This document provides an overview of antihistamines and allergies. It defines antihistamines as drugs that reduce the effects of histamine, which is released during allergic reactions. The document discusses the causes of allergies and the role of histamine. It also outlines the different classes of antihistamines, including first generation antihistamines and their associated side effects, as well as newer second generation antihistamines that are more selective. The clinical uses of antihistamines and future directions for allergy treatment are also briefly mentioned.
This document discusses histamine and antihistamines. It begins by introducing histamine, describing its discovery and roles in allergic reactions and as a neurotransmitter. It then covers histamine's chemistry, distribution in the body, synthesis, storage, and metabolism. The document discusses the four types of histamine receptors (H1-H4) and histamine's pharmacological effects. It also provides details on antihistamines, including their pharmacokinetics, mechanisms of action, side effects, and classifications of first versus second generation antihistamines. The document concludes by mentioning clinical uses of histamine and antihistamines for conditions like allergies and gastric hypersecretions.
This document provides information about autacoids, which are local hormones that include histamine and serotonin. It focuses on histamine, discussing its sources from mast cells and basophils, mechanisms of release, effects on organ systems, and use of antihistamines to treat allergic reactions. Serotonin is also discussed, including its role in mood, appetite, sleep, and vasoconstriction. The document summarizes the different types of serotonin receptors and their functions.
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
This document discusses drugs that act on the autonomic nervous system. It focuses on the parasympathetic nervous system neurotransmitter acetylcholine and drugs that interact with acetylcholine receptors. Acetylcholine is the major neurotransmitter of the parasympathetic nervous system and activates muscarinic and nicotinic receptors. Drugs that mimic acetylcholine, called cholinergic drugs, directly activate muscarinic receptors or indirectly increase acetylcholine levels by inhibiting the acetylcholinesterase enzyme. Examples include pilocarpine, neostigmine, and organophosphate pesticides. Anticholinergic drugs such as atropine competitively block muscarinic receptors, producing effects like tachy
Histamine is a chemical messenger that mediates allergic and inflammatory reactions. It is synthesized and stored in mast cells and basophils before being released in response to stimuli. Histamine binds to H1, H2, H3, and H4 receptors, with the H1 and H2 receptors being clinically relevant drug targets. Antihistamines are used to treat allergic conditions by blocking H1 receptors, and H2 receptor blockers inhibit gastric acid secretion. First-generation antihistamines have greater sedative and anticholinergic side effects than second-generation drugs due to interactions with other receptors.
Introduction to autacoids and classificationDikshakaushal8
Local hormones, also known as autacoids, are physiologically active substances produced locally in the body that have short-lived, localized effects. Some key classes of local hormones include amine derivatives like histamine and serotonin, peptide derivatives like bradykinin and angiotensins, and lipid derivatives like prostaglandins, leukotrienes, and platelet activating factor. These endogenous compounds play important roles in physiological and pathological processes through their actions on local tissues.
Histamine is a chemical released during allergic reactions that causes symptoms like sneezing, itching, and runny nose. It works by binding to H1 receptors, especially in the nose, lungs, and skin. Antihistamines block this binding and relieve allergy symptoms. First-generation antihistamines like diphenhydramine can cause drowsiness by crossing the blood-brain barrier, while second-generation drugs like loratadine and fexofenadine mainly work in the periphery and have fewer side effects. Antihistamines are used to treat allergic conditions, nausea, motion sickness, and other issues involving the H1 receptor.
This document discusses histamine and antihistamines. It begins by introducing histamine, describing its discovery and roles in allergic reactions and as a neurotransmitter. It then covers histamine's chemistry, distribution in the body, synthesis, storage, and metabolism. The document discusses the four types of histamine receptors (H1-H4) and histamine's pharmacological effects. It also provides details on antihistamines, including their pharmacokinetics, mechanisms of action, side effects, and classifications of first versus second generation antihistamines. The document concludes by mentioning clinical uses of histamine and antihistamines for conditions like allergies and gastric hypersecretions.
This document provides information about autacoids, which are local hormones that include histamine and serotonin. It focuses on histamine, discussing its sources from mast cells and basophils, mechanisms of release, effects on organ systems, and use of antihistamines to treat allergic reactions. Serotonin is also discussed, including its role in mood, appetite, sleep, and vasoconstriction. The document summarizes the different types of serotonin receptors and their functions.
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
This document discusses drugs that act on the autonomic nervous system. It focuses on the parasympathetic nervous system neurotransmitter acetylcholine and drugs that interact with acetylcholine receptors. Acetylcholine is the major neurotransmitter of the parasympathetic nervous system and activates muscarinic and nicotinic receptors. Drugs that mimic acetylcholine, called cholinergic drugs, directly activate muscarinic receptors or indirectly increase acetylcholine levels by inhibiting the acetylcholinesterase enzyme. Examples include pilocarpine, neostigmine, and organophosphate pesticides. Anticholinergic drugs such as atropine competitively block muscarinic receptors, producing effects like tachy
Histamine is a chemical messenger that mediates allergic and inflammatory reactions. It is synthesized and stored in mast cells and basophils before being released in response to stimuli. Histamine binds to H1, H2, H3, and H4 receptors, with the H1 and H2 receptors being clinically relevant drug targets. Antihistamines are used to treat allergic conditions by blocking H1 receptors, and H2 receptor blockers inhibit gastric acid secretion. First-generation antihistamines have greater sedative and anticholinergic side effects than second-generation drugs due to interactions with other receptors.
