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PubMedDate not supplied

[The effects of intracerebral injections of kynurenine on conditioned reflex activity and on the serotonin level of the blood in dogs].

Higher nervous activity of dogs was studied by classical Pavlovian method of alimentary salivary conditioned reflexes and serotonin content in blood was measured. Kynurenine sulfate in a dose of 300 + 300 mkg (bilaterally) was injected in the dorsal hippocampus region through chemiotrodes. In most cases the injection of the substance led to changes towards excitation (increase of conditioned and unconditioned alimentary salivation in the day of injection and the next day) and also to a rise of serotonin content in animals blood.

Animals↗
PubMed1990

Patient selection criteria for electrostimulation of salivary production in the treatment of xerostomia secondary to Sjogren's syndrome.

Electrostimulation has been introduced as a technique for increasing salivary output in the treatment of patients with xerostomia (dry mouth) secondary to Sjogren's syndrome. The procedure uses an electrostimulation device (salivation electrostimulator) to increase salivary production from existing glandular tissue. The device delivers a low-voltage electrical stimulus to the mouth via a probe. Patients with residual salivary tissue in the oral and pharyngeal regions who demonstrate a decrease in the flow rate of saliva are potential candidates for this procedure. It is estimated that more than one million people in the United States, predominantly middle-aged and elderly women, suffer from Sjogren's syndrome. Patients with chronic xerostomia complain of a continual feeling of oral dryness and have difficulty eating dry foods. These patients are susceptible to increased caries, oral pain, infection, and have difficulty speaking, chewing, and swallowing. The approach to the treatment of xerostomia in Sjogren's patients is usually determined by the level of severity of the symptoms. Appropriate management of patients with xerostomia requires that those patients whose salivary flow can be increased by means of sialagogues be distinguished from those patients whose salivary flow is either unaffected or insufficiently stimulated. To alleviate some of the complications due to salivary dysfunction in those patients who respond to stimuli, pharmacologic sialagogues as well as sialagogues that include sugarless gums, mints and candies are prescribed in order to increase salivary flow. Recently, electrostimulation via a hand-held stimulus probe has been introduced as a method of treatment in xerostomia secondary to Sjogren's syndrome.(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗
PubMed1992

Behavioral characterization of the new potent nonselective dopamine agonist pergolide.

Pergolide (LY127809, CAS 66104-23-2), a non-selective dopamine agonist, was evaluated for broad behavioral properties in a wide range of pharmacological tests. The selective dopamine2(D2) agonist, bromocriptine, served as a reference standard for those tests where behavioral activity was noted with pergolide. Pergolide and bromocriptine were administered orally to mice at doses of 0.3-30 and 3-300 mg/kg, respectively. Both compounds produced biphasic effects on spontaneous activity, increased hexobarbital-induced sleep time, and lowered mouse body temperature. Qualitative changes with pergolide were observed with some mice showing hyporeactiveness, ptosis, slowed respiration and placing loss. Reserpine-induced hypothermia was reversed by pergolide with significant increases in the body temperature of reserpine-treated mice. However, a further reduction in the body temperature of reserpinized hypothermic mice was seen following bromocriptine administration. Acetic acid-induced writhing and performance on the rotarod were both impaired by higher doses of pergolide. Bromocriptine administration also reduced writhing at higher doses but did not alter performance on the rotarod. Pergolide had no effect on seizure activity as evaluated by electroshock, pentylenetetrazol (pentetrazol) or strychnine. Oxotremorine-induced tremors and salivation, grip strength, and tail-flick were not affected by pergolide. Neither pergolide nor bromocriptine altered established shuttle-avoidance behavior in rats at oral doses of 0.1 to 30 mg/kg. Behavioral assessment of pergolide in dogs was complicated by severe emetic responses at clinically relevant doses greater than 0.003 mg/kg. In summary, these data suggest that pergolide produces a behavioral profile which is characteristic of dopaminergics.(ABSTRACT TRUNCATED AT 250 WORDS)

Analgesics↗
PubMed1992

[Odontostomatological changes induced by drugs. I].

