Plasma Levels of Fluphenazine Decanoate

1988 ◽  
Vol 153 (3) ◽  
pp. 382-384 ◽  
Author(s):  
Som D. Soni ◽  
David Wiles ◽  
A. A. Schiff ◽  
J. S. Bamrah
Keyword(s):  
Maintenance Therapy ◽  
Injection Site ◽  
Plasma Levels ◽  
Muscular Exercise ◽  
Blood Levels ◽  
Fluphenazine Decanoate ◽  
Physicochemical Composition ◽  
Depot Neuroleptics ◽  
Long Acting

Depot neuroleptics are now commonly used for maintenance therapy of schizophrenia. Their physicochemical composition makes them ideal for such use because they are long-acting and show stable blood levels for prolonged periods. Their absorption from the site of injection may, however, be affected by local muscle factors. This paper describes three such factors in relation to fluphenazine decanoate: varying the site of injection; massage of the injection site; and effects of muscular exercise. Our results suggest that fluphenazine pharmacokinetics are not significantly affected by any of these factors.

Two years of maintenance therapy with paliperidone long-acting in schizophrenia and schizoaffective disorder: a study with plasma levels

2016 ◽  
Vol 26 ◽  
pp. S556-S557
Author(s):  
S. Paletta ◽  
C. Di Pace ◽  
A. Reggiori ◽  
G. Cirnigliaro ◽  
M.C. Mauri ◽  
...  
Keyword(s):  
Maintenance Therapy ◽  
Schizoaffective Disorder ◽  
Plasma Levels ◽  
Long Acting

scholarly journals Plasma levels of long-acting injectable antipsychotics in outpatient care: a retrospective analysis

2020 ◽  
Author(s):  
Martin Hýža ◽  
Šilhán Petr ◽  
Češková Eva ◽  
Skřont Tomáš ◽  
Kacířová Ivana ◽  
...  
Keyword(s):  
Clinical Practice ◽  
Plasma Levels ◽  
Drug Application ◽  
Individual Variability ◽  
Therapeutic Drug ◽  
Fluphenazine Decanoate ◽  
Blood Samples ◽  
Usual Clinical Practice ◽  
Long Acting ◽  
The Individual

Abstract Background The antipsychotic efficacy in schizophrenia depends on its availability in the organism. Although therapeutic outcomes remain still far from satisfactory, therapeutic drug monitoring is not a common part of clinical practice during a treatment with long-acting injectable antipsychotics (LAI AP). The real effectiveness of LAI AP is thus uncertain. Methods We made a retrospective evaluation of plasma levels of LAI AP. Collection of blood samples was performed just before the drug application and one week later. Fourty patients with a stabilized clinical condition and steady-state plasma levels were included. Results In the observed cohort of patients, flupentixol decanoate (n = 23) was the most often used drug, followed by fluphenazine decanoate (n = 7), haloperidol decanoate (n = 5), paliperidon palmitate (n = 3), and risperidone microspheres (n = 2). Just 5 of 40 patients were treated with a monotherapy. At the time before the application, 60% of the patients did not reach the therapeutic reference range (TRR) and 20% of the patients had an undetectable plasma level. At the time of collection of the second blood samples performed after 7 days, 24% of the patients were under the TRR. Conclusion We have found the surprisingly high incidence of plasma levels under the TRR in patients treated with LAI AP. Notwithstanding the individual variability in pharmacokinetics, it seems the LAI AP may be underdosed in the usual clinical practice.

“Long-acting” olanzapine in maintenance therapy of schizophrenia: A study with plasma levels

2014 ◽  
Vol 19 (2) ◽  
pp. 99-105 ◽  
Author(s):  
Massimo C. Mauri ◽  
Michele Maffini ◽  
Chiara Di Pace ◽  
Alessandra Reggiori ◽  
Silvia Paletta ◽  
...  
Keyword(s):  
Maintenance Therapy ◽  
Plasma Levels ◽  
Long Acting

The Novel Antipsychotic Drug Cariprazine and Cognition Enhancing Drugs: Indications for Their Use as an Add-on Therapy in Schizophrenia

