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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DARICON (DARICON).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Potential for anticholinergic effects in infant; use caution. |
| 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 |
■ FDA Black Box Warning
None
| Serious Effects |
Absolute: Hypersensitivity to oxyphencyclimine or any component; narrow-angle glaucoma; obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy); obstructive gastrointestinal tract disease (e.g., pyloroduodenal stenosis, achalasia); paralytic ileus; intestinal atony in elderly or debilitated patients; severe ulcerative colitis; toxic megacolon; myasthenia gravis (unless used under specialist supervision). Relative: Hyperthyroidism, coronary artery disease, congestive heart failure, cardiac arrhythmias, hypertension, hiatal hernia associated with reflux esophagitis, autonomic neuropathy, hepatic or renal impairment.
| 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. |
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| 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. |