This document discusses various topics related to pharmacokinetics including absorption, distribution, metabolism and elimination of drugs. It begins with defining key terms in pharmacology. It then covers the basic concepts of pharmacokinetics and pharmacodynamics. The major processes of pharmacokinetics - absorption, distribution, metabolism and elimination are introduced. Various routes of drug administration both local and systemic are outlined. Factors affecting absorption and bioavailability are also discussed.
Histamine is a biogenic amine present in many animal and plant tissues. It is implicated as a mediator in hypersensitivity and tissue injury reactions. Histamine is present and stored in mast cells, especially in the skin, lungs, and gastrointestinal mucosa. It is synthesized from the amino acid histidine and acts on H1, H2, and H3 receptors to cause various pharmacological effects like vasodilation, increased capillary permeability, smooth muscle contraction, and increased gastric acid secretion. Serotonin is another amine present in enterochromaffin cells of the gastrointestinal tract. It is synthesized from tryptophan and acts on multiple 5-HT receptor subtypes to cause vasoconstriction, intestinal per
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive functioning. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Drugs used in myasthenia gravis and galucomaAshviniGovande
This document provides information about myasthenia gravis (MG) and drugs used to treat it, as well as information about glaucoma and drugs used to treat glaucoma.
MG is an autoimmune disorder causing muscle weakness due to antibodies blocking acetylcholine receptors at the neuromuscular junction. Drugs used to treat MG include acetylcholinesterase inhibitors like pyridostigmine to increase acetylcholine levels, immunosuppressants to reduce antibody production, and thymectomy to remove the thymus gland source of antibodies.
Glaucoma involves increased fluid pressure in the eye damaging the optic nerve. The most common type is primary open-angle glaucoma. Drugs
This document summarizes parasympatholytic drugs, also known as anticholinergic or antimuscarinic drugs. It discusses the pharmacological properties and uses of atropine and scopolamine, which are belladonna alkaloids that act as competitive inhibitors at muscarinic receptors in the parasympathetic nervous system. It also describes newer anticholinergic drugs that have more selective actions, such as ipratropium bromide and tiotropium bromide for bronchodilation in respiratory disorders, and oxybutynin for urinary incontinence.
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
This document summarizes a seminar on sympathomimetic drugs presented by Mohd Fahad and guided by Mohd. Khushtar. It discusses different types of adrenergic drugs including direct, indirect, and mixed acting sympathomimetics. It describes the actions of adrenergic drugs on various organs mediated by alpha and beta receptors. Important drugs are discussed in detail including their uses, doses, preparations, and adverse effects. The document provides an overview of adrenergic pharmacology and the therapeutic uses of sympathomimetic drugs.
Histamine is a biogenic amine present in many animal and plant tissues. It is implicated as a mediator in hypersensitivity and tissue injury reactions. Histamine is present and stored in mast cells, especially in the skin, lungs, and gastrointestinal mucosa. It is synthesized from the amino acid histidine and acts on H1, H2, and H3 receptors to cause various pharmacological effects like vasodilation, increased capillary permeability, smooth muscle contraction, and increased gastric acid secretion. Serotonin is another amine present in enterochromaffin cells of the gastrointestinal tract. It is synthesized from tryptophan and acts on multiple 5-HT receptor subtypes to cause vasoconstriction, intestinal per
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive functioning. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Drugs used in myasthenia gravis and galucomaAshviniGovande
This document provides information about myasthenia gravis (MG) and drugs used to treat it, as well as information about glaucoma and drugs used to treat glaucoma.
MG is an autoimmune disorder causing muscle weakness due to antibodies blocking acetylcholine receptors at the neuromuscular junction. Drugs used to treat MG include acetylcholinesterase inhibitors like pyridostigmine to increase acetylcholine levels, immunosuppressants to reduce antibody production, and thymectomy to remove the thymus gland source of antibodies.
Glaucoma involves increased fluid pressure in the eye damaging the optic nerve. The most common type is primary open-angle glaucoma. Drugs
This document summarizes parasympatholytic drugs, also known as anticholinergic or antimuscarinic drugs. It discusses the pharmacological properties and uses of atropine and scopolamine, which are belladonna alkaloids that act as competitive inhibitors at muscarinic receptors in the parasympathetic nervous system. It also describes newer anticholinergic drugs that have more selective actions, such as ipratropium bromide and tiotropium bromide for bronchodilation in respiratory disorders, and oxybutynin for urinary incontinence.
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
This document summarizes a seminar on sympathomimetic drugs presented by Mohd Fahad and guided by Mohd. Khushtar. It discusses different types of adrenergic drugs including direct, indirect, and mixed acting sympathomimetics. It describes the actions of adrenergic drugs on various organs mediated by alpha and beta receptors. Important drugs are discussed in detail including their uses, doses, preparations, and adverse effects. The document provides an overview of adrenergic pharmacology and the therapeutic uses of sympathomimetic drugs.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
Centrally acting muscle relaxants work in the central nervous system to reduce muscle tone and involuntary movements without affecting consciousness or voluntary movement. They are useful for relieving muscle spasms associated with conditions like tetanus, strychnine poisoning, and various spastic disorders. Common centrally acting muscle relaxants include mephenesin, methacarbamol, and chlorsoxazone. These drugs provide relief from muscle spasms and tremors through their sedative effects in the central nervous system. Common side effects include drowsiness, dizziness, weakness, and nausea.
Classification and mechanism of action of alzheimers drugs SajalChowdhury4
This document discusses Alzheimer's disease and the drugs used to treat it. It begins by defining Alzheimer's as a neurodegenerative disease that causes brain cell deterioration and memory loss. It then outlines the symptoms of Alzheimer's. The document categorizes the approved drugs for Alzheimer's into two classes: cholinesterase inhibitors like donepezil, rivastigmine, and galantamine, and the NMDA antagonist memantine. It provides details on the mechanisms of action of memantine, tacrine, and galantamine, explaining how they work to increase acetylcholine levels in the brain and inhibit acetylcholinesterase.
