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PubMedDate not supplied

Kinetics of distribution and adipose tissue storage as a function of lipophilicity and chemical structure. II. Benzodiazepines.

Distribution kinetics of flurazepam, medazepam, prazepam, and clobazam were determined in rats. Concentration-time curves of unchanged drugs and non-polar metabolites in plasma, adipose tissue, liver, brain, and muscle after a single iv administration were obtained using GLC/electron capture detector analysis. Pharmacokinetic parameters were calculated for plasma and tissues. Adipose tissue storage was quantified with the adipose storage index (ASI). Including data of benzodiazepines from the literature, a correlation between ASI and log P (over a range 1.6-3.8) was nonexistent and the influence of individual functional groups was not easily discernible. However, benzodiazepines with a pKa (base) within the range 1.6-6.2 were stored in adipose tissue (ASI greater than 1), whereas those with pKa greater than 7 were not (ASI less than 1). Since many other basic lipophilic drugs with pKa greater than 7 are not stored in adipose tissue, and this is likely due to lysosomal trapping in lean tissues, which requires a pKa value above 7, it is suggested that within the series of benzodiazepines, adipose tissue storage is mainly influenced by the basicity of the drugs.

Adipose Tissue↗
PubMed1986

Spectrophotometric determination of some 1,4-benzodiazepines by use of orthogonal polynomials.

A direct spectrophotometric method for the determination of some 1,4-benzodiazepines, namely, nitrazepam, prazepam and dipotassium chlorazepate, in the presence of their degradation products, is presented. The method depends upon the use of orthogonal polynomials, to eliminate interferences by degradation products to the absorption spectra of the intact drugs. The method was proved using synthetic mixtures of the intact drugs with their respective degradation products and its suitability to monitor for the stability of the drugs was demonstrated. The method has been applied to the determination of these drugs in dosage forms, with a coefficient of variation less than 2%.

Anti-Anxiety Agents↗
PubMedDate not supplied

[A new scale of quantitative and qualitative evaluation of anxiety: the Ferrerri Anxiety Rating Diagram (FARD)].

This new instrument to evaluate anxiety, the F.A.R.D. (Ferreri anxiety rating diagram - 1987) has been conceived to appreciate the repercussions of anxiety on the activity of the subject. It realizes a special image of anxiety. It has been studied, by both psychiatrists and general practitioners in 320 patients included on generalised anxiety disorders criteria (following DMS III). The validation has been realised in a study of prazepam for 81 patients. The F.A.R.D. is based upon 12 items. The factor analysis has retained 4 factors explaining 66% of the whole variance. These 4 factors composed by 3 items each are: relational, somatic, vigilance, cognitive. This new instrument, the F.A.R.D.: evaluates the intensity of anxiety, precision, the shape of anxiety, specifies sub-groups of anxiety, allows a following of evolution, appreciates the pharmaco-clinical profile of the anxiolytic drug prescribed.

Adult↗
PubMed1979

Identification of some benzodiazepines of forensic interest.

Ten benzodiazepines--clorazepate, nitrazepam, clonazepam, oxazepam, lorazepam, chlordiazepoxide, N-desmethyldiazepam, diazepam, prazepam, and flurazepam--in solid dosage form are identified by ultraviolet (UV) and infrared (IR) spectrophotometry and by high pressure liquid chromatography (HPLC). UV absorption data and IR spectra of the 10 benzodiazepines are provided and HPLC separation methods are described.

Benzodiazepines↗
PubMed1980

Pharmacokinetics of benzodiazepines. Short-acting versus long-acting.

Among the various benzodiazepines large differences exist with regard to their pharmacokinetic properties and metabolism in man. Some are eliminated from the body at a relatively slow rate (e. g. diazepam), others are metabolized rather rapidly (e. g. oxazepam, temazepam, triazolam). Several benzodiazepines have the long-acting metabolite N-desmethyldiazepam in common (diazepam, fosazepam, prazepam, clorazepate). Such differences may be very important clinically because pharmacokinetic factors will determine the duration of drug effect and pharmacokinetic parameters constitute the basis for a rational dosage regimen. For the various clinical indications of benzodiazepines the required duration of drug action differs quite fundamentally. In anticonvulsant and anti-anxiety treatment continuous treatment is pursued, so that compounds with long elimination half-lives of parent drug or active metabolites are of advantage. If on the other hand a benzodiazepine is taken as a hypnotic, the duration of action should be restricted to the night, hence a compound with a short elimination half-life is to be preferred. A review is given of the pharmacokinetics of the major benzodiazepines presently available.

