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PubMedDate not supplied

Clinical pharmacokinetics of the depot antipsychotics.

The clinical pharmacokinetics of the 4 depot antipsychotics for which plasma level studies are available (i.e. fluphenazine enanthate and decanoate, haloperidol decanoate, clopenthixol decanoate and flupenthixol decanoate) are reviewed. The proper study of these agents has been handicapped until recently by the necessity of accurately measuring subnanomolar concentrations in plasma. Their kinetic properties, the relationship of plasma concentrations to clinical effects, and conversion from oral to injectable therapy are discussed. The depot antipsychotics are synthesised by esterification of the active drug to a long chain fatty acid and the resultant compound is then dissolved in a vegetable oil. The absorption rate constant is slower than the elimination rate constant and therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of the absorption rate, and the concentration at steady-state is a function of the elimination rate. Fluphenazine is available as both an enanthate and decanoate ester (both dissolved in sesame oil), although the decanoate is more commonly used clinically. The enanthate produces peak plasma concentrations on days 2 to 3 and declines with an apparent elimination half-life (i.e. the half-time of the apparent first-order decline of plasma concentrations) of 3.5 to 4 days after a single injection. The decanoate produces an early high peak which occurs during the first day and then declines with an apparent half-life ranging from 6.8 to 9.6 days following a single injection. After multiple injections of fluphenazine decanoate, however, the mean apparent half-life increases to 14.3 days, and the time to reach steady-state is 4 to 6 weeks. Withdrawal studies with fluphenazine decanoate suggest that relapsing patients have a more rapid plasma concentration decline than non-relapsing patients, and that the plasma concentrations do not decline smoothly but may exhibit 'lumps' due to residual release from previous injection sites or multicompartment redistribution. Cigarette smoking has been found to be associated with a 2.33-fold increase in the clearance of fluphenazine decanoate. In 3 different studies, fluphenazine has been proposed to have a therapeutic range from less than 0.15 to 0.5 ng/ml with an upper therapeutic range of 4.0 ng/ml. Plasma concentrations following the decanoate injection are generally lower than, but clinically equivalent to, those attained with the oral form of the drug. Haloperidol decanoate plasma concentrations peak on the seventh day following injection although, in some patients, this peak may occur on the first day.(ABSTRACT TRUNCATED AT 400 WORDS)

Aging↗
PubMed1975

[Advantages of the initial therapy of acute schizophrenia with large doses of droperidol/A comparative study (author's transl)].

The treatment of acute schizophrenic disorders with large doses of droperidol was compared to clozapine and clopenthixol in a special study. Apart from the clinical protocol, psychometric test for the assessment of social behaviour and thought disorders were used. The advantages of the treatment with droperidol, especially in highly disturbed acute schizophrenic patients, are shown and discussed by means of the results of psychological tests and clinical experience.

Acute Disease↗
PubMed1985

Chemotherapy with neuroleptics. Clinical and pharmacokinetic aspects with a particular view to depot preparations.

Attempting to improve long-term neuroleptic treatment of schizophrenic patients several injectable depot neuroleptics have been developed. Moreover pharmacokinetic data increasingly have been clinically applied. On this background the purpose of the present paper has been to make an updated review of the clinical and pharmacokinetic knowledge of depot neuroleptic treatment. First, general aspects of antipsychotics have been summarized, and an outline of methodological questions relevant to clinical-pharmacological trials are given. Subsequently general aspects including pros & cons of depot administration are examined. Finally the available data of the various depot preparations have been scrutinized. It is concluded that our present pharmacokinetic knowledge of the particular preparations is incomplete. Thus more information of clinical relevant aspects are needed, e.g., the existence of a therapeutic range, maximum/minimum concentration ratio, and the significance of active metabolites. Comparing the various depot neuroleptics, no significant differences are seen regarding the clinical effects. However, the decanoate esters seem clinical superior to the corresponding enanthate esters explained by the more flat concentration curve of the decanoates. Apart from that, a comparison of the pharmacokinetic data is difficult because of the heterogenecy of the available data. Haloperidol, clopenthixol and perphenazine decanoates are among the best examined preparations in pharmacokinetic respects. A controlled double-blind comparative study of these preparations would be of interest.

Administration, Oral↗
PubMedDate not supplied

Open multicentre trial of zuclopenthixol in mania and schizophrenia based on the AMDP scales.

