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54 Cards in this Set
- Front
- Back
Diphenhydramine competitively blocks
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H1-receptors.
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Many drugs with H1-receptor antagonist properties have considerable ___________________________ activity
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Many drugs with H1-receptor antagonist
properties have considerable antimuscarinic, or atropine-like, activity (eg, dry mouth), or antiserotonergic activity (antiemetic). |
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H2-blockers reduce the perioperative risk of aspiration pneumonia by 2X
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by decreasing gastric fluid volume and raising the pH of gastric contents.
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Metoclopramide works 3 ways
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increases lower esophageal sphincter tone,
speeds gastric emptying, and lowers gastric fluid volume by enhancing the stimulatory effects of acetylcholine on intestinal smooth muscle. |
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Ondansetron, granisetron, and dolasetron selectively block
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Ondansetron, granisetron, and dolasetron selectively block serotonin 5-HT3
receptors, with little or no effect on dopamine receptors. |
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5-HT3 receptors play an important role in
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the initiation of the vomiting reflex.
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Ketorolac is
works by |
Ketorolac is a parenterally administered nonsteroidal antiinflammatory drug
that provides analgesia by inhibiting prostaglandin synthesis. |
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Clonidine useful in management of patients with
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neuropathic pain who become increasingly
resistant to epidural opioid infusions. |
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Dexmedetomidine is a
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parenteral selective a2-agonist with sedative
properties. It appears to be more selective for the a2-receptor than clonidine. |
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Naloxone reverses
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the agonist activity associated with endogenous or
exogenous opioid compounds. |
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useful in the reversal of benzodiazepine sedation and the treatment of benzodiazepine overdose.
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Flumazenil
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Aspiration does not necessarily result in aspiration pneumonia. The
seriousness of the lung damage depends on |
the volume and composition of the aspirate.
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Patients are at risk for aspiration pneumonia if 2X
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their gastric volume is greater than 25 mL (0.4 mL/
kg) and their gastric pH is less than 2.5. |
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Histamine is found in 3X
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the central nervous system, in the gastric mucosa, and in
other peripheral tissues. |
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Histaminergic neurons are primarily located in
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the posterior hypothalamus but have wide
projections in the brain. |
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Histamine also normally plays a major role in the secretion of
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hydrochloric acid by parietal cells in the stomach
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The highest concentrations of histamine are found in
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the storage granules of circulating basophils and
mast cells throughout the body. |
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Mast cells tend to be concentrated in
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connective tissue
just beneath epithelial (mucosal) surfaces. |
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Histamine release (degranulation) from mast cells can be triggered by 3X
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chemical, mechanical, or immunological stimulation
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Secretion of hydrochloric acid is normally mediated by
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gastrin-induced histamine release from
enterochromaffin-like cells in the stomach. |
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Two receptors, _____ ans _____ mediate the effects of histamine.
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H1 and H2,
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The H1-receptor
activates |
phospholipase C,
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H2-receptor activates
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increases intracellular cyclic
adenosine monophosphate (cAMP). |
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An H3-receptor is primarily located on
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histaminesecreting
cells and mediates negative feedback, inhibiting the synthesis and release of additional histamine. |
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Cardiovascular
Histamine |
reduces arterial blood pressure but increases heart rate and myocardial
contractility |
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Cardiovascular
H1-Receptor stimulation increases |
capillary permeability and enhances
ventricular irritability, |
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Cardiovascular
H2-receptor stimulation |
increases heart rate and increases contractility.
