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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 29 year tenure till date Aug 2016, Around 30 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 13 lakh plus views on New Drug Approvals Blog in 212 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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GLIPTINS: BETTER APPROACH FOR TYPE 2 DIABETES


 

GLIPTINS: BETTER APPROACH FOR TYPE 2 DIABETES

Diabetes Mellitus is a metabolic disorder which results from defects in insulin secretion, insulin action, or both, further characterized by hyperglycemia, and causes long term damage and failure of various organs. It is estimated that 366 million people had Diabetes Mellitus in 2011; by 2030 this would have risen to 552 million. Many oral hypoglycaemic agents are…

read more: http://www.pharmatutor.org/articles/gliptins-better-approach-type-2-diabetes

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Otsuka Receives Complete Response Letter From U.S. Food And Drug Administration For Tolvaptan For Use In Patients With Autosomal Dominant Polycystic Kidney Disease


Tokyo, Japan – August 30, 2013 – Otsuka Pharmaceutical Co., Ltd announced today the company has received a Complete Response Letter (CRL) from the U.S. Food and Drug Administration (FDA) regarding the new drug application (NDA) for tolvaptan for the treatment of adult patients with rapidly progressing autosomal dominant polycystic kidney disease (ADPKD). The FDA issues CRLs to convey that their initial review of an application is complete; however, they cannot approve the application in its present form and request additional information.
In its letter to Otsuka, the FDA requested Otsuka provide additional data to further evaluate the efficacy and safety of tolvaptan in patients with ADPKD.
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OLD ARTICLE PASTED

Otsuka Pharmaceutical Submits New Drug Application in Japan for Tolvaptan for the Treatment of Autosomal Dominant Polycystic Kidney Disease (ADPKD)

JUNE 10, 2013 3:46 AM

TOLVAPTAN

may 30 2013

  • Tolvaptan was discovered by Otsuka in Japan, and its primary results from a global clinical trial involving 1,400 ADPKD patients from 15 countries, which demonstrated a statistically significant reduction in the rate of total kidney volume, were published in New England Journal of Medicine in 2012. It is also currently under a fast track review in the US, following our announcement of FDA accepting to review the application in April 2013.
  • ADPKD is a hereditary and often physically and mentally burdensome disease characterized by the development of multiple cysts in the kidneys. ADPKD is often associated with pain, hypertension, decreased kidney function and ultimately, kidney failure that may result in hemodialysis or kidney transplantation.
  • There are estimated to be approximately 31,000 ADPKD patients in Japan, and the diagnosed prevalence is estimated to be between 1:1000 and 1:4000 globally.

(Tokyo, Japan, May 30, 2013) – Otsuka Pharmaceutical Co., Ltd. Today announced it filed an application with the Pharmaceutical and Medical Devices Agency in Japan (PMDA) to market its novel compound tolvaptan for the treatment of Autosomal Dominant Polycystic Kidney Disease (ADPKD). Phase III clinical trial results that form the basis of the regulatory filing were published in the New England Journal of Medicine in November 2012. The MHLW has designated tolvaptan as an Orphan Drug.http://www.otsuka.co.jp/en/release/2013/0603_02.html

Tolvaptan (INN), also known as OPC-41061, is a selective, competitive vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated withcongestive heart failurecirrhosis, and the syndrome of inappropriate antidiuretic hormone(SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca and in India is manufactured & sold by MSN laboratories Ltd. under the trade name Tolvat & Tolsama.

Tolvaptan is also in fast-track clinical trials[2] for polycystic kidney disease. In a 2004 trial, tolvaptan, when administered with traditional diuretics, was noted to increase excretion of excess fluids and improve blood sodium levels in patients with heart failure without producing side effects such as hypotension (low blood pressure) or hypokalemia(decreased blood levels of potassium) and without having an adverse effect on kidney function.[3] In a recently published trial (TEMPO 3:4 ClinicalTrials.gov number, NCT00428948) the study met its primary and secondary end points. Tolvaptan, when given at an average dose of 95 mg per day over a 3-year period, slowed the usual increase in kidney volume by 50% compared to placebo (2.80% per year versus 5.51% per year, respectively, p<0.001) and reduced the decline in kidney function when compared with that of placebo-treated patients by approximately 30% (reciprocal serum creatinine, -2.61 versus -3.81 (mg/mL)-1 per year, p <0.001)[4]