Physiological salt solutions, also known as Ringer's solution, are artificially prepared solutions used to maintain isolated animal tissues in an experimental setting. They are designed to mimic the composition of extracellular fluids and keep tissue alive outside the body. The main components of physiological salt solutions are sodium, potassium, calcium, chloride, magnesium, and glucose dissolved in distilled water. Each ingredient plays an important role like maintaining electrolyte and osmotic balance, nerve and muscle function. Care must be taken when preparing the solutions to maintain the proper pH and prevent bacterial growth. Different types of physiological salt solutions exist that are tailored to the specific needs of different tissue types.
The document discusses neurohumoral transmission via the autonomic nervous system. It describes how the ANS is comprised of the sympathetic and parasympathetic nervous systems which modulate involuntary functions via neurotransmitters. The two main divisions differ in their origins, neurotransmitters, and target organ effects. Neurotransmission occurs via the binding of neurotransmitters like acetylcholine and norepinephrine to receptors, producing excitatory or inhibitory post-synaptic potentials that mediate various physiological responses. Neurotransmitters are synthesized, stored in vesicles, released upon neuronal firing, and degraded or reabsorbed to terminate synaptic transmission.
Drug distribution involves the reversible transfer of drugs between compartments like blood and tissues. Several factors affect how drugs are distributed, including tissue permeability, organ size and blood flow, and binding to tissue components. Drugs with certain physicochemical properties like small molecular size and appropriate lipophilicity more easily pass through barriers and cell membranes into tissues. Additionally, tissues with greater blood flow and perfusion rates allow for faster drug distribution. Finally, the extent to which drugs bind to proteins and other components in blood and tissues impacts their distribution.
Adrenergic blocking agents, also known as adrenergic antagonists, block alpha and/or beta receptor sites and have the opposite effect of adrenergic agents. They are classified based on the type of adrenergic receptor they block, including alpha1, alpha2, beta1, beta2, and beta3 receptors. Common uses include treatment of hypertension, heart failure, and benign prostatic hyperplasia. Side effects may include hypotension, tachycardia, and bronchospasm.
5-Hydroxytryptamine & it’s Antagonist is a Topic in Pharmacology which will defiantly Help You in pharmacy field All information is related to pharmacology drug acting and it's effect on body. it is collage project given by our department i would like to share with you.
This document discusses enzyme induction and inhibition. It defines enzymes as biological catalysts that speed up reactions without being permanently altered. Enzyme activity can be altered by small molecules binding to the active site or other sites. Inhibitors reduce enzymatic reaction rates by blocking the active site without destroying enzymes, and can be reversible or irreversible. Inhibitors are classified as competitive, non-competitive, uncompetitive, or mixed based on whether they bind to the active site or other sites and how they impact substrate binding and catalysis. Enzyme induction increases enzyme production and activity through a homeostatic regulatory mechanism, often by combining with a regulatory protein to increase gene expression.
Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter synthesized from tryptophan. It is present mainly in the gastrointestinal tract and blood platelets, with some in the central nervous system. Serotonin acts through multiple receptor subtypes and has diverse physiological effects including regulation of mood, appetite, sleep, and cardiovascular and gastrointestinal functions. Antagonists of serotonin receptors are used to treat conditions like migraine, hypertension, nausea/vomiting, and carcinoid syndrome. Common antagonists include cyproheptadine, ketanserin, ondansetron, and ergot alkaloids.
This ppt provides the detailed about the bradykinin and their physiological and pharmacological actions and their generation and their mechanisms in detailed manner.
Serotonin (5-HT) is an important neurotransmitter that is synthesized from tryptophan. It acts through 14 different receptor subtypes located throughout the body. 5-HT is involved in many physiological functions like mood, vomiting, smooth muscle contraction, and platelet aggregation. Drugs that modulate 5-HT receptors or reuptake can be used to treat conditions like migraine, anxiety, vomiting, and gastrointestinal disorders. Specifically, triptans like sumatriptan are effective acute treatments for migraine while methysergide and propranolol can be used preventatively due to 5-HT's role in trigeminal nerve activation and neurogenic inflammation during migraine attacks.
This document discusses serotonin, its receptors, and drugs that affect the serotonin system. Serotonin is a neurotransmitter found in the gastrointestinal tract and central nervous system that regulates mood, sleep, and body temperature. It acts through various receptor subtypes (5-HT1-7) located on neurons and other cells. Drugs that affect serotonin include selective serotonin reuptake inhibitors for depression, triptans for migraine, cisapride for gastrointestinal issues, and antagonists for conditions like nausea. Serotonin receptors and their roles are important targets for psychotherapeutic drugs.
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
This document provides an introduction to autonomic pharmacology and discusses cholinergic and anticholinergic drugs. It describes the autonomic nervous system, including its sympathetic and parasympathetic divisions. Cholinergic transmission is mediated by acetylcholine and hydrolyzed by cholinesterase. Cholinergic drugs such as acetylcholine act on muscarinic and nicotinic receptors to affect various organs. Anticholinesterases inhibit cholinesterase and amplify the effects of endogenous acetylcholine. They are used to treat conditions like glaucoma, myasthenia gravis, and postoperative ileus. Their overdose requires supportive care and antidotes like atropine.
