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Pharmacotherapy of Local anaesthetic drugsManoj Kumar
Local anesthetics are drugs that reversibly block sensation, especially pain, in a localized area without loss of consciousness or control of vital functions. They can be administered topically, via injection, or infiltration. The ideal local anesthetic has rapid onset, sufficient duration, is potent, stable in solutions, and does not interfere with tissue healing or cause toxicity. Common techniques for local anesthesia include infiltration, field block, nerve block, spinal anesthesia, epidural anesthesia, and intravenous regional anesthesia. Proper administration and monitoring can prevent potential toxic effects on the central nervous system and cardiovascular system.
Physiological factors like age, sex, pregnancy, and disease states can impact drug effects in the body. A multitude of host and environmental factors influence individual drug response. Understanding these modifying factors is important for choosing the appropriate drug, dose, and regimen for each patient. Physicians must consider factors like changes in absorption, distribution, metabolism, and excretion when treating different patient populations like pediatrics, geriatrics, and pregnant women.
Pharmacokinetics is the study of how the body affects drugs. It involves absorption, distribution, metabolism and excretion of drugs. Absorption refers to how drugs enter systemic circulation from the site of administration. Distribution is the movement of drugs between tissues via blood flow. Metabolism involves chemical alteration of drugs by oxidation, reduction and conjugation reactions. Excretion is the removal of drugs and metabolites from the body. Together, these processes determine the effects of drugs over time.
Introduction to Autonomic Nervous System PharmacologyRahul Kunkulol
The document discusses the human nervous system and its functions. It controls vital bodily processes like blood pressure, smooth muscle movement, glands, and metabolism. The autonomic nervous system regulates these functions below the conscious level through the sympathetic and parasympathetic divisions. It uses neurotransmitters like acetylcholine and norepinephrine to transmit signals between neurons through synapses in the peripheral nervous system.
This document summarizes the pharmacokinetics and pharmacology of local anesthetics. It discusses the uptake, distribution, metabolism, and excretion of local anesthetics. It also covers the cardiovascular, neurological, and toxic effects that can occur at high blood levels, including seizures. Specifically, it describes how local anesthetics are absorbed into the bloodstream and distributed to tissues, metabolized primarily in the liver, and excreted by the kidneys. Their effects include CNS depression and potential excitation that can lead to seizures at high concentrations.
1. Drug metabolism involves enzymatic modification of drugs by the body with the goal of making them more water soluble and easier to excrete.
2. Metabolism can occur in many tissues like the liver, kidneys, lungs, and intestines and is primarily carried out by the cytochrome P450 enzyme system.
3. Metabolism can result in inactive, active, or more active drug metabolites and influences the drug's pharmacokinetic and pharmacodynamic properties. Certain drugs are able to induce or inhibit the cytochrome P450 enzyme system, altering metabolism of other drugs metabolized by the same enzymes.
This document provides information on the pharmacotherapy of shock. It defines shock and describes the different types including hypovolemic, cardiogenic, obstructive, distributive, and septic shock. It discusses the mechanisms and clinical presentations of hypovolemic and septic shock in detail. It outlines the management of various shock states, emphasizing fluid resuscitation and hemodynamic support, treatment of underlying causes, and use of vasopressors when needed. Case studies are provided to demonstrate application of the management principles.
Local anesthetics reversibly depress the central nervous system to relieve pain without loss of consciousness. They work by binding to voltage-gated sodium channels in nerve cell membranes, inhibiting the generation of action potentials and reducing nerve excitability. Local anesthetics are classified as amides or esters depending on their chemical structure. Amides are more stable but esters have a faster onset of action. Both types contain an aromatic ring connected by an amide or ester linkage to a hydrophilic amine group, allowing them to penetrate cell membranes. The presence of electron-withdrawing groups on the aromatic ring and lipophilic chains influence their potency and duration. Common applications of local anesthetics include dentistry, dermat
Pharmacotherapy of Local anaesthetic drugsManoj Kumar
Local anesthetics are drugs that reversibly block sensation, especially pain, in a localized area without loss of consciousness or control of vital functions. They can be administered topically, via injection, or infiltration. The ideal local anesthetic has rapid onset, sufficient duration, is potent, stable in solutions, and does not interfere with tissue healing or cause toxicity. Common techniques for local anesthesia include infiltration, field block, nerve block, spinal anesthesia, epidural anesthesia, and intravenous regional anesthesia. Proper administration and monitoring can prevent potential toxic effects on the central nervous system and cardiovascular system.
Physiological factors like age, sex, pregnancy, and disease states can impact drug effects in the body. A multitude of host and environmental factors influence individual drug response. Understanding these modifying factors is important for choosing the appropriate drug, dose, and regimen for each patient. Physicians must consider factors like changes in absorption, distribution, metabolism, and excretion when treating different patient populations like pediatrics, geriatrics, and pregnant women.
Pharmacokinetics is the study of how the body affects drugs. It involves absorption, distribution, metabolism and excretion of drugs. Absorption refers to how drugs enter systemic circulation from the site of administration. Distribution is the movement of drugs between tissues via blood flow. Metabolism involves chemical alteration of drugs by oxidation, reduction and conjugation reactions. Excretion is the removal of drugs and metabolites from the body. Together, these processes determine the effects of drugs over time.
Introduction to Autonomic Nervous System PharmacologyRahul Kunkulol
The document discusses the human nervous system and its functions. It controls vital bodily processes like blood pressure, smooth muscle movement, glands, and metabolism. The autonomic nervous system regulates these functions below the conscious level through the sympathetic and parasympathetic divisions. It uses neurotransmitters like acetylcholine and norepinephrine to transmit signals between neurons through synapses in the peripheral nervous system.
This document summarizes the pharmacokinetics and pharmacology of local anesthetics. It discusses the uptake, distribution, metabolism, and excretion of local anesthetics. It also covers the cardiovascular, neurological, and toxic effects that can occur at high blood levels, including seizures. Specifically, it describes how local anesthetics are absorbed into the bloodstream and distributed to tissues, metabolized primarily in the liver, and excreted by the kidneys. Their effects include CNS depression and potential excitation that can lead to seizures at high concentrations.
1. Drug metabolism involves enzymatic modification of drugs by the body with the goal of making them more water soluble and easier to excrete.
2. Metabolism can occur in many tissues like the liver, kidneys, lungs, and intestines and is primarily carried out by the cytochrome P450 enzyme system.
3. Metabolism can result in inactive, active, or more active drug metabolites and influences the drug's pharmacokinetic and pharmacodynamic properties. Certain drugs are able to induce or inhibit the cytochrome P450 enzyme system, altering metabolism of other drugs metabolized by the same enzymes.
This document provides information on the pharmacotherapy of shock. It defines shock and describes the different types including hypovolemic, cardiogenic, obstructive, distributive, and septic shock. It discusses the mechanisms and clinical presentations of hypovolemic and septic shock in detail. It outlines the management of various shock states, emphasizing fluid resuscitation and hemodynamic support, treatment of underlying causes, and use of vasopressors when needed. Case studies are provided to demonstrate application of the management principles.
