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Ascorbic Acid

Pronunciation

Pronunciation

(a SKOR bik AS id)

Index Terms

  • Ascorbate Sodium
  • Ascorbic Acid/Ascorbate Sodium
  • Vitamin C

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule Extended Release, Oral:

C-Time: 500 mg

Generic: 500 mg

Capsule Extended Release, Oral [preservative free]:

Generic: 500 mg

Crystals, Oral:

Vita-C: (120 g, 480 g) [animal products free, gelatin free, gluten free, lactose free, no artificial color(s), no artificial flavor(s), starch free, sugar free, yeast free]

Granules, Oral:

Generic: (1 g [DSC])

Liquid, Oral:

BProtected Vitamin C: 500 mg/5 mL (236 mL) [contains propylene glycol, saccharin sodium, sodium benzoate; citrus flavor]

Generic: 500 mg/5 mL (473 mL)

Powder, Oral:

Ascocid: (227 g)

Generic: (113 g, 120 g, 480 g)

Powder Effervescent, Oral:

Ascocid-ISO-pH: (150 g) [corn free, rye free, wheat free]

Solution, Injection:

Generic: 500 mg/mL (50 mL)

Solution, Injection [preservative free]:

Ascor L 500: 500 mg/mL (50 mL)

Ascor L NC: 500 mg/mL (50 mL [DSC]) [corn free]

Mega-C/A Plus: 500 mg/mL (50 mL)

Solution, Injection, as sodium ascorbate [preservative free]:

Ortho-CS 250: 250 mg/mL (100 mL) [contains edetate disodium, water, sterile]

Generic: 250 mg/mL (30 mL)

Syrup, Oral:

Generic: 500 mg/5 mL (118 mL, 473 mL [DSC])

Tablet, Oral:

Asco-Tabs-1000: 1000 mg [color free, starch free, sugar free]

Generic: 100 mg, 250 mg, 500 mg, 1000 mg

Tablet, Oral [preservative free]:

Generic: 250 mg, 500 mg

Tablet Chewable, Oral:

Chew-C: 500 mg

Fruit C 500: 500 mg [animal products free, gelatin free, gluten free, kosher certified, lactose free, no artificial color(s), no artificial flavor(s), starch free, sugar free, yeast free]

Fruit C: 100 mg [animal products free, gelatin free, gluten free, lactose free, no artificial color(s), no artificial flavor(s), starch free, sugar free, yeast free]

Fruity C: 250 mg

VitaChew Vit C Citrus Burst: 125 mg

Generic: 100 mg, 250 mg, 500 mg

Tablet Chewable, Oral [preservative free]:

C-500: 500 mg [animal products free, gluten free, soy free, starch free, yeast free]

Generic: 500 mg

Tablet Extended Release, Oral:

Cemill: 500 mg

Cemill SR: 1000 mg

Generic: 500 mg, 1000 mg, 1500 mg

Tablet Extended Release, Oral [preservative free]:

Generic: 1000 mg [DSC]

Wafer, Oral [preservative free]:

Acerola C 500: 500 mg (50 ea) [corn free, no artificial color(s), no artificial flavor(s), wheat free, yeast free; contains acerola (malpighia glabra)]

Brand Names: U.S.

  • Acerola C 500 [OTC]
  • Asco-Tabs-1000 [OTC]
  • Ascocid [OTC]
  • Ascocid-ISO-pH [OTC]
  • Ascor L 500
  • Ascor L NC [DSC]
  • BProtected Vitamin C [OTC]
  • C-500 [OTC]
  • C-Time [OTC]
  • Cemill SR [OTC]
  • Cemill [OTC]
  • Chew-C [OTC]
  • Fruit C 500 [OTC]
  • Fruit C [OTC]
  • Fruity C [OTC]
  • Mega-C/A Plus
  • Ortho-CS 250
  • Vita-C [OTC]
  • VitaChew Vit C Citrus Burst [OTC]

Pharmacologic Category

  • Vitamin, Water Soluble

Pharmacology

Ascorbic acid is an essential water soluble vitamin that acts as a cofactor and antioxidant. Ascorbic acid is an electron donor used for collagen hydroxylation, carnitine biosynthesis, and hormone/amino acid biosynthesis. It is required for connective tissue synthesis as well as iron absorption and storage (IOM, 2000).

