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Background: While effective, DAc injections for submental fat (SMF) reduction carry risks, including vascular damage and skin necrosis when improperly administered. This study presents a novel approach to SMF reduction using blunt microcannulas for DAc injections, coupled with 3D stereophotogrammetry quantification (3D-SQ). Clinical presentation: A 47-year-old female with SMF underwent two DAc applications. 3D-SQ was performed before and after each treatment using a 3D-SQ system. The patient experienced a substantial total volume reduction of 14.81 mL in the submental area after two DAc applications. 3D-SQ analysis showed a gradual reduction in submental volume over time. Importantly, no serious adverse events were reported, with only minor pain and warmth at the treated site. The reduction of SMF through DAc injections involves adipocyte cell lysis, emphasizing the importance of proper injection technique to avoid adverse events. The use of blunt microcannulas offers a safer alternative, minimizing the risk of skin necrosis, ulceration, and intra-arterial injections. Additionally, cannulas reduce bruising due to their blunt design and fan technique, enhancing patient comfort and safety. Conclusion: This case report highlights the efficacy of a novel cannula approach for DAc SMF reduction, assessed by 3D-SQ. Blunt microcannulas may represent a safer option compared to hypodermic needles, reducing the likelihood of severe complications.
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Lipolytic substance injections to reduce localized fat have been extensively used because it is a low-invasive method. This review aimed to evaluate the efficacy and safety of deoxycholic acid in submental fat reduction compared to a placebo and investigate the potential industry sponsorship bias in the results of randomized clinical trials on this topic. Ten electronic databases were extensively searched for randomized clinical trials without restriction on language and year of publication. Two reviewers extracted the data and assessed the individual risk of bias in the studies with the RoB 2.0 tool. The industry sponsorship bias was evaluated according to citations in the articles regarding industry funding/sponsorship throughout the texts. Fixed and random effects meta-analyses were performed, and the results were reported in Risk Ratio (RR) at a 95% Confidence Interval (95% CI). The initial search provided 5756 results, of which only five were included. Only two studies had a low risk of bias. All studies showed a potential industry bias. The meta-analysis showed that patients treated with deoxycholic acid had significant positive results for all efficacy outcomes and a higher risk of fibrosis, pain, erythema, numbness, swelling, edema, pruritus, nodules, headache, and paresthesia. The low to moderate certainty of evidence found allows concluding that deoxycholic acid is effective in submental fat reduction, causing well-tolerated adverse effects. However, all eligible studies showed a potential industry bias.
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Ácido Desoxicólico , Dor , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , ViésRESUMO
Abstract Lipolytic substance injections to reduce localized fat have been extensively used because it is a low-invasive method. This review aimed to evaluate the efficacy and safety of deoxycholic acid in submental fat reduction compared to a placebo and investigate the potential industry sponsorship bias in the results of randomized clinical trials on this topic. Ten electronic databases were extensively searched for randomized clinical trials without restriction on language and year of publication. Two reviewers extracted the data and assessed the individual risk of bias in the studies with the RoB 2.0 tool. The industry sponsorship bias was evaluated according to citations in the articles regarding industry funding/sponsorship throughout the texts. Fixed and random effects meta-analyses were performed, and the results were reported in Risk Ratio (RR) at a 95% Confidence Interval (95% CI). The initial search provided 5756 results, of which only five were included. Only two studies had a low risk of bias. All studies showed a potential industry bias. The meta-analysis showed that patients treated with deoxycholic acid had significant positive results for all efficacy outcomes and a higher risk of fibrosis, pain, erythema, numbness, swelling, edema, pruritus, nodules, headache, and paresthesia. The low to moderate certainty of evidence found allows concluding that deoxycholic acid is effective in submental fat reduction, causing well-tolerated adverse effects. However, all eligible studies showed a potential industry bias.
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The intestine has a very important role in the homeostasis of the internal medium. Bile acids play a regulatory role in the digestion and absorption of nutrients. Among them, deoxycholic acid, when its luminal concentration increases due to bacterial overgrowth, modifies hydroelectrolytic transport, producing an increase in the volume of water and electrolytes in stools.
