Prodrugs are inactive compounds that are metabolized in the body to an active drug. Prodrugs can improve therapeutic efficacy and reduce adverse effects by increasing solubility, permeability, bioavailability, and targeted delivery to tissues. Site-specific delivery is achieved through enzymatic activation of the prodrug only at the desired site of action, such as the brain or infected cells. Examples of prodrugs discussed include oseltamivir, l-dopa, and bambuterol. Challenges in prodrug design include interindividual variability in metabolizing enzymes and ensuring sufficient conversion of the prodrug to the active drug.
Basic concepts of Prodrug & their application in pharmacy fieldsSHUVAM SAR
Definition of prodrugs along with their uses in pharmacy have been discusses here in brief. Also includes the basic objectives of their formulation with examples.
Metabolism,Excretion,prodrug,Therapeutic Drug monitoringSrinivasSree11
1. Metabolism and excretion are important processes that determine the duration and intensity of a drug's effects in the body. Metabolism involves chemical alteration of drugs through phase I and phase II reactions, while excretion removes drugs and metabolites from the body through renal, hepatic, pulmonary and other routes.
2. Factors like age, diet, diseases, genetic factors and simultaneous administration of other drugs can influence drug metabolism by inducing or inhibiting drug-metabolizing enzymes. Metabolism can convert drugs to active, inactive or less active forms.
3. Prodrugs are inactive forms administered to deliver the active drug selectively or improve pharmacokinetics. They are converted to active drugs through metabolic processes
The document presents a project on water soluble and insoluble prodrugs by Sunil Saini. It defines prodrugs as pharmacologically inactive derivatives of active drugs that are designed to maximize the amount of active drug that reaches its site of action. The project discusses how various prodrugs are used to increase drug absorption, improve site-specific delivery, prolong drug action, and decrease side effects.
The document discusses various enzyme inhibitors including xanthine oxidase inhibitors, cytochrome P450 inhibitors, DHFR inhibitors, and gastric proton pump inhibitors. It provides details on the mechanisms of several specific inhibitors such as allopurinol, ciprofloxacin, trimethoprim, and omeprazole. The document was presented by Sanjay Gopi to Dr. S.D. Joshi of the Department of Pharmaceutical Chemistry at SET's College of Pharmacy in Dharwad, India.
The document discusses the rationale and various approaches for prodrug design. It summarizes that prodrugs can be designed to (1) modify physicochemical properties like eliminating volatility, improving stability or solubility; (2) minimize toxicity by masking reactive functional groups; (3) encourage patient acceptance by modifying taste, odor or injection pain; and (4) improve absorption, distribution and site specificity by altering membrane permeability or targeting enzymes. Specific examples are given like methenamine as a urinary tract antiseptic, ester prodrugs of aspirin to reduce gastric toxicity, and amino acid esters of antiviral drugs to enhance solubility. The document highlights how prodrugs can overcome pre-systemic metabolism, provide
A prodrug is an inactive or less active pharmacological substance that is converted into an active drug through normal metabolic processes. Prodrugs are designed to improve properties like absorption, distribution, metabolism, and excretion of the intended drug. Prodrugs can be classified as Type I, which are activated intracellularly, or Type II, which are activated extracellularly such as in digestive fluids or circulation. Common examples of prodrugs include enalapril, which is converted to enalaprilate; oseltamivir (Tamiflu), which is converted to oseltamivir carboxylate; and famciclovir, which is converted to penciclovir.
Pro-Drug and Active Drug In Medicinal Chemistry.pptPrachi Pandey
The document provides an overview of prodrugs and their applications in medicinal chemistry. It defines prodrugs as biologically inert derivatives of drug molecules that undergo enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. The document discusses various classifications of prodrugs and their purposes in improving drug properties like solubility, stability, absorption and reducing toxicity. It also summarizes key pharmaceutical applications of prodrugs in masking taste/odor, reducing irritation, improving solubility, prolonging drug action, and enabling site-specific drug delivery.
Basic concepts of Prodrug & their application in pharmacy fieldsSHUVAM SAR
Definition of prodrugs along with their uses in pharmacy have been discusses here in brief. Also includes the basic objectives of their formulation with examples.
Metabolism,Excretion,prodrug,Therapeutic Drug monitoringSrinivasSree11
1. Metabolism and excretion are important processes that determine the duration and intensity of a drug's effects in the body. Metabolism involves chemical alteration of drugs through phase I and phase II reactions, while excretion removes drugs and metabolites from the body through renal, hepatic, pulmonary and other routes.
2. Factors like age, diet, diseases, genetic factors and simultaneous administration of other drugs can influence drug metabolism by inducing or inhibiting drug-metabolizing enzymes. Metabolism can convert drugs to active, inactive or less active forms.
3. Prodrugs are inactive forms administered to deliver the active drug selectively or improve pharmacokinetics. They are converted to active drugs through metabolic processes
The document presents a project on water soluble and insoluble prodrugs by Sunil Saini. It defines prodrugs as pharmacologically inactive derivatives of active drugs that are designed to maximize the amount of active drug that reaches its site of action. The project discusses how various prodrugs are used to increase drug absorption, improve site-specific delivery, prolong drug action, and decrease side effects.
