GI Drugs -Proton pump inhibitors (PPIs)

Proton pump inhibitors (PPIs)

• Omeprazole,
• Pantoprazole
• Rabeprazole
• Dexlansoprazole
• Esomeprazole
• Lansoprazole

1.Omeprazole

Mechanism of Action:

Reduces gastric acid secretion and increases gastric mucus and bicarbonate production, creating protective coating on gastric mucosa and easing discomfort from excess gastric acid

Pharmacokinetics

Bioavailability: 30-40%

Protein bound: 95-96%

Metabolism: Metabolized extensively by hepatic CYP2C19; slow metabolizers are deficient in CYP2C19 enzyme system; plasma concentration can increase by 5-fold or higher in comparison with that found in persons with the enzyme

Half-life: 0.5-1 hr; increases to 3 hr with hepatic impairment

Excretion: Urine (77%); feces (16-19%; mainly in bile)

Monitor magnesium level before starting drug and periodically thereafter in patients expected to be on long-term treatment or who take proton pump inhibitors with other drugs such as digoxin or drugs that may cause hypomagnesemia.

Patient teaching

• Tell patient to take 30 to 60 minutes before a meal, preferably in morning.
• Instruct patient to swallow capsules or tablets whole and not to chew or crush them. If he can’t swallow capsule, tell him he may open it, carefully sprinkle and mix entire contents into 1 tbsp of cool applesauce, and swallow immediately with glass of water.
• Instruct patient on how to use delayed-release oral suspension: Empty contents of a 2.5-mg packet of powder into a container with 5 ml of water or 10-mg packet of powder into a container with 15 ml of water; don’t use other liquids or foods. Stir and allow drug to thicken for 2 to 3 minutes. Stir well and drink within 30 minutes. If any drug remains after drinking, add more water to container, stir, and drink immediately.
•   Inform patient taking OTC delayedrelease tablets for heartburn that full effect may take 1 to 4 days. Advise him not to take tablets for more than 14 days without consulting health care professional.
• Advise patient to avoid St John’s wort while taking this drug.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
•   As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

2.Pantoprazole

Mechanism of Action:

Reduces gastric acid secretion and increases gastric mucus and bicarbonate production, creating protective coating on gastric mucosa

Contraindications

● Hypersensitivity to drug or any substituted benzimidazole

Administration:

• Be aware that oral granules may be mixed with applesauce or apple juice and given 30 minutes before a meal. Once mixed, give drug within 10 minutes.
• Know that oral granules may be mixed with 10 ml apple juice and administered into nasogastric tube using 60-ml catheter-tip syringe. Rinse syringe with additional apple juice so that no granules remain in syringe.
•  For I.V. administration, use in-line filter provided. If Y-site is used, place filter below Y-site closest to patient.
• Dilute I.V. form with 10 ml of normal saline solution; further dilute in dextrose 5% in water, normal saline solution, or lactated Ringer’s solution, as directed. Give over 15 minutes at a rate no faster than 3 mg/minute.
•  Don’t give I.V. form with other I.V. solutions.
• Know that I.V. form is indicated for short-term treatment of GERD in patients with history of erosive esophagitis as alternative to P.O. therapy.
• Be aware that symptomatic response doesn’t rule out gastric cancer.

Pharmacokinetics

Bioavailability: 77% (PO; neither food nor antacid alters bioavailability)

Protein bound: 98%

Metabolism: Metabolized extensively by hepatic P450 enzyme CYP2C19; second pathway through CYP3A4

Half-life: 1 hr; increased to 3.5-10 hr with CYP2C19 deficiency

Peak plasma serum: 2.8 hr (PO); at end of infusion (IV)

Excretion:  Urine (71%); feces (18%)

Precautions:

• severe hepatic disease
• atrophic gastritis with long-term use
• increased risk of osteoporosis-related hip, wrist, or spine fractures with longterm use or multiple daily doses
• concurrent use of atazanavir, nelfinavir, or methotrexate
• pregnant or breastfeeding patients

Adverse reactions

• CNS: dizziness, headache
• CV: chest pain
• EENT: rhinitis
• GI: vomiting, diarrhea, abdominal pain, dyspepsia
• Metabolic: hyperglycemia
• Musculoskeletal: hip, wrist, spine fractures (with long-term daily use)
• Skin: rash, pruritus
• Other: injection site reaction

Patient monitoring

• Assess for symptomatic improvement.
• Monitor blood glucose level in diabetic patient.

Patient teaching

• Tell patient to swallow delaye drelease tablets whole without crushing, chewing, or splitting
• Tell patient he may take tablets with or without food.
• Explain that antacids don’t affect drug absorption.
• Instruct diabetic patients to monitor blood glucose level carefully and stay alert for signs and symptoms of hyperglycemia.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

3.Rabeprazole

Mechanism of Action:

Reduces gastric acid secretion and increases gastric mucus and bicarbonate production, creating a protective coating on gastric mucosa

Pharmacokinetics

Bioavailability: 52%

Protein bound: 95-98%

Metabolism: Liver; extensively by hepatic P450 enzyme CYP2C19

Half-life: 1-2 hr; depending on dose

Peak plasma serum: 2-5 hr(tablet) 1-6.5 hr (capsule)

Excretion:  Urine (90%); feces (10%)

Administration

• Don’t crush or split tablets.