Introduction to autacoids and classificationDikshakaushal8
Local hormones, also known as autacoids, are physiologically active substances produced locally in the body that have short-lived, localized effects. Some key classes of local hormones include amine derivatives like histamine and serotonin, peptide derivatives like bradykinin and angiotensins, and lipid derivatives like prostaglandins, leukotrienes, and platelet activating factor. These endogenous compounds play important roles in physiological and pathological processes through their actions on local tissues.
Histamine is a chemical released during allergic reactions that causes symptoms like sneezing, itching, and runny nose. It works by binding to H1 receptors, especially in the nose, lungs, and skin. Antihistamines block this binding and relieve allergy symptoms. First-generation antihistamines like diphenhydramine can cause drowsiness by crossing the blood-brain barrier, while second-generation drugs like loratadine and fexofenadine mainly work in the periphery and have fewer side effects. Antihistamines are used to treat allergic conditions, nausea, motion sickness, and other issues involving the H1 receptor.
cholinergic receptors definetion and classifcation to 1-nicotinic and 2-muscarinic ...and their subtybes ..... then the sites and the mechanism ... and last the drugs effect
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 provides an overview of cholinergic drugs, which act on the parasympathetic nervous system. It begins with an introduction to cholinergic transmission and the discovery of acetylcholine. It describes the different types of cholinoceptors and their locations. The document then discusses the pharmacological actions of direct and indirect cholinergic drugs. It provides examples of therapeutic uses for various drugs in conditions like glaucoma and myasthenia gravis. Screening methods for cholinergic drugs are also summarized. The document concludes by stating that cholinergic pharmacology is an established field but further research is still needed for cognitive enhancing drugs.
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 discusses biguanides and thiazolidinediones as oral hypoglycemic drugs. It describes metformin as the main biguanide currently used, noting its mechanism of action involves suppressing glucose production in the liver and enhancing glucose disposal in muscles. Pioglitazone is the only available thiazolidinedione, which works by enhancing insulin sensitivity. Potential side effects and appropriate uses are provided for both classes. Acarbose is also summarized as an alpha-glucosidase inhibitor that reduces glucose absorption from the gut. Clinical uses of glucagon for treating hypoglycemia are briefly mentioned.
This document discusses drugs used to treat cough. It begins by defining cough and classifying it based on duration and characteristics. Nonspecific therapies for cough include demulcents to soothe the throat, expectorants to enhance mucus secretion or reduce viscosity, and antitussives to suppress the cough center. Demulcents include lozenges and cough drops. Expectorants include bronchial secretagogues like guaifenesin and mucolytics like bromhexine that break down mucus. Antitussives include opioids like codeine, nonopioids like dextromethorphan, and antihistamines. Specific treatments depend on the underlying cause of cough such as antibiotics for infection
Thyroid hormones like triiodothyroxine (T3) and thyroxine (T4) are synthesized in the thyroid gland and regulated by thyroid stimulating hormone (TSH). Anti-thyroid drugs work by inhibiting thyroid hormone synthesis, iodine trapping, or hormone release. Common anti-thyroid drugs include propylthiouracil, methimazole, carbimazole, iodine, and radioactive iodine. These drugs are used to treat hyperthyroidism and can control overactive thyroid function by various mechanisms of action like inhibiting thyroid peroxidase or iodide uptake into the thyroid gland.
This document discusses bioassay methods for quantifying histamine using isolated guinea pig ileum and anesthetized animal models. Histamine is synthesized in mast cells, enterochromaffin cells, and neurons. It mediates effects by binding H1-H4 receptors and causes symptoms like rash and bronchospasm upon mast cell release. Bioassay on guinea pig ileum determines histamine potency by recording contractions, which are induced by H1 receptor agonism. In anesthetized cats or dogs, a standard histamine dose producing a 20mmHg blood pressure fall is used to interpolate test sample doses. These bioassays allow estimation of histamine concentration and pharmacological effects in living tissues.
Generic name: Cetirizine hydrochloride.
Chemical name: [2- [4- [(4-chlorophenyl) phenylmethyl] -1- piperazinyl] ethoxy]acetic acid, dihydrochloride.
Cetirizine, a metabolite of hydroxyzine, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors.
Cetirizine was rapidly absorbed with a time to maximum concentration of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers.
Cetirizine hydrochloride syrup is indicated for the relief of symptoms associated with perennial allergic rhinitis due to allergens such as dust mites, animal dander and molds.
Cetirizine is a second generation drug.
Second generation antihistamines are developed to avoid or reduce the sedative effects of drug.
Second-generation antihistamines cross the blood–brain barrier to a much lower degree than the first-generation antihistamines. Their main benefit is they primarily affect peripheral histamine receptors and therefore are less sedating.
