Butalpen

Approved Indications:

• Gastrointestinal Disorders:
• Relief of abdominal cramping, pain, and spasms in irritable bowel syndrome (IBS).
• Treatment of gastrointestinal smooth muscle spasm, including gastritis, peptic ulcers, and enteritis.
• Biliary Tract Disorders:
• Relief of biliary colic and pain associated with cholelithiasis (gallstones).
• Adjunct treatment in cholecystitis.
• Genitourinary Tract Disorders:
• Management of renal colic and bladder spasms.
• Supportive treatment for dysuria associated with overactive bladder or urinary tract infections.
• Procedural Use:
• Pre-medication for diagnostic imaging (e.g., endoscopy, radiography) to reduce smooth muscle spasm in the gastrointestinal or genitourinary tract.

Clinically Accepted Off-label Uses:

• Relief of menstrual cramps (primary dysmenorrhea).
• Used under supervision to ease uterine cramps during labor in certain obstetric cases.
• Occasionally included in motion sickness treatment when used in specific combination products.

Route of Administration:

• Oral (tablets)
• Rectal (suppositories)
• Intramuscular (IM), Subcutaneous (SC), or Intravenous (IV) injection

Adult Dosage:

• Oral:
  10 mg tablet, taken 3 to 5 times daily.
  Maximum daily dose: 60 mg.
• Injectable (IM/SC/IV):
  20 mg every 6 to 8 hours, as needed.
  In severe cases, 20 mg IV may be repeated up to 100 mg/day under supervision.
• Rectal Suppositories:
  10–20 mg suppository, up to 3 times daily.

Pediatric Dosage:

• Children 6–12 years (Oral):
  5–10 mg, 3 times daily.
• Children 1–5 years (Injectable):
  0.3–0.6 mg/kg/dose, IM or SC, up to 3 times daily.

Note: Oral dosage forms are not recommended in children under 6 years unless directed by a physician.

Elderly:

• Start at the lowest effective dose.
• Monitor for anticholinergic side effects such as confusion or urinary retention.

Renal/Hepatic Impairment:

• No formal dose adjustment required.
• Use with caution in severe impairment; monitor for adverse effects.

Administration Notes:

• Oral tablets must be swallowed whole with water—do not crush or chew.
• IV injections should be administered slowly.
• Ensure correct positioning for rectal use.

Hyoscine Butylbromide is a peripheral antimuscarinic agent that blocks muscarinic cholinergic receptors in the smooth muscle of the gastrointestinal, biliary, and genitourinary tracts. This competitive inhibition of acetylcholine reduces smooth muscle contractions, thereby relieving painful spasms and colicky discomfort. As a quaternary ammonium compound, it does not cross the blood-brain barrier, which limits central nervous system side effects such as sedation or dizziness.

• Absorption:
  Poorly absorbed orally (<8%) due to its quaternary ammonium structure.
  Injectable forms provide rapid and complete absorption.
• Distribution:
  Minimal central distribution. Does not cross the blood-brain barrier.
  Low plasma protein binding (~4.4%).
• Metabolism:
  Rapidly hydrolyzed by plasma and hepatic esterases to inactive metabolites.
• Excretion:
• Primarily via urine (~50%, as metabolites).
• Minor excretion via feces.
• Half-life:
  ~4–5 hours after parenteral administration.
• Onset of Action:
• Oral: 30–60 minutes
• IV/IM: 5–10 minutes
• Duration of Action:
  3–6 hours

• Pregnancy:
  Classified as FDA Category C.
  Animal studies do not indicate direct fetal harm, but human data are insufficient.
  Use only if the benefit outweighs the potential risk, especially during the first trimester.
• Lactation:
  Unknown if excreted in breast milk.
  Use with caution during breastfeeding.
  Monitor infant for signs of anticholinergic effects (e.g., dry mouth, drowsiness).

Due to minimal systemic absorption with oral/rectal use, fetal and infant exposure is likely low.

• Primary Class: Antispasmodic
• Subclass: Anticholinergic (Peripheral Muscarinic Receptor Antagonist)
• Chemical Category: Quaternary Ammonium Compound

• Hypersensitivity to hyoscine butylbromide or any component of the formulation
• Myasthenia gravis
• Narrow-angle glaucoma
• Megacolon, especially toxic megacolon
• Mechanical obstruction of the gastrointestinal tract
• Prostatic hypertrophy with urinary retention
• Tachyarrhythmia

• Use with caution in:
• Elderly patients
• Individuals with cardiovascular disease (e.g., tachycardia)
• Patients with urinary retention or prostatic enlargement
• Those with impaired bowel motility or partial obstruction
• Avoid prolonged use without medical supervision.
• May impair ability to drive or operate machinery due to visual disturbances and drowsiness.
• IV administration may lead to hypotension or tachycardia; monitor vital signs.
• Observe for anticholinergic toxicity in overdose (e.g., flushing, confusion, urinary retention, dry mouth).

Common Adverse Effects:

• Gastrointestinal: Dry mouth, nausea, constipation
• Neurological: Dizziness, headache, drowsiness
• Visual: Blurred vision, difficulty focusing

Less Common:

• Palpitations, flushing, increased heart rate
• Urinary retention
• Skin reactions (rash, itching)

Rare but Serious:

• Anaphylaxis (especially after injection)
• Paralytic ileus in patients with intestinal disorders
• Severe hypotension (after IV administration)

Major Drug-Drug Interactions:

• Other anticholinergics (e.g., atropine, ipratropium): Additive effects; increased risk of dry mouth, constipation, urinary retention.
• Tricyclic antidepressants (e.g., amitriptyline): Enhanced anticholinergic toxicity.
• Antipsychotics (e.g., clozapine): Potentiated anticholinergic effects.
• Opioids (e.g., morphine): Combined risk of reduced bowel motility.

Drug-Food Interactions:

• Food may slightly delay oral absorption, but clinical significance is minimal.

Drug-Alcohol Interaction:

• Alcohol may intensify CNS effects such as dizziness or drowsiness.

Enzyme Involvement:

• Not significantly metabolized by CYP450 enzymes—low risk for enzyme-based interactions.

• EMA and national health authorities reaffirmed the safety of parenteral formulations with a warning to monitor cardiovascular parameters in elderly patients.
• Some product inserts now include diagnostic imaging as a formally approved indication.
• Regulatory updates emphasize proper IV technique and monitoring to minimize adverse cardiovascular events.

Oral Tablets:

• Store at 20°C to 25°C (68°F to 77°F)
• Protect from light, moisture, and excessive heat
• Keep in original packaging

Injectable Form:

• Store between 2°C to 8°C (refrigerated)
• Do not freeze
• Protect from light
• Discard if solution becomes discolored or cloudy

Suppositories:

• Store below 25°C
• Protect from humidity and heat

General Handling Notes:

• Shake ampoules gently before IV use
• Keep out of reach of children
• Check expiration date before administration