GIT Flashcards
T/F: Nausea and vomiting may be manifestation of a wide
variety of condition including adverse effects from
medication; systemic disorder or infections; pregnancy;
vestibular dysfunction; CNS infection or increased
pressure
T
SEROTONIN 5-HT3 ANTAGONISTs
Ondansetron, Granisetron, Dolasetron, Palonosteron
Potent antiemetic properties that are mediated in part
through central 5-HT3 receptor
SEROTONIN 5-HT3 ANTAGONIST (Ondansetron, Granisetron, Dolasetron, Palonosteron)
T/F:SEROTONIN 5-HT3 ANTAGONIST (Ondansetron, Granisetron, Dolasetron, Palonosteron) may be used in cancer chemotherapy
T
SEROTONIN 5-HT3 ANTAGONIST that has a serum t1/2 of 4 to 9 hrs and is administered orally or IV
Ondansetron, Granisetron, Dolasetron
SEROTONIN 5-HT3 ANTAGONIST that has greater affinity to the 5-HT3 receptor
Palonosteron
T/F: All SEROTONIN 5-HT3 ANTAGONIST
undergoes hepatic metabolism and are eliminated by
renal and hepatic excretion
T
SEROTONIN 5-HT3 ANTAGONIST does not inhibit ___________
dopamine or muscarinic receptor
blocks the 5-HT3 receptor found on the vomiting center
and on your chemoreceptor trigger zone
SEROTONIN 5-HT3 ANTAGONIST
HISTAMINE ANTAGONISTs
Diphenhydramine, Dimenhydrinate
Meclizine
Weak antiemetic, particularly useful for prevention or
treatment of motion sickness
HISTAMINE ANTAGONIST
1st generation H1 antagonist
Diphenhydramine, Dimenhydrinate
H1 antagonist that has significant anticholinergic properties
Diphenhydramine, Dimenhydrinate
H1 antagonist that may cause Sedation as its side effect
Diphenhydramine, Dimenhydrinate
H1 antihistamine agent with minimal anticholinergic
properties that also causes less sedation
Meclizine
H1 antihistamine agent that is used to prevent motion sickness and the treatment of
vertigo due to labyrinth dysfunction
Meclizine
CORTICOSTEROIDs
Dexamethasone and Methylprednisolone
Enhance the efficacy of 5-HT3 receptor antagonist for
prevention of acute and delayed nausea and vomiting
CORTICOSTEROID
patient experiences N&V within 24 hrs after
taking chemotherapeutic agents
Acute nausea and vomiting
patient experiences
N&V after 24 hrs
Delayed nausea and vomiting
Corticosteroid is usually used in an ______ form
IV
Corticosteroid is useful in __________ regimen
cancer chemotherapeutic
NEUROKININ RECEPTOR ANTAGONISTs
Aprepitant Fosaprepitant
NK1 receptor antagonist have __________ properties that
are mediated through central blockade in the area
_____________
antiemetic; postrema
NK1 may also be given to patients that experiences
Cancer Induces
Nausea and Vomiting (CINV)
Highly selective NK1 receptor antagonist that crosses the
blood-brain barrier and occupies brain NK1 receptor found
in CTZ
Aprepitant
NK1 receptor that has no affinity for serotonin and dopamine or
corticosteroid receptor
Aprepitant
NK1 receptor that is associated with fatigue, dizziness and diarrhea
Aprepitant
Apprepritant is metabolized by ________ and may inhibit the metabolism of
other drugs metabolized by ________
CYP3A4; CYP3A4
Aprepitant is available in
Oral form
Intravenous NK1 formulation that converted within 30 minutes
after infusion to aprepitant (active form)
Fosaprepitant
MUSCARINIC ANTAGONISTs
Hyoscine / Scopolamine
Prototypic muscarinic receptor antagonist
Hyoscine / Scopolamine
Often used in preoperative analgesia, seasickness, motion
sickness, ocular irritation and irritable bowel syndrome
Hyoscine / Scopolamine
Hyoscine / Scopolamine is used as an
antiemetic
Hyoscine / Scopolamine may produce very high incidence of anticholinergic effects when given _____ or ___________
orally or parenterally
DOPAMINE 2 BLOCKERs
Phenothiazine
Droperidol
Antipsychotic agents that can be used for their potent
antiemetic and sedative properties
Phenothiazine
Phenothiazine inhibits _______ and _________receptor
dopamine and muscarinic receptor