A total of 95 schizophrenic or manic patients received zuclopenthixol (cis(Z)-clopenthixol) either intramuscularly or orally during a period of 2 to 4 weeks in mean daily doses of 25 mg (i.m.) or 75 mg (p.o.). They were rated with the CGI, VAS, MSS, BPRS, and AMDP scales. Zuclopenthixol proved to be a potent antimanic, anti-aggressive and antidelusional neuroleptic already from the second day of injection. Very few anticholinergic and extrapyramidal side effects as well as little somnolence were seen and the local tolerance was excellent. The 14-factor AMDP profile proved valid, sensitive to change and highly differentiated.

Administration, Oral↗
PubMedDate not supplied

[Clinical pharmacokinetics of haloperidol decanoate. Comparison with other prolonged-action neuroleptics].

Precise pharmacokinetic data of long-acting neuroleptics: apparent half life (T 1/2), time of peak plasma concentration (Tmax), bioavailability, has been a major contribution to determine optimal dosage of the drug. If the aim of the depot neuroleptic is to obtain a stable plasma concentration of the neuroleptic after I.M. injection of the ester form equivalent to that following oral administration, it is logical to obtain the same pharmacological effect; this is true for haloperidol decanoate. Mean value of T 1/2 of clopenthixol decanoate and haloperidol decanoate are 19 and 21 days, respectively, they thereby justify monthly administration. Flupenthixol decanoate and fluphenazine enanthate should be injected with dosing intervals of 3 and 1 weeks, respectively in respect with their half-lives: 17 and 4 days. Fluphenazine decanoate have a half-life of 14 days, however, the longer time the treatment, the longer the apparent half-life, suggesting to reduce the dose or to enlarge the dosing interval. Optimal dose has been determined from the bioavailability of the oral formulation and the interval between two injections, it averages 15, 20 times the oral daily dose for haloperidol decanoate. A lower conversion factor is frequently used (0.5 to 5 times) for other depot-neuroleptics such as pipotiazine palmitate, fluphenazine enanthate or decanoate; these low factors are not entirely explainable by the low bioavailability of the oral forms and produces more lower plasma concentration than after oral administration.

Biological Availability↗
PubMedDate not supplied

[Zuclopenthixol acetate and haloperidol in acute psychoses. Results of the AMDP subgroup in a multicenter Belgian study].

The efficacy of i.m. cis(Z)-clopenthixol in aggressive, agitated and delusional patients is well established but it necessitates, as for all other parenteral neuroleptics, several injections daily. Zuclopenthixol acetate is the first injectable neuroleptic characterized simultaneously by a short latency of action (2-3 h) and by a long duration of action (2-3 days). Within the frame of a Belgian multicentre study of zuclopenthixol acetate and haloperidol, a group of French-speaking psychiatrists added the AMDP scales to the basic protocol. The results of this AMDP subsample of 20 Acetate vs. 13 Haloperidol patients do not allow the demonstration of statistically significant differences between both neuroleptics because of the smallness and unbalance of the sample, but they indicate that both antipsychotics are very active and that a comprehensive rating scale such as the AMDP gives a much better differentiated clinical picture of a new drug than the total scores of short, so-called "economical" rating scales.

Adolescent↗
PubMed2003

Separation of (Z)- and (E)-isomers of thioxanthene and dibenz[b,e]oxepin derivatives with calixarenes and resorcinarenes as additives in nonaqueous capillary electrophoresis.