Local anesthetics reversibly depress the central nervous system to relieve pain without loss of consciousness. They work by binding to voltage-gated sodium channels in nerve cell membranes, inhibiting the generation of action potentials and reducing nerve excitability. Local anesthetics are classified as amides or esters depending on their chemical structure. Amides are more stable but esters have a faster onset of action. Both types contain an aromatic ring connected by an amide or ester linkage to a hydrophilic amine group, allowing them to penetrate cell membranes. The presence of electron-withdrawing groups on the aromatic ring and lipophilic chains influence their potency and duration. Common applications of local anesthetics include dentistry, dermat
This document discusses drug-drug interactions, which occur when one drug alters the effect of another drug. Interactions can be desired or undesired. Clinically important interactions involve drugs with steep dose-response curves, known enzyme inhibitors/inducers, drugs metabolized by saturation, drugs requiring precise dosing, and drugs used together to treat the same disease. Interactions can be pharmacodynamic, occurring when drugs act on the same target site, or pharmacokinetic, altering a drug's plasma concentration through effects on absorption, distribution, metabolism, or excretion. Examples of various types of interactions and their effects are provided.
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.
Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. For the treatment of human diseases, nasal and pulmonary routes of drug delivery are gaining increasing importance. These routes provide promising alternatives to parenteral drug delivery particularly for peptide and protein therapeutics. For this purpose, several drug delivery systems have been formulated and are being investigated for nasal and pulmonary delivery. These include liposomes, proliposomes, microspheres, gels, prodrugs, cyclodextrins, among others. Nanoparticles composed of biodegradable polymers show assurance in fulfilling the stringent requirements placed on these delivery systems, such as ability to be transferred into an aerosol, stability against forces generated during aerosolization, biocompatibility, targeting of specific sites or cell populations in the lung, release of the drug in a predetermined manner, and degradation within an acceptable period of time.
Local anesthetics work by blocking nerve conduction, specifically the entry of sodium ions through voltage-gated channels. This prevents the initiation and propagation of nerve impulses in the area of administration. Local anesthetics can be classified based on their linkage as esters or amides. Amides such as lidocaine are preferred due to lower risk of allergic reactions. Techniques of local anesthesia include infiltration, nerve blocks, and regional techniques like epidural and spinal anesthesia. Proper administration and dosage of local anesthetics is important to avoid potential toxicities.
1) Analgesics are important therapeutic agents in dentistry for treating pain. Common analgesics include acetaminophen, NSAIDs like ibuprofen, and opioids like codeine.
2) Combining analgesics that work through different mechanisms can provide better pain relief than single agents alone. Acetaminophen is often combined with opioids. NSAIDs allow for lower opioid doses to reduce side effects.
3) The combination of acetaminophen with codeine, hydrocodone, or tramadol provides effective relief of mild to moderate dental pain with fewer side effects than opioids alone. Ibuprofen combined with codeine or oxycodone also enhances analgesia.
This document discusses nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin. It provides details on their mechanism of action as cyclooxygenase inhibitors, reducing prostaglandin synthesis and inflammation. Common uses include analgesia, antipyresis, and reducing the risk of cardiovascular events like heart attacks. Adverse effects include gastrointestinal irritation and bleeding. Aspirin is prototypical and its pharmacology and therapeutic uses are discussed in depth.
Centrally acting muscle relaxants work in the central nervous system to reduce muscle tone without affecting consciousness. They selectively depress polysynaptic reflexes in the spinal cord and brain that are involved in regulating muscle tone. They also depress pathways in the brainstem that maintain wakefulness, but to a lesser degree. Common classes of centrally acting muscle relaxants include mephenesin congeners, benzodiazepines, GABA mimetics, and central α2 agonists. Examples are carisoprodol, diazepam, baclofen, and tizanidine. These drugs are used to treat muscle spasms, spasticity, and pain conditions involving muscle spasms.
This document discusses pharmacokinetics and provides details about absorption, distribution, and bioavailability of drugs. It defines key pharmacokinetic terms and describes factors that influence absorption such as solubility, concentration, route of administration, and mechanisms of absorption including passive diffusion, active transport, and pinocytosis. Membrane permeability and drug properties like pH and lipid solubility are discussed. The document also covers volume of distribution, plasma protein binding, tissue storage, and barriers to drug distribution like the blood-brain barrier.
This document provides information on general anaesthetics including their cardinal features, history, stages of anaesthesia, measurement of potency, mechanisms of action, classification, inhalational anaesthetics, intravenous anaesthetics, and conscious sedation. It discusses key figures and discoveries in the history of anaesthesia such as Humphry Davy, Horace Wells, William Morton, and John Snow. It also summarizes the stages of anaesthesia, factors that determine anaesthetic potency including oil-gas and blood-gas partition coefficients, and the pharmacokinetics and mechanisms of action of various inhalational and intravenous anaesthetic agents.
NSAIDs are the chemically diverse class of drugs that have anti-inflammatory, analgesic & antipyretic properties.
They are also called as Non Narcotic, Non Opioid, Aspirin like analgesics.
They are among the widely used therapeutic agents world wide and often taken without prescription for minor aches and pain.
They are used to suppress the symptoms of inflammation associated with rheumatic disease.
Helminth infections affect over two billion people worldwide. Anthelmintic drugs are used to kill or expel parasitic helminths. Major anthelmintic drug classes include piperazines, benzimidazoles, heterocyclics, and natural products. Mebendazole is a commonly used benzimidazole with broad-spectrum activity against intestinal worms and low incidence of side effects. Albendazole is similarly broad-spectrum but also treats cystic diseases. Diethyl carbamazine selectively kills microfilariae and is used to treat filariasis. Ivermectin is the treatment of choice for onchocerciasis and strongyloidiasis by enhancing chloride
This document discusses pharmacokinetics, specifically absorption, distribution, metabolism, and excretion of drugs. It covers the following key points:
- Drug absorption occurs through various routes like the gastrointestinal tract, lungs, skin and is influenced by factors like pH, blood flow and lipid solubility.
- Distribution of drugs depends on capillary permeability, blood flow, protein binding and is described using the volume of distribution.
- Metabolism occurs mainly in the liver through cytochrome P450 enzymes and conjugation reactions, and can inactivate drugs, produce active metabolites, or activate prodrugs.
- Absorption, distribution and metabolism determine the bioavailability of drugs and their delivery to sites of action.
1. NSAIDs work by inhibiting the cyclooxygenase (COX) enzymes, mainly COX-1 and COX-2, which decreases prostaglandin synthesis and produces their pharmacological effects. Selective COX-2 inhibitors have fewer side effects than non-selective NSAIDs.
2. NSAIDs have analgesic, antipyretic, and anti-inflammatory effects. Common side effects include gastric irritation, ulcers, renal impairment, and platelet dysfunction.
3. Aspirin has antiplatelet effects useful for cardiovascular protection. Indomethacin is potent but non-selective. Paracetamol is safer for those with bleeding risks but less effective at inflammation. COX-
Drug interactions can occur when two or more drugs are taken together. The effects of one drug may be altered by another drug through various mechanisms. Some key points:
1) Drug interactions can be pharmacokinetic, involving effects on absorption, distribution, metabolism and excretion of one or both drugs.
2) They can also be pharmacodynamic, where one drug alters the effects of another without changing its levels. This can include synergistic or antagonistic effects.
3) Common causes of interactions include effects on drug metabolizing enzymes like CYP450, protein binding displacement, renal tubular secretion competition and changes to gastrointestinal pH or motility.
4) Outcomes range from loss of
Factors affecting biotransformation of drugsZubia Arshad
The biotransformation of drugs can be affected by various chemical, biological, physiological, temporal, and environmental factors. Chemical factors include enzyme induction and inhibition, which can increase or decrease the metabolism of drugs. Biological factors like age, gender, genetics, diet, and disease states can impact drug metabolism rates. Physiological changes during pregnancy, with hormonal imbalances, or disease states can also alter drug biotransformation. Additional influencing factors are temporal variations, the route of drug administration, and environmental exposures. Careful consideration of all these potential factors is important for safe and effective drug therapy.
