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lola_smily
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Flashcards on untitled 2, created by lola_smily on 06/22/2015.

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lola_smily
Created by lola_smily almost 4 years ago
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Question Answer
b9df6aea-c614-414b-811c-b004650e1b3b.png (image/png) Acetylcholine -muscarinic receptor agonist
c477bc10-1af0-452e-98e6-867b35a442b6.png (image/png) Metacholine - muscarinic receptor agonist - modification of the ethylene bridge - S(+) equipotent to ACH - beta methyl substitution => more selective to Muscarininc receptor - more resistant to AChE => slow hydrolysis
9f51afcf-7624-4543-b3f7-580c2dbad047.gif (image/gif) Carbachol -muscarinic receptor agonist - modification of the acetoxy group - converting ester to carbamate - similar ACh potency, same profile -hydrolysis by AChE
63408f7a-772d-4db8-9cc0-ed41d197c459.png (image/png) Bethanechol - muscarinic receptor agonist - beta methyl substitution - potent and selective Muscarinic agonist -S(+) more potent
3c34ee4c-5d21-44fd-b4fe-464cfefc2228.png (image/png) choline ethyl ether - muscarinic receptor agonist - exception to the classical SAR of muscarinic activity
f74ae557-df2b-4254-897a-4ce19f17a492.PNG (image/PNG) alkyl amino ketones - muscarinic receptor agonist - exception to the classical SAR of muscarinic activity
aea93951-5ab0-4211-8f99-7cc96f3eb461.PNG (image/PNG) L(+)- Muscarine Chloride
34d9b391-c298-4c3a-bcc7-1b7d9a0c2aa1.png (image/png) epimuscarine
cdceb9c9-9ad9-42d7-8422-e313dc39ed8c.PNG (image/PNG) pilocarpine - alkaloid, produced from Pilocarpus jaborandi - Potent muscarinic agonist - chemically unstable => ring opening
9485bac8-5956-49df-8b69-a2e1b5cf5da4.PNG (image/PNG) pilocarpic acid - inactive - product of hydrolysis of pilocarpine
e075f06c-a8f2-4f5e-93c0-2f5615765bf3.PNG (image/PNG) isopilocarpine - epimerization of pilocarpine - inactive product
2302521a-e8a0-441c-a0fb-b0759f8acb1b.PNG (image/PNG) Physostigmine -indirectly acting parasympathomimetics - reversible AChE - 3ary alkaloid obtained from the Calabar Bean, Physostigma venosum - exhibits high affinity to AChE of 10^-9 to carbachol of 10^-4 -used to treat glaucoma and over dose of anticholinergic -light sensitive -undergoes hydrolysis in aqueous solutions
1ecc9881-ca08-45a0-8678-d545a2948104.PNG (image/PNG) eseroline inactive degradation product of physostigmmine in aqueous solutions
3bef07b9-51dc-4817-9fc0-ff46d0ca8205.PNG (image/PNG) rubreserine -inactive degradation product of physostigmmine in aqueous solutions - red color
9413039c-4cd3-4105-93aa-5c020ef6f9e9.PNG (image/PNG) neostigmine -indirectly acting parasympathomimetics - reversible AChE synthetic ionized -indicated for Myastenia Gravis
3b060536-9946-418b-8b63-c81638cd1fd7.PNG (image/PNG) pyridostigmine -indirectly acting parasympathomimetics - reversible AChE synthetic ionized -indicated for Myastenia Gravis
b9fff074-4b34-47d7-9b2a-d2271842e8c4.PNG (image/PNG) donepezil hydrochloride -indirectly acting parasympathomimetics - reversible AChE - lack hepatotoxicity - used for Alzheimer's disease
0cb896e3-ace7-4e6b-9ce7-2f89f9b26e39.PNG (image/PNG) tacrine indirectly acting parasympathomimetics - reversible AChE - cause hepatotoxicity - used for Alzheimer's disease
ea94c267-9bf2-4aef-aee6-1c9121127443.PNG (image/PNG) rivastigmine indirectly acting parasympathomimetics - reversible AChE - lack hepatotoxicity - used for Alzheimer's disease
4367c659-1714-4009-831d-543bb2e44191.PNG (image/PNG) Edrophonium -used for diagnostic purposes - improve Myastenia Gravis -worsen cholinergic chrisis
