The document discusses adrenoceptor agonists and antagonists. It begins by providing an overview of the sympathetic nervous system and drugs that act on it. It then describes direct-acting sympathomimetic drugs that mimic norepinephrine and epinephrine by acting on alpha and beta receptors. Various agonists are discussed in depth, including their mechanisms of action, effects, uses, and adverse reactions. The document also covers adrenoceptor antagonists that block alpha and beta receptors, describing examples like prazosin and propranolol along with their clinical applications.
Ganglionic stimulants like nicotine can activate nicotinic receptors in autonomic ganglia, resulting in the stimulation of both sympathetic and parasympathetic responses. Although they have limited medical use, nicotine has been used experimentally to help identify nerve fibers. Ganglionic blockers are competitive antagonists at nicotinic receptors that reduce autonomic tone, and were once used to treat hypertension and peptic ulcers but caused intolerable side effects. Trimethaphan is a short-acting ganglionic blocker occasionally used for controlled hypotension. Mecamylamine has been studied for smoking cessation by blocking nicotine's rewarding effects but also causes constipation. Currently there is no significant
This document summarizes 5 major categories of transducer mechanisms:
1) G-protein coupled receptors which activate downstream effectors like adenylyl cyclase or phospholipase C.
2) Ion channel receptors which directly open or close ion channels.
3) Transmembrane enzyme-linked receptors which activate intracellular protein kinases.
4) Transmembrane JAK-STAT binding receptors which activate the JAK/STAT signaling pathway.
5) Receptors regulating gene expression which bind intracellularly to directly regulate gene transcription.
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
The autonomic nervous system (ANS) innervates the heart, smooth muscles, glands and viscera and is divided into the parasympathetic and sympathetic nervous systems. The parasympathetic system participates in tissue building and the sympathetic system enables responses to stress. Both systems have efferent neurons that travel from the CNS to effector organs via a two-neuron chain, with preganglionic neurons synapsing in ganglia and postganglionic neurons innervating the organs. The sympathetic system originates in the thoracic and lumbar spinal cord and parasympathetic system originates in the cranial and sacral regions. The sympathetic system prepares the body for fight or flight while the parasympathetic
This document summarizes parasympathomimetics (cholinergic agonists). It discusses how the parasympathetic nervous system uses acetylcholine as a neurotransmitter and how cholinergic agonists mimic acetylcholine's actions. It classifies cholinergic agonists into direct-acting and indirect-acting types. Direct agonists bind receptors, while indirect agonists inhibit acetylcholinesterase to increase acetylcholine levels. Examples of both types are provided along with their structures, mechanisms of action, and uses. The document also covers acetylcholine synthesis and catabolism as well as structure-activity relationships of parasympathomimetics.
Adrenergic antagonists alpha and beta blockersZulcaif Ahmad
The document discusses various types of adrenergic receptor antagonists including alpha blockers like prazosin and terazosin which are used to treat hypertension and benign prostatic hyperplasia, as well as non-selective antagonists like phentolamine and beta blockers like propranolol which are used to treat conditions like hypertension, angina, and arrhythmias. The mechanisms, classifications, clinical uses and side effects of these different adrenergic antagonists are explained in detail across multiple pages.
This document discusses adrenergic receptors and their classification into alpha and beta receptors. It describes the differences between alpha and beta adrenergic receptors and provides details about various types of drugs that act as adrenergic antagonists including:
- Alpha blockers which are used to treat hypertension and benign prostatic hyperplasia. They cause vasodilation and reduce blood pressure. Examples include prazosin and doxazosin.
- Beta blockers which are classified as non-selective or cardioselective. Non-selective blockers are contraindicated in asthma while cardioselective blockers reduce their side effects. Examples of beta blockers mentioned are propranolol and atenolol.
Ganglionic stimulants like nicotine can activate nicotinic receptors in autonomic ganglia, resulting in the stimulation of both sympathetic and parasympathetic responses. Although they have limited medical use, nicotine has been used experimentally to help identify nerve fibers. Ganglionic blockers are competitive antagonists at nicotinic receptors that reduce autonomic tone, and were once used to treat hypertension and peptic ulcers but caused intolerable side effects. Trimethaphan is a short-acting ganglionic blocker occasionally used for controlled hypotension. Mecamylamine has been studied for smoking cessation by blocking nicotine's rewarding effects but also causes constipation. Currently there is no significant
This document summarizes 5 major categories of transducer mechanisms:
1) G-protein coupled receptors which activate downstream effectors like adenylyl cyclase or phospholipase C.
2) Ion channel receptors which directly open or close ion channels.
3) Transmembrane enzyme-linked receptors which activate intracellular protein kinases.
4) Transmembrane JAK-STAT binding receptors which activate the JAK/STAT signaling pathway.
5) Receptors regulating gene expression which bind intracellularly to directly regulate gene transcription.
Seretonin (5HT) and Its Antagonists PharmacologyPranatiChavan
Serotonin is a chemical that has a wide variety of functions in the human body. It is sometimes called the happy chemical, because it contributes to wellbeing and happiness.
The scientific name for serotonin is 5-hydroxytryptamine, or 5-HT. It is mainly found in the brain, bowels, and blood platelets.
Serotonin is used to transmit messages between nerve cells, it is thought to be active in constricting smooth muscles, and it contributes to wellbeing and happiness, among other things. As the precursor for melatonin, it helps regulate the body’s sleep-wake cycles and the internal clock.
It is thought to play a role in appetite, the emotions, and motor, cognitive, and autonomic functions. However, it is not known exactly if serotonin affects these directly, or if it has an overall role in co-ordinating the nervous system.