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive functioning. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Acetylcholinesterase inhibitors : Dr Rahul KunkulolRahul Kunkulol
This document discusses anticholinesterase drugs and their mechanisms and uses. It describes how anticholinesterases inhibit the enzyme acetylcholinesterase, preventing the breakdown of acetylcholine and thereby increasing cholinergic neurotransmission. The main types discussed are reversible carbamate drugs like physostigmine and neostigmine, and irreversible organophosphate inhibitors. Their uses include treating glaucoma, myasthenia gravis, and as antidotes for organophosphate poisoning. The mechanisms and characteristics of specific drugs like physostigmine, neostigmine, and edrophonium are also compared.
Histamine is a chemical messenger produced in mast cells and basophils that mediates allergic reactions and inflammatory responses. It is found throughout the body, including in the lungs, skin, blood vessels, and GI tract. Antihistamines work by blocking the H1 and H2 receptors that histamine binds to. First generation antihistamines block H1 receptors and cause sedation, while second generation antihistamines do not cross the blood brain barrier and are less sedating. H2 receptor blockers like cimetidine and ranitidine are used to reduce gastric acid production.
Histamine and bradykinin are important autacoids or local hormones that act near their site of synthesis to exert physiological effects. Histamine is released from mast cells and basophils during allergic reactions and binds to H1, H2, H3 and H4 receptors, causing effects like vasodilation, increased vascular permeability, and bronchioconstriction. It is involved in allergic diseases. Bradykinin is produced from kininogen and acts on B1 and B2 receptors to cause vasodilation, smooth muscle contraction, increased vascular permeability and pain. Both histamine and bradykinin are inactivated by enzymatic degradation and their effects can be blocked by receptor antagonists.
This document discusses drugs for cough. It begins by describing the mechanism and causes of cough. Cough can be voluntary or reflexive, and has afferent and efferent pathways involving various nerves. Causes include upper respiratory infections, pneumonia, and other conditions. The document then classifies drugs for cough into four main categories: pharyngeal demulcents to soothe the throat; expectorants to increase or thin mucus; antitussives to suppress coughing; and bronchodilators to relieve cough caused by bronchospasm. Specific drugs and combinations are provided as examples for each category. The document concludes by describing specific treatments for cough based on its underlying cause.
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
Adrenergic agonists and antagonists act on adrenergic receptors. Agonists like epinephrine and norepinephrine directly stimulate receptors, whereas antagonists like prazosin competitively block receptor activation. These drugs have widespread effects throughout the body due to the sympathetic nervous system's role in functions like heart rate, blood pressure, bronchodilation and uterine contraction. Care must be taken with certain drugs that can cause severe side effects like hypotension or bronchospasm.
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
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 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.
Antihistamines are drugs that reduce or eliminate the effects of histamine, which is released during allergic reactions. There are several classes of antihistamines including first generation, second generation, and third generation. First generation antihistamines are effective but cause more side effects like sedation due to their ability to cross the blood brain barrier. Newer generations have been developed with greater selectivity for peripheral histamine receptors, resulting in fewer side effects. Research continues on developing more selective antihistamines and exploring the anti-inflammatory properties and potential for new treatments.
This document provides an overview of antihistamines. It defines antihistamines as drugs that reduce the effects of histamine, which is released during allergic reactions. The document discusses the causes of allergies and the role of histamine. It outlines the history and classes of antihistamines, including first generation types. The document also discusses the future of antihistamine treatment and research related to new histamine receptor subtypes.
cholinergic receptors definetion and classifcation to 1-nicotinic and 2-muscarinic ...and their subtybes ..... then the sites and the mechanism ... and last the drugs effect
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 provides an overview of cholinergic drugs, which act on the parasympathetic nervous system. It begins with an introduction to cholinergic transmission and the discovery of acetylcholine. It describes the different types of cholinoceptors and their locations. The document then discusses the pharmacological actions of direct and indirect cholinergic drugs. It provides examples of therapeutic uses for various drugs in conditions like glaucoma and myasthenia gravis. Screening methods for cholinergic drugs are also summarized. The document concludes by stating that cholinergic pharmacology is an established field but further research is still needed for cognitive enhancing drugs.
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 discusses biguanides and thiazolidinediones as oral hypoglycemic drugs. It describes metformin as the main biguanide currently used, noting its mechanism of action involves suppressing glucose production in the liver and enhancing glucose disposal in muscles. Pioglitazone is the only available thiazolidinedione, which works by enhancing insulin sensitivity. Potential side effects and appropriate uses are provided for both classes. Acarbose is also summarized as an alpha-glucosidase inhibitor that reduces glucose absorption from the gut. Clinical uses of glucagon for treating hypoglycemia are briefly mentioned.
This document discusses drugs used to treat cough. It begins by defining cough and classifying it based on duration and characteristics. Nonspecific therapies for cough include demulcents to soothe the throat, expectorants to enhance mucus secretion or reduce viscosity, and antitussives to suppress the cough center. Demulcents include lozenges and cough drops. Expectorants include bronchial secretagogues like guaifenesin and mucolytics like bromhexine that break down mucus. Antitussives include opioids like codeine, nonopioids like dextromethorphan, and antihistamines. Specific treatments depend on the underlying cause of cough such as antibiotics for infection
Thyroid hormones like triiodothyroxine (T3) and thyroxine (T4) are synthesized in the thyroid gland and regulated by thyroid stimulating hormone (TSH). Anti-thyroid drugs work by inhibiting thyroid hormone synthesis, iodine trapping, or hormone release. Common anti-thyroid drugs include propylthiouracil, methimazole, carbimazole, iodine, and radioactive iodine. These drugs are used to treat hyperthyroidism and can control overactive thyroid function by various mechanisms of action like inhibiting thyroid peroxidase or iodide uptake into the thyroid gland.
