Name of the Non-Specific Antidiarrheal Drugs- Antimotility
- Codeine
- Diphenoxylate /atropine
- Loperamide
1.Codeine
| Codeine |
| Availability Tablets: 15 mg, 30 mg, 60 mg |
| Indications and dosages ➣ Mild to moderately severe pain Adults: 15 to 60 mg P.O. q 4 hours as needed. Doses above 60 mg may fail to give commensurate pain relief and may be associated with an increased incidence of undesirable adverse effects. |
Mechanism of Action
May produce analgesia through partial metabolism to morphine. Drug binds with mu, delta, and kappa receptors in the spinal cord and with mu1 and kappa3 receptors higher in the CNS, decreasing intracellular cAMP, which inhibits adenylate cyclase activity and prevents release of pain neurotransmitters, such as substance P and dopamine, and altering perception of and emotional response to pain. Drug also suppresses cough by acting on opiate receptors in the cough center.
Pharmacokinetics:
- Onset: 30-60 min (PO); 10-30 min (IM)
- Peak plasma time: 0.5-1 hr
- Protein bound: 25%
- Half-life: 3-4 hr
- Excretion: Urine, feces
Administration
- If GI upset occurs, give with food.
- Titrate dosage for appropriate analgesic effect.
- If overdose occurs, give naloxone I.V. as prescribed. Repeat administration as needed (up to manufacturer’s recommended maximum dosage) to reverse toxic effects.
Adverse reactions
- CNS: confusion, sedation, malaise, agitation, euphoria, floating feeling, headache, hallucinations, unusual dreams, apathy, mood changes
- CV: hypotension, bradycardia, peripheral vasodilation, reduced peripheral resistance
- EENT: blurred or double vision, miosis, reddened sclera
- GI: nausea, vomiting, constipation, decreased gastric motility
- GU: urinary retention, urinary tract spasms, urinary urgency
- Respiratory: suppressed cough reflex, respiratory depression
- Skin: flushing, sweating
- Other: physical or psychological drug dependence, drug tolerance
Contraindications
- Hypersensitivity to drug, its components, or other opioids
- Respiratory depression, severe bronchial asthma, hypercarbia
- Paralytic ileus or suspected paralytic ileus
Precautions:
- Severe renal, hepatic, or pulmonary disease
- Adrenal insufficiency, circulatory shock, hypotension, pancreatic or biliary tract disease, urethral stricture, seizures, head trauma, hypothyroidism, increased intracranial pressure, prostatic hypertrophy, undiagnosed abdominal pain, alcoholism
- Concomitant use of alcohol, other opioids, illicit drugs
- Elderly or debilitated patients
- Pregnant or breastfeeding patients
- Labor and delivery patients
- Children younger than age 18 (safety and efficacy not established).
Patient monitoring
- Monitor vital signs and CNS status.
- Assess pain level and efficacy of pain relief.
- Evaluate patient for adverse reactions.
- Stay alert for overdose signs and symptoms, such as CNS and respiratory depression, GI cramping, and constipation.
- Assess other drugs in patient’s drug regimen for those that could cause additive or adverse interactions.
- Monitor patient for signs and symptoms of drug dependence or tolerance.
Patient teaching
- Teach patient to minimize adverse GI effects by taking doses with food or milk.
- Tell patient to notify prescriber promptly if he experiences shortness of breath or difficulty breathing or if nausea, vomiting, or constipation become pronounced.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, alertness, vision, coordination, and physical dexterity.
- Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure decrease.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.
Nursing Considerations
- Evaluate patient for therapeutic response, including decreased pain, cough, and facial grimacing.
- Take safety precautions, if needed.
- Monitor respiratory depth, effort, and rate. Notify prescriber immediately if respiratory rate drops below 10 breaths/min.
- Assess urine output to detect retention
- Rotate sites for subcutaneous delivery. Repeated injection in same site may cause tissue irritation, pain, and induration
2.Diphenoxylate atropine
| Diphenoxylate atropine |
| Availability Liquid: 2.5 mg diphenoxylate and 0.025 mg atropine/5 ml Tablets: 2.5 mg diphenoxylate and 0.025 mg atropine |
| Indications and dosages ➣ Diarrhea Adults: Initially, 5 mg P.O. three to four times daily, then 5 mg/day as needed (not to exceed 20 mg/day). Decrease dosage when desired response occurs. Children: Initially, 0.3 to 0.4 mg/kg P.O. (liquid only) daily in four divided doses. Decrease dosage when desired response occurs. |
Mechanism of Action
Diphenoxylate: Acts on smooth muscle of intestinal tract, inhibiting GI motility and excessive GI propulsion (like morphine)
Atropine: Subtherapeutic quantity of atropine is added to discourage deliberate overdose of diphenoxylate
Pharmacokinetics:
- Onset: 45 min-1 hr
- Peak plasma time: 2 hr
- Bioavailability: 90%
- Metabolism: Extensively metabolized in liver to active metabolite, diphenoxylic acid (difenoxin), which is 5 times more potent than diphenoxylate
- Half-life: 2.5 hr (diphenoxylate); 3-14 hr (diphenoxylic acid)
- Renal clearance: 1483 mL/min
- Excretion: Feces via bile (49%), urine (14%)
Administration
- Don’t confuse brand name Lomotil with Lamictal (an anticonvulsant). Serious errors have been reported.
- Withhold drug if patient has severe fluid or electrolyte imbalance.
- Administer with food if GI upset occurs.
