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Iron deficiency is the most common nutritional deficiency globally, leading to many individuals taking iron supplements. This article discusses the oral bioavailability - the proportion of an unchanged drug that enters circulation into the body and has an active effect - of iron supplements.
People may have low iron levels for a number of reasons such as poor absorption, bleeding and reduced intake.
Iron is often taken orally as a first line treatment option in a number of pharmacological forms. The most common form is iron (II) sulphate (also known as ferrous sulphate) and a wide range of other salts including gluconate and carbonyl iron.
Vitamin C (ascorbic acid) may be included to aid better absorption of iron.
When regular iron supplements such as ferrous fumarate are not tolerated or absorbed by individuals, Heme iron polypeptide is used, with a single study highlighting its ability to significantly increase serum iron levels.
Further studies are required to verify if these findings are replicated in a number of different experimental settings.
Oral iron therapies are known to cause a number of adverse side effects including diarrhoea, constipation and abdominal cramping/pain. It has been evidenced that treatment with iron (II) sulphate results in more adverse side effects than iron (III)-hydroxide polymaltose complex or amino acid chelate.
Parenteral iron therapy, administered either intravenously or intramuscularly, is often given as a secondary line treatment when oral therapies have failed or cannot be given for a particular reason. This may include:
There are some circumstances in which parenteral iron therapy cannot be given, such as the first trimester of pregnancy when an unacceptably high risk of harm to the unborn child is present. In general, parenteral therapy is not offered as a first line treatment as a result of its cost and invasive nature. It is preferred clinically for the treatment of certain medical conditions and is the preferred method of administration in some countries for patients who have chronic renal failure.
There are some rare allergic reactions associated with particular supplements.
Iron sucrose has an allergy risk of 1 in 1000, with a recommended maximum dosage of 200mg three times a week to prevent adverse side effects.
More commonly, many individuals who take iron supplements experience a change in their senses, with 1 in 10 patients experiencing an increasingly metallic taste in their mouths and/or when eating. To prevent accidental toxicity or overdose, chelating agents (capable of forming multiple bonds) are included in some iron supplements to remove the toxicity of free iron –the side effects of this action are diarrhoea and possible hematemesis (the vomiting of blood).
Non-heme iron supplements, when taken in conjunction with a number of other supplements, can decrease the efficacy and absorption of both the iron and other pharmacological solutions taken at the same time. As such, it is recommended that supplements taken with drugs such as quinolones, biophosphates and levodopa are all discussed with a family doctor or pharmacist to discuss any possible negative interactions or significant drops in efficacy.
By definition, supplements that are administered intravenously have the highest rates of bioavailability. Medicines that are administered orally generally decrease in bioavailability as a result of incomplete absorption or first-pass metabolism (the process of a drug losing its efficacy before reaching systemic circulation and being able to have an effect on the patient). Many studies often compare oral and intravenous administration of iron therapy without directly considering its oral bioavailability, instead focusing on clinical outcomes and health benefits for patients.
A systematic review of a wide range of studies, published at the beginning of 2015, considered the role of oral iron supplementation in treating anaemia in older people. It found them to raise haemoglobin levels, but without any tangible health benefit.
The two main iron salts forms (ferric and ferrous irons) and common formulations (carbonyl iron, amino-acid chelates) are commonly used in practice. All dietary iron has to be reduced to the ferrous form in order to be active, and is absorbed three times more readily than its ferrous counterpart. The addition of Vitamin C to aid addition has been shown to be effective in increasing the active component of iron supplements. Taking iron supplements on an empty stomach has also been proven to improve their efficacy, with food decreasing absorption by an estimated 40-50%.