Gave Baby Too Much Vitamin D

Gave Baby Too Much Vitamin D

Vitamin D Supplementation and Risk of Toxicity in Pediatrics: A Review of Current Literature

Maria G. Vogiatzi,

1Weill Cornell Medical College (M.G.V.), New York, New York 10065;

*Address all correspondence and requests for reprints to: Maria Vogiatzi, MD, Weill Cornell Medical College, Pediatric Endocrinology, Box 103, 525 East 68th Street, New York, NY 10065.

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Elka Jacobson-Dickman,

2SUNY Downstate Medical Center (E.J.-D.), Brooklyn, New York 11203;

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Mark D. DeBoer,

3University of Virginia Health System (M.D.D.), Charlottesville, Virginia 22908

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for the Drugs, and Therapeutics Committee of The Pediatric Endocrine Society

for the Drugs, and Therapeutics Committee of The Pediatric Endocrine Society

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Received:

30 September 2013

Accepted:

13 January 2014

Context:

Although vitamin D toxicity is rare in children, increased use of vitamin D formulations, re-examination of optimal vitamin D levels, and use of higher doses lend potential for an increased incidence of vitamin D toxicity.

Evidence Acquisition:

A PubMed search was conducted through May 2013 for cases of vitamin D intoxication and vitamin D trials in pediatrics. Safety data were collected and reviewed.

Evidence Synthesis:

A small number of pediatric studies tested vitamin D doses at or above the currently recommended upper tolerable intake. In children and adolescents, vitamin D excess was rare and usually asymptomatic. Recent cases of intoxication relate to errors in manufacturing, formulation, or prescription; involve high total intake in the range of 240 000 to 4 500 000 IU; and present with severe hypercalcemia, hypercalciuria, or nephrocalcinosis. However, mild hypercalcemia and hypervitaminosis using currently recommended doses have been reported in infants with rickets.

Conclusions:

Although rare, cases of vitamin D intoxication that present with dramatic life-threatening symptoms still occur in children. Moreover, recent studies in infants raise a potential need for monitoring vitamin D levels when doses at or above the currently recommended upper range are used. Further studies are needed to clarify these findings. The Drugs and Therapeutics Committee of the Pediatric Endocrine Society suggests obtaining serum 25-hydroxyvitamin D levels in infants and children who receive long-term vitamin D supplementation at or above the upper level intake that is currently recommended.

Over the past decade, there has been increased focus on the benefits of vitamin D on bone health and, potentially, other disease states (1–3). Re-examination of optimal serum levels and multiple reports regarding high rates of vitamin D insufficiency and deficiency resulted in revised recommendations for minimum vitamin D intake and new guidelines for treatment with high vitamin D doses (4–13). In light of a growing body of research, recent reports of vitamin D intoxication (14–36) and increased use of vitamin D supplementation, the Drugs and Therapeutics committee of the Pediatric Endocrine Society (PES) undertook a systematic review of the safety of currently recommended high vitamin D doses as well as reported cases of intoxications in pediatrics. Herein, we present these outcomes and describe changes in vitamin D metabolism during intoxication, causes and symptoms of toxicity, and current management. Finally, we propose recommendations for the monitoring of children who receive vitamin D supplementation and those with evidence or suspicion of intoxication.

Search Strategy

We performed a PubMed search through May 2013 of publications in English. We searched for vitamin D trials in pediatrics. Publications that involved administration of high vitamin D doses were reviewed, and information on vitamin D excess and toxicity (ie, hypercalcemia, hypercalciuria) was gathered. A similar PubMed search was performed for cases of vitamin D intoxication in both adults and pediatrics. All reported cases were reviewed, and data on the causes, symptoms, biochemical abnormalities, and treatment were summarized for this report. The following terms were used for the search: "vitamin D excess," "vitamin D intoxication," "hypervitaminosis," "vitamin D trial and child," "vitamin D and hypercalcemia," "vitamin D and hypercalciuria," "calcitriol and intoxication," and "calcitriol and hypercalcemia."

Vitamin D Metabolism and Pathophysiology During Vitamin D Intoxication

Vitamin D is available in two forms: ergocalciferol or vitamin D2 and cholecalciferol or vitamin D3. Vitamin D2 and D3 are found as dietary supplements (Table 1) and in various food items naturally or after fortification. Vitamin D3 is also generated from endogenous 7-dehydrocholesterol via sun exposure (1, 3) (Figure 1).

Figure 1.

Diagram showing the main steps of vitamin D synthesis and metabolism. Cholecalciferol or vitamin D3 is produced from 7-dehydrocholesterol in the skin by exposure to sunlight. Vitamin D3 formed in this fashion as well as vitamin D3 and D2 taken from dietary sources or commercially available supplements circulate in the bloodstream bound to the DBP. They are converted to 25OHD in the liver in a constitutive process, which is largely dependent on substrate availability. 25OHD is further hydroxylated in the kidney to the active form 1,25(OH)2D in a tightly regulated process. The primary regulatory pathways that control the production of 1,25(OH)2D and activity of CYP27B1, which catalyzes the conversion of 25OHD to 1,25(OH)2D, are depicted here (dotted arrows). Specifically, hypercalcemia inhibits 1,25(OH)2D synthesis, whereas hypocalcemia stimulates its production primarily due to an increase in PTH secretion. Hypophosphatemia and PTH up-regulate CYP27B1 and increase renal production of 1,25(OH)2D, whereas FGF-23 does the opposite. 1,25(OH)2D regulates its own synthesis by down-regulating CYP27B1 activity and suppressing PTH secretion. 1,25(OH)2D, the active vitamin D form, binds to the VDR to increase intestinal calcium absorption and exert the other vitamin D-related actions. Finally, 1,25(OH)2D increases CYP24A1 activity to catabolize 25OHD and 1,25(OH)2D to water-soluble products that are excreted in the bile. The enzymes involved in each step, all cytochrome P450s (CYP), are shown in red.