The autonomic nervous system (ANS) innervates the heart, smooth muscles, glands and viscera and is divided into the parasympathetic and sympathetic nervous systems. The parasympathetic system participates in tissue building and the sympathetic system enables responses to stress. Both systems have efferent neurons that travel from the CNS to effector organs via a two-neuron chain, with preganglionic neurons synapsing in ganglia and postganglionic neurons innervating the organs. The sympathetic system originates in the thoracic and lumbar spinal cord and parasympathetic system originates in the cranial and sacral regions. The sympathetic system prepares the body for fight or flight while the parasympathetic
This document summarizes parasympathomimetics (cholinergic agonists). It discusses how the parasympathetic nervous system uses acetylcholine as a neurotransmitter and how cholinergic agonists mimic acetylcholine's actions. It classifies cholinergic agonists into direct-acting and indirect-acting types. Direct agonists bind receptors, while indirect agonists inhibit acetylcholinesterase to increase acetylcholine levels. Examples of both types are provided along with their structures, mechanisms of action, and uses. The document also covers acetylcholine synthesis and catabolism as well as structure-activity relationships of parasympathomimetics.
Adrenergic antagonists alpha and beta blockersZulcaif Ahmad
The document discusses various types of adrenergic receptor antagonists including alpha blockers like prazosin and terazosin which are used to treat hypertension and benign prostatic hyperplasia, as well as non-selective antagonists like phentolamine and beta blockers like propranolol which are used to treat conditions like hypertension, angina, and arrhythmias. The mechanisms, classifications, clinical uses and side effects of these different adrenergic antagonists are explained in detail across multiple pages.
This document discusses adrenergic receptors and their classification into alpha and beta receptors. It describes the differences between alpha and beta adrenergic receptors and provides details about various types of drugs that act as adrenergic antagonists including:
- Alpha blockers which are used to treat hypertension and benign prostatic hyperplasia. They cause vasodilation and reduce blood pressure. Examples include prazosin and doxazosin.
- Beta blockers which are classified as non-selective or cardioselective. Non-selective blockers are contraindicated in asthma while cardioselective blockers reduce their side effects. Examples of beta blockers mentioned are propranolol and atenolol.
This document discusses the adrenergic system including adrenergic receptors, location and functions of different receptor types, adrenergic drugs, and pharmacological actions. It also covers adrenergic receptor antagonists including classifications of alpha-blockers and beta-blockers, their uses and adverse effects. The key points are: there are alpha and beta adrenergic receptors which are located in various organs and tissues and have different functions; common adrenergic drugs act as pressor agents, bronchodilators or cardiac stimulants; and adrenergic receptor antagonists like alpha-blockers and beta-blockers are used to treat conditions like hypertension, angina, heart failure and gl
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 summarizes a seminar on sympathomimetic drugs presented by Mohd Fahad and guided by Mohd. Khushtar. It discusses different types of adrenergic drugs including direct, indirect, and mixed acting sympathomimetics. It describes the actions of adrenergic drugs on various organs mediated by alpha and beta receptors. Important drugs are discussed in detail including their uses, doses, preparations, and adverse effects. The document provides an overview of adrenergic pharmacology and the therapeutic uses of sympathomimetic drugs.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
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 adrenergic agonists and antagonists. It describes the synthesis, storage, release, and degradation of catecholamines like norepinephrine. It outlines the different subtypes of alpha and beta adrenergic receptors, their locations, and the effects of agonist binding. Key adrenergic drugs like epinephrine, norepinephrine, dopamine, and dobutamine are explained in terms of their mechanisms of action, therapeutic uses, dosages, and adverse effects. Interactions between adrenergic drugs and other medications are also noted.
This document discusses drugs that inhibit the renin-angiotensin system for treating hypertension and other conditions. It describes how ACE inhibitors work by inhibiting the angiotensin converting enzyme and decreasing angiotensin II formation, while also increasing bradykinin levels. Angiotensin receptor blockers competitively block the angiotensin II receptor. Both classes lower blood pressure by vasodilation and reduced sodium retention. They are used to treat hypertension, heart failure, diabetic nephropathy, and myocardial infarction. Adverse effects include hypotension, hyperkalemia, and cough with ACE inhibitors.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
This document outlines a lecture on medicinal chemistry related to the cholinergic system. It will review concepts of acetylcholine mimetics and acetylcholinesterase inhibitors. For muscarinic agonists, it will discuss biosynthesis and metabolism of acetylcholine, structure activity relationship studies of various muscarinic agonists. For acetylcholinesterase inhibitors, it will cover the mechanism of acetylcholine hydrolysis, reversible and irreversible inhibitors, and the antidote for irreversible inhibitors. Learning objectives and resources are also provided.
This document summarizes parasympatholytic drugs, also known as anticholinergic or antimuscarinic drugs. It discusses the pharmacological properties and uses of atropine and scopolamine, which are belladonna alkaloids that act as competitive inhibitors at muscarinic receptors in the parasympathetic nervous system. It also describes newer anticholinergic drugs that have more selective actions, such as ipratropium bromide and tiotropium bromide for bronchodilation in respiratory disorders, and oxybutynin for urinary incontinence.
This document summarizes the classification, mechanisms of action, pharmacokinetics, and clinical uses of α-adrenergic receptor antagonists (α-blockers). It discusses non-selective α-blockers that block both α1 and α2 receptors like phentolamine and phenoxybenzamine, as well as selective α1-blockers like prazosin, doxazosin, tamsulosin, and selective α2-blockers like yohimbine. The major uses of α-blockers include treatment of pheochromocytoma, hypertension, peripheral vascular disease, benign prostatic hyperplasia, migraine, and congestive heart failure. Common side effects include hypotension
The document discusses drugs used to treat congestive heart failure (CHF). It first defines CHF as a condition where the heart cannot pump enough blood to the body's organs. It then discusses the causes of CHF including narrowed arteries, past heart attacks, and high blood pressure. The document focuses on cardiac glycosides, which work by increasing the force of cardiac contraction, as a primary treatment for CHF. It describes the mechanisms of action and pharmacological effects of cardiac glycosides like digitalis on the heart and electrophysiology. Potential adverse drug reactions and drug interactions are also reviewed.
This ppt provides the detailed about the bradykinin and their physiological and pharmacological actions and their generation and their mechanisms in detailed manner.
The document provides an overview of the renin-angiotensin-aldosterone system (RAAS). It discusses the classical components of RAAS including renin, angiotensinogen, angiotensin peptides, angiotensin receptors, and angiotensin converting enzyme. It also covers newer concepts such as local tissue RAAS, intracellular RAAS, receptor heterodimerization, and the roles of angiotensin converting enzyme 2 and angiotensin (1-7). The document highlights functions of RAAS in various organs and pathophysiological processes.
