Brand name: Aquasol A Parenteral
Drug class: Vitamin A
ATC class: A11CA01
VA class: VT050
CAS number: 11103-57-4

Medically reviewed by Drugs.com on Jan 12, 2024. Written by ASHP.

Introduction

Fat-soluble vitamin.

Uses for Vitamin A

Vitamin A Deficiency

Used to treat and prevent symptoms of vitamin A deficiency such as xerophthalmia and night blindness.

Used as a dietary supplement to prevent vitamin A deficiency in patients with GI diseases (e.g., malabsorption syndromes) and those with abnormal storage and transport of vitamin A (e.g., abetalipoproteinemia, protein deficiency, diabetes mellitus, hyperthyroidism, fever, liver disease, cystic fibrosis with hepatic involvement).

Guidelines from WHO, the United Nations Children's Fund (UNICEF), and the International Vitamin A Consultative Group (IVACG, now the Micronutrient Forum) recommend high-dose vitamin A supplements in the prevention and treatment of severe vitamin A deficiency in certain populations. In developing countries where vitamin A deficiency is a public health problem, periodic supplementation with high-dose vitamin A (50,000–200,000 units, depending on age) has been recommended in certain high-risk populations (i.e., postpartum women, children), with reduced doses recommended for pregnant women. Such high doses of vitamin A generally are not used in the US except in individuals with vitamin A deficiency.

WHO and IVACG consider patients with active xerophthalmia (e.g., night blindness, conjunctival xerosis with Bitot's spots, corneal xerosis, corneal ulceration, keratomalacia) to be in imminent danger of corneal destruction and recommend immediate treatment with high dosages of vitamin A. (See Xerophthalmia under Dosage and Administration.)

Children with severe measles have been found to have low serum concentrations of vitamin A; WHO and AAP recommend that vitamin A supplements be given to all children with acute measles, regardless of their country of residence.

Dietary Requirements

Adequate intake needed to prevent vitamin A deficiency and ocular complications (e.g., xerophthalmia) associated with vitamin A deficiency.

Adequate intake of vitamin A usually can be accomplished through consumption of foodstuffs that contain preformed vitamin A (e.g., liver, dairy products, fish) and provitamin A carotenoids (e.g., darkly colored fruits and vegetables).

Adequate intake (AI) established for infants ≤6 months of age based on observed mean vitamin A intake of infants fed principally human milk; AI for infants 7–12 months of age based on the AI for younger infants and the observed mean vitamin A intake from human milk and from solid food.

The Estimated Average Requirement (EAR) and Recommended Dietary Allowance (RDA) for children 1–18 years of age based on data in adults.

Other Uses

Because of the risk of hypervitaminosis A, some clinicians recommend against the use of vitamin A preparations except in vitamin A deficiency and in appropriate preventive situations.

Related/similar drugs

beta-carotene, Aquasol A

Vitamin A Dosage and Administration

General

• Correct poor dietary habits and consider a multivitamin preparation containing vitamin A in patients with vitamin deficiencies since poor dietary habits often result in concurrent deficiencies.

• Risk of irreversible tissue damage from keratomalacia in patients with severe xerophthalmia; therefore, treat immediately.

• Requirements for vitamin A based on adequate liver stores of vitamin A. Liver storage of vitamin A should be adequate before discontinuing therapy.

Administration

Administer orally or by IM injection.

Do not administer by IV injection.

Oral Administration

Oral administration generally preferred over parenteral therapy.

Oral vitamin A capsules containing high strengths (e.g., 50,000 units) no longer commercially available in the US but may be available from various organizations (e.g., UNICEF, the International Dispensary Association [IDA]) for treatment of deficiencies in developing countries.

IM Administration

Administer by IM injection when oral administration is not feasible (e.g., anorexia, nausea, vomiting, pre- and postoperative conditions) or when malabsorption syndrome is present.