This document provides an overview of the history and development of pharmacology. It discusses early contributions from ancient civilizations like India, Egypt, China and Greece. Key figures from different eras that advanced the field are mentioned, such as Hippocrates, Galen, Paracelsus, Magendie, and Ehrlich. Milestones like the discovery of insulin, penicillin, and modern chemotherapy drugs are summarized. The document also reviews the development of pharmacology in India and different branches of modern pharmacology including pharmacotherapeutics, clinical pharmacology, and pharmacogenetics. In conclusion, it defines what constitutes a drug and provides a high-level overview of the basic principles of pharmacokinetics and pharmacod
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
Centrally acting muscle relaxants work in the central nervous system to reduce muscle tone and involuntary movements without affecting consciousness or voluntary movement. They are useful for relieving muscle spasms associated with conditions like tetanus, strychnine poisoning, and various spastic disorders. Common centrally acting muscle relaxants include mephenesin, methacarbamol, and chlorsoxazone. These drugs provide relief from muscle spasms and tremors through their sedative effects in the central nervous system. Common side effects include drowsiness, dizziness, weakness, and nausea.
Classification and mechanism of action of alzheimers drugs SajalChowdhury4
This document discusses Alzheimer's disease and the drugs used to treat it. It begins by defining Alzheimer's as a neurodegenerative disease that causes brain cell deterioration and memory loss. It then outlines the symptoms of Alzheimer's. The document categorizes the approved drugs for Alzheimer's into two classes: cholinesterase inhibitors like donepezil, rivastigmine, and galantamine, and the NMDA antagonist memantine. It provides details on the mechanisms of action of memantine, tacrine, and galantamine, explaining how they work to increase acetylcholine levels in the brain and inhibit acetylcholinesterase.
Physiological salt solutions, also known as Ringer's solution, are artificially prepared solutions used to maintain isolated animal tissues in an experimental setting. They are designed to mimic the composition of extracellular fluids and keep tissue alive outside the body. The main components of physiological salt solutions are sodium, potassium, calcium, chloride, magnesium, and glucose dissolved in distilled water. Each ingredient plays an important role like maintaining electrolyte and osmotic balance, nerve and muscle function. Care must be taken when preparing the solutions to maintain the proper pH and prevent bacterial growth. Different types of physiological salt solutions exist that are tailored to the specific needs of different tissue types.
The document discusses neurohumoral transmission via the autonomic nervous system. It describes how the ANS is comprised of the sympathetic and parasympathetic nervous systems which modulate involuntary functions via neurotransmitters. The two main divisions differ in their origins, neurotransmitters, and target organ effects. Neurotransmission occurs via the binding of neurotransmitters like acetylcholine and norepinephrine to receptors, producing excitatory or inhibitory post-synaptic potentials that mediate various physiological responses. Neurotransmitters are synthesized, stored in vesicles, released upon neuronal firing, and degraded or reabsorbed to terminate synaptic transmission.
Drug distribution involves the reversible transfer of drugs between compartments like blood and tissues. Several factors affect how drugs are distributed, including tissue permeability, organ size and blood flow, and binding to tissue components. Drugs with certain physicochemical properties like small molecular size and appropriate lipophilicity more easily pass through barriers and cell membranes into tissues. Additionally, tissues with greater blood flow and perfusion rates allow for faster drug distribution. Finally, the extent to which drugs bind to proteins and other components in blood and tissues impacts their distribution.
Adrenergic blocking agents, also known as adrenergic antagonists, block alpha and/or beta receptor sites and have the opposite effect of adrenergic agents. They are classified based on the type of adrenergic receptor they block, including alpha1, alpha2, beta1, beta2, and beta3 receptors. Common uses include treatment of hypertension, heart failure, and benign prostatic hyperplasia. Side effects may include hypotension, tachycardia, and bronchospasm.
5-Hydroxytryptamine & it’s Antagonist is a Topic in Pharmacology which will defiantly Help You in pharmacy field All information is related to pharmacology drug acting and it's effect on body. it is collage project given by our department i would like to share with you.
This document discusses enzyme induction and inhibition. It defines enzymes as biological catalysts that speed up reactions without being permanently altered. Enzyme activity can be altered by small molecules binding to the active site or other sites. Inhibitors reduce enzymatic reaction rates by blocking the active site without destroying enzymes, and can be reversible or irreversible. Inhibitors are classified as competitive, non-competitive, uncompetitive, or mixed based on whether they bind to the active site or other sites and how they impact substrate binding and catalysis. Enzyme induction increases enzyme production and activity through a homeostatic regulatory mechanism, often by combining with a regulatory protein to increase gene expression.
Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter synthesized from tryptophan. It is present mainly in the gastrointestinal tract and blood platelets, with some in the central nervous system. Serotonin acts through multiple receptor subtypes and has diverse physiological effects including regulation of mood, appetite, sleep, and cardiovascular and gastrointestinal functions. Antagonists of serotonin receptors are used to treat conditions like migraine, hypertension, nausea/vomiting, and carcinoid syndrome. Common antagonists include cyproheptadine, ketanserin, ondansetron, and ergot alkaloids.
This ppt provides the detailed about the bradykinin and their physiological and pharmacological actions and their generation and their mechanisms in detailed manner.
Serotonin (5-HT) is an important neurotransmitter that is synthesized from tryptophan. It acts through 14 different receptor subtypes located throughout the body. 5-HT is involved in many physiological functions like mood, vomiting, smooth muscle contraction, and platelet aggregation. Drugs that modulate 5-HT receptors or reuptake can be used to treat conditions like migraine, anxiety, vomiting, and gastrointestinal disorders. Specifically, triptans like sumatriptan are effective acute treatments for migraine while methysergide and propranolol can be used preventatively due to 5-HT's role in trigeminal nerve activation and neurogenic inflammation during migraine attacks.
