1. The document discusses drug receptor interaction theories including occupation theory, rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state receptor model.
2. It classifies ligands that bind to receptors as full agonists, partial agonists, or antagonists and describes different types of agonists and antagonists.
3. The key forces involved in drug-receptor binding are described as well as interactions that stabilize drug-receptor complexes such as ionic interactions, hydrogen bonding, and hydrophobic interactions.
The document discusses drug distribution and protein binding in the body. It notes that drugs can bind intracellularly to primary receptors for therapeutic effects, or extracellularly to silent receptors with no pharmacological action. Drugs are generally reversibly bound, though some irreversible covalent bonding can occur. Drug distribution occurs via plasma proteins, blood cells, and binding to tissues like the liver, kidneys, lungs and bones. Albumin is the most important plasma protein for binding drugs. Factors that influence protein binding include drug properties, protein concentrations, and drug interactions that can cause competition or allosteric changes. Tissue binding influences apparent volume of distribution compared to real volume related to body water content.
This document discusses immunopharmacology and the immune system. It describes how immunopharmacology studies how drugs modify immune mechanisms in the body, including autoimmune disorders, allergies, and cancer. The immune system involves cells like lymphocytes, neutrophils, and monocytes. Antigens stimulate antibody production while antibodies help fight antigens. Immunopharmacology therapies aim to suppress, modulate, or enhance the immune system through immunosuppressants, immunomodulators, or immunoenhancers respectively.
This document discusses different types of drug interactions, including pharmacokinetic, pharmacodynamic, and pharmaceutical interactions. Pharmacokinetic interactions involve effects on the absorption, distribution, metabolism and excretion of drugs. Pharmacodynamic interactions involve effects of drugs on receptors and include agonism, antagonism, addition, synergism and potentiation. Pharmaceutical interactions refer to incompatible drugs that cannot be administered together intravenously. Drug interactions can increase the risk of adverse drug reactions and should be considered when multiple drugs are prescribed.
Drug-plasma protein binding plays a key role in drug pharmacokinetics and pharmacodynamics. Proteins, particularly albumin and alpha-1-acid glycoprotein, bind drugs reversibly through mechanisms like hydrogen bonding, hydrophobic interactions, and van der Waals forces. Only the unbound fraction of a drug is active, as protein-bound drug is inert and cannot cross membranes or exert effects. Several factors influence protein binding, including drug properties, protein concentrations, and disease states. The degree of protein binding impacts drug absorption, distribution, metabolism, and elimination.
Protein binding of drugs can significantly impact a drug's pharmacokinetic and pharmacodynamic properties. There are two main classes of protein binding - binding to blood components like plasma proteins and blood cells, and binding to extravascular tissue proteins in organs like the liver, kidneys, lungs, and muscles. The extent of protein binding is influenced by factors related to the drug, such as its lipophilicity and concentration, factors related to the binding protein, such as its concentration and number of binding sites, and patient-related factors like age and disease state. Protein binding impacts a drug's absorption, distribution, metabolism, elimination, and ability to reach its receptor site and produce an effect. It can inactivate drugs by sequestering
This document discusses combinatorial chemistry, which is a technique used to rapidly generate large libraries of compounds for screening and drug discovery. It defines combinatorial chemistry as producing large numbers of similar molecules using the same reaction conditions. The key principles are that it allows preparation of thousands of compounds per month using parallel synthesis techniques like solid and solution phase chemistry. This increases the chances of identifying hit compounds for pharmaceutical development compared to traditional synthetic methods. Applications of combinatorial chemistry include drug discovery, agrochemical and biotechnology research by creating molecular diversity libraries for high-throughput screening.
Chronopharmacology is the branch of science which deals with the pharmacological action of a drug in relation to biological rhythm.
(Chronos: time; Pharmacon: drug; Logos: study)
It is concerned with the effects of drugs upon the timing of biological events and rhythms.
It is important to enhance the therapeutic efficacy, optimization of drug effects, minimization of adverse effects by using timing medications in relation to biological rhythm.
History:
Jean-Jaques d’Ortous de Mairan: Described circardian rhythm in plants in the 18th century.
Franz Halberg : coined the term ‘Circardian’ in 20th century (about 24 hr or about a day)
Franz Halberg : Founder of Chronobiology.
Biological Rhythm:
Biological rhythm: It is the determined rhythmic biological process or function within a defined time period.
TYPES OF RHYTHM
Circadian (last for 24 hr) – Sleep wake cycle
Infradian (> 24 hr) – Menstrual cycle
Ultradian (< 24 hr) – Neuronal firing time
Biological Clock:
An internal biological clock located in mammals, in the suprachiasmatic nucleus of the hypothalamus (SCN), delivering its message of time throughout the body.
It is responsible for circadian rhythms and annual/seasonal rhythm.
The SCN uses its connections with the autonomic nervous system for spreading its time-of-day message, either by setting the sensitivity of endocrine glands (thyroid, adrenal, ovary) or by directly controlling an endocrine output of pineal gland (i.e. melatonin synthesis)
Application:
Chronotherapy found useful in
Asthma therapy, Strokes, Sleep disorders, GI tract disorders, Allergies, Oncology etc
Recent Advances:
Casein Kinase 1 (CK-1) inhibitor: Potential new drug
Reset the circadian clock enzymes.
Uses: Jet lag, sleep disorder, bipolar disorder
Animal trials completed.
Clinical trials are awaited.
