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L01 Toxicokinetics and parmaco
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kilo-chicken-harry-fifteen-golf-south
Status
Last Update
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Published
06/22/2023
The basic principle of toxicology:The {{c2::dose}} makes the {{c1::poison}}
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06/22/2023
What is an antidote?A medicine or remedy to {{c1::counteract the effects of a poisin, toxin}}
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What is Pharmacokinetics?The study of how medications move through the body and what the body {{c1::does to the drug at therapeutic doses. }}
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What are components of Pharmacokinetics?{{c1::Absorption}}{{c1::Distribution}}{{c1::Metabolism}}{{c1::Elimination of Drugs}}
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What are the Pharmacokinetic factors of absorption?{{c1::Route, Formulation, Bioavailability}}
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What is toxicokinetics? It is the study of the kinetics of ADME under the conditions in which {{c1:: doses above the therapeutic dose may result …
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Doses above the "therapeutic dose" may result in altered ADME including:- 1. {{c1::Slowed absorption }}- 2. {{c1::Altered distribution }}- 3…
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Pharmacodynamics is what the {{c1::drug}} does the body while Toxicodynamics is what the {{c1::toxicant}} does to the body
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Most commonly, it is the {{c1::dose}} that changes the dynamics from {{c2::pharmacodynamics}} to {{c2::toxicodynamics}}
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Absorption is the process by which {{c1::a xenobiotic enters the body}}The rate and extent of absorption are important because it helps predict …
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What are some things that alter rate and extent of absorption? - {{c1::Formulation of product }}- {{c1::Bioavailability (1st pass effect)}}
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What can slow or decrease Gi absorption?{{c1::- Anticholinergic agents - Hypotension - Concretions / pharmacobezoar/glob of pills}}{{c1::Agg…
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Can ionized molecules cross the phospholipid bilayer?{{c1::NO}}. Only {{c1::unionized}} molecules can cross the phospholipid bilayer
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Which equation can be used to describe the ratio of ionized to unionized molecules at a particular pH?The {{c1::Henderson-Hasselbach}} equatio…
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Ionization state can be {{c1::exploited and used therapeutically}} (i.e. urine alkalization traps ionized weak-acid chemical moieties in urine).&nb…
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Bioavailability affected by: TF FLIPS{{c1::Transporters }}{{c1::First-pass effect}}{{c1::Formulation}}{{c1::Lipophilicity}}{{c1::Ionization}}{{c1::…
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{{c1::Liquids}} have faster rates of absorption.
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{{c2::Bezoars}} are concretions of {{c1::foreign material}} that {{c1::adhere together}} in the {{c3::stomach.}}{{c4::Pharmacobezoars}} are a subtyp…
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Risk of bezoar formation increases with xenobiotics that delay {{c1::gastric emptying, induce pylorospasm, or are enteric-coated.}} …
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What is the First pass effect?It is the {{c1::Metabolism of a xenobiotic before}} it reaches the systemic circulation. Most metabolism is performed…
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What is Activated Charcoal?Activated Charcoal is used to treat {{c1::poisining }}{{c1::Whole bowel irrigation (WBI)}} refers to the administ…
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What is Bioavailabilty? The {{c1::% or fraction of an administered dose that reaches systemic circulation }}
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What is "1st pass effect"? It is a process by which a {{c1::large percentage of medication is extracted}} prior to leaving the liver during the 1…
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Distribution describes the {{c1::reversible transfer of a medication/toxin to and from the site of measurement}} A substance has to {{c1::reach i…
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What are some things that alter distribution?- {{c1::Protein Binding}} - {{c1::Molecular}} Size - {{c1::Lipid}} Solubility - {{c1::Ioni…
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Xenobiotics reach steady state after {{c1::3-5 half-lives (~5 in most cases) }}
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06/22/2023
What is Enterohepatic Recirculation? Enterohepatic Recirculation: Involves substances (e.g. bile salts, drugs) that are {{c1::metaboliz…
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What is the Volume of Distribution? Volume of Distribution is a large factor in determining the feasibility of a substance being dialyzed. S…
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06/22/2023
What is the significance of protein binding when it comes to distribution? Substances can bind to plasma proteins, namely albumin. Changes in {{c…
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06/22/2023
{{c1::Salicylic acid::asprin}} is a weak acid which exists primarily in {{c2::ionized}} state at physiologic pH which is {{c2::impermeable}} to cell m…
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06/22/2023
What is the formula for Volume of Distribution?Vd L/kg = {{c1::dose (mg/kg) / Cp (mcg/ml)}}
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For a medication to be active it has to be {{c1::free::free or bound}} to protein.