This document discusses serotonin, its receptors, and drugs that affect the serotonin system. Serotonin is a neurotransmitter found in the gastrointestinal tract and central nervous system that regulates mood, sleep, and body temperature. It acts through various receptor subtypes (5-HT1-7) located on neurons and other cells. Drugs that affect serotonin include selective serotonin reuptake inhibitors for depression, triptans for migraine, cisapride for gastrointestinal issues, and antagonists for conditions like nausea. Serotonin receptors and their roles are important targets for psychotherapeutic drugs.
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
This document provides an introduction to autonomic pharmacology and discusses cholinergic and anticholinergic drugs. It describes the autonomic nervous system, including its sympathetic and parasympathetic divisions. Cholinergic transmission is mediated by acetylcholine and hydrolyzed by cholinesterase. Cholinergic drugs such as acetylcholine act on muscarinic and nicotinic receptors to affect various organs. Anticholinesterases inhibit cholinesterase and amplify the effects of endogenous acetylcholine. They are used to treat conditions like glaucoma, myasthenia gravis, and postoperative ileus. Their overdose requires supportive care and antidotes like atropine.
This document provides an overview of the history and development of pharmacology. It discusses early contributions from ancient civilizations like India, Egypt, China and Greece. Key figures from different eras that advanced the field are mentioned, such as Hippocrates, Galen, Paracelsus, Magendie, and Ehrlich. Milestones like the discovery of insulin, penicillin, and modern chemotherapy drugs are summarized. The document also reviews the development of pharmacology in India and different branches of modern pharmacology including pharmacotherapeutics, clinical pharmacology, and pharmacogenetics. In conclusion, it defines what constitutes a drug and provides a high-level overview of the basic principles of pharmacokinetics and pharmacod
Introduction to drug metabolism case studies for its impacts on drug discover...SAPA-GP
2014/10/02 SAPA-GP Webinar:
Introduction to drug metabolism case studies for its impacts on drug discovery and development
Zhoupeng Zhang
Dept of Pharmacokinetics, Pharmacodynamics, and Drug Metabolism
Merck Research Laboratories
Sino-American Pharmaceutical Professionals Association (SAPA)
– A lecture for Medicinal Chemists
(October 2, 2014)
The document discusses drug excretion and elimination from the body. It notes that the most important route of elimination is through the kidneys into urine. It describes the processes of glomerular filtration, tubular secretion and reabsorption that influence drug excretion in urine. Other routes of drug excretion include the feces, exhaled air, saliva, sweat and breast milk. The kinetics of drug elimination including clearance, orders of elimination, plasma half-life and factors affecting half-life are also summarized.
The document discusses pharmacogenomics, which examines how an individual's genetic inheritance affects their response to medications. It provides examples of genetic factors that influence drug metabolism and response, such as variants affecting warfarin effectiveness and isoniazid metabolism. While pharmacogenomic testing could optimize drug therapy, barriers include cost and ethical concerns regarding discrimination and access to care.
The document discusses pharmacokinetics and pharmacodynamics. It describes the four main processes of pharmacokinetics - absorption, distribution, metabolism and elimination - and how they determine the effects of drugs in the body. It also discusses factors that influence absorption and distribution of drugs. The document then covers pharmacodynamics concepts such as dose-response relationships, therapeutic indices, and interactions between drugs. Mechanisms of drug interactions including pharmacokinetic and pharmacodynamic interactions are explained. Common types of drug interactions and ways to prevent adverse drug effects are also summarized.
Introduction and Pharmacokinetics for BPHPravin Prasad
1) The document provides an overview of key pharmacology concepts including pharmacokinetics, which is the study of how the body affects drugs. It describes the processes of absorption, distribution, metabolism and elimination (ADME).
2) Absorption depends on factors like solubility, concentration and route of administration. Distribution is influenced by cardiac output, blood flow and protein binding. Metabolism alters drugs through oxidation and synthetic reactions.
3) Elimination excretes water-soluble drug metabolites through urine, bile or breath. The half-life is the time for a drug amount to halve and indicates how long the drug remains in the body.
4. pharmacokinetics and pharmacodynamics of gamithromycinMerial EMEA
Gamithromycin is a macrolide antibiotic that demonstrates:
1) Fast and complete absorption within 1 hour of subcutaneous administration.
2) Extensive tissue distribution, particularly in lung tissue, due to ion trapping in acidic environments like macrophages.
3) Concentrations in lung tissue that exceed the MIC for common bacterial pathogens for 10-15 days, providing long-lasting therapeutic levels.
This document discusses the principles of pharmacokinetics and pharmacodynamics. It defines key concepts like absorption, distribution, metabolism, and elimination that describe how drugs move through the body over time. Major processes in each stage are identified, such as passive diffusion and active transport in absorption. Compartment models are described to quantify drug distribution and elimination. Factors influencing drug clearance like hepatic and renal function are also covered. The goal is to understand how biological and pharmacological factors impact drug concentrations over time and their effects.
Transporter superfamilies in the human genomeAkash Agnihotri
This document summarizes transporter superfamilies in the human genome. It discusses the two main superfamilies - solute carrier (SLC) and ATP-binding cassette (ABC) transporters. The SLC superfamily includes 52 families and around 395 genes encoding mostly facilitative transporters. The ABC superfamily includes 7 families with 49 genes encoding active transporters that use ATP hydrolysis to transport substrates against gradients. Key transporters from these families play important roles in drug absorption, distribution, and elimination. Polymorphisms in various transporters have been associated with human diseases and drug interactions.
MP_Unit1_Class1_Introduction to targeted drug delivery system.pptxGirijaSoori
The document discusses targeted drug delivery systems. It begins with an introduction to targeted drug delivery and notes that these systems enhance efficacy and minimize side effects by selectively delivering drugs to sites of action. It then describes various biological processes involved in drug targeting like cellular uptake, transport across barriers, extravasation, and lymphatic uptake. The document also covers pharmacokinetic considerations and lists some advantages and disadvantages of targeted drug delivery systems.
