{"id":45614,"date":"2019-08-02T21:17:27","date_gmt":"2019-08-02T20:17:27","guid":{"rendered":"http:\/\/localhost\/wordpress\/?page_id=929"},"modified":"2019-09-16T08:58:25","modified_gmt":"2019-09-16T08:58:25","slug":"agonists-antagonists-and-drug-toxicity","status":"publish","type":"page","link":"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/","title":{"rendered":"Agonists, Antagonists and Drug Toxicity"},"content":{"rendered":"\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125602\/Cells-dividing-2.jpg);background-position:97% 100%\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:right\">A\/Prof. Ken Rodgers School of Life Sciences<\/h1>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<p style=\"text-align:center\" class=\"has-large-font-size utsbackground-blue\"><strong>Contents<\/strong><\/p>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03113208\/uts-dark-black.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#agonistsandantagonists\">What are agonists and antagonists?<\/a><\/p>\n\n\n\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#affinityvsefficacy\">Affinity vs efficacy<\/a><\/p>\n\n\n\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#partialagonists\">Partial agonists and spare receptors<\/a><\/p>\n\n\n\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#receptorantagonism\">Types of receptor antagonism<\/a><\/p>\n\n\n\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#desensitization\">Desensitization and tachyphylaxis<\/a><\/p>\n\n\n\n<p style=\"text-align:center\" class=\"has-text-color has-very-light-gray-color\"><a href=\"#drugtoxicity\">Drug toxicity<\/a><\/p>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">References<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson, G (2016)&nbsp;<em>Pharmacology<\/em>, 8th Edition, Churchill Livingstone, Sydney.<\/li><li>How drugs act: general principles\u2013 Section 1, part 2<\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"agonistsandantagonists\">What are Agonists and Antagonists?<\/h1>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">What is an agonist?<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>Drug, hormone, toxin, autacoid or neurotransmitter that elicits a biological effect when it interacts with receptors \u2013&nbsp;<strong>bethanechol<\/strong>&nbsp;(used for urinary retention) combines with muscarinic ACh receptor<\/li><li><strong>Bethanechol<\/strong>mimics action of ACh (the neurotransmitter at these receptors)<\/li><li>Magnitude of signal depends on number of receptors occupied and\/or rate of formation of drug-receptor complexes<\/li><li>Signal amplified by intracellular mechanism<\/li><\/ul>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-1 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2022\" height=\"311\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125836\/bethanechol-00.png\" alt=\"\" data-id=\"45740\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/bethanechol-00\/\" class=\"wp-image-45740\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2022\" height=\"311\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125832\/bethanechol-03.png\" alt=\"\" data-id=\"45737\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/bethanechol-03\/\" class=\"wp-image-45737\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2022\" height=\"311\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125833\/bethanechol-02.png\" alt=\"\" data-id=\"45738\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/bethanechol-02\/\" class=\"wp-image-45738\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2022\" height=\"311\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125835\/bethanechol-01.png\" alt=\"\" data-id=\"45739\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/bethanechol-01\/\" class=\"wp-image-45739\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-2 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2208\" height=\"1045\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131018\/nicotinic-011.png\" alt=\"\" data-id=\"45744\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/nicotinic-011\/\" class=\"wp-image-45744\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2208\" height=\"1045\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131017\/nicotinic-021.png\" alt=\"\" data-id=\"45743\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/nicotinic-021\/\" class=\"wp-image-45743\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2208\" height=\"1045\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131015\/nicotinic-031.png\" alt=\"\" data-id=\"45742\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/nicotinic-031\/\" class=\"wp-image-45742\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<h2 class=\"wp-block-heading\" style=\"text-align:left\">What is an antagonist?