Unit-1: General pharmacology :Introduction to pharmacologySabaShaikh76
Introduction to Pharmacology- Definition and scope of pharmacology, nature and source of drugs, essential drugs concept and routes of drug administration, spare receptors, addiction, tolerance, dependence, tachyphylaxis, idiosyncrasy, allergy
The document discusses novel drug delivery systems. It begins with an overview of conventional drug delivery routes and their limitations. It then outlines the need for and goals of newer drug delivery modalities, which aim to control drug absorption, distribution, metabolism, and elimination. Several novel delivery routes are described in detail, including oral, sublingual, inhalation, transdermal, intranasal, and targeted delivery. Polymer-based delivery systems such as microspheres, nanoparticles, and intelligent delivery are also discussed. The document concludes by noting that advanced delivery technologies are playing an increasingly important role in improving drug safety, efficacy, and patient experience.
Individuals vary in their response to drugs due to several factors:
1. Body size influences drug concentration - larger individuals may require higher doses and smaller individuals like children require adjusted doses based on age and weight.
2. Age also impacts drug metabolism - children and elderly metabolize and excrete drugs differently than adults.
3. Other factors like sex, diet, alcohol use, genetics, disease states, and psychological factors can increase or decrease a drug's effects between patients. Doses often need adjusting based on these individual characteristics to achieve the desired therapeutic response without toxicity.
Sympathomimetic drugs mimic the actions of norepinephrine and epinephrine by binding to adrenergic receptors. They can be classified as direct-acting agonists like epinephrine, indirect-acting agonists like amphetamines, or mixed-action agonists like ephedrine. Common uses include pressor agents, cardiac stimulants, bronchodilators, nasal decongestants, CNS stimulants, and anorectics. Examples discussed in more detail include epinephrine, norepinephrine, dopamine, dobutamine, ephedrine, amphetamines, phenylephrine, and pseudophedrine.
This document provides an overview of pharmacology, which is defined as the study of how drugs act on living systems. It discusses key concepts including how drugs bind to receptors and cellular targets, different types of drug responses, factors affecting drug absorption and metabolism, and parameters used to evaluate drug safety and efficacy such as therapeutic index. The document outlines the progression of studies from in vitro to animal to clinical trials in drug development.
Bioavailability refers to the amount of drug that enters systemic circulation and is available at the site of action. It depends on the rate and extent of drug absorption from its dosage form. Many physiological and drug-specific factors can affect bioavailability such as pH, enzymes, blood flow, and food interactions. Careful evaluation and standardization of bioavailability is important for drug development and quality control to ensure accurate and safe dosing.
This document discusses 16 factors that can modify the effects of drugs in the body. These include:
1) Body weight, age, sex, species, and genetic differences can impact drug absorption and metabolism.
2) Route of administration determines speed and intensity of drug action. Oral drugs are slower than IV.
3) Diet, tobacco, alcohol and the environment can induce or inhibit drug metabolizing enzymes.
4) Psychological factors like expectations can impact drugs' efficacy through the placebo effect.
5) Disease states can increase or decrease drug absorption and levels in the body.
This document discusses drug-drug interactions, which occur when one drug alters the effect of another drug. Interactions can be desired or undesired. Clinically important interactions involve drugs with steep dose-response curves, known enzyme inhibitors/inducers, drugs metabolized by saturation, drugs requiring precise dosing, and drugs used together to treat the same disease. Interactions can be pharmacodynamic, occurring when drugs act on the same target site, or pharmacokinetic, altering a drug's plasma concentration through effects on absorption, distribution, metabolism, or excretion. Examples of various types of interactions and their effects are provided.
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.
Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. For the treatment of human diseases, nasal and pulmonary routes of drug delivery are gaining increasing importance. These routes provide promising alternatives to parenteral drug delivery particularly for peptide and protein therapeutics. For this purpose, several drug delivery systems have been formulated and are being investigated for nasal and pulmonary delivery. These include liposomes, proliposomes, microspheres, gels, prodrugs, cyclodextrins, among others. Nanoparticles composed of biodegradable polymers show assurance in fulfilling the stringent requirements placed on these delivery systems, such as ability to be transferred into an aerosol, stability against forces generated during aerosolization, biocompatibility, targeting of specific sites or cell populations in the lung, release of the drug in a predetermined manner, and degradation within an acceptable period of time.
Local anesthetics work by blocking nerve conduction, specifically the entry of sodium ions through voltage-gated channels. This prevents the initiation and propagation of nerve impulses in the area of administration. Local anesthetics can be classified based on their linkage as esters or amides. Amides such as lidocaine are preferred due to lower risk of allergic reactions. Techniques of local anesthesia include infiltration, nerve blocks, and regional techniques like epidural and spinal anesthesia. Proper administration and dosage of local anesthetics is important to avoid potential toxicities.
1) Analgesics are important therapeutic agents in dentistry for treating pain. Common analgesics include acetaminophen, NSAIDs like ibuprofen, and opioids like codeine.
2) Combining analgesics that work through different mechanisms can provide better pain relief than single agents alone. Acetaminophen is often combined with opioids. NSAIDs allow for lower opioid doses to reduce side effects.
3) The combination of acetaminophen with codeine, hydrocodone, or tramadol provides effective relief of mild to moderate dental pain with fewer side effects than opioids alone. Ibuprofen combined with codeine or oxycodone also enhances analgesia.
This document discusses nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin. It provides details on their mechanism of action as cyclooxygenase inhibitors, reducing prostaglandin synthesis and inflammation. Common uses include analgesia, antipyresis, and reducing the risk of cardiovascular events like heart attacks. Adverse effects include gastrointestinal irritation and bleeding. Aspirin is prototypical and its pharmacology and therapeutic uses are discussed in depth.
Centrally acting muscle relaxants work in the central nervous system to reduce muscle tone without affecting consciousness. They selectively depress polysynaptic reflexes in the spinal cord and brain that are involved in regulating muscle tone. They also depress pathways in the brainstem that maintain wakefulness, but to a lesser degree. Common classes of centrally acting muscle relaxants include mephenesin congeners, benzodiazepines, GABA mimetics, and central α2 agonists. Examples are carisoprodol, diazepam, baclofen, and tizanidine. These drugs are used to treat muscle spasms, spasticity, and pain conditions involving muscle spasms.
This document discusses pharmacokinetics and provides details about absorption, distribution, and bioavailability of drugs. It defines key pharmacokinetic terms and describes factors that influence absorption such as solubility, concentration, route of administration, and mechanisms of absorption including passive diffusion, active transport, and pinocytosis. Membrane permeability and drug properties like pH and lipid solubility are discussed. The document also covers volume of distribution, plasma protein binding, tissue storage, and barriers to drug distribution like the blood-brain barrier.
This document provides information on general anaesthetics including their cardinal features, history, stages of anaesthesia, measurement of potency, mechanisms of action, classification, inhalational anaesthetics, intravenous anaesthetics, and conscious sedation. It discusses key figures and discoveries in the history of anaesthesia such as Humphry Davy, Horace Wells, William Morton, and John Snow. It also summarizes the stages of anaesthesia, factors that determine anaesthetic potency including oil-gas and blood-gas partition coefficients, and the pharmacokinetics and mechanisms of action of various inhalational and intravenous anaesthetic agents.
NSAIDs are the chemically diverse class of drugs that have anti-inflammatory, analgesic & antipyretic properties.
They are also called as Non Narcotic, Non Opioid, Aspirin like analgesics.
They are among the widely used therapeutic agents world wide and often taken without prescription for minor aches and pain.
They are used to suppress the symptoms of inflammation associated with rheumatic disease.
