Notes in 04DrugBiotransformation

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Published	07/30/2024	The {{c1::liver}} is the primary organ for metabolism
Published	07/30/2024	Biotransformation is AKA {{c1::Metabolism}}
Published	07/30/2024	VR 1. Presence of active metabolites 2. Drug action durationA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 will not af…
Published	07/30/2024	VR 1. Metabolism 2. Effect of Levodopa (a prodrug)A. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Ans…
Published	07/30/2024	{{c1::Minoxidil}} is an antihypertensive/vasodilator prodrug that is now used as a hair grower instead because of its side effects.
Published	07/30/2024	VR 1. Metabolism 2. Effect of amoxicillin (an active drug)A. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect…
Published	07/30/2024	{{c1::Prodrugs}} are drugs that are inactive when administered and become activated when metabolized.
Published	07/30/2024	{{c1::Active → inactive::Determine the Mechanism of Drug Metabolism:}}Paracetamol is converted into a biologically inactive derivative to be excreted.
Published	07/30/2024	{{c1::Inactive → active::Determine the Mechanism of Drug Metabolism:}}Minoxidil is enters the body and exerts its effects once it's converted into min…
Published	07/30/2024	{{c1::Active → active metabolites::Determine the Mechanism of Drug Metabolism:}}Diazepam is metabolized into desmethyldiazepam, which has the same eff…
Published	07/30/2024	{{c1::False::True or False}}All drugs are first modified by the body before elimination.
Published	07/30/2024	{{c1::Phase I (AKA non-synthetic)}} reactions convert the parent drug to a more polar conjugate or inactive product by {{c2::introducing/umasking…
Published	07/30/2024	VR 1. Polar functional groups introduced 2. Drug reabsorptionA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no eff…
Published	07/30/2024	{{c1::Phase II (AKA synthetic)}} reactions convert the parent drug to a more polar conjugate or inactive product by {{c2::conjugating an end…
Published	07/30/2024	VR 1. Methylation 2. Drug excretionA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Answer: {{c1::A}}
Published	07/30/2024	QC Number of drugs that follow this sequence of reactions. 1. Phase II → Phase I 2. Phase I → Phase IIA. 1>2B. 1<2C. 1=2Answer: {…
Published	07/30/2024	The {{c2::Smooth Endoplasmic Reticulum (SER)::organelle}} of the liver has high concentrations of {{c1::Phase I::Phase I/Phase II}} enzymes.
Published	07/30/2024	The class of enzymes for oxidative drug metabolism in the liver is called {{c1::Mixed Function Oxidases (MFOs)}} or {{c1::Monooxygenases}}
Published	07/30/2024	{{c1::True::True or False}}Some compounds are metabolized into reactive intermediates whose toxic reactions are apparent when alternative detoxificati…
Published	07/30/2024	QC Acetaminophen metabolism 1. Glucuronidation (phase II) and sulfation 2. GSH ConjugationA. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	{{c1::r(N-acetylbenzoiminoquinone)::Paracetamol toxic metabolite}} is a reactive metabolite toxic to the liver that generates reactive O2 species (ROS…
Published	07/30/2024	VR 1. r(N-acetylbenzoiminoquinone) 2. Liver cellsA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Answ…
Published	07/30/2024	QC Amount of reactive toxic metabolites of acetaminophen 1. With GSH Conjugation 2. Without GSH ConjugationA. 1>2B. 1<2C. 1=2Answer: {{c1::B}}
Published	07/30/2024	{{c1::Genetic Polymorphism}} is the occurrence of a variant allele of a gene at a population frequency of {{c2::≥1}}%, resulting in altered expre…
Published	07/30/2024	QC Risk in getting adverse drug reactions (ADRs) 1. People with a gene for metabolism of a drug 2. People without a gene for metabolism of a drugA. 1&…
Published	07/30/2024	QC Succinylcholine breakdown 1. Plasma cholinesterase 2. ButyrylcholinesteraseA. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	QC Length of effects of succinylcholine (neuromuscular paralysis) with 1. Plasma cholinesterase 2. ButyrylcholinesteraseA. 1>2B. 1<2C. 1=2A…
Published	07/30/2024	QC Acetylating capacity/speed of 1. Caucasians 2. AsiansA. 1>2B. 1<2C. 1=2Answer: {{c1::B}}
Published	07/30/2024	QC Toxic responses to normal doses of amines 1. Slow acetylators 2. Fast acetylatorsA. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	QC Required dose of Isoniazid 1. Slow acetylators 2. Fast acetylatorsA. 1>2B. 1<2C. 1=2Answer: {{c1::B}}
Published	07/30/2024	{{c1::True::True or False}}Oxidation by P450 isoenzymes are genetically predetermined.