3300fbc3-3eed-4e7e-b548-4f2b2f938f5d.PNG (image/PNG) Malathion irreversible AChEi organophosphate thio group
c500dcba-8ef0-4f0e-aa6a-b35518edbb9c.PNG (image/PNG) parathion irreversible AChEi organophosphate thio group low Anti-AChE activity
d668d05c-4287-4b9c-95dd-b4133fa89360.PNG (image/PNG) sarin irreversible AChEi organophosphate
8759a48d-df22-4a1c-a347-96ca04dfc4a9.PNG (image/PNG) paraoxon irreversible AChEi organophosphate oxo group high Anti-AChE activity
8ccd63ec-c3e3-457e-8e16-e102f0a4711d.PNG (image/PNG) echothiophate iodide irreversible AChEi organophosphate ionized => clnical application for glaucoma
e9aec5bf-40a6-4a40-97ff-3f61d185fe7b.PNG (image/PNG) oxime reactivation of AChE
766c402e-85b4-41f0-8cfa-7f9c08abf8a8.PNG (image/PNG) Pralidoxime chloride (2 -PAM) reactivation of AChE
0eb3b729-e5f4-4995-891a-7e7e83d0db9e.PNG (image/PNG) obidoxime reactivation of AChE
60c0fb84-adee-4982-a265-e1185ef2938d.PNG (image/PNG) diacetylmonoxime reactivation of AChE
ab3b96f1-d976-40eb-a1f0-2b987c2fedaf.PNG (image/PNG) atropine parasympatholytics muscarine receptor antagonist alkaloid obtained from atropa belladonna atropine also found in datura stramonium
f49b0036-11aa-436c-8515-9f70498fedfd.PNG (image/PNG) scopolamine parasympatholytics muscarine receptor antagonist alkaloid obtained from atropa belladonna aslo found in Hyascyamus niger
bf4e955b-0795-4cf2-8373-f1019167fcf8.jpg (image/jpg) glycopyrrolate -antiholinergic -amino alcohol ester -ionized, exert effect locally in GI
6869d417-aa4b-406d-aeee-f85e9e776d49.png (image/png) propantheline antiholinergic -amino alcohol ester -ionized, exert effect locally in GI
e6612041-aa48-49a0-8c99-a297877d83c4.png (image/png) clinidium antiholinergic -amino alcohol ester -ionized, exert effect locally in GI
5c5734e1-94bb-4b2c-8eca-83e64b852f40.png (image/png) ipratronium antiholinergic -amino alcohol ester -ionized, exert effect locally in GI
935a66df-ec0e-41b5-a88a-6ae7e3f993c8.png (image/png) flavoxate antiholinergic -amino alcohol ester -ionized, exert effect locally in GI
5569ac6b-8938-419a-84da-59cb710d4a41.png (image/png) oxyphencyclimine anticholinergic amino alcohol ester 3ary amine, used for Parkinson treatment systemic, can cross BBB
db733a77-4e5f-4c13-bce0-40de05ab21f6.PNG (image/PNG) procyclidine anticholinergic amino alcohol 3ary amine, systemic effect
3e324692-6737-4f5a-9368-5cb139d395a8.PNG (image/PNG) trihexyphenidyl anticholinergic amino alcohol 3ary amine, systemic effect
8cd106c7-77d7-4bc9-bf14-894ca1f4d306.JPG (image/JPG) benztropine anticholinergic amino ethers
9237c083-5902-4b93-ae9f-6428e5296b3e.PNG (image/PNG) orphenadrine anticholinergic amino ether antihistaminic anticholinergic> antihistaminic
3083a59a-baba-4d13-9919-909926eb6324.PNG (image/PNG) pirenzepine - selective M1 receptor antagonist - they are competitive antagonists -have antispasmodic effects -produce mydriasis -antisecretory: -decrease gastric secretions -decrease saliva secretions -decrease bronchial secretions
d74f4eb7-40a5-4114-aaa8-c813aa5a9c28.PNG (image/PNG) telenzepine selective M1 receptor antagonist - they are competitive antagonists -have antispasmodic effects -produce mydriasis -antisecretory: -decrease gastric secretions -decrease saliva secretions -decrease bronchial secretions
4c826250-837a-4ace-a752-2b6164408512.PNG (image/PNG) hexamethonium - ganglionic blocking agent - bisquaternary ammonium -MOA: they block autonomic ganglia => inhibit ganglionic transmission - main therapeutic indication: antihypertensive
e13ec343-927d-480b-b732-8eeaba56cb51.PNG (image/PNG) trimethophan ganglionic blocking agent - sulfonium -MOA: they block autonomic ganglia => inhibit ganglionic transmission - main therapeutic indication: antihypertensive
