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PubMed1986

Determination of metapramine, imipramine, trimipramine and their major metabolites in plasma by reversed-phase column liquid chromatography.

The determination of metapramine, imipramine, trimipramine and their desmethyl metabolites after alkaline diethyl ether extraction from plasma is achieved by column liquid chromatography using two internal standards and mu Bondapak C18 column. Elution is carried out isocratically at 1 or 0.6 ml min-1 with two mixtures of acetonitrile-potassium dihydrogen phosphate-distilled water (45:55:10 for metapramine and its metabolites; 45:50:5 for imipramine, trimipramine and their metabolites). Detection is monitored by absorption at 254 nm. The detection limit is less than 5 ng ml-1 for each compound. The coefficients of variation (within-day and day-to-day) for the eight compounds are less than 11.3%. Interference from several possible co-medications is discussed. The technique can be used for routine therapeutic monitoring of the antidepressants as well as analytical toxicology. However, the three antidepressants cannot be analysed simultaneously by this method because metapramine requires a different elution system and imipramine interferes with monodesmethyltrimipramine (retention times 8.90 and 8.60 min, respectively).

Antidepressive Agents, Tricyclic↗
PubMed1997

Sensitive microanalysis of imipramine and desipramine in single rat thyroids by gas chromatography-mass spectrometry.

A new sensitive method for the quantitative determination of imipramine and desipramine in single rat thyroids using gas chromatography-mass spectrometry with selected ion monitoring, after enzymatic hydrolysis and liquid-liquid extraction has been developed. The technique was deemed suitable for microanalysis of single rat thyroids and for other solid tissues, using smaller sample sizes than usually required for traditional determination methods. The quantification was linear from 10 to 200 nmol/l (i.e., from 0.25 to 5 microg/g) for imipramine and from 100 nmol/l to 2000 nmol/l (i.e., from 2.4 to 47 microg/g) for desipramine, and the limits of detection (less than 25 ng/g tissue for both compounds) were better than those previously reported. Recoveries, repeatability and reproducibility of this technique were satisfactory. It has been successfully applied in a preliminary study of the concentration-time profiles of imipramine and desipramine in the thyroid of rats treated with either of these drugs.

Animals↗
PubMed1997

Simultaneous determination of imipramine, desipramine and their 2- and 10-hydroxylated metabolites in human plasma and urine by high-performance liquid chromatography.

A simultaneous assay for imipramine, desipramine and their 2- and 10-hydroxy-metabolites using high-performance liquid chromatography (HPLC) is described. The drugs and internal standard, pericyazine, were extracted from plasma or urine at pH 9.6 with diethyl ether and back-extracted into 0.1 M orthophosphoric acid. The recovery of the compounds ranged from 78.6% for imipramine to 94.3% for 2-hydroxydesipramine. The extracts were analysed by reversed-phase HPLC with electrochemical detection using a mobile phase of 30% acetonitrile in 0.1 M K2HPO4 at pH 6.0 delivered at 2 ml/min. All compounds were resolved in a run time of 15 min with lower limits of quantification of 1.5 ng/ml for hydroxy-metabolites and 3 ng/ml for imipramine and desipramine. The intra- and inter-day coefficients of variation at 50 ng/ml were 5.2% and 6.8%, respectively (n=8).

Adult↗
PubMed2003

Determination of imipramine in presence of iminodibenzyl and in pharmaceutical dosage form.

Two spectrophotometric methods for the determination of imipramine in presence of iminodibenzyl as an impurity are described. The first method is a ratio-spectra first derivative spectrophotometry, the signals were measured at 240.2 nm for imipramine. Calibration graph was found linear in the range 5-30 microg ml(-1). The second method is based on the reaction of imipramine base, being an electron donor, with p-chloranilic acid, being pi acceptor, to form a purple colored charge transfer complex. The absorbance was measured at 520.5 nm without interference with iminodibenzyl. Both methods are rapid, simple and do not require any preliminary separation or treatment of the samples. Furthermore, the two methods were applied to pharmaceutical dosage form.

