Exam 4-4 Acid Controlling Drugs Flashcards

1
Q

Cells of the gastric gland

A
  • Parietal Cells

* Mucous Cells

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2
Q

Parietal Cells

A
  • Produce and secrete HCI

* Primary site of action for many acid-controller drugs

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3
Q

Mucous Cells

A
  • Mucus-secreting cells (surface epithelial cells)
  • Provide a protective mucus coat
  • Protect against self-digestion by HCL
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4
Q

Hydrochloric Acid

A

*Secreted by the parietal cells when stimulated by food
*Maintains stomach pH 1-4
*Secretion also stimulated by:
large fatty meals
excessive amounts of alcohol
emotional stress

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5
Q

Acid-Related Diseases: Characteristics

A
  • Caused by imbalance of the three cells of the gastric gland and their secretions
  • Most common: hyperacidity
  • Lay terms for overproduction of HCI by the parietal cells:
  • ingestion, sour stomach, heartburn, acid stomach
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6
Q

Acid-Related Disease:

A

PUD- peptic ulcer disease
GERD- gastoesophageal reflux disease
Helicobacter pylori (H. pylori)

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7
Q

Helicobacter pylori (H. pylori)

A
  • Bacterium found in GI tract of 90% of patients with duodenal ulcers and 70% of those with gastric ulcers
  • Can be detected by serum antibody tests
  • Antibiotics are used to eradicate H. pylori
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8
Q

Types of Acid-Controlling Drugs

A
  • Antacids
  • H2 antagonists
  • Proton pump inhibitors
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9
Q

Antacids: Mechanism of Action

A

*Neutralize stomach acid
-promote gastric mucosal defense mechanisms
Secretion of:
-Mucus protective barrier against HCI
-Bicarbonate helps buffer acidic properties of HCI
-Prostaglandins: prevent activation of proton pump

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10
Q

Antacids do not prevent

A

the overproduction of acid

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11
Q

Antacids neutralize the

A

acid once it is in the stomach

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12
Q

Antacids: Drug Effects

A

Reduction of pain associated with acid-related disorders:

  • Raising gastric pH from 1.3 to 1.6 neutralizes 50% of the gastric acid
  • Raising gastric pH 1 point (1.3 to 2.3) neutralizes 90% of the gastric acid
  • Reducing acidity reduces pain
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13
Q

Antacids

A
  • OTC formulations available as:
  • Capsules and tablets
  • Powders
  • Chewable tablets
  • Suspensions
  • Effervescent granules and tablets
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14
Q

Antacids used alone or in combination with:

A
  • Aluminum salts
  • Magnesium salts
  • Calcium salts
  • Sodium bicarbonate
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15
Q

Antacids: Aluminum Salts

A

*Have constipating effects
*Often used with magnesium to counteract contispation
*Often recommended for patients with renal disease (More easily excreted)
-examples
aluminum carbonate: Basaljel
Hydroxide salt AlternaGEL
Combination Maalox, Mylanta, Di-Gel

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16
Q

Antacids: Magnesium Salts

A
  • Commonly cause diarrhea: usually used with other drugs to counteract this effect
  • Dangerous when used with renal failure- the failing kidney cannot excrete extra magnesium, resulting in accumulation
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17
Q

Magnesium Salts-Examples

A
  • Hydroxide salt- magnesium hydroxide (MOM)
  • Carbonate salt- Gaviscon (also a combination product)
  • Combination products such Maalox, Mylanta (aluminum and magnesium)
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18
Q

Antacids: Calcium Salts/Characteristics

A
  • Many forms, but carbonate is most common
  • May cause constipation, kidney stones
  • Also not recommended for patients with renal disease- may accumulate to toxic levels
  • Long duration of acid action-may cause increased gastric acid secretion (Hyperacidity rebound)
  • Often advertised as an extra source of dietary calcium
  • example: Tums (calcium carbonate)
19
Q

Antacid: Sodium Bicarbonate/Characteristics

A
  • Highly soluble
  • Buffers the acidic properties of HCL
  • Quick, onset, but short duration
  • May cause metabolic alkalosis
  • Sodium content may cause problems in patients with HF, hypertension, or renal insufficiency
20
Q

Antiflatulents are used for

A

to relieve the painful symptoms associated with gas

-drugs are used to bind or alter intestinal gas and are often added to antacid combination products

21
Q

OTC antiflatulents

A
  • Activated charcoal
  • Simethicone
  • alters elasticity of mucus-coated bubbles, causing them to break
  • used often, but there are limited data to support effectiveness
22
Q