7baab063-b8a1-46f9-bc53-47f845f69850.PNG (image/PNG) pentolinium ganglionic blocking agent - bisquaternary ammonium -MOA: they block autonomic ganglia => inhibit ganglionic transmission - main therapeutic indication: antihypertensive
ce879bfe-6caa-4d64-a5a4-e74ee1711845.PNG (image/PNG) mecamylamine ganglionic blocking agent - secondary amines -MOA: they block autonomic ganglia => inhibit ganglionic transmission - main therapeutic indication: antihypertensive
2c32f638-c255-40f8-9efe-8b05a9f101c8.PNG (image/PNG) pempidine ganglionic blocking agent - tertiary amine -MOA: they block autonomic ganglia => inhibit ganglionic transmission - main therapeutic indication: antihypertensive
31fbbcd8-1ddd-4607-a5f4-2773f8884556.PNG (image/PNG) succinylcholine chloride - depolarizing NMJ blocker - produce a 2 phase block phase 1: stimulation phase 2: depression block by receptor desensitization - therapeutic use : muscle relaxation - reversal of effects of depolarizing : give antagonist to sensitize the receptor
6eec61ca-a30b-4976-b5f4-4437dc42147d.PNG (image/PNG) tubocurarine - non depolarizing NMJ blocker - cc: benzylisoquinoline - they are competitive receptor antagonist - all are ionized - lack CNS side effect - therapeutic use: muscle relaxation - reversal of effects of non depolarizing: AChI
2c238d07-c747-4d7d-bd79-28c82022d4c7.PNG (image/PNG) atracurium besylate - non depolarizing NMJ blocker - cc: benzylisoquinoline - they are competitive receptor antagonist - all are ionized - Exception: CNS side effects - therapeutic use: muscle relaxation - reversal of effects of non depolarizing: AChI
394f66a0-107d-439b-b020-1ed69fa4268f.PNG (image/PNG) mivacurium chloride non depolarizing NMJ blocker - cc: benzylisoquinoline - they are competitive receptor antagonist - all are ionized - lack CNS side effect - therapeutic use: muscle relaxation - reversal of effects of non depolarizing: AChI
52153828-c8a0-4189-bffa-df517d845e33.PNG (image/PNG) doxacurium chloride non depolarizing NMJ blocker - cc: benzylisoquinoline - they are competitive receptor antagonist - all are ionized - lack CNS side effect - therapeutic use: muscle relaxation - reversal of effects of non depolarizing: AChI
1049b7c0-5b33-45fa-a526-409aabcb17bd.PNG (image/PNG) L-Tyrosine
1f5d2e35-ecb4-40ae-9727-8de2174359a0.PNG (image/PNG) L-Dopa
3ca868d2-8f9f-4218-81f2-cd8a649ea6d9.PNG (image/PNG) Dopamine
72877ee8-e1eb-4cf4-9551-e29a5c36c0df.PNG (image/PNG) Norepinephrine - released NE : binding to receptor postsynaptic and presynaotic uptake 1( recycling NE) uptake 2 ( degradation, metabolism ) - receptor selectivity: alpha 1, 2, beta 1
c46b29ad-350d-4df0-b010-d07fff9bcb37.png (image/png) epinephrine - increasing the size of R1 ( CH3) increase beta and decrease alpha adrenergic activity - receptor activity: Beta 2 > alpha 1,2, beta 1
707dbbb5-dbe3-43f0-b230-0b54d12f978d.PNG (image/PNG) Isoproterenol increasing the size of R1 (isopropyl) increase beta and decrease alpha adrenergic activity - receptor activity: Beta 2, Beta 1
bd73dba3-b10a-4d43-8d75-24b3ac734950.PNG (image/PNG) Colterol - increase the size of R1 to t-butyl group increase selectivity to beta 2 agonistic activity -cc: phenylethanolamines -receptor selectivity :beta 2 > beta 1 beta 2 agonist
132d2fd3-017f-4e6b-afe2-5a3a4b1e1cce.PNG (image/PNG) ritodrine -increasing the size of R1 => increase selectivity to beta 2 agonistic activity - at least one hydroxyl group is required to form hydrogen bonding with receptor