A consideration of the exploitation and apparent under-exploitation of transporters in the clinic.
Links are included to the relevant targets and drugs in www.GuidetoPHARMACOLOGY.org
This document presents an overview of transporters as targets for drugs. Transporters are membrane proteins that control the movement of drugs across biological barriers through various transport mechanisms. There are two main types of transporters - ATP-binding cassette (ABC) transporters and solute carrier (SLC) transporters. ABC transporters use ATP hydrolysis to actively transport substrates while SLC transporters use ion gradients to facilitate transport. Transporters play important roles in pharmacokinetic and pharmacodynamic pathways but can also contribute to drug resistance. Targeting transporters offers opportunities to modulate drug absorption, distribution, and resistance.
Pharmacokinetics of Drugs: Introduction to PharmacologyAkash Agnihotri
Pharmacokinetics of drugs is the study of (ADME) Absorption, Distribution, Metabolims, and Excretion.
Pharmacokinetics is all about understanding how drugs move, change, and leave the body.
This is one of the basic unit of pharmacology, to understand the subject pharmacology.
This ppt will be use for MBBS, Nursing and Pharmacy students.
Pharmacokinetics - drug absorption, drug distribution, drug metabolism, drug ...http://neigrihms.gov.in/
A power point presentation on general aspects of Pharmacokinetics suitable for undergraduate medical students beginning to study Pharmacology. Also suitable for Post Graduate students of Pharmacology and Pharmaceutical Sciences.
This document discusses pharmacokinetics, which is the quantitative study of how the body affects drugs. It covers key pharmacokinetic processes like absorption, distribution, metabolism and excretion. Absorption depends on factors like drug properties, route of administration and physiological factors. Distribution is the movement of drugs from blood to tissues. The extent of distribution is determined by properties like lipid solubility and protein binding.
This document discusses drug metabolism and pharmacokinetics (DMPK). It defines DMPK as the study of what the body does to drugs (pharmacokinetics) and what drugs do to the body (pharmacodynamics). Understanding DMPK allows prediction of safe and effective drug doses. The key processes that affect drug behavior in the body are absorption, distribution, metabolism and excretion (ADME). Factors like solubility, permeability and first-pass metabolism impact drug absorption. Distribution is affected by properties like lipophilicity and plasma protein binding. Metabolism alters drugs through phases I and II to enhance excretion, and occurs mainly in the liver via cytochrome P450 enzymes. Drugs
Biomarkers – in Toxicology and Clinical Researchsuruchi71088
This document presents information about biomarkers presented by Ms. Suruchi Ramkumar Sharma at the M.E.T Institute of Pharmacy under the guidance of Dr. Vaishali Dixit. It defines biomarkers as characteristics that can objectively measure normal biological, pathogenic, or pharmacological responses. Examples provided include serum LDL for cholesterol and blood pressure for stroke. The document discusses disease-related biomarkers, drug-related biomarkers, and how biomarkers can be classified based on their characteristics. It explores the discovery of molecular biomarkers and various assay techniques used in toxicology and clinical trials. Various biomarkers are mentioned that can help with early diagnosis, drug development, and determining toxic effects.
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptxHolistified Wellness
We’re talking about Vedic Meditation, a form of meditation that has been around for at least 5,000 years. Back then, the people who lived in the Indus Valley, now known as India and Pakistan, practised meditation as a fundamental part of daily life. This knowledge that has given us yoga and Ayurveda, was known as Veda, hence the name Vedic. And though there are some written records, the practice has been passed down verbally from generation to generation.
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Oleg Kshivets
Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
Muktapishti is a traditional Ayurvedic preparation made from Shoditha Mukta (Purified Pearl), is believed to help regulate thyroid function and reduce symptoms of hyperthyroidism due to its cooling and balancing properties. Clinical evidence on its efficacy remains limited, necessitating further research to validate its therapeutic benefits.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
Adhd Medication Shortage Uk - trinexpharmacy.comreignlana06
The UK is currently facing a Adhd Medication Shortage Uk, which has left many patients and their families grappling with uncertainty and frustration. ADHD, or Attention Deficit Hyperactivity Disorder, is a chronic condition that requires consistent medication to manage effectively. This shortage has highlighted the critical role these medications play in the daily lives of those affected by ADHD. Contact : +1 (747) 209 – 3649 E-mail : sales@trinexpharmacy.com
Basavarajeeyam is a Sreshta Sangraha grantha (Compiled book ), written by Neelkanta kotturu Basavaraja Virachita. It contains 25 Prakaranas, First 24 Chapters related to Rogas& 25th to Rasadravyas.
Histololgy of Female Reproductive System.pptxAyeshaZaid1
Dive into an in-depth exploration of the histological structure of female reproductive system with this comprehensive lecture. Presented by Dr. Ayesha Irfan, Assistant Professor of Anatomy, this presentation covers the Gross anatomy and functional histology of the female reproductive organs. Ideal for students, educators, and anyone interested in medical science, this lecture provides clear explanations, detailed diagrams, and valuable insights into female reproductive system. Enhance your knowledge and understanding of this essential aspect of human biology.
Cell Therapy Expansion and Challenges in Autoimmune DiseaseHealth Advances
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TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Kat...
Pharmacology ADME
1. Manipal College of Pharmaceutical Sciences
26-Aug-18
Pharmacology: ADME
Dr Yogendra Nayak
yogendra.nayak@manipal.edu; yogendranayak@gmail.com
Mobile: 9448154003
2. Manipal College of Pharmaceutical Sciences - MAHE Manipal 2
What are Medicines/ Drugs?
• What is a drug/ drugs?
• What is Pharmacology?
