• Journal of Oral Medicine and Pain
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• 제19권2호
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• pp.25-45
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• 1994

The purposes of this study were to investigate the effect of pilocarpine-containing chewing gum for the treatment of xerostomia and to compare the effect of pilocarpine-containing chewing gum with that of pilocarpine oral administration. The 20 subjective and objective xerostomic patients were included in this study and divided into 3 groups. Five subjects were included in gum base chewing group, 10 in pilocarpine-containing gum chewing, and 5 in pilocarpine oral administration. The author measured unstimulated whole salivary flow rate, stimulated parotid salivary flow rate, pH of resting whole saliva, viscosity of stimulated whole saliva, and subjective symptoms and discomforts using VAS(visual analogue scale) at the beginning of the experiment. And the author investigated the changes of these factors at 1, 2, 3, and 4 week after. The obtained results were as follows : 1. There were significant increases in the unstimulated whole salivary flow rate in pilocarpine-containing gum chewing and pilocarpine oral administration groups. But there was no significant difference between pilocarpine-containing gum chewing and pilocarpine oral administration groups. 2. There was a significant increase in the stimulated parotid salivary flow rate in pilocarpine- containing gum chewing group. But there was no significant difference between pilocarpine- containing gum chewing and pilocarpine oral administration groups. 3. The change of salivary pH showed the increasing pattern in all groups. But there was no significant difference among groups. 4. There were no significant changes in the values of salivary viscosity in all groups through the experimental period. 5. There were significant decreases of VAS(visual analogue scale) in the degree of subjective symptoms and discomforts in pilocarpine-containing gum chewing and pilocarpine oral administration groups. But there was no significant difference between pilocarpine- containing gum chewing and pilocarpine oral administration groups.

• Journal of Oral Medicine and Pain
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• 제40권1호
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• pp.10-16
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• 2015

Purpose: Pilocarpine has the effects on improvement of salivary flow and subjective symptoms for xerostomic patients. Because of unwanted side effects following its systemic administration, topical pilocarpine has been paid attention as an alternative. This study aimed to investigate effects of pilocarpine solution as mouthwash on salivary flow and adverse effects compared to systemic administration of 5 mg pilocarpine tablet in healthy subjects. Methods: The study was a double blind, placebo-controlled, crossover clinical trial. Five milligrams pilocarpine tablets, 4 mL of 2% pilocarpine solution and placebo solution were given to 12 healthy volunteers (6 males and 6 females) in a predetermined order with wash-out period of at least two days and unstimulated whole saliva was collected before and after administration of each drug. Blood pressure and pulse rate was also measured and subjective effect and potential side effects were evaluated by a self-administrated questionnaire. Results: Systemic (5 mg tablet) and topical (2% solution) use of pilocarpine significantly increased salivary flow rate in healthy subjects compared to placebo (p<0.001). In both the pilocarpine solution and tablet groups, salivary flow rates at 120 minutes after administration remained increased. Subjective effect on salivation was the largest in the pilocarpine tablet group, followed by the pilocarpine solution group (p<0.05). There was no significant difference in blood pressure and pulse rate after administration of all three drugs. Fewer side effects reported in the pilocarpine solution group than in the tablet group. Conclusions: Two percents pilocarpine solution as mouthwash increases salivary flow rate, definitely superior to placebo solution and comparable to pilocarpine tablet, with fewer side effects in healthy subjects. It indicates a possibility of pilocarpine solution as a useful alternative of pilocarpine tablets for the xerostomic patients with systemic diseases.

• The Korean Journal of Physiology
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• 제11권1호
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• pp.11-20
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• 1977

The action of pilocarpine on the sodium plus potassium activated ATPase activity in the rabbit red cell membrane has been investigated and the experiments were also designed to determine the mechanism of action of pilocarpine on the ATPase activity. The following results were observed. 1. The activity of the NaK ATPase from red cell membrane is stimulated by pilocarpine, and the concentration of pilocarpine for maximal activity is about 3 mM. The pH optimum for the pilocarpine sensitive component is 8.0. 2. The activating effect of pilocarpine on the ATPase, with a given concentration of sodium .in the medium, is increased by raising the potassium concentration but activity ratio is decreased 3. The activating effect of pilocarpine on the ATPase, with a given concentration of Potassium in the medium, is increased by raising the sodium concentration but activity ratio is decreased 4. The NaK ATPase activity is increased by small amounts of calcium but decreased by 'larger amounts. The activity ratio of the enzyme by pilocarpine is decreased by small amounts .of calcium but decreased by larger amounts. 5. The activating effect of pilocarpine on the ATPase was not related to the sulfhydryl group of cysteine, the hydroxyl group of threonine or the imidazole group of histidine. 6. The activating effect of pilocarpine on the ATPase is due to amino group and carboxyl group of the enzyme of NaK ATPase

• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.331-335
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• 1997

