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MagusB81
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Nerve impulses are conducted by electrical and chemical means; the chemical protion of nerve transsmission is referred to as a?
Neurotransmitter
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The neurotransmitter at the myoneural(neuromuscular) junction , at ganglia, and at the parasympathetic sites is?
acetycholine
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The neurotransmitter at sympathetic end sites except sweat glands, adrenal medulla?
norepinephrine
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circulating epinephrine stimulates all recptors responding too _______, even if no sympathetic nerves are present.
norepinephrine
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THis system allows discrete control in the body.
Parasympathetic
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This system causes a widespread reaction in the body
Sympathetic
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This nervous system control is essential to life and is concidered a more discrete, finely regulated system. Effects day-to-day bodily functions of digestion, bladder and rectal discharge, and basal secretion of bronchial mucus.
Parasympathetic
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Overstimulation of the parasympathetic branch would render the body incapable of violent action, resulting in what is termed the SLUD syndrome:
salivation, lacrimation, urination, and defecation
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What iss the effect of parasympathetic system on heart rate?
Slows rate (vagus)
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What is thee effect of parasympathetic system on the bronchial smooth muscle?
constriction
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What is the effect of parasympathetic system on the exocrine glands?
increased secretions
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Two additional terms are used to refer to stimulation of receptor sites for Ach; they are derived from the action in the body of two substances:
muscarine and nicotine
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refers to cholinergic receptors at parasympathetic end sites.
muscarinic
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Muscarinic receptors are distinguished into subtypes
M1-M5
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Where are M2 receptors located?
in the heart
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Where are M3 receptors located?
on airway smooth muscle, mediating bronchoconstriction
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a natural product from the mushroom Amanita muscaria, stimulates Ach (cholinergic) receptors at the parasympathetic terminal sites: exocrine glands (lacrimal, salivary, and bronchial mucous glands), cardiac muscle, and smooth muscle (gastrointestinal tract).
Muscarine
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Ach receptor sites that are effected by musarine are termed as
muscarinic
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A muscarinic effect well known to respiratory care clinicians is the increase in airway secretions after administration of Ach-like drugs such as
Neostigmine
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a parasympathomimetic effect is the same as a
muscarinic effect
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a parasympatholytic effect is referred to as an
antimuscarinic effect
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refers to cholinergic receptors on ganglia and at the neuromuscular junction
nicotinic
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a substance in tobacco products, stimulates Ach (cholinergic) receptors at autonomic ganglia (parasympathetic and sympathetic) and at skeletal muscle sites.
Nicotine
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Ach receptors at autonomic ganglia and at the skeletal muscle are termed and as are the effects on these sites of stimulation
Nicotinic
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Parasympathetic receptors and cholinergic receptors in general with or without corresponding nerve fibers are classified further into subtypes. These differences among cholinergic or muscarinic (M) receptors are based on different responses to different drugs, or recognition through use of DNA probes. Five muscarinic receptor subtypes have been identified:
M1-M5
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When using indirect-acting cholinergic agents such as neostigmine to increase nerve function at the neuromuscular junction, Ach activity at parasympathetic sites such as salivary and nasopharyngeal glands also increases. These undesirable muscarinic effects can be blocked by pretreatment with a parasympatholytic or antimuscarinic drug such as
Atropine
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form an irreversible bond with cholinesterase (also called acetylcholinesterase). used as insecticides, and occasionally patients are seen with toxic exposure and absorption. The effects of these agents can be lethal, and because of this, they have also been used as �nerve gas".
Organophosphates
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parathion and malathion and the drug echothiophate are what kind of drug?
Organophosphates
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The bonding of irreversible inhibitors with cholinesterase is slow, taking up to 24 hours. Once formed, however, the duration is limited only by the body's ability to produce new cholinesterase, which takes
1-2 weeks
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block Ach receptors and act as cholinergic antagonists. Parasympatholytic (antimuscarinic) agents such as atropine and drug classes such as neuromuscular blockers and ganglionic blockers
Anticholinergic agents
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is usually considered the prototype parasympatholytic, occurs naturally as the levo isomer in Atropa belladonna, the nightshade plant, and in Datura stramonium, or jimsonweed. The drug is referred to as a belladonna alkaloid.