This presentation deals with the use of various drugs in the treatment of heart failure such as Digoxin, ace inhibitors, beta bloockers, calcium channel blockers
This document discusses antihypertensive agents used to treat hypertension. It begins by defining hypertension as blood pressure above 140/90 mmHg. It then discusses the renin-angiotensin-aldosterone pathway which controls blood pressure. Various classes of antihypertensive agents are described, including beta-blockers, ACE inhibitors, calcium channel blockers, and diuretics. Specific drugs from each class are provided along with their mechanisms and uses for treating hypertension. The mechanisms of action are summarized for each drug class, such as how beta-blockers work by blocking epinephrine to slow the heart rate and lower blood pressure.
This document discusses drugs used to treat congestive heart failure (CHF). CHF occurs when the heart cannot pump enough blood to meet the body's needs. Key drugs mentioned include digitalis glycosides like digoxin, which increase the force of heart contractions; diuretics like furosemide that reduce fluid buildup; ACE inhibitors and ARBs that lower blood pressure and prevent further heart damage; and inotropic drugs like dobutamine that strengthen heart contractions. Adverse effects, mechanisms of action, and guidelines for use are provided for several common CHF medications.
Beta-adrenoceptor agonists (β-agonists) bind to β1 and β2 receptors in the heart, blood vessels, and other tissues. In the heart, this increases heart rate, contractility, conduction velocity and relaxation through activation of Gs proteins, cAMP, and downstream targets like calcium channels and myosin phosphorylation. In blood vessels, β-agonists cause smooth muscle relaxation through similar cAMP-mediated inhibition of myosin light chain kinase. Therapeutically, β-agonists are used to treat acute and refractory heart failure as well as circulatory shock by increasing cardiac output and vasodilation.
Sympatholytics, also known as adrenergic antagonists or blocking agents, work in opposition to adrenergic agents by blocking alpha and beta receptor sites. They are classified based on the type of adrenergic receptor they block, including alpha1, alpha2, beta1, beta2, and beta3 receptors. Common alpha blockers include phenoxybenzamine, ergot alkaloids, phentolamine, tolazoline, prazosin, terazosin, doxazosin, and tamsulosin. Common beta blockers mentioned include propanolol, acetabutolol, atenolol, betaxolol, carvedilol, metoprol
This document discusses adrenergic agonists, which are drugs that act on pathways mediated by the endogenous catecholamines norepinephrine and epinephrine. These drugs target various steps in catecholamine synthesis, storage, release, binding, and removal and are used to treat conditions like hypertension, depression, shock, asthma, and angina. Adrenergic agonists are classified as direct-acting if they act directly on receptors, or indirect-acting if they increase catecholamine levels in the synapse. The document also describes the subtypes of alpha and beta adrenergic receptors, their locations, mechanisms of action, and the effects of prolonged receptor stimulation.
The document discusses adrenergic drugs and their mechanisms of action. It notes that some adrenergic drugs act directly on adrenergic receptors to activate them, while others block receptor action. It provides tables listing examples of direct-acting, indirect-acting, and mixed-action adrenergic agonists. The document then discusses specific adrenergic drugs in more detail, including epinephrine, norepinephrine, isoproterenol, dopamine, dobutamine, oxymetazoline, phenylephrine, methoxamine, and clonidine. It explains their structures, receptor selectivities, and physiological effects.
This document discusses the adrenergic system including adrenergic receptors, location and functions of different receptor types, adrenergic drugs, and pharmacological actions. It also covers adrenergic receptor antagonists including classifications of alpha-blockers and beta-blockers, their uses and adverse effects. The key points are: there are alpha and beta adrenergic receptors which are located in various organs and tissues and have different functions; common adrenergic drugs act as pressor agents, bronchodilators or cardiac stimulants; and adrenergic receptor antagonists like alpha-blockers and beta-blockers are used to treat conditions like hypertension, angina, heart failure and gl
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 summarizes a seminar on sympathomimetic drugs presented by Mohd Fahad and guided by Mohd. Khushtar. It discusses different types of adrenergic drugs including direct, indirect, and mixed acting sympathomimetics. It describes the actions of adrenergic drugs on various organs mediated by alpha and beta receptors. Important drugs are discussed in detail including their uses, doses, preparations, and adverse effects. The document provides an overview of adrenergic pharmacology and the therapeutic uses of sympathomimetic drugs.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
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 adrenergic agonists and antagonists. It describes the synthesis, storage, release, and degradation of catecholamines like norepinephrine. It outlines the different subtypes of alpha and beta adrenergic receptors, their locations, and the effects of agonist binding. Key adrenergic drugs like epinephrine, norepinephrine, dopamine, and dobutamine are explained in terms of their mechanisms of action, therapeutic uses, dosages, and adverse effects. Interactions between adrenergic drugs and other medications are also noted.
This document discusses drugs that inhibit the renin-angiotensin system for treating hypertension and other conditions. It describes how ACE inhibitors work by inhibiting the angiotensin converting enzyme and decreasing angiotensin II formation, while also increasing bradykinin levels. Angiotensin receptor blockers competitively block the angiotensin II receptor. Both classes lower blood pressure by vasodilation and reduced sodium retention. They are used to treat hypertension, heart failure, diabetic nephropathy, and myocardial infarction. Adverse effects include hypotension, hyperkalemia, and cough with ACE inhibitors.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
This document outlines a lecture on medicinal chemistry related to the cholinergic system. It will review concepts of acetylcholine mimetics and acetylcholinesterase inhibitors. For muscarinic agonists, it will discuss biosynthesis and metabolism of acetylcholine, structure activity relationship studies of various muscarinic agonists. For acetylcholinesterase inhibitors, it will cover the mechanism of acetylcholine hydrolysis, reversible and irreversible inhibitors, and the antidote for irreversible inhibitors. Learning objectives and resources are also provided.
