Renal clearance 2k19 08-26
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This document discusses renal clearance, which is the volume of plasma cleared of drug per unit of time by the kidneys. Renal clearance is determined graphically by plotting the rate of drug excretion in urine against the plasma drug concentration to calculate the slope, which equals clearance. Factors that can affect renal clearance include physicochemical drug properties, plasma concentration, distribution/binding characteristics, urine pH, blood flow to the kidneys, and disease states. The concept of clearance is now applied to describe drug elimination by organs like the liver, lungs and bile.
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1. After entering systemic circulation, drugs undergo disposition processes like distribution and elimination. Distribution involves the reversible transfer of drugs between compartments while elimination causes the irreversible loss of drugs from the body.
2. Several factors affect the distribution of drugs between compartments including tissue permeability, which depends on a drug's physicochemical properties and ability to pass physiological barriers. Organ size and blood flow rates also influence distribution.
3. Binding of drugs to blood components or extracellular tissues can impact distribution by altering a drug's ability to pass between compartments. Other miscellaneous factors like age, disease states, and drug interactions also affect distribution.
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This document discusses renal clearance, which is the volume of plasma cleared of drug per unit time through the kidneys. Renal clearance is affected by physicochemical drug properties, plasma concentration, distribution, binding, urine pH, blood flow to kidneys, and disease states. Physiological processes involved in renal clearance include glomerular filtration, tubular secretion, and tubular reabsorption. The clearance ratio compares a drug's clearance to inulin clearance to determine the excretion mechanism. Renal clearance can be determined graphically or using model-independent methods involving the amount of drug excreted in urine and area under the plasma concentration-time curve.
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2. Irrational drug use can occur due to issues like lack of information, over-prescription, and promotional activities by pharmaceutical companies. It can lead to harmful effects like increased resistance and adverse drug reactions.
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Pharmacology introduction to a.n.s
The autonomic nervous system regulates involuntary bodily functions and is divided into the sympathetic and parasympathetic divisions. The sympathetic division is responsible for the "fight or flight" response and increases heart rate and blood pressure. The parasympathetic division acts to slow the heart and aid digestion. Most organs receive dual innervation from both divisions to allow dynamic regulation of functions. Neurotransmission within the autonomic nervous system uses acetylcholine or norepinephrine/epinephrine as neurotransmitters. Postsynaptic responses are mediated through direct ion channel coupling or via second messenger systems to regulate various cellular processes.
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Absorption Pharmacokinetics.pptx
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Factors affecting distribution of drug
1. After entering systemic circulation, drugs undergo disposition processes like distribution and elimination. Distribution involves the reversible transfer of drugs between compartments while elimination causes the irreversible loss of drugs from the body.
2. Several factors affect the distribution of drugs between compartments including tissue permeability, which depends on a drug's physicochemical properties and ability to pass physiological barriers. Organ size and blood flow rates also influence distribution.
3. Binding of drugs to blood components or extracellular tissues can impact distribution by altering a drug's ability to pass between compartments. Other miscellaneous factors like age, disease states, and drug interactions also affect distribution.
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This document discusses pharmacokinetic variability due to renal disease. It defines pharmacokinetic variability as differences in drug concentration at the site of action due to inter-individual differences in absorption, distribution, metabolism and excretion of drugs. Renal disease affects these processes and increases pharmacokinetic variability compared to healthy individuals. Creatinine clearance is used to assess renal function and determine appropriate dose adjustments for drugs eliminated renally. The effects of renal impairment on drug absorption, distribution, metabolism and elimination are explained. Dose regimens should be adjusted based on creatinine clearance levels to prevent toxic drug accumulation.
comprehensive-clinical-nephrology-e-book.pdf
This document discusses the assessment of glomerular filtration rate (GFR). It begins by explaining that GFR is the best measure of kidney function and declines with kidney disease. It then describes how GFR is estimated using equations that incorporate factors like creatinine, cystatin C and urea levels. It explains the limitations and sources of error in measuring and estimating GFR. The document provides details on measuring GFR directly using clearance of exogenous markers like inulin and endogenously through clearance of creatinine, cystatin C and urea. It compares the properties and use of these endogenous markers in estimating equations.