Diagram showing the main steps of vitamin D synthesis and metabolism. Cholecalciferol or vitamin D3 is produced from 7-dehydrocholesterol in the skin by exposure to sunlight. Vitamin D3 formed in this fashion as well as vitamin D3 and D2 taken from dietary sources or commercially available supplements circulate in the bloodstream bound to the DBP. They are converted to 25OHD in the liver in a constitutive process, which is largely dependent on substrate availability. 25OHD is further hydroxylated in the kidney to the active form 1,25(OH)2D in a tightly regulated process. The primary regulatory pathways that control the production of 1,25(OH)2D and activity of CYP27B1, which catalyzes the conversion of 25OHD to 1,25(OH)2D, are depicted here (dotted arrows). Specifically, hypercalcemia inhibits 1,25(OH)2D synthesis, whereas hypocalcemia stimulates its production primarily due to an increase in PTH secretion. Hypophosphatemia and PTH up-regulate CYP27B1 and increase renal production of 1,25(OH)2D, whereas FGF-23 does the opposite. 1,25(OH)2D regulates its own synthesis by down-regulating CYP27B1 activity and suppressing PTH secretion. 1,25(OH)2D, the active vitamin D form, binds to the VDR to increase intestinal calcium absorption and exert the other vitamin D-related actions. Finally, 1,25(OH)2D increases CYP24A1 activity to catabolize 25OHD and 1,25(OH)2D to water-soluble products that are excreted in the bile. The enzymes involved in each step, all cytochrome P450s (CYP), are shown in red.

Figure 1.

Diagram showing the main steps of vitamin D synthesis and metabolism. Cholecalciferol or vitamin D3 is produced from 7-dehydrocholesterol in the skin by exposure to sunlight. Vitamin D3 formed in this fashion as well as vitamin D3 and D2 taken from dietary sources or commercially available supplements circulate in the bloodstream bound to the DBP. They are converted to 25OHD in the liver in a constitutive process, which is largely dependent on substrate availability. 25OHD is further hydroxylated in the kidney to the active form 1,25(OH)2D in a tightly regulated process. The primary regulatory pathways that control the production of 1,25(OH)2D and activity of CYP27B1, which catalyzes the conversion of 25OHD to 1,25(OH)2D, are depicted here (dotted arrows). Specifically, hypercalcemia inhibits 1,25(OH)2D synthesis, whereas hypocalcemia stimulates its production primarily due to an increase in PTH secretion. Hypophosphatemia and PTH up-regulate CYP27B1 and increase renal production of 1,25(OH)2D, whereas FGF-23 does the opposite. 1,25(OH)2D regulates its own synthesis by down-regulating CYP27B1 activity and suppressing PTH secretion. 1,25(OH)2D, the active vitamin D form, binds to the VDR to increase intestinal calcium absorption and exert the other vitamin D-related actions. Finally, 1,25(OH)2D increases CYP24A1 activity to catabolize 25OHD and 1,25(OH)2D to water-soluble products that are excreted in the bile. The enzymes involved in each step, all cytochrome P450s (CYP), are shown in red.

Diagram showing the main steps of vitamin D synthesis and metabolism. Cholecalciferol or vitamin D3 is produced from 7-dehydrocholesterol in the skin by exposure to sunlight. Vitamin D3 formed in this fashion as well as vitamin D3 and D2 taken from dietary sources or commercially available supplements circulate in the bloodstream bound to the DBP. They are converted to 25OHD in the liver in a constitutive process, which is largely dependent on substrate availability. 25OHD is further hydroxylated in the kidney to the active form 1,25(OH)2D in a tightly regulated process. The primary regulatory pathways that control the production of 1,25(OH)2D and activity of CYP27B1, which catalyzes the conversion of 25OHD to 1,25(OH)2D, are depicted here (dotted arrows). Specifically, hypercalcemia inhibits 1,25(OH)2D synthesis, whereas hypocalcemia stimulates its production primarily due to an increase in PTH secretion. Hypophosphatemia and PTH up-regulate CYP27B1 and increase renal production of 1,25(OH)2D, whereas FGF-23 does the opposite. 1,25(OH)2D regulates its own synthesis by down-regulating CYP27B1 activity and suppressing PTH secretion. 1,25(OH)2D, the active vitamin D form, binds to the VDR to increase intestinal calcium absorption and exert the other vitamin D-related actions. Finally, 1,25(OH)2D increases CYP24A1 activity to catabolize 25OHD and 1,25(OH)2D to water-soluble products that are excreted in the bile. The enzymes involved in each step, all cytochrome P450s (CYP), are shown in red.

Table 1.