Phenothiazine’s sedative properties are due to their
antihistamine activity
Phenothiazine drugs
Prochlorperazine, Promethazine, and Thiethylperazine
Antipsychotic butyrophenone also possess antiemetic
properties due to their central dopaminergic blockade
Droperidol
Droperidol is given as
IM or IV
SUBSTITUTED BENZAMIDE
Metoclopramide and Trimethobenzamide
Primary mechanism of SUBSTITUTED BENZAMIDE’ antiemetic action is believed to be
______________
dopamine receptor blockade
SUBSTITUTED BENZAMIDE that has weak antihistaminic activity, for
prevention and treatment of nausea and vomiting
Trimethobenzamide
Principal adverse effect of these central dopamine
antagonist are extrapyramidal
SUBSTITUTED BENZAMIDE
extrapyramidal ADE of SUBSTITUTED BENZAMIDE
restlessness, dystonia and
parkinsonian symptoms
BENZODIAZEPINEs
Lorazepam and Diazepam
Used before the initiation of chemotherapy to reduce
anticipatory vomiting or vomiting caused by anxiety
BENZODIAZEPINE
when patient previously had
chemo and experienced N&V
Anticipatory vomiting:
CANNABINOIDS
Dronabinol, Nabilone
T/F: Cannabinoids as oral medications, is fairly effective
T
Almost completely absorbed but undergoes significant
first-pass hepatic metabolism
CANNABINOIDS
Associated with an increase appetite
CANNABINOIDS
T/F: CANNABINOIDS is also used in in cancer chemotherapeutic regimen
T
T/F: CANNABINOIDS are More effective than marijuana
T
IBD comprise 2 distinct disorder: ___________ and ___________
ulcerative colitis and
Crohn’s disease
AMINOSALICYLATES 5-ASA
Sulfazalazine, Olsalazine, Balsalazide and various forms
of Mesalamine
AMINOSALICYLATES 5-ASA differs from salicylic acid only by the addition of an _____________ at the 5 (meta) position
amino
group
AMINOSALICYLATES 5-ASA work topically in areas of ____________
diseased gastrointestinal
mucosa
Aqueous 5-ASA is absorbed from the ______________ and
(reaches/does not reach) the distal small bowel or colon in
appreciable quantities
small intestine; does not reach
_____________is readily/rapidly absorbed from the
small intestine, absorption of 5-ASA from the colon is
_____________
Unformulated 5-ASA; extremely low
Absorbed 5-ASA undergoes _____________ in the gut
epithelium and liver to a metabolite that does not possess
significant anti-inflammatory activity
N-acetylation
GLUCOCORTICOIDs
Budesonide
inhibit production of inflammatory
cytokines and chemokines to reduce the expression of
inflammatory cell adhesion molecules and inhibit gene
transcription of nitric oxide synthase, phospholipase A2,
Cyclooxygenase-2 and NF- KB
Glucocorticoids
Glucocorticoids inhibit production of inflammatory
_________________ to reduce the expression of
inflammatory cell adhesion molecules and inhibit gene
transcription of __________, __________, __________ and __________
cytokines and chemokines; nitric oxide synthase, phospholipase A2,
Cyclooxygenase-2 and NF- KB
Potent synthetic analog of prednisolone
Budesonide
High affinity for glucocorticoid receptor but is subject to
rapid first-pass hepatic metabolism
Budesonide
Widely used in transplantation medicine and autoimmune
disease
AZATHIOPRINE, 6-MERCAPTOPURINE
Prodrug for mercaptopurine
AZATHIOPRINE
Moderately to severe Crohn’s disease or chronically active
Crohn’s disease
AZATHIOPRINE, 6-MERCAPTOPURINE
Associated with low risk of lymphoma causality uncertain
AZATHIOPRINE
Also used in children at lower doses
AZATHIOPRINE
Other uses include rheumatoid arthritis and systemic
lupus erythematosus
AZATHIOPRINE
Interferes with nucleic acid synthesis, affecting B and T
cell function
6-MERCAPTOPURINE
Antimetabolite and antifolate drug
METHOTREXATE
Interferes with nucleic acid synthesis, and the folic acid
pathway
METHOTREXATE
Inhibits dihydrofolate reductase
METHOTREXATE
Underused in Crohn’s disease, but is essential for
management of IBD.