Helminth infections affect over two billion people worldwide. Anthelmintic drugs are used to kill or expel parasitic helminths. Major anthelmintic drug classes include piperazines, benzimidazoles, heterocyclics, and natural products. Mebendazole is a commonly used benzimidazole with broad-spectrum activity against intestinal worms and low incidence of side effects. Albendazole is similarly broad-spectrum but also treats cystic diseases. Diethyl carbamazine selectively kills microfilariae and is used to treat filariasis. Ivermectin is the treatment of choice for onchocerciasis and strongyloidiasis by enhancing chloride
This document discusses pharmacokinetics, specifically absorption, distribution, metabolism, and excretion of drugs. It covers the following key points:
- Drug absorption occurs through various routes like the gastrointestinal tract, lungs, skin and is influenced by factors like pH, blood flow and lipid solubility.
- Distribution of drugs depends on capillary permeability, blood flow, protein binding and is described using the volume of distribution.
- Metabolism occurs mainly in the liver through cytochrome P450 enzymes and conjugation reactions, and can inactivate drugs, produce active metabolites, or activate prodrugs.
- Absorption, distribution and metabolism determine the bioavailability of drugs and their delivery to sites of action.
1. NSAIDs work by inhibiting the cyclooxygenase (COX) enzymes, mainly COX-1 and COX-2, which decreases prostaglandin synthesis and produces their pharmacological effects. Selective COX-2 inhibitors have fewer side effects than non-selective NSAIDs.
2. NSAIDs have analgesic, antipyretic, and anti-inflammatory effects. Common side effects include gastric irritation, ulcers, renal impairment, and platelet dysfunction.
3. Aspirin has antiplatelet effects useful for cardiovascular protection. Indomethacin is potent but non-selective. Paracetamol is safer for those with bleeding risks but less effective at inflammation. COX-
Drug interactions can occur when two or more drugs are taken together. The effects of one drug may be altered by another drug through various mechanisms. Some key points:
1) Drug interactions can be pharmacokinetic, involving effects on absorption, distribution, metabolism and excretion of one or both drugs.
2) They can also be pharmacodynamic, where one drug alters the effects of another without changing its levels. This can include synergistic or antagonistic effects.
3) Common causes of interactions include effects on drug metabolizing enzymes like CYP450, protein binding displacement, renal tubular secretion competition and changes to gastrointestinal pH or motility.
4) Outcomes range from loss of
Factors affecting biotransformation of drugsZubia Arshad
The biotransformation of drugs can be affected by various chemical, biological, physiological, temporal, and environmental factors. Chemical factors include enzyme induction and inhibition, which can increase or decrease the metabolism of drugs. Biological factors like age, gender, genetics, diet, and disease states can impact drug metabolism rates. Physiological changes during pregnancy, with hormonal imbalances, or disease states can also alter drug biotransformation. Additional influencing factors are temporal variations, the route of drug administration, and environmental exposures. Careful consideration of all these potential factors is important for safe and effective drug therapy.
Unit-1: General pharmacology :Introduction to pharmacologySabaShaikh76
Introduction to Pharmacology- Definition and scope of pharmacology, nature and source of drugs, essential drugs concept and routes of drug administration, spare receptors, addiction, tolerance, dependence, tachyphylaxis, idiosyncrasy, allergy
The document discusses novel drug delivery systems. It begins with an overview of conventional drug delivery routes and their limitations. It then outlines the need for and goals of newer drug delivery modalities, which aim to control drug absorption, distribution, metabolism, and elimination. Several novel delivery routes are described in detail, including oral, sublingual, inhalation, transdermal, intranasal, and targeted delivery. Polymer-based delivery systems such as microspheres, nanoparticles, and intelligent delivery are also discussed. The document concludes by noting that advanced delivery technologies are playing an increasingly important role in improving drug safety, efficacy, and patient experience.
Individuals vary in their response to drugs due to several factors:
1. Body size influences drug concentration - larger individuals may require higher doses and smaller individuals like children require adjusted doses based on age and weight.
2. Age also impacts drug metabolism - children and elderly metabolize and excrete drugs differently than adults.
3. Other factors like sex, diet, alcohol use, genetics, disease states, and psychological factors can increase or decrease a drug's effects between patients. Doses often need adjusting based on these individual characteristics to achieve the desired therapeutic response without toxicity.
Sympathomimetic drugs mimic the actions of norepinephrine and epinephrine by binding to adrenergic receptors. They can be classified as direct-acting agonists like epinephrine, indirect-acting agonists like amphetamines, or mixed-action agonists like ephedrine. Common uses include pressor agents, cardiac stimulants, bronchodilators, nasal decongestants, CNS stimulants, and anorectics. Examples discussed in more detail include epinephrine, norepinephrine, dopamine, dobutamine, ephedrine, amphetamines, phenylephrine, and pseudophedrine.
This document provides an overview of pharmacology, which is defined as the study of how drugs act on living systems. It discusses key concepts including how drugs bind to receptors and cellular targets, different types of drug responses, factors affecting drug absorption and metabolism, and parameters used to evaluate drug safety and efficacy such as therapeutic index. The document outlines the progression of studies from in vitro to animal to clinical trials in drug development.
Bioavailability refers to the amount of drug that enters systemic circulation and is available at the site of action. It depends on the rate and extent of drug absorption from its dosage form. Many physiological and drug-specific factors can affect bioavailability such as pH, enzymes, blood flow, and food interactions. Careful evaluation and standardization of bioavailability is important for drug development and quality control to ensure accurate and safe dosing.
This document discusses 16 factors that can modify the effects of drugs in the body. These include:
1) Body weight, age, sex, species, and genetic differences can impact drug absorption and metabolism.
2) Route of administration determines speed and intensity of drug action. Oral drugs are slower than IV.
3) Diet, tobacco, alcohol and the environment can induce or inhibit drug metabolizing enzymes.
4) Psychological factors like expectations can impact drugs' efficacy through the placebo effect.
5) Disease states can increase or decrease drug absorption and levels in the body.
Bioavailability refers to the fraction of an administered drug that reaches systemic circulation. It is determined by comparing plasma drug levels after oral versus intravenous administration. Factors like first-pass metabolism, solubility, and drug formulation can influence bioavailability. The area under the plasma concentration-time curve (AUC) and other pharmacokinetic parameters are used to assess bioavailability and determine bioequivalence between products. The volume of distribution represents the theoretical space required to distribute the total amount of drug at the observed plasma concentration.
Pharmacology is a broad medical specialty that studies how drugs interact with living systems. It includes the study of drug synthesis, mechanisms of action, effects, and movement through the body. Some key areas are medicinal chemistry, pharmacodynamics, pharmacokinetics, chemotherapy, and toxicology. Drugs are given brand/trade names and have chemical/generic names. Pharmacists complete advanced degrees and dispense drugs through pharmacies and hospitals. Drug actions can be additive, synergistic, induce tolerance, or have idiosyncratic, side, or toxic effects. Major drug classes include analgesics, anesthetics, antibiotics, anticoagulants, antidepressants, antidiabetics, antihistamines, cardiovascular
The document discusses the history of adverse drug reactions and defines an adverse drug reaction. It describes several important incidents that increased awareness and regulation of drug safety, such as reactions to sulfanilamide in 1937 which led to the establishment of the FDA. It also discusses the thalidomide incident in the 1960s and the teratogenic effects it caused. The document estimates the incidence of adverse drug reactions for hospital inpatients and admissions. It examines various types of adverse drug reactions and factors that can influence them.
It will provide you a complete journey through the routes of drug administration, with all the basics covered I hope this presentation will make your fundamentals crystal clear.
