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Sunday, December 15, 2019

Duloxetine




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Duloxetine, is a medication used to treat major depressive disorder, generalized anxiety disorder, fibromyalgia, and neuropathic pain. It is taken by mouth.


PHARMACOLOGY


Duloxetine inhibits the reuptake of serotonin and norepinephrine (NE) in the central nervous system. Duloxetine increases dopamine (DA) specifically in the prefrontal cortex, where there are few DA reuptake pumps, via the inhibition of NE reuptake pumps (NET), which is believed to mediate reuptake of DA and NE. Duloxetine has no significant affinity for dopaminergic, cholinergic, histaminergic, opioid, glutamate, and GABA reuptake transporters, however, and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NE transporters. Duloxetine undergoes extensive metabolism, but the major circulating metabolites do not contribute significantly to the pharmacologic activity.

Major depressive disorder is believed to be due in part to an increase in pro-inflammatory cytokines within the central nervous system. Antidepressants including ones with a similar mechanism of action as duloxetine, i.e. serotonin metabolism inhibition, cause a decrease in proinflammatory cytokine activity and an increase in anti-inflammatory cytokines; this mechanism may apply to duloxetine in its effect on depression but research on cytokines specific to duloxetine therapy is lacking.


The analgesic properties of duloxetine in the treatment of diabetic neuropathy and central pain syndromes such as fibromyalgia are believed to be due to sodium ion channel blockade.

Absorption: Duloxetine is acid labile, and is formulated with enteric coating to prevent degradation in the stomach. Duloxetine has good oral bioavailability, averaging 50% after one 60 mg dose. There is an average 2-hour lag until absorption begins with maximum plasma concentrations occurring about 6 hours post dose. Food does not affect the Cmax of duloxetine, but delays the time to reach peak concentration from 6 to 10 hours.

Distribution: Duloxetine is highly bound (>90%) to proteins in human plasma, binding primarily to albumin and α1-acid glycoprotein. Volume of distribution is 1640L.

Metabolism: Duloxetine undergoes predominately hepatic metabolism via two cytochrome P450 isozymes, CYP2D6 and CYP1A2. Circulating metabolites are pharmacologically inactive.


Elimination: Duloxetine has an elimination half-life of about 12 hours (range 8 to 17 hours) and its pharmacokinetics are dose proportional over the therapeutic range. Steady-state is usually achieved after 3 days. Only trace amounts (<1%) of unchanged duloxetine are present in the urine and most of the dose (approx. 70%) appears in the urine as metabolites of duloxetine with about 20% excreted in the feces.





Common side effects include dry mouth, nausea, feeling tired, dizziness, agitation, sexual problems, and increased sweating. Severe side effects include an increased risk of suicide, serotonin syndrome, mania, and liver problems. Antidepressant withdrawal syndrome may occur if stopped. There are concerns that use during the later part of pregnancy can harm the baby. It is a serotonin–norepinephrine reuptake inhibitor. How it works is not entirely clear.
Duloxetine was approved for medical use in the United States in 2004. It is available as a generic medication.


Tuesday, September 10, 2019

HERBS AND SUPPLEMENTS FOR DIABETES


        Diabetes is a disease in which your blood glucose, or blood sugar, levels are too high. Glucose comes from the foods you eat. Insulin is a hormone that helps the glucose get into your cells to give them energy. With type 1 diabetes, your body does not make insulin. With type 2 diabetes, the more common type, your body does not make or use insulin well. Without enough insulin, the glucose stays in your blood. You can also have prediabetes. This means that your blood sugar is higher than normal but not high enough to be called diabetes. Having prediabetes puts you at a higher risk of getting type 2 diabetes.

Over time, having too much glucose in your blood can cause serious problems. It can damage your eyes, kidneys, and nerves. Diabetes can also cause heart disease, stroke and even the need to remove a limb. Pregnant women can also get diabetes, called gestational diabetes.

Blood tests can show if you have diabetes. One type of test, the A1C, can also check on how you are managing your diabetes. Exercise, weight control and sticking to your meal plan can help control your diabetes. 
     
        1.   ALOEVERA  (കറ്റാർവാഴ)



Aloe vera is a common plant with many different uses. Many people are aware of its benefits for skin care, but it may also have other benefits, including slowing the progress of type 2 diabetes.
One review, published in 2013, looked at the use of aloe vera to treat symptoms of diabetes in rats. Findings suggested that aloe vera might help protect and repair the beta cells in the pancreas that produce insulin. The researchers believed this might be due to aloe's antioxidant effects.
The researchers called for more research into aloe and its extracts to be sure of these effects.
Ways of taking aloe include:
adding juiced pulp to a drink or smoothie
taking capsules that contain aloe as supplements
People should not eat aloe vera skin care products.
Aloe vera juice may offer a number of health benefits. Find out more here.