• What is Pharmacotherapy, Clinical Pharmacology,
Chemotherapy, Toxicology?
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Introduction
• Pharmacokinetics
– What body does to the drugs
• Pharmacodynamics
– What drugs does to the body
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Pharmacokinetics - A D M E
• Absorption
• Distribution
• Metabolism
• Elimination
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Routes of Drug Administration
• Local route (Topical)
• Systemic route
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Thalidomide Tragedy
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Factors Regulating Absorption of Drugs
• Aqueous solubility/ Lipid solubility
• Concentration gradient/ Particle size/
Disintegration/ Dissolution
• Absorption area
• Absorbing surface vascularity
• pH of the media/ GIT/ Ionisation of drugs
• Route of administration
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Different Mechanism of Drug Absorption
• Passive transport
– Diffusion
• Simple diffusion
• Facilitated diffusion
– Osmosis: Aquaporins
• Active transport
– Energy is required for this process
– Primary & secondary active transport mechanism
• Vesicular transport
– Endocytosis
• Receptor mediated endocytosis
• Phagocytosis
• Bulk phase endocytosis (pinocytosis)
– Exocytosis
– Transcytosis: Placental circulation of antibody from mother to
fetus
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Passive Diffusion
• Lipid solubility of drugs
– General Anaesthetic gases
– Local anaesthetics
– CNS drugs – sedative hypnotics/ anticonvulsants etc
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Passive Diffusion: Influence of pH
• A. Dissociation of a weak acid, pKa = 4.4
• B. Weak acid in plasma (pH 7.4) &
Gastric acid (pH 1.4)
• Aspirin at Gastric region &
Atropine at small intestine
• Chlordiazepoxide
• Second generation H1 receptor
antagonists
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Distribution
• Drug distribute after absorption
• Factors affecting distribution
– Tissue Affinity
– O/W ration [Partition coefficient/ lipid solubility]
– pKa
– Plasma protein binding
– Blood flow
– Disease states
– Gender & Age
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Distribution
• Apparent volume of distribution (aVd)
– “Volume that would accommodate all the drug
in the body, if the concentration throughout was
the same as in plasma"
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Transporters in Pharmacokinetic Pathways
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Hepatic Drug Transporters
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O/W coefficient [Partition coefficient/ lipid solubility]
logP =
Drug[Octanol]
Drug[Water]log
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Distribution
• Plasma protein binding
– Estrogen or Testosterone sex hormone–binding
globulin
– Thyroxine thyroxin-binding globulin
• Tissue binding
– Quinacrine Liver; Thyroid Iodine
• Fat as reservoir
– Thiopental 70% dose in fat of obese
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Distribution
• Bone
– Etidronate
• Redistribution
– Thiopental sodium short duration of action
• CNS and Cerebrospinal Fluid
– 2nd gen antihistamines Loratadine lower brain
concentrations than diphenhydramine
• Placental Transfer of Drugs Thalidomide
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Plasma Protein Binding
• Acidic/ Neutral drugs
Albumin
• Basic drugs α1 acid
glycoprotein
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Plasma Protein Binding
• Acidic/ Neutral drugs
Albumin
– Barbiturates
– Benzodiazepines
– NSAIDs
– Valproic acid
– Phenytoin
– Penicillins
– Sulfonamides
– Tetracyclines
– Tolbutamide
– Warfarin
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Clinically Implications of Plasma Protein Binding (PPB)
• Highly PPB vascular compartment ↓ Vd
• PPB Acts as temporary storage site
• Highly PPB ↓ metabolism/excretion ↑ duration of
action
• Plasma level of drug = plasma free drug + protein bound
drug cannot relate the effect!
60. Manipal College of Pharmaceutical Sciences - MAHE Manipal 61
Clinically Implications of Plasma Protein Binding (PPB)
• Drug-drug interaction Competing for binding Toxicities
– Eg., Salicylates Sulfonylurea
– Indomethacin/ Phenytoin Warfarin
• High PPB Haemodialysis
• Hypoalbuminemia ↑ Free drug Toxicity
• Some disease/ pregnancy Alter binding
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[F] Bioavailability (L) =
Quantity of Drug at Cite of Action
≈ Plasma/ Serum (g/L)
Quantity of Drug Administered (g)
Dose = Quantity of Drug Administered (g)
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Factors Affecting Absorption & Bioavailability
• Physico-chemical Properties of Drugs
– Drug solubility & dissolution rate
– Particle size
– Lipophilicity of drug
– pKa of drug
– Salt form of drug
• Dosage form Characteristics
– Disintegration time
– Dissolution time
– Pharmaceutical variables
– Nature and type of dosage form
– Manufacturing variables
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Factors Affecting Absorption & Bioavailability
• Pharmacological Factors
– Age
– Gastric emptying
– Intestinal transit time
– Gastrointestinal pH
– Disease states
– Blood flow through GIT
– GI contents
– Presystemic metabolism
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PlasmaConcentration
Time (h)
Drug-Concentration-Time Profile
AUC
Minimum effective
Concentration
Minimum Toxic
Concentration
Bioavailability = AUC
65. Manipal College of Pharmaceutical Sciences - MAHE Manipal 66
PlasmaConcentration
Time (h)
Drug-Concentration-Time Profile after Oral Administration
AUC
Minimum effective
Concentration
Minimum Toxic
Concentration
Bioavailability = AUC
Onset of
Action
Duration
of Action
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PlasmaConcentration
Time (h)
Minimum effective
concentration
A
B C
Drug-Concentration-Time Profile by Different Drugs
67. Manipal College of Pharmaceutical Sciences - MAHE Manipal 68
PlasmaConcentration
Time (h)
Minimum effective
concentration
Oral
I.V.
Drug-Concentration-Time Profile by Different Route of Administration
I.M.
