Gastroesophageal Reflux Disease (GERD) & Peptic Ulcer Disease Flashcards
class:
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Parietal cells in the epithelial lining of the stomach secrete hydrochloric acid (HCl) through the _________________________ also know as the ___________
H+/K+ adenosine triphosphatase (ATPase) pump
proton pump
The pump and secretion of HCl is stimulated by __________, __________ and _________
histamine
acetylcholine (ACh)
gastrin (a hormone which also has added role of stimulating stomach muscle contractions to aid in digestion)
Acidic gastric contents are normally prevented from backflow into the esophagus by a protective ring of muscle fibers called the ________________
(LES) lower esophagus sphincter
Patients with (GERD) gastroesophageal reflux disease have ___________________ and gastric contents can backflow into the esophagus.
reduced LES pressure
Typical GERD symptoms:
- heartburn (daytime or nocturnal)
- hypersalivation
- regurgitation of acidic contents into the mouth or throat
LESS common symptoms:
- epigastric pain, nausea, cough, sore throat, chest pain, hoarseness
Diagnosis: Is based on patient-reported symptoms
Duration
Daytime and/or nighttime
frequency (> or = to 2 times per week) & risk factors
GERD can decrease quality of life and lead to ___________, ___________ and ____________.
If a patient has alarm symptoms or there is concern for a more serious condition, _____________ can be performed to further investigate the problem.
- esophageal erosion
- strictures
- Barrett’s esophagus (abnormal cell growth in the esophageal lining which can lead to esophageal cancer)
- endoscopy
ALARM symptoms include:
odynophagia (painful swallowing)
dysphagia (difficulty swallowing)
frequent nausea/vomiting
hematemesis (blood in vomit)
black bloody stools
unintentional weight loss
Key drugs that can worsen GERD symptoms:
They worsen GERD symptoms because they can contribute to _________
- aspirin/NSAIDs
- bisphosphonates
- dabigatran
- estrogen products
- fish oil products
- iron supplements
- nicotine replacement
- steroids
- tetracyclines
lowering of the LES pressure
_____________ can increase the LES pressure
Protein rich foods
Patients should be referred for further evaluation if they DO NOT respond to lifestyle-modifications and/or __________________ or if _______________
two weeks of self-treatment with OTC products
alarm symptoms are present
Treatment should include: ____________ AND ____________
lifestyle modifications
drugs
Infrequent heartburn (< 2 times per week) can be treated with ____________________
as needed (PRN) OTC antacids or histamine-2 receptor antagonists (H2RAs)
An _______________________ of a _________________ is the initial drug treatment of choice for GERD and is used to heal any erosive esophagitis.
After _________________, treatment should be interrupted; if symptoms return, maintenance therapy is needed.
8-week coarse
Proton Pump inhibitor
8-weeks
Are there any major differences in efficacy between available PPIs (proton pump inhibitors)?
No
What drugs are NOT recommended for GERD treatment?
metoclopramide (Reglan, Gimoti)
sucralfate (Carafate)
** Are used in (PUD) Peptic Ulcer Disease**
GERD Treatment Algorithm:
-
-
-
- Weight loss (if overweight or recently gained weight)
- elevate the head of the bed with foam wedges or blocks
- avoid eating high fat meals within 2-3 hours of bedtime
- avoid foods/beverages that trigger reflux (patient specific):
caffeine, chocolate, acidic/spicey food, carbonated beverages
GERD Treatment Algorithm:
Initial Drug Treatment-
Proton Pump Inhibitor (PPI) once daily for 8-weeksw
- can increase to twice daily if partial response or if nocturnal symptoms are present
- STOP treatment at 8 weeks; if symptoms return, start maintenance therapy
GERD Treatment Algorithm:
Maintenance therapy-
1st line: PPI at the lowest effective dose**
Alternative: H2RAs, if there is NO erosive esophagitis and it relieves symptoms
Do NOT Use metoclopramide or sucralfate (NOT recommended)
- Weight loss has the best evidence for improvement of symptoms
** Can include intermittent or on-demand dosing
Antacids:
How do they work?
How fast do they work?
How long do they provide relief for?
