Antiadrenergics

• Inhibit activity of the sympathetic nervous system

• Effective in decreasing heart rate,force of myocardial contraction, cardiac output, and blood pressure
Alpha
• Alpha 1 adrenergics receptor blocking agents dilate vessels and Antiadrenergics-Alpha 1
decrease peripheral vascular resistance • Cardura (doxazosin)
• Can experience first dose phenomenon with orthostatic • Minipress (prazosin)
hypotension, dizziness, syncope,possible sodium and fluid retentin • Hytrin (terazosin)
Centrally-Acting Drugs
Alpha-Methyldopa: a prodrug Clonidine: Imidazoline derivative, partial
• Precursor of Dopamine and NA agonist of central alpha-2 receptor
• Methyldopa in adrenergic nerve • Not frequently used now because of tolerance and withdrawal
endings to α-methylNE, which stimulates α2-adrenoceptors receptors hypertension
in brain and causes inhibition of adrenergic discharge in medulla – fall • Clonidine rebound hypertension if suddenly withdrawn
in PVR and fall in BP
• in the medulla and decr sympathetic outflow.
Side-effect: drowsiness, hemolytic anemia.
cognitive impairement, postural hypotension
β
β-Blockers β-Blockers β-Receptors Cardioselective β-Blockers
• Inhibit renin release • Adverse effects: • Distributed throughout the • Greater affinity for β1 than β2
◦ weak association with ◦ bradycardia body ◦ concentrate differently in receptors ◦ inhibit β1 receptors at
antihypertensive effect ◦ atrioventricular conduction certain organs & low to moderate dose ◦ higher
• Negative chronotropic & abnormalities tissues doses block β2 receptors
inotropic cardiac effects reduce ◦ acute heart failure • β1 receptors: • Safer in patients with
CO ◦ abrupt discontinuation may ◦ heart, kidney ◦ stimulation bronchospastic
◦ β-blockers with intrinsic cause unstable increases HR, contractility, renin disease, peripheral arterial
sympathomimetic angina, myocardial infarction, & Release disease,diabetes ◦ may
at high enough doses activity death in patients with high • β2 receptors: exacerbate bronchospastic
(ISA) coronary disease risk ◦ lungs, liver, pancreas, arteriolar disease when selectivity lost at
do not reduce CO lower BP ◦ bronchospastic pulmonary smooth high doses
decrease peripheral resistance disease muscle ◦ dose where selectivity lost
◦ Membrane-stabilizing action on ◦ stimulation causes varies from patientto patient
cardiac cells bronchodilation
 β-Blockers Nonselective β-Blockers
• Cardioselective • Inhibit β1 & β2 receptors at all doses
a ◦ atenolol, betaxolol, bisoprolol, metoprolol,nebivolol • Can exacerbate bronchospastic disease
• Nonselective • Additional benefits in:
◦ nadolol, propranolol, timolol ◦ essential tremor ◦ migraine headache ◦ thyrotoxicosis
• Intrinsic sympathomimetic activity ◦ acebutolol, carteolol,penbutolo • Nadolol, Propranolol
l, pindolol • Avoid in patients with reactive airways disease
• Mixed α- and β-blockers
◦ carvedilol, labetolol
Beta Blockers Side Effects
• Bronchospasm
• Diminished exercise capacity
• Negative inotropy
• Sexual dysfunction
• Bradyarrhythmia
• Masking of hypoglycemia
• Hair loss