Why Do We Need Peptides?

You or your families might have been given tamiflu to cure him of a bout of bird-flu, but did you end up with a stomach-ache too? Like tamiflu, many medicines have side-effects. In the future, we may have a new form of medicine called peptides that won’t have any side-effects!

One reason we need new drugs is that medicines are not a natural part of our body. We know how they go right, like we know penicillin kills bacteria, or paracetamol reduces fever. But we’ve got to accept that they don’t work perfectly, yet.

That does not mean all medicines are unsafe. For example, tamiflu prevents viruses from escaping infected cells, so they cannot infect new cells. But if you’ve not eaten properly or took some other medicine, a tablet of Tamiflu might give you a mild stomach-ache. Taken properly, most drugs have no bad effects.

Most of the molecules in our body are proteins, which do things like digesting food and taking oxygen to all cells of the body. Every medicine has its correct target protein. For example, tamiflu blocks the action of a protein, which is made by the flu virus. There is a spot on the protein which is important for the virus to work. Tamiflu goes and sits exactly in that spot, stopping the protein dead in its tracks. However, it doesn’t sit very tightly, and in time gets knocked off. So you have to give more Tamiflu after some time to keep the protein under control.

Glutathione (in picture) is an important peptide found in our bodies. It helps to clean up oxygen radicals, which are produced during normal activities of our body. These radicals can damage cells, causing pain, paralysis or poisoning. In patients who have low glutathione levels due to some illness (like AIDS), giving glutathione from outside can help. However, it gets digested in the stomach, so it can’t be taken as a pill. Instead a peptide called N-acetylcysteine is given as a drug. The body converts this to glutathione.

Another peptide being tested in labs now is DSIP(Deltasleep-inducing peptide). Studies show that it can help people who are trying to get off their addiction to heroin or alcohol. It also helps fight narcolepsy, a condition in which the patient feels very sleepy throughout the day (Although we think giving less homework might have the same effect). And it also helps children recovering from the effects of chemotherapy (which is a way to treat cancer).

There are a lot more peptides being tested against all kinds of diseases, cancer and other disorders. If you choose to become a chemist, we hope you’ll make a peptide medicine that’ll solve a major medical problem!

What Are the Benefits of Diosmin?

Diosmin is a natural flavonoid that is extracted from various plant sources and sold as a daily supplement either by itself or combined with similar flavonoids. People use this chemical to make medicine.

Diosmin might help treat hemorrhoids by reducing swelling (inflammation), and restoring normal vein function. It is used for treating various disorders of blood vessels including hemorrhoids, varicose veins, poor circulation in the legs (venous stasis), and bleeding (hemorrhage) in the eye or gums. It is also used to treat swelling of the arms (lymphedema) following breast cancer surgery, and to protect against liver toxicity. It is often taken in combination with hesperidin, another plant chemical.

Companies throughout the world offer diosmin in pill form. According to some experts, diosmin is often combined with a similar compound called hesperidin to maximize its effects.

Diosmin improves blood circulation and strengthens vein walls by improving the elasticity of blood vessels while inhibiting certain pro-inflammatory lipids. It helps your blood to flow against gravity and return from your legs to your heart. This has the effect of reducing or eliminating varicose and spider veins, while preventing recurrence by treating their cause.

Citrus fruits, especially lemons, are rich sources of diosmin, according to “Food Chemistry.” Lemons produce a number of useful flavonoids, including diosmin, in both the mature fruit and the leaves. Buddha’s finger, a type of citron, is also rich in diosmin. According to the “Journal of Agricultural and Food Chemistry,” green Meyer lemons and Buddha’s finger fruits contain the highest diosmin levels, especially when treated with hormones during the early growth stages.

The relief that diosmin offers from poor circulation, varicose and spider veins, and hemorrhoids can enable you to enjoy more physical activity and less interruptions in your social life.  It does cause some side effects, including digestive discomfort and headache. More time can be spent with family and friends, enjoying your favorite activities without the discomfort caused by poor circulation.

Is Prandin Useful For Weight Loss?

Prandin is the brand name for repaglinide. Diet, exercise and possibly other medications are used together with Prandin for people with Type II diabetes as a way to decrease blood sugar levels. Be aware of the precautions regarding Prandin and take the drug only on the advice and guidance of a physician. The medication causes the pancreas to produce insulin, thus helping to lower blood sugar.

