Database of Receptors and Channels

The following two sites give updated and detailed description of all known Receptors and ion Channels.:
1) IUPHAR Database of G Protein-Coupled Receptors and the IUPHAR Database of Voltage-Gated and Ligand-Gated Ion Channels.
2) Guide to Receptors and Channels (GRAC), 3rd edition published by British Pharmacological society.

A Study of Nigella sativa Linn. seeds for antimicrobial activity against multidrug resistant clinical strains of Pseudomonas aeruginosa.

A Study of Nigella sativa Linn. seeds for antimicrobial activity against multidrug resistant clinical strains of Pseudomonas aeruginosa. Hippocratic Journal of Unani Medicine. 4(4). 2009. 95-104.
Authors: Mohd T Salman(1),*, Rahat A Khan(1), Indu Shukla(2)
Address: (1)Department of Pharmacology, (2)Department of Microbiology, Jawaharlal Nehru Medical College, Aligarh Muslim University, Aligarh, India. 202002.
*Corresponding Author: Present address- Department of Pharmacology, Era’s Lucknow Medical College, Sarfarazganj, Hardoi Road, Lucknow. India. 202003.
Abstract
Nigella sativa (black cumin) seed oil and extracts were tested in varying dilutions against strains of Pseudomonas aeruginosa resistant to a number of clinically used antibiotics isolated from patients attending JN Medical College Hospital, Aligarh, using disc agar diffusion technique on inoculated Muellar Hinton agar plates under standard laboratory conditions. Both the oil and Methanolic extract showed remarkable dose dependant antibacterial activity against the tested strains upto a dilution of 1:50 as evident from the zones of inhibition. No cross resistance was noticed with any of the tested antibiotics.

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Circumcision

Published Online First: 15 December 2008. doi:10.1136/sti.2008.032334
Sexually Transmitted Infections 2009;85:116-120

Copyright © 2009 by the BMJ Publishing Group Ltd.

EPIDEMIOLOGY

Male circumcision and Neisseria gonorrhoeae, Chlamydia trachomatis and Trichomonas vaginalis: observations after a randomised controlled trial for HIV prevention

J Sobngwi–Tambekou¹, D Taljaard², M Nieuwoudt³, P Lissouba¹, A Puren³ and B Auvert⁴

¹ INSERM U687, Hôpital Paul Brousse, Villejuif, France
² Progressus, Johannesburg, South Africa
³ National Institute for Communicable Diseases, Johannesburg, South Africa
⁴ INSERM U687, Assistance Publique-Hôpitaux de Paris, University of Versailles, France

Correspondence to:
Dr Bertran Auvert, INSERM U687, 12 avenue Paul Vaillant-Couturier, 94804 Villejuif Cedex, France; bertran.auvert@uvsq.fr

Objective: To assess the association between male circumcision and Neisseria gonorrhoeae, Chlamydia trachomatis and Trichomonas vaginalis using data from a male circumcision randomised controlled trial.

Methods: We used data collected during the male circumcision trial conducted in Orange Farm (South Africa) among men aged 18–24 years. Altogether, 1767 urine samples collected during the final follow-up visit were analysed using PCR. Prevalence of N gonorrhoeae, C trachomatis and T vaginalis was assessed as a function of male circumcision using odds ratios (OR) given by univariate and multivariate logistic regression.

Results: In an intention-to-treat analysis, prevalence of N gonorrhoeae, C trachomatis and T vaginalis among intervention and control groups were 10.0% versus 10.3% (OR 0.97; p = 0.84), 2.1% versus 3.6% (OR 0.58; p = 0.065) and 1.7% versus 3.1% (OR 0.54; p = 0.062), respectively. The association between T vaginalis and male circumcision remained borderline when controlling for age, ethnic group, number of lifetime partners, marital status, condom use and HIV status (AOR 0.48; p = 0.069). In the as-treated analysis, this association became significant (OR 0.49, p = 0.030; AOR 0.41, p = 0.030).

Conclusions: This study demonstrates for the first time that male circumcision reduces T vaginalis infection among men. This finding explains why women with circumcised partners are less at risk for T vaginalis infection than other women. The protective effect on T vaginalis is an additional argument to recommend male circumcision in Africa where it is acceptable.

Trial registration number: NCT00122525.

Some new drug approvals in June 2009

Simponi
Pharmacological class: TNF blocker.
Active Ingredient: Golimumab 50mg/0.5mL; soln for SC inj; preservative-free.
Indication: Moderately to severely active rheumatoid arthritis (RA), in combination with methotrexate (MTX). Active psoriatic arthritis (PsA), alone or with MTX. Active ankylosing spondylitis (AS).
Company: Centocor Ortho Biotech, Inc.