<\/h2>\n\n\n\n<p>A drug which interacts with a receptor, does not elicit a biological effect and blocks or reverses the effect of an agonist <\/p>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-3 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2135\" height=\"804\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131158\/atropine-01.png\" alt=\"\" data-id=\"45746\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/atropine-01\/\" class=\"wp-image-45746\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2135\" height=\"804\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131200\/atropine-02.png\" alt=\"\" data-id=\"45747\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/atropine-02\/\" class=\"wp-image-45747\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-4 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2129\" height=\"1396\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131321\/receptor-01.png\" alt=\"\" data-id=\"45751\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/receptor-01\/\" class=\"wp-image-45751\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2129\" height=\"1396\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131320\/receptor-02.png\" alt=\"\" data-id=\"45750\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/receptor-02\/\" class=\"wp-image-45750\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2129\" height=\"1396\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131319\/receptor-03.png\" alt=\"\" data-id=\"45749\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/receptor-03\/\" class=\"wp-image-45749\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover aligncenter\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131655\/clearpill.jpg)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"text-align:center\" class=\"has-text-color has-large-font-size has-very-dark-gray-color\"><strong>Agonist v antagonist<\/strong><\/p>\n\n\n\n<p style=\"background-color:#ebebeb\" class=\"has-text-color has-background has-very-dark-gray-color\"><img loading=\"lazy\" decoding=\"async\" width=\"766\" height=\"434\" class=\"wp-image-45754\" style=\"width: 500px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03131806\/agonistvsantagonist.png\" alt=\"\"><\/p>\n\n\n\n<p><\/p>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"affinityvsefficacy\">Affinity vs efficacy<\/h1>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Other definitions 1<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>What is affinity?<\/strong><ul><li>Relative tendency of a drug to combine with its receptor<\/li><\/ul><\/li><li><strong>What is intrinsic activity or efficacy?<\/strong><ul><li>Capacity of a drug to produce a pharmacological effect after binding to its receptor ie the maximal possible effect than can be produced by the drug (E<sub>max<\/sub>)<\/li><\/ul><\/li><li><strong>Agonists possess?<\/strong><ul><li>Affinity and intrinsic activity<\/li><\/ul><\/li><li><strong>Antagonists possess?<\/strong><ul><li>Affinity but lack intrinsic activity<\/li><\/ul><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right\"><figure class=\"wp-block-media-text__media\"><img loading=\"lazy\" decoding=\"async\" width=\"1080\" height=\"562\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132331\/drug-a-b-cell.png\" alt=\"\" class=\"wp-image-45757\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Affinity<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>The response of the cell is a product of&nbsp;affinity&nbsp;and&nbsp;efficacy (intrinsic activity)<\/li><\/ul>\n\n\n\n<ul class=\"wp-block-list\"><li>Drug A&nbsp;fits the receptor better than&nbsp;Drug B<\/li><li>Drug A&nbsp;has a greater&nbsp;affinity&nbsp;for this receptor than&nbsp;Drug B<\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utsbackground-red\"><figure class=\"wp-block-media-text__media\"><img loading=\"lazy\" decoding=\"async\" width=\"1080\" height=\"564\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132330\/cell-response-drug-A-C.png\" alt=\"\" class=\"wp-image-45756\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Intrinsic activity\/efficacy<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>The response of the cell is due to affinity and&nbsp;<\/strong><strong>intrinsic activity<\/strong><\/li><li><strong>Drug C&nbsp;<\/strong><strong>has a greater&nbsp;<\/strong><strong>intrinsic activity<\/strong><strong>&nbsp;at this receptor than&nbsp;<\/strong><strong>Drug A<\/strong><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"partialagonists\">Partial agonists and spare receptors<\/h1>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utspills\" style=\"grid-template-columns:auto 10%\"><figure class=\"wp-block-media-text__media\"><img decoding=\"async\" src=\"http:\/\/localhost\/wordpress\/wp-content\/uploads\/2019\/08\/clear-1024x576.png\" alt=\"\" class=\"wp-image-2271\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"utsblack wp-block-heading\">Other definitions 2<\/h2>\n\n\n\n<ul class=\"utsblack2 wp-block-list\"><li><strong>Partial agonist<\/strong><ul><li>Compound which interacts with a receptor but produces less than the maximum effect \u2013 less intrinsic activity or efficacy. Even with 100% receptor binding it does not produce a maximal response.