GIT Flashcards by Kim Grace

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

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SEROTONIN 5-HT3 ANTAGONISTs

Ondansetron, Granisetron, Dolasetron, Palonosteron

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Potent antiemetic properties that are mediated in part
through central 5-HT3 receptor

SEROTONIN 5-HT3 ANTAGONIST (Ondansetron, Granisetron, Dolasetron, Palonosteron)

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T/F:SEROTONIN 5-HT3 ANTAGONIST (Ondansetron, Granisetron, Dolasetron, Palonosteron) may be used in cancer chemotherapy

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SEROTONIN 5-HT3 ANTAGONIST that has a serum t1/2 of 4 to 9 hrs and is administered orally or IV

Ondansetron, Granisetron, Dolasetron

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SEROTONIN 5-HT3 ANTAGONIST that has greater affinity to the 5-HT3 receptor

Palonosteron

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T/F: All SEROTONIN 5-HT3 ANTAGONIST
undergoes hepatic metabolism and are eliminated by
renal and hepatic excretion

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SEROTONIN 5-HT3 ANTAGONIST does not inhibit ___________

dopamine or muscarinic receptor

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blocks the 5-HT3 receptor found on the vomiting center
and on your chemoreceptor trigger zone

SEROTONIN 5-HT3 ANTAGONIST

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HISTAMINE ANTAGONISTs

Diphenhydramine, Dimenhydrinate
Meclizine

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Weak antiemetic, particularly useful for prevention or
treatment of motion sickness

HISTAMINE ANTAGONIST

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1st generation H1 antagonist

Diphenhydramine, Dimenhydrinate

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H1 antagonist that has significant anticholinergic properties

Diphenhydramine, Dimenhydrinate

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H1 antagonist that may cause Sedation as its side effect

Diphenhydramine, Dimenhydrinate

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H1 antihistamine agent with minimal anticholinergic
properties that also causes less sedation

Meclizine

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H1 antihistamine agent that is used to prevent motion sickness and the treatment of
vertigo due to labyrinth dysfunction

Meclizine

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CORTICOSTEROIDs

Dexamethasone and Methylprednisolone

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Enhance the efficacy of 5-HT3 receptor antagonist for
prevention of acute and delayed nausea and vomiting

CORTICOSTEROID

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patient experiences N&V within 24 hrs after
taking chemotherapeutic agents

Acute nausea and vomiting

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patient experiences
N&V after 24 hrs

Delayed nausea and vomiting

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Corticosteroid is usually used in an ______ form

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Corticosteroid is useful in __________ regimen

cancer chemotherapeutic

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NEUROKININ RECEPTOR ANTAGONISTs

Aprepitant Fosaprepitant

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NK1 receptor antagonist have __________ properties that
are mediated through central blockade in the area
_____________

antiemetic; postrema

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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

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/F: CANNABINOIDS are More effective than marijuana

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)