Molecular size. [C] Formulation Factors:- 1. villi/microvilli of intestinal tract) and if there is a large blood supply for the drug to move down its concentration gradient. Drug Biotechnology Absorption Drugs Non Oral Extravascular Sites 1 more Online Exam Quiz. . 2) Particle Size and Effective Surface Area of the Drug. Heinrich Keberle, Chemical Research Laboratories, Pharmaceutical Division, CIBA Limited, Basle, Switzerland. Drug absorption. Search for more papers by this author. The drug factors would include tissue binding, plasma protein binding and physicochemical properties of drug (size, charge, pKa, lipid solubility, water solubility)." 2. Binding of drug to blood. The distribution of drugs is dependent . Factors affecting absorption from site of administration • Quantitative aspects of absorption are important for GI, lung and topical routes Absorptive surface area. Factor. . Search for more papers by this author. Some chemicals in the environment are thought to impact the effectiveness of drug-metabolizing enzymes. This animation presents 4 major factors that effect a drugs distribution in the body: Organs of high perfusion, protein binding, molecular size, and polarity. Factors Affecting Adme Pharmacokinetics Of Drugs. Physiological barriers. • List two physiologic factors that can alter each of the processes of absorption, distribution, and excretion. These factors include the concentration of drug transporters in blood, pH, perfusion, body water composition, body fat composition, and most certainly disease conditions (e.g., volume depletion, burns, third spacing). Describe how drug absorption may be affected by a disease that causes changes in intestinal blood flow and/or motility. Distribution 4. Patient-specific factors affecting the drug absorption (physiological variables) include age, gastric emptying time, intestinal transit time, disease status, blood flow at the absorption site, pre-systemic metabolism, and GI content. Molecular size. Excretion. 1. Drugs that affect gastric emptying (eg, parasympatholytic drugs) affect the absorption rate of other drugs. Binding of drug to extra vascular component. 3. Ginsberg etal. The capillaries are typically . The factors that influence the rate and extent of absorption depend upon the route of administration. compartments b) ELIMINATION: is a irreversible . Factors Affecting ADME. Heinrich Keberle, 250+ TOP MCQs on Drug Distribution - Affecting Factors and Answers. Food may enhance the extent of absorption for poorly soluble drugs (eg, griseofulvin ), reduce it for drugs degraded in the stomach (eg, penicillin G), or have little or no effect. a) Aged. Bioavailability 7. Factors affecting drug absorption and distribution Shruti Chillistone Jonathan Hardman Abstract The pharmacokinetic properties of a drug comprise the relationship between its absorption, distribution and inactivation. Degree of ionization. have a general knowledge of the factors affecting the rate and extent of drug absorption, distribution, metabolism and excretion This page was last modified: Tuesday 25 May 2010 at 09:01 PM Water solubility. in the way their bodies handle drugs . C : D : View Answer. Large interindividual variations in drug response can arise from multiple genetic and environmental factors affecting drug absorption, distribution, biotransformation, excretion, interaction with receptor sites, or combinations of these. Factors affecting drug absorption and distribution @article{Chillistone2008FactorsAD, title={Factors affecting drug absorption and distribution}, author={Shruti Chillistone and Jonathan G. Hardman}, journal={Anaesthesia \& Intensive Care Medicine}, year={2008}, volume={9}, pages={167-171} } Shruti Chillistone, J. Hardman Factors Affecting Drug Absorption. B : False. 1 Numerous gastrointestinal changes occur as part of the ageing process however, this doesn't appear to have a significant impact on drug absorption. Particle size. 6) Drug pKa and Lipophilicity and GI pH—pH Partition Hypothesis. 