Vitamin D Preparations Available in the United States, Showing Various Formulations Among Vitamin D Products

Ergocalciferol (vitamin D2)
    Solution, 8000 IU/mL Requires prescription
    Gel-cap, 50 000 IU Requires prescription
    Tablets and capsules, eg, 200–5000 IU Over the counter
Cholecalciferol (vitamin D3)
    Solution, eg, 400 and 5000 IU/mL Over the counter
    Drops, eg, 400–2000 IU/drop Over the counter
    Tablets and capsules, eg, 200, 400, 1000, 5000, 10 000, and 50 000 IU Over the counter
Calcitriol (1,25-dihydroxycholecalciferol)
    Capsules, 0.25 and 0.5 μg Requires prescription
    Injectable solution, 1 or 2 μg/mL Requires prescription
Ergocalciferol (vitamin D2)
    Solution, 8000 IU/mL Requires prescription
    Gel-cap, 50 000 IU Requires prescription
    Tablets and capsules, eg, 200–5000 IU Over the counter
Cholecalciferol (vitamin D3)
    Solution, eg, 400 and 5000 IU/mL Over the counter
    Drops, eg, 400–2000 IU/drop Over the counter
    Tablets and capsules, eg, 200, 400, 1000, 5000, 10 000, and 50 000 IU Over the counter
Calcitriol (1,25-dihydroxycholecalciferol)
    Capsules, 0.25 and 0.5 μg Requires prescription
    Injectable solution, 1 or 2 μg/mL Requires prescription

Table 1.

Vitamin D Preparations Available in the United States, Showing Various Formulations Among Vitamin D Products

Ergocalciferol (vitamin D2)
    Solution, 8000 IU/mL Requires prescription
    Gel-cap, 50 000 IU Requires prescription
    Tablets and capsules, eg, 200–5000 IU Over the counter
Cholecalciferol (vitamin D3)
    Solution, eg, 400 and 5000 IU/mL Over the counter
    Drops, eg, 400–2000 IU/drop Over the counter
    Tablets and capsules, eg, 200, 400, 1000, 5000, 10 000, and 50 000 IU Over the counter
Calcitriol (1,25-dihydroxycholecalciferol)
    Capsules, 0.25 and 0.5 μg Requires prescription
    Injectable solution, 1 or 2 μg/mL Requires prescription
Ergocalciferol (vitamin D2)
    Solution, 8000 IU/mL Requires prescription
    Gel-cap, 50 000 IU Requires prescription
    Tablets and capsules, eg, 200–5000 IU Over the counter
Cholecalciferol (vitamin D3)
    Solution, eg, 400 and 5000 IU/mL Over the counter
    Drops, eg, 400–2000 IU/drop Over the counter
    Tablets and capsules, eg, 200, 400, 1000, 5000, 10 000, and 50 000 IU Over the counter
Calcitriol (1,25-dihydroxycholecalciferol)
    Capsules, 0.25 and 0.5 μg Requires prescription
    Injectable solution, 1 or 2 μg/mL Requires prescription

The most important steps in vitamin D metabolism are shown in Figure 1. Vitamin D hydroxylation to 25-hydroxyvitamin D (25OHD) in the liver depends on substrate availability, and therefore, 25OHD concentrations rise in circulation during excess or intoxication (37). In contrast, the subsequent 1α-hydroxylation to 1,25-dihydroxyvitamin D [1,25(OH)2D] in the kidney is tightly regulated by PTH and under negative feedback by calcium, phosphorus, fibroblast growth factor 23 (FGF-23), and 1,25(OH)2D itself (37). Consequently, in vitamin D intoxication, serum 1,25(OH)2D concentrations are usually normal and do not correlate with serum calcium concentrations.

The body kinetics of vitamin D2 and D3 and 25OHD have significant implications on symptomatology and management during intoxication. Both vitamin D2 and D3 are lipophilic and rapidly removed from the circulation by various tissues such as adipose and muscle where they may remain stored for almost 2 months (1–3, 37, 38). Their metabolite, 25OHD, has high affinity for its transport protein, vitamin D binding protein (DBP), which results in a long half-life of 2–3 weeks. 25OHD is also lipophilic and can be stored in adipose tissue, remaining there for months, depending on the extent of vitamin D stores (1–3, 37, 38). Hence, vitamin D intoxication may take weeks to resolve and require a prolonged course of treatment. Although both vitamin D2 and D3 undergo the same hydroxylation steps and are equipotent in treating rickets, vitamin D2 has been found less toxic in animal studies and less efficacious in raising serum 25OHD concentration than vitamin D3, when administered in the form of boluses (39). However, according to a recent meta-analysis, this difference between D2 and D3 is lost with daily administration, implying differences in the catabolism of these two vitamin D forms (40). Pediatric data comparing the efficacy of D2 and D3 are sparse, and hence, further studies are needed to confirm similar events in children.

Animal studies and a limited number of observations from human cases offer insight into alterations in vitamin D metabolism during states of intoxication (37, 38, 41, 42). Under physiological conditions, 1,25(OH)2D has high affinity for the vitamin D receptor (VDR), making it the active vitamin D metabolite. The precise vitamin D metabolite responsible for the hypercalcemia during vitamin D intoxication is still a matter of debate, although evidence points to 25OHD as the main culprit (36–38). During intoxication, 25OHD concentrations rise in the circulation and, at sufficiently high levels, can bind to VDR and stimulate transcription (Figure 1). In addition, the elevated 25OHD concentrations can compete and displace 1,25(OH)2D from its transport protein DBP, thus increasing the "free" and biological active component of 1,25(OH)2D. Indeed, increased free 1,25(OH)2D concentrations with normal total 1,25(OH)2D levels were reported in adults with vitamin D intoxication (43).