This document discusses bioassay methods for quantifying histamine using isolated guinea pig ileum and anesthetized animal models. Histamine is synthesized in mast cells, enterochromaffin cells, and neurons. It mediates effects by binding H1-H4 receptors and causes symptoms like rash and bronchospasm upon mast cell release. Bioassay on guinea pig ileum determines histamine potency by recording contractions, which are induced by H1 receptor agonism. In anesthetized cats or dogs, a standard histamine dose producing a 20mmHg blood pressure fall is used to interpolate test sample doses. These bioassays allow estimation of histamine concentration and pharmacological effects in living tissues.
Generic name: Cetirizine hydrochloride.
Chemical name: [2- [4- [(4-chlorophenyl) phenylmethyl] -1- piperazinyl] ethoxy]acetic acid, dihydrochloride.
Cetirizine, a metabolite of hydroxyzine, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors.
Cetirizine was rapidly absorbed with a time to maximum concentration of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers.
Cetirizine hydrochloride syrup is indicated for the relief of symptoms associated with perennial allergic rhinitis due to allergens such as dust mites, animal dander and molds.
Cetirizine is a second generation drug.
Second generation antihistamines are developed to avoid or reduce the sedative effects of drug.
Second-generation antihistamines cross the blood–brain barrier to a much lower degree than the first-generation antihistamines. Their main benefit is they primarily affect peripheral histamine receptors and therefore are less sedating.
The document discusses the benefits of exercise for mental health. Regular physical activity can help reduce anxiety and depression and improve mood and cognitive functioning. Exercise causes chemical changes in the brain that may help protect against mental illness and improve symptoms.
Acetylcholinesterase inhibitors : Dr Rahul KunkulolRahul Kunkulol
This document discusses anticholinesterase drugs and their mechanisms and uses. It describes how anticholinesterases inhibit the enzyme acetylcholinesterase, preventing the breakdown of acetylcholine and thereby increasing cholinergic neurotransmission. The main types discussed are reversible carbamate drugs like physostigmine and neostigmine, and irreversible organophosphate inhibitors. Their uses include treating glaucoma, myasthenia gravis, and as antidotes for organophosphate poisoning. The mechanisms and characteristics of specific drugs like physostigmine, neostigmine, and edrophonium are also compared.
Histamine is a chemical messenger produced in mast cells and basophils that mediates allergic reactions and inflammatory responses. It is found throughout the body, including in the lungs, skin, blood vessels, and GI tract. Antihistamines work by blocking the H1 and H2 receptors that histamine binds to. First generation antihistamines block H1 receptors and cause sedation, while second generation antihistamines do not cross the blood brain barrier and are less sedating. H2 receptor blockers like cimetidine and ranitidine are used to reduce gastric acid production.
Histamine and bradykinin are important autacoids or local hormones that act near their site of synthesis to exert physiological effects. Histamine is released from mast cells and basophils during allergic reactions and binds to H1, H2, H3 and H4 receptors, causing effects like vasodilation, increased vascular permeability, and bronchioconstriction. It is involved in allergic diseases. Bradykinin is produced from kininogen and acts on B1 and B2 receptors to cause vasodilation, smooth muscle contraction, increased vascular permeability and pain. Both histamine and bradykinin are inactivated by enzymatic degradation and their effects can be blocked by receptor antagonists.
This document discusses drugs for cough. It begins by describing the mechanism and causes of cough. Cough can be voluntary or reflexive, and has afferent and efferent pathways involving various nerves. Causes include upper respiratory infections, pneumonia, and other conditions. The document then classifies drugs for cough into four main categories: pharyngeal demulcents to soothe the throat; expectorants to increase or thin mucus; antitussives to suppress coughing; and bronchodilators to relieve cough caused by bronchospasm. Specific drugs and combinations are provided as examples for each category. The document concludes by describing specific treatments for cough based on its underlying cause.
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
Adrenergic agonists and antagonists act on adrenergic receptors. Agonists like epinephrine and norepinephrine directly stimulate receptors, whereas antagonists like prazosin competitively block receptor activation. These drugs have widespread effects throughout the body due to the sympathetic nervous system's role in functions like heart rate, blood pressure, bronchodilation and uterine contraction. Care must be taken with certain drugs that can cause severe side effects like hypotension or bronchospasm.
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
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 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.
Antihistamines are drugs that reduce or eliminate the effects of histamine, which is released during allergic reactions. There are several classes of antihistamines including first generation, second generation, and third generation. First generation antihistamines are effective but cause more side effects like sedation due to their ability to cross the blood brain barrier. Newer generations have been developed with greater selectivity for peripheral histamine receptors, resulting in fewer side effects. Research continues on developing more selective antihistamines and exploring the anti-inflammatory properties and potential for new treatments.
