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Neuropharmacology 1
Sympatholytic Drugs (Blockers/Antagonists) (Direct and Indirect Acting)
| Drug | Indication | MOA | |
|---|---|---|---|
| Metyrosine (Demser) | Indirect Sympatholytic Target NE Synthesis | Treatment of Hypertension (pheochromocytoma) 2ndary treatment to phenoxybenzamine and other alpha adrenergic blocking drugs for hypertension | Inhibit tyrosine hydroxylase Deplete catecholamines in SNS nerve terminal, adrenal medulla, CNS ADR: Hypotension, Diarrhea, Nasal Stuffiness (vasodilation) |
| Reserpine (Serpasil) | Indirect Sympatholytic Target NE Storage (in vesicles) | Treatment of Hypertension (rarely used); Low dose combined with diuretics to control BP in elderly Contraindicated for patients with peptic ulcers and mental depression | Irreversibly blocks catecholamine uptake into nerve terminal storage granules (leading to long-term depletion of catecholamines) ADR: Depletion of dopamine and serotonin; sedation/inability to concentrate/complex tasks; psychotic depression/suicide |
| Clonidine, Methyldopa, Guanfacine | Indirect Sympatholytic Alpha 2 Agonist (decrease NE release) | ||
| Guanethidine, bretylium | Indirect Sympatholytic Vesicular Fusion Blocker | Inhibit vesicular fusion to membrane | |
| Regitine | Direct Sympatholytic Non-Selective Alpha 1/2 Receptor Antagonist Phentolamine | Pheochromocytoma & treatment of hypertensive crisis due to pheochromocytoma; Reverse toxicity of α-agonist; Prevent or treat necrosis after extravasation of IV NE or other α-agonists | Inhibition type: Reversible, competitive |
| Oraverse | Direct Sympatholytic Non-Selective Alpha 1/2 Receptor Antagonist Phentolamine | Reverse local anesthesia after dental procedure | Inhibition type: Reversible, competitive |
| Dibenzyline | Direct Sympatholytic Non-Selective Alpha 1/2 Receptor Antagonist Phenoxybenzamine | Hypertensive crisis due to pheochromocytoma (tumors of adrenal medulla) or due to sympathomimetics | Inhibition type: Irreversible |
| Doxazosin (Cardura) Prazosin (Minipress) Terazosin (Hytrin) | Direct Sympatholytic Selective Alpha 1 Antagonist | Hypertension and BPH; Used with other hypertension drugs to treat hypertension | α1B > α1A, α1D (high affinity for 1B- found in blood vessels); ADR: “first dose effect” Symptomatic orthostatic hypotension occurs within 30-90 min of the initial dose of the drug. |
| Alfuzosin (UROXATRAL) | Direct Sympatholytic Selective Alpha 1 Antagonist | BPH | α1B > α1A, α1D; Selectively accumulates in prostate tissue No orthostatic hypotension |
| Tamsulosin (FLOMAX) Silodosin (RAPAFLO) | Direct Sympatholytic Selective Alpha 1 Antagonist | BPH | α1A > α1B = (Lower chance of orthostatic hypotension); Less need for dose titration; metabolized by CYP3A4 so potential drug interactions with CYP3A4 inhibitors |
| Major Adverse Effects of Alpha Blockade | 1. Orthostatic Hypotension (Drop in BP upon Standing via blocking receptors on arteries and veins (Venous tone))- blood pools in veins when standing 2. Nasal Congestion (dilate blood vessels of nasal mucosa) | 3. Inhibition of ejaculation (decrease in semen; major reason for noncompliance) 4. Miosis 5. Reflex tachycardia (decrease BP leads to reflex tachycardia)(blocking of alpha 2 receptor = increased release of NE and increase B1 receptor stimulation**) | 6. Intraoperative Floppy Iris Syndrome (during cataract surgery): iris bulges toward cornea 7. Priapism (permanent impotence) Drug Interactions: PDE5 inhibitors (sildenafil, tadalafil, vardenafil) Epinephrine Reversal (Pressor to depressor response) |
| Yohimbine and Atipamezole (Antisedan) | Direct Sympatholytic Alpha 2 Antagonist | ED, Hypotension, Weight Loss; Raises BP & HR (more SNS effect) | blocks alpha2 receptors to elicit increased central sympathetic activity, increased NE release ADR: anxiety, increased blood pressure |
| Carvedilol (Coreg); Labetalol (Trandate); Nadolol (Corgard); Propranolol (Inderal); Sotalol (Betapace) CLPSN | Direct Sympatholytic Beta Antagonist B1/B2 (Beta Blocker 1st Gen) | Hypertension (Inhibit Renin Activity); Angina ,MI , and Congestive heart failure (Decrease O2 demand); SVT (slow AV condition); Open angle glaucoma (decrease aq humor synthesis); Anxiety/Alcohol withdrawal (Decrease SNS responses) ; | Migraine Prophylaxis Block B1 receptor of thamlus to normalize vascular tone in brain); MOA: 1. Negative inotropic/ chronotropic effects (decrease cardiac output) 2. Decrease renin secretion from kidney (prevent renin--> angiotensin II= decrease CO) |
