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level: Level 2

Questions and Answers List

level questions: Level 2

Question	Answer
Physiologic Factors Influencing Protein Binding	1 Age 2 Gender 3 Pregnancy
Age 1 LOWER concentrations in NEONATES THAN IN ADULTS 2 __ normal substances that BIND ALBUMIN, thus drug-binding to albumin and alpha-1-acid glycoprotein is lower in neonates.	. 1 albumin, alpha-1-acid glycoprotein 2 higher concentrations of FATTY ACIDS and BILIRUBIN
the concentration of both albumin and alpha-1-acid glycoprotein are found to be LOWER IN ADULT __	FEMALES (nonpregnant) explains the slight decrease in the bound fraction of some drugs
1 ALTERATIONS IN THE BINDING OF ALBUMIN-BINDING DRUGS can occur in the __ of pregnancy 2 Since albumin concentration is LOWER and there is an INCREASE IN THE CONCENTRATION of __, the binding of ALBUMIN-BINDING DRUGS IS REDUCED, and HIGHER UNBOUND FRACTIONS are observed	1 (mainly in the THIRD TRIMESTER) 2 free fatty acids
a MAJOR DETERMINANT of drug disposition (distribution)	The BINDING OF DRUG to PLASMA (AND TISSUE) PROTEINS
a VERY IMPORTANT EFFECT ON DRUG DYNAMICS since only the free (unbound) drug interacts with receptors	Binding
Factors of drug-binding to proteins:	1 DISPLACEMENT OF BODY HORMONES or coadministered agent 2 CHANGE IN THE CONFIGURATION OF PROTEIN to another structure capable of binding a coadministered agent 3 INACTIVATION OF THE DRUG BIOLOGICALLY by forming a drug-protein complex
Effects of drug-binding to proteins:	1 FACILITATE THE DISTRIBUTION of drugs 2 INACTIVATE THE DRUG by preventing a sufficient concentration of free drug to develop at a receptor site 3 RETARD THE EXCRETION OF A DRUG
TWO IMPORTANT PLASMA PROTEINS commonly involved in binding with drugs	1. ALBUMIN 2. ∂1-ACIDGLYCOPROTEIN
SYNTHESIZED IN THE LIVER, it is THE MOST IMPORTANT PROTEIN that binds to drug molecule due to its high concentration compared with other proteins MAJOR COMPONENT of plasma proteins RESPONSIBLE FOR REVERSIBLE DRUG BINDING WEAK ACIDIC(ANIONIC) and NEUTRAL COMPOUNDS will tend to BOND WITH IT 5% OF THE TOTAL PLASMA RESPONSIBLE FOR MAINTAINING THE OSMOTIC PRESSURE of the blood and for the transport of endogenous and exogenous substances	ALBUMIN
Also known as __ BINDS TO NUMEROUS DRUGS Have GREATER AFFINITY for BASIC (cationic) SUBSTANCES BINDS ONLY BASIC and HIGHLY LIPOPHILIC DRUGS	∂1-ACIDGLYCOPROTEIN also known as: OROSOMUCOID (∂1-GLOBULIN)
Drug–protein binding may be a __ process.	reversible or an irreversible
a RESULT OF CHEMICAL ACTIVATION OF THE DRUG, which then ATTACHES STRONGLY TO THE PROTEIN or macromolecule by COVALENT CHEMICAL BONDING. It ACCOUNTS FOR CERTAIN TYPES OF DRUG TOXICITY that may occur over a long time period For example, the hepatotoxicity of high doses of acetaminophen is due to the formation of reactive metabolite intermediates that interact with liver proteins.	Irreversible drug–protein binding
implies that the drug binds the protein with WEAKER CHEMICAL BONDS, such as HYDROGEN BONDS OR VANDER WAALS FORCES (WEAK ELECTRIC FORCES)	Reversible drug–protein binding