This document provides an overview of antihistamines. It defines antihistamines as drugs that reduce the effects of histamine, which is released during allergic reactions. The document discusses the causes of allergies and the role of histamine. It outlines the history and classes of antihistamines, including first generation types. The document also discusses the future of antihistamine treatment and research related to new histamine receptor subtypes.
This document provides an overview of antihistamines. It defines antihistamines as drugs that reduce the effects of histamine, which is released during allergic reactions. The document discusses the causes of allergies and the role of histamine. It outlines the history and classes of antihistamines, including first generation types. The document also discusses the future of antihistamine treatment and research related to new histamine receptors.
The document discusses antihistamines and histamine. It begins by defining antihistamines as drugs that reduce the effects of histamine, which is released during allergic reactions. It then discusses the structure, functions, and synthesis of histamine. The document outlines the causes and types of allergies and describes the clinical uses and adverse effects of various classes of antihistamines, including first-generation and newer second-generation drugs. It discusses the actions of histamine at different receptor sites and concludes by summarizing the classification and structures of representative antihistamines.
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
Autacoids, also known as local hormones, are naturally occurring substances that have different structures and pharmacological actions. They include decarboxylated amino acids, polypeptides, and eicosanoids. Histamine is one of the most important autacoids and is stored in mast cells. It is released through immunologic or non-immunologic mechanisms to modulate inflammatory and immune responses. Antihistamines work by blocking the H1 receptor and are used to treat various allergic conditions by reducing the effects of histamine. First generation antihistamines are less selective and have more side effects while second generation antihistamines have fewer side effects.
This document discusses antihistamines, which are medicines used to treat allergies and other hypersensitive reactions. It begins by defining antihistamines and explaining how they work by blocking the effects of histamine at receptor sites. It then describes what causes allergies and the role of histamine. The document is divided into sections on the history of antihistamines, classes of antihistamines including first and second generation types, their uses, side effects, and the future of allergy treatment.
This document discusses histamine and antihistamines. It provides details on histamine including its synthesis, storage, receptors, and role in allergic reactions and inflammation. It then describes first and second generation antihistamines that act as H1 receptor antagonists to relieve symptoms of allergic rhinitis, urticaria, and other conditions by blocking the effects of histamine. The patient described has seasonal allergic rhinitis, so a second generation antihistamine with fewer side effects would be most suitable. First generation antihistamines that cause drowsiness should be avoided.
Histamine is an autacoid that acts as a local hormone and neurotransmitter. It has various functions including mediating inflammation, regulating gut function, and acting as a neurotransmitter. It is produced by basophils and mast cells and stored in these cells as well as neurons. Upon stimulation, histamine is released and binds to four types of G protein-coupled histamine receptors (H1-H4) to produce various effects. First generation antihistamines block H1 receptors and penetrate the blood-brain barrier, causing sedation as an adverse effect. Second generation antihistamines are more selective for H1 receptors and do not cross the blood-brain barrier, reducing adverse effects. Common first and
Med chem lecture on Antihistaminicdrugssagar joshi
This document summarizes information about histamine and antihistamines. It discusses:
- Histamine's roles in the body as a mediator of inflammation and local immune responses, in regulating gut function, and as a neurotransmitter.
- How histamine is produced and stored in mast cells and basophils and is released during immune responses.
- The four types of histamine receptors (H1-H4), their locations and functions. H1 antihistamines are used to treat allergies.
- Details on first and second generation H1 antihistamines, including their structures, mechanisms of action, uses, and side effects. Second generation antihistamines avoid the
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.
H1 and H2 receptor blockers, also known as antihistamines, are drugs that block the effects of the histamine receptor. There are four types of histamine receptors: H1, H2, H3, and H4. H1 receptor blockers, also called first-generation antihistamines, are used to treat allergic disorders by blocking the H1 receptor. Second-generation antihistamines selectively target only peripheral H1 receptors, reducing side effects. H2 receptor blockers are used to reduce stomach acid production and treat ulcers by blocking the H2 receptor in the stomach. The structures, mechanisms of action, uses and side effects of various first-generation and second-generation
Histamine is an autacoid that acts as a local hormone near its site of synthesis. It is synthesized from the amino acid histidine. There are four types of histamine receptors: H1, H2, H3, and H4. H1 receptors mediate various physiological effects like gastric acid secretion, allergic responses, and cardiovascular effects. Antihistamines like chlorpheniramine and cetirizine act as antagonists at H1 receptors to relieve allergy symptoms. H2 receptor antagonists like cimetidine and ranitidine are used to reduce gastric acid secretion. H3 receptors are presynaptic autoreceptors that regulate histamine release, and their antagonists have potential for improving cognition
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.
Histamine, Bradykinin, and Their Antagonists.pptxAUGUSTINE KANYI
Histamine plays a key role in allergic inflammation and immune responses by binding to four histamine receptor subtypes (H1-H4). When released from mast cells and basophils during allergic reactions, histamine causes symptoms by activating H1 receptors and mediates downstream immune effects. Antihistamines effectively treat allergic diseases by competitively blocking the H1 receptor and preventing histamine's effects. They are classified into non-sedating second generation and more sedating first generation types based on their ability to cross the blood-brain barrier.