El intestino tiene un papel muy importante en la homeostasis del medio interno. Los ácidos biliares cumplen una función reguladora en la digestión y absorción de nutrientes. Entre ellos el ácido deoxicólico, cuando aumenta su concentración luminal por sobrecrecimiento bacteriano, modifica el transporte hidroelectrolítico produciendo aumento del volumen de agua y electrolitos en las deposiciones.
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Animais , Ratos , Equilíbrio Hidroeletrolítico , Ácido Desoxicólico , Intestinos , Sódio/metabolismo , Ratos Sprague-Dawley , Homeostase , Canais IônicosRESUMO
The accumulation of submental fat (SMF) can negatively impact facial harmony appearance, and one alternative treatment for this condition is the application of deoxycholic acid (DOC). The objective of this systematic review was to answer the following question: "Is DOC able to reduce SMF and increase patient satisfaction when compared to the placebo groups?". Therefore, a detailed search strategy was carried out in 6 scientific databases (PubMed, Scopus, Embase, Lilacs, SciELO, and Web of Science) as primary search sources, while OpenGrey and OpenThesis were also used to capture the "grey literature". Only six studies met all inclusion criteria and were considered in this review analysis. The selected sample included prospective clinical studies published from 2014 to 2018, covering a total sample of 3488 patients, with an average age ranging from 46 to 49.5 years old. All selected articles evaluated the effect of DOC at concentrations of 1 mg/cm² or 2 mg/cm², using saline or placebo as control solutions for the comparative analysis. The application interval was 28 days in all studies analyzed, and the treatment duration ranged from 4 to 6 weeks. In all studies evaluated, there was a reduction in SMF and patient satisfaction with the application of DOC was higher than in the control groups at the end of a 12-week period. Thus, it is possible to conclude that the application of DOC has a positive effect on reducing SMF and improving patient satisfaction concerning their facial appearance.
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Técnicas Cosméticas , Ácido Desoxicólico , Humanos , Pessoa de Meia-Idade , Satisfação do Paciente , Injeções Subcutâneas , Estudos ProspectivosRESUMO
OBJECTIVE: We aimed to evaluate the effects of the deoxycholic acid (DCA) in the submental and subplantar regions of rats, and to histologically analyze the changes caused in the submandibular glands, soft tissues of the paw, and inguinal adipose tissue. MATERIAL AND METHODS: Sixty male Wistar rats were divided into DCA and control (CG) groups. DCA was injected in the submental, inguinal, and subplantar regions, and saline was injected in the CG. The animals were euthanized after 24 h and at 7 and 21 days. RESULTS: The DCA group showed edema in the submental region in 24 h and in the paw in all experimental times. In the paw there were also erythema and ulceration in 7 days, and alopecia after 21 days. At 21 days, a few animals also showed erythema and ulceration in paw; however, there was no significant difference from CG. Histological analysis of the paw showed an intense inflammatory process, with a predominance of neutrophils, lymphocytes, and plasma cells in 24 h and 7 days. In the adipose tissue, we observed loss of architecture and inflammatory infiltrate, followed with a lower number of adipose cells, and at 21 days, fibroplasia. In the submandibular glands we observed inflammatory infiltration, loss of tissue architecture, and fibrosis. CONCLUSIONS: DCA produces a significant inflammatory process in the structures. It can cause skin ulcerations and, in salivary glands, it causes loss of tissue architecture and fibrosis. CLINICAL RELEVANCE: There has been growing increase in the use of DCA for aesthetic purposes by health care providers. Due to the presence of important anatomical structures in the submental region, constant vigilance is required to report new adverse effects.
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Ácido Desoxicólico , Glândula Submandibular , Tecido Adiposo , Animais , Ácido Desoxicólico/toxicidade , Estética Dentária , Masculino , Ratos , Ratos WistarRESUMO
A busca por procedimentos estéticos voltados para a perda de definição do submento é crescente. Um correto diagnóstico é imperativo para o sucesso do tratamento e redução das complicações. Adiposidade localizada, flacidez cutânea e perda da estrutura óssea são os principais achados. Um algoritmo de tratamento foi discutido nesta revisão, lembrando-se, claro, da possibilidade de tratamentos combinados e sequenciais para melhores resultados
The search for aesthetic procedures aimed at the loss of submental definition is increasing. A correct diagnosis is imperative for successful treatment and the reduction of complications. Localized adiposity, skin flaccidity, and loss of bone structure are the main findings. A treatment algorithm was discussed in this review, remembering, of course, the possibility of combined and sequential treatments for better results.