Anti-Anxiety Agents↗
PubMed1980

A sensitive benzodiazepine radioimmunoassay of broad specificity.

Four benzodiazepine radioimmunoassays are described, the most sensitive of which can detect sub-therapeutic levels of bromazepam, chlordiazepoxide, clobazam, demoxepam, desalkylflurazepam, desmethyldiazepam, diazepam, flunitrazepam, lorazepam, medazepam, nitrazepam, oxazepam, prazepam, temazepam and triazolam. The standard curve for diazepam has a concentration range of 0-2.5 ng ml-1. The assay is particularly applicable to blood samples of forensic interest that may be haemolysed or decomposing. A 75 microliter sample is required. The antiserum and [3H]flunitrazepam used are commercially available.

Benzodiazepines↗
PubMed1981

Cimetidine-benzodiazepine drug interaction.

The effect of cimetidine on the metabolism of benzodiazepines is discussed. Studies of cimetidine's inhibition of benzodiazepine metabolism by liver microsomal enzyme pathways are described. Cimetidine is known to have this effect on the metabolism of diazepam and chlordiazepoxide, and because chlorazepate and prazepam are similarly metabolized, cimetidine is likely to have the same effect on the metabolism of these drugs. Oxazepam and lorazepam are two benzodiazepines not metabolized by liver microsomal enzymes, but are thought to be glucuronidated in peripheral tissue by glucuronyl transferase. Cimetidine has been shown not to alter the pharmacokinetics of lorazepam or oxazepam when administered concurrently with either of these benzodiazepines. When it is necessary to treat a patients receiving cimetidine with a benzodiazepine, oxazepam or lorazepam may be the drug of choice.

Animals↗
PubMed1982

Does chlordesmethyldiazepam have a specific anti-erotic effect? Report on five observations.

Five observations in adult subjects (4 female, 1 male) in which the administration of chlordesmethyldiazepam (2-4 mg/day) alone, or in association with other psychodrugs has demonstrated a specific anti-erotic action, with a short therapeutic latency period, reversible, and not found in other benzodiazepines (chlordiazepoxide, diazepam, lorazepam, flunitrazepam, prazepam) which the patients had previously taken, are presented in detail. One of the cases was diagnosed with Clérambault Syndrome of seven years' duration [Acta psychiat. belg., 82, 555-564 (1982)].

Adult↗
PubMed1982

Gas-chromatographic determination of verapamil and norverapamil, with a nitrogen-selective detector.

We present a procedure for the determination of verapamil and its metabolite, norverapamil, in serum. The drugs are extracted under basic conditions into n-heptane/2-butanol (96/4 by vol) and then extracted again into 1 mol/L H2SO4. The acidic solution is made basic with sodium hydroxide, re-extracted with diethyl ether, and the extract evaporated. The residue is redissolved in ethanol and analyzed by gas chromatography with a nitrogen-selective detector. By use of two internal standards, prazepam and D-517 (a verapamil analog), concentration and instrument response are linearly related from 50 micrograms/L to 5 mg/L. Within-run precision (CV) was 3 and 5% for both verapamil and norverapamil at concentrations of 100 and 250 micrograms/L; between-run precision was 11 and 9% at those respective concentrations. Interference studies indicate that most commonly prescribed basic drugs will not interfere with this procedure.

Chromatography, Gas↗
PubMed1982

Liquid-chromatographic measurement of nitrazepam in plasma.

In this simple and rapid "high-performance" liquid-chromatographic method for determining nitrazepam in plasma, serum, or whole blood, the sample at pH 7.4 is extracted into diethyl ether with an internal standard (prazepam), chromatographed, and detected at 280 nm with a fixed-wavelength ultraviolet detector. A specimen, together with standards and a quality control, can be analyzed in duplicate within 90 min. The limit of sensitivity is 5 micrograms/L (nitrazepam and 7-acetamidonitrazepam) and 50 micrograms/L (7-aminonitrazepam), and no interferents have been found. This method has the advantages of a small sample requirement and complete resolution of nitrazepam and the above-mentioned major metabolites. We have used this method for analysis of therapeutic and overdose concentrations of nitrazepam, and to investigate the stability of the drug in blood.