| Atenolol (Tenormin); Bisoprolol (Zebeta); Esmolol (Brevibloc); Metoprolol (Lopressor); Nebivolol (Bystolic) AB-MEN | Direct Sympatholytic Beta 1 Antagonist (Beta Blocker 2nd Gen) | Hypertension (Inhibit Renin Activity); Angina ,MI , and Congestive heart failure (Decrease O2 demand); SVT (slow AV condition); Open angle glaucoma (decrease aq humor synthesis); Anxiety/Alcohol withdrawal (Decrease SNS responses) ; | Migraine Prophylaxis Block B1 receptor of thamlus to normalize vascular tone in brain); MOA: 1. Negative inotropic/ chronotropic effects (decrease cardiac output) 2. Decrease renin secretion from kidney (prevent renin--> angiotensin II= decrease CO) |
| Adverse Effects of Beta-Blockers | 1. Unfavorable lipid profile (high LDL; TAG, VLDL and lower HDL); AV block; sinus bradycardia; worsen CHF; rebound cardiac excitation if suddenly discontinued; reduce response to exercise; | 2. Inhibit warning sign of hyperthyroidism )due to tachycardia 3. Increases serum potassium (hyperkalemia) 4. Loss of libido 5. Depression | Precaution: Diabetics (B2 effect on pancreases control of insulin secretion (Blockade decrease secretion of insulin in response to hyperglycemia= hypoglycemia) Pheochromocytoma (small tumor secretes NE and EPI) |
| Adverse Effects of Beta-Blockers | Contraindications: CHF, Bradycardia, slow heart beats, asthma and COPD (especially non-selective beta blockers); pulmonary edema | Drug interactions: increase the pressor response of alpha agonists (Beta 2 receptors are in blood vessels; inhibiting them leads to vasoconstriction) ; increase the effect of other antihypertensive | |
| Acebutolol(Spectral) Propranolol (Inderal) | Direct Sympatholytic Beta 1 Antagonist (Membrane Stabilizing Effect ) | inhibit fast sodium channels | (also known as type I antidysrhythmic activity) are said to possess membrane-stabilizing activity. |
| Acebutolol (Spectral) Pindolol (Visken) | Direct Sympatholytic Beta 1 Antagonist (Intrinsic Sympathomimetic Activity ) | Advantageous to treat people with asthma | Partial agonists at β-adrenergic receptors and are said to have intrinsic sympathomimetic activity (ISA). |
| Acebutolol (Spectral) Sotalol (Betapace) Ignore everything below | Direct Sympatholytic Beta 1 Antagonist (Potassium Channel Blockade) | Both prolongs the action potential duration and is manifested on the electrocardiogram (ECG) by a prolonged QT interval. | Sotalol blocks the delayed rectifier potassium current responsible for repolarization. Acebutolol blocks outward potassium channels |
| Carvedilol (Coreg) Labetalol (Trandate) | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Vasodilation | Beta Blockers with alpha1 antagonist activity |
| Nebivolol (Bystolic) Carteolol (Ocupress) Celiprolol (Selectol) | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Nebivolol: Hypertension and CHF | β1 selective antagonist + increase NO synthesis (reduce inotropic effects of β1 stimulation. protect effects of excessive SNS stimulation) Increase NO synthase activity in endothelial cells =increase release of NO (nitric oxide) =vasodilation. |
| Bucindolol(Sandonorm) Carteolol (Ocupress) Celiprolol (Selectol) | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Vasodilation | Beta Blockers with Beta2 adrenergic receptor agonist activity |
| Betaxolol (Kerlone, Betoptic) Carvedilol (Coreg) | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Coreg: Hypertension; CHF | Beta blockers with some calcium channel blocking properties Coreg: nonselective β antagonist + α1 receptor antagonist advantage: greater antihypertensive effect disadvantage: greater incidence of orthostatic hypotension |
| Esmolol (BREVIBLOC) IV | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Fast onset (2-10’) and short duration of action (10-30’) | β1 selectivity and onset / duration kinetics enable treatment of intra-operative and post-op tachycardia, severe hypertension |
| Timolol (Timoptic, Betimol) | Direct Sympatholytic Beta 1 Antagonist 3rd Gen | Treatment for increased intraocular pressure from glaucoma (buildup of pressure in eye) | no local anesthetic effect good penetration into ocular tissue ADR: absorption into systemic circulation may result in cardiovascular and respiratory ADRs |
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toppharmacist
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