Name of the Non-specific Antidiarrheal Drugs- Antisecretory
- Sulfasalazine
- Mesalazine
- Olsalazine
- Balsalazide
- Bismuth subsalicylate
- Octreotide,
1.Sulfasalazine
| Sulfasalazine |
| Availability Tablets: 500 mg Tablets (Azulfidine EN-tabs—delayedrelease, enteric-coated): 500 mg |
| Indications and dosages ➣ Ulcerative colitis Adults: Initially, 1 to 2 g P.O. daily in equally divided doses q 6 to 8 hours, then 3 to 4 g P.O. daily in equally divided doses q 6 to 8 hours. For maintenance, 500 mg q 6 hours. Children ages 6 and older: 40 to 60 mg/kg P.O. daily in three to six divided doses. For maintenance, 30 mg/kg P.O. q 6 hours in four divided doses. ➣ Acute rheumatoid arthritis Adults: Initially, 500 mg to 1 g (delayedrelease) P.O. daily for 1 week; then increase by 500 mg/day P.O. q week up to 2 g/day in two divided doses. If no benefit after 12 weeks, increase to 3 g/day given in two divided doses. ➣ Polyarticular-course juvenile rheumatoid arthritis Children ages 6 and older: 30 to 50 mg/kg P.O. daily in two evenly divided doses. Maximum dosage is 2 g daily. |
Mechanism of Action
Unknown. Thought to inhibit prostaglandin synthesis by interfering with secretions in colon and causing local anti-inflammatory action.
Pharmacokinetics
- Bioavailability: <15% of parent drug; 60% (sulfapyridine); 10-30% (5-ASA)
- Peak plasma time: 6 hr; 10 hr (sulfapyridine and 5-ASA)
- Protein bound: >99% to albumin; 70% (sulfapyridine)
- Half-life: 10.4-14.8 hr (sulfapyridine)
- Renal clearance: 37%
- Excretion: Urine (systematically absorbed sulfapyridine and 5-ASA); feces (majority of 5-ASA)
Administration
- Give after meals and space doses evenly to reduce GI effects.
- Give with a full glass of water.
- Administer delayed-release tablets whole. Don’t let patient crush or chew them.
Adverse reactions
- CNS: headache, depression, hallucinations, insomnia, drowsiness, vertigo, fatigue, apathy, anxiety, ataxia, polyneuritis, peripheral neuropathy, seizures
- CV: allergic myocarditis or pericarditis
- EENT: periorbital edema, optic neuritis, transient myopia, tinnitus
- GI: nausea, vomiting, abdominal pain, stomatitis, glossitis, pancreatitis, dry mouth, anorexia, pseudomembranous colitis
- GU: hematuria, proteinuria, orangeyellow urine, reversible oligospermia, crystalluria, toxic nephrosis with oliguria and anuria, renal failure
- Hematologic: megaloblastic anemia, agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia, hemolytic anemia
- Hepatic: jaundice, hepatitis, hepatocellular necrosis
- Respiratory: shortness of breath, pleuritis, cyanosis, allergic pneumonitis, pulmonary infiltrates, fibrosing alveolitis
- Skin: generalized skin eruption, urticaria, pruritus, alopecia, local irritation, orange-yellow skin discoloration, exfoliative dermatitis, photosensitivity reaction, erythema multiforme, epidermal necrolysis, Stevens-Johnson syndrome
- Other: reversible immunoglobulin suppression, chills, drug fever, hypersensitivity reactions including anaphylaxis, serum sickness, lupuslike syndrome
Contraindications
- Hypersensitivity to drug, its metabolites, other sulfonamides, or salicylates
- Porphyria
- Urinary tract or intestinal obstruction
Precautions :
- Renal or hepatic disease, bronchial asthma, G6PD deficiency, group A beta-hemolytic streptococcal infections, blood dyscrasias
- History of multiple allergies
- Pregnant or breastfeeding patients
- Children younger than age 2.
Patient monitoring
- Monitor CBC with white cell differential. Watch for evidence of blood dyscrasias.
- Stay alert for signs of erythema multiforme. Report early signs before condition can progress to StevensJohnson syndrome.
- Monitor patient for signs and symptoms of superinfection, including fever, tachycardia, and chills.
- Monitor liver function tests; watch for signs and symptoms of hepatitis.
- Check kidney function tests weekly. Evaluate patient’s fluid intake, urine output, and urine pH. Report hematuria, oliguria, or anuria right away.