3.1 A schematic diagram showing the enteral routes of drug administration (oral, sublingual and rectal) and their relative susceptibility to first-pass elimination, influencing the absorption and bioavailability of a drug. The rate and extent of drug absorption is dependent on the chemical nature of the drug itself, such as its polarity, pKa, drug formulation and protein binding. As stated in Chapter 18, the intravenous route offers direct access to the systemic circulation and the total dose administered via this route is available in the plasma for distribution into other body tissues and the site(s) of action of the drug. compared the pharmacokinetic parameters of 45 drugs in children and adults and con-cluded that there was a tendency towards larger volumes of distribution of these compounds in children of all age groups [31]. This value is almost 1.2L/min and remains constant. absorption from any of the various extravascular sites, the drug is subjected to a number of processes called as disposition processes. This factor affects only drugs whose absorption is pH sensitive. The Absorption, Distribution, and Excretion of Drugs OBJECTIVES After studying this chapter, the reader should be able to: • Explain the meaning of the terms absorption, distribu-tion, metabolism, and excretion. b) Adults Of age more than 20. c) Infants. Factors Influencing Drug Response Intrinsic Genetic Absorption, distribution, metabolism, excretion Genetic conditions Genetic polymorphism of drug-metabolizing enzymes Height Race Receptor . The passage of drugs across cell membranes is a key part of most pharmacokinetic processes. These drug interactions may lead to drug toxicity when CYP450 activity is inhibited or an inadequate drug level when CYP450 activity is induced. Dhanvanthari Institute of Pharmaceutical Sciences, Kothagudem, Khammam. Integrity of absorptive surface. as well as many drugs which affect pulmonary function, are administered as aerosols. Lipid solubility. The excessively rapid movement of GIT impairs absorption. 2. Particle size. Following oral administration, Drug A is 100 % absorbed but 40 % bioavailable, while Drug B is 80 % absorbed and 60 % bioavailable. • Factors that accelerate gastric emptying increases the bioavailability. Environmental factors can affect drug metabolism. Molecular size Larger the size, less is the distribution. Factors Affecting Blood Concentration of a Drug: The following factors can affect the blood concentrations of a drug: (i) The route of drug administration. Degree of Ionization Drugs exist as weak acids or weak bases when being distributed. Bioavailability = Quantity of a drug reaching systemic circulation/ Quantity of the drug administered Table 1. • After the drug enters in to the systemic circulation by different routes the drug is subjected to number of process calledDISPOSITION(arrangements/transfer) • The 2 major dispositions are a) DISTRIBUTION: is a reversible process of transfer of drug between. A drug once administered is absorbed, distributed, metabolized, and excreted. Distribution is the delivery of drug from the systemic circulation to tissues. Some disorders like diabetic neuropathy causes gastric stasis and decrease the drug absorption. Smaller the molecular size of the drug, rapid is the absorption. Factors Related to the Drug: 1. Fig. Pharmacokinetic is a quantitative study of drugs in the body absorption, distribution, metabolism and excretion of the law. FACTORS INFLUENCING DRUG DISTRIBUTION. Options. 18. Passage of Drug Molecule Across Membranes 2. pKa 3. pH - pka Partion Concept 4. pH-Partition Hypothesis 5. tablets, capsules, solutions) the route of administration (e.g. -Gastrointestinal Diseases • There are many gastrointestinal diseases which have an effect on drug absorption, read more is best defined as what the body does to the drug; it includes -The dispersion of drugs from their site of absorption to the site of their action -Only a small amount of the drug will eventually reach it's target site of action due to several factors Six Factors Which Affect the Distribution Rate of Drugs Welling, Peter G. "Influence of food and diet on gastrointestinal drug absorption: a review." Journal of Pharmacokinetics and Biopharmaceutics 5.4 (1977): 291-334.. Levine, Ruth R. "Factors affecting gastrointestinal absorption of drugs." Digestive diseases and sciences 15.2 (1970): 171-188.. Prescott, L. F. "Pathological and physiological factors affecting drug absorption, distribution . a drug compound) is processed by a living organism. A : True. 1971;29 Suppl 3:30-47. doi: 10.1111/j.1600-0773 . It has large effect. Clinical Significance Drug Biotechnology Multiple Choice Questions on "Drug Distribution - Affecting Factors". + + + The factors are: 1. Plasma protein binding rate The rate of absorption following subcutaneous or intramuscular injection depends on the site of injection and physiological factors such as local blood flow. Absorption from the site of injection can be increased by the application of heat or massage, both of which increase local blood flow. Physiological considerations in absorption are blood flow, total surface area, time of arrival of the drug and time of drug at absorption site. Binding of drugs to tissue components. some other factors which significantly affect the drug absorption are the type of mechanism involved in absorption and gastrointestinal physiology such as gi movement, emptying rate, postcrandial. 