In vivo pharmacodynamic and pharmacokinetic interactions of Hibiscus sabdariffa calyces extracts with simvastatin.

WHAT IS KNOWN AND OBJECTIVES: Increasing number of patients use herbs with their medications. Such practice may result in beneficial or harmful herb-drug interactions. A recent survey reported that some participants co-administered Hibiscus sabdariffa, a widely used beverage, or tea, with their antihyperlipidaemic medications. This study therefore evaluated the effect of concomitant administration of Hibiscus sabdariffa calyces' extracts with simvastatin on hyperlipidaemia and pharmacokinetics of the drug in vivo. METHODS: Factorial experimental designs were used to evaluate the comparative effectiveness and interactions between simvastatin and aqueous extract of Hibiscus sabdariffa (AEHS) on lipid profile parameters in hyperlipidaemia-induced Wistar rats. Different combinations of low (AEHS 250 mg/kg; simvastatin 10 mg/kg) and high doses (AEHS 500 mg/kg; simvastatin 20 mg/kg) were administered individually and concurrently daily for 2 and 4 weeks. Lipid profile parameters were assessed at these treatment periods. Subsequently, the effect of aqueous beverage of Hibiscus sabdariffa (ABHS) on the pharmacokinetics of single-dose 40 mg simvastatin was also evaluated in six healthy human volunteers using two-period randomized crossover design. Blood samples were collected at predetermined times for 24 hours. The plasma obtained was analysed for simvastatin using RP-HPLC/UV method. RESULTS: Aqueous extract of Hibiscus sabdariffa reduced total cholesterol (Tc ) better than simvastatin (P = .031). Low-dose AEHS and low-dose simvastatin used concomitantly caused 38.3% and 57.4% reductions in Tc and triglyceride levels, respectively, compared with low-dose simvastatin (P < .05). Also, ABHS increased clearance and reduced peak concentration of simvastatin by 44.6% and 18.0%, respectively (P < .05). The geometric mean ratio of simvastatin AUC0-∞ with or without ABHS was 0.646 with the 90% confidence interval (0.564, 0.758) falling outside the bioequivalent range. WHAT IS NEW AND CONCLUSION: Aqueous extract of Hibiscus sabdariffa lowered Tc better than simvastatin and enhanced the antihyperlipidaemic activity of the drug when co-administered at low doses in an animal model. However, aqueous beverage of Hibiscus sabdariffa caused a significant herb-drug interaction resulting in overall reduction in exposure to simvastatin in humans. Caution should thus be placed on clinical judgement or recommendations based on the animal results. Nevertheless, co-administration of the beverage with simvastatin should be discouraged until more clinical data are available.

Knowledge, Perception and Practice of Medication Use Review among Community Pharmacists in Southwestern Nigeria

Background: Medication use review (MUR) is an emerging concept in medicine management that has recorded success in many developed countries.Purpose: To evaluate knowledge, perception and practice of MUR among community pharmacists (CP) in southwestern Nigeria.Method: A cross-sectional study was carried out among 100 CP recruited from Oyo and Osun states between January and March, 2015, using a pre-tested questionnaire. Demographic information and CP's knowledge, perception and current practice of MUR were evaluated using open-ended, closed-ended and Likert-scale questions. Respondents' scores for 6-item knowledge test questions and description of specific component of MUR services were categorised as score>3 (good knowledge) and score≤3 (poor knowledge). Descriptive statistics were used to summarize data. Ranked variables were evaluated using Kruskal-Wallis test at p<0.05.Results: Fifty-nine (59.0%) CP from Oyo and 41(41.0%) from Osun state participated. Sixty-five (70.7%) had score>3 indicating "good" knowledge of MUR, while 27 (29.3%) had score≤3 suggesting "poor" knowledge. Forty-two (42.0%) claimed to provide MUR service; of this, 14 (33.3%) had scores>3 indicating those who gave correct description of specific component of MUR. Lack of adequate time for counselling (49; 49.5%) and lack of specialized training for pharmacists (45;45.5%) were cited as barriers to MUR practice. Majority (51; 51.5%) agreed that MUR service should be incorporated into community pharmacy practice.Conclusion: Knowledge of MUR concept among community pharmacists in Oyo and Osun states is considerable, but description of specific component of MUR services by respondents was poor. There is therefore a need for continuous training on emerging concepts among pharmacists, so as to stimulate interest in patient-oriented service