This document summarizes parasympatholytic drugs, also known as anticholinergic or antimuscarinic drugs. It discusses the pharmacological properties and uses of atropine and scopolamine, which are belladonna alkaloids that act as competitive inhibitors at muscarinic receptors in the parasympathetic nervous system. It also describes newer anticholinergic drugs that have more selective actions, such as ipratropium bromide and tiotropium bromide for bronchodilation in respiratory disorders, and oxybutynin for urinary incontinence.
This document summarizes the classification, mechanisms of action, pharmacokinetics, and clinical uses of α-adrenergic receptor antagonists (α-blockers). It discusses non-selective α-blockers that block both α1 and α2 receptors like phentolamine and phenoxybenzamine, as well as selective α1-blockers like prazosin, doxazosin, tamsulosin, and selective α2-blockers like yohimbine. The major uses of α-blockers include treatment of pheochromocytoma, hypertension, peripheral vascular disease, benign prostatic hyperplasia, migraine, and congestive heart failure. Common side effects include hypotension
The document discusses drugs used to treat congestive heart failure (CHF). It first defines CHF as a condition where the heart cannot pump enough blood to the body's organs. It then discusses the causes of CHF including narrowed arteries, past heart attacks, and high blood pressure. The document focuses on cardiac glycosides, which work by increasing the force of cardiac contraction, as a primary treatment for CHF. It describes the mechanisms of action and pharmacological effects of cardiac glycosides like digitalis on the heart and electrophysiology. Potential adverse drug reactions and drug interactions are also reviewed.
This ppt provides the detailed about the bradykinin and their physiological and pharmacological actions and their generation and their mechanisms in detailed manner.
The document provides an overview of the renin-angiotensin-aldosterone system (RAAS). It discusses the classical components of RAAS including renin, angiotensinogen, angiotensin peptides, angiotensin receptors, and angiotensin converting enzyme. It also covers newer concepts such as local tissue RAAS, intracellular RAAS, receptor heterodimerization, and the roles of angiotensin converting enzyme 2 and angiotensin (1-7). The document highlights functions of RAAS in various organs and pathophysiological processes.
This presentation deals with the use of various drugs in the treatment of heart failure such as Digoxin, ace inhibitors, beta bloockers, calcium channel blockers
This document discusses antihypertensive agents used to treat hypertension. It begins by defining hypertension as blood pressure above 140/90 mmHg. It then discusses the renin-angiotensin-aldosterone pathway which controls blood pressure. Various classes of antihypertensive agents are described, including beta-blockers, ACE inhibitors, calcium channel blockers, and diuretics. Specific drugs from each class are provided along with their mechanisms and uses for treating hypertension. The mechanisms of action are summarized for each drug class, such as how beta-blockers work by blocking epinephrine to slow the heart rate and lower blood pressure.
This document discusses drugs used to treat congestive heart failure (CHF). CHF occurs when the heart cannot pump enough blood to meet the body's needs. Key drugs mentioned include digitalis glycosides like digoxin, which increase the force of heart contractions; diuretics like furosemide that reduce fluid buildup; ACE inhibitors and ARBs that lower blood pressure and prevent further heart damage; and inotropic drugs like dobutamine that strengthen heart contractions. Adverse effects, mechanisms of action, and guidelines for use are provided for several common CHF medications.
Beta-adrenoceptor agonists (β-agonists) bind to β1 and β2 receptors in the heart, blood vessels, and other tissues. In the heart, this increases heart rate, contractility, conduction velocity and relaxation through activation of Gs proteins, cAMP, and downstream targets like calcium channels and myosin phosphorylation. In blood vessels, β-agonists cause smooth muscle relaxation through similar cAMP-mediated inhibition of myosin light chain kinase. Therapeutically, β-agonists are used to treat acute and refractory heart failure as well as circulatory shock by increasing cardiac output and vasodilation.
Sympatholytics, also known as adrenergic antagonists or blocking agents, work in opposition to adrenergic agents by blocking alpha and beta receptor sites. They are classified based on the type of adrenergic receptor they block, including alpha1, alpha2, beta1, beta2, and beta3 receptors. Common alpha blockers include phenoxybenzamine, ergot alkaloids, phentolamine, tolazoline, prazosin, terazosin, doxazosin, and tamsulosin. Common beta blockers mentioned include propanolol, acetabutolol, atenolol, betaxolol, carvedilol, metoprol
This document discusses adrenergic agonists, which are drugs that act on pathways mediated by the endogenous catecholamines norepinephrine and epinephrine. These drugs target various steps in catecholamine synthesis, storage, release, binding, and removal and are used to treat conditions like hypertension, depression, shock, asthma, and angina. Adrenergic agonists are classified as direct-acting if they act directly on receptors, or indirect-acting if they increase catecholamine levels in the synapse. The document also describes the subtypes of alpha and beta adrenergic receptors, their locations, mechanisms of action, and the effects of prolonged receptor stimulation.
The document discusses adrenergic drugs and their mechanisms of action. It notes that some adrenergic drugs act directly on adrenergic receptors to activate them, while others block receptor action. It provides tables listing examples of direct-acting, indirect-acting, and mixed-action adrenergic agonists. The document then discusses specific adrenergic drugs in more detail, including epinephrine, norepinephrine, isoproterenol, dopamine, dobutamine, oxymetazoline, phenylephrine, methoxamine, and clonidine. It explains their structures, receptor selectivities, and physiological effects.
This document discusses adrenergic agonists and antagonists that affect the sympathetic and parasympathetic nervous systems. It describes the main uses and adverse effects of selective and non-selective adrenergic agonists as well as adrenergic antagonists. Specifically, it discusses drugs like epinephrine, phenylephrine, clonidine, isoproterenol, dobutamine, albuterol, salmeterol, formoterol, yohimbine, reserpine, cocaine, methamphetamine, amphetamine, and various beta blockers. It provides information on their mechanisms of action, locations of adrenergic receptors, and controversies regarding their use and safety.
