Shared Flashcard Set

Details

Pharm 2
Nausea and Vomiting - exam 1
91
Pharmacology
Graduate
05/12/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Centrally acting agents - CTZ
Definition
prochlorperazine maleate (Compazine)
promethazine (Phenergan)
metoclopramide (Reglan)
Term
promethazine (dose)
Definition
centrally acting agent - CTZ
Phenergan

IV, IM, rectal suppository, tablets, liquid

12.5-25 mg PO q4h-q6h
Term
metoclopramide (dose)
Definition
centrally acting agent - CTZ
Reglan

IV*, IM, PO

5-10 mg PO/IM/IV q6h-q8h
Term
scopolamine (dose)
Definition
vertigo and motion sickness - anticholinergic agent

Transderm Scop

1.5 mg over 3 days in a patch applied behind the ear
Term
vertigo and motion sickness antihistamines
Definition
Block H1 receptors, OTC agents

dimenhydrinate (Dramamine)
diphenhydramine (Benadryl)
meclizine (Antivert)
Term
meclizine (dose)
Definition
Antihistamine for vertigo or motion sickness
Antivert

Rx: 25-50 mg PO qd
> 12 years
Term
What % of patients with inferior MI present with nausea and vomiting?
Definition
70%
Term
What % of patients with diabetic ketoacidosis present with nausea and vomiting?
Definition
70%
Term
What % of patients with Addisonian chrisis, acute pancreatitis, or acute appendicitis present with nausea and vomiting?
Definition
80-90%
Term
How is nausea and vomiting stimulated?
Definition
many different ways - but they all stimulate the medullary vomiting center (directly or indirectly)
Term
Describe the CTZ.
Definition
chemoreceptor trigger zone

area postrema - circumventricular organ
located in the brain stem
highly vascularized area of brain
lacks a true blood/brain barrier
activated by noxious stimuli - uremia, acidosis, toxins (ex. chemo)
secondarily activated by serotonin, dopamine, and neurokinin (has receptors)
Term
What neurotransmitters have receptors in the CTZ?
Definition
serotonin (5-HT3)
dopamine (D2)
neurokinin (NK1)
Term
How does reduced GI motility cause nausea and vomiting?
Definition
enterochromaffin cells of the GI tract can trigger the afferent Vagus nerve which leads to serotonin and dopamine stimulation of the vomiting center and/or CTZ
Term
How does vestibular input cause nausea and vomiting?
Definition
release of histamine and acetylcholine which stimulates the medullary vomiting center and/or CTZ

can be caused by conditions that affect the labyrinths (infection, Meniere's Disease, tumors), increase in intracranial pressure (migraine, tumor), or emotional or physical stressors (anorexia or bulimia)
Term
T/F
CNS etiologies for nausea and vomiting are unlikely without other neurologic symptoms.
Definition
True
Term
What 3 things does the vomiting center control? (associated with vomiting)
Definition
1. salivation
2. respiratory change
3. muscle contractions - pharyngeal, GI, and abdominal muscles
Term
What are the key receptors involved in the mechanism of vomiting?
Definition
serotonin (5-HT3)
dopamine
neurokinin (NK-1)

also: histamine, endorphins, acetylcholine, cannaboids, and GABA
Term
magnesium hydroxide
Definition
antacid - base, osmotic diarrhea
Term
aluminum hydroxide
Definition
base, constipation
Term
Why are Mg hydroxide and Al hydroxide often used together as antacid?
Definition
Mg causes osmotic diarrhea and Al causes constipation but both are basic and neutralize acid

Milk of magnesia contains both
Term
calcium carbonate
Definition
antacid - base, constipation

also practical source of calcium for treating osteoporosis
Term
What is the M of A of antacids?
Definition
reduce stomach acid, reduce intestinal irritation, and reduce visceral stimulation
Term
What are the side effects of prochlorperazine maleate (Compazine)?
Definition
sedation
BBW: dementia-related psychosis
QT prolongation (sudden death)
blood dyscrasias
Term
What is the Black Box Warning for prochlorperazine maleate (Compazine)?
Definition
dementia-related psychosis

risk in elderly patients on conventional or atypical antipsychotics due to infection or cardiovascular events
Term
In what modalities are prochlorperazine maleate (Compazine) and promethazine (Phenergen) available?
Definition
IV, IM, rectal suppositories, tablets, and liquid
Term
What is the M of A of prochlorperazine maleate (Compazine)?
Definition
selectively antagonizes dopamine (D2) receptors in the CTZ
Term
What is the M of A of promethazine (Phenergan)?
Definition
non-selective antihistamine

