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Efficacy and safety of diphenylcyclopropenone among Chinese patients with steroid resistant and extensive alopecia areata

Luk NM, Chiu LS, Lee KC, Chau CT, Lee VW, Chang M, et al.

J Eur Acad Dermatol Venereol, 2013 Mar;27(3):e400-5.
PMID: 23057682 DOI: 10.1111/jdv.12009

BACKGROUND: Topical immunotherapy has recently been found useful in the treatment of chronic and extensive Alopecia Areata (AA).
OBJECTIVE: To evaluate the efficacy and safety of diphenylcyclopropenone (DPCP) use among Chinese patients with steroid resistant and extensive AA in our institute.
METHODS: The medical records of 31 Chinese patients treated with DPCP were analysed retrospectively. The efficacy, adverse effects, and relapse rate of DPCP treatment were reviewed.
RESULTS: Thirty-one (16 male, 15 female) Chinese patients with extensive, steroid resistant Alopecia Areata and a mean age of 28.9 years (SE 10.4) were treated. The mean age of onset was 17.8 years (SE 8.8) with an average disease duration of 11.2 years (SE 7.7). Ten patients had a history of atopy and 4 had a history of thyroid disease. Nail changes were found in 14 patients and a family history of AA was found in 2 patients. Thirteen patients (41.9%) had experienced total hair loss. Two patients abandoned the treatment due to severe side effects. Of the remaining 29 patients, 4 (13.8%), 7 (24.1%), 5 (17.2%), and 13 (44.8%) achieved >90% complete response, >50-90% partial response, >10-50% minimal response, and <10% no response hair regrowth, respectively. Adverse effects included pruritus, erythema, vesiculation, scaling, cervical lymphadenopathy, dyspigmentation and urticarial reactions. Relapse occurred (>25% hair loss) in 69.23% of patients after 18 months of follow up.
CONCLUSIONS: DPCP is an effective and tolerable treatment for Chinese patients with extensive, steroid resistant AA.

Matched MeSH terms: Cyclopropanes/adverse effects; Cyclopropanes/therapeutic use*
Development of LC-MS/MS method and application to bioequivalence study of a light sensitive drug montelukast

Wong EYL, Loh GOK, Tan YTF, Peh KK

Drug Dev Ind Pharm, 2021 Feb;47(2):197-206.
PMID: 33300818 DOI: 10.1080/03639045.2020.1862177

OBJECTIVE: The aim of the study was to develop a simple, highthroughput and sensitive LC-MS/MS method and apply to a bioequivalence study of montelukast, a light sensitive drug.
METHOD: The effects of organic modifiers in mobile phase, protein precipitation agent to plasma sample ratio, and light on montelukast stability in unprocessed and processed human plasma, were evaluated. Validation was conducted in accordance with European Medicines Agency Guideline on bioanalytical method validation.
RESULTS: No interference peak was observed when acetonitrile was used as an organic modifier. Acetonitrile to plasma ratio of 4:1 produced clean plasma sample. Approximately 3 % of cis isomer was detected in unprocessed plasma samples while 21 % of cis isomer was detected in processed plasma samples after exposing to fluorescent light for 24h. The standard calibration curve was linear over 3.00-1200.00 ng/mL. All method validation parameters were within the acceptance criteria.
CONCLUSION: The validated method was successfully applied to a bioequivalence study of two montelukast formulations involving 24 healthy Malaysian volunteers. The light stability of a light sensitive drug in unprocessed and processed human plasma samples should be studied prior to pharmacokinetic/bioequivalence studies. Measures could then be taken to protect the analyte in human plasma from light degradation.

Matched MeSH terms: Cyclopropanes/pharmacology*; Cyclopropanes/chemistry
Fulltext Extending ‘Kampuchea’ guava shelf-life at 27oC using 1-methylcyclopropene

Phebe, D., Ong, P.T.

