Displaying publications 1 - 20 of 31 in total

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  1. Lim TH, Yap E, Norhatizah BS
    Med J Malaysia, 2019 Oct;74(5):447-449.
    PMID: 31649228
    PHACE syndrome describes the association of large segmental haemangioma with extracutaneous features (posterior fossa anomalies, arterial, cardiac, eye and endocrine anomalies). We report a case of segmental facial infantile haemangioma with PHACE syndrome treated successfully with oral propranolol without neurological sequelae.
    Matched MeSH terms: Propranolol
  2. Meka VS, Songa AS, Nali SR, Battu JR, Kukati L, Kolapalli VR
    Invest Clin, 2012 Sep;53(3):223-36.
    PMID: 23248967
    The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.
    Matched MeSH terms: Propranolol*
  3. Salman SA, Sulaiman SA, Ismail Z, Gan SH
    Toxicol. Mech. Methods, 2010 Mar;20(3):137-42.
    PMID: 20128736 DOI: 10.3109/15376511003602112
    Many previous published methods for the quantitative determination of propranolol (PRN) in human plasma have poor recoveries and were not validated according to the FDA guideline. The aim of this study is to develop a simple HPLC method for detecting PRN in human plasma and to validate it so that it can be applied to a clinical study. Chromatographic separation was achieved using a mixture of a mobile phase consisting of 160 ml water, 180 ml methanol, 70 ml acetonitrile, 2.5 ml acetic acid, and 125 microl triethylamine (v/v). The pH of the whole mixture was adjusted to 3.4. A flow rate of 0.5 ml/min was employed throughout with a 15 microl injection volume. Detection was done using a UV detector at 291 nm. The validated method was linear for concentrations ranging from 15-180 ng/ ml with a good separation and specificity for both PRN and its internal standard, oxprenolol (OXP), with excellent recoveries, precision, and accuracies. The limit of detection (LOD) and limit of quantification (LOQ) were 1 and 10 ng/ml, respectively. The stability studies demonstrated that PRN is stable in the autosampler vials and also up to 3.5 months. To the authors' knowledge, the recovery, that ranged between 97.9-102.7%, is the highest among all previously reported methods that used HPLC with UV detection. The developed and validated method for PRN analysis is excellent and applicable to a clinical study.
    Matched MeSH terms: Propranolol/blood*; Propranolol/chemistry
  4. Zaharuddin ND, Noordin MI, Kadivar A
    Biomed Res Int, 2014;2014:735891.
    PMID: 24678512 DOI: 10.1155/2014/735891
    The effectiveness of Okra gum in sustaining the release of propranolol hydrochloride in a tablet was studied. Okra gum was extracted from the pods of Hibiscus esculentus using acetone as a drying agent. Dried Okra gum was made into powder form and its physical and chemical characteristics such as solubility, pH, moisture content, viscosity, morphology study using SEM, infrared study using FTIR, crystallinity study using XRD, and thermal study using DSC and TGA were carried out. The powder was used in the preparation of tablet using granulation and compression methods. Propranolol hydrochloride was used as a model drug and the activity of Okra gum as a binder was compared by preparing tablets using a synthetic and a semisynthetic binder which are hydroxylmethylpropyl cellulose (HPMC) and sodium alginate, respectively. Evaluation of drug release kinetics that was attained from dissolution studies showed that Okra gum retarded the release up to 24 hours and exhibited the longest release as compared to HPMC and sodium alginate. The tensile and crushing strength of tablets was also evaluated by conducting hardness and friability tests. Okra gum was observed to produce tablets with the highest hardness value and lowest friability. Hence, Okra gum was testified as an effective adjuvant to produce favourable sustained release tablets with strong tensile and crushing strength.
    Matched MeSH terms: Propranolol/administration & dosage*; Propranolol/pharmacology*
  5. Meka VS, Murthy Kolapalli VR
    Curr Drug Deliv, 2016;13(6):971-81.
    PMID: 26452534
    A central composite design was applied to design a novel gastric floating drug delivery system comprising propranolol HCl in Terminalia catappa gum and to evaluate the buoyancy, in vitro drug release behavior, and pharmacokinetic parameters. All formulations exhibited good buoyancy properties in vitro reflected by floating lag time of 1-110 sec, total floating time of 9-16 h and prolonged release behaviour (upto 12 h). Statistically optimised formulation (PBGRso) was orally administered to human volunteers under both fasted and fed conditions to evaluate gastric floating behavior under different food conditions by X-ray evaluation. In vivo studies of optimised formulations revealed that the gastric residence time of floating tablets was enhanced in the fed but not in the fasted state. Pharmacokinetic studies of the optimised Terminalia catappa formulation and a commercial product (Ciplar LA 80) carried out on healthy human volunteers showed a significant improvement in the bioavailability (132%) of propranolol HCl released from from the experimental Terminalia catappa formulations compared with Ciplar LA 80.