1. The document discusses drug receptor interaction theories including occupation theory, rate theory, induced fit theory, macromolecular perturbation theory, activation-aggregation theory, and two-state receptor model.
2. It classifies ligands that bind to receptors as full agonists, partial agonists, or antagonists and describes different types of agonists and antagonists.
3. The key forces involved in drug-receptor binding are described as well as interactions that stabilize drug-receptor complexes such as ionic interactions, hydrogen bonding, and hydrophobic interactions.
The document discusses drug distribution and protein binding in the body. It notes that drugs can bind intracellularly to primary receptors for therapeutic effects, or extracellularly to silent receptors with no pharmacological action. Drugs are generally reversibly bound, though some irreversible covalent bonding can occur. Drug distribution occurs via plasma proteins, blood cells, and binding to tissues like the liver, kidneys, lungs and bones. Albumin is the most important plasma protein for binding drugs. Factors that influence protein binding include drug properties, protein concentrations, and drug interactions that can cause competition or allosteric changes. Tissue binding influences apparent volume of distribution compared to real volume related to body water content.
This document discusses immunopharmacology and the immune system. It describes how immunopharmacology studies how drugs modify immune mechanisms in the body, including autoimmune disorders, allergies, and cancer. The immune system involves cells like lymphocytes, neutrophils, and monocytes. Antigens stimulate antibody production while antibodies help fight antigens. Immunopharmacology therapies aim to suppress, modulate, or enhance the immune system through immunosuppressants, immunomodulators, or immunoenhancers respectively.
This document discusses different types of drug interactions, including pharmacokinetic, pharmacodynamic, and pharmaceutical interactions. Pharmacokinetic interactions involve effects on the absorption, distribution, metabolism and excretion of drugs. Pharmacodynamic interactions involve effects of drugs on receptors and include agonism, antagonism, addition, synergism and potentiation. Pharmaceutical interactions refer to incompatible drugs that cannot be administered together intravenously. Drug interactions can increase the risk of adverse drug reactions and should be considered when multiple drugs are prescribed.
Drug-plasma protein binding plays a key role in drug pharmacokinetics and pharmacodynamics. Proteins, particularly albumin and alpha-1-acid glycoprotein, bind drugs reversibly through mechanisms like hydrogen bonding, hydrophobic interactions, and van der Waals forces. Only the unbound fraction of a drug is active, as protein-bound drug is inert and cannot cross membranes or exert effects. Several factors influence protein binding, including drug properties, protein concentrations, and disease states. The degree of protein binding impacts drug absorption, distribution, metabolism, and elimination.
Protein binding of drugs can significantly impact a drug's pharmacokinetic and pharmacodynamic properties. There are two main classes of protein binding - binding to blood components like plasma proteins and blood cells, and binding to extravascular tissue proteins in organs like the liver, kidneys, lungs, and muscles. The extent of protein binding is influenced by factors related to the drug, such as its lipophilicity and concentration, factors related to the binding protein, such as its concentration and number of binding sites, and patient-related factors like age and disease state. Protein binding impacts a drug's absorption, distribution, metabolism, elimination, and ability to reach its receptor site and produce an effect. It can inactivate drugs by sequestering
This document discusses combinatorial chemistry, which is a technique used to rapidly generate large libraries of compounds for screening and drug discovery. It defines combinatorial chemistry as producing large numbers of similar molecules using the same reaction conditions. The key principles are that it allows preparation of thousands of compounds per month using parallel synthesis techniques like solid and solution phase chemistry. This increases the chances of identifying hit compounds for pharmaceutical development compared to traditional synthetic methods. Applications of combinatorial chemistry include drug discovery, agrochemical and biotechnology research by creating molecular diversity libraries for high-throughput screening.
Chronopharmacology is the branch of science which deals with the pharmacological action of a drug in relation to biological rhythm.
(Chronos: time; Pharmacon: drug; Logos: study)
It is concerned with the effects of drugs upon the timing of biological events and rhythms.
It is important to enhance the therapeutic efficacy, optimization of drug effects, minimization of adverse effects by using timing medications in relation to biological rhythm.
History:
Jean-Jaques d’Ortous de Mairan: Described circardian rhythm in plants in the 18th century.
Franz Halberg : coined the term ‘Circardian’ in 20th century (about 24 hr or about a day)
Franz Halberg : Founder of Chronobiology.
Biological Rhythm:
Biological rhythm: It is the determined rhythmic biological process or function within a defined time period.
TYPES OF RHYTHM
Circadian (last for 24 hr) – Sleep wake cycle
Infradian (> 24 hr) – Menstrual cycle
Ultradian (< 24 hr) – Neuronal firing time
Biological Clock:
An internal biological clock located in mammals, in the suprachiasmatic nucleus of the hypothalamus (SCN), delivering its message of time throughout the body.
It is responsible for circadian rhythms and annual/seasonal rhythm.
The SCN uses its connections with the autonomic nervous system for spreading its time-of-day message, either by setting the sensitivity of endocrine glands (thyroid, adrenal, ovary) or by directly controlling an endocrine output of pineal gland (i.e. melatonin synthesis)
Application:
Chronotherapy found useful in
Asthma therapy, Strokes, Sleep disorders, GI tract disorders, Allergies, Oncology etc
Recent Advances:
Casein Kinase 1 (CK-1) inhibitor: Potential new drug
Reset the circadian clock enzymes.
Uses: Jet lag, sleep disorder, bipolar disorder
Animal trials completed.
Clinical trials are awaited.
