Ascorbic Acid Injection - Pharmacological Aspect

Overview:

Ascorbic acid is a nutrient found in foods and supplements. It protects cells and plays an important role in collagen production, a protein that strengthens and supports tissues. Ascorbic acid can be taken orally or by IV (intravenous) injection. It can reach higher levels in the bloodstream through IV than orally. Research shows that IV Ascorbic acid might improve the quality of life and reduce the side effects of cancer. In general, IV administration of Ascorbic acid has had few side effects in clinical trials. However, it can cause serious problems for people with kidney issues, G6PD (glucose-6 phosphate dehydrogenase) deficiency, or hemochromatosis. The Food and Drug Administration approved Ascorbic acid on October 2nd, 2017.

Available Doses and Dosage Forms:

The Ascorbic acid injection contains 25,000 mg (milligram) of vitamin C in a 50 mL (milliliter) bottle (500 mg per mL). It comes as a clear, colorless to pale yellow solution, packaged for use in a pharmacy.

The recommended rates for giving Ascorbic acid injection through an IV are:

• 1.3 mg per minute for babies five months to under 12 months.

• 3.3 mg per minute for children one to under 11 years.

• 33 mg per minute for adults and children 11 years and older.

Ascorbic acid injection for intravenous use comes in:

• One Vial: 25,000 mg in 50 mL (500 mg per mL), with NDC 67157-101-50.

• Twenty-Five Vials: Each vial is 25,000 mg in 50 mL (500 mg per mL), with NDC 67157-101-51.

For Patients:

What Is Scurvy?

Scurvy is an illness caused by a serious vitamin C deficiency. It occurs when a person does not get enough vitamin C in their diet.

How Does Ascorbic Acid Injection Work?

Ascorbic acid injection treats scurvy in people who cannot take the medicine orally. Doctors prescribe it for a short period, no longer than a week. This treatment should be administered by the doctor or under their guidance.

What Is the Dosage of Ascorbic Acid Injection?

• When giving intravenous (IV) injections, mix it in fluid (normal saline, water for injection, or glucose) to reduce side effects.

• The typical daily dose of vitamin C for adults is 70 to 150 mg.

• Higher doses of 300 mg to one gram in a day are recommended for treating scurvy, though up to six grams can be given safely.

• To help with wound healing, 300 to 500 mg daily for a week to ten days before and after surgery is usually enough.

• For severe burns, doses of one to two grams daily are suggested.

• Three to five times the usual daily amount is often sufficient for other conditions requiring extra vitamin C.

How Effective Is Ascorbic Acid Injection?

Ascorbic acid injection treats scurvy (a lack of vitamin C) in people who cannot take the medicine by mouth. It is only used for a short period, up to one week. This injection should be given by the doctor or with their direct supervision.

What Are the Things to Inform the Doctor Before Taking the Ascorbic Acid Injection?

• Please inform the doctor and pharmacist if the person is allergic to Ascorbic acid or any other medicines or ingredients in Ascorbic acid products.

• Let the doctors know about any other medicines, vitamins, supplements, or herbal products the person is taking or plans to take.

• The doctor might need to adjust the medication doses or closely monitor side effects.

• Inform the doctor about having health conditions in the past or present.

• If a person is pregnant, planning to become pregnant, or breastfeeding, let the doctor know about it beforehand.

• If the person gets pregnant while using Ascorbic acid, contact the doctor.

• Let the doctor know if you have a smoking habit since smoking can make Ascorbic acid less effective and might need a higher dose. Discuss this with the doctor or pharmacist if using tobacco.

How Is Ascorbic Acid Injection Administered?

• Take this vitamin orally, either with or without food, usually once to twice daily. Follow the instructions on the package or the doctor’s advice.

• If you are taking extended-release capsules, swallow them whole. Do not crush or chew them; this can release all the medicine at once and increase side effects. Unless the doctor says otherwise, take them with a full glass of water (eight ounces per 240 milliliters).

• For wafers or chewable tablets, chew them well before swallowing. For Lozenges, let them dissolve slowly in the mouth.

• If a person uses vitamin powder, they should mix it well with the recommended amount of liquid or soft food and drink it immediately. Preparation should be avoided. Use a measuring device rather than a regular kitchen spoon for liquid vitamins to get the correct dose.

