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NU 624
Exam 2 - Metabolic Pathways
| Question | Answer |
|---|---|
| What are three types of reactions in Phase I metabolism? | Oxidation, reduction, hydrolysis |
| In pharmaceutical metabolism, the word "substrate" refers to the ______________. | Drug |
| What happens in a Phase I reaction? | The original architecture of the drug is changed in preparation for Phase II metabolism. |
| Phase I metabolism is also referred to as ____________. | Biotransformation |
| What types of enzymes are employed in Phase I metabolism | Hepatic microsomal enzymes |
| What is the major enzyme system of Phase I reactions? | CYP450 enzymes |
| What occurs in an oxidation reaction? | Oxygen is added to a molecule, or its oxidative state is changed so the oxygen content is increased |
| Molecular oxygen contains how many atoms? | 2 |
| In an oxidation reaction, the molecule of oxygen is split. What happens to each oxygen atom? | One atom oxidizes each molecule of a drug while the other is incorporated into a molecule of water |
| The loss of an electron is referred to as _____________. | Oxidation |
| Phase I reactions require a (donor/acceptor) electron along with molecular __________. | Donor, oxygen |
| The donor electron in a Phase I reaction occurs in the form of ______________. | Reduced nicotinamide adenine dinucleotide |
| What types of enzymes catalyze both oxidation and reduction reactions in drug metabolism? | CYP450 |
| What change occurs when insufficient amounts of oxygen are available to compete for electrons? | CYP450 enzymes donate electrons to substrates instead of oxygen |
| A reduction reaction results in the ___________ of an electron. | Gain |
| What does the reduction of a drug create? | Free radicals that can attach to cells |
| True/False: The reductive metabolism of drugs is not capable of producing harmful products. | False - the reduction of drugs creates free radicals that can attach to cells to cause toxic outcomes |
| What occurs in a hydrolysis reaction? | Water is added to an ester or an amide to break a bond and form two smaller molecules |
| Adding water to an ester creates what two products? | Alcohol, acid |
| Adding water to an amide creates what two products? | Amine, acid |
| True/False: Amide-type drugs are frequently metabolized via hydrolysis. | False - Amides rarely undergo hydrolysis |
| Name 6 commonly used drugs in anesthesia that undergo hydrolysis. | Succinylcholine, cocaine, neostigmine, esmolol, remifentanil, cisatracurium |
| BONUS: Succinylcholine is utilized in __________ for patients who are categorized as ___________. | RSI, full stomach |
| BONUS: What effect does succinylcholine have on vocal cords? | Causes relaxation |
| BONUS: What purpose is neostigmine serve in anesthesia? | Reversal of nondepolarizing NMBDs |
| BONUS: The cholinergic side effects of neostigmine is offset with the use of what two medications? | Atropine or glycopyrrolate |
| BONUS: Which neuromuscular blockers can have their effects reversed? | nondepolarizing NMBDs |
| After undergoing a Phase I reaction, a drug is now (more/less) polar. | More |
| The addition of _______ or _________ groups in Phase I metabolism allows for Phase II reactions to occur. | Carboxy, hydroxy |
| Give 5 examples of oxidation reactions. | Hydroxylation, deamination, desulfuration, dealkylation, dehalogenation |
| What is hydroxylation? | Process that introduces one or more hydroxy groups (OH-) into a compound |
| Give an example of a hydroxylation reaction. | A minor metabolite of phenobarbital undergoes aliphatic hydroxylation to turn it into an alcohol |
| Phenobarbital is converted to an acid by what metabolic process? | Aliphatic hydroxylation |
| What occurs in a deamination reaction? | An amino radical is removed from a compound |
| Give two examples of deamination reactions. | 1)Cytosine deaminates to uracil 2)d-methylcytosine deamintes to thymine |
| What is the process by which epinephrine and norepinephrine are metabolized? | Deamination |
| What is the end metabolite of epinephrine and norepinephrine deamination? | Vanyllyl mandelic acid (VMA) |
| What occurs in a desulfuration reaction? | A sulfur atom is removed from a molecule and replaced by an oxygen atom |
| What types of medications undergo desulfuration reactions? | Thiobarbiturates |
| What does the prefix "thio" indicate in a medication? | It contains sulfur |
| What does the desulfuration of a thiobarbiturate yield? | oxybarbiturate |
| What do oxybarbiturates further break down into? | Inactive metabolites |
| What is the only halogenated alkane? | Halothane |
| What are the methods of metabolism that break down halothane? | Oxidation, dehalogenation, reduction |
| What does the oxidation of halothane produce? | TFA |
| What does the dehalogenation of halothane produce? | Inorganic bromine and chlorine |
| What does the reduction of halothane produce? | Fluoride and volatile byproducts |
| What two conditions must exist for halothane hepatitis to occur? | Enzyme induction, hepatocyte hypoxia |
| What do the volatile byproducts of the reductive metabolism of halothane cause? | Hepatoxicity and halothane hepatitis |
| Phase II reactions are referred to as _____________ reactions. | Synthesis |
| What does the body do in a Phase II reaction? | Synthesizes a new compound by donating a functional group |
| The donated functional group in a Phase II reaction is usually derived from what type of molecule? | Endogenous acid |
| The new compound formed as a result of a synthesis reaction is referred to as a __________. | Conjugate |
| Give examples of common molecules that synthesize with drugs to form compounds that can be eliminated by the body. (5) | Glucuronic acid, sulfuric acid, acetic acid, glycine, methyl group |
| True/False: The products of Phase II metabolism usually have high levels of bioactivity. | False |
| Conjugation yields a (more/less) polar compound. | More |
| The compound produced in a Phase 2 reaction is highly (ionized/nonionized) at physiologic pH and therefore easily extractable by the kidneys. | ionized |
| The hepatic microsomal enzymes responsible for biotransformation reside in the ________________. | Smooth endoplasmic reticulum |
| What does the name “mixed-function oxidase system” refer to? | CYP450 enzymes include both oxidation and reduction reactions |
| How many CYP iso-enzymes in body are responsible for drug metabolism? | 6 |
| What are the 6 CYP iso-enzymes that metabolize drugs? | 1A2, 2C9, 2C19, 2D6, 2E1, 3A |
| What accounts for the variability of drug metabolism between individuals? | Differences in the amino-acid sequence of CYP iso-enzymes |
| How is hepatic enzyme activity determined? | Genetics and lifestyle habits |
| What is enzyme induction? | The increased activity of hepatic enzymes |
| What is the usually cause of enzyme induction? | Prolonged exposure to drugs or certain chemical compounds |
| What is one substance that can lead to enzyme induction after repeated exposure? | ETOH |
| What are 4 different drugs that have the ability to cause enzyme induction? | Phenobarbital, dilantin, rifampin, carbamazepine |
| Hepatic enzymes can not only be induced, they can also be __________. | Inhibited |
| What antibiotic inhibits CYP enzyme activity? | Erythromycin |
| What are 2 medications affected by the enzyme inhibiting effects of erythromycin? | theophylline, cimetidine |
Created by:
philip.truong
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