Histamine is a biogenic amine involved in inflammatory and hypersensitivity reactions. It is synthesized and stored in mast cells and basophils and released during allergic reactions. Histamine acts on H1, H2, and H3 receptors to produce various pharmacological effects including vasodilation, increased capillary permeability, smooth muscle contraction, and gastric acid secretion. Antihistamines competitively antagonize histamine H1 receptors to treat conditions like allergic rhinitis, urticaria, and motion sickness. First-generation antihistamines are more sedating due to anticholinergic effects, while second-generation antihistamines have fewer side effects but some were banned due to cardiac issues when taken with
This document discusses histamine, an amine that acts as a chemical messenger in many cellular responses. It is released from mast cells and basophils during allergic reactions and causes symptoms like congestion and itching. Antihistamines block the H1 receptor to reduce these symptoms. H2 blockers inhibit gastric acid secretion by blocking the H2 receptor. Research continues on the roles and potential drug targets of other histamine receptors like H3, H4, and ligands that may treat conditions like sleep disorders, pruritus, and autoimmune disease.
Histamine is a biogenic amine present in many tissues that functions as a neurotransmitter and is involved in inflammatory and hypersensitivity reactions. It is synthesized from the amino acid histidine. Histamine acts through multiple receptor subtypes and is involved in various physiological processes like gastric acid secretion, smooth muscle contraction, and allergic responses. Antihistamines competitively inhibit histamine receptors, with first generation antihistamines having sedative effects and second generation ones having minimal side effects. They are used to treat allergic disorders, as antiemetics, and for gastric acid reduction with H2 blockers. Concerns have been raised about impurities in the H2 blocker ranitidine. While H3
Histamine is a biogenic amine involved in local immune responses and is released during allergic reactions. It binds to four histamine receptor subtypes (H1-H4) and causes effects like vasodilation, bronchioconstriction, and gastric acid secretion. Antihistamines work by competitively blocking histamine receptors. First generation antihistamines are more sedating due to crossing the blood brain barrier while second generation drugs are more selective for peripheral receptors with fewer side effects. Antihistamines are used to treat allergic conditions like rhinitis, conjunctivitis, hives, and anaphylaxis. Interactions with CYP3A4 inhibitors can increase risks of arrhythm
Histamine is a biogenic amine present in many animal and plant tissues. It is implicated as a mediator in hypersensitivity and tissue injury reactions. Histamine is present and stored in mast cells, especially in the skin, lungs, and gastrointestinal mucosa. It is synthesized from the amino acid histidine and acts on H1, H2, and H3 receptors to cause various pharmacological effects like vasodilation, increased capillary permeability, smooth muscle contraction, and increased gastric acid secretion. Serotonin is another amine present in enterochromaffin cells of the gastrointestinal tract. It is synthesized from tryptophan and acts on multiple 5-HT receptor subtypes to cause vasoconstriction, intestinal per
This document discusses various autacoids, including histamine, serotonin, prostaglandins, and thromboxanes. It provides details on their classification, synthesis, mechanisms of action, pharmacological effects, clinical uses, and antagonists. Histamine and serotonin are classified as amine autacoids derived from amino acids and act as inflammatory mediators. Prostaglandins and thromboxanes are eicosanoids derived from arachidonic acid that play important roles in inflammation and platelet aggregation. The document outlines the physiological roles and clinical applications of agonists and antagonists that target histamine, serotonin, and prostaglandin receptors.
The document discusses antihistamines and antiallergics. It begins with an introduction to histamine, including its discovery, biosynthesis from histidine, storage in mast cells, and role in allergic responses. It then covers the mechanisms of action of histamine at H1, H2, H3, and H4 receptors. The document discusses first and second generation antihistamines that work by blocking these receptors. Finally, it lists common indications for antihistamine use and potential side effects.
This document discusses histamine and antihistamine drugs. It begins by introducing histamine as a biogenic amine involved in inflammatory and hypersensitivity reactions. Histamine is synthesized from the amino acid histidine and stored in mast cells. It is involved in processes like gastric acid secretion and allergic responses. Antihistamines work by blocking the action of histamine at receptors. First generation antihistamines are more sedating while second generation ones have less side effects. Common antihistamines and their uses in conditions like allergies and vertigo are described. The document provides an overview of histamine function and the mechanisms of antihistamine drugs.
This document discusses histamine, an amine that acts as a chemical messenger in many cellular responses. It is released from mast cells and basophils during allergic reactions and causes symptoms like congestion and itching. Antihistamines block the H1 receptor to reduce these symptoms. H2 blockers inhibit gastric acid secretion by blocking the H2 receptor. Research continues on the roles and potential drug targets of other histamine receptors like H3, H4, and ligands that may treat conditions like sleep disorders, pruritus, and autoimmune disease.
