Description
DESCRIPTION
Formulation
Every One-Six-Twelve pill comprises:
Vitamin B1 (thiamine)……………..100 mg
Vitamin B6 (pyridoxine) …………. 200 mg
Vitamin B12 (cyanocobalamin)…. 200 mcg
MECHANISM OF ACTION
Nutritional vitamins are natural substances required by the physique in small quantities for numerous metabolic process3es involving progress and bone growth, copy, tissue upkeep and muscular integrity amongst others. Though nutritional vitamins happen naturally in numerous meals, sufficient diet isn’t at all times attainable for all.
CHEMISTRY AND ASSAY
Thiamine was the primary member of the vitamin B advanced to be recognized. Thiamine is a generic time period utilized to all substances possessing vitamin B1 exercise, whatever the anion connected to the molecule.
Thiamine compounds are often readily soluble in water or in alcohol however insoluble in fats solvents. They’re steady in acid resolution and could also be heated with out decomposition however are unstable in impartial or alkaline resolution. At impartial or alkaline pH, splitting happens on the methylene bridge upon heating within the presence of moisture. Splitting of the molecule takes place quantitatively within the presence of bisulfate ions, a response that’s mad use of in getting ready dietary constituents freed from thiamine for bioassay functions (Remington, twentieth version).
Pyridoxine (Vitamin B6) doesn’t denote a single substance however is moderately a collective time period for a gaggle of naturally occurring pyridines which are metabolically and functionally interrelated, particularly, pyridoxine, pyridoxal and pyridoxamine. They’re interconvertible in vivo of their phosphorylated type. There isn’t a info on the relative organic exercise of the three compounds in people, and since pyridoxine is probably the most steady, it in all probability contributes probably the most vitamin exercise to the eating regimen (Remington, twentieth version).
Pyridoxine because the free base has a bitter style and is quickly soluble in water, alcohol or acetone. It crystallizes because the hydrochloride and is ready on this type for business use. Pyridoxine is likely one of the extra steady nutritional vitamins and within the alcohol type withstands heating in acid or alkaline resolution. Beneath most circumstances of processing and storage of meals and pharmaceutical preparations, the vitamin is retained nicely. (Remington, twentieth version).
Cyanocobalamin (B12), was remoted from liver fractions in crystalline type. It’s a advanced water-soluble compound that crystallizes as small crimson needles which have a selected rotation in dilute aqueous resolution of -59 levels Centigrade. (Remington, twentieth version)
Commercially, vitamin B12 is obtained from fermentation by Streptomyces griseus. Vitamin B12 is likely one of the most lively organic elements recognized; its exercise for micro organism is measured by way of millimicrograms. Due to this sensitivity of some micro organism to such low ranges of the vitamin and the truth that meals comprise exceptionally low concentrations of the vitamin, microbiological strategies are extensively used. (Remington, twentieth version)
PHARMACOLOGY
Nutritional vitamins may be divided into two varieties:
The water soluble nutritional vitamins, e.g. Vitamin B advanced, and so forth. are used readily and metabolized to be quickly excreted within the urine. They don’t seem to be saved within the physique. For this reason they’re wanted every day to ensure that the physique to keep up wholesome ranges.
The fats soluble nutritional vitamins, e.g. Nutritional vitamins A,D,E and Okay have an accumulative impact and are saved within the physique which may be probably harmful.
Thiamine
Thiamine (Vitamin B1) is concerned in energy-yielding metabolic techniques, particularly these concerned in carbohydrate metabolism. It’s an important coenzyme that mixes with adenosine triphosphate (ATP) to type a coenzyme, thiamine pyrophosphate (thiamine diphosphate, cocarboxylase), that are concerned in oxidative decarboxylation.
It’s important for carbohydrate metabolism, power launch and wholesome coronary heart, mind, nervous system and muscle perform. It’s utilized within the physique to synthesize neurotransmitters, together with Acetylcholine and gamma-aminobutyric acid (GABA).
Absorption of the same old dietary quantities of thiamine from the gastrointestinal tract happens by Na+ dependent lively transport; at greater concentrations, passive diffusion can be vital.
Thiamine is a vitamin with antioxidant, erythropoietic, cognition-and mood-modulatory, antiatherosclerotic, putative ergogenic, and cleansing properties.