The document discusses various enzyme inhibitors including xanthine oxidase inhibitors, cytochrome P450 inhibitors, DHFR inhibitors, and gastric proton pump inhibitors. It provides details on the mechanisms of several specific inhibitors such as allopurinol, ciprofloxacin, trimethoprim, and omeprazole. The document was presented by Sanjay Gopi to Dr. S.D. Joshi of the Department of Pharmaceutical Chemistry at SET's College of Pharmacy in Dharwad, India.
The document discusses the rationale and various approaches for prodrug design. It summarizes that prodrugs can be designed to (1) modify physicochemical properties like eliminating volatility, improving stability or solubility; (2) minimize toxicity by masking reactive functional groups; (3) encourage patient acceptance by modifying taste, odor or injection pain; and (4) improve absorption, distribution and site specificity by altering membrane permeability or targeting enzymes. Specific examples are given like methenamine as a urinary tract antiseptic, ester prodrugs of aspirin to reduce gastric toxicity, and amino acid esters of antiviral drugs to enhance solubility. The document highlights how prodrugs can overcome pre-systemic metabolism, provide
A prodrug is an inactive or less active pharmacological substance that is converted into an active drug through normal metabolic processes. Prodrugs are designed to improve properties like absorption, distribution, metabolism, and excretion of the intended drug. Prodrugs can be classified as Type I, which are activated intracellularly, or Type II, which are activated extracellularly such as in digestive fluids or circulation. Common examples of prodrugs include enalapril, which is converted to enalaprilate; oseltamivir (Tamiflu), which is converted to oseltamivir carboxylate; and famciclovir, which is converted to penciclovir.
Pro-Drug and Active Drug In Medicinal Chemistry.pptPrachi Pandey
The document provides an overview of prodrugs and their applications in medicinal chemistry. It defines prodrugs as biologically inert derivatives of drug molecules that undergo enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. The document discusses various classifications of prodrugs and their purposes in improving drug properties like solubility, stability, absorption and reducing toxicity. It also summarizes key pharmaceutical applications of prodrugs in masking taste/odor, reducing irritation, improving solubility, prolonging drug action, and enabling site-specific drug delivery.
Biologically inert derivatives of drug molecules that undergo an enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. Classification of pro- drugs.
this article include useful information about antibiotic working in DNA inhibitor may direct action as sulfonamide or indirect action as fluroquinolone groups.
the presentation show mechanism of actions,uses , adverse effect ,also resistance and pharma-cokinetic properties of each drug.
in simple way and a lot of picture to describe information this work is done .
thanks
Systemic fungal infections can be life-threatening, especially in immunocompromised patients. Anti-fungal drugs target the fungal cell membrane and include polyenes like amphotericin B, azoles, and antimetabolites like flucytosine. Amphotericin B has a broad spectrum of activity but significant toxicity, while azoles like itraconazole are better tolerated and used for both superficial and systemic fungal infections. These drugs differ in their mechanisms of action, pharmacokinetics, spectra of activity, and adverse effect profiles.
The document discusses macrolide antibiotics such as erythromycin, clarithromycin, and azithromycin. It also discusses the antimalarial chloroquine and its mechanism of action, inhibiting heme polymerization in plasmodium parasites. The prodrug concept and applications are explained, including improving drug properties like taste, solubility, and bioavailability.
Prodrugs an approach to solve problems related to admeJyotsna Patil
prodrugs an approach to overcome problems related to ADME, for MPharm students
sub- modern pharmaceutical and medicinal chemistry
branch- quality assurance
The document discusses the basic concepts and applications of prodrug design. It defines a prodrug as an inactive derivative of an active drug that undergoes biotransformation in the body to release the pharmacologically active drug. The objectives of prodrug design include improving pharmaceutical and pharmacokinetic properties like solubility, stability, absorption and reducing toxicity. Prodrugs are classified based on their structure and site of bioactivation. Applications of prodrugs include masking taste/odor, reducing irritation, enhancing solubility/bioavailability, prolonging duration of action, reducing toxicity and enabling site-specific drug delivery.
This document summarizes information about the drug dapsone, including:
1. Dapsone was invented in the early 20th century and is commonly used to treat leprosy in combination with other drugs.
2. It is absorbed after oral administration and metabolized in the liver. Common side effects include anemia, nausea, and rashes.
3. Analytical methods like HPLC and spectroscopy can be used to detect and quantify dapsone in samples.
An Outline on Various Methods Used in Formulation and Evaluation of Lansopraz...IRJET Journal
This document discusses the formulation and evaluation of lansoprazole liposomes and pro-liposomes. Lansoprazole is a drug used to treat gastric ulcers and acid reflux. The abstract outlines methods for creating lansoprazole liposomes and pro-liposomes using techniques like film deposition and spray drying. It also discusses evaluation methods for characterizing the formulations, such as particle size, zeta potential, and drug release studies. The goal is to develop a biocompatible liposomal formulation of lansoprazole that improves solubility, stability and bioavailability for treating conditions like ulcers and inflammation.