Benzylamines↗
PubMed2000

Different regulation of phospholipase D activity in glioma C6 cells by sphingosine, propranolol, imipramine and phorbol ester.

In has been found that sphingosine, propranolol, imipramine and phorbol ester (12-O-tetradecanoylphorbol-13-acetate, TPA) have a stimulatory effect on phospholipase D activity in glioma C6 cells. The cells were prelabelled with [1-(14)C]palmitic acid and phospholipase D-mediated synthesis of [(14)C]phosphatidylethanol was measured. The enhancing effect of TPA was almost completely blocked by a specific protein kinase C inhibitor, GF 109203X. In contrast, GF 109203X failed to inhibit the sphingosine, imipramine and propranolol stimulatory effects, indicating that their stimulation was independent of protein kinase C. The effect of TPA on phospholipase D was also blocked by imipramine and propranolol, whereas sphingosine additively potentiated TPA-mediated phospholipase D activity, both at shorter and longer (2-60 min) times of incubation. These results suggest that in glioma C6 cells, sphingosine is not only involved in a different phospholipase D activation than the TPA regulatory system, but also that it operates in a different compartment of the cell.

Animals↗
PubMed1998

A comparative study of sertraline versus imipramine in postpsychotic depressive disorder of schizophrenia.

The objective of this study was to compare the efficacy and reliability of sertraline versus imipramine in the treatment of postpsychotic depressive disorder of schizophrenia. The diagnosis was based on DSM-IV research criteria. The Sympson-Angus Scale and SANS were performed in order to discriminate between depressive symptoms, the extrapyramidal side-effects of neuroleptics and the negative symptoms of schizophrenia. A 10-day placebo treatment period was applied to eliminate the possible influence of the placebo effect. The degree of severity of depression was determined using the Hamilton Depression Scale and the Clinical Global Impression Scale. The patients were randomly divided into two subgroups, each consisting of 20 people, who were given either 50 mg/day sertraline or 150 mg/day imipramine, and their progress was followed for 5 weeks. The diagnosis and treatment results were evaluated using the double-blind method. In conclusion, although both drugs were found to be effective, sertraline was found to be more advantageous than imipramine in terms of rapid onset of action; frequency, severity and duration of side-effects, and relapse risk of schizophrenia.

Adult↗
PubMed1991

Affinity modulation of [3H]imipramine, [3H]paroxetine and [3H]citalopram binding to the 5-HT transporter from brain and platelets.

The dissociations of [3H]imipramine, [3H]paroxetine and [3H]citalopram from the 5-HT (serotonin 5-hydroxytryptamine) transporter were found to be markedly influenced by several drugs, although concentrations in the microM range were needed. Most of these drugs attenuated the dissociation rate, i.e. increased the affinity between the ligand and the binding site. A few increased the dissociation rate however. The binding of drugs to the affinity-modulating site was specific, although of low affinity and probably changing the conformation of the high-affinity binding site, thereby changing the fit between the ligand and the interacting amino acid side-chains. Although the drugs usually affected the dissociation rates of the three ligands in the same manner, there were some which had different effects on [3H]imipramine, [3H]paroxetine and [3H]citalopram. For example, 5-HT markedly attenuated the dissociation of [3H]imipramine, had a moderate effect on [3H]paroxetine and very little effect on [3H]citalopram dissociation. This indicates that the three ligands are bound to different domains on the 5-HT transporter. [3H]Citalopram dissociation from human brain and rat brain were differently affected by several drugs. Indalpine augmented the dissociation rate of the [3H]citalopram 5-HT transport complex in human brain but attenuated it in rat brain, thus revealing a species difference of the 5-HT transporter.

Animals↗
PubMed1987

Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues.

