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Month: December 2018

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Diabetic Neuropathy and its Management

About more than a half of population in India suffers from diabetes mellitus nowadays.  Out of which, most of them are grappled with its complications like diabetic retinopathy, diabetic nephropathy and diabetic neuropathy etc. The diabetic neuropathy is the most prevalent and common complication found amongst all.  This complication can range from merely aggravating to disabling or even life-threatening. It can lead to dysfunction or sometimes amputation of the particular body part.  The elevated blood glucose level found to be the major factor responsible for diabetic neuropathy.

There are several mechanisms which lead to diabetic neuropathy. The prolonged condition of hyperglycemia triggers several factors like the polyol pathway, advanced glycation product, polymerase pathway and oxidative stress etc. All these factors lead to the destruction of nerve tissue which further becomes a reason for amputation of the damaged body part.

The symptoms of diabetic neuropathy are:

  • Tingling
  • Buzzing and prickling sensation on the feet
  • Hot and cold sensation
  • Loss of knee reflex
  • Proximal leg weakness
  • Numbness or paraesthesia
  • Sharp pain or cramps
  • Loss of balance and coordination
  • Serious foot problems, such as ulcers, infections, deformities and bone and joint pain

The degree and duration of hyperglycemia is the major risk factor of diabetic neuropathy. Insulin resistance is also associated with the endothelial dysfunction that leads to diabetic neuropathy. Moreover, several other risk factors for diabetic neuropathy are the low level of HDLP, cigarette smoking and hypertension etc.

Metformin is an antidiabetic drug which belongs to subclass biguanide. It is mostly employed in the treatment of type 2 diabetes. This medication is used to decrease hepatic glucose production, to decrease glucose absorption and to increase target cell insulin sensitivity. An increased level of glucose elevates the level of an advanced glycation end product in blood. The advanced glycation end products are harmful compounds that are formed when protein or fat combine with sugar in the bloodstream. These compounds accumulate and damage the nerve tissue, which ultimately leads to neuropathy. It has been found in several studies that metformin is capable to reduce the amount advanced glycation end product.

Diabetes-induced oxidative stress is also one of the major cause of neuropathy. Oxidative stress is defined as the excess formation and insufficient removal of a highly reactive molecule such as reactive oxygen species and reactive nitrogen species. In diabetes, the antioxidant enzyme level is reduced in peripheral nerves due to oxidative stress. The elevated level of reactive oxygen species contributes to nerve damage. Metformin also has proved for scavenging reactive oxygen and hydroxyl species. The in vitro and in vivo studies proved the fact that metformin reduces the oxidative stress as well as increase the superoxide dismutase activity. Superoxide dismutase is an enzyme that alternately catalyzes the dismutation or partitioning of the superoxide (O2−) radical into either ordinary molecular oxygen (O2) or hydrogen peroxide (H2O2).

Hence, Metformin is very much effective in diabetic neuropathy. It lowers the blood glucose level as well as also contributes in the removal of oxidative stress and decrease the level of advanced glycation end products in the blood, which regarded as the prime factors responsible for diabetic neuropathy.  

These days many Pharmaceutical manufacturing companies are promoting metformin and glimepiride combinations to help patients to fight diabetes and its complications.  It is very crucial that third party manufacturing or contract manufacturing of Metformin and its combinations must be of high quality with accurate dissolution profile.  They must meet new quality standards established by the Government.  The critical point of third-party manufacturing of Metformin and Glimiperide combination are as follows :

  1.  Both the drugs should be analysed while dissolution testing.
  2. Bi-layered tablets are the one which matches government analytical recommendations.
  3. Drug content should be uniform.

 

References

https://www.sciencedirect.com/science/article/pii/S0014299999003428

https://www.sciencedirect.com/science/article/pii/S001429991530073X

https://www.sciencedirect.com/science/article/pii/S0168822710005826

https://www.sciencedirect.com/science/article/pii/S0026049503000064

https://www.mayoclinic.org/diseases-conditions/diabetic-neuropathy/symptoms-causes/syc-20371580

https://www.webmd.com/diabetes/diabetes-neuropathy#1

https://www.healthline.com/health/metformin-oral-tablet

 

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METHYLCOBALAMIN STIMULATES SEROTONIN CREATION

We all are aware of the fact that, how vitamins are essential for our body. Different vitamins regulate different functions in our body and protect the body from several deficiencies and diseases.  Methylcobalamin is one of them. It is also called as Vitamin B12 and used as dietary supplement. A low level of vitamin B12 makes you feel tired, weak,  slow thinking,  nerve damage, digestive issues and other neurological problems like depression and memory loss. Therefore, many people turn to vitamin B12 supplements to help meet their needs and prevent a deficiency. There are two forms of vitamin B12, Methylcobalamin and cyanocobalamin. Methylcobalamin is the natural form of Vit B12 and cyanocobalamin is manmade. While methylcobalamin contains a methyl group, cyanocobalamin contains a cyanide molecule.