The prodrug concept was first proposed in 1958 as a way to temporarily modify drugs' physicochemical properties to improve their usefulness and decrease toxicity. Prodrugs are converted to the active drug within the body through enzymatic or non-enzymatic reactions. This allows for improved solubility, delivery, stability, and decreased adverse effects. Ideal prodrugs are inactive or less active than the parent drug, are cleaved in vivo to release the parent drug, and produce non-toxic metabolic fragments. Common prodrug modifications include esterification of carboxylic acids and alcohols as well as derivatization of carbonyl groups. Successful prodrugs have been developed to improve patient acceptance, reduce gastric irritation,
Drug acting on Leprosy, Antileprotic drugs KundanSable1
This document discusses drugs used to treat leprosy (Hansen's disease), which is caused by the bacterium Mycobacterium leprae. It describes several classes of antileprotic drugs, including sulfones like dapsone, phenazine derivatives like clofazimine, and antitubercular drugs like rifampin and ethionamide. For each drug class, it outlines the mechanism of action, pharmacokinetics, adverse effects, and other details. Other antibiotics discussed for treating leprosy include ofloxacin, minocycline, clarithromycin, and moxifloxacin.
The document provides information on prodrugs. It defines a prodrug as a biologically inert derivative of a drug molecule that undergoes conversion in vivo to release the active parent drug. The objectives of prodrug design include improving solubility, stability, absorption, and decreasing toxicity. Examples are given of common prodrugs and how they achieve various objectives like masking taste, reducing irritation, and prolonging duration of action. Prodrug strategies can also be used for targeted drug delivery in chemotherapy through approaches like antibody-directed enzyme prodrug therapy.
This document discusses genetic polymorphisms in enzymes. It provides examples of polymorphisms in alcohol dehydrogenase, aldehyde dehydrogenase, dihydropyrimidine dehydrogenase, glutathione S-transferases, and butyrylcholinesterase. These polymorphisms can result in variations in enzyme activity levels and impact drug metabolism and toxicity. The document also discusses how certain polymorphisms are associated with increased risks of diseases like cancer when combined with environmental exposures like smoking or drinking alcohol.
The document discusses nasal drug delivery systems. It covers the anatomy and physiology of the nose, mechanisms of nasal absorption, factors affecting absorption like molecular weight and pH, strategies to improve absorption like penetration enhancers, and considerations for nasal drug formulations including pH, osmotic agents, and absorption enhancers. The nasal route offers advantages like avoiding first-pass metabolism and rapid drug absorption but faces limitations such as low bioavailability and enzymatic degradation.
The document discusses basic concepts and applications of prodrug design. It defines prodrugs as biologically inert derivatives of drug molecules that undergo enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. The objectives of prodrug design include improving pharmaceutical and pharmacokinetic properties as well as decreasing toxicity. Applications of prodrugs include masking taste/odor, reducing irritation, enhancing solubility/stability, improving bioavailability, preventing presystemic metabolism, prolonging duration of action, reducing toxicity, and enabling site-specific drug delivery such as in chemotherapy through directed enzyme prodrug therapy.
The document discusses various drugs that act on blood and blood forming agents as well as the renal system. It begins by classifying anticoagulants as those used in vitro like heparin and calcium complexing agents, and those used in vivo like heparin, heparinoids, hirudin, and oral anticoagulants. It then describes the mechanisms and pharmacological actions of heparin and oral anticoagulants like warfarin. The document also discusses diuretics, classifying them as high efficacy loop diuretics like furosemide, medium efficacy thiazide diuretics, and weak adjunctive diuretics. It provides details on the mechanisms and
increase membrane permeability by prodrug design.keshob ghosh
This presentation discusses prodrugs and how they can improve membrane permeability and drug absorption. A prodrug is a medication that is metabolized into an active drug after administration. Prodrugs are used to improve patient acceptability, alter absorption and distribution, alter metabolism and elimination, and allow drugs that do not cross biological barriers like the blood brain barrier to do so. The presentation provides examples of prodrugs like oseltamivir and valacyclovir and explains how they work to improve permeability through passive diffusion or carrier-mediated transport by increasing lipophilicity or allowing recognition by transporters.
This document provides an overview of prodrug design. It defines a prodrug as an inactive derivative of a drug molecule that undergoes biotransformation to release the active drug. Prodrugs are classified based on their structure and include carrier-linked, bipartite, tripartite, mutual, and bioprecursor prodrugs. The document discusses various rationales for prodrug design such as improving solubility, absorption, patient acceptability, and site-specific drug delivery. Common functional groups used in prodrugs include esters, amides, phosphates, and carbamates. The document also covers practical considerations and approaches for overcoming limitations like pre-systemic metabolism and blood-brain barrier penetration.
This document provides information on propofol, an intravenous anesthetic. It discusses propofol's history, chemical properties, formulations, pharmacokinetics, mechanisms of action, effects on organ systems, uses, adverse effects, and interactions. Propofol is a widely used anesthetic due to its rapid onset and offset of action. It acts by potentiating GABA receptors in the brain and has numerous clinical applications beyond general anesthesia induction. The document provides detailed information on propofol's properties and clinical use.