The M1-selective antiulcer drug pirenzepine (1) is a tricyclic compound with close resemblance to tricyclic psychotropic agents such as imipramine (2). Despite this fact, pirenzepine is devoid of any psychotropic effects, exhibiting measurable antagonistic effects in biochemical assays and receptor binding studies only toward the muscarinic receptor system. To understand how different groups in these tricyclic molecules affect binding affinities, a set of nine compounds structurally related to pirenzepine (1) and imipramine (2) has been selected for analysis, comprising three different tricycles and three different side chains. The compounds were tested for their affinity to the imipramine and muscarinic receptors in homogenized rat cortex tissue. The result of these studies suggests that it is the nature and placement of accessory groups that determine the differences in receptor recognition and the binding process. In the case of pirenzepine (1), preferential binding toward the muscarinic receptor is brought about by the endocyclic amide group, by the positioning of the protonated N atom of the side chain, and to a minor extent by the exocyclic amide group. From these findings a putative model for the explanation of selective binding of pirenzepine (1) to the muscarinic receptor has been derived.

Animals↗
PubMed2003

Long-term imipramine treatment increases nitrate levels in the rat hypothalamus.

1. Animal experiments have shown nitric oxide synthase inhibitors to have antidepressant-like properties. However, the effects of clinically available antidepressants on nitric oxide production in the brain remain unclear. In the present study, we examined whether imipramine, a conventional antidepressant, changes the levels of type-II nitric oxide synthase mRNA and nitrate, a final nitric-oxide-oxidation product measurable in vivo, in the rat brain. 2. Type-II nitric oxide synthase mRNA was detected using a reverse transcription-polymerase chain reaction method and nitrate was measured with a combination of high-performance liquid chromatography and the Griess reaction. 3. In untreated rats, type-II nitric oxide synthase mRNA was not detected in the hypothalamus, hippocampus, cerebral cortex, brain stem, or cerebellum. However, after 28-day oral administration of imipramine, it was detected in every brain region tested. Nitrate levels in the hypothalamus and cerebral cortex increased after 28-day treatment. In the hypothalamus, nitrate levels increased dose-dependently. These dose-dependent nitrate level changes were prevented by pretreatment with a nitric oxide synthase inhibitor. Moreover, the preventive effect of NG-nitro-L-arginine methyl ester was reversed by coadministration of L-arginine, a nitric oxide substrate. 4. These results suggest that chronic imipramine treatment induces nitric oxide synthase gene expression in the brain, followed by augmented NO production.

Animals↗
PubMed1994

Imipramine and sexual dysfunction during the long-term treatment of recurrent depression.

Ninety patients in the maintenance therapy phase of the Pittsburgh Study of Maintenance Therapies in Recurrent Depression (Frank et al., 1990) were studied to determine possible relationships between the type of therapy (imipramine versus no drug) and the level of sexual functioning. The level of sexual functioning was determined by a composite subscale score of the Social Adjustment Scale which assessed (1) current level of enjoyment and interest in sex; (2) change in interest; (3) current frequency of sexual intercourse; (4) change in frequency; and (5) pain and/or difficulty reaching orgasm. Loss of libido was assessed by both the Hamilton Rating Scale for Depression and the SCL-90. Logistic regression analysis revealed no relationship between treatment with active imipramine and sexual functioning for the total group, or for females alone. Analysis of males alone revealed a decreased interest in sex among those treated with imipramine, but no significant differences in frequency or problems. The implications for maintenance pharmacotherapy and the cost/benefit ratio of unacceptable side effects versus drug efficacy are discussed.

Adult↗
PubMed1999

Imipramine for successful treatment of retrograde ejaculation caused by retroperitoneal surgery.

Retrograde ejaculation is a known complication following retroperitoneal lymph node dissection. Without further therapy, achieving paternity may be impossible. We evaluated the use of the tricyclic antidepressant imipramine in a new ovarian cycle-dependent dose regime for reversal of retrograde ejaculation in 11 patients desiring fertility. Ten patients with retroperitoneal lymph node dissection performed because of testicular cancer, and one with aortic surgery (thromboendarterectomy) were treated in an open, uncontrolled study with imipramine given at a daily oral dose increasing from 25 to 50 mg for 7 days prior to the planned ejaculation or the expected ovulation of the female partner. In all 11 patients, antegrade ejaculation could be induced (sperm counts: 3.9-276.0 x 10(6)/mL). Major side-effects were not observed, but half of the patients complained of minor degrees of dizziness, weakness, nausea or sweating during medication. Under treatment, two patients with normal sperm concentrations induced a spontaneous pregnancy. One ICSI cycle each was performed in 2 patients, with successful fertilization, out no pregnancy. In conclusion, temporary oral intake of imipramine is an effective and safe treatment to re-establish antegrade ejaculation in patients with retrograde ejaculation following retroperitoneal surgery, thus providing possibilities for paternity either through intercourse or by assisted fertilization.