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Objective: To investigate the efficacy and safety of deoxycholic acid (DOC) for SMF reduction.Methods: We conducted a systematic review and meta-analysis of randomized controlled trials. We searched PubMed/MEDLINE, EMBASE, and Cochrane databases until June 2020. Efficacy outcomes: Clinician-Reported Submental Fat Rating Scale; Patient-Reported Submental Fat Rating Scale; Subject Self-Rating Scale; SMF reduction measured using caliper and resonance magnetic imaging; Early therapeutic success. Safety outcomes: Withdrawals due to adverse events (AEs), Rates of AEs, Skin laxity.Results: Five studies were included, comprising 1,838 participants. DOC (1 or 2 mg/cm2) had greater improvement in all efficacy measures compared to placebo. No differences were seen between both doses of DOC. Withdrawals due to AEs were low with 1 and 2 mg/cm2 of DOC (6.8% vs. 9.9%, respectively), and there was no difference between the two doses (p = 0.22). AEs were usually associated with the injection site, were predominantly transient, and commonly resolved within the treatment session interval. Injection site pain, hematoma, anesthesia/numbness, erythema, and swelling/edema were the most common AEs. There was no difference in their prevalence between both doses of DOC.Conclusions: DOC is effective and safe for SMF reduction with no differences between doses of 1 and 2 mg/cm2.
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Técnicas Cosméticas , Ácido Desoxicólico/administração & dosagem , Gordura Subcutânea/efeitos dos fármacos , Queixo , Colagogos e Coleréticos/administração & dosagem , Colagogos e Coleréticos/efeitos adversos , Ácido Desoxicólico/efeitos adversos , Humanos , Injeções Subcutâneas , Imageamento por Ressonância Magnética , Pescoço , Ensaios Clínicos Controlados Aleatórios como AssuntoRESUMO
BACKGROUND: Deoxycholic acid (DCA) was developed by the pharmaceutical industry for aesthetical use in submental fat reduction. It represents the first lipolytic substance approved by the Food and Drug Administration (FDA) for fat reduction in that area. AIMS: This study presents an update of properties and the use of DCA, as well as adverse events and possible complications. METHODS: A search in MEDLINE/PubMed, Cochrane, and Bireme/LILACS databases was performed using the terms: "deoxycholic acid" OR "ATX-101" AND "injection" NOT "amphotericin" NOT "biliary" NOT "bile." Experimental studies developed in animals, clinical trials, literature reviews, case reports, and letters to the editor that included the DCA mechanism of action, dose, manner of use, adverse effects, and complications were selected. RESULTS: The most frequent adverse events are edema, local pain, bruise, and numbness, which usually spontaneously regress. However, complications, including, skin necrosis, nerve injury, alopecia, and vascular events, can occur, demanding complex management without specific protocols. CONCLUSION: Although DCA is beneficial for lysis of adipose tissue, clinicians should be aware about the adverse effects and risks involved with the use of this substance. The knowledge of local anatomy, properties, and adverse effects are fundamental to treatment with DCA.
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Técnicas Cosméticas , Ácido Desoxicólico , Tecido Adiposo , Animais , Técnicas Cosméticas/efeitos adversos , Ácido Desoxicólico/efeitos adversos , Injeções , LipóliseRESUMO
The search for new drugs for the treatment of leishmaniasis is an important strategy for improving the current therapeutic arsenal for the disease. There are several limitations to the available drugs including high toxicity, low efficacy, prolonged parenteral administration, and high costs. Steroids are a diverse group of compounds with various applications in pharmacology. However, the antileishmanial activity of this class of molecules has not yet been explored. Therefore, in the present study, we investigated the antileishmanial activity and cytotoxicity of novel steroids against murine macrophages with a focus on the derivatives of cholesterol (CD), cholic acid (CA), and deoxycholic acid (DA). Furthermore, the mechanism of action of the best compound was assessed, and in silico studies to evaluate the physicochemical and pharmacokinetic properties were also conducted. Among the sixteen derivatives, schiffbase2, CD2 and deoxycholic acid derivatives (DOCADs) were effective against promastigotes of Leishmania species. Despite their low toxicity to macrophages, the majority of DOCADs were active against intracellular amastigotes of L. amazonensis, and DOCAD5 exhibited the best biological effect against these parasitic stages (IC50 = 15.34 µM). Neither the CA derivatives (CAD) nor DA alone inhibited the intracellular parasites. Thus, the absence of hydroxyl in the C-7 position of the steroid nucleus, as well as the modification of the acid group in DOCADs were considered important for antileishmanial activity. The treatment of L. amazonensis promastigote forms with DOCAD5 induced biochemical changes such as depolarization of the mitochondrial membrane potential, increased ROS production and cell cycle arrest. No alterations in parasite plasma membrane integrity were observed. In silico physicochemical and pharmacokinetic studies suggest that DOCAD5 could be a good candidate for an oral drug. The data demonstrate the potential antileishmanial effect of certain steroid derivatives and encourage new in vivo studies.