Factors contributing to non adherence to oral hypoglycemic medications among ambulatory type 2 diabetes patients in Southwestern Nigeria / Factores que contribuyen al incumplimiento de hipoglucemiantes orales entre los pacientes ambulatoriales diabéticos tipo 2 en el suroeste de Nigeria

Objective: The overall goal of the study was to evaluate the probable reasons for patients’n on adherence to prescribed oral hypoglycemic medications in an ambulatory care setting in Nigeria with a view to identifying points for necessary intervention to improve adherence and treatment outcomes. Also, the recommended non-drug management options for diabetes patients with emphasis on self-monitoring of blood glucose were assessed. Methods: A cross-sectional study was conducted at a 200-bed secondary health care facility in Southwestern Nigeria between 2nd April and 31stMay 2008. Copies of pre-tested questionnaire were administered directly to 121 ambulatory patients with type 2 diabetes at the study site. Information on socio-demographic characteristic, probable barriers that affect adherence to prescribed oral hypoglycemic medications, non-drug treatment options for diabetes, and patients' self management efforts were obtained. Descriptive and chi-square statistics were used to evaluate the distribution of respondents' opinion. Results: The response rate was almost 100%. The commonly cited intentional non adherence practice included dose omission (70.2%). Almost 50%respondents were fed up with daily ingestion of drugs and 19.8% were inconvenienced with taking medications outside home and gave these as reasons for the dose omission. Forgetfulness(49.6%) and high cost of medication (35.5%) were mentioned as major non-intentional reasons for non-adherence. Aside oral medications, 82.6% and 95.0% of respondents respectively, reported moderate exercise and dietary restrictions as part of the prescribed treatment modalities. More than two third of respondents (81.8%) had never monitored blood glucose by themselves. Significant association exist between sex, occupation and patients' tendencies to forget doses of prescribed oral medications (p<0.05) (AU)

Objetivo: El objetivo general de este estudio fue evaluar las razones probables del incumplimiento de los pacientes con los medicamentos hipoglucemiantes orales en régimen ambulatorio de Nigeria, con la intención de identificar elementos para la intervención necesaria que mejore el cumplimiento y los resultados del tratamiento. También se evaluaron las opciones recomendadas de manejo de la diabetes no medicamentosas con especial énfasis en la auto-medición de la glucosa. Métodos: Se realizó un estudio transversal en una clínica de 200 camas del Sur Oeste de Nigeria entre el 2 de abril y el 31 de mayo de 2008. Se administraron directamente copias de un cuestionario pre-validado a 121 pacientes ambulatoriales con diabetes tipo 2. Se obtuvo la información de las características sociodemográficas, barreras probables que afectan el cumplimiento del hipoglucemiante prescrito, tratamiento no medicamentoso para la diabetes, y esfuerzos de auto-cuidado del paciente. Se utilizó estadística descriptiva y pruebas chi-cuadrado para evaluar la distribución de la opinión de los respondientes. Resultados: La tasa de respuesta fue de casi el100%. Las prácticas más frecuentemente citadas de incumplimiento voluntario incluían la omisión de una dosis (70,2%). Casi el 50% de los respondentes estaba harto de tomar diariamente medicamentos y el 19,8% estaba disgustado con tomar medicamentos fuera de casa y dieron estas razones como motivo de la omisión de dosis. El olvido(49,6%) y el alto coste de los medicamentos(35,5%) fueron mencionados como causas principales del incumplimiento no voluntario. Además de la medicación oral, el 82,6% y el 95,0%de los respondentes comunicaron ejercicio moderado y restricciones dietéticas como parte delos tratamientos. Más de dos tercios de los respondentes (81,8%) nunca se habían medico la glucosa solos (AU)

Anxiolytic and sedative effects of extracts of Hibiscus sabdariffa Linn (family Malvaceae).