Methylcobalamin is the activated form of vitamin B12 and is being used to treat some nutritional diseases and other diseases in the clinic, such as Alzheimer’s disease and rheumatoid arthritis. Methylcobalamin also promotes the release and formation of several hormones, Serotonin is one of them. Serotonin is one of the essential hormones of the body, produced by nerve cells. Serotonin impacts every part of our body, from emotions to motor skills. Serotonin is considered a natural mood stabilizer. It’s the chemical that helps with sleeping, eating, and digesting. Serotonin also helps in reducing depression, regulate anxiety, heal wounds maintain bone health.

Methylcobalamin has specific biomedical influences in the human body. The body needs B12 to convert homocysteine to methionine, protect DNA and RNA, support energy, protect nerve and brain cells, stimulate serotonin production. Vitamin B12 can only naturally be found in animal products like fish, meat, eggs, milk, etc. Methylcobalamin is the only form of B12 that can cross the blood-brain barrier without help or conversion. Its methyl group stimulates serotonin creation, a neurotransmitter responsible for mood support. It also works directly on brain cells to protect against damage.

There are some other benefits of methylcobalamin like the formation of red blood cells and prevent from anaemia. Methylcobalamin also plays a key role in the pregnancy. The deficiency of vitamin B12 during pregnancy may increase the risk of birth defects, such as neural tube defects. Methylcobalamin is important for the prevention of brain and spinal cord birth defects. An Adequate level of methylcobalamin decreases homocysteine levels in the blood. This may help prevent the development of age-related macular degeneration. Vitamin B12 is involved in energy production in our body. Thus, methylcobalamin is an essential vitamin that contributes in almost all the body functions in our body.

 

https://www.patientslikeme.com/treatment/vitamin-b12-methylcobalamin

https://www.everydayhealth.com/drugs/vitamin-b-12

https://www.practo.com/medicine-info/methylcobalamin-179-apivv

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4772032/

https://www.ncbi.nlm.nih.gov/books/NBK28242/

http://www.jhrr.org/article.asp?issn=2394-2010;year=2014;volume=1;issue=1;spage=5;epage=9;aulast=Mahmood

 

 

 

 

 

 

 

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Is aceclofenac and Paracetamol safe in Pregnancy ?

Pregnancy is regarded as the most delicate period for every woman. The physicians are very careful at this stage for prescribing the medicine to a pregnant lady as during pregnancy health of both mother and child are at stake. There are plenty of drugs prohibited during the pregnancy.

Whenever we suffer from fever and pain, we mostly use the combination of Aceclofenac and paracetamol. The trend of combining drugs is merely used to increase the efficacy of salts and provide the maximum benefits to the patients.  So, let us know about both of the drugs

Aceclofenac

Aceclofenac belongs to NSAIDs (Nonsteroidal anti-inflammatory drugs). NSAIDs are being widely used all over the world for anti-inflammatory, analgesic and antipyretic activities. Aceclofenac is a new NSAID which belongs to a phenylacetic acid group. It is also a prodrug of Diclofenac sodium. Aceclofenac inhibits COX (Cyclo-oxygenase) enzyme which is responsible for the production of prostaglandins. The Prostaglandins are inflammatory mediators which cause pain, inflammation, redness, and fever. Aceclofenac is given orally in the form of a tablet as well as in suspension form. Aceclofenac is also reported to be effective in other painful conditions such as dental pain, rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.

Paracetamol

Paracetamol also belong to NSAIDs (Nonsteroidal anti-inflammatory drugs).

Paracetamol is the most common drug used in fever and pain. Paracetamol is often recommended as the first line treatment for pain, as it is safe for most the people to take and with very fewer side effects. It can be taken as tablets, capsules, liquids, soluble tablets, suppositories, and injection. It also is known as acetaminophen. Paracetamol is a weak inhibitor of prostaglandins. But does not selectively inhibit the COX-2, due which inflammation is not suppressed by paracetamol. Its antipyretic effect makes paracetamol more prominent for the treatment of fever.  Paracetamol lowers the fever by direct action on the thermoregulatory centre in the Hypothalamus and blocks the effects of endogenous pyrogen.

Is Aceclo-para is safe in Pregnancy?

Though the safety profile of Aceclofenac and Paracetamol during pregnancy is not clear, it is suggested to be unsafe for Pregnancy. As Aceclofenac belongs to NSAIDs, these drugs can cause a rare form of fetal anomalies. NSAIDs can cause fetal cardiovascular changes, including the closure of the ductus arteriosus and persistent pulmonary hypertension in the newborn. These drugs are contraindicated in the third trimester of pregnancy. Moreover, it also delays the onset of labour with an increased risk of excessive bleeding in the mother as well as the fetus. Paracetamol can also increase the risk of attention-deficit and hyperactivity disorder (ADHD) when used during pregnancy. The frequencies of fetal abnormalities caused by NSAIDs in human are low. So, women taking Aceclo-para combination in Pregnancy must consult the gynaecologist before using it.