2020 ◽  
Vol 26 ◽  
Author(s):  
Felix-Martin Werner ◽  
Rafael Coveñas
Keyword(s):  
Clinical Trials ◽  
Maintenance Therapy ◽  
Antipsychotic Drug ◽  
Cognitive Functions ◽  
Antipsychotic Drugs ◽  
Psychotic Disorders ◽  
Therapeutic Effects ◽  
Treatment Resistant ◽  
Long Acting ◽  
Novel Antipsychotic

Background: Schizophrenia and schizoaffective disorder are treated with antipsychotic drugs. Some patients show treatment-resistant forms of psychotic disorders and, in this case, they can be treated with clozapine. In these patients and based on previous reviews on novel antipsychotic drugs, it is important to know whether an add-on therapy with new drugs can ameliorate the positive and negative schizophrenic scale (PANSS) total score. Objective: The aim of this review is to suggest an appropriate treatment for patients with treatment-resistant forms of psychotic disorders. A combination of current available antipsychotic drugs with novel antipsychotic or modulating drugs might improve negative schizophrenic symptoms and cognitive function and thereby social functioning and quality of life. Results: The mechanisms of action, the therapeutic effects and the pharmacokinetic profiles of novel antipsychotic drugs such as cariprazine, brexipiprazole and lumateperone are up-dated. Published case reports of patients with treatmentresistant psychoses are also discussed. These patients were treated with clozapine but a high PANSS total score was observed. Only an add-on therapy with cariprazine improved the score and, above all, negative schizophrenic symptoms and cognitive functions. To ensure a constant antipsychotic drug concentration, long-acting injectable antipsychotic drugs may be a choice for a maintenance therapy in schizophrenia. New modulating drugs, such as receptor positive allosteric modulators (N-methyl-D-aspartate receptor; subtype 5 of the metabotropic glutamatergic receptor) and encenicline, an alpha7 nicotinic cholinergic receptor agonist, are being investigated in preclinical and clinical trials. Conclusion: In clinical trials, patients with treatment-resistant forms of psychosis should be examined to know whether a combination therapy with clozapine and a novel antipsychotic drug can ameliorate the PANSS total score. In schizophrenia, long-acting injectable antipsychotic drugs are a safe and tolerable maintenance therapy. In further clinical studies, it should be investigated whether patients with treatment-resistant forms of psychoses can improve negative schizophrenic symptoms and cognitive functions by an add-on therapy with cognition enhancing drugs.

Pharmacokinetics, safety, and tolerability of four 28-day cycle intramuscular injections for risperidone-ISM 75 mg in patients with schizophrenia: A phase-2 randomized study (PRISMA-2)

2016 ◽  
Vol 33 (S1) ◽  
pp. s240-s241 ◽  
Author(s):  
L. Anta ◽  
J. Llaudó ◽  
I. Ayani ◽  
B. Gorostidi ◽  
M. Monreal ◽  
...  
Keyword(s):  
Injection Site ◽  
Drug Administration ◽  
Randomized Study ◽  
Deltoid Muscle ◽  
Study Medication ◽  
Open Label ◽  
Active Moiety ◽  
Intramuscular Injections ◽  
Competing Interest ◽  
Long Acting

IntroductionRisperidone-ISM is a new long acting intramuscular formulation of risperidone, for monthly administration without oral supplementation.ObjectiveTo characterize the pharmacokinetic of risperidone over multiple intramuscular injections in patients with schizophrenia.MethodA multicenter, open label, two-arm, parallel design clinical trial was performed. Each patient received 4 intramuscular injections of 75 mg of risperidone-ISM in either, gluteal or deltoid muscle at 28-day intervals.ResultsA total of 70 patients were randomized, 67 received at least one dose of study medication. Preliminary data show that mean Cmax of the active moiety was achieved 24-48 hours (Tmax) after each administration and ranged over four consecutive doses from 39.6-53.2 ng/mL and 54.1-61 ng/mL, when given in gluteal or deltoid, respectively. All subjects achieved therapeutic levels (> 7.5 ng/mL for the active moiety) between 2-8 hours after drug administration. The mean concentrations were maintained above therapeutic levels throughout the 4-week dosing period. No significance changes across the study were observed, either on Positive and Negative Syndrome Scale or Extrapyramidal Symptoms Scale. Overall, 63 subjects (94%) experienced at least 1 Treatment Emergent Adverse Event (TEAE) during the study. One serious TEAE (dystonia) was related to study treatment. One death not related to study medication was informed. The most frequently reported TEAEs were hyperprolactinaemia (57.7%) and injection site pain (32.8%).ConclusionsRisperidone-ISM achieved therapeutic levels from the first hours after drug administration and provided a sustained release throughout the 4-weeks dosing period over multiple intramuscular injections independently of the injection site. Risperidone-ISM was found to be safe and well tolerated.Disclosure of interestThe authors have not supplied their declaration of competing interest.