  2.CINNAMON (കറുവപ്പട്ട)



Cinnamon is a fragrant spice that comes from the bark of a tree. It is a popular ingredient in sweets, baked goods, and other dishes.
It has a taste that can add sweetness without any additional sugar. It is popular with people with type 2 diabetes for this reason alone, but it may also offer other benefits.
A 2010 review found evidence from studies involving humans that cinnamon may improve levels of:
glucose
insulin and insulin sensitivity
lipids, or fats, in the blood
antioxidant status
blood pressure
lean body mass
digestion

In another review published in 2013, researchers concluded that cinnamon might lead to:
lower fasting blood glucose levels
less total cholesterol and "bad" low-density lipoprotein (LDL) cholesterol
higher levels of "good" high-density lipoprotein (HDL) cholesterol
a reduction in triglycerides, or fat, in the blood
increased insulin sensitivity
It did not appear to have a significant impact on hemoglobin A1C. The A1C test is a standard test for diagnosing and monitoring diabetes.
Nevertheless, lipids, cholesterol, and insulin sensitivity are all important markers for people with diabetes.

In both studies, the researchers note that the results may depend on:
the type of cinnamon, as the amount of active ingredient depends on the type
the amount or dose
the individual's response to cinnamon
other medications the person may be taking




3.      3. BITTER MELON (പാവക്ക)


Momordica charantia, or bitter melon, is a medicinal fruit. Practitioners of traditional Chinese and Indian medicine have used bitter melon for centuries. People can cook the fruit and use it in many dishes. Some scientists have been looking into its potential medicinal uses.

There is some evidence that bitter melon may help with the symptoms of diabetes. One review has noted that people have used many parts of the plant to help treat diabetes.

Research has shown that taking bitter melon in the following forms can lead to a reduction in blood sugar levels in some people:

seeds
blended vegetable pulp
juice
supplements
Eating or drinking the bitter melon can be an acquired taste, but taking supplements may make it more palatable.

There is not enough evidence to support using bitter melon instead of insulin or medication for diabetes.

However, it may help people rely less on those medications or lower their dosages.

Learn more here about the impact bitter melon can have on blood sugar levels.

Bitter melon capsules are available for purchase online.



4. MILK THISTLE  (കീഴാർനെല്ലി )

 


People have used milk thistle since ancient times for many different ailments, and especially as a tonic for the liver.


Silymarin, the extract from milk thistle that has received the most attention from scientists, is a compound with antioxidant and anti-inflammatory properties. These are the properties that may make milk thistle a useful herb for people with diabetes.

Many of the studies on silymarin are promising, but the research is not strong enough to recommend the herb or extract alone for diabetes care, according to one review published in 2016.

There appear to be no reports of significant side effects, and many people take milk thistle as a supplement. However, it is best to speak to a doctor first before using any supplements.




5. FENUGREEK SEED  (ഉലുവ )



 Fenugreek is another seed that may help lower blood sugar levels.


The seeds contain fibers and chemicals that help to slow down the digestion of carbohydrates and sugar.

There is also some evidence that the seeds may help delay or prevent the onset of type 2 diabetes.

Findings of a 3-year investigation published in 2015 noted that people with prediabetes were less likely to receive a diagnosis of type 2 diabetes while taking powdered fenugreek seed.

The researchers concluded that taking the seed led to:

increased levels of insulin in the body, leading to a reduction in blood sugar
lower cholesterol levels
The study involved 66 people with diabetes who took 5 grams (g) of the seed preparation twice a day before meals, and 74 controls, who did not take it.

A person can:
include fenugreek as a herb in certain dishes
add it to warm water
grind into a powder
take it as a supplement in capsule form
A range of fenugreek capsules is available for purchase here.



6. GYMNEMA (ചക്കരക്കൊല്ലി)



Gymnema sylvestre is a herb that comes from India. Its name means "sugar destroyer."

A 2013 review noted that people with both type 1 and type 2 diabetes who took gymnema showed signs of improvement.

In people with type 1 diabetes who took the leaf extract for 18 months, fasting blood sugar levels fell significantly, compared with a group who received only insulin.

Other tests using gymnema found that people with type 2 diabetes responded well to both the leaf and its extract over various periods.

Some people experienced:

lower blood sugar levels
higher insulin levels
Using either the ground leaf or leaf extract may be beneficial. But once again, talk to your doctor about using it before starting.