- Don’t give within 14 days of MAO inhibitors.
Adverse reactions
- CNS: dizziness, confusion, drowsiness, headache, insomnia, nervousness
- CV: tachycardia
- EENT: blurred vision, dry eyes
- GI: nausea, vomiting, constipation, epigastric distress, ileus, dry mouth
- GU: urinary retention
- Skin: flushing
Contraindications
- Hypersensitivity to drug
- Obstructive jaundice
- Diarrhea associated with pseudomembranous colitis or enterotoxinproducing bacteria
- Angle-closure glaucoma
- Concurrent MAO inhibitor use
- Children younger than age 2
Precautions:
- Inflammatory bowel disease; prostatic hypertrophy; severe hepatic disease (use with extreme caution)
- Concurrent use of drugs that cause physical dependence, history of physical drug dependence
- Elderly patients
- Pregnant or breastfeeding patients
- Children (safety not established in children younger than age 12).
Patient monitoring
- Assess for and report abdominal distention and signs or symptoms of decreased peristalsis.
- Watch for signs and symptoms of dehydration.
- Assess frequency and consistency of bowel movements.
Patient teaching
- Instruct patient to report persistent diarrhea.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
- Tell patient that prolonged use may lead to dependence.
- As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above
3.Loperamide
| Loperamide |
| Availability Capsules: 2 mg Solution: 1 mg/5 ml Tablets: 2 mg Tablets (chewable): 2 mg |
| Indications and dosages ➣ Acute diarrhea Adults: Initially, 4 mg P.O., then 2 mg after each loose stool. Usual maintenance dosage is 4 to 8 mg P.O. daily in divided doses, not to exceed 16 mg daily. Children ages 8 to 12 or weighing more than 30 kg (66 lb): Initially, 2 mg P.O. t.i.d., then 1 mg/10 kg after each loose stool, not to exceed 6 mg daily Children ages 6 to 8 or weighing 20 to 30 kg (44 to 66 lb): Initially, 2 mg P.Ob.i.d., then 1 mg/10 kg after each loose stool, not to exceed 4 mg daily Children ages 2 to 5 or weighing 13 to 20 kg (29 to 44 lb): Initially, 1 mg P.O. t.i.d., then 1 mg/10 kg after each loose stool, not to exceed 3 mg daily ➣ Acute diarrhea (treated with overthe-counter loperamide) Adults and children ages 12 and older: Two caplets with 4 to 8 oz water after first loose stool, then one caplet (with 4 to 8 oz water) after each subsequent loose stool. Don’t exceed four caplets in 24 hours. Or give equivalent dosage in liquid form. Children ages 9 to 11 who weigh 27 to 43 kg (60 to 95 lbs): One caplet with 4 to 8 oz water after first loose stool, then 1 ⁄2 caplet (with 4 to 8 oz water) after each subsequent loose stool. Don’t exceed three caplets in 24 hours. Or give equivalent dosage in liquid form. Children ages 6 to 8 who weigh 22 to 27 kg (48 to 59 lbs): One caplet with 4 to 8 oz water after first loose stool, then 1 ⁄2 caplet with 4 to 8 oz water after each subsequent loose stool. Don’t exceed two caplets in 24 hours. Or give equivalent dosage in liquid form. Children younger than age 6: Consult physician. ➣ Chronic diarrhea Adults: Initially, 4 mg P.O., then 2 mg after each loose stool; reduce dosage as tolerated. Don’t exceed 16 mg daily for more than 10 days. |
Mechanism of Action
Slows intestinal motility through opioid receptor; has direct effects on circular and longitudinal muscle; reduces fecal volume; increases viscosity
Pharmacokinetics:
- Bioavailability: 0.3%
- Peak plasma time: 5 hr (capsule); 2.5 hr (liquid)
- Metabolism: Significant first-pass metabolism, resulting in very low plasma level of drug
- Elimination half-life: 7-14 hr
- Excretion: Feces (30-40%), urine (1%)
Administration
Use patient’s weight to determine appropriate dosage (especially in children).
Adverse reactions
- CNS: drowsiness, dizziness
- GI: nausea; vomiting; constipation; abdominal pain, distention, or discomfort; dry mouth; toxic megacolon (in patients with acute ulcerative colitis)
- Other: allergic reactions
Contraindications
- Hypersensitivity to drug
- Abdominal pain of unknown cause (especially with fever)
- Acute diarrhea caused by enteroinvasive Escherichia coli, Salmonella, or Shigella
- Acute ulcerative colitis
- Bloody diarrhea with temperature above 38.3 °C (101 °F) (with OTC product)
- Pseudomembranous colitis associated with broad-spectrum antiinfectives
- Children younger than age 6
Precautions
- Hepatic disease
- Elderly patients
- Pregnant or breastfeeding patients
- Children.
Patient monitoring
- Watch for signs and symptoms of abdominal distention, which may signal toxic megacolon in patient with ulcerative colitis.
- Assess bowel movements to evaluate drug efficacy and determine need for repeat doses.
- Monitor stool cultures as indicated.
- Check stool for occult blood as indicated.
- Evaluate fluid intake and output.
- Stay alert for CNS effects, especially in children.
Patient teaching
- Stress importance of maintaining high fluid intake to prevent dehydration.
- Instruct patient or parents to report fever, mucus in stool, or history of hepatic disease before using drug.
- Caution patient or parents to discontinue drug if symptoms worsen or diarrhea lasts longer than 2 days.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors 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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