    Matched MeSH terms: Propranolol/administration & dosage*; Propranolol/pharmacokinetics*
  6. Rasool AH, Rahman AR, Ismail R, Hatim S, Abdullah AR, Singh R, et al.
    Int J Clin Pharmacol Ther, 2000 May;38(5):260-9.
    PMID: 10839470
    OBJECTIVE: To determine whether racial differences in response to blockade of beta receptors occur among racial groups in Malaysia that are the Malays, Indians and Chinese. SUBJECTS, MATERIALS AND METHOD: 35 healthy male volunteers representing the 3 main racial groups in Malaysia (12 Malays, 12 Chinese and 11 Indians) were studied in a randomized, placebo-controlled, crossover and single-blind design. Propranolol 80 mg 12-hourly was given orally for 48 hours. Six hours after the last dose subjects attended an exercise session where resting and exercise heart rate, blood pressure, plasma potassium and glucose levels, resting FEV1 and plasma propranolol concentrations were recorded.

    RESULTS: No significant difference in plasma propranolol (mean +/- SEM) levels was seen between races six hours after the last dose (Malays, 59.7 +/- 8.8 ng/ml, Indians, 67.6 +/- 19.3 ng/ml, Chinese, 58.4 +/- 7.9 ng/ml). Chinese were least sensitive to the bradycardic and hypotensive effects of propranolol at rest and exercise. Indians and Malays had significant reduction of supine systolic blood pressure with propranolol but not Chinese. Comparison of percentage reductions of systolic blood pressure at supine, sitting and exercise by repeated measure analysis showed the Malays to have significantly higher change compared to the Chinese (p = 0.022). Similarly, comparison of percentage reductions of heart rate at supine, sitting and exercise by repeated measure analysis showed the Malays to have significantly higher change compared to the Chinese (p = 0.040). Average change in potassium concentrations at peak exercise and recovery showed the Indians to have significantly higher increase in potassium levels with propranolol compared to the Malays (p = 0.038). However, no significant interethnic difference was seen in the reduction of glucose levels at rest, peak exercise or recovery. Also, no significant interethnic difference was seen in reduction of FEV1 values.

    CONCLUSION: We, therefore, conclude that ethnic differences in response to blockade of beta-receptors exist among racial groups in Malaysia. These differences were seen at similar plasma drug levels between races suggesting ethnic differences in drug sensitivity, rather than differences in drug disposition.

    Matched MeSH terms: Propranolol/pharmacokinetics; Propranolol/pharmacology*
  7. Salman SA, Amrah S, Wahab MS, Ismail Z, Ismail R, Yuen KH, et al.
    J Clin Pharm Ther, 2010 Dec;35(6):691-6.
    PMID: 21054461 DOI: 10.1111/j.1365-2710.2009.01147.x
    Eurycoma longifolia (E. longifolia), a herb commonly consumed for its aphrodisiac properties, is widely used by Asian males. This may include hypertensive patients receiving propranolol which may cause sexual dysfunction as one of its side-effects. There is no published study of the potential pharmacokinetic interaction between propranolol and the herb.
    Matched MeSH terms: Propranolol/blood; Propranolol/pharmacokinetics*; Propranolol/pharmacology
  8. Venkata Srikanth M, Songa AS, Nali SR, Battu JR, Kolapalli VR
    Drug Dev Ind Pharm, 2014 Jan;40(1):33-45.
    PMID: 23317339 DOI: 10.3109/03639045.2012.744416
    The objective of the present investigation was to study the applicability of thermal sintering technique for the development of gastric floating tablets of propranolol HCl. Formulations were prepared using four independent variables, namely (i) polymer quantity, (ii) sodium bicarbonate concentration, (iii) sintering temperature and (iv) sintering time. Floating lag time and t95 were taken as dependent variables. Tablets were prepared by the direct compression method and were evaluated for physicochemical properties, in vitro buoyancy and dissolution studies. From the drug release studies, it was observed that drug retarding property mainly depends upon the sintering temperature and time of exposure. The statistically optimized formulation (PTSso) was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry studies, and no significant chemical interaction between drug and polymer was observed. Optimized formulation was stable at accelerated conditions for a period of six months. PTSso was evaluated for in vivo buoyancy studies in humans for both fed and fasted states and found that gastric residence time of the floating tablets were enhanced by fed stage but not in fasted state. Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT). There was a significant increase in the bioavailability of the propranolol HCl from PTSso formulation, which was evident from increased AUC levels and larger MRT values than Ciplar LA 80.