This document discusses adrenergic agonists and antagonists. It begins by classifying adrenergic agonists as direct acting, mixed acting, or indirect acting. It then discusses specific alpha-1, alpha-2, beta-1, and beta-2 adrenergic receptor agonists like phenylephrine, clonidine, dobutamine, and terbutaline. It details their mechanisms of action and clinical indications. The document concludes by discussing classes of adrenergic antagonists including alpha receptor antagonists, beta receptor antagonists, and specific drugs like propranolol, prazocin, and yohimbine.
This document discusses adrenergic drugs and their mechanisms of action. It describes how adrenergic receptors are classified into alpha and beta receptors, which have subtypes. It explains how various drugs like adrenaline, isoprenaline, dopamine, dobutamine, phenylephrine, and alpha methyl dopa act as agonists at these receptor subtypes, and outlines their therapeutic uses and adverse effects. Selective beta-2 agonists like salbutamol are also covered, which are used for conditions like bronchial asthma and premature labor.
Antiadrenergic drugs, also known as alpha blockers or alpha antagonists, work by blocking the effects of adrenaline and other related drugs at receptor sites. They occupy both alpha-1 and alpha-2 adrenergic receptors without activating them. Clinically, they are used to modify the responses of endogenous catecholamines like adrenaline and noradrenaline in both physiological and pathophysiological conditions. Common uses include treating pheochromocytoma, hypertension, Raynaud's disease, and benign prostatic hyperplasia. Individual drugs vary in their selectivity and duration of action at different receptor subtypes. Side effects may include postural hypotension, nasal congestion, and inhibition of ejac
This document discusses catecholamines and their roles in the sympathetic nervous system. It details the pathways of catecholamine synthesis from tyrosine to epinephrine. It describes catecholamine receptors, uptake and metabolism. It lists target organs and effects of norepinephrine, epinephrine, and dopamine. Adrenergic drugs used to stimulate or block catecholamine receptors are also outlined.
This document discusses adrenergic drugs and their mechanisms of action. It describes:
1. The synthesis, action, and fate of norepinephrine in the autonomic nervous system. Norepinephrine is synthesized from tyrosine and stored in vesicles until release.
2. The different types of adrenergic receptors (α and β) and their typical locations. Receptor stimulation activates different signaling pathways.
3. The clinical uses and side effects of various adrenergic drugs that either stimulate or block adrenergic receptors. Drugs like epinephrine and norepinephrine are used to treat low blood pressure and shock. Bronchodilators target β receptors. Antiadrener
This document discusses catecholamines and non-catecholamines used as autonomic drugs. It describes the classifications of autonomic drugs and their mechanisms of action. Specific catecholamines discussed include norepinephrine, epinephrine, isoproterenol, and dopamine. Non-catecholamines discussed include ephedrine, pseudoephedrine, amphetamine, methylphenidate, phenylpropanolamine, and oxymetazoline. Their pharmacological effects, clinical uses, and dosages are summarized for various conditions and species. The document provides an overview of important adrenergic drugs and their mechanisms and applications in veterinary medicine.
This document summarizes the actions and clinical applications of major adrenergic drugs, including:
1) Sympathomimetics like amphetamine and ephedrine act indirectly by releasing catecholamines from neurons, while direct-acting drugs interact directly with adrenoceptors.
2) Sympatholytics include direct-acting antagonists that block adrenoceptors and indirect-acting drugs that interfere with norepinephrine release or synthesis.
3) Adrenergic drugs have applications for conditions like hypotension, shock, asthma, and hypertension. Common side effects include hypotension, tachycardia, and sedation.
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.
This document discusses cholinergic agonists, which are drugs that act on receptors activated by acetylcholine in the autonomic nervous system. It describes the synthesis and mechanisms of acetylcholine as a neurotransmitter. It then discusses various direct-acting cholinergic agonists like bethanechol, carbachol, and pilocarpine and their actions and uses. Pilocarpine is used topically to treat glaucoma by contracting the iris and ciliary muscles. The document also covers indirect agonists known as anticholinesterases, which inhibit the enzyme acetylcholinesterase and thereby increase acetylcholine levels. Physostigmine is an example of a reversible anticholinesterase
This document discusses cholinergic drugs and receptors. It describes two main types of cholinergic receptors - muscarinic and nicotinic receptors. It also classifies cholinergic drugs into direct-acting drugs like choline esters and alkaloids, and indirect-acting drugs that inhibit cholinesterase enzymes. Finally, it provides details on the properties and uses of some choline ester drugs like acetylcholine, bethanechol, carbachol, and methacholine.
The document discusses drugs that affect the autonomic nervous system, including adrenergic agents and adrenergic-blocking agents. It describes how adrenergic agents stimulate the sympathetic nervous system by mimicking norepinephrine and epinephrine. It also discusses the different types of adrenergic receptors, their locations, and their responses to stimulation. Finally, it covers the therapeutic uses, side effects, and interactions of both adrenergic agents and adrenergic-blocking agents.
This document discusses adrenergic receptors and modulators. It describes the sympathetic nervous system and neurotransmitters like norepinephrine, epinephrine, and dopamine. Norepinephrine is stored in synaptic vesicles and released via calcium-dependent fusion. Release can be modulated by prejunctional autoreceptors and heteroreceptors. There are alpha and beta adrenergic receptors which are G-protein coupled and have various effects. Drugs can affect receptors as agonists or antagonists and are used to treat conditions like hypertension and heart failure.
This document discusses the physiology and pharmacology of the sympathetic nervous system and its receptors. It begins by describing epinephrine as an important regulator of heart and vascular responses to exercise and stress. It then defines sympathomimetic drugs as those that mimic epinephrine's actions. The document goes on to detail the different alpha and beta receptor subtypes, their locations, and examples of agonists and antagonists. It discusses sympathetic neurotransmission and the mechanisms of drug-induced effects. Overall, the document provides a comprehensive overview of the sympathetic nervous system and its clinical applications.