Dosage

Available as retinol, vitamin A palmitate, or vitamin A acetate; dosage expressed in terms of retinol (i.e., as retinol equivalents [RE] or retinol activity equivalents [RAE]) and in USP units or International Units (IU, units). USP units and International Units are equivalent.

One USP vitamin A unit is equivalent to 0.3 mcg of all-trans-retinol; one RE is the specific biologic activity of 1 mcg of all-trans-retinol; one RAE is equal to 1 mcg of all-trans-retinol, 12 mcg of all trans-β-carotene, or 24 mcg of other provitamin A carotenoids.

Dosage expressed in RAE is preferred when calculating and reporting the amount of total vitamin A in mixed foods or assessing the amount of dietary and supplemental vitamin A consumed.

Consider the dietary intake of vitamin A when determining the dosage to avoid toxicity.

Pediatric Patients

Vitamin A Deficiency

Treatment of Deficiency

Oral

Children >8 years of age: Some manufacturers have recommended a dosage of 100,000 units (30,000 RE) daily for 3 days, followed by 50,000 units (15,000 RE) daily for 2 weeks, then 10,000–20,000 units (3000–6000 RE) daily for 2 months.

IM, then Oral

Low-birthweight infants: Manufacturer states dosage not established.

Infants <1 year of age: Initially, 7500–15,000 units IM daily for 10 days, follow with 5000–10,000 units orally daily for 2 months.

Children 1–8 years of age: Initially, 17,500–35,000 units IM daily for 10 days, follow with 5000–10,000 units orally daily for 2 months.

Children >8 years of age: 100,000 units IM daily for 3 days, then 50,000 units IM daily for 2 weeks. Follow with 10,000–20,000 units of vitamin A orally daily for 2 months.

Xerophthalmia

Oral

Infants <6 months of age: Initially, 50,000 units daily for 2 days; repeat with 50,000 units at least 2 weeks later (total of 3 doses).

Children 6–12 months of age: Initially, 100,000 units daily for 2 days, then 100,000 units at least 2 weeks later (total of 3 doses).

Children >12 months of age: Initially, 200,000 units daily for 2 days, then 200,000 units at least 2 weeks later (total of 3 doses).

Prevention of Deficiency

Oral

Children living in underdeveloped countries where vitamin A deficiency resulting in keratomalacia and blindness is common: 50,000–200,000 units every 4–6 months have been given . Consult guidelines from appropriate international organizations (e.g., WHO, IVACG) for additional information.

Children with Measles

Oral or IM

Infants <6 months of age: 50,000 units once daily for 2 days; administer a third dose 2–4 weeks later if clinical manifestations of vitamin deficiency are present.

Children 6–11 months of age: 100,000 units once daily for 2 days; administer a third dose 2–4 weeks later if clinical manifestations of vitamin deficiency are present.

Children ≥12 months of age: 200,000 units once daily for 2 days; administer a third dose 2–4 weeks later if clinical manifestations of vitamin deficiency are present.

Dietary Requirements

Oral

Infants ≤6 months of age: Recommended AI is 400 mcg of RAE (1320 units) daily.

Infants 7–12 months of age: Recommended AI is 500 mcg of RAE (1650 units) daily.

Children 1–3 years of age: RDA is 300 mcg of RAE (1000 units) daily.

Children 4–8 years of age: RDA is 400 mcg of RAE (1320 units) daily.

Children 9–13 years of age: RDA is 600 mcg of RAE (2000 units) daily.

Girls 14–18 years of age: RDA is 700 mcg of RAE (2310 units) daily.

Boys 14–18 years of age: RDA is 900 mcg of RAE (3000 units) daily.

Adults

Vitamin A Deficiency

Treatment of Deficiency

Oral

Some manufacturers have recommended a dosage of 100,000 units (30,000 RE) daily for 3 days, followed by 50,000 units (15,000 RE) daily for 2 weeks, then 10,000–20,000 units (3000–6000 RE) daily for 2 months.

IM, then Oral

100,000 units IM daily for 3 days, follow with 50,000 units IM daily for 2 weeks, then 10,000–20,000 units orally daily for 2 months.