Polymerase Chain Reaction (PCR) is a technique that amplifies a specific DNA sequence. It involves denaturing DNA, annealing primers to the DNA, and extending the primers to replicate the DNA. Through repeated cycles of heating and cooling, the targeted DNA sequence is exponentially amplified, allowing it to be detected and manipulated. PCR is used to identify infectious organisms like viruses, detect genetic mutations, and replicate DNA for further analysis. Careful primer design is important for PCR to specifically amplify the desired DNA sequence.
test Item Charecterization importance in Toxicology.pptxSourinDe2
Test item characterization and methods are important in regulatory toxicology. Proper characterization of test items involves identification of chemical constituents and impurities that may impact safety assessment. Brief methods for characterizing test items include analytical techniques like chromatography that can provide purity and identity information required for regulatory toxicology studies.
Biologically inert derivatives of drug molecules that undergo an enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. Classification of pro- drugs.
this article include useful information about antibiotic working in DNA inhibitor may direct action as sulfonamide or indirect action as fluroquinolone groups.
the presentation show mechanism of actions,uses , adverse effect ,also resistance and pharma-cokinetic properties of each drug.
in simple way and a lot of picture to describe information this work is done .
thanks
Systemic fungal infections can be life-threatening, especially in immunocompromised patients. Anti-fungal drugs target the fungal cell membrane and include polyenes like amphotericin B, azoles, and antimetabolites like flucytosine. Amphotericin B has a broad spectrum of activity but significant toxicity, while azoles like itraconazole are better tolerated and used for both superficial and systemic fungal infections. These drugs differ in their mechanisms of action, pharmacokinetics, spectra of activity, and adverse effect profiles.
The document discusses macrolide antibiotics such as erythromycin, clarithromycin, and azithromycin. It also discusses the antimalarial chloroquine and its mechanism of action, inhibiting heme polymerization in plasmodium parasites. The prodrug concept and applications are explained, including improving drug properties like taste, solubility, and bioavailability.
Prodrugs an approach to solve problems related to admeJyotsna Patil
prodrugs an approach to overcome problems related to ADME, for MPharm students
sub- modern pharmaceutical and medicinal chemistry
branch- quality assurance
The document discusses the basic concepts and applications of prodrug design. It defines a prodrug as an inactive derivative of an active drug that undergoes biotransformation in the body to release the pharmacologically active drug. The objectives of prodrug design include improving pharmaceutical and pharmacokinetic properties like solubility, stability, absorption and reducing toxicity. Prodrugs are classified based on their structure and site of bioactivation. Applications of prodrugs include masking taste/odor, reducing irritation, enhancing solubility/bioavailability, prolonging duration of action, reducing toxicity and enabling site-specific drug delivery.
This document summarizes information about the drug dapsone, including:
1. Dapsone was invented in the early 20th century and is commonly used to treat leprosy in combination with other drugs.
2. It is absorbed after oral administration and metabolized in the liver. Common side effects include anemia, nausea, and rashes.
3. Analytical methods like HPLC and spectroscopy can be used to detect and quantify dapsone in samples.
An Outline on Various Methods Used in Formulation and Evaluation of Lansopraz...IRJET Journal
This document discusses the formulation and evaluation of lansoprazole liposomes and pro-liposomes. Lansoprazole is a drug used to treat gastric ulcers and acid reflux. The abstract outlines methods for creating lansoprazole liposomes and pro-liposomes using techniques like film deposition and spray drying. It also discusses evaluation methods for characterizing the formulations, such as particle size, zeta potential, and drug release studies. The goal is to develop a biocompatible liposomal formulation of lansoprazole that improves solubility, stability and bioavailability for treating conditions like ulcers and inflammation.
The prodrug concept was first proposed in 1958 as a way to temporarily modify drugs' physicochemical properties to improve their usefulness and decrease toxicity. Prodrugs are converted to the active drug within the body through enzymatic or non-enzymatic reactions. This allows for improved solubility, delivery, stability, and decreased adverse effects. Ideal prodrugs are inactive or less active than the parent drug, are cleaved in vivo to release the parent drug, and produce non-toxic metabolic fragments. Common prodrug modifications include esterification of carboxylic acids and alcohols as well as derivatization of carbonyl groups. Successful prodrugs have been developed to improve patient acceptance, reduce gastric irritation,
Drug acting on Leprosy, Antileprotic drugs KundanSable1
This document discusses drugs used to treat leprosy (Hansen's disease), which is caused by the bacterium Mycobacterium leprae. It describes several classes of antileprotic drugs, including sulfones like dapsone, phenazine derivatives like clofazimine, and antitubercular drugs like rifampin and ethionamide. For each drug class, it outlines the mechanism of action, pharmacokinetics, adverse effects, and other details. Other antibiotics discussed for treating leprosy include ofloxacin, minocycline, clarithromycin, and moxifloxacin.