e61824e8-621a-4e6c-a256-6e1b2b501c8c.png (image/png) Ethylnorepinephrine substation on Carbon 2, R2: ethyl increase beta activity chiral center at C2 -receptor activity: beta > alpha
8276d71d-8191-4a79-8fad-7413d390ab54.PNG (image/PNG) alpha- methylnorepinephrine (1R, 2S) 1R, 2S isomer : maximum direct activity 1R, 2R isomer: indirect activity receptor activity: alpha 2 > alpha 1
c6d0207d-7e27-4249-8472-bd2a02040b23.PNG (image/PNG) terbutaline 3', 5'- dihydroxy substitution: orally active no COMT metabolism receptor activity: beta 2> beta 1
88a27493-2fc7-49cb-a5a0-e33a54c408a5.PNG (image/PNG) albuterol 3' hydroxymethyl,4'hydroxy substitution non cathechol => orally active receptor activity: beta 2 > beta 1
104d8a39-97d6-4bdc-8f0d-0108933794a2.PNG (image/PNG) Phenylephrine 3' hydroxyl substitution => alpha 1 activity
e2b99fcc-62d7-4f4d-8794-237982474c4a.PNG (image/PNG) Metaraminol 3' hydroxyl substitution => alpha 1 activity
b0ab5898-24bb-4c5e-8e9f-f063e93747ea.PNG (image/PNG) Methoxamine 2',5' -dimethoxy substitution => alpha 1 activity
85b786aa-13c5-484b-9ed4-86432b06bbcb.PNG (image/PNG) pirbuterol beta 2 agonist cc: phenylethanolamies
defac464-062f-47ab-95b1-d25946a99707.PNG (image/PNG) salmeterol beta 2 agonist cc: phenylethanolamines
c7e284cf-3fb0-4c24-a504-237ffab41e6d.png (image/png) bitolterol -beta 2 agonist - phenylethanolamine - non catechol : orally active - bi- toluoylester ( more lipophilic) - given by inhalation -hydrolyzed by esterase in the lungs to give colterol - twice the DOA than catechol
de085dd9-3422-4040-abae-4a219cb5efd5.PNG (image/PNG) Dobutamine (-) dobutamine : alpha agonist + beta 1 agonist (+) dobutamine: alpha antagonist + beta 1 agonist ( 10x) racemic mixture: selective beta 1 activity exception to SAR
6f65d693-dbd5-421a-b116-0d0e5e6e529c.PNG (image/PNG) dopamine - not strictly adrenergic agonist - DA receptor agonist => dialates renal blood vessels - at higher dose acts on beta 1 receptor - at much higher dose acts on alpha 1 receptor - not orally active
f1cb2c65-4bae-4502-a188-76696144662c.PNG (image/PNG) (+,-) ephedrine - mixed acting sympathomimetics - alkaloid from Ephedra species (Ma Huang) - non cathechol : orally active more lipophilic - 1R, 2S: direct + indirect acting -used as nasal decongestant - cc: phenylethanoloamines
de701f62-d62c-4d0b-a301-531df76be846.PNG (image/PNG) pseudoephedrine - 1S, 2R and 1S, 2S : indirectly acting sympathomimetics
d3ee43da-1b23-4c11-844f-884c53a3a264.PNG (image/PNG) amphetamine indirectly acting sympathomimetics dextro> levo non cathechol: orally active no hydrolysis: no 0H, very lipophilic, CNS stimulant
cf60a3cb-68dd-44af-b242-71a1022b97b7.PNG (image/PNG) metamphetamine indirectly acting sympathomimetics dextro> levo non cathechol: orally active no hydrolysis: no 0H, very lipophilic, CNS stimulant
89d86f09-cf6f-4c79-b222-16c07f49f421.png (image/png) propylhexedrine indirectly acting sympathomimetics same as metamphetamine dextro> levo non cathechol: orally active no hydrolysis: no 0H, very lipophilic, POTENT CNS stimulant
6cf573f4-a1ee-4383-94c6-5704fd91e533.PNG (image/PNG) xylometazoline - alpha 1 adrenergic agonists - cc: imidazoline derivatives - contain a carbon between C2 of imidazoline and a phenyl ring - contain phenylethylamine moiety ortho methyl: agonistic activity at alpha 1 and alpha 2 receptors - bulky group at para position: increase alpha 1 and decrease alpha 2 activity - mainly used as nasal decongestant
86b258f7-2314-420c-87fb-2ed0878d515c.PNG (image/PNG) oxymetazoline - alpha 1 adrenergic agonists - cc: imidazoline derivatives contain a carbon between C2 of imidazoline and a phenyl ring - contain phenylethanolamine moiety ortho methyl: agonistic activity at alpha 1 and alpha 2 receptors - bulky group at para position: increase alpha 1 and decrease alpha 2 activity - mainly used as nasal decongestant