Expt 10 Effects of skeletal muscle relaxants using rota-rod apparatusMirza Anwar Baig
This document presents a study on the effects of the skeletal muscle relaxant diazepam using a rota-rod apparatus. Mice were given injections of diazepam and their ability to remain on a rotating rod was measured and compared to untreated mice. Treatment with diazepam significantly decreased the time mice could spend on the rotating rod, indicating that diazepam has muscle relaxing properties. The study aims to evaluate diazepam's muscle relaxation effects using a non-invasive method that observes the loss of muscle grip in animals.
The document discusses various classes of sedative and hypnotic drugs including barbiturates, benzodiazepines, and newer non-benzodiazepine drugs. It describes the mechanism of action of these drugs as potentiating the effects of the inhibitory neurotransmitter GABA in the brain through binding to GABAA receptors or barbiturate sites. This results in increased chloride conductance, membrane hyperpolarization, and central nervous system depression. The document also provides structure-activity relationships and examples of specific drugs from each class like diazepam, zolpidem, and pentobarbital along with their medical uses, side effects, and synthesis when relevant.
This document discusses the classification, structure-activity relationships, and mechanisms of action of sympathomimetic and adrenergic drugs. It categorizes these drugs based on their chemical nature, mode of action, receptor selectivity, and therapeutic effects. Key points include:
1) Sympathomimetics are classified as catecholamines which contain a catechol nucleus, or non-catecholamines which do not.
2) They can act directly on receptors, indirectly by releasing norepinephrine, or by both mechanisms.
3) Drugs show selectivity for alpha-1, alpha-2, beta-1, or beta-2 adrenergic receptors.
4) Ther
Enhancement of dissolution rate and bioavailability of poorly soluble drugsNagaraju Ravouru
This document discusses methods to enhance the dissolution rates and bioavailability of poorly soluble drugs. It begins by noting that about 95% of new drug candidates have poor solubility and bioavailability. It then discusses the Biopharmaceutical Classification System and how Class II drugs in particular need enhanced dissolution for increased bioabsorption. Several methods to enhance dissolution are covered, including increasing drug solubility through various approaches, and increasing surface area through micronization and solid dispersions. Specific technologies like cyclodextrin complexes and nanonization are also summarized. The conclusion reiterates the importance of ongoing research to develop delivery technologies to improve insoluble drugs.
This document discusses several anti-viral drugs including acyclovir, valacyclovir, ribavirin, and tromantadine HCL. It describes the mechanisms of viruses and how each drug works to inhibit viral replication. Acyclovir is a nucleoside analogue that is phosphorylated inside cells and inhibits viral DNA polymerase. Valacyclovir is a prodrug of acyclovir that is absorbed more efficiently. Ribavirin has a broad antiviral spectrum and works by inhibiting viral RNA and mRNA synthesis. Tromantadine inhibits early and late events in the herpes virus lifecycle including penetration and uncoating.
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.
Absorption of drugs from non per os extravascular administrationSuvarta Maru
Non-oral routes of drug administration provide advantages over oral routes by bypassing the gastrointestinal tract and avoiding first-pass metabolism. Common non-oral routes discussed include buccal/sublingual, rectal, topical, intramuscular, subcutaneous, pulmonary, intranasal, intraocular, and vaginal administration. Absorption through these routes occurs primarily via passive diffusion, carrier-mediated transport, or pore transport depending on the drug properties and administration site. Non-oral routes allow for rapid drug absorption, higher bioavailability compared to oral routes, and targeted delivery for local or systemic effects.
Phase I Vs Phase II Drug metabolism and factors affectiing drug metabolism.
Enzyme induction, Enzyme inhibitor, physicochemical properties wthich acan affect the drug metabolism
Quinolones are synthetic antibacterial agents derived from nalidixic acid. Modern fluoroquinolones are classified into generations based on potency and spectrum of activity, with later generations having broader coverage. They work by inhibiting bacterial DNA gyrase and topoisomerase IV, preventing DNA replication. Common quinolones include norfloxacin for urinary tract infections, ciprofloxacin with activity against Pseudomonas, and sparfloxacin active against streptococci and anaerobes.
The document discusses pro-drugs, which are inactive precursors designed to improve the delivery of active drug molecules. It describes how pro-drugs can be used to mask tastes/odors, modify formulations, enhance solubility, reduce side effects like GI irritation, and target drug delivery. Pro-drugs are metabolized in the body to release the active drug. Types include carrier-linked prodrugs, bioprecursor prodrugs, and mutual prodrugs, which release two active drugs. Applications include taste masking, solubility enhancement, and site-specific delivery to improve drug therapies.
Prodrugs are inactive compounds that are converted into active drugs inside the body. They are designed to overcome issues like acid sensitivity, poor membrane permeability, toxicity, bad taste, and short duration of action. When designing prodrugs, it is important to ensure they are effectively converted into the active drug and that any cleaved groups are non-toxic. Some examples of prodrugs include esters which improve membrane permeability, levodopa which is a prodrug for dopamine, and diazepam which prolongs the activity of nordazepam. Prodrugs can also mask drug toxicity, provide slow release of toxic drugs, and alter solubility.
This document discusses drug interactions at plasma and tissue binding sites. It describes the mechanisms of protein drug binding, including reversible and irreversible binding via hydrogen bonds, hydrophobic bonds, ionic bonds, and Vander Waal's forces. It explains how drugs can bind to blood components like plasma proteins, albumin, alpha-1-acid glycoprotein, lipoproteins, globulins, and blood cells. It also discusses how drugs can bind to extravascular tissues in organs like the liver, kidneys, lungs, and muscles. The significance of protein and tissue binding on drug absorption, distribution, elimination, therapy and drug targeting is explained.