- Monitor neurologic status. Report seizures, hallucinations, or depression.
- If patient takes drug for rheumatoid arthritis, monitor therapeutic response 4 to 12 weeks after therapy begins
Patient teaching
- Tell patient to take on regular schedule as prescribed, along with a full glass of water. Instruct him to drink plenty of fluids to minimize crystal formation in urine.
- Urge patient to complete full course of treatment, even if he feels better after a few days.
- Instruct patient to watch for and immediately report signs and symptoms of hypersensitivity reaction, especially rash.
- Tell patient drug can cause blood disorders, GI and liver problems, serious skin reactions, and other infections. Describe key warning signs and symptoms (easy bruising or bleeding, severe diarrhea, unusual tiredness, yellowing of skin or eyes, sore throat, rash, cough, mouth sores, fever). Instruct him to report these right away.
- Advise patient to promptly report scant or bloody urine or inability to urinate.
- Instruct patient to contact prescriber if he develops depression.
- Teach patient effective ways to counteract photosensitivity effect. Tell him that dong quai and St. John’s wort increase phototoxicity risk and should be avoided during therapy.
- Inform patient that drug may discolor skin and body fluids orangeyellow and may permanently stain contact lenses.
- Advise female patient to inform prescriber if she is pregnant. Caution her not to take drug near term or when breastfeeding.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.
2.Mesalazine
| Mesalazine |
| Availability Capsules (extended-release): 250 mg, 500 mg, 0.375 g (Apriso) Rectal suspension: 4 g/60 ml Suppositories: 1,000 mg Tablets (delayed-release): 400 mg (Pentasa), 800 mg (Asacol HD), 1.2 g (Lialda) |
| Indications and dosages ➣ Active ulcerative colitis Adults: 800 mg P.O. (Asacol delayedrelease tablets) t.i.d. for 6 weeks ➣ To induce remission in mildly to moderately active ulcerative colitis Adults: 1 g P.O. (Pentasa extendedrelease capsules) q.i.d. for a total dosage of 4 g daily for up to 8 weeks. Or, two to four 1.2 g (Lialda) extendedrelease tablets P.O. once daily for total daily dose of 2.4 or 4.8 g for up to 8 weeks. ➣ Active distal ulcerative colitis, proctosigmoiditis, or proctitis Adults: 4-g enema (Rowasa 60 ml) P.R. daily at bedtime, retained for 8 hours. Continue for 3 to 6 weeks. ➣ Active ulcerative proctitis Adults: 500 mg (Canasa suppository) P.R. b.i.d., increased to t.i.d. if response inadequate after 2 weeks. Or 1,000 mg (suppository) P.R. at bedtime, continued for 3 to 6 weeks. ➣ To maintain remission of ulcerative colitis Adults: 1.6 g (Asacol) P.O. daily in divided doses. Or, 1.5 g (Apriso) P.O. daily in the morning. |
Mechanism of Action:
Unknown. Thought to act in colon, where it blocks cyclooxygenase and inhibits prostaglandin synthesis.
Pharmacokinetics
- Bioavailability: Immediate-release is extensively and rapidly absorbed; extended-release 20-30% absorbed
- Protein bound: 43% (5-ASA); 78% (N-acetyl-5-ASA)
- Metabolism: Rapidly acetylated in colon wall and liver, independent of pt acetylator status, into N-acetyl-5-aminosalicylic acid
- Half-life: 0.5-10 hr (5-ASA); 2-15 hr (N-acetyl-5-ASA )
- Excretion: Feces 72%; urine: 19-30%
Administration
- Give Apriso capsules with or without food. Don’t give concurrently with antacids.
- Give Lialda tablets with meal.
- Make sure patient swallows tablets whole without crushing or chewing.
- For best effect, have patient retain suppository for 1 to 3 hours.
Adverse reactions
- CNS: headache, dizziness, malaise, weakness
- CV: chest pain, mesalamine-induced cardiac hypersensitivity reactions (myocarditis and pericarditis)
- EENT: rhinitis, pharyngitis
- GI: nausea, vomiting, diarrhea, eructation, flatulence, anal irritation (with rectal use), pancreatitis
- GU: interstitial nephritis, renal failure
- Musculoskeletal: back pain
- Skin: alopecia, rash
- Other: fever, acute intolerance syndrome, anaphylaxis, acute intolerance syndrome
Contraindications
- Hypersensitivity to drug, its components, or salicylates
Precautions :
- Severe hepatic or renal impairment
- Allergy to sulfasalazine
- Pyloric stenosis (delayed-release tablets)
- Conditions predisposing to development of myocarditis or pericarditis
- Pregnant or breastfeeding patients
- Children younger than age 18 (safety and efficacy not established).