- work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
- Since antacids DO NOT require systemic absorption, they provide relief within minutes
- Duration of relief is short (30-60min)
Antacids containing only:
Calcium Carbonate
Tums
Antacids containing only:
calcium carbonate + magnesium
Mylanta Supreme
Rolaids
Antacids containing only:
calcium carbonate + simethicone
Phazyme
Antacids containing only:
magnesium hydroxide
Milk of Magnesia
Antacids containing only:
magnesium hydroxide + aluminum
Antacids containing only:
magnesium hydroxide + aluminum + simethicone
Mylanta Classic
Antacids containing only:
sodium bicarbonate +aspirin + citric acid
Alka-Selzer
Patients should be made aware of the serious bleeding risk if used too frequently due to aspirin**
Which antacid products are constipating?
Calcium containing
Aluminum containing
Which antacid products are diarrhea causing?
magnesium containing
Antacids combining ___________ and _________ are used to lower stomach acid w/o producing undesirable constipation or diarrhea.
Al AND mg
Alka-Seltzer contains > 500mg Na per tablet which can worsen edema in patients with heart failure or cirrhosis.
Tums
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Calcium Carbonate
class: Antacid
Indications: GERD symptoms
MOA: work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
Dosage forms:
Dosing: varies based on products (4-6 times per day)*
Contraindications:
Warnings:
**aluminum & magnesium: can accumulate with severe dysfunction (NOT recommended if CrCl < 30mL/min); risk of bleeding with aspirin containing products.
Side Effects:
- unpleasant taste
Monitoring:
Pearls/Notes:
* *calcium containing antacids are preferred in pregnancy
- FAST Acting AND SHORT-acting
-Antacids: OTC
– provide relief within minutes (FAST acting)
– Duration of relief: 30-60min (SHORT duration)
Drug-Drug/Food interactions:
Mylanta
class:
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class: Antacid
Indications: GERD symptoms
MOA: work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
Dosage forms:
Dosing: varies based on products (4-6 times per day)*
Contraindications:
Warnings:
**aluminum & magnesium: can accumulate with severe dysfunction (NOT recommended if CrCl < 30mL/min); risk of bleeding with aspirin containing products.
Side Effects:
- unpleasant taste
Monitoring:
Pearls/Notes:
* *calcium containing antacids are preferred in pregnancy
- FAST Acting AND SHORT-acting
-Antacids: OTC
– provide relief within minutes (FAST acting)
– Duration of relief: 30-60min (SHORT duration)
Drug-Drug/Food interactions:
Maalox
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class: Antacid
Indications: GERD symptoms
MOA: work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
Dosage forms:
Dosing: varies based on products (4-6 times per day)*
Contraindications:
Warnings:
**aluminum & magnesium: can accumulate with severe dysfunction (NOT recommended if CrCl < 30mL/min); risk of bleeding with aspirin containing products.
Side Effects:
- unpleasant taste
Monitoring:
Pearls/Notes:
* *calcium containing antacids are preferred in pregnancy
- FAST Acting AND SHORT-acting
-Antacids: OTC
– provide relief within minutes (FAST acting)
– Duration of relief: 30-60min (SHORT duration)
Drug-Drug/Food interactions:
Milk of Magnesia
class:
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class: Antacid
Indications: GERD symptoms
MOA: work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
Dosage forms:
Dosing: varies based on products (4-6 times per day)*
Contraindications:
Warnings:
**aluminum & magnesium: can accumulate with severe dysfunction (NOT recommended if CrCl < 30mL/min); risk of bleeding with aspirin containing products.
Side Effects:
- unpleasant taste
Monitoring:
Pearls/Notes:
* *calcium containing antacids are preferred in pregnancy
- FAST Acting AND SHORT-acting
-Antacids: OTC
– provide relief within minutes (FAST acting)
– Duration of relief: 30-60min (SHORT duration)
Drug-Drug/Food interactions:
Alka-Seltzer
class:
Indications:
MOA:
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class: Antacid
Indications: GERD symptoms
MOA: work by neutralizing gastric acid (producing salt and water) which increases gastric pH, making it more alkaline.
Dosage forms:
Dosing: varies based on products (4-6 times per day)*
Contraindications:
Warnings:
**aluminum & magnesium: can accumulate with severe dysfunction (NOT recommended if CrCl < 30mL/min); risk of bleeding with aspirin containing products.