Chemical synthesis:[5] Tolvaptan.png

  1. Shoaf S, Elizari M, Wang Z, et al. (2005). “Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias”. J Cardiovasc Pharmacol Ther 10 (3): 165–71. doi:10.1177/107424840501000304PMID 16211205.
  2.  Otsuka Maryland Research Institute, Inc.
  3. Gheorghiade M, Gattis W, O’Connor C, et al. (2004). “Effects of tolvaptan, a vasopressin antagonist, in patients hospitalized with worsening heart failure: a randomized controlled trial”. JAMA 291 (16): 1963–71. doi:10.1001/jama.291.16.1963PMID 15113814.
  4. (2012) Tolvaptan in Patients with Autosomal Dominant Polycystic Kidney Disease
  5. Kondo, K.; Ogawa, H.; Yamashita, H.; Miyamoto, H.; Tanaka, M.; Nakaya, K.; Kitano, K.; Yamamura, Y.; Nakamura, S.; Onogawa, T.; et al.; Bioor. Med. Chem. 1999, 7, 1743.
  6. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm350185.htm?source=govdelivery
  • Gheorghiade M, Niazi I, Ouyang J et al. (2003). “Vasopressin V2-receptor blockade with tolvaptan in patients with chronic heart failure: results from a double-blind, randomized trial”. Circulation 107 (21): 2690–6. doi:10.1161/01.CIR.0000070422.41439.04.PMID 12742979.

Bayer’s Stivarga® (regorafenib) Tablets Approved in Europe


WHIPPANY, N.J. and SOUTH SAN FRANCISCO, Calif., Aug. 30, 2013 /PRNewswire/ — Bayer HealthCare and Onyx Pharmaceuticals, Inc. (NASDAQ: ONXX) announced today that the European Commission has approved Stivarga® (regorafenib) tablets for the treatment of adult patients with metastatic colorectal cancer (mCRC).

In September 2012, Stivarga was approved by the U.S. Food and Drug Administration (FDA) for the treatment of patients with mCRC who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy.

READ ALL AT http://www.pharmalive.com/ec-approves-bayer-s-stivarga

OLD ARTICLE PASTED

File:Regorafenib.svg

Regorafenib

cas 755037-03-7

4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide hydrate

February 25, 2013 — The U.S. Food and Drug Administration today expanded the approved use of Stivarga (regorafenib) to treat patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to other FDA-approved treatments for this disease.

GIST is a tumor in which cancerous cells form in the tissues of the gastrointestinal tract, part of the body’s digestive system. According to the National Cancer Institute, an estimated 3,300 to 6,000 new cases of GIST occur yearly in the United States, most often in older adults.

Stivarga, a multi-kinase inhibitor, blocks several enzymes that promote cancer growth. With this new approval, Stivarga is intended to be used in patients whose GIST cancer cannot be removed by surgery or has spread to other parts of the body (metastatic) and is no longer responding to Gleevec (imatinib) and Sutent (sunitinib), two other FDA-approved drugs to treat GIST.

“Stivarga is the third drug approved by the FDA to treat gastrointestinal stromal tumors,” said Richard Pazdur, M.D., director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research. “It provides an important new treatment option for patients with GIST in which other approved drugs are no longer effective.”

Stivarga was approved in September 2012 to treat colorectal cancer. It is marketed by Bayer HealthCare Pharmaceuticals, based in Wayne, N.J. Gleevec is marketed by East Hanover, N.J.-based Novartis, and Sutent is marketed by New York City-based Pfizer.

Regorafenib (BAY 73-4506, commercial name Stivarga) is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targetedVEGFR2-TIE2 tyrosine kinase inhibition. It is currently being studied as a potential treatment option in multiple tumor types.[1]

Metastatic colorectal cancer

Regorafenib demonstrated to increase the overall survival of patients with metastaticcolorectal cancer[2] and has been approved by the US FDA on September 27, 2012.[3]Stivarga is being approved with a Boxed Warning alerting patients and health care professionals that severe and fatal liver toxicity occurred in patients treated with Stivarga during clinical studies. The most common side effects reported in patients treated with Stivarga include weakness or fatigue, loss of appetite, hand-foot syndrome (also called palmar-plantar erythrodysesthesia), diarrhea, mouth sores (mucositis), weight loss, infection, high blood pressure, and changes in voice volume or quality (dysphonia).[4]

  1.  “Bayer Announces New Data on Oncology Portfolio To Be Presented at the ECCO-ESMO Congress 2009″. Retrieved 2009-09-19.
  2. “Phase III Trial of Regorafenib in Metastatic Colorectal Cancer Meets Primary Endpoint of Improving Overall Survival”. Retrieved 2011-10-26.
  3. “FDA approves new treatment for advanced colorectal cancer”. 27 Sep 2012.
  4. “FDA Prescribing Information”. 27 Sept 2012.