During intoxication, high concentrations of either 25OHD or free 1,25(OH)2D lead to hypercalcemia by increasing intestinal calcium absorption and bone resorption (44, 45). In turn, hypercalcemia increases the calcium load that is filtered through the kidney, resulting in hypercalciuria via a mechanism that involves increased calcium excretion in the distal tubule (46–48). Persistently elevated serum calcium concentrations may also cause polyuria and dehydration because of an inability of the kidneys to appropriately concentrate urine. The mechanisms behind this renal concentration defect are incompletely understood and may involve tubular interstitial injury because of calcium deposition in the medulla, down-regulation of aquaporin-2 water channel, or activation of the calcium-sensing receptors (49–51).

In addition to various vitamin D2 and D3 preparations, 1,25(OH)2D or calcitriol is also available for the treatment for the hypocalcemia and secondary hyperparathyroidism of renal failure (52) or rare conditions such as hypoparathyroidism, pseudohypoparathyroidism, or hypophosphatemic rickets. Reports of intoxication caused by excessive calcitriol intake in these patients are extremely rare (53–55). Hypercalcemia due to ingestion of calcitriol usually lasts only 1 to 2 days because of the relatively short biological half-life of calcitriol. Thus, stopping the calcitriol and hydration with iv saline may be the only therapy that is needed. Because calcitriol is not used as a supplement or prescribed for the treatment of vitamin D deficiency or insufficiency in children, we restrict our discussion only to safety and toxicity related to vitamin D2 or D3.

Current Recommendations on Daily Vitamin D Intake and Treatment of Insufficiency or Deficiency

The most recent pediatric recommendations for daily requirements, upper level intake, and vitamin D doses for the treatment of vitamin D insufficiency and deficiency are presented in Table 2 (5, 7, 10–13). The table indicates considerable lack of consensus. The difference in recommendations reflects an ongoing debate about what constitutes optimal or adequate vitamin D levels for skeletal health (5–13). The Endocrine Society with its published guidelines advocates for 25OHD concentrations above 30 ng/mL (75 nmol/L) as ideal for bone health and defines deficiency as levels less than 20 ng/mL (50 nmol/L). The Institute of Medicine (IOM) accepts levels above 20 ng/mL as sufficient. The debate is based primarily on data from the adult literature. Only a limited number of studies have evaluated the effect of vitamin D on bone mass at doses that raise serum 25OHD concentrations above 30 ng/mL in pediatrics (56–59). The results are so far inconsistent. Therefore, the higher vitamin D cutoffs of 30 ng/mL have not been the official recommendation of the American Academy of Pediatrics, PES, or their European counterparts (10–13). However, the discussion has generated confusion among treating physicians and the public about appropriate vitamin D levels and supplementation.

Table 2.

Recent Pediatric Recommendations of Vitamin D Intake

Age Maintenance Vitamin D Doses
AAP and PES IOM Endocrine Society for Patients at Risk for Vitamin D Deficiency b EFSA and ESPGHAN d
Daily Requirement, IU a Recommended Dietary Allowance, IU Upper Level Intake, IU Daily Requirement, IU Upper Level Intake, IU Recommended Daily Supplementation, IU Upper Level Intake, IU
0–6 mo 400 c 1000 400–1000 2000 400 1000
6–12 mo 400 c 1500 400–1000 2000 400 1000
1–3 y 400 600 2500 600–1000 4000 None 2000
4–8 y 400 600 3000 600–1000 4000 None 2000
9–10 y 400 600 4000 600–1000 4000 None 2000
11–18 y 400 600 4000 600–1000 4000 None 4000
Age Maintenance Vitamin D Doses
AAP and PES IOM Endocrine Society for Patients at Risk for Vitamin D Deficiency b EFSA and ESPGHAN d
Daily Requirement, IU a Recommended Dietary Allowance, IU Upper Level Intake, IU Daily Requirement, IU Upper Level Intake, IU Recommended Daily Supplementation, IU Upper Level Intake, IU
0–6 mo 400 c 1000 400–1000 2000 400 1000
6–12 mo 400 c 1500 400–1000 2000 400 1000
1–3 y 400 600 2500 600–1000 4000 None 2000
4–8 y 400 600 3000 600–1000 4000 None 2000
9–10 y 400 600 4000 600–1000 4000 None 2000
11–18 y 400 600 4000 600–1000 4000 None 4000
Age Treatment of vitamin D deficiency or insufficiency
PES Endocrine Society b
0–1 mo 1000 IU/d for 2–4 wk 2000 IU/d or 50 000 IU/wk for 6 wk
1–12 mo 1000–5000 IU/d for 2–4 wk
>12 mo >5000 IU/d for 2–4 wk
Age Treatment of vitamin D deficiency or insufficiency
PES Endocrine Society b
0–1 mo 1000 IU/d for 2–4 wk 2000 IU/d or 50 000 IU/wk for 6 wk
1–12 mo 1000–5000 IU/d for 2–4 wk
>12 mo >5000 IU/d for 2–4 wk

Abbreviations: AAP, American Academy of Pediatrics; PES, Pediatric Endocrine Society; IOM, Institute of Medicine; EFSA, European Food Safety Authority; ESPGHAN, European Society for Pediatric Gastroenterology, Hepatology, and Nutrition.

a

PES recommendations for premature infants, dark-skinned infants and children, and for those residing at higher latitudes (above 40°): 800 IU/d.

b

Obesity. Malabsorption, use of medications such as anticonvulsants or ketoconazole: increase recommended doses by two or three times.

c

Adequate intake is 400 IU/d.

d

Recommendations do not cover children with chronic diseases or preterm infants.