METHOTREXATE
TUMOR NECROSIS FACTOR ANTAGONISTs
Infliximab, Adalimumab, Golimumab, and Certolizumab
TUMOR NECROSIS FACTOR ANTAGONIST binds _______ and _______ TNF with high affinity,
preventing the cytokine from binding to its receptor
soluble; membrane-bound
Causes reverse signaling that suppresses cytokine release
TUMOR NECROSIS FACTOR ANTAGONIST
is a family of adhesion molecule on the surface of
leukocytes that may interact with another class of
adhesion molecules on the surface of the vascular
endothelium known as selectins allowing circulating
leukocytes to adhere to the vascular endothelium and
subsequently move through the vessel wall into the tissue.
Integrin
Integrin is a family of __________ molecule on the surface of
leukocytes that may interact with another class of
adhesion molecules on the surface of the vascular
endothelium known as ___________ allowing circulating
leukocytes to adhere to the vascular endothelium and
subsequently move through the vessel wall into the tissue
adhesion; selectins
ANTI-INTEGRIN THERAPY Drugs
Natalizumab
Blocks integrins on circulating leukocytes
Natalizumab
May be associated with multifocal leukoencephalopathy
Natalizumab
Restricted to patients with severe Crohn’s disease
Natalizumab
PANCREATIC REPLACEMENT THERAPY Drug
Natalizumab
Not producing sufficient amount of pancreatic enzyme
Exocrine pancreatic insufficiency
When secretion of pancreatic enzyme falls below 10% of
normal, fat and protein digestion is impaired and can lead
to __________
steatorrhea, azotorrrhea, vitamin malabsorption and
weight loss
These product (from pigs) substitute for pancreatic lipase
Natalizumab
Natalizumab is inactivated at pH levels below _______
4.0
Natalizumab is taken as
enteric coated capsule
GALLSTONE PREVENTION Drugs
Ursodiol (Ursodeoxycholic acid)
Cholesterol stones are caused by the ___________ of
cholesterol out of solution in the bile
precipitation
Ursodiol decrease cholesterol content of bile by
○ Decreasing cholesterol uptake by the intestine
○ Breaking up micelles containing cholesterol
● Decreasing hepatic cholesterol secretion
Also used to relieve itching in pregnancy caused by
obstetric cholestasis
Ursodiol (Ursodeoxycholic acid)
DRUGS USED TO TREAT VARICEAL HEMORRHAGE
Somatostatin and Octreotide
Vasopressin, Terlipressin
Portal hypertension most commonly occur as a
consequence of chronic liver disease
VARICEAL HEMORRHAGE
Agents that cause constriction so that the bleeding in the
variceal blood vessels would be inhibited.
Somatostatin and Octreotide
Antidiuretic hormone secreted by the hypothalamus
Vasopressin
Potent arterial vasoconstrictor
Vasopressin
Vasopressin analog
Terlipressin
Drugs that can be used in Cancer Chemotherapy
SEROTONIN 5-HT3 ANTAGONIST (Ondansetron, Granisetron, Dolasetron, Palonosteron)
CORTICOSTEROID (Dexamethasone and Methylprednisolone)
NEUROKININ RECEPTOR ANTAGONIST (Aprepitant, Fosaprepitant)
CANNABINOIDS (Dronabinol, Nabilone)