TABLE 1.
FDA/EMA approved muscarinic receptor antagonists and agonists.
| Generic (Trade) name | Activity/MR selectivity | Dose range/Route | Approved indications |
|---|---|---|---|
| Benztropine (Cogentin) Bolden et al. (1992) | M1R Ant | 0.5–6 mg/day IM/IV/PO | Parkinson’s disease, extrapyramidal symptoms, dystonia |
| Biperiden (Akineton) Eltze and Figala (1988) | M1R Ant | 1–16 mg/day PO, 2.5–5 mg IM/IV | Parkinson’s disease, extrapyramidal symptoms |
| Dicyclomine (Bentyl) Giachetti et al. (1986) | M1R Ant | 20–160 mg/day PO | Irritable bowel syndrome |
| Pirenzipine (Gastrozepin) Bolden et al. (1992) | M1R Ant | 100–150 mg/day PO | Peptic ulcer disease |
| Trihexyphenidyl (Artane) Giachetti et al. (1986) | M1R Ant | 5–15 mg/day PO | Parkinson’s disease |
| Cevimeline/AF-102B (Evoxac) Weber and Keating (2008b) | M1R, M3R Agonist | 90 mg/day PO | Xerostomia in Sjogren’s syndrome |
| Oxybutynin (Ditropan) Andersson and Chapple (2001) | M1R, M3R Ant | 5–30 mg/day PO; topical and transdermal | Overactive bladder |
| Aclidinium (Tudorza Pressair) Beier et al. (2013) | M3R Ant | 800 mcg/daily inhaled | Chronic obstructive pulmonary disease |
| Darifenacin (Enablex) Yamada et al. (2006) | M3R Ant | 7.5–15 mg/day PO | Overactive bladder |
| Solifenacin (VESIcare) Oki et al. (2005) | M3R Ant | 5–10 mg/day PO | Overactive bladder |
| Aceclidine* (Glaunorm) Erickson and Schroeder (2000) | NS Agonist | Topical | Glaucoma |
| Bethanechol (Urecholine) | NS Agonist | 30–200 mg/day PO | Urinary retention |
| Methacholine | NS Agonist | 1–380 mcg | Bronchial airway hyperactivity |
| Pilocarpine (Salagen, Isopto Carpine) Zimmerman (1981) | NS Agonist | 15–30 mg/day PO | Xerostomia, glaucoma |
| Atropine (Atropen) | NS Ant | 0.5–3 mg IV/IM; available as inhalant | Bradycardia, inhibit secretions; mushroom/organophosphate poisoning |
| Scopolamine (Transderm-Scop) | NS Ant | 1.5 mg skin patch; available PO, IM, IV | Nausea, sedation, GI and genitourinary spasm |
| Tolterodine (Detrol) Hills et al. (1998) | NS Ant | 2–4 mg/day PO | Overactive bladder |
Ant, antagonist; EMA, European Medicines Agency; FDA, United States Food and Drug Administration; IM, intramuscular; IV, intravenous; NS, nonselective; PO, oral. *, not FDA approved.