Table 2.

Recent Pediatric Recommendations of Vitamin D Intake

Age Maintenance Vitamin D Doses
AAP and PES IOM Endocrine Society for Patients at Risk for Vitamin D Deficiency b EFSA and ESPGHAN d
Daily Requirement, IU a Recommended Dietary Allowance, IU Upper Level Intake, IU Daily Requirement, IU Upper Level Intake, IU Recommended Daily Supplementation, IU Upper Level Intake, IU
0–6 mo 400 c 1000 400–1000 2000 400 1000
6–12 mo 400 c 1500 400–1000 2000 400 1000
1–3 y 400 600 2500 600–1000 4000 None 2000
4–8 y 400 600 3000 600–1000 4000 None 2000
9–10 y 400 600 4000 600–1000 4000 None 2000
11–18 y 400 600 4000 600–1000 4000 None 4000
Age Maintenance Vitamin D Doses
AAP and PES IOM Endocrine Society for Patients at Risk for Vitamin D Deficiency b EFSA and ESPGHAN d
Daily Requirement, IU a Recommended Dietary Allowance, IU Upper Level Intake, IU Daily Requirement, IU Upper Level Intake, IU Recommended Daily Supplementation, IU Upper Level Intake, IU
0–6 mo 400 c 1000 400–1000 2000 400 1000
6–12 mo 400 c 1500 400–1000 2000 400 1000
1–3 y 400 600 2500 600–1000 4000 None 2000
4–8 y 400 600 3000 600–1000 4000 None 2000
9–10 y 400 600 4000 600–1000 4000 None 2000
11–18 y 400 600 4000 600–1000 4000 None 4000
Age Treatment of vitamin D deficiency or insufficiency
PES Endocrine Society b
0–1 mo 1000 IU/d for 2–4 wk 2000 IU/d or 50 000 IU/wk for 6 wk
1–12 mo 1000–5000 IU/d for 2–4 wk
>12 mo >5000 IU/d for 2–4 wk
Age Treatment of vitamin D deficiency or insufficiency
PES Endocrine Society b
0–1 mo 1000 IU/d for 2–4 wk 2000 IU/d or 50 000 IU/wk for 6 wk
1–12 mo 1000–5000 IU/d for 2–4 wk
>12 mo >5000 IU/d for 2–4 wk

Abbreviations: AAP, American Academy of Pediatrics; PES, Pediatric Endocrine Society; IOM, Institute of Medicine; EFSA, European Food Safety Authority; ESPGHAN, European Society for Pediatric Gastroenterology, Hepatology, and Nutrition.

a

PES recommendations for premature infants, dark-skinned infants and children, and for those residing at higher latitudes (above 40°): 800 IU/d.

b

Obesity. Malabsorption, use of medications such as anticonvulsants or ketoconazole: increase recommended doses by two or three times.

c

Adequate intake is 400 IU/d.

d

Recommendations do not cover children with chronic diseases or preterm infants.

Safety Data of High Vitamin D Doses in Pediatrics

Although vitamin D deficiency is detrimental for bone health, the consequent approach that higher doses are protective and confer a reduced risk for disease has been challenged by recent data in adults that indicate that high doses of vitamin D raise the incidence of falls and fractures (60, 61). These events were linked to the mode of vitamin D administration as stoss therapy, ie, as a single large bolus compared to smaller intermittent doses (62). Beyond skeletal health, similar curvilinear or U-shaped response has been described for other vitamin D outcomes, including all-cause mortality, cardiovascular disease, and selected cancers, so that the IOM cautions against maintaining serum 25OHD concentrations above 50 ng/mL (125 nmol/L) (6). Experts call for more studies, and this statement cannot be more compelling than in pediatrics where data on the safety and long-term use of high vitamin D doses are limited.

In the late 1930s, treatment of infants with high vitamin D doses was reported to impair growth (63). The pediatric experience with stoss therapy indicates that single doses of 600 000 IU in infants with rickets were associated with high rates of hypercalcemia, whereas doses in the range of 100 000 to 200 000 IU had no ill effects (64–67). Hypercalcemia was also observed in a few infants who received single doses of 300 000 IU (65). More recently, a number of trials in healthy children tested vitamin D doses at the upper levels set by the IOM and with the goal of increasing serum concentrations above 30 ng/mL. Specifically, Gordon et al (68) randomized 40 infants and toddlers with 25OHD levels <20 ng/mL to either 2000 IU vitamin D2 or D3 daily or 50 000 IU D2 weekly for 6 weeks. Only a few children attained serum 25OHD levels above 100 ng/mL, although without a significant rise in serum calcium (68). In a birth cohort study that examined the effect of vitamin D on the risk for type I diabetes, infants treated with 2000 IU daily for 1 year suffered no undesired effects (69). However, serum 25OHD and calcium concentrations were not monitored. Two randomized dose-escalating trials used vitamin D3 doses up to 1600 IU/d in full-term healthy infants and documented a dose-dependent rise in 25OHD concentrations with increasing vitamin D supplementation (56, 59). The first one, a short-term study of 3 months that involved 113 newborns, showed no case of vitamin D excess and associated hypercalcemia or hypercalciuria (56). The second included 132 1-month-old term infants randomized to receive vitamin D3 at 400, 800, 1200, and 1600 IU/d for 11 months. Again, no harm was documented (59). High doses at 1600 IU/d did not result in improved skeletal outcomes despite mean 25OHD concentrations of 72 ng/mL (measured by liquid chromatography tandem mass spectrometry). Of interest, 25OHD concentrations were also measured for safety purposes during the course of the trial by an immunoassay, which provided readings frequently above 100 ng/mL resulting in premature discontinuation of this arm (59). These events underscore the variability among vitamin D assays. The authors concluded that the dose of 1600 IU/d "exceeded the healthy population target range of 50 ng/mL" without extra benefits.

