Excretion of drugs in humans
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This document discusses drug excretion, which is the removal of drugs and their metabolites from the body. It notes that the kidneys are the primary organs of excretion, known as renal excretion, while other organs like the lungs, bile, intestines, salivary glands and skin also contribute to non-renal excretion. Renal excretion involves glomerular filtration, tubular secretion and reabsorption. Glomerular filtration non-selectively filters compounds, while tubular secretion and reabsorption actively transport substances. Non-renal excretion occurs through bile, lungs, saliva, milk, skin, gastrointestinal tract and genital secretions by passive diffusion depending on factors like pH, molecular
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INTRODUCTION
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Excretion of unchanged or intact drug is important in the termination of its pharmacological action.
The principal organs of excretion are kidneys. Excretion of drug by kidneys is called as renal excretion.
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Drug absorption from GIT
Drug absorption from git , Drug absorption from git , DIGESTION AND ABSORPTION , Transcellular / intracellular , transport , .Passive Transport Processes , Passive diffusion , Pore transport , Ion- pair transport , Facilitated or mediated diffusion
, Active transport processes , Primary , Secondary , Symport (Co-transport) , Antiport (Counter transport) , Paracellular / Intercellular Transport , Permeation through tight junctions of epithelial cells , Persorption , Vesicular or Corpuscular Transport (Endocytosis) , Pinocytosis , Phagocytosis , FACTORS INFLUENCING ABSORPTION OF DRUGS , DRUG DISSOLUTION , Factors affecting dissolution rate , DISSOLUTION APPARATUS , IVIVC (In vitro- in vivo correlation) , ROLE OF DOSAGE FORM , Transport model , pH Microclimate , Intracellular pH environment , Tight junction complex
EXCRETION OF DRUGS.pptx
This document discusses the various processes and routes by which drugs are excreted from the body. The major routes of excretion are renal excretion through glomerular filtration, tubular secretion, and reabsorption in the kidneys; hepatobiliary excretion through bile secretion and enterohepatic recycling in the liver; and pulmonary excretion through expiration from the lungs. Other minor routes include excretion in sweat, saliva, breast milk, and feces. The rate of excretion influences the duration of a drug's effects in the body.
PHARMACOKINETICS & PHARMACDINEMICS.pptx
PHARMACOKINETICS & PHARMACDINEMICS.pptxUniversity Institute of Pharmaceutical Sciences, Panjab University Chandigarh
This document provides an overview of pharmacology and drug absorption. It defines pharmacology as the science of drugs and describes pharmacokinetics as what the body does to drugs and pharmacodynamics as what drugs do to the body. The key parameters of pharmacokinetics - absorption, distribution, metabolism and excretion - are explained. Drug absorption mechanisms like passive diffusion, carrier-mediated transport and active transport are summarized. Factors affecting drug absorption like solubility, concentration and route of administration are also highlighted. The document concludes by defining bioavailability and bioequivalence.Drug-Elimination pharmacology .pptx
https://www.slideshare.net/sultanrpmc/examination-of-cvs-29254373?from_search=9https://www.slideshare.net/BhadraTrivedi/cvs-examination-ug-1?from_search=17
Non renal routes of excretion For pharmacy students
Non-renal routes of excretion are those by which metabolites and medications are removed from the body by means of systems other than the kidneys. Two such pathways are pulmonary excretion, which expels volatile chemicals via the lungs, and biliary excretion, which secretes molecules into the bile and excretes them in feces. Moreover, medications may be eliminated via saliva, perspiration, and breast milk. Whereas the respiratory route is important for gaseous anesthetics and alcohol, the liver is essential in the metabolism of medications for biliary excretion. Especially in individuals with compromised kidney function, controlling medication dosage and reducing toxicity need an understanding of these non-renal pathways.
Drug Pharmacokinetics
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
Drug excretion
The document discusses drug excretion from the body through various routes. It describes the principal organs involved in excretion as the kidneys, lungs, biliary system, intestines, saliva, and milk. Renal excretion through the kidneys is the primary route for water soluble drugs and involves glomerular filtration, tubular secretion, and tubular reabsorption. Other routes include biliary excretion into the feces, pulmonary excretion of volatile substances through the lungs, and excretion into saliva, sweat, and breast milk in small amounts for some drugs. Factors like a drug's molecular size, charge, lipid solubility, and degree of protein binding determine which excretion pathways it undergoes.
Clearance & Elimination detail explanation.pptx
I am a pharmacist these slides describe detail explanation on clearance and elimination. I hope pharmacy department students get more benefits about it.
Drug Elimination
This document discusses drug elimination through excretion. It defines excretion as the process of transferring drugs and metabolites from the internal to external environment. The principal organs of excretion are the kidneys, through which drugs are excreted via renal excretion. Other routes of non-renal excretion include the lungs, biliary system, intestines, and sweat glands. The key processes determining renal excretion are glomerular filtration, tubular secretion, and tubular reabsorption. Drugs can be cleared from the body through renal clearance or non-renal clearance via routes like biliary, pulmonary, salivary, dermal and gastrointestinal excretion.