Side Effects:
- unpleasant taste
Monitoring:
Pearls/Notes:
* *calcium containing antacids are preferred in pregnancy
- FAST Acting AND SHORT-acting
-Antacids: OTC
– provide relief within minutes (FAST acting)
– Duration of relief: 30-60min (SHORT duration)
Drug-Drug/Food interactions:
What type of antacids are preferred in pregnancy?
Calcium containing antacids.
Treatment Principles:
PPIs
H2RAs
Antacids
PPIs - Most effective agents, Caution with chronic use
H2RAs- Moderately effective, be careful in elderly
Antacids- Less effective for maintenance, Least effective
Which Histamine-2 receptor antagonist is available as an injection?
famotidine
Which Proton Pump Inhibitors are available as an injection?
pantoprazole
esomeprazole
which Histamine-2 receptor antagonists are available OTC?
famotidine
cimetidine
Which proton pump inhibitors are available OTC?
omeprazole (Prilosec)
esomeprazole (Nexium)
lansoprazole (Prevacid, Prevacid SoluTab)
Which Proton Pump inhibitors are available as an ODT?
omeprazole
lansoprazole (Prevacid SoluTab)
Which Proton Pump inhibitors some in packets for a suspension?
esomeprazole
omeprazole
pantoprazole
Pepcid
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
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Monitoring:
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Drug-Drug/Food interactions:
famotidine
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
*OTC- 10-20mg 1-2 times daily PRN
*RX- 20mg BID
-** if CrCl < 60mL/min: decrease dose
Warnings:
Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]; vitamin B12 deficiency with prolonged Use ( > or = 2 years)
Famotidine: ECG changes (QT prolongation) with renal dysfunction
Side Effects:
CNS effects (especially in elderly)
headache, agitation/vomiting in children < 1 year
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
- to relieve symptoms, take PRN.
- to prevent symptoms, take PRN 30-60 minutes before food or beverages that cause heartburn
- tachyphylaxis (tolerance to effects) can occur if used on a scheduled basis
Drug-Drug/Food interactions:
Zantac 360
class:
Indications:
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famotidine
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
OTC- 10-20mg 1-2 times daily PRN
RX- 20mg BID
**IF CrCl < 60mL/min: DECREASE DOSE
Warnings:
*Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]
Side Effects:
headache, agitation/vomiting in children < 1 year
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
- to relieve symptoms, take PRN.
- to prevent symptoms, take PRN 30-60 minutes before food or beverages that cause heartburn
- tachyphylaxis (tolerance to effects) can occur if used on a scheduled basi
Drug-Drug/Food interactions:
Pepcid Complete
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
famotidine + calcium carbonate + magnesium hydroxide
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
OTC-
RX-
Max dose:
Contraindications:
Warnings:
*Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]
Side Effects:
headache, agitation/vomiting in children < 1 year
Monitoring:
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
Drug-Drug/Food interactions:
Tagamet HB
class:
Indications:
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cimetidine
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
*OTC- 200mg 1-2 times daily PRN
*RX- 400mg every 6 hours
If CrCl < 30mL/min- DECREASE DOSE
Contraindications:
Warnings:
*Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]; vitamin B12 deficiency with prolonged Use ( > or = 2 years)
Side Effects:
CNS effects (especially in elderly)
headache, agitation/vomiting in children < 1 year
**Cimetidine (high doses) gynecomastia (swollen male breasts), impotence
Monitoring:
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
-* cimetidine can increase SCr, without causing renal impairment
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
- to prevent symptoms, take PRN 30-60min before food or beverages that cause heartburn
- to relieve symptoms, take PRN
- to relieve symptoms, take PRN.
- to prevent symptoms, take PRN 30-60 minutes before food or beverages that cause heartburn
- tachyphylaxis (tolerance to effects) can occur if used on a scheduled basi
Drug-Drug/Food interactions:
nizatidine
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
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Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
RX- 150mg BID
Max dose:
Contraindications:
Warnings:
*Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]
Side Effects:
headache, agitation/vomiting in children < 1 year
Monitoring:
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
Drug-Drug/Food interactions:
*Zantac
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ranitidine
** Has been removed from the market**
class: Histamine-2 receptor Antagonist (H2RAs)
Indications: used PRN for infrequent or mild heart burn, maintenance Tx for GERD after initial 8 weeks of PPI therapy, if there are no esophageal erosions and the patient can remain symptom free.