Histamine is a biogenic amine present in many tissues that functions as a neurotransmitter and is involved in inflammatory and hypersensitivity reactions. It is synthesized from the amino acid histidine. Histamine acts through multiple receptor subtypes and is involved in various physiological processes like gastric acid secretion, smooth muscle contraction, and allergic responses. Antihistamines competitively inhibit histamine receptors, with first generation antihistamines having sedative effects and second generation ones having minimal side effects. They are used to treat allergic disorders, as antiemetics, and for gastric acid reduction with H2 blockers. Concerns have been raised about impurities in the H2 blocker ranitidine. While H3
Histamine is a biogenic amine involved in local immune responses and is released during allergic reactions. It binds to four histamine receptor subtypes (H1-H4) and causes effects like vasodilation, bronchioconstriction, and gastric acid secretion. Antihistamines work by competitively blocking histamine receptors. First generation antihistamines are more sedating due to crossing the blood brain barrier while second generation drugs are more selective for peripheral receptors with fewer side effects. Antihistamines are used to treat allergic conditions like rhinitis, conjunctivitis, hives, and anaphylaxis. Interactions with CYP3A4 inhibitors can increase risks of arrhythm
Histamine is a biogenic amine present in many animal and plant tissues. It is implicated as a mediator in hypersensitivity and tissue injury reactions. Histamine is present and stored in mast cells, especially in the skin, lungs, and gastrointestinal mucosa. It is synthesized from the amino acid histidine and acts on H1, H2, and H3 receptors to cause various pharmacological effects like vasodilation, increased capillary permeability, smooth muscle contraction, and increased gastric acid secretion. Serotonin is another amine present in enterochromaffin cells of the gastrointestinal tract. It is synthesized from tryptophan and acts on multiple 5-HT receptor subtypes to cause vasoconstriction, intestinal per
This document discusses various autacoids, including histamine, serotonin, prostaglandins, and thromboxanes. It provides details on their classification, synthesis, mechanisms of action, pharmacological effects, clinical uses, and antagonists. Histamine and serotonin are classified as amine autacoids derived from amino acids and act as inflammatory mediators. Prostaglandins and thromboxanes are eicosanoids derived from arachidonic acid that play important roles in inflammation and platelet aggregation. The document outlines the physiological roles and clinical applications of agonists and antagonists that target histamine, serotonin, and prostaglandin receptors.
The document discusses antihistamines and antiallergics. It begins with an introduction to histamine, including its discovery, biosynthesis from histidine, storage in mast cells, and role in allergic responses. It then covers the mechanisms of action of histamine at H1, H2, H3, and H4 receptors. The document discusses first and second generation antihistamines that work by blocking these receptors. Finally, it lists common indications for antihistamine use and potential side effects.
This document discusses histamine and antihistamine drugs. It begins by introducing histamine as a biogenic amine involved in inflammatory and hypersensitivity reactions. Histamine is synthesized from the amino acid histidine and stored in mast cells. It is involved in processes like gastric acid secretion and allergic responses. Antihistamines work by blocking the action of histamine at receptors. First generation antihistamines are more sedating while second generation ones have less side effects. Common antihistamines and their uses in conditions like allergies and vertigo are described. The document provides an overview of histamine function and the mechanisms of antihistamine drugs.
Histamine is a local hormone that is involved in physiological and pathological processes. It is stored in mast cells and released during allergic reactions. Histamine acts through four histamine receptors (H1-H4) and causes effects such as vasodilation, increased capillary permeability, bronchconstriction, and gastric acid secretion. Antihistamines are drugs that competitively block the H1 receptor and are used to treat allergic conditions. First generation antihistamines are sedating while second generation antihistamines are non-sedating but have fewer adverse effects. Histamine and antihistamines play important roles in allergic inflammation and disease.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
This document discusses emesis (vomiting) including its pathophysiology and treatment. It notes that emesis is a protective mechanism that eliminates harmful substances via stimulation of the emetic center in the medulla oblongata. Multiple pathways can trigger vomiting including the chemoreceptor trigger zone and nucleus tractus solitarius, which are important relay areas. Emetics and antiemetics are then described. Emetics include apomorphine, mustard, and ipecacuanha, while antiemetics include anticholinergics, H1 antihistamines, neuroleptics, prokinetic drugs, 5-HT3 antagonists, and adjuvant medications. Various drugs that
Histamine
Is a protein substance manufactured & found in human tissues
Its also a component of some venoms & secretions of stinging insects
Storage of histamine
In tissue mast cells (mainly)
In basophils
Enterochromaffin-like (ECL) cells of fundus of the stomach
Histamine release from mast cells;
Its released in response to;
1.Direct chemical /physical trauma to tissue mast cells
2. Drugs like morphine which displace histamine from their storage sites
3. Immunologic reactions esp the type 1allergic reactions coz degranulation of mast cells
Mechanism of action of histamine
Actions of histamine are mediated via histamines receptors found on cell membranes of different tissues
Types of histamine receptors;
H1 receptors
H₂ receptors
H₃ receptors
H₄ receptors
The document provides information about antihistamines and histamine. It discusses how histamine is synthesized and stored in mast cells and non-mast cells. It also describes the four types of histamine receptors (H1-H4) and their roles. The mechanisms and pharmacological actions of histamine are explained. Finally, the document summarizes the types, uses, pharmacokinetics and side effects of different generations of antihistamines used to treat conditions caused by histamine such as allergies and motion sickness.