The document provides information on prodrugs. It defines a prodrug as a biologically inert derivative of a drug molecule that undergoes conversion in vivo to release the active parent drug. The objectives of prodrug design include improving solubility, stability, absorption, and decreasing toxicity. Examples are given of common prodrugs and how they achieve various objectives like masking taste, reducing irritation, and prolonging duration of action. Prodrug strategies can also be used for targeted drug delivery in chemotherapy through approaches like antibody-directed enzyme prodrug therapy.
This document discusses genetic polymorphisms in enzymes. It provides examples of polymorphisms in alcohol dehydrogenase, aldehyde dehydrogenase, dihydropyrimidine dehydrogenase, glutathione S-transferases, and butyrylcholinesterase. These polymorphisms can result in variations in enzyme activity levels and impact drug metabolism and toxicity. The document also discusses how certain polymorphisms are associated with increased risks of diseases like cancer when combined with environmental exposures like smoking or drinking alcohol.
The document discusses nasal drug delivery systems. It covers the anatomy and physiology of the nose, mechanisms of nasal absorption, factors affecting absorption like molecular weight and pH, strategies to improve absorption like penetration enhancers, and considerations for nasal drug formulations including pH, osmotic agents, and absorption enhancers. The nasal route offers advantages like avoiding first-pass metabolism and rapid drug absorption but faces limitations such as low bioavailability and enzymatic degradation.
The document discusses basic concepts and applications of prodrug design. It defines prodrugs as biologically inert derivatives of drug molecules that undergo enzymatic and/or chemical conversion in vivo to release the pharmacologically active parent drug. The objectives of prodrug design include improving pharmaceutical and pharmacokinetic properties as well as decreasing toxicity. Applications of prodrugs include masking taste/odor, reducing irritation, enhancing solubility/stability, improving bioavailability, preventing presystemic metabolism, prolonging duration of action, reducing toxicity, and enabling site-specific drug delivery such as in chemotherapy through directed enzyme prodrug therapy.
The document discusses various drugs that act on blood and blood forming agents as well as the renal system. It begins by classifying anticoagulants as those used in vitro like heparin and calcium complexing agents, and those used in vivo like heparin, heparinoids, hirudin, and oral anticoagulants. It then describes the mechanisms and pharmacological actions of heparin and oral anticoagulants like warfarin. The document also discusses diuretics, classifying them as high efficacy loop diuretics like furosemide, medium efficacy thiazide diuretics, and weak adjunctive diuretics. It provides details on the mechanisms and
increase membrane permeability by prodrug design.keshob ghosh
This presentation discusses prodrugs and how they can improve membrane permeability and drug absorption. A prodrug is a medication that is metabolized into an active drug after administration. Prodrugs are used to improve patient acceptability, alter absorption and distribution, alter metabolism and elimination, and allow drugs that do not cross biological barriers like the blood brain barrier to do so. The presentation provides examples of prodrugs like oseltamivir and valacyclovir and explains how they work to improve permeability through passive diffusion or carrier-mediated transport by increasing lipophilicity or allowing recognition by transporters.
This document provides an overview of prodrug design. It defines a prodrug as an inactive derivative of a drug molecule that undergoes biotransformation to release the active drug. Prodrugs are classified based on their structure and include carrier-linked, bipartite, tripartite, mutual, and bioprecursor prodrugs. The document discusses various rationales for prodrug design such as improving solubility, absorption, patient acceptability, and site-specific drug delivery. Common functional groups used in prodrugs include esters, amides, phosphates, and carbamates. The document also covers practical considerations and approaches for overcoming limitations like pre-systemic metabolism and blood-brain barrier penetration.
This document provides information on propofol, an intravenous anesthetic. It discusses propofol's history, chemical properties, formulations, pharmacokinetics, mechanisms of action, effects on organ systems, uses, adverse effects, and interactions. Propofol is a widely used anesthetic due to its rapid onset and offset of action. It acts by potentiating GABA receptors in the brain and has numerous clinical applications beyond general anesthesia induction. The document provides detailed information on propofol's properties and clinical use.
Similar to PRODRUG 1[988].pptx [Read-Only].pptx (20)
Polymerase Chain Reaction (PCR) is a technique that amplifies a specific DNA sequence. It involves denaturing DNA, annealing primers to the DNA, and extending the primers to replicate the DNA. Through repeated cycles of heating and cooling, the targeted DNA sequence is exponentially amplified, allowing it to be detected and manipulated. PCR is used to identify infectious organisms like viruses, detect genetic mutations, and replicate DNA for further analysis. Careful primer design is important for PCR to specifically amplify the desired DNA sequence.
test Item Charecterization importance in Toxicology.pptxSourinDe2
Test item characterization and methods are important in regulatory toxicology. Proper characterization of test items involves identification of chemical constituents and impurities that may impact safety assessment. Brief methods for characterizing test items include analytical techniques like chromatography that can provide purity and identity information required for regulatory toxicology studies.