<\/li><li>Eg.&nbsp;<strong>buprenorphine<\/strong>&nbsp;(partial agonist at \u00b5 opioid receptor) produces less analgesia than&nbsp;<strong>morphine<\/strong>&nbsp;(full agonist)<\/li><\/ul><\/li><li><strong>Spare receptors<\/strong><ul><li>Implied, when the maximum effect is produced with less than 100% receptor occupancy. Requires functional as well as binding studies.<\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132443\/testtubes.jpg)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"color:#000000;text-align:center\" class=\"has-text-color has-large-font-size\">Biased agonism<\/p>\n\n\n\n<p style=\"color:#000000\" class=\"has-text-color utsblack3\">Two agonists bind at the same site on the receptor yet the red agonist is better at evoking response 1 and the green agonist is better at evoking response 2.<\/p>\n\n\n\n<p style=\"text-align:center\"><img loading=\"lazy\" decoding=\"async\" width=\"566\" height=\"717\" class=\"wp-image-45760\" style=\"width: 400px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132529\/biased-agonism.png\" alt=\"\"><\/p>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"receptorantagonism\">Types of receptor antagonism<\/h1>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Type of receptor antagonism<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Competitive<\/strong><ul><li>Compete for the binding site<ul><li>Reversible<\/li><li>Irreversible<\/li><\/ul><\/li><\/ul><\/li><li><strong>Non-competitive (Allosteric modulation)<\/strong><ul><li>Bind elsewhere eg. Ion channel blockers<\/li><\/ul><\/li><\/ul>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-5 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"1089\" height=\"468\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132746\/Type-of-receptor-antagonism-02.png\" alt=\"\" data-id=\"45763\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/type-of-receptor-antagonism-02\/\" class=\"wp-image-45763\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"1089\" height=\"468\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132744\/Type-of-receptor-antagonism-03.png\" alt=\"\" data-id=\"45762\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/type-of-receptor-antagonism-03\/\" class=\"wp-image-45762\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"1021\" height=\"246\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132747\/Type-of-receptor-antagonism-01.png\" alt=\"\" data-id=\"45764\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/type-of-receptor-antagonism-01\/\" class=\"wp-image-45764\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utsclinic\" style=\"grid-template-columns:auto 10%\"><figure class=\"wp-block-media-text__media\"><img decoding=\"async\" src=\"http:\/\/localhost\/wordpress\/wp-content\/uploads\/2019\/08\/clear-1024x576.png\" alt=\"\" class=\"wp-image-2271\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Types of antagonism 1<\/h2>\n\n\n\n<ul class=\"utsblack4 wp-block-list\"><li><strong>Reversible competitive&nbsp;<\/strong><strong>antagonist<\/strong><ul><li>Agonist competes with antagonist for same receptor<\/li><li>\uf0c7&nbsp;[antagonist] progressively inhibits the agonist response<\/li><li>Parallel shift of dose response (DR)-curve to the right and ED<sub>50<\/sub>&nbsp;is altered<\/li><li>But blockade&nbsp;CAN&nbsp;be reversed by a higher dose of agonist<\/li><li>ie the same E<sub>max<\/sub>&nbsp;is reached<ul><li>eg&nbsp;<strong>atropine<\/strong>&nbsp;(<em>muscarinic receptor antagonist<\/em>)<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<ul class=\"wp-block-gallery alignwide columns-1 is-cropped wp-block-gallery-6 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2106\" height=\"1227\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03133001\/reversible-comp-antagonism-01.png\" alt=\"\" data-id=\"45768\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/reversible-comp-antagonism-01\/\" class=\"wp-image-45768\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2106\" height=\"1227\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03132955\/reversible-comp-antagonism-02.png\" alt=\"\" data-id=\"45767\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/reversible-comp-antagonism-02\/\" class=\"wp-image-45767\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2106\" height=\"1227\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03133006\/reversible-comp-antagonism-04.png\" alt=\"\" data-id=\"45769\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/reversible-comp-antagonism-04\/\" class=\"wp-image-45769\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utsbackground-red\" style=\"grid-template-columns:auto 