Drug Profile:

Aminophylline:

 Pharmacologic Class: Methylxanthine

 Therapeutic Class: Bronchodilator, Anti-inflammatory

How Supplied:

 Oral Tablets: 100 mg, 200 mg

 Injection (IV): 25 mg/mL in vials/ampoules

Pharmacokinetics:

 Absorption:
o Rapidly absorbed after oral administration, with 100% bioavailability. IV form
bypasses first-pass metabolism.
 Distribution:
o Widely distributed, including the lungs, heart, CNS, and kidneys.
o Plasma protein binding: 55-60%.
 Metabolism:
o Metabolized primarily in the liver by cytochrome P450 enzymes, mainly
CYP1A2.
 Excretion:
o Excreted primarily via the kidneys. Half-life: 3–9 hours (can vary with liver
function, age, or kidney status).
 Route:
o Oral, intravenous
 Onset:
o Oral: 1–2 hours; IV: 15 minutes to 1 hour
 Peak:
o Oral: 2 hours; IV: 1–2 hours
 Duration:
o Oral: 6–8 hours; IV: 6 hours
Pharmacodynamics:

 Mechanism of Action:
o Aminophylline work by inhibiting the enzyme phosphodiesterase (PDE), which
increases cyclic AMP (cAMP) levels. This leads to relaxation of smooth muscle
in the airways, resulting in bronchodilation and improved airflow.
o Antagonize adenosine receptors, which decreases bronchoconstriction and
promotes bronchodilation.
o Additionally, these drugs have mild anti-inflammatory properties by reducing the
release of inflammatory mediators like histamines and leukotrienes.

Indications and Dosage:

 Indications:
o Acute asthma exacerbations.
o Chronic obstructive pulmonary disease (COPD) exacerbations.
o Bronchospasm in conditions like emphysema and chronic bronchitis.
o Short-term treatment of bronchospasm.
 Dosage:
o Adults (Oral):
 Initial: 10 mg/kg/day (divided doses)
 Maintenance: 5–6 mg/kg/day (divided doses)
o Adults (IV):
 Loading dose: 5 mg/kg (administered over 20–30 minutes)
 Maintenance dose: 0.5–0.8 mg/kg/hr (IV infusion)
 Pediatric Dosage:
o Adjust based on weight, with close monitoring for side effects.

Adverse Reactions:

 Common Adverse Reactions:

o Nausea, vomiting, diarrhea.
o Tachycardia, arrhythmias (e.g., atrial fibrillation).
o Insomnia, headache, dizziness, tremors.
 Serious Adverse Reactions:
 o Seizures (may require urgent intervention).
o Life-threatening arrhythmias.
o Hypokalemia

Drug Interactions:

 CYP450 Inhibitors (e.g., erythromycin, ciprofloxacin): Increase aminophylline levels,

increasing the risk of toxicity.
 CYP450 Inducers (e.g., rifampin, phenytoin, smoking): Decrease aminophylline
levels, potentially reducing efficacy.
 Beta-blockers and Calcium Channel Blockers: Can potentiate arrhythmias.
 Alcohol: Can increase CNS effects such as dizziness.

Contraindications and Precautions:

 Contraindications:
o Hypersensitivity to aminophylline or theophylline.
o Active peptic ulcer disease.
o Acute myocardial infarction (especially with arrhythmias).
 Precautions:
o Use with caution in patients with arrhythmias, cardiovascular disease, liver or
kidney dysfunction.
o Not recommended in pregnancy unless absolutely necessary.
o Dose adjustment needed in smokers and patients with altered metabolism (e.g.,
liver disease).

Nursing Considerations:

Assessment:

 Baseline Assessment:
o Obtain vital signs (heart rate, respiratory rate).
o Assess for signs of toxicity, such as nausea, vomiting, seizures, or arrhythmias.
o Measure serum theophylline or aminophylline levels regularly (target range: 10-
20 µg/mL for theophylline, 5-15 µg/mL for aminophylline).
  Continuous Monitoring:
o Monitor ECG for arrhythmias, as both drugs can cause tachycardia or other
serious heart conditions.
o Monitor for signs of toxicity, particularly in elderly or liver-compromised
patients.

Nursing Diagnoses:

 Ineffective Airway Clearance: Related to bronchospasm and inflammation in the lungs.

 Risk for Injury: Due to potential adverse effects, including seizures or arrhythmias.
 Imbalanced Nutrition: Less than body requirements due to nausea and vomiting.
 Anxiety: Related to the potential side effects (e.g., tremors, restlessness).