68. Manipal College of Pharmaceutical Sciences - MAHE Manipal 69
PlasmaConcentration
Time (h)
Minimum effective
concentration
I.V. Bolus
Drug-Concentration-Time Profile by I.V. Bolus & I.V. Infusion
I.V. Infusion
Stop
69. Manipal College of Pharmaceutical Sciences - MAHE Manipal 70
PlasmaConcentration
Time (h)
Time Course of Drug in Each Compartment
Drug at
Abs Site
Plasma
Drug
Metabolite
Excreted drug
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Drugs After Absorption - 3 Possible Fates
• Metabolic transformation by enzymes
– Active drug to inactive metabolite
– Inactive (Prodrug) drug to active drug
– Active drug to active metabolite
• Spontaneous structural change
– e.g. Atracurium (Hofmann elimination)
• Excretion unchanged
– e.g.. Aminoglycosides (streptomycin), pancuronium
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Biotransformation – Enzyme Induction
• Enzyme induction
– DNA interaction to increase production of
enzymes
– Alchohol, Phenobarbitone, Rifampicin,
Griseofulvin, Phenytoin
– DDT, & other pesticides
– Cigarette smoking ↑ Elimination of
theophylline
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Factors Affecting Drug Metabolism
• Age
• Disease
• Species Differences
• Heredity/ Genetics
• Sex; Pregnancy
• Environmental Factors
• Drug Dose
• Enzyme Induction
• Enzyme Inhibition
• Diet
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First Pass Metabolism
• Enzymes present in Liver, Intestine etc
• May occur in skin
– Determines oral bioavailability
• Clinical Significance
– Considerably high oral dose
– Liver disease Increased oral bioavailability
– Variation in oral dose among individuals
90. Manipal College of Pharmaceutical Sciences - MAHE Manipal 104
First Pass Metabolism, Examples
Low Intermediate High
Not given orally High oral dose
Phenobarbitone
Phenylbutazone
Tolbutamide
Theophylline
Pindolol
Isosorbide
mononitrate
Aspirin
Quinidine
Desipramine
Nortriptyline
Chlorpromazine
Pentazocine
Metoprolol
Isoprenaline
Lidocaine
Hydrocortisone
Testosterone
Propranolol
Alprenolol
Verapamil
Salbutamol
Glyceryl trinitrate
Morphine
Pethidine
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Elimination
• Urine
• Faeces
• Exhaled air
• Saliva & Sweat
• Breast Milk
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Species Differences
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Renal Excretion
• Distinct processes
– Glomerular filtration
– Active tubular secretion
– pH dependent passive
tubular reabsorption
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Glomerular Filtration (GF)
• Glomerulus Larger pores (75-100A)
• GF depends on PPB & Renal Blood Flow
• Non protein bound drugs (lipid soluble,
insoluble) are filtered
• GFR ↓ in 50 years & above & in renal
failure
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Tubular Reabsorption/ Secretion
• Passive diffusion
• Active tubular secretion
• Passive diffusion - Depends on lipid
solubility & ionization at urinary pH
• Lipid soluble, unionized drugs back diffuse –
reabsorbed
• Lipid insoluble, ionized drugs - excreted
96. Manipal College of Pharmaceutical Sciences - MAHE Manipal 111
Urinary pH Affects Tubular Reabsorption
• Basic drugs better excreted in acidic urine
– e.g. morphine, amphetamine
• Acidic drugs better excreted in alkaline urine
– e.g. barbiturates, salicylates
– Principle is utilized for facilitating elimination in
poisoning
• Drugs with pKa 5-8 greatest effect
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Active Tubular Secretion
• PCT contain efflux transporter
– Luminal membrane of tubular cells
– P-glycoprotein, MRP2
• Active transport free drug in tubular vessels
dissociation of protein bound drugs
• Transporter
– Organic base (OATP): Penicillin, Salicylates,
Probenecid
– Organic acid (OCT): Thiazides, quinine, amiloride
– Both transport processes are bidirectional
• Drugs & metabolites Secretion into lumen
• Endogenous substrates uric acid, reabsorption
98. Manipal College of Pharmaceutical Sciences - MAHE Manipal 113
Transporter Affinity in Tubular Filtration
• Probenecid & Penicillin Penicillin excretion ↓
• Probenecid & Uric acid Uric acid excretion ↑
• Tubular transportation not well developed at birth
– ↑ duration of action penicillin, aspirin
• Salicylates
– Block uricosuric action of probenecid & Sulfinpyrazone
– Decrease tubular secretion of methotrexate.