The purpose of the present review is to describe the unwanted effects of drugs or chemicals in the orofacial region. The authors take into consideration the alterations of salivation such as xerostomia and ptyalism, disturbances of sense of taste, halitosis and pain and swelling of the salivary glands. The dental surgeon who suspects that an oral alteration might be a drug reaction can play an important role in preventing the development of more severe toxic effects. All this points to the importance of the knowledge of pharmacology for dental practitioners.

Drug-Related Side Effects and Adverse Reactions↗
PubMed2005

Sialorrhea: a review of a vexing, often unrecognized sign of oropharyngeal and esophageal disease.

Saliva is produced by the major salivary glands (parotid, submandibular, and sublingual), as well as several smaller glands. Salivary flow can be altered by multiple entities. There is much written regarding xerostomia ("dry mouth"), the condition related to inhibited or decreased salivary flow. This condition is widely recognized in certain systemic diseases, particularly Sjögren syndrome, diabetes mellitus, after anticholinergic, antihistamine, and decongestant medications, as well as states of enhanced sympathetic drive, such as anxiety or emotional disturbances and various other psychosocial conditions. On the other hand, sialorrhea or ptyalism, the condition of increased salivary flow, is rarely discussed in the clinical literature. Sialorrhea can occur with various neurologic disorders, infections, the secretory phase of the menstrual cycle, heavy metal poisoning, Wilson disease, Angelman syndrome, as well as a relatively unknown condition called idiopathic paroxysmal sialorrhea. Normal salivation may be altered by drugs (such as clozapine, risperidone, nitrazepam, lithium, and bethanecol) that have a cholinergic effect that induces sialorrhea. This report focuses on sialorrhea as it relates to disorders of the oropharynx and esophagus. The patient typically recognizes a problem with excessive "foamy mucus" but does not understand its origin. Infections and obstruction are the most common oropharyngeal causes. Increased salivary flow occurs as a typically subtle manifestation of gastroesophageal reflux disease. This occurrence is referred to as water brash. Idiopathic achalasia and megaesophagus due to the parasite Trypanosoma cruzi are regularly associated with sialorrhea. Esophageal obstruction (foreign body, cancer, or stricture formation), infection, and nasogastric intubation are the more common conditions associated with the symptomatic sequelae of sialorrhea. Sialorrhea-related respiratory and pulmonary complications are greatest in those with a diminished sensation of salivary flow and hypopharyngeal retention. Extremes of age, the chronically debilitated, or those in chronic care facilities, especially associated with cerebrovascular accidents and esophageal cancer, typically comprise this population. For the patient with an intact awareness of saliva, sialorrhea can present with significant social stigmas. Occult drooling or regular oral evacuation into a tissue or "spit cup" is socially incapacitating. This report provides a review of the physiology, pathogenesis, clinical manifestations, and therapeutic options for sialorrhea. Physicians and other healthcare professionals should recognize the importance of sialorrhea as a possible indicator or complication of a variety of disease states of the oropharynx and esophagus as well as its impact on the patient's physical and social quality of life.

Animals↗
PubMedDate not supplied

Autonomic disorders in cluster headache syndrome.

The unilateral headache in patients with cluster headache syndrome is associated with a number of autonomic accompanying phenomena. Investigation of sweating of the forehead, salivation, nasal secretion and tearing is described and sympathetic parasympathetic firing in connection with headache attacks is discussed.

Arousal↗
PubMedDate not supplied

Pathophysiology and management of radiation-induced xerostomia.

Radiotherapeutic treatment of head and neck cancer patients often causes long-term dysfunction involving their salivary function, swallowing capabilities, and taste. Salivary gland dysfunction from radiation therapy is often the most unpleasant side effect of treatment. This article will review current knowledge concerning the anatomy and function of glands involved with salivation, measurement of salivary gland function, surgical and pharmacologic prevention and treatment of xerostomia, and methods to administer radiation while causing the least amount of damage to salivary glands.

