If you find any errors or missing drugs, please e-mail me: cr426@cam.ac.uk, so I can improve the next version.
How to use this spreadsheet: * The tab "Drug List" contains the full and reduced list of drugs of the academic year 2011/12. * Each numbered tab contains one lecture series. By default, the drugs are ordered alphabetically, but you can reorder and filter them by using the autofilter in the most righthand columns named "tag" (little up and down arrows in each cell of the table heading). Alternatively you can use the autofilter on any other columns to filter by anything you wish. * Once you have selected your drugs of interest, you can print the table. Always select the individual pages you'd like to print, otherwise you'll print tens of useless pages. * The very final tab lets you print empty lists so you can test yourself, again by being able to select the subset of drugs you'd like to study. * For a movie on how to use this spreadsheet, check here: http://www.youtube.com/watch?v=TFHI-X0C2ZM
Good luck and a final piece of advice ;-):
QuickTime and a decompressor are needed to see this picture. QuickTime and a decompressor are needed to see this picture. This is the drug list of the academic year 2011/2012.
Black font indicates the drug is on the full list (~334 drugs). Blue font indicates the drug is on the reduced list (~224 drugs). To display the full and reduced lists, use the autofilter on the columns containing numbers. For comparison of the full vs reduced lists sort drugs alphabetically using the autofilter. drugs (full/reduced) 36/25 drugs (full/reduced) 70/55 drugs (full/reduced) 49/36 drugs (full/reduced) 34/25 drugs (full/reduced) 6/6 drugs (full/reduced) 41/27 drugs (full/reduced) 62/50 1 Acetyl-beta- methylcholine/methacholi ne 2 7-nitroindazole [7-NI] 1 Abciximab 1 Amyl Nitrite 1 Ether 1 Adalimumab 24 5-Fluorouracil 2 Adenosine 1 alpha-latrotoxin 2 Acetazolamide 35 Amyl Nitrite 7 Ether 2 Alemtuzumab 1 Aciclovir [acyclovir] 37 Adenosine 71 alpha-latrotoxin 50 Acetazolamide 2 Bisoprolol 2 Etomidate 42 Alemtuzumab 63 Aciclovir [acyclovir] 7 alpha-Bungarotoxin 3 alpha-methyl tyrosine [methyltyrosine] 3 Alteplase 36 Bisoprolol 8 Etomidate 3 Aspirin 2 Amantadine 42 alpha-Bungarotoxin 4 alpha-methyldopa [methyldopa] 51 Alteplase 3 Clofibrate 3 Halothane 43 Aspirin 64 Amantadine 3 Atropine 72 alpha-methyldopa [methyldopa] 33 a-Methylnoradrenaline 37 Clofibrate 9 Halothane 4 Azathioprine 3 Amoxicillin 38 Atropine 5 Amitriptyline 52 a-Methylnoradrenaline 4 Clonidine 4 Nitrous oxide 44 Azathioprine 4 Amphotericin B 4 Bay K 8644 73 Amitriptyline 4 Amiloride 5 Colestyramine 10 Nitrous oxide 5 Chloroquine 65 Amphotericin B 39 Bay K 8644 6 Atenolol 53 Amiloride 38 Colestyramine 5 Propofol 6 Cimetidine 5 Ampicillin 5 Benzilylcholine mustard 74 Atenolol 5 Aminocaproic Acid 6 Doxazosin 11 Propofol 45 Cimetidine 6 Augmentin 40 Benzilylcholine mustard 7 ATP [adenosine triphosphate] 54 Aminocaproic Acid 39 Doxazosin 6 Thiopental 7 Clarithromycin 7 Bacitracin 6 Benzocaine 75 ATP [adenosine triphosphate] 6 Amiodarone 7 Ezetimibe 12 Thiopental 46 Clarithromycin 66 Bacitracin 41 Benzocaine 8 Atracurium 55 Amiodarone 40 Ezetimibe 8 Cromolyn sodium 8 Bleomycin 8 Cholera toxin 76 Atracurium 7 Amrinone 8 Fibroblast Growth Factor 9 Cyclosporin 67 Bleomycin 43 Cholera toxin 9 Atropine 8 Anistreplase 41 Fibroblast Growth Factor 47 Cyclosporin 9 Cephalosporin 9 Danazol 77 Atropine 56 Anistreplase 9 Flecainide 10 Dexamethasone 68 Cephalosporin 10 Diazoxide 10 Benzilylcholine mustard 9 Aspirin 42 Flecainide 48 Dexamethasone 10 Chloramphenicol 11 Diltiazem 13 beta-Bungarotoxin 10 Atenolol 10 Glyceryl Trinitrate 11 Dimenhydrinate 69 Chloramphenicol 44 Diltiazem 80 beta-Bungarotoxin 11 Bisoprolol 43 Glyceryl Trinitrate 49 Dimenhydrinat e 11 Chloroquine 12 d-Tubocurarine 11 Bethanechol 57 Bisoprolol 11 Guanfacine 12 Ergotamine 70 Chloroquine 45 d-Tubocurarine 78 Bethanechol 12 Bosentan 12 Hexamethonium 13 Fexofenadine 12 Ciprofloxacin 13 Ethinylestradiol 12 Botulinum toxins 58 Bosentan 13 Hydralazine 14 Infliximab 71 Ciprofloxacin 46 Ethinylestradiol 79 Botulinum toxins 13 Caffeine 44 Hydralazine 50 Infliximab 13 Cisplatin Professor J. M. Edwardson Pharmacology of Peripheral Neural Transmission Dr C. R. Hiley Drug Interactions with Receptors and Ion Channels Dr R. M. Henderson Cardiovascular and Renal Pharmacology Dr R. M. Henderson Human Cardiovascular and Renal Pharmacology Professor J. M. Edwardson Chemotherapy Dr. R. Murrell- Lagnado Pharmacokinetics and General Anaesthetics Prof P.A. McNaughton Pharmacology of Inflammation and Immunosuppressio Professor J. M. Edwardson Pharmacology of Peripheral Neural Transmission Dr C. R. Hiley Drug Interactions with Receptors and Ion Channels Dr R. M. Henderson Cardiovascular and Renal Pharmacology Dr R. M. Henderson Human Cardiovascular and Renal Pharmacology Professor J. M. Edwardson Chemotherapy Dr. R. Murrell- Lagnado Pharmacokinetics and General Anaesthetics Prof P.A. McNaughton Pharmacology of Inflammation and Immunosuppressio 14 Fludrocortisone 14 Butaxamine/Butoxamine 14 Captopril 14 Hypoxia-inducible Factor-1a (HIF- 1a) 15 Ipratropium 72 Cisplatin 15 Glibenclamide 81 Butaxamine/Butoxamine 59 Captopril 45 Hypoxia-inducible Factor-1a (HIF-1a) 51 Ipratropium 14 Clavulanate 47 Glibenclamide 15 Caffeine 15 Carvedilol 15 Isosorbide Dinitrate 16 Loratidine 73 Clavulanate 16 Isoprenaline 82 Caffeine 16 Clonidine 46 Isosorbide Dinitrate 52 Loratidine 15 Co-trimoxazole 48 Isoprenaline 16 Carbachol 60 Clonidine 16 Ivabradine 17 Mepyramine 74 Co-trimoxazole 17 Lidocaine/lignocaine 17 Carbidopa 17 Clopidogrel 47 Ivabradine 18 Methotrexate 16 Cyclophosphamide 49 Lidocaine/lignocaine 83 Carbidopa 61 Clopidogrel 17 Labetalol 53 Methotrexate 75 Cyclophosphamide 18 Lithium 18 Clonidine 18 Digoxin 48 Labetalol 19 Metoclopramide 17 Daunomycin 19 Mifepristone 84 Clonidine 62 Digoxin 19 Minoxidil 54 Metoclopramid e 18 D-cycloserine 20 Minoxidil 19 Clorgiline [clorgyline] 19 Diltiazem 