7. GINGER  (ഇഞ്ചി)

Ginger is another herb that people have used for thousands of years in traditional medicine systems.

People often use ginger to help treat digestive and inflammatory issues.

However, in 2015, a review suggested that it may also help treat diabetes. The results showed that ginger lowered blood sugar levels, but did not lower blood insulin levels.

Because of this, they suggest that ginger may reduce insulin resistance in the body for type 2 diabetes.

However, the researchers were uncertain as to how ginger might do this, and they called for more research to confirm these findings.

People can take ginger:

by adding ginger powder or chopped, fresh ginger root to raw or cooked food
brewed into tea
as a supplement in capsule form

by drinking it in a ginger ale



Saturday, July 6, 2019

BICALUTAMIDE





Bicalutamide is used to treat prostate cancer. This medication works by blocking the action of male hormones in the prostate, slowing the growth of cancer cells.
Bicalutamide is an oral non-steroidal anti-androgen , it is comprised of a racemic mixture that is 50:composition of (R)-bicalutamide and (S)-bicalutamide enantionmers Bicalutamide binds to the androgen receptor.



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Bicalutamide may also be used to treat excessive hair growth in women, as a component of feminizing hormone therapy for transgender women, to treat early puberty in boys, and to prevent overly long-lasting erections in men.


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Side effects
Hot flashes, breast swelling/tenderness/pain, nausea, vomiting, constipation, diarrhea, stomach upset, weight changes, headache, trouble sleeping, drowsiness, or dizziness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Precautions
Before taking bicalutamide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, diabetes, heart disease.
This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
This medication should not be used in women, especially during pregnancy or breast-feeding. It may harm an unborn or breast-feeding baby. Consult your doctor for more details. Male patients and their female partners should use reliable forms of birth control during and for 130 days after treatment with bicalutamide since this medication may damage sperm.




 BRANDS
BICALUTAMIDE 50 MG TAB AVAILABLE IN JAN AUSHADHI AT RS 131.00 MOST LEAST PRICE IN INDIA
CALURAN50
TABI 50
UTAMIDE 50
BICALPRO 50
BIPROSTA
ZYLUTA
BICATERO 50

CASSOTIDE 50

CALUDEC 50

CASODEX 50

GUNCEF 50

BIPROSTIVA 50

Wednesday, January 23, 2019

THYROXINE SODIUM


The thyroid hormones act on nearly every cell in the body. They act to increase the basal metabolic rate, affect protein synthesis, help regulate long bone growth (synergy with growth hormone) and neural maturation, and increase the body's sensitivity to catecholamines (such as adrenaline) by permissiveness. The thyroid hormones are essential to proper development and differentiation of all cells of the human body. These hormones also regulate protein, fat, and carbohydrate metabolism, affecting how human cells use energetic compounds. They also stimulate vitamin metabolism. Numerous physiological and pathological stimuli influence thyroid hormone synthesis.
Both T3 and T4 are used to treat thyroid hormone deficiency (hypothyroidism). They are both absorbed well by the gut, so can be given orally. Levothyroxine is the pharmaceutical name of the manufactured version of T4, which is metabolised more slowly than T3 and hence usually only needs once-daily administration. 



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LEVOTHYROXINE Available at JAN AUSHADHI STORES 
PRICE
50 mcg- 45 Rs /100 tab
100 mcg-Rs 56/100 tab




Levothyroxine, also known as L-thyroxine, is a manufactured form of the thyroid hormone, THYROXINE (T4). It is used to treat thyroid hormone deficiencyincluding the severe form known as myxedema coma. It may also be used to treat and prevent certain types of thyroid tumors. It is not indicated for weight loss. Levothyroxine is taken by mouth or given by injection into a vein. Maximum effect from a specific dose can take up to six weeks to occur.
Side effects from excessive doses include weight loss, trouble tolerating heat, sweating, anxiety, trouble sleeping, tremor, and fast heart rate. Use is not recommended in people who have had a recent heart attack. Use during pregnancy has been found to be safe. It is recommended that dosing be based on regular measurements of TSH and T4 levels in the blood. Much of the effect of levothyroxine is following its conversion to triiodothyronine (T3).
Levothyroxine was first made in 1927. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Levothyroxine is available as a generic medication. 


