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Key terms
Agonists drugs with a specific receptor Affinity that mimic the body's natural chemicals example hormones or neurotransmitters
Angina paroxysmal (sudden) chest pain caused by myocardial ischemia
Antagonist drugs that bind to a specific receptor and inhibit or block the response of The receptors
Dysrhythmias irregular heart rhythms generally called arrhythmia and clinical practice
Extravasation the leaking of fluid from a blood vessel into the surrounding tissues as in the case of infiltrated intravenous infusion
First dose phenomenon severe and sudden drop in blood pressure after the administration of the first dose of an alpha adrenergic blocker
Acrocyanosis decreased amount of oxygen delivered to the extremities causing the feet or hands to turn blueAdrenergic receptors specific receptor sites located throughout the body for the endogenous sympathetic neurotransmitters norepinephrine and epinephrineAgonists drugs with a specific receptor Affinity that mimic the body's natural chemicals example hormones or neurotransmitters Angina paroxysmal (sudden) chest pain caused by myocardial ischemia Antagonist drugs that bind to a specific receptor and inhibit or block the response of The receptors Dysrhythmias irregular heart rhythms generally called arrhythmia and clinical practice Extravasation the leaking of fluid from a blood vessel into the surrounding tissues as in the case of infiltrated intravenous infusion First dose phenomenon severe and sudden drop in blood pressure after the administration of the first dose of an alpha adrenergic blocker Intrinsic sympathomimetic activity the paradoxical action of some beta blocking drugs that mimics the action of the sympathetic nervous system Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Adrenergic receptors specific receptor sites located throughout the body for the endogenous sympathetic neurotransmitters norepinephrine and epinephrineAgonists drugs with a specific receptor Affinity that mimic the body's natural chemicals example hormones or neurotransmitters Angina paroxysmal (sudden) chest pain caused by myocardial ischemia Antagonist drugs that bind to a specific receptor and inhibit or block the response of The receptors Dysrhythmias irregular heart rhythms generally called arrhythmia and clinical practice Extravasation the leaking of fluid from a blood vessel into the surrounding tissues as in the case of infiltrated intravenous infusion First dose phenomenon severe and sudden drop in blood pressure after the administration of the first dose of an alpha adrenergic blocker Intrinsic sympathomimetic activity the paradoxical action of some beta blocking drugs that mimics the action of the sympathetic nervous system Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Agonists drugs with a specific receptor Affinity that mimic the body's natural chemicals example hormones or neurotransmitters Angina paroxysmal (sudden) chest pain caused by myocardial ischemia Antagonist drugs that bind to a specific receptor and inhibit or block the response of The receptors Dysrhythmias irregular heart rhythms generally called arrhythmia and clinical practice Extravasation the leaking of fluid from a blood vessel into the surrounding tissues as in the case of infiltrated intravenous infusion First dose phenomenon severe and sudden drop in blood pressure after the administration of the first dose of an alpha adrenergic blocker Intrinsic sympathomimetic activity the paradoxical action of some beta blocking drugs that mimics the action of the sympathetic nervous system Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules
Intrinsic sympathomimetic activity the paradoxical action of some beta blocking drugs that mimics the action of the sympathetic nervous system Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Pheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation
Lipophilicity the chemical attraction of a substance example drug molecule two lipid or fat molecules Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Orthostatic hypotension a sudden drop in blood pressure when a person stands up. Also referred to as postural hypotension or Ortho stasisPheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Pheonchromocytoma avascular adrenal gland tumor that is usually benign but secretes epinephrine and norepinephrine and thus often causes CNS stimulation and substantial blood pressure elevation Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Raynaud's disease a narrowing of small arteries that limits the amount of blood circulation in the extremities, causing numbness of the nose, fingers, toes, and ears and their response to cold temperatures or stress
Sympatholytics drugs that inhibit the postganglionic functioning of the sympathetic nervous system
Overview
The autonomic nervous system consists of the parasympathetic and sympathetic nervous system the class of drugs discussed in this chapter Works primarily on the sympathetic nervous system androgenic blockers have the opposite effect and therefore referred to as antagonist. They bind to adrenergic receptors comma but in doing so inhibit or block stimulation by the CNS. They are also referred to as sympatholytics because they lyse or inhibit SMS to mulation. That alpha-1 adrenergic receptors are located on the tissue, muscle, or organ that the nervous stimulating postsynaptic effector cells. The Alpha 2 adrenergic receptors are located on the actual nerves that stimulate the presynaptic effector cells. The Alpha 2 receptors are inhibitory and nature. Thus, it is actually the stimulation of Alpha 2 receptors that causes the inhibitory effects of the CNS. Alpha to active drugs example clonidine are discussed in chapter 22. The beta 1 receptors are located primarily in the Heart. The beta-2 receptors are located primarily in the smooth muscle of the bronchioles and blood vessels. It is at these various receptors that and Androgen blockers Act. They are classified by the type of engine ergic receptor they block. Alpha or beta or in some cases both. Hence, they are called alpha blockers, beta blockers comma or alpha beta blockers.