Axert approved for migraine treatment in adolescents

The FDA has approved Axert (almotriptan malate tablets, from Ortho-McNeil Janssen), a selective 5-HT1B/1D receptor agonist, for the acute treatment of migraine headache in adolescents 12-17 years of age with a history of migraine attacks lasting ≥4 hours.

Reclast approved for biennial dosing regimen to prevent female osteoporosis

The FDA has approved Reclast (zoledronic acid, from Novartis) injection for the prevention of osteoporosis in women for two years with a single dose.

Lamictal XR approved for treatment of epilepsy

GlaxoSmithKline announced that the FDA has approved Lamictal XR (lamotrigine extended-release tablets) as a once-a-day add-on therapy for epilepsy patients ≥13 years of age with partial onset seizures.

Nuvigil launched for excessive sleepiness

Nuvigil (armodafinil tablets) is now available from Cephalon in 50mg, 150mg, and 250mg dosage strengths.

Vyvanse approved for pediatric ADHD control 13 hours post-dose

Shire Pharmaceuticals has received FDA approval for a labeling change for its once-daily Attention Deficit Hyperactivity Disorder (ADHD) treatment Vyvanse (lisdexamfetamine dimesylate capsules).

Cycloset -a new antidiabetic

The U.S. FDA approved Cycloset, a new quick-release oral formulation of bromocriptine mesylateis, which is the first therapy directly targeting the body’s dopamine activity to improve glycemic control. It is also the only drug to be approved subsequent to the FDA's guidelines that require studies demonstrating that diabetes drugs do not increase cardiovascular risk.

Preclinical studies indicate that while an increase in dopamine activity leads to improvements in diabetes, the time of day of the increased dopamine activity is also important. Studies in diabetic animals have shown that increased dopaminergic activity at a particular time of day is most effective in “resetting” the biological clock neurochemistry to a physiology that improves diabetic dysmetabolism. Taken orally, once-a-day, in the morning, Cycloset provides a single brief pulse of dopamine agonist activity shortly after its administration. Morning Cycloset improves post-prandial (after-meal) glucose without increasing plasma insulin concentrations, and the beneficial effects of Cycloset on post-meal glycemic control in patients with Type 2 diabetes are demonstrable many hours after the drug has been substantially cleared from the circulation, for example at lunch and dinner.

Mechanism: Bromocriptine mesylate, an ergot derivative, is a sympatholytic dopamine D2 agonist that exerts inhibitory effects on serotonin turnover in the central nervous system. It has been proposed that bromocriptine can reverse many of the metabolic alterations associated with obesity by resetting central (hypothalamic) circadian organization of monoamine neuronal activitties. Indeed, bromocriptine, if administered systemically or into the cerebral ventricle during the early hours of the light cycle, prevents or reverses seasonal fattening, insulin resistance, and decreased endogenous (hepatic) glucose production in mammals. Moreover, timed bromocriptine treatment decreased body weight and improved glucose tolerance in obese individuals who were instructed to follow a hypocaloric diet . Bromocriptine has also been shown to reduce mean daylong plasma glucose, triglyceride, and free fatty acid (FFA) levels in the absence of a change in body weight in obese nondiabetic women.

Drugs Modifying The Epigenetic Status

Several chemical entities that affect the DNA methylation landscape of the genome are now being used.

• The earliest of these, 5-azacytidine and azacytidine, are chemical analogs of the nucleoside cytidine and its deoxy derivative, decitabine. Through incorporation into DNA (during replication) and RNA (during transcription), they inhibit methyltransferases and thereby cause demethylation of the sequence. Their lack of specificity, has also been deemed to potentiate the carcinogenic process, given the impending effect on genomic stability.
• Zebularine is a cytidine analog that inhibits DNA methylation;
• MG98, an antisense oligonucleotide targets the 3′-untranslated region of the maintenance methyltransferase DNMT1, thereby inhibiting it.
• RG108 effectively blocks DNMTs, particularly DNMT1, and inhibits their activity.
• Psammaplins, a natural product derived from the sea sponge Pseudoceratina purpurea inhibits DNMTs as well as histone deacetylases.

Increasing work is being carried out in developing drugs that affect histone modifications.

• Histone deacetylase inhibitors have been objects of attention in anticancer drug development as they are seen as presenting a potential strategy to reverse aberrant epigenetic changes associated with cancer