Patient monitoring
- Monitor carefully for mesalamineinduced cardiac hypersensitivity reactions (myocarditis and pericarditis).
- Closely monitor patients with history of allergic reactions to sulfasalazine or sulfite sensitivity (if using enema).
- Assess kidney and liver function before and periodically during therapy.
- Monitor for suppository efficacy, which should appear in 3 to 21 days. However, know that treatment usually continues for 3 to 6 weeks. 2Watch for signs and symptoms of intolerance syndrome, such as cramping, acute abdominal pain, bloody diarrhea, fever, headache, and rash. If these occur, discontinue drug and notify prescriber.
- Watch for signs and symptoms of intolerance syndrome, such as cramping, acute abdominal pain, bloody diarrhea, fever, headache, and rash. If these occur, discontinue drug. Drug may be restarted later only if clearly needed, under close medical supervision and at reduced dosage.
Patient teaching
- Instruct patient to swallow tablets or capsules whole.
- Tell patient to contact prescriber if partially intact tablets repeatedly appear in stools.
- Advise patient using suppository to avoid excessive handling and to retain suppository for 1 to 3 hours or longer for maximum benefit.
- Teach patient about proper enema administration. Tell him to stay in position for at least 30 minutes and, if possible, retain medication overnight.
- Advise patient to immediately report breathing difficulties, allergic symptoms, cramping, acute abdominal pain, bloody diarrhea, fever, headache, or rash.
- As appropriate, review all other significant and life-threatening adverse reactions, especially those related to the drugs mentioned above.
3.Olsalazine
| Olsalazine |
| Availability Capsules: 250 mg |
| Indications and dosages ➣ Ulcerative colitis in patients who can’t tolerate sulfasalazine Adults: 500 mg P.O. b.i.d. |
Mechanism of Action
Converted to 5-aminosalicylic acid (mesalamine) by gastrointestinal flora which is thought to be the therapeutically active component; works topically rather tha systemically
Pharmacokinetics:
- Protein bound: 99%
- Metabolism:>90% converted to 5-ASA in the gut
- Half-Life:0.9 hr
- Excretion
- Urine: 20% (mostly N-Ac-5-ASA)
- Feces: 80% (both 5-ASA & N-Ac-5-ASA)
Administration
Give with meals to reduce GI irritation.
Adverse reactions
- CNS: headache, fatigue, depression, vertigo
- GI: nausea, vomiting, diarrhea, abdominal pain, cramps, dyspepsia, bloating, stomatitis
- Musculoskeletal: joint pain
- Respiratory: upper respiratory infection
- Skin: rash, itching
Contraindications
- Hypersensitivity to drug or other salicylates
Precautions :
- hepatic or renal impairment, severe allergy, bronchial asthma
- pregnant or breastfeeding patients
- children younger than age 14.
Patient monitoring
- Monitor neurologic status. Stay alert for depression.
- Assess GI symptoms. Encourage adequate fluid intake to avoid dehydration.
- Monitor urinalysis, blood urea nitrogen, and creatinine in patients with renal impairment.
Patient teaching
- Instruct patient to take with food and to continue taking drug even after symptoms improve.
- Tell patient to eat appropriate foods in small, frequent servings to minimize GI upset.
- Advise patient to contact prescriber if symptoms worsen or don’t improve after 1 to 2 months of therapy.
- Tell patient he may require periodic proctoscopy and sigmoidoscopy to determine response to drug.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects mood and wakefulness.
