Aspasom

Approved Indications:

• Gastrointestinal Disorders:
• Treatment of acute abdominal pain, intestinal colic, biliary colic, and painful spasms of the gastrointestinal tract.
• Management of irritable bowel syndrome (IBS) and functional bowel disorders associated with visceral spasm.
• Urological Disorders:
• Relief of ureteral colic, bladder spasms, and painful urinary tract contractions.
• Gynecological Disorders:
• Used in dysmenorrhea, painful uterine contractions, and spasmodic pelvic pain.

Clinically Accepted Off-label Use:

• Adjunct treatment in radiological or endoscopic procedures to reduce spasms of hollow organs (e.g., during barium enema).

Adults:

• Oral:
• Typical dose: 50 mg tablet, 2 to 4 times daily, depending on severity of symptoms.
• Injectable:
• IV/IM: 5–10 mg every 6–8 hours as needed.

Pediatrics:

• Not routinely recommended unless under strict medical supervision. Use cautiously with weight-based dose adjustments.

Elderly:

• Same adult dosage may be used with caution. Monitor for anticholinergic side effects (e.g., dry mouth, confusion).

Special Populations:

• Renal impairment: Use with caution; adjust dose if necessary based on clinical response.
• Hepatic impairment: No specific dose adjustment data; initiate at lower end of dosing range and monitor.

Route of Administration:

• Oral tablets and injectable solutions (IV or IM).

Duration:

• Duration depends on the underlying cause and clinical improvement, typically short-term use (3–7 days).

Tiemonium Methylsulfate is a quaternary ammonium antimuscarinic agent. It acts as a competitive antagonist of muscarinic acetylcholine receptors, primarily in the smooth muscles of the gastrointestinal, urinary, and genital tracts. By blocking parasympathetic nervous system stimulation, it reduces smooth muscle contractions and spasms. This results in pain relief and reduced motility of the affected organs, improving symptoms such as colic, cramps, and spasm-related discomfort without crossing the blood-brain barrier, thereby minimizing central nervous system effects.

• Absorption: Rapidly absorbed following oral or intramuscular administration; oral bioavailability is moderate.
• Distribution: Limited central nervous system penetration due to its quaternary ammonium structure.
• Metabolism: Partially metabolized in the liver via non-specific hydrolysis.
• Elimination: Primarily excreted via urine as unchanged drug and metabolites.
• Half-life: Approximately 3–4 hours.
• Onset of Action: Within 30–60 minutes after oral administration; faster via IM/IV route.

• Pregnancy Category: Not formally classified by the FDA. However, animal studies have not demonstrated teratogenicity. Use is not recommended during the first trimester unless clearly necessary.
• Lactation: Unknown if excreted into breast milk. Use caution during breastfeeding; temporary discontinuation may be considered if essential.

• Primary Class: Antispasmodic Agent
• Subclass: Muscarinic Receptor Antagonist (Quaternary Ammonium Anticholinergic)

• Known hypersensitivity to Tiemonium Methylsulfate or any component of the formulation
• Glaucoma (especially narrow-angle)
• Prostatic hypertrophy with urinary retention
• Myasthenia gravis
• Severe hepatic or renal impairment
• Paralytic ileus or toxic megacolon

• Use cautiously in elderly patients due to increased risk of anticholinergic effects (e.g., confusion, constipation).
• Monitor intraocular pressure in patients at risk of glaucoma.
• Use with caution in patients with cardiac arrhythmias, hyperthyroidism, or chronic constipation.
• Avoid use in pregnancy (especially 1st trimester) unless necessary.
• Caution in lactating women—safety not established.
• May cause urinary retention in predisposed individuals.

Common:

• Gastrointestinal: Dry mouth, constipation, nausea
• Neurological: Dizziness, light-headedness
• Ophthalmic: Blurred vision, dry eyes
• Genitourinary: Urinary hesitancy or retention

Less Common/Rare:

• Tachycardia
• Hypotension (particularly with injectable form)
• Allergic reactions (rash, pruritus)
• Palpitations
• Abdominal distension

Serious:

• Acute urinary retention
• Angle-closure glaucoma
• Severe hypersensitivity (rare)

Major Interactions:

• Other anticholinergics (e.g., atropine, hyoscine): Additive anticholinergic effects (dry mouth, urinary retention, constipation).
• Tricyclic antidepressants (e.g., amitriptyline): Enhanced anticholinergic activity.
• MAO inhibitors: Potential for increased sympathetic stimulation.
• Antihistamines, antipsychotics: Risk of cumulative CNS and anticholinergic effects.
• Alcohol: May enhance sedative effects.

Metabolism Involvement:

• Limited CYP450 metabolism; no significant CYP-mediated drug-drug interactions documented.

• No major guideline revisions or regulatory changes as of the latest international updates.
• Some national formularies have restricted long-term use due to anticholinergic burden.
• Bangladesh Drug Administration continues to approve Tiemonium for short-term spasm-related gastrointestinal and urinary indications.

• Temperature: Store below 30°C.
• Protection: Protect from light and excessive humidity.
• Handling Precautions: Do not freeze injectable solution.
• Tablet Form: Keep in original blister until use; store in a dry place.
• Injection Form: Discard any unused solution after opening. Shake if signs of separation occur in suspension forms.