10%\"><figure class=\"wp-block-media-text__media\"><img decoding=\"async\" src=\"http:\/\/localhost\/wordpress\/wp-content\/uploads\/2019\/08\/clear-1024x576.png\" alt=\"\" class=\"wp-image-2271\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Types of antagonism 1<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Reversible competitive&nbsp;<\/strong><strong>antagonist<\/strong><ul><li>Agonist competes with antagonist for same receptor.<\/li><li>Parallel shift of DR-curve to the right and ED<sub>50<\/sub>&nbsp;is altered.<\/li><li>But blockade&nbsp;CAN&nbsp;be reversed by a higher dose of agonist.<\/li><li>The same E<sub>max<\/sub>&nbsp;is reached<ul><li>eg&nbsp;<strong>atropine<\/strong>&nbsp;(<em>muscarinic receptor antagonist<\/em>)<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Types of antagonism 3<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Irreversible competitive<\/strong><strong>&nbsp;antagonist<\/strong><ul><li>Antagonist binds at&nbsp;<strong>same site.<\/strong><\/li><li>Antagonist&nbsp;<strong>dissociates slowly, or not&nbsp;<\/strong>at all, from the receptors \u2013 irreversible bond (eg covalent bond)<\/li><li>No change in the antagonist occupancy takes place when the agonist is applied.<\/li><li>Thus blockade&nbsp;CANNOT&nbsp;be reversed by higher dose of agonist<\/li><li>Prevent agonists from producing any effect \u2013 E<sub>max<\/sub>&nbsp;is&nbsp;\uf0c8&nbsp;but the agonist acts normally at the unoccupied receptors<\/li><li>Thus no shift in DR-Curve ie. no change in ED<sub>50<\/sub>&nbsp;for agonist<ul><li>eg.&nbsp;<strong>methysergide<\/strong>&nbsp;(<em>5-HT receptor antagonist<\/em>) used in R<sub>x<\/sub>&nbsp;of migraine<\/li><li>eg.&nbsp;\u03b1<strong>-neurotoxins<\/strong>&nbsp;from snake venom (<em>nicotinic receptor antagonist<\/em>)<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Types of antagonism 4<\/h2>\n\n\n\n<ul class=\"wp-block-gallery alignwide columns-1 is-cropped wp-block-gallery-7 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"1899\" height=\"1190\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03134115\/irreversible-comp-antagonism-01.png\" alt=\"\" data-id=\"45775\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/irreversible-comp-antagonism-01\/\" class=\"wp-image-45775\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"1899\" height=\"1190\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03134111\/irreversible-comp-antagonism-02.png\" alt=\"\" data-id=\"45774\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/irreversible-comp-antagonism-02\/\" class=\"wp-image-45774\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utspinkpills\" style=\"grid-template-columns:auto 10%\"><figure class=\"wp-block-media-text__media\"><img decoding=\"async\" src=\"http:\/\/localhost\/wordpress\/wp-content\/uploads\/2019\/08\/clear-1024x576.png\" alt=\"\" class=\"wp-image-2271\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\"> Types of antagonism 3 <\/h2>\n\n\n\n<ul class=\"utsblack3 wp-block-list\"><li><strong>Irreversible competitive&nbsp;antagonist<\/strong> <ul><li>Antagonist dissociates slowly, or not at all, from the receptors \u2013 irreversible bond (eg covalent bond)<\/li><li>No change in the antagonist occupancy takes place when the agonist is applied<\/li><li>Thus blockade&nbsp;CANNOT&nbsp;be reversed by higher dose of agonist<\/li><li>Prevent agonists from producing any effect \u2013 E<sub>max<\/sub>&nbsp;is&nbsp;\uf0c8&nbsp;but the agonist acts normally at the unoccupied receptors<\/li><li>Thus no shift in DR-Curve ie. no change in ED<sub>50<\/sub>&nbsp;for agonist<ul><li>eg.&nbsp;<strong>methysergide<\/strong>&nbsp;(<em>5-HT receptor antagonist<\/em>) used in R<sub>x<\/sub>&nbsp;of migraine<\/li><li>eg.&nbsp;\u03b1<strong>-neurotoxins<\/strong>&nbsp;from snake venom (<em>nicotinic receptor antagonist<\/em>)<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Types of antagonism 5<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Non-competitive antagonism or allosteric modulation of receptor function<\/strong><ul><li>Bind at a site close to but distinct from the agonist receptor site<\/li><li>Only have an effect on receptors that are activated<\/li><li>May be an ion channel or G-protein linked to the receptor ie block in receptor-effector linkage since it acts at different site<ul><li>Eg.&nbsp;<strong>suxamethonium<\/strong>(depolarising muscle relaxant)desensitises nicotinic receptor ion channel<\/li><li>Eg.