15 patients with mild to moderate chronic renal failure treated in the medical examination of friendship hospital during 1996-1998. Benazepril was administrated at dose of 1 tablet every morning. The study found that after 6 months of treatment the blood creatinine concentration and glomerular filtration level were not different from these at the beginning of treatment which prove the capacity of delaying the progress of chronic renal failure. 12/15 patients had a significant reduction of 24 hours urinary protein. 3/15 patients had a negative urinary protein after 6 months of the treatment.
Kidney Failure, Chronic ; Benzazepines

OBJECTIVETo prepare Form A and Form B of benazepril hydrochloride and to compare the differences in spectrums, thermodynamics and crystal structure between two polymorphic forms.

METHODSForm A and Form B of benazepril hydrochloride were characterized by Fourier transform infrared spectroscopy (IR), thermal gravimetric analysis (TG), differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD) and single crystal x-ray diffraction (SCXRD).

RESULTSPreparation method, crystal structure and polymorphic stability of Form A and Form B of benazepril hydrochloride were obtained. Based on the analysis of crystal structure of both polymorphs, Form A belonged to monoclone space group P2(1) with a=7.8655(4)Å, b= 11.7700(6)Å, c= 13.5560(7)Å, β= 102.9470(10)°, V=1223.07 (11)Å(3) and Z=2, while Form B belonged to orthorhombic space group P212121, with a=7.9353(8)Å, b=11.6654(11)Å, c=26.6453(16)Å, V=2466.5(4)Å(3) and Z=4. From the DSC and XRD results, Form B of benazepril hydrochloride could be transformed into Form A after heating treatment.

CONCLUSIONForm A and Form B of benazepril hydrochloride are both anhydrous and displayed different polymorphs due to different molecular configuration. Furthermore, Form A exhibits more stable than Form B at high temperatures.

OBJECTIVE: In humans, a single exposure to phencyclidine (PCP) can induce a schizophrenia-like psychosis which can persist for up to two weeks. In rats, an acute dose of PCP increases dopaminergic activity and causes changes in dopamine related behaviours some of which are sexually dimorphic. To better understand the effects of PCP on dopamine receptor adaptations in the short term we examined dopamine D1-like receptors (D1R) and D2-like receptors (D2R) in the mesolimbic and nigrostriatal dopamine pathways, 4 hours after exposure to PCP in female rats. METHODS: Animals received a single dose of 40 mg/kg PCP and were sacrificed 4 hours later. In vitro autoradiography was carried out using [3H] SCH 23390 and [3H] raclopride that target D1R and D2R respectively, in cryostat brain sections. RESULTS: Two way analysis of variance (ANOVA), revealed an overall effect of PCP treatment (F [1,63]=9.065; p=0.004) on D1R binding with an 18% decrease (p<0.01) in binding in the medial caudate putamen. PCP treatment also had an overall effect on D2R binding (F [1,47]=5.450; p=0.024) and a trend for an increase in D2R binding across all the brain regions examined. CONCLUSION: These results suggest opposing D1R and D2R adaptations in striatal subregions of female rats following acute exposure to PCP that may occur through indirect mechanisms.
Animals ; Autoradiography ; Benzazepines ; Brain ; Dopamine ; Female ; Humans ; Phencyclidine ; Psychotic Disorders ; Putamen ; Raclopride ; Rats ; Receptors, Dopamine

BACKGROUND: Varenicline is recently known as smoking cessation medicine has no results of researches conducted in the actual practice settings except for incipient clinical trials. This research attempted to analyze the factors for smoking cessation by using Varenicline prescribed in the family clinic, and the efficacy of Varenicline. METHODS: Brief smoking cessation education was conducted on 140 people who visited the Department of Family Medicine at Dankook University and Varenicline was prescribed for them. This research checked whether smoking was stopped or not after six months and analyzed the factors for succeeding in smoking cessation. RESULTS: Varenicline was prescribed for the 140 people. After six months, 46 smokers were successful in smoking cessation, representing the rate of success of 35.4%, and after 12 months, 31 people of 83 people were successful in smoking cessation, representing the rate of success of 37.3%. The group less smoke than 24.3 cigarettes/day (the average daily smoking amount) has higher quit rate than the group more smoke than 24.3 by 4.9 times. The group takes Varenicline longer than 26.7 days (the average Varenicline dosage period) has higher quit rate than the group takes Varenicline shorter than 26.7 by 4 times. Smoking-cessation rate was 4.5 times when trying to stop smoking by the doctor's recommendation. It was higher than when trying to stop smoking by self-determination. In the multivariate analysis, there were significant relationships in daily smoking amount, dosage and period of Varenicline, and motivation of visits. CONCLUSION: Varenicline is one of the useful medication for quitting smoking in family practice setting. Better compliance of medicine shows better quitting rate.
Benzazepines ; Compliance ; Family Practice ; Humans ; Motivation ; Multivariate Analysis ; Quinoxalines ; Smoke ; Smoking ; Smoking Cessation ; Varenicline