32095ea2-a98c-4004-822a-6d93516a81fe.PNG (image/PNG) tetrahydrozoline alpha 1 adrenergic agonists - cc: imidazoline derivatives contain a carbon between C2 of imidazoline and a phenyl ring - contain phenylethylamine moiety ortho methyl: agonistic activity at alpha 1 and alpha 2 receptors - mainly used as nasal decongestant
ca14cad7-8a73-43a4-8e7c-afb2b522e069.PNG (image/PNG) naphazoline alpha 1 adrenergic agonists - cc: imidazoline derivatives contain a carbon between C2 of imidazoline and a phenyl ring - contain phenylethylamine moiety ortho methyl: agonistic activity at alpha 1 and alpha 2 receptors - mainly used as nasal decongestant
909d5459-06d1-419c-bee7-b90c4ef2d364.PNG (image/PNG) clonidine - potent alpha 2 adrenergic receptor agonist -cc: imidazoline derivatives - developed as nasal vasoconstrictor - produce marked hypotensive effects, maily centrally mediated throughpostsynaptic alpha2 adrenergic receptor - used as antihypertensive agent - effects on peripheral postsynaptic alpha 2 receptors: vasoconstriction - effects on peripheral presynaptic: negative feedback, decrease NE - pka 8.5, 80% ionized, 20% NI
be91d9a3-284a-493f-b4cd-a5e18e3772aa.PNG (image/PNG) Apraclonidine alpha 2 adrenergic agonist imidazoline moiety
104eed15-31d9-4a53-913f-5557531faea9.PNG (image/PNG) brimonidine alpha 2 adrenergic agonist imidazoline moiety
3d9f6619-3d57-4671-9172-8f8e05aa12bd.PNG (image/PNG) guanabenz potent alpha 2 adrenergic agonist non imidazoline, clonidine like same indication as clonidine
0cc05e44-e141-4411-a94a-652c57758284.PNG (image/PNG) guanfacine potent alpha 2 adrenergic agonist non imidazoline, clonidine like same indication as clonidine
47de6057-17da-473a-8fac-96e88e243ffb.PNG (image/PNG) alpha -methyldopamine alpha 2\ adrenergic antagonist non imidazoline derivative undergoes bioinactivation
55ebcd84-f57b-42ee-b4f3-b909fed2338f.PNG (image/PNG) phenoxybenzamine - adrenergic antagonist - irreversible alpha blocker - non selective ( alpha 1 and 2 ) - Beta-haloalkylamine derivative - slow onset of action: because it is a prodrug, must undergoe bioactivation ( alkylated receptor active ) -limited use in pheochromocytoma (cancer of adrenal medulla)
fd52dd5b-88a9-4dab-a012-a0e3c4396b99.PNG (image/PNG) tolazoline - adrenergic receptor antagonist - reversible - non selective ( blocks alpha 1 and 2 ) - similar to xylometazoline BUT no ortho substitution: no alpha agonistic effects - limited use in treatment of symptoms of pheochromocytoma - rapid onset of action
a12d015c-143d-46e0-840d-4f6753190f01.PNG (image/PNG) phentolamine - adrenergic receptor antagonist - reversible - non selective ( blocks alpha 1 and 2 ) - limited use in treatment of symptoms of pheochromocytoma - rapid onset of action
acd21863-abb9-4f73-af5f-4e47e8f16fad.PNG (image/PNG) prazosin - selective alpha 1 receptor antagonist reversible - quinazoline derivative -contain 4-amoni-6-7-dimethoxyquinazoline ring connected to piperazine at C2 -lower Blood Pressure
4fdae2a7-4fdf-4543-974f-f7f6c73e1547.PNG (image/PNG) terazosin selective alpha 1 receptor antagonist reversible - quinazoline derivative -contain 4-amoni-6-7-dimethoxyquinazoline ring connected to piperazine at C2 -lower Blood Pressure
7f0a2c37-31bf-45a2-9e37-6c22a852318f.PNG (image/PNG) doxazosin selective alpha 1 receptor antagonist reversible - quinazoline derivative -contain 4-amoni-6-7-dimethoxyquinazoline ring connected to piperazine at C2 -lower Blood Pressure
