16 August, 2010

Fenofibric acid

Fenofibric acid is a lipid regulating agent available as delayed release capsules for oral administration.
Fenofibric acid activates the peroxisome proliferator activated receptor a (PPARa).
PPARs affect the expression of target genes involved in cell proliferation, cell differentiation and in immune and inflammation responses.

fenofibric Acid is specifically indicated for

1) Co-administration Therapy with Statins for the Treatment of Mixed Dyslipidemia
To reduce TG and increase HDLC in patients with mixed dyslipidemia and CHD or a CHD risk equivalent who are on optimal statin therapy to achieve their LDL-C goal.
2) Treatment of Severe Hypertriglyceridemia
3) Treatment of Primary Hyperlipidemia or Mixed Dyslipidemia
To reduce elevated LDL-C, Total-C, TG, and Apo B, and to increase HDL-C.

The recommended intial dose of the drug for co-administration therapy with statins for the treatment of mixed dyslipidemia is 135 mg daily. Co-administration with the maximum dose of a statin should be avoided.

The recommended initial dose of the drug for severe hypertriglyceridemia is 45 to 135 mg once daily.

The recommended initial dose of the drug for primary hyperlipidemia or mixed dyslipidemia is 135 mg once daily.


Mechanism of Action


fenofibric acid is a lipid regulating agent available as delayed release capsules for oral administration. Fenofibric acid activates the peroxisome proliferator activated receptor a (PPARa). Through this mechanism, fenofibric acid increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of Apo CIII (an inhibitor of lipoprotein lipase activity). The resulting decrease in triglycerides produces an alteration in the size and composition of LDL from small, dense particles to large buoyant particles, which have a greater affinity for cholesterol receptors and are catabolized rapidly. PPARa activation also induces an increase in the synthesis of HDL-C and Apo AI and AII.

Side Effects


* Muscle Pain
* Tenderness
* Weakness
* Tiredness
* Fever
* Abdominal Pain
* Nausea
* Vomiting

Bromocriptine & Type 2 Diabetes

Bromocriptine (Parlodel, Cycloset), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), Hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.

Indications


Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug. In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset (VeroScience). It is currently unknown how this drug improves glycemic control, but it has been shown to reduce HbA1c by ~0.5%.

Side effects


Most frequent side effects are nausea, orthostatic hypotension, headaches and vomiting through stimulation of the brainstem vomiting centre.
Bromocriptine can cause worsening of liver problems.
Vasospasms with serious consequences such as myocardial infarction and strong have been reported in connection with the puerperium, appears to be extremely rare event.
Bromocriptine use has been anecdotically associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).
Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.

30 July, 2010

Gymnema sylvestre


Gymnema sylvestre is a herb native to the tropical forests of southern and central India where it has been used as a naturopathic treatment for diabetes.

Sanskrit Name : Meshasringi, Madhinasini or madhoolika, Hindi: Gurmar, Tamil and Malayalam are Sirukurinchaan(சிறுகுரிஞ்சான்), Amudhapushpam, Chakkarakkolli.


Chemical composition

The major bioactive constituents of Gymnema sylvestris are a group of oleanane type triterpenoid saponins known as gymnemic acids. The latter contain several acylated (tigloyl, methylbutyroyl etc.,) derivatives of deacylgymnemic acid (DAGA) which is 3-O-glucuronide of gymnemagenin (3, 16, 21, 22, 23, 28-hexahydroxy-olean-12-ene)2. The individual gymnemic acids (saponins) include gymnemic acids I-VII, gymnemosides A-F, gymnemasaponins

G. sylvestre leaves contain triterpene saponins belonging to oleanane and dammarene classes. Oleanane saponins are gymnemic acids and gymnemasaponins, while dammarene saponins are gymnemasides. Besides this, other plant constituents are flavones, anthraquinones, hentri-acontane, pentatriacontane, α and β- chlorophylls, phytin, resins, d-quercitol, tartaric acid, formic acid, butyric acid, lupeol, β-amyrin related glycosides and stigmasterol. The plant extract also tests positive for alkaloids. Leaves of this species yield acidic glycosides and anthroquinones and their derivatives.

Gymnemic acids have antidiabetic, antisweetener and anti-inflammatory activities. The antidiabetic array of molecules has been identified as a group of closely related gymnemic acids after it was successfully isolated and purified from the leaves of Gymnema sylvestre. Later, the phytoconstituents of Gymnema sylvestre were isolated, and their chemistry and structures were studied and elucidated.


While it is still being studied, and the effects of the herb are not entirely known, the herb has been shown to reduce blood sugar levels when used for an extended period of time. Additionally, Gymnema reduces the taste of sugar when it is placed in the mouth, thus some use it to fight sugar cravings. From extract of the leaves were isolated glycosides known as Gymnemic acids, which exhibit anti-sweet activity.


This effect lasts up to about 2 hours. Some postulate that the herb actually reduces cravings for sugar by blocking sugar receptors in the tongue. This effect was observed in rats in a 2003 study conducted by CH Lemon, et al. It is currently being used in an all natural medication for diabetes with other ingredients such as cinnamon, chromium, zinc, biotin, banaba plant, huckleberry and bitter melon.
The active ingredient is thought to be gurmenic acid which has structure similar to saccharose. Extracts of Gymnema is not only claimed to curb sweet tooths but also for treatment of as varied problems as hyperglycemia, obesity, high cholesterol levels, anemia and digestion. According to the Sushruta of the Ayurveda it helps to treat Madhumeha ie glycosuria.

