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GI Pharmacology > ? > Flashcards

? Flashcards

1
Q

Name prokinetic agents

A

Cholinergics: Neostigmine

Dopamine receptor antagonists: Domperidone

Serotonin receptor agonist: Metoclopramide
Macrolides: Erythromycin

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2
Q

Neostigmine

Mechanism
Use
Why is it not used so often anymore

A

reversible inhibition of acetylcholinesterase

perioperatively for acute colonic pseudo-obstruction or paralytic ileus

too diffuse a manner to be generally useful

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3
Q

Domperidone

Mechanism
FDA approved
Side effects

A

Mechanism

  • Dopamine improves gastric motility (D2 receptor) and reduces lower esophageal and intragastric pressure by reducing acetylcholine release
  • Domperidone inhibits the effects of dopamine in the myenteric plexus, but does not penetrate the BBB/CNS

FDA approved
- No?

Side effects
- Phenothiazines, are effective, but produce extrapyramidal side effects

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4
Q

Metoclopramide

Mechanism
Use
BBW

A

Mechanism

  1. 5-HT4 receptor agonist
  2. D2 receptor antagonism

Use

  • 5-HT4: improves motility
  • increased resting esophageal sphincter tone
  • improved gastric tone and peristalsis
  • relaxes pyloric sphincter
  • augmented duodenal peristalsis
  • no effect on gastric, pancreatic, or biliary secretion and only minimal contractual effect on the large intestine

SE
- extrapyramidal effects

BBW
- tardive dyskinesia ( in eldery esp. women

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5
Q

Erythromycin

Mechanism
Use
Which receptor
SE
Newest agent
A

Mechanism
Motilin agonist

Use
- Gastroparesis

Which receptor

  • GPCR
  • GI tract, expressed in smooth muscle cells from the antrum, duodenum and colon, and neurons of the myenteric plexus

SE
- utility of macrolide antibiotics is limited by tolerance and antibiotic effects (Bacterial resistance)

Newest agent
- Camicinal

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6
Q

Name antiematic agents

A

Dopamine receptor antagonists: Metoclopramide, Phenothiazine
Serotonin receptor antagonist: Ondansetron
Cannabinoids: Dronabinol
Histamine antagonists: Diphenhydramine

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7
Q

Metoclopramide, Phenothiazine

Class
Mechanism
Use
High dose use?
SE
A

Class
5-HT3 receptor antagonist

Mechanism
metoclopramide enhances gastric emptying, thus minimizing stasis which precedes vomiting

Use
acute or emergency situations, but have too many extrapyramidal side effects to warrant chronic use.

High dose
chemotherapy-induced nausea due to its prokinetic effects

SE
but high doses can result in extrapyramidal effects

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8
Q

Ondansetron

A

Class
5HT3R antagonist

Mechanism

  • Peripheral & central action
  • vagal afferents in the gut and in the area postrema

Use
- Chemotherap & radiation nausea
- Not eeffective in
Motion sickness

Efficacy
- Same as metocpromide but no CNS side effects

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9
Q

Dronabinol
Class
Use
SE

A

Class
cannabinoid

Use
chemotherapy-related nausea
Appetite stimulation

SE
high potential for abuse and adverse effects related to complex CNS actions

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10
Q

Diphenhydramine
Class
Use

A

Class
Antihistamine H1 antagonists

Use
motion sickness

Scoplomine
Vestibular disorders
Motion sikness

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11
Q

Name antacids

A

Mg, Al hydroxides

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12
Q

Mg, Al hydroxides

Mechanism
SE
Which is more effective (liquid or tablets)

A

Mechanism
Neutralize secreted acid; do not alter acid secretion

SE
Magnesium hydroxide has laxative properties (Mg = must go)

Aluminum hydroxide can cause constipation

Liquids more effective

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13
Q

Cimetidine

Class
SE

A

Class
H2-receptor antagonists

CYP450 inhibition

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14
Q

Omeprazole

Class
Mechanism
Use
SE
- Short term & long term
A

Class
Proton pump inhibitors

Mechanism

  • Prodrug
  • Covalent drugs
  • Irreversible binding to proton pump
Use
GERD (gastroesophageal reflux disease)
Peptide ulcer disease
Erosive esophagitis
H. pylori eradication (“triple therapy” in combination with 2 antibiotics
SE
Short Term
mild and self-limiting
- Pnnumonia
- headache
- Nausea
- Abdominal pain
- Flatulence and diarrhea
Long Term
C. difficile infections
Risk of fractures
Acute interstitia nephritis
Hypomagnesemia,
Thrombocytopenia
Fe deficiency
Vitamin B12 deficiency
Rhabdomyolysis
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15
Q

Diarrhea treatment

A

Metamucil

Loperamide

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16
Q

Metamucil

Mechani

A

Bulk forming agents (Metamucil (psyllium seed husks), etc.), whose mechanism of action is unknown

17
Q

Loperamide

A

Opioids can act as antidiarrheal agents. Loperamide (Imodium and Imodium-AD) is 40-50 times more potent than morphine, as an antidiarrheal agent, and has a limited ability to enter the CNS. It is orally active, and very safe

18
Q

IBS Treatment

A

Serotonin receptor modulators: Alosetron; Tegaserod

19
Q

Alosetron

Class
Use
Mechanism

A

.Class
- 5-HT3 receptor antagonist

Use

  • women severe diarrhea-predominant IBS (IBS-D)
  • severe IBS-D who have failed to respond to conventional treatment for IBS

Mechanism
- Reduces motility and intestinal sensitivity to distension

SE
- , life-threatening, gastrointestinal side effects (ischemic colitis).