• Give without regard to food.

Adverse reactions

CNS: headache

Metabolic: hypomagnesemia

Musculoskeletal: fractures of hip, wrist, spine (with long-term daily use)

Patient monitoring

• Stay alert for symptomatic response, but know that a positive response doesn’t rule out gastric cancer.
• Monitor magnesium level before starting therapy and periodically thereafter in patients expected to be on prolonged therapy or who take proton pump inhibitors with drugs such as digoxin or drugs that may cause hypomagnesemia (such as diuretics).

 Patient teaching

• Tell patient he may take with or without food. Instruct him not to crush, chew, or split tablets.
• Caution female patient not to breastfeed during therapy.
• As appropriate, review all significant adverse reactions and interactions, especially those related to the drugs mentioned above.

4.Dexlansoprazole

Mechanism of Action:

Suppresses gastric acid secretion by specific inhibition of (H+, K+)-ATPase in the gastric parietal cell.

Administration

Administer with or without food

Contraindications

Hypersensitivity to drug or its components

Metabolism &Elimination:

Peak plasma time: 1-2 hr and 4-5 hr (dual release)

Protein bound: >96%

Metabolism: Hydroxylation mainly by CYP2C19 and oxidation to sulfone by CYP3A4

Half-life: 1-2 hr

Excretion:   Feces (48% as metabolites), urine (51% as metabolites)

Precautions:

• moderate renal impairment
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Adverse reactions

• CNS: asthenia, dizziness, headache, migraine headache, memory impairment, paresthesia, psychomotor hyperactivity, tremor, trigeminal neuralgia, abnormal dreams, anxiety, depression, insomnia,seizures
• CV: angina, bradycardia, chest pain, palpitations, tachycardia, hypertension, deep vein thrombosis, arrhythmias, myocardial infarction
• EENT: eye irritation, eye swelling, ear pain, tinnitus, vertigo, nasopharyngitis, pharyngitis, sinusitis
• GI: nausea; vomiting; diarrhea; abdominal pain, discomfort, tenderness; flatulence; abnormal feces; anal discomfort; Barrett’s esophagus;bezoar; abnormal bowel sounds; breath odor; microscopic colitis; colon and gastric polyps; constipation; dry mouth; duodenitis; dyspepsia; dysphagia; enteritis; eructation; esophagitis; gastritis; gastroenteritis; GI disorders; GI hypermotility disorders; GERD; ulcers and perforation; hematemesis; hematochezia; hemorrhoids; impaired gastric emptying; irritable bowel syndrome; mucus stools; oral mucosa blistering; painful defecation; proctitis; oral paresthesia; oral herpes; rectal hemorrhage
• GU: vulvovaginal infection, libido changes, dysuria, micturition urgency, dysmenorrhea, dyspareunia, menorrhagia, menstrual disorder
• Hematologic: anemia, lymphadenopathy Hepatic: biliary colic, cholelithiasis, hepatomegaly
• Metabolic: goiter
•  Musculoskeletal: arthralgia, arthritis, cramps, musculoskeletal pain, myalgia; hip, wrist, spine fracture (with longterm daily use) Respiratory: upper respiratory tract infection, aspiration, asthma, bronchitis, cough, dyspnea, hyperventilation, respiratory tract congestion, sore throat
• Skin:rash, sunburn, acne, dermatitis, erythema, pruritus, lesions, urticaria
• Other: edema, chills, abnormal feeling, inflammation, mucosal inflammation, nodule, pain, pyrexia, candidal infection, viral infection, influenza, falls, overdose, procedural pain, weight gain, appetite changes, altered taste, hiccups, hot flushes, hypersensitivity

Patient monitoring

• Monitor renal function tests closely.

Patient teaching

• Instruct patient to take drug with or without food.
• Tell patient to swallow capsule whole or open capsule and sprinkle contents on 1 tablespoon of applesauce and swallow immediately.
• Instruct patient to report allergic reactions (such as rash or itching) to prescriber.  As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above

5.Esomeprazole

Mechanism of Action:

Reduces gastric acid production by inhibiting enzyme activity in gastric parietal cells, preventing transport of hydrogen ions into gastric lumen

Administration

• Give 1 hour before or 2 hours after a meal.
•   Know that contents of capsules may be mixed with applesauce.
•   Don’t crush capsules or pellets.
•   Be aware that hypomagnesemia has been reported rarely in patients treated with proton pump inhibitors for at least 3 months. For patients expected to be on prolonged treatment or who take proton pump inhibitors with drugs such as digoxin or drugs that may cause hypomagnesemia (such as diuretics), consider monitoring magnesium level before starting treatment.