scholarly journals Efficacy, Safety, and Durability of Long-Acting Cabotegravir and Rilpivirine in Adults With HIV-1 Infection: ~5-Year Results From the LATTE-2 Study

2021 ◽  
Author(s):  
Graham H R Smith ◽  
W Keith Henry ◽  
Daniel Podzamczer ◽  
Maria Del Mar Masiá ◽  
Christopher J Bettacchi ◽  
...  
Keyword(s):  
Antiretroviral Therapy ◽  
Adverse Events ◽  
Maintenance Therapy ◽  
Comparable Efficacy ◽  
Maintenance Period ◽  
Injection Site Reactions ◽  
Long Acting ◽  
Hiv 1 ◽  
Extension Period

Abstract Background In the LATTE-2 phase IIb study, long-acting (LA) injectable cabotegravir + rilpivirine dosed every 8 weeks (Q8W) or 4 weeks (Q4W) demonstrated comparable efficacy with daily oral antiretroviral therapy (ART) through 96 weeks in ART-naive adults with HIV-1. Here we report efficacy, tolerability, and safety of cabotegravir + rilpivirine LA over ~5 years. Methods After 20 weeks of oral cabotegravir + abacavir/lamivudine, participants were randomized to cabotegravir + rilpivirine LA Q8W or Q4W or continue oral ART through the 96-week maintenance period. In the extension period through Week 256, participants continued their current LA regimen (randomized Q8W/Q4W groups) or switched from oral ART to Q8W or Q4W LA therapy (extension-switch groups). Endpoints assessed included proportion of participants with HIV-1 RNA <50 copies/mL (Snapshot algorithm) and adverse events (AEs). Results At Week 256, 186 (81%) of 230 participants in randomized Q8W/Q4W groups and 41 (93%) of 44 participants in extension-switch groups had HIV-1 RNA <50 copies/mL. No protocol-defined virologic failures occurred after Week 48. Injection-site reactions infrequently resulted in discontinuation (4 [2%] and 1 [2%] participants in randomized Q8W/Q4W and extension-switch groups, respectively). Three participants in randomized Q8W/Q4W groups experienced drug-related serious AEs, including 1 fatal serious AE (Q4W group); none occurred in extension-switch groups. Of 25 participants with AEs leading to withdrawal, 20 were in the randomized Q4W group; no AE leading to withdrawal occurred in >1 participant. Conclusions Cabotegravir + rilpivirine LA exhibited long-term efficacy and tolerability, demonstrating its durability as maintenance therapy for HIV-1 infection (ClinicalTrials.gov, NCT02120352).

Long-acting antibacterial agents

1970 ◽  
Vol 8 (26) ◽  
pp. 101-103
Keyword(s):  
Plasma Proteins ◽  
Antibacterial Agents ◽  
Renal Excretion ◽  
Slow Release ◽  
Blood Levels ◽  
Prolonged Action ◽  
Procaine Penicillin ◽  
High Doses ◽  
Long Acting ◽  
Release Form

A number of antibacterial agents have recently been developed which are recommended because they need to be administered infrequently. Examples are Deteclo (Lederle), Kelfizine W (Pharmitalia), and Vibramycin (Pfizer). The advantage claimed for these preparations is that adequate blood levels can be maintained with infrequent dosage. A prolonged action may be achieved in various ways - for example, by using a mixture of antibiotics which are absorbed and excreted at different rates, as in Deteclo;1 by giving high doses of a well absorbed preparation which is slowly excreted, e. g. doxycycline (Vibramycin),2 by administration in a slow-release form, e. g. procaine penicillin; or by giving probenecid to lessen renal excretion. Where prolongation of action depends on increased binding to plasma proteins, the drug may be more likely to act as a hapten and so to induce allergic reactions.

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