This document discusses adrenergic and cholinergic agents. It describes how adrenergic agents stimulate the adrenergic nervous system through catecholamines like norepinephrine and epinephrine or through non-catecholamines. Common adverse effects of adrenergic agents include palpitations, tachycardia, dizziness and tremors. Cholinergic agents act through the parasympathetic nervous system to slow the heart rate, increase GI motility and secretions, and trigger other effects. Common adverse effects of cholinergic agents include nausea, vomiting, diarrhea, dizziness and hypotension. Both agent types require monitoring of vital signs and clients with certain health conditions are
Amphetamine, also known by many street names, is a stimulant drug that can be injected, snorted, smoked, or taken orally in pill form. It is classified as an "upper" that causes both short term effects like increased heart rate and energy, as well as long term risks like heart and brain damage. While amphetamine was first produced in 1887 and found medical uses, it is now illegal without a prescription due to its high potential for abuse and health risks.
Dr. Viraj Shinde's document provides an overview of sympathommimetic drugs. It defines them as drugs that mimic the actions of norepinephrine or epinephrine. It discusses the sympathetic and parasympathetic nervous systems, classification of sympathommimetic drugs, examples like epinephrine, mechanisms of action, therapeutic uses, and adverse effects. Receptor types, locations, agonists, and antagonists are outlined. The document also covers neurotransmitters, their criteria and the neurotransmission process. Specific drugs discussed include dopamine, isoproterenol, dobutamine, fenoldopam, phenylephrine, clonidine, and beta-2 selective agents.
Dr. Viraj Ashok Shinde's document discusses sympathommimetic drugs. It defines them as drugs that partially or completely mimic the actions of norepinephrine or epinephrine. It describes the sympathetic and parasympathetic nervous systems, classifications of sympathommimetic drugs, examples like epinephrine, mechanisms of action, therapeutic uses, and side effects. The summary provides an overview of the key topics covered in the document.
This document discusses sympathomimetic drugs and adrenergic agonists. It describes how sympathomimetics mimic the effects of sympathetic nerve stimulation by acting on adrenergic receptors. It classifies adrenergic agonists as catecholamines or non-catecholamines and discusses their differences. It also summarizes the endogenous catecholamines, their synthesis, storage, and release. Additionally, it provides details on adrenergic receptors and the therapeutic uses, pharmacological actions, and side effects of various adrenergic drugs including epinephrine, dopamine, isoproterenol, dobutamine, ephedrine, and mephenteramine.
The document summarizes the sympathetic nervous system and adrenergic receptors and their ligands. It describes the key neurotransmitter norepinephrine and its receptors (alpha and beta). It then discusses various adrenergic drugs including agonists like epinephrine, norepinephrine, isoproterenol, and antagonists/blockers like phenoxybenzamine, phentolamine, prazosin and their mechanisms and uses.
This document discusses the adrenergic system including synthesis and release of norepinephrine, adrenergic receptors, adrenergic agonists, and specific adrenergic drugs. It describes the two main families of adrenergic receptors, α and β, which are further divided into subtypes. Various adrenergic drugs are discussed including epinephrine, norepinephrine, isoproterenol, dopamine, fenoldopam, dobutamine, oxymetazoline, phenylephrine, clonidine, albuterol/terbutaline, salmeterol/formoterol, mirabegron, and indirect-acting agonists like amphetamine.
This document provides an overview of sympathomimetic drugs, also known as adrenergic drugs. It defines them as drugs that have actions similar to adrenaline or sympathetic stimulation. It classifies them as direct, indirect, or mixed sympathomimetics and discusses examples of each. It then describes their pharmacological actions in detail, focusing on their effects on the cardiovascular system, respiration, eyes, gastrointestinal tract, bladder, uterus, skeletal muscle, central nervous system, and metabolism. Specific drugs discussed include adrenaline, noradrenaline, isoprenaline, dopamine, dobutamine, and phenylephrine. Therapeutic uses and adverse effects are also summarized.
This document discusses adrenergic agonists, which are drugs that activate adrenergic receptors stimulated by norepinephrine or epinephrine. It describes the different types of adrenergic receptors (α1, α2, β1, β2, β3) and the effects of activating each receptor type, such as vasoconstriction, cardiac stimulation, vasodilation, and bronchodilation. It then covers specific adrenergic agonists like epinephrine, isoproterenol, dopamine, phenylephrine, terbutaline, and ephedrine, describing their receptor selectivity, therapeutic uses, and potential adverse effects.
Pharmacology of-vasopressors-and-inotropesCorey Ahmad
The document discusses the pharmacology of vasopressors and inotropes. It describes how these drugs work via the autonomic nervous system, especially on alpha, beta, and dopamine receptors. Adrenaline is discussed as the most commonly used drug and acts on multiple receptor types. Other vasopressors mentioned include ephedrine, methoxamine, metaraminol, and phenylephrine. Inotropes given by infusion include noradrenaline, dopamine, dobutamine, dopexamine, isoprenaline, and phosphodiesterase inhibitors. A clinical case study reviews the use of ephedrine to treat hypotension during a lower segment Caesarean
Sympathomimetic drugs act on adrenergic receptors to mimic the effects of the sympathetic nervous system. Noradrenaline is the major neurotransmitter released by postganglionic sympathetic neurons. Catecholamines such as adrenaline, noradrenaline, and dopamine can be synthesized naturally or synthetically. They are released from neurons via exocytosis and cleared via reuptake or metabolism.
Adrenergic drugs include direct-acting sympathomimetics that activate receptors directly, indirect drugs that promote neurotransmitter release, and mixed drugs. Their effects are mediated via alpha and beta receptors. Common therapeutic uses include treating anaphylaxis, asthma, cardiac issues, and bleeding. Side effects can
Sympathomimetic drugs mimic the actions of norepinephrine and epinephrine by binding to adrenergic receptors. Norepinephrine is the primary neurotransmitter of the sympathetic nervous system and is involved in the "fight or flight" response. It causes various effects such as increased heart rate and blood pressure by constricting blood vessels through activation of alpha-1 receptors and relaxing vessels through beta-2 receptors. Norepinephrine is synthesized from tyrosine in neurons and stored in vesicles for release into synapses.
SYMPATHOMIMTIC AND SYMPATHOLYTICS DRUGS.pptxMsSapnaSapna
Drugs that bind to these receptors and augment the system are called sympathomimetics, while those that bind to these receptors and inhibit or prevent the binding of endogenous ligands are called sympatholytics.