Hyponatremia is the most common electrolyte disorder in hospitalized patients. Many studies documented that it was related to increased morbidity and mortality in patients with congestive heart failure, liver cirrhosis, and neurologic diseases. Although knowledge of hyponatremia has been cumulated, the optimal management of hyponatremia remains incompletely established in clinical practice because of the diversity of underlying disease states, and its multiple causes with differing pathophysiologic mechanisms. Since vasopressin receptor antagonists have unique aquaretic effect to selectively increase electrolytes-free water excretion, clinicians could apply a more effective method to treat hyponatremia. Tolvaptan has significant evidence that it improves serum sodium levels in patients with euvolemic or hypervolemic hyponatremia related with heart failure, cirrhosis or syndrome of inappropriate anti-diuretic hormone. Tolvaptan has acceptable safety and tolerability for long-term usage in chronic hyponatremia, and the beneficial effects on serum Na+ occurred in patients with both mild and marked hyponatremia.
Benzazepines ; Fibrosis ; Heart Failure ; Humans ; Hyponatremia ; Liver Cirrhosis ; Receptors, Vasopressin ; Sodium ; Water

Repeated psychostimulants induce electroencephalographic (EEG) changes, which reflect adaptation of the neural substrate related to dopaminergic pathways. To study the role of dopamine receptors in EEG changes, we examined the effect of apomorphine, the dopamine D1 receptor antagonist, SCH-23390, and the D2 receptor antagonist, haloperidol, on EEG in rats. For single and repeated apomorphine treatment groups, the rats received saline or apomorphine for 4 days followed by a 3-day withdrawal period and then apomorphine (2.5 mg/kg, i.p.) challenge after pretreatment with saline, SCH-23390, or haloperidol on the day of the experiment. EEGs from the frontal and parietal cortices were recorded. On the frontal cortex, apomorphine decreased the power of all the frequency bands in the single treatment group, and increased the theta (4.5~8 Hz) and alpha (8~13 Hz) powers in the repeated treatment group. Changes in both groups were reversed to the control values by SCH-23390. On the parietal cortex, single apomorphine treatment decreased the power of some frequency bands, which were reversed by haloperidol but not by SCH-23390. Repeated apomorphine treatment did not produce significant changes in the power profile. These results show that adaptation of dopamine pathways by repeated apomorphine treatment could be identified with EEG changes such as increases in theta and alpha power of the frontal cortex, and this adaptation may occur through changes in the D1 receptor and/or the D2 receptor.
Animals ; Apomorphine ; Benzazepines ; Dopamine ; Electroencephalography ; Haloperidol ; Rats ; Receptors, Dopamine ; Receptors, Dopamine D1 ; Receptors, Dopamine D2

We previously demonstrated that repeated exposure to extremely low frequency magnetic fields (ELF-MF) increases locomotor activity via stimulation of dopaminergic D1 receptor (J. Pharmacol. Sci., 2007;105:367-371). Since it has been demonstrated that activator protein-1 (AP-1) transcription factors, especially 35-kDa fos-related antigen (FRA), play a key role in the neuronal and behavioral adaptation in response to various stimuli, we examined whether repeated ELF-MF exposure induces FRA-immunoreactivity (FRA-IR) in the striatum and nucleus accumbens (striatal complex) of the mice. Repeated exposure to ELF-MF (0.3 or 2.4 mT, 1 h/day, for consecutive fourteen days) significantly induced hyperlocomotor activity and FRA-IR in the striatal complex in a field intensity-dependent manner. ELF-MF-induced FRA-IR lasted for at least 1 year, while locomotor activity returned near control level 3 months after the final exposure to ELF-MF. Pretreatment with SCH23390, a dopaminergic D1 receptor antagonist, but not with sulpiride, a dopaminergic D2 receptor antagonist, significantly attenuated hyperlocomotor activity and FRA-IR induced by ELF-MF. Our results suggest that repeated exposure to ELF-MF leads to prolonged locomotor stimulation and long-term expression of FRA in the striatal complex of the mice via stimulation of dopaminergic D1 receptor.
Animals ; Benzazepines ; Magnetic Fields ; Magnetics ; Magnets ; Mice ; Motor Activity ; Neurons ; Nucleus Accumbens ; Sulpiride ; Transcription Factor AP-1 ; Transcription Factors