International Food Research Journal, 2010;17(1):63-69.
MyJurnal

‘Kampuchea’ guavas were treated with 300, 600 and 900 nL L‾¹ 1-methylcyclopropene (1-MCP) for 0,
3 and 6 h, and stored at 27˚C with 70% relative humidity. The C* values, soluble solids concentration, titratable acidity and pH of these fruits were not affected by both the 1-MCP concentrations and exposure duration while h˚ values and flesh firmness were affected by these treatments. The L* values, vitamin C content and weight loss were affected by the concentrations of 1-MCP, but not by the exposure duration. Less weight loss and disease incidence in fruit treated with 600 and 900 nL L-1 1-MCP. Fruit exposed to 6 h 1-MCP showed lowest disease incidence compared to other exposure duration in 5 days of storage. Treating Kampuchea guava fruit with 600 nL L‾¹ 1-MCP and exposure duration of 6 h was able to retain fruit colour, flesh firmness and delayed disease development for 5 days.

Matched MeSH terms: Cyclopropanes
Fulltext Laboratory evaluation of three commercial coil products for protection efficacy against Anopheles gambiae from southern Ghana: a preliminary study

Avicor SW, Wajidi M FF, Jaal Z

Trop Biomed, 2015 Jun;32(2):386-9.
PMID: 26691267 MyJurnal

Residents in irrigated urban agricultural sites face numerous mosquito problems such as increased mosquito populations and reduced insecticides susceptibility due to the creation of mosquito breeding sites and agricultural use of insecticides and hence require effective protective products against them. In this study, the protection effectiveness of three pyrethroid formulated mosquito coils of Malaysian origin against Anopheles gambiae sensu lato from an irrigated urban agricultural site in Ghana were evaluated for their potential use. Sucrose fed An. gambiae s.l. were exposed to insecticide-containing coils in a 70 cm x 70 cm x 70 cm glass chamber to assess the insecticidal effect of the coils. The 0.005% metofluthrin coil caused the most rapid knockdown of 50% of the test mosquitoes. The mean lethal effect of the coils on An. gambiae s.l. were as follows; 0.005% metofluthrin (86%), 0.3% d-allethrin (74.33%), 0.15% d-trans allethrin (72%) and the 0.25% d-allethrin reference coil (69%). The 0.005% metofluthrin coil achieved the highest insecticidal effect on An. gambiae s.l. compared to the other coils and hence performed better than the others as an anti-mosquito product. All the three test coils were effective against An. gambaie s.l. from the irrigated agricultural site compared to the reference coil.

Matched MeSH terms: Cyclopropanes/pharmacology
Fulltext Lack of insecticidal effect of mosquito coils containing either metofluthrin or esbiothrin on Anopheles gambiae sensu lato mosquitoes

Lukwa N, Chiwade T

Trop Biomed, 2008 Dec;25(3):191-5.
PMID: 19287356

Use of mosquito coils for personal protection against malaria and mosquito nuisance is advocated under mosquito and malaria control programmes. We performed field studies of mosquito coils containing either metofluthrin or esbiothrin in experimental huts situated in Kamhororo village, Gokwe district, Zimbabwe. All tests were performed on 3-5 day old reared female Anopheles gambiae sensu lato mosquitoes. The burning times were 9hr 20min for mosquito coils containing metofluthrin and 8 hr for those containing esbiothrin and the results were significantly different (p = <0.001). The mean knock down rate for mosquito coils containing metofluthrin was 90% and that for esbiothrin was 73.3% and the results were significantly different (p = 0.00). Mosquito coils containing metofluthrin had a mean repellence of 92.7% as compared to 85.4% for esbiothrin and the results were not significantly different (p=0.27). The protection time as required by EPA (1999) was 6 hr for mosquito coils containing metofluthrin and 5 hr for those containing esbiothrin. The mean insecticidal effect of mosquito coils containing metofluthrin was 84% as compared to 83% for those containing esbiothrin and the results were not significantly different (p = 0.56). Both mosquito formulations could not be classified as having insecticidal effect since none of them met the 95% mortality rate criteria.