MOA: drug reversibly inhibits Histamine-2 receptors on gastric parietal cells, which decreases gastric acid secretion.
Dosage forms: tablet, injection, chewable tablet, suspension
Dosing:
OTC- 75-150mg 1-2 times daily PRN
RX- 150mg BID
Max dose:
Contraindications:
Warnings:
*Confusion, usually reversible [risk factors: elderly, severely ill, renal impairment]
Side Effects:
headache, agitation/vomiting in children < 1 year
Monitoring:
Pearls/Notes:
- * also Used for Ulcer healing or hypersecretory conditions (Zollinger-Ellison syndrome), higher doses are needed
Onset of relief: 60 minutes
Duration: 4-10 hours
may be used in pregnancy when clinically indicated
Avoid Cimetidine due to Drug Interactions AND Side Effects
Drug-Drug/Food interactions:
Ma-al-ox
Magnesium- Aluminum- hydroxide
When would we use H2RAs with a PPI?
Side effects associated from chronic use of proton pump inhibitors include:
- C. difficile associated diarrhea (increased risk of GI infections)
- Increased risk of fractures (osteoporosis related fractures)
- Hypomagnesemia
If Histamine-2 receptor antagonists (H2RAs) are used for ____________ or ____________, then higher doses are needed
ulcer healing
hypersecretory conditions (ex. Zollinger-Ellison syndrome)
Which proton pump inhibitors are available prescription only?
dexlansoprazole (Dexilant), pantoprazole (Protonix), rabeprazole (Aciphex)
Which proton pump inhibitors are available IV?
esomeprazole AND pantoprazole
Risks associated with Proton Pump Inhibitor (Acid-Suppression Therapy) Therapy:
- Long term use of PPIs causes chronic changes in gastric pH. This can promote growth of microorganisms and increase the risk of GI infections, including C. difficile and possibly pneumonia (due to reflux of gastric contents beyond the oral cavity).
- PPIs also increase the risk of osteoporosis and fractures. The Beers Criteria recommend that PPIs not be used beyond 8 weeks in elderly patients unless there is a clear indication (ex. high risk for GI bleed due to chronic NSAID use, demonstrated need for maintenance).
Risks associated with Acid-Suppression Therapy) Therapy:
- C. difficile and possibly pneumonia
- decreased magnesium absorption
- decreased calcium carbonate absorption, osteoporosis and fractures
The Beers Criteria recommend that PPIs not be used beyond 8 weeks in elderly patients unless there is a clear indication (ex. high risk for GI bleed due to chronic NSAID use, demonstrated need for maintenance). - H2RAs can cause adverse CNS effects, risk delirium in elderly
Patients should not be on both __________ and __________ chronically, to people that do not need them.
PPIs and H2RAs
Nexium
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
esomeprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: tablet, capsule, IV solution for injection, packet for oral suspension
Dosing:
*OTC- 20mg daily
*RX- 20-40mg daily
Timing: *At least 60 minutes before breakfast
Contraindications:
Warnings:
-*C. difficile- associated diarrhea (CDAD), *hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years).
- Osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
*PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk. *
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea.
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* All PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
Do NOT crush, cut or chew tablets or capsules (exceptions: dexlansoprazole, esomeprazole, lansoprazole, omeprazole, and rabeprazole capsules CAN BE OPENED (NOT CRUSHED), mixed in applesauce and swallowed immediately without chewing
Drug-Drug/Food interactions:
Vimovo
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
esomeprazole + naproxen
class:
Indications:
- For patients that need to be on an NSAID but are at high risk of GI bleeding.