    Matched MeSH terms: Propranolol/administration & dosage*; Propranolol/pharmacokinetics; Propranolol/chemistry
  9. Leung AKC, Leong KF, Lam JM
    Paediatr Child Health, 2020 04 24;26(2):e70-e72.
    PMID: 33747313 DOI: 10.1093/pch/pxaa050
    The majority of infantile hemangiomas are benign and will resolve on their own. We report a 4-month-old infant with an ulcerated giant segmental infantile hemangioma involving the left upper limb who developed a contracture of the left elbow despite treatment with oral propranolol, proper wound care, and regular intense physiotherapy. To our knowledge, contracture resulting from an infantile hemangioma has not been reported previously.
    Matched MeSH terms: Propranolol
  10. Raju SS, Gopalakrishna HN, Venkatadri N
    Pharmacol Res, 1998 Dec;38(6):449-52.
    PMID: 9990653
    A comparative effect of propranolol and nifedipine administered individually and in combination at graded dose levels; and that of phenytoin at 30 mg kg-1 on maximal electroshock (MES)-induced seizure in mice was investigated. Propranolol in doses of 10 mg kg-1 and 20 mg kg-1, and nifedipine in doses of 8 mg kg-1 and 16 mg kg-1 significantly modified MES activity. Propranolol (40 mg kg-1), and a combination of propranolol (20 mg kg-1) and nifedipine (8 mg kg-1), produced antiMES activity, which was comparable to that of phenytoin (30 mg kg-1). In mice treated with propranolol and nifedipine combination, the tonic flexor and tonic extensor phase ratios (F/E ratio) were significantly higher than individual drug responses. Our findings suggest that a combination of propranolol and nifedipine has either synergistic or an additive effect in controlling MES-induced seizures in mice.
    Matched MeSH terms: Propranolol/pharmacology*
  11. Seng LK, Mahadaven M, Musa A
    Br J Surg, 1993 Sep;80(9):1149.
    PMID: 8402117
    Matched MeSH terms: Propranolol/adverse effects
  12. Koay AC, Choo MM, Nathan AM, Omar A, Lim CT
    J Ocul Pharmacol Ther, 2011 Jun;27(3):309-11.
    PMID: 21542771 DOI: 10.1089/jop.2011.0013
    The purpose of this report was to describe 2 cases of periocular infantile hemangiomas (IHs) that were successfully treated with low-dose oral propranolol alone and in combination with oral prednisolone.
    Matched MeSH terms: Propranolol/administration & dosage; Propranolol/therapeutic use*
  13. Venkatesh G, Ramanathan S, Mansor SM, Nair NK, Sattar MA, Croft SL, et al.
    J Pharm Biomed Anal, 2007 Mar 12;43(4):1546-51.
    PMID: 17157469
    A simple, sensitive and specific reversed phase high performance liquid chromatographic (RP-HPLC) method with UV detection at 251 nm was developed for simultaneous quantitation of buparvaquone (BPQ), atenolol, propranolol, quinidine and verapamil. The method was applicable in rat in situ intestinal permeability study to assess intestinal permeability of BPQ, a promising lead compound for Leishmania donovani infections. The method was validated on a C-4 column with mobile phase comprising ammonium acetate buffer (0.02 M, pH 3.5) and acetonitrile in the ratio of 30:70 (v/v) at a flow rate of 1.0 ml/min. The retention times for atenolol, quinidine, propranolol, verapamil and BPQ were 4.30, 5.96, 6.55, 7.98 and 8.54 min, respectively. The calibration curves were linear (correlation coefficient > or =0.996) in the selected range of each analyte. The method is specific and sensitive with limit of quantitation of 15 microg/ml for atenolol, 0.8 microg/ml for quinidine, 5 microg/ml for propranolol, 10 microg/ml for verapamil and 200 ng/ml for BPQ. The validated method was found to be accurate and precise in the working calibration range. Stability studies were carried out at different storage conditions and all the analytes were found to be stable. This method is simple, reliable and can be routinely used for accurate permeability characterization.
    Matched MeSH terms: Propranolol/analysis*; Propranolol/pharmacokinetics; Propranolol/chemistry
  14. Al-Akwaa AA, Asmawi MZ, Dewa A, Mahmud R
    Heliyon, 2020 Jul;6(7):e04588.