Regorafenib from the structure consists of three simple aromatic ring structure, which fragments can be connected from urea by the corresponding two aniline with phosgene or triphosgene prepared by oxygen fragments can be connected SNAr from the corresponding phenol by reaction of. Carboxylic acid 1 by esterification of Thionyl Chloride 2 , methyl amine solution to 2 the ester group is converted to an amide to obtain 3 , 3 , and 4 in alkaline conditions by SNAr reaction of 5 , 5 , and then the isocyanate 6 ( from the corresponding aniline with phosgene or triphosgene was obtained) to obtain the Regorafenib.

Drug firms and cancer………… Lucrative lifesavers


http://www.economist.com/news/business/21584333-hopes-and-perils-betting-cancer-treatments-lucrative-lifesavers

 

The hopes and perils of betting on cancer treatments

NEW weapons are emerging in the war on cancer. That is good news not just for patients but also for drug companies. The biggest ones, faced with falling sales as their existing medicines go off-patent, are investing in smaller firms with promising cancer treatments under development, hoping to secure the next blockbuster.

http://www.economist.com/news/business/21584333-hopes-and-perils-betting-cancer-treatments-lucrative-lifesavers

 

NATURE’S VIAGRA-Health benefits of pomegranate by – By Dr. Janardhana V Hebbar, Ayurveda Expert


Image

Countless studies have shown the seemingly countless benefits of fruits for a person’s health.

The U.S. Government recommends that people get some servings of fruits every day. Of all the fruits ready in the shop today,

one fruit is at its height of popularity because of its legendary Greek mythology connection and its exoticism-the pomegranate fruit.

READ COMPLETE ARTICLE AT

http://www.askveda.in/blog/health-benefits-of-pomegranate/

 

 

Capecitabine Intermediate-cxpharma


 

 

 

   

Jiangsu Chengxin Pharmaceutical Co., Ltd with total area 60,000m2 and total invested amount of RMB 300 million, is a high-tech joint-stock enterprise established in 2012, located in Binjiang Pharm-Chem Industry Park, Qidong, the outstanding cultural city well known as the Rivers and Seas Pearl in Jiangsu Province, close to Chongming Island with merely one separated river. It takes around 1 hour by car from the manufacturing site to Shanghai, the Yangtze River Delta economic metropoli……More

http://www.cxpharma.com/en/about.asp?id=8

Dear sir,

We are just a manufacturer and very strong in the following intermediates:

Intermediates for Capecitabine:

2′,3′-Di-O-acetyl-5′-deoxy-5-fluorocytidine (CAS: 161599-46-8)

1,2,3-Triacetyl-5-deoxy-D-ribose (CAS: 62211-93-2)

Methyl-5-deoxy-2,3-O-isopropylidene-beta-D-ribofuranoside (CAS: 23202-81-5)

We have the dedicated workshop for Capecitabine intermediate. Our capacity is more than 20MT per month. Our company is complied with the requirement from EU GMP, US FDA and Chinese GMP. Just for your information.

If you are interested in any of above, please let me know.

Looking forward to your early reply.

Best regards,


Runya Wang(Ms) / Sales Department 

Add:     No.338 Shanghai Road, Binjiang Pharm-Chem

Industry Park, Qidong, Jiangsu, P.R.China 226221

Tel:       0086-513-86029596

Fax:      0086-513-86105399

Email:   runya.wang@cxpharma.com

Web:     www.cxpharma.com

http://www.cxpharma.com/en/home.asp   in english

Roche reports positive Phase II results for experimental eye drug


Lampalizumab

Roche reports positive Phase II results for experimental eye drug
Lampalizumab, an experimental eye drug from Roche, has helped slow down the progression of an advanced form of age-related macular degeneration (AMD) in a Phase II study, the company announced this week.

READ ALL AT

 http://www.pharmaceutical-technology.com/news/newsroche-reports-positive-phase-ii-results-experimental-eye-drug?WT.mc_id=DN_News

SEE ALSO

Lampalizumab effective in Phase II clinical trial for macular degeneration

Roche’s new drug for age-related macular degeneration, lampalizumab, showed effective in slowing the progression of AMD in patients with advanced disease, shrinking the area of geographic atrophy by 20%. Read More >>

 

Lampalizumab (INN) is a humanized monoclonal antibody designed for the treatment of geographic atrophy secondary to age-related macular degeneration. It binds to CFD.[1][2]

This drug was developed by Genentech/Roche.