Safety data of high vitamin D doses in older children and adolescents are quite limited. Vitamin D3 supplementation at 1000 IU daily for 8 weeks as part of a calcium absorption study in preteen children raised the average 25OHD value above 30 ng/mL but did not result in excess (70). The daily dose of 2000 IU D3 for 16 weeks caused no toxicity or adverse effects in adolescent boys and girls (71). Similarly, preteen and teen children who received the equivalent of 2000 IU daily for 1 year experienced no adverse effects. Vitamin D excess, ie, 25OHD concentrations >100 ng/mL, were reported in 1.5% of the subjects without associated hypercalcemia (57, 58). No recent study has addressed the safety of vitamin D supplementation with doses as high as 4000 IU daily in children. The current recommendations of 4000 IU/d as the upper tolerable vitamin D intake in children (Table 1) were based on a "variety of observations dated back to 1940" (5–7).

There are important lessons to be gleaned from vitamin D studies in children with various disorders that make them particularly vulnerable to vitamin D deficiency. In children and adolescents with inflammatory bowel disease and serum 25OHD levels <20 ng/mL, oral doses of 2000 IU vitamin D2 or D3 daily or 50 000 IU D2 weekly for 6 weeks raised levels above 20 ng/mL in 75–95% of subjects without toxicity (72). Similar findings were observed in another randomized trial of calcium and vitamin D supplementation in children with inflammatory bowel disease that used 50 000 IU of vitamin D2 monthly for 6 months (73). In cystic fibrosis, a few studies examined the effect of high vitamin D doses including 50 000 IU given daily or three times weekly (74–76). In these studies, daily intake of 50 000 IU vitamin D2 for 28 days was required to raise 25OHD concentrations above 30 ng/mL (76). Although no toxicity was reported, serum calcium concentrations were not monitored, and occasional subjects achieved 25OHD levels in the 250–310 ng/mL range (76). The immune effects of high vitamin D doses were tested in a few trials in children and adolescents infected with HIV. Vitamin D3 doses of 100 000 IU once every 2 months or 50 000 IU monthly did not result in excess or other toxicity (77–79). Similar findings were observed in preteen children treated with doses equivalent to 1600 IU daily (80).

Based on the present literature, vitamin D intake that approaches the upper ranges that are currently recommended caused no significant ill effects in children, although vitamin D excess was observed in some studies. However, the data are limited, and most of the studies are short term. Clearly, more extensive longitudinal data are required in both healthy and high-risk children to reinforce long-term use of high-dose vitamin D therapy. Furthermore, special attention should be paid to those with high calcium intake or an underlying condition that predisposes to hypercalcemia (such as Williams syndrome) because high vitamin D doses may provoke or exacerbate hypercalcemia in such cases.

Vitamin D Excess and Intoxication in Children: Definitions and Associations With Hypercalcemia

Serum concentrations exceeding 150 ng/mL (375 nmol/L) have been proposed by The Endocrine Society to define intoxication, whereas levels up to 100 ng/mL (250 nmol/L) are cited as safe for both children and adults (7). These cutoffs, which are based on a few older studies, are accepted by the PES (10). The specific vitamin D intake that results in excess or intoxication and the severity of corresponding hypercalcemia have not been clearly established in pediatrics. Hence, we looked into the current cases of intoxication to determine associations between serum 25OHD concentrations and hypercalcemia.

Reports on vitamin D intoxication in infants and young children (24–35) typically describe cases that received extremely large doses, in the range of 240 000 to 4 500 000 IU, or approximately 40 000 to 560 000 IU/kg. This intake resulted in serum 25OHD levels in the range of 250–670 ng/mL leading to severe hypercalcemia (24–35). Serum calcium concentrations in the range of 14–18 mg/dL (3.5–4.5 mmol/L) were reported, with occasional values as high as 20 mg/dL (Figure 2). Among these cases, there is significant variability in the amount of vitamin D administered and the resulting serum 25OHD concentrations. Furthermore, even with comparable serum 25OHD levels, the severity of hypercalcemia and symptomatology is unpredictable. Some of this variability may be explained by differences in vitamin D assay (81, 82) or length of time between ingestion and laboratory evaluation.

Figure 2.