20 Moxonidine 20 Metronidazole 76 D-cycloserine 50 Minoxidil 85 Clorgiline [clorgyline] 63 Diltiazem 49 Moxonidine 21 mycophenolate 19 Doxorubicin 21 Muscarine 20 Cocaine 20 Dipyridamole 21 Nicorandil 55 Mycophenolate 77 Doxorubicin 22 Nicorandil 86 Cocaine 21 Dobutamine 22 Nicotinic Acid 22 Omalizumab 20 Erythromycin 51 Nicorandil 21 D-amphetamine [dexamfetamine] 22 Duteplase 50 Nicotinic Acid 56 Omalizumab 78 Erythromycin 23 Nicotine 87 D-amphetamine [dexamfetamine] 23 Enalapril 23 Paclitaxel (Taxol) 23 Omeprazole 21 Etoposide 24 Nifedipine 22 Darifenacin 64 Enalapril 51 Paclitaxel (Taxol) 57 Omeprazole 79 Etoposide 52 Nifedipine 88 Darifenacin 24 Eptifibatide 24 Phentolamine 24 Ondansetron 22 Fansidar 25 Norethisterone 23 Decamethonium 65 Eptifibatide 52 Phentolamine 58 Ondansetron 80 Fansidar 53 Norethisterone 24 Dipyridamole 25 Furosemide 25 Pindolol 25 Paracetamol 23 Fluconazole 26 Pertussis toxin 89 Dipyridamole 66 Furosemide 53 Pindolol 59 Paracetamol 81 Fluconazole 54 Pertussis toxin 25 Disulfiram 26 Heparin 26 Prazosin 26 Penicillamine 25 Flutamide 27 Prednisolone 26 Dobutamine 67 Heparin 27 Quinidine 27 Prednisolone 82 Flutamide 55 Prednisolone 90 Dobutamine 27 Hydrochlorothiazide 28 Rosiglitazone 60 Prednisolone 26 Fosfomycin 28 Procaine 27 D-tubocurarine [curare/tubocurarine] 68 Hydrochlorothiazide 54 Rosiglitazone 28 Prednisone 83 Fosfomycin 29 Quinidine 91 D-tubocurarine [curare/tubocurarine] 28 Isobutylmethylxanthine (IBMX) 29 Simvastatin 61 Prednisone 27 Fusidic acid 56 Quinidine 28 Dyflos [diisopropyl fluorophosphate/DFP] 29 Levosimendan 55 Simvastatin 29 Promethazine 84 Fusidic acid 30 QX 314 92 Dyflos [diisopropyl fluorophosphate/DFP] 69 Levosimendan 30 Sirolimus 30 Ranitidine 28 Gentamycin 31 Spironolactone 29 Edrophonium 30 Lignocaine/lidocaine 56 Sirolimus 31 Rofecoxib 29 Gramicidin A 57 Spironolactone 93 Edrophonium 31 Losartan 31 Sodium Nitroprusside 32 Scopolamine 30 Imatinib Professor J. M. Edwardson Pharmacology of Peripheral Neural Transmission Dr C. R. Hiley Drug Interactions with Receptors and Ion Channels Dr R. M. Henderson Cardiovascular and Renal Pharmacology Dr R. M. Henderson Human Cardiovascular and Renal Pharmacology Professor J. M. Edwardson Chemotherapy Dr. R. Murrell- Lagnado Pharmacokinetics and General Anaesthetics Prof P.A. McNaughton Pharmacology of Inflammation and Immunosuppressio 32 Tamoxifen 30 Entacapone 70 Losartan 57 Sodium Nitroprusside 62 Scopolamine 85 Imatinib 58 Tamoxifen 94 Entacapone 32 Mannitol 32 Trimetaphan 33 Sirolimus 31 Isoniazid 33 Tetrodotoxin 31 Ergotamine 71 Mannitol 58 Trimetaphan 63 Sirolimus 86 Isoniazid 59 Tetrodotoxin 32 Guanethidine 34 Milrinone 33 Vascular Endothelial Growth Factor (VEGF) 34 Sulfasalazine 32 Leucovorin 34 Tolbutamide 95 Guanethidine 72 Milrinone 59 Vascular Endothelial Growth Factor 64 Sulfasalazine 87 Leucovorin 35 Tyrphostins 33 Hemicholinium 35 Minoxidil 34 Verapamil 35 Sumatriptan 33 Lomustine 60 Tyrphostins 96 Hemicholinium 73 Minoxidil 18 -Methyldopa 65 Sumatriptan 34 Melarsen 36 Verapamil 34 Hexamethonium 37 Nicotine 36 Tacrolimus 88 Melarsen 61 Verapamil 97 Hexamethonium 74 Nicotine 66 Tacrolimus 35 Melphalan 35 Idazoxan 38 Nifedipine 37 Terfenadine 36 Methicillin 98 Idazoxan 36 Ouabain 39 Theophylline 89 Methicillin 36 Imipramine 75 Ouabain 38 Triamcinolone 37 Methotrexate 99 Imipramine 39 Pimobendan 40 Zafirlukast 90 Methotrexate 37 Isoprenaline 76 Pimobendan 67 Zafirlukast 38 Miconazole 100 Isoprenaline 40 Propranolol 41 Zileuton 91 Miconazole 38 Isosorbide dinitrate 77 Propranolol 68 Zileuton 39 Mitomycin C 39 Labetalol 41 Reserpine 92 Mitomycin C 101 Labetalol 78 Reserpine 40 Mitoxantrone 40 L-NIO [N-iminoethyl-L-ornithine] 42 Saralasin 93 Mitoxantrone 41 L-NMMA 79 Saralasin 41 Nevirapine 102 L-NMMA 43 Sildenafil 94 Nevirapine 42 Malathion 80 Sildenafil 42 Penicillin 103 Malathion 44 Spironolactone 95 Penicillin 43 Mecamylamine 45 Streptokinase 43 Polymixin 104 Mecamylamine 81 Streptokinase 44 Prednisone 44 Methacholine 46 Tirofiban 96 Prednisone 45 Muscarine 82 Tirofiban 45 Pyrimethamine 105 Muscarine 47 Tranexamic Acid 97 Pyrimethamine 46 Neostigmine 83 Tranexamic Acid 46 Rifampin 106 Neostigmine 48 Triamterene 98 Rifampin 47 Nicotine 84 Triamterene 47 Saquinavir 107 Nicotine 49 Warfarin 99 Saquinavir 48 Nitroglycerin [glyceryl trinitrate] 85 Warfarin 48 Streptomycin 108 Nitroglycerin [glyceryl trinitrate] 100 Streptomycin 49 Octopamine 49 Sulfadoxin 50 Pancuronium 101 Sulfadoxin 109 Pancuronium 50 Sulfamethoxazole Professor J. M. Edwardson Pharmacology of Peripheral Neural Transmission Dr C. R. Hiley Drug Interactions with Receptors and Ion Channels Dr R. M. Henderson Cardiovascular and Renal Pharmacology Dr R. M. Henderson Human Cardiovascular and Renal Pharmacology Professor J. M. Edwardson Chemotherapy Dr. R. Murrell- Lagnado Pharmacokinetics and General Anaesthetics Prof P.A. McNaughton Pharmacology of Inflammation and Immunosuppressio 51 Phenoxybenzamine 102 Sulfamethoxazole 52 Phentolamine 51 Suramin 110 Phentolamine 103 Suramin 53 Phenylephrine 52 Tamoxifen 111 Phenylephrine 104 Tamoxifen 54 Pilocarpine 53 Taxol 112 Pilocarpine 105 Taxol 55 Pirenzepine 54 Tetracycline 56 Pralidoxime 106 Tetracycline 113 Pralidoxime 55 Topotecan 57 Prazosin 56 Trifluridine 114 Prazosin 57 Trimethoprim 58 Propranolol 107 Trimethoprim 115 Propranolol 58 Valinomycin 59 Reserpine 108 Valinomycin 116 Reserpine 59 Vancomycin 60 Salbutamol 109 Vancomycin 117 Salbutamol 60 Vinblastine 61 Selegiline 110 Vinblastine 118 Selegiline 61 Zanamivir 62 Sildenafil 111 Zanamivir 119 Sildenafil 62 Zidovudine (azidothymidine, AZT) 63 Suxamethonium 112 Zidovudine (azidothymidine, AZT) 120 Suxamethonium 64 Tetanus toxin 121 Tetanus toxin 65 Tranylcypromine 122 Tranylcypromine 66 Trimetaphan 67 Tyramine 123 Tyramine 68 Vesamicol 124 Vesamicol 69 Xylazine 125 Xylazine 70 Yohimbine Contents of Hiley Lecture series on Receptors and Ion channels: (not in exact order) - ligand-binding (important for the practical exam) this section contains mainly ACh-R relating drugs, which are mostly repeated again in 2nd lecture series - info on ligand receptors in general - hormone receptor drugs - tyrosine kinase receptor drugs - ion channel drugs: Na+, Ca2+, K+ - TOXINS (please see separate tab for a list of all toxins) Legend * to do with acetylcholine * to do with hormone receptors * to do with Na+ receptors * to do with K+ receptors * to do with Ca2+ receptors