Five acidic calix[4]arenes with carboxylic or sulfonic groups at either the upper or lower rim of the cavity and one resorc[4]arene were investigated to separate three thioxanthenes (flupentixol, clopenthixol, chlorprothixene) and a dibenz[b,e]oxepin derivative (doxepin) with cis-/trans-isomerism by nonaqueous capillary electrophoresis (NACE). Partial filling of the capillary with the UV-absorbing selectors led to a low detection limit and an advantageous signal-to-noise ratio (S/N). A sufficient electrophoretic mobility of the calixarenes towards the anode was necessary to outweigh the oppositely directed electroosmotic flow (EOF). This depended from the functional groups, the dissociation and the hydrodynamic radius of the cyclophanes. In contrast, the resorcinarene was useable only by addition of sodium dodecyl sulfate (SDS) because only the complex of the two selectors had an anodic apparent electrophoretic mobility. p-Sulfonyl-calix[4]arene (ss-a1) was the most capable selector for all E/Z-isomers with maximal alpha-values ranging from 1.056 for doxepin to 1.224 for chlorprothixene. This was due to the sufficient migration in reversed direction to the EOF even at low pH* values of 3.0. Otherwise, electrostatic as well as hydrophobic interactions with the positively charged isomers seem to contribute to a superior recognition. Increasing the concentration up to 15 mM ss-a1 and using acidic media (pH* 5.0) led to high separation efficiency. Changing the organic solvent provides a powerful tool to improve selectivity with N,N-dimethylformamide-methanol (DMF-MeOH)-mixtures for thioxanthenes. Further electrophoretic parameters were optimized, such as the concentration of the electrolytes, the addition of SDS, the kind of electrolytes and the voltage. Distinct differences in selectivities were found between the derivatives with thioxanthene and dibenzo[b,e]oxepin ring system, respectively. Further, the different basic side chain was responsible for the different selectivity at higher pH* values. In contrast, the substitution at position 2 of the thioxanthenes played a secondary role. Based on the studies of single parameters a method for a simultaneous separation of the four pairs of isomers within 13 min was developed.

Calixarenes↗
PubMed1985

Pharmacological differentiation of dopamine D-1 and D-2 antagonists after single and repeated administration.

In single-dose experiments neuroleptics antagonize dopamine (DA)-agonist-induced stereotypies in animals. The antagonistic potency correlates with their clinical antipsychotic effects. In a series of experiments where DA-agonist-induced stereotyped gnawing in mice and rats was inhibited by neuroleptics it was shown that the antagonistic effect of butyrophenones was greatly attenuated by concomitant treatment with anticholinergics. The effect of phenothiazines was slightly attenuated and that of thioxanthenes and SCH 23390 remained unchanged. After repeated administration a differentiation is also seen in the ability of the antagonists to suppress DA-agonist-induced stereotypies. The differentiation in these experiments is similar to that seen in dopamine D-1 and D-2 receptor binding. The compounds can be classified into three pharmacological subgroups: butyrophenones (e.g., haloperidol) with affinity for D-2 receptors; phenothiazines (e.g., fluphenazine and perphenazine) with affinity for both D-2 and D-1 receptors but with preference for the D-2 receptors; and thioxanthenes (e.g., cis(Z)-flupentixol and cis(Z)-clopenthixol) with equal affinity for D-1 and D-2 receptors, and the selective D-1 antagonist SCH 23390. This compound has the same antistereotypic effect as is seen with the neuroleptics. We have also investigated the effect of the above-mentioned neuroleptics and SCH 23390 after 12 days' treatment and 3-5 days withdrawal. They were given either alone or in combination. When they were given alone a clear differentiation was seen between the groups when mice were tested for methylphenidate antagonism. The thioxanthenes and SCH 23390 retain their ability to antagonize the stereotyped gnawing; the phenothiazines show a reduced effect; and the butyrophenones have almost lost their ability to antagonize the stereotyped behavior.

Animals↗
PubMed1988

Dose-response curves of homovanillic acid in pre-frontal cortex and caudate following antipsychotic drugs: relation to clinical potencies.

Dose-response curves for the elevation of homovanillic acid (HVA) levels, determined by high performance liquid chromatography using electrochemical detection, in the pre-frontal cortex and caudate of rats after acute treatment with 12 antipsychotic drugs are presented. The order of potency in both brain regions was: haloperidol greater than or equal to fluphenazine greater than loxapine greater than trifluoperazine greater than thiothixene greater than molindone greater than clopenthixol greater than chlorpromazine greater than metoclopramide greater than thioridazine greater than clozapine greater than sulpiride. This ranking is roughly correlated with that based on clinical potencies. The relative elevation of the content of HVA was weaker in the pre-frontal cortex than in the caudate for all drugs tested, except clozapine at a high dose.

Animals↗
PubMed1993

Serotonergic and dopaminergic aspects of neuroleptic-induced extrapyramidal syndromes in nonhuman primates.

