Dicyclomine
Dicyclomine
Generic Name
Dicyclomine
Brand Names
Bentyl®, other generic formulations) is a long‑acting antimuscarinic antispasmodic used primarily for irritable bowel syndrome (IBS) and other functional abdominal disorders. It reduces smooth‑muscle spasm by antagonizing muscarinic receptors in the gastrointestinal tract.
Mechanism
- Selective muscarinic antagonist: Binds competitively to M1, M2, and M3 muscarinic receptors in the gut, inhibiting acetylcholine‑induced contraction.
- Smooth‑muscle relaxation: Decreases tone of intestinal and urethral sphincters, reducing cramping and abdominal pain.
- Minimal central effects: Its relatively low lipophilicity limits blood‑brain‑barrier penetration, causing fewer CNS adverse reactions compared with other anticholinergics.
Pharmacokinetics
- Absorption: Rapid oral uptake; peak plasma concentrations within 1–2 h.
- Distribution: Low penetration into CNS; mainly systemic antimuscarinic activity.
- Metabolism: Hepatic hydroxylation → active metabolite (desmethyldicyclomine); glucuronide conjugation.
- Elimination: Renal excretion of unchanged drug + conjugates; half‑life ≈ 10–12 h (single‑dose) but extends up to 21 h with multiple dosing.
- Drug interactions: Minimal CYP interactions; may increase systemic exposure when renal function is impaired.
Indications
- Irritable bowel syndrome (IBS): Relieves abdominal cramping, pain, and bloating.
- Other functional GI disorders: Such as functional abdominal pain or dyspepsia when antispasmodic effect is desired.
- Adjunctive therapy: In patients refractory to lifestyle modifications or low‑dose antispasmodics.
Contraindications
- Absolute contraindications
* Acute colonic obstruction or bowel perforation
* Suspected bowel obstruction or diverticulitis
* Glaucoma due to risk of increased intraocular pressure
* Urinary retention or obstruction; myasthenia gravis
* Severe hepatic or renal impairment (renal dosing adjustments required)
• Pregnancy & Lactation
* Category C: Limited data; use only if benefits outweigh risks.
• Warnings
* Anticholinergic toxicity (dry mouth, blurred vision, tachycardia, urinary retention)
* Caution in elderly with cognitive or cardiovascular disease
* Monitor for signs of constipation or a paralytic ileus
Dosing
| Formulation | Typical adult dose | Frequency | Notes |
| Oral (capsule) | 25 mg | 4–6 × day | Start at 2–4 mg BID; titrate to 25 mg q4–6 h; max 150 mg/day |
| Oral (tablet) | 25 mg | 6 × day | Same as capsule; may separate dosing: 2 × day & 4 × day |
| Theft‑injested | 10–20 mg | For acute abdominal spasms | Can be given as an oral slurry (dissolve in water) |
| Intramuscular (2.5 mg/0.5 mL) | 1–2 × day | For patients who cannot tolerate oral | Short‑acting; monitor for systemic anticholinergic signs |
• First‑dose adjustments: Use minimal effective dose; titrate based on symptom relief and tolerability.
• Long‑term use: Recommended for patients with chronic symptoms; reassess yearly for efficacy and adverse events.
Adverse Effects
Common (≥5 %)
• Dry mouth, blurred vision, constipation
• Urinary retention, tachycardia, dizziness
• Heat intolerance, sexual dysfunction (erectile dysfunction; decreased libido)
Serious (≤1 %)
• Severe anticholinergic syndrome (hyperthermia, seizures, hallucinations)
• Acute urinary retention or bladder distension
• Glaucoma attacks (intraocular pressure ↑)
• Cardiac arrhythmias (QT prolongation).
Monitoring
- Baseline: Blood pressure, heart rate, baseline hepatic and renal function; visual acuity if glaucoma history.
- During therapy: Monitor for anticholinergic symptoms, urinary retention, constipation.
- Laboratory: Renal function at baseline and every 3–6 months in chronic therapy.
Clinical Pearls
- “Double‑dose, double‑tired”: Dosing 25 mg q4–6 h ensures a therapeutic drug level while minimizing adverse events; avoid >150 mg/day.
- Avoid in “Frog‑legs”: Patients with chronic constipation or a history of urinary retention should receive careful titration or consider alternative antispasmodics (e.g., hyoscine).
- Switch back with caution: Gradual tapering prevents rebound cramping; abruptly stopping can worsen IBS symptoms.
- Drug‑drug synergy: Concomitant use with other anticholinergics (e.g., antihistamines, antipsychotics) increases risk—dose reduction or discontinuation may be warranted.
- Age‑adjustment: In elderly patients, start at the lowest possible dose (e.g., 2.5 mg BID) to evaluate tolerability before escalating.
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• *This drug card is intended for medical educational purposes and should not replace the evaluation of complete prescribing information.*