Histamine is a biologically active amine released from mast cells and basophils in response to allergens and other stimuli, causing allergic reactions and lowering blood pressure. It binds to H1 and H2 receptors. H1 receptors mediate allergic symptoms, lowering blood pressure, bronchoconstriction, and gastric acid secretion. Antihistamines like chlorpheniramine and loratadine block H1 receptors, treating allergies, motion sickness, and insomnia with varying side effects. H2 receptor blockers like cimetidine and ranitidine inhibit gastric acid secretion, treating ulcers and reflux. Second generation antihistamines have fewer anticholinergic and sedative side
This document summarizes histamine and antihistaminic drugs. It discusses the history, synthesis, storage, and release of histamine. There are four types of histamine receptors (H1, H2, H3, H4) that mediate different physiological effects. Histamine plays a pathophysiological role in allergic reactions, gastric acid secretion, inflammation, and as a neurotransmitter. First generation antihistamines are effective but cause sedation, while second generation antihistamines like fexofenadine, loratadine and cetirizine are equally effective with fewer side effects.
This document discusses serotonin (5-HT), its pharmacological actions, and drugs that affect the serotonin system. Serotonin acts on various systems in the body like the cardiovascular, respiratory, and gastrointestinal systems. Drugs can affect serotonin by inhibiting or enhancing its synthesis, reuptake, storage, or degradation. Some drugs are serotonin receptor agonists or antagonists that target specific receptor subtypes. Serotonin receptor antagonists are used to treat conditions like migraines, nausea/vomiting, and schizophrenia.
This document discusses antihistamines and their classification, mechanisms of action, and effects. It describes first and second generation antihistamines. First generation drugs like dimenhydrinate are highly sedating and act as H1 receptor antagonists to reduce allergic reactions. Second generation drugs like astemizole have less sedation and do not cross the blood brain barrier. Antihistamines are used to treat allergic conditions by blocking the effects of histamine at receptor sites and providing relief from symptoms.
This document provides an overview of histamine and antihistamines. It discusses the synthesis, storage, and release of histamine as well as its four receptor types (H1, H2, H3, H4). It describes the pharmacological actions of histamine and the uses of first-generation antihistamines. Second-generation antihistamines are introduced which have fewer side effects and are commonly used to treat allergic disorders like rhinitis, dermatitis, and conjunctivitis. Specific second-generation drugs discussed include fexofenadine, loratadine, cetirizine, levocetirizine, and azelastine.
This document discusses autacoids and serotonin. It defines autacoids as biological agents that act locally at the site of synthesis and release, like local hormones. Two important amine autacoids are histamine and serotonin. Histamine is stored in mast cell granules and plays roles in hypersensitivity, tissue injury, and gastric acid secretion. Serotonin is synthesized from tryptophan and acts as a neurotransmitter and in gastrointestinal functions. The document describes the receptors, biosynthesis, metabolism, and pharmacological actions of histamine and serotonin, as well as the mechanisms and uses of antihistamines and anti-serotonin drugs.
This document discusses antihistamines and their mechanisms of action. It begins by defining autocoids and histamine as mediators involved in allergic inflammatory responses. It then covers the different types of histamine receptors (H1, H2, H3, H4) and their locations and functions. The document discusses the biosynthesis, metabolism, storage and release of histamine. It provides classifications of antihistamines including H1 receptor antagonists, H2 receptor antagonists, and dual-action drugs. Specific antihistamines are discussed within each class. The mechanisms of proton pump inhibitors for inhibiting gastric acid secretion are also summarized.
This document discusses autacoids, which are locally acting hormones. It focuses on histamine, an important inflammatory mediator. Histamine is formed from the amino acid histidine and is released from mast cells and basophils. It plays a role in inflammation, allergies, and gastric acid secretion. Antihistamines work by competing with histamine for binding sites at H1 receptors. First generation antihistamines easily cross the blood brain barrier and cause sedation, while second generation antihistamines have less side effects. Histamine causes effects in various organ systems, and antihistamines are used to treat allergic diseases, colds, motion sickness, and other conditions.
This document discusses autacoids, which are locally acting hormones. It specifically focuses on histamine and serotonin, which are amine-derived autacoids. Histamine is produced from the amino acid histidine and is important in inflammation and allergic reactions. It is released from mast cells and basophils. Histamine causes effects through various organ systems and is broken down by histamine-N-methyltransferase and diamine oxidase. Antihistamines work by competing with histamine for H1 receptors. Serotonin is derived from tryptophan and is important in vasoconstriction, mood, sleep, and appetite, among other roles. It is found abundantly in the gastrointestinal tract and blood
This document discusses serotonin (5-HT), an amine autacoid that acts as a local hormone. Some key points:
1. Serotonin is synthesized from the amino acid tryptophan and is widely distributed in the body, especially in the gastrointestinal tract and brain.