Neuroleptic drug-induced acute extra-pyramidal syndromes are one of the major reasons why patients discontinue their antipsychotic medicines. The typical (e.g., haloperidol) neuroleptic drug produces acute extrapyramidal symptoms in the majority of patients, whereas the atypical (clozapine) neuroleptic produces only minimal motor system side effects. Serotonin S2 antagonists often reduce or prevent catalepsy in rodents, but the limited number of studies in nonhuman primates have produced conflicting results. The hypothesis of a high serotonin S2/dopamine D2 antagonism ratio as a mechanism underlying atypical neuroleptic effects in preventing acute extrapyramidal syndromes deserves further evaluation in nonhuman primate models because extrapyramidal symptoms in monkeys closely resemble those in patients. Cebus monkeys (22-28 years old) were tested with compounds that ranged from low to high S2/D2 antagonism ratios. These were haloperidol, fluphenazine, clopenthixol, melperone, tefludazine, setoperone, risperidone, and clozapine. A saline control was included with a wide dose range of each of these drugs that was tested in a once-weekly, blindly-scored random drug administration schedule. Dystonia was scored on four different symptoms by an experienced rater who was blind to drug dosage. All the compounds, with the exception of clozapine, produced clinically indistinguishable dose-related dystonia. The only difference was the dose at which dystonia appeared. In contrast to rodent studies, these nonhuman primate investigations with drugs, spanning a wide range of S2/D2 antagonism ratios, produced clinically similar extrapyramidal symptoms. Thus, adding an S2 antagonism component to neuroleptics does not appear to provide an explanation for the motor side effect profile of atypical neuroleptics, or a method for designing neuroleptic drugs that will be free of extrapyramidal symptoms.

Animals↗
PubMed1985

Behavioural stimulation is induced by separate dopamine D-1 and D-2 receptor sites in reserpine-pretreated but not in normal rats.

The dopamine (DA) D-1 agonist SK&F 38393 as well as the D-2 agonist pergolide and the mixed D-1/D-2 agonist apomorphine induced strong hypermotility and oral stereotypy in rats pretreated with a daily dose of reserpine for 2 and in particular for 4 days (3 and 5 injections, respectively). SK&F 38393 had no behavioural stimulant effect in saline-pretreated rats, whereas pergolide and apomorphine produced stimulation, although only after higher doses. Agonists at 5-HT and muscarinic receptors and at alpha 1-adrenoceptors were ineffective in reserpine-pretreated rats whereas the alpha 2-adrenoceptor agonist, clonidine, and the muscarinic antagonist, scopolamine, produced weak locomotor stimulation. The hypermotility induced by SK&F 38393 in reserpinized rats was blocked by pretreatment with the DA D-1 antagonists, SCH 23390 and SK&F 83566c, whereas the DA D-2 antagonists, YM 09151-2, clebopride and spiroperidol were weak or ineffective. In contrast pergolide-induced hypermotility was blocked by low doses of the D-2 antagonists but was weakly or not influenced by the D-1 antagonists. Selectivity ratios between drug potencies in the two models ranged from 65 to more than 600. The mixed D-1/D-2 antagonists, cis(Z)-flupentixol and cis(Z)-clopenthixol, blocked the effect of both SK&F 38393 and pergolide. The alpha 1-adrenoceptor antagonist, prazosin, and the 5-HT2 receptor antagonist, ketanserin, did not modify the effect of SK&F 38393 or pergolide. Stereotyped behaviour induced by a high pergolide dose in normal rats was, in contrast to the effect in reserpinized rats, blocked by low doses of either SCH 23390 or spiroperidol. Finally, the hypermotility induced by apomorphine in reserpinized rats was markedly antagonized by both SCH 23390 and spiroperidol. The results suggest a close relation between D-1 and D-2 receptor sites in normal rats. After prolonged reserpine treatment, the D-1 agonist acquires full DA agonist efficacy. Furthermore, behavioural stimulation under these conditions is mediated by two separate D-1 and D-2 receptor sites which can be manipulated independently by antagonists. The mechanism by which this phenomenon occurs is unknown but the adaptational changes show close similarities to those observed after 6-hydroxyDA-induced denervation.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed1984

125I-Spiperone: a novel ligand for D2 dopamine receptors.

125I-Spiperone binds with high affinity (KD 0.3 nM) to a single specific site (Bmax 34 pmol/g wet weight) in homogenates of rat corpus striatum. Specific binding is about 40-60 percent of total binding and is displaced stereo-specifically by butaclamol and clopenthixol. Neuroleptic drugs of various classes are potent inhibitors of 125I-spiperone binding (Ki's 1-10 nM). Selective dopamine antagonists such as sulpiride (Ki 50 nM) and dopamine agonists such as apomorphine (Ki 200 nM) are also potent inhibitors. The drug specificity of 125I-spiperone binding correlates well with that of 3H-spiperone binding, providing good evidence that 125I-spiperone labels D2 dopamine receptors in striatal membranes. 125I-Spiperone, with its high specific activity (2200 Ci/mmol) may prove to be a useful ligand in studies examining D2 dopamine receptors in soluble preparations and by autoradiography. Furthermore iodinated spiperone may be useful in radioreceptor assays of neuroleptic drug levels and, in a 123I-labeled form, for imaging of dopamine receptors, in vivo, using single photon tomography.