Matched MeSH terms: Cyclopropanes/pharmacology*
Fulltext Effects of 1-methylcyclopropene and modified atmosphere packaging on the antioxidant capacity in pepper "Kulai" during low-temperature storage

Tan CK, Ali ZM, Ismail I, Zainal Z

ScientificWorldJournal, 2012;2012:474801.
PMID: 22919322 DOI: 10.1100/2012/474801

The objective of the present study was to simultaneously evaluate the effect of a postharvest treatment on the pepper's antioxidant content and its ability to retain its economical value during the postharvest period. The fruits were pretreated by modified atmosphere packaging (MAP) with or without treatment with 1-methylcyclopropene (1-MCP) before cold storage at 10°C. Changes in the levels of non-enzymatic antioxidants, including the total phenolic, ascorbic acid levels and the total glutathione level, as well as enzymatic antioxidants, including ascorbate peroxidase (APX), glutathione reductase (GR), and catalase (CAT), were determined. Both treatments successfully extended the shelf life of the fruit for up to 25 days, and a high level of antioxidant capacity was maintained throughout the storage period. However, 1-MCP treatment maintained the high antioxidant capacity for a longer period of time. The 1-MCP-treated peppers maintained high levels of phenolic content, a high reduced glutathione (GSH)/oxidised glutathione (GSSG) ratio, decreased levels of ascorbic acid and CAT activity, and increased levels of APX and GR compared with the peppers that were not treated with 1-MCP. The overall results suggested that a combination of 1-MCP and MAP was the most effective treatment for extending shelf life while retaining the nutritional benefits.

Matched MeSH terms: Cyclopropanes/chemistry*
Bioefficacy Evaluation of Commercial Mosquito Coils Containing Metofluthrin, d-Allethrin, d-Trans Allethrin, and Prallethrin Against Aedes albopictus (Diptera: Culicidae) in Malaysia

Chen CD, Chin AC, Lau KW, Low VL, Lee HL, Lee PKY, et al.

J Med Entomol, 2018 10 25;55(6):1651-1655.
PMID: 30085203 DOI: 10.1093/jme/tjy130

The bioefficacy of commercial mosquito coils containing four different active ingredients, namely metofluthrin, d-allethrin, d-trans allethrin, and prallethrin against Aedes albopictus (Skuse) (Diptera: Culicidae) from 10 states in Malaysia, was evaluated using the glass chamber method. In this study, Ae. albopictus exhibited various knockdown rates (50% knockdown time, KT50), ranging from 2.50 to 5.00 min, 2.50 to 7.00 min, 3.00 to 8.00 min, and 5.00 to 17.00 min for metofluthrin, d-trans allethrin, d-allethrin, and prallethrin, respectively. Overall, all strains of Ae. albopictus were most susceptible to metofluthrin, with mortality rates >80%. On the other hand, mortality rates ranging from 5.0 to 100% were observed from all populations exposed to d-trans allethrin, d-allethrin, and prallethrin. In addition, significant correlations between KT50 of metofluthrin and d-allethrin (r = 0.758, P = 0.011), metofluthrin and prallethrin (r = 0.676, P = 0.032), d-allethrin and d-trans allethrin (r = 0.832, P = 0.003), d-allethrin and prallethrin (r = 0.921, P = 0.000), and d-trans allethrin with prallethrin (r = 0.941, P = 0.000) were detected, suggesting some levels of cross-resistance within the pyrethroid insecticides. This study demonstrated that metofluthrin can induce high insecticidal activity in Ae. albopictus in Malaysia, followed by d-trans allethrin, d-allethrin, and prallethrin.

Matched MeSH terms: Cyclopropanes
Population pharmacokinetics of ravidasvir in adults with chronic hepatitis C virus infection and impact of antiretroviral treatment

Panjasawatwong N, Avihingsanon A, Menétrey C, Ribeiro I, Salvadori N, Swanson A, et al.