References

  1. ^ World Health Organization (2012). “International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 107” (PDF). WHO Drug Information 26 (2).
  2. ^ Statement On A Nonproprietary Name Adopted By The USAN Council – Lampalizumab, American Medical Association.

FDA grants priority review to Pharmacyclics drug


ibrutinib

FDA grants priority review to Pharmacyclics drug

Pharmacyclics is getting a priority review of its blood cancer treatment by federal regulators. A priority review shortens a drug evaluation by the U.S. Food and Drug Administration from 10 months to six. The acceptance of the application triggers a $75 million milestone payment to Pharmacyclics from Johnson & Johnson’s Janssen unit.

http://www.rdmag.com/news/2013/08/fda-grants-priority-review-pharmacyclics-drug?et_cid=3451362&et_rid=523036890&type=cta

Ibrutinib (USAN[1]), also known as PCI-32765, is an experimental drug candidate for the treatment of various types of cancer. It is an orally-administered, selective and covalent inhibitor of the enzyme Bruton tyrosine kinase (Btk).[2][3][4] Ibrutinib is currently under development by Pharmacyclics, Inc and Johnson & Johnson’s Janssen Pharmaceutical division for B-cell malignancies including chronic lymphocytic leukemia, mantle cell lymphoma, diffuse large B-cell lymphoma, and multiple myeloma.[6][7][8]. Ibrutinib was first designed and synthesized at Celera Genomics by Zhengying Pan, who along with a team of chemists and biologists reported in 2007 a structure-based approach for creating a series of small molecules that inactivate BTK through covalent binding to cysteine-481 near the ATP binding domain of BTK[2]. These small molecules irreversibly inhibited BTK by using a Michael acceptor for binding to the target cysteine. In April 2006, Pharmacyclics acquired Celera’s small molecule BTK inhibitor discovery program, which included a compound, PCI-32765 (known as compound 13 in the Pan et al paper) that was subsequently chosen for further preclinical development based on the discovery of anti-lymphoma properties in vivo [5]. Since 2006, Pharmacyclics’ scientists have advanced the molecule into clinical trials and identified specific clinical indications for the drug. [2][3][4] [5] [6][7][8] It also has potential effects against autoimmune arthritis.[9]

Clinical trials

It has given good results in two phase II clinical trials.[10]

Mechanism

In preclinical studies on chronic lymphocytic leukemia (CLL) cells, ibrutinib has been reported to promote apoptosis, inhibit proliferation, and also prevent CLL cells from responding to survival stimuli provided by the microenvironment.[11] In this study, treatment of activated CLL cells with ibrutinib resulted in inhibition of Btk tyrosine phosphorylation and also effectively abrogated downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. Additionally, ibrutinib inhibited proliferation of CLL cells in vitro, effectively blocking survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-α), fibronectin engagement and stromal cell contact.

In early clinical studies, the activity of ibrutinib has been described to include a rapid reduction in lymphadenopathy accompanied by a transient lymphocytosis, suggesting that the drug might have direct effects on cell homing or migration to factors in tissue microenvironments.[12]

Ibrutinib has been reported to reduce CLL cell chemotaxis towards the chemokines CXCL12 and CXCL13, and inhibit cellular adhesion following stimulation at the B cell receptor.[13][14] Together, these data are consistent with a mechanistic model whereby ibrutinib blocks BCR signaling, which drives cells into apoptosis and/or disrupts cell migration and adherence to protective tumor microenvironments.