Pharmacokinetics is the quantitative study of how the body affects a drug after administration through processes of absorption, distribution, metabolism, and excretion. Absorption involves a drug entering systemic circulation through various routes and is affected by properties of the drug and biological membranes. Distribution involves a drug passing through body compartments depending on its physicochemical properties. Metabolism chemically alters drugs in the liver to make them more excretable, while excretion removes drugs and metabolites through the kidneys, lungs, bile, intestines, skin, and other routes.
1. The document discusses the processes involved in a drug molecule traveling through the human body from administration to reaching its target site, known as pharmacokinetics.
2. Pharmacokinetics involves absorption of the drug into systemic circulation, distribution of the drug via blood plasma to tissues and organs, and elimination of the drug from the body through biotransformation or excretion.
3. For a drug to have an effect, it must reach the biophase, or site of action, at an appropriate concentration by passing through biological barriers in the body via processes like passive diffusion, carrier-mediated transport, vesicular transport, or paracellular transport between cells.
This document discusses the pharmacokinetics of drug absorption and distribution. It begins by defining pharmacokinetics as the quantitative study of how the body acts on drugs. It then discusses the different mechanisms of drug transportation across cell membranes, including passive diffusion, filtration, and carrier-mediated transport like facilitated diffusion and active transport. It describes factors that affect drug absorption like solubility, concentration, and route of administration. It also discusses concepts like bioavailability, bioequivalence, distribution, redistribution, barriers to drug movement, and plasma protein binding. In summary, it provides an overview of how drugs move into, through, and out of the body after administration.
This document discusses the pharmacokinetics of drug absorption and distribution. It covers several key topics in 3 paragraphs:
Membrane transporters, including passive diffusion, carrier-mediated transport processes like facilitated diffusion and active transport, allow drugs to be absorbed into the bloodstream. Factors like a drug's solubility, size and lipid solubility determine which transport mechanisms are used.
Absorption refers to the movement of drugs from the site of administration into circulation. The rate and extent of absorption depends on factors like solubility, concentration, administering area, vascularity and route. Oral drugs are affected by things like acidity, particle size and food. Injection routes see faster absorption.
Distribution
The document discusses the mechanisms of drug absorption from the gastrointestinal tract. There are several mechanisms for drug absorption including passive diffusion, active transport, and paracellular transport. Passive diffusion is the most common mechanism and involves drugs crossing cell membranes down their concentration gradients without expending energy. Active transport mechanisms use energy to transport drugs against concentration gradients and include primary active transport using ATP and secondary active transport coupling to other ion gradients.
Pharmacokinetics is the study of how the body affects drugs over time through absorption, distribution, metabolism, and excretion. Drugs move into, within, and out of the body through various transport mechanisms like passive diffusion, facilitated diffusion, and active transport. Factors like plasma protein binding, organ function, and route of administration influence a drug's absorption, distribution to tissues, metabolism by the liver, and excretion by the kidneys, lungs, bile, sweat, saliva or breast milk. Understanding these pharmacokinetic principles is important for predicting how drugs will behave in the body.
Presentation covers the basics of pharmacokinetic. Mechanism for the transport of drug molecule. Absorption, factors affecting on absorption of drugs. Concept of bioavailability. Distribution, plasma protein binding, tissue binding, barriers.
This document discusses the key concepts of pharmacokinetics including absorption, distribution, and bioavailability of drugs in the human body. It explains that pharmacokinetics is the quantitative study of how drugs move through the body and the factors that determine absorption rates like solubility, vascularity, and route of administration. It also describes the different mechanisms of transport including passive diffusion, carrier transport, and active transport. Distribution of drugs depends on factors like plasma protein binding and volume of distribution, which is the theoretical volume in which the drug is evenly distributed based on plasma concentration.
This document provides an overview of principles of pharmacokinetics, pharmacodynamics, and pharmacogenetics. It discusses key topics including absorption, distribution, metabolism, and excretion of drugs. Absorption involves drugs being taken up into systemic circulation and is influenced by route of administration, drug properties, and gastrointestinal factors. Distribution of drugs to tissues depends on blood flow, permeability, protein binding, lipophilicity, and tissue storage. Metabolism transforms drugs via phase I and phase II reactions, mainly in the liver, and can activate or inactivate compounds.
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.
Pharmacokinetics is the study of how the body affects drugs. It involves absorption, distribution, metabolism, and excretion of drugs. Absorption is how drugs enter the bloodstream and distribution is how drugs spread to tissues. Metabolism converts drugs to inactive forms through phase I (oxidation) and phase II (conjugation) reactions. Excretion eliminates drugs from the body. Together, these processes determine the effects of drugs over time.
This document discusses pharmacokinetics, which is the quantitative study of how drugs move through the body. It describes how drugs are transported across biological membranes via passive diffusion, facilitated diffusion, or active transport. It then discusses absorption, distribution, metabolism, and excretion of drugs. Absorption is affected by factors like solubility, concentration, and route of administration. Distribution depends on lipid solubility, protein binding, and regional blood flow. Drugs undergo biotransformation primarily in the liver and are metabolized to inactive or active forms. Excretion occurs primarily through urine or feces, with some drugs excreted in sweat, saliva, exhaled air, or milk.
1. Drug absorption involves the movement of a drug from its site of administration into the bloodstream or lymphatic system without being chemically altered.
2. There are several mechanisms of drug absorption including passive diffusion, carrier-mediated transport, endocytosis, exocytosis, and pore transport.
3. Factors that influence the rate and extent of drug absorption include the drug's physical and chemical properties, the dosage form characteristics, physiological factors in the body, and the route of administration. Understanding these factors is important for determining drug bioavailability and dosing.
The document discusses pharmacokinetics, which is the quantitative study of how drugs move through the body. It covers the key processes of absorption, distribution, metabolism, and excretion (ADME) that drugs undergo. Absorption governs how drugs enter circulation after administration. Distribution determines where drugs go in tissues. Metabolism, or biotransformation, alters drugs' chemical structures, often making them more water-soluble for excretion. These processes determine a drug's effects over time.
Pharmacokinetics is the study of how drugs move through the body, including absorption, distribution, metabolism, and excretion. Absorption is the process by which drugs enter systemic circulation from the site of administration. Several factors influence a drug's absorption, including its physicochemical properties, dosage form characteristics, and patient factors. The document discusses various mechanisms of drug absorption like passive diffusion, facilitated diffusion, active transport, and endocytosis. It also covers concepts like pH partition theory, factors affecting dissolution, and the importance of a drug's ionization for absorption.
chap no 1 INTRODUCTION TO PHARMACOLOGY 2.pptxMahnoorFatima92
This document provides an introduction to pharmacology and drug administration routes. It discusses the objectives of understanding drug resources, administration routes, absorption mechanisms, and key terminology. Several drug administration routes are defined, including intra-articular, intrathecal, intraosseous, and intraperitoneal injections. Factors that influence drug absorption like pH, blood flow, surface area, and P-glycoprotein expression are explained. Key terms like bioavailability, bioequivalence, therapeutic equivalence, and half-life are defined in regards to measuring drug properties and effects in the body.
This document provides an introduction to pharmacology concepts. It discusses what drugs are and how they work in the body. It covers absorption, distribution, metabolism, and excretion of drugs. Absorption involves passive diffusion, carrier-mediated transport, and endocytosis. Distribution depends on blood flow, protein binding, and accumulation in tissues. Metabolism occurs mainly in the liver through phase I and phase II reactions. Excretion involves renal and hepatic systems with water-soluble drugs or metabolites excreted in urine or bile.