Antimicrob Agents Chemother, 2024 Jul 09;68(7):e0000824.
PMID: 38767383 DOI: 10.1128/aac.00008-24

Ravidasvir (RDV) is a novel NS5A inhibitor that exhibits potent pan-genotypic inhibition of hepatitis C virus (HCV) replication. Sofosbuvir (SOF) plus RDV was demonstrated to be efficacious and safe in adults with active HCV infection, including those living with HIV (LWHIV), in the STORM-C-1 trial. We assessed the population pharmacokinetics (PK) of RDV in a sub-study nested within STORM-C-1 conducted in Thailand and Malaysia. SOF (400 mg) plus RDV (200 mg) was administered orally once daily for 12 weeks to adults with chronic HCV infection, but without cirrhosis and for 24 weeks to those with compensated cirrhosis. Intensive and sparse PK samples were collected at 4, 8, and 12 weeks after treatment initiation. Population PK parameters of RDV and the impact of covariates were evaluated using nonlinear mixed-effects modeling. Five hundred ninety-four participants were included, 235 (40%) had compensated cirrhosis, and 189 (32%) were LWHIV. RDV plasma concentrations were best described by a two-compartment model with first-order elimination. Oral clearance (CL/F) and volume of distribution (Vd/F) parameters were allometrically scaled on fat-free mass. Concomitant antiretroviral treatment (ART) increased RDV CL/F by 30%-60%, with efavirenz-based ART having the largest impact. Females had 16% lower RDV CL/F than males, and higher albumin levels reduced RDV central volume of distribution. While several covariates impact RDV CL/F and Vd/F, the effect on RDV exposures was not clinically relevant based on the efficacy data reported in this diverse Asian adult population. There were no meaningful drug-drug interactions in adults LWHIV on ART.

Matched MeSH terms: Cyclopropanes
Fulltext Treatment outcomes of sofosbuvir/velpatasvir/voxilaprevir among NS5A inhibitor-experienced patients with hepatitis C: Real-world data from a multicenter Asian registry

Wong YJ, Kumar R, Kumar R, Tan J, Liu CH, Hui VK, et al.

J Gastroenterol Hepatol, 2022 Aug;37(8):1642-1644.
PMID: 35723645 DOI: 10.1111/jgh.15918
Matched MeSH terms: Cyclopropanes
Fulltext Evaluation of Selected Outcomes of Combination Antiretroviral Therapy: Yemen Cohort Retrospective Descriptive Studies

Nabih MF, Puteh SEW, Nur AM

Sci Rep, 2019 12 27;9(1):19923.
PMID: 31882645 DOI: 10.1038/s41598-019-56314-0

In 2007, HIV treatment services were established in five main governorates out of twenty-two which resulted in low access to services and poor treatment outcomes. The main goal of this study was to evaluate and analyse the selected treatment outcomes of eight cohorts of PLHIV who were treated with cART during 2007-2014. The method used was a retrospective descriptive study of 1,703 PLHIV who initiated cART at five public health facilities. The results: Retention rate was less than 80%, male: female ratio 1.661, with a mean age of 35 years (±9.2 SD), 85% had been infected with HIV via heterosexual contact. 65% of patients presented with clinical stages 3 and 4, and 52% of them were initiated cART at a CD4 T-cell count ≤200 cells/mm. 61% of cART included Tenofovir and Efavirenz. TB treatment started for 5% of PLHIV, and 22% developed HIV-related clinical manifestations after cART initiation. 67% of PLHIV had experienced cART substitution. The mean AIDS-mortality rate was 15% and the mean LTFU rate was 16%. Conclusion: Although cART showed effectiveness in public health, mobilization of resources and formulation of better health policies are important steps toward improving access to cART and achieving the desired treatment outcomes.

Matched MeSH terms: Cyclopropanes