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1 > Upper GI Pharmacology > Flashcards

Upper GI Pharmacology Flashcards

1
Q

Antacid pharmacokinetics

A 
tablets/powder, suspension
Poorly absorbed (unless poor renal function), thus minimal undesired systemic side effects
Di/tri-valent cations; may chelate other drugs, separate dosing
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2
Q

Antacid MOA

A

Locally buffer H+ to increase pH

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3
Q

Antacid indications

A

heartburn, dyspepsia

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4
Q

Antacid SE

A

Mg-containing: osmotic diarrhea (explosive)
Ca-containing: constipation, hypercalcemia, calculi, bloating, nausea (due to CO2 liberated)
Al-containing: constipation, hyperphosphatemia

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5
Q

H2 antagonist prototypes

A

ranitidine, cimetidine

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6
Q

H2 antagonist PK

A

po; some iv and im
rapidly absorbed
renal elimination (filtration and secretion) - adjust dosing in renally impaired patients

Cimetidine: notorious CYP450 blocker

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7
Q

H2 antagonist MOA

A

H2 receptors on parietal cells mediate basal, nocturnal, and meal-stimulated release of acid (histamine binding stimulates H/K ATPase via cAMP)
Reversible blockage

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8
Q

H2 antagonist indications

A

GERD
PUD
Dyspepsia
Prevention of bleeding from stress-related gastritis

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9
Q

H2 antagonist SE

A

generally well-tolerated
diarrhea/constipation, headache, fatigue, MSK pain
Cimetidine only: gynecomastia and galactorrhea

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10
Q

PPI prototypes

A

omeprazole, pantoprazole

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11
Q

PPI PK

A

must be absorbed into systemic circulation
act locally on GI tract cells (parietal cells)
Prodrugs: activated in acidic canaliculi of parietal cells
hepatic clearance - adjust dosing in liver impaired patients

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12
Q

PPI MOA

A

antagonist of proton-secreting pump in stomach (K/H pump) on parietal cells
irreversible

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13
Q

PPI indications

A

gastric and duodenal ulcers, NSAID-induced ulcers
GERD
Pathological hypersecretory conditions (Zollinger-Ellison, where levels of hormone are increased due primarily to gastrinoma tumour of non-beta islet cells in the pancreas)

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14
Q

PPI SEs

A

generally well-tolerated short term
nausea, ab pain, constipation/diarrhea, flatulence (alteration in intestinal flora due to pH change)
less common: hypergastrinemia, due to rebound secretion of gastric acid if PPI is stopped after short-term use

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15
Q

Misoprostol PK

A

short half-life

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16
Q

Misoprostol MOA

A

PG analogue
endogenous PGE2 binds EP3 on parietal cells –> reduces activity of proton pump and stimulates mucin and bicarb secretion to bolster mucosal barrier
endogenous PGE2 is made by COX1
PGE-1 analogues (misoprostol) given as adjuncts in patients on NSAIDs

17
Q

Misoprostol indications

A

NSAID-induced gastric ulcer

18
Q

Misoprostol SEs

A

diarrhea, abd cramping (stimulates smooth muscle contraction in GI and uterus)

19
Q

Sucralfate PK

A

local GI action, minimal absorption (fecally excreted)
activated by acid
contains Al, which is excreted renally - adjust for renal impaired patients

20
Q

Sucralfate MOA

A

complex of sucrose and AlOH –> viscous paste in acid aqueous media (direct
stimulates PG synthesis of mucus and bicarb secretion (indirect)

21
Q

Sucralfate indications

A

Tx and prevention of gastric and duodenal ulcer

22
Q

Sucralfate SE

A

constipation (Al)

minimal systemic effects due to poor absorption

23
Q

Bismuth MOA

A

form protective barrier on ulcer
enhance PG, mucus, bicarb secretion
inhibit H. pylori growth and adherence

24
Q

Bismuth indications

A

Adjunctive therapy in H. pylori eradication

acute diarrhea

25
Q

Bismuth SE

A

black tarry stool (benign discolouration, commonly mistaken for blood)
benign discolouration of tongue
constipation
tinnitus

26
Q

Prokinetic prototypes

A

metoclopramide, domperidone

27
Q

Prokinetic PKs

A

metoclopramide: rapidly absorbed, hepatic metabolism, renal excretion, oral/parental dosage

Domperidone: rapidly absorbed, low oral bioavailability because of extensive first pass mechanism (increased availability with food)

28
Q

Prokinetic MOAs

A

endogenous dopamine inhibits GI motility, since D2 receptors inhibit ACh release
D2 antagonists –> increase LES tone, stimulates GI contraction (upper)
also anti-nauseants via central inhibition of vomiting centre

29
Q

Prokinetic indications

A

gastroparesis, nausea/vomiting (anti-emetic)
GERD
facilitate small bowel intubation

30
Q

Antacid prototypes

A

Ca carbonate

Mg, Al hydroxide

1 (17 decks)

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