Animals↗
PubMed1984

Pharmacological effects of a specific dopamine D-1 antagonist SCH 23390 in comparison with neuroleptics.

Neuroleptics such as thioxanthenes (cis(Z)-flupentixol and cis(Z)-clopenthixol) and phenothiazines (fluphenazine and perphenazine), which block both dopamine (DA) D-1 and D-2 receptors and the butyrophenones (haloperidol and spiroperidol), which block D-2 receptors only, are equipotent both behaviorally and clinically. A new compound SCH 23390 which selectively blocks DA D-1 receptors, resembles many neuroleptics in its pharmacological profile: antistereotypic effects in mice, rats and dogs, cataleptogenic effect and inhibitory effect on amphetamine circling. In contrast SCH 23390 has no effect on apomorphine-induced vomiting in dogs and little effects on 6-OHDA-denervated supersensitive DA receptors, stimulated by the DA agonist 3-PPP. In a series of experiments where methylphenidate-induced stereotyped gnawing in mice was inhibited by neuroleptics, it was shown that concomitant treatment with scopolamine or diazepam attenuated the effect of butyrophenones (D-2 antagonists). The same treatment attenuated the effect of phenothiazines, to a lesser extent, and hardly attenuated the effect of thioxanthenes and SCH 23390 at all. It is concluded that DA D-1 receptors are as important as D-2 receptors for the expression of neuroleptic activity in most animal models believed to be predictive of antipsychotic and extrapyramidal side-effect potential. However, the D-1 antagonist is less sensitive than D-2 antagonists to antimuscarinic compounds and benzodiazepines.

Adrenergic alpha-Antagonists↗
PubMed2000

Fluorimetric determination of some thioxanthene derivatives in dosage forms and biological fluids.

A simple and highly sensitive method is proposed for the fluorimetric determination of four thioxanthene derivatives, namely: chlorprothixene, clopenthixol, flupentixol and thiothixene, in dosage forms and biological fluids. The method involves the use of nitrous acid as an oxidant to produce the corresponding fluorescent thioxanthenone sulphoxides. The experimental parameters were carefully studied and incorporated into the procedures. The results obtained compare favourably with those obtained by the official methods. The concentration-fluorescence plots were rectilinear over the range of 0.04-0.4 microg/ml for thiothixene, and 0.02-0.25 microg/ml for the other compounds, with minimum detectability (S/N = 2) of 2 ng/ml for all the studied compounds except thiothixene which was 4 ng/ml. The proposed method was applied to the determination of the studied compounds in dosage forms. The results obtained were in good agreement with those obtained adopting the USP XIII method. The proposed method was further applied to the determination of flupentixol in spiked human urine and plasma, the percentage recoveries were 94.39 +/- 1.81 and 96.46 +/- 0.28, respectively. A proposal of the reaction pathway was presented.

Dosage Forms↗
PubMed1989

Which atypical antipsychotics are identified by screening tests?

Only two tests were specific for antipsychotic potential. All effective antipsychotics blocked pharmacologically induced locomotion and affected firing in the mesolimbic DA neurons. The remaining single- (Table 1) and repeated- (Table 2) dose tests identified the atypical antipsychotics. Clozapine, thioridazine, sulpiride, tiospirone, and molindone were atypical in both types of study. Pimozide, pipamperone, aceperon, methylperon, and clotiapine were atypical in single-dose studies, clopenthixol in repeated-dose studies. Since the biochemical abnormality causing psychoses is unknown, it may be that current methods of screening for new antipsychotics are inadequate and possibly inappropriate. If a neurotransmitter other than DA is the primary cause, then totally new tests may be needed. Present tests, especially those involving behavioral paradigms, may continue to select out compounds that cause EPS side-effects. New methods such as positron emission tomography scanning and other brain-imaging techniques hold the promise of studying specific types and subtypes of receptors in the living human brain. The recent discovery of chromosomal abnormalities in psychotic illness may provide new insights into the biochemical causes of such disorders and lead to completely new compounds that will be both safer and more effective. In the meantime we plan to review the literature on the clinical use of the compounds identified as atypical in this article and to develop research protocols to assess their efficacy in treatment-resistant psychoses and intractable conditions such as tardive dyskinesia.