Aqueous (A), hydroalcoholic (AE) and ethanolic (E) extracts and fractions of dried calyxes of Hibiscus sabdariffa were evaluated for anxiolytic property using elevated-plus maze (EPM), and sedative properties using ketamine-induced sleep in animal models. The extracts exhibited a dose-dependent increase in the time spent in the open arm with ethanol extracts having the best anxiolytic activity. The extracts at A 5 mg/kg, AE 5 mg/kg and A 50 mg/kg did not cause an increase in time spent in the open arms (p < 0.05) but other doses significantly did when compared with the vehicle control. The fractions of the hydroalcoholic extracts showed no significant anxiolytic activity. Neither the extracts nor the fractions significantly reduced or increased latency to sleep after a single dose except AE 300 (p < 0.01). There was significant reduction in onset of sleep, and increase in sleeping time with A and AE extracts with multiple doses at A 300, AE 50 and AE 300 mg/kg dose groups (p < 0.001, p < 0.01 and p < 0.05 respectively). A reduction in sleeping time after several daily doses of ethanol extracts doses was observed. A single dose of one of the fractions (EAC at 50 mg/kg) caused a significant reduction (p < 0.05) in sleep duration. The study showed that extracts of Hibiscus sabdariffa possess anxiolytic and sedative effects which become more pronounced with administration of repeated doses of the extracts.

Evaluation of adverse drug reactions to artemisinin-based combination therapy in a Nigeria University Community

Purpose : The study was carried out to evaluate the incidence of adverse reactions to antimalarial drugs among residents of a Nigeria university community with a focus on arte- misinin-based combination therapy (ACT). Specifically; the profile of use; and the reporting culture of people with respect to experienced reactions were noted. Method : Ques- tionnaires were administered to respondents at the university health centre between November 2006 and January 2007. Information on demographic characteristics; nature of experienced adverse reactions and the most frequently used ACT; among other questions; were collected. Descriptive statistics and Fisher's Exact test were used to evaluate the distribution of respondent's opinion. Result: The study achieved a response rate of 86. The results revealed that 210 (70.0) of respondents said they had used artemisinin-based combination drugs while 134 (44.7) said they used artemisinin derivatives alone as monotherapy for malaria treatment. Artesunate plus amodiaquine 94 (31.3) as a co-packaged product was the most commonly used ACT. Incidence of the experienced adverse reactions to ACT was reported to be generally mild and well tolerated. Conclusion : Efforts to improve the use of ACT in the management of acute uncomplicated P. falciparum malaria is recommended. Furthermore; an effective mechanism to improve reporting of adverse effects of ACT is also recommended

Effects of water extract of Hibiscus sabdariffa, Linn (Malvaceae) 'Roselle' on excretion of a diclofenac formulation.

The effect of beverages prepared from the dried calyx of the flowers of Hibiscus sabdariffa on the excretion of diclofenac was investigated using a controlled study in healthy human volunteers. A high pressure liquid chromatographic method was used to analyse the 8 h urine samples collected after the administration of diclofenac with 300 mL (equivalent to 8.18 mg anthocyanins) of the beverage administered daily for 3 days. An unpaired two-tailed t-test was used to analyse for significant difference observed in the amount of diclofenac excreted before and after administration of the beverage. There was a reduction in the amount of diclofenac excreted and the wide variability observed in the control with the water beverage of Hibiscus sabdariffa (p < 0.05). There is an increasing need to counsel patients against the use of plant beverages with drugs.

