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Sesion 2 pharm1

Pharm -1- Pharmacokinetics clinical pharmacology

QuestionAnswer
What does ADME stand for Absorption, Distribution, Metabolism(Biotransformation), and Excretion
What is meant by normality Assuming the patient has normal functioning organs especially liver and kidney
A disorder in which organ system would most likely effect absorption of drugs GI tract
Why is knowing pharmacokinetics so important allows effective medication prescribing
What is the goal at the target organ when administering drugs reaching a sustained drug concentration
What is responsible for the distribution portion of the ADME model of pharm Blood Plasma
What is the organ responsible for drug excretion Kidney
What are the 4 processes that we must have an understanding of with pharmacotherapy. Hint 1st one deals with compliance 1)Pharmaceutical process:drug getting into patient 2)Pharmacokinetic Process: drug getting to site of action (absorption/distribution) 3)Pharmacodynamic Process: drug producing pharmacologic effects(desensitization) 4)Therapeutic Process: getting resul
What is the rational/way of thinking when prescribing drugs 1st which drug group to use 2nd which specific drug 3rd dosage 4th regimen
What are things that will effect your drug prescribing Patient Variables pediatric (dosage calculation) Geriatric (go low go slow) Polypharm pathological condition (is the patient not in a normality) Pregnancy
What needs to occur first to allow you to prescribe correctly Hint first one deals with accurate something 1)Accurate Diagnosis 2) know pathophysiology of disease 3)know basic pharmacology and kinetics of drugs in normal and diseased patients 4)translate above into bedside action
What are the different routes of administration in order of fastest absorption and distribution IV, IM, Sub Q, Oral/Anal,
What are the advantages to IV admin immediate absorption, rapid distribution, allows titration, bypasses caustic stomach, reduces irritation, can be given to unconscious patients
What are the disadvantages to IV admin once given can't be removed, possible infection, discomfort, requires skilled admin easy overdose, allergy and irritation
****What is Drug Bioavailability fraction of unchanged drug that reaches systemic circulation. IE how much of the drug survives first pass metabolism in portal circulation.
How is bioavailability measured Compare level of drug after administration with levels of drug if you did IV admin
What is First Pass Metabolism oral administration absorbs through GI tract which goes to portal circulation which first goes through liver for metabolism before going to systemic circulation for distribution
What drug factors affect bioavailability Drug Solubility- lipophilic drugs get absorped better, molecular weight/size Chemical Stability- can it survive low pH of stomach Drug Formulation- particle size, salt form, etc
List the routes of administration from highest to lowest bioavailability IV(100)(R), Transdermal (80-100)slow sustained, IM (75-100), Sub Q (75-100), Rectal (30-100), Oral (5-80), Inhalation (5-100) low because poor administration.
What is drug 1/2life T1/2 time it takes to reduce plasma concentration of drug by 50% only works for 1st order drugs and as long as you don't exceed bodies elimination systems.
What is a steady state of drug admin and how many half lives does it gen take to reach it balance between elimination and input of drug so you get a constant drug concentration in plasma. need 4-5 half lives to reach steady state
What is a therapeutic window the dosage between minimum effective concentration(trough) and minimum toxic level(peak). Some drugs have a large therapeutic window others a small window.
When do you need to redose a patient before you drop back below minimum effective concentration
What are the four mechanisms for absorption Passive diffusion Active transport filtration through pores pinocytosis
what are the characteristics of passive diffusion no energy, drug moves according to concentration gradient, Lipis soluble drugs absorb more readily. Most drugs are lipid soluble and use passive diffusion
What are the characteristics of active transport Uses energy in form of ATP, Highly Specific, uses specific carrier proteins, Saturable. Places that use active transport alot Brain and Placenta
What is Drug distribution process by which drug leaves blood and enters interstitium,
What effects drug distribution blood flow, capillary permeability, drug binding to plasma proteins
How effectively can drugs bind to plasma albumin and why is this important with drug administration upto 98% binding such as with warfarin which if you have a patient take another drug it could know the warfarin off the albumin and cause toxic effects
What is Alpha acid glycoprotein AAG another plasma protein that binds drugs
What is volume of distribution equals Dose/blood concentration of the drug. is amount of drug in body vs amount of drug in the blood
What is biotransformation metabolism of the drug in the body major mode for drug elimination
What is a prodrug drug that needs to be metabolized to activate it
what is the major site of metabolism liver
What can effect biotransformation of a drug Prior Administration of a drug, physiological status of patient, age , genetics and liver function
What can biotrasformation/metabolism result in the drug being changed into. IE inactive metabolite make inactive metabolite, toxic metabolite, active metabolite, change potency, change drug actions.
What is the major cytochrome for biotransformation phase 1 Cytochrome P450
What does cytochrome 3A4 do and what are some of the other cytochromes pretty much metabolizes everything 70% of drugs, others are 1A2, 2A6, 2C19
Phase 2 biotransformation involves what 4 catalyzing agents glucuronyl transferase, sulfotransferase, transacylases, inacivation of and increased water solubility of drugs.
What Drugs does Glucoronidation take care of acetaminophen, diazepam, morphine
What drugs does sulfate conjugation by sulfotransferase take care of acetaminophen, methyldopa
What drugs does acetylation take care of and what condition can result if you are a poor acetylater Isoniazid, sulfonamides, slow acetylators can develop drug induced SLE especially from Hydralazine, Isonazid, procainazide
What is the average GFR 125 ml/min
What is net renal excretion drug filitered at glomerulus+drug actively transported - drug passively reabsorbed throughout tubule
How are drug elimination and excretion different Drugs can be eliminated by metabolism which modifies them, excretion is removing unmodified/metabolized drugs from the body
What is Zero Order Elimination drug is eliminated at a constant rate regardless of concentration
What is clearance volume of plasma that is cleared of a drug per unit time. can be by excretion or metabolism
What is a first order elimination drug is eliminated in proportion to its concentration increase concentration increase elimination most drugs follow first order kinetics
What can effect biotransformation of a drug Prior Administration of a drug, physiological status of patient, age , genetics and liver function
What can biotrasformation/metabolism result in the drug being changed into. IE inactive metabolite make inactive metabolite, toxic metabolite, active metabolite, change potency, change drug actions.
What is the major cytochrome for biotransformation phase 1 Cytochrome P450
What does cytochrome 3A4 do and what are some of the other cytochromes pretty much metabolizes everything 70% of drugs, others are 1A2, 2A6, 2C19
Phase 2 biotransformation involves what 4 catalyzing agents glucuronyl transferase, sulfotransferase, transacylases, inacivation of and increased water solubility of drugs.
What Drugs does Glucoronidation take care of acetaminophen, diazepam, morphine
What drugs does sulfate conjugation by sulfotransferase take care of acetaminophen, methyldopa
What drugs does acetylation take care of and what condition can result if you are a poor acetylater Isoniazid, sulfonamides, slow acetylators can develop drug induced SLE especially from Hydralazine, Isonazid, procainazide
What is the average GFR 125 ml/min
What is net renal excretion drug filitered at glomerulus+drug actively transported - drug passively reabsorbed throughout tubule
How are drug elimination and excretion different Drugs can be eliminated by metabolism which modifies them, excretion is removing unmodified/metabolized drugs from the body
What is Zero Order Elimination drug is eliminated at a constant rate regardless of concentration
What is clearance volume of plasma that is cleared of a drug per unit time. can be by excretion or metabolism
What is a first order elimination drug is eliminated in proportion to its concentration increase concentration increase elimination most drugs follow first order kinetics
Created by: smaxsmith