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
Q

Antacids: Drug Interactions-Increased Urinary pH-

A
  • increased excretion of acidic drugs

* decreased excretion of basic drugs

26
Q

Histamine 2 (H2) Antagonists

A
  • 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
Q

H2 Antagonists: Mechanism of Action

A
  • Block histamine at the (H2) receptors of acid-producing parietal cells
  • Production of hydrogen ions is reduced, resulting in decreased production of HCl
28
Q

H2 Antagonists: Drug Effect

A

Suppressed acid secretion in the stomach

29
Q

H2 Antagonists: Indications

A
  • GERD
  • PUD
  • Erosive esophagitis
  • Adjunct therapy in control of upper GI bleeding
  • Pathologic gastric hypersecretory conditions
30
Q

H2 Antagonist: Adverse Effects

A

*Overall very few adverse effects
*Cimetidine may induce impotence and gynecomastia
May see:
-Headaches, lethargy, confusion, diarrhea, urticaria, sweating, flushing

31
Q

H2 Antagonists: Drug Interactions/cimetidine

A
  • 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
Q

Smoking has been shown to-

A

decrease the effectiveness of H2 blockers

33
Q

Proton Pump Inhibitors

A
  • 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
Q

Proton Pump Inhibitors: Mechanism of Action

A

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
Q

Proton Pump Inhibitors: Drug Effect

A
  • Inhibition of gastric acid secretion
  • lansoprazole (Prevacid)
  • omeprazole (Prilosec)
  • rabeprazole (Aciphex)
  • pantopraxole (Protonix), (IV form available)
  • esomeprazole (Nexium)
36
Q

Proton Pump Inhibitors: Indications

A
  • 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
Q

Proton Pump Inhibitors: Adverse Effects

A

Adverse effects uncommon

38
Q

Other Durgs

A
  • sucralfate (Carafate)
  • misoprostol (Cytotec)
  • simethicone (Mylicon)
39
Q

Sucralfate (Carafate)/Characteristics

A
  • 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
Q

Sucralfate (Carafate)/Characteristics continued

A
  • 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
Q

Misoprostol (Cytotec)

A
  • 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
Q

Misoprostol (Cytotec) is used for

A

prevention of NSAIDS -induced gastric ulcers

43
Q

Simethicone

A
  • 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