Gastrointestinal Diseases Flashcards
Drugs used in Acid-Peptic Diseases
Anti secretory agents
Histamine 2 receptor antagonists
Proton pump inhibitors
Anti muscarinic
Drugs used in Acid-Peptic Diseases
Mucosal protective agents
Sucralfate
Prostaglandin analogs
Colloidal bismuth compounds
Carbenoxolone
Drugs used in Acid-Peptic Diseases
Antacids
A measure for the overall buffering capacity against acidification for a solution.
Acid-Neutralization Capacity (ANC)
Drugs used in Acid-Peptic Diseases
Antacids
ANC defined as the difference between what?
Cation of strong bases and
Anions of strong acids
Drugs used in Acid-Peptic Diseases
Antacids
ANC, the amount of acid needed to change the pH value from the sample’s value to a chosen different value. Depends on?
Rate of dissolution
Water solubility
Rate of reaction with acid
Rate of gastric emptying
Drugs used in Acid-Peptic Diseases
Antacids
Weak bases + gastric acid =
Salt and water
Drugs used in Acid-Peptic Diseases
Antacids
MOA
Reduction of intra gastric acidity
Stimulate mucosal PG production
Promote mucosal defense mechanism
Drugs used in Acid-Peptic Diseases
Antacids
Dosage
156 mEq given 1 hour after meal
Neutralize up to 2 hours
Drugs used in Acid-Peptic Diseases
Antacids
Particulate antacids (non systemic)
Magnesium OH
Aluminum OH
Drugs used in Acid-Peptic Diseases
Antacids
No particulate antacids (systemic)
Sodium bicarbonate (baking soda, alka seltzer) Calcium carbonate (Tums, Os-Cal)
Drugs used in Acid-Peptic Diseases
Antacids
Non particulate antacids
Reacts rapidly with HCL Metabolic acidosis Gastric distention and belching Exacerbate fluid retention HTN Renal insufficiency
Drugs used in Acid-Peptic Diseases
Antacids
Less soluble
Calcium carbonate
Drugs used in Acid-Peptic Diseases
Antacids
Non particulate
Adverse effects
Hypercalcemia
Renal insufficiency
Metabolic alkalosis
Milk alkali syndrome
Drugs used in Acid-Peptic Diseases
Antacids
Particulate antacids (non systemic)
Reacts slowly with HCL
Drugs used in Acid-Peptic Diseases
Antacids
Particulate
Reacts slowly with HCL
MgCl or AlCl and water
Drugs used in Acid-Peptic Diseases
Antacids
Particulate
Unabsorbed magnesium lead to
Osmotic diarrhea
Drugs used in Acid-Peptic Diseases
Antacids
Particulate
Unabsorbed aluminum
Constipation
Drugs used in Acid-Peptic Diseases
Antacids
Particulate
Combined to minimize effects
Gelusil
Maalox
Mylanta
Drugs used in Acid-Peptic Diseases
Antacids
Particulate
Minimally absorbed
Excreted by kidneys
Drug interactions of all antacids
Tetracyclines
Fluoroquinolones
Itraconazole
Iron
Drugs used in Acid-Peptic Diseases
Antacids
Reduce absorption by?
Antacid binding with the drugs
Increase intra gastric pH
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
MOA
Competitive inhibition at parietal cell H2 receptors
Suppress basal and meal-stimulated acid secretion
Reduce gastric secretion
Reduce concentration of pepsin
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Drugs
Cimetidine
Ranitidine
Famotidine
Nizatidine
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Drugs that has a first pass hepatic metabolism and bioavailability of 50%
Cimetidine
Ranitidine
Famotidine
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Drug that has little first pass and almost 100% bioavailability
Nizatidine
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
2 mechanisms in reduction of acid secretion stimulated by
Histamine
Gastrin
Cholinomimetic agents
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Memorize the table
Stop answering then memorize the table
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Clinical uses
GERD
PUD
Non ulcer Dyspepsia
Prevention of bleeding from stress-related gastritis
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
GERD
6-10 hours duration
BID before meals
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
PUD
OD at HS
Prevent occurence- half
NSAID associated - rapid healing if NSAID is DC
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Adverse effects
Diarrhea Headache Fatigue Myalgia Constipation Pregnant and nursing
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Adverse effects in CNS
Mental status changes
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Adverse effects in elderly
Renal or hepatic dysfunction
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Adverse effects, endocrine effects:cimetidine
Gynecomastia
Impotence
Inhibit metabolism of estradiol
Galactorrhea
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Rare adverse effects
Blood dyscrasias
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Interferes with hepatic cytochrome P450 drug metabolism pathways
Prolonged half lives
Cimetidine
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Binds 4-10 times less
Ranitidine
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Drug interactions
Compete with creatine and certain drugs like
Procainamide
Drugs used in Acid-Peptic Diseases
Anti secretory: H2 - receptor antagonists
Drug interactions
Inhibit first pass metabolism of ethanol except
Famotidine
Anti secretory proton pump inhibitors
Drugs
Omeprazole (losec) Lansoprazole (Prevacid) Rebeprazole (pariet) Dexlanzoprazole (dexilant) Pantoprazole (pantoloc) Esomeprazole (nexium)
Anti secretory proton pump inhibitors
Pro drugs
Lipophylic weak bases
Anti secretory proton pump inhibitors
Bioavailability
Decreased 50% by food
Anti secretory proton pump inhibitors
Given when
1 hour before meal
Anti secretory proton pump inhibitors
Short serum plasma half life
1.5 hours
Anti secretory proton pump inhibitors
Long duration of acid inhibition
Up to 24 hours
Anti secretory proton pump inhibitors
Required to reach full acid inhibiting potential
3-4 days daily medication
Anti secretory proton pump inhibitors
How many hours are required for synthesis of new ATPase pump
18 hours
Anti secretory proton pump inhibitors
Clinical uses
GERD
Most effective treatment for
Long term maintenance
Erosive reflux disease
Anti secretory proton pump inhibitors
Clinical uses
GERD
Most effective treatment for
Intermittent courses
Non erosive reflux disease
Anti secretory proton pump inhibitors
Clinical uses
GERD
Most effective treatment for esophageal complications of reflux disease
Peptic stricture
Barrett’s esophagitis
Anti secretory proton pump inhibitors
Clinical uses
GERD
Most effective treatment for
Extra esophageal manifestations of reflux disease
Asthma
Chronic cough
Laryngitis
Non cardiac chest pain
Anti secretory proton pump inhibitors
Clinical uses
GERD
Once daily
85-90% symptom relief and tissue healing