Chromatography, High Pressure Liquid↗
PubMed1982

Liquid-chromatographic procedure for simultaneous analysis for eight benzodiazepines in serum.

We describe an efficient extraction and liquid-chromatographic method for separating commonly encountered benzodiazepine drugs and their pharmacologically active metabolites. After a single extraction of the drugs from serum, chlordiazepoxide, demoxepam, N-desmethyl-chloriazepoxide, diazepam, N-desmethyldiazepam, N-desalkylflurazepam, oxazepam, and prazepam can be resolved and quantified by using a C18 reversed-phase "high-performance" column and a ternary-solvent gradient system. Three separate solutions [60 mmol/L ammonium acetate (pH 7.69), 60 mmol/L acetic acid (pH 2.8), and acetonitrile] were incorporated into a gradient mobile phase such that changes in pH and solvent composition occur. Complete chromatographic resolution of the benzodiazepines resulted, permitting quantification of all within 15 min. The standard curve is linear to at least 8 mg/L for each drug, and the detection limit for each was 0.05-0.10 mg/L. The day-to-day precision for both high and low concentrations yielded CVs of 5 to 9%. Extraction of each drug from serum was 95 to 100% complete. Exogenous and endogenous interferences are minimal. Finally, we circumvented the instability problem of benzodiazepine standards in solution by using a simple reduced-pressure drying process that produces a working standard that is stable for at least nine months.

Benzodiazepines↗
PubMed1995

[Parkinson syndrome induced by veralipride].

Veralipride, an antidopaminergic drug commonly prescribed to counteract postmenopausal symptoms, may cause reversible parkinsonism. A 49-year-old healthy woman reported a 5 month history of progressive slowing of voluntary movements, postural changes, e.g. sit-to-stand manouevres, and gait. Clinical examination revealed moderate hypokinesia, hypomimia and plastic rigidity of the four limbs. Locomotor oscillations of the upper limbs were decreased. She had been taking 100 mg of veralipride daily to counteract postmenopausal symptoms (vasomotor flushes and irritability) for 17 months uninterruptedly. The drug was withdrawn. The patient's clinical picture fully normalized within 20 days. One year later she reported to be still asymptomatic. This seems to be a case of parkinsonism induced by veralipride, a drug known to cause other extrapiramidal signs such as bucco-facial or limb dyskinesia. To our knowledge, only one other such case has been published (a 77-year-old French woman who had been taking veralipride, prazepam and nicergolin). In both cases, the drug had been administered for longer and without intervals. In our patient the motor disturbances could not have been associated with either advanced age or interaction with concurrent medications. Therefore, this case is suspected for veralipride-associated parkinsonism. In conclusion, intoxication should be thought in case of parkinsonism arising in women taking this drug.

Dopamine Antagonists↗
PubMed1993

[Studies on identification of drugs of abuse by diode array detection. I. Screening-test and identification of benzodiazepines by HPLC-DAD with ICOS software system].

For the establishment of screening-test and identification of 20 benzodiazepines (Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Clotiazepam, Cloxazolam, Diazepam, Estazolam, Fludiazepam, Flunitrazepam, Flurazepam, Lorazepam, Lormetazepam, Medazolam, Midazepam, Nimetazepam, Nitrazepam, Oxazepam, Prazepam, Triazolam), the optimum separation condition on HPLC was investigated by using Interactive Computer Optimization for HPLC Separation (ICOS) software. The two eluent systems of 0.02M KH2PO4 (pH 3.1)-methanol-acetonitrile (66.4:5.7:27.9) and 0.1% TFA-methanol-acetonitrile (61.6:16.1:22.3) were selected by HPLC analyses using ICOS. These optimum separation conditions enabled the screening test and identification of the 20 benzodiazepines on HPLC with photodiode array detection.

Benzodiazepines↗
PubMedDate not supplied

[Double-blind study of mianserin and fluoxetine in ambulatory therapy of depressed patients].