Atropine
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is a competitive antagonist to Ach at muscarinic receptor sites (glands, gastrointestinal tract, heart, and eyes) and can form a reversible bond with these cholinergic receptors. It is nonspecific for muscarinic receptor subtypes and blocks M1, M2, and M3 receptors.
Atropine
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Atropine blocks salivary secretion and causes
dry mouth
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atropine decreases secretion by mucous glands and relaxes bronchial smooth muscle by blocking parasympathetically maintained
basal tone
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Sympathetic effects on the cardiopulmonary system include:
Increased heart rate/contractile force/BP/secretions in airway
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The primary method of terminating the action of norepinephrine at the postsynaptic membrane is through a reuptake process, back into the presynaptic neuron. This is termed
Uptake - 1
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The neurotransmitter action can be ended by two other mechanisms as well: uptake into tissue sites around the nerve terminal, a process termed
Uptake-2
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norepinephrine can stimulate autoreceptors on the presynaptic neuron, which inhibits further neurotransmitter release. These autoreceptors have been identified as
Alpha 2 receptors
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This process is a mediated uptake of exogenous amines (chemicals such as norepinephrine) in nonneuronal tissues.
Uptake - 2
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Agent that stimulates sympathetic nervous fibers, which allow relaxation of smooth muscle in the airway. Also known as sympathomimetic bronchodilator or �2 agonist.
Adrenergic bronchodialtor
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Causes vasoconstriction and vasopressor effect; in the upper airway (nasal passages), this can provide decongestion.
Alpha-recptor stimulation
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Refers to the increasing incidence of asthma morbidity, and especially asthma mortality, despite advances in the understanding of asthma and availability of improved drugs to treat asthma.
Asthma paradox
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Causes increased myocardial conductivity and increased heart rate as well as increased contractile force.
Beta 1- receptor stimulation
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Causes relaxation of bronchial smooth muscle, with some inhibition of inflammatory mediator release and stimulation of mucociliary clearance.
Beta 2 - receptor stimulation
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Narrowing of the bronchial airways, caused by contraction of smooth muscle.
Bronchospasm
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Group of similar compounds having sympathomimetic action; they mimic the actions of epinephrine.
Catecholamines
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Nucleotide produced by Beta2 -receptor stimulation; it affects many cells, but causes relaxation of bronchial smooth muscle.
Cyclic adenosine 3�, 5�-monophosphate (cAMP)
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Nucleotide producing the opposite effect of cAMP; that is, it causes bronchoconstriction.
Cyclic guanosine monophosphate (cGMP)
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Long-term desensitization of Beta receptors to Beta 2 agonists, caused by a reduction in the number of Beta receptors.
Downregulation
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Drug that exhibits its pharmacologic activity when it is converted, inside the body, to its active form
prodrug
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Producing effects similar to those of the sympathetic nervous system.
Sympathomimetic
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The adrenergic bronchodilator group is used for the treatment of reversible airway obstruction in diseases such as
Asthma and COPD
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adrenergic bronchodilators produce bronchodialation by stimulating?