Acupuncture Therapy↗
PubMed2006

[Salivary glands secretory activity in patients with terminal chronic renal insufficiency on programmed dialysis].

Saliva secretion speed and some biochemical mixed saliva characteristics were studied in patients with a terminal stage of chronic renal insufficiency. There was reduction of salivary function by more than 2 times and an increase of urea and creatinine concentrations in mixed saliva before the dialysis start. In case of higher urea content in saliva the speed of salivation was the highest that could evidence for an adequate response of the salivary glands to toxic action of nitrogen metabolism end products. The function restoration after hemodialysis took place not in all the patients. Amino acid catabolism product concentration in mixed saliva fell after hemodialysis and correlated directly with the amount of urea and creatinine in blood plasma. It took place also in "urea ricochet" when its content in blood increased sharply 1 hour after hemodialysis due to urea washout from the tissues.

Adult↗
PubMedDate not supplied

Reduction of sleep bruxism using a mandibular advancement device: an experimental controlled study.

PURPOSE: The objective of this experimental study was to compare the effect on sleep bruxism and tooth-grinding activity of a double-arch temporary custom-fit mandibular advancement device (MAD) and a single maxillary occlusal splint (MOS). MATERIALS AND METHODS: Thirteen intense and frequent bruxors participated in this short-term randomized crossover controlled study. All polygraphic recordings and analyses were made in a sleep laboratory. The MOS was used as the active control condition and the MAD was used as the experimental treatment condition. Designed to temporarily manage snoring and sleep apnea, the MAD was used in 3 different configurations: (1) without the retention pin between the arches (full freedom of movement), (2) with the retention pin in a slightly advanced position (< 40%), and (3) with the retention pin in a more advanced position (> 75%) of the lower arch. Sleep variables, bruxism-related motor activity, and subjective reports (pain, comfort, oral salivation, and quality of sleep) were analyzed with analysis of variance and the Friedman test. RESULTS: A significant reduction in the number of sleep bruxism episodes per hour (decrease of 42%, P < .001) was observed with the MOS. Compared to the MOS, active MADs (with advancement) also revealed a significant reduction in sleep bruxism motor activity. However, 8 of 13 patients reported pain (localized on mandibular gums and/or anterior teeth) with active MADs. CONCLUSIONS: Short-term use of a temporary custom-fit MAD is associated with a remarkable reduction in sleep bruxism motor activity. To a smaller extent, the MOS also reduces sleep bruxism. However, the exact mechanism supporting this reduction remains to be explained. Hypotheses are oriented toward the following: dimension and configuration of the appliance, presence of pain, reduced freedom of movement, or change in the upper airway patency.

Adult↗
PubMed1991

Assessment of toxicosis induced by high-dose administration of milbemycin oxime in collies.

Fifteen Collies, previously having mild reactions to ivermectin challenge (120 micrograms/kg of body weight; 20 times the recommended dosage level), were studied to evaluate the effects of milbemycin oxime administration at 5 and 10 mg/kg (10 and 20 times the manufacturer's recommended dosage). Five replicates, comprising 3 dogs each, were formed on the basis of body weight. Within replicates, each dog was randomly allocated to treatment with 5 or 10 mg of milbemycin/kg or served as a untreated control. Dogs were examined repeatedly for signs of toxicosis for 4 days after treatment and daily thereafter. Two of 5 dogs treated at 5 mg/kg (10x) developed signs of mild depression on the day of treatment, but were normal 24 hours after treatment. All 5 dogs treated at 10 mg/kg (20x) developed signs of mild depression and ataxia by 6 hours. Signs persisted for 24 hours in 3 dogs. Two of these dogs also had mydriasis, whereas 3 salivated excessively. All dogs recovered completely by day 2 after treatment. The results of this study demonstrated that Collies sensitive to the effects of 120 micrograms of ivermectin (20x)/kg show similar sensitivity to the effects of milbemycin oxine administered at 10 mg/kg (20x). We conclude that ivermectin and milbemycin commercial formulations have similar margins of safety and that milbemycin toxicosis appears to be dose-dependent in Collies with a demonstrated sensitivity to ivermectin.

