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Pharm Term 4 > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q 
Domperidone
Metoclopramide
Ondasteron
Omeprazole
Cemitidine
Sulfasalazine/Mesalamine
Azathioprine/6-mercaptopurine
Corticosteroids
Infliximab
A

Domperidone&raquo_space; dopamine antagnonist inc. GI motility
Metoclopramide&raquo_space; 5HT4 agonist inc. GI motility
Ondasteron&raquo_space; 5HT3 antagonist dec emesis
Omeprazole&raquo_space; PPI irreversible
Cemitidine&raquo_space; H2 antagonist (competitive) dec. acid
Sulfasalazine/Mesalamine&raquo_space; Cox Inh. used for IBD and RA
Azathioprine/6-mercaptopurine&raquo_space; imm. suppressant via inh. DNA recycling HGPRT (hypoxanthine)
Corticosteroids&raquo_space; Imm suppression
Infliximab&raquo_space; antibodies neutralize TNF-alpha

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2
Q 
What are the effects on GI motility?
Ach
Substance P
VIP
NO
ATP
DA (D2)
5HT3R
5HT4R
A 
Ach >> inc
Substance P >> inc
VIP >> inh
NO >> inh
ATP >> inh
DA (D2) >> inh
5HT3R >> inc (inh NO release)
5HT4R >> inc (inc Ach and Sub P release)
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3
Q 
What is Doperidone?
Action?
Mechanism?
Special quality?
Side effects?
A

D2 antagonist and prokinetic agent
D2 inhibits GI motility by dec. ACh release
Does NOT enter the BBB, only works on myenteric plexus
SE&raquo_space; arrhythmias and QT prolongation

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4
Q 
What is Metoclopramide?
Action?
Mechanism?
Specific organs involved or not involved?
Side effect?
A

5HT4 agonist and pro kinetic agent
5HT4&raquo_space; inc. ACh and Sub P
Inc esophagus resting tone, gastric tone and peristalsis, relaxes pyloric sphincter, duodenal peristalsis
Does not effect Pan or biliary tract
Extrapyramidal Symptoms, esp in younger pt

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5
Q

What is Erythromycin and its effects on GI?
What is the mechanism?
What organs are involved or not involved?

A

Prokinetic and antibiotic
Erythromycin and Motilin both bind to the motilin receptor (MTLR)
MTLR is a GPCR that inc GI motility of Stomach, but not of Colon
It is useful in Gastroparesis

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6
Q

Recap: What are the Prokinetics?

A

Donperidone
Metoclopramide
Erythromycin

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7
Q

How does Metoclopramide function as an antiemetic?

A

inc. gastric emptying
dec. gastric stasis
Gastric stasis increases emesis
But has CNS side effects (EPS)

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8
Q 
What is Ondasteron?
What are its effects on GI?
What are is effects of CNS?
What are its side effects?
What are specific indications?
A

5HT3 Antagonist
GI&raquo_space; 5HT3 inh. NO release. NO inn ACh release&raquo_space; 5HT3 antagonist is a pro kinetic
CNS&raquo_space; 5HT3 R in CNS are anti-emetic
Has same level of anti-emesis as metoclopramide, but without CNS side effects (no EPS)
Effective for N/V but not for motion sickness

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9
Q

Cannabinoids: Dronabinol

A

Useful for N/V and inc. appetite in HIV pts

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10
Q

H1 antagonists: Diphenhydramine

A

Useful in motion sickness (scopolamine would be better)

Not useful in chemo nausea

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11
Q

What are OTC Antacids?

A

Aluminum or Mg OH
Neutralize secreted acid, but do not change symptoms
Inactivates pepsin
Can lead to constipation and increase blood levels of Al and Mg

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12
Q

What is Cemitidine?
What is its action?
What times of day is it used?
What are safety concerns and side effects?

A
  • Competitive H2 antagonist
  • Decreases basal H+ production, esp nocturnal and in btw meals
  • High safety because H2R are only important in ST
  • Metabolized by P450, so there are side effects from byproducts
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13
Q

What is Omperazole?
What is the mechanism?
What is its concern regarding other medications?
What is its interaction with H2 blockers?

