2-Propylvaleric acid sodium salt

2-Propylvaleric acid sodium salt is also called sodium 2-propylpentanoate,sodium valproate,Valproate Sodium,Its cas registry number is 1069-66-5. It can be used as a medicine to cure the disease of epilepsy, anorexia nervosa, panic attack, anxiety disorder, posttraumatic stress disorder, migraine and bipolar disorder, as well as other psychiatric conditions requiring the administration of a mood stabilizer.

2-Propylvaleric acid sodium salt is an anticonvulsant. 2-Propylvaleric acid sodium salt can be used to control acute episodes of mania and acute stress reaction. Side effects can include tiredness, tremors, nausea, vomiting and sedation.The intravenous formulations are used when oral administration is not possible.

2-Propylvaleric acid sodium salt is a weak blocker of sodium ion channels; it is also a weak inhibitor of enzymes that deactivate GABA such as GABA transaminase. It may also stimulate the synthesis of GABA, but the direct mechanism is not known. Because of its many mechanisms of action,  2-Propylvaleric acid sodium salt has efficacy in all partial and generalised seizures including absence seizures.

2-Propylvaleric acid sodium salt works by stabilising electrical activity in the brain, and so reducing fits.

Histone deacetylase inhibitor (IC 50 = 400 μ M) that exhibits anticancer, anti-inflammatory and neuroprotective effects. Displays anticonvulsive activity via an increase in GABA levels and decreases A β production in animal models of Alzheimer's disease. Also attenuates NMDA-mediated excitation, blocks voltage-gated Na + channels and modulates firing of neurons. Enables induction of pluripotent stem cells from somatic cells by Oct4 and Sox2.

Name:2-Propylvaleric acid sodium salt

EINECS:213-961-8

Molecular Formula:C8H15NaO2

CAS Registry Number:1069-66-5

Appearance:white powder

Molecular Weight:166.19

Boiling Point:220°C at 760 mmHg

Melting Point:300℃

Flash Point:STABILITY

Storage Temperature:Store in a cool, dry place. Store in a tightly closed container.

Stability:Stable under normal temperatures and pressures.

Usage:Antiepileptic; increases levels of GABA in the brain

Biomedical Effects of 1A,25-dihydroxycholecalciferol

1,25-dihydroxycholecalciferol, also called Calcitriol or 1,25-dihydroxyvitamin D3, is the hormonally active form of vitamin D with three hydroxyl groups which was identified

32222-06-3

Many 1A,25-dihydroxycholecalciferol analogs are readily absorbed from the GI tract following oral administration if fat absorption is normal. The presence of bile is required for absorption of ergocalciferol and the extent of GI absorption may be decreased in patients with hepatic, biliary, or GI disease (e.g., Crohn's disease, Whipple's disease, sprue). Because vitamin D is fat soluble, it is incorporated into chylomicrons and absorbed via the lymphatic system; approximately 80% of ingested 1A,25-dihydroxycholecalciferol appears to be absorbed systemically through this mechanism, principally in the small intestine. Although some evidence suggested that intestinal absorption of vitamin D may be decreased in geriatric adults, other evidence did not show clinically important age-related alterations in GI absorption of the vitamin in therapeutic doses. It currently is not known whether aging alters the GI absorption of physiologic amounts of 1A,25-dihydroxycholecalciferol.

After oral administration of calcitriol, there is about a 2-hour lag-time before calcium absorption in the GI tract increases. Maximal hypercalcemic effect occurs in about 10 hours, and the duration of action of calcitriol is 3-5 days.

Time to peak serum concentration: Oral: Approximately 3 to 6 hours.

The primary route of excretion of 1A,25-dihydroxycholecalciferol is the bile; only a small percentage of an administered dose is found in urine.

1A,25-dihydroxycholecalciferol and its metabolites undergo extensive enterohepatic recirculation, and patients who have undergone intestinal bypass surgery or who otherwise have severe shortening or inflammation of the small intestine fail to reabsorb vitamin D sufficiently to maintain normal 1A,25-dihydroxycholecalciferol nutriture.

Stored mainly in liver and other fat depots.

The metabolites of vitamin D analogs are excreted principally in bile and feces. Although some vitamin D that is excreted in bile is reabsorbed in the small intestine, enterohepatic circulation does not appear to be an important mechanism for conservation of the vitamin. Following oral or IV administration of a single dose of radiolabeled calcitriol, 19-41% of radioactivity is recovered in urine within 6-10 days.
It is not known whether this drug is excreted in human milk.

A specific 1,25-dihydroxycholecalciferol-binding protein was detected in high-salt cytosols prepared from human medullary thyroid carcinomas. The binding protein had the same equilibrium dissociation constant and sedimentation coefficient on sucrose gradients as that seen in established 1A,25-dihydroxycholecalciferol target tissues. This protein was not detected in normal thyroid cytosols, which may reflect the low proprotion of C-cells within the gland.

