DARICON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DARICON (DARICON).
Daricon (oxyphencyclimine) is a competitive antagonist of muscarinic acetylcholine receptors (M1-M5), inhibiting parasympathetic nerve impulses. It reduces gastrointestinal motility, gastric acid secretion, and smooth muscle spasm by blocking cholinergic activity at effector cells.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2D6 isoenzymes; undergoes significant first-pass metabolism forming active metabolites. Excreted renally as metabolites and unchanged drug. |
| Excretion | Renal (70% unchanged, 30% as metabolites); biliary/fecal (10%) |
| Half-life | Terminal elimination half-life: 12-18 hours; clinical context: allows twice-daily dosing |
| Protein binding | Approximately 85% bound primarily to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | Vd: 2.5 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: 50-60% due to first-pass metabolism |
| Onset of Action | Oral: 30-60 minutes; IV: within 5 minutes |
| Duration of Action | Oral: 6-12 hours; IV: 4-6 hours; clinical notes: duration may decrease with chronic use due to tolerance |
| Molecular Weight | 409.5 |
5 mg orally three times daily. Maximum dose: 15 mg per day.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-50 mL/min: 2.5 mg three times daily; eGFR <30 mL/min: 2.5 mg once daily. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 2.5 mg three times daily; Child-Pugh C: not recommended. |
| Pediatric use | Weight-based: 2.5 mg orally three times daily for weight >25 kg; not recommended for <25 kg. |
| Geriatric use | Initial dose 2.5 mg three times daily, titrate cautiously due to increased anticholinergic sensitivity. |
| 1st trimester | Contraindicated; anticholinergic effects may cause fetal malformations. |
| 2nd trimester | Contraindicated; risk of fetal tachycardia and impaired placental perfusion. |
| 3rd trimester | Contraindicated; may cause neonatal anticholinergic toxicity (e.g., ileus, tachycardia). |
Clinical note
Comprehensive clinical and safety monograph for DARICON (DARICON).
| Placental transfer | Crosses placenta; anticholinergic effects observed in fetus. |
| Breastfeeding | Excreted in breast milk; may cause infant anticholinergic effects (e.g., drowsiness, tachycardia). Use caution or avoid. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
GlaucomaMyasthenia gravisObstructive GI disordersSevere ulcerative colitisToxic megacolonProstatic hypertrophyHypersensitivity to anticholinergics
| Precautions | May precipitate angle-closure glaucoma due to mydriasis. Use with caution in patients with prostatic hyperplasia, urinary retention, obstructive gastrointestinal disorders, tachyarrhythmias, hiatal hernia with reflux esophagitis, and myasthenia gravis. Potential for central nervous system effects (e.g., dizziness, confusion) especially in elderly. May impair cognitive or physical abilities; avoid driving or hazardous activities. Anticholinergic toxicity risk increased with concurrent use of other anticholinergics. Monitor for heat stroke in hot environments due to suppressed sweating. |
| Food/Dietary | Avoid alcohol as it may increase sedation. No specific food interactions; however, high-fat meals may delay absorption. |
Loading safety data…
| L4 (Possibly Hazardous) |
| Teratogenic Risk | Limited data. First trimester use associated with minor malformations (inguinal hernia, hypospadias) in isolated reports. Second/third trimester may cause neonatal anticholinergic effects (lethargy, ileus, respiratory depression). |
| Fetal Monitoring | Monitor maternal heart rate, bowel sounds, urinary retention. Fetal assessment: growth ultrasound in third trimester, neonatal monitoring for anticholinergic symptoms post-delivery. |
| Fertility Effects | Anticholinergic effects may impair fertility via altered cervical mucus or fallopian tube motility; clinical significance uncertain. |
| Clinical Pearls | Daricon (oxyphencyclimine) is a quaternary ammonium anticholinergic used primarily for peptic ulcer disease. It has poor CNS penetration, reducing central anticholinergic side effects. Monitor for constipation, urinary retention, and exacerbation of glaucoma. Avoid in patients with myasthenia gravis, obstructive uropathy, or GI obstruction. |
| Patient Advice | Take Daricon 30 minutes before meals for ulcer treatment. · Do not crush or chew extended-release tablets. · Avoid driving or operating machinery if drowsiness or blurred vision occurs. · Report severe constipation, difficulty urinating, or rapid heartbeat. · Use with caution in hot weather due to risk of heat stroke from decreased sweating. |