Adult↗
PubMed1978

[The effects of imipramine and lofepramine on EEG and their dependence on relative alpha-intensity (author's transl)].

The effects of imipramine (single dose of 100 mg orally) and lofepramine (single dose of 140 mg orally) in comparison to placebo on the EEG power spectra were examined in 24 non-selected healthy male volunteers. All subjects received the three drugs in a completely counterbalanced sequence. On the basis of their relative alpha-intensity the Ss were divided in two groups of 12 Ss each (high and low alpha-intensity). Two-way analyses of variance were computed for the absolute power in the alpha-, beta-, delta- and theta-frequency-bands. Imipramine increased the intensity of the delta-, theta- and beta-frequency-bands and decreased the power in the alpha-band. Lofepramine increased the intensity of the beta-band. The effects of imipramine and lofepramine are dependent on the relative power in the alpha-band of the Ss.

Adult↗
PubMed2003

Effects of imipramine treatment on delta-opioid receptors of the rat brain cortex and striatum.

Imipramine (CAS 113-52-0) is being utilized widely for the treatment of major depression. In recent years, there has been evidence of the involvement of the endogenous opioid system in major depression and its treatment. There is some evidence indicating that opioid receptors could be involved in the antidepressant mechanism of action. Regarding this topic, mood-related behavior of endogenous enkephalins seems to be mediated by delta-opioid receptors. In this work, the effects of subacute (5 day) and chronic (15 day) treatments of imipramine on the density and the affinity of the delta-receptors in the striatum and in the parietal and frontal cortices of the rat brain are described. Studied parameters (Bmax and Kd) were calculated by a saturation binding assay with the delta-opioid agonists [3H]-DPDPE (tyrosyl-2,6-3H(N)-(2-D-penicillamine-5-D-penicillamine)-enkephalin) as specific ligand and DSLET ([D-serine2]-D-leucine-enkephalin-threonine) as non-radioactive competing ligand. It was found that 15 days treatment significantly decreased the delta-opioid receptor density,without changing the affinity, in the frontal cortex of the rat brain. That decrease was confirmed by delta-opioid receptor immunostaining. These results suggest that delta-opioid receptors could play a role in the chronic action mechanism of imipramine.

Analgesics, Opioid↗
PubMed2003

The prototypic antidepressant drug, imipramine, but not Hypericum perforatum (St. John's Wort), reduces HPA-axis function in the rat.

Dysregulation in corticotropin-releasing hormone (CRH) secretion in the hypothalamus-pituitary-adrenal (HPA) axis may be involved in the etiology of major depressive disorder (MDD). Chronic therapy with standard antidepressant drugs, such as imipramine, can downregulate HPA axis function, indicating that the HPA axis may be an important target for antidepressant action. We tested several doses of a standardized commercial preparation of Hypericum perforatum plant extract (popularly known as St. John's Wort), a medicinal herb used for treating mild depressive symptoms, to determine whether it also modulated HPA axis function. Chronic imipramine treatment (daily injections for 8 weeks) of male Sprague-Dawley rats significantly downregulated circulating plasma levels of adrenocorticotropic hormone (ACTH) and corticosterone compared to animals treated with saline. However, chronic St. John's Wort treatment (daily gavage for 8 weeks) had no effect on plasma ACTH or corticosterone, even at the highest doses tested. Our results confirm previous findings that imipramine may have significant peripheral HPA axis-mediated effects. However, our data does not support any role for H. perforatum in modulation of HPA axis function, suggesting that alternative pathways may be involved in mediating its antidepressant effects.

Adrenal Glands↗
PubMed1991

Adinazolam, diazepam, imipramine, and placebo in major depressive disorder: a controlled study.