• The amount needed depends on the person’s health condition and response to the treatment.

• Take the vitamin regularly for better results. Take it at the same time each day for maximum benefits and to avoid missing the dose. If a person has a serious health issue, they should get medical help immediately.

What Are the Side Effects of Ascorbic Acid Injection?

• Kidney issues, like oxalate nephropathy and kidney stones.

• Breakdown of red blood cells (hemolysis) in people with G6PD deficiency.

Other possible side effects of vitamin C:

• Reactions at the injection site, such as pain and swelling.

• Ascorbic acid injection should be given slowly through an IV. Rapid administration of more than 250 mg per minute can cause temporary side effects like lightheadedness, nausea, tiredness, flushing, dizziness, and headache.

Dietary Considerations:

Certain Ascorbic acids contain sodium, so if a person has to cut down on salt, they should avoid the forms containing sodium.

Missed Dose:

If a person needs to remember to take a dose, it should be taken as soon as they remember. If it is time for the next dose, they should skip the missed dose and stick to the regular schedule. They should only take one dose at a time to make up for the missed one since it leads to overdosing.

Overdose:

An overdose of Ascorbic acid can cause symptoms like:

• Nausea.

• Vomiting.

• Diarrhea.

• Facial flushing.

• Rash.

• Headache.

• Tiredness.

• Trouble sleeping.

Storage:

Store the Ascorbic acid vials in the refrigerator at two to eight degrees Celsius (36 to 46 degrees Fahrenheit) and away from light, as the product does not contain preservatives.

For Doctors:

Indication:

• Ascorbic acid injection is used for the short-term (up to one week) treatment of scurvy in adults and children over five months old.

• Ascorbic acid is used in the slow healing of wounds and bones.

• Ascorbic acid makes urine less acidic.

• Ascorbic acid injection is not meant to treat general vitamin C deficiency in the absence of scurvy.

Dose:

• Injectable solutions are available at 250 mg per mL and 500 mg per mL.

• The recommended daily allowance (RDA) for men is 90 mg per day; for women 75 mg per day, and pregnant women 85 mg per day, not to exceed 2,000 mg per day (80 mg if under 18, not to exceed 1,800 mg per day). Nursing women 120 mg per day, not to exceed 2,000 mg per day (115 mg if under 18, not to exceed 1,800 mg per day).

• Oral Treatment: Follow the recommended daily intake. Take 250 mg by mouth four times a day for one week.

• IV Treatment: If oral vitamin C is not an option or is not effective for treating scurvy, an IV dose of 200 mg should be administered daily, and the treatment should not last longer than seven days. If symptoms do not improve, treatment should be continued until either the symptoms are sorted out or until the doctor gives some other alternative option.

Dosing Considerations:

• Ascorbic acid should be used with caution for patients with kidney issues.

• This medication should only be used to treat vitamin C deficiency if the patient is showing symptoms of scurvy.

• It is not used for treating vitamin C deficiency without scurvy symptoms.

What Are the Pharmacological Aspects of Ascorbic Acid Injection?

• Pharmacodynamics: Ascorbic acid is a water-soluble vitamin used to prevent and treat scurvy, a disease caused by vitamin C deficiency.

• Mechanism of Action: The mechanism of action for ascorbic acid has yet to be completely understood. It is difficult to know how it works on scurvy and on what basis it works to treat scurvy. But oral Ascorbic acid helps to boost the body’s vitamin C levels.

• Pharmacokinetics: A study was made on eight healthy adults. A high dose of 1000 mg of Ascorbic acid (five times the usual single dose) was given through an IV over 30 minutes, and the maximum level of Ascorbic acid concentration was introduced in their blood at the end of the 30 minutes.

  • Distribution: Ascorbic acid spreads throughout the body, especially in the liver, white blood cells, platelets, gland tissues, and the eye lens. It also moves into breast milk and can cross the placenta.

  • Elimination: When the body has enough Ascorbic acid, the amount in the blood is roughly the same as the amount the kidneys can handle. Excess ascorbic acid is filtered out through urine, and when there is less Ascorbic acid in the body, only a small amount is excreted in the urine.

  • Metabolism: It is broken into urinary oxalate, which can be oxidized after the formation of dehydroascorbic acid.