Filtering Hiley: Drug Interactions with Receptors and Ion Channels p Drug Class Target Mechanism of Action Points of Interest Application Indicatio n Side- effects Metabolism p.24 Bay K 8644 DHP Voltage-sensitive Ca2+ channel (L-type) 0 * highly lipid soluble as aromatic * favours mode 2 (open) same binding site as nifedipine p.24 Amlodipine DHP Voltage-sensitive Ca2+ channel (L-type) Antagonist * highly lipid soluble as aromatic * favours mode 0 (closed) * Calcium antagonist p.24 Nifedipine DHP Voltage-sensitive Ca2+ channel (L-type) Antagonist (of Bay K 8644) * highly lipid solumble as aromatic * favours mode 0 (closed) therefore more active on vascular Ca2+ channels where inactive channels predominate due to different resting potential (less -ve) * Calcium antagonist * more effect on vascular smooth muscle * reflex tachycardia p.25 Diltiazem (IV) benzo- thiazepine Voltage-sensitive Ca2+ channel (L-type) Antagonist * rate neutral * more effect on smooth muscle in comparison to Verapamil * Calcium antagonist * rate neutral * side- effects from vasodilation: flushing, headache * well absorbed in GI --> given by mouth * extensively metabolised p.25 Verapamil (IV) phenylalkyla mine Voltage-sensitive Ca2+ channel (L-type) blocker * slows heart rate * negative inotropic action * USE-dependent block * Calcium antagonist * affects heart muscle more than vasculature * by mouth *SVT but Adenosine used instead * AV block and cardiac slowing but reflexes act against * constipation Ca2+ antagonists: block entry of Ca2+ from extracellular, rather than ER Vaughan williams classification of disarrhythmics **SUR/K+ antagonists: ATP/ADP ratio determines the KATP channel activity normal: K+ out if glucose up, ATP up, less K+ out, --> depolarisation! depolarisation causes insulin release!!!!!!!! Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Clearance tag1 tag2 tag3 Ca 1 Ca 2 Ca 3 Ca 4 Ca 5 Contents of Edwardson Lecture series on Peripheral Neural Transmission: This is one of THE MOST IMPORTANT lecture series of the course, it is also very important for the practical. - cholinergic transmission
- noradrenergic transmission
- non-cholinergic and non-adrenergic (NANC) transmission
Legend * to do with ACh transmission * to do with NA transmission * to do with NO * to do with nucleotides
To visualise the individual groups of drugs, filter by the custom filter of the "tag1" column on the far right, then sort by "tag2", etc... Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Professor Edwardson: Pharmacology of Peripheral Neural Transmission p Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects p.2 8 Adrenaline alpha and beta adrenoR (non- selective) agonist * alpha > beta * anaphylactic shock, increase TPR and reduce bronchospasm p.2 9 Atenolol beta1 adrenoR (little bit beta2) antagonist * pretty beta1 selective p.2 6 c Bisoprolol beta1 adrenoR antagonist * third generation * chronic heart failure * over- inhibition p.2 8 Butaxamine /Butoxamine beta1 and beta2 adrenoR antagonist * pretty beta2 selective * beta2 > beta1 p.2 9 Phenoxybenzamine alpha adrenoR (non-selective) irreversible antagonist * for preparation of patients with phaeochromocytoma for surgery as tumour may secrete high amounts of amines * alpha1 = alpha2 * postural hypertension p.2 8 Noradrenaline alpha and beta adrenoR (non- selective) agonist beta2<beta1/alpha2<alph a1 p.2 9 Phentolamine alpha adrenoR antagonist * non-selective * obsolete * alpha1 = alpha2 * antihypertensive * learge increase in HR (reflex tachycardia) * postural hypertension p.2 8 / p.2 5 c Dobutamine beta1 adrenoR agonist * use per IV * inotropic > chronotropic * used in acute cardiogenic shock * shock * inc O2 demand * inc HR -> arrthythmias * hypertension p.2 6 C Carvedilol alpha1, beta1 beta2 adrenoR antagonist * third generation * third generation * chronic heart failure * over- inhibition p.2 3 Octopamine sympathomi metic amine alpha and beta adrenoR (non- selective) very weak agonist * metabolyte of tyramine p.2 8 Labetalol alpha1, beta1 and beta2 adrenoR antagonist * four isomers with different actions * does not bind alpha2 R * treat hypertension in pregnancy p.2 8 Methyl NA alpha adrenoR agonist p.2 6 Isoprenaline similar to adrenaline beta adrenoR non-selective agonist * was used in asthma but side-effects * increased HR from beta1 stim p.5 h Doxazosin alpha1 and alpha2 adrenoR antagonist * alpha1 selective * hypertension * causes vasodil in resistance and capacitance vessels * less tachycardia than non-selectives * postural hypertension * impotence p.2 9 Ergotamine alpha adrenoR, 5-HT R partial agonist * migraine * St Anthony's fire = intense peripheral vasoconstriction (when ingested eating ergo- infected cereals) p.2 8 Phenylephrine alpha1 and beta1 adrenoR agonist * alpha1 selective * raise blood pressure in acute hypotension p.2 7 Prazosin alpha1 and alpha2 adrenoR antagonist * alpha1 selective * hypertension * causes vasodil * less tachycardia than non-selectives * postural hypertension * impotence p.