NABIL

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

Dosage

Children: Refer to the specific drug formulation for pediatric dosing guidelines.

Adults: Refer to the specific drug formulation for dosing guidelines.

Mechanism of action

The mechanism of action of hydrochloride salts varies depending on the active drug they are associated with. Generally, these salts improve the pharmacokinetic properties of the parent drug, aiding in its absorption through the gastrointestinal tract and enhancing its therapeutic effects.

Pharmacodynamics

The pharmacodynamics of hydrochloride salts also depend on the specific active ingredient. Typically, hydrochloride formulations are designed to provide immediate or extended release of the active compound, affecting its therapeutic efficacy and duration of action. The pharmacodynamic profile will be influenced by the drug's target receptors and its subsequent biological effects.

Pharmacokinetics

The pharmacokinetics of hydrochloride salts include absorption, distribution, metabolism, and excretion characteristics that can differ based on the specific drug. Generally, hydrochloride salts are well absorbed from the gastrointestinal tract. Distribution can vary widely, as can metabolism, which is often hepatic. Excretion is primarily renal, with the rate dependent on the active ingredient's characteristics.

Contra-indications

• Hypersensitivity to hydrochloride or any of its components
• Severe renal impairment
• Acidosis

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Hypokalemia
• Dizziness
• Headache
• Fatigue

Interactions

• May enhance the toxicity of other drugs that cause electrolyte imbalances
• May interact with diuretics, leading to increased risk of hypokalemia
• Concurrent use with other CNS depressants may enhance sedation

Precautions

• Use with caution in patients with hepatic impairment
• Monitor electrolytes regularly during prolonged therapy
• Caution in patients with a history of gastrointestinal disorders

Pregnancy

Hydrochloride should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Consult healthcare providers for specific guidance.

Breast-feeding

Caution is advised when using hydrochloride during breastfeeding, as it may be excreted in breast milk. Consult healthcare providers for recommendations.

Storage

Store at room temperature, away from moisture and light. Keep out of reach of children.

Formulations

• Tablets
• Solutions
• Injectable forms

Indications

• Nutritional supplementation
• Support in metabolic disorders
• Energy source for children and adults with increased energy requirements
• Adjunctive therapy in recovery from illness or surgery

Dosage

Children: Refer to specific product guidelines for pediatric dosing, as individual needs may vary.

Adults: Refer to specific product guidelines for dosing, as polmaltose formulations may vary.

Mechanism of action

Polmaltose serves as a source of glucose, which is metabolized through glycolysis to produce ATP. The digestion of polmaltose begins in the mouth with salivary amylase and continues in the small intestine where it is broken down into glucose and other monosaccharides by various enzymes, including maltase and isomaltase. The resultant glucose is then absorbed into the bloodstream, providing energy for cellular functions.

Pharmacodynamics

Polmaltose provides energy through its carbohydrate content, which is gradually released into the bloodstream as glucose. This slow release helps to maintain stable blood glucose levels and can be particularly beneficial in managing energy levels in patients with specific metabolic conditions or those recovering from illness. Its osmotic properties can also help in maintaining hydration status when consumed with adequate fluids.

Pharmacokinetics

Polmaltose is absorbed primarily in the small intestine. The rate of absorption can vary based on the formulation and presence of other nutrients. Peak blood glucose levels typically occur within 30 to 60 minutes after ingestion, depending on the individual’s metabolic rate and the presence of other foods. The elimination half-life of glucose is short, as it is rapidly utilized by the body for energy or stored as glycogen in the liver and muscles.

Adverse effects

• Gastrointestinal discomfort
• Nausea
• Diarrhea
• Abdominal pain

Precautions

• Use with caution in patients with diabetes due to potential effects on blood glucose levels
• Monitor for gastrointestinal side effects in sensitive individuals

Pregnancy

No adequate and well-controlled studies have been conducted in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether polmaltose is excreted in human milk. Exercise caution when administering to a nursing mother.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral liquid
• Oral suspension