e6578c86-b251-4686-98cf-739c791b53d2.PNG (image/PNG) tamsulosin selective alpha 1 receptor antagonist reversible high affinity to alpha 1 A subtype present in prostate gland => used to treat BHP ( benign prostatic hyperplasia) - cc: sulfonamide phenylpropylamine
45387ed6-afe2-4a5c-a08f-954bb6cbefe3.PNG (image/PNG) indoramin - reversible selective alpha 1 receptor antagonist and H1 (histamine) and 5receptor antagonistHT (serotonin) - indole derivative
ef76c1c3-629e-4a7f-bd52-b6ba79efd98c.PNG (image/PNG) yohimbine - reversible selective alpha 2 blocker - indole alkaloid from Yohimbe bark - increase Blood Pressure AND Heart Rate - very limited use to treat male sexual impotency
81859e30-8cdd-4cc9-8084-a18ccda1ad9d.png (image/png) practolol - Beta adrenergic receptor antagonist - aryloxypropanolamine with p-acylamino -change of acylamino to ortho or meta => loss of selectivity - inhibited isoproterenol induced tachycardia with minimal effects on isoproterenol induced hypotension -withdrawn from the market due to visual loss
ed6b2a45-176f-45b3-b4a4-0aa3ef75deae.PNG (image/PNG) pronethalol - beta adrenergic receptor antagonist non selective -arylethanolamine - no partial agonistic activity - carcinogenic in animals
48d6d598-a6c9-4368-8c0b-c026f062d5a8.PNG (image/PNG) propranolol -aryloxypropanolamine -beta adrenergic receptor non selective -10X> potent -no partial agonistic activity -not carcinogenic - used in hypertension, agnia pectoris, arrhythmia, migraine
264675f4-05e0-4d82-93cf-119e512ec965.PNG (image/PNG) bunolol -non selective beta adrenergic receptor antagonist
1a1df086-de80-4daa-8a08-7a2013d422c7.PNG (image/PNG) carteolol -non selective beta adrenergic receptor antagonist
0dbf0f64-3bbb-4f32-9070-8b832da7b8b0.PNG (image/PNG) metipranolol -non selective beta adrenergic receptor antagonist - exception para postion - ester hydrolysis=> short acting
9ba2744f-cfc1-4979-8adb-67332b717a47.PNG (image/PNG) nadolol -non selective beta adrenergic receptor antagonist
f0842278-ee70-4a55-bf6f-7b094a4847e3.PNG (image/PNG) penbutolol -non selective beta adrenergic receptor antagonist
f3cd7c5b-8651-4320-a108-d2455d3ece25.PNG (image/PNG) pindolol -non selective beta adrenergic receptor antagonist
5bddb303-f1e8-4194-a06a-827eaa0ea931.PNG (image/PNG) sotalol -non selective beta adrenergic receptor antagonist - aryl sulfonamide ethanolamine derivative
82e84805-0d83-46e2-930f-ac9efdd0ac96.PNG (image/PNG) timolol -non selective beta adrenergic receptor antagonist
227d9656-bf66-4ac6-bb53-d6a5b49d4336.PNG (image/PNG) acebutolol -selective beta 1 adrenergic receptor antagonist cardio slective
55fa9e38-f351-45e6-b996-b38b6a4535bc.PNG (image/PNG) atenolol -selective beta 1 adrenergic receptor antagonist cardio slective
8c93d9e5-2044-4967-ba33-6855a7278620.PNG (image/PNG) betaxolol - selective beta 1 adrenergic receptor antagonist cardio selective
f6c5f47e-5757-460b-85bf-b76ca7e10a69.PNG (image/PNG) esmolol - selective beta 1 adrenergic receptor antagonist cardio slective
22c75384-21dd-44bf-9733-49a09f0b0606.PNG (image/PNG) metoprolol selective beta 1 adrenergic receptor antagonist cardio slective
9d435a2b-519a-4343-9b43-dadd8901a0dc.PNG (image/PNG) bisoprolol selective beta 1 adrenergic receptor antagonist cardio slective
a97e4a2c-3a58-49e5-8299-80e31c6f54b4.PNG (image/PNG) labetolol non selective beta blocker and alpha 1 blocker mixed acting
0f4a35e3-98fb-49de-ad64-d21c37564f1f.PNG (image/PNG) carvedilol non selective beta blocker and alpha 1 blocker mixed acting
9b74cf04-68c2-4772-b255-70ce2ae92e27.PNG (image/PNG) metyrosine - drugs affecting NE biosynthesis - tyrosine hydroxylase inhibitor
bc388943-cbf4-4a49-b914-2d297a0f8623.PNG (image/PNG) carbidopa - drugs affecting NE biosynthesis - L-Dopa decarboxylase inhibitor