(3 )2 Caffeine alpha1 adrenoR antagonist, potentiates cAMP signalling * most efficient after prolongued wakefulness * also breaks down inhibits phosphodiesterase which breaks down cyclic nucleotides p.2 6, p.2 8 Clonidine alpha2 and alpha1 adrenoR agonist * alpha2 > alpha 1 * anti-hypertensive agent * can lead to rebound hypertension if dose omitted p.2 8 Idazoxan synthetic yohimbine alpha2 and alpha1 adrenoR antagonist * alpha2 selective * experimental * postural hypertension p.5 h Pindolol beta adrenoR partial agonist / antagonist * mild effects on CO * beta blocker p.2 8 Xylazine alpha2 adrenoR agonist * alpha2 > alpha1 p.2 9 Propranolol beta adrenoR antagonist * beta1 = beta 2 * beta blocker p.2 8 Salbutamol beta2 adrenoR agonist * beta2 > beta 1 p.6 h Guanfacine alpha2 adrenoR agonist * more potent than clonidine but less efficacy as hypertensive agent * postural hypertension p.2 8 Yohimbine alpha1, alpha2 adrenoR antagonist * alpha2 > alpha1 * experimental * postural hypertension *sympathetic* side effects: exc. on CNS, urinary retention, sm. muscle relaxation, inh. on GI, dilated pupil, decrease in near vision, dry mouth, tachycardia, BP unaffected Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Metabolism Clearance tag 1 tag 2 tag 3 tag 4 adreno alpha, beta 1 ag adreno beta 5 ant adreno beta 6 ant adreno beta 7 ant adreno alpha 1 ant adreno alpha, beta 2 ag adreno alpha 2 ant adreno beta 6 ag adreno alpha, beta 3 ant adreno alpha, beta 3 ag adreno alpha, beta 4 ant adreno alpha 4 ag adreno beta 5 ag adreno alpha 5 ant adreno alpha 5 ag adreno alpha 6 ag adreno alpha 6 ant misc, adreno 16, alpha 7 ant adreno alpha 7 ag adreno alpha 8 ant adreno beta 2 ag/ant adreno alpha 8 ag adreno beta 1 ant adreno beta 7 ag adreno alpha 9 ag adreno alpha 9 ant exc. on CNS, urinary retention, sm. muscle relaxation, inh. on GI, dilated pupil, decrease in near vision, dry mouth, tachycardia, BP unaffected Contents of Henderson Lecture series on Cardiovascular and Renal Pharmacology: This lecture series starts out feeling quite repetitive, but it still contains quite a lot of info to absorb. My advice would be not to underestimate it! It covers roughly three types of drugs - drugs to with the heart and circulation
- drugs to do with blood coagulation (I recommend studying these alongside the cardiovascular handout of the Pathology lecture series) - renal drugs
Legend * heart * kidney * blood
To visualise the individual groups of drugs, sort by the custom filter of the "tag1" column on the far right, then sort by "tag2", etc... Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Henderson: Cardiovascular and Renal Pharmacology p Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects Metabolism Clearance p.29 Abciximab receptor that binds vitronectin R on platelets * integrin antagonist * inhibits GpIIb/IIIa glycoprotein receptors on platelets that bind fibrinogen for subsequent conversion to fibrin by thrombin! * prevents fibrinogen bridging between platelets and adhesion * clot lysis * used with coronary angioplasty p.38 Acetazolamide inhibits carbonic anhydrase * blocks NaHCO3 reabsorption * first used as diuretics now obsolete * inhibit production of acqueous humour in glaucoma * altitude sickness p.41 Aliskiren renin inhibitor Allopurinol - p.29 Alteplase plasminogen activator * clot lysis a-methyl- NA - p.36 Amiloride K+sparin g blocks apical Na+ ch in DCT * prevent Na+ reabs in DCT * K+ sparing diuretic p.30 Aminocaproic acid similar to lysine inhibits plasminogen activation REVERSE clot lysis if bleeding * inhibit clot lysis p.22 Amiodarone * beta-blocker and K+-ch blocker-like actions in nodes * resembles thyrroid hormone -> toxicity * class III anti- dyshythmic * thyrroid problems Amrinone - p.29 Anistreplase combination of plasminogen and anisoylated streptokinase * more prolonged activity than streptokinase * clot lysis p.29 Aspirin COX inhibitor * anti platelet p.36 Bendroflumet hiazide thiazide block Na/Cl cotransport * prevent Na+ reabs in DCT * inhibit formation of diluated urine * act in thick ascending limb or distal tubule * bind to Cl- site * diuretic * similar to loop-diuretics (milder) but retain Ca2+, good for osteoporosis * erectile dysfunction! p.26 Bisoprolol adreno receptor antagonist * third generation * chronic heart failure * over- inhibition p.28 Bosentan endothelin receptor antagonist * non-specific * pulmonary hypertension p.35 Bumetanide sulfon- amide NKCl2 co- transporter in LOH * prevent Na+ reabs in LOH * loop diuretic p.(3 )2 Caffeine methyl- xanthine alpha1 adrenoR antagonist, potentiates cAMP signalling * most efficient after prolongued wakefulness * also breaks down inhibits phosphodiesterase which breaks down cyclic nucleotides p.27 Caffeine methyl- xanthine non-selective phosphodiester ase, adenosine R non-selective inhibitor, antagonist * +ve chronotropic and inotropic effect * disrhythmias p.41 Captopril ACE inhibitor * reduce vascular resistance * hypertension * heart failure p.26 Carvedilol adreno receptor antagonist * third generation * chronic heart failure * over- inhibition p.29 Clopidogrel inhibitor of platelet aggregation * anti platelet Dabigatran - p.24 Digoxin cardiac glycoside Na+/K+ ATPase inhibitor * inc IC (Na+) by 1- 1.5mM only but Ca2+ depends on Na+^3! * produce +ve inotropic effect without an inc requirement for O2 * stimulates vagus by central action => also antidysrhythmic * used to strengthen the heart beat * now more dysrrhythmia than heart failure via depression of the vagus *affects synaptic neuro- transmission * bigeminy (premature beat) * watch when combined with diuretics as side- effects worse when K+plasma low! p.5 Diltiazem Diltiazem (IV) benzo- thiazepine Voltage-sensitive Ca2+ channel (L-type) Antagonist * rate neutral * more effect on smooth muscle in comparison to Verapamil * Calcium antagonist * rate neutral * side-effects from vasodilation: flushing, headache * well absorbed in GI --> given by mouth * extensively metabolised p.27 Dipyridamole phosphodiester ase type V inhibit cAMP breakdown * also inhibits adenosine reuptake p.26 Dobutamine beta1 adreno receptor agonist b1 agonist * use per IV * inotropic > chronotropic * shock * inc O2 demand * inc HR -> arrthythmias * hypertension p.29 Duteplase plasminogen activator * clot lysis p.41 Enalapril ACE inhibitor p.30 Eptifibatide cyclic heptapept ide inhibitor cyclic heptapeptide inhibitor * integrin antagonist * inhibits GpIIb/IIIa glycoprotein receptors on platelets that bind fibrinogen for subsequent