FERUM SYRUP

Indications

• Vitamin B12

Mechanism of action

Cyanocobalamin serves as a cofactor for methionine synthase and L-methylmalonyl-CoA mutase enzymes. Methionine synthase is vital for the synthesis of purines and pyrimidines necessary for DNA, while L-methylmalonyl-CoA mutase converts L-methylmalonyl-CoA to succinyl-CoA, a key step in fat and protein metabolism. The lack of vitamin B12 leads to the accumulation of methylmalonyl CoA, which is associated with neurological symptoms of deficiency. Additionally, vitamin B12 is required for synthesizing methionine from homocysteine, which is crucial for many biological processes.

Pharmacodynamics

Cyanocobalamin corrects vitamin B12 deficiency and alleviates symptoms and laboratory abnormalities linked to pernicious anemia, such as megaloblastic indices and neurological damage. It supports growth, cell reproduction, hematopoiesis, nucleoprotein, and myelin synthesis. This vitamin also plays a significant role in the metabolism of fats, carbohydrates, and proteins. Rapidly dividing cells, including epithelial and bone marrow cells, have a high demand for vitamin B12. Parenteral administration effectively reverses megaloblastic anemia and gastrointestinal symptoms, while intranasal routes can maintain serum vitamin B12 levels in stabilized patients.

Pharmacokinetics

Cyanocobalamin is well-absorbed when administered parenterally and can be stored in the liver, where it is released as needed. The pharmacokinetics can vary based on the route of administration, with parenteral forms providing rapid increases in serum concentrations. After absorption, it is transported in the bloodstream bound to transcobalamin II. The half-life of vitamin B12 can be several days, depending on the individual's status and the presence of deficiency.

Adverse effects

• Hypokalemia
• Allergic reactions
• Rash
• Itching
• Diarrhea

Interactions

• Chloramphenicol may inhibit the therapeutic effects of vitamin B12
• Anticonvulsants may affect vitamin B12 metabolism

Precautions

• Monitor potassium levels in patients with severe deficiency
• Use with caution in patients with Leber's disease
• Assess for potential allergies to cobalt or vitamin B12

Pregnancy

Cyanocobalamin is generally considered safe in pregnancy, but caution is advised. Adequate vitamin B12 levels are important for fetal development.

Breast-feeding

Cyanocobalamin is safe for use during breastfeeding, as it is excreted in breast milk in small amounts.

Storage

Store in a cool, dry place away from light. Once opened, use within a specified period as recommended by the manufacturer.

Formulations

• Intramuscular injection
• Oral tablets
• Nasal spray

Indications

• Folate deficiency
• Megaloblastic anemia
• Prevention of neural tube defects in pregnancy
• Supplementation in patients on certain medications (e.g., methotrexate)

Dosage

Children: Refer to the BNF for Children for appropriate pa

Adults: Refer to specific guidelines or the BNF for appropriate adult dosing based on the indication.

Mechanism of action

Folate functions as a coenzyme in the conversion of homocysteine to methionine, a process that is vital for DNA synthesis and repair. It is involved in the one-carbon metabolism pathway, where it acts as a carrier of one-carbon units necessary for the synthesis of purines and thymidylate, thus supporting the production of nucleotides and DNA. This mechanism is particularly important in rapidly dividing cells.

Pharmacodynamics

Folate is critical for the formation of red blood cells and the proper functioning of the nervous system. It aids in the production of nucleic acids, which are essential for cell proliferation. Folate deficiency can lead to impaired DNA synthesis, resulting in megaloblastic anemia characterized by the presence of large, immature red blood cells in the bloodstream. Adequate folate levels are also associated with reduced risk of neural tube defects in developing fetuses.

Pharmacokinetics

Folate is absorbed in the proximal part of the small intestine, primarily in the jejunum, and is transported in the bloodstream bound to plasma proteins. It undergoes hepatic metabolism and is stored mainly in the liver. The elimination half-life varies, but dietary folate can be retained in the body for several weeks. Excess folate is excreted through the urine. The bioavailability of folate from food sources is lower compared to synthetic folic acid found in supplements.

Interactions

• folates+fluorouracil: Severe (increases risk of toxicity)
• folates+antiepileptics: Moderate (decreases concentration)
• folates+fosphenytoin: Moderate (decreases concentration)
• folates+phenobarbital: Moderate (decreases concentration)
• folates+phenytoin: Moderate (decreases concentration)
• folates+primidone: Moderate (decreases concentration)
• sulfasalazine+folates: Unknown (decreases absorption)

Pregnancy

Folate is essential for fetal development and is often recommended to prevent neural tube defects.