References

  1. ^ Statement on a Nonproprietary Name Adopted by the USAN Council
  2. ^ Pan, Z; Scheerens, H; Li, SJ; Schultz, BE; Sprengeler, PA; Burrill, LC; Mendonca, RV; Sweeney, MD et al. (2007). “Discovery of selective irreversible inhibitors for Bruton’s tyrosine kinase”. ChemMedChem 2 (1): 58–61. doi:10.1002/cmdc.200600221. PMID 17154430|displayauthors= suggested (help)
  3. ^ Celera Genomics Announces Sale of Therapeutic Programs to Pharmacyclics
  4. ^ United States patent 7514444
  5. ^ Honigberg, LA; Smith, AM; Sirisawad, M; Verner, E; Loury, D; Chang, B; Li, S; Pan, Z; Thamm, DH; Miller, RA; Buggy (2010). “The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy”. Proceedings of the National Academy of Sciences of the United States of America 107 (29): 13075–80. doi:10.1073/pnas.1004594107. PMID 20615965.  Unknown parameter |firs11= ignored (help)
  6. ^ Janssen Biotech, Inc. Announces Collaborative Development and Worldwide License Agreement for Investigational Anti-Cancer Drug, PCI-32765
  7. ^ Clinical trials involve PCI-32765
  8. ^ Clinical trials involve ibrutinib
  9. ^ Chang, BY; Huang, MM; Francesco, M; Chen, J; Sokolove, J; Magadala, P; Robinson, WH; Buggy, JJ (2011). “The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells”. Arthritis Research & Therapy 13 (4): R115. doi:10.1186/ar3400. PMID 21752263.
  10. ^ Good News Continues for Ibrutinib in CLL. 8 Dec 2012
  11. ^ Herman SE, Gordon AL, Hertlein E, Ramanunni A, Zhang X, Jaglowski S, Flynn J, Jones J, Blum KA, Buggy J.J., Hamdy A, Johnson AJ, Byrd JC. (2011) Bruton’s tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood 117: 6287-6296
  12. ^ The Bruton’s tyrosine kinase (BTK) inhibitor PCI-32765 (P) in treatment-naive (TN) chronic lymphocytic leukemia (CLL) patients (pts): Interim results of a phase Ib/II study.J Clin Oncol 30, 2012 (suppl; abstr 6507)
  13. ^ Ponader S, Chen SS, Buggy JJ, Balakrishnan K, Gandhi V, Wierda WG, Keating MJ, O’Brien S, Chiorazzi N, Burger JA. (2012) The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood 119: 1182-1189.
  14. ^ de Rooij MF, Kuil A, Geest CR, Eldering E, Chang BY, Buggy JJ, Pals ST, Spaargaren M. (2012) The clinically active BTK inhibitor PCI-32765 targets B-cell receptor (BCR)- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia. Blood 119: 2590-2594.

External links

The U.S. Food and Drug Administration (FDA) has approved Mirvaso (brimonidine) topical gel for the topical treatment of the facial erythema (redness) of rosacea in adults 18 years of age or older


 

brimonidine

Mirvaso

Generic Name: brimonidine
Date of Approval: August 23, 2013
Company: Galderma Laboratories, L.P.

Treatment for: Facial Erythema (Redness) of Rosacea

READ ALL AT

http://www.drugs.com/mirvaso.html

Brimonidine (bri-MOE-ni-deen, brand names Alphagan and Alphagan-P) is a drug used to treat open-angle glaucoma or ocular hypertension.

It acts via decreasing synthesis of aqueous humor, and increasing the amount that drains from the eye through uveoscleral outflow. As a treatment for glaucoma, it is usually given in eyedrop form.

Mechanism of action

Brimonidine is an α2 adrenergic agonist.

Alpha 2 agonists, through the activation of a G protein-coupled receptor, inhibit the activity of adenylate cyclase. This reduces cAMP and hence aqueous humour production by the ciliary body.

Peripheral alpha 2 agonist activity results in vasoconstriction of blood vessels (as opposed to central alpha 2 agonist activity that decreases sympathetic tone, as can be seen by the medication clonidine). This vasoconstriction may explain the acute reduction in aqueous humor flow. The increased uveoscleral outflow from prolonged use may be explained by increased prostaglandin release due to alpha adrenergic stimulation. This may lead to relaxed ciliary muscle and increased uveoscleral outflow.[1]

Clinical uses

Brimonidine is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It is also the active ingredient of Combigan along with timolol maleate.

In 2013, the FDA approved topical application of brimonidine 0.33% (Mirvaso) for facial erythema or rosacea.

References

 

  1.  Toris, C.; Camras, C.; Yablonski, M. (1999). “Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients”. American journal of ophthalmology 128 (1): 8–14. PMID 10482088.  edit
  • Mosby’s Drug Guide for Nurses (7th edition; Skidmore) 2007.

External links

Portuguese medicine expenditure in hospitals keeps increasing


August 29, 2013 | By Márcio Barra

The Portuguese Government spends almost as much money on the NHS hospitals’ expenses with medicines as with the reimbursement of all drugs sold in pharmacies, according to data revealed by the Portuguese Ministry of Health.

The numbers disclosed show that, in 2012, the state spent about $ 2,200 million with drugs, 1.200 million of which with the reimbursement of medicines sold in pharmacies and 1.000 million with medicines provided in hospitals.

While the expenses on drugs sold in pharmacies are in control, thanks to successive price cuts by the Government over the years – just in 2013, about 1.400 brand drugs had mandatory a 7% price discount – the expenses with medicines in hospitals and debts to the Pharmaceutical Industry grew again this year, both in value and in average payments. This upward trend is ongoing for six consecutive months.

In July, the value…

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