Xerostomia is caused by organic or functional changes affecting the salivary system at different levels. Patients suffering from xerostomia may also complain of an oral burning sensation, ulceration or soreness, difficulty in swallowing, and poor denture retention. And pilocarpine is administered orally to induce salivary secretion. In Seoul National University Hospital(SNUH) pharmacy, the pilocarpine chewing tablets are prepared and supplied to patients of xerostomia in request of the dental hospital in SNUH. And we tested the salivary flow induction and the dissolution patterns of these products in saliva by a double-blind, sequential cross-over trials to eight healthy human volunteers with placebo. The pilocarpine chewing tablet contained 5 mg of pilocarpine, and placebo consisted of same materials as test drug, but didn't contain pilocarpine. In vivo experiment, all subjects were instructed to chew as 60-80 times/min. Mixed saliva was collected in the ranges of intervals such as 0-2, 2-5, 5-10, 10-15, 15-20, 20-30, 30-45 and 45-60 min after pilocarpine chewing tablet or placebo administration. Saliva volume was measured in each collecting time interval, and saliva pilocarpine concentrations were determined by reversed phase HPLC. The 82.5 percent $(4.13{\pm}0.69\;mg)$ of pilocarpine was extracted from chewing tablets during mastication of 60-80 times per minute for 60 minutes. Among these dissolved amounts, 90 percent was extracted within 20 minutes. The salivary flow rates were more increased in a group who administered pilocarpine chewing tablet at the interval of 5-10, 10-15, 20-30 and 45-60 min rather than a placebo-group, but only extracted amount of pilocarpine at 45-60 min interval is significanly different between two groups (p<0.05). But total amounts of saliva secreted for 1 hour in two group-pilocarpine and placebo treated- were $46.36{\pm}9.72\;ml\;and\;39.09{\pm}7.81\;ml$, respectively, and were not significantly different between two groups.

• 한국치위생학회지
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• 제13권3호
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• pp.517-523
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• 2013

Objectives : The aim of the study is to investigate the antimicrobial activity of jaborandi and sorbitol to various oral microbes. Methods : Jaborandi leaves contain pilocarpine. The conditions for extraction were optimized on the basis of substances, temperatures and pHs. Total pilocarpine content after extraction was analyzed by HPLC. The herbal antimicrobial activity of jaborandi and sorbitol were evaluated for oral microbes containing ATCC 25175 S. mutans, ATCC 13419 S. salivarius, ATCC 6249 S. mitis, ATCC 33398 S. equi, ATCC 29213 S. aureus, ATCC 14053 C. albicans. Results : The optimum conditions for highest yielding extraction were pilocarpine content after boiling at $100^{\circ}C$ for 1 hour at pH 3. The level of total pilocarpine content was analyzed at 833 mg/kg by HPLC. The most effective antimicrobial activity was obtained by combination of pilocarpine and sorbitol rather than pilocarpine, menthol and sorbitol, respectively. Conclusions : This results supported the preventive oral health care using safe and convenient jaborandi herb.

• 대한치과의사협회지
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• 제10권3호
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• pp.159-162
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• 1972

Body weight and weight of submandibular gland of mice given subleathal doses of puromycin were studied after Pilocarpine. 1. Body weight showed a significant decrease during the firse 10 days after puromycin alone. 2. Injections of pilocarpine abolished the increase in glandular weight of the submandibular gland. 3. This was thought to indicate the possibility that the increase in organ weight might be due to the inability of the organs to release synthesized secretory Products.

• Journal of Oral Medicine and Pain
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• 제36권1호
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• pp.21-24
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• 2011

구강건조증이란 주관적인 구강 내 건조감으로 정의되며, 이는 약물, 타액선 질환, 방사선 치료, 쉐그렌 증후군, 심리적 요인 등과 같은 다양한 원인에서 비롯된다. 구강 건조증 환자 중 현저한 타액선 기능 감소가 존재하는 경우 구강캔디다증, 치아우식증, 치주질환, 미각변화, 구취 등의 병발증이 나타날 수 있다. 이러한 구강건조증의 치료로는 우선적으로 구강건조를 유발하는 원인요소를 제거하거나, 환자의 불편감을 감소시키기 위한 대증요법이 주가 되며 실제로 타액 분비 기능이 감소된 경우 이로 인한 합병증을 예방하기 위한 치료와 타액분비를 자극할 수 있는 약물치료를 시행할 수 있다. 이 중 타액분비를 촉진시키는 약물인 필로카핀은 구강건조증 치료제로 널리 사용되어 왔다. 하지만 발한작용, 비뇨기 및 위장관계의 비정상적인 기능유도, 심혈관계 및 호흡기계에 대한 위험 등의 부작용이 있어 천식, 만성폐질환, 심혈관계 질환자에게는 주의 깊은 사용이 요구되며, 특히 조절되지 않는 천식환자의 경우 필로카핀의 절대적 금기증으로 사용이 금지된다. 이처럼 구강건조증 치료에 있어 필로카핀은 부작용으로 인해 전신적인 투여에 많은 제한이 있다. 따라서, 필로카핀의 부작용을 최소화하기 위해 국소적으로 사용되는 방법 중의 하나인 필로카핀 양치액을 이용하여 치료한 증례를 통해 그 효과를 확인해보고자 하였다.