Serum calcium concentrations plotted against 25OHD concentrations (left) and vitamin D intake (right) in infants and children with vitamin D intoxication. Data are derived from reported cases of intoxication (24–35). Depicted values are those on clinical presentation and before any therapeutic intervention. As patients came to medical attention at various time points after ingestion, the peak 25OHD concentrations may have been missed in some of these reports.

Serum calcium concentrations plotted against 25OHD concentrations (left) and vitamin D intake (right) in infants and children with vitamin D intoxication. Data are derived from reported cases of intoxication (24–35). Depicted values are those on clinical presentation and before any therapeutic intervention. As patients came to medical attention at various time points after ingestion, the peak 25OHD concentrations may have been missed in some of these reports.

Figure 2.

Serum calcium concentrations plotted against 25OHD concentrations (left) and vitamin D intake (right) in infants and children with vitamin D intoxication. Data are derived from reported cases of intoxication (24–35). Depicted values are those on clinical presentation and before any therapeutic intervention. As patients came to medical attention at various time points after ingestion, the peak 25OHD concentrations may have been missed in some of these reports.

Serum calcium concentrations plotted against 25OHD concentrations (left) and vitamin D intake (right) in infants and children with vitamin D intoxication. Data are derived from reported cases of intoxication (24–35). Depicted values are those on clinical presentation and before any therapeutic intervention. As patients came to medical attention at various time points after ingestion, the peak 25OHD concentrations may have been missed in some of these reports.

Beyond these cases, mild asymptomatic hypercalcemia associated with 25OHD concentrations above 75 ng/mL was recently reported in three young children with rickets who received therapy according to currently accepted guidelines and believed to be safe (36). These cases raise the concern that even recommended treatment doses have the potential for toxicity.

The variability in both serum 25OHD concentrations and resulting hypercalcemia for a given amount of vitamin D needs also to be interpreted in light of recent developments in genetics. Polymorphisms in genes that regulate the synthesis and hydroxylation of vitamin D as well as the synthesis of DBP have been shown to influence circulating 25OHD levels (83–85). Furthermore, defects in 24-hydroxylation caused by CYP24A1 loss-of-function mutations lead to decreased degradation of 1,25(OH)2D and the syndrome of idiopathic infantile hypercalcemia (IIH) (86–89). Affected individuals manifest increased sensitivity to vitamin D and may develop severe hypercalcemia and hypercalciuria, even with small vitamin D doses. Although this syndrome is rare, it exemplifies the role of genotype on vitamin D metabolism and response to supplementation. It also raises the question whether genetics should be taken into account when prescribing vitamin D, a subject that warrants further studies (90). Although we hope to have these answers in the future, at the moment the data support special consideration and evaluation of individual cases who respond to vitamin D supplementation in an unorthodox way.

Causes of Vitamin D Intoxication

Vitamin D intoxication is a rare event. However, the exact incidence is unclear because there are no systematic studies that have addressed this question.

Vitamin D intoxication from dietary sources has been reported over the last 20 years. Examples include accidental use of veterinary vitamin D concentrate that was mistaken as cooking oil (43) or excessive milk fortification (70 to 600 times above the state limit) by a home delivery dairy in the state of Massachusetts (91, 92). In adults, recent reports describe cases of accidental or intentional intake of excessive vitamin D caused by a variety of circumstances such as misinterpretation of prescription instruction or inappropriate prescription of excessive vitamin D doses for vague musculoskeletal complaints without monitoring 25OHD concentrations (14–23, 93, 94). In both the United States and Europe, intoxication has been reported after manufacturing errors of over-the-counter vitamin D formulations that contained substantially higher concentrations than claimed on the label (14, 17, 18). Because the production of such supplements is not overseen by the Food and Drug Administration, their content can be quite variable. In a recent study, just over one-half of over-the-counter preparations and only one-third of the compounded pills met the US Pharmacopeial Convention standards containing 90–110% of the active ingredient, whereas the rest had either higher or lower concentrations than expected (95).

Pediatric reports include an outbreak of hypercalciuria in the United Kingdom during the 1950s attributed to overfortification of infant formula (96). However, some of these cases are now attributed to other disorders, such as Williams syndrome or IIH caused by CYP24A1 mutations (86–89). Over the last decade, a number of infants with suspected rickets who were prescribed high vitamin D doses without prior measurement of 25OHD concentrations presented with severe life-threatening hypercalcemia (24, 29–32). Intoxication also occurred after intentional ingestion of products bought through the internet for "good health" (28) or dosing errors because of parent misinterpretation of the prescribed doses (25, 30). One case involved an infant who received a 30-fold overdose of vitamin D when the mother switched over-the-counter formulations from one that contained 400 IU/mL to another that contained 400 IU per drop. Unaware of the change in concentration, the mother continued to administer 1 mL, resulting in a daily vitamin D intake of 12 000 IU (33).

Symptoms and Diagnosis of Vitamin D Intoxication

Children with vitamin D intoxication present with symptoms of hypercalcemia, such as poor appetite, weight loss, abdominal pain, vomiting, constipation, polyuria, and polydipsia, and in severe cases, life-threatening dehydration (24–32). Because the complaints of hypercalcemia are nonspecific, symptoms can be present for prolonged periods before a child worsens and comes to medical attention. In some cases, the concentration of calcium in the glomerular filtrate may exceed its solubility, resulting in calcium precipitation in the renal tubules and nephrocalcinosis. This complication occurs in approximately 25% of patients with vitamin D intoxication, whereas in some pediatric series, vitamin D intoxication accounts for about 10% of all cases of nephrocalcinosis (97). Dehydration, decreased glomerular filtration rate, and nephrocalcinosis may all compromise renal function resulting in renal tubular acidosis and insufficiency. Metastatic vascular calcifications have also been reported (24–32).

