups (ligands) combine with a central ion. The ligands are polydentate (i.e. multiple bonded) |
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Term
| What are the two types of metal ion complexes? |
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Definition
1. Inorganic metal ion complex
2. Chelate |
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Term
| Define organic molecular complexes |
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Definition
A substrate-ligand interaction held together by weak forces (noncovalent)
Can form between two small or a small and a large molecule |
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Term
| Define inclusion compounds |
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Definition
| A complex that results from the architecture of the molecules rather than their chemical affinity |
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Term
| Define cyclodextin complex |
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Definition
The most common inclusion complex.
Donut-shaped cyclic D-glucopyranose with a drug molecule incorporated inside (host+guest) |
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Term
| What is the size range of a cyclodextrin cavity? |
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Definition
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Term
| What is the difference between alpha, beta, and gamma cyclodextrins? |
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Definition
How many glucose molecules are in the ring
Alpha- 6 glucose
Beta- 7 glucose
Gamma- 8 glucose |
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Term
| Define channel latice type inclusion compound |
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Definition
Cholic acids in combination with paraffins, organic acids, and aromatic compounds
Similar structures result from urea or starch-iodine |
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Term
| Define layer type inclusion compounds |
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Definition
Drug between layers
Ex. bentonite |
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Term
| Define clathrate type inclusion compounds |
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Definition
Cage-like lattice, but no bonds inside cage
Ex. Warfarin sodium |
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Term
| Give the equation for Ka between protein and ligand |
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Definition
Ka=[PL]/[P][L]
Ka has units 1/M |
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Term
| Define capacity of binding (v) |
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Definition
| The number of ligand binding sites in a protein molecule |
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Term
| What is the most important plasma protein? |
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Definition
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Term
| What is the molecular weight of albumin? |
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Definition
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Term
| What kind of drugs bind to albumin? |
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Definition
| Many acidic (anionic) drugs, including warfarin and ibuprofen |
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Term
| What is hypoalbumeninemia, and what can cause it? |
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Definition
Low levels of protein-binding albumin
Can be caused by liver disease, such as cirrhosis |
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Term
| What is hyperalbumeninemia, and what can cause it? |
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Definition
High levels of protein-binding albumin
Can be caused by dehydration and some neurological disorders
(Very rare, hypoalbumeninemia is much more common) |
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Term
| What are the three major drug-binding plasma proteins? |
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Definition
1. Albumin
2. α1-Acid glycoprotein
3. Lipoproteins |
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Term
| Why is it necessary to adjust the dose of warfarin in the presence of salicylates? |
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Definition
Because they compete for binding to albumin, and will each end up with more in the active, free form.
So it can lead to overdose of warfarin |
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Term
| What is the molecular weight of α1-Acid glycoprotein? |
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Definition
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Term
| What kind of drugs bind to α1-Acid glycoprotein? |
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Definition
Many basic (cationic) and neutral drugs
Ex. lidocaine, propanolol
But note- some drugs that bind to α1-Acid glycoprotein can also bind to albumin |
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Term
| It is more common to have low levels of albumin than high levels. Is this the same for α1-Acid glycoprotein? |
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Definition
| No, it is more common to have high α1-Acid glycoprotein levels |
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Term
| What is the plasma concentration of lipoproteins? |
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Definition
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Term
| What kind of drugs, generally, bind to liporproteins? |
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Definition
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Term
| Where are all major drug-binding proteins synthesized? |
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Definition
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Term
| How is Km, Ka, and affinity related? |
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Definition
Km and affinity are inversely related
Ka and affinity are directly related |
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Term
| Other than the major binding proteins, what blood components are known to bind drugs? |
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Definition
| Immunoglobulins and erythrocytes |
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