Antacids: Adverse Effects

A
  • Aluminum and calcium
  • constipation
  • Magnesium
  • diarrhea
  • Calcium carbonate
  • produces gas and belching often combined with simethicone
23
Q

Antacids: Drug Interactions

A

*Absorption of other drugs to antacids
-reduces the ability of the other drug to be absorbed into the body
Chelation
-chemical binding, or inactivation, of another drug
-produces insoluble complexes
-result reduced absorption

24
Q

Antacids: Drug Interactions-Increased stomach pH-

A
  • increased absorption of basic drugs

* decreased absorption of acidic drugs

25
Antacids: Drug Interactions-Increased Urinary pH-
* increased excretion of acidic drugs | * decreased excretion of basic drugs
26
Histamine 2 (H2) Antagonists
* Reduce acid secretion * All available OTC in lower dosage forms * Most popular drugs for treatment of acid-related disorders - cimetidine (Tagamet) - nizatidine (Axid) - famotidine (Pepcid) - ranitidine (Zantac)
27
H2 Antagonists: Mechanism of Action
* Block histamine at the (H2) receptors of acid-producing parietal cells * Production of hydrogen ions is reduced, resulting in decreased production of HCl
28
H2 Antagonists: Drug Effect
Suppressed acid secretion in the stomach
29
H2 Antagonists: Indications
* GERD * PUD * Erosive esophagitis * Adjunct therapy in control of upper GI bleeding * Pathologic gastric hypersecretory conditions
30
H2 Antagonist: Adverse Effects
*Overall very few adverse effects *Cimetidine may induce impotence and gynecomastia May see: -Headaches, lethargy, confusion, diarrhea, urticaria, sweating, flushing
31
H2 Antagonists: Drug Interactions/cimetidine
* Binds with P-450 microsomal oxidase system in the liver, inhibiting oxidation of many drugs and increasing drug levels * All H2 antagonists may inhibit the absorption of drugs that require an acidic GI environment for absorption
32
Smoking has been shown to-
decrease the effectiveness of H2 blockers
33
Proton Pump Inhibitors
* The parietal cells release positive hydrogen ions (protons) during HCI production * This process is called the proton pump * H2 blockers and antihistamines do not stop the action of this pump
34
Proton Pump Inhibitors: Mechanism of Action
Irreversibly bind to H+/K+ ATPase enzyme - this bond prevents the movement of hydrogen ions from the parietal cell into the stomach - result achlorhydria-gastric acid secretion is temporarily blocked * in order to return to normal acid secretion, the parietal cells must synthesize new H+/K+ ATPase
35
Proton Pump Inhibitors: Drug Effect
* Inhibition of gastric acid secretion - lansoprazole (Prevacid) - omeprazole (Prilosec) - rabeprazole (Aciphex) - pantopraxole (Protonix), (IV form available) - esomeprazole (Nexium)
36
Proton Pump Inhibitors: Indications
* GERD maintenance therapy * Erosive esophagitis * Short term treatment of active duodenal and benign gastric ulcers * Zollinger-Ellison syndrome * Treatment of H. pylori- induced ulcers - Administered with an antibiotic
37
Proton Pump Inhibitors: Adverse Effects
Adverse effects uncommon
38
Other Durgs
* sucralfate (Carafate) * misoprostol (Cytotec) * simethicone (Mylicon)
39
Sucralfate (Carafate)/Characteristics
* Cytoprotective drug * Used for stress ulcers, PUD * Attracted to and binds to the base of ulcers and erosions, forming a protective barrier over these areas * Protects these areas from pepsin, which normally breaks down proteins (Making ulcers worse)
40
Sucralfate (Carafate)/Characteristics continued
* Little absorption from the gut * May cause constipation, nausea and dry mouth * May impair absorption of other drugs-give other drugs at least 2 hours before sucralfate * Do not administer with other medications * Binds with phosphate; may be used in chronic renal failure to reduce phosphate levels
41
Misoprostol (Cytotec)
* Synthetic prostaglandin analog * Prostaglandins have cytoprotective activity - Protect gastric mucosa from injury by enhancing local production of mucus or bicarbonate - Promote local cell regeneration - Help to maintain mucosal blood flow
42
Misoprostol (Cytotec) is used for
prevention of NSAIDS -induced gastric ulcers
43
Simethicone
* Antiflatulent drug * Used to reduce the discomforts of gastric or intestinal gas (flatulence) * Alters elasticity of mucus-coated gas bubbles, breaking them into smaller ones * Decreases gas pain and increases expulsion via mouth or rectum