The diagnosis of vitamin D intoxication is based on elevated serum 25OHD concentrations, which are associated with hypercalcemia or hypercalciuria, whereas serum 1,25(OH)2D levels are normal and PTH is suppressed. In contrast, hypercalcemia and hypercalciuria in the presence of normal serum 25OHD concentrations, increased 1,25(OH)2D levels, and suppressed PTH raise the suspicion of IIH. In such cases, 24,25-dihydroxyvitamin D concentrations are low or undetectable (86–89).

Treatment of Vitamin D Intoxication

Treatment efforts target children and adolescents with symptomatic hypercalcemia. As a first step, the source of vitamin D is removed, and the levels are allowed to decrease with time, an event that typically occurs over several weeks. Because vitamin D has a long half-life, serum 25OHD concentrations may occasionally continue to climb after discontinuation of vitamin D administration. Therefore, it is prudent to monitor symptoms and serum calcium concentrations for those asymptomatic patients with excessively high 25OHD levels.

The first line of therapy of hypercalcemia is iv hydration with normal saline at 1.5–2.5 maintenance to increase the glomerular filtration rate and calcium excretion. Intravenous hydration can be combined with specific diuretics that increase calcium excretion, such as loop diuretics. Furosemide at 1–2 mg/kg/d, as divided doses every 4–6 hours, is usually given. Thiazides, on the other hand, should be avoided because they increase calcium reabsorption at the distal tubule and, therefore, can further exacerbate hypercalcemia.

Glucocorticoids and calcitonin can be added if symptomatic hypercalcemia persists despite hydration and diuretics. Glucocorticoids prevent renal calcium reabsorption and inhibit the production and activity of 1,25(OH)2D, thus decreasing intestinal calcium absorption (98). Prednisone at 1–2 mg/kg/d (or 20–40 mg/m2/d), given as divided doses every 4 hours up to 2 weeks, has been used in children with vitamin D intoxication (34); onset of action is expected within 24–72 hours. Steroids can be combined with sc calcitonin, given at doses of 2–4 IU/kg every 6 to 12 hours, because of its a rapid effect on serum calcium. However, its therapeutic value is limited because of tachyphylaxis. Anaphylactic shock has also been reported (99).

Bone resorption is increased in vitamin D intoxication (100, 101), and therefore, antiresorptive therapy with bisphosphonates, such as pamidronate and alendronate, can successfully lower serum calcium levels in intoxicated children and adults (29–32, 100, 101). Doses of 5 or 10 mg alendronate or 0.5–1 mg/kg/dose of pamidronate have been used in pediatrics. In a recent series of six infants with vitamin D intoxication, oral alendronate achieved normocalcemia four times faster than steroids (34). Repeated courses over a period of weeks may be required in cases of persistent 25OHD elevations.

As a last resort, hemodialysis can lower serum calcium rapidly and can be used in life-threatening cases that do not respond to treatment with other means, such as acute or chronic renal failure or hypercalcemic crisis.

Conclusion and Recommendations

Awareness of the benefits of vitamin D has increased both in the medical community and the general population. As such, over-the-counter and prescribed vitamin D intake has followed suit. Unregulated supplements and formulations of vitamin D are readily available in pharmacies and health food stores alike. Because both underdosing and overtreatment with vitamin D can have considerable consequences, the need to regulate the available formulations must be recognized. Furthermore, vitamin D intoxication has been reported after misunderstanding of physician instructions, emphasizing the need for improved communication regarding dosing. Based on this most recent review of the literature, we suggest the following guidelines for the prevention and management of vitamin D excess and intoxication in pediatrics:

  1. 1.

    Health care providers should be aware of the various vitamin D preparations and counsel patients on both desirable doses and variability among formulations.

  2. 2.

    Empirical therapy of vitamin D deficiency with high vitamin D doses, such as stoss therapy, is discouraged without previous documentation of 25OHD concentrations and monitoring of 25OHD and serum calcium levels.

  3. 3.

    Health care providers should consider monitoring vitamin D levels in infants and children receiving treatment doses at the upper ranges currently recommended (5, 7). Although there is insufficient evidence to guide the frequency of such testing, we suggest 25OHD measurements no more than every 6 months.

  4. 4.

    Vitamin D excess or intoxication should be included in the differential of children who present with hypercalcemia or hypercalciuria.

  5. 5.

    Serum calcium concentrations should be monitored in children with serum 25OHD concentrations above 150 ng/mL (375 nmol/L) measured by a reliable assay such as liquid chromatography tandem mass spectrometry.

  6. 6.

    For asymptomatic patients with vitamin D intoxication, we suggest monitoring of clinical symptoms and serum 25OHD and calcium levels until serum 25OHD values start declining.

Acknowledgments

We thank the following members of the Pediatric Endocrine Society Drug and Therapeutics Committee for careful review of the manuscript and constructive comments: Patricia Fechner, Chirag Kapadia, Bradley Miller, Susan Myers, Todd Nebesio, Sripriya Raman, J. B. Quintos, David Weinstein