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Prevacid
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
lansoprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: capsule, ODT, suspension
Dosing:
OTC (capsule, ODT)- 15mg daily
RX (suspension)- 15-30mg daily
Timing: * 30-60 minutes Before breakfast
Max dose:
Contraindications:
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea
Monitoring:
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
Do NOT crush, cut or chew tablets or capsules (exceptions: dexlansoprazole, esomeprazole, lansoprazole, omeprazole, and rabeprazole capsules CAN BE OPENED (NOT CRUSHED), mixed in applesauce and swallowed immediately without chewing
Drug-Drug/Food interactions:
First-Lansoprazole
Prilosec
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
omeprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: capsule, tablet, packet for oral suspension
Dosing:
OTC (capsule, tablet)- 20mg daily
RX (packet for oral suspension)- 20-40mg daily
Timing: * 30-60 minutes before breakfast
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
Do NOT crush, cut or chew tablets or capsules (exceptions: dexlansoprazole, esomeprazole, lansoprazole, omeprazole, and rabeprazole capsules CAN BE OPENED (NOT CRUSHED), mixed in applesauce and swallowed immediately without chewing
Drug-Drug/Food interactions:
Dexilant
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
dexlansoprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: capsule
Dosing:
*RX- 30-60mg daily
Timing: Without regard to meals
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
Do NOT crush, cut or chew tablets or capsules (exceptions: dexlansoprazole, esomeprazole, lansoprazole, omeprazole, and rabeprazole capsules CAN BE OPENED (NOT CRUSHED), mixed in applesauce and swallowed immediately without chewing
Drug-Drug/Food interactions:
Protonix
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
pantoprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: tablet, solution for IV injection, packet for oral suspension
Dosing:
*Rx- 40mg daily
Timing:
tablet- without regard to meals
suspension- 30 minutes before a meal
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea.
IV pantoprazole- cases of thrombophlebitis, severe skin reactions (SJS/TEN)
Monitoring:
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
**Do NOT crush, cut or chew tablets or capsules
Drug-Drug/Food interactions:
Zegerid
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
omeprazole + sodium bicarbonate
class: Proton Pump Inhibitor +
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: capsule, packet for oral suspension
Dosing:
OTC-
RX-
Timing: *At least 60 minutes before breakfast
Max dose:
Contraindications:
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
-* Zegerid 20mg and 40mg have the same Na bicarbonate content (1100mg); DO NOT substitute two 20mg capsules/packets for one 40mg capsule/packet because the patient will receive twice the amount of Na; Caution in patients on Na-restricted diet (heart failure, cirrhosis)
Drug-Drug/Food interactions:
Yosprala
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
omeprazole + aspirin
Aciphex
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
rabeprazole
class: Proton Pump Inhibitor
Indications: GERD prevention and maintenance treatment,
MOA: drug irreversibly binds to the gastric H+/K+-ATPase pump “the proton pump” in parietal cells. This shuts down the pump and blocks gastric acid secretion.
Dosage forms: tablet, capsule sprinkle (Aciphex sprinkle)
Dosing:
*Rx- 20mg daily
Timing:
tablet- without regard to meals
capsule sprinkles- 30 minutes before meals
Warnings:
C. difficile- associated diarrhea (CDAD), hypomagnesemia, vitamin B12 deficiency with prolonged use (> or = to 2 years), osteoporosis-related bone fractures with high doses or long-term use (> or = to 1 year).
PPIs may diminish the therapeutic effect of clopidogrel, DO NOT USE omeprazole or esomeprazole while taking clopidogrel; rabeprazole or pantoprazole have less risk.
Side Effects:
Generally, well tolerated. Can cause headache, abdominal pain, nausea, diarrhea
Pearls/Notes:
-* PPIs are the Most Effective medications for GERD
-* an 8-week course of treatment is recommended for relief of symptoms and to heal erosions that may be present.
* all PPIs have similar efficacy
-* if used long term as maintenance treatment, the lowest effective dose should be assessed regularly
Onset: 1-3 hours
Duration: > 24 hours for most PPIs
May be used in pregnancy when clinically indicated
Do NOT crush, cut or chew tablets or capsules (exceptions: dexlansoprazole, esomeprazole, lansoprazole, omeprazole, and rabeprazole capsules CAN BE OPENED (NOT CRUSHED), mixed in applesauce and swallowed immediately without chewing
Drug-Drug/Food interactions:
When to refer patient Out:
- no response to lifestyle modifications
- symptoms remain after 2 weeks of self treatment with OTC products
- **Alarm Symptoms:
– odynophagia (painful swallowing)
– dysphagia (difficulty swallowing)
– frequent nausea and vomiting
– hematemesis (blood in vomit)
– Black bloody stools
– unintentional weight loss
Other Agents historically used for GERD treatment include:
cytoprotective drugs: misoprostol (Cytotec) & sucralfate (Carafate)
prokinetic drugs: metoclopramide (Reglan)
However: Currently there is no role for these medications in the management of GERD and they are NOT recommended by guidelines.