This document discusses antihistamines, which are drugs that reduce or eliminate the effects of histamine. Histamine is released during allergic reactions and binds to histamine receptors, causing inflammation. Antihistamines work by competing with histamine for binding sites on receptors. The document describes different types of antihistamines including first generation drugs that have anticholinergic effects and second generation drugs that are more selective. It also discusses the structures, classifications, and mechanisms of antihistamines.
Outline:
What is the antihistamines.
What is histamine.
What is the receptors.
What is the clinical uses of antihistamines.
Side effects of antihistamines.
What is the contraindications.
Histamine is a biogenic amine found throughout the body. It is synthesized from the amino acid histidine and stored in mast cells and basophils. Upon release, histamine binds to H1, H2, H3, and H4 receptors, exerting various effects. H1 receptor antagonists, also known as antihistamines, are used to treat allergic reactions by blocking the effects of histamine. Common first-generation antihistamines have anticholinergic effects which can cause sedation as a side effect. Newer second-generation antihistamines are more specific to H1 receptors with fewer side effects. Serotonin is synthesized from tryptophan and found primarily in the
Antihistamines are drugs that reduce or eliminate the effects of histamine by competing for binding sites on histamine receptors. Histamine is released during allergic reactions from mast cells and basophils and acts on H1, H2, H3, and H4 receptors throughout the body. Common antihistamines include first generation sedating antihistamines like diphenhydramine and hydroxyzine as well as newer second generation antihistamines with less sedation like cetirizine, loratadine, and fexofenadine. Antihistamines are used to treat allergic conditions, insomnia, and ulcers by blocking the H1 or H2 receptors through which
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The document discusses drug excretion through the renal system. It defines excretion as the elimination of drugs and metabolites from the body through the urinary system. Drugs are excreted either unchanged or after being metabolized. The kidneys eliminate polar compounds more efficiently than lipid-soluble substances. The kidneys remove waste through glomerular filtration, tubular secretion, and tubular reabsorption in the nephrons. Several factors influence renal excretion, such as a drug's ionization, concentration, pH, extent of plasma protein binding, glomerular filtration rate, and renal blood flow.
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1. Outline
What is an antihistamine?
What causes allergies and what are they, what is histamine?
History of antihistamines
Classes of antihistamines
Future of antihistamines and allergy treatment in general
2. What is an antihistamine
A drug that reduces or eliminates the effects mediated by the chemical
histamine
Histamine is released by body during an allergic reaction and acts on a
specific histamine receptor
True antihistamines are only the agents that produce a therapeutic effect
that is mediated by negative modulation of histamine receptors
The term antihistamine only refers to H1 receptor antagonists (actually
inverse agonists)
Antihistamines compete with histamine for binding sites at the receptors.
Antihistamine cannot remove the histamine if it is already bound
3. What are allergies?
Allergies are caused by a hypersensitivity reaction of the antibody class
IgE which are located on mast cells in the tissues and basophils in the
blood.
When an allergen is encountered, it binds to IgE, which excessively
activates the mast cells or basophils, leading them to release massive
amounts of histamines.
These histamines lead to inflammatory responses ranging from runny
nose to anaphylactic shock
If both parents have allergies, you have a 70% of having them, if only
one parent does, you have a 48% chance
(American Academy of Asthma, Allergies and Immunology, Spring 2003).
4.
5. Mast Cells
Histamine is distributed in Mast Cells in all peripheral tissues of the
body and basophils, which circulate in the blood
6. Allergies
Structure of Histamine
When it is released, histamine causes inflammation by
increasing vasodilation,
capillary permeability,
causing smooth muscle contraction,
mucus secretion,
parasympathetic nerve stimulation
7.
8. Synthesis of Histamine
• Formed from the amino acid Histadine in a decarboxylation reaction
with the enzyme histadine decarboxylase
• Occurs primarily in mast cells and basophils
http://www.fao.org/docrep/006/y4743e/y4743e0k.gif
9. The different Histamine receptors
Location Type of
receptor
Effect Treatment
H1 Throughout the body, specifically in
smooth muscles, on vascular
endothelial cells, in the heart and the
CNS
G-protein coupled,
linked to
intercellular Gq,
which activates
phospholipase C
Mediate an increase in
vascular permeability at
sites of inflammation
induced by histamine
Allergies, nausea,
sleep disorders
H2 In more specific locations in the body
mainly in gastric parietal cells, a low
level can be found in vascular smooth
muscle, neutrophils, CNS, heart,
uterus
G-protein coupled,
linked to
intercellular Gs
Increases the release of
gastric acid
Stomach ulcers
H3 Found mostly in the CNS, with a high
level in the thalamus, caudate nucleus
and cortex, also a low level detected
in small intestine, testis and prostate.
G-protein coupled,
possibly linked to
intercellular Gi
Neural presynaptic
receptor, may function
to release histamine
Unknown
H4 They were recently discovered in
2000. They are widely expressed in
components of the immune system
such as the spleen, thymus and
leukocytes.