Pharmacokinetics

• Bioavailability: PO: 89-90%; food decreases AUC by 33-53%; take 1 hr before meal
• Protein bound:97%
• Metabolism: Liver; extensively metabolized by hepatic P450 enzyme;
• Half-life:1.2-1.5 hr
• Peak plasma time: PO: 1-1.6 hr
• Excretion:  Urine (80%); feces (20%)

Contraindications

 Hypersensitivity to proton pump inhibitors

Precautions:

•  severe hepatic impairment
•  increased risk of hip, wrist, and spine fractures
•  pregnant or breastfeeding patients
•   children younger than age 18 (safety not established).

Adverse reactions

• CNS: headache, dizziness, asthenia, vertigo, apathy, anxiety, paresthesia, insomnia, abnormal dreams
• EENT: sinusitis, epistaxis
• GI: nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, dry mouth
• Metabolic: hypomagnesemia
• Musculoskeletal: hip, wrist, spine fractures (with long-term daily use)
• Respiratory: upper respiratory tract infection, cough
• Skin: rash, inflammation, urticaria, pruritus, alopecia, dry skin

Patient monitoring

• Monitor neurologic status, especially for dizziness, headache, paresthesia, and asthenia.
• Watch for signs and symptoms of EENT and respiratory infections.
• Assess nutritional and hydration status in light of adverse GI effects.
• Check for rash and other signs of hypersensitivity.
• Monitor liver function test results if patient is on long-term therapy.
• Continue to monitor patients periodically who are expected to be on prolonged treatment or who take proton pump inhibitors with drugs such as digoxin or drugs that may cause hypomagnesemia.

Patient teaching

• Instruct patient to take drug 1 hour before or 2 hours after a meal.
• If patient has trouble swallowing capsule, tell him to open it, sprinkle pellets into soft food (such as applesauce), and take right away.
• Instruct patient to recognize and report signs or symptoms of hypomagnesemia.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise female patient to tell prescriber if she’s pregnant or breastfeeding.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

6.Lansoprazole

Mechanism of Action:

Inhibits activity of proton pump in gastric parietal cells, decreasing gastric acid production

Pharmacokinetics

• Bioavailability: 81-91%; decreased 50-70% if given 30 min after meals
• Protein bound: 97-99%
• Metabolism: Metabolized by hepatic CYP2C19; slow metabolizers are deficient in CYP2C19 enzyme and can have plasma concentration increase of 5-fold or higher
• Half-life:0.9-1.5 hr
• Peak plasma time: 1.7 hr; food increases time to 3.7 hr
• Excretion: feces (bile), 67%; urine, 33%

Administration

 Give oral form before meals.

•  If patient has difficulty swallowing delayed-release capsule, open it and sprinkle contents onto small amount of soft food, such as applesauce or pudding. Don’t crush or let patient chew drug.
•  When giving orally disintegrating tablet, place tablet on patient’s tongue and let it disintegrate until particles can be swallowed.
•  Know that orally disintegrating tablet contains phenylalanine.
•  When giving oral suspension, empty packet contents into container with 2 tbsp water. Stir contents well, and have patient drink immediately. Don’t give oral suspension through nasogastric (NG) tube.
•  When injecting contents of delayedrelease capsule through NG tube, open capsule and mix granules with 40 ml apple juice. Then rinse tube with additional apple juice to clear.

Contraindications

 Hypersensitivity to drug or its components

Precautions:

• phenylketonuria (orally disintegrating tablets), severe hepatic impairment
•   elderly patients
• pregnant or breastfeeding patients
• children younger than age 18.

Adverse reactions

• CNS: headache, confusion, anxiety, malaise, paresthesia, abnormal thinking, depression, dizziness, syncope, cerebrovascular accident
• CV: chest pain, hypertension, hypotension, myocardial infarction, shock
• EENT: visual field deficits, otitis media, tinnitus, epistaxis
• GI: nausea, diarrhea, abdominal pain, cholelithiasis, ulcerative colitis, esophageal ulcer, hematemesis, stomatitis, dysphagia, GI hemorrhage
• GU:renal calculi, erectile dysfunction, abnormal menses, breast tenderness, gynecomastia
• Hematologic: anemia
• Musculoskeletal: hip, wrist, spine fractures (with long-term daily use)
• Respiratory: cough, bronchitis, asthma
• Skin: urticaria, alopecia, acne, pruritus, photosensitivity

Patient monitoring

 Monitor for GI adverse reactions.

 Assess nutritional status and fluid balance to identify significant problems.

Patient teaching

• Instruct patient to take before meals.
• If patient has difficulty swallowing, tell him to open delayed-release capsule and sprinkle contents onto small amount of soft food (such as applesauce or pudding). Emphasize that he must not crush or chew drug.
• Tell patient to take orally disintegrating tablet by placing it on tongue and letting it disintegrate.
• Instruct patient to take oral suspension by emptying packet contents into container with 2 tbsp water. Tell him to stir contents well and drink immediately.
• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and herbs mentioned above.

REFERENCES

1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
5. Nursebro.com, Search – Nursebro

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