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Colesterol/farmacologia , Ácido Desoxicólico/farmacologia , Descoberta de Drogas/métodos , Leishmania/efeitos dos fármacos , Leishmaniose/tratamento farmacológico , Macrófagos Peritoneais/efeitos dos fármacos , Tripanossomicidas/farmacologia , Administração Oral , Animais , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Colesterol/análogos & derivados , Colesterol/síntese química , Colesterol/farmacocinética , Ácido Cólico/síntese química , Ácido Cólico/farmacocinética , Ácido Cólico/farmacologia , Ácido Desoxicólico/análogos & derivados , Ácido Desoxicólico/síntese química , Ácido Desoxicólico/farmacocinética , Relação Dose-Resposta a Droga , Leishmania/crescimento & desenvolvimento , Leishmania/metabolismo , Leishmaniose/parasitologia , Macrófagos Peritoneais/parasitologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Modelos Biológicos , Estrutura Molecular , Estresse Oxidativo/efeitos dos fármacos , Testes de Sensibilidade Parasitária , Relação Estrutura-Atividade , Tripanossomicidas/síntese química , Tripanossomicidas/farmacocinéticaRESUMO
Segundo relato de caso da literatura de alopecia em região de barba observada após terceira sessão de injeções de desoxicolato a 1% para redução de gordura submentoniana.
Second case report in the literature regarding beard alopecia observed after the third session of injections of 1% deoxycholic acid for reduction of submental fat.
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An improved synthesis route for obtaining known brassinosteroid analogues, i.e., methyl 2α,3α-dihydroxy-6-oxo-5α-cholan-24-oate (11), methyl 3α-hydroxy-6-oxo-7-oxa-5α-cholan-24-oate (15) and methyl 3α-hydroxy-6-oxa-7-oxo-5α-cholan-24-oate (16), from hyodeoxycholic acid (4) maintaining the native side chain is described. In the alternative procedure, the di-oxidized product 6, obtained in the oxidation of methyl hyodeoxycholate 5, was converted almost quantitatively into the target monoketone 7 by stereoselective reduction with NaBH4, increasing the overall yield of this synthetic route to 96.8%. The complete ¹H- and (13)C-NMR assignments for all compounds synthesized in this work have been made by 1D and 2D heteronuclear correlation gs-HSQC and gs-HMBC techniques. Thus, it was possible to update the spectroscopic information of ¹H-NMR and to accomplish a complete assignment of all (13)C-NMR signals for analogues 5-16, which were previously reported only in partial form.
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Ácido Desoxicólico , Fitosteróis/química , Fitosteróis/síntese química , Ácido Desoxicólico/análogos & derivados , Ácido Desoxicólico/química , Espectroscopia de Ressonância MagnéticaRESUMO
ABSTRACTPURPOSE:To assess whether deoxycholic acid (DOC) and lithocholic acid (LCA) administered in a period of six months in a concentration of 0.25% may have a carcinogenic role in mice colon.METHODS:The study used C57BL6 female mice divided into four groups. The control group received a balanced diet and the others received diets supplemented with 0.25% DOC, 0.25% LCA and 0.125% DOC+0.125% LCA, respectively. After euthanasia, the lesions found in the resected gastrointestinal tracts were stained with hematoxylin-eosin and examined microscopically.RESULTS:No gastrointestinal tract changes were observed in the control group, while hyperplastic Peyer's patches in the small intestine, flat adenomas with mild dysplasia and chronic colitis at the level of the colon were found in all three test groups. The colonic lesions prevailed in the proximal colon. The highest number of flat adenoma lesions (8), hyperplasia of Peyer's patches (25) and chronic colitis (2) were found in mice fed with diet and LCA.CONCLUSION: Precancerous or cancerous pathological lesions could not be identified. Instead, adenomatous colonic injuries occurred in a shorter period of time (six months), compared to the reported data.