Thiamine performs a key function in intracellular glucose metabolism and it’s thought that thiamine inhibits the impact of glucose and insulin on arterial clean muscle cell proliferation. Inhibition of endothelial cell proliferation can also promote atherosclerosis. Endothelial cells in tradition have been discovered to have a decreased proliferative fee and delayed migration in response to hyperglycemic circumstances. Thiamine has been proven to inhibit this impact of glucose on endothelial cells.
Thiamine can be important in serving to the physique convert carbohydrates and fats into power. It’s wanted for regular progress and growth and helps to keep up correct functioning of the center and the nervous and digestive techniques. Thiamine can’t be saved within the physique; nonetheless, as soon as absorbed, the vitamin is concentrated in muscle tissue.
Indicators of deficiency on this vitamin embrace excessive weak spot (corresponding to beriberi in growing nations with poor eating regimen), melancholy, numbness and tingling within the extremeties, poor reminiscence, headache and disturbed sleep.
Pyridoxine
Vitamin B6 (pyridoxine) is a water-soluble vitamin used within the prophylaxis and remedy of vitamin B6 deficiency and peripheral neuropathy in these receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been discovered to decrease systolic and diastolic blood strain in a small group of topics with important hypertension.
A research confirmed that pyridoxine hydrochloride inhibits ADP- or epinephrine-induced platelet aggregation and lowers complete levels of cholesterol and enhance HDL-cholesterol ranges, once more in a small group of topics. Vitamin B6, within the type of pyridoxal 5′-phosphate, was discovered to guard vascular endothelial cells in tradition from harm by activated platelets. Endothelial harm and dysfunction are essential initiating occasions within the pathogenesis of atherosclerosis. Human research have demonstrated that vitamin B6 deficiency impacts mobile and humoral responses of the immune system. Vitamin B6 deficiency leads to altered lymphocyte differentiation and maturation, diminished delayed-type hypersensitivity (DTH) responses, impaired antibody manufacturing, decreased lymphocyte proliferation and decreased interleukin (IL)-2 manufacturing, amongst different immunologic actions.
Pyridoxine is a precursor to pyridoxal, which features within the metabolism of protein, carbohydrates, and fat; pyridoxal additionally aids within the launch of liver and muscle – saved glycogen and within the synthesis of GABA (inside CNS) and heme. Research have proved that correct quantity of B6 relieves vomiting or nausea in ladies throughout being pregnant. The advisable dietary allowances for vitamin B6 ranges from 1.3 to 2 mg, which additional will depend on numerous elements like age, intercourse and so forth. Its deficiency could lead to pores and skin problems, nausea, anemia, clean tongue, dizziness, convulsions, and kidney stones. Indicators of deficiency embrace irritability and nervousness, flaky pores and skin across the eyes, nostril and mouth, sore tongue.
Along with Vitamin B12, Vitamin B6 aids in protecting homocysteine ranges low. Elevated homocysteine ranges are related to neurodegeneration and coronary heart illness.
Cyanocobalamin
Cyanocobalamin (Vitamin B12) is a water-soluble organometallic compound with a trivalent cobalt ion sure inside a corrin ring. It’s a dietary important for man. Deficiency on this vitamin leads to faulty synthesis of DNA in any cell that makes an attempt chromosomal replication and division.
It contributes in direction of wholesome nervous and cardiovascular techniques, formation of crimson blood cells and bone marrow, manufacturing of genetic materials and metabolism of fat, proteins and carbohydrates.
Low ranges of vitamin B12 are generally discovered amongst dementia sufferers. Deficiency on this vitamin is likewise seen in sufferers with pernicious anemia in whom the specialised abdomen cells required for Vitamin B12 absorption are destroyed by an autoimmune response.
Indicators of deficiency on this vitamin embrace exhaustion, anemia, pallor, pins and needles in palms and toes, irritability, melancholy and shortness of breath on exertion.
Vitamin B12 is required within the means of S-adenosylmethionine (SAM-e) synthesis, the biologically lively type of the important amino acid methionine. Moreover, vitamin B12 supplementation is assumed to lower ranges of the neurotoxin, homocysteine.
