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Journal of Glaucoma Aug 1996
Review
Topics: Glaucoma, Angle-Closure; Humans; Iris; Miotics; Pilocarpine; Premedication
PubMed: 8795764
DOI: No ID Found -
Ophthalmology Jan 1981
Topics: Glaucoma; Humans; Pilocarpine
PubMed: 7243232
DOI: 10.1016/s0161-6420(81)35072-6 -
International Journal of Pharmaceutical... 2020Although pilocarpine hydrochloride tablets are currently indicated for the treatment of xerostomia, their adverse effects are frequently reported. The development of a...
Although pilocarpine hydrochloride tablets are currently indicated for the treatment of xerostomia, their adverse effects are frequently reported. The development of a new, low-dose pilocarpine solution for topical oral-cavity use is needed. This article discusses a few clinical trials to formulate a topical low-dose solution of pilocarpine hydrochloride for the treatment of xerostomia and presents two low dose, stable formulations of pilocarpine topical spray that can improve the patient's quality of life with minimal adverse effects.
Topics: Head and Neck Neoplasms; Humans; Muscarinic Agonists; Pilocarpine; Quality of Life; Xerostomia
PubMed: 32196472
DOI: No ID Found -
Drugs Jan 1995Pilocarpine is a cholinergic agonist which stimulates salivary secretion both in individuals with normal salivary gland function and in those with impaired salivary flow... (Review)
Review
Pilocarpine is a cholinergic agonist which stimulates salivary secretion both in individuals with normal salivary gland function and in those with impaired salivary flow (xerostomia or oral dryness). A rapid increase in salivary flow rate is observed following oral pilocarpine administration and peak levels are maintained for at least 1 to 2 hours. Mean salivary flow rates after administration of pilocarpine are 2- to 10-fold higher than after placebo, and no evidence of tolerance to the pharmacological effects of the drug has been observed during prolonged administration for up to 5 months. The clinical efficacy of oral pilocarpine in relieving symptoms of xerostomia (resulting from radiation therapy to the head and neck region or salivary gland dysfunction), including oral dryness and difficulty in chewing, swallowing and speaking, has been demonstrated in double-blind placebo-controlled clinical trials. In these studies, pilocarpine 5 to 10mg 3 times daily increased salivary flow and improved symptoms of xerostomia in a significantly higher percentage of patients than did placebo (54 versus 25% in one study). Preliminary findings indicate that administration of pilocarpine during radiation therapy may reduce the severity of xerostomia; however, this requires further investigation. The majority of patients receiving oral pilocarpine therapy for xerostomia experience adverse events (most commonly sweating); however, these are generally mild and tolerable in nature. Thus, pilocarpine is an effective agent for the treatment of xerostomia, increasing salivary flow and reducing symptom severity to a significantly greater extent than placebo. Further clinical trials should evaluate the potential beneficial effects of pilocarpine on the incidence of dental caries and oral candidiasis during prolonged therapy, its prophylactic efficacy during radiation therapy and its efficacy relative to that of other salivary stimulants.
Topics: Controlled Clinical Trials as Topic; Humans; Pilocarpine; Radiotherapy; Randomized Controlled Trials as Topic; Salivary Glands; Salivation; Xerostomia
PubMed: 7705213
DOI: 10.2165/00003495-199549010-00010 -
Drug and Therapeutics Bulletin Jun 1978
Topics: Delayed-Action Preparations; Glaucoma; Humans; Pilocarpine
PubMed: 657963
DOI: No ID Found -
Molecules (Basel, Switzerland) Jun 2021Furan-2-carboxylic acid was used as a starting material for the synthesis of dehydro-homopilopic acid. Esterification, hydrogenation and enzymatic hydrolysis followed by...
Furan-2-carboxylic acid was used as a starting material for the synthesis of dehydro-homopilopic acid. Esterification, hydrogenation and enzymatic hydrolysis followed by the reduction of Weinreb amides and a single-step attachment of a 1-methyl-imidazole residue allowed for the concise synthesis of both enantiomers of pilocarpine.