The serum concentrations of total calcium and 1,25-dihydroxyvitamin D3 (I) were measured in women during a menstrual cycle. A rise in the serum I level was observed on day 15 of the cycle without a detectable change in the serum calcium level. The I level on day 15 was double the values observed at days 1 and 8 of the cycle. The peak of I on day 15 was not observed in women ingesting oral contraceptives, suggesting that ovulation or its hormonal control was involved in the peak on day 15. A small but significant fall in the serum calcium concentration occured in the women ingesting oral contraceptives. In view of these findings the serum concentrations of I in women with functioning ovaries must be interpreted in the context of the stage of the menstrual cycle when the blood sample was obtained.

1A,25-dihydroxycholecalciferol application

1A,25-dihydroxycholecalciferol is a form of vitamin D that is used to treat and prevent low levels of calcium in the blood of patients whose kidneys or parathyroid glands (glands in the neck that release natural substances to control the amount of calcium in the blood) are not working normally. It is also called Calcitriol.Low blood levels of calcium may cause bone disease. 1A,25-dihydroxycholecalciferol is in a class of medications called vitamins. It works by helping the body to use more of the calcium found in foods or supplements.

1A,25-dihydroxycholecalciferol

1.Uses

Therapeutic doses of specific vitamin D analogs are used in the treatment of chronic hypocalcemia, hypophosphatemia, rickets, and osteodystrophy associated with various medical conditions including chronic renal failure, familial hypophosphatemia, and hypoparathyroidism (postsurgical or idiopathic, or pseudohypoparathyroidism).

1A,25-dihydroxycholecalciferol is prescribed for:
*Treatment of hypocalcaemia – hypoparathyroidism, osteomalacia (adults), rickets (infants, children), renal osteodystrophy, chronic renal dialysis
*Treatment of osteoporosis
*Prevention of corticosteroid-induced osteoporosis

1A,25-dihydroxycholecalciferol is also sometimes used topically in the treatment of psoriasis, however the evidence to support its efficacy is not well established.The vitamin D analogue calcipotriol is more commonly used for psoriasis. Research on the noncalcemic actions of 1A,25-dihydroxycholecalciferol and other VDR-ligand analogs and their possible therapeutic applications has been reviewed.

1A,25-dihydroxycholecalciferol is also administered orally for the treatment of psoriasis and psoriatic arthritis.


2.Side Effect

The main adverse drug reaction associated with calcitriol therapy is hypercalcaemia – early symptoms include: nausea, vomiting, constipation, anorexia, apathy, headache, thirst, sweating, and/or polyuria. Compared to other vitamin D compounds in clinical use (cholecalciferol, ergocalciferol), 1A,25-dihydroxycholecalciferol has a higher risk of inducing hypercalcaemia. However, such episodes may be shorter and easier to treat due to its relatively short half-life.

3.Storage

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Protect this medication from light. Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

1A,25-dihydroxycholecalciferol

1.Basic information

Product Name: 1alpha,25-Dihydroxycholecalciferol
Synonyms: Vitamin D3, 1a,25-Dihydroxy-; 1alpha,25-Dihydroxyvitamin D3; 1a,25-Dihydroxyvitamin; 1alpha,25-dihydroxycholecalciferol; (5z,7e)-(1s,3r)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol; 1α,25-dihydroxycholecalciferol; Calcitriol; 1,25-dihydroxyvitamin D3
CAS: 32222-06-3 MF: C27H44O3
MW: 416.64
EINECS: 250-963-8
Product Categories: Miscellaneous Biochemicals;Vitamin D3 analogs;API;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File: 32222-06-3.mol
mp:  119-1210C
storage temp:  2-8°C
Stability: Air and Light Sensitive

2.Safety Information

Hazard Codes:  T ,Xn
Risk Statements : 26/27/28-63-36/37/38-20/21/22
Safety Statements:  36/37/39-45-36-26
RIDADR:  UN 2811 6.1/PG
WGK Germany : 3
RTECS:  FZ4645000
F:  8-10-19
HazardClass:  6.1(a)
PackingGroup : I
HS Code:  29061900
Hazardous Substances Data: 32222-06-3

3.Biologically information

Chemical Properties: White Crystalline Powder
Usage :The biologically active form of vitamin D3. Calcium regulator; vitamin (antirachitic); antihyperparathyroid; antineoplastic; antipsoriatic
Biological Activity: Active metabolite of vitamin D 3 that activates the vitamin D receptor (VDR). Displays calcemic actions; stimulates intestinal and renal Ca 2  absorption and regulates bone Ca 2  turnover. Exhibits antitumor activity; inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells.

How dose the medicine of Bezafibrate work?

Bezalip tablets contain the active ingredient bezafibrate, which is a type of medicine known as a fibrate. (Bezafibrate is also available without a brand name, ie as the generic medicine.) Bezafibrate is used to lower the levels of fats (lipids) called cholesterol and triglycerides in the blood.

For the sake of simplicity, there are two sorts of cholesterol; a 'bad' sort called low density lipoprotein (LDL) and a 'good' sort called high density lipoprotein (HDL). LDL is deposited in the arteries and increases the risk of heart disease by clogging and narrowing the arteries (atherosclerosis), while HDL actually protects the arteries against this.