blocks central and peripheral H1 receptors
some effect on dopamine receptors in the CTZ
Term
What is the main side effect of promethazine (Phenergan)?
Definition
sedation
Term
What are the Black Box Warnings for promethazine (Phenergan)?
Definition
respiratory depression in those under 2 years
injection may cause tissue necrosis and gangrene
Term
What modalities is metoclopramide (Reglan) available?
Definition
IV/IM/PO

most often IV
Term
What is the M of A of metoclopramide (Reglan)?
Definition
blocks dopamine receptors in the CTZ

enhances release of acetylcholine to stimulate upper GI motility
Term
What are the side effects of metoclopramide (Reglan)?
Definition
bradycardia
BBW - extrapyramidal symptoms, dystonia
Term
What are the black box warnings for metoclopramide (Reglan)?
Definition
extrapyramidal symptoms and dystonia
Term
What is used to treat vertigo and motion sickness?
Definition
anticholinergic agents and antihistamines
Term
What is the M of A of scopolamine (Transderm Scop)?
Definition
antagonizes acetylcholine at muscarine receptors
Term
What are the side effects of scopolamine (Transderm Scop)?
Definition
sedation, urinary retention, dry mouth, withdrawal symptoms if used for more than 3 days
Term
What is a counter-indication for scopolamine (Transderm Scop)?
Definition
narrow-angle glaucoma
Term
What drugs can have drug-drug interactions with scopolamine (Transderm Scop)?
Definition
cannabinoids and alpha blockers
Term
What is the M of A of antihistamines?
Definition
block H-1 receptors
Term
How long before activity should you take dimenhydrinate (dramamine)?
Definition
0.5-1 hr
Term
What is the M of A of meclizine (Antivert)?
Definition
antagonizes acetylcholine receptors and blocks H-1 (histamine) receptors
Term
What are the side effects of meclizine (Antivert)?
Definition
sedation, dry mouth, and urinary retention
Term
What antiemetic is used during pregnancy?
Definition
preferably none - don't use until patients present with dehydration, weight loss, or electrolyte abnormalities

pyridoxine (B6) - category A
ginger is also used

antihistamines - doxylamine and promethazine (category C)
Term
what is hyperemesis gravidarum? What is the treatment?
Definition
extreme, persistent nausea and vomiting
during pregnancy that may lead to dehydration

rule out hyperthyroidism, H. pylori

tx: replace fluids and electorlytes
antiemetic therapy
Term
What pregnancy category is pyridoxine?
Definition
A
Term
What drugs are used to combat nausea and vomiting associated with chemotherapy?
Definition
5-HT3 receptor antagonists

(serotonin receptor antagonists)
Term
5-HT3 receptor antagonists for chemotherapy nausea and vomiting
Definition
dolasetron (Anzemet)
granisetron (Kytril)
ondansetron (Zofran)
palonosetron (Aloxi)
Term
When are 5-HT3 receptor antagonists given to fight nausea and vomiting from chemo?
Definition
30 min - 1 hour before treatment
Term
List the 5-HT3 receptor antagonist medications from shortest half life to longest half life.
Definition
dolasetron = 10 min
ondansetron = 5.7 hours
granisetron = 6.2 hours
palonosetron = 40 hours
Term
T/F
Palonosetron (Aloxi) was found to be as effective as ondansetron (Zofran).
Definition
True
Term
T/F
A single dose of palonosetron (Aloxi) is as effective as 3 dose regimen of granisetron (Kytril) when used with dexamethasone for cisplatin therapy.
Definition
True
Term
How do serotonin agents help with nausea and vomiting?
Definition
block serotonin receptors in small bowel, vagus nerve, and CTZ
Term
What drugs did serotonin agents replace in treating chemo nausea and vomiting and why?
Definition
replaced antipsychotics to reduce danger of extrapyramidal symptoms in chemo pts

often used with single dose of corticosteroid before first dose of chemo
Term
What is the gold standard for antiemetic therapy during chemo?
Definition
5-HT3 receptor antagonists
Term
T/F
The 5-HT3 receptor antagonists are equally efficacious.
Definition
True
Term
T/F
Palonosetron (Aloxi) has 100x the binding of 5-HT3 as the other 5-HT3 receptor antagonists.
Definition
True
Term
What are the side effects of 5-HT3 receptor antagonists?
Definition
HA - 10-15%
Constipation - 10-15%

rarely: anxiety, dizziness, diarrhea, fatigue
Term
T/F
Poor metabolizers of CYP2D6 have a low incidence of CINV. Ultrafast metabolizers have a high incidence.
Definition
True
Term
Which drugs does ondanestron (Zofran) interact with?
Definition
paroxetine (Paxil) and tramadol (Ultram)
Term
T/F
Granisetron (Kytril) with aprepitant (Emend) does not exhibit any drug-drug interactions.
Definition
True
Term
aprepitant
Definition
substance P antagonist
antiemetic
Term
Which of the 5-HT3 receptor antagonists causes QT prolongation?
Definition
dolasetron (Anzemet) and ondansetron (Zofran) - higher doses
Term
What is the DOC for the National Comprehensive Cancer Network for triple therapy in high risk patients?
Definition
palonosetron (Aloxi) - more effective than dolesetron or odansetron
Term
Why is granisetron (Kytril) a good choice for use against CINV?
Definition
can be given IV or PO
length of effect
side effect profile
Term
aprepitant (Emend)
Definition
neurokinin-1 receptor antagonist