- As appropriate, review all significant adverse reactions and interactions, especially those related to the drugs and foods mentioned above
4.Balsalazide
| Balsalazide |
| Availability Capsules: 750 mg |
| Indications and dosages ➣ Mildly to moderately active ulcerative colitis Adults: Usual dosage, three 750-mg capsules P.O. t.i.d. (6.75 g daily) for up to 8 weeks; some patients may require 12 weeks Children ages 5 to 17: Usual dosage, either three 750-mg capsules P.O. t.i.d. (6.75 g daily) for up to 8 weeks, or one 750-mg capsule P.O. t.i.d. (2.25 g daily) for up to 8 weeks |
Mechanism of Action
Metabolized to mesalamine by intestinal flora
Mesalamine (5-aminosalicylic acid) has anti-inflammatory effect; active component of sulfasalazine, specific MOA unknown; probably inhibits prostaglandin & leukotrienes synthesis & release in colon
Pharmacokinetics:
- Bioavailability: Low absorption
- Peak plasma time: 1-2 hr
- Protein bound: 99%
- Half-life: Undetermined due to large intersubjective variability
- Excretion: Feces (as metabolites) >65%; urine (as metabolites) >25%
Administration
- Advise patient to swallow capsules whole, either always with or always without food.
- For those patients who can’t swallow capsules whole, carefully open capsules and sprinkle contents on applesauce and have patient swallow contents immediately without chewing
Adverse reactions
- CNS: headache, insomnia, dizziness, anxiety, confusion, agitation, coma
- EENT: blurred vision, eye irritation, tinnitus, earache, epistaxis, sinusitis, sore throat, nasopharyngitis
- GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia, oral blisters, oral candidiasis, GI hemorrhage
- GU: urinary tract infection
- Musculoskeletal: arthralgia; myalgia; bone, back, neck, or limb pain
- Respiratory: cough, upper respiratory tract infection
- Skin: erythema
- Other: generalized pain
Contraindications
- Hypersensitivity to balsalazide, salicylates, or mesalamine
Precautions :
- Renal impairment
- Pyloric stenosis
- Breastfeeding patients
- Children younger than age 5 (safety and efficacy not established).
Patient monitoring
- Assess character and frequency of stools.
- Monitor CBC and liver and kidney function test results.
Patient teaching
- Instruct patient to take drug only as directed.
- Instruct patient to carefully open capsules and sprinkle contents on applesauce and swallow contents immediately without chewing if patient can’t swallow capsules whole.
- Tell patient that teeth and tongue staining may occur when drug is taken by sprinkling on applesauce.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.
5.Bismuth subsalicylate
| Bismuth subsalicylate |
| Availability Liquid: 130 mg/15 ml, 262 mg/15 ml, 525 mg/15 ml (maximum strength) Tablets: 262 mg Tablets (chewable): 262 mg, 300 mg |
| Indications and dosages ➣ Adjunctive therapy for mild to moderate diarrhea, nausea, abdominal cramping, heartburn, and indigestion accompanying diarrheal illnesses Adults: Two tablets or 30 ml P.O. (15 ml of maximum strength) q 30 minutes, or two tablets or 60 ml (30 ml of extra/maximum strength) q 60 minutes as needed. Don’t exceed 4.2 g in 24 hours. Children ages 9 to 12: One tablet or 15 ml P.O. (7.5 ml of maximum strength) q 30 to 60 minutes. Don’t exceed 2.1 g in 24 hours. Children ages 6 to 9: 10 ml (5 ml of maximum strength) P.O. q 30 to 60 minutes. Don’t exceed 1.4 g in 24 hours. Children ages 3 to 6: 5 ml (2.5 ml of maximum strength) P.O. q 30 to 60 minutes. Don’t exceed 704 mg in 24 hours. ➣ Ulcer disease caused by H. pylori Adults: Two tablets or 30 ml P.O. q.i.d. (15 ml of maximum strength) |
Mechanism of Action
Antimicrobial anti-inflammatory action (bismuth); antisecretory effect (salicylate)
Pharmacokinetics:
- Bioavailability: Bismuth, <1%; salicylate, 80%
- Peak plasma time: Bismuth, 1.8-5 hr
- Protein bound: Bismuth, 90%; salicylate, >90%
- Half-life: Bismuth, 21-72 days; salicylate, 2.5 hr
- Excretion: Bismuth, feces (99%) and urine (0.003%); salicylate, urine (95%)
Administration
- Know that tablets should be chewed or dissolved in mouth before swallowing.
- Be aware that drug is usually given with antibiotics (such as tetracycline or amoxicillin) when prescribed for ulcer disease.
Adverse reactions
- EENT: tinnitus, tongue discoloration
- GI: nausea, vomiting, diarrhea, constipation, gray-black stools, fecal impaction
- Respiratory: tachypnea
- Other: salicylate toxicity
Contraindications
- Hypersensitivity to aspirin
- Elderly patients with fecal impaction
- Children or adolescents during or after recovery from chickenpox or flulike illness
Precautions:
- Diabetes mellitus, gout
- Patients taking concurrent aspirin
- Elderly patients
- Pregnant or breastfeeding patients
- Infants.