Animals↗
PubMed1990

Central effect of the potent long-acting H1-antihistamine levocabastine.

The effects of levocabastine (R 50 547; CAS 79516-68-0) on the central nervous system were studied in comparison with those of diphenhydramine, ketotifen and azelastine. At high doses, levocabastine caused a decrease in locomotor activity, prolongation of thiopental-induced sleep, depression of acetic acid-induced writhing in mice and inhibition of active avoidance response in rats, but these adverse effects were much less potent than those seen in diphenhydramine, ketotifen and azelastine. Oxotremorine-induced tremor and salivation in mice were delayed after extremely high dosage of levocabastine; however, these were much less effective than those seen after diphenhydramine and ketotifen. Levocabastine did not affect the tonic extensor seizure induced by maximal electroshock in mice which is different from that of diphenhydramine. In EEG analysis, levocabastine at a dose of 20 mg/kg caused no significant changes in the EEG recorded from the frontal cortex, occipital cortex, hippocampus and amygdala in rats with chronic electrodes.

Acetates↗
PubMed1991

Enantiomers of oxybutynin: in vitro pharmacological characterization at M1, M2 and M3 muscarinic receptors and in vivo effects on urinary bladder contraction, mydriasis and salivary secretion in guinea pigs.

The major side effects of racemic oxybutynin (OXY), which is used in the treatment of urinary incontinence are dry mouth (xerostomia) and blurred vision (mydriasis). Highly purified enantiomers of OXY [(R)OXY, (S)OXY] were compared with the racemate both in vitro in functional studies and in vivo in guinea pigs to evaluate their pharmacological action relative to their adverse effects. The affinity of (R)OXY and (S)OXY for different muscarinic receptor subtypes was determined using field stimulated rabbit vas deferens (M1) and guinea pig atria (M2) or bladder (M3) strips. Stereoselective antimuscarinic effects [(R)OXY greater than or equal to (R/S) OXY much greater than (S)OXY] were evident at all three receptor subtypes; the isomeric ratio [(S)OXY/(R)OXY] ranged from 12 to 88. Both (R)OXY and (R/S)OXY were slightly more selective (2-4-fold, P less than .01) for M1 and M3 relative to M2 muscarinic receptors. Stereoselectivity was also evident in vivo for volume-induced urinary bladder contractions as measured by cystometrogram parameters [(S)OXY/(R)OXY approximately 21], mydriasis [(S)OXY/(R)OXY approximately 136] and salivary gland secretory responses [(S)OXY/(R)OXY approximately 30]. The absolute potencies of (R)OXY or (R/S)OXY for mydriasis and salivation were similar to those for inhibition of intravesical bladder pressure. Also, (R)OXY and (R/S)OXY equipotently antagonized cholinergic-mediated CNS effects in mice. Collectively, the data suggest that the activity of (R/S)OXY resides predominantly in the (R)-enantiomer. However, it appears that (R)OXY may offer no significant pharmacological advantage over (R/S)OXY in terms of its principal therapeutic and side effect profile.

Animals↗
PubMed1990

Metrifonate in healthy volunteers: interrelationship between pharmacokinetic properties, cholinesterase inhibition and side-effects.

Metrifonate concentrations in plasma, its inhibition of blood cholinesterase, and side-effects were studied in 16 healthy volunteers who received a single oral dose of 2.5, 5, 7.5 or 15 mg/kg in a randomized double-blind study (4 subjects for each dose). Metrifonate was determined by a gas chromatographic method. Peak plasma levels were reached within 2 hours; the half-life in plasma, oral clearance, and normalized Cmax and AUCs did not differ significantly between the four groups. Plasma cholinesterase (BuchE) was inhibited to low levels in all subjects, while erythrocyte cholinesterase (AchE) was affected in a dose-dependent fashion. The occurrence of side-effects correlated strongly with peak plasma levels but not with maximum AchE inhibition or with increase in salivation. This study shows that the absorption of metrifonate was not significantly different for doses between 2.5 and 15 mg/kg. The plasma levels of this drug correlated with the occurrence of side-effects.