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Animais , Feminino , Ácidos e Sais Biliares/toxicidade , Carcinógenos/toxicidade , Colagogos e Coleréticos/toxicidade , Colo/efeitos dos fármacos , Ácido Desoxicólico/toxicidade , Ácido Litocólico/toxicidade , Adenoma/induzido quimicamente , Testes de Carcinogenicidade , Colite/induzido quimicamente , Colo/patologia , Neoplasias do Colo/induzido quimicamente , Modelos Animais de Doenças , Fezes/química , Nódulos Linfáticos Agregados/efeitos dos fármacos , Fatores de TempoRESUMO
To assess whether deoxycholic acid (DOC) and lithocholic acid (LCA) administered in a period of six months in a concentration of 0.25% may have a carcinogenic role in mice colon. The study used C57BL6 female mice divided into four groups. The control group received a balanced diet and the others received diets supplemented with 0.25% DOC, 0.25% LCA and 0.125% DOC+0.125% LCA, respectively. After euthanasia, the lesions found in the resected gastrointestinal tracts were stained with hematoxylin-eosin and examined microscopically. No gastrointestinal tract changes were observed in the control group, while hyperplastic Peyer's patches in the small intestine, flat adenomas with mild dysplasia and chronic colitis at the level of the colon were found in all three test groups. The colonic lesions prevailed in the proximal colon. The highest number of flat adenoma lesions (8), hyperplasia of Peyer's patches (25) and chronic colitis (2) were found in mice fed with diet and LCA. Precancerous or cancerous pathological lesions could not be identified. Instead, adenomatous colonic injuries occurred in a shorter period of time (six months), compared to the reported data.(AU)
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Animais , Feminino , Ácidos e Sais Biliares/toxicidade , Carcinógenos/toxicidade , Colagogos e Coleréticos/toxicidade , Colo , Ácido Desoxicólico/toxicidade , Ácido Litocólico/toxicidade , Adenoma/induzido quimicamente , Testes de Carcinogenicidade , Colite/induzido quimicamente , Colo/patologia , Neoplasias do Colo/induzido quimicamente , Modelos Animais de Doenças , Fezes/química , Camundongos Endogâmicos C57BL , Nódulos Linfáticos Agregados , Fatores de TempoRESUMO
The potential of the buccal mucosa as an alternative route for the systemic delivery of donepezil (DPZ) hydrochloride, and the impact of various skin penetration enhancers on DPZ buccal permeability, was assessed using an in vitro model. DPZ was applied to porcine buccal mucosa in modified Ussing chambers either alone (20 µg/mL) or with different treatment protocols of various enhancers including Azone® (AZ), deoxycholic acid (DA), polyethylene glycol (PEG) 400, and oleic acid (OA)-PEG 400. DPZ permeated the buccal mucosa very rapidly with a permeability coefficient of 35.6 ± 4.9 × 10(-6) cm/s, which was not significantly affected by AZ pretreatment. Coapplication of DA 0.6% (w/w), but not DA 0.01% (w/w), reduced the buccal permeation of DPZ (3.5-fold), and PEG 400 reduced the absorption of DPZ in a dose-dependent manner (1.6- and 18.0-fold reduction at 5% and 50%, w/w, PEG 400, respectively). Coapplication of a combination of OA 1% (v/w) and PEG 400 5% (w/w) further reduced DPZ permeability (5.5-fold), which was demonstrated to result from excipient-induced DPZ precipitation as assessed by light microscopy analysis. These results confirm the feasibility of a novel buccal delivery system for Alzheimer's disease, and suggest various approaches that may be exploited for controlled buccal delivery of DPZ.