Effects of Paliperidone Palmitate on Coagulation: An Experimental Study

Abstract

Objective. The aim of the present study was to examine the effects of a new antipsychotic drug paliperidone palmitate on hemogram and coagulation parameters in rats. Materials and Methods. Experiments were performed on 22 female albino Wistar rats (8–12 weeks old). Control group was given drinking water as vehicle (0.3 mL). PAL-1 rats were given 1 mg/kg paliperidone palmitate (in 0.3 mL drinking water) by oral gavage once a day for ten days and PAL-3 rats received 3 mg/kg paliperidone palmitate (in 0.3 mL drinking water) by oral gavage for ten days. Blood samples were drawn from the heart 24 hours after the last drug dose, and hemogram and coagulation parameters were measured with automated analyzers. Results. Hemogram did not change in the paliperidone treated groups compared to the controls. Factor VIII levels decreased in the PAL-1 and PAL-3 groups; and this decrease was significantly greater in the PAL-3. Factor IX levels decreased in PAL-3 rats, but its levels also increased in PAL-1 rats compared to the control. Discussion. Paliperidone has led to changes in the serum levels of coagulation factors VIII and IX in rats. As a result, paliperidone may be causing thromboembolism or bleeding in a dose-independent manner.

Transcriptome alterations of mitochondrial and coagulation function in schizophrenia by cortical sequencing analysis

“…It also contains GRIA2, SNPs within GRIA2 has been report to influence the response to antipsychotic treatment in schizophrenia[ 76 ]. However, the new antipsychotic such as paliperidone has changed the serum level of coagulation factors VIII and IX in rats[ 77 ]. One of the mediator genes of cluster 39, NCS-1 gene can mediate desensitization of D2 dopamine receptors[ 78 ].…”

Physico-Chemical Characterization of Paliperidone Palmitate and Compatibility Studies with its Pharmaceutical Excipients

“…Drug-excipient compatibility studies during the formulation development is a significant process in getting to know about the physical and chemical interaction between the substance and excipients [6][7][8]. This process of knowing the in compatibility, by comparing the thermal curves of substance with pharmaceutical excipients used in formulation in the ratio of 1:1 for their evaluation.…”

Pulmonary thromboembolism associated with the use of new antipsychotics in a paediatric patient

“…Sedation, metabolic syndrome and hyperprolactinaemia are possible related factors. 6 Increased platelet aggregation has also been suggested for typical antipsychotics 7 through hyperprolactinaemia although aripiprazole (with partial dopamine agonism) and clozapine (weak antagonism) hardly have this side effect. 8 In another study, clozapine, risperidone and haloperidol, structurally different, significantly interfered with platelet aggregation; however, with a similar molecule olanzapine, this did not occur.…”

“…8 In another study, clozapine, risperidone and haloperidol, structurally different, significantly interfered with platelet aggregation; however, with a similar molecule olanzapine, this did not occur. 6 A strong affinity between serotonin 5-HT2A receptors and atypical antipsychotics can induce platelet aggregation. 9 We consider paliperidone as the main predisposing factor for DVT in our patient, especially given its recent introduction.…”

“…The underlying mechanisms are not well understood. Sedation, metabolic syndrome and hyperprolactinaemia are possible related factors 6 . Increased platelet aggregation has also been suggested for typical antipsychotics 7 through hyperprolactinaemia although aripiprazole (with partial dopamine agonism) and clozapine (weak antagonism) hardly have this side effect 8 .…”