conversion to fibrin by thrombin! * prevents fibrinogen bridging between platelets * clot lysis p.22 Flecainide Na+ channel inhibitor * class IC p.35 Furosemide sulfon- amide NKCl2 co- transporter in LOH * prevent Na+ reabs in LOH * acts in <10 mins * unexplained vasodil. Effect * weak carbonic anhydrase inhibitors * bind to Cl-site * loop diuretic * heart failure * pulmon. Oedema * cirrhosis + ascites * renal failure * hypokalaemia * hypovolaemia * metabolic alkalosis * gout * kidney failure p.30 Heparin naturally occuring, glycosami no glycan = poly- saccharid e activates antithrombin III (ATIII) prevents thrombin formation * causes confo change in ATIII * inhibition of Xa * lack of thrombin activation * has to be given by injection * inhibits blood clotting cascade * unstable angina, after MI, DVT p.36 Hydrochloroth iazide thiazide block Na/Cl cotransport * prevent Na+ reabs in DCT * diuretic [.27 Isobutylmethyl xanthine non-selective phosphodiester ase inhibitors * similar to caffeine p.27 Levosimendan calcium sensitiser troponin enhances Ca2+ binding * not licensed in UK * also cause vasodilatation * heart failure * used in humans p.5 Lidocaine/lign ocaine Lidocain e/lignocai ne (Ib) Amineester Voltage-sensitive Na+ channel physically blocks channel: stabilises inactivated state * weak base (+active, neutral can cross membrane, active from inside) * inhibits C and Ad fibres best (=small) * use-dependent at high rates of stimulation * local anaestetic * antiarrhythmic * used for neuropathic pain * can give per IV * CNS * cardio- vascular * amides metabolised in liver p.41 Losartan non- peptide angiotensin II antagonist, angiotensin receptor blockers (ARBs) * blocks AT1 R * acts on AT1 R * hypertension Lovastatin - p.39 Mannitol acts by osmosis * retains water in tubule * osmotic diuretic p.27 Milrinone phosphodiester ase type III inhibit cAMP breakdown * dysrhythmias Minoxidil - p.5 Nifedipine Nifedipin e DHP Voltage-sensitive Ca2+ channel (L-type) Antagonist (of Bay K 8644) * highly lipid solumble as aromatic * favours mode 0 (closed) * Calcium antagonist * more effect on vascular smooth muscle * reflex tachycardia p.24 Ouabain cardiac glycoside Na+/K+ ATPase inhibitor Phenytoin - p. 27 Pimobendan calcium sensitiser increase Ca2+ sensitivity, inhibits phosphodiester ase III * inodilator * peripheral vasodilator * calcium sensitiser of troponin * used in animals p.36 Probenecid uric acid transporter in distal tubule inhibits uric acid reabsorption * gout p.17 Propranolol beta adrenoR antagonists * beta blocker * beta1 = beta 2 p. 22 Quinidine (Ia) Ester Voltage- sensitive Na+ channel physically blocks channel * use-dependent at low rates of stimulation * local anaestetic * antiarrhythmic * CNS * cardio- vascular * esters rapidly hydrolysed by esterases p.43 Reserpine VMAT-2 (vesicular monoamine transporter) inhibits VMAT, causes depletion of NA sture * acts in periphery and theb rain * recovery requires synthesis of new vesicles * profound psychological depression * anti- hypertensive! misc Reteplase - p.41 Saralasin peptide Antiogensin II partial agonist * not suitable for oral administration p.27 Sildenafil phosphodiester ase type V (downstream of NO) inhibit cAMP breakdown * breaks down cGMP (downstream product of NO!) viagra! Sotalol - p.37 Spironolacton e K+sparin g aldosterone antagonist * binds aldosteroneR * metabolite canrenone has activity * slow onset * K+ sparing diuretic * more antihypertensiv e than diuretic * prevent hypokalaemia * hyperkalaemia * gynecomastia, menstrual disorders, testicular atrophy p.29 Streptokinase streptococ cal protein binds to plasminogen activator causes plasmin generation to degrade fibrin clots * clot-lysis p.27 Theophylline methylxa nthine phosphodiester ase, adenosine R non-selective inhibitor, antagonist * +ve chronotropic and inotropic effect * disrhythmias p.29 Tirofiban non- peptide clotting cascade * integrin antagonist * inhibits GpIIb/IIIa glycoprotein receptors on platelets that bind fibrinogen for subsequent conversion to fibrin by thrombin! * prevents fibrinogen bridging between platelets * can be used like heparin * clot lysis p.30 Tranexamic Acid aminocap roic acid analogue inhibits plasminogen activation REVERSE clot lysis if bleeding * analogue of aminocaproic acid * inhibit clot lysis p.37 Triamterene K+sparin g blocks apical Na+ ch in DCT * prevent Na+ reabs in DCT * K+ sparing diuretic p.5 Verapamil phenylalk ylamine Voltage- sensitive Ca2+ channel (L-type) blocker * slows heart rate * negative inotropic action * Calcium antagonist * affects heart muscle more than vasculature * by mouth *SVT but Adenosine used instead * AV block and cardiac slowing but reflexes act against * constipation p.30 Warfarin inhibits syn of II, VII, IX and X prevents thrombin formation vitamin K antagonist * can be given orally * monitor INR * inhibits blood clotting cascade * similar to heparin * given with AF and after prostetic valve Xylazine - Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. tag1 tag2 tag3 tag 4 tag 5 blood 5 kidney 8 kidney 13 left out left out blood 6 left out kidney 5 blood 12 heart no left out left out blood 7 blood 1 kidney 3 heart no heart single kidney 1 inodil 1 heart inodil 2 kidney 10 heart blood 2 left out left out heart CG heart no heart inodil 6 heart no blood 8 kidney 11 blood 3 kidney 2 blood 10 kidney 4 heart inodil 4 heart inodil 9 heart no kidney 14 left out left out kidney 9 heart inodil 5 no heart no heart CG left out heart inodil 8 kidney 15 heart no heart no heart no left out kidney 12 heart inodil 7 left out kidney 7 blood 9 heart inodil 3 blood 4 blood 13 kidney 6 heart no blood 11 left out Contents of Edwardson Lecture series on Human Aspects of Cardiovascular and Renal Pharmacology: Again, don't underestimate this lecture series. This table only contains NON-REDUNDANT drugs. The drugs acting on NO have been combined with those of lecture series 1 and can be found in the "Drug Receptor Interaction" tab.