94d6ea3a-ab35-4c98-8e28-d792adba2b63.PNG (image/PNG) reserpine -drugs affecting NE storage ( catecholamine depleting agents) - indole alkaloid -isolated from Rauwolfa Serpentina - inhibit catecholamine storage in storage vesicle => depletion of catecholamines
11d97081-12ef-49b3-8ff5-7245591fa2c3.PNG (image/PNG) guanadrel - drugs affecting NE release ( adrenergic neuronal blocking agents)
80b196b5-b14c-474a-acc5-9fc3679b2dc5.PNG (image/PNG) guanethidine - drugs affecting NE release ( adrenergic neuronal blocking agents)
50e5fc05-2f5f-422d-bd0e-3c5a7a22e3bb.PNG (image/PNG) bretylium - drugs affecting NE release ( adrenergic neuronal blocking agents)
4f85b9f3-617d-4553-831a-651625ff5677.PNG (image/PNG) ergot alkaloid - produced by calviceps purourea, a fungus that infects grains
56c78eb5-4778-4a28-88bf-d424c20a1fed.png (image/png) ergotamine - ergot alkaloid - produced by calviceps purourea, a fungus that infects grains -mixed agonist/ antagonist - potent smooth muscle contraction - also used for migraine treatment
4b9b8461-a28d-4faa-8bee-3b79343302ee.jpg (image/jpg) ergonovine -ergot alkaloid -mixed agonist/ antagonist - potent smooth muscle contraction - also used for migraine treatment - potent inducer of uterine - because of better bioavailability, used to replace ergotmaine
30f5b20c-e25a-4c2c-8d55-e510407dd16a.png (image/png) methylergonovine -ergot alkaloid -mixed agonist/ antagonist - potent smooth muscle contraction - also used for migraine treatment - potent inducer of uterine - because of better bioavailability, used to replace ergotmaine
a9ee0e45-d565-4ecf-b617-70a89775e907.png (image/png) methylseregide -ergot alkaloid -mixed agonist/ antagonist -mainly used for migraine treatment
4d15808c-67c1-411b-ba1a-9ab00accc4a0.PNG (image/PNG) morphine - cc: phenantrene - teriary amine group, N-methyl: good agonist Removal of N-methyl: decrease activity increase size of alkyl group: antagonist
60a74ddc-690d-41f3-a284-600a7f9674b0.PNG (image/PNG) phenanthrene
7fe26f21-3fd0-41cf-a5f6-1c6f2220367f.PNG (image/PNG) benzoquinone -oxidation od morphine product
5058ee32-57ac-403d-969d-3445bace410f.png (image/png) codeine - weak mu agonist - potent antitussive agent -partial O-demethylated => morphine
cab243fc-b7af-4bcb-8b38-fd9ebdcccd2c.PNG (image/PNG) Heroin -3,6-diacetyl derivative of morphine - weak affinity to mu receptor -more lipophilic: penetrates BBB - hydrolyzed in the brain to give: 3-acetylmorphine (3-MAM) 6-acetylmorphine (6-MAM) - 6-MAM has potent mu agonist
34fd6c75-d680-4d76-b47b-b9d4bd4afa6a.PNG (image/PNG) oxymorphone - 3-hydroxy-N-methyl derivative 10X as potent as morphine - 14 beta hydroxyl enhances mu agonist activity and decrease antitussive activity
f8f914aa-c2b6-4af1-88fd-3c9f59ce6aa3.PNG (image/PNG) oxycodone -3-hydroxyl-N-methyl derivative same activity as morphine but better oral bioavailability - 14 beta hydroxyl enhances mu agonist activity and decrease antitussive activity
3d47a52b-717a-41bd-b291-89833b5c67f8.PNG (image/PNG) naloxone - N-allyl oxymorphone - pure non selective opioid receptor antagonist
f90aa81d-017b-4b1f-96cb-b468c3d50ae0.png (image/png) nalorphine - N-allyl substitution for N-methyl 7,8-double bond reduction 6-keto reduction u
67b8fd36-d021-4517-9569-e62023c9edc8.PNG (image/PNG) morphinan - removal of 4,5 epoxide bridge (modification of E ring)
42cbef73-3d06-45b5-a8f2-cdd73b8cedc8.PNG (image/PNG) levorphanol -removal of 4,5 epoxide bridge - 8X more potent mu receptor agonist
c5fb733f-bb32-40ac-84a4-dd742227b1dd.PNG (image/PNG) butorphanol -removal of 4,5 epoxide bridge - mu antagonist and kappa agonist