Adult↗
PubMed1990

[Basic investigation of saliva SIgA].

Saliva, which contributes to maintaining health in the oral environment, is affected by the physiological functions of the organism and their condition. Dental caries and periodontosis, both of which are oral diseases with frequent occurrence, require the presence of bacteria to occur. SIgA (secretory IgA), an immune globulin that is found in large quantities in substances secreted during salivation, has an antibacterial action. Thus, in conducting a basic investigation on the relationship between these factors, the author investigated what effect the speed of saliva secretion, a physiological factor of the saliva component, has on the SIgA value. Results showed that, regarding the relationship between the salivary SIgA value and the speed of salivary secretion, a negative correlation exists although this is weak in terms of relevance. The fact that the correlation displayed a tendency toward scattering indicates a need to pay attention when measuring the elements in the saliva to those factors that evidently have an effect on the composition of the saliva.

Humans↗
PubMed1990

Enhanced sensitivity to behavioral effects of naltrexone in rats.

Rats were trained on a fixed-ratio schedule under which every 30th response produced food reinforcement. Five 3-min periods of fixed-ratio reinforcement were each preceded by a 10-min time-out in which responding had no scheduled consequence. Cumulative dose-effect functions for naltrexone were determined once per week by administering increasing doses during each successive time-out. Initially, only a dose of 100 mg/kg suppressed fixed-ratio responding. After eight exposures to cumulative naltrexone, however, a dose of 10 mg/kg suppressed responding. This shift to the left of the dose-effect function, or supersensitivity, persisted for at least 10-wk when naltrexone was not injected. Pretreatment with either morphine (3.0 mg/kg) or ethylketocyclazocine (0.1 and 1.0 mg/kg) partially prevented the naltrexone-induced decreases in response rates. Neither chlordiazepoxide nor [D-pen2, D-pen5]enkephalin pretreatments appreciably altered the effects of naltrexone. When cumulative doses of 1.0-10.0 mg/kg naltrexone were followed by two saline injections instead of the higher doses of naltrexone, over 8 wk, the naltrexone dose-effect function shifted back to the right. The return to normal naltrexone sensitivity after elimination of the two highest doses suggests that a reliable association between the lower and higher doses in a cumulative dosing procedure can result in conditioned effects to the lower doses. Similar observations of salivation elicited by cumulative naltrexone injections further support the hypothesis that the present naltrexone supersensitivity may involve conditioning processes.

Animals↗
PubMed1989

Studies on the salivary secretion induced by substance P in perfused submandibular gland of rat.

The purpose of these experiments was to clarify the effects of substance P (SP) on the salivary secretion in comparison with those of autonomic agents. Salivary secretion from rat submandibular gland (SMG) was induced by intravenous infusion into the femoral vein or partial perfusion of SMG with isotonic solution containing SP or autonomic stimulants. Blood and salivary flow rates, and electrolyte concentrations of saliva were measured. The relationship between electrolyte concentrations and salivary flow rate after intravenous infusion of SP was similar to that obtained using parasympathomimetic agents. Salivary flow rates induced by phenylephrine and isoproterenol were significantly increased by the further addition of SP, while the pilocarpine-induced flow rate was not affected. SP alone caused a significant increase in blood flow rate of perfused rat SMG. SP with atropine or phentolamine somewhat increased the blood flow. However, concomitant perfusion of atropine and phentolamine completely inhibited the SP effect. Salivary secretion induced by SP perfusion was reduced by atropine or phentolamine. Both blood flow elevation and salivary secretion induced by SP were reduced with increasing doses of a SP-antagonist. Also blood and salivary flow responses induced by phenylephrine were severely reduced by the SP-antagonist. On the other hand, the salivary secretion induced by pilocarpine was moderately reduced by the SP-antagonist. These results indicate that the salivation and especially the glandular vasodilation induced by SP were partially modified by the autonomic agents.