Alpha blockers mechanism of action and drug effects
The alpha adrenergic blocking drugs are alpha blockers, interrupt stimulation of the SNS at the alpha-1 adrenergic receptors. More specifically, alpha blockers work either by direct competition with norepinephrine or by non-competitive process. Alpha blockers have a greater affinity for Alpha and genetic receptors than the norepinephrine does and therefore can chemically replace norepinephrine molecules from the receptor. And adrenergic blockade at these receptor lead two effects such as basal dilation comma reduce blood pressure comma meiosis pupillary constriction comma and reduced smooth muscle tone and organs such as the bladder and prostate.
Alpha blockers indications
The alpha blockers such as doxazosin comma prazosin, terazosin cars both arterial and venous dilation, which reduce peripheral vascular resistance and blood pressure. These drugs are used to treat hypertension. There are also alpha-adrenergic receptors in the prostate and bladder. By blocking stimulation of alpha 1 receptors, these drugs reduce smooth muscle contraction of the bladder neck and the prostatic portion of the urethra. For this reason, alpha blockers are given to patients with BPH to decrease resistance two urinary outflow. This reduces urinary obstruction and relieve some of the effects of BPH.
Alpha blockers contraindications
Contraindications to the use of alpha blocking drugs include known drug allergies and peripheral vascular disease and may include hepatic and renal disease, coronary artery disease, peptic ulcer, and sepsis
Alpha blockers adverse effects
The primary adverse effects of alpha blockers are those related to the effects of vasculature. First dose phenomenon which is the severe and sudden drop in blood pressure after the administration of the first dose of an alpha adrenergic blocker comma can cause the patient's to fall or pass out. All patients must be warned about this verse effect before they take their first dose of an alpha blocker. Patients should be warned to get up slowly from a Supine position. Common adverse effects include dizziness, headache, and constipation.
Alpha blockers toxicity and management of overdose
With over doses of both oral and injectable forms, sympathetic and supportive measures are to be instituted as needed blood pressure is supported with the administration of fluids, volume expanders, and vasopressor drugs comma and anticonvulsant such as diazepam are administered for the control seizures.
Alpha blockers interactions
The most of your drug interactions with alpha blockers are those that potentiate the effects of the alpha blockers. Alpha blockers are very highly protein-bound and compete for binding sites with other drugs that are highly protein-bound. Because of the limited sites for binding and proteins and the increased competition for these sites comma more free Alpha blocker molecules circulate in the bloodstream. More active drug results in a more pronounced drug effect.
Alpha blockers drug profiles
Phentolamine is an alpha blocker that reduces peripheral vascular resistance and is also used to treat hypertension.
Tamsulosin is an alpha blocker used primarily to treat BPH and as exclusively indicated for male patients. Blocks Alpha Androgen receptors on smooth muscle within the prostate and bladder. This results in relaxation of the smooth muscle fibers and improved urinary flow. Contraindications of tamsulosin include known drug allergy and concurrent use of erectile dysfunction drugs such as Cedella Phil. Adverse effects include headache and normal ejaculation, rhinitis. Interacting drugs include other alpha blockers, calcium channel blockers, ED drugs.
Beta blockers mechanism of action and drug effects
The beta adrenergic blocking drugs beta blockers black SNS stimulation of the beta adrenergic receptor by competing with norepinephrine and epinephrine. The beta blockers can be either selective or non-selective depending on the type of beta adrenergic receptor if they antagonize. Beta-1 adrenergic receptors are located primarily in the heart. Beta blockers that are selective for these receptors are called cardioselective beta blockers or beta 1 blocking drugs. Other beta blockers black both they don't one and beta-2 adrenergic receptors and are referred to as non selective beta-blockers. Beta-2 receptors are located primarily on the smooth muscle of the bronchioles and blood vessels. Drugs with intrinsic sympathetic activity not only block beta adrenergic receptors but also primarily stimulate them. Two beta blockers, Carvedilol and labetalol, also have Alpha receptor blocking activity especially in higher doses. Cardioselective beta 1 blockers block the beta 1 receptors on the surface of the heart. This reduces myocardial stimulation which in turn reduces heart rate, so is conduction through the AV node, prolongs SA node recovery, and decreases myocardial oxygen Demand by decreasing myocardial contractile Force. Nonselective beta-blockers not only have these cardiac effects, but they block beta-2 receptors on the smooth muscle of the bronchioles and blood vessels as well.
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