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Abstract

There is disclosed a method for treating a patient suffering from xerostomia, xerophthalmia or excessive intraocular pressure. The method comprises administering to said patient a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof, in an amount sufficient to maintain a blood serum level of pilocarpine in said patient of from about 5 to about 40 ng/ml, for a period of at least 6 hours. Controlled release unit dosage forms containing pilocarpine are also disclosed.

Other References

• Schuller et al., "Treatment of radiation side effects with oral pilocarpine" J. Surg. Oncol. (1989) 42:272-276
• Severin, "Keatoconjunctivitis sicca " Vet. Clin. North Am. (1973) 3:407-422
• Pavan-Langston, "Potential use of ocular-insert therapy in dry eyes" Int. Opthalmol. Clin. (1973) 13:231-238
• Deshpande et al., "Sustained release ophthalmic formulations of pilocarpine" J. Pharm. Pharmacol. (1988) 41:197-200
• Fox et al., "Pilocarpine treatment of salivary gland hypofunction and dry mouth (Xerostomia)" Arch. Intern. Med. (1991) 151:1149-1152
• Fox et al., "Xerostomia: evaluation of a symptom with increasing significance" J. Am. Dent. Assoc, (1985) 110:519-525
• Chencharick et al., "Nutritional consequences of the radiotherapy of head and neck cancer" Cancer (1983) 51:811-815
• Fox, "Management of salivary gland hypofunction and dry mouth (xerostomia)" Head and Neck Canceer, Fee et al., eds., (1990) pp. 322-324
• Fox, "Systemic therapy of salivary gland hypofunction" J. Dent. Res. (1987) 66:689-692
• LeVeque et al., "A multicenter, radomized, double-blind, placebo-controlled, dose-titration study of oral pilocarpine for treatment of radiation-induced xerostamia in head and neck cancer patients" J. Clin. Oncol. (1993) 11:1124-1131
• Johnson et al., "Oral pilocarpine for post-irradiation xerostomia in patients with head and neck cancer" N. Engl. J. Med. (1993) 329:390-395
• Greenspan et al., "Effectiveness of pilocarpine in postradiation xerostomia" Cancer (1987) 59:1123-1125
• Dawes, "The composition of human saliva secreted in response to a gustatory stimulus and to pilocarpine" J. Physiol. (London) (1966) 183:360-368
• Mandel et al., "The effect of pharmacologic agents on salivary secretion and composition. II. Isoproterenol, alpha and beta adrenergic blockers" J. Oral. Ther. Pharmacol. (1968) 4:260-269
• Fox et al., "Pilocarpine for the treatment of xerostomia associated with salivary gland dysfunction" Oral Surg. Oral Med. Oral Pathol. (1986) 61:243-248
• Rhodus et al., "Effects of pilocarpine on salivary flow in patients with Sjogren's syndrome" Oral Surg. Oral Med. Oral pathol. (1991) 72:545-549
• Greco et al., "Systemic pilocarpine toxicity in the treatment of angle closure glaucoma" Ann. Opthalmol. (1973) 5:57-59
• Kastl, "Inadvertent systemic injection of pilocarpine. Case report" Arch. Opthalmol. (1987) 105:28-29
• Littmann et al., "Severe symptomatic atrioventricular block induced by pilocarpine eye drops" Arch. Intern. Med. (1987) 147:586-587
• Weaver et al., "Pilocarpine disposition and salivary flow responses folowing intravenous administration to dogs" Pharm. Res. (1992) 9:1064-1069
• Valdez et al., "Interactions of the salivary and gastrointestinal systems. II Effects of salivary gland dysfunction on the gastrointestinal tract" Dig. Dis. (1991) 9:210-218
• Hughes et al., "Oral-pharyngeal dysphagia: A common sequela of salivary gland dysfuntion" Dysphagia (1987) 1:173-177
• Caruso et al., "Objective measures of swallowing in patients with primary Sjogren's syndrome" Dysphagia (1989) 4:101-105
• Helm, "Role of saliva in esophageal function and disease" Dysphagia (1989) 4:76-84
• Korsten et al., "Chronic xerostomia increases esophageal acid exposure and is associated with esophageal injury" Am. J. Med. (1991) 90:701-706
• Lehr et al., "A surface energy analysis of mucoadhesion: Contact angle measurements on polycarbophil and pig intestinal mucosa in physiologically relevant fluids" Pharm. Res. (1992) 9:70-75
• Abstract of Mamtani et al., "Comparison of total costs of administrating calcium polycarbophil and psyllium mucilloid in an institutional setting" Clin. Therap. (1990) 12:22-25
• Physician's Desk Reference for Ophthalmology, Walsh, J.B. et al., eds., 16th Edition (1988) pp. 3,1