In summary, the clinical results of this double-blind study clearly show that imipramine, as expected, demonstrated significant antidepressive properties in outpatients suffering from major depressive disorders. In contrast, adinazolam showed rather mild and weak antidepressive properties, and in no measures did its response differ significantly from that of diazepam. These findings are quite in contrast to those obtained by the authors in an earlier study with alprazolam (Rickels et al., 1987) in which alprazolam and imipramine produced rather similar results and both were significantly better than placebo, while diazepam was not. While the rather high dropout rate may well be considered a limitation of the study, the dropout rate is equally distributed between all four treatments. And since both decreasing sample size and endpoint analyses which include all patients with at least one week data, provide rather similar results, the findings can be considered as robust despite the high dropout rate. While the authors consider those findings the most robust in which endpoint and completer analyses results are rather similar, when high dropout rates occur, endpoint analyses should be given more weight than completer analyses as they are more representative of actual clinical practice. The present findings therefore suggest that adinazolam clearly possesses less antidepressive properties than imipramine and not more than diazepam and these findings are in agreement with other studies which found lack of significant antidepressant activity for such benzodiazepines as diazepam (Covi et al., 1974) and chlordiazepoxide (Lipman et al., 1986). The presence of only borderline antidepressive effects combined with rebound symptoms occurring already after only 6 weeks of therapy does not recommend adinazolam for use in depression.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1989

Rolipram in major depressive disorder: results of a double-blind comparative study with imipramine.

Rolipram improves signal transmission in central noradrenergic neurones at a pre- and postsynaptic level, and is thus a novel approach in antidepressant therapy. In order to prove efficacy, tolerance, and safety, several controlled studies are underway. Results of a randomized double-blind comparative trial versus imipramine involving 64 in-patients with Major Depressive Disorder (DSM III) in six independent centers will be presented and discussed. The chosen biometric model provided evidence that towards the end of the study imipramine was superior to Rolipram. The particular clinical relevance of this difference is discussed. As regards tolerance, nausea emerged as the typical side-effect of Rolipram, whereas imipramine precipitated mainly anticholinergic side-effects.

Adult↗
PubMed1987

Quantitative pharmaco-electroencephalographic differentiation between the CNS effects of bromocriptine and imipramine, drugs with qualitatively different antidepressant properties.

Two double-blind, placebo-controlled studies were carried out at two different centers using the same protocol. Eight young healthy male volunteers were recruited for each of the studies, which were both undertaken to investigate the effect of single doses of 0.6, 1.25 and 2.5 mg bromocriptine (Parlodel) in comparison with 25 and 50 mg imipramine (Tofranil) on the electroencephalogram (EEG), subjective mental and emotional states, blood pressure, heart rate, and plasma prolactin levels. Side effects were also noted. The changes in the resting EEG power spectrum after imipramine were an increase in slow wave and fast beta activity and a decrease in alpha activity. At the same time imipramine depressed subjective mental and emotional states. Bromocriptine slowed the alpha activity of the resting EEG power spectrum, depressed subjective mental and emotional states, lowered blood pressure, and reduced prolactin secretion.

Adolescent↗
PubMed1983

Quantitative autoradiographic localization of [3H]imipramine binding sites in the brain of the rat: relationship to ascending 5-hydroxytryptamine neuron systems.

Quantitative autoradiography shows that there is a close relationship between [3H]imipramine binding sites and the distribution of 5-hydroxytryptamine (5-HT) neurons in the rat brain. High labeling is observed in the midbrain raphe nuclei, the areas of the dopamine cell groups of the substantia nigra and of the ventral tegmental area of Tsai, the ventral amygdaloid nucleus, the midline thalamic area, and parts of the hypothalmus. Thus, antidepressant drugs that have high affinity for [3H]imipramine binding sites can exert an influence at the 5-HT cell body as well as at the 5-HT nerve terminal level. The present results underline the possibility that the 5-HT and dopamine hypotheses for the mechanism of action of antidepressant drugs are not mutually exclusive, because both 5-HT and dopamine neurons can be regulated by large numbers of [3H]imipramine binding sites.

Animals↗