Prandin works to decrease blood sugar levels by spurring the pancreas to create insulin. This drug is specifically for non-insulin dependant patients with Type II diabetes only. The drug may cause a drastic decrease in blood sugar, so you should be familiar with the symptoms of hypoglycemia, which include nausea, hunger, anxiety, numbness and irregular heartbeat. If you experience these symptoms, you should drink or eat something with sugar or take a glucagon injection as instructed by your doctor.

Hypoglycemia is a potential side effect of taking Prandin. Hypoglycemia can occur from prolonged exercise, alcohol, stress or missing meals. Symptoms of low blood glucose include hunger, tremors, headache, irritability and difficulty concentrating. Test your blood sugar, and if your blood sugar is low, take a simple carbohydrate such as orange juice or hard candy or whatever is recommended by your physician. Seek medical attention if symptoms persist.

Check your blood sugar often when following a repaglinide(the CAS number is 135062-02-1) regimen. Check to make sure your blood sugar is not too high. While Prandin is not used specifically for weight loss, it is associated with it for two main reasons. The goal of a diabetic diet to provide nutrients to the body without all the fats and sugars associated with a higher calorie diet. By counting your carbohydrates and sugar intake, you naturally take in fewer calories and lose weight. When you couple this with the suggested exercise, weight loss is almost guaranteed.

Prandin is a prescription drug and should never be taken by anyone without Type II diabetes. If you use it wrongly as a weight loss drug, you may find yourself becoming hypoglycemic. One of the classic symptoms of hypoglycemia is a voracious hunger, so you will most likely gain weight if this happens.

How Does Altabax Work?

Altabax (retapamulin), is an antibacterial ointment used to treat the highly contagious bacterial skin infection impetigo. Manufactured by GlaxoSmithKline (GSK), Altabax is classified as a pleuromutilin antibiotic, and retapamulin was the first of this class to be developed for topical use in humans.

Impetigo
The U.S. Food and Drug Administration (FDA) approved Altabax in 2007 as a topical treatment for impetigo. Altabax is not effective in treating skin infections not caused by bacteria.

Impetigo is most common in children, but adults can also get impetigo. The bacteria usually enter through an insect bite, scrape, or cut. Impetigo can be spread through direct contact with an infected person’s sores, or by coming in contact with clothing or other items used by the person. In young children, blisters may appear on the body. Another type of impetigo forms sores on the legs and feet that can leave scars. Some forms of impetigo are itchy; some are painful. Typically, red sores appear on the face around the mouth and nose. The sores blister. When ruptured, they ooze fluid or pus. A crust then forms around the sore.

Usage
The patient should apply a thin layer of Altabax ointment twice daily for five days and may use the medication longer with the doctor’s recommendation. Patients can cover the skin areas with a bandage or gauze. It is not to be used in the nose or eyes or in the vaginal or rectal areas. It has not been determined if Altabax is safe for use during breast-feeding. Wear gloves when applying the Altabax ointment and use the ointment for the prescribed length of time. If necessary, bandage the infected area to prevent bacteria from spreading to other areas.

Retapamulin is intended for use on the outside of the body only and is not to be taken orally.  It is intended for use specifically to treat infections caused by Staphlococcus aureus or Streptococcus pyogenes. Altabax will not be effective if used for other forms of the impetigo infection and can cause the patient to develop a super infection or antibiotic resistance.

Side Effects
Children using Altabax can experience generalized itching and itching at the application site, diarrhea, sore nasal passages and throat, headache, fever and eczema. Side-effects experienced by adults using Altabax are headache, skin irritation at the application site, nausea, diarrhea and sore nasal passages and throat. If you experience a severe reaction or severe irritation at the application site, the ointment should be wiped off immediately and discontinued. Your doctor can prescribe an alternative treatment.

Flomax Used For BPH

As men grow older, the prostate becomes an important aspect of health and check ups. Yearly prostate checks can help detect a host of different potentially lethal disorders that can attack your health and affect your quality of life. Although enlargement of the prostate is a benign condition, it may eventually lead to prostate cancer. So men also need some treaments to improve quality of life. One of these treatment options is Flomax.

