26744847
Description
Flashcards by Majd Fawaz, updated more than 1 year ago
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Created by Majd Fawaz
over 3 years ago
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| Question | Answer |
| - 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 | |
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Image:
L Dopa (binary/octet-stream)
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- 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 | |
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Image:
Vma (binary/octet-stream)
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- 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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