2. It has diverse physiological and pharmacological actions, including effects on mood, sleep, gastrointestinal motility, respiration, and cardiovascular function.
3. Serotonin signals through multiple receptor subtypes, and drugs that target specific receptors are used to treat conditions like anxiety, depression, migraine, and nausea/vomiting.
4. Dysregulation of serotonin signaling is implicated in diseases such as carcinoid syndrome and mood
This document discusses antihistamines and their mechanisms of action. It provides information on first-generation antihistamines like diphenhydramine and doxylamine, as well as second-generation antihistamines like cimetidine, ranitidine, and famotidine. It explains that antihistamines work by competitively binding to histamine receptors, reducing the effects of the neurotransmitter histamine, and describes their uses in treating allergies, nausea, and acid reflux diseases. The document is authored by Assoc. Prof. Imran Khan of Adina Institute of Pharmaceutical Sciences in Sagar, India.
This document provides information on autacoids, including histamine and serotonin. It defines autacoids as diverse substances produced locally in the body that have intense biological activity. Autacoids are classified as amine-derived, peptide-derived, or lipid-derived. Histamine is an amine autacoid derived from the amino acid histidine. It plays important roles in inflammation, allergic reactions, and gastric acid secretion. Serotonin is also an amine autacoid derived from tryptophan with roles as a neurotransmitter and in platelet aggregation and intestinal motility. The document discusses the synthesis, receptors, functions, and clinical uses of histamine and serotonin.
This presentation discusses histamines and antihistamines. Histamines are released by the body during allergic reactions and cause symptoms like swelling and itchiness. They are produced locally from the amino acid histidine. Antihistamines work by blocking histamine receptors in the body and are used to treat allergic conditions. There are first and second generation antihistamines that differ in their side effects and ability to cross the blood-brain barrier. The presentation also covers histamine intolerance, conditions that release histamines, and the classification of antihistamines.
This document discusses histamines, antihistamines, and 5-hydroxytryptamine (5-HT, serotonin) and their antagonists. It describes how histamines are synthesized and stored in mast cells and basophils and released during allergic reactions. The pharmacological actions of histamines are also explained. Antihistamines are described as drugs that block the actions of histamine by competing for H1 receptors. The document also covers the synthesis, receptors, pharmacological actions and functions of 5-HT as well as some 5-HT antagonists and their clinical uses.
This document discusses common problems in the elderly population and principles of geriatric care. It outlines several key issues:
1. Common geriatric syndromes include impaired cognition, urinary incontinence, falls, depression, and polypharmacy. Chronic diseases such as hypertension, diabetes, and osteoarthritis are also prevalent.
2. Effective geriatric care requires a comprehensive approach that considers multimorbidity, screening for underdiagnosed conditions, and goals of maintaining function rather than cure.
3. Key principles of care include considering aging itself is not a disease, screening for cognitive and affective disorders, preventing iatrogenic illnesses, and providing interprofessional and person-centered care.
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Similar to histamineandantihistaminics AHS Gowtham sap
Histamine is a local hormone that is involved in physiological and pathological processes. It is stored in mast cells and released during allergic reactions. Histamine acts through four histamine receptors (H1-H4) and causes effects such as vasodilation, increased capillary permeability, bronchconstriction, and gastric acid secretion. Antihistamines are drugs that competitively block the H1 receptor and are used to treat allergic conditions. First generation antihistamines are sedating while second generation antihistamines are non-sedating but have fewer adverse effects. Histamine and antihistamines play important roles in allergic inflammation and disease.
Autacoids - pharmacological actions and drugs related to them. SIVASWAROOP YARASI
Autacoids or "autocoids" are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis. The word autacoids comes from the Greek "autos" (self) and "acos" (relief, i.e. drug).