Xerophthalmia

Oral

Initially, 200,000 units daily for 2 days, then 200,000 units at least 2 weeks later (total of 3 doses).

Dietary Requirements

Oral

Women ≥19 years of age: RDA is 700 mcg of RAE (2310 units) daily.

Men ≥19 years of age: RDA is 900 mcg of RAE (3000 units) daily.

Prescribing Limits

Pediatric Patients

Vitamin A Deficiency

Oral

Infants 3–6 months of age: 18,500 units daily as water-miscible vitamin A for 1–3 months can cause hypervitaminosis A. (See Hypervitaminosis A Syndrome under Cautions.)

Adults

Vitamin A Deficiency

Oral

Long-term (6–15 months) administration of large dosages (4000 units/kg daily) can cause hypervitaminosis A. (See Hypervitaminosis A Syndrome under Cautions.)

Special Populations

Women of Childbearing Age

Xerophthalmia

Women of childbearing age with night blindness or Bitot's spots: 5000–10,000 units of oral vitamin A once daily for at least 4 weeks; alternatively, may give ≤25,000 units once weekly. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

High dosages of vitamin A may be required if acute corneal lesions are present since blindness occurs within 24–48 hours in most individuals with such severe symptoms; balance risk of teratogenicity against benefits of treatment (e.g., prevention of blindness). WHO recommends that women of childbearing age with active corneal lesions be treated with the same doses of vitamin A used in other groups for treatment of xerophthalmia.

Pregnant Women

Dietary Requirements

Pregnant women 14–18 years of age: RDA is 750 mcg of RAE (2500 units) daily.

Pregnant women 19–15 years of age: RDA is 770 mcg of RAE (2565 units) daily.

See Fetal/Neonatal Morbidity and Mortality under Cautions.

Xerophthalmia

High dosages of vitamin A may be required if acute corneal lesions are present since blindness occurs within 24–48 hours in most individuals with such severe symptoms; balance risk of teratogenicity against benefits of treatment (e.g., prevention of blindness). WHO recommends that pregnant women with active corneal lesions be treated with the same doses of vitamin A used in other groups for treatment of xerophthalmia.

Lactation

Lactating women 14–18 years of age: RDA is 1200 mcg of RAE (4000 units) daily.

Lactating women 19–50 years of age: RDA is 1300 mcg of RAE (4300 units) daily, respectively.

Cautions for Vitamin A

Contraindications

• IV administration.

• Oral high-dose preparation of vitamin A (no longer commercially available in the US): Malabsorption syndromes.

• Hypervitaminosis A.

• Known sensitivity to vitamin A or any ingredient in the formulations.

• Dosages exceeding RDA contraindicated in women who are or may become pregnant. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm in high dosages (i.e., dosages exceeding the RDA); teratogenicity demonstrated in animals.

Human fetal malformations (e.g., cranial neural crest defects) reported following maternal ingestion of large dosages of vitamin A (≥10,000 units daily) shortly before and during pregnancy.

If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.

Use caution in women of childbearing age; intake of preformed vitamin A (obtained from animal products, fortified foods, and dietary supplement) generally should not exceed the RDA.

Despite risks, dosages exceeding the RDA may be necessary in some women of childbearing age with vitamin A deficiency (e.g., active xerophthalmia, corneal lesions). (See Special Populations under Dosage and Administration.)

Hypervitaminosis A Syndrome

Toxic manifestations from excess vitamin A intake include fatigue, malaise, lethargy, irritability, psychiatric changes mimicking severe depression or schizophrenic disorder, anorexia, abdominal discomfort, nausea and vomiting, mild fever, and excessive sweating. If vitamin A toxicity occurs, withdraw the vitamin and provide symptomatic and supportive treatment.

Sensitivity Reactions

Anaphylactic shock and death have been reported following IV administration. (See Contraindications.)

Allergic reactions and anaphylactoid type reaction have been reported rarely.

