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1.
Ceylon Med J ; 58(2): 82-3, 2013 Jun.
Article in English | MEDLINE | ID: mdl-23817940

ABSTRACT

The Department of Family Medicine, University of Kelaniya conducted a health camp in Puthukudiyiruppu in March 2011. Height and weight measurements were carried out and data of 303 participants were analysed. The rate of stunting among children below six years in this population was 62% compared to 19.3% nationally. Thirty four percent of children and adolescents (6-18yrs) were underweight and 21.4% of adults had a BMI less than 18.5kg/m2.


Subject(s)
Body Height , Growth Disorders , Humans , Thinness/epidemiology
2.
J Family Med Prim Care ; 1(1): 30-3, 2012 Jan.
Article in English | MEDLINE | ID: mdl-24478997

ABSTRACT

INTRODUCTION: Paracetamol is a widely used over the counter drug for pyrexia and mild to moderate pain in all age groups. OBJECTIVE: To assess the knowledge and practices of paracetamol administration among caregivers of the pediatric age group patients attending the university family practice. MATERIALS AND METHODS: A clinic-based descriptive cross-sectional survey was carried out among clients attending the family practice of the Faculty of Medicine, University of Kelaniya, Sri Lanka using pretested interviewer administrated questionnaire. RESULTS: Ninety eight caregivers Participated. Majority were females (97%) with a mean age of 32 years. Age of the patients ranged from 1 to 132 (mean: 48 months). The commonest indication for paracetamol was fever (98%) and in 99% of the patients, mother was the administrator. Forty three percent of the children received a supra-therapeutic dose (>15 mg/kg/dose). None exceeded 20 mg/kg/dose. 16% exceeded the recommended dosing frequency. Children above 3 years were at an increased risk of receiving incorrect paracetamol dose (χ(2) =19.55, df=1, P>0.001) A majority (75%) said they followed doctors' advice on paracetamol dose. There was no association between level of education of care giver, deciding dose as directed by doctor and product information leaflet and dosing accuracy. Only one caregiver was able to calculate the paracetamol dose according to weight. A majority (85%) knew about paracetamol poisoning but it was not associated with dosing accuracy. CONCLUSION AND RECOMMENDATIONS: Administration of supratheraputic doses of paracetamol is common and risk increased with child's age. Knowledge on calculating the weight appropriate paracetamol dose is poor. Physicians should educate care givers on judicious use of paracetamol.

3.
Bioorg Med Chem ; 5(7): 1257-65, 1997 Jul.
Article in English | MEDLINE | ID: mdl-9377085

ABSTRACT

A series of tetracyclic and tricyclic trioxane dimers has been prepared with ether and ester tethers of varying length and flexibility. Several of these trioxane dimers have been found to have potent and potentially therapeutically valuable antimalarial, antiproliferative, and antitumor activities in vitro.


Subject(s)
Antimalarials/chemical synthesis , Antimalarials/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Heterocyclic Compounds/chemical synthesis , Heterocyclic Compounds/pharmacology , Cell Division/drug effects , Dimerization , Drug Screening Assays, Antitumor , Humans , Tumor Cells, Cultured
4.
J Med Chem ; 40(2): 236-41, 1997 Jan 17.
Article in English | MEDLINE | ID: mdl-9003522

ABSTRACT

N-Acyl analogues 8, 9, and 12-26 of butitaxel (3) were prepared in one or two steps from amines 5 and 6 through Schotten-Baumann acylation. Seventeen novel analogues, consisting of aliphatic carbamates, alicyclic amides, and heteroaromatic amides, were synthesized. They were evaluated for their in vitro ability to stimulate the formation of microtubules, their cytotoxicity toward B16 melanoma cells, and their solubility in water. The most potent analogue found in this study was N-debenzoyl-N-(2-thenoyl)butitaxel (20), possessing ca. 2-fold better tubulin assembly properties and cytotoxic activity against B16 melanoma cells than paclitaxel. Compound 20 was ca. 25 times more water soluble than paclitaxel.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Paclitaxel/analogs & derivatives , Taxoids , Animals , Drug Screening Assays, Antitumor , Melanoma, Experimental/drug therapy , Mice , Microtubules/drug effects , Paclitaxel/chemical synthesis , Paclitaxel/chemistry , Paclitaxel/pharmacology , Solubility , Structure-Activity Relationship
5.
J Med Chem ; 38(19): 3821-8, 1995 Sep 15.
Article in English | MEDLINE | ID: mdl-7562913

ABSTRACT

3'-(tert-Butyl) 3'-dephenyl analogs of paclitaxel were synthesized from 10-deacetylbaccatin III and oxazolidinecarboxylic acid 7 followed by acylation of intermediate amines 10 and 11. Oxazolidinecarboxylic acid 7 was prepared in five steps and in good overall yield from L-tert-leucine. Twelve analogs were synthesized and evaluated for their in vitro ability to stimulate the formation of microtubules and for their cytotoxicity against B16 melanoma cells. Amide, carbamate, urea, and thiourea congeners were prepared. The most potent derivatives found in this study are the docetaxel analog 13, the N-[(tert-amyloxy)carbonyl] analog 17, and the 3'-phenylurea and 3'-tert-butylurea derivatives 20 and 23. Six of these analogs were shown to be ca. 90 times more soluble in water than paclitaxel and ca. 4-5 times more water-soluble than docetaxel.


Subject(s)
Antineoplastic Agents, Phytogenic/chemical synthesis , Antineoplastic Agents, Phytogenic/pharmacology , Paclitaxel/analogs & derivatives , Paclitaxel/pharmacology , Taxoids , Antineoplastic Agents, Phytogenic/chemistry , Docetaxel , Humans , Melanoma, Experimental/drug therapy , Microtubules/drug effects , Microtubules/metabolism , Molecular Structure , Paclitaxel/chemical synthesis , Paclitaxel/chemistry , Solubility , Tumor Cells, Cultured
6.
J Med Chem ; 37(24): 4258-60, 1994 Nov 25.
Article in English | MEDLINE | ID: mdl-7990125

ABSTRACT

4-Deacetyltaxol and 10-acetyl-4-deacetyltaxotere were synthesized for the first time from 7-(triethylsilyl)-4-deacetylbaccatin III. These analogs were found to be inactive in the microtubule assembly assay.


Subject(s)
Antineoplastic Agents, Phytogenic/chemical synthesis , Paclitaxel/analogs & derivatives , Taxoids , Antineoplastic Agents, Phytogenic/pharmacology , Docetaxel , Microtubules/drug effects , Molecular Conformation , Paclitaxel/chemical synthesis , Paclitaxel/pharmacology
7.
J Med Chem ; 37(18): 2981-4, 1994 Sep 02.
Article in English | MEDLINE | ID: mdl-7915328

ABSTRACT

Taxol and taxotere analogs with one carbon homologated side chains were synthesized from 10-deacetylbaccatin III and a key oxazolidineacetic acid intermediate, which was synthesized in four steps from (S)-(+)-2-phenylglycine. 10-Deacetyl-1a'-homotaxol and 1a'-homotaxotere were at least 27 times less active than taxol in the microtubule assembly assay. The inability of these homologs to induce microtubule formation may be due to unfavorable solution conformations, preventing productive interactions with the taxol binding site on microtubules.


Subject(s)
Paclitaxel/analogs & derivatives , Taxoids , Docetaxel , In Vitro Techniques , Molecular Conformation , Paclitaxel/chemical synthesis , Paclitaxel/pharmacology , Structure-Activity Relationship , Tubulin/drug effects , Tubulin/metabolism
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