This document summarizes 5 major categories of transducer mechanisms:
1) G-protein coupled receptors which activate downstream effectors like adenylyl cyclase or phospholipase C.
2) Ion channel receptors which directly open or close ion channels.
3) Transmembrane enzyme-linked receptors which activate intracellular protein kinases.
4) Transmembrane JAK-STAT binding receptors which activate the JAK/STAT signaling pathway.
5) Receptors regulating gene expression which bind intracellularly to directly regulate gene transcription.
This document discusses factors that affect drug distribution in the body. It begins by explaining how drugs diffuse from capillaries into interstitial spaces. It then discusses various physiological barriers drugs must cross, including the capillary endothelial barrier, cell membrane barrier, blood-brain barrier, blood-CSF barrier, and blood-placental barrier. The document outlines several factors that influence drug distribution, such as a drug's physicochemical properties, tissue permeability, organ perfusion rates, binding to tissue components, and patient-specific factors like age, pregnancy, and disease states. It also covers concepts of volume of distribution and drug-protein binding interactions.
The document discusses protein-drug binding, including the two main classes of binding: intracellular and extracellular. It describes the reversible mechanisms of binding such as hydrogen bonds and hydrophobic bonds. Key factors that affect protein-drug binding are the physicochemical properties of the drug and protein, their concentrations, and the number of binding sites. The significance of protein binding is that the bound fraction of a drug is pharmacologically inactive.
The document discusses principles and types of bioassay. It begins by defining a bioassay as a comparative assessment of the potency of a test compound to a standard compound on living tissue. It then outlines the principles of bioassays, including using a standard and test sample with the same mechanism of action and comparing them using a reproducible pharmacological technique. The document categorizes bioassays as either graded, involving measuring a biological response on a scale, or quantal, involving measuring an endpoint response. It provides details on specific graded bioassay methods and discusses quantal bioassays, LD50 determination, and bioassays of antagonists.
This document provides information on renal excretion of drugs. It discusses how the kidney is the primary route of elimination for water soluble, non-volatile and small molecule drugs. The basic functional unit of the kidney is the nephron, which filters drugs from the blood and reabsorbs or secretes them via processes like glomerular filtration, tubular secretion and reabsorption. Factors that influence renal excretion include the physicochemical properties of drugs as well as physiological and pathological factors. Renal impairment decreases drug clearance leading to prolonged drug exposure. Methods to assess renal function and adjust drug dosing based on renal function are also described.
The document discusses various Phase II biotransformation reactions. It describes conjugation reactions like conjugation with glucuronic acid, sulphate moieties, alpha amino acids, and glutathione. Conjugation with glucuronic acid is the most common reaction where glucuronic acid is attached to form glucuronides. Conjugation with sulphate occurs less frequently. Amino acid conjugation forms amide bonds between carboxylic acids and amino acids like glycine. These conjugation reactions make compounds more polar and water soluble for excretion.
This document discusses preformulation studies, which are important steps in developing an effective dosage form for a new drug. The objectives of preformulation studies are to establish the physico-chemical properties of the drug substance and generate information to design an optimal drug delivery system. Key aspects investigated include solubility, stability, compatibility with excipients, and parameters like particle size, bulk density and flow properties. Thorough preformulation work provides a foundation for formulation development and identifies potential problems to address.
Introduction:
History & Development:
Physicochemical Properties in relation to biological action:
Ionization
Solubility
Partition Coefficient
Hydrogen Bonding:
Protein Binding:
Chelation:
Bioisosterism:
Optical & Geomentrical Isomerism
Drug Metabolism:
Drug Metabolism Principles: Phase I & Phase II
Factors Affecting Drug Metabolism including steriochemical Aspects
Expt 10 Effects of skeletal muscle relaxants using rota-rod apparatusMirza Anwar Baig
This document presents a study on the effects of the skeletal muscle relaxant diazepam using a rota-rod apparatus. Mice were given injections of diazepam and their ability to remain on a rotating rod was measured and compared to untreated mice. Treatment with diazepam significantly decreased the time mice could spend on the rotating rod, indicating that diazepam has muscle relaxing properties. The study aims to evaluate diazepam's muscle relaxation effects using a non-invasive method that observes the loss of muscle grip in animals.
The document discusses various classes of sedative and hypnotic drugs including barbiturates, benzodiazepines, and newer non-benzodiazepine drugs. It describes the mechanism of action of these drugs as potentiating the effects of the inhibitory neurotransmitter GABA in the brain through binding to GABAA receptors or barbiturate sites. This results in increased chloride conductance, membrane hyperpolarization, and central nervous system depression. The document also provides structure-activity relationships and examples of specific drugs from each class like diazepam, zolpidem, and pentobarbital along with their medical uses, side effects, and synthesis when relevant.
This document discusses the classification, structure-activity relationships, and mechanisms of action of sympathomimetic and adrenergic drugs. It categorizes these drugs based on their chemical nature, mode of action, receptor selectivity, and therapeutic effects. Key points include:
1) Sympathomimetics are classified as catecholamines which contain a catechol nucleus, or non-catecholamines which do not.
2) They can act directly on receptors, indirectly by releasing norepinephrine, or by both mechanisms.
3) Drugs show selectivity for alpha-1, alpha-2, beta-1, or beta-2 adrenergic receptors.