This document describes a learning session on the effects of drugs on the rat cardiovascular system using computer-aided learning (CAL). The objectives are for students to demonstrate and understand the effects of various drugs on hemodynamic parameters in a simulated pithed rat model. The CAL interface allows selection of parameters like arterial blood pressure, left ventricular pressure, and heart rate. Students will demonstrate drug effects, record data, and answer questions to assess their understanding. Examples analyzed include adrenaline, which causes an initial biphasic blood pressure response, and acetylcholine, which produces effects mediated by muscarinic receptors.
The document discusses sympathomimetic drugs, which mimic the effects of sympathetic nervous system stimulation. It defines various adrenergic receptor subtypes and describes their signal transduction pathways. It also explains the mechanisms of action and effects of direct-acting, indirect-acting, and mixed-acting sympathomimetics. Examples are provided of commonly used drugs in each class and their therapeutic applications.
This document provides an overview of inotropes and vasoactive drugs, explaining how they work to increase cardiac output by enhancing contractility, heart rate, preload, and manipulating vascular resistance through their effects on adrenergic receptors and other mechanisms. It discusses various drugs like adrenaline, noradrenaline, dobutamine, vasopressin, GTN, and others, explaining their receptor targets, clinical applications, and nursing considerations for safe administration. The goal is to help nurses better understand these important hemodynamic medications and feel more confident in their use.
Sympathomimetic drugs mimic the actions of norepinephrine and epinephrine by binding to adrenergic receptors. They can be classified as direct-acting agonists like epinephrine, indirect-acting agonists like amphetamines, or mixed-action agonists like ephedrine. Common uses include nasal decongestants, bronchodilators, cardiovascular drugs, and anorectics. Key mechanisms of action involve effects on heart rate, blood pressure, smooth muscles, metabolism and more through alpha-1, alpha-2, and beta-1/beta-2 receptor subtypes.
Sympathomimetic drugs mimic the actions of norepinephrine and epinephrine by binding to adrenergic receptors. They can be classified as direct-acting agonists like epinephrine, indirect-acting agonists like amphetamines, or mixed-action agonists like ephedrine. Common uses include pressor agents, cardiac stimulants, bronchodilators, nasal decongestants, CNS stimulants, and anorectics. Examples discussed in more detail include epinephrine, norepinephrine, dopamine, dobutamine, ephedrine, amphetamines, phenylephrine, and pseudophedrine.
The document discusses the anatomy and function of the sympathetic nervous system. It summarizes that the sympathetic nervous system arises from the thoracolumbar region of the spinal cord and uses acetylcholine and norepinephrine as neurotransmitters. It also classifies adrenoceptors and discusses the effects of activating different receptor subtypes on various organ systems.
The document discusses the anatomy and function of the sympathetic nervous system. It summarizes that preganglionic fibers arise from the thoracolumbar spinal cord and terminate in sympathetic ganglia, while postganglionic fibers arise from the ganglia and innervate organs. It also classifies adrenoceptors and discusses the effects of activating different receptor subtypes. Finally, it summarizes several commonly used sympathomimetic drugs and their mechanisms and effects.
This presentation includes basic of PCOS their pathology and treatment and also Ayurveda correlation of PCOS and Ayurvedic line of treatment mentioned in classics.
The simplified electron and muon model, Oscillating Spacetime: The Foundation...RitikBhardwaj56
Discover the Simplified Electron and Muon Model: A New Wave-Based Approach to Understanding Particles delves into a groundbreaking theory that presents electrons and muons as rotating soliton waves within oscillating spacetime. Geared towards students, researchers, and science buffs, this book breaks down complex ideas into simple explanations. It covers topics such as electron waves, temporal dynamics, and the implications of this model on particle physics. With clear illustrations and easy-to-follow explanations, readers will gain a new outlook on the universe's fundamental nature.
ISO/IEC 27001, ISO/IEC 42001, and GDPR: Best Practices for Implementation and...PECB
Denis is a dynamic and results-driven Chief Information Officer (CIO) with a distinguished career spanning information systems analysis and technical project management. With a proven track record of spearheading the design and delivery of cutting-edge Information Management solutions, he has consistently elevated business operations, streamlined reporting functions, and maximized process efficiency.
Certified as an ISO/IEC 27001: Information Security Management Systems (ISMS) Lead Implementer, Data Protection Officer, and Cyber Risks Analyst, Denis brings a heightened focus on data security, privacy, and cyber resilience to every endeavor.
His expertise extends across a diverse spectrum of reporting, database, and web development applications, underpinned by an exceptional grasp of data storage and virtualization technologies. His proficiency in application testing, database administration, and data cleansing ensures seamless execution of complex projects.
What sets Denis apart is his comprehensive understanding of Business and Systems Analysis technologies, honed through involvement in all phases of the Software Development Lifecycle (SDLC). From meticulous requirements gathering to precise analysis, innovative design, rigorous development, thorough testing, and successful implementation, he has consistently delivered exceptional results.
Throughout his career, he has taken on multifaceted roles, from leading technical project management teams to owning solutions that drive operational excellence. His conscientious and proactive approach is unwavering, whether he is working independently or collaboratively within a team. His ability to connect with colleagues on a personal level underscores his commitment to fostering a harmonious and productive workplace environment.
Date: May 29, 2024
Tags: Information Security, ISO/IEC 27001, ISO/IEC 42001, Artificial Intelligence, GDPR
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A Strategic Approach: GenAI in EducationPeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
Exploiting Artificial Intelligence for Empowering Researchers and Faculty, In...Dr. Vinod Kumar Kanvaria
Exploiting Artificial Intelligence for Empowering Researchers and Faculty,
International FDP on Fundamentals of Research in Social Sciences
at Integral University, Lucknow, 06.06.2024
By Dr. Vinod Kumar Kanvaria
A workshop hosted by the South African Journal of Science aimed at postgraduate students and early career researchers with little or no experience in writing and publishing journal articles.