Unknown, most
likely also G-protein
coupled
Unknown In addition to benefiting
allergic conditions,
research in the h4
receptor may lead to the
treatment of autoimmune
diseases. (rheumatoid
arthritis and IBS)
11. Adverse side effects
Associated with the first generation H1-antihistamines and due to their
lack of selectivity for the H1 receptor and anti-cholinergic activity.
Side effects are due to CNS depression:
• Sedation
• Dizziness
• Tinnitus (ringing in the ear)
• Blurred vision
• Euphoria
• Uncoordination
• Anxiety
• Insomnia
• Tremor
• Nausea/vomitting
12. First antihistamine
• Piperoxan
• Discovered in 1933 by Jeff Forneau and Daniel Bovent while
developing a guinea pig animal model of anaphylaxis
• They received the Nobel Prize in 1957
http://www.registech.com/images/ce.jpg
13. Classes of first generation H1 receptor antagonist
antihistamines
• Ethylenediamines
• Ethanolamines
• Alkylamines
• Piperazines
• Tricyclics
14. Common Structural Features of classical first generation
antihistamines
• 2 aromatic rings, connected to a central carbon, nitrogen, or oxygen
• Spacer between central atom and the amine, usually 2-3 carbons in length.
(Can be linear, ring, branched, saturated or unsaturated)
• The amine is substituted with small alkyl groups
• Chirality at X and having the rings in different planes increases potency of
the drug
16. Ethanolamines
• This class has significant anticholinergic side effects and sedation,
however reduced the gastroinestnal side effects
Diphenhydramine (Benedryl)
• Oldest and most effective antihistamine on
the market
• Available over the counter
• Because it induces sedation, it’s used in
nonprescription sleep aids such as Tylenol
PM
• Also inhibits the reuptake of serotonin,
which led to the search for viable
antidepressants with similar structures
(prozac)
17. Ethanolamines
Carbinoxamine(Clistine) Doxylamine succinate
•2nd in effectiveness of anti-allergy
activity only to Benadryl
•Active ingredient in NyQuil
•Potent anti-cholinergic effects
•Is used to treat Hay fever and is
especially popular to children due
its its mild taste
•After 21 reported deaths in
children under 2, its now only
marketed to children above 3
18. Ethanolamines
Clemastine (Tavist) Dimenhydrinate ramamine)
•Exhibits fewer side effects
than most antihistamines
•Widely used as an
antiprurtic (stops itching)
•Anti-emetic (anti nausea)
•Also causes strong sedation
•Readily crosses the BBB
19. Alkylamines
• Isomerism is an important factor in this class of drugs, which is due to
the positioning and fit of the molecules in the H1-receptor binding site
• These drugs have fewer sedative and GI adverse effects, but a greater
incidence of CNS stimulation
• These drugs lack the “spacer molecule” (which is usually a nitrogen
or oxygen) between the two aromatic rings and at least one of the
rings has nitrogen included in the aromatic system
20. Akylamines
Chlorphenamine Brompheniramine (Dimetapp)
•Originally used to prevent
allergic conditions
•Shown to have antidepressant
properties and inhibit the
reuptake of serotonin
•The first SSRI was made as a
derivative of chlorphenamine
•Available over the counter
•Used to treat the common cold by
relieving runny nose, itchy, watery
eyes and sneezing
21. Akylamines
Triprolidine hydrochloride Pheniramine (Avil)
•Used to alleviate the
symptoms associated with
allergies
•Can be combined with other
cold medicine to relieve “flu-
like” symptoms
•Used most often to treat hay fever
or urticaria (hives)
•Antihistamine component of
Visine-A
22. Piperazines
• Structurally related to the ethylenediamines and the ethanolamines
and thus produce significant anti-cholinergic effects
• Used most often to treat motion sickness, vertigo, nausea and
vomiting
•Used to treat the symptoms associated with
motion sickness, vertigo and post-op following
administration of general anaesthesia and opiods
•Mechanism of inhibiting motion sickness is not
well understood, but it may act on the labyrinthine
apparatus and the chemoreceptor trigger zone
(area of the brain which receives input and
induces vomiting)
Cyclizine
24. Piperazines
Meclizine Cetirizine (Zyrtec)
•It is most commonly used to
inhibit nausea and vomiting as
well as vertigo, however it
does cause drowsiness
•This drug treats indoor and outdoor
allergies and is safe to use in
children as young as 2
25. Tricyclics
• These drugs are structurally related to tricyclic antidepressants, which
explains why they have cholinergic side effects
Promethazine (Phenegran)
•This drug has extremely strong anticholinergic
and sedative effects
•It was originally used as an antipsychotic,
however now it is most commonly used as a
sedative or antinausea drug (also severe
morning sickness) and requires a prescription
26. Tricyclics
Cyproheptadine Ketotifen (Zaditor)
•This drug both an antihistamine and an
antiserotonergic agent
•It is a 5-HT2 receptor antagonist and also
blocks calcium channels
•Used to treat hay fever and also to stimulate
appetite in people with anorexia
•It is also rarely used to treat SSRI induced
sexual dysfunction and also Cushing’s
Syndrome (high level of cortisol in the blood)
and migraine headaches
•This drug is available in two
forms: an ophthalmic form used
to treat allergic conjunctivitis or
itchy red eyes and an oral form
used to prevent asthma attacks
•It has several adverse side
effects including drowsiness,
weight gain, dry mouth,
irritability and increased
nosebleeds
27. Tricyclics
Alimemazine (Vallergan) Azatadine
(Optimine or Trinalin)
•This drug is used to treat itchiness
and hives that results from allergies
•Since it causes drowsiness, it is
useful for rashes that itch worse at
night time
•It is also used to sedate young
children before operations
•This drug is used to treat
symptoms of allergies and the
common cold such as sneezing,
runny nose, itchy watery eyes,
itching, hives and rashes
28. Second generation H1-receptor antagonists
• These are the newer drugs and they are much more selective for the
peripheral H1-receptors involved in allergies as opposed to the H1-
receptors in the CNS
• Therefore, these drugs provide the same relief with many fewer
adverse side effects
• The structure of these drugs varies and there are no common
structural features associated with them
• They are however bulkier and less lipophilic than the first generation
drugs, therefore they do not cross the BBB as readily
• Recent studies have also showed that these drugs also have anti-
inflammatory activity and therefore, would be helpful in the
management of inflammation in allergic airways disease (Devalia and
Davies).
