Adrenergic Drugs

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Lebanese American University - Medicinal Chemistry 1
Majd Fawaz
Fichas por Majd Fawaz, actualizado hace más de 1 año
Majd Fawaz
Creado por Majd Fawaz hace más de 3 años
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Resumen del Recurso

Pregunta Respuesta
- 3',4'-Dihydroxy Mandelic Acid - Inactive Metabolite of EPI/NE
- 3',4'-Dihydroxyphenyl Ethelyne Glycol - Inactive Metabolite of EPI/NE
- 3',4'-Dihydroxyphenyl Glycoaldehyde - Inactive Metabolite of EPI/NE
- 3'-Methoxy-4'-Hydroxyphenyl Ethelyne Glycol - Inactive Metabolite of EPI/NE
- Albuterol - b2 Agonist - Orally Active
- a-Methyl Norepinephrine - a2 > a1 - 1R,2S (Direct ==> Receptor Affinity) - 1R,2R (Indirect ==> No Receptor Affinity)
- Bitolterol (Prodrug) - Very Lipophilic (bi-toluoylester) - Inhalled to Treat Asthama - Metabolized by Esterase in the Lungs - x2 DOA Colterol Note: Esters improve DOA but not Oral Activity
- Colterol - b2 Agonist - Orally Inactive - Short Acting - Used for Asthma
- Dobutamine - Selective b1 Agonist - Increase Heart Rate - Exception to the SAR - Administered in a Racemic Mix (50%+/50%-)
- Dopamine (DA Receptors) - Exception to SAR - Class: Phenylethylamine - Dilates Renal Blood Vessels - Not Orally Active (Given IV) - High Dose --> b1 Agonist - Higher Dose --> a1 Agonist
- EPI - b2 > a1, a2, b1 - Syn in the Adrenal Medulla - NE + SAM + Phenylethanolamine N-methyl Trasferase (PENT)
- Ethylnorepinephrine - b > a
- Ephidrene (1R,2S) - Mixed Acting - Alkaliod (Ma Huang) - Orally Active (CNS Side Effects) - Used as Nasal Decongestant - 1S,2S /1S,2R Pseudoephidren (Indirectly Acting)
- Isoproterenol - b1+b2 - Used to Treat Bradycardia
- L-DOPA - Dihydroxyphenylalanine
- L-Tyrosine - Amino Acid
- Metaraminol - a1 Agonist - Class: Phenylethanolamine
- Methoxamine Exception to SAR - a1 Agonist - Class: Phenylethanolamine
- NE - a1,a2,b1 - Some Selectivity to b1
- Normetanephrine - Inactive Metabolite of EPI/NE
- Phenylephrine - a1 Agonist - Class: Phenylethanolamine
- Pirbuterol - b2 Agonist - Orally Active
- Ritodrine - b2 Agonist - Orally Active - Used for Premature Labor
- Salmeterol - b2 Agonist - Orally Active
- Terbutaline - b2 Agonist - Orally Active - Used for Asthma
- Vanillyl Mandelic Acid (VMA) - 3'-Methoxy-4'-Hydroxy Mandelic Acid - Inactive End Product of EPI/NE Metabolism
- a-Methyl Dopa (Prodrug) - Gives a-Methyl NE ==> a2 Agonist (Similar to Clonidine) - Shares Enzymes with L-DOPA (Enzyme Inhbitor) - Used as Antihypertensive (Via CNS + Enzyme Inhibition )
- D-Amphetamine (+ > -) - Indirectly Acting (Increase NE Release ) - Class: Phenylethylamines - Orall Active - Very Lipophilic (CNS Stimulant) - Causes Loss of Appetite, Tachycardia, Hypertension
- Apraclonidine - a2 Agonist - Class: Imidazoline - Works Similar to Clonidine
- Brimonidine - a2 Agonist - Class: Imidazoline - Works Similar to Clonidine
- Clonidine - Potent a2 Agonist - Original Use: Nasal Decongestant - Current Use: Anti-Hypertensive - 20% Unionized - 80% Centerally - Effect: Transient Hypertension --> Sustained Hypotension
- Guanabenz - Potent a2 Agonist - Class: Gaunine - Antihypertensive (Similiar to Clonidine)
- Guanfacine - Potent a2 Agonist - Class: Gaunine - Antihypertensive (Similiar to Clonidine)
- D-Methamphetamine (+ > -) - Indirectly Acting (Increase NE Release ) - Class: Phenylethylamines - Orall Active - Very Lipophilic (CNS Stimulant) - Causes Loss of Appetite, Tachycardia, Hypertension - FYI: Crystal Meth
- Naphazoline - a1,a2 (No Para Sub.) - Class: Imadazoline - Nasal Decongestant