2. Welling, Peter G. "Influence of food and diet on gastrointestinal drug absorption: a review." Journal of Pharmacokinetics and Biopharmaceutics 5.4 (1977): 291-334.. Levine, Ruth R. "Factors affecting gastrointestinal absorption of drugs." Digestive diseases and sciences 15.2 (1970): 171-188.. Prescott, L. F. "Pathological and physiological factors affecting drug absorption, distribution . Organ/tissue size and perfusion rate 3. 4) Hydrates/Solvates (Pseudopolymorphism) 5) Salt form of the drug. • This is because the drug is exposed to the larger surface area of the small intestine. Thus highly perfused organs like the heart, liver, kidney and brain receive the largest amount of drug immediately after absorption. What factors affect volume of distribution? The drugs absorbed in body fluids or skin, will diffuse through biological membrane barriers into the bloodstream. Gastric motility. Abstract When a drug enters the body, it undergoes absorption, distribution and metabolism before it is excreted. Urine flow rate does not affect the drug if excreted by glomerular filtration and tubular secretion. Physico-chemical factors of drugs affecting absorption, distribution, and excretion Acta Pharmacol Toxicol (Copenh). Lipid Solubility Greater the lipid solubility, more is the distribution and vice versa. The following table highlights some of these other factors. The drug-related factors include blood and tissue binding proteins, pH, and perfusion. Intestinal transit rate. What is drug distribution in pharmacology? Once a drug has entered the blood compartment, the rate at which it penetrates tissues and other body fluids depends on several factors. Drug distribution is a subject that is covered in a branch of pharmacology called pharmacokinetics. Factors affecting distribution of drug. the intravenous (IV) administered drugs begins direct distribution into the body as they avoid first pass effect. Factors Effecting on Drug Distribution Ashok Kari 1, Gandhu Sateesh , Bharatha Suresh , Bodavula Samba Siva Rao2* 1. 1. Who has more intracellular and extracellular water more in their body? Smaller sized drugs are more extensively distributed. Tissue Permeability of Drugs a) Physicochemical Properties of drug like: Molecular size, pKa, o/w Partition Coefficient b) Physiological barriers to diffusion of drugs 2. Factors Related to Drugs: 1. Absorption characteristics of an orally administered drug show complex dynamics that depend upon physicochemical and physiological factors of the drug and gut mucosa 3 and probably an interaction . Slide 8: Factors that affect drug absorption. oral, buccal, sublingual, rectal, parenteral, topical, or inhaled) the rate of gastric emptying. For most drugs, two- to five-fold . o And Ko/w = Distribution of drug in organic phase (octanol) Distribution of drug in aq phase o As Ko/w i.e. Physiology-related. Distribution The distribution of drugs affects efficacy and duration of action. Distribution of a drug is not uniform throughout the body because different tissues receive the drug from plasma at different rates and to different extents. List the major factors that affect drug absorption from oral and nonoral routes of drug administration. Gastric emptying time. Facilitated Diffusion 7. rapid and important age related physiologic changes in drug metabolism and elimination occur in children esp. Several factors impact drug distribution. ADME is the abbreviation for Absorption, Distribution, Metabolism and Excretion . There are four factors that will influence the pharmacokinetic drugs test: water-solubility; fat-soluble; dissociation degree and molecular weight. Describe various methods that may be used to study oral drug absorption from the gastrointestinal transit. The initial distribution of a drug is primarily dependent on the cardiac output and the local blood flow in various body organs. 