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Pharmacodynamics of drug
Pharmacodynamics is defined as the study of how drugs act on the body. Drugs can act through transport mechanisms like symporters and antiporters, or through enzymes, ion channels, and receptors. Drugs typically inhibit enzymes rather than stimulate them. Enzyme inhibition can be non-specific by denaturing the protein, or specific by competitively or non-competitively inhibiting a targeted enzyme without affecting other enzymes in the pathway. Symporters move one ion across the membrane along with another ion, while antiporters move one ion in opposite directions using the electrochemical gradient of the other.
Factors affecting excretion of drug from body
The excretion of drugs is affected by various physicochemical and biological factors. Drugs with larger molecular weights and those that are more lipid soluble are excreted less than drugs with smaller molecular weights or lower lipid solubility due to decreased glomerular filtration and increased distribution in tissues. Additionally, drugs that have higher volumes of distribution, are highly protein bound, or have lower renal blood flow are excreted less through the kidneys compared to drugs with opposite properties. Other factors like ionization, urine pH, age, and presence of diseases can also influence a drug's renal clearance and excretion.
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Lipids
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2. Lipids serve as an energy store and structural component of cell membranes. Major sources include nuts, seeds, milk, eggs, liver, and fish oils.
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Absorption of Drugs in human body
This document discusses drug absorption mechanisms. It defines absorption as the entry of drug molecules into systemic circulation from the site of administration. It then describes the main mechanisms of drug absorption as passive diffusion, filtration, and carrier-mediated transport including facilitated diffusion and active transport. Passive diffusion involves diffusion of lipophilic drugs down their concentration gradient without carriers. Filtration and carrier-mediated transport help absorb other types of drugs.
Carbohydrates
Carbohydrates are widely distributed in plants and animals. They function primarily as a fuel in the body by liberating energy through oxidation. Certain carbohydrate products also promote further oxidation of foods and can be used as starting materials for other biological compounds. Chemically, carbohydrates contain carbon, hydrogen, and oxygen in proportions similar to water, with glucose having the formula C6H12O6. Carbohydrates can be classified based on the number of carbon atoms in their molecular structure, ranging from di- to heptoses.
Route of administration of drugs
This document discusses various routes of drug administration. The enteral route, which includes oral and sublingual administration, is the safest, most economical and convenient. Oral administration has advantages like ease of self-administration but disadvantages like variable drug absorption in the GI tract. Sublingual administration allows rapid drug absorption bypassing first-pass metabolism but only small doses can be used. The rectal route uses suppositories inserted into the rectum.
Pharmacology
This document provides definitions and classifications related to the field of pharmacology. It defines pharmacology as the study of drugs and their actions in the body. Key topics covered include the definitions of pharmacokinetics, pharmacodynamics, pharmacoepidemiology, pharmacoeconomics, pharmacogenomics, toxicology, pharmacovigilance, therapeutics, clinical pharmacology, receptors, ligands, potency, and tolerance. It also discusses sources of drug information like pharmacopeias and the expanding scope of pharmacology to incorporate new approaches like computer-assisted drug design and novel drug delivery methods.
Factor effecting drug absorption
The document discusses factors that influence drug absorption in the gastrointestinal tract, noting that the small intestine has the greatest absorption due to presence of enzymes and water absorption, while the stomach and colon have less absorption. It also outlines how pH levels, binding proteins, metabolism, age, sex, body weight, food, medications, and disease states can impact drug absorption in the GI tract. Specifically, it indicates that unionized drugs are absorbed faster than ionized drugs due to greater lipid solubility.
Skeletal system
The skeletal system comprises bones and cartilages that support the body, allow for movement, protect internal organs, and produce blood cells. There are two main types of bones - long bones in the limbs and flat/irregular bones in the skull, vertebrae, and pelvis. Bones form through either intramembranous or endochondral ossification and are constantly remodeled throughout life. The axial skeleton includes the skull, vertebral column, and thoracic cage, providing structure and protection to the head, neck and trunk.
Hypersensitivity reactions
The document discusses hypersensitivity reactions, which occur when the immune system overreacts to substances that are normally harmless. It defines four main types of hypersensitivity reactions:
Type I are immediate reactions mediated by IgE antibodies. Type II involve cytotoxic antibodies against self-cells. Type III occur when antigen-antibody complexes activate the complement system. Type IV are delayed hypersensitivity reactions.
The document provides examples like allergies, transfusion reactions, and serum sickness. It explains the underlying immunology and describes associated symptoms, laboratory tests, and management approaches for different hypersensitivity reactions like rhinitis, asthma, and anaphylaxis.
Epilepsy
Epilepsy is a neurological disorder characterized by recurrent seizures caused by excessive neuronal activity in the brain. A seizure occurs when nerve cell activity in the brain is disturbed, causing changes in movement, behavior, sensation (including "auras"), or consciousness. Epilepsy is defined as having two or more unprovoked seizures. Seizures have many potential causes including genetics, brain injury, and unknown factors. Treatment involves medications called anti-epileptic drugs which help control seizures by various mechanisms such as enhancing GABA inhibition or blocking sodium channels. Diagnosis involves a detailed history and examination, and may include tests like EEG, MRI, and genetic testing.