- Oxymetazoline - a1 > a2 (Para Sub.) - Class: Imadazoline - Nasal Decongestant
- Propylhexedrine - Orall Active - Indirectly Acting
- Tetrahydrozoline - a1,a2 - Class: Imadazoline - Nasal Decongestant
- Xylometazoline - a1 > a2 - Class: Imadazoline - Nasal Decongestant
- Dichloroisoproterenol - Non Selective b-Blocker With Partial Agonist Effect
- Doxazosin - Reversible Selective a1-Blockers - Class: Quinazoline - Hypotensive Effect
- Indoramin - Reversible Selective a1-Blockers Class: Indole - Histamine and Serotonin Atagonist
- Phenoxybenzamin (Prodrug) - Irreversible Nonselective a-Blocker - Class: B-Haloalkylamine - Slow Onset of Action - Limited Use in Pheochromocytoma (Still EPI Release)
- Phentolamine - Reversible Nonselective a-Blocker - Class: Imidazoline - No Agonist Effect - Limited Use in Pheochromocytoma (Still EPI Release)
- Practolol - Selective b1-Blocker - Inhibit Isoproterenol Induced Tachycardia (b1) -Minimal Effect on Isoproterenol Induced Hypotension (b2) - Withdrawn due to Visual Loss
- Prazosin - Reversible Selective a1-Blockers - Class: Quinazoline - Hypotensive Effect
- Pronethalol - Non Selective b-Blocker with partial Agonist Effect - Class: Arylethanolamine - Was Carcinogenic in Animals
- Propranolol - Non Selective b-Blocker - Class: Aryloxypropanolamine - x10 Potent Pronethalol - Not Carcinogenic - No Agonist Effect - Used in Hypertension, Angina Pectoris, Arrhythmias, Migraine Clearance: Hepatic
- Tamsulosin -Reversible Selective a1-Blockers Class: ArylSulfonamide - High Affinity to a1 A-subtype in the Prostate - Treat Benign Prostatic Hyperplasia
- Terazosin - Reversible Selective a1-Blockers - Class: Quinazoline - Hypotensive Effect
- Tolazoline - Reversible Nonselective a-Blocker - Class: Imidazoline - No Agonistic Effect - Limited Use in Pheochromocytoma (Still EPI Release)
- Yohimbine - Reversible Selective a2-Blockers - Class: Indole - Alkaloid (Yohimbe Bark) - Increase BP (Block -ve Feedback) -Increase HR (Block -ve Feedback) - Limited Use for Male Sexual Impotency
- Levobunolol - Non Selective b-Blocker
- Carteolol - Non Selective b-Blocker
- Metipranolol - Non Selective b-Blocker
- Nadolol - Non Selective b-Blocker - Clearance: Renal
- Penbutolol - Non Selective b-Blocker
- Pindolol - Non Selective b-Blocker - Clearance: Hepatic + Renal
-Sotalol - Non Selective b-Blocker
- Timolol - Non Selective b-Blocker
- Acebutolol - Selective b1-Blocker
- Atenolol - Selective b1-Blocker - Clearance: Renal
- Betaxolol - Selective b1-Blocker
- Esmolol - Selective b1-Blocker
- Metoprolol - Selective b1-Blocker - Clearance: Hepatic
- Bisoprolol - Selective b1-Blocker
- Labetalol - Non Selective b and a1 Blocker - Antihypertensive
- Carvedilol - Non Selective b and a1 Blocker - Antihypertensive
- Metirosine - Tyrosine Hydroxylaze Inhibitor
- Carbidopa - L-DOPA Decarboxylaze Inhibitor
- Reserpine - Class: Indole - Alkaloid (Rauwolfia Serpentina) - Inhibits catecholamine storage in storage vesicles
- Guanadrel - Neuronal Blocking Agents
- Guanethidine - Neuronal Blocking Agents
- Bretylium - Neuronal Blocking Agents
- Ergotamine - Alkaloid (Claviceps Purourea) - Mixed Agonist/Antagonist - Potent Inducer of Uterine Contraction (Not Used) - Migraine Treatment
- Ergonovine - Alkaloid (Claviceps Purourea) - Potent Inducer of Uterine Contraction (Used) - Better Bioavailability than Ergotamine
- Methylergonovine - Alkaloid (Claviceps Purourea) - Potent Inducer of Uterine Contraction (Used) - Better Bioavailability than Ergotamine
- Methylsergide - Alkaloid (Claviceps Purourea) - Migraine Treatment
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