BPH
Flomax is a prescription medication used to treat benign prostatic hypertrophy, or BPH. BPH is a common condition in older men; it is also known as prostate enlargement. BPH occurs when large nodules form inside the prostate gland. This enlarges the size of the prostate which can narrow your urethra, causing issues urinating as well as an increased risk of a urinary tract infection.

Function
Morniflumate is reported as an ingredient of Flomax.It works by relaxing the muscles in and around the prostate and urinary tract. Although it is only approved for use in BPH, it is also occasionally prescribed to treat other urinary problems such as certain spinal cord injuries and neurogenic bladder leakage. Flomax does not treat the underlying condition of BPH, but it does improve the symptoms for most men who take it. As the name indicates, Flomax helps with difficulty urinating; this is one of the most common symptoms of BPH.

Urination
Once the veins and arteries relax around the affected prostate and bladder neck, regardless of the size of the prostate, there is an increased amount of room in the urinary tract. This allows urine to flow freely out of the bladder and reduces the risk of a urinary tract infection. It also reduces some of the symptoms associated with BPH such as the frequent urge to urinate and some of the pain associated with urinating.

Considerations
Flomax(Morniflumate) should not be taken by anyone who has shown symptoms of an allergy to this medication or similar medications in the past. It should be used with caution by people who have orthostatic hypotension (feeling dizzy or fainting when standing up). Adequate studies of Flomax during pregnancy and breastfeeding have not been done because the drug is only FDA approved to treat men with BPH.

Like any medication, Flomax may have effects other than improving the condition it treats. The most common side effects are dizziness, headache, weakness, diarrhea, back pain and abnormal ejaculation. In rare cases, Flomax can cause blurry vision, sleepiness or priapism (an erection that lasts too long).

The Facts About An Antiparasitic

An antiparasitic is a type of medication that designed to eradicate infections of parasites on or in human or animal bodies. Some of these are well-known and don’t need prescriptions. An antiparasitic drug can be stronger and might come in oral formulations to kill parasite infestations that are internal. Yet lice shampoos can easily be purchased in over the counter formulations and applied topically. There are different medications suited to different types of parasites and they may be prescribed.

Many are used to treat different forms of internal worm infestations. Worm infestations might either occur as a result of ingestion or through things like bites from mosquitoes. Some of these medicines, such as pyrantel pamoate or mebendazole, will work with most nematodes or worms, and other medicines are best used with just a few types of parasites. Antinematodes are one group that can address infection with things like pinworms, tapeworms, roundworms or Filaria.

Some medicines treat parasitic infections caused by protozoa that enter the body. One of the most familiar protozoan infections is Giardia. An antiprotozoal like tinidazole may be prescribed for treatment.

A few infections, especially of parasites like tapeworm could require more specific treatment with a separate antiparasitic class. Both praziquantel and niclosamide are called anticestodes. These target tapeworm, which are technically nematodes.

The complex nature of parasitic infections means observing a few rules when taking an antiparasitic. Just as with antibiotics, people are urged to completely finish medicine as directed by a doctor, and to not stop treatment even if they start to feel better. It’s possible for an infection to rebound without completing prescribed medications. Some infections can also be tenacious, and it may be necessary to extend treatment in certain instances or to switch medicines.

Rafoxanide (one of its intermediates is 3,5-Diiodosalicylic acid) is used for the treatment and control of liver fluke in sheep and cattle. Given the variety of antiparasitic types available, it is usually difficult to discuss things like side effects or treatment length. Some people might need extensive treatment if an infection is severe and hard to eliminate. Others could only need treatment for a few weeks. A simple infection of pinworms might mean taking a few pills over a two-week period. Provided this is accompanied by good hygiene, the infection is likely to resolve.

Getting a mosquito bite or acquiring lice usually says nothing about a person’s basic hygiene. In other cases, hygiene and food and water safety can prevent some infections, avoiding need to take an antiparasitic. People are advised to drink safe water, to always wash hands using restrooms, and to thoroughly cook meat. These preventatives may save people infection with many worm species, and different amoebic and protozoan species.

Fluorine Can Be Used In The Synthesis Of Pharmaceuticals

A schematic representation of the four different stereoisomers of the fluorinated amino acid derivatives that can be synthesized using the fluorination and hydroxy/amino derivative technique.