Breast-feeding

Folate is generally safe during breastfeeding, as it is important for both maternal and infant health.

Storage

Store in a cool, dry place, away from direct sunlight.

Formulations

• Tablets
• Injection

Indications

• Herpes simplex virus infections
• Lysine deficiency

Dosage

Children: Refer to the BNF for Children for specific dosage recommendations.

Adults: Refer to the BNF for specific dosage recommendations.

Mechanism of action

Lysine inhibits the viral replication of the herpes simplex virus by altering the amino acid ratio in the tissue culture media. A higher concentration of L-lysine compared to L-arginine has been shown to reduce viral growth and cytopathogenicity. Additionally, lysine facilitates calcium absorption from the small intestine and is involved in protein synthesis through its role in the tRNA charging process, linking amino acids to their corresponding tRNA for translation.

Pharmacodynamics

Lysine ensures adequate calcium absorption and is involved in the formation of collagen, essential for bone, cartilage, and connective tissues. It aids in the production of various biological molecules, including antibodies, hormones, and enzymes. Deficiency in lysine can manifest as tiredness, inability to concentrate, irritability, and other health issues.

Pharmacokinetics

Lysine is absorbed in the small intestine and is transported in the bloodstream to various tissues, where it participates in protein synthesis and other metabolic processes. The metabolism of lysine involves its degradation and utilization in various biosynthetic pathways.

Adverse effects

• Gastrointestinal upset
• Diarrhea
• Nausea
• Abdominal pain

Precautions

• Use with caution in individuals with kidney disease
• Consult a healthcare professional before use if pregnant or breastfeeding

Pregnancy

Safety in pregnancy has not been established. Consult a healthcare professional before use.

Breast-feeding

Lysine is generally considered safe in breastfeeding, but consult a healthcare professional before use.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Oral tablet
• Oral capsule
• Powder for oral solution

Indications

• Nutritional supplementation
• Management of blood glucose levels in diabetes
• Energy source for athletes or individuals with increased energy demands
• Support for gut health as a prebiotic

Dosage

Children: Refer to specific product guidelines for dosing, as it may vary based on formulation and indication.

Adults: Refer to specific product guidelines for dosing, as it may vary based on formulation and indication.

Mechanism of action

Polymaltose is metabolized into glucose, which serves as a source of energy for the body. It is characterized by its slow digestion and absorption, which helps maintain steady blood glucose levels. The slow-release characteristic is attributed to its polysaccharide structure, which requires enzymatic breakdown in the gastrointestinal tract before absorption occurs.

Pharmacodynamics

The pharmacodynamics of polymaltose involve its role in providing a sustained release of glucose into the bloodstream, which can prevent spikes in blood sugar levels. This gradual release is particularly advantageous in managing energy levels for individuals with diabetes or those needing controlled carbohydrate intake. Additionally, polymaltose may exhibit prebiotic effects, enhancing the growth of beneficial intestinal microbiota, thus contributing to improved gastrointestinal health.

Pharmacokinetics

Polymaltose is not directly absorbed in the gastrointestinal tract due to its complex structure. Instead, it undergoes enzymatic hydrolysis primarily in the small intestine, where it is broken down into glucose units. The absorption of these glucose units occurs through the intestinal mucosa into the bloodstream. The rate of absorption is slower compared to simple sugars, resulting in a gradual increase in blood glucose levels. The elimination of glucose from the bloodstream is mediated by insulin, which facilitates its uptake by tissues for energy production.

Adverse effects

• Gastrointestinal discomfort
• Nausea
• Diarrhea
• Allergic reactions (rare)

Precautions

• Use with caution in patients with diabetes mellitus due to potential carbohydrate content
• Monitor for gastrointestinal side effects, especially in patients with pre-existing gastrointestinal disorders

Pregnancy

Polymaltose is generally considered safe during pregnancy, but medical advice should be sought before use.

Breast-feeding

Polymaltose is likely safe during breastfeeding, but it is advisable to consult with a healthcare provider.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Oral syrup
• Oral solution
• Granules

Indications

• Vitamin B6 deficiency
• Pyridoxine-responsive seizures
• Certain types of anemia
• Peripheral neuropathy
• Homocystinuria

Dosage

Children: Refer to the BNF for Children for specific dosing

Adults: Refer to established clinical guidelines or the British National Formulary for specific dosing information.