4) Ther
Enhancement of dissolution rate and bioavailability of poorly soluble drugsNagaraju Ravouru
This document discusses methods to enhance the dissolution rates and bioavailability of poorly soluble drugs. It begins by noting that about 95% of new drug candidates have poor solubility and bioavailability. It then discusses the Biopharmaceutical Classification System and how Class II drugs in particular need enhanced dissolution for increased bioabsorption. Several methods to enhance dissolution are covered, including increasing drug solubility through various approaches, and increasing surface area through micronization and solid dispersions. Specific technologies like cyclodextrin complexes and nanonization are also summarized. The conclusion reiterates the importance of ongoing research to develop delivery technologies to improve insoluble drugs.
This document discusses several anti-viral drugs including acyclovir, valacyclovir, ribavirin, and tromantadine HCL. It describes the mechanisms of viruses and how each drug works to inhibit viral replication. Acyclovir is a nucleoside analogue that is phosphorylated inside cells and inhibits viral DNA polymerase. Valacyclovir is a prodrug of acyclovir that is absorbed more efficiently. Ribavirin has a broad antiviral spectrum and works by inhibiting viral RNA and mRNA synthesis. Tromantadine inhibits early and late events in the herpes virus lifecycle including penetration and uncoating.
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.
Absorption of drugs from non per os extravascular administrationSuvarta Maru
Non-oral routes of drug administration provide advantages over oral routes by bypassing the gastrointestinal tract and avoiding first-pass metabolism. Common non-oral routes discussed include buccal/sublingual, rectal, topical, intramuscular, subcutaneous, pulmonary, intranasal, intraocular, and vaginal administration. Absorption through these routes occurs primarily via passive diffusion, carrier-mediated transport, or pore transport depending on the drug properties and administration site. Non-oral routes allow for rapid drug absorption, higher bioavailability compared to oral routes, and targeted delivery for local or systemic effects.
Phase I Vs Phase II Drug metabolism and factors affectiing drug metabolism.
Enzyme induction, Enzyme inhibitor, physicochemical properties wthich acan affect the drug metabolism
Quinolones are synthetic antibacterial agents derived from nalidixic acid. Modern fluoroquinolones are classified into generations based on potency and spectrum of activity, with later generations having broader coverage. They work by inhibiting bacterial DNA gyrase and topoisomerase IV, preventing DNA replication. Common quinolones include norfloxacin for urinary tract infections, ciprofloxacin with activity against Pseudomonas, and sparfloxacin active against streptococci and anaerobes.
The document discusses pro-drugs, which are inactive precursors designed to improve the delivery of active drug molecules. It describes how pro-drugs can be used to mask tastes/odors, modify formulations, enhance solubility, reduce side effects like GI irritation, and target drug delivery. Pro-drugs are metabolized in the body to release the active drug. Types include carrier-linked prodrugs, bioprecursor prodrugs, and mutual prodrugs, which release two active drugs. Applications include taste masking, solubility enhancement, and site-specific delivery to improve drug therapies.
Prodrugs are inactive compounds that are converted into active drugs inside the body. They are designed to overcome issues like acid sensitivity, poor membrane permeability, toxicity, bad taste, and short duration of action. When designing prodrugs, it is important to ensure they are effectively converted into the active drug and that any cleaved groups are non-toxic. Some examples of prodrugs include esters which improve membrane permeability, levodopa which is a prodrug for dopamine, and diazepam which prolongs the activity of nordazepam. Prodrugs can also mask drug toxicity, provide slow release of toxic drugs, and alter solubility.
This document discusses drug interactions at plasma and tissue binding sites. It describes the mechanisms of protein drug binding, including reversible and irreversible binding via hydrogen bonds, hydrophobic bonds, ionic bonds, and Vander Waal's forces. It explains how drugs can bind to blood components like plasma proteins, albumin, alpha-1-acid glycoprotein, lipoproteins, globulins, and blood cells. It also discusses how drugs can bind to extravascular tissues in organs like the liver, kidneys, lungs, and muscles. The significance of protein and tissue binding on drug absorption, distribution, elimination, therapy and drug targeting is explained.
This document summarizes 5 major categories of transducer mechanisms:
1) G-protein coupled receptors which activate downstream effectors like adenylyl cyclase or phospholipase C.
2) Ion channel receptors which directly open or close ion channels.
3) Transmembrane enzyme-linked receptors which activate intracellular protein kinases.
4) Transmembrane JAK-STAT binding receptors which activate the JAK/STAT signaling pathway.
5) Receptors regulating gene expression which bind intracellularly to directly regulate gene transcription.
This document discusses factors that affect drug distribution in the body. It begins by explaining how drugs diffuse from capillaries into interstitial spaces. It then discusses various physiological barriers drugs must cross, including the capillary endothelial barrier, cell membrane barrier, blood-brain barrier, blood-CSF barrier, and blood-placental barrier. The document outlines several factors that influence drug distribution, such as a drug's physicochemical properties, tissue permeability, organ perfusion rates, binding to tissue components, and patient-specific factors like age, pregnancy, and disease states. It also covers concepts of volume of distribution and drug-protein binding interactions.
The document discusses protein-drug binding, including the two main classes of binding: intracellular and extracellular. It describes the reversible mechanisms of binding such as hydrogen bonds and hydrophobic bonds. Key factors that affect protein-drug binding are the physicochemical properties of the drug and protein, their concentrations, and the number of binding sites. The significance of protein binding is that the bound fraction of a drug is pharmacologically inactive.
