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    Classification of Sympatholytic Drugs

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    HlaSoe Win
    This document summarizes various classes of sympatholytic drugs including: 1. Alpha receptor blocking agents such as selective α1 antagonists (e.g. prazosin), non-selective alpha blockers (e.g. tolazoline), and selective α2 antagonists (e.g. yohimbine). 2. Beta receptor blocking agents including non-selective first generation drugs (e.g. propranolol), selective β1 second generation drugs (e.g. atenolol), and third generation drugs with additional actions (e.g. carvedilol, labetalol). 3. Other sympatholytic drugs like clonidine are discussed along with their mechanisms

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    Classification of Sympatholytic Drugs

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    HlaSoe Win
    533 views4 pages
    This document summarizes various classes of sympatholytic drugs including: 1. Alpha receptor blocking agents such as selective α1 antagonists (e.g. prazosin), non-selective alpha blockers (e.g. tolazoline), and selective α2 antagonists (e.g. yohimbine). 2. Beta receptor blocking agents including non-selective first generation drugs (e.g. propranolol), selective β1 second generation drugs (e.g. atenolol), and third generation drugs with additional actions (e.g. carvedilol, labetalol). 3. Other sympatholytic drugs like clonidine are discussed along with their mechanisms

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    Sympatholytic Drugs

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    This document summarizes various classes of sympatholytic drugs including: 1. Alpha receptor blocking agents such as selective α1 antagonists (e.g. prazosin), non-selective alpha blockers (e.g. tolazoline), and selective α2 antagonists (e.g. yohimbine). 2. Beta receptor blocking agents including non-selective first generation drugs (e.g. propranolol), selective β1 second generation drugs (e.g. atenolol), and third generation drugs with additional actions (e.g. carvedilol, labetalol). 3. Other sympatholytic drugs like clonidine are discussed along with their mechanisms

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    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    533 views4 pages

    Classification of Sympatholytic Drugs

    Uploaded by

    HlaSoe Win
    This document summarizes various classes of sympatholytic drugs including: 1. Alpha receptor blocking agents such as selective α1 antagonists (e.g. prazosin), non-selective alpha blockers (e.g. tolazoline), and selective α2 antagonists (e.g. yohimbine). 2. Beta receptor blocking agents including non-selective first generation drugs (e.g. propranolol), selective β1 second generation drugs (e.g. atenolol), and third generation drugs with additional actions (e.g. carvedilol, labetalol). 3. Other sympatholytic drugs like clonidine are discussed along with their mechanisms

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    The key takeaways are the different classes of sympatholytic drugs including alpha blockers, beta blockers, and drugs with both alpha and beta blocking properties. Their main uses are for hypertension, congestive heart failure, and benign prostatic hyperplasia and potential adverse effects include hypotension, fatigue, and sexual dysfunction.

    The different types of sympatholytic drugs discussed are alpha blockers including prazosin and doxazosin, non-selective alpha blockers like phenoxybenzamine, beta blockers which can be selective or non-selective, and drugs with both alpha and beta blocking properties like labetalol and carvedilol.

    The main uses of sympatholytic drugs are for hypertension, congestive heart failure, benign prostatic hyperplasia, treatment of variant angina, reduction of afterload in valvular insufficiency, and control of pheochromocytomas in emergencies.

    Classification of Sympatholytic Drugs

    1. The α receptor blocking agents


    A. α 1 Selective antagonists
    Prazosin and relative drugs: Prazosin, terazosin, doxazosin, alfuzosin,
    Tamsulosin and silodosin (uroselective)
    B. Non-selective α blockers
    Tolazoline, Phentolamine, Phenoxybenzamine
    C. α 2 Selective antagonists - Yohimbine, idazoxan ( not use clinically )
    D. Miscellaneous agents which have alpha blocking action
    - Indoramin (piperidine antiadrenergic), Ketanserin (used as antihypertensive), Urapidil (sympatholytic antihypertensive
    and alpha 1 antagonist and 5-HT1A agonist)
    - Neuroleptic agents (chlorpromazine, haloperidol) and Ergot derivatives