    PMID: 32775735 DOI: 10.1016/j.heliyon.2020.e04588
    Background: Vitex pubescens has been used traditionally in hypertension treatment but not yet scientifically assessed. The objective of the study is to investigate the antihypertensive and vasorelaxant activities of V. pubescens, study its underlying pharmacological mechanisms, and identify the relevant vasoactive compounds.

    Methods: Successive extractions of V. pubescens leaf were carried out to produce petroleum ether (VPPE), chloroform (VPCE), methanol (VPME), and water (VPWE) extracts. Spontaneously hypertensive rats (SHRs) received a daily oral administration of the extracts (500 mg/kg/day; n = 6) or verapamil (15 mg/kg/day; n = 6) for 2 weeks, while the systolic and diastolic blood pressures were measured using non-invasive tail-cuff method. Vasorelaxation assays of the extracts were later conducted using phenylephrine (PE, 1 μM) pre-contracted aortic ring preparation. Mechanisms of vasorelaxation by the most potent fraction were studied using vasorelaxation assays with selected blockers/inhibitors. GC-MS was conducted to determine the active compounds.

    Results: VPPE elicited the most significant diminution in systolic and diastolic blood pressure of treated SHRs and produced the most significant vasorelaxation in the aortic rings. Vasorelaxant effects of F2-VPPE were significantly reduced in endothelium-denuded aortic rings by glibenclamide (1 μM), whereas calcium chloride and PE-induced contractions were significantly suppressed. Endothelium removal of the aortic rings or incubation with indomethacin (10 μM), atropine (1 μM), methylene blue (10 μM), propranolol (1μM) and L-NAME (10 μM) did not significantly alter F2-VPPE-induced vasorelaxation. Seven compounds were identified using GC-MS, including spathulenol.

    Conclusion: F2-VPPE exerted its endothelium-independent vasorelaxation by inhibition of vascular smooth muscle contraction induced by extracellular Ca+2 influx through trans-membrane Ca+2 channels and/or Ca+2 release from intracellular stores, and by activation of KATP channels. The vasorelaxation effects of V. pubescens could be mediated by the compound, spathulenol.

    Matched MeSH terms: Propranolol
  15. Huang YH, Lee MT, Hsueh HY, Knutson DE, Cook J, Mihovilovic MD, et al.
    Neurotherapeutics, 2023 Mar;20(2):399-418.
    PMID: 36696034 DOI: 10.1007/s13311-023-01342-y
    Ethanol has been shown to suppress essential tremor (ET) in patients at low-to-moderate doses, but its mechanism(s) of action remain unknown. One of the ET hypotheses attributes the ET tremorgenesis to the over-activated firing of inferior olivary neurons, causing synchronic rhythmic firings of cerebellar Purkinje cells. Purkinje cells, however, also receive excitatory inputs from granule cells where the α6 subunit-containing GABAA receptors (α6GABAARs) are abundantly expressed. Since ethanol is a positive allosteric modulator (PAM) of α6GABAARs, such action may mediate its anti-tremor effect. Employing the harmaline-induced ET model in male ICR mice, we evaluated the possible anti-tremor effects of ethanol and α6GABAAR-selective pyrazoloquinolinone PAMs. The burrowing activity, an indicator of well-being in rodents, was measured concurrently. Ethanol significantly and dose-dependently attenuated action tremor at non-sedative doses (0.4-2.4 g/kg, i.p.). Propranolol and α6GABAAR-selective pyrazoloquinolinones also significantly suppressed tremor activity. Neither ethanol nor propranolol, but only pyrazoloquinolinones, restored burrowing activity in harmaline-treated mice. Importantly, intra-cerebellar micro-injection of furosemide (an α6GABAAR antagonist) had a trend of blocking the effect of pyrazoloquinolinone Compound 6 or ethanol on harmaline-induced tremor. In addition, the anti-tremor effects of Compound 6 and ethanol were synergistic. These results suggest that low doses of ethanol and α6GABAAR-selective PAMs can attenuate action tremor, at least partially by modulating cerebellar α6GABAARs. Thus, α6GABAARs are potential therapeutic targets for ET, and α6GABAAR-selective PAMs may be a potential mono- or add-on therapy.
    Matched MeSH terms: Propranolol
  16. Cheah JM, Ng D, Low MY, Foo SH
    J ASEAN Fed Endocr Soc, 2019;34(2):206-209.