It’s a cofactor in two enzymes which are basic in facilitating progress. As methylcobalamin, vitamin B12 is the cofactor of methionine synthase and, as adenosylcobalamin, is the cofactor in methylmalonyl-CoA mutase. Each reactions are concerned in selling the fast progress and proliferation of the cells of the bone marrow.
The event of vitamin B12 deficiency throughout grownup life isn’t often the results of a poor eating regimen; moderately, it displays some defect in gastrointestinal absorption. Classical Addisonian pernicious anemia is attributable to a lack of gastric parietal-cell perform and manufacturing of the glycoprotein gastric intrinsic issue. The parietal cells could fail as a result of the presence of cytotoxic autoantibodies.
Dietary vitamin B12, within the presence of gastric acid and pancreatic proteases, is launched from a salivary binding protein and is instantly sure to intrinsic issue, a glycoprotein.
Any of a lot of intestinal ailments or defects can intervene with the absorption of the intrinsic factor-B12 advanced. The mix of gastric achlorhydria and decreased secretion of intrinsic issue secondary to gastric atrophy or gastric surgical procedure is a standard reason for vitamin B12 deficiency in adults. The requirement for pancreatic proteases to launch vitamin B12 from binding proteins, such that it could then bind to intrinsic issue, explains the malabsorption of the vitamin in pancreatic problems.
As soon as absorbed, vitamin B12 binds to transcobalamin II, a plasma beta-globulin, for transport to tissues. Vitamin B12 sure to transcobalamin II is quickly cleared from plasma and is preferentially distributed to hepatic parenchymal cells.
TOXICOLOGY
Toxicity following acute overdosage is unlikely except an enormous dose has been ingested. Giant overdoses of water soluble nutritional vitamins are readily excreted within the urine therefore, are prone to produce no acute poisonous signs.
PHARMACOKINETICS
Small quantities of thiamine are nicely absorbed from the GI tract after oral doses, however the absorption of doses bigger that about 5 mg is proscribed. It’s extensively distributed to most physique tissues and seems in breast milk. Thiamine isn’t saved to any considerable extent within the physique and extra quantities of the physique’s necessities are excreted within the urine both unchanged or as metabolites.
Pyridoxine is saved primarily within the liver the place there may be oxidation to 4-pyridoxic acid and different inactive metabolites that are excreted within the urine. It crosses the placenta and is distributed into breast milk.
Vitamin B12 substances bind to intrinsic issue, a glycoprotein secreted by the gastric mucosa after which actively absorbed from the gastrointestinal tract. Absorption may also happen by way of passive diffusion whereby little of the vitamin stays in meals as soon as absorbed on this method. Cyanocobalamin is extensively sure to plasma proteins. It’s saved within the liver, excreted in bile and undergoes in depth enterohepatic recycling; a part of a dose is excreted within the urine, most of it throughout the first 8 hours. Nonetheless, urinary excretion solely accounts a small fraction within the discount of the full physique shops acquired by dietary means. Vitamin B12 diffuses throughout the placenta and in addition seems in breast milk.
INDICATIONS
Thiamine is very helpful for individuals who smoke or drink closely, do strenuous bodily work, with a eating regimen excessive in sugar and refined carbohydrates, coronary heart probles, on a progress spurt or below a number of stress.
Polyneuritis (dysfunctioning of the nervous system) or beriberi is the frank illness related to thiamine deficiency in people. Peripheral neuritis is a pathological situation of the nerves of the extremities; often each legs are affected and generally the arms as nicely. The signs embrace lack of sensation, muscle weak spot and paralysis. In beriberi this situation is also related to edema and irregular electrocardiogram patterns. Signs of thiamine deficiency have been noticed amongst continual alcoholics, who use alcohol rather than meals as a supply of power. Deficiency additionally happens in circumstances of continual diarrhea, by which absorption is interfered with over a time period and through being pregnant sophisticated with anorexia and nausea. (Remington, twentieth version)
Heart problems of dietary origin is noticed in continual alcoholics, pregnant ladies, individuals with gastrointestinal problems and people whose eating regimen is poor for different causes. When the prognosis of heart problems attributable to thiamine deficiency has been accurately made, the response to the administration of thiamine is placing. One of many pathognomonic options of the syndrome is an elevated blood stream attributable to arteriolar dilatation inside a number of hours after the administration of thiamine, the cardiac output is diminished and the utilization of oxygen begins to return to regular. If edema is current and attributable to myocardial insufficiency, diuresis outcomes after correct remedy. (Goodman and Gilman’s)
Though there isn’t a doubt that pyridoxine is crucial in human diet, the medical syndrome of easy pyridoxine deficiency is uncommon. However, it could be presumed that a person with a deficiency of different members of the B advanced can also have a deficiency of pyridoxine. Subsequently, pyridoxine ought to be a element of remedy for people affected by a deficiency of different members of the B advanced. On the idea that pyridoxine is crucial in human diet; it’s integrated into many multivitamin preparations for prophylactic use. It has been identified that 30% or extra of alcoholics have biochemically demonstrable deficiency of vitamin B6.
