Therapeutic Class

Erythropoiesis agent

Indications

Treatment of megaloblastic anemia due to folic acid deficiency and in anemias of nutritional origin, pregnancy, infancy, or childhood.

Oral
Folate-deficient megaloblastic anaemia
Adult: 5 mg daily for 4 mth, up to 15 mg daily in malabsorption states. Continued dosing at 5 mg every 1-7 days may be needed in chronic haemolytic states, depending on the diet and rate of haemolysis.
Oral
Prophylaxis of megaloblastic anaemia in pregnancy
Adult: 0.2-0.5 mg daily.
Oral
Prophylaxis of neural tube defect in pregnancy
Adult: 4 or 5 mg daily starting before pregnancy and continued through the 1^st trimester.
Oral
As supplement for women of child-bearing potential
Adult: 0.4 mg daily.

Contraindications

Undiagnosed megaloblastic anaemia; pernicious, aplastic or normocytic anaemias.

Warnings / Precautions

Treatment resistance may occur in patients with depressed haematopoiesis, alcoholism, deficiencies of other vitamins. Neonates.

Not for monotherapy in pernicious anemia and other megaloblastic anemias with B12 deficiency. May obscure pernicious anemia in dosage >0.1mg/day. Decreased B12 serum levels with prolonged therapy.

Adverse Reactions

GI disturbances, hypersensitivity reactions, bronchospasm, Allergic sensitization.

Drug Interactions

Antiepileptics, oral contraceptives, anti-TB drugs, alcohol, aminopterin, methotrexate, pyrimethamine, trimethoprim and sulphonamides may result to decrease in serum folate concentration. Decreases serum phenytoin concentrations.

Antagonizes phenytoin effects. Increased seizures with phenytoin, primidone, and phenobarbital reported. Tetracycline may cause false low serum and red cell folate due to suppression ofLactobacillus casei.

Mechanism of Actions

Acts as cofactor for transformylation reactions in biosynthesis of purines and thymidylates of nucleic acids; acts on megaloblastic bone marrow to produce normoblastic marrow; required for nucleoprotein synthesis and maintenance of normal erythropoiesis.
Onset: Peak effect: Oral: 0.5-1 hr.
Absorption: Rapidly absorbed mainly from the duodenum and jejunum.
Distribution: Extensively bound to plasma protein. Principal site of storage is the liver. It is also concentrated in the CSF and enters the breast milk.
Metabolism: Undergoes conversion in the plasma and liver to the metabolically active 5-methyltetrahydrofolate.
Excretion: Via urine (as unchanged drug and metabolites). Removed by haemodialysis.

Assesment

Assess for alcoholism, chronic infection, and pernicious, megaloblastic, and hemolytic anemias, and for possible drug interactions.

Monitoring

Monitor for allergic/hypersensitivity reactions

Patient Counselling

Advise to seek medical attention if symptoms of allergic/hypersensitivity reaction occur.

Administration

Administration: Oral route.

Storage : 20-25°C (68-77°F).

Pregnancy Category

A: Adequate and well-controlled human studies have failed to demonstrate a risk to the fetus in the first trimester of pregnancy (and there is no evidence of risk in later trimesters

ATC Classification

B03BB01

GenericPedia Classification

• Vitamin B Complex ,
• Vitamins & minerals

Form

Packing (Max Retail Price)

Hyacinth tab