Patient monitoring
- Monitor fluid intake and electrolyte levels.
- Monitor stool frequency and appearance.
- Assess infants and debilitated patients for fecal impaction.
Patient teaching
- Instruct patient to chew tablets or dissolve them in mouth before swallowing.
- Inform patient that drug may turn stools gray-black temporarily.
- Tell patient to notify prescriber if he has diarrhea with fever for more than 48 hours.
- As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above
6.Octreotide
| Octreotide |
| Availability Depot injection: 10 mg, 20 mg, 30 mg Injection: 0.05 mg/ml, 0.1 mg/ml, and 0.5 mg/ml in 1-ml ampules; 0.2 mg/ml and 1 mg/ml in 5-ml vials |
| Indications and dosages ➣ Diarrhea and flushing associated with carcinoid tumors Adults: 100 to 600 mcg (Sandostatin) subcutaneously or I.V. daily in two to four divided doses for 2 weeks. Then, depending on response, 20 mg (LAR Depot) I.M. q 4 weeks for 2 months. ➣ Diarrhea caused by vasoactive intestinal peptide tumors (VIPomas) Adults: 200 to 300 mcg (Sandostatin) subcutaneously or I.V. daily in two to four divided doses for 2 weeks. Then, depending on response, 20 mg (LAR Depot) I.M. q 2 weeks for 2 months. ➣ Acromegaly Adults: 50 to 100 mcg (Sandostatin) subcutaneously or I.V. two or three times daily. Then, depending on response, 20 mg (LAR Depot) I.M. q 4 weeks for 3 months. Then adjust based on growth hormone level. |
Mechanism of Action
Somatostatin analog; decreases GH secretion, secretion of gastrin, VIP, glucagon, secretin, serotonin release and pancreatic polypeptide; in acromegaly, octreotide decreases growth hormone and IGF-1 secretion; suppresses LH response to GnRH secretion and decreases splanchnic blood flow
Pharmacokinetics:
- Bioavailability: SC, 100%; IM, 60%
- Peak plasma time: IV, immediately after injection; SC, 15-30 min; PO, 90-120 min; IM, 60 min
- Protein bound: 65% binds to lipoprotein
- Metabolized by liver
- Half-life: 1.7 hr
- Total body clearance: 10 L/hr
- Excretion: Urine (32%)
Administration
- When giving subcutaneously, rotate administration site with each injection.
- Don’t give LAR Depot I.V.
- Mix I.M. solution and inject deep into gluteal muscle over 3 minutes. Don’t use deltoid.
- For I.V. administration, dilute in 50 to 200 ml of dextrose 5% in water or normal saline solution. Infuse over 15 to 30 minutes.
- Know that octreotide suppression test and octreotide scintigraphy may be done to determine if drug will aid carcinoid tumor treatment.
- Drug may be kept at room temperature for 2 weeks. Refrigerate ampules.
Adverse reactions
- CNS: dizziness, drowsiness, fatigue, headache, weakness
- CV: edema, bradycardia, conduction abnormalities, arrhythmias
- EENT: vision disturbances
- GI: nausea, vomiting, diarrhea, abdominal pain, cholelithiasis, fat malabsorption
- Skin: flushing
- Metabolic: hypothyroidism, hyperglycemia, hypoglycemia
- Other: injection site pain
Contraindications
- Hypersensitivity to drug or its components
Precautions:
- Gallbladder disease, renal impairment, hyperglycemia or hypoglycemia, fat malabsorption
- Pregnant or breastfeeding patients
- Children.
Patient monitoring
- Assess bowel sounds and stool frequency and consistency.
- Monitor vital signs and fluid intake and output. Stay alert for dehydration or edema.
- Evaluate diabetic patient for hypoglycemia or hyperglycemia.
- Know that in women with active acromegaly, normalization of growth hormone and insulin-like growth factor-1 may restore fertility
Patient teaching
- Tell patient being treated for carcinoid tumor to keep track of number of daily stools or flushing episodes.
- Instruct patient to weigh himself daily and report significant changes.
- Advise female with childbearing potential to use adequate contraception while taking drug.
- If patient will use drug at home, teach correct methods for injection, storage, and needle disposal
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, and alertness.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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