20
Q

Tegaserod

Class
Use
Mechanism

A

.Class
5-HT4 agonist

Use
IBS-C, or chronic constipation

Mechanism
Relieves pain, bloating and constipation.
Can induce mild to severe diarrhea, which is dose-dependent.
There may also be increased risk of ischemic colitis

SE
heart attack, stroke, and unstable angina (compared to placebo)

21
Q

IBD Treatment (4 agents)

A

5-Aminosalycilates: Sulfasalazine/Mesalamine
Glucocorticoids: Prednisone; Budesonide
Immunosuppressive agents: Azathioprine/6-mercaptopurine and Methotrexate
Biologicals: Infliximab

22
Q

Sulfasalazine/Mesalamine

A

Use
- UC

Mechanism

  • Pro drug ceave dby gut bacteria to Mesalamine (5-aminosalicylic acid, or 5-ASA)
  • Give prodrug so that it can make it to large bowel else only effective in the small bowel
  • Anti-inflamatory

SE
- Sulfa/salicalte agents

23
Q

Prednisone; Budesonide

Use
Budesonide:
Kinetics
SE

A

Use
- Acute treatment is used to manage active disease and flareups

Budesonide
Kinetic: High first past in the liver
SE: Fewer

24
Q

Azathioprine/6-mercaptopurine

Use
Which is pro durg
Limitations
SE

A

Use

  • Immunosuppressive agents to treat moderate to severe IBD
  • Maintain remission

Produrg- azithroprine

Limitations
take several weeks to produce effects in ulcerative colitis and Crohn’s disease. However, they reduce the requirement for steroids to maintain patients in remission

SE
bone marrow depression, leukopenia, teratogenesis

25
Q

Methotrexate

A

USE

  • Crohns
  • IBD that is steroid-resistant or steroid-dependent

MECHANISM
through inhibition of dihydrofolate reductase
Anti-inflammatory mechanism is not fully understood

26
Q

Infliximab

Mechanism

A

Class/Mechanism
mAbs targeting TNF-α (infliximab, adalimumab, and certolizumab) induce the formation of regulatory macrophages with immunosuppressive properties

27
Q

Inverse agonist

A

A ligand that stabilizes the inactive conformation of a receptor or ion channel

28
Q

Functional antagonist

A

A substance that prevents a receptor response by a another mode of action

29
Q

Ghrelin agonist which is prokinetic

A

relamorelin (RM-131).

30
Q

Where is the emetic center

A

Medulla

31
Q

Which agent used most commonly for chemotherapy nausea

A

Dexamtheasone

32
Q

Natural antiematic
Use
Active agent

A

Ginger

Use
nausea from motion sickness, morning sickness, and after surgery

Active agent
shogaols and gingerols, thought to stimulate the flow of saliva, bile and gastric secretions through 5HT-3 receptors

33
Q

Before trying medications constipation should be treated with

A

Fiber rich diarrhea
Physical exam
Bowel routine

34
Q

Newer IBS C drug (just read the card)

A

Lubiprostone (Amitiza) for IBS-C

FDA approved in 2006; approved indications:
IBS-C (adult women)
Chronic idiopathic constipation (CIC in adults)
Opioid-induced constipation (OIC in adults w/chronic non-cancer pain)
Mechanism:
Original model: Activates ClC-2 chloride channel in epithelial cells lining the intestinal tract. [Cl-] in the intestinal lumen increases; as chloride moves into the intestinal lumen, Na+ ions and fluids passively follow
Not entirely accepted; alternative MOA involves CFTR-dependent Cl- and fluid secretion

35
Q

Newer treatment for IBS-C & CIC (just read the card)

A

Mechanism:
Guanylate cyclase-C (GC-C) agonist (First in class)
Increases [cGMP]; increases [Cl-] in intestinal lumen; as chloride moves into the intestinal lumen, increase in intestinal fluid and faster transit

PK & metabolism:
Minimally absorbed with low systemic availability following oral admin.
Metabolized within the GI tract to its principal, active metabolite by loss of the terminal Tyr. Linaclotide and metabolite are proteolysed within intestinal lumen to smaller peptides and naturally occurring amino acids

36
Q

An alternative way to use Ab to reduce inflammation

A

Target integrins

Natalizumab, a humanized mAb specific for α4, was found to be effective in the treatment of MS, then for Crohn’s disease

Vedolizumab, humanized mAb specific for α4β7, shown effective in CD

GI Pharmacology (1 decks)

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