a7b9532b-aa77-4659-b890-dcd9421d5b24.PNG (image/PNG) dextromethorphan -removal of 4,5 epoxide bridge (+) levorphanol = dextrophan - lacks analgesia - antitussive activity
bc7ed405-eac8-4372-96f4-c632b3d46735.PNG (image/PNG) benzomorphans - lacks the epoxide ring and the C ring - retain opioid activity
079b33f5-a7dc-42b7-8996-c67e458340b0.png (image/png) cyclazocine - R: N-cyclopropyl methyl - mixed agonist/ antagonist kappa agonist mu antagonist
57748db2-14dd-4cf0-ae51-fe0e860eb505.png (image/png) phenazocine - R: N-ethylphenyl -potent mu agonist about 10X> morphine
0865dd0f-3156-4426-9598-c60ab5cf2057.png (image/png) pentazocine -R: N-methyl of 2-methyl-2-butene - mixed agonist/antagonist kappa agonistic activity: analgesic mu antagonistic activity -only one marketed in US
d51d1257-b510-431b-b23a-d9306ac75682.png (image/png) metazocine -R: CH3 - mu agonist -metasocine > morphine
b27bd026-5e6d-45a4-b914-664bb975c71d.PNG (image/PNG) meperidine - A and D ring analogs of morphine - cc: phenylpiperidine -first synthesized agent with mu agonist activity of 1/4 of morphine -short DOA (useful in some medical procedure)
e365ef44-a563-4480-8f8b-34d6384ebe09.PNG (image/PNG) MPTP 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine -damages DA neurons => parkinsonism - product of reversed ester of meperidine
575d20de-b98a-4ba9-8d1c-fa62ce52e667.PNG (image/PNG) fentanyl - cc: anilidopiperidine - 80X> potent than morphine
a22881b9-1887-4e84-89ad-734c43a33c2e.PNG (image/PNG) sufentanil - cc: anilidopiperidine - 10X> potent than fentanyl (fentanyl 80X> morphine)
63d8d371-699d-4def-af96-e58983f624a7.PNG (image/PNG) remifentanyl - cc: anilidopiperidine - 25X> potent than morphine
cbed4602-fed5-445e-9dde-5a22f3b4e924.PNG (image/PNG) alfentanil - cc: anilidopiperidine - 20X> potent than morphine
f2a57aac-32bc-4d64-89fe-8ed2886f38bc.PNG (image/PNG) methadone -cc: diphenylheptanone - orally active and long DOA - useful for maintenance therapy of opoids addicts and for pain suppression of terminally ill patients
8482cc30-e4a6-4fd2-95bf-95ba820fd84b.PNG (image/PNG) isomethadone
943a7191-5d96-4112-a191-2c94c1cbee99.png (image/png) diphenoxylate -cc: diphenylheptanone - structural modification of methadone -antidiarrheal opioids
798c5cd8-a9ba-4b87-ab56-7424950acb57.png (image/png) loperamide -cc: diphenylheptanone - structural modification of methadone -antidiarrheal opioids
83745219-b97c-46cf-8c70-50446606edbe.PNG (image/PNG) thebaine -oripavine derivative - from papaver bracteatum no activity as opioid agonist
e826514a-6301-4add-a279-763fdb2d2804.png (image/png) etorphine - oripavine derivative - 1000 X> morphine - severe respiratory depression -low therapeutic index in humans, used for veterinary medicine
e2d7ed34-6842-4402-a366-cb13bf06323d.PNG (image/PNG) buprenorphine -orpavine derivative - 20-50X> morphine - mixed agonist / antagonist -does not produce tolerance and addiction
5f91aeb7-b626-47f1-b17f-ade113ebd047.PNG (image/PNG) tramadol - synthetic mu agonist - orally active - possess opioid and non opioid analgesic activity -analgesic not reversed by naloxone -O-dimethyl metabolite is 6X> parent drug -less respiratory depression than morphine
b98a2c87-0efb-4c4b-9d1d-fe9956b2ac6d.PNG (image/PNG) dezocine -mixed agonist / antagonist -only primary amine opoid agent - exact receptor selectivity is not known - equipotent with morphine
ec8a006f-221f-415d-8630-fcbbeb84ae9e.PNG (image/PNG) nalbuphine - N-cyclobutylmethyl substitution for N-methyl 7,8-double bond reduction 6 keto reduction -mu antagonist and kappa agonist
df91cf6f-a053-48a6-a1cb-c68628dce791.PNG (image/PNG) naltrexone -N-cyclopropyl-methyl oxymorphone - pure non selective opioid antagonist