Absorption

Oral: Readily absorbed in the intestine; an active process thought to be saturable and dose dependent (30 to 180 mg/day: 70% to 90%; >1,000 mg/day: ≤50%) (IOM, 2000)

Distribution

Pituitary and adrenal glands, leukocytes, eye tissues and humors, and brain; lower concentrations in the plasma and saliva (IOM, 2000)

Metabolism

Reversibly oxidized to dehydroascorbic acid (DHA); both ascorbic acid and DHA are active. Unabsorbed ascorbic acid is degraded in the intestine (IOM, 2000)

Excretion

Urine (with high serum concentrations) (IOM, 2000); there is an individual specific renal threshold for ascorbic acid; when blood levels are high, ascorbic acid is excreted in urine, whereas when the levels are subthreshold (doses up to 80 mg/day) very little if any ascorbic acid is excreted into urine

Onset of Action

Reversal of scurvy symptoms: 2 days to 3 weeks

Half-Life Elimination

10 hours (Schwedhelm 2003). Biological half-life: 8 to 40 days (IOM, 2000)

Protein Binding

25%

Use: Labeled Indications

Ascorbic acid deficiency: Treatment of symptoms of mild deficiency; use in conditions requiring an increased intake (eg, burns, wound healing)

Dietary supplement: As a dietary vitamin C supplement

Scurvy: Prevention and treatment of scurvy

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Recommended daily allowance (RDA) (IOM, 2000): Upper limit of intake should not exceed 2,000 mg daily

Males: 90 mg daily

Females: 75 mg daily

Pregnant females:

19 to 50 years: 85 mg daily; upper limit of intake should not exceed 2,000 mg daily

Lactating females:

19 to 50 years: 120 mg daily; upper limit of intake should not exceed 2,000 mg daily

Adult smoker: Add an additional 35 mg daily

Ascorbic acid deficiency: IM, IV, SubQ: 70 to 150 mg daily is an average protective dose; doses 3 to 5 times the RDA may be adequate for conditions with increased requirements.

Burns: IM, IV, SubQ: 1 to 2 g daily for severe burns; dose may be determined by extent of tissue injury

Wound healing: IM, IV, SubQ: 300 to 500 mg daily for 7 to 10 days pre- and post-operatively; larger doses have also been used

Scurvy:

IM, IV, SubQ: 300 to 1,000 mg daily; dose and duration of therapy should be individualized; doses up to 6 g per day have been administered (per manufacturer).

Oral: 100 to 300 mg daily until body stores are replenished; dose and duration of therapy should be individualized; doses as low as 10 mg may be effective (Hirschmann, 1999; Popovich, 2009; Weinstein, 2001).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Recommended adequate intake (AI) (IOM, 2000):

0 to 6 months: 40 mg daily

7 to 12 months: 50 mg daily

Recommended daily allowance (RDA) (IOM, 2000):

1 to 3 years: 15 mg daily; upper limit of intake should not exceed 400 mg daily

4 to 8 years: 25 mg daily; upper limit of intake should not exceed 650 mg daily

9 to 13 years: 45 mg daily; upper limit of intake should not exceed 1,200 mg daily

14 to 18 years: Upper limit of intake should not exceed 1,800 mg daily

Males: 75 mg daily

Females: 65 mg daily

Pregnant females: 80 mg daily; upper limit of intake should not exceed 1,800 mg daily

Lactating females: 115 mg daily; upper limit of intake should not exceed 1,800 mg daily

Scurvy: Oral: 100 to 300 mg daily until body stores are replenished; dose and duration of therapy should be individualized (Popovich, 2009; Weinstein, 2001)

Dosing: Renal Impairment

Mild to severe impairment: There are no dosage adjustments provided in the manufacturer's labeling. Use large doses with caution with renal disorders or patients prone to recurrent renal calculi; may have increased risk of adverse events (IOM, 2000).

ESRD (requiring hemodialysis):

Adults: IV, Oral: 60 to 100 mg once daily is sufficient to prevent serious ascorbate deficiency due to loss from dialysis; doses >100 mg daily may lead to secondary oxalosis and renal oxalate stone formation (Rolton 1991; ASPEN 2012).

Children: IV, Oral: The KDOQI guidelines for nutrition in children recommend combined dietary and supplement intake should not greatly exceed the age-appropriate dietary reference intake; use caution in providing supplementation (KDOQI 2008).

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer's labeling. Based on the pharmacokinetics of ascorbic acid, a water-soluble vitamin, a dosage adjustment does not seem necessary.

Reconstitution

Prior to IV administration, dilute in a large volume parenteral solution (eg, NS, glucose). Note: Pressure may develop in the vial during storage.