misoprostol (Cytotec) and sucralfate (Carafate) can be used for ____________
Peptic Ulcer Disease
metoclopramide (Reglan) and _______________ are most commonly used when patients have coexisting ____________
erythromycin (Ery-Tab)
gastroparesis (delayed gastric emptying)
Metoclopramide is a __________1_______. At higher doses, it blocks _____2____ receptors in the chemoreceptor “trigger” zone of the CNS which helps with nausea and vomiting.
Metoclopramide enhances the response to ______3____ in the upper GI tract, causing increased motility, accelerated gastric emptying (peristaltic speed) and increases (LES) lower esophageal sphincter tone.
1) dopamine antagonist
2) serotonin
3) acetylcholine
Reglan/Gimoti
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
metoclopramide
class: antiemetic, dopamine antagonist, prokinetic, 5-HT4 receptor agonist
Indications: gastroparesis
MOA:
Dosage forms: tablet, ODT, oral solution, injection, nasal solution
Dosing:
10-15mg QID 30minutes before meals* and at bedtime*.
Has a short duration of action.
*Food must be present in the gut.
Not recommended for use > 12 weeks
If CrCl < 60mL/min: decrease dose by 50% (to avoid side effects, including CNS/EPS side effects).
Boxed Warning:
* Can cause tardive dyskinesias (a serious movement disorder, often irreversible); there is increased risk with high doses, long term treatment (> 12 weeks) and in elderly patients.
Contraindications:
- GI obstruction, perforation or hemorrhage, history of seizures, pheochromocytoma, use in combination with other drugs likely to cause EPS
Warnings:
**- EPS (including acute dystonia), parkinsonian-like symptoms, rare NMS, depression, suicidal ideation
*- Avoid use in patients with Parkinson disease
Side Effects:
*- drowsiness, restlessness, fatigue, hypertension, diarrhea
Pearls/Notes:
-* Do NOT Use in patients receiving medications for Parkinson Disease (antagonistic effect).
Drug-Drug/Food interactions:
- Do NOT Use in combination with antipsychotic drugs, droperidol and promethazine due to increased risk of adverse effects.
- When used in combination with SSRIs, SNRIs, or TCAs, monitor for possible EPS, NMS and serotonin syndrome.
Some Drugs Require an ACIDIC gut for absorption, including enteric coated or delayed release products that can dissolve and release drug prematurely if the gastric pH is increased.
Drugs that have decreased absorption when given concurrently with antacids, H2RAs and PPIs.
Drugs that require an ACIDIC gut
(so, absorption is decreased from antacids, H2RAs, and PPIs)
- Antiretrovirals: delavirdine (NNRTI), rilpivirine (NNRTI), atazanavir (PI)
- Antivirals: ledipasvir, velpatasvir/sofosbuvir
- Azole Antifungals: Sporanox (itraconazole capsules), ketoconazole, posaconazole oral suspension
- Cephalosporins (oral): cefpodoxime, cefuroxime
- Iron products
- Mesalamine oral
- Risedronate delayed release
- Tyrosine Kinase inhibitors: dasatanib, erlotinib, pazopanib
** absorption decreased by H2RAs and PPIs only
Oral drugs/drug classes that Antacids bind:
Due to the short duration of action of Antacids, this type of interaction can often be alleviated by separating administration**
The timing of separation varies for most products, avoid antacids 2-4 hours before or 2-6 hours after is recommended**
- Antiretrovirals (INSTIs*): bictegravir, dolutegravir, elvitegravir, raltegravir
- Bisphosphonates
- Isoniazid
- Levothyroxine
- Mycophenolate
- Quinolones
- Sotalol
- Steroids (especially budesonide)
- Tetracyclines
- Thyroid products
Peptic Ulcer Disease (PUD):
occurs when there is mucosal erosion within the gastrointestinal tract.
Unlike gastritis, the ulcers in PUD extend deeper into the mucosa.
Most ulcers occur in the duodenum, but a small percentage occur in the stomach. Ulcers can be observed with an upper gastrointestinal endoscopy.