Animals↗
PubMed1989

[Excitatory responses of superior salivatory nucleus neurons to stimulation of orbital gyrus in the cat].

The responses of superior salivatory nucleus (SSN) neurons to electrical stimulation of ipsilateral orbital gyrus were investigated in ketamine anesthetized cats. A total of 52 SSN neurons were identified by the antidromic spike responses to stimulation of the right chorda tympani nerve. Thirty-three (63%) neurons responded with spikes to stimulation of the orbital gyrus. These neurons were also activated by stimulation of ipsilateral lingual nerve. Eleven (21%) neurons received the inputs from only the lingual nerve. Remaining 8 (16%) neurons failed to respond to stimulation of neither orbital gyrus nor lingual nerve. The latency of orbital cortically evoked responses was 16.5-42.0 msec (mean +/- S.D. = 28.6 +/- 6.9 msec, n = 33), and that to stimulation of lingual nerve was 6.5-15.5 msec (9.9 +/- 2.4 msec, n = 46), respectively. In this study, convergence of excitatory inputs from orbital gyrus and sensory nerve was found in 63% of SSN neurons. These inputs would play an important role in submandibular and sublingual salivation.

Animals↗
PubMed1989

General pharmacology of beraprost sodium. 2nd communication: effect on the autonomic, cardiovascular and gastrointestinal systems, and other effects.

Beraprost sodium (sodium (+/-)-(1R*,2R*,3as*,8bS*)-2,3,3a,8b-tetrahydro-2- hydroxy-1-[(E)-(3S*)-3-hydroxy-4-methyl-1-octen-6-ynyl]-1H- cyclopenta[b]benzofuran-5-butyrate, TRK-100) is an orally active epoprostenol (prostaglandin I2, PGI2) analogue. Its general pharmacological effects on peripheral organs were studied. 1. In isolated organs, beraprost sodium relaxed the trachea and increased atrial beating rate (2.4 x 10(-5) mol/l). It also dose-dependently contracted the stomach, aorta, ileum and uterus (2.4 x 10(-7)-2.4 x 10(-4) mol/l). These effects of beraprost sodium were similar, but inferior to those of PGI2 and PGE1. 2. Intravenous administration of beraprost sodium produced a dose-related decrease in blood pressure (BP), its potency being about 1/3 times that of PGI2 in anesthetized rats and dogs. Beraprost sodium and PGI2 had no effects on heart rate (HR), and enhanced respiration in conjugation with a decrease in BP. Oral administration of beraprost sodium in high doses (1-3 mg/kg in rats and 0.3 mg/kg in dogs) caused a decrease in BP. A compensatory tachycardia and an elevated plasma renin activity (PRA) occurred after low doses (0.1-0.3 mg/kg) in rats. In contrast, a change of HR and PRA in rabbits and dogs was mild. 3. Beraprost sodium produced suppression of digestive organs: markedly, gastric motility and secretion and intestinal transport; slightly, but significantly, biliary secretion. On the other hand, it enhanced ileal motility at a high dose (300 micrograms/kg i.v.). 4. Oral administration of beraprost sodium caused a decrease in urinary volume and electrolyte excretion in rats. 5. Oral administration of beraprost sodium prolonged bleeding time in mice, while it had no effect on the blood coagulation system in vitro. In addition, beraprost sodium had no hemolytic action. 6. The other effects of beraprost sodium were weak. Beraprost sodium had no local anesthetic activity and no effect on salivation, pupil size and neuromuscular transmission in the skeletal muscle. Beraprost sodium slightly contracted the uterus of non-pregnant rats in situ and dose-independently inhibited carrageenin-induced paw edema. In conclusion, beraprost sodium produced various effects on the autonomic, cardiovascular, and gastrointestinal systems. Probably, these effects may be based on its own action like PGI2.

Anesthetics, Local↗