This document discusses emesis (vomiting) including its pathophysiology and treatment. It notes that emesis is a protective mechanism that eliminates harmful substances via stimulation of the emetic center in the medulla oblongata. Multiple pathways can trigger vomiting including the chemoreceptor trigger zone and nucleus tractus solitarius, which are important relay areas. Emetics and antiemetics are then described. Emetics include apomorphine, mustard, and ipecacuanha, while antiemetics include anticholinergics, H1 antihistamines, neuroleptics, prokinetic drugs, 5-HT3 antagonists, and adjuvant medications. Various drugs that
Histamine
Is a protein substance manufactured & found in human tissues
Its also a component of some venoms & secretions of stinging insects
Storage of histamine
In tissue mast cells (mainly)
In basophils
Enterochromaffin-like (ECL) cells of fundus of the stomach
Histamine release from mast cells;
Its released in response to;
1.Direct chemical /physical trauma to tissue mast cells
2. Drugs like morphine which displace histamine from their storage sites
3. Immunologic reactions esp the type 1allergic reactions coz degranulation of mast cells
Mechanism of action of histamine
Actions of histamine are mediated via histamines receptors found on cell membranes of different tissues
Types of histamine receptors;
H1 receptors
H₂ receptors
H₃ receptors
H₄ receptors
The document provides information about antihistamines and histamine. It discusses how histamine is synthesized and stored in mast cells and non-mast cells. It also describes the four types of histamine receptors (H1-H4) and their roles. The mechanisms and pharmacological actions of histamine are explained. Finally, the document summarizes the types, uses, pharmacokinetics and side effects of different generations of antihistamines used to treat conditions caused by histamine such as allergies and motion sickness.
Histamine is a biologically active amine released from mast cells and basophils in response to allergens and other stimuli, causing allergic reactions and lowering blood pressure. It binds to H1 and H2 receptors. H1 receptors mediate allergic symptoms, lowering blood pressure, bronchoconstriction, and gastric acid secretion. Antihistamines like chlorpheniramine and loratadine block H1 receptors, treating allergies, motion sickness, and insomnia with varying side effects. H2 receptor blockers like cimetidine and ranitidine inhibit gastric acid secretion, treating ulcers and reflux. Second generation antihistamines have fewer anticholinergic and sedative side
This document summarizes histamine and antihistaminic drugs. It discusses the history, synthesis, storage, and release of histamine. There are four types of histamine receptors (H1, H2, H3, H4) that mediate different physiological effects. Histamine plays a pathophysiological role in allergic reactions, gastric acid secretion, inflammation, and as a neurotransmitter. First generation antihistamines are effective but cause sedation, while second generation antihistamines like fexofenadine, loratadine and cetirizine are equally effective with fewer side effects.
This document discusses serotonin (5-HT), its pharmacological actions, and drugs that affect the serotonin system. Serotonin acts on various systems in the body like the cardiovascular, respiratory, and gastrointestinal systems. Drugs can affect serotonin by inhibiting or enhancing its synthesis, reuptake, storage, or degradation. Some drugs are serotonin receptor agonists or antagonists that target specific receptor subtypes. Serotonin receptor antagonists are used to treat conditions like migraines, nausea/vomiting, and schizophrenia.
This document discusses antihistamines and their classification, mechanisms of action, and effects. It describes first and second generation antihistamines. First generation drugs like dimenhydrinate are highly sedating and act as H1 receptor antagonists to reduce allergic reactions. Second generation drugs like astemizole have less sedation and do not cross the blood brain barrier. Antihistamines are used to treat allergic conditions by blocking the effects of histamine at receptor sites and providing relief from symptoms.
This document provides an overview of histamine and antihistamines. It discusses the synthesis, storage, and release of histamine as well as its four receptor types (H1, H2, H3, H4). It describes the pharmacological actions of histamine and the uses of first-generation antihistamines. Second-generation antihistamines are introduced which have fewer side effects and are commonly used to treat allergic disorders like rhinitis, dermatitis, and conjunctivitis. Specific second-generation drugs discussed include fexofenadine, loratadine, cetirizine, levocetirizine, and azelastine.
This document discusses autacoids and serotonin. It defines autacoids as biological agents that act locally at the site of synthesis and release, like local hormones. Two important amine autacoids are histamine and serotonin. Histamine is stored in mast cell granules and plays roles in hypersensitivity, tissue injury, and gastric acid secretion. Serotonin is synthesized from tryptophan and acts as a neurotransmitter and in gastrointestinal functions. The document describes the receptors, biosynthesis, metabolism, and pharmacological actions of histamine and serotonin, as well as the mechanisms and uses of antihistamines and anti-serotonin drugs.
This document discusses antihistamines and their mechanisms of action. It begins by defining autocoids and histamine as mediators involved in allergic inflammatory responses. It then covers the different types of histamine receptors (H1, H2, H3, H4) and their locations and functions. The document discusses the biosynthesis, metabolism, storage and release of histamine. It provides classifications of antihistamines including H1 receptor antagonists, H2 receptor antagonists, and dual-action drugs. Specific antihistamines are discussed within each class. The mechanisms of proton pump inhibitors for inhibiting gastric acid secretion are also summarized.
This document discusses autacoids, which are locally acting hormones. It focuses on histamine, an important inflammatory mediator. Histamine is formed from the amino acid histidine and is released from mast cells and basophils. It plays a role in inflammation, allergies, and gastric acid secretion. Antihistamines work by competing with histamine for binding sites at H1 receptors. First generation antihistamines easily cross the blood brain barrier and cause sedation, while second generation antihistamines have less side effects. Histamine causes effects in various organ systems, and antihistamines are used to treat allergic diseases, colds, motion sickness, and other conditions.