• Annals of Clinical Neurophysiology
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• 제2권2호
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• pp.119-124
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• 2000

Background : We studied EEG changes during pilocarpine-induced status epilepticus(SE), a widely used model whose EEG characteristics have not been fully described previously. Methods : Male Sprague-Dawley rats weighing 250-350 grams were used as subjects. SE was induced 5-7 days after placement of chronic epidural electrodes, using 360-380 mg/Kg pilocarpine IP. Rats were observed with continuous EEG recording following pilocarpine injection until end of the SE episode. Results : SE occurred in 10/12 rats studied. SE began with a series of discrete seizures $11.1{\pm}3.93$ minutes after pilocarpine injection. $5.2{\pm}2.71$ seizures occurred over $10.9{\pm}4.62$ minutes, until the EEG converted to a waxing and waning pattern, during which the amplitude and frequency of epileptiform activity increased. After $1.4{\pm}1.82$ minutes, a pattern of continuous high amplitude rapid spiking was established. Continuous spiking continued for $3.4{\pm}0.48$ hours with a very gradual decline in amplitude and frequency, until periodic epileptiform discharges(PEDs) began to occur. The EEG consisted primarily of PEDs for another $7.4{\pm}3.09$ hours, until electrographic generalized seizures began to occur. These continued for $5.8{\pm}4.82$ hours until death. Duration of SE was $17.0{\pm}5.88$ hours. Flat periods were a prominent feature during all EEG patterns in this model. Conclusion : EEG features distinctive in pilocarpine SE(but not unique to it) include flat periods during all patterns and resumption of continuous spiking episodes after the onset of PEDs. The sequence of discrete seizures to waxing and waning to continuous spiking to PEDs was identical to that which has been described in humans and other animal models.

• The Korean Journal of Physiology and Pharmacology
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• 제21권1호
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• pp.125-131
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• 2017

Status epilepticus is the most common serious neurological condition triggered by abnormal electrical activity, leading to severe and widespread cell loss in the brain. Lithium has been one of the main drugs used for the treatment of bipolar disorder for decades, and its anticonvulsant and neuroprotective properties have been described in several neurological disease models. However, the therapeutic mechanisms underlying lithium's actions remain poorly understood. The muscarinic receptor agonist pilocarpine is used to induce status epilepticus, which is followed by hippocampal damage. The present study was designed to investigate the effects of lithium post-treatment on seizure susceptibility and hippocampal neuropathological changes following pilocarpine-induced status epilepticus. Status epilepticus was induced by administration of pilocarpine hydrochloride (320 mg/kg, i.p.) in C57BL/6 mice at 8 weeks of age. Lithium (80 mg/kg, i.p.) was administered 15 minutes after the pilocarpine injection. After the lithium injection, status epilepticus onset time and mortality were recorded. Lithium significantly delayed the onset time of status epilepticus and reduced mortality compared to the vehicle-treated group. Moreover, lithium effectively blocked pilocarpine-induced neuronal death in the hippocampus as estimated by cresyl violet and Fluoro-Jade B staining. However, lithium did not reduce glial activation following pilocarpine-induced status epilepticus. These results suggest that lithium has a neuroprotective effect and would be useful in the treatment of neurological disorders, in particular status epilepticus.

• 대한약리학회지
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• 제5권2호
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• pp.135-140
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• 1969

In order to investigate the effect of autonomic nervous system on salivary gland, the authors have observed the effects of various drugs acting on the autonomic nervous system to the rat submaxillary gland by comparing the changes of gland weight, the amylase activity and various electrolyte contents with control group. The results are as follows; 1. The pilocarpine, physostigmine, norepinephrine, atropine and DMPP increased the rat submaxillary gland weight. 2. The amylase activities of rat submaxillary gland were increased by pilocarpine, physostigmine and norepinephrine, but decreased by atropine and DMPP. 3. Calcium contents of rat submaxillary gland were highly increased by pilocarpine and physostigmine, hut slightly increased by norepinephrine. 4. Magnesium contents of rat submarillary gland were increased by DMPP, but decreased by pilocarpine, physostigmine and norepinephrine. 5. Sodium contents of rat subnaxillary gland were increased by pilocarpine, physostigmine, norepinephrine and DMPP, but decreased by atropine. 6. Potassium contents of rat submaxillary gland were highly increased by atropine, and slightly increased by DMPP and norepinephrine, but decreased by pilocarpine and physostigmine.