The document discusses drug absorption and bioavailability. It defines absorption as the movement of an unchanged drug from the site of administration into systemic circulation. The mechanisms of drug absorption include passive diffusion, pore transport, ion pair transport, carrier-mediated transport, and endocytosis. Factors that can affect drug absorption are discussed such as pH, blood flow, surface area and contact time, multidrug resistance, solubility, drug instability, and the first pass effect. Bioavailability is then defined as the rate and extent to which the active drug becomes available at the site of action. Types of bioavailability include absolute and relative bioavailability.
Similar to Pharmacokinetics /prosthodontic courses (20)
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Chapter wise All Notes of First year Basic Civil Engineering
Syllabus
Chapter-1
Introduction to objective, scope and outcome the subject
Chapter 2
Introduction: Scope and Specialization of Civil Engineering, Role of civil Engineer in Society, Impact of infrastructural development on economy of country.
Chapter 3
Surveying: Object Principles & Types of Surveying; Site Plans, Plans & Maps; Scales & Unit of different Measurements.
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Chapter 4
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Chapter 6
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Text Books:
1. Palancharmy, Basic Civil Engineering, McGraw Hill publishers.
2. Satheesh Gopi, Basic Civil Engineering, Pearson Publishers.
3. Ketki Rangwala Dalal, Essentials of Civil Engineering, Charotar Publishing House.
4. BCP, Surveying volume 1
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LAND USE LAND COVER AND NDVI OF MIRZAPUR DISTRICT, UPRAHUL
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significant role in maintaining the ecological equilibrium of our planet.Land serves as the foundation for all human activities and provides the necessary materials for
these activities. As the most crucial natural resource, its utilization by humans results in different
'Land uses,' which are determined by both human activities and the physical characteristics of the
land.
The utilization of land is impacted by human needs and environmental factors. In countries
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to significant land degradation, adversely affecting the region's land cover.
Therefore, human intervention has significantly influenced land use patterns over many
centuries, evolving its structure over time and space. In the present era, these changes have
accelerated due to factors such as agriculture and urbanization. Information regarding land use and
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providing crucial environmental data for scientific, resource management, policy purposes, and
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changes, conversion trends, and other related patterns. The spatial dimensions of land use and
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Pharmacokinetics /prosthodontic courses
1. PHARMACOKINETICS
Pharmacokinetics is a quantitave study of drug movement
in,through and out of the body
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2. Pharmocokinetics include
Transport of the across the membrane
Absorpiton of the drug
Distribution of drug
Biotranformation or metabolism of drug
Excretion of the drug
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4. DRUGS ARE TRANSPORTED ACROSS THE MEMBRANES BY
Passive diffusion and filtration
Specilized transport
Passive diffusion :
The drug Diffuses across the membrane in the direction
of its conc. gradient, the membrane playing no active role
in the process.
It is the most important mechanism for majority of the drugs
Lipid soluble drugs diffuse by dissolving in the
Lipoidal matrix of the membrane, the rate of transport
Being proportional to the lipid: water partition coefficient of the drug
A lipid soluble drug attains higher conc. in the membrane and diffuses quickly
Also , greater the difference in the conc. of the drug on the two sides of the
membrane, faster is the diffusion.
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5. INFLUENCE OF PH
Weakly acidic drugs, which forms salts with cations
ionize more at alkaline ph
Eg: sodium phenobarbitone,pottasium pencillin v
Weakly basic drugs,which forms salts with anions
ionize more at acidic ph
Eg: atrophine sulphate
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6. FILTRATION
Filtration is the passage of drugs through the
acqueous pores in the membrane or through
paracellular spaces
This can be accelerated if hydrodynamic flow of the
solvent is occuring under hydrostatic or osmotic
pressure gradient
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8. CARRIER TRANSPORT : all cell membranes express a
host of transmembrane proteins which serve as carrier
or transporters for physiologically important ions ,
neutrients , metabolitestransmitters etc across the
membrane
Carrier transport is specific for substrate ,saturable,
competitively inhibited, analogues which utilizes the
same transporter, and is much slower than flux through
channels
Depending on requirement of energy ,carrier transport
is two types
Facilitated diffusion
Active transport
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9. FACILITATED DIFFUSION
The transporter belonging to the super family of solute
carreier(slc) transporters, operates passively without
needing energy and translocates the substrates in the
direction of its electrochemical gradient that is from
higher to lower concenteration
It mearly facilitates permeation of a poorly diffusable
substrate
Eg: the entry of glucose into the muscle and fat cells by
Gut
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10. ACTIVE TRANSPORT
It requires energy , is inhibited by metabolic poisons, and
transport the solute against its electrochemical gradient i.e low
to higher conc , resulting in selective accumulation of the
substance on one side of the membrane
Active transport can be primary or secondary depending on
the sourse of the driving force
Primary active transport: energry is obtained diretcly by the
hydrolosis of atp
The transportrs belong to the super family of atp binding
cassete (abc) transpoters whose intracelluar loops have atpase
activity they mediate only afflux of the solute from the
cytoplasm eighter to ecf or into an intracellular organelle
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11. Secondary active transport: In this type of active
transport effected by another set of SLC
transporters, the energy to pump one solute is
derived from the down hill movement of another
solute (mostly NA) .
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12. ABSORPTION
It is the movement of drug from its site of
administration into the circulation
Not only the fraction of administered dose that gets
absorbed,but also the rate of absorption is also
important
Except when given i.v ,the drug has to cross bilogical
membrane ;absorption is governed by the above
described principles.other factors affecting absorption
are acqueos solubility , the concentration.area of
absorbing surface ,vascularity of the absorbing surface
,route of administration
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13. BIOAVAILABILITY
Bioavailabilty refers to the rate and extent of absorption of
drug from a dosage form as determined by its conc –time
curve in blood or by its excretion in urine.
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14. It is a measure of the fraction F of administered dose of a
drug that reaches the systemic cirulation in the unchanged
form
Bioavailability of drug injected Iv is 100%, but is frequently
lowered as per oral injesion because
a) The drug may be incompletely absorbed
b) the absorbed drug may undergo first pass metabolism , in
the intestinal wall or liver or the excreted in bile.
Incomplete bioavaiability after sc or im injection is less
common ,but may occur due to local binding of the drug
Differences in bioavailability may arise due to variations in
disintegration and dissolution rate .
Differences in bioavalabilty are mostly seen with poorly
soluble and slowly absorbed drug .
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15. DISTRIBUTION
Once a drug has gained access to the blood stream , its gets
distributed to other tissues that initially had no drug ,
concentration gradient is in the direction of plasma-tissues
The extent of distibution of a drug depends on its lipid
solubility , ionisation at physiologic ph( a function of its pka ),
extend of binding to plasama and tissue proteins, presence of
tissue specific transporters and differences in the region of
blood flow
Movement of a drug proceeds untill an equilibrium is
established between unbound drug in plasma and tissue fluids
subsequently, there is parallel decline in both due to
elimination
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16. APPARENT VOLUME OF DISTRIBUTION
The volume that would accommodate all the drug in the body ,is
the conc through out was the same ,as in plasma.
Thus it describes the maount of drug present in the body as a
multiple of that contained in a unit volume of plasma.
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17. REDISTRIBUTION
Highly lipid soluble drugs gets intilayy distributed to
organs with high bolld flow i.e brain heart kidney
etc.;later, less vascular but more bulky tissues
(muscle,fat) take up the drug –plasma conc falls and the
drug is withdrawn from these sites
If the site of action of the drug was in one of the highly
perfused organs, redistribution results in termination of
drug action.
