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Exam #4 - Antiemetics & Antitussives
n/a
23
Pharmacology
Graduate
11/14/2009

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Term
Anticholinergics
Definition
produce antiemetic effects by blocking transmission of afferent information from vestibular system; effective in treating or preventing motion sickness & vertigo, they have little effect in treatment of other types of nausea
Term
Dopamine Antagonists
Definition
drugs that produce main effects on CRZT; effective in treating N/V resulting from stimulation of CRTZ (post-op, chemo, radiation sickness); little to no effect on treating motion sickness & vertigo
Term
Antihistamines
Definition
drugs have pronounced anticholinergic activity --> most effective in treating N/V from motion sickness & vertigo; some may also affect CRTZ & vomiting center but are less effective than dopamine antagonists
Term
scopolamine [Transderm Scop]
Definition
anticholinergic drug that acts primarily on vestibular system; used in treating & preventing vertigo & motion sickness; SEs: dry mouth, constipation, urine retention, loss of visual accomodation, sedation, confusion, amnesia
Term
Antihistamines (dimenhydrinate [Dramamine], meclizine [Bonine, Antivert], promethazine [Phenergan], diphenhydramine [Benadryl])
Definition
drugs that have primary effect on vestiular system but some may also have weak effects on CRTZ; used in treating & preventing motion sickness & vertigo; some may also have more general antiemetic activity though not the most effective in treating N/V caused by activation of CRTZ; SEs: dry mouth, constipation, urine retention, loss of visual accomodation, SEDATION
Term
prochlorperazine [Compazine], metoclopramide [Reglan]
Definition
dopamine (D2) antagonist with primary action on CRTZ; used as antiemetic for post-op nausea, cytotoxic drugs, radiation sickness, & toxins; SEs: parkinsonism, postural hypotension, anticholinergic effects, sedation, lethargy, psychomotor slowing; possible teratogenic effects but no strong evidence
Term
metoclopramide [Reglan]
Definition
dopamine antagonist in CRTZ but also acts on enteric nerves to increase GI tone & motility & increases tone in lower esophageal sphincter; used in treating N/V during cancer chemotherapy; also useful in post-op N/V, toxin-induced V, & V associated with radiation; also used to treat a variety of GI problems including gastric stasis & GERD; commonly used as pre-op med to prevent possible aspiration of vomitus; SEs: sedation, extrapyramidal motor problems (parkinsonism, acute dystonia)
Term
ondansetron [Zofran], granisetron [Kytril]
Definition
5-HT3 (serotonin) antagonists used in preventing N/V during cancer chemotherapy & post-op N/V; very effective in 80% of pts; depresses CRTZ & inhibits serotonin-mediated afferent input from GI tract; given IV or ORALLY; Main ADRs: headache, constipation
Term
dronabinol [MARINOL]
Definition
cannabinoid; main active constituent of marijuana; used in controlling N/V during cancer chemo in pts who don't respond to other drugs; SEs: CNS - sedation, confusion, disorientation, loss of control, altered sensation, paranoia, psychotic reactions - not tolerated well by elderly pts; smoking may be more effective than ORAL PILL use
Term
Bendectine
Definition
doxylamine + pyridoxine
Term
amphetamine
Definition
used in military to prevent motion sickness; can counteract sedative effects; not used routinely because of CNS effects & abuse potential
Term
ginger
Definition
OTC herbal product that has anti-emetic activities
Term
Uses of Antiemetic Drugs
Definition
treatment of prevention of motion sickness & vertigo, post-op N/V, radiation sickness, drug-induced vomiting; avoid in pregnancy if possible
Term
Rationale for Antitussive Therapy
Definition
1) remove cause of irritation; 2) increase airway secretions to mobilize irritants; 3) desensitize peripheral receptors; 4) act on CNS component
Term
opioids (codeine, hydrocodone)
Definition
most effective antitussive; used in moderate to severe cough; doses are lower than analgesic doses; SEs: sedation, light-headedness, confusion, nausea, dizziness, & constipation; can be abused & potential for physical dependence
Term
dextromethorphan [Benylin DM, Pertussin, Vicks Formula 44]
Definition
chemically similar to opioids but does not have their effects; used for mild-moderate cough; antitussive effect results from blockage of NMDA receptors in cough control centers; SEs: mild - sedation, dizziness, confusion; much lower abuse potential but high doses are being abused by young people
Term
benzonatate (Tessalon)
Definition
antitussive with local anesthetic activity that claims to desensitize receptors in airway; may also have some effect on cough control center; available in capsule ORAL form; SEs: mild - constipation, nasal congestion, nausea, drowsiness, skin rashes
Term
menthol
Definition
agent that acts on receptors in airway; found in many preparations like cough drops, syrups, etc
Term
guaifenesin [Mucinex]
Definition
most widely used expectorant; efficacy has been questioned; acts as mild irritant in GI tract & activate reflexes leading to increased mucus production in airway
Term
acetylcysteine [Mucomyst]
Definition
mucolytic agent that breaks mucus plugs & makes them easier to mobilize; acts to disrupt disulfide linkages, decreasing viscosity of mucus; administered via NEBULIZER; used in conditions where mucus plugs may be a problem (following surgery, tracheotomy care, severe bronchitis, emphysema); also used as antidote in APAP poisoning
Term
antihistamines (diphenhydramine, promethazine)
Definition
alleviate coughing by antagonizing effects of histamine, decreasing irritation or constriction of airway; cause sedation & have weak effect on cough control center; found in a wide variety of antitussives & cold remedies
Term
bronchodilators (beta-2 agonists)
Definition
decreases airway resistance; particularly useful in asthma where bronchoconstriction is key problem
Term
demulcents
Definition
"syrupy" materials that exert coating & soothing action - often included in cough preparations
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