Vitamin B6 is helpful for these expertise morning illness, PMS, insomnia and delicate types of nervousness and melancholy. It’s likewise advisable for girls taking the contraceptive tablet or on long-term HRT since these can result in the depletion of vitamin B6.
Vitamin B6 within the type of pyridoxal phosphate or pyridoxamine phosphate features in carbohydrate, fats and protein metabolism; its main features are most intently associated to protein and amino acid metabolism. (Remington, twentieth version)
Vitamin B12 is indicated for these affected by anemia, fatigue, digestive issues, psychological or nervous issues. Vegans and vegetarians can develop into poor in vitamin B12 since it’s primarily present in animal produce.
Vitamin B12 is crucial for the traditional functioning of all cells, however notably for cells of the bone marrow, the nervous system and the GI tract. It seems to facilitate discount reactions and take part within the switch of methyl teams. Proof exists that vitamin B12 is concerned in protein, carbohydrate and fats metabolism. (Remington, twentieth version)
Vitamin B12 is a requisite for regular blood formation and sure macrocytic anemias reply to its administration. Vitamin B12 deficiency is acknowledged clinically by its impression on each the hematopoietic and the nervous techniques. The sensitivity of the hematopoietic system pertains to its excessive fee of turnover of cells. (Goodman and Gilman’s)
Because of an insufficient provide of vitamin B12, DNA replication turns into extremely irregular. This consequence within the manufacturing of morphologically irregular cells or dying of cells throughout maturation, a phenomenon known as ineffective hematopoiesis.
Vitamin B12 deficiency may end up in irreversible injury to the nervous system. Progressive swelling of myelinated neurons, demyelination and cell dying are seen within the spinal column and cerebral cortex. This causes a variety of neurological indicators and signs, together with paresthesias of the palms and toes, diminutions of vibration and place senses with resultant unsteadiness, decreased deep-tendon reflexes, and, within the later levels, lack of reminiscence, confusion, moodiness and even a lack of central imaginative and prescient.
Because the neurological injury may be dissociated from the adjustments within the hematopoietic system, vitamin B12 deficiency should be thought of as a risk in aged sufferers with dementia and psychiatric problems, even when they don’t seem to be anemic.
DOSAGE AND ADMINISTRATION
One-Six-Twelve Forte could also be taken one to 2 tablets 3 occasions day by day or as prescribed by the doctor.
CONTRAINDICATIONS
One-Six-Twelve Forte shouldn’t be given to sufferers with hypersensitivity to any element within the formulation (could comprise inactive elements that may trigger allergic reactions or different issues).
DRUG INTERACTIONS
One-Six-Twelv Forte shouldn’t be used on sufferers on levodopa monotherapy. Vitamin B6 accelerates peripheral metabolism of levodopa to dopamine, decreasing the supply of dope for conversion to dopamine, and impairing the therapeutic exercise of levodopa. As little as 5 mg pyroxidine day by day can lower the efficacy of levodopa within the remedy of parkinsonism. Therfore, ONE-SIX-TWELVE FORTE pill isn’t advisable for sufferers taking levodopa alone.
ADVERSE EFFECTS
Allergic and idiosyncratic reactions are potential at low ranges.
STORAGE
Retailer at a temperature not exceeding 30oC. Defend from gentle.
KEEP OUT OF REACH OF CHILDREN.
Evaluations
There are not any evaluations but.
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