Immunomodulators are drugs that modify the immune system by either suppressing or stimulating it. This document discusses various immunomodulators including immunosuppressants like cyclosporine and tacrolimus which are used to inhibit immune responses in organ transplantation and autoimmune diseases. It also discusses immunostimulants like interferons and interleukins which activate the immune system to fight pathogens and cancer. Several in vitro and in vivo screening methods are described to test new immunomodulators for effects on processes like histamine release, lymphocyte proliferation, and hypersensitivity reactions.
This document provides information about a student named Sourin De in the 5th semester of the 3rd year of study. Sourin is enrolled in Med Chem 2 and has a roll number of 12401918036. The document expresses gratitude at the end.
This document discusses primer design for polymerase chain reaction (PCR). It explains that PCR is used to amplify specific DNA sequences. Well-designed primers are important for PCR to work properly. Some key considerations for primer design include length, melting temperature, GC content, secondary structures, and repeats. Primers should be 18-24 base pairs, have a melting temperature of 52-58°C, about 60% GC content, and avoid hairpins, primer dimers, and long runs of single bases. The document provides an example of using a set of 600 primers designed with a melting temperature of 57°C to detect structural variations in the CDKN2A locus by PAMP design.
The document discusses the physiological and pathological role of opioid autocoids. It defines autocoids as self-healing substances that originate from diffuse tissues and act as neurotransmitters or neuromodulators. It notes that opioids work by binding to opioid receptors in the central nervous system, peripheral nervous system, and gastrointestinal tract. These receptors mediate both the beneficial and side effects of opioids. The document then classifies opioids and describes their mechanisms of action, functions, and pharmacological actions, which include analgesic effects, respiratory depression, sedation, myosis, bradycardia, and decreased blood pressure.
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
Cell Therapy Expansion and Challenges in Autoimmune DiseaseHealth Advances
There is increasing confidence that cell therapies will soon play a role in the treatment of autoimmune disorders, but the extent of this impact remains to be seen. Early readouts on autologous CAR-Ts in lupus are encouraging, but manufacturing and cost limitations are likely to restrict access to highly refractory patients. Allogeneic CAR-Ts have the potential to broaden access to earlier lines of treatment due to their inherent cost benefits, however they will need to demonstrate comparable or improved efficacy to established modalities.
In addition to infrastructure and capacity constraints, CAR-Ts face a very different risk-benefit dynamic in autoimmune compared to oncology, highlighting the need for tolerable therapies with low adverse event risk. CAR-NK and Treg-based therapies are also being developed in certain autoimmune disorders and may demonstrate favorable safety profiles. Several novel non-cell therapies such as bispecific antibodies, nanobodies, and RNAi drugs, may also offer future alternative competitive solutions with variable value propositions.
Widespread adoption of cell therapies will not only require strong efficacy and safety data, but also adapted pricing and access strategies. At oncology-based price points, CAR-Ts are unlikely to achieve broad market access in autoimmune disorders, with eligible patient populations that are potentially orders of magnitude greater than the number of currently addressable cancer patients. Developers have made strides towards reducing cell therapy COGS while improving manufacturing efficiency, but payors will inevitably restrict access until more sustainable pricing is achieved.
Despite these headwinds, industry leaders and investors remain confident that cell therapies are poised to address significant unmet need in patients suffering from autoimmune disorders. However, the extent of this impact on the treatment landscape remains to be seen, as the industry rapidly approaches an inflection point.
Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
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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.
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.
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TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
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TEST BANK For Basic and Clinical Pharmacology, 14th Edition by Bertram G. Katzung, Verified Chapters 1 - 66, Complete Newest Version.
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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.
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2. Prodrugs are inactive compounds which are metabolized
either chemically or enzymatically in a controlled or
predictable manner to the parent active drug inside the
body.
Prodrugs can enhance the therapeutic efficacy and/or
reduce the adverse effect via different mechanisms
including increased solubility, improved permeability and
bioavailability , prolonged half life and tissue target
delivery.
3. The release of active drug only occurs at its site of action ,
thereby:
oReduce toxic side effects due to high plasma concentration
or
oReduce non-specific updates by other body tissues.
Site specific drug delivery is achieved by:
oSite directed drug delivery
oSite directed bioactivation
4. Site directed drug delivery
Anticonvulsant activity of Pragabide
oGABA is too polar to cross BBB.
oLipophilic analog of GABA crosses the BBB and releases
GABA inside the brain .
oThus shows anti convulsant activity
o
PRAGABIDE
GABA
5. Increased lipid solubility may enhance uptake in other
tissue with a resultant increase in toxicity.
These problems may be overcome by utilizing a
dihydropyridine-pyridine-pyridinium salt type redox
system.
The drug [D] which is aimed to be delivered to the brain ,
is coupled to a quaternary carrier QC [ ie. N-methyl
nicotinic acid ].
QC is reduced to neutral, lipophilic dihydro form [D-DHC]
D + QC D-QC reduced to D-DHC[prodrug]
D-DHC oxidation D-QC hydrolysis QC + D
6. After administration , this compound is distributed
throughout the body including the brain.
D-DHC is then enzymatically oxidized back to the original
D-QC .
The ionic form is trapped in the brain and undergo slow
enzymatic cleavage releasing the active agent.