1. solubility) drug formulation (e.g. Interfering substances. Diet is known to affect drug metabolism because the specific chemicals in certain foods may change the effectiveness of the body's drug-metabolizing enzymes. Due to drug treatment some time motility is increased or decreased. How to Download Notes in PDF from Solution Pharmacy Facebook Group Using Laptophttps://youtu.be/cE5MAt0J6hs Using Mobile https://youtu.be/ntzXKi2pA5UFree mod. (2) Factors affecting the distribution of drugs in the body. Nitroglycerin ADME • V. d ~200 L • t. 1/2 ~1-4 min • Metabolism: 1,3- & 1,2- dinitroglycerol (active, t. 1/2. Drug absorption, distribution, metabolism and excretion is affected by a complex relationship involving the gut microbiome; membrane-bound transporters at the intestinal epithelium, hepatocytes, and renal tubular epithelial cells; the expression of enzymes in enterocytes, hepatocytes, and renal tubular epithelial cells; and filtration mechanisms of the renal system. Drug Biotechnology Different Routes Excretion. Drugs administered via IV: Begin distribution into the body immediately. 1) Drug solubility & dissolution rate. These include: physicochemical properties (e.g. Drug absorption is affected by several factors ( Table 1 ). In addition to protein availability, other factors may affect drug absorption and distribution in the body as a whole or at specific sites within the body. Environmental factors. What are 4 factors that affect absorption of a drug? 6 FACTORS AFFECTING DISTRIBUTION OF DRUGS 1. What are the factors influencing the effect of drugs? The main factors which govern the distribution of a drug are: 704 Words3 Pages. Physico-Chemical Factors of Drugs Affecting Absorption, Distribution, and Excretion. Factors Affecting Distribution of Drugs. The blood pH don't directly affect the renal . 6. Blood flow to the kidney. Thus highly perfused organs like the heart, liver, kidney and brain receive the largest amount of drug immediately after absorption. Plasma protein binding rate Factors affecting drug distribution Rate of distribution - Membrane permeability : Blood perfusion : Extent of Distribution - Lipid Solubility : pH - pKa : Plasma protein binding : Intracellular binding: Rate of distribution Membrane permeability We have already covered some material about membrane permeability. List and describe the four factors that affect the rate of drug distribution. Absorption of Drug 3. Diet may also affect development of CYP450 activity in children (1 Metabolism and elimination reference Pharmacokinetics refers to the processes of drug absorption, distribution, metabolism, and . blood is influenced by biologic and physicochemical factors (discussed in detail below), and by the dosage form. combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. Drug distribution is impacted by several factors related to the drug and the body. The main factors which govern the distribution of a drug are: 3) Polymorphism and Amorphism. Nome nclature 6. What do you mean by Adme of a drug explain different factors affecting drug action? Physico‐Chemical Factors of Drugs Affecting Absorption, Distribution, and Excretion. These in-clude (1) capillary permeability, (2) blood flow-tissue mass ratio (i.e., perfusion rate), (3) extent of plasma protein and . Factors affecting distribution of drugs. Age. Factors that affect gastric drug absorption include: Lipid solubility of the drug. Disease state of a patient can influence drug distribution across the body. Other Factors Affecting Drug Absorption and Distribution. The factors affecting absorption of drugs are related both to the drugs and to the body. Active Transport 6. Physico chemical Property. a knowledge of age ‐ related changes in drug absorption , distribution , and clearance is essentialto optimize drug efficacyand to avoid toxicity. Drug-specific factors that affect drug absorption include the physicochemical and pharmaceutical variables of drugs. "Patient factors could include age, gender, muscle mass, fat mass and abnormal fluid distribution (oedema, ascites, pleural effusion). Lipid water solubility Lipid water solubility coefficient is the ratio of dissolution of drug in lipid as compared to water. Drug Distribution . Apparent Volume of Distribution (VP) 8. Drug Biotechnology Dosage Form Factors Affecting Drug Absorption 1 Presented by Prof.J.P.Bayas M.Pharm 2. during first year of life . ADME in pharmacology and pharmacokinetics is Absorption, Metabolism, and Excretion of a drug or pharmaceutical compound within a living organism. Among the various routes of administration, the most studied is the absorption of drugs in the digestive tract, especially the absorption of drugs in the small intestine. Pore or Convective Transport. Formulation. drug delivery: Nasal irritation is minimized when products are Some of the physicochemical, formulation and delivered with a pH range of 4.5 to 6.5. 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The four factors that affect gastric drug absorption from site of administration factors affecting drug absorption and distribution, buccal sublingual!
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