peptic diseases pharmacology Flashcards

1
Q

Pharmacological treatment of PU categories?

A

Agents affecting gastric secretion

Mucosal Protective Agents

Post secretoryagents

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2
Q

Agents affecting gastric secretion?

A

PPI

Anti H2 -histamines

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3
Q

Mucosal Protective Agents?

A

Prostaglandins

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4
Q

Post secretoryagents?

A

Anti-acids

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5
Q

receptors on parietal cells?

A

H2 histamin (Gi)
colicystokinin B (gastrin, Gq)
M3 (Ach, Gq)
E2 (PG, Gi)

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6
Q

PPI targets?

A

inhibitors of the gastric H+, K+-ATPase

covalent inhibition

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7
Q

PPI mechanism of action?

A
p/o prodrug
blood
entrocytes canaliculi (acid inviroment)
activation
H+, K+-ATPase covalent inhibition
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8
Q

PPI paradox?

A

lond lasting effect

short half life (0.5-2h)

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9
Q

How to prevent degradation of proton pump inhibitors by acid

A

enteric coated prodrug

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10
Q

PPI drug examples

A
omeprazole
lansoprazole 
rabeprazole
pantoprazole
(prazole)
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11
Q

PPI side effects?

A

generaly safe

common side effects:
Diarrhea, headache, and abdominal pain

prolonged: subnormal B12 levels (intrinsic factor, PH)

Respiratory and Enteric Infections due to PH change

rebound hypersecretion of gastric acid upon discontinuation of therapy

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12
Q

histamine receptors characteristics?

A

H1 + H2 are peripherial
H1 s.muscle, endothel, brain (Gq)
H2 gastric mucosa, cardiac muscle, mast cells, brain (Gs)
both basolaterl in parietal cells

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13
Q

H2-receptor antagonists indications?

A

Gastric and duodenal ulcers

Uncomplicated GERD

Stress ulcers (prevent the occurrence)

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14
Q

H2-receptor antagonists examples?

A

cimetidine (1) > rantidine (4-10) > nizatidine (4-10) > famotidine (20-50)
most usable are rentidine anf famotidien

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15
Q

H2 receptor antagonists most common side effects?

A
Diarrhea
headache
fatigue
myalgias
constipation
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16
Q

H2-receptor antagonists IV administration side effects?

A

mental status change

17
Q

cimitidine side affects?

A
inhibits binding of dihydrotestosterone to androgen
receptors
inhibits metabolism of estradiol
increases serum prolactin levels
genicomastia
18
Q

PG Mechanism of action?

A

reducing histamine-stimulated cAMP production in parietal cells
bicarbonate secretion
enhance mucosal blood flow

19
Q

PG ananlougs example?

A

misoprostol- synthetic analogue of PGE1

-prevention of NSAID-induced ulcers in high-risk patients

20
Q

Mucosal Protective Agents examples?

A

Sucralfate

Bismuth chelate

21
Q

Sucralfate Mechanism of action?

A

salt of sucrose complexed to sulfated aluminum hydroxide

polymerization (6 hrs) ⇒ Stick to ulcer craters

22
Q

Bismuth chelate Mechanism of action?

A

stong affinity for mucosal glycoproteins, especially in the necrotic tissue of the ulcer craters ⇒
polymerization

23
Q

Pink bismuth contraindication?

A

bismuth subsalicylate ⇒ subsalicylate like compounds (Asperin) cause Ray’s syndrome in fever acompanied diseases (as viral infections)

24
Q

Anti-acids mechanism of action?

A

Neutralize HCl to form H2O + salt
Sodium bicarbonate → NaCl+ CO2
Calcium bicarbonate → CaCl2 + CO2 (slower
reaction with HCl)
Magnesium hydroxyde → MgCl2+ H20
Aluminium hydroxyde → AlCl3+ H20
hydroxydes can be given simultaniously

Imidiate but temporary relief 20-30 min

affect the absorption of other medications
by binding the drug
or
by increasing intragastric pH

should not be given within 2h before tetracyclines, fluoroquinolones, itraconazole, iron and others

25
Q

Sodium bicarbonate Adverse effects?

A

Gastric distention

Belching

Metabolic alkalosis in patients with renal insufficiency

Exacerbate fluid retention in patients with heart failure, hypertension, and renal insufficiency

26
Q

Calcium bicarbonate Adverse effects?

A

Belching

Metabolic alkalosis

Excessive doses of calcium (dairy) lead to hypercalcemia, renal insufficiency, and metabolic alkalosis (milk-alkali syndrome)

27
Q

Aluminum hydroxide Adverse effects?

A

May cause constipation

Patients with renal insufficiency should not take these agents long-term (can aggregate)

28
Q

Magnesium hydroxide Adverse effects?

A

May cause diarrhea

Patients with renal insufficiency should not take these agents long-term (can aggregate)