Animals↗
PubMed1997

Therapeutic drug monitoring databases for postmarketing surveillance of drug-drug interactions: evaluation of a paired approach for psychotropic medication.

The present study investigated the potential of therapeutic drug monitoring data to document pharmacokinetic drug interactions with psychotropic medication, both in terms of methodology and applicability. It focused on 105 patients exposed to one of five agents known for their capacity to induce (phenytoine, phenobarbital, and carbamazepine) or to inhibit (thioridazine and levomepromazine) the metabolism of psychotropic drugs. These patients were matched by gender, age, and monitored psychotropic medication to 105 patients randomly selected from a pool of subjects nonexposed to target comedication. Such a paired approach was shown to be effective in reducing variability for a majority of substances. Power analysis suggested that eight to 10 pairs of exposed and nonexposed patients would effectively allow the detection of twofold effects of interacting substances. In keeping with the literature, analysis of the ratios of dose-normalized exposed to nonexposed concentrations indicated that phenothiazine comedication led to significantly higher concentrations of desmethylated metabolites but not parent compounds, when clomipramine, imipramine, or amitriptyline were administered. A similar, as yet undocumented interaction was observed for the tetracyclic antidepressant mianserine. In contrast, the present study revealed that maprotiline concentrations were increased, but its metabolite was largely unaffected by phenothiazine comedication. Increased concentrations were also observed for moclobemide, but not citalopram or its metabolite. In addition to its long recognized capacity to decrease haloperidol concentrations, carbamazepine was shown to induce the metabolism of clopenthixol and possibly flupenthixol. The consistency of such a picture substantiates the need to consider therapeutic drug monitoring databases as cost-effective and reliable tools for postmarketing surveillance.

Adolescent↗
PubMed1979

The characteristics of [3H]-clonidine binding to an alpha-adrenoceptor in membranes from guinea-pig kidney.

1. [3H]-clonidine binds to membranes prepared from guinea-pig kidney. 2. At 25 degrees C the binding is rapid and saturable. 3. Scatchard analysis of the binding data showed that the Kd for [3H]-clonidine binding in kidney membranes is 8.54 nM and the density of binding sites 12.5 pmol/g wet wt. tissue. 4. Hill plots of the binding data showed that there were no cooperative site interactions associated with binding. 5. [3H]-clonidine binding could be displaced by drugs, the most potent being drugs with a high affinity for the alpha-adrenoceptor. The neuroleptic drugs (+)-butaclamol, cis-clopenthixol and cis-flupenthixol at high concentration also displaced [3H]-clonidine binding. 6. Drugs acting as agonists or antagonists of beta-adrenoceptors, histamine receptors, acetylcholine receptors as well as prostaglandins E1, E2, F1alpha and F2alpha, angiotensin II, arginine vasopressin, naloxone, nalorphine and pargyline had little effect on binding. 7. It is likely that the binding site labelled by [3H]-clonidine in guinea-pig kidney membranes is an alpha-adrenoceptor similar in some pharmacological aspects to an alpha2-adrenoceptor.

Animals↗
PubMed1989

Trimipramine and other antipsychotics inhibit Campylobacter pylori in vitro.

A series of conventional anti-ulcer drugs, tricyclic antidepressants and neuroleptics (and some CNS non-active isomers) were tested in vitro for possible inhibition of Campylobacter pylori. These bacteria are claimed to play an etiological role in peptic ulcer disease, at least in gastritis B. While cimetidine, famotidine, ranitidine and pirenzepine were inactive, all the antipsychotic agents and their isomeric derivatives were active to various degrees with IC50 of 26-59 microM. Of special interest is trimipramine (Surmontil) that has been demonstrated to be effective against duodenal ulcers in some trials. The activity of the non-neuroleptic stereo-isomers of clopenthixol and chlorprothixene may lead to investigation in patients with peptic ulcer disease of this kind of agents. However, a firm connection between the antimicrobial activity of these compounds, their possible anti-ulcer effect and the etiological role of Campylobacter pylori in peptic ulcer disease must first be established.

Anti-Ulcer Agents↗