    PMID: 33442157 DOI: 10.15605/jafes.034.02.12
    Thyroid crisis is a life-threatening form of thyrotoxicosis characterized by multi-system dysfunction. Therapeutic plasma exchange has been reported to be effective in removing excessive circulating thyroid hormones. We present a 46-year-old female with recently diagnosed Graves' disease associated with thyrotoxic cardiomyopathy admitted for thyroid crisis complicated by propranolol-induced circulatory collapse, acute kidney injury and ischemic hepatitis. The tachyarrhythmia was refractory to conventional therapy. Initiation of TPE resulted in rapid clinical and biochemical stabilization.
    Matched MeSH terms: Propranolol
  17. Venkatesh G, Ramanathan S, Nair NK, Mansor SM, Sattar MA, Khan MA, et al.
    Biomed Chromatogr, 2007 May;21(5):484-90.
    PMID: 17294505
    A simple and sensitive RP-HPLC-UV method was developed and validated for simultaneous determination of atenolol and propranolol and subsequently applied to investigate the effect of dimethyl sulfoxide in rat in situ intestinal permeability studies. Atenolol (400 microm) and propranolol (100 microm) were perfused in the small intestine of anaesthetized (pentobarbitone sodium 60 mg/kg, i.p.) male Sprague-Dawley rats either in the presence (1, 3 and 5%) or in the absence of dimethyl sulfoxide. There was no significant alteration (p > 0.05) in the permeability of atenolol and propranolol, which indicated there was no effect of various concentrations of dimethyl sulfoxide (1-5%) on the membrane integrity of the rat intestinal tissues. The analytical method was validated on a C(4) column with a mobile phase comprising ammonium acetate buffer (pH 3.5, 0.02 m) and acetonitrile in the ratio of 30:70 (v/v) at a flow rate of 1.0 mL/min. The validated method was found to be accurate and precise and stability studies were carried out at different storage conditions and both analytes were found to be stable. These findings are applicable for determining the absorbability of water-insoluble drugs and new chemical entities for the purpose of classifying them in the biopharmaceutical classification system.
    Matched MeSH terms: Propranolol/pharmacokinetics*
  18. Al-Jubouri MA, Inkster GD, Nee PA, Andrews FJ
    Ann. Clin. Biochem., 2006 Jul;43(Pt 4):323-5.
    PMID: 16824287 DOI: 10.1258/000456306777695681
    A 35-year-old Malaysian man presented with rapid onset of flaccid quadriparesis associated with nausea and vomiting. General blood tests revealed severe hypokalaemia (serum potassium 1.5 mmol/L) and hypophosphataemia (serum phosphate 0.29 mmol/L) as a potential cause of the flaccid paralysis. Arterial blood gases showed mixed acid base disturbance of respiratory alkalosis and metabolic acidosis with hyperlactataemia. Thyrotoxic periodic paralysis (TPP) was suspected as the underlying cause of this presentation and thyroid function tests showed severe hyperthyroid results (free T4 > 77.2 pmol/L, free T3 19.3 pmol/L, thyroid-stimulating hormone [TSH] < 0.05 mIU/L). Treatment with intravenous potassium and phosphate infusion and oral propranolol resulted in rapid resolution of his symptoms. A discussion of the clinical and pathophysiological features and treatment of TPP (a very rare encounter in UK clinical practice) is presented, and to our knowledge associated hyperlactataemia has not been previously described.
    Matched MeSH terms: Propranolol/administration & dosage
  19. Zaiton Z, Merican Z, Khalid BA, Mohamed JB, Baharom S
    Gen. Pharmacol., 1993 Jan;24(1):195-9.
    PMID: 8482496
    1. The mean levels of lipid peroxidation products, namely conjugated diene and malonaldehyde, were increased in the soleus muscles of hyperthyroid cats, while the mean glutathione peroxidase activity was decreased. No corresponding similar changes were noted in the fast extensor digitorum longus muscles and serum. 2. Propranolol administration prevented the increase in conjugated diene level in the soleus muscles of hyperthyroid cat but not the malonaldehyde level. It also prevented the reduction in glutathione peroxidase activity in the slow oxidative soleus muscles of hyperthyroid cats. 3. Maximal twitch tension, subtetanic tension and maximum tetanic tension of soleus and EDL muscles were reduced in hyperthyroid cats. Propranolol administration for 5 weeks to hyperthyroid cats did not prevent the reduction in tension of contractions of these muscles. 4. It is suggested that lipid peroxidation might not be responsible for the myopathy in hyperthyroidism and propranolol administration does not improve skeletal muscle function in hyperthyroid animals.
    Matched MeSH terms: Propranolol/pharmacology*
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