&nbsp;<em>calcium antagonists&nbsp;<\/em>(eg&nbsp;<strong>verapamil<\/strong>&nbsp;and&nbsp;<strong>nifedipine<\/strong>) non-specific block of contractions by other drugs<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n\n\n\n<h2 class=\"wp-block-heading\">Types of antagonism 6<\/h2>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter\"><img loading=\"lazy\" decoding=\"async\" width=\"1289\" height=\"864\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03134622\/non-comp-antagonism6-01.png\" alt=\"non-comp antagonism\" class=\"wp-image-45777\" \/><\/figure><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right utscolor-pills\" style=\"grid-template-columns:auto 10%\"><figure class=\"wp-block-media-text__media\"><img decoding=\"async\" src=\"http:\/\/localhost\/wordpress\/wp-content\/uploads\/2019\/08\/clear-1024x576.png\" alt=\"\" class=\"wp-image-2271\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Types of antagonism 7<\/h2>\n\n\n\n<ul class=\"utsblack3 wp-block-list\"><li><strong>Physiological Antagonism<\/strong><ul><li>Blockade of an effect due to production of an effect in the opposite direction (acts via separate cells or separate physiological systems or opposing receptors)<\/li><li>Eg. In gut \u2013 ACh contraction mediated through muscarinic receptor antagonised by noradrenaline (Nad) relaxation mediated through beta receptor<\/li><\/ul><\/li><li>Weak partial agonists can also seem to be like competitive antagonists<\/li><li>If receptors are constitutively active the addition of a weak agonist can actually decrease receptor activation these are known as \u2018inverse agonists\u2019<\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"desensitization\">Desensitization and tachyphylaxis<\/h1>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Desensitization and tachyphylaxis 1<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>Synonymous terms \u2013 a drug effect which gradually diminishes over a few seconds to minutes<\/li><\/ul>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Causes<\/strong><ul><li>Change in receptors<ul><li>Receptor resulting in tight binding of agonist without opening of ion channel<\/li><\/ul><\/li><li>Exhaustion of mediators<ul><li>Depletion of neurotransmitters or second messengers<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Tolerance&nbsp;(days or weeks to develop)<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li><strong>Causes<\/strong><ul><li>Increased metabolic degradation<ul><li>Induction of metabolic enzymes eg barbiturates\/ethanol in liver<\/li><\/ul><\/li><li>Physiological adaptation<ul><li>Eg. side effects (nausea, sleepiness) sometimes tend to subside<\/li><\/ul><\/li><li>Translocation of receptors (hours)<ul><li>Receptors may be internalised by endocytosis and degraded in lysosomes eg. gonadotrophin-releasing hormone inhibits gonadotrophin release by continuous receptor stimulation (usually pulsatile) used in prostatic cancer.<\/li><\/ul><\/li><\/ul><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/06122811\/UTS-blue-0f4beB.png)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<h1 class=\"wp-block-heading\" style=\"text-align:left\" id=\"drugtoxicity\">Drug Toxicity<\/h1>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull has-media-on-the-right\" style=\"grid-template-columns:auto 24%\"><figure class=\"wp-block-media-text__media\"><img loading=\"lazy\" decoding=\"async\" width=\"542\" height=\"1127\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03134903\/paracelsus.png\" alt=\"\" class=\"wp-image-45780\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Drug toxicity 1<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>\u201c<em>All things are poisons, nothing is without poisonous qualities. It is only the dose which makes a thing a poison<\/em>\u201d<\/li><\/ul>\n\n\n\n<p>Paraphrased from Paracelsus (1493-1541)<\/p>\n\n\n\n<ul class=\"wp-block-list\"><li>Potency provides little information about the dose of drug at which toxic effects manifest themselves<\/li><li>Determined from the LD<sub>50<\/sub>&nbsp;(median lethal dose)<ul><li>Dose of drug that is lethal to 50% of subjects<\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-media-text alignfull\" style=\"grid-template-columns:20% auto\"><figure class=\"wp-block-media-text__media\"><img loading=\"lazy\" decoding=\"async\" width=\"259\" height=\"194\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03134926\/drugsarebad.jpg\" alt=\"\" class=\"wp-image-45782\" \/><\/figure><div class=\"wp-block-media-text__content\">\n<h2 class=\"wp-block-heading\">Drug Toxicity 2<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>Thus therapeutic index (<sup>LD50<\/sup>\/<sub>ED50<\/sub>) gives an idea of the relative margin of safety of a drug<\/li><li>Greater this ratio the safer the drug<ul><li>Must be &gt;1.0 to be therapeutic agent, &lt;2.0 typically see toxicity at therapeutic dose<\/li><\/ul><\/li><li>Therapeutic index:<ul><li><strong>Digoxin<\/strong>&nbsp;(R<sub>x<\/sub>&nbsp;heart failure)= 1.5-2.0, vs.