A double blind controlled trial was carried out in 65 depressed out-patients to compare the efficacy and tolerance of mianserin with fluoxetine. The two compounds present very different pharmacological activities. Mianserin is an antagonist of the alpha 2-adrenergic receptors, while fluoxetine is an inhibitor of recapture specific to serotonin. Requirements for inclusion were: depressive episode of less than 2 months duration, meeting the criteria for one of the sub-types of depression described in DSM III, with a minimum score of 25 on the Montgomery Asberg Depressive Rating Scale (MADRS). The patient's ages ranged from 18 to 65. The only psychotropic medication allowed in association to the treatment was prazepam (up to 40 mg/day). Patients gave their written consent to the study. Assessment, using the Montgomery Asberg Depression Rating Scale (MADRS), the HARD diagram, the check list for somatic symptoms and side-effects was carried out before treatment and at the end of weeks 2, 4, 8. Assessment of anxiety using the Hamilton Anxiety Rating Scale (HARS) and of sleep disturbances using a sleep questionnaire was carried out before treatment and at week 4. The 8 items of the sleep questionnaire covers the complaints listed in criteria for insomnia disorders (307.42 DSM III-R). Clinical Global Impression (CGI), Therapeutic Index (TI), Tolerance Global Impression were assessed at end-point. The 2 groups were strictly comparable in respect to the clinical status at base line (diagnosis, history and duration of the depressive illness, MADRS and HARD diagram scores).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1977

Micromethod for determination of diazepam by electron-capture gas-liquid chromatography.

We used 100 microliters of plasma for the determination of diazepam. After the internal standard, prazepam, is added, the serum is directly extracted with diethyl ether, the extract is evaporated, the residue is dissolved in ethanol, and the drug is measured by gas-liquid chromatography, with use of an electron capture detector. With this procedure, 2.5 ng of diazepam in the sample can be speedily measured with specificity, accuracy, and reproducibility (CV = 4.5%).

Chromatography, Gas↗
PubMedDate not supplied

[Intensive hospital monitoring of adverse reactions to benzodiazepines and neuroleptic agents].

BACKGROUND: The main aims of the programme were to highlight the incidence of adverse reactions to the drugs monitored and to define the risk/benefit ratio taking account of the main physiological and physiopathological variations of patients. This paper reports the results of the programme regarding to adverse effects correlated to the use of some psychiatric drugs (benzodiazepines and neuroleptics). METHODS: A total of 73 records were compiled for 64 patients treated with benzodiazepines and/or neuroleptics. RESULTS: A very high mean incidence of adverse events was documented (48%) without any severe undesirable effects. 92% of patients treated with neuroleptics reported adverse events. Haloperidol, which caused adverse effects in 80% of patients, revealed mild or moderate forms of parkinsonism (15%), spasm (15%), rigidity (10%), akathisia (5%), reversible postural hypotension (10%), temporary reduction of the visual field (10%), delayed menstrual flow (5%), xerostomia (10%), excessive sweating (10%) and sialorrhea (10%). All the patients treated with clozapine showed adverse effects including postural hypotension (29%), persistent tachycardia (14%), sialorrhea (29%), excessive sweating (14%) and akathisia (14%). Spasms (25%), rigidity (25%) and akathisia (25%) were correlated to the use of clothiapine, whereas postural hypotension was referred to clopenthixol. 44% of patients treated with benzodiazepines showed undesired effects. 20% of those taking chlordemethyldiazepam showed somnolence (33%), sedation (22%) and dysar-thria (44%). Prolonged sedation was observed in 30% of all patients treated with lorazepam. Prazepam was correlated with adverse effects in 75% of cases. No adverse event was documented with bromazepam. CONCLUSIONS: A higher incidence of adverse events was documented than literature data. Further periods of intensive monitoring will be required to obtain a greater quantity of data from the intensive monitoring of adverse events through the MIO '97 programme.

Antipsychotic Agents↗
PubMed1979

Benzodiazepines: some aspects of their clinical pharmacology.

Benzodiazepine derivatives are the most commonly prescribed anti-anxiety agents in clinical practice. Six benzodiazepine anxiolytics are now available in the United States. Additional drugs are used in other parts of the world, and many others are in various stages of clinical testing. All these benzodiazepine derivatives have similar neuropharmacological properties--they reduce anxiety, produce sedation and sleep, have anticonvulsant effects, and can produce muscle relaxation. Faced with this bewildering array of drugs from the same class which are very similar in intrinsic effects upon the brain, the clinician may well ask how best to make a rational choice among the available derivatives. Despite neuropharmacological similarities, there are differences among benzodiazepines in patterns of absorption, distribution, and elimination by the human body. These pharmacokinetic differences may in turn lead to apparent differences in clinical action. This review summarizes pertinent pharmacokinetic characteristics of benzodiazepine anti-anxiety agents.

Anti-Anxiety Agents↗