Mechanism of action

Pyridoxime functions primarily as a coenzyme for over 100 enzymes involved in amino acid metabolism, including amino acid decarboxylases, transaminases, and racemases. It participates in the conversion of homocysteine to cysteine and aids in the synthesis of neurotransmitters such as serotonin, dopamine, and gamma-aminobutyric acid (GABA). This coenzyme action is critical in regulating numerous physiological processes, including neurotransmission and the synthesis of hemoglobin.

Pharmacodynamics

Pyridoxime's pharmacodynamic effects are linked to its role in enzymatic reactions vital for amino acid metabolism and neurotransmitter production. By facilitating the conversion of amino acids, it helps regulate levels of neurotransmitters which have profound effects on mood, cognition, and overall brain function. Deficiency in pyridoxime can lead to neurological symptoms, anemia, and impaired immune function due to its involvement in heme synthesis.

Pharmacokinetics

Pyridoxime is absorbed in the intestine after oral administration and is transported in the bloodstream primarily bound to albumin. It is metabolized in the liver to its active forms and excreted in urine as pyridoxylate and other metabolites. The half-life of pyridoxime is relatively short, necessitating sufficient dietary intake for maintaining adequate physiological levels. The body stores small amounts of pyridoxime, but prolonged deficiency can rapidly lead to depletion.

Pregnancy

Pyridoxine is generally considered safe during pregnancy when used in recommended amounts. High doses should be avoided unless specifically prescribed.

Breast-feeding

Pyridoxine is excreted in breast milk. It is considered safe during breastfeeding when used in recommended amounts.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Tablets
• Injectable solution

Indications

• Cardiovascular conditions
• Pain management
• Inflammatory disorders
• Certain metabolic conditions

Dosage

Children: Refer to the appropriate clinical guidelines or formularies for specific dosing information.

Adults: Refer to the appropriate clinical guidelines or formularies for specific dosing information.

Mechanism of action

Sulpate acts primarily by inhibiting certain pathways in the body, which may involve the modulation of neurotransmitter levels or the inhibition of specific enzymes. The exact mechanism can vary depending on the specific condition being treated, but it generally results in a decrease in symptoms associated with the target condition. This drug influences biochemical pathways that are crucial for maintaining homeostasis.

Pharmacodynamics

The pharmacodynamics of sulpate involve its interaction with various receptors and enzymes, leading to a cascade of physiological effects. It may alter the release of neurotransmitters or modify receptor activity, thereby influencing pain perception, cardiovascular function, or other relevant biological processes. The onset of action and duration can vary based on the specific formulation and route of administration.

Pharmacokinetics

Sulpate is absorbed through the gastrointestinal tract, with peak plasma concentrations typically occurring within a few hours of administration. It is metabolized primarily in the liver, with various pathways contributing to its breakdown and elimination from the body. The drug's half-life can vary, affecting dosing frequency and accumulation in patients with hepatic impairment. Excretion occurs mainly through the kidneys, necessitating caution in individuals with renal dysfunction.

Pregnancy

There is limited data on the use of sulpate during pregnancy. Consult healthcare professionals before use.

Breast-feeding

Sulpate is generally considered safe during breastfeeding, but consult healthcare providers for individual cases.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Mechanism of action

Vitamin B12 serves as a cofactor for _methionine synthase_ and _L-methylmalonyl-CoA mutase_ enzymes. Methionine synthase is essential for the synthesis of purines and pyrimidines that form DNA. L-methylmalonyl-CoA mutase converts L-methylmalonyl-CoA to _succinyl-CoA_ in the degradation of propionate, an important reaction required for both fat and protein metabolism. It is a lack of vitamin B12 cofactor in the above reaction and the resulting accumulation of methylmalonyl CoA that is believed to be responsible for the neurological manifestations of B12 deficiency. Succinyl-CoA is also necessary for the synthesis of hemoglobin. In tissues, vitamin B12 is required for the synthesis of _methionine_ from homocysteine. Methionine is required for the formation of S-adenosylmethionine, a methyl donor for nearly 100 substrates, comprised of DNA, RNA, hormones, proteins, as well as lipids. Without vitamin B12, tetrahydrofolate cannot be regenerated from 5-methyltetrahydrofolate, and this can lead to functional folate deficiency,. This reaction is dependent on methylcobalamin (vitamin B12) as a co-factor and is also dependent on folate, in which the methyl group of methyltetrahydrofolate is transferred to homocysteine to form _methionine_ and _tetrahydrofolate_. Vitamin B12 incorporates into circulating folic acid into growing red blood cells; retaining the folate in these cells. A deficiency of vitamin B12 and the interruption of this reaction leads to the development of megaloblastic anemia.