General Precautions

Patient Monitoring

Carefully supervise patients receiving prolonged daily dosages >25,000 units.

Specific Populations

Pregnancy

Category X. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Distributed into milk.

Unless the maternal diet is grossly inadequate, infants can usually obtain sufficient vitamin A from nursing; however, the effect of large maternal dosages of vitamin A on nursing infants is not known.

Pediatric Use

Vitamin A is a well-established and effective treatment of deficiency states in the pediatric population.

Polysorbates found in the vitamin A injection have been associated with E-Ferol syndrome (thrombocytopenia, renal dysfunction, hepatomegaly, cholestasis, ascites, hypotension, and metabolic acidosis) in low birth-weight infants.

Common Adverse Effects

Usually nontoxic at therapeutic doses.

Drug Interactions

Specific Drugs and Laboratory Tests

Vitamin A Pharmacokinetics

Absorption

Bioavailability

Readily and completely absorbed from the GI tract.

Water-miscible preparations of retinol or its esters are absorbed more rapidly from the GI tract than oil solutions.

Following oral administration of retinol in an oil solution, peak plasma concentrations of retinol esters are attained in about 4–5 hours.

Following oral administration of water-miscible retinol, peak plasma concentrations of retinol esters are attained in about 3–4 hours.

Higher plasma concentrations are obtained after administration of a water-miscible preparation of vitamin A than after an oil solution.

Onset

Ocular symptoms of vitamin A deficiency usually respond quickly and recovery occurs in a few days.

Special Populations

Absorption is incomplete following administration of large doses and in patients with fat malabsorption, low protein intake, or hepatic or pancreatic disease.

Distribution

Extent

Stored mainly in the liver as retinyl palmitate and small amounts of retinol and retinal. Also stored in the kidneys, lungs, adrenals, retinas, and intraperitoneal fat in lesser amounts as retinyl palmitate. Normal adult body stores of vitamin A are sufficient to meet the body’s requirements for several months to 2 years.

Does not readily cross the placenta; distributed into milk. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Released from the liver bound to a specific α₁-globulin, retinol-binding protein (RBP).

Elimination

Metabolism

Retinol esters are hydrolyzed in the GI lumen by pancreatic enzymes.

Retinol is conjugated with glucuronic acid; the β-glucuronide undergoes enterohepatic circulation and oxidation to retinal and retinoic acid. Retinoic acid undergoes decarboxylation and further conjugation with glucuronic acid.

Retinol is reesterified, mainly to retinyl palmitate.

Elimination Route

Retinoic acid is excreted in feces via biliary elimination. Retinal, retinoic acid, and other water-soluble metabolites are excreted in urine and feces. Generally, unchanged retinol is not excreted in the urine.

Special Populations

In patients with pneumonia or chronic nephritis, unchanged retinol may be excreted in the urine.

Stability

Storage

Oral

Capsules and Tablets

Tight, light-resistant containers.

Parenteral

Injection

2–8°C; do not freeze. Protect from air and light.

Actions

• A fat-soluble vitamin required for human growth and bone development, vision, reproduction, and the integrity of mucosal and epithelial surfaces.

• Retinal combines with the rod pigment, opsin, in the retina to form rhodopsin, necessary for visual dark adaptation.

• Cofactor in various biochemical reactions including mucopolysaccharide synthesis, cholesterol synthesis, and hydroxysteroid metabolism.

Advice to Patients

• Advise women of child-bearing age to limit their intake of dietary sources (e.g., liver) containing high concentrations of vitamin A to avoid possible teratogenic effects. Inform these patients to choose fortified foods that contain vitamin A in the form of beta-carotene (e.g., fruits and vegetables) rather than preformed vitamin A.

• Keep out of reach of children.

• Importance of proper dietary habits, including taking appropriate AI or RDA of vitamin A.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. (See Fetal/Neonatal Morbidity and Mortality under Cautions.) Advise lactating women that their vitamin A requirements increase to ensure adequate concentration of the vitamin in milk.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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