Drugs for upper GI Flashcards

1
Q

What are the 8 drug classes we learned from this lecture

A

1) Antacids
2) hIstamine 2 receptor agonists
3) Proton pump inhibitors
4) Antiemetics
5) Protective barriers
6) Misoprostol
7) Prokinetic drugs
8) Antimuscarinics
90) Gastrin receptor antagonists

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2
Q

What are the 3 antacids we know?

A

Mg(OH)2- milk of magnesia
CaCO3- Tums
Al(OH)3- Gaviscon

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3
Q

What is the MOA of Antacids

A

increase gastric pH

neutralize acid

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4
Q

What are the pharmacokinetics of Anacitds

A

AL,ca and mg no absobed
May chelate other drugs, affecting their absorption
altered pH may affect drug absorption

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5
Q

When to use antacids (2)

A

Heartburn/mild Gerd

dyspepsia

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6
Q

Are there any contraindications for Antacids

A

no major ones :)

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7
Q

Side effects of Antacids

A

Bleching
Ca-hypercalcemia->possibel calculi formation

Al-containing- constipation and hyophosphatmia
Mg- diarrhea

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8
Q

What is the end sound for H2 receptor antagonists

A

tidine

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9
Q

what is MOA of H2 receptor antagonists

A

Competitive selective block of histamine h2 receptors

Reduced but not eliminated acid secretion
up to 60-70% reduction
because ACh and Gastrin pathways still available in response to food-related stimulus

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10
Q

What is the most effective drug at reducing nocturnal acid secretion

A

H2 receptor antagonists

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11
Q

Pharmacokinetics of H2 receptor antagonists

A

oral and intramuscular and intravenous fomulation
only 50% oral bioavaliblity
peak absorption at 1-3 hrs

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12
Q

What are the indications for H2 receptor antagonists (4)

A

Dyspepsia
GERD
Peptic ulcer disease
Prevention of bleeding from stress-related gastritis

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13
Q

What are the contraindications for H2 receptor antagonists

A

none

no known harm to fetus

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14
Q

Side effects of H2 receptor antagonists

A

diarrhea/consitpation
headache
drowsiness/fatigue
muscle pain

Rare CNS symtoms

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15
Q

What is the ending of PPI’s

A

prazole

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16
Q

MOA of PPI’s

A

Irreversible inactivation of proton pump common to all triggers of gastric acid secretion vell affected will never secrete again

Decrease H+ secretion by 90-98%

restoration of function requires new Proton pump synth-> 18-24 hrs

once-daily oral treatment

relatively selective for parietal cell proton pumps

17
Q

Indication for PPIs

A
Gystic and duodenal ulcer
h.pylori associated
Nsaid induced
GERD
prevention of bleeding from stress-related gastritis
Gastric hypersecretory conditions
like Zollinger-Ellison syndrome
18
Q

Contriinidcation for PPIs

A

None :)

19
Q

Side effects PPIs

A
non really but
flatulence
nausea 
abdominal pain
diarrhea or consitpation
20
Q

Antimuscarinics for Stomach

A

pirenzipine

utile effective but side effects

21
Q

Gastrin receptor antagonists

A

Proglumide

pathway inhibited at pH

22
Q

H.pylori triple therapy

A

for 2 weeks
PPI+clarithromycin + (metonidizole or amoxicillan)

then 6week just PPI

23
Q

What does Misoprostol do

A

Misoprostol is a Prostaglandin E1(PGE1) analogue and inhibits parietal cells and stimulates mucus cells

24
Q

Pharmacokinetics of Misoprostol

A

Short half-life -frequent dosing

no impact on cytochrome P450 enzyme

25
Q

Indication for Misoprostol

A

NSAID induced ulcers

26
Q

Contraindication for Misoprostol

A

pregnancy its a strong uterine stimulant

27
Q

Side effects of misoprostol

A

Diarrhea
abdominal cramping
uterine contraction

28
Q

What is Sucralfate and what is its MOA

A
Al(OH)3- sucrose sulfate complex 
acid release anionic sulphated sucrose
binds to charged proteins in ulcer
viscous sticky, protective barrier
indirect stimulation of PGE2-production
29
Q

Pharmacokinetics of sucralfate

A

Take on empty stomach
localized action /minimal systemic absorption
short effect (~6hrs)

30
Q

Indication for Sucralfate

A

Gastic and duodenal ulcer

31
Q

Contraindications for Sucralfate

A

None

32
Q

Side effects of Sucralfate

A

Al3 induced constipation

may reduce the absorption of other drugs

33
Q

What is the mechanism of action of bismuth subsalicylate (Peptobismul)

A

Coat ulcers-> physical protective barrier
increase PGE2, HCO3 and mucus production
antimicrobial
reduces stool frequency

34
Q

Pharmacokinetics of bismuth subsalicylate (Peptobismul)

A

dissocaites in stomach acts locally

only salicylate substantially absorbed

35
Q

indication for bismuth subsalicylate (Peptobismul)

A

H.pylori ulcer

acute diarrhea

36
Q

Contraindication of bismuth subsalicylate (Peptobismul)

A

Children with viral infection-> reyes syndrome

allergies to ASA (30 mL~325 mg tablet

37
Q

Side effects of bismuth subsalicylate (Peptobismul)

A

Black stool
black tounge
constipation

38
Q

What are the two prokinetic drugs we know

A

Metoclopramide and domperidone