• Probenecid
– ↓ nitrofurantoin in urine
– ↑ duration of action of penicillin/ ampicillin
– Impairs secretion of methotrexate
• Sulfinpyrazone inhibits tolbutamide
• Quinidine ↓ renal & biliary clearance of digoxin by
inhibiting P-gp
99. Manipal College of Pharmaceutical Sciences - MAHE Manipal 114
Drugs Excretion: Other Routes
• Liver actively transports into bile the organic
acids (drug glucuronides), organic bases
– Larger molecules (MW>300) are eliminated in
bile
– Enterohepatic cycling - ultimate excretion in urine
– Unabsorbed drugs, its metabolites in bile are
excreted in faeces
• Drugs excreted directly into colon Senna,
heavy metals
• Lungs : exhaled air GA, Volatile liquids
etc. irrespective of their lipid solubility
100. Manipal College of Pharmaceutical Sciences - MAHE Manipal 115
Drugs Excretion: Other Routes
• Sweat & saliva Lithium , KI, Rifampin,
heavy metals
• Milk- is slightly acidic, (pH -7 ) than
plasma. Basic drugs gets excreted by
passive diffusion
– More lipid soluble & less protein bound drugs
are excreted
– Small amount transferred to Suckling infant
– So drugs are prescribed to lactating mothers
when absolutely necessary
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Elimination Kinetics
• Fundamentals of
Pharmacokinetics
– Bioavailability (F)
– Volume of distribution (V)
– Clearance (CL)
102. Manipal College of Pharmaceutical Sciences - MAHE Manipal 117
PlasmaConcentration
Time (h)
Drug-Concentration-Time Profile after Oral Administration
AUC
Minimum effective
Concentration
Minimum Toxic
Concentration
Bioavailability = AUC
Onset of
Action
Duration
of Action
Therapeutic
Window
Desired Response
Adverse Response
Side effects
Sub-therapeutic effects
kabs kexc
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PlasmaConcentration
Time (h)
Drug-Concentration-Time Profile after Oral Administration
Therapeutic
Window
Side effects
Sub-therapeutic effects
kabs kexc
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Elimination Kinetics
• CL = Rate of elimination/ C
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Elimination Kinetics
• First order (exponential) kinetics
– kel is directly proportional to C
– CL remains constant or a constant
fraction present in the body is
eliminated in unit time
• Zero order (linear) kinetics
– kel remains constant irrespective of C
– CL decreases with increase in C; or
a constant amount is eliminated in
unit time, eg: Ethyl alcohol
108. Manipal College of Pharmaceutical Sciences - MAHE Manipal 123
Elimination Kinetics
• First order (exponential) kinetics
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Elimination Kinetics
• Plasma half-life (t½)
– Definition: time taken for its plasma
concentration to be reduced to half
of its original
– t½ = [Natural log 2] / kel
– t½ = [0.639/kel ]
– But, kel = [CL / V] – by definition
– t½ = [0.639 X V] / CL
110. Manipal College of Pharmaceutical Sciences - MAHE Manipal 125
Elimination Kinetics
• Plasma half-life (t½) implications
– Complete elimination in 4-5 half
lives
– First order kinetics t½ remains
constant V & CL do not change
with dose
– Zero order kinetics - t½ increases
with dose CL progressively
decreases as dose is increased
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Elimination Kinetics
• Repeated drug administration
– Drug accumulates in the body till Elimination = intake
– Steady State Plasma concentration (Cpss) = [ Dose rate ] / CL
– Dose rate = Target Cpss x CL --- [for i.v route]
– Dose rate = [Target Cpss X CL ] / F --- [for oral route]
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Elimination Kinetics
• First order (exponential) kinetics &
Zero order kinetics
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Elimination Kinetics
• Repeated drug administration
Plateau Principle
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Elimination Kinetics
• Repeated drug administration
Plateau Principle
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Elimination Kinetics
• Loading dose
– Single or few quickly repeated doses given to attain target
concentration rapidly
– Loading dose = [ Cp X V ] / F
– Governed by V & not by CL or t½
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Elimination Kinetics
• Maintenance dose
– Dose that is repeated at uniform intervals after attainment of
target Cpss to maintain the same by balancing elimination rate
– Dose rate = [ Target Cpss X CL ] / F
– Governed by CL and t½ of the drug
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Elimination Kinetics
• Monitoring of plasma concentration of drugs
– Therapeutic drug monitoring (TDM)
1. Drugs with low margin of safety Digoxin, anticonvulsants,
antiarrhythmics, theophylline, aminoglycoside antibiotics, lithium,
tricyclic antidepressants
2. Large individual variations Antidepressants, lithium
3. Potentially toxic drugs used in presence of renal failure
aminoglycoside antibiotics, vancomycinIn
4. Poisoning
5. Failure of response without any apparent reason antimicrobials
6. To check patient compliance psychopharmacological agents
119. Manipal College of Pharmaceutical Sciences - MAHE Manipal 134
Pharmacokinetics of Prolonging Drug Actions
• Advantages
1. Reduces Frequency of administration
2. Improved patient compliance
3. Plasma level fluctuations are avoided Less side
effects
4. Drug effect could be maintained overnight without
disturbing sleep, e.g. antiasthmatics, anticonvulsants,
etc.
120. Manipal College of Pharmaceutical Sciences - MAHE Manipal 135
Methods of Prolonging Drug Actions
• Prolonging absorption
– Oral Route of administration
• Sustained release/ Controlled release
• Coated tablets/ Enteric coated
• Usage of semipermeable membrane in formulations
121. Manipal College of Pharmaceutical Sciences - MAHE Manipal 136
Methods of Prolonging Drug Actions
• Prolonging absorption
– Parenteral
• Parenteral depot (for i.m. and s.c.)
• Pellet implantation
• Sialistic preparation
• Addition of vasoconstrictor/ nerve block
122. Manipal College of Pharmaceutical Sciences - MAHE Manipal 137
Methods of Prolonging Drug Actions
• Prolonging absorption
– Transdermal
• Patches
• Strips
• Ointments etc.
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Methods of Prolonging Drug Actions
• Increasing plasma protein binding
– Drug Congeners
• Sulfadoxine
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Methods of Prolonging Drug Actions
• Retarding rate of metabolism
– Allopurinol inhibits metabolism of
mercaptopurine
– Ethinyl group addition to estradiol
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Methods of Prolonging Drug Actions
• Retarding renal excretion
– Probenecid prolongs action of penicillin &
ampicilliin
126. Manipal College of Pharmaceutical Sciences 141
Thank you
Ph: 9448154003
yogendra.nayak@manipal.edu; yogendranayak@gmail.com
Editor's Notes
Assuming the body behaves as a single homogeneous compartment with volume V into which drug gets immediately & uniformly distributed
Assuming the body behaves as a single homogeneous compartment with volume V into which drug gets immediately & uniformly distributed
Assuming the body behaves as a single homogeneous compartment with volume V into which drug gets immediately & uniformly distributed