Triglycerides are another type of 'bad fat' that increase the risk of hardened arteries.
Bezafibrate works mainly by stimulating the action of two enzymes that breakdown triglycerides. These are called lipoprotein lipase (found in muscle and fat tissue) and hepatic lipase (found in the liver). Stimulating these enzymes increases the breakdown of triglycerides in the blood. Bezafibrate also decreases the production of triglycerides by the liver. As a result of both these actions, bezafibrate lowers the levels of triglycerides in the blood.

In addition, bezafibrate decreases the production of LDL cholesterol by the liver, which causes the liver cells to take up excess LDL cholesterol from the blood. It also increases levels of HDL cholesterol. The overall effect is lowered levels of "bad fats" and raised levels of "good fats" in the blood.

Fibrates have an important role in the prevention of coronary heart disease. They reduce the risk of excess cholesterol and triglycerides being deposited in the major blood vessels of the heart (atherosclerosis). Atherosclerosis limits the amount of blood and therefore oxygen being carried to the heart muscle. This can cause chest pain (angina) and in severe cases can result in a heart attack (myocardial infarction).

Fibrates are used to lower triglycerides and cholesterol in people who have high levels either due to genetics or as a result of diet and lifestyle. This helps to reduce the risk of atherosclerosis and the problems it can cause.

It is important to continue to follow a cholesterol-lowering diet and exercise regime while taking bezafibrate. Discuss this with your doctor.

How can bezafibrate affect other medicines?

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. These usually improve as your body adjusts to the new medicine, Something has to be pay attention to when you taking this medicine with others medicines at the same time.

It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with bezafibrate. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to make sure that the combination is safe.
There is an increased risk of side effects on the muscles (myopathy) if bezafibrate is taken with other fibrate medicines or statins used for lowering cholesterol, such as simvastatin. Statins should be used with caution in combination with this medicine. Statins should not be used in combination with bezafibrate in people who may be more at risk of muscle side effects, for example people with decreased kidney function, an underactive thyroid gland (hypothyroidism), hormone or electrolyte disturbances, or who drink large amounts of alcohol.

There may also be an increased risk of side effects on the muscles if bezafibrate is taken in combination with colchicine or daptomycin.

If you are prescribed any of the medicines listed above in combination with your bezafibrate, it is important to let your doctor know if you experience any unexplained muscle symptoms, such as pain or tenderness, muscle weakness or muscle cramps.
Bezafibrate increases the anti-blood-clotting effect of anticoagulant medicines such as warfarin, which increases the risk of bleeding in people taking these medicines. For this reason, if you are taking an anticoagulant your doctor may want to check your blood-clotting time (INR) and adjust your anticoagulant dose when you start or stop treatment with bezafibrate, and if your bezafibrate dose is altered.

Bezafibrate may increase the blood sugar lowering effect of antidiabetic medicines, including insulin. This may be unpredictable and the dose of the antidiabetic may need adjusting. People with diabetes should monitor their blood sugar more frequently when first starting this medicine.

There may be an increased risk of a decline in kidney function if this medicine is taken by people who have had an organ transplant and are being treated with ciclosporin. These people should have their kidney function closely monitored.

There may be an increased risk of gallstones if this medicine is taken in combination with ezetimibe.

Colestipol and colestyramine can reduce the absorption of bezafibrate from the gut. If you are taking one of these medicines with bezafibrate, each dose of bezafibrate should be taken either at least two hours before or two hours after it. Ask your pharmacist for further advice.

The manufacturer of this medicine states that it should not be taken in combination with monoamine oxidase inhibitor antidepressants (MAOIs).

Information of Bezafibrate

Bezafibrate (CAS:41859-67-0) is a medicine which is used in hyperlipidaemia.

Bezafibrate

1.Before taking bezafibrateSome medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking bezafibrate it is important that your doctor or pharmacist knows: 
*If you are pregnant, trying for a baby or breast-feeding.
*If you have liver, kidney or gallbladder problems.
*If you have an underactive thyroid.
*If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, such as herbal and complementary medicines.
*If you have ever had an allergic reaction to a medicine.
2.How to take bezafibrateBefore you start this treatment, read the manufacturer's printed information leaflet from inside the pack. The leaflet will give you more information about the brand of bezafibrate that you have been given, and a full list of side-effects which are possible from taking it.

Take bezafibrate exactly as your doctor has told you. Your doctor or pharmacist will tell you how often to take the tablets. This will be once daily if you have been given a prolonged-release tablet, and three times daily if not. Your dose will be on the label of the pack to remind you.

Try to take bezafibrate at the same times of day each day, as this will help you to remember to take your doses. Take the tablets with or immediately after a meal.
If you have been given prolonged-release tablets (Bezalip® Mono and Fibrazate® XL brands), it is important that you swallow the tablets whole - do not chew, crush, or break them.

If you forget to take a dose, take one as soon as you remember unless it is nearly time for your next dose, in which case skip the missed dose. Do not take two doses at the same time to make up for a forgotten dose.

3.How to store bezafibrate*Keep all medicines out of the reach and sight of children.
*Store in a cool, dry place, away from direct heat and light.