Actifer

Actifer Uses, Dosage, Side Effects, Food Interaction and all others data.

vitamin C, the water-soluble vitamin, is readily absorbed from the gastrointestinal tract and is widely distributed in the body tissues. It is believed to be involved in biological oxidations and reductions used in cellular respiration. It is essential for the synthesis of collagen and intracellular material. Vitamin C deficiency develops when the dietary intake is inadequate and when increased demand is not fulfilled. Deficiency leads to the development of well defined syndrome known as scurvy, which is characterized by capillary fragility, bleeding (especially from small blood vessels and the gums), anaemia, cartilage and bone lesions and slow healing of wounds.

Ascorbic Acid (vitamin C) is a water-soluble vitamin indicated for the prevention and treatment of scurvy, as ascorbic acid deficiency results in scurvy. Collagenous structures are primarily affected, and lesions develop in bones and blood vessels. Administration of ascorbic acid completely reverses the symptoms of ascorbic acid deficiency.

Folic acid is essential for the production of certain coenzymes in many metabolic systems such as purine and pyrimidine synthesis. It is also essential in the synthesis and maintenance of nucleoprotein in erythropoesis. It also promotes WBC and platelet production in folate-deficiency anaemia.

Folic acid is a water-soluble B-complex vitamin found in foods such as liver, kidney, yeast, and leafy, green vegetables. Also known as folate or Vitamin B9, folic acid is an essential cofactor for enzymes involved in DNA and RNA synthesis. More specifically, folic acid is required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. Folic acid is the precursor of tetrahydrofolic acid, which is involved as a cofactor for transformylation reactions in the biosynthesis of purines and thymidylates of nucleic acids. Impairment of thymidylate synthesis in patients with folic acid deficiency is thought to account for the defective deoxyribonucleic acid (DNA) synthesis that leads to megaloblast formation and megaloblastic and macrocytic anemias. Folic acid is particularly important during phases of rapid cell division, such as infancy, pregnancy, and erythropoiesis, and plays a protective factor in the development of cancer. As humans are unable to synthesize folic acid endogenously, diet and supplementation is necessary to prevent deficiencies. In order to function properly within the body, folic acid must first be reduced by the enzyme dihydrofolate reductase (DHFR) into the cofactors dihydrofolate (DHF) and tetrahydrofolate (THF). This important pathway, which is required for de novo synthesis of nucleic acids and amino acids, is disrupted by anti-metabolite therapies such as Methotrexate as they function as DHFR inhibitors to prevent DNA synthesis in rapidly dividing cells, and therefore prevent the formation of DHF and THF.

In general, folate serum levels below 5 ng/mL indicate folate deficiency, and levels below 2 ng/mL usually result in megaloblastic anemia.

Vitamin-B complex contains the most important members of the vitamin B group in pure form and in therapeutically balanced proportions. The members of the vitamin B group contained in Vitamin-B complex are components of enzyme systems that regulate various stages of carbohydrate, fat and protein metabolism, each of the components playing a specific biological role. Deficiency of B vitamin causes glossitis, stomatitis, cheilosis, polyneuritis, beriberi, pellagra and vascularisation of cornea.

Trade Name Actifer
Generic Ascorbic Acid + Folic Acid + Iron Salts + Vitamin B Complex
Type Capsule
Therapeutic Class
Manufacturer Zain Pharmaceutical
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Actifer
Actifer

Uses

Vitamin C is used for prevention and treatment of scurvy. It may be used for pregnancy, lactation, infection, trauma, burns, cold exposure, following surgery, fever, stress, peptic ulcer, cancer, methaemoglobinaemia and in infants receiving unfortified formulas. It is also prescribed for haematuria, dental caries, pyorrhea, acne, infertility, atherosclerosis, fractures, leg ulcers, hay fever, vascular thrombosis prevention, levodopa toxicity, succinyl-choline toxicity, arsenic toxicity etc. To reduce the risk of stroke in the elderly, long-term supplementation with Vitamin C is essential.