Planning and Implementation:

 Plan:
o Ensure monitoring of vital signs, especially heart rate and blood pressure.
o Monitor serum drug levels to ensure they are within therapeutic ranges.
o Administer the drug via the appropriate route (oral or IV) as prescribed.
 Implementation:
o Administer as ordered, ensuring proper hydration and electrolyte balance.
o Provide safety measures (e.g., fall precautions) for patients at risk of seizures or
arrhythmias.
o Encourage deep breathing and other measures to promote airway clearance.

Patient Teaching:

 Signs of Toxicity: Teach the patient to recognize signs of toxicity such as nausea,
vomiting, tremors, dizziness, and seizures. Advise immediate medical consultation if
these occur.
 Drug Adherence: Instruct patients to take the medication consistently and not skip
doses. Emphasize that abrupt discontinuation may lead to exacerbation of symptoms.
 Avoid Drug Interactions: Advise patients to avoid smoking and alcohol, as they can
alter drug metabolism. Also, inform them of medications that can increase or decrease
theophylline/aminophylline levels.
 Monitoring: Stress the importance of regular follow-up appointments to monitor serum
drug levels, especially when changing dosage or adding new medications.
Evaluation:

 Effectiveness: Monitor for improvements in symptoms (e.g., reduced wheezing,

improved airflow).
 Therapeutic Drug Levels: Regularly check serum levels to ensure the drug is within the
therapeutic range and adjust as needed.
 Adverse Reactions: Reassess vital signs, serum drug levels, and for any side effects such
as arrhythmias, seizures, or gastrointestinal distress.
Drug Study: Antidiarrheal

Generic Name: Loperamide

Pharmacologic Class: Opioid receptor agonist
Therapeutic Class: Antidiarrheal

How Supplied

 Oral Tablets: 2 mg
 Oral Solution: 1 mg/5 mL

Pharmacokinetics

Absorption:

 Rapidly absorbed after oral administration, with low systemic bioavailability due to
significant first-pass metabolism in the liver.

Distribution:

 Primarily localized in the gastrointestinal tract due to P-glycoprotein efflux from the
central nervous system.
 Plasma protein binding: ~97%.

Metabolism:

 Metabolized extensively in the liver, predominantly by cytochrome P450 enzymes

(CYP3A4 and CYP2C8).

Excretion:

 Excreted primarily through feces (~80–90%), with minimal renal elimination (~2%).
 Half-life: Approximately 9–14 hours.

Route, Onset, Peak, and Duration

  Route: Oral
 Onset: 1–3 hours
 Peak: 4–6 hours
 Duration: Up to 24 hours

Pharmacodynamics

Loperamide works by binding to mu-opioid receptors in the intestinal wall. This action
decreases peristalsis, prolonging transit time in the intestines. By allowing increased water and
electrolyte absorption, it reduces stool frequency and improves stool consistency.

Indications and Dosage

Indications:

 Symptomatic treatment of acute diarrhea.

 Chronic diarrhea associated with inflammatory bowel disease (IBD).
 Management of stool output in patients with ileostomies.

Dosage:

Adults:

 Acute diarrhea:
o Initial dose: 4 mg, followed by 2 mg after each loose stool.
o Maximum daily dose: 16 mg.
 Chronic diarrhea:
o 4–8 mg daily in divided doses, adjusted as needed.

Pediatric Use (Ages 6–12):

 Adjust dosage based on weight and age. Initial doses typically range from 1–2 mg after
each loose stool.

Adverse Reactions

Common:

 Constipation
 Nausea
  Abdominal cramps
 Drowsiness

Serious:

 Paralytic ileus
 Toxic megacolon in infectious diarrhea
 High-dose cardiac events such as QT prolongation and torsades de pointes

Drug Interactions

 CYP3A4/CYP2C8 inhibitors (e.g., ketoconazole): Increase systemic levels of

loperamide, raising toxicity risk.
 P-glycoprotein inhibitors (e.g., quinidine): May allow the drug to cross the blood-brain
barrier, increasing CNS effects.
 CNS depressants (e.g., alcohol, benzodiazepines): Enhance sedative and drowsiness
effects.

Contraindications and Precautions

Contraindications:

 Hypersensitivity to loperamide or excipients

 Infectious diarrhea with high fever or blood in stools
 Pseudomembranous colitis or bacterial enterocolitis

Precautions:

 Use cautiously in patients with hepatic impairment due to reduced metabolism.

 Avoid in pediatric patients under two years of age.
 Monitor patients with a history of prolonged QT interval or cardiac arrhythmias.

Nursing Considerations

Assessment:

 Assess stool consistency, frequency, and hydration status.

 Monitor for signs of dehydration, such as dry mucous membranes and decreased urine
output.
 Evaluate for adverse effects such as abdominal distension or toxic megacolon.
Nursing Diagnoses:

 Diarrhea related to gastrointestinal irritation or infection.

 Deficient fluid volume related to excessive stool loss.
 Risk for imbalanced electrolytes related to prolonged diarrhea.