Drug dose adjustment for liver diseases
This document discusses drug dose adjustment for liver diseases. It explains that the liver is important for drug elimination and abnormalities can affect drug clearance and metabolism. Diseases like hepatitis, carcinoma, necrosis and cirrhosis impact drug elimination by decreasing hepatic clearance and increasing half-life. The hepatic extraction ratio determines if a drug is highly, intermediately or poorly extracted by the liver, affecting how liver disease impacts dosing. Drugs with low hepatic extraction are more dependent on liver function, so doses may need adjustment for liver disease. Antipyrine, which is only eliminated by the liver, is used to assess hepatic abnormalities.
Antibiotic Dosing During Renal Failure
This document discusses antibiotic dosing during renal failure. It explains the importance of dose adjustments with renal impairment due to decreased drug elimination. It compares methods to calculate glomerular filtration rate (GFR) and creatinine clearance, such as the Modification of Diet in Renal Disease (MDRD) and Cockroft-Gault equations. It also describes different types of dialysis and considerations for dosing antibiotics in patients receiving dialysis or continuous renal replacement therapy.
2010 uptodate adequacy dp
1) Recent studies have suggested that lower levels of weekly solute clearance through peritoneal dialysis are adequate, challenging previous guidelines recommending higher targets.
2) The ADEMEX and Hong Kong trials found no difference in patient survival between higher and lower dialysis dose groups, suggesting a minimum delivered weekly Kt/V of 1.7 may be sufficient.
3) The 2006 KDOQI guidelines established a minimum delivered weekly Kt/V target of 1.7 based on these studies, lower than the previous target of 2.1. Maintaining solute clearance above this minimum is recommended to optimize patient outcomes and longevity on peritoneal dialysis.
Drug Dosing in Renal Failure.pdf
This document discusses drug dosing considerations in patients with renal failure or impaired kidney function. It provides information on how the kidneys normally clear drugs from the body and how renal dysfunction impacts drug elimination. Factors that affect renal clearance are described. Methods for assessing renal function, such as creatinine clearance, are outlined. The document also discusses how drug dosages need to be adjusted in patients with renal disease to account for decreased drug clearance and elimination. Equations for estimating glomerular filtration rate and creatinine clearance are presented to aid in renal function determination and dosage adjustment.
35 effects of renal disease on pharmacokinetics
This document discusses the effects of renal disease on pharmacokinetics. It covers how renal disease impacts drug elimination through the kidneys, drug metabolism in the liver, and drug distribution. Key points include that renal drug clearance declines with impaired kidney function, which can impact drug dosing. Protein binding changes can also affect drug levels as kidney function declines.
Clinical pharmacokinetics and its application
Clinical pharmacokinetics and its application--
1)definition
2) APPLICATIONS OF CLINICAL PHARMACOKINETICS
Design of dosage regimens:
a) Nomograms and Tabulations in designing dosage regimen,
b) Conversion from intravenous to oral dosing,
c) Determination of dose and dosing intervals,
d) Drug dosing in the elderly and pediatrics and obese patients.
Pharmacokinetics of Drug Interaction:
a) Pharmacokinetic drug interactions
b) Inhibition and Induction of Drug metabolism
c) Inhibition of Biliary Excretion.
Therapeutic Drug monitoring:
a) Introduction
b) Individualization of drug dosage regimen (Variability – Genetic, Age and Weight, disease, Interacting drugs).
c) Indications for TDM. Protocol for TDM.
d) Pharmacokinetic/Pharmacodynamic Correlation in drug therapy.
e) TDM of drugs used in the following disease conditions: cardiovascular disease, Seizure disorders, Psychiatric conditions, and Organ transplantations
Dosage adjustment in Renal and Hepatic Disease.
a. Renal impairment
b. Pharmacokinetic considerations
c. General approach for dosage adjustment in renal disease.
d. Measurement of Glomerular Filtration rate and creatinine clearance.
e. Dosage adjustment for uremic patients.
f. Extracorporeal removal of drugs.
g. Effect of Hepatic disease on pharmacokinetics.
Population Pharmacokinetics.
a) Introduction to Bayesian Theory.
b) Adaptive method or Dosing with feedback.
c) Analysis of Population pharmacokinetic Data
Chapter08 - 10 Bioavailability & Bioequivalance.ppt
This document discusses bioavailability and the parameters used to assess it. Bioavailability is defined as the rate and extent of drug absorption from its dosage form. Parameters like plasma concentration over time (Cmax, tmax, AUC), urine concentration over time (Du∞, dDu/dt, t∞), acute pharmacological effects, and in vitro dissolution studies provide information about a drug's bioavailability. Absolute bioavailability compares systemic exposure from a non-IV route to IV, while relative bioavailability compares different formulations administered by the same route. Together these parameters allow evaluation of a drug's bioavailability from different dosage forms.