Topics: 4-Butyrolactone; Amides; Carboxylic Acids; Esterification; Furans; Hydrogenation; Hydrolysis; Pilocarpine; Stereoisomerism
PubMed: 34208623
DOI: 10.3390/molecules26123676 -
Journal of Pharmaceutical Sciences Oct 1975The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the...
The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the d-enantiomer via the alpha-methylbenzylamine salt. The penultimate intermediate, 2-mercaptopilocarpine, was desulfurized by oxidation with dilute hydrogen peroxide, minimizing isomerization to isopilocarpine. Procedures for the analysis of pilocarpine-isopilocarpine mixtures by high-pressure liquid chromatography are also described.
Topics: 4-Butyrolactone; Isomerism; Methods; Pilocarpine; Stereoisomerism; Sulfhydryl Compounds
PubMed: 1185540
DOI: 10.1002/jps.2600641026 -
General Dentistry 1996
Review
Topics: Administration, Oral; Cranial Irradiation; Drug Approval; Head and Neck Neoplasms; Humans; Parasympathomimetics; Pilocarpine; Salivation; Stimulation, Chemical; United States; United States Food and Drug Administration; Xerostomia
PubMed: 8940567
DOI: No ID Found -
Biological & Pharmaceutical Bulletin 2022Sjogren's syndrome and radiation therapy for head and neck cancers are often accompanied by xerostomia. Oral pilocarpine (PCP) to treat xerostomia produces systemic side...
Sjogren's syndrome and radiation therapy for head and neck cancers are often accompanied by xerostomia. Oral pilocarpine (PCP) to treat xerostomia produces systemic side effects, such as runny nose and lacrimation. To improve the therapeutic efficacy of PCP and reduce the aforementioned side effects, we developed a topical delivery system for PCP using freeze-dried sheets of hyaluronic acid (HA). The advantages of HA sheets over conventional oral formulations were examined through in vivo pharmacokinetic and pharmacodynamic studies after their application to oral tissues and salivary glands. The concentration of PCP in the submucosal tissue of the oral cavity was determined using the microdialysis (MD) method after buccal application of HA sheets containing PCP to hamsters. The concentration of PCP in the MD outflow was quite low after gastric administration, whereas the PCP concentration in plasma was high. In contrast, after buccal application of HA sheets containing PCP, the concentration of the drug in the MD outflow increased, despite the negligible concentration in plasma. These findings indicated that both enhancement of saliva secretion and the avoidance of systemic side effects could be achieved through buccal administration of PCP-loaded HA sheets. In addition, the pharmacodynamic study showed that when compared with intravenous and gastric administration, salivary application of HA sheets containing PCP resulted in similar volumes of saliva secretion and reduced lacrimal secretions. In conclusion, freeze-dried HA sheets allow for the development of a novel buccal delivery system with enhanced therapeutic efficacy and safety to treat xerostomia.
Topics: Head and Neck Neoplasms; Humans; Pilocarpine; Salivary Glands; Salivation; Xerostomia
PubMed: 35370264
DOI: 10.1248/bpb.b21-00763 -
Texas Dental Journal Oct 1996This article is intended to familiarize dental practitioners with a new drug preparation, Salagen, which is specifically indicated for treatment of dry mouth. Salagen,... (Review)
Review
This article is intended to familiarize dental practitioners with a new drug preparation, Salagen, which is specifically indicated for treatment of dry mouth. Salagen, an oral form of the drug pilocarpine, is a parasympathetic agonist which causes widespread effects on many vital tissues and organs, including the heart, blood vessels, smooth muscle, and exocrine glands. The safety and efficacy of pilocarpine relies greatly on the accurate diagnosis of the underlying cause of dry mouth and an understanding of its mechanism of action. The purpose of this article is to provide dental practitioners with a brief review of the physiology of salivary secretion and the pharmacology of pilocarpine, including its mechanism of action. It is hoped that this information will provide a better understanding of the appropriate use of this medication.
Topics: Administration, Oral; Chemistry, Pharmaceutical; Humans; Parasympathomimetics; Pilocarpine; Salivary Glands; Xerostomia
PubMed: 9518825
DOI: No ID Found