This document discusses autacoids, which are locally acting hormones. It specifically focuses on histamine and serotonin, which are amine-derived autacoids. Histamine is produced from the amino acid histidine and is important in inflammation and allergic reactions. It is released from mast cells and basophils. Histamine causes effects through various organ systems and is broken down by histamine-N-methyltransferase and diamine oxidase. Antihistamines work by competing with histamine for H1 receptors. Serotonin is derived from tryptophan and is important in vasoconstriction, mood, sleep, and appetite, among other roles. It is found abundantly in the gastrointestinal tract and blood
This document discusses serotonin (5-HT), an amine autacoid that acts as a local hormone. Some key points:
1. Serotonin is synthesized from the amino acid tryptophan and is widely distributed in the body, especially in the gastrointestinal tract and brain.
2. It has diverse physiological and pharmacological actions, including effects on mood, sleep, gastrointestinal motility, respiration, and cardiovascular function.
3. Serotonin signals through multiple receptor subtypes, and drugs that target specific receptors are used to treat conditions like anxiety, depression, migraine, and nausea/vomiting.
4. Dysregulation of serotonin signaling is implicated in diseases such as carcinoid syndrome and mood
This document discusses antihistamines and their mechanisms of action. It provides information on first-generation antihistamines like diphenhydramine and doxylamine, as well as second-generation antihistamines like cimetidine, ranitidine, and famotidine. It explains that antihistamines work by competitively binding to histamine receptors, reducing the effects of the neurotransmitter histamine, and describes their uses in treating allergies, nausea, and acid reflux diseases. The document is authored by Assoc. Prof. Imran Khan of Adina Institute of Pharmaceutical Sciences in Sagar, India.
This document provides information on autacoids, including histamine and serotonin. It defines autacoids as diverse substances produced locally in the body that have intense biological activity. Autacoids are classified as amine-derived, peptide-derived, or lipid-derived. Histamine is an amine autacoid derived from the amino acid histidine. It plays important roles in inflammation, allergic reactions, and gastric acid secretion. Serotonin is also an amine autacoid derived from tryptophan with roles as a neurotransmitter and in platelet aggregation and intestinal motility. The document discusses the synthesis, receptors, functions, and clinical uses of histamine and serotonin.
This presentation discusses histamines and antihistamines. Histamines are released by the body during allergic reactions and cause symptoms like swelling and itchiness. They are produced locally from the amino acid histidine. Antihistamines work by blocking histamine receptors in the body and are used to treat allergic conditions. There are first and second generation antihistamines that differ in their side effects and ability to cross the blood-brain barrier. The presentation also covers histamine intolerance, conditions that release histamines, and the classification of antihistamines.
This document discusses histamines, antihistamines, and 5-hydroxytryptamine (5-HT, serotonin) and their antagonists. It describes how histamines are synthesized and stored in mast cells and basophils and released during allergic reactions. The pharmacological actions of histamines are also explained. Antihistamines are described as drugs that block the actions of histamine by competing for H1 receptors. The document also covers the synthesis, receptors, pharmacological actions and functions of 5-HT as well as some 5-HT antagonists and their clinical uses.
Similar to histamineandantihistaminics AHS Gowtham sap (20)
This document discusses common problems in the elderly population and principles of geriatric care. It outlines several key issues:
1. Common geriatric syndromes include impaired cognition, urinary incontinence, falls, depression, and polypharmacy. Chronic diseases such as hypertension, diabetes, and osteoarthritis are also prevalent.
2. Effective geriatric care requires a comprehensive approach that considers multimorbidity, screening for underdiagnosed conditions, and goals of maintaining function rather than cure.
3. Key principles of care include considering aging itself is not a disease, screening for cognitive and affective disorders, preventing iatrogenic illnesses, and providing interprofessional and person-centered care.
This document discusses immunity, including innate immunity present at birth and acquired immunity developed during life through exposure to pathogens. Innate immunity provides non-specific resistance and includes mechanical barriers, secretions, cellular factors, fever and inflammation. Acquired immunity is either active (developed from natural infection or vaccination) or passive (from transfer of antibodies). Active immunity induces antibody production and cellular responses, providing durable protection. Passive immunity transfers pre-formed antibodies, offering short-term protection until the antibodies degrade.
Supraglottic airway devices (SGAs) are placed above the glottis to allow ventilation, oxygenation, and administration of anesthetic gases without endotracheal intubation. Examples include the Laryngeal Mask Airway (LMA), Intubating LMA, Proseal LMA, I-gel, and Combitube. The LMA is placed blindly in the oropharynx and its cuff seals the lateral and posterior pharyngeal walls to allow ventilation through ports. SGAs are easy to insert without laryngoscopy or muscle relaxants, do not require specific cervical spine positioning, and are reusable. However, they do not prevent aspiration and should not be used
Urine analysis is performed to examine urine composition and detect abnormalities. A 24-hour urine sample allows quantitative analysis of proteins, metabolites, and microorganisms. Urine is examined macroscopically for volume, color, odor, pH, and specific gravity. Chemical examination detects proteins, sugars, ketones, bilirubin, urobilinogen, and blood. Microscopic examination identifies crystals, casts, epithelial cells, and red and white blood cells. Urine dipsticks provide a convenient, rapid, qualitative analysis of various urine components.