Prophylaxis of megaloblastic anaemia in pregnancy, Supplement for women of child-bearing potential, Folate-deficient megaloblastic anaemia, Prophylaxis of neural tube defect in pregnancy

Each Tablet/ Capsule contains:

  • Thiamine Hydrochloride 5 mg
  • Riboflavin 2 mg
  • Pyridoxine hydrochloride 2 mg
  • Nicotinamide 20 mg

Each 5 ml Syrup contains:

  • Thiamine Hydrochloride 5 mg
  • Riboflavin 2 mg
  • Pyridoxine hydrochloride 2 mg
  • Nicotinamide 20 mg

Each 2 ml Injection contains:

  • Thiamine Hydrochloride 50 mg
  • Riboflavin 4 mg
  • Pyridoxine hydrochloride 10 mg
  • Nicotinamide 100 mg
  • D-Panthenol 5 mg

Vitamin-B complex is used for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi Vitamin-B complex is used for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. These include: Conditions causing depletion, or reduced absorption or bioavailability of essential B-vitamins manifested by glossitis, stomatitis, cheilosis, beriberi

Actifer is also used to associated treatment for these conditions: Common Cold, Deficiency, Vitamin A, Deficiency, Vitamin D, Fever, Flu caused by Influenza, Folate deficiency, Iron Deficiency (ID), Iron Deficiency Anemia (IDA), Oral bacterial infection, Scurvy, Vitamin C Deficiency, Vitamin Deficiency, Nutritional supplementation, Vitamin supplementationAnaemia folate deficiency, Folate deficiency, Iron Deficiency (ID), Iron Deficiency Anemia (IDA), Latent Iron Deficiency, Neural Tube Defects (NTDs), Vitamin Deficiency, Methotrexate toxicity, Nutritional supplementation

How Actifer works

In humans, an exogenous source of ascorbic acid is required for collagen formation and tissue repair by acting as a cofactor in the posttranslational formation of 4-hydroxyproline in -Xaa-Pro-Gly- sequences in collagens and other proteins. Ascorbic acid is reversibly oxidized to dehydroascorbic acid in the body. These two forms of the vitamin are believed to be important in oxidation-reduction reactions. The vitamin is involved in tyrosine metabolism, conversion of folic acid to folinic acid, carbohydrate metabolism, synthesis of lipids and proteins, iron metabolism, resistance to infections, and cellular respiration.

Folic acid, as it is biochemically inactive, is converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase (DHFR). These folic acid congeners are transported across cells by receptor-mediated endocytosis where they are needed to maintain normal erythropoiesis, synthesize purine and thymidylate nucleic acids, interconvert amino acids, methylate tRNA, and generate and use formate. Using vitamin B12 as a cofactor, folic acid can normalize high homocysteine levels by remethylation of homocysteine to methionine via methionine synthetase.

Dosage

Actifer dosage

vitamin C is usually administered orally. When oral administration is not feasible or when malabsorption is suspected, the drug may be administered IM, IV, or subcutaneously. When given parenterally, utilization of the vitamin reportedly is best after IM administration and that is the preferred parenteral route.

For intravenous injection, dilution into a large volume parenteral such as Normal Saline, Water for Injection, or Glucose is recommended to minimize the adverse reactions associated with intravenous injection.

The average protective dose of vitamin C for adults is 70 to 150 mg daily. In the presence of scurvy, doses of 300 mg to 1 g daily are recommended. However, as much as 6 g has been administered parenterally to normal adults without evidence of toxicity.

To enhance wound healing, doses of 300 to 500 mg daily for a week or ten days both preoperatively and postoperatively are generally considered adequate, although considerably larger amounts have been recommended. In the treatment of burns, doses are governed by the extent of tissue injury. For severe burns, daily doses of 1 to 2 g are recommended. In other conditions in which the need for vitamin C is increased, three to five times the daily optimum allowances appear to be adequate.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever the solution and container permit.

Supplement for women of child-bearing potential: 0.4 mg daily.

Folate-deficient megaloblastic anaemia: 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.

Prophylaxis of neural tube defect in pregnancy: 4 or 5 mg daily starting before pregnancy and continued through the 1st trimester.

Prophylaxis of megaloblastic anaemia in pregnancy: 0.2-0.5 mg daily.