The document discusses principles and types of bioassay. It begins by defining a bioassay as a comparative assessment of the potency of a test compound to a standard compound on living tissue. It then outlines the principles of bioassays, including using a standard and test sample with the same mechanism of action and comparing them using a reproducible pharmacological technique. The document categorizes bioassays as either graded, involving measuring a biological response on a scale, or quantal, involving measuring an endpoint response. It provides details on specific graded bioassay methods and discusses quantal bioassays, LD50 determination, and bioassays of antagonists.
This document provides information on renal excretion of drugs. It discusses how the kidney is the primary route of elimination for water soluble, non-volatile and small molecule drugs. The basic functional unit of the kidney is the nephron, which filters drugs from the blood and reabsorbs or secretes them via processes like glomerular filtration, tubular secretion and reabsorption. Factors that influence renal excretion include the physicochemical properties of drugs as well as physiological and pathological factors. Renal impairment decreases drug clearance leading to prolonged drug exposure. Methods to assess renal function and adjust drug dosing based on renal function are also described.
The document discusses various Phase II biotransformation reactions. It describes conjugation reactions like conjugation with glucuronic acid, sulphate moieties, alpha amino acids, and glutathione. Conjugation with glucuronic acid is the most common reaction where glucuronic acid is attached to form glucuronides. Conjugation with sulphate occurs less frequently. Amino acid conjugation forms amide bonds between carboxylic acids and amino acids like glycine. These conjugation reactions make compounds more polar and water soluble for excretion.
This document discusses preformulation studies, which are important steps in developing an effective dosage form for a new drug. The objectives of preformulation studies are to establish the physico-chemical properties of the drug substance and generate information to design an optimal drug delivery system. Key aspects investigated include solubility, stability, compatibility with excipients, and parameters like particle size, bulk density and flow properties. Thorough preformulation work provides a foundation for formulation development and identifies potential problems to address.
Introduction:
History & Development:
Physicochemical Properties in relation to biological action:
Ionization
Solubility
Partition Coefficient
Hydrogen Bonding:
Protein Binding:
Chelation:
Bioisosterism:
Optical & Geomentrical Isomerism
Drug Metabolism:
Drug Metabolism Principles: Phase I & Phase II
Factors Affecting Drug Metabolism including steriochemical Aspects
This document provides an overview of preformulation studies. Preformulation studies characterize the physical and chemical properties of a drug substance alone and with excipients in order to develop a safe, effective, and stable dosage form. The goals of preformulation are to formulate an elegant, safe, and efficacious dosage form with good bioavailability. Key characterization parameters studied in preformulation include physicochemical properties, solubility analysis, and drug-excipient compatibility. Preformulation studies generate essential data needed to develop stable dosage forms that can be manufactured on a commercial scale.
Drug Excipient Interaction, Different Methods, Stability Testing.
drug excipient Compatibility and Incompatibility, Goals of drug excipient compatibility Methods, Factors Influencing stability Testing, Significant changes that might occur during satability Analysis
Phsicochemical properties according to pci syllubus.
The ability of a chemical compound to elicit a pharmacological/ therapeutic effect is related to the influence of various physical and chemical (physicochemical) properties of the chemical substance on the bio molecule that it interacts with.
1)Physical Properties : Physical property of drug is responsible for its action
2)Chemical Properties :The drug react extracellularly according to simple chemical reactions like neutralization, chelation, oxidation etc.
The ability of a chemical compound to elicit a pharmacological/ therapeutic effect is related to the influence of various physical and chemical (physicochemical) properties of the chemical substance on the bio molecule that it interacts with.
1)Physical Properties : Physical property of drug is responsible for its action
2)Chemical Properties :The drug react extracellularly according to simple chemical reactions like neutralization, chelation, oxidation etc.
This document discusses the physicochemical properties of drug molecules that influence drug kinetics and performance. It covers properties like ionization, partition coefficients, solubility, and polymorphism. Ionization affects drug absorption, binding and elimination based on a drug's pKa and the pH. Partition coefficients influence membrane permeability. Solubility and polymorphic forms impact oral absorption. Other properties like hygroscopicity, surface activity, and ability to form hydrogen bonds or chelates also influence drug behavior in the body. Steric features like conformational isomers and optical isomers can determine a drug's specificity for receptor binding and pharmacological effects.
PHYSICOCHEMICAL PROPERTIES OF DRUG MOLECU;E.pptxbreenaawan
This document discusses various physicochemical properties of drug molecules that influence their absorption and activity. It defines properties like ionization, partition coefficients, solubility, and polymorphism. It explains how these properties impact absorption in the gastrointestinal tract and interaction with targets. Factors like pH, buffers, and functional groups are described as influencing whether a drug is in an ionized or un-ionized form. The relationships between these physicochemical characteristics and a drug's behavior provide a framework for understanding drug activity.
The document discusses various physicochemical properties of drugs that influence their biological activity and effects. It covers properties like solubility, partition coefficient, dissociation constant, hydrogen bonding, ionization, complexation, and stereochemistry. Solubility and partition coefficient affect absorption and distribution of drugs in the body. Ionization influences what form a drug is in and its ability to cross membranes. Hydrogen bonding and complexation can impact properties like boiling point and drug availability. Protein binding and stereochemistry also influence a drug's pharmacological effects. Understanding these physicochemical properties is important for drug design and development.