BACKGROUND: Varenicline is an effective smoking cessation aid. However, smokers prescribed with varenicline do not always receive varenicline for 12 weeks, as recommended. This study analyzed the subjects who received varenicline and investigated the effect of varenicline treatment duration on the success rate of 6-month smoking cessation. METHODS: This study retrospectively analyzed 78 subjects, who received varenicline, out of the 105 smokers that had visited the smoking cessation clinic after medical examination from September 2007 to December 2009. RESULTS: The subjects were all males. Twenty-two subjects (28.2%) had varenicline treatment for 12 weeks or longer; 18 subjects (23.1%) for 8~12 weeks; 22 subjects (28.2%) for 4~8 weeks; and 16 subjects (20.5%) for less than 4 weeks. The total success rate of the 6-month smoking cessation was 47.4%. The success rate of the 6-month smoking cessation was 63.6% in the group that received varenicline for 12 weeks or longer, which was higher than 41.1% of the group that early terminated the varenicline treatment (p=0.074). The period of varenicline treatment was extended for one more week, the odds ratio of the 6-month smoking cessation success increased to 1.172-folds (p=0.004; 95% confidence interval, 1.052~1.305). Adverse events occurred in 30.8% of the subjects who received varenicline, but no serious adverse events were found. CONCLUSION: If varenicline treatment period is extended, the odds ratio of the success rate for the 6-month smoking cessation increases. Therefore, an effort to improve drug compliance for varenicline in clinical practices could be helpful for the long-term success of smoking cessation.
Benzazepines ; Compliance ; Health Promotion ; Humans ; Male ; Medication Adherence ; Odds Ratio ; Quinoxalines ; Retrospective Studies ; Smoke ; Smoking ; Smoking Cessation ; Varenicline

Craving has been well known to be the most important clinical phenomenon in smoking cessation treatment and one that physicians always encounter. For successful and prolonged abstinence, understanding, evaluation, and management of craving are essential. The concept and definition of craving is still under debate, although its importance, relevance, and role in smoking relapse is evident. There are two types of craving, 'abstinence-induced craving' and 'cue-induced craving' according to time dynamic and causes. The evaluation of craving mainly depends on self-reported measures in the clinical field. Pharmacological treatments such as the nicotine patch, bupropion, and varenicline are effective for abstinence-induced craving. Psychosocial treatment and a few pharmacological agents such as nicotine gum and lozenges are useful for reducing cue-induced craving. This review was aimed at conveying up-to-date information on the characteristics, evaluation, and treatment of craving. Development of objective measurement tool for evaluation of craving is needed. The effects of pharmacological treatments on 'cue-induced craving' remain to be discovered. An active effort to alleviate each type of craving is necessary to enhance and prolong a patient's abstinence.
Benzazepines ; Bupropion ; Gingiva ; Nicotine ; Quinoxalines ; Recurrence ; Smoke ; Smoking ; Smoking Cessation ; Tobacco Use Cessation Products ; Tobacco Use Disorder ; Varenicline

To explore the role of D(1)-dopamine receptor in the modulation of basic respiratory rhythm, neonatal (0-3 d) Sprague-Dawley rats of either sex were used. The medulla oblongata slice was prepared and the surgical procedure was performed in the modified Kreb's solution (MKS) with continuous ventilating 95% O2 and 5% CO2 and ended in 3 min. A 600-700 mum single transverse slice containing the hypoglossal nerve roots and some parts of the ventral respiratory group was cut. The preparation was quickly transferred to a recording chamber and continuously perfused with oxygen-saturated MKS at a rate of 4-6 mL/min at 27-29 degrees C. Ten medulla oblongata slice preparations were randomly divided into two groups. In group I, the preparations were perfused with perfusion solution containing D(1)-dopamine receptor specific agonist cis-(+/-)-1-(Aminomethyl)-3,4-dihydro-3-phenyl-1H-2-Benzopyran-5,6-Diolhy-drochlo-ride (A68930, 5 mumol/L) for 10 min first; after washing out, the preparations were then perfused with perfusion solution containing D(1)-dopamine receptor specific antagonist R(+)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH-23390, 2 mumol/L) for 10 min. In group II, after perfusion with A68930 for 10 min, the preparations were perfused with additional A68930 + SCH-23390 for 10 min. Respiratory rhythmical discharge activity (RRDA) of the rootlets of hypoglossal nerve was recorded by suction electrodes. The results showed that A68930 shortened the respiratory cycle (RC) and expiratory time (TE) with an increase in the integral amplitude (IA). However, SCH-23390 significantly prolonged RC and TE, and decreased IA with a decrease in inspiratory time (TI). Moreover, the effect of A68930 on the respiratory rhythm was partially reversed by additional application of A68930 + SCH-23390. These results indicate that D(1)-dopamine receptor is possibly involved in the modulation of the RRDA in the isolated neonatal rat brainstem slice.
Animals ; Animals, Newborn ; Benzazepines ; pharmacology ; Biological Clocks ; Chromans ; pharmacology ; Female ; In Vitro Techniques ; Male ; Medulla Oblongata ; physiology ; Rats ; Rats, Sprague-Dawley ; Receptors, Dopamine ; physiology ; Respiration