Studies on the absorption of practically water-insoluble drugs following injection. IV. An approach for predicting relative intramuscular absorption rates of a drug in oily solution,aqueous suspension and aqueous surfactant solution in rats.

Hirano, Koichiro; Yamada, Hideo

doi:10.1248/cpb.29.1410

Cited by 14 publications

(5 citation statements)

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“…Good injection technique (proper administration into striated muscle fibers, slow injection, sufficient shaking of the suspension prior to injection) not only gives proper disposition but it also mitigates pain and injury . Owing to the aqueous nature of PP formulations (aqueous solutions aid in rapid absorption, injection site pain was minimal at baseline and started declining with subsequent injections. Patients experiencing more pain regardless of volume at deltoid muscles (higher VAS scores) may be explained by the fact that deltoid muscles are smaller than gluteal muscles.…”

Section: Discussionmentioning

confidence: 99%

An assessment of injection site reaction and injection site pain of 1-month and 3-month long-acting injectable formulations of paliperidone palmitate

Sliwa

Savitz

Nuamah

et al. 2018

Perspect Psychiatr Care

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Section: Discussionmentioning

confidence: 99%

An assessment of injection site reaction and injection site pain of 1-month and 3-month long-acting injectable formulations of paliperidone palmitate

Sliwa

Savitz

Nuamah

et al. 2018

Perspect Psychiatr Care

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“…The first LAI introduced to the pharmaceutical market was fluphenazine in the form of enanthate and decanoate. These formulations were approved in 1966 in the context of the huge deinstitutionalisation of subjects with serious psychiatric diseases and the subsequent need for effective community-based therapy [ 36 ]. Table 2 summarizes FGAs and SGAs available in the form of LAIs.…”

Section: Long-acting Injectable (Lai) Antipsychoticsmentioning

confidence: 99%

“…Therapy with LAIs should be considered for subjects with recent-onset schizophrenia and those with risk factors for medication non-compliance (such as a history of non-adherence, severe symptoms, comorbid substance use, cognitive impairment, etc.) [ 36 ]. They are intended for individuals requiring a long-term antipsychotic therapy lasting at least several months [ 37 ].…”

Section: Long-acting Injectable (Lai) Antipsychoticsmentioning

confidence: 99%

Long-Acting Injectable Antipsychotics—A Review on Formulation and In Vitro Dissolution

Markowicz-Piasecka,

Kubisiak,

Asendrych-Wicik

et al. 2023

Pharmaceutics

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Long-acting injectable (LAI) neuroleptics constitute an effective therapeutical alternative for individuals suffering from persistent mental illness. These injectable pharmaceuticals help patients manage their condition better and improve long-term outcomes by preventing relapses and improving compliance. This review aims to analyse the current formulation aspects of LAI neuroleptics, with particular emphasis on analysis of drug release profiles as a critical test to guarantee drug quality and relevant therapeutical activity. While there is no officially approved procedure for depot parenteral drug formulations, various dissolution tests which were developed by LAI manufacturers are described. In vitro dissolution tests also possess a critical function in the estimation of the in vivo performance of a drug formulation. For that reason, thorough inspection of the in vitro–in vivo correlation (IVIVC) is also discussed.

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“…It has been reported that firstgeneration LAI antipsychotics may be associated with a higher rate of pain and injection site reactions due to the oily vehicle they are administered in. [12][13][14][15] Frequent large volume administrations of these oil-based injections have also been reported to be associated with the development of muscle fibrosis and granuloma. 15 Considering the relatively limited attention that has been paid to non-systemic side effects associated with LAI antipsychotics, and which are rarely reported in clinical trials, this study aims to systematically review all the available evidence reporting injection-site adverse effects associated with the administration of LAI antipsychotics.…”

Section: Introductionmentioning

confidence: 99%

Long-Acting Injectable Antipsychotics: A Systematic Review of Their Non-Systemic Adverse Effect Profile

Zolezzi¹,

Abouelhassan²,

Eltorki³

et al. 2021

NDT

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Introduction Long acting injectable (LAI) antipsychotics are commonly used in the treatment of schizophrenia to improve adherence and clinical outcomes. Concerns have been reported in relation to their non-systemic or injection site adverse effect profile. As such, this study aims to review and evaluate all evidence reporting injection site adverse effects with LAI antipsychotics. Methods An electronic search was systematically conducted through four databases (PubMed, Embase, SCOPUS, Cochrane) in order to identify studies investigating injection-site reactions associated with LAI antipsychotics. Unpublished studies such as conference proceedings and clinical trial registries were also searched. The search was limited to literature published in English without year limits. Results Of a total of 189 citations that were identified from the electronic database search, 12 were selected for inclusion in this review. Various injection site reactions were reported in these studies, including pain, bleeding, and swelling. Overall, the studies reported a low incidence of these injection site reactions. Only a minority of the included articles compared injection site reactions between different LAI antipsychotics. Conclusion Injection site pain was the most commonly reported injection site adverse effect across all articles reviewed. The low incidence of injection site adverse effects associated with LAI antipsychotics indicates that these formulations appear to be well tolerated by patients. More head-to-head trials comparing second generation LAI antipsychotics are needed.

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Studies on the absorption of practically water-insoluble drugs following injection. IV. An approach for predicting relative intramuscular absorption rates of a drug in oily solution,aqueous suspension and aqueous surfactant solution in rats.

Cited by 14 publications

References 1 publication

An assessment of injection site reaction and injection site pain of 1-month and 3-month long-acting injectable formulations of paliperidone palmitate

An assessment of injection site reaction and injection site pain of 1-month and 3-month long-acting injectable formulations of paliperidone palmitate

Long-Acting Injectable Antipsychotics—A Review on Formulation and In Vitro Dissolution

Long-Acting Injectable Antipsychotics: A Systematic Review of Their Non-Systemic Adverse Effect Profile

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