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Excretion of drugs in humans
- 1. EXCREATION ASIYABI.M ASSISTANT PROFESSOR DEPARTMENT OF PHARMACOLOGY
- 2. DEFINITION Excretion remove drug and their metabolite from the body . Kidney are principal organs for excretion and excretion through kidney is termed as RENAL EXCRETION. Non-renal excretion is the term used to describe excretion by all other organs except the kidneys . The other organs include lungs , biliary system,intestine, salivary glands and sweat glands.
- 3. Process of excretion Renal excretion of dugs: Kidneys are responsible for the excretion of nearly all drugs as well as their metabolite to a certain extent. Water soluble, non-volatile , small molecular size ( less than 500 daltons) agents thet undergo slow metabolism undergo excretion via urine. Drug excretion via urine is determined by the following processes namely glomerular filtration, active tubular secretion, and active or passive tubular re –absorption. Rate of excretion = Rate of filtration + rate of secretion- Rate of reabsorption
- 4. Glomerular filtration: This is a process involving the filtration of most compound irrespective of whether they are ionise or unionised with an exception of macromolecules ( that bounded to plasma proteins or blood cells). It is a non-selective process which occurs in one direction only. The glomerulus also behaves as a negatively charged selective barrier which promotes the retention of negatively charged compounds. Only 10% of cardiac output is filtered through the glomeruli out of the 25% of blood/min thatreaches the kidneys through the ranal artery.The rate of filtration is knpwn as glomerular filtration rate.
- 5. Although around 180 litres of protein and free ultra filtrate of cells,passes through the glomeruli every day , yet, nearly 1.5litres only is excreated as urine.The ramaining filtrate undergoes reabsorption from the tubules. Active Tubular Secretion: This is a carrier-mediated process. Compounds are transported in a direction opposite to that of the concentration gradient during active secretion by utilising energy.Two mechanisms of active tubular secretion have been identified:
- 6. a) A system that secretes organic acids or anions (eg penicillin, salicylates, glucuronides, silfates) this system is similar to tha one which secretes endogenous acid like uric acid. b) A system that secretes organic bases or cations ( eg: morphine, mecamylamine, hexamethonium). Tubular Re-absorption: This follows the process of glomerular filtration. Tubular re-absorption can take place either of the two ways. a) Active Tubular Re-absorption: High threshold endogenous substance or nutrients like electrolytes, glucose,vitamins,amino acids, which need to be conserved by the body, usually active tubular re-absorption.Acive re- absorption is shown by very few drugs eg: oxopurinol.
- 7. Passive Tubular Re-absorption: Numerous exogenous substance including drugs commonly exhibit passive tubular re-absorption. The back diffusion or re-absorption of water along with sodium and other inorganic ions estabilishes the concentration gradient. NON RENAL EXCRETION OF DRUG i) Biliary excretion of drug-enterohepatic cycling: Bile acid is produced by the hepatic cells present along the bile canaliculi. The production as well as secretion of bile is an active process.Re-absorption of nearly 90% of the secreted bile acid in an active process.
- 8. ii) Pulmonary excretion: The process of simple diffusion through the lungs ,aids in the absorption of gaseous and volatile substance . In the same way diffusion can also help in their excretion .Gaseous anaesthetic those are not vey soluble in blood eg: nitrous oxide. iii) Salivary excretion: This involve excretion of drugs through the saliva and this process involve passive diffusion. The ph-partition hypothesis forms the basis for the prediction of salivary excretion of drugs. Through salivary ph ranges from 5.8 to8.4 its mean value in human is 6.4 . Drugs that exist in unionised forms and that are soluble in lipids at the mean ph undergo passive salivary excretion.
- 9. iv) Mammary excretion: A drug that is excreted in milk can enter to breast feedind infants and therefore, it Is significant .Drug excretion in milk is not a passive process it depend on: a) pH-partition behaviour b) Molecular weight c) Lipid solubility d) Degree of ionisation The Ph of milk ranges from 6.4 to 7.6 and possesses a mean pH of 7.0 free, unionised lipid soluble drugs show passive diffusion in the alveolar cells of the mammary gland. Since milk bears acidic nature as compared to plasma drugs that are weakly basic in nature show a greater concentration in milk just like in case of saliva.
- 10. v) Skin excretion: pH- partition hypothesis also regulates the excretion of drugs through skin via sweat. Drugs and their metabolites that are passively excreted through the skin are accountable to some extent for urticaria and dermatitis in addition to other hypersenitivity reaction. Sweat shows the excretion of compounds like benzoic acid, salicylic acid, alcohol and antipyrine along with heavy metal such as lead, mercury, and arsenic. vi) Gastrointestinal excretion: Generally drugs are seen to be excreted in the GIT when they have been administered parentrally and their concentration gradient favour passive diffusion. The process of GI excretion of drug is opposite that of GI absorption.
- 11. vii) Genital excretion: Drug may also be excreted in the reproductive tract and genital secretion.
- 12. THANK YOU