The 3 most common causes of Peptic Ulcer Disease (PUD):
1
2
3
- Helicobacter pylori (H. pylori) - positive ulcer—- responsible for majority of peptic ulcers (70-95%)
- NSAID induced ulcer
- Stress ulcers which occur in critically ill and mechanically ventilated patients
The primary symptom of PUD is __________
dyspepsia “indigestion”, a gastric pain that can feel like a gnawing or burning sensation in the middle or upper stomach.
Under Normal Conditions, a physiologic balance exists between GASTRIC ACID SECRETION and the GUT’s MUCOSAL DEFENSE AND REPAIR MECHANISMS, which include:
- mucus and bicarbonate secretion
- mucosal blood flow
- prostaglandin synthesis
- cellular regeneration
- epithelial cell renewal
” these mechanisms protect the GI mucosa from damage caused by NSAIDs (including aspirin), H. pylori, acid, pepsin and other GI irritants”
If the ulcer is duodenal, usually caused by ___________.
Pain is typically worse _________________.
Eating food or ___________ lessens the pain. This is because when eating, __________ is released into the duodenum and this neutralizes incoming acidic contents
H. pylori
2-3 hours AFTER EATING (when the stomach is empty)
taking antacids
bicarbonate
If it is a gastric ulcer, usually caused by ____1_______.
_______2___ generally worsens the pain. This is because ______3___ cause an increase in _____4______ and pepsin, but also cause a decrease in _____5_______
Other symptoms include:
1) NSAIDs primarily
2) eating
3) NSAIDS
4) HCl
5) mucus secretion
- heartburn
- belching
- bloating
- cramping
- nausea
H. Pylori Detection AND management
Diagnostic Tests:
1)
2)
_________, _______, and __________ should be discontinued two weeks prior to these tests to avoid false negative results
1) Urea breath test (UBT)- which detects gas produced by the bacteria.
2) Fecal antigen test- which detects H. pylori in the stool.
- PPIs
- bismuth
- antibiotics
H. pylori infection if left untreated can lead to gastric cancer. There are several combination regimens available to treat H. pylori. Due to failure rates with triple therapy (often caused by clarithromycin resistance), the American College of Gastroenterology (ACG) guideline recommend ____________ first line.
The use of triple therapy first line is only recommended if __________________________ AND __________________.
Do NOT make _______________ in H. pylori eradication regimens.
quadruple therapy
clarithromycin resistance rates are low (<15%) AND the patient has no previous history of taking a macrolide antibiotic (for any reason)
drug substitutions
(ex. H2RAs should NOT be substituted for a PPI, unless the patient cannot tolerate a PPI). Other antibiotics within a class should NOT be substituted (for example, do NOT use ampicillin instead of amoxicillin).
Bismuth Quadruple Therapy for H. Pylori includes:
1
2
3
4
duration is for __________
**Use FIRST-line especially if local resistance rates to clarithromycin are high > or = 15%, the patient has had a previous macrolide exposure or penicillin allergy, or triple therapy failed (if used first).
1) Bismuth subsalicylate 300mg 4 times a day
+
2) *Metronidazole 250-500mg 4 times a day
+
3) Tetracycline 500mg 4 times a day
+
4) Proton Pump Inhibitor 2 times a day
Duration 10-14 days
**Tinidazole may be substituted for metronidazole
Triple Therapy for H. pylori includes:
1
2
3
Use this regimen ONLY if resistance rates to clarithromycin are low < 15% AND the patient has had no previous exposure to a macrolide; this is preferred over clarithromycin triple therapy.
Duration:
“triple therapy” represents
1) Amoxicillin 1000mg BID
+
2) Clarithromycin 500mg BID
+
3) Metronidazole 250-500mg QID
+
4) Proton Pump Inhibitor BID
Duration is for 10-14 days
3 antibiotics + 1 PPI
- Tinidazole may be substituted for metronidazole
Pylera
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
bismuth subcitrate potassium 420mg
metronidazole 375mg
tetracycline 375mg
Take 3 capsules 4 times a day along with a PPI BID for the treatment of H. pylori
Non-Steroidal Anti-Inflammatory Drug Induced Ulcers:
NSAIDs including aspirin, can cause gastric mucosal damage by two mechanisms:
1
2
1) direct irritation of the gastric epithelium
AND
2) systemic inhibition of prostaglandin synthesis (by inhibiting COX-1)
The chronic use of NSAIDs increases the risk for ___________.