A
  • PPI
  • Drug of choice for GERD
  • Binds to the H+ pump in acid environments
  • May affect the absorption of other drugs that require an acid environment
  • H2 blockers DECREASE omperazole’s effectiveness
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14
Q

What is the most important Tx for Diarrhea?

A

NaCl + Glucose

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15
Q

What are two medications used for Diarrhea?

A

Metamucil&raquo_space; Forms bulk in the stool

Opioids&raquo_space; Loperamide 50x more potent than morphine, but does NOT enter the CNS

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16
Q

What is the most important Tx for constipation?

A

Fiber, fluids, physical activity

17
Q

What are the categories of Rx for constipation?

A
  • Lumen agents&raquo_space; osmotics, stool softeners
  • Non-Specific Irritants&raquo_space; low-grade inflammation&raquo_space; water accumulation
  • Prokinetic agents&raquo_space; ex: 5HT4 agonists, D2 blocker, erythromycin
18
Q

Plasma serotonin levels with
IBS-C&raquo_space;
IBS-D&raquo_space;

A

IBS-C&raquo_space; low serotonin

IBS-D&raquo_space; high serotonin

19
Q

What are serotonin
Antagonist for IBS-D
Agonist for IBS-C

A

Alosteron is a 5HT3 antagonist for IBS-D

Tegaserod is a 5HT4 agonist for IBS-C

20
Q

What is Alosteron?

A

5HT3 antagonist for IBS-D

Dec. motility

21
Q

What is Tegaserod?

A

Tegaserod is a 5HT4 agonist for IBS-C

may cause heart attacks

22
Q

What are medications for IBD?
For mild cases?
For severe cases, short term and long term?

A
  • Mild&raquo_space; Sulfasalazine/mesalamine + corticosteroids

* Severe&raquo_space; short term: MTX. long term: azathioprine/6-MP mecaptopurine

23
Q

What is Sulfasalazine?

A

Combo of Mesalamine and Sulfapyridine
Mes&raquo_space; inh. COX and LOX in gastric mucosa
Sul&raquo_space; free O2 scavenger effective in joints
Not absorbed in ST or SI&raquo_space; used for IBD
More toxic than MTX and Leflunomide

24
Q

What corticosteroids are used for IBD?

A

Prednisone

Budesonide

25
Q

Note: IBD patients are classified as
Steroid responsive
Steroid unresponsive
Steroid dependent

A

.

26
Q

What is Budesonide?

Why is it used?

A

Locally active corticosteroid used for mild-moderate CD involving the ileum and ascending colon
Fewer side effects, but less effective and expensive

27
Q

What is Azothioprine/6-mercaptopurine?

What are the side effects?

A

For severe IBD and maintain remission with less steroids
Takes weeks to produce effects
Causes bone marrow depression&raquo_space; leukopenia and teratogenesis
Note: azothioprine is a prodrug MP is its metabolite

28
Q

What is MTX?
What are side effects?
Contraindication?
What is this the first line med for?

A

DMARD
inh folate metabolism (non toxic at low dose)
GI distress, oral ulcers, hepatotoxicity
Contraindicated: prego, LV/KD problems, DM, obesity
First line med for RA, better used in Crohn’s disease, but also in UC
Reserved for IBD pt that are steroid unresponsive or dependent, but is largely replaced by biologics

29
Q

What are Infliximab (remicade) and Adalimumab (humira)?

What is different about them?

A

Both Anti-TNF-alpha mAb
Both use murine Ab
Humira is more human, so has less side effects
Potentially dangerous in pt with chronic infections, cancers, or ID

30
Q

What are indications for
Infliximab (remicade)
Adalimumab (humira)

A

arthritis (RA, PsA, AS, Juv RA), psoriasis

Infliximab is also indicated for Behcet’s syndrome and Crohn’s

Pharm Term 4 (3 decks)

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