Hypoglycemic effect of Treculia africana Decne root bark in normal and alloxan-induced diabetic rats.

The solvent partitioned purified fractions of the hydro-acetone root bark extract of the African breadfruit (Treculia africana Decne) were evaluated for hypoglycemic activities in normal and diabetic albino rats. Fasting blood glucose levels were estimated by the use of a glucometer at pre-determined intervals after oral administration of the test extracts/fractions. Results revealed that the test fractions have only a slight effect on blood sugar level of normal rats. On short term and chronic administration in diabetic rats however, diethyl ether-soluble (DEF) and the water-soluble (WSF) fractions significantly reduced the fasting blood sugar levels (p<0.05) at differing rates when compared with the control group of animals. The diethyl ether soluble fraction (10 mg kg(-1) dose level) was found to exhibit the highest activity giving 69.4% reduction in blood sugar level (at 240 hours) which was in comparable range with the reference standard glibenclamide (0.5 mg kg(-1)) which reduced blood sugar levels by 65.8% below the initial baseline values.

Evaluation of valuation of toxicity profile of an alkaloidal fraction of the stem bark of Picralima nitida (fam. Apocynacaes).

Dermal and acute toxicity evaluation of the basic alkaloidal fraction of the stem bark of Picralima nitida, which has been shown to have pronounced activity against causative organisms of dermatomycosis in man, was carried out in animals. Acute intraperitoneal toxicity tests showed a dose-dependent toxicity. There was inflammation and necrosis of liver hepatocytes accompanied by reduction in neutrophilic count and a corresponding increase in lymphocytic count. There was no sign of reddening or irritation when applied into the eye conjunctiva. Dermal tests also showed that the fraction caused no sensitization, inflammation or death in the animal models used.

Therapeutic monitoring of chloroquine in pregnant women with malaria.

Therapeutic monitoring of chloroquine was carried out in pregnant women with confirmed laboratory and clinical malaria after administration of 10 mg/kg body weight of the drug at 0 and 24th hour and 5 mg/kg body weight at the 48th hour. Venous blood was withdrawn at scheduled intervals. Plasma chloroquine level was determined using a highly sensitive and specific liquid chromatographic method. The time of peak plasma concentration, (t(max)) after the first dose was found to be 3.5 hours while peak plasma concentrations, (Cp(max)) were obtained at 2, 28, and 52 hours with values of 204. 36, 343.51 and 257.04 ng/ml respectively. There was total parasitaemia clearance before the end of 96 hours in all the subjects.

Evaluation of the antimicrobial property of the stem bark of Picralima nitida (Apocynaceae).

The basic fraction (BF) of the methanol extract of the stem bark of Picralima nitida (family Apocynaceae) exhibited significant antimicrobial activity against a wide range of Gram-positive bacteria and fungi, but limited activity against Gram-negative bacteria. The BF had a similar minimum inhibitory concentration (MIC) for S. aureus to the control drug ampicillin, and lower MIC values against A. flavus and A. niger than those of tiaconazole. Values of the minimum bactericidal concentration (MBC) of the BF against microorganisms tested were generally much higher than those for the control drugs ampicillin and gentamicin. The results suggest that some constituents of the stem bark could be isolated and developed into effective antimicrobial agents.

Antimicrobial activity of Mallotus oppositifolium extractives.

A bioactivity monitored phytochemical examination of the morphological parts of Mallotus oppositifolium utilizing the hole-in-plate bioassay procedure against gram-positive, gram-negative bacteria and fungal isolates resulted in the location of significant antimicrobial activity in the acidic fraction (HAF) of the hexane extract of the powdered leaves. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values were 32.5 microg/ml and 65 microg/ml against Pseudomonas aeruginosa NCTC 6750 and 25 microg/ml and 50 microg/ml against Staphylococcus aureus NCTC 6571 respectively. These activities were found comparable with standard drugs.