Solid state stability and shelf-life assignment, Stability protocols,reports ...Durga Bhavani
This document discusses guidelines for solid state stability and shelf-life assignment studies as outlined by ICH. It provides definitions of stability, the need for stability studies, and factors that influence drug degradation like temperature, moisture, light and interactions. The document outlines the types of studies, including real-time and accelerated stability studies. It discusses stability protocols, reports, and test conditions recommended by ICH to determine a drug's shelf life.
This document provides an introduction to biopharmaceutics. It defines biopharmaceutics as the study of how the physicochemical properties of drugs and dosage forms affect drug absorption rates and levels. Key factors discussed include drug protection/stability, release rates, dissolution rates, and availability at the site of action. The document also discusses the significance of biopharmaceutics studies in understanding relationships between physical/chemical drug properties, dosage forms, administration routes, and systemic drug absorption levels and therapeutic effects.
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Medicinal Chemistry.pptx
1. MEDICINAL CHEMISTRY
PHYSICOCHEMICAL PROPERTIES IN RELATION TO BIOLOGICAL ACTION
SCHOOL OF PHARMACY(PARUL UNIVERSITY)
B.PHARM 2ND YEAR(4TH SEMESTER)
PRESENTED BY:
SWAGAT RATH
SARTHAK JHA
PRATHAM ROHIT
ANITA KUNWAR
2. CONTENTS
• PHYSICOCHEMICAL PROPERTIES OF DRUGS
• IONIZATION
• SOLUBILITY
• PARTITION COEFFICIENT
• HYDROGEN BONDING
• PROTEIN BINDING
• CHELATION
• BIOISOSTERISM
• OPTICAL AND GEOMETRICAL ISOMERISM
3. PHYSICOCHEMICAL PROPERTIES OF DRUGS
• PHYSICOCHEMICAL PROPERTIES OF DRUGS REFER TO THE PHYSICAL AND CHEMICAL
CHARACTERISTICS OF A DRUG MOLECULE THAT CAN INFLUENCE ITS BEHAVIOR IN THE BODY.
THESE PROPERTIES CAN IMPACT THE ABSORPTION, DISTRIBUTION, METABOLISM, AND
EXCRETION OF A DRUG, AS WELL AS ITS PHARMACOLOGICAL ACTIVITY.
• THIS INCLUDE PROPERTIES LIKE IONIZATION, SOLUBILITY, PARTITION COEFFICIENT, ETC
4. IONIZATION
• IONIZATION REFERS TO THE PROCESS OF A DRUG MOLECULE BECOMING CHARGED, EITHER
POSITIVELY OR NEGATIVELY, BY GAINING OR LOSING ELECTRONS. THIS PROCESS CAN
INFLUENCE THE BIOLOGICAL ACTION OF A DRUG IN SEVERAL WAYS.
• ABSORPTION: THE IONIZATION STATE OF A DRUG CAN AFFECT ITS SOLUBILITY AND
PERMEABILITY, WHICH IN TURN CAN INFLUENCE ITS ABSORPTION INTO THE BLOODSTREAM.
• DISTRIBUTION: IONIZED DRUGS TEND TO BE MORE HYDROPHILIC AND LESS LIPID-SOLUBLE,
WHICH CAN LIMIT THEIR DISTRIBUTION INTO LIPID-RICH TISSUES.
• METABOLISM: SOME DRUGS ARE METABOLIZED BY ENZYMES IN THE LIVER, WHICH CAN BE
INFLUENCED BY THEIR IONIZATION STATE. FOR EXAMPLE, IONIZED DRUGS MAY BE MORE
EASILY EXCRETED BY THE KIDNEYS, REDUCING THEIR AVAILABILITY FOR METABOLISM BY LIVER
ENZYMES.
5. SOLUBILITY
• SOLUBILITY REFERS TO THE MAXIMUM AMOUNT OF A DRUG THAT CAN DISSOLVE IN A SOLVENT
(USUALLY WATER) AT A GIVEN TEMPERATURE AND PRESSURE, FORMING A CLEAR AND
HOMOGENEOUS SOLUTION.
• FACTORS INFLUENCING THE SOLUBILITY OF DRUG :
• PH: THE PH OF THE SURROUNDING ENVIRONMENT CAN IMPACT THE IONIZATION STATE OF THE
DRUG, WHICH CAN IN TURN IMPACT ITS SOLUBILITY. FOR EXAMPLE, ACIDIC DRUGS WILL TEND TO BE
MORE SOLUBLE IN ACIDIC ENVIRONMENTS, WHILE BASIC DRUGS WILL TEND TO BE MORE SOLUBLE IN
BASIC ENVIRONMENTS.
• TEMPERATURE: INCREASED TEMPERATURE CAN GENERALLY INCREASE THE SOLUBILITY OF DRUGS IN A
SOLVENT, AS IT INCREASES THE ENERGY OF THE SOLUTE PARTICLES AND MAKES IT EASIER FOR THEM
TO DISSOLVE.
6. PARTITION COEFFICIENT
• THE PARTITION COEFFICIENT IS A MEASURE OF THE RELATIVE DISTRIBUTION OF A DRUG
BETWEEN TWO IMMISCIBLE PHASES, SUCH AS BETWEEN A LIPID PHASE AND AN AQUEOUS PHASE.
THIS PROPERTY CAN IMPACT THE DISTRIBUTION OF A DRUG WITHIN THE BODY, WITH
LIPOPHILIC DRUGS TENDING TO DISTRIBUTE MORE READILY INTO LIPID-RICH TISSUES SUCH AS
THE BRAIN OR ADIPOSE TISSUE.
