Description
DESCRIPTION
Formulation
Each One-Six-Twelve tablet contains:
Vitamin B1 (thiamine)…………..100 mg
Vitamin B6 (pyridoxine) …………. 5 mg
Vitamin B12 (cyanocobalamin)….50 mcg
PHARMACOLOGY
Thiamine
Thiamine is an essential coenzyme that combines with adenosine triphosphate (ATP) to form a coenzyme, thiamine pyrophosphate (thiamine diphosphate, cocarboxylase), which is necessary for carbohydrate metabolism.
Thiamine is a vitamin with antioxidant, erythropoietic, cognition-and mood-modulatory, antiatherosclerotic, putative ergogenic, and detoxification properties. Thiamine has been found to protect against lead-induced lipid peroxidation in rat liver and kidney. Thiamine deficiency results in selective neuronal death in animal models. The neuronal death is associated with increased free radical production, suggesting that oxidative stress may play an important early role in brain damage associated with thiamine deficiency.
Thiamine plays a key role in intracellular glucose metabolism and it is thought that thiamine inhibits the effect of glucose and insulin on arterial smooth muscle cell proliferation. Inhibition of endothelial cell proliferation may also promote atherosclerosis. Endothelial cells in culture have been found to have a decreased proliferative rate and delayed migration in response to hyperglycemic conditions. Thiamine has been shown to inhibit this effect of glucose on endothelial cells.
Thiamine is also essential in helping the body convert carbohydrates and fat into energy. It is needed for normal growth and development and helps to maintain proper functioning of the heart and the nervous and digestive systems. Thiamine cannot be stored in the body; however, once absorbed, the vitamin is concentrated in muscle tissue.
Pyridoxine
Vitamin B6 (pyridoxine) is a water-soluble vitamin used in the prophylaxis and treatment of vitamin B6 deficiency and peripheral neuropathy in those receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been found to lower systolic and diastolic blood pressure in a small group of subjects with essential hypertension.
A study showed that pyridoxine hydrochloride inhibits ADP- or epinephrine-induced platelet aggregation and lowers total cholesterol levels and increase HDL-cholesterol levels, again in a small group of subjects. Vitamin B6, in the form of pyridoxal 5′-phosphate, was found to protect vascular endothelial cells in culture from injury by activated platelets. Endothelial injury and dysfunction are critical initiating events in the pathogenesis of atherosclerosis. Human studies have demonstrated that vitamin B6 deficiency affects cellular and humoral responses of the immune system. Vitamin B6 deficiency results in altered lymphocyte differentiation and maturation, reduced delayed-type hypersensitivity (DTH) responses, impaired antibody production, decreased lymphocyte proliferation and decreased interleukin (IL)-2 production, among other immunologic activities.
Pyridoxine is a precursor to pyridoxal, which functions in the metabolism of protein, carbohydrates, and fats; pyridoxal also aids in the release of liver and muscle – stored glycogen and in the synthesis of GABA (within CNS) and heme. Studies have proved that proper amount of B6 relieves vomiting or nausea in women during pregnancy. The recommended dietary allowances for vitamin B6 ranges from 1.3 to 2 mg, which further depends on various factors like age, sex etc. Its deficiency may result in skin disorders, nausea, anemia, smooth tongue, dizziness, convulsions, and kidney stones.
Cyanocobalamin
Cyanocobalamin (Vitamin B12) is a water-soluble organometallic compound with a trivalent cobalt ion bound inside a corrin ring. It is needed for nerve cells and red blood cells, and to make DNA. Vitamin B12 deficiency is the cause of several forms of anemia.
Vitamin B12 is used in the body in two forms: methylcobalamin and 5-deoxyadenosyl cobalamin. The enzyme methionine synthase requires methylcobalamin as a cofactor to convert the amino acid homocysteine into methionine. Methionine in turn is required for DNA methylation. 5-Deoxyadenosyl cobalamin is a cofactor needed by the enzyme that converts L-methylmalonyl-CoA to succinyl-CoA. This conversion is an important step in the extraction of energy from proteins and fats. Furthermore, succinyl CoA is necessary for the production of hemoglobin, the substances that carries oxygen in red blood cells.
PHARMACOKINETICS
Small amounts of thiamine are well absorbed from the GI tract after oral doses, but the absorption of doses larger that about 5 mg is limited. It is widely distributed to most body tissues and appears in breast milk. Thiamine is not stored to any appreciable extent in the body and excess amounts of the body’s requirements are excreted in the urine either unchanged or as metabolites.
Pyridoxine is stored mainly in the liver where there is oxidation to 4-pyridoxic acid and other inactive metabolites which are excreted in the urine. It crosses the placenta and is distributed into breast milk.
Vitamin B12 substances bind to intrinsic factor, a glycoprotein secreted by the gastric mucosa and then actively absorbed from the gastrointestinal tract. Absorption can also occur by means of passive diffusion wherein little of the vitamin remains in food once absorbed in this manner. Cyanocobalamin is extensively bound to plasma proteins. It is stored in the liver, excreted in bile and undergoes extensive enterohepatic recycling; part of a dose is excreted in the urine, most of it within the first 8 hours. However, urinary excretion only accounts a small fraction in the reduction of the total body stores acquired by dietary means. Vitamin B12 diffuses across the placenta and also appears in breast milk.
INDICATIONS
One-Six-Twelve is a combination of B vitamins used in the prevention or treatment of deficiencies on the relevant vitamins that may be attributed to poor diet, certain illnesses, alcoholism, or during pregnancy. It can also be used to treat patients with increased homocysteine levels in the blood.
DOSAGE AND ADMINISTRATION
One-Six-Twelve may be taken with meals to reduce GI discomfort. It may be administered 1 tablet once daily or as directed.
CONTRAINDICATIONS
One-Six-Twelve should not be given to patients with hypersensitivity to any component in the formulation (may contain inactive ingredients that can cause allergic reactions or other problems).
ADVERSE EFFECTS
Most frequently reported adverse effects with One-Six-Twelve include abdominal discomfort, abdominal infection, black stools, constipation, nausea, vomiting, dizziness, diarrhea, redness of skin and itching. In very rare cases, one could experience very severe effects which include allergic reactions, itching and rashes and the development of kidney stones.
DRUG INTERACTIONS
One-Six-Twelve should not be used on patients on levodopa monotherapy. Vitamin B6 accelerates peripheral metabolism of levodopa to dopamine, reducing the availability of dope for conversion to dopamine, and impairing the therapeutic activity of levodopa. As
PREGNANCY AND LACTATION
Adequate and well-controlled studies have failed to demonstrate a risk to the fetus in the first trimester of pregnancy.
STORAGE
Store at a temperature not exceeding 30oC. Protect from light.
KEEP OUT OF REACH OF CHILDREN.
REFERENCES
S.Sweetman. Martindale: The Complete Drug Reference 36th edition. 2009
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