29. Second generation H1-receptor antagonists
Acrivastine (Semprex-D) Astemizole (Hismantol)
•This drug has a long duration of action
•It suppresses the formation of edema and
puritus
•It doesn’t cross the BBB
•It has been taken off the market in most
countries because of adverse interactions
with erythromycin and grapefruit juice
•This drug relieves itchy
rashes and hives
•It is non-sedating because it
does not cross the BBB
30. Second generation H1-receptor antagonists
Loratadine (Claritin) Terfenadine (Seldane)
It is the only drug of its class
available over the counter
It has long lasting effects and
does not cause drowsiness
because it does not cross the BBB
It was formerly used to treat
allergic conditions
In the 1990’s it was removed
from the market due to the
increased risk of cardiac arrythmias
31. Second generation H1-receptor antagonists
Azelastine (Astelin
or Optivar)
Levocabastine (Livostin)
It is a mast cell
stablilizer
Available as a nasal
spray (Astelin) or eye
drops for pink eye
(Optivar)
Both of these drugs are used as eye drops to
treat allergic conjunctivitis
Olopatadine (Patanol)
32. Third generation H1-receptor antagonists
• These drugs are derived from second generation antihistamines
• They are either the active enantiomer or metabolite of the second
generation drug designed to have increased efficacy and fewer side
effects
Levocetirizine (Zyzal)
•This drug is the active enantiomer of
cetirizine and is believed to be more effective
and have fewer adverse side effects.
•Also it is not metabolized and is likely to be
safer than other drugs due to a lack of
possible drug interactions (Tillement).
•It does not cross the BBB and does not cause
significant drowsiness
•It has been shown to reduce asthma attacks
by 70% in children
33. Third generation H1-receptor antagonists
Deslortadine (Clarinex) Fexofenadine (Allegra)
•It is the active metabolite of
Lortadine
•Even though it is thought to
be more effective, there is no
concrete evidence to prove
this
•It was developed as an
alternative to Terfenadine
•Fexofenadine was proven to
be more effective and safe
34. The future of antihistamines
• The anti-inflammatory activity of second generation antihistamines,
about which little is known, will continue to be researched and
possibly lead to an effective alternative to corticosteriods in the
treatment of allergic airways conditions.
• The action of the H4 receptor will also continue to be researched and
will possibly lead to effective treatment of autoimmune dieseases.
• Creating antihistamines with higher selectivity and less adverse side
effects will continue to be the goal
35. References
Cuss, F.M. “Beyond the histamine receptor: effect of antihistamine on mast cells.” Clinical and
Experimental Allergy Review 1999; 29: 54-59.
Devalia, J.L. and R.J. Davies. “Effect of antihistamines on epithelial cells.” Clinical and
Experimental Allergy Review 1999; 29: 64-68.
Mosges, R. and N. Krug. “Efficacy of antihistamines: from the precision of challenge models
to the alchemy of clinical practice.” Clinical and Experimental Allergy Review 2006; 6: 20-24.
Tillement, J.P. “Pharmacological profile of the new antihistamines.” Clinical and Experimental
Allergy Review 2005; 5:7-11
http://www.netdoctor.co.uk/medicines/100002712.html
http://www.drugs.com
http://en.wikipedia.org/wiki/Antihistamines
http://www.drugbank.com
Editor's Notes
The anticholinergic side effects may include: motor impairment, dry mouth/throat, flushed skin, rapid or irregular heart beat, blurred vision, sensitivity to light, pupil dilation, urinary retention, constipation, difficulty concintrating, short term memory loss, visual disturbances, hallucinations, confusion, erectile dysfunction, and delirium
Dramamine is actually a combination of two drugs: diphenhydramine (Benadryl) and 8-chlorotheophillinate (similar to caffeine and is a mild CNS stimulator)
They thought that adding the 8-chlorotheophillinate would counteract the affects of the diphenhydramine, however that is not that case and sedation still occurs