USE
Levothyroxine is typically used to treat hypothyroidism, and is the treatment of choice for people with hypothyroidism, who often require lifelong thyroid hormone therapy. It may also be used to treat goiter via its ability to lower thyroid-stimulating hormone (TSH), a hormone that is considered goiter-inducing. Levothyroxine is also used as interventional therapy in people with nodular thyroid disease or thyroid cancer to suppress thyroid-stimulating hormone (TSH) secretion. A subset of people with hypothyroidism treated with an appropriate dose of levothyroxine will describe continuing symptoms despite TSH levels in the normal range. In these people, further laboratory and clinical evaluation is warranted as they may have another cause for their symptoms. Furthermore, it is important to review their medications and possible dietary supplements as several medications can affect thyroid hormone levels.

Levothyroxine is also used to treat subclinical hypothyroidism which is defined by an elevated TSH level and a normal-range free T4 level without symptoms. Such people may be asymptomatic and whether they should be treated is controversial. One benefit of treating this population with levothyroxine therapy is preventing development of hypothyroidism. As such, it is recommended that treatment should be taken into account for patients with initial TSH levels > 10 mIU/L, people with elevated thyroid peroxidase antibody titers, people with symptoms of hypothyroidism and TSH levels between 5–10 mIU/L, and women who are pregnant or want to become pregnant. Oral dosing for patients with subclinical hypothyroidism is 1 µg/kg/day.

It is also used to treat myxedema coma, which is a severe form of hypothyroidism characterized by mental status changes and hypothermia. As it is a medical emergency with a high mortality rate, it should be treated in the intensive care unit with thyroid hormone replacement and aggressive management of individual organ system complications.












Friday, January 4, 2019

BENEFITS OF FERROUS ASCORBATE




      WHO and UNICEF have recommended taking oral iron supplements for adolescents and young children in the countries where 40 percent of anaemia is prevalent in the population. Most of the oral iron formulations are available in the form of ferrous sulphate as well as in the form of ferric compounds consisting of iron polymaltose complex. These iron compounds differ in their safety, bio-availability, cost and side effects.Apart from the different chemical states of iron formulations available in the market, they also exist in different galenic forms.

Clinically, iron salts that are bivalent like ferrous sulphate, ferrous fumarate and ferrous gluconate are widely used than the ferric iron forms. The bio-availability of ferric forms of iron are 3 to 4 times less than the ferrous forms (10 to 15 percent bio-availability). Ferric forms of iron are poorly soluble in alkaline solutions and hence they have to be transformed into ferrous forms before they are absorbed.

Oral iron preparations have followed the conventional‘prolonged-release’ formulation, which improves the toleration capacity of the gastrointestinal tract and enhances the bio-availability. After the ferrous form absorption, iron reaches its maximum in the blood for about 7 hours and stays in that state for 24 hours.

Ferrous ascorbate results from the reaction of ascorbic acid with iron. Iron is absorbed very well in the presence of ascorbic acid, as this compound is known to convert ferric iron into ferrous iron. Ferrous form of iron is soluble at neutral pH and can be absorbed three times higher than the ferric form. Oxidation is prevented by Ascorbic acid, which can thus act as reducing agent as well as maintain the iron in ferrous form. Ferrous ascorbate is known to exist intact inside the gastrointestinal tract due to the stable chelation of iron with ascorbate. This compound does not dissociate due to any of the food inhibitors.  Iron gets absorbed easily in vivo from ferrous ascorbate than from ferrous sulfate. It is found that ferrous ascorbate dissociates in aqueous solution into ascorbate ion and ferrous ion where ascorbate ion acts as a monodentate. Ferrous ascorbate is known to dissociate at pH5. At pH6 to 8, the solubility effect is enhanced by ascorbate, which is beneficial for the absorption of iron from ferrous ascorbate.

A clinical study was conducted comparing the ferrous ascorbate formulation with that of ferrous sulphate in 18 healthy volunteers. The intestinal absorption was not different when measured after 21 days. But, hemoglobin content has come to baseline values in both the groups. Another study by the same research group was conducted in which the bio-availability of trivalent iron form (FeIII hydroxide polymaltose) was compared with the bivalent form (ferrous ascorbate). The iron absorption in the intestines was evaluated in the fasting state by the estimation of plasma iron tolerance curves and whole body iron retention values. The estimation of plasma iron showed lower FeIII content (1.2+/-0.1percent) compared to 43.7+/-7.1percent of ferrous ascorbate. After taking a meal, there was a change in divalent iron absorption than the trivalent iron absorption.

The increase in hemoglobin levels after prescribing 100mg dosage of iron for 28 days was higher in the case of divalent formulations than that of the trivalent formulations. A few other similar studies have proved that divalent form of iron or ferrous ascorbate has greater bio-availability than the trivalent form of iron. Hence, ferrous salts and especially ferrous ascorbate is chosen over other iron forms for preparing the drugs as they are efficient, cost effective and have tolerability.