Administration

Oral administration is preferred unless malabsorption is suspected. IM administration is preferred when the parenteral route is required. Oral products may be administered with food.

Injection: For IM (preferred), IV, or SubQ administration. Avoid rapid IV injection; may cause temporary faintness or dizziness.

Dietary Considerations

Some products may contain sodium.

High dietary sources of ascorbic acid are citrus fruit, tomatoes/tomato juice, and potatoes; also found in other fruits, broccoli, cabbage, cauliflower, spinach, and strawberries. Absorption from diet and supplements is similar (IOM, 2000).

Compatibility

Stable in D5NS, D51/4NS, D5W, D10W, LR, NS.

Y-site administration: Incompatible with etomidate, propofol, thiopental.

Compatibility in syringe: Incompatible with cefazolin, doxapram.

Storage

Injection: Store under refrigeration (2°C to 8°C); protect from light. Use within 4 hours of vial entry; discard remaining portion.

Oral: Store at room temperature.

Drug Interactions

Aluminum Hydroxide: Ascorbic Acid may increase the absorption of Aluminum Hydroxide. Consider therapy modification

Amphetamines: Ascorbic Acid may decrease the serum concentration of Amphetamines. Monitor therapy

Bortezomib: Ascorbic Acid may diminish the therapeutic effect of Bortezomib. Management: Patients should avoid taking vitamin C supplements and vitamin C-containing multivitamins during their bortezomib therapy. It is probably unnecessary to advise patients to avoid foods/beverages that contain vitamin C (e.g., citrus fruits, etc.). Consider therapy modification

Copper: May decrease the serum concentration of Ascorbic Acid. Management: To minimize the risk for ascorbic acid degradation, add multivitamin product to TPN solution immediately prior to infusion or administer multivitamin and copper in separate containers. Consider therapy modification

CycloSPORINE (Systemic): Ascorbic Acid may decrease the serum concentration of CycloSPORINE (Systemic). Monitor therapy

Deferoxamine: Ascorbic Acid may enhance the adverse/toxic effect of Deferoxamine. Left ventricular dysfunction is of particular concern. Management: Avoid ascorbic acid doses greater than 200 mg/day. Lower doses may be given to patients without cardiac failure, after one month of regular treatment with deferoxamine alone, ideally soon after setting up the infusion pump. Monitor cardiac function. Consider therapy modification

Estrogen Derivatives: Ascorbic Acid may increase the serum concentration of Estrogen Derivatives. Monitor therapy

Test Interactions

False-negative urinary glucose test; false-negative stool occult blood 48 to 72 hours after ascorbic acid ingestion

Adverse Reactions

1% to 10%: Endocrine & metabolic: Hyperoxaluria (with large doses)

<1% (Limited to important or life-threatening): Dizziness, fatigue, flank pain, headache

Warnings/Precautions

Disease-related concerns:

• Diabetes: Patients with diabetes mellitus should not take excessive doses for extended periods of time.

• Glucose-6-phosphatase dehydrogenase (G6PD) deficiency: Use large doses with caution in patients with G6PD deficiency; may have increased risk of adverse events (IOM, 2000).

• Hemochromatosis: Use large doses with caution in patients with hemochromatosis; may have increased risk of adverse events (IOM, 2000).

• Renal disorders: Use large doses with caution with renal disorders or patients prone to recurrent renal calculi; may have increased risk of adverse events (IOM, 2000).

Dosage form specific issues:

• Aluminum: The parenteral product may contain aluminum; toxic aluminum concentrations may be seen with high doses, prolonged use, or renal dysfunction. Premature neonates are at higher risk due to immature renal function and aluminum intake from other parenteral sources. Parenteral aluminum exposure of >4 to 5 mcg/kg/day is associated with CNS and bone toxicity; tissue loading may occur at lower doses (Federal Register, 2002). See manufacturer’s labeling.

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.

• Injection: Avoid rapid IV injection; may cause temporary faintness or dizziness.

• Sodium: Some products may contain sodium; use with caution in sodium restricted patients.

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted. Maternal plasma concentrations of ascorbic acid decrease as pregnancy progresses due to hemodilution and increased transfer to the fetus. Some pregnant women (eg, smokers) may require supplementation greater than the RDA (IOM, 2000).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience diarrhea, nausea, vomiting, or injection site irritation. Have patient report immediately to prescriber back pain, abdominal pain, or hematuria (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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