Despite its small size, the fluorine atom has had a vast impact on the pharmaceutical industry. More often than not, introducing fluorine to a drug molecule improves the drug’s biological activity, earning it a reputation as a ‘magic element’.

Amino acids are not only the building blocks of proteins, they are commonly found in pharmaceutical drugs. Now, Mikiko Sodeoka and colleagues at the RIKEN Advanced Science Institute, Wako, have developed a synthesis technique that can selectively and efficiently combine fluorine and amino acids into the same organic molecule.

The starting materials are alpha-keto esters that contain a carbonyl group and an ester group. The first reaction of the team’s technique is the substitution of a hydrogen atom, on the carbon atom adjacent to the carbonyl group, for a fluorine atom. As there are two hydrogen atoms that could be replaced, two mirror images, or enantiomers could result.
Sodeoka and colleagues use a palladium catalyst that preferentially forms one of these enantiomers. This renders the reaction enantioselective; that is, one enantiomer is selectively formed over the other. The carbon atom to which the fluorine attaches becomes a stereogenic center as it has four different substituents. The interchange of any two substituents gives a pair of enantiomers. In the wider picture, these enantiomers are stereoisomers—molecules that differ only by their 3D orientation of the atoms.

Next, the carbonyl group of the fluorinated alpha-keto ester transforms to a hydroxyl group. Again, two possible stereoisomers of the molecule could form. By exploiting the existing stereogenic center and using different reagents, the researchers could synthesize one stereoisomer in preference to the other.

Hence, the technique not only introduces fluorine, but two stereogenic centers to the molecule. The formation of two stereogenic centers creates the possibility of four different stereoisomers. By tuning the reagents, the team isolated all four stereoisomers in separate reaction sequences. Overcoming the chemical instability of the intermediate (such as 1-Amino Cyclobutanecarboxylic acid, its CAS No. is 22264-16-0), however, is challenging. “The fluorinated alpha-keto esters easily convert to their hydrated form, so care is required to exclude water from the reaction mixture,” Sodeoka explains. “However, the hydroxy and amino acid derivatives are stable and easy to handle.”

In the future, Sodeoka and colleagues hope to widen the scope of the fluorination reaction to other starting materials. This would create the possibility of making numerous biologically active compounds.

The Research & Development Of Osanetant

 

Developed by Sanofi-Aventis (formerly Sanofi-Synthelabo), Osanetant is a neurokinin 3 receptor antagonist which are useful for the treatment of disorders associated with dysfunction of the dopaminergic and noradrenergic systems.

 

First identified in the 1930s, neurokins are neurotransmitters found in the substantia nigra and striatum areas of the brain. Unlike most of the neurotransmitters identified to date, they are made from peptides rather than amino acids. They are and believed to be involved in the control of movement. Their potential as therapeutic targets for drug development has only recently been realised but is seen an area of rich research. Several antagonists to these neurokinins are now in development. With GSK’s talnetant, osanetant was one of two NK3 antagonists in development for schizophrenia.

 

It has now been found that osanetant and its pharmaceutically acceptable salts are useful for the treatment of mood disorders, in particular for the treatment of depression. By depression is meant in particular, major depressive disorders, minordepressive disorders, dysthymia, depressive disorders associated with anxiety and depressive disorders associated with bipolar disorders.

 

The potential antipsychotic properties of osanetant were identified in a special study protocol termed a Metatrial. The objective was to test concomitantly for both safety and efficacy four compounds which were judged to have antipsychotic properties based on their pharmacological profiles.

 

The effect of osanetant (an intermediate of this drug is called as 3,4-Difluorophenylacetonitrile, the CAS number is 658-99-1 ) on major depressive disorders has been investigated in patients of between 18 and 65 years of age. The patients were given osanetant (200 mg/day) for a period of about 6 weeks. The improvement in the depressive syndrome was measured from the significant reduction in the scores on the Hamilton scale and by recording the impressions of the clinician and the patient’soverall impressions.

 

Thus, the object of the present invention is the use of osanetant and its pharmaceutically acceptable salts for the preparation of medicinal products for use in the treatment of mood disorders, in particular in the treatment of depression.

 

Osanetant and its pharmaceutically acceptable salts are prepared according to European Patent Application EP 673 928; similarly, the pharmaceutical preparations can be prepared as described in this same patent application.