Tablet/ capsule:usual recommended dose is 1-2 tablet/capsule 3 times daily or as directed by the physician.

Syrup:2-3 teaspoonful daily or as directed by the physician.

Injection:It is for intramuscular and intravenous administration. Usual recommended dose is 2 ml daily or as directed by the physician. In addition withThiamine, Riboflavin, Nicotinamide, Pyridoxine; injectable dosage from containsD-Panthenol 5 mg.

May be taken with or without food.

Side Effects

Ascorbic acid does not seem to have any important adverse effects at dosages less than 4 mg/day. Larger dose may cause diarrhoea or formation of renal calculi of calcium oxalate in patients with renal impairment. Ingestion of more than 600 mg daily have a diuretic action.

GI disturbances, hypersensitivity reactions; bronchospasm.

Adverse reactions have been reported with specific vitamins and minerals, but generally at levels substantially higher than those in Vitamin-B complex. However, allergic and idiosyncratic reactions are possible at lower levels. Iron, even at the usual recommended level has been associated with gastrointestinal intolerance in some patients.

Toxicity

IPR-MUS LD50 85 mg/kg,IVN-GPG LD50 120 mg/kg, IVN-MUS LD50 239 mg/kg, IVN-RAT LD50 500 mg/kg, IVN-RBT LD50 410 mg/kg

Precaution

Ingestion of megadose (more than 1000 mg daily) of vitamin C during pregnancy has resulted in scurvy in neonates. Vitamin C in mega-doses has been contraindicated for patients with hyperoxaluria. Vitamin C itself is a reactive substance in the redox system and can give rise to false positive reactions in certain analytical tests for glucose, uric acid, creatine and occult blood.

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

Interaction

Potentially hazardous interactions: Ascorbic acid is incompatible in solution with aminophylline, bleomycin, erythromycin, lactobionate, nafcillin, nitrofurantoin sodium, conjugated oestrogen, sodium bicarbonate, sulphafurazole diethanolamine, chloramphenicol sodium succinate, chlorthiazide sodium and hydrocortisone sodium succinate.

Useful interactions: Ascorbic acid increases the apparent half-life of paracetamol and enhances iron absorption from the gastrointestinal tract.

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

As little as 5 mg pyridoxine daily can decrease the efficacy of levodopa in the treatment of parkinsonism. Therefore, Vitamin-B complex is not recommended for patients undergoing such therapy

Volume of Distribution

Tetrahydrofolic acid derivatives are distributed to all body tissues but are stored primarily in the liver.

Elimination Route

70% to 90%

Folic acid is absorbed rapidly from the small intestine, primarily from the proximal portion. Naturally occurring conjugated folates are reduced enzymatically to folic acid in the gastrointestinal tract prior to absorption. Folic acid appears in the plasma approximately 15 to 30 minutes after an oral dose; peak levels are generally reached within 1 hour.

Half Life

16 days (3.4 hours in people who have excess levels of vitamin C)

Elimination Route

After a single oral dose of 100 mcg of folic acid in a limited number of normal adults, only a trace amount of the drug appeared in the urine. An oral dose of 5 mg in 1 study and a dose of 40 mcg/kg of body weight in another study resulted in approximately 50% of the dose appearing in the urine. After a single oral dose of 15 mg, up to 90% of the dose was recovered in the urine. A majority of the metabolic products appeared in the urine after 6 hours; excretion was generally complete within 24 hours. Small amounts of orally administered folic acid have also been recovered in the feces. Folic acid is also excreted in the milk of lactating mothers.

Pregnancy & Breastfeeding use

The drug is safe in normal doses in pregnant women, but a daily intake of 5 gm or more is reported to have caused abortion. The drug may be taken safely during lactation.

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).

It is safe to use Vitamin-B complex in pregnancy and lactation.

Contraindication

Undiagnosed megaloblastic anaemia; pernicious, aplastic or normocytic anaemias.

Vitamin-B complex is contraindicated in patients hypersensitive to any of its components.

Storage Condition

Should be stored in a dry place below 30˚C.

Store at 15-30° C.

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