- drugs that lower blood lipids and cholesterol - angina drugs Please also download the separate "Cardiovascular and Renal Drug" overview from the website. Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Henderson: Human aspects of cardiovascular and renal pharmacology p Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects Metabolism Clearance p.12 Clofibrate fibrate activates lipoprotein lipase lowers VLDL and LDL * lower blood cholesterol * hypertension p.10 Simvastatin statin inhibits HNG- CoA reductase inhibits cholesterol synthesis * pleiotropic = many beneficial effects * lower blood cholesterol * hypertension p.12 Rosiglitazone activates PPAR-gamma promotes cholesterol- uptake from periphery via LXR and ABCA1 * lower blood cholesterol * used in T2DM!!!! * hypertension p.13 Colestyramine anion exchange resin prevents bile re-uptake from small intestine * lower blood cholesterol * hypertension p.13 Ezetimibe intestinal sterol transporter inhibits cholesterol absorption * circulates entero- hepatically, repeated action * lower blood cholesterol * hypertension p.13 Fish oil reduces hypertriglycer inaemia prevents platelet aggregation * lowers blood triglycerides * contains unsaturated FA that affect eicosanoids * hypertension p.7 Hydralazine unknown smooth muscle relaxant * only short term effect * in 3rd world as cheep * hypertension p.13 Nicotinic Acid inhibits triglyceride production and VLDL secretion * lower blood cholesterol * hypertension p.6 Moxonidine imidazoline imidazolineR * GPCR activation leading to generation of diacylglycerol and arachidonic acid *sympatholyti c * hypertension * fewer than alpha2 agonists Ivabradine HCN channel * slows HR * angina * much fewer than beta- blockers Fibroblast Growth Factor * induce angiogenesis * angina Hypoxia- inducible Factor-1a (HIF-1a) * induce angiogenesis * angina Vascular Endothelial Growth Factor * induce angiogenesis * angina p.18 Paclitaxel (Taxol) * coat stent to prevent neointimal proliferation * angina p.18 Sirolimus * coat stent to prevent neointimal proliferation * angina tag 1 tag 2 tag 3 blood lipids/chol 1 angina, blood lipids/chol 6 2 blood lipids/chol 3 blood lipids/chol 4 blood lipids/chol 5 blood lipids/chol 6 blood lipids/chol 8 blood lipids/chol 9 blood lipids/chol? 10 angina 1 angina 2 angina 3 angina 3 angina 5 angina
Contents of Murrell-Lagnado lecture series on Anaesthetics.
Thankfully only 7 drugs to learn here!
Dr M-L Anaesthetics p Drug Class blood/gas partition coefficient oil/gas partition coefficien Points of Interest Application Indication Side-effects Metabolism Clearance p.2 f Nitrous oxide volatile 0.47 1.4 * very fast induction and recovery * least potent * requires highes partial pressure to achieve anaesthesia * more suitable for maintenance * generally not much metabolism * exhalation via the lungs p.2 f Halothane volatile 2.4 220 * effect blocked by mutations in the GABAaR a-subunit * S270W mutation abolishes effect * also enhancement of Gly receptor currents * pore-domain K+channels TREK1 * generally not much metabolism * exhalation via the lungs p.2 f Ether volatile 12 65 * hangover * generally not much metabolism * exhalation via the lungs p.9 Methoxy- fluorane volatile 13 950 * slow induction and recovery * most potent * requires lowest partial pressure for anaesthesia * severe hangover * generally not much metabolism * exhalation via the lungs Drug Class Target Mechanism Points of Interest Application Indication Side-effects Metabolism Clearance p.2 f Etomidate IV GABAaR (amongst others) * enhance inhibitory GABAa receptor currents * more recent * prefers b2 and b3 subunit * more suitable for induction * generally by liver * more rapidly than thiopentone p.2 f Propofol IV GABAaR (amongst others) * enhance inhibitory GABAa receptor currents * more recent * prefers b subunits * N265M mutation reduces susceptibility to anaesthetics and corresponding loss of reflexes * maintenance as well as induction, but IV rate must be adjusted frequencly * generally by liver * more rapidly than thiopentone p.2 f Thiopental/ Thiopentone IV, barbiturat e * introducted in 1930's * causes unconsciousness in 20s for 5-10mins (rapid onset and short lived) * main example to explain redistribution phases * generally by liver tag 1 2 3 4 5 6 7 Contents I found it useful to read this lecture series alongside the corresponding Path and Neuro lectures. - drugs to do with histamine receptors - drugs to do with serotonin receptors - NSAIDs - corticosteroids - anti - anti - immunosuppressive drugs p p.21 p.21 p.10 ? p.23 p.16 p.22 p.18 p.22 p.18 p.7- 9 p.11 p.7- 9 p.22 p.18 p.21 p.18 p.7- 9 p.7- 9 p.22 p.10 p.22 p.21 p.10 p.22 p.10 p.20 p.7- 9 p.23 p.10 p.23 p.20 p.22 p.11 p.22 p.7- 9 p.20 p.20 p.11 p.20 p.20 Contents of McNaughton Lecture series on Inflammation: I found it useful to read this lecture series alongside the corresponding Path and Neuro lectures. - drugs to do with histamine receptors - drugs to do with serotonin receptors - NSAIDs - corticosteroids - anti-asthma drugs - anti-rheumatic drugs - immunosuppressive drugs Legend * histamine H1R drugs * histamine H2R drugs * migraine drugs * antiemetics (ae) * NSAIDS * steroids and asthma drugs * antibodies * rheumatoid arthritis (RA) drugs * Immunosuppressant (IS) drugs
Filtering McNaughton Inflammation Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects Metabolism Clearance Adalimumab AB TNFa opsonises * "~mab" chimeric mouse + human AB * Rheumatoid arthritis * Crohn's disease Infliximab AB TNFa opsonises * Rheumatoid arthritis * Crohn's disease Alosetron 5-HT3R antagonist antiemetic Anakinra IL-1 R antagonist Aprepitant NK1 R antagonist antagonises substance P Aspirin COX irreversible inhibitor * in platelets: TXA2 synthesis inhibited, causing decrease in platelet aggregation --> antithrombotic effect (platelets can't make more COX) * acetylates serine * anti- inflammatory * anti-clotting * analgesic * antipyretic * salicylate poisoning * reye's syndrome * hyper- sensitivity reactions Cyclosporine calcineurin inhibitor * interferes with T- cell action by suppressing IL-2 expression immunosuppr essant * nephrotoxic but no bone marrow suppression Celecoxib COX2 specific inhibitor * too bulky to enter COX1 active site Chloroquine prevents haeme breakdown, inhibits lymphocyte proliferation, phospholipase A, antigen presentation in dendritic cells, release of enzymes from lysosomes, release of reactive oxygen species from macrophages, and production of IL1 * DMARD * also used as antimalarial drugX * only used for RA if other drugs have failed rheumatoid arthritis Cimetidine H2R antagonist stomach ulcers Clarythromyci n kill h.pylori antibiotic stomach ulcers Hydrocortison e cortic oster oid GCR-alpha