Planning and Implementation:

 Administer loperamide as prescribed, ensuring patients stay hydrated.

 Limit the dose to avoid the risk of severe constipation or toxicity.
 Monitor serum electrolytes in patients with prolonged diarrhea.

Patient Teaching:

 Instruct patients to discontinue the drug and consult a healthcare provider if diarrhea
persists beyond 48 hours or is accompanied by fever or abdominal pain.
 Encourage proper hydration and electrolyte replacement.
 Advise against misuse of the medication to prevent severe cardiac or CNS effects.

Evaluation:

 Monitor for decreased stool frequency and improved stool consistency.

 Assess hydration status for signs of improvement.
 Reevaluate therapy if symptoms persist or adverse reactions occur.
Drug Study: Laxative

Generic Name: Lactulose

Pharmacologic Class: Osmotic laxative
Therapeutic Class: Laxative, ammonia detoxicant

How Supplied

 Solution (Oral): 10 g/15 mL

 Powder (Oral): 10 g/sachet

Pharmacokinetics

Absorption:

 Poorly absorbed from the gastrointestinal tract.

Distribution:

 Acts locally in the colon; systemic distribution is negligible.

Metabolism:

 Metabolized by colonic bacteria into lactic acid, acetic acid, and other short-chain fatty
acids.

Excretion:

 Excreted in feces (active and metabolized forms).

 Minimal renal excretion of unmetabolized lactulose.

Route, Onset, Peak, and Duration

 Route: Oral or rectal

 Onset:
o Oral: 24–48 hours
 o Rectal: 2–4 hours
 Peak: Not well-defined due to localized action in the colon.
 Duration: Varies with patient response and hydration status.

Pharmacodynamics

Lactulose is a synthetic disaccharide that works by drawing water into the colon via osmosis,
softening stool and increasing stool frequency. It also lowers colonic pH, converting ammonia to
ammonium, which reduces its absorption and is useful in hepatic encephalopathy management.

Indications and Dosage

Indications:

 Relief of chronic constipation.

 Treatment and prevention of portal-systemic encephalopathy (PSE) or hepatic
encephalopathy.

Dosage:

For Constipation:

Adults:

 Oral: 15–30 mL daily, adjusted based on response (up to 60 mL/day).

Pediatrics:

 Oral: 1 mL/kg daily (max: 60 mL/day).

For Hepatic Encephalopathy:

Adults:

 Oral: 30–45 mL 2–4 times daily.

 Rectal: 300 mL of lactulose solution diluted in 700 mL of water or saline as a retention
enema; retain for 30–60 minutes, repeated every 4–6 hours as needed.

Adverse Reactions
Common:

 Abdominal discomfort (cramping, bloating)

 Flatulence
 Diarrhea (with high doses)

Serious:

 Severe dehydration
 Electrolyte imbalances (e.g., hypokalemia, hypernatremia)

Drug Interactions

 Antacids: May reduce the acidification of the colon, decreasing lactulose's efficacy.
 Other Laxatives: Concurrent use may potentiate diarrhea and dehydration.
 Oral Antibiotics: May reduce lactulose efficacy by altering colonic bacteria.

Contraindications and Precautions

Contraindications:

 Known hypersensitivity to lactulose or its components.

 Patients on a low-galactose diet (due to the presence of galactose in lactulose).

Precautions:

 Use cautiously in patients with diabetes, as lactulose contains sugars.

 Monitor closely for electrolyte imbalances in long-term use or high doses.

Nursing Considerations

Assessment:

 Assess for baseline bowel patterns, stool frequency, and consistency.

 Monitor for symptoms of hepatic encephalopathy (e.g., confusion, lethargy) if used for
this condition.
 Check hydration status and monitor for signs of dehydration or electrolyte imbalances.

Nursing Diagnoses:
  Constipation: Related to dietary habits or decreased bowel motility.
 Risk for Electrolyte Imbalance: Related to excessive bowel movements.

Planning and Implementation:

 Administer lactulose with or after meals to minimize abdominal discomfort.

 Dilute with water, juice, or milk to improve palatability if needed.
 Ensure availability of bathroom facilities, especially after dosing.

Patient Teaching:

 Advise patients that it may take 24–48 hours for the laxative effect.
 Stress the importance of maintaining adequate hydration during treatment.
 Teach patients to report persistent diarrhea, cramping, or signs of dehydration.
 For hepatic encephalopathy, educate patients and caregivers about recognizing early
symptoms of elevated ammonia levels.

Evaluation:

 Relief of constipation, evidenced by regular and soft stool formation.

 Improvement in symptoms of hepatic encephalopathy (if treated for this condition).
 Absence of adverse effects such as severe diarrhea or dehydration.