Only small amount of free drug is released in the blood.
Eg : dopamine , phenytoin , penicillin
7. Beta-lactam antibiotics are used in the treatment of
bacterial meningitis.
oThey are hydrophilic , enter the brain very slowly.
oDihydropyridine-penicillin prodrug deliver beta-lactam
antibiotics in higher concentration into the brain.
8. Site specific bio-activation
Designing a prodrug that require activation by an enzyme
found predominantly at the desired site.
Eg : acyclovir , antiviral agent
o Acyclovir thymidine kinase acyclovir monophosphate
oAcyclovir monophosphate cellular kinase Acyclovir di
and
triphosphate
oTriester formation takes place much greater extend in herpes
–infected cells, than uninfected cells.
10. pH dependent bio-activation
Omeprazole : antiulcer drug
Omeprazole prodrug is converted to their active
sulphonamide in the acidic condition of parietal cell.
H+
OMEPRAZOLE
[inactive]
sulfonamide intermediate
[active]
Disulphide complex
11. It can be achieved by making a long chain aliphatic ester
because these ester hydrolysis slowly.
Fluphenazine antipsychotic drug
oFluphenazine has shorter duration of action[6-8 hrs]
oFluphenazine enanthate and decanoate [prodrug] has
duration of action about a month.
13. Vasopressin used for the treatment of bleeding
varicose veins in the lower end of the esophagus .
oVasoconstrictor action of drug stops bleeding .
oBut short duration of action
oIncreasing dose leads to toxic side effect
oGlypressin [gly-gly-gly-lys-vacopressin] prodrug of
vasopressin
oMinimize possibility of unwanted side effects caused by
high blood pressure
14. The rationale for prodrug design is to achieve favourable
physicochemical characteristics [ chemical stability,
solubility, taste or odor ], biopharmaceutical properties
[oral absorption, first-pass metabolism, permeability
across biological membranes such as blood brain barrier ,
reduced toxicity] or pharmacodynamic properties [ reduced
pain or irritation].
15. Improving formulation and administration.
Enhancing permeability and absorption.
Changing the distribution profile.
Protecting from rapid metabolism and excretion.
Overcoming toxicity problems.
Managing life cycle.
16. Dissolution rate limiting step of absorption.
Prodrugs are an alternative way to increase the aqueous
solubility of parent drug molecule by improving
dissolution rate via attached ionizable or polar neutral
groups such as phosphates, amino acids, or sugar moiety.
Phosphate esters are widely used to increase the aqueous
solubility of orally and parenterally administered drug.
17. Prednisolone sodium phosphate is an example of phosphate
prodrug.
oIt is highly water soluble [ 30 times greater than prednisolone]
oThe phosphate prodrug moiety is linked directly to a free
hydroxyl group on prednisolone.
oThe orally administered prodrug rapidly hydrolyzed by gut
epithelial alkaline phosphatases to their respective parent drug.
Phosphatase
Prednisolone sodium
phosphate[prodrug]
Prednisolone
18. Amino acid esters or amides are also commonly used
ionizable groups which can be introduced into the hydroxyl,
thiol, amine or carboxylic acid functionalities of parent
drugs.
A variety of esterases , amidases, peptidases can bioconvert
their prodrug into active counterparts.
Sugar moiety glucose , galactose, or glucuronic acid
Enzymes glucosidases, galactosidases, or glucuronidase
19. A hydrophilic hydroxyl, thiol, carboxyl, phosphate or
amine group on parent drug can be converted to more
lipophilic alkyl or aryl esters .
oThese prodrugs are readily converted to their active
species by ubiquitous esterase.
Oseltamivir is an orally active ethyl ester prodrug .
oSelective inhibitor of viral neuraminidase glycoprotein .
oUsed in the treatment of influenza type A and type B .
20. oAfter absorption , oseltamivir undergoes rapid bioconversion to
its parent drug mostly by the action of carboxylesterase.
oBioavailability of oseltamivir is 80%comparing to free
carboxylate which is 5%.
Oseltamivir [prodrug]
Carboxylesterase
21. Tazarotene is an example of marketed ethyl ester prodrug
with enhanced transdermal drug delivery.
oTazarotene is used for psoriasis and acne treatment and
causes less skin irritation than the parent drug
tazarotenic acid .
Dipivefrin improve ocular absorption .
oDipivefrin is dipivalyl diester of epinephrine.
oDipivefrin penetrates the human cornea 17 times more
rapidly than epinephrine.
oLower the intraocular pressure.
22. A great many prodrug have increased efficacy and safety
profile because of their targeting properties.
Anti-Parkinson agent L-DOPA .
oDopamine[hydrophilic] not able to cross BBB .
oAmino acid prodrug of dopamine , L-DOPA enable the
uptake and accumulation in the brain.
23. Dopa
decarboxylase
Levodopa [prodrug] Dopamine
o L type amino transporter 1 for the uptake of L DOPA
o After uptake LDOPA is bioactivated by aromatic L amino
acid decarboxylase to hydrophilic dopamine.