inhibit enzymes, transcription factor, short acting * TF = 3 mechanisms of action: 1. Direct TF 2. Direct activation of other TF 3. Indirect activation of other TF (inhibition of other TF) * anti- inflammatory * asthma * polyphagia, diabetes * osteoporosis * muscle weakness * skin thinning * decreased wound healing, increased infection risk Tacrolimus calcineurin inhibitor * interferes with T- cell action by suppressing IL-2 expression * also binds immunophillin immunosuppr essant Prednisone cortic oster oid GCR-alpha inhibit enzymes, transcription factor, short acting * genes upregulated: - lipocortin-1 - secretory leukocyte inhibitory protein - IL1 receptor antagonist - IkBa * anti- inflammatory * Cushings: - moon face - buffalo hump - abdo fat Dimenhydrinat e H1R antagonist via inhibition of muscarinic cholinergic in periphery? motion sickness motion sickness well abs, metabolised in liver, excreted in urine Ergotamine 5-HT1R antagonist, partial agonist * also alpha2 agonist * therapeutic Fexofenadine H1R antagonist 3rd generation antihistamine cardiosafe well abs, metabolised in liver, excreted in urine Gold prevents neutrophil migration to site of inflammation * DMARD Triamcinolone cortic oster oid GCR-alpha inhibit enzymes, transcription factor, intermediate acting * genes downregulated: - IL1 - TNFalpha - iNOS - COX2 * anti- inflammatory " Ibuprofen COX * mild anti-platelet effect * arthritis * antipyretic Icatibant pepti domi metic B2R antagonist * inhibits bradykinin!!! * allergic disease * asthma Omalizumab AB IgE opsonises * "~zumab" = fully humanised AB * IgE mediated asthma Dexamethason e cortic oster oid GCR-alpha inhibit enzymes, transcription factor, long acting " * anti- inflammatory " Loratidine H1R antagonist 3rd generation antihistamine cardiosafe well abs, metabolised in liver, excreted in urine Mepyramine H1R antagonist 1st generation antihistamine cross BBB --> sedate well abs, metabolised in liver, excreted in urine Methotrexate folate antagonist inhibits folate synthesis * DMARD * cytotoxic and immunosuppressant activity rheumatoid arthritis Metocloprami de D2R antagonist Metronidazole kill h.pylori antibiotic stomach ulcers Misoprostol NSAID Sirolimus mTOR inhibitor * major regulator of cell growth and proliferation, upstream of PKB immunosuppr essant Alemtuzumab AB CD52 opsonises * "Campath" * B-cell lymphoma * MS Omeprazole PPI inhibitor stomach ulcers Ondansetron 5-HT3R antagonist antiemetic Paracetamol COX * detail not well understood, perhaps via COX3 * CNS effects * antipyretic and analgesic but less anti-inflammatory * antipyretic * analgesic * gastric ulcers, GI damage, bleeding anaemia * nephropathy * prolonged gestation Penicillamine dimet hyl- cystei ne, chelat or reduces T-cell numbers, inhibits macrophage function * DMARD * penicillin derivative without antibiotic function * no general anti- inflammatory action * slow onset * monitor blood rheumatoid arthritis * blood dyscrasia * liver cirrhosis * rashes * stomatitis * don't combined with gold! Phenothiazine D2R antagonist Cromolyn sodium leukotriene receptor antagonist * interferes with mediator release * mast cell stabiliser Promethazine H1R antagonist 1st generation antihistamine cross BBB --> sedate well abs, metabolised in liver, excreted in urine Ranitidine H2R antagonist stomach ulcers Rapamycin mTOR inhibitor * major regulator of cell growth and proliferation, upstream of PKB immunosuppr essant Salbutamol Scopolamine mAchR antagonist Azathioprine purin e analo gue purine synthesis inhibitor * inhibitor of DNA synthesis immunosuppr essant * bone marrow depression Sodium cromoglicate leukotriene receptor antagonist * interferes with mediator release * mast cell stabiliser Sulfasalazine sulfon amide and salicyl ate unkown, but interferes with lymphocyte function, toxic oxygen scavenger? * DMARD * induces remission * monitor blood! rheumatoid arthritis GI disturbance, headache, leukopenia, skin rxns, reduced sperm count, bone marrow suppression, anaphylaxia, . Sumatriptan trip- tans 5-HT1R agonist * therapeutic Mycophenolat e sodium inosine monophospha te dehydrogenas e, purine synthesis inhibitor * inhibitor of DNA synthesis immunosuppr essant Terfenadine H1R antagonists 2nd generation antihistamine cardiac toxicity with P450 inhibitor such as grapefruit juice well abs, metabolised in liver, excreted in urine Zafirlukast leukotriene receptor antagonist * Asthma Zileuton 5- lipoxygenase inhibitor * Asthma Valproic acid histone deacetylase inhibitor * preventative Ipratropium mAChR antagonist * reduces Ca2+ release --> relaxation * COPD! Theophylline beta2 adrenoR agonist * increases cAmp mediated relaxation Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. tag1 tag2 tag3 tag 4 tag 5 AB 1 AB 2 ae 1 RA ae 6 NSAID IS 1 NSAID RA H2 1 H2 4 steroid, asthma 1 IS 2 steroid, asthma 2 H1 6 migraine H1 4 RA steroid, asthma 3 NSAID AB 3 steroid, asthma 4 H1 5 H1, ae 1 RA ae 3 H2 5 IS 3 AB 4 H2 3 ae 2 NSAID RA ae 4 asthma 5 H1 2 H2 2 IS 4 ae 5 IS 5 asthma 6 RA migraine IS 6 H1 3 NSAID, asthma 7 NSAID, asthma 8 migraine asthma 9 asthma 10 Edwardson Chemotherapy p Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects Metabolism p.38 Cyclophosphamide nitrog en- musta rd DNA * alkylating * reactive * prodrug, converted in liver to active form * CC phase unspecific * cpa in particular: - pronounced effect on lymphocytes, immunosuppressant chemotherapy: lymphoid, leukaemia, breast, lung, ovary, endometrium most commonly used * depress bone marrow * GI disturbances * gametogenesis depression * leukaemia well absorbed orally, liver metabolism activates it p.38 Melphalan L-Phe mustard!!!, derivative of Mechlorethamine nitrog en- musta rd DNA * alkylating * designed to be tissue specific * F = melanin precursor => accumulates in melanomas! chemotherapy for melanoma, chronic myeloid leukaemia p.38 Mechlorethamine, nitrogen-mustard proper nitrog enmu stard DNA, guanine * alkylating * chlorethyl side-chain can form cyclic immonium ion (hetero(N)-cyclo-propyl) * attacks guanine at 7- nitrogen * 2nd R-group can do the same with the adjacent strand => intra and inter xlink! chemotherapy, lymphoma, skin lymphoma, melanoma, kidney and lung tumours, brain cancers as can treat BBB effects: * xlinks to same strand or different one * if single strand then introduces anomalous bp with T * GC => AT! Contents of Edwardson Lecture series on Chemotherapy: This is another massive handout. Even though the section on drug resistance is relatively short, make sure you learn it well. A disproportionately large amount on questions deal with drug resistance. - antibiotics - antifungals - antivirals - anticancer agents
Legend
NO colour coding here because there is so much overlap!
Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. p Drug Class Target Mechanism of Action Points of Interest Application Indication Side-effects Metabolism p.38 Lomustine nitros o- ureas DNA * alkylating * carbamoy- lating * lipid soluble and crosses BBB * interstrand xlinks N7 and O6 * reactive intermediate: carbonium ion chemotherapy, esp. brain p.38 Cisplatin platin um comp ounds DNA * alkylating * intrastrand xlink between two neighbouring guanidines * local DNA denaturation * cis-form = active chemotherapy, ovary and testes, sarcomas, carcinomas, lymphomas * severe nausea, treat with ondansetron * tinnitus
Clearance tag1 tag2 tag3 tag 4 tag 5 cancer covalent 1 cancer covalent 2 cancer covalent 3 Filtering To visualise the individual groups of drugs, click on the arrows in the far right column named "tag1" and select the custom filter. Select "contains" and enter your search term. You can now reorder the drugs using "tag2". Click on the arrows and select "sort ascending". Now you can print your subset of drugs. Select the desired pages. Clearance tag1 tag2 tag3 tag 4 tag 5 cancer covalent 4 cancer covalent 6 Vaughan Williams Drugs OVERVIEW GROU P Drug Class Target Mechanism of Action Points of Interest Application Indication Side- effects Meta- bolism Ia Procaine- amide * lengthen AP Ia Quinidine Ester Voltage- sensitive Na+ channel physically blocks channel * lengthen AP * use- dependent at low rates of stimulation * local anaesthetic * antiarrhythmi * CNS * cardio- vascular Ib Lidocaine/lig nocaine Amineester Voltage- sensitive Na+ channel physically blocks channel: stabilises inactivated state * shorten AP * weak base (+active, neutral can cross membrane, active from inside) * inhibits C and Ad fibres best (=small) * use- dependent at high rates of stimulation * local anaestetic * antiarrhythmi c * used for neuropathic pain * can give per IV * CNS * cardio- vascular Ic Flecainide * no effect on length of AP GROU P Drug Class Target Mechanism of Action Points of Interest Application Indication Side- effects Meta- bolism II Atenolol beta1 adrenoR (little bit beta2) antagonist * pretty beta1 selective II Bisoprolol beta1 adrenoR antagonist * third generation * chronic heart failure * over- inhibition II Butaxamine /Butoxamine beta1 and beta2 adrenoR antagonist * pretty beta2 selective * beta2 > II Carvedilol alpha1, beta1, beta2 adrenoR antagonist * third generation * third generation * chronic heart failure * over- inhibition II Labetalol alpha1, beta1 and beta2 adrenoR antagonist * four isomers with different actions * does not bind alpha2 R * treat hypertension in pregnancy II Propranolol beta adrenoR antagonist * beta1=beta2 * beta blocker III Amiodarone * beta-blocker and K+-ch blocker-like actions in nodes * resembles thyrroid hormone -> toxicity * class III anti- dyshythmic * thyrroid problems GROU P Drug Class Target Mechanism of Action Points of Interest Application Indication Side- effects Meta- bolism IV Amlodipine DHP Voltage- sensitive Ca2+ channel (L-type) Antagonist * highly lipid solumble as aromatic * favours mode 0 (closed) * Calcium antagonist IV Bay K 8644 DHP Voltage- sensitive Ca2+ channel (L-type) Agonist (to Nifedipine) * highly lipid solumble as aromatic * favours mode 2 (open) IV Nifedipine DHP Voltage- sensitive Ca2+ channel (L-type) Antagonist (of Bay K 8644) * highly lipid solumble as aromatic * favours mode 0 (closed) * Calcium antagonist * more effect on vascular smooth muscle * reflex tachycardia IV Diltiazem (IV) benzo- thiazepine Voltage- sensitive Ca2+ channel (L-type) Antagonist * rate neutral * more effect on smooth muscle in comparison to Verapamil * Calcium antagonist * rate neutral * side- effects from vasodilatio n: flushing, headache * well absorbed in GI --> given by mouth * exten- sively metabolis ed GROU P Drug Class Target Mechanism of Action Points of Interest Application Indication Side- effects Meta- bolism IV Verapamil (IV) phenylalkyla mine Voltage- sensitive Ca2+ channel (L-type) blocker * slows heart rate * negative inotropic action * Calcium antagonist * affects heart muscle more than vasculature * by mouth *SVT but Adenosine used instead * AV block and cardiac slowing but reflexes act against * constipatio n Clearance * esters rapidly hydrolysed by esterases * amides metabolised in liver Clearance Clearance Clearance Toxins OVERVIEW Makes sure you learn your toxins, they LOVE them for the exam! p Drug Class Target Mechanism of Action Points of Interest Application Indication Curare nicotinic AchR Antagonist * south-american arrow poison p.4 d-Tubo- curarine nicotinic AChR Antagonist * active substance of Curare alpha- Bungarotoxin nicotinic AchR at NMJ and brain alpha5! irreversible inhibitor * snake poison * works at NMJ but not on ganglionic receptors or in the brain p.10 beta- Bungarotoxin localises to K+channel in the membrane blocks ACh release (check wikipedia, as it says the opposite!), has phospholipase A2 activity * snake poison p.10 alpha- latrotoxin neurexins (TM proteins on the nerve membrane) and latrophillins * neurexins help glue together neurons at the synapse * causes insertion into the membrane => pore formation * massive ACh release * black widow spider toxin p.10 Botulinum toxins cleaves SNARES, e.g. synaptobrevin blocks ACh release in cholinergic neuron, e.g. aMN * AB toxin * causes muscle weakness p.7 Tetanus toxin cleaves (?) SNARES, e.g. synaptobrevin blocks Ach release in inhibitory inter-neuron * AB toxin * causes muscle spasm and suppression of PNS p.15 Cholera toxin alpha S subunit of G-protein ribosylates GDP to render the adenylyl cyclase always "on" p.15 Pertussis toxin alpha i subunit of G-protein ribosylates GDP to render the adenylyl cyclase always "off" p.24 Tetrodotoxin guanidinium Voltage-sensitive Na+ channel physically blocks channel * no use-dependence * from japanese puffer fish * works exclusively from the EC side Ouabain Na+/K+ ATPase inhibitor * similar to action of cardiac glycosides Makes sure you learn your toxins, they LOVE them for the exam! Side-effects Metabolism * paralysis * respiratory failure *resp failure muscle weakness muscle spasm Drug Class Target Mechanism of Action Drug Class Target Mechanism of Action Adrenaline Carvedilol Clonidine Doxazosin Ergotamine Guanfacine Idazoxan Labetalol Methyl NA Noradrenaline Octopamine Phenoxybenzam ine Phentolamine Phenylephrine Prazosin Xylazine Yohimbine tag1 tag2 tag3 tag4 tag5 tag6 LECTURER tag1 tag2 tag3 tag4 tag5 tag6 LECTURER adreno alpha beta Edwardson1 adreno alpha beta Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha beta Edwardson1 adreno alpha beta Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 adreno alpha Edwardson1 SERIES NUMBER SERIES NUMBER 2 40 2 60 2 61 2 70 2 76 2 78 2 81 2 86 2 94 2 99 2 100 2 102 2 103 2 104 2 110 2 124 2 125