S NO
|
BELSOMRA
|
|
1.
|
NAME
|
BELSOMRA
|
2.
|
CATEGORY
|
Medical Neurology
|
3.
|
COMPANY
|
Merck’s
|
4.
|
INDICATION DEVELOPED FOR
|
Insomnia
|
5.
|
MECHANISM OF ACTION
|
Orexin antagonist
|
6.
|
MORE DETAILED M.O.A
|
Induces sleep by blocking binding of two wakefulness
neuropeptide Orexin A and Orexin B to their receptor OX1R and OX2R
|
7.
|
NOVEL
|
yes/
|
8.
|
STAGE OF DEVELOPMENT
|
Phase 3 completed
and entering Phase 4
|
9.
|
US FDA APPROVAL
|
yes/
|
10.
|
DATE OF APPROVAL BY FDA
|
August 13 2014
|
11.
|
INDICATION APPROVED FOR BY FDA
|
-
|
12.
|
INDIAN SCIENARIO
|
-
|
13.
|
ANYTHING SPECIAL WITH THIS DRUG
|
Instead of traditional way of inducing sleepiness, it
fight against wakefulness
|
14.
|
BACKGROUND KNOWLEDGE REQUIRED
|
Orexin-A
and B are excitatory neuropeptide hormones
that promote wakefulness by sending inhibitory
signals to the ventrolateral preoptic nucleus, an
area of the hypothalamus with a high concentration
of GABA-producing neurons.
|
15.
|
ISSUES WITH THE DRUG
|
· To
be cautious on next day driving
· Sleep
pattern does not resemble to that of normal physiological sleep, it favours
REM sleep over NREM sleep
· People
who took this drug experienced somnolence
|
16.
|
this is about the point of view of me in relation to becoming doctor and my field of specialisation clinical pharmacologist..........
Sunday, September 13, 2015
BELSOMRA- a new drug for insomnia
Friday, September 4, 2015
YOU HAVE FOUND A NEW DRUG.HOW TO MOVE ABOUT NOW. DOSE AND DURATION OF TREATMENT FOR THE NEW DRUG.
FIRST SELECT THE BEST ANIMAL MODEL FOR THE DISEASE IN WHICH YOU HAVE DECIDED TO WORK.
YOU HAVE A NEW DRUG IN YOUR HAND AND IS CONFUSED WHAT IS THE DOSE IN WHICH THE DESIRED EFFECT WILL COME
Lowest dose which show maximum protection or effect is the rule
How to find the best
dose/standardization of doses for a new drug in an animal model??
You take multiple criteria
for evaluating the disease progress or severity and then administer the different probable doses among which you are
confused . Your aim is to find what will be your best suitable dose which will have a significant effect in decreasing the disease severity or produce maximum protection effect.
The thing to note is that you will have the data of effect of the different doses on the same parameter which you wish to check.
This dose
at which maximum benefit is seen is the best dose to give for the indication we
intend to give.
How to find the duration of the treatment for a new drug in an animal model???
In the dose selected above now your aim is to find the duration of the therapy.You give treatment and then analyze the model at different time interval to find the best time duration in which the drug maximum effect has been obtained. The thing to note is if you administer the drug more than this time ,some may argue that there will be no detrimental effect. Yes, of course but administering more than this time wont add to any beneficial effect too.
Thursday, September 3, 2015
DIFFERENCE BETWEEN PUBMED AND MEDLINE
As early as 1879, US National Library of Medicine started
maintaining a bibliography of all the articles in various journals, the name of
the compilation was Index
Medicus MEDLINE is the electronic
version of original raw data that is
Index Medicus with the US National Library of Medicine. The database is updated
very frequently by them and is robust. The electronic version was initially
only with the librarians and the computers used by the librarians was known as MEDLARS.
The MEDLINE was open
for public in 1996 through which the public can search it from different location
around the world. This is essential as the super computer database is in USA. The public
interface for MEDLINE is known as PUBMED.
You should also know that there are other interfaces by which you can operate the raw data of
National Library of Medicine , they are EBSCO
and ISI
That is the same source of
information “MEDLINE” can be read via Pubmed , EBCSO and ISI
Tuesday, September 1, 2015
ANAEROBIC ACTIVITY OF CEFOPERAZONE SULBACTAM
ANAEROBIC ACTIVITY OF CEFOPERAZONE SULBACTAM
Antagonistic activity between the Cefoperazone and sulbactam has not been noted.(1)
In a study done for assessing the anaerobic activity of sulbactam in combination with Cefoperazone against Bacteroides fragilis it was found that out of 42 % of Bacteroides fragilis which was found initially resistant to Cefoperazone alone, 94% among them were converted to susceptible on the addition of sulbactam.(1) Out of all the strains of Bacteroides fragilis studied 67% was susceptible to Cefoperazone sulbactam and 27%was moderately susceptible.(1)
One more invitro study where the activity of the Cefoprazone alone and in combination with sulbactam was compared , it was shown that Cefoprazone sulbactam has anaerobic activity and inhibited 90-100% of all bacteria but Cefoperazone has activity of 63%. The percent susceptible against Bacteroides fragilis group is 99 to 100% for cefoperazone-sulbactam and for Cefoperazone, 49%.(2)
In one more study where 374 selected beta-lactamase-producing gram-negative anaerobes (including 22 cefoxitin-resistant strains and 36 strains refractory to the enhancing effect of beta-lactamase inhibitors) and 20 beta-lactamase-negative strains were tested against antimicrobials. The organisms included in the study consists of 217 Bacteroides fragilis group strains, 137 non-B. fragilis group Bacteroides spp., and 40 fusobacteria. (3)
The study showed that in Bacteroides fragilis group 95% were susceptible to cefoperazone-sulbactam. For the beta-lactamase-positive non-B. fragilis group Bacteroides spp., greater than or equal to 94% were susceptible cefoperazone-sulbactam. . For the beta-lactamase-positive fusobacteria, greater than or equal to 97% were susceptible cefoperazone-sulbactam.(3)
DRAWBACK:
Cefoperazone-sulbactam lacked activity against some cefoxitin-resistant B. fragilis group strains but had excellent activity against other organisms.
CONCLUSION:
Adddition of Metronidazole to Cefoperazone -sulbactam routinely is not needed. As Cefoperazone -sulbactam itself will cover most of anaerobe, addition of Metronidazole will add to unnecessary cost of treatment to the patient without any increase in benefit and also will lead to development of resistance to the Cefoperazone-sulbactam.
REFERENCES
1. D'Amato RF, Hochstein L, Frankel H. In vitro activity of cefoperazone/sulbactam and other antimicrobials against anaerobic bacteria. Diagnostic microbiology and infectious disease. 1990 Jan-Feb;13(1):51-5. PubMed PMID: 2331850. Epub 1990/01/01. eng.
2. Wexler HM, Finegold SM. In vitro activity of cefoperazone plus sulbactam compared with that of other antimicrobial agents against anaerobic bacteria. Antimicrobial agents and chemotherapy. 1988 Mar;32(3):403-6. PubMed PMID: 3364960. Pubmed Central PMCID: PMC172186. Epub 1988/03/01. eng.
3. Appelbaum PC, Spangler SK, Jacobs MR. Susceptibilities of 394 Bacteroides fragilis, non-B. fragilis group Bacteroides species, and Fusobacterium species to newer antimicrobial agents. Antimicrobial agents and chemotherapy. 1991 Jun;35(6):1214-8. PubMed PMID: 1929264. Pubmed Central PMCID: PMC284313. Epub 1991/06/01. eng
Subscribe to:
Posts (Atom)