24. Rapid metabolic break down of the drug can be protected
by prodrug.
This is carried out by masking the metabolically labile but
pharmacologically essential functional groups of the drug.
Terbutaline is a bronchodilator and beta 2 agonist, used
in the treatment of asthma.
oTerbutaline undergo rapid pre systemic metabolism.
oIt is prevented by converting its phenol group to bis
dimethyl carbamate [bambuterol]
25. Bambuterol [prodrug] is slowly bioactivated to Terbutaline
predominantly by non specific butyrylcholine esterase
outside the lungs.
As a result of slower release and prolonged action , once
daily administration of bambuterol provides relief of
asthma.
butyrylcholinesterase
Bambuterol [prodrug] Terbutaline
26. Kidneys are the principle organ of excretion.
It efficiently eliminate water soluble substance from the
body.
Therefore use of lipophilic promoieties to decrease the
solubility is one way to prolong the duration of action of
very water soluble drug.
27. Reduced toxicity can be achieved by targeting drug to
desired cells and tissues via site selective drug delivery .
Therefore antibody directed enzyme prodrug therapy and
gene-directed enzyme prodrug therapy and virus directed
enzyme prodrug therapy are widely used , especially with
high toxic compounds.
28. Prodrug can offer a valuable opportunity to improve the life
cycle management of parent drug.
Fosamprenavir is water soluble prodrug.
oThis phosphate ester of the HIV protease inhibitor amprenavir
was originally designed to improve solubility and oral
bioavailability.
oAt the same time, this prodrug will continue the life cycle of
amprenavir.
oBecause the fosamprenavir patent will last until 2017, whereas
patent on amprenavir will expire on 2013
29. Prodrug research encounter various challenges.
Many enzymes involved in the prodrug activation are
subjected to interindividual variabilities in their activities.
Intrinsic factor : polymorphism in the gene coding the
enzymes.
Extrinsic factor :interaction caused by other drugs or
xenobiotics.
Both these factors may cause insufficient or excessive
conversion of prodrug into their active form.
30. Esterase catalyzed hydrolysis of prodrug
The majority of carboxylesterases are found in 2 isozyme
families : CES1 and CES2.
In human CES1 is highly expressed in the liver .
CES2 is highly expressed throughout the intestine and
kidney.
The difference in both localization of CES1 and CES2 I
humans and their substrate specificities can take into
account in prodrug design.
CES1 prefer the hydrolysis of esters with large acyl and
small alcohol groups.
31. CES2 hydrolyses esters of smaller acyl and larger alcohol
groups.
CES1 can hydrolysis , Temocapril [small alcohol group and
large acyl group] with higher efficiency than CES2.
Temocapril [prodrug]
CES1
Temocaprilat
32. Prodrug bioactivation by cytochrome P450
enzymes
The P450 enzymes are super family enzymes accounting
for up to 75% of all metabolism of drugs, including
prodrugs.
Genetic polymorphism of prodrug activating P450s
contribute substantially to the variability in prodrug
activation .
Thus affect the efficacy and safety of drugs using this
bioactivation pathway.
Several drug-metabolizing P450 genes are known to be
polymorphic including CYP2A4, CYP2B6 etc…
33. In particular , the CYP2D6 gene is highly polymorphic
with 75 different major alleles currently known.
Some of these alleles are associated with reduced enzyme
activity or even the absence of enzyme function.
Anti cancer drugs [cyclophosphamide, ifosfamide and
trofosfamide] are prodrugs .
oBioconversion of these cyclic phosphate drugs to the
corresponding cytotoxic species is initiated by P450
enzymes.
34.
35. AIM : targeting hypoxia condition of solid tumor by
hypoxia activated prodrug [HAP]
INTRODUCTION
Hypoxia is an important characteristics of solid
malignancies.
Hypoxia is closely related to tumor prognosis and
therapeutic resistance.
HAP
Hypoxia activated prodrug are bioreductive prodrug that
are activated in the hypoxia condition .
It is a site specific drug delivery targeting the hypoxia
region of solid tumor.
This will reduce toxicity to normal tissues.
36. Tirapazamine
1st activated prodrug reported in 1986.
In hypoxic condition , Tirapazamine undergo 1 electron
reduction by the enzyme CYP450 and form free radicals
37. Chromosomal aberration and DNA double strand break
Preclinical and clinical effect
As of 2006, Tirapazamine is undergoing phase 3 clinical
trial .
In preclinical studies , Tirapazamine effectively inhibited
tumor in hypoxia cells.
But Tirapazamine has only limited effect on clinical trial ,
The affinity of Tirapazamine for hypoxia tissue is much
lower in vivo compared to in vitro.
Clinical trial also report significant toxicity like
ototoxicity, muscle cramping , nausea, vomiting etc…
38. Prodrug from serendipity to rational design : Kristiina M.
Huttunen, Hannu Raunio and Jarkko Rautio
:pharmacological review :63:750-771, 2011
Drug design : Dr. V.M Kulkarni and Dr. K.G. Bothara
K ,.Ilango vol 1 : text book of medicinal chemistry