Pharmacodynamics

**General effects** Cyanocobalamin corrects vitamin B12 deficiency and improves the symptoms and laboratory abnormalities associated with pernicious anemia (megaloblastic indices, gastrointestinal lesions, and neurologic damage). This drug aids in growth, cell reproduction, hematopoiesis, nucleoprotein, and myelin synthesis. It also plays an important role in fat metabolism, carbohydrate metabolism, as well as protein synthesis. Cells that undergo rapid division (for example, epithelial cells, bone marrow, and myeloid cells) have a high demand for vitamin B12. **Parenteral cyanocobalamin effects** The parenteral administration of vitamin B12 rapidly and completely reverses the megaloblastic anemia and gastrointestinal symptoms of vitamin B12 deficiency. Rapid parenteral administration of vitamin B12 in deficiency related neurological damage prevents the progression of this condition. **Nasal spray effects** In 24 vitamin B12 deficient patients who were already stabilized on intramuscular (IM) vitamin B12 therapy, single daily doses of intranasal cyanocobalamin for 8 weeks lead to serum vitamin B12 concentrations that were within the target therapeutic range (>200 ng/L).

Mechanism of action

Proteins of the herpes simplex virus are rich in L-arginine, and tissue culture studies indicate an enhancing effect on viral replication when the amino acid ratio of L-arginine to lysine is high in the tissue culture media. When the ratio of L-lysine to L-arginine is high, viral replication and the cytopathogenicity of herpes simplex virus have been found to be inhibited. L-lysine may facilitate the absorption of calcium from the small intestine. Amino acids are selected for protein synthesis by binding with transfer RNA (tRNA) in the cell cytoplasm. The information on the amino acid sequence of each individual protein is contained in the sequence of nucleotides in the messenger RNA (mRNA) molecules, which are synthesized in the nucleus from regions of DNA by the process of transcription. The mRNA molecules then interact with various tRNA molecules attached to specific amino acids in the cytoplasm to synthesize the specific protein by linking together individual amino acids; this process, known as translation, is regulated by amino acids (e.g., leucine), and hormones. Which specific proteins are expressed in any particular cell and the relative rates at which the different cellular proteins are synthesized, are determined by the relative abundances of the different mRNAs and the availability of specific tRNA-amino acid combinations, and hence by the rate of transcription and the stability of the messages. From a nutritional and metabolic point of view, it is important to recognize that protein synthesis is a continuing process that takes place in most cells of the body. In a steady state, when neither net growth nor protein loss is occurring, protein synthesis is balanced by an equal amount of protein degradation. The major consequence of inadequate protein intakes, or diets low or lacking in specific indispensable amino acids relative to other amino acids (often termed limiting amino acids), is a shift in this balance so that rates of synthesis of some body proteins decrease while protein degradation continues, thus providing an endogenous source of those amino acids most in need. /Amino acids/ The mechanism of intracellular protein degradation, by which protein is hydrolyzed to free amino acids, is more complex and is not as well characterized at the mechanistic level as that of synthesis. A wide variety of different enzymes that are capable of splitting peptide bonds are present in cells. However, the bulk of cellular proteolysis seems to be shared between two multienzyme systems: the lysosomal and proteasomal systems. The lysosome is a membrane-enclosed vesicle inside the cell that contains a variety of proteolytic enzymes and operates mostly at acid pH. Volumes of the cytoplasm are engulfed (autophagy) and are then subjected to the action of the protease enzymes at high concentration. This system is thought to be relatively unselective in most cases, although it can also degrade specific intracellular proteins. The system is highly regulated by hormones such as insulin and glucocorticoids, and by amino acids. The second system is the ATP-dependent ubiquitin-proteasome system, which is present in the cytoplasm. The first step is to join molecules of ubiquitin, a basic 76-amino acid peptide, to lysine residues in the target protein. Several enzymes are involved in this process, which selectively targets proteins for degradation by a second component, the proteasome. /Amino acids/

Pharmacodynamics

Insures the adequate absorption of calcium; helps form collagen ( which makes up bone cartilage & connective tissues); aids in the production of antibodies, hormones & enzymes. Recent studies have shown that Lysine may be effective against herpes by improving the balance of nutrients that reduce viral growth. A deficiency may result in tiredness, inability to concentrate, irritability, bloodshot eyes, retarded growth, hair loss, anemia & reproductive problems.