What’s The Information Of Apixaban?

Apixaban is an anticoagulant used to prevent blood clots. It is not available to the public yet, though initial studies show that it is an effective treatment. This medication is given to patients who have recently undergone surgery of the knees or hips and to those with atrial fibrillation.

The drug interferes with factor Xa, while other anticoagulants prevent blood clots by interfering with other enzymes. Though apixaban is in the anticoagulant class, its mechanism of action is unlike other anticoagulants. There are a number of enzymes that play a part in the process of forming blood clots.

When it was tested against a competing medication in 2007, it was shown to be as effective at preventing blood clots from forming following knee surgery. Further studies in 2010 showed that it is more effective than its competitors at preventing dangerous blood clots that can form as a result of hip surgery. Recent studies of the drug have shown apixaban to be as or more effective than competing drugs.

According to the Los Angeles Times ‘The study, called APPRAISE-2, was testing the drug in…patients with acute coronary syndrome, a group of problems characterised by chest pain caused by insufficient blood supply to the heart muscle. Though it seemed that apixaban was performing well in trials, it caused dangerous bleeding in patients who were suffering from acute coronary syndrome and who were receiving antiplatelet therapy in addition to apixaban.

The main side effect of taking an anticoagulant such as apixaban is that a patient can experience life-threatening bleeding. With the ability to create blood clots compromised, bleeding continues unchecked which can lead to severe blood loss. This is a risk associated with taking any anticoagulant, and, in most patients, apixaban has not been shown to cause more or less risk of bleeding than any other drug. 5-Bromovaleryl chloride (the CAS number is 4509-90-4) is an intermediate of this madecation.

While clotting is necessary in order to control bleeding, under certain circumstances it can pose a serious risk to the life of the patient. Joint surgery on the knees or the hips can place a patient at particular risk for developing clots in the large blood vessels of the legs. Many patients who undergo these types of surgeries are given anticoagulants, such as apixaban, to help reduce the risk of this.

Scientists can now block heroin, morphine addiction

In a major breakthrough, an international team of scientists has proven that addiction to morphine and heroin can be blocked, while at the same time increasing pain relief.

The team from the University of Adelaide and University of Colorado has discovered the key mechanism in the body’s immune system that amplifies addiction to opioid drugs. The team has focused its research efforts on the immune receptor known as Toll-Like receptor 4 (TLR4). Laboratory studies have shown that the drug (+)-naloxone (pronounced: PLUS nal-OX-own) will selectively block the immune-addiction response.

“Our studies have shown conclusively that we can block addiction via the immune system of the brain, without targeting the brain’s wiring,” says the lead author of the study, Dr Mark Hutchinson, ARC Research Fellow in the University of Adelaide’s School of Medical Sciences.

“Both the central nervous system and the immune system play important roles in creating addiction, but our studies have shown we only need to block the immune response in the brain to prevent cravings for opioid drugs.”

The results – which could eventually lead to new co-formulated drugs that assist patients with severe pain, as well as helping heroin users to kick the habit – will be published tomorrow in the Journal of Neuroscience.

“Opioid drugs such as morphine and heroin bind to TLR4 in a similar way to the normal immune response to bacteria. The problem is that TLR4 then acts as an amplifier for addiction,” Dr Hutchinson says.

“The drug (+)-naloxone automatically shuts down the addiction. It shuts down the need to take opioids, it cuts out behaviours associated with addiction, and the neurochemistry in the brain changes – dopamine, which is the chemical important for providing that sense of ‘reward’ from the drug, is no longer produced.”

“The drug that we’ve used to block addiction, naloxone (CAS No.:465-65-6), is a non-opioid mirror image drug that was created by Dr Kenner Rice in the 1970s. We believe this will prove extremely useful as a co-formulated drug with morphine, so that patients who require relief for severe pain will not become addicted but still receive pain relief . This has the potential to lead to major advances in patient and palliative care,” Professor Watkins says.

Senior author Professor Linda Watkins, from the Center for Neuroscience at the University of Colorado Boulder, says: “This work fundamentally changes what we understand about opioids, reward and addiction. We’ve suspected for some years that TLR4 may be the key to blocking opioid addiction, but now we have the proof. The researchers say clinical trials may be possible within the next 18 months.