General anaesthesia involves drugs that cause reversible loss of sensation and consciousness. Common general anaesthetics include inhalation gases like nitrous oxide, volatile liquids like halothane and isoflurane, and intravenous drugs like thiopentone, propofol, and ketamine. Anaesthesia involves stages including loss of consciousness, excitement, and surgical anaesthesia. Complications can occur during or after anaesthesia involving respiratory, cardiac, or organ issues. Pre-anaesthetic medication is used to relieve anxiety, cause amnesia, decrease secretions, and provide analgesia and antiemetic effects to make anaesthesia safer.
Capnography is a method to measure carbon dioxide levels in exhaled breath and can help diagnose respiratory depression and airway disorders, especially during anesthesia. It provides more safety in monitoring patients during surgery. There are two main types: mainstream capnography directly measures carbon dioxide at the airway and is invasive, while sidestream capnography transports a gas sample and is non-invasive but can delay measurements. Capnography works by passing infrared light through exhaled gas and measuring the amount of light absorbed by carbon dioxide. It displays carbon dioxide levels over time in a waveform that clinicians use to evaluate breathing rates and exhaled carbon dioxide levels.
Antiarrhythmic drugs are used to treat and prevent cardiac arrhythmias by blocking sodium, potassium, or calcium channels, or through beta-blockade. Class I drugs like quinidine and procainamide block sodium channels and prolong the heart's repolarization phase. Class III drugs like amiodarone block potassium channels and prolong action potential duration. Calcium channel blockers like verapamil and diltiazem (Class IV) inhibit calcium influx and reduce contractility. Other agents include adenosine for paroxysmal supraventricular tachycardia, beta-blockers for arrhythmias associated with exercise or emotion, and atropine for sinus bradycardia. Antiarrhythmics
This document discusses the pharmacotherapy of cough. It begins by defining cough and describing the cough reflex mechanism. Common causes of cough are then listed, including respiratory infections, allergies, smoking, and others. Drugs are classified as antitussives to suppress cough, expectorants to increase mucus secretion, and mucolytics to reduce mucus viscosity. Specific antitussives discussed include codeine, pholcodeine, noscapine, and dextromethorphan. Expectorants include guaiphenesin and potassium iodide. Mucolytics include acetylcysteine, carbocysteine, bromhexine, and ambroxol. Other treatment modalities involve hydration
Angina pectoris is chest pain due to ischemia of the heart muscle. It is usually felt as a tightness or pressure in the middle of the chest that may spread to the neck, jaw, or arm. There are three main types - stable angina brought on by exertion, unstable angina that occurs at rest, and Prinzmetal or variant angina caused by coronary artery spasm. Treatment involves medications to relieve symptoms like nitrates, beta blockers, calcium channel blockers, and newer drugs that open potassium channels or have a cytoprotective effect. Combination therapy with two or more classes is often used for better management of angina.
1. Antianginal drugs work to balance myocardial oxygen supply and demand by decreasing factors that increase demand such as heart rate, contractility, and blood pressure, and by increasing factors that affect supply such as coronary blood flow.
2. The main classes of antianginal drugs are organic nitrates, beta blockers, and calcium channel blockers. Nitrates work by vasodilating veins and arteries to reduce preload and afterload. Beta blockers reduce heart rate, contractility and blood pressure to decrease oxygen demand. Calcium channel blockers block calcium channels to cause vasodilation and reduce cardiac work.
3. Combination therapy using drugs with different mechanisms is often used for more severe
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3. Histamine
• Histamine: Tissue amine
N N
NH2
H
1
2
3
4
5
Histamine
1. Present mostly in mast cells:
Skin, lungs, GIT Mucosa, liver,
placenta
2. Non mast cell histamine:
Brain, Gastric Mucosa, Epidermis.
β imidazolylethylamine
4. Histamine
Histamine is a biogenic amine present in many animal
and plant tissues
Also present in blood, body secretions, venom &
stinging nettle, pathological fluids
One of the mediators involved in inflammatory &
hypersensitivity reactions
Present within storage granules of mast cells.