    Selective α 1 blockers: Prazosin, Terazosin, Doxazosin


    Mechanism of Action
    1. Selectively blocks the α 1 receptors of arteries (afterload) and veins (preload) – vasodilation – decrease BP
    2. Persistant α 2 action – decrease central sympathetic outflow, decrease BP
    Pharmacological actions
    1. Fall in BP (not associated with reflex tachycardia in therapeutic dose)
    2. Reduced afterload and preload due to vasodilation
    3. Reduced plasma triglycerides, LDL cholesterol and increase HDL
    4. Relax smooth muscle tone of bladder neck (sphincter) (suitable for pt with BPH)

    Uses

    1. Essential hypertension – Prazosin, doxazosin (especially in pt with heart failure, BPH)


    2. Acute heart failure
    3. BPH

    Pharmacokinetics

    - Route – orally
    - 90 % protein binding
    - Doxazosin – long duration of action (single dose)

    Untoward effects of Prazosin

    1. First dose phenomenon (severe orthostatic hypotension)


    2. Dizziness, headache. Nasal stuffiness, red sclera
    3. Failure of ejaculation in male (block alpha 1 at sphincter muscle)
    4. Micturition incontinence in women (block alpha 1 at sphincter muscle)

    Therapeutic Uses of Sympatholytic Drugs

    A. Hypertension
    B. Congestive Heart Failure
    C. Benign Prostatic Hyperplasia (BPH)
    D. Other Disorders
    3. Treatment of variant angina (Prinzmetal’s angina) due to vasospasm
    4. Treatment of mitral or aortic valvular insufficiency because of reduction of afterload
    Adverse Effects
    5. First-dose effect – postural hypotension and syncope
    6. Increase risk of intra-operative floppy iris syndrome (flaccid and prolapse) in patient receiving oral tamsulosin and
    undergoing cataract surgery
    7. Alfuzosin – increase risk of QT prolong
    8. Non-specific – headache, dizziness, and asthenia (abnormal physical weakness or lack of energy)

    Non-Selective α Adrenergic Antagonists: Phenoxybenzamine and Phentolamine

    9. Phenoxybenzamine - very long duration of action


    10. Phentolamine – short duration of action
    Uses
    11. Pheochromocytomas
    12. Control episodes of severe hypertension and minimize adverse effects of catecholamines
    13. Hypertensive crises (Phentolamine) , follow abrupt withdrawal of clonidine or ingestion of tyramine-containing
    foods during the use of non-selective MAO inhibitors
    Adverse Effects
    14. Postural hypotension, reflex tachycardia, cardiac arrhythmias, myocardial ischaemia and infraction, nasal
    stuffiness, nausea and vomiting, reversible inhibition of ejaculation
    15. Phentolamine stimulate GI smooth muscle and enhance gastric gastric acid secretion due to histamine release

    The β receptor blocking agents

    Classical non-selective β blockers: First generation

    - Propranolol ( prototype)
    - Penbutolol
    - Pindolol
    - Nadolol
    - Timolol
    β 1 selective beta blockers: Second generation
    - Atenoolol
    - Acebutolol
    - Bisoprolol
    - Esmolol
    - Metoprolol
    Non-selective β blockers with additional actions: Third Generation
    - Carvedilol
    - Labetalol
    - Carteolol
    Beta 1 selective β blockers with additional action: Third generation
    - Betaxolol
    - Celiprolol
    - Nevivolol
    Pharmacological Actions:
    Due to blockade of β adrenergic receptors:
    1. Lower BP
    Negative inotropic action – reduce BP, COP
    Inhibit RAA System
    A central action, reduce sympathetic activity
    2. Negative chronotropic action, slow AV conduction – bradycardia and heart block ( little effect on normal heart at
    rest, but profound effect during exercise or stress)
    3. Bronchoconstriction (block β 2 receptor)
    4. Eye – decrease IOP by decrease aqueous humour secretions from ciliary epithelium
    5. Metabolic and endocrine effect
    a) Regulation of lipid – non-selective β blocker elevate plasma TG and lower HDL
    b) Hypoglycaemia – decrease glycogenolysis and decrease glucagon secretion (Masking the sign and symptom of
    hypoglycaemia)
    6. Reduce peripheral blood flow due to reduce CO and cause cold extremities
    Not due to blockade of β adrenergic receptors:
    1. Membrane stabilizing effect (quinidine-like effect) give antiarrhythmic effect
    2. An intrinsic sympathetic activity (ISA)
    3. CNS effects similar to reserpine (with lipid soluble β blockers)