2. Overview
The study of the sympathetic nervous system is
important from a clinical perspective. The SNS is
involved in controlling heart rate, contractility, blood
pressure, vasomotor tone, carbohydrate and fatty
acid metabolism etc. Stimulation of the SNS occurs in
response to physical activity, psychological stress,
allergies etc. Drugs influencing the SNS are used in
treatment of hypertension, shock, cardiac failure and
arrhythmias, asthma and emphysema, allergies and
anaphylaxis.
3. Sites of Drug Action – Modulation of
Neurotransmission
↓1
2. intake of
precursor
3. synthesis
4. storage
5. metabolism
7. reuptake 6. release 8. degradation
9. receptor
5. Sympathomimetics:
Drugs that mimic or facilitate the actions of the
sympatho-adrenal system.
a) Direct acting:
– Drugs that can act directly or specific adrenergic receptors
– Mimic the effects of NE and Epi
b) Indirect acting:
– Drugs that do not activate the adrenergic receptor directly
i. Facilitate release of NE
ii. Block neuronal uptake of NE
iii. Block metabolism of NE
9. Direct Acting Sympathomimetics:
Ahlquist designated the receptors as α or β based
on observations that catecholamines act on 2
principal receptors:
α1:
Epi ≥ NE >> INE
α2:
β1: INE > Epi = NE
β2: INE > Epi >> NE
14. adverse reactions
1.local ischemia and necrosis
2.acute renal failure
contraindications
HT
In pregnant females, NE should not be
used because it stimulates alpha 1
receptors in the uterus that cause
contraction
15.
16. Effect of NE to intact CVS
Mean arterial pressure
(MAP) = DBP + 1/3 of
(SBP-DBP)
α 1 ,α 2 ,β 1
17. metaraminol (aramine )
Mechanisms: 1.direct actions 2.indirect actions
Characteristics:
1.action is weaker and longer than NA
2.little adverse reactions: renal failure,
arrhythmias
3.stable, im.
4.tachyphylaxis
Uses: substitute for NA in treatment of shock
22. Epinephrine Reversal
(m m H g )
200
180
M e a n Arte ri a l Pre s s u re
160
phenoxybenzamine] 140
120 Epi PBZ
Epi
100
80
0 1 2 3 4 5 6 7 8 9 10
Tim e (re lative )
23. 5.BP
Low doses: β-adrenergic effects predominate
↑ HR, vasodilation of vascular smooth muscle
in skeletal muscle, other smooth muscle
effects
High doses: α-adrenergic effects predominate
Vasoconstriction of blood vessels in skin and
peritoneal cavity
↑ BP and reflex slowing of the heart
(baroreceptor reflex)
24. clinical uses
1. Relief of bronchospasm
2. Relief of hypersensitivity reactions and
anaphylaxis
3. To prolong the duration of action of local
anesthetics.
4. As a topical hemostatic to control superficial
bleeding from skin and mucosae
5. To restore cardiac rhythm in patients with
cardiac arrest.
25. Adverse effects:
Extensions of their effects in the CVS and the
CNS
Anxiety, tenseness, headache and paranoia
tachycardia, dysrhythmias
Large dose IV – cerebral hemorrhage,
pulmonary edema
Route of administration:
Inhalation
Injection (IM, SC, IV), not PO
Topical application
Rapidly degraded
27. Adrenergic Drugs cont’d:
Ephedrine
Acts directly and indirectly
Acts on α and β receptors and causes release of NE
Less potent and longer acting than epinephrine
Available OTC
Orally administered
Clinical use
Bronchodilation
Nasal decongestant
28. α, β,DA-R agonists
dopamine (DA)
Pharmacokinetics:
ivd, MAO/COMT; short t1/2, not across BBB
pharmacological actions
activate DA, α, β1-R
31. Effect of DA to intact CVS
DA1, Beta1
Moderate Dose
32. clinical uses
1.shock
2.chronic heart failure(CHF)
3.acute renal failure(ARF)
toxicity
high doses of DA is similar to that noted above
for NE. Since the drug has an extremely short
half life in plasma, DA toxicity usually disappear
quickly if the administration is terminated.
36. dobutamine
1.selective β1-R agonist
2.inotropic effect>chronotropic effect in
therapeutic dose
3.short-term treatment for CO↓
following cardiac surgery or CHF
caused by AMI
4.tachyphylaxis
37. Clinical Use of Adrenergic Agonists:
α – agonists:
Anaphylactic shock
Hypotension
Nasal congestion
Hemorrhage
Co-administration with local anesthetics
β – agonists:
Congestive heart failure – short term
Asthma – bronchial dilation
Tocolytic – stopping premature labour
39. Epinephrine Reversal
(m m H g )
200
180
M e a n Arte ri a l Pre s s u re
160
phenoxybenzamine] 140
120 Epi PBZ
Epi
100
80
0 1 2 3 4 5 6 7 8 9 10
Tim e (re lative )
40. phentolamine (regitine)
pharmacological actions
1.vessels : vessels dilate; BP ↓
“adrenaline reversal ”
2.heart: excited, CO ↑ HR ↑
a. vessel relaxation>BP ↓, baroreflex (+)
b. alpha2 blockade , NE release↑
3.other effects: cholinergic action
histamine-like action
41. Clinical uses
1.peripheral vasospasmatic disorders
2.local vasoconstrictor excess (eg, NA)
3.diagnosis and treatment of
pheochromocytoma
4.shock
5.CHF and AMI
6.others: male sexual dysfunction
43. tolazoline
The action of blocking α1-R is more
weakly than regitine.
While cholinergic action and histamine-
like action are stronger than regitine.
44. phenoxybenzamine
Pharmacokinetics: only iv, high liposolubility
pharmacological actions:
similar to phentolamine, but slow, strong and
long. it also can block the receptors of 5-HT
and HA.
45. Prazosin
the prototype of a family of potent and very selective
alpha 1 receptor antagonists. It has 1000X greater
affinity for alpha 1 vs alpha 2 receptors.
It blocks all alpha one receptor subtypes
equipotently. It is a short acting drug with a duration
of action of about 7 to 10 hours. Prazosin causes a
decrease in total peripheral resistance, but not an
increase in heart rate (since alpha 2 receptors are not
inhibited).