Greater the lipid solubility of the drug , faster is its
redistribuiton
Anastetic action of thiopentene sodium injected I.V
isdominated in few minutes due to redistribution
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19. PLASMA PROTEIN BINDING
Most drugs posesses physicochemical affinity for plasma proteins
Acidic drugs generally bind to plasma albumin
Basic drugs to alpha 1 acid glycoprotein.
Binding to albumin is quantitaively importanat
Higly plasmaprotein bound drugs are largely restricted to the vascular
compartment because the protein bound drug doesnot cross the membrane
they tend to have smaller volumes of distribution
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20. The bound fraction is not available for action however ,it is a
equlibrium with a fee drug in plasma and dissociates when
the conc of the late r is reduced due to elimination plasma
protein binding thus tantamounts to the temporary storage of
the drug .
HIGH DEGREE OF PROTEIN BINDING generally makes the
drug long acting because bound fraction is not available for
metabolism or excretion, unless it is actvely extracted in the
liver or kidney tubules
Generally expressed plasma concentration of the drug refer to
ound as well as free drug
One drug can bind to may sites on the albumin molecule.
Conversly, more than one drug can bind to same site this can
give rise to displacement interactions among drugs bound to
the same site.
Eg: salicylates displace sulfonyl urea
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21. BIOTRANSFORMATION
Biotranspformation means chemical alteration of the
drug in the body
It is needed to render nonpolar(lipid soluble)
compounds polar(lipid insoluble) so that there are not
reabsorbed in the renal tubules and are excreted .
Most hydrophillic drugs eg: strptomycin are little
biotransformed they are largely excreted unchanged
Mechanisms which metabolise drugs( essentially
foregin substances ) have developed to protect body
from injested toxins
Primary site for drug metabolism is liver others are
kidneys,intestines,plasma
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22. Biotransformation of drugs leads to following :
A) Inactivation
B) Active metabolite from inactive drug
C) Activation of inactive drug
Inactivation: most drugs ad their active metabolite are rendered
inactive or less active eg: ibuprofen,PCT,lidocaine
Active metabolite form inactive drug:many drugs have been
found to be partially converted to one or more active
metabolite
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23. Activation of inactive drug: few drugs are inactive
as such and need conversion in the body in one or
more active metabolites such a drug is called
prodrug .prodrug may offer advantages over the
active form in being more stable , having better
bioavailability less side effects and toxicity
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24. Biotransoformation reaction can be classified into
non synthetic or phase 1 or function alization
reactions
Metabolite may be actve or inactive .
Oxidation
Reduction
Hydrolysis
Cyclization
Decyclization
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25. Synthetic or phase 2 reaction :
Metabolite is mostly inactive
Glucuronide conjugation
Acetylation
Methylation
Sulfate conjugation
Glycine conjugation
Glutathione conjugation
Libonucleoside or nulceotide snthesis
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26. INHIBITION OF DRUG METABOLISM
one drug can competetively inhibit metabolism of
another if it utilizes the same enzyme or cofactor
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27. CON SEQUENCES MICROSOMAL ENZYME INDUCTION
Decreased intensity and or duration of action of drugs
that are inactivated by metabolism
Eg: failure of contraception with oral contraceptives
Increased intensity of action of drugs that are activated
by metabolism acute PCT toxicity is due to one of its
metabolites –toxicity occurs at lower dosage in patients
receing enzyme inducers
Intermittent use of an inducer may interfere with the
adjustment of those of another drug prescribed on
regular bases eg: oral anticoagulants ,oral
hypoglycemics ,anti epileptics and anti hypertensives
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28. POSSIBLE USES OF ENZYME INDUCTION
Congenital non hemolytic jaundice it is due to deficinet
glucoridation of bilurubin ; phenobarbitone hastens
cleareance of jaundice
Cushings syndrome phenatoin may reduce the
manifestation sof enhancing the degradation of
adrenosteroids
Chronic poisoinings by faster metabolism of the
accumulated poisonous substance
Liver disease
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29. FIRST PASS (PRESYSTAMIC) METABOLISM
This refers to metabolism of a drug during its passage from
the site of absortion into the systemic circulation
All orally administerd drugs are exposed to drug
metabolizing enzymes in the intestina wall and liver( where
they first reach through portal vein)
The extent of first pass metabolism differs for different drus
and is important for determinant of oral bioavailabilty
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30. Attributes of drugs with hisg first pass metabolism
A) oral dosage cosiderably higher than sub lingual or
parenteral dose
B) there is marked individual varation in the oral dose
due to differences in the xtents of first pass metabolism
C)oral bioavailabiltity is apparently increased in
patients with severe liver diseases
D) oral bioavailability of a drug is increased if another
drug competeing with it in first pass metabolism is
given concurrently
Eg: chlorpromazine and propanalol
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31. EXCRETION
Excretion is the passage out of systemically absorbed
drugs
Drugs and their metabolites are excreted in
Urine
Feaces
Exhaled air
Saliva and sweat
Milk
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32. RENAL EXCRETION
Net renal excretion = (glomerular filtration +tubular
secretion)- tubular reabsorption
Weak bases ionise more and are less reabsorbed in acidic urine
Weak acids ionise more and less reabsorbed in alkaline urine
Drugs utilizing the same active transport comete with each
other
Eg: probencid an organic acid which has high affinity for the
tubular oatp it blocks the active transport of both pencillin and
uric acid
Many dug interaction occur due to competetion ofr tubular
secretion
Salicylates block uricosuric action of probencid
And sulfinperazone and decrease tubular secretion of
methotrexate
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33. KINETICS OF ELIMINATION
They are 3 fundamental formacokinetics parameters namely
Bioavailability(F)
Volume of distribution(v)
Cleareance (Cl)
Drug elimiation is the sumtotal of metabolic inactivation and
excretion
Drug is eliminated only from the central compartment (blood)
which is in equlibrium with perepheral compartments
including the site of action
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34. Depending upon the ability of the body to elimianate a
drug, is again the fraction of the central compartment
may be considered to be totally “cleared” of that drug in
a given period of time to account for elimination over
that period
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35. CLEREANCE
Clereance of a drug in the theoritical volume of plasma from
which the drug is ocmpletey removed in a unit time
It can be caluclated as cl=rate of elimiation /C
WHERE C IS THE PLASMA CONC.
FOR MAJORITY OF DRUGS THE PREOCESS INVOLVED IN
ELIMINIATION ARE NOT SATURATED OVER THE
CLINICALLY OBTAINED CONCENTRATIONS
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36. First order (exponential )kinetics: The rate of elimitation is
directly proportional to drug concentraton,CL remains
constant
Zero order kinetics:The rate of elimination remains constant
irrespective of drug concentration ,CL decreases with increase
in concentration
plasma half-life: The plasma half life (t1/2) of a drug is the
time taken for its plasma concentration to be reduced to half
of its original value
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37. PHARMOCOCKINETICS OF NSAID
Aspirin: it is absorbed from stomach and small intestine its
poor water solubility is a limiting factor in absoorption .
Microfining the drug particles and inclusion of an alkali
enhances absorption
Aspirin is readily deacytylated in gut wall ,liver plasma,and
other tiuuses to release salycylic acid which is a major
circulating and active form
It is 80% bound to plasma protein and has a volume of
distribution 0.17 lit/kg
It slowly enters the brain but freely crosses plaacenta
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38. ASPIRIN CONT’D
Both aspirin and salycylic acid are conjugated in liver
by glycine to give salicyluric acid (major part) and with
glucorinic acid.