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Therapeutic dose vs over dose protein binding- Binding capacity becomes {{c1::saturated}}- Free/bound ratio tends to {{c1::increase}}- More free =>…
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How can we describe metabolism?Metabolism is a complex multi-step process in which Xenobiotic can be metabolized for {{c1::elimination, intermediate m…
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Two phases exist to increase the {{c2::hydrophilicity}} of the compound: Phase 1 – {{c3::oxidation-reduction reactions}} (expose polar groups)Ex:&n…
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Antidotal therapy alters {{c1::alcohol dehydrogenase activity}}
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What is elimination?Elimination is a multi-organ process to rid the body of {{c1::xenobiotics and their metabolites}}. It is an {{c1::irreversible los…
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What causes compounds to display non-linear kinetic elimination profiles?Xenobiotics that undergo the {{c1::same metabolic pathways}} can compete with…
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06/22/2023
Elimination is {{c2::irreversible}} loss of substance from the site of measurement.{{c1::Metabolism}} and {{c1::Excretion}}Total clearance = {{c4::ren…
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Clearance is the {{c1::volume of blood}} that an organ can clear a substance from per unit of time
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Half-life is the amount of time it takes for plasma concentrations of a xenobiotic to {{c1::reduce by half.}} It may be {{c1::constant}} (fir…
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Elimination kinetics can be classified by {{c1::zero-order, first-order, or Michaelis-Menten kinetics. }}
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Zero-order kinetics: {{c1::Fixed amount}} of xenobiotic is eliminated per unit time. Examples: ethanol, phenytoin, sal…
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First-order kinetics: {{c1::Fixed proportion}} of xenobiotic is eliminated per unit time. A large majority (~95%) subst…
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Michaelis-Menten kinetics: A non-linear kinetic state with both {{c1::zero- and first-order kinetics. }}
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Kinetics are dependent on concentration: {{c1::Low}} concentrations ([C] <<< km) = first-order kinetics {{c1::High…
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Enhanced elimination treatments include: {{c1::Multidose activated charcoal::MDAC}}{{c1::whole bowel irrigation, WBI::PEG}}{{c1::urinary alkal…
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What is difference between sustained release vs non-sustained release?Sustained-release (or extended-release) drugs maintain drug release over {{c1::a…
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In regards to bioavailability • IV = {{c1::100%}} bioavailable
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– Lithium• Distribution from plasma to interstitial fluids is{{c1::faster}} then distribution into brain
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Why may t1/2 be slower then expected?– Literature reflects therapeutic doses– Clearance may change in the {{c1::OD}} situation • 1st order to zero ord…
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06/22/2023
Grape juice {{c1::inhibits::inhibits or activates}} cytp450.
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L01:S39EKG with poison patients:What are differences between {{c1::QRS, QTC, and HR}}
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06/22/2023
ANTICHOLINERGIC Toxic Sources: {{c2::anticholinergics}} like {{c3::atropine}}, {{c3::scopolamine}}, {{c3::glycopyrrolate}}or {{c2::anti…
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06/22/2023
CHOLINERGIC Toxic Source: {{c2::Organophosphates}} like {{c3::Carbamates}}, or {{c3::Arecholine}}, or {{c3::Choline}}, or {{c3::Me…
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06/22/2023
OPIODToxic Sources: {{c2::morphine}}, or {{c3::codine}}, or {{c3::tramadol}}, or {{c3::Heroine}}, or {{c3::Fentanyl}}, or {{c3::methadone}}, or {…
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SYMPATHOMIMETICToxic Sources: {{c2::caffeine}}, or {{c3::cocaine}}, or {{c3::amphetamine}}, or {{c3::Ritalin}}, or {{c3::LSD}}, or {{c3::MDMA}}, …
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06/22/2023
SEDATIVE/HYPNOTICToxic Sources: {{c3::anti-anxiety agents}}, or {{c3::muscle relaxants}}or {{c2::antiepileptics}}/{{c2::preanesthetics}} lik…
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Dosis sola facit venenum translates to:
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Which of the following can be a toxin?
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06/22/2023
What is an antidote?
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06/22/2023
Pharmacokinetics is the study of ________, whereas toxicokinetics is the study of _________.
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06/22/2023
Which of the following alters the rate and extent of absorption?
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Which route of administration has 100% bioavailability?
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The first-pass effect refers to:
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06/22/2023
What is a clinical implication of enterohepatic recirculation?
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Distribution is a major component in the ______ to clinical toxicity.
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06/22/2023
What is the significance of protein binding in drug pharmacokinetics?
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The major organ(s) involved in drug metabolism is the_____
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How does half-life relate to the duration of toxicity?
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What is a potential consequence of toxin-induced alteration in metabolism and elimination?
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What does toxicodynamics refer to?
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New Jersey Poison Information Education Service
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