|
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Respiratory
Histamine |
constricts bronchiolar smooth muscle via the H1-receptor. H2-Receptor
stimulation may produce mild bronchodilation. |
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Respiratory
Histamine H1-receptor |
appears to mediate some pulmonary
vasodilation |
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Respiratory
Histamine H2-receptor |
histamine-mediated
pulmonary vasoconstriction. |
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Gastrointestinal
Activation of H2-receptors |
parietal cells increases gastric acid secretion
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Gastrointestinal
Stimulation of H1-receptors |
leads to contraction of intestinal smooth muscle
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histamine Dermal
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The classic wheal-and-flare response of the skin to histamine results from
increased capillary permeability and vasodilation and is primarily via H1-receptor activation. |
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Immunological
Histamine |
is a major mediator of type 1 hypersensitivity reactions (see Chapter
46). H1-Receptor stimulation attracts leukocytes and induces synthesis of prostaglandin. In contrast, the H2-receptor appears to activate suppressor T lymphocytes. |
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diphenhydramine blocks
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competitively blocks H1-receptors
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Promethazine is a
blocking properties 2x |
phenothiazine derivative with H1-
receptor antagonist activity as well as antidopaminergic and -adrenergic–blocking properties. |
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Antacids neutralize the acidity of gastric fluid by
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providing a base (usually
hydroxide, carbonate, bicarbonate, citrate, or trisilicate) that reacts with hydrogen ions to form water. |
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Metoclopramide acts peripherally as
centrally as |
acts peripherally as a cholinomimetic (ie, facilitates acetylcholine
transmission at selective muscarinic receptors) and centrally as a dopamine antagonist. |
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Metoclopramide produces an antiemetic effect by
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blocking dopamine receptors in
the chemoreceptor trigger zone of the central nervous system |
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metoclopramide is
contraindicated in |
patients with complete intestinal obstruction
|
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(Prilosec), lansoprazole (Prevacid), rabeprazole
(Aciphex), and pantoprazole (Protonix) work by |
bind to the proton pump of parietal cells in the
gastric mucosa and inhibit secretion of hydrogen ions. |
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Ondansetron (Zofran), granisetron (Kytril), and dolasetron (Anzemet) selectively
block serotonin |
5-HT3 receptors, with little or no effect on dopamine receptors
|
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Ketorolac is a parenterally administered nonsteroidal antiinflammatory drug (NSAID) that provides analgesia by
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by inhibiting prostaglandin synthesis
|
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ketorolac has a duration of action
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duration of action (6–8 h).
|
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ketorolac
heme wise |
ketorolac inhibits platelet aggregation and prolongs bleeding time
|
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ketorolac elimination
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ketorolac depends on elimination by the kidneys, it should not be given to patients in renal failure. Ketorolac is contraindicated in patients allergic to aspirin or NSAIDs.
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Mechanism of Action
Clonidine |
imidazoline derivative with predominantly a2-adrenergic agonist activity
penetrates the blood–brain barrier activates inhibitory neurons. The overall effect is to decrease sympathetic activity, enhance parasympathetic tone, and reduce circulating catecholamines |
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clonidine
diabetic patients |
Lastly, clonidine can mask the symptoms of hypoglycemia in diabetic patients
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Mechanism of Action
Dexmedetomidine (Precedex) |
Dexmedetomidine (Precedex) is a parenteral selective 2-agonist with sedative properties
|
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Dexmedetomidine
principal side effects |
bradycardia, heart block, and hypotension
|
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Dexmedetomidine
recommended initial loading dose |
1 mcg/kg intravenously over 10 min with a maintenance infusion rate of 0.2–0.7 mcg/kg/h. Dexmedetomidine has a rapid onset and terminal half-life of 2 h.
|
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Mechanism of Action
Naloxone |
competitive antagonist at opioid receptors.
Naloxone has no significant agonist activity. |
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Naloxone reverses
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the agonist activity associated with endogenous (enkephalins, endorphins) or exogenous opioid compounds.
|
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narcan
Abrupt reversal of opioid analgesia can result in |
sympathetic stimulation (tachycardia, ventricular irritability, hypertension, pulmonary edema) caused by pain perception, an acute withdrawal syndrome in patients who are opioid dependent or vomiting. The extent of these side effects is proportional to the amount of opioid being reversed and the speed of the reversal.
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