In 2005, a study made by King’s College, London, United Kingdom, showed that a water-soluble extract of Gymnema Sylvestre, caused reversible increases in intracellular calcium and insulin secretion in mouse and human β-cells when used at a concentration (0.125 mg/ml) without compromising cell viability. Hence forth these data suggest that extracts derived from Gymnema Sylvestre may be useful as therapeutic agents for the stimulation of insulin secretion in individuals with Type 2 Diabetes.

Alternative names
The plants also goes under many other names such as; Gurmari, Gurmarbooti, Gurmar, periploca of the woods and Meshasringa. The Hindi word Gur-mar (Madhunaashini in Sanskrit, Chakkarakolli in Tamil), literally means sugar destroyer. Meshasringa (Sanskrit) translates as "ram's horn", a name given to the plant from the shape of its fruits. Gymnema probably derives from the Latin word meaning naked and sylvestre means from the forest.

30 June, 2010

Fenugreek (Trigonella foenum-graecum)


Fenugreek (Trigonella foenum-graecum) is an herbal supplement often claimed to be beneficial for the following uses:

Lowering blood sugar in people with diabetes
Helping with a loss of appetite
Lowering cholesterol
Lowering triglycerides
Stimulating milk production in breastfeeding women.



Fenugreek contains sotolon, trigonelline, and 4-hydroxyisoleucine, compounds that are thought to be the active components of it. 4-hydroxyisoleucine may stimulate the secretion of insulin, which is why fenugreek may theoretically lower blood sugar. The seeds also contain fiber and pectin, a complex carbohydrate, both of which may slow down the digestive tract, which can help lower blood sugar. However, it is important to know that there is not enough scientific evidence to show that fenugreek is indeed effective for these uses.

Fenugreek may also contain "blood-thinning" compounds known as coumarins, but it is not known if these compounds are present in high enough quantities to actually make a difference in humans. The herb may also stimulate the uterus, heart, and intestines. However, it is important to know that there is not sufficient scientific evidence to show that fenugreek is effective for these uses.

Side Effects

Fenugreek can cause several side effects

Diarrhea
Indigestion or heartburn
Low blood sugar (hypoglycemia)
Body and urine odors that smell like maple syrup.


Is Fenugreek Safe?

Normal doses are probably safe for most people when taken in normal amounts, such as amounts found in food, although higher doses can cause problems. Some people may be more likely to experience problems than others.
Therefore, you should talk with your healthcare provider prior to taking this supplement if you have:

Diabetes
A bleeding disorder
Any allergies, including allergies to foods, dyes, or preservatives.


Also, let your healthcare provider know if you are:

Pregnant or thinking of becoming pregnant
Breastfeeding.

Make sure to tell your healthcare provider about all other medicines you are taking, including prescription and non-prescription medicines, vitamins, and herbal supplements.

It is not known exactly what to expect from a fenugreek overdose, but it is reasonable to assume that taking too much may cause the usual side effects of fenugreek, but they may be more severe. Theoretically, an overdose could cause severe problems, such as internal bleeding or dangerously low blood sugar.

RETINOPATHY IN DIABETES!!


Retina has tiny blood vessels that are easy to damage. Having high blood glucose and high blood pressure for a long time can damage these tiny blood vessels.

Initially these tiny blood vessels swell and weaken. Some blood vessels then become clogged and do not let enough blood through. most patients do not experience any symptoms in this stage

One eye may be damaged more than the other, or both eyes may have the same amount of damage. As diabetic retinopathy becomes worse, new blood vessels grow. These new blood vessels are weak. They break easily and leak blood into the vitreous of eye. The leaking blood keeps light from reaching the retina.

In this stage patients may experience floating spots or almost total darkness. Sometimes, the blood will clear out by itself, in other cases surgery is required to remove it.

Over the years, the swollen and weak blood vessels can form scar tissue and pull the retina away from the back of the eye. If the retina becomes detached, you may see floating spots or flashing lights. You may feel as if a curtain has been pulled over part of what you are looking at. This condition can cause loss of sight or blindness if you don't take care of it right away.

Symptoms

Often, there are no symptoms in the early stages of this diabetic eye disease. Vision may not change until the disease becomes severe, nor is there any pain. Blurred vision may occur when the macula -- the part of the retina that provides sharp, central vision -- swells from the leaking fluid. This condition is called macular edema.

If new blood vessels have grown on the surface of the retina, they can bleed into the eye, blocking vision. Even in more advanced cases, the disease may progress a long way without any noticeable symptoms, so regular eye examinations for people with diabetes are important.

Treatment

There are a number of treatment options for diabetic retinopathy. Your eye doctor may suggest laser treatment, which involves a light beam aimed into the retina of the damaged eye. The beam closes off leaking blood vessels, which may stop blood and fluid from leaking into the vitreous and slow down the loss of sight.

If a lot of blood has leaked into your vitreous and your sight is poor, your eye doctor might suggest you have surgery called a vitrectomy. This procedure removes blood and fluids from the vitreous of your eye. Then, clean fluid is put back into the eye. The surgery often makes your eyesight better.

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