    Therapeutic Uses:
    1. Hypertension – propranolol has central sympathoplegic and tranquilizing action like reserpine,
    Not induce postural hypotension because it does not inhibit reflexes
    2. Arrhythmias
    3. Angina pectoris – reduce cardiac workload and oxygen consumption
    4. Myocardial infraction – cardioprotective effect
    5. Phaeochromocytoma – together with alpha blockers not use alone
    6. Hyperthyroidism – reduce unpleasant symptoms of sympathetic overactivity
    7. Hepatic portal hypertension and esophageal variceal bleeding
    8. Anxiety –palpitation and tremor
    9. Migraine – prophylaxis
    10. Benign essential tremor
    11. Alcohol and opioid withdrawal symptoms – suppress rebound ANS hyperactivity
    12. Glaucoma, chronic open angle glaucoma – timolol, carteolol, betaxolol eye drops ( beta blocker few side
    effects than anticholinesterases or muscarinic agonists)
    13. Hypertrophic subaortic stenosis, Hypertropic Obstructive Cardiomyopathy
    14. Maintainance therapy of clinically table or controlled congested heart failure (carvedilol, bisoprolol,
    metorolol)

    Adverse Effects:
    Due to β blockade:
    1. Bronchospasm (β 2 block) – more common no-selective group
    2. Precipitation of cardiac failure
    3. Heart block
    4. Incapacity for vigorous exercise (exercise intolerance)
    5. Masking the sign and symptoms of hypoglycaemia (such as tachycardia, sweating, tremors)
    6. Hypotension
    7. Cold extremities
    8. Unopposed alpha action – hypertension eg., phaeochromocytoma
    9. Lipid metabolism – decrease HDL, increase TG

    Not due to beta blockade

    1. Fatigue due to reduced CO and muscle perfusion in exercise


    2. Depression, feeling of weakness, gastrointestinal upsets
    3. Bad dreams – mainly highly lipid soluble beta blocker (propranolol)
    4. Abrupt cessation of beta blockers can be dangerous in hypertension, arrhythmia, angina (withdrawal –
    gradual)

    Caution

    1. Pt with antidiabetic treatment (insulin, sulphonyureas)


    2. Patient with hypertriglyceridaemia (can increase TG)

    Contraindications – impending CHF, Acute CHF, cardiogenic shock, heart block, asthma and hypotension

    β receptor blocking agents with additional (α 1 blocking activity)


    cardiovascular effects

    “Third generation” β blockers (hypertensive emergency)

    Labetalol (Injection)
    - Reversible β blockers with concurrent α 1 blocking actions – reduce BP
    - Use in chronic hypertension, emergency control of severe hypertension
    - Alternative to methyldopa in pregnancy induced hypertension
    - Useful for elderly or black hypertensive patients
    - Completely absorb from GI, half-life – 4 hours, extensively metabolized in hepatic first pass
    - Hepatic injury in a few patients

    Carvedilol
    - Antioxidant action, anti-inflammatory action and membrane stabilizing action
    - Decrease lipid peroxidation and vascular wall thickening – benefit heart failure
    - Treatment of hypertension, in stable or controlled congestive heart failure (low dose) and left ventricular dysfunction
    following myocardial infraction

    Clonidine

    - Used to treat - high blood pressure, attention deficit hyperactivity disorder( ADHD), drug withdrawal (alcohol, opioids,
    or smoking), menopausal flushing, diarrhea certain pain conditions and Resistant Hypertension
    - By mouth, by injection, or skin patch. Onset of action is typically within an hour with the effects on blood pressure lasting
    for up to eight hours.
    - Common side effect - dry mouth, dizziness, headaches, and sleepiness. Dizziness, Orthostatic hypotension, Somnolence
    (dose-dependent), Headache (dose-dependent), Fatigue, Skin reactions (if given transdermally),Hypotension
    - Severe side effects - seeing or hearing things that other people do not, heart arrhythmias, and confusion
    - If rapidly stopped - withdrawal effect
    - During pregnancy or breastfeeding is not recommended
    - Lower blood pressure by stimulating α 2 receptors in the brain, which results in relaxation of many arteries.
    -

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