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54 Cards in this Set

  • Front
  • Back
Diphenhydramine competitively blocks
H1-receptors.
Many drugs with H1-receptor antagonist properties have considerable ___________________________ activity
Many drugs with H1-receptor antagonist
properties have considerable antimuscarinic, or atropine-like, activity (eg, dry
mouth), or antiserotonergic activity (antiemetic).
H2-blockers reduce the perioperative risk of aspiration pneumonia by 2X
by decreasing gastric fluid volume and raising the pH of gastric contents.
Metoclopramide works 3 ways
increases lower esophageal sphincter tone,

speeds gastric emptying,

and lowers gastric fluid volume by enhancing the stimulatory effects of
acetylcholine on intestinal smooth muscle.
Ondansetron, granisetron, and dolasetron selectively block
Ondansetron, granisetron, and dolasetron selectively block serotonin 5-HT3
receptors, with little or no effect on dopamine receptors.
5-HT3 receptors play an important role in
the initiation of the vomiting reflex.
Ketorolac is

works by
Ketorolac is a parenterally administered nonsteroidal antiinflammatory drug
that provides analgesia by inhibiting prostaglandin synthesis.
Clonidine useful in management of patients with
neuropathic pain who become increasingly
resistant to epidural opioid infusions.
Dexmedetomidine is a
parenteral selective a2-agonist with sedative
properties. It appears to be more selective for the a2-receptor than clonidine.
Naloxone reverses
the agonist activity associated with endogenous or
exogenous opioid compounds.
useful in the reversal of benzodiazepine sedation and the treatment of benzodiazepine overdose.
Flumazenil
Aspiration does not necessarily result in aspiration pneumonia. The
seriousness of the lung damage depends on
the volume and composition of the aspirate.
Patients are at risk for aspiration pneumonia if 2X
their gastric volume is greater than 25 mL (0.4 mL/
kg) and their gastric pH is less than 2.5.
Histamine is found in 3X
the central nervous system, in the gastric mucosa, and in
other peripheral tissues.
Histaminergic neurons are primarily located in
the posterior hypothalamus but have wide
projections in the brain.
Histamine also normally plays a major role in the secretion of
hydrochloric acid by parietal cells in the stomach
The highest concentrations of histamine are found in
the storage granules of circulating basophils and
mast cells throughout the body.
Mast cells tend to be concentrated in
connective tissue
just beneath epithelial (mucosal) surfaces.
Histamine release (degranulation) from mast cells can be triggered by 3X
chemical, mechanical, or immunological stimulation
Secretion of hydrochloric acid is normally mediated by
gastrin-induced histamine release from
enterochromaffin-like cells in the stomach.
Two receptors, _____ ans _____ mediate the effects of histamine.
H1 and H2,
The H1-receptor
activates
phospholipase C,
H2-receptor activates
increases intracellular cyclic
adenosine monophosphate (cAMP).
An H3-receptor is primarily located on
histaminesecreting
cells and mediates negative feedback, inhibiting the synthesis and release of
additional histamine.
Cardiovascular
Histamine
reduces arterial blood pressure but increases heart rate and myocardial
contractility
Cardiovascular
H1-Receptor stimulation increases
capillary permeability and enhances
ventricular irritability,
Cardiovascular
H2-receptor stimulation
increases heart rate and increases contractility.
Respiratory
Histamine
constricts bronchiolar smooth muscle via the H1-receptor. H2-Receptor
stimulation may produce mild bronchodilation.
Respiratory
Histamine

H1-receptor
appears to mediate some pulmonary
vasodilation
Respiratory
Histamine

H2-receptor
histamine-mediated
pulmonary vasoconstriction.
Gastrointestinal

Activation of H2-receptors
parietal cells increases gastric acid secretion
Gastrointestinal
Stimulation of H1-receptors
leads to contraction of intestinal smooth muscle
histamine Dermal
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.
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.
diphenhydramine blocks
competitively blocks H1-receptors
Promethazine is a

blocking properties 2x
phenothiazine derivative with H1-
receptor antagonist activity as well as antidopaminergic and -adrenergic–blocking
properties.
Antacids neutralize the acidity of gastric fluid by
providing a base (usually
hydroxide, carbonate, bicarbonate, citrate, or trisilicate) that reacts with hydrogen ions to
form water.
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.
Metoclopramide produces an antiemetic effect by
blocking dopamine receptors in
the chemoreceptor trigger zone of the central nervous system
metoclopramide is
contraindicated in
patients with complete intestinal obstruction
(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.
Ondansetron (Zofran), granisetron (Kytril), and dolasetron (Anzemet) selectively
block serotonin
5-HT3 receptors, with little or no effect on dopamine receptors
Ketorolac is a parenterally administered nonsteroidal antiinflammatory drug (NSAID) that provides analgesia by
by inhibiting prostaglandin synthesis
ketorolac has a duration of action
duration of action (6–8 h).
ketorolac

heme wise
ketorolac inhibits platelet aggregation and prolongs bleeding time
ketorolac elimination
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.
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
clonidine

diabetic patients
Lastly, clonidine can mask the symptoms of hypoglycemia in diabetic patients
Mechanism of Action

Dexmedetomidine (Precedex)
Dexmedetomidine (Precedex) is a parenteral selective 2-agonist with sedative properties
Dexmedetomidine

principal side effects
bradycardia, heart block, and hypotension
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.
Mechanism of Action

Naloxone
competitive antagonist at opioid receptors.

Naloxone has no significant agonist activity.
Naloxone reverses
the agonist activity associated with endogenous (enkephalins, endorphins) or exogenous opioid compounds.
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.