<\/li><li><strong>Penicillin<\/strong>&nbsp;(antibiotic) &gt;100 (non-allergic patients)<\/li><\/ul><\/li><\/ul>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135008\/pink-tablets.jpg)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"text-align:center\" class=\"has-large-font-size\"><img loading=\"lazy\" decoding=\"async\" width=\"1689\" height=\"1145\" class=\"wp-image-45784\" style=\"width: 500px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135137\/therapeutic-index.png\" alt=\"\"><\/p>\n<\/div><\/div>\n\n\n\n<h2 class=\"wp-block-heading\">Drug Toxicity 2<\/h2>\n\n\n\n<ul class=\"wp-block-list\"><li>Thus therapeutic index (<sup>LD50<\/sup>\/<sub>ED50<\/sub>) gives an idea of the relative margin of safety of a drug<\/li><li>Greater this ratio the safer the drug and must be &gt;1.0 to be therapeutic agent, &lt;2.0 typically see toxicity at therapeutic dose<\/li><li>Therapeutic index:<ul><li><strong>Digoxin<\/strong>&nbsp;(R<sub>x<\/sub>&nbsp;heart failure) = 1.5-2.0, vs.<\/li><li><strong>Penicillin<\/strong>&nbsp;(antibiotic) &gt;100 (non-allergic patients)<\/li><\/ul><\/li><li>Depends on therapeutic use \u2013 certain situations (eg. anaesthesia) may require higher dose of drugs than other situations (eg. sedation, sleep)<\/li><li>Since the ED<sub>50<\/sub>&nbsp;goes up while the LD<sub>50<\/sub>&nbsp;remains unchanged, the therapeutic index goes down (ie greater risk of toxicity)<\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<h2 class=\"wp-block-heading\"> Therapeutic Index<\/h2>\n\n\n\n<ul class=\"wp-block-gallery alignfull columns-1 is-cropped wp-block-gallery-8 is-layout-flex wp-block-gallery-is-layout-flex\"><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135419\/therapeuticindex-01.png\" alt=\"\" data-id=\"45795\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-01\/\" class=\"wp-image-45795\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135416\/therapeuticindex-02.png\" alt=\"\" data-id=\"45793\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-02\/\" class=\"wp-image-45793\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135414\/therapeuticindex-03.png\" alt=\"\" data-id=\"45792\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-03\/\" class=\"wp-image-45792\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135417\/therapeuticindex-04.png\" alt=\"\" data-id=\"45794\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-04\/\" class=\"wp-image-45794\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135412\/therapeuticindex-05.png\" alt=\"\" data-id=\"45790\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-05\/\" class=\"wp-image-45790\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135410\/therapeuticindex-06.png\" alt=\"\" data-id=\"45789\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-06\/\" class=\"wp-image-45789\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135423\/therapeuticindex-07.png\" alt=\"\" data-id=\"45798\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-07\/\" class=\"wp-image-45798\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135422\/therapeuticindex-08.png\" alt=\"\" data-id=\"45797\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-08\/\" class=\"wp-image-45797\" \/><\/figure><\/li><li class=\"blocks-gallery-item\"><figure><img loading=\"lazy\" decoding=\"async\" width=\"2205\" height=\"1182\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03135420\/therapeuticindex-09.png\" alt=\"\" data-id=\"45796\" data-link=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/therapeuticindex-09\/\" class=\"wp-image-45796\" \/><\/figure><\/li><\/ul>\n\n\n\n<div style=\"height:100px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03140538\/multiple-samples-blue.jpg)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p class=\"has-text-color has-large-font-size has-very-dark-gray-color utsblack3\">Drug targets: receptors<\/p>\n\n\n\n<p style=\"text-align:center\"><img loading=\"lazy\" decoding=\"async\" width=\"370\" height=\"193\" class=\"wp-image-45804\" style=\"width: 500px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03203901\/drugtargets-receptors.png\" alt=\"\"><\/p>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03140613\/yellowpills.jpg);background-position:54.50000000000001% 100%\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"color:#000000\" class=\"has-text-color has-large-font-size utsblack3\">Drug targets: enzymes<\/p>\n\n\n\n<p style=\"text-align:center\"><img loading=\"lazy\" decoding=\"async\" width=\"370\" height=\"198\" class=\"wp-image-45807\" style=\"width: 500px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03204042\/drugtargets-enzymes.png\" alt=\"\"><\/p>\n<\/div><\/div>\n\n\n\n<div