Published	07/30/2024	{{c1::True::True or False}}Charcoal-broiled food induces certain enzymes that can speed up or inhibit metabolism.
Published	07/30/2024	{{c1::Grapefruit}} juice contains {{c2::Furanocoumarin::enzyme inhibitor}} which {{c3::inhibits::enhances/inhibits}} metabolism of co-administered dru…
Published	07/30/2024	VR 1. Cigarette smoking 2. Theophylline (anti-asthma medication) metabolism speedA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Incr…
Published	07/30/2024	QC Drug metabolism rate 1. Males 2. FemalesA. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	VR (Beyond childhood) 1. Age 2. Drug metabolism rateA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2A…
Published	07/30/2024	QC Metabolic rate in 1. Hypothyroidism 2. HyperthyroidismA. 1>2B. 1<2C. 1=2Answer: {{c1::B}}
Published	07/30/2024	VR 1. Alcoholic hepatitis 2. Drug metabolismA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Answ…
Published	07/30/2024	VR 1. Enzyme induction 2. Pharmacologic action/effect of drugsA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has …
Published	07/30/2024	VR 1. Enzyme induction 2. Enzyme synthesis rateA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2A…
Published	07/30/2024	VR 1. Enzyme induction 2. Metabolite-mediated toxicityA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effec…
Published	07/30/2024	QC Enzyme induction 1. Ritonavir (short-term) 2. Ritonavir (long-term)A. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	VR 1. Enzyme inhibition 2. Drug effectsA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Answer: {…
Published	07/30/2024	VR 1. Enzyme inhibition 2. CP450 activityA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has no effect on 2Answer:…
Published	07/30/2024	{{c1::Suicide Inhibitors}} {{c2::irreversibly::reversibly/irreversibly}} inhibit P450s via {{c2::covalent::covalent/electrostatic/hydrophobi…
Published	07/30/2024	VR 1. Cholestyramine (bile acid sequestrant) 2. Digoxin effectsA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has…
Published	07/30/2024	VR 1. Albumin binding 2. Drug travelling to other compartmentsA. Increase in 1, increase in 2B. Increase in 1, decrease in 2C. Increase in 1 has …
Published	07/30/2024	Altered {{c1::Metabolism::Mechanism of drug interaction that produces variation in drug metabolism rate}} can be due to enzyme inhibitors, enzyme…
Published	07/30/2024	QC Acid (& Penicillin) excretion 1. With Probenecid 2. Without ProbenecidA. 1>2B. 1<2C. 1=2Answer: {{c1::B}}
Published	07/30/2024	QC In Additive drug interactions 1. Response elicited by the drugs when combined 2. Combined response of the individual drugsA. 1>2B. 1<2C. 1=2A…
Published	07/30/2024	QC In Synergistic drug interactions 1. Response elicited by the drugs when combined 2. Combined response of the individual drugsA. 1>2B. 1<2C. 1…
Published	07/30/2024	QC In Potentiation drug interactions, the effect of the second drug when: 1. The first drug is present 2. The first drug is absentA. 1>2B. 1<2C.…
Published	07/30/2024	QC In Antagonism drug interactions 1. Response elicited by the drugs when combined  2. Response elicited by the drugs when not combinedA. 1>2B…
Published	07/30/2024	Monooxygenase enzyme activity requires {{c1::NADPH::reducing agent}} and {{c1::molecular oxygen}}
Published	07/30/2024	The two miicrosomal enzymes that play a key role in oxidation-reduction processes in the liver are {{c1::Oxidoreductase (POR)}} and {{c1::Cytochrome P…
Published	07/30/2024	QC Heparin pharmacologic effect as anticoagulant when taken with 1. Cimetidine 2. ProtamineA. 1>2B. 1<2C. 1=2Answer: {{c1::A}}
Published	07/30/2024	Mechanisms of Drug Metabolism in the Body{{c1::1. Active Drug → Inactive Drug2. Active Drug → Active Metabolites3. Inactive (Prodrug) →…
Published	07/30/2024	Phase 1/Non-synthetic reactions:{{c1::HydrolysisOxidationReductionDeamination}}
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