  • Excretion: It is excreted by the kidneys in huge amounts only when its concentration in the blood exceeds a specific limit, roughly about 1.4 mg per 100 mL.

Warnings and Precautions:

• Oxalate Nephropathy and Kidney Stones: Taking high doses of vitamin C for a long time can cause serious kidney problems like kidney damage and kidney stone formation. Vitamin C can make the urine more acidic, leading to the buildup of certain types of stones (like cysteine, urate, or oxalate). People with kidney disease, with a history of oxalate stones, and who are older adults may have a higher risk of developing these issues when using vitamin C. Children under two years old are also at risk because their kidneys are not fully developed. It is important to monitor kidney function in these higher-risk patients during treatment. If kidney problems develop, stop using Ascorbic acid injections immediately and treat the condition. Ascorbic acid injection should be used for up to one week.

• Hemolysis in Patients with G6PD Deficiency: In people with glucose-6-phosphate dehydrogenase (G6PD) deficiency, vitamin C can destroy red blood cells (hemolysis). Patients with vitamin C deficiency are at risk for serious bleeding when treated with Ascorbic acid injections, and blood tests should be performed to monitor hemoglobin and blood levels. The dose of Ascorbic acid injection should be lowered. If signs of hemolysis appear, stop the treatment immediately and treat accordingly.

• Lab Test Interference: Vitamin C is known to cause a variety of interferences, especially with lab tests based on oxidation-reduction reactions. This includes blood and urine glucose tests, nitrite, bilirubin, and white blood cell counts. Ideally, these lab tests should be done 24 hours after the last ascorbic acid injection infusion to avoid the chances of getting the wrong result.

Drug Interactions of Ascorbic Acid Injection

• Antibiotics: Vitamin C reduces the effectiveness of antibiotics like Erythromycin, Kanamycin, Streptomycin, Doxycycline, and Lincomycin. It also inactivates Bleomycin in lab settings. If the antibiotic is not working well because of taking an Ascorbic acid injection simultaneously, stop using it.

• Amphetamines & Other Drugs Affected by Urine Acidity: Vitamin C can make urine more acidic, which can lower the levels of Amphetamine in the body by causing it to be excreted faster. If Amphetamines become less effective, stop using Ascorbic acid injection. This acidity can affect other medications that depend on urine pH, like Fluphenazine, by reducing their effectiveness, and hence, regular monitoring is recommended.

• Warfarin: A few reports suggest that vitamin C may interfere with the blood-thinning effects of Warfarin. However, when patients took up to 1000 mg of vitamin C per day for two weeks, no problems were found. However, Warfarin therapy should be monitored continuously while administering Ascorbic acid injection.

• Lab Test Interference: Vitamin C can affect lab tests that depend on oxidation-reduction reactions, including glucose tests, nitrite, bilirubin tests, and white blood cell counts. Because of this, test results may be inaccurate (show false negatives) if done within 24 hours or 24 hours after taking Ascorbic acid injection.

Specific Considerations:

• Pregnancy: Vitamin C has been used safely by pregnant women for many years, with no reported negative effects on development. There are specific dosage guidelines for pregnant women.

• Lactation: There is not enough information on how much vitamin C passes into breast milk after an IV dose, but oral vitamin C intake is present in breast milk as per the study. Taking more than the recommended dose does not affect the vitamin C level in breast milk or the amount the baby gets. The doctor considers the benefits of breastfeeding along with the mother’s need for Ascorbic acid injection and any potential risks to the baby due to it. Always follow the recommended dosage for lactating women when using Ascorbic acid injection.

• Pediatric Use: Ascorbic acid injection can be used short-term (up to one week) to treat scurvy in children five months and older if they cannot take vitamin C orally. The safety usage of Ascorbic acid injection in children is similar to that of adults. Children under two years old may be at higher risk for kidney issues because their kidneys are still developing; hence, Ascorbic acid injection is not recommended for children under five months of age.

• Geriatric Use: As people age, kidney function declines, which may increase the risk of kidney problems from Ascorbic acid injection in the elderly.

• Renal Impairment: Use Ascorbic acid injection cautiously in people with kidney problems or a history of kidney stones. Patients with kidney disease, like those on dialysis or with diabetic kidney issues, may be at higher risk for kidney damage if given high doses of Ascorbic acid injection.