Beta 2 receptors on airway smooth muscle
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are indicated for relief of acute reversible airflow obstruction in asthma or other obstructive airway diseases. Short-acting agents are termed �rescue� agents
Short-acting beta 2 agonists such as albuterol, levalbuterol, or pirbuterol
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Long-acting agents such as salmeterol, formoterol, and arformoterol are indicated for the maintenance of bronchodilation and control of
bronchospasms
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NAEPP EPR 3 guidelines and GINA consider salmeterol, formoterol, and arformoterol �controllers�; the slow time to peak effect makes long-acting agents ___________?
poor rescue drugs
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is often used, either as an inhaled aerosol or by direct lung instillation, for its strong a-adrenergic vasoconstricting effect to reduce airway swelling after extubation or during epiglottitis, croup, or bronchiolitis or to control airway bleeding during endoscopy
Racemic epinephrine
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There are three subgroups of adrenergic bronchodilators based on distinct differences in duration of action:
Ultra-short-acting, short-acting, and long-acting
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What is the duration of ultra-short-acting adrenergic bronchodilators?
less than 3hrs
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What is the duration of short-acting adernergic bronchodilators?
4-6hrs
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what is the duration of long-acting adernergic bronchodilators?
12 hours
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Some examples of ultra-shor-acting adernergic bronchodilators?
Epinephrine, and racemic epinephrine
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Some examples of short-acting adernergic bronchodilators?
Albuterol, levalbuterol, metaproterenol, and pirbuterol
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Some examples of long-acting adernergic bronchodilators?
Salmeterol, formmoterol, and arformeterol
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is a chemical structure consisting of an aromatic catechol nucleus and a dialiphatic amine side chain
catecholamine
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dopamine, epinephrine, norepinephrine, isoproterenol, and isoetharine are all examples of what?
catecholamines or sympathomometic amines
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mimic the actions of epinephrine more or less precisely, causing tachycardia, elevated blood pressure, smooth muscle relaxation of bronchioles and skeletal muscle blood vessels, glycogenolysis, skeletal muscle tremor, and central nervous system (CNS) stimulation
sympathomimetic amines
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rotation on a central carbon atom, produces two nonsuperimposable mirror images
enatiomers or isomers
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have similar physical and chemical properties but different physiologic effects
enatiomers
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is a potent catecholamine bronchodilator that stimulates alpha and beta receptors. is a high prevalence of side effects such as tachycardia, blood pressure increase, tremor, headache, and insomnia.
epinephrine
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Epinephrine occurs naturally in the adrenal medulla and has a rapid onset but a short duration because of metabolism by
catechol O-methyltransferase (COMT)
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The theory that explains the shift from alpha activity to Beta 2 specificity. The larger the side chain attachment to a catechol base, the greater the Beta 2 specificity. If the catecholamine structural pattern is seen as a keylike shape, then the larger the �key� (side chain), the more Beta 2 specific the drug
Keyhole Theory
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catecholamines are rapidly inactivated by the cytoplasmic enzyme
COMT
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Catecholamines are also unsuitable for oral administration because they are inactivated in the gut and liver by conjugation with
sulfate or glucuronide at the carbon-4 site
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Catecholamines are also readily inactivated to inert adrenochromes by
heat, light, or air
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racemic epinephrine is stored in an
amber-colored bottle or a foil-protected wrapper
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Nebulizer rainout (i.e., nebulized particles that condense and fall, under the influence of gravity) in the tubing may appear pinkish after treatment, and a patient's sputum may even appear pink-tinged after using aerosols of
catecholamines
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The basic catecholamine structure, consisting of a catechol ring connected to an amine side chain, directly influences activity. �2-receptor specificity is considered to be due to side chain bulk. What is the name of this Theory?
Keyhole theory
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The short duration of action of catecholamines is due to metabolism by the enzyme
COMT
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Because metaproterenol is not inactivated by COMT, it has a significantly longer duration of action of
4-6 hours
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is the pure (R)-isomer of racemic albuterol
Levalbuterol
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is the single (R)-isomer form of racemic albuterol and is available in an HFA-propelled MDI, with nebulization solution in three strengths: 0.31-mg, 0.63-mg, and 1.25-mg unit doses.
Levalbuterol
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Levalbuterol is also available as a concentrate, __________.
1.25 mg in 0.5 mL.
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The 1.25-mg levalbuterol dose showed a higher peak effect on forced expiratory volume in 1 second (FEV1) with an 8-hour duration compared with
racemic epinephrine
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