5. Synthesis, storage & metabolism of histamine
• Synthesized by decarboxylation of amino acid
histidine
• Degrades rapidly by oxidation & methylation
8. 1. Blood vessels:
Marked dilatation of smaller BV including arterioles, capillaries &
venules
S.C inj- flushing, ↑HR & CO, No fall in BP
Rapid IV inj – Fall in BP
Dilatation of cranial vessels – Pulsatile HA
Vasodilatation by H1→mediated by EDRF (NO)
Vasodilatation by H2 → located directly on the vascular SM
Pharmacological actions
9. Pharmacological actions
2. CVS:
– Dilates arterioles, capillaries, venules,
• IV injection- decreased BP
• Intradermal- Triple response Red spot
(Capillary dilatation)
Wheal (exudation of
fluid from capillaries
& venules)
Flare (Reflex
arteriolar dilatation)
15. Pharmacological actions
1. CNS depression: (More with first generation)
– Sedation and drowsiness
– Some have antiemetic and antiparkinsonian effects
2. Antiallergic action – type 1 HSV reaction
3. Anticholinergic actions (More with first generation)
• Antagonize muscarinic actions of ACh
– Dryness of mouth , Blurring of vision
– Constipation
– Urinary retention
16. Pharmacological Actions
4. Antagonism of histamine:
Block the histamine induced bronchoconstriction, triple
response, fall in BP, release of adrenaline.
5. Local anaesthetic: Membrane stabilizing property
Pheniramine, promethazine, diphenhydramine
6. BP: fall in BP on IV injection (direct smooth muscle
relaxation)
17. PHARMACOKINETICS
• Well absorbed oral and parenteral routes
• Metabolized- Liver
• Excretion – Urine
• Widely distributed in the body and enter brain.
• DOA → 4 – 6hours
• Except Meclozine, CPM, loratadine, cetrizine &
fexofenadine → 12 – 24hours
• Newer drugs doesn’t cross BBB – less sedative
25. Advantages of second generation
antihistaminics
1. Absence of CNS depressant property.
2. No impairment of psychomotor performance , produce no
subjective effects, no sedation.
3. Do not potentiate alcohol or benzodiazepines.
4. Higher H1 selectivitiy
5. No anticholinergic side effects.
6. Additional antiallergic mechanisms apart from histamine blockade
7. Inhibit late phase allergic reaction by acting on leukotrienes
8. or by antiplatelet activating factor effect
26. Banned antihistaminics
1. Terfenadine
First non-sedating SGA that was withdrawn
Due to polymorphic VT (torsades de pointes) due to higher
doses
When it was co-administered with CYP3A4
inhibitors(erythromycin, clarithromycin, ketoconazole,
itraconazole)
Blockade of delayed rectifier k+ channels in the heart at
higher concentrations.
2. Astemizole is another SGA banned for the same reason
27. 1. Fexofenadine
1. Active metabolite of terfenadine
2. Does not prolong QTc interval.
3. No interaction with CYP3A4 inhibitors
4. Free of arrhythmogenic potential
2. Loratadine
1. Long & fast acting
2. Lacks CNS depressant
3. Partly metabolized by CYP3A4 & t½ of 17 hour
4. No cardiac arrhythmia
5. Seizures are reported
6. Uses: Urticaria and atopic dermatitis
3. Desloratadine
1. Active metabolite of loratadine
2. Cardiac safety are documented
4. Cetrizine
1. Metabolite of hydroxyzine
2. Upper respiratory allergies, pollinosis
3. Urticaria and atopic dermatitis;
4. Used as adjuvant in seasonal asthma
28. 5. Levocetirizine
1. Active R(–) enantiomer of cetirizine.
2. Effective at half the dose
3. Less sedation
6. Azelastine
1. Good topical activity
2. Nasal spray - seasonal and perennial allergic rhinitis
3. Side effects- Stinging in the nose, altered taste
perception, weight gain
7. Mizolastine 1. Non-sedating antihistaminic,
2. Effective in allergic rhinitis and urticaria
8. Ebastine 1. Converted to the active metabolite carbastine.
2. Non-sedating
3. Nasal and skin allergies.
4. Prolong Q-Tc interval and CYP3A4 interaction
31. VERTIGO
Diuretics
• They decrease labyrinthine fluid pressure—acetazolamide, thiazides,
furosemide.
Anxiolytics, antidepressants - diazepam, amitriptyline
• These drugs appear to modify the sensation of vertigo
Corticosteroids
• They suppress intra labyrinthine edema due to viral infection or other
causes.
Sir Henry Dale,
discovered histamine Histamine was first discovered in 1910 by Sir Henry Hallett Dale as a contaminant of ergot generated by bacterial action. It was first synthesized before its significance was known, and due to its wide range of biological activity, has become one of the most important biologically produced amines in medicine and biology
Meniere`s disease: betahistine acts by improving blood flow in inner ear. The side efects are nausea, vomiting, headache and pruritis. It should be avoided in patients with bronchial asthma and peptic ulcer.
Azelastine
H1 blocker, also decrease histamine release, PAF & Leukotriene release
Good topical activity
T ½ = 24 hrs, also have active metabolite
Nasal spray: 0.14 mg/puff/nasal spray, 2 puffs per day for seasonal and perennial allergic rhinitis