The complex interplay between liver metabolising enzymes and transporters
The interplay between liver metabolising enzymes and transporters is a complex process. To address this, Ms. Neuhoff together with other experts in the field published a white paper on the mechanistic framework for in vitro–in vivo extrapolation of liver membrane transporters and their interplay with liver metabolizing enzymes. Read more about the methods used and conclusions in the whitepaper below: "A Mechanistic Framework for In Vitro–In Vivo Extrapolation of Liver Membrane Transporters: Prediction of Drug–Drug Interaction Between Rosuvastatin and Cyclosporine": http://bit.ly/Slideshare_NeuhoffWP
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Renal clearance 2k19 08-26
- 2. Prepared By:- Ravi Raj Sharma B.Pharm, GMCTHRC,Pokhara 8/26/2019 2Biopharmaceutics
- 3. CONTENTS 8/26/2019 3Biopharmaceutics About Renal Clearance Mechanism of Renal Clearance Comparison of drug excretion methods Determination of Renal Clearance Factors Affecting Renal Clearance Conclusion References
- 4. RENAL CLEARANCE Volume of plasma that is cleared of drug per unit of time through the kidney. Constant fraction of VD in which the drug is contained that is excreted by the kidney per unit of time. Mathematically, 8/26/2019 4Biopharmaceutics
- 5. RENAL CLEARANCE Contd… Consider the mass balance of drug cleared by the kidney and ultimately excreted in urine. Rate of drug passing through kidney = rate of drug excreted in urine = renal clearance = plasma drug concentration = rate of urine flow = urine drug concentration excretion rate = Cp 8/26/2019 5Biopharmaceutics
- 7. COMPARISON OF DRUG EXCRETION METHODS ClR = Rate of (filtration + secretion – reabsorption) Plasma drug concentration. Renal clearance ratio = ClR of drug ClR of creatinine. Actual clearance is not obtained by direct measurement. Compared to that of standard reference standard such as insulin. Clearance ratio indication for the mechanism of renal excretion of the drug. 14 8/26/2019 7Biopharmaceutics
- 8. 16 DETERMINATIONOF RENAL CLEARANCE First one is Described as it is important in Biopharmaceutics 8/26/2019 8Biopharmaceutics
- 9. GRAPHICAL METHODS Slope of the curve obtained by plotting rate of drug excretionin urine (dDu/dt) against Cp. For a drug that is excreted rapidly, dDu/dt is large, the slope is steeper, and clearance is greater. For a drug that is excreted slowly through the kidney , the slope is smaller. Clr = Urinary drug excretion rate dDu/dt Plasma drug concentration Cp 17 = 8/26/2019 9Biopharmaceutics
- 10. GRAPHICAL METHODS slope = renal clearanceRate of drug excretion Plasma level(Cp) A B 18 Contd… 8/26/2019 10Biopharmaceutics
- 11. GRAPHICAL METHODS Multiplying both sides by Cp gives By rearranging and integrating 19 Contd… 8/26/2019 11Biopharmaceutics
- 12. GRAPHICAL METHODS Slope= ClR Drug excreted in urine(Du) Slope= ClR 20 Contd… 8/26/2019 12Biopharmaceutics
- 13. FACTORS AFFECTING RENAL CLEARANCE Physicochemical properties of drug Plasma concentration of drug Distribution and binding characteristics of drug Urine pH Blood flow to the kidney Biological factors Drug interactions Disease state 8/26/2019 13Biopharmaceutics
- 14. CONCLUSION The clearance concept was first introduced to describe renal excretion of endogenous compounds in order to measure the kidney function. The term is now applied to all organs involved in drug elimination like liver, lungs, biliary system etc. Clearance values gives useful estimates regarding a lot of disease states. 33 8/26/2019 14Biopharmaceutics
- 15. REFERENCES Brahmankar DM , Jaiswal Sunil B . Biopharmaceutics and pharmacokinetics: A TREATISE. 3rd edition(2015)/(Reprint 2016). p.206- 10. https://www.sciencedirect.com/topics/medicine-and-dentistry/renal- clearance 8/26/2019 15Biopharmaceutics