• LIPOPHILICITY IS OFTEN QUANTIFIED AS THE LOGARITHM OF THE PARTITION COEFFICIENT,
WHICH IS KNOWN AS THE LOGP VALUE. DRUGS WITH HIGH LOGP VALUES ARE MORE LIPOPHILIC
AND WILL TEND TO PARTITION INTO LIPID-RICH ENVIRONMENTS, WHILE DRUGS WITH LOW
LOGP VALUES ARE MORE HYDROPHILIC AND WILL TEND TO REMAIN IN AQUEOUS
ENVIRONMENTS.
7. HYDROGEN BONDING
• HYDROGEN BONDING IS AN ATTRACTIVE INTERACTION BETWEEN A HYDROGEN
ATOM COVALENTLY BONDED TO ONE ELECTRONEGATIVE ATOM (SUCH AS
NITROGEN, OXYGEN, OR FLUORINE) AND ANOTHER ELECTRONEGATIVE ATOM.
THIS INTERACTION RESULTS IN A HIGHLY POLAR BOND THAT CAN HAVE
SIGNIFICANT EFFECTS ON THE PHYSICAL AND CHEMICAL PROPERTIES OF
MOLECULES.
• IMPACT ON BIOLOGICAL ACTION: CAN IMPACT THE SOLUBILITY AND STABILITY
OF A DRUG
• FACTORS INFLUENCING HYDROGEN BONDING: PH, TEMPERATURE, AND THE
PRESENCE OF OTHER SUBSTANCES
8. PROTEIN BINDING
• PROTEIN BINDING REFERS TO THE PROCESS BY WHICH A DRUG MOLECULE BINDS TO A PROTEIN
IN THE BLOOD OR TISSUES. THIS CAN IMPACT THE DISTRIBUTION, METABOLISM, AND
EXCRETION OF A DRUG, AS WELL AS ITS BIOAVAILABILITY AND EFFICACY.
• FACTORS THAT CAN INFLUENCE PROTEIN BINDING INCLUDE THE PH OF THE SURROUNDING
ENVIRONMENT, THE TEMPERATURE, AND THE PRESENCE OF OTHER DRUGS OR SUBSTANCES
THAT CAN COMPETE FOR BINDING SITES ON THE PROTEIN. FOR EXAMPLE, DRUGS THAT ARE
HIGHLY PROTEIN-BOUND WILL TEND TO HAVE A LONGER HALF-LIFE, AS THEY WILL BE LESS
LIKELY TO BE METABOLIZED OR EXCRETED FROM THE BODY.
9. CHELATION
• CHELATION REFERS TO THE PROCESS BY WHICH A MOLECULE (OFTEN A METAL ION) IS
SURROUNDED AND HELD BY A COMPLEX OF LIGANDS (MOLECULES OR IONS) TO FORM A
STABLE COORDINATION COMPOUND. IN THE CONTEXT OF DRUG BIOLOGICAL ACTION,
CHELATION REFERS TO THE BINDING OF A DRUG TO A METAL ION, TYPICALLY WITH THE GOAL
OF MODIFYING ITS PHARMACOLOGICAL PROPERTIES OR THERAPEUTIC EFFECT.
• IMPACT ON BIOLOGICAL ACTION: CAN IMPACT THE ABSORPTION, DISTRIBUTION, METABOLISM,
AND EXCRETION OF A DRUG, AS WELL AS ITS BIOAVAILABILITY AND EFFICACY
10. BIOISOSTERISM
• BIOISOSTERISM REFERS TO THE PHENOMENON IN WHICH TWO OR MORE CHEMICALLY
DIFFERENT COMPOUNDS EXHIBIT SIMILAR BIOLOGICAL ACTIVITY. THIS CAN IMPACT THE
PHARMACOLOGICAL PROPERTIES OF A DRUG, SUCH AS ITS EFFICACY, TOXICITY, AND
PHARMACOKINETICS.
• BIOISOSTERIC COMPOUNDS CAN BE DESIGNED TO HAVE SIMILAR STRUCTURES OR FUNCTIONAL
GROUPS, OR TO EXHIBIT SIMILAR PHYSICAL OR CHEMICAL PROPERTIES, WITH THE GOAL OF
PRESERVING OR ENHANCING THE DESIRED BIOLOGICAL ACTIVITY WHILE REDUCING OR
MITIGATING UNWANTED SIDE EFFECTS. FOR EXAMPLE, BIOISOSTERIC COMPOUNDS MAY HAVE
SIMILAR BINDING AFFINITIES FOR A TARGET RECEPTOR, OR SIMILAR PHARMACOKINETIC
PROPERTIES.
11. OPTICAL & GEOMETRICAL ISOMERISM
• OPTICAL ISOMERISM- THE PHENOMENON IN WHICH TWO OR MORE COMPOUNDS HAVE THE
SAME MOLECULAR FORMULA BUT DIFFER IN THE ARRANGEMENT OF THEIR ATOMS IN SPACE
• GEOMETRICAL ISOMERISM- THE PHENOMENON IN WHICH TWO OR MORE COMPOUNDS HAVE
THE SAME MOLECULAR FORMULA BUT DIFFER IN THE ARRANGEMENT OF THEIR ATOMS IN
SPACE
• IMPACT ON BIOLOGICAL ACTION: CAN IMPACT THE PHARMACOLOGICAL PROPERTIES OF A
DRUG, SUCH AS ITS EFFICACY, TOXICITY, AND PHARMACOKINETICS