enhances the effect of 5-HT3 receptor antagonists

selectively antagonizes substance P at NK-1 receptors

given on days 1, 2, and 3
fosaprepitant is the IV/injectable form
Term
T/F
5-HT3 receptor antagonists are more effective when administered with a corticosteroid.
Definition
True

methylprednisone (Medrol)
dexamethasone (most often used)
Term
What is the triple therapy used for severe nausea caused by chemotherapy?
Definition
1. Any 5-HT3 receptor antagonist
(usually palonosetron (Aloxi))
2. dexamethasone
3. aprepitant (Emend)
Term
What is delayed emesis from chemo?
Definition
emesis at least 24 hours after therapy that may last up to 5 days
Term
T/F
The subcommittee on acute gastroenteritis recommends not to use antiemetics in pediatrics.
Definition
False - no recommendation

they recommend not using antidiarrheal agents
Term
What are some potential side effects of anti-emetics in pediatrics?
Definition
extrapyramidal symptoms - akinesia, akathisia
seizure
Term
What is the most important part of treating emesis in pediatrics?
Definition
rehydration measures
Term
Which drug is used to treat emesis in dehydrated children and is considered safe?
Definition
ondansetron (Zofran)
Term
What is the DC for nausea and vomiting in pediatrics?
Definition
promethazine (Phenergan)

PR/IM/IV
usually given per rectum
Term
What is the black box warning for promethazine (Phenergan) for pediatrics?
Definition
respiratory depression < 2 years
injection site reactions (if IM)
Term
Name 2 drugs used to treat nausea and vomiting in pediatric patients.
Definition
promethazine (Phenergan) - DOC
trimethobenzamide (Tigan)
Term
If untreated, what proportion of patients who undergo surgery will have PONV within 24 hours?
Definition
1/3
Term
T/F
PONV is the leading cause of hospital admission after a planned ambulatory surgery.
Definition
True
Term
What are the possible risks of PONV?
Definition
aspiration, suture dehiscence, esophageal rupture, and bilateral pneumothoraxes
Term
Risk for PONV depend on what 3 things?
Definition
patient
anesthetic
surgical procedure
Term
What are the patient risk factors for PONV?
Definition
female
nonsmoker
Hx of motion sickness, emesis during pregnancy, or PONV
Term
What are the anesthetic risk factors for PONV?
Definition
Use of volatile anesthetics
use of nitrous oxide
use of opiods - perioperatively
Term
What are the surgical procedure risk factors for PONV?
Definition
duration of surgery
type of procedure - abdominal, gynecologic, ENT
Term
What are the most important risk factors for PONV?
Definition
female
nonsmoker
hx of motion sickness, emesis during pregnancy or PONV
use of opiods perioperatively
Term
What is the Apfel score?
Definition
a score to predict the probabitlity of POBV

assigns 1 point each to risk factors:
female
nonsmoker
history of PONV or motion sickness
postoperative opiod tx is planned

Score
0 - 10%
1 - 21%
2 - 39%
3 - 61%
4 - 78%
Term
What are the rescue agents used for PONV?
Definition
ondansetron (Zofran) - DOC in PACU
promethazine (Phenergan) - 2nd or 3rd line
dexamethasone
Term
T/F
Inhaled isopropyl alcohol is used to treat PONV and is equally as efficacious as ondansetron.
Definition
True
Term
In the low risk patient, how is PONV treated?
Definition
No prophylaxis
5-HT3 receptor antagonists used as rescue meds
Term
In the moderate risk patient, how is PONV treated?
Definition
droperidol (Inapsine) prophylaxis

5-HT3 receptor antagonists for breakthrough nausea
Term
In the high risk patient, how is PONV treated?
Definition
droperidol (Inapsine) prophylaxis
dexamethasone prophylaxis

5-HT3 receptor antagonists for breakthrough nausea
Term
droperidol (Inapsine)
Definition
anesthetic

may block dopamine receptors in the caudate nucleus and nucleus accumbens

lasts 2-4 hours, but alteration of alertness may last 12 hours

Binding of GABA receptors in CTZ - antiemetic effect
Term
PONV prophylactic drugs
Definition
dolasetron (Anzemet)
granisetron (Kytril)
ondansetron (Zofran)
palonosetron (Aloxi)
Supporting users have an ad free experience!