Patients are at high risk if they have risk factors including:
gastric ulcers
- Age > 60 years old
- History of PUD (including H. pylori induced)
- High dose NSAIDs
- Using > 1 NSAID (ibuprofen plus aspirin)
- Concomitant use of anticoagulant, steroids, SSRIs or SNRIs
All NSAIDs elevate the blood pressure and decrease renal blood flow; they should be used with caution in any person with __________________
cardiovascular or renal disease
When selecting an NSAID, it is important to weigh these risks with the risks for GI ulcers and bleeding. NSAIDs with selective inhibition of COX-2 (e.g. celecoxib) have decreased ______________ but increased ______________ compared to non-selective NSAIDs.
GI risk
cardiovascular risk
Patients with high GI risk (or history of ulcers) who take non-selective NSAIDs can use _________________
PPI to prevent or decrease the risk of ulcers and bleeding. BUT long term risks need to be considered.
NSAIDs that approach the selectivity of celecoxib are ______________, _________
meloxicam (Mobic/Anjeso)
nabumetone (Relafen)
diclofenac (Cambia/Lofena)
etodolac (Lodine)
Combination products specifically marketed to reduce the risk of NSAID-induced ulcers include:
- Vimovo (naproxen/esomeprazole)
- Duexis (ibuprofen/famotidine)
- Arthrotec (diclofenac/misoprostol)
- these are indicated to relieve symptoms of osteoarthritis and rheumatoid arthritis in patients at risk of GI ulcers*
- Yosprala (aspirin/omeprazole): is approved for secondary prevention of cardiovascular and cerebrovascular events in patients at risk for aspirin associated ulcers.
If an ulcer develops, it should be treated with a ____________ for _____________ AND the ___________ should be discontinued. IF patient can not tolerate then _________
PPI
8 weeks
NSAID
H2RA or sucralfate are other options.
Cytotec
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
misoprostol
class: cytoprotective agent/ prostaglandin E1 analog that replaces the gastro-protective prostaglandins removed by NSAIDs
Indications: prevention of PUD, abortifacient
MOA:
Dosage forms:
Dosing:
200mcg PO QID with food; if not tolerated may decrease dose to 100mcg QID take with meals and at bedtime.
*Boxed Warning: an abortifacient, DO NOT USE to decrease NSAIS induced ulcers in females of childbearing potential unless capable of complying with effective contraceptive measures; warn patients not to give this drug to others.
Contraindications:
Warnings:
Side Effects:
* Diarrhea, abdominal pain*
Monitoring:
Pearls/Notes:
- An option for ulcer treatment in patients who cannot tolerate or use PPI or H2RA.
- Use of psyllium (Metamucil) can help decrease diarrhea.
Drug-Drug/Food interactions:
Carafate
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
sucralfate
class: cytoprotective agent/ sucrose-sulfate-aluminum complex and can interact with albumin and fibrinogen to form a physical barrier over an open ulcer. This protects the ulcer from further insult by HCl acid, pepsin and bile, and allows it to heal.
Indications: treatment of PUD NSAID induced ulcer
MOA:
Dosage forms:
Dosing:
*1 gram PO QID BEFORE MEALS (on an empty stomach) and at bedtime
Max dose:
Contraindications:
Warnings:
*Caution in renal impairment; sucralfate is in an aluminum complex and can accumulate
Side Effects:
*constipation- due to Al
Monitoring:
Pearls/Notes:
- An option for ulcer treatment in patients who cannot tolerate or use PPI or H2RA.
- Drink adequate fluids and use laxatives PRN for constipation
- *Difficult to use due to binding interactions (separate from antacids by 30 minutes and take other drugs 2 hours before or 4 hours after
Drug-Drug/Food interactions:
H2RAs need to be renally dose adjusted:
famotidine
ranitidine
nizatidine
cimetidine
other drugs that need renally dose adjustment:
metoclopramide
famotidine <60
ranitidine <50
nizatidine <50
cimetidine <30
metoclopramide < 60mL/min