class=\"wp-block-cover alignfull\" style=\"background-image:url(https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/08\/29010756\/doctorCoat.jpg)\"><div class=\"wp-block-cover__inner-container is-layout-flow wp-block-cover-is-layout-flow\">\n<p style=\"color:#000000\" class=\"has-text-color has-large-font-size utsblack3\">Drug targets: enzymes<\/p>\n\n\n\n<p style=\"text-align:center\"><img loading=\"lazy\" decoding=\"async\" width=\"370\" height=\"212\" class=\"wp-image-45809\" style=\"width: 500px\" src=\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03204215\/drugtargets-enzymes02.png\" alt=\"\"><\/p>\n<\/div><\/div>\n","protected":false},"excerpt":{"rendered":"<p>Contents References Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson, G (2016)&nbsp;Pharmacology, 8th Edition, Churchill Livingstone, Sydney. How drugs act: general principles\u2013 Section 1, part 2 What is an agonist? Drug, hormone, toxin, autacoid or neurotransmitter that elicits a biological effect when it interacts with receptors \u2013&nbsp;bethanechol&nbsp;(used for urinary retention) combines with muscarinic ACh [&hellip;]<\/p>\n","protected":false},"author":4934,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"page-template\/generic-template.php","meta":{"_acf_changed":false,"footnotes":""},"class_list":["post-45614","page","type-page","status-publish","hentry"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v26.4 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Agonists, Antagonists and Drug Toxicity - UTS Pharmacology<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Agonists, Antagonists and Drug Toxicity - UTS Pharmacology\" \/>\n<meta property=\"og:description\" content=\"Contents References Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson, G (2016)&nbsp;Pharmacology, 8th Edition, Churchill Livingstone, Sydney. How drugs act: general principles\u2013 Section 1, part 2 What is an agonist? Drug, hormone, toxin, autacoid or neurotransmitter that elicits a biological effect when it interacts with receptors \u2013&nbsp;bethanechol&nbsp;(used for urinary retention) combines with muscarinic ACh [&hellip;]\" \/>\n<meta property=\"og:url\" content=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/\" \/>\n<meta property=\"og:site_name\" content=\"UTS Pharmacology\" \/>\n<meta property=\"article:modified_time\" content=\"2019-09-16T08:58:25+00:00\" \/>\n<meta property=\"og:image\" content=\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/wp-content\/uploads\/sites\/8\/2019\/09\/bethanechol-00.png\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data1\" content=\"6 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/\",\"url\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/\",\"name\":\"Agonists, Antagonists and Drug Toxicity - UTS Pharmacology\",\"isPartOf\":{\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/#website\"},\"primaryImageOfPage\":{\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/#primaryimage\"},\"image\":{\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/#primaryimage\"},\"thumbnailUrl\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/wp-content\/uploads\/sites\/8\/2019\/09\/bethanechol-00.png\",\"datePublished\":\"2019-08-02T20:17:27+00:00\",\"dateModified\":\"2019-09-16T08:58:25+00:00\",\"breadcrumb\":{\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/\"]}]},{\"@type\":\"ImageObject\",\"inLanguage\":\"en-US\",\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/#primaryimage\",\"url\":\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125836\/bethanechol-00.png\",\"contentUrl\":\"https:\/\/wordpress-futures-prod.s3.ap-southeast-2.amazonaws.com\/wp-content\/uploads\/sites\/8\/2019\/09\/03125836\/bethanechol-00.png\",\"width\":2022,\"height\":311},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"Home\",\"item\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Agonists, Antagonists and Drug Toxicity\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/#website\",\"url\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/\",\"name\":\"UTS Pharmacology\",\"description\":\"\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/educationexpress.uts.edu.au\/pharmacology\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-US\"}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"Agonists, Antagonists and Drug Toxicity - UTS Pharmacology","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/educationexpress.uts.edu.au\/pharmacology\/agonists-antagonists-and-drug-toxicity\/","og_locale":"en_US","og_type":"article","og_title":"Agonists, Antagonists and Drug Toxicity - UTS Pharmacology","og_description":"Contents References Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson, G (2016)&nbsp;Pharmacology, 8th Edition, Churchill Livingstone, Sydney. 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