 

https://www.medicineindia.org/pharmacology-for-generic/177/aceclofenac-paracetamol

https://www.webmd.com/drugs/2/drug-57595/paracetamol-oral/details

https://cashkaro.com/blog/how-to-take-aceclofenac-paracetamol-uses-dosage-side-effects-and-more/25027

https://www.ncbi.nlm.nih.gov/pubmed/15662292

https://www.tabletwise.com/questions/is-aceclofenac-paracetamol-safe-in-pregnancy-5101791028969472

https://www.medizzine.com/en/pregnancy/risk.php?name=Aceclofenac

https://www.ahajournals.org/doi/abs/10.1161/01.STR.32.7.1607

https://journals.sagepub.com/doi/abs/10.1111/ijs.12053

https://europepmc.org/abstract/med/8971314

https://europepmc.org/abstract/med/2663407

https://europepmc.org/abstract/med/8823693

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5335881/

https://journals.lww.com/anesthesia-analgesia/Fulltext/2010/04000/Combining_Paracetamol__Acetaminophen__with.30.aspx
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Therapeutic effectiveness of Cefixime

Therapeutic effectiveness of Cefixime

We all are familiar with Antibiotics, their effectiveness in several bacterial infections. These antibiotics are classified as broad spectrum and narrow spectrum. Various classes and subclasses of antibiotics are effective against different types of bacteria. Cefixime is one of the majorly used antibiotics in numerous bacterial infections. It comes under the class of broad-spectrum antibiotics, which means it is effective against a wide variety of different types of bacteria. Cefixime is the third generation cephalosporin antibiotic. Cefixime was approved for medical use in the United States in 1989. It is on the World Health Organization’s List of Essential Medicines, the most effective and safe medicines needed in a health system.

How Cefixime kills the bacteria?

Antibiotics are also classified as bactericidal and bacteriostatic. Cefixime comes under bactericidal antibiotic. It works by interfering with the formation of the bacterial cell wall. Cefixime binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. Moreover, it inhibits transpeptidase which prevents cross-linking of the bacterial cell wall. Inhibition in the cell wall formation leads to the death of bacteria.

Cefixime is much stable in the presence of β-lactamase enzymes hence many organisms resistant to penicillin’s and some cephalosporins may be susceptible to Cefixime. It is highly active against gram-negative cocci, gram-negative bacilli and anaerobes than gram-positive cocci and bacilli. It is not active against pseudomonas

Cefixime is effective against:

Gram-positive

  • Streptococcus pneumoniae
  • Streptococcus pyogenes

Gram-negative Organisms

  • E.coli
  • H. influenzae
  • Moraxella catarrhalis
  • Proteus mirabilis
  • N. gonorrhea

Cefixime is used in the various infections

  • Tonsillitis
  • Pharyngitis
  • Otitis media
  • Bronchitis
  • Urinary tract infections
  • Gonorrhea

Cefixime has been studied in numerous clinical trials for different bacterial infections.  Cefixime found effective in these clinical trials. It has been found in a clinical study that was held in Japan that complicated urinary tract infection treated with a daily divided dose of Cefixime 200mg or a single dose of 400mg.

It has been found in the multicenter trial in Germany that Cefixime at a dose of 400mg orally for 5-10 days gives a significant improvement of the patients suffering from acute bronchitis. As compared to amoxicillin, the improvement rate of patients of respiratory infections who were treated with 400mg Cefixime is much larger than amoxicillin.

In comparison with penicillin, Cefixime is more effective in the treatment of Pharyngitis. An open-label randomized trial was conducted to compare the efficacy and safety of Cefixime, 8 mg/kg once daily and penicillin V, 250 mg 3 times daily. At the end of the therapy, the bacteriologic eradication rate of Cefixime was 97% and in case of Penicillin, it was 77% which shows that Cefixime is much effective than penicillin in Pharyngitis.

Even a single dose of 400 mg of Cefixime at once provides a remarkable improvement in Gonorrhea. It has also noted that Cefixime also effective in otitis media at a dose of 8mg/kg/day when it has been given to the children at the age of 6-12 years old for 10-14 days.

Typhoid fever is most common in developing countries. Various clinical trials are conducted on the efficacy of Cefixime in typhoid fever. An open-labelled, non-comparative, study was conducted in 112 subjects to evaluate the efficacy and safety of Cefixime on typhoid fever in multiple hospitals of Nepal. A dose of 200mg of Cefixime was given twice to the patients for 7 days. A significant reduction was seen in patients at the end of the study. This study proves that Cefixime is safe and efficacious for the treatment of typhoid fever.

Cefixime is regarded as a safe drug. It can also prescribe to pregnant as well as breastfeeding women. Any carcinogenic and mutagenic activity doesn’t report yet in the various animal as well as in vitro studies.

 

References

 

https://europepmc.org/abstract/med/1454432

https://link.springer.com/article/10.1007/BF01742990

https://aac.asm.org/content/45/9/2450.short

https://link.springer.com/article/10.2165/00003495-199549060-00010

https://www.tandfonline.com/doi/abs/10.1080/1120009X.1989.11738903

https://www.amjmed.com/article/0002-9343(88)90457-3/fulltext

https://www.amjmed.com/article/0002-9343(88)90457-3/fulltext

 

 

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