Few other metabolites are also formed
Excretion : the metabolites are excreted by GF as well as
tubular secretion normally only 1/10th is excreted as
free salycylic acid ,it can be increased by alkalysation
Plasma half life of aspirin as such is 50-20min , but taken
together with that of released salycylic acid it is 3- 5 hrs
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39. IBUPROFEN
It is absorbed orally
Higly bound to plasma proteins ( 90-99%), but
displacement interactions are not clinically significant-
dose of anticoagulants and oral hypoglycemics need not
to be altered becoz they inhibit platelet function , use
with anticoagulants should, neverthless, be avoided.
All propionic acid derivitives enters brain ,synovial fluid
and cross placenta
They are largely metabolized in liver by hydroxylation
and glucuronide conjugation and excreted in urine as
well as bile
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40. DICLOFENAC SODIUM
It is well absorbed orally ,99% protein bound,
metabolised and excreted both in urine and bile
Plasma life is approximately 2hrs however, it had good
tissue penetrability and conc in synovial fluid is
maintaianed for 3 times longer period than in plasma,
exerting extended herpatic action in joints
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41. KETOROLAC
It is rapidly absorbed oral & im administration
It is higly plasma protein bound and 60% excreted
unchanged in urine.
Major metabolic pathway is glucorodination
Plasma half life 5- 7hrs
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42. NIMUSULIDE
It is almost completely absorbed orally
99% plasma protein bound
Extensively metabolised and excreted mainly in urine
2-5 hrs plasma half life
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43. PARACETMOL
Dethylated active metaboite of phenacetin
It is well absorbed orally, only about ¼th is proein
bound in plasma and it is uniforamly distributed in the
body
Metabolism occurs mainly by conjugation with
glucuronic acid and sulphate
Conjugates are rapidly excreted in urine
Plasma half is 2-3 hrs
Effect after an oral dose lasts for 3- 5 hrs
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44. INSULIN
Insulin is distributed only extracellularly
It is a peptide, gets degraded in git given orally
In injected insulin or that released from pancrease is
metabolised primarly in liver and to a smaller extent in kidney
and muscles
Nearly half of the insulin entering portal vein from pancrease
is inactivated in the first passage through liver
thus normally liver is exposed to much higher conc of insulin
than other tissues
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45. During biotransformation the disulphide bonds are
reduced – A n B chains are seperated.these are further
broken down to the constituent amino acids
Plasma half life 5- 9 mins
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46. PHENATOIN
Absoprtion of phenotoin by oral route is slow mainly
because of its poorly acqueous solubility
80-90% bound to plasma protein
Widely distribute in the body
Metabolised in liver by glucoridination conjugation
only 5% unchanged pheotoin is excreted in urine
Plasma life is 12- 24 hrs
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47. CARBAMAZEPINE
Oral absorption of c is slow and variable because of
poor water solubility
It is 75 % bound to plasma protein
It is meabolised in liver by oxidation to an active
metabolite (10-11 ipoxycarbazepine) as well as by
hydroxylation and conjugation to inactive ones
It s a substrate as well as inducer of CYP3A4 and other
drug metabolizing enzyme
Initially its plasma half life is 20 -40 hrs , but, decreases
to 10 to 20 hrs on chronic medication due to
autoinduction of metabolism
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48. PHARMOCOKINETICS OF ANTIBIOTICS
Ciprofloxacin: it is rapidly absorbed orally but food delays
absorption and first pass metabolism occurs
The most prominent featue of ciprofloxacin is high tissue
pennetrability ,conc in lung ,sputum,muscle , bone, prostrate
and phagocytes
Exceeds that of plasma, csf and acqueous levels are lowered .
It is excreted primarly in urine both by glomerular filtration and
tubular secretion
Urinary and biliary conc are 10-50 fold higher than plasma
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49. OFLOXACIN
It is relatively lipid soluble
Oral bioavailability is high
Attains high plasma conc.
Food doesnot interfere with its absorption
It is excreted largely unchanged in urine
Dose needs to be reduced in renal failure
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50. PENCILLIN G
PENCILLIN G IS acid labile destroyed by gastric acid as such
less than 1/3rd of an oral dose is absorbed in the active form
Absorption of sod.P.g from im site is rapid and complete
Peak plasma level is attained in 30 min
It is distributed mainly extracellularly
Reaches most body fluids, but penetration in serous cavities
and csf is poor
60% plasma protein bound
It is little metabolised due to rapid excretion
The pharmacokinetics of PmG is dominated by very rapid
renal excretion; about 105 by glomerular filteration and the
rest by tubular secretion
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51. Plasma half life of pencillin g is 30min in healthy
adults
Neonates have slower tubular secretion – plasma
half life is longer ;but appraches adult value by
3months and its even shorter in childhood
Aged and those with renal failure excrete pencillin
slowly
Tubular secretion of penG CAN be blocked by
probencid – higher and longer lasting plasma conc
are achieved
Probencid also decreases the volume of distribution
of pencillins
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52. AMPICILLIN
Ampicillin is not degraded by gastric acid
Oral absorption is incompete but adequate
Food interferes with absorption
It is parly exctreted in bile and reabsorbed-
enterohepatic cirulation occurs
However,primary zone of excretion is kidney. But
tubular secretion is slower than png
Plasma half life 1hr
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53. AMOXCILIN
It is a close congener of ampicillin (but not a
prodrug);similar to it in all respects except oral
absorption is better
Food doesnot interfere with absorption
High but sustain blood levels are obtained
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54. CLAVULONIC ACID
It has rapid oral absorption and bioavailabilty of 60%
,can also be injected
Plasma half 1hr and tissue distribution matches
amoxcillin with which it is used ( 3rd coamoxiclav).
However,it is eliminated mainly by glomerular
filteration and its excretion is not effetced by pobenicid.
Also. It is largely hydrolysed and decarboxylated before
excretion, while amox is primarly excreted unchanged
by tubular secretion
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55. TETRACYCLINE
older tetracyclines are incompletely absorbed from git
Absorption is better if taken in empty stomach
Dox & mino are compltely absorbed irrespective of food
Tetracycline have celating propertie-insoluble and
unabsorbable complexes with calcium and other metals
.
Milk,iron preparation, nonsystemic antacids and
sucrolfate reduce their absorption
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56. The csf conc of most tetracyclines is about one half of the
plasma conc ,whether meninges are inflamed or not
Most tetracyclines are excreted in urine by glomerular
filteration
Dose has to be reduced in renal failure;dox is an exception to
this
They are partly metabolized and significant amounts enter
bile –some degree of enterohepatic circulation occurs
They are secreted in milk I amounts sufficient to effect the
suckling infant
Interaction: Enzyme inducers like phenobarbitone and
phenatoin enhance metabolism and reduces the half life of
dox
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57. ACYCLOVIR
Only about 20% of an oral dose of acyclovir is absorbed
It is plasma protein bound and is widely distributed
attaining csf concentration that is 50% of plasma
concentration
Excreted unchanged in urine
T1/2: 2-3 hrs
Renal impairment necessitates dose reduction
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58. CORTICOSTEROIDS
All natural & synthetic steroids are absorbed by
oral mucosa
Hydrocortisone undergoes high first pass
metabolism ,,90% bound to plasma
Steroids are metabolised by hepatic microsomal
enzymes
Metabolites are excreted in urine
T1/2 life is 1.5 hrs
Interaction: phenobarbitone and phenytoin induce
metabolism of hydrocortisone and prednisolone
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59. MUSCLE RELAXANTS
All neuromusculr blockers are not absorbed orally
They are always given iv
Atracurium is inactivated in plasma by spontaneous
noenzymal degradation
Excreted in urine n bile
Interaction : thiopentone sodium & SCH should be
mixed in the same syringe-react chemically
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