Pharmaceutical Drugs and Dosage: Complexation and protein binding - Review questions answers
Review questions
6.1 Name the
following coordination compounds?
A. [CoBr(NH3)5]SO4
B. [Fe(NH3)6][Cr(CN)6]
C. [Co(NH3)5Cl]SO4
D. [Fe(OH)(H2O)5]2+
E. (C5H5)Fe(CO)2CH3
6.2 Write
the molecular formulas of the following coordination compounds?
A. Hexaammineiron(III)
nitrate
B. Ammonium
tetrachlorocuprate(II)
C. Sodium
monochloropentacyanoferrate(III)
D. Potassium
hexafluorocobaltate(III)
6.3 Identify
the most prominent human plasma protein?
A. α1-acid glycoprotein (AAG)
B. Human serum albumin
(HSA)
C. Globulin
D. Insulin
6.4 Which of
the following forces are involved in molecular complexes?
A. Hydrogen bonding
B. Hydrophobic
interactions
C. Van der Waals forces
D. Covalent bonding
E. Ionic bonding
6.5 Which of
the following forces are involved in coordination complexes?
A. Hydrogen
bonding
B. Hydrophobic
interactions
C. Van der
Waals forces
D. Covalent
bonding
E. Ionic
bonding
6.6 What are the
important parameters for characterizing drug–plasma protein binding?
A. Protein
concentration
B. Drug concentration
C. Binding affinity
D. Binding capacity
E. Rate of binding
6.7 Explain
the factors affecting plasma protein binding of drugs.
6.8 What is
the effect of plasma protein binding on the dosing regimen of a drug?
Answer:
6.1 A. Pentaamminebromocobalt(III)
sulfate
B. Hexaammineiron(III) hexacyanochromate (III)
C.
Pentaamine cholorocobalt (III) sulfate
D. pentaaquahydroxoiron (III) ion
E.
Cyclopentadienyliron dicarbonyl dimmer
6.2 A. [Fe(NH3)6](NO3)3
B. (NH4)2[CuCl4]
C. Na3[FeCl(CN)5]
D.
K3[CoF6]
6.3 B.
6.4 A, B,
C.
6.5 E.
6.6 A, B,
C.
6.7 The
factors affecting plasma protein binding of drugs are as follows:
• The extent of protein binding of many drugs is a linear function
of partition coefficient P.
• Plasma protein binding may determine the characteristics of drug
action or transport.
• Protein binding changes with drug concentration and protein concentration.
• On increasing the drug/protein ratios, saturation of some sites
can occur and there may be a decrease in binding.
6.8 Only a free drug is
able to cross the capillary endothelium. When protein binding occurs with high
affinity and the total amount of drug in the body is low, the drug will be
present almost exclu-sively in the plasma. As plasma proteins are large
molecules, drugs that are bound to proteins cannot pass out of vascular space.
Thus, plasma protein binding will control the distribution of drugs. As plasma protein
binding increases, the extent of distribution decreases. However, some drugs
may exhibit both a high degree of plasma protein binding and a large volume of
distribution. Binding of drugs to plasma proteins is a dynamic equilibrium. If
the unbound (or free) drug is able to cross biological membranes, the drug may
exhibit an extensive volume of distribution, despite a high degree of protein
binding. As a free drug moves across the membranes and out of vascular space,
the equilibrium will shift, in essence drawing the drug off the plasma protein
to replenish the free drug lost from
vas-cular space. This free drug is now also able to traverse membranes and
leave vascular space. In this way, a drug with a very low free fraction (i.e.,
a high degree of plasma protein binding) can exhibit a large volume of
distribution. Disease states that alter plasma protein concentration may alter
the protein binding of drugs. If the concen-tration of protein in plasma is
reduced, there may be an increase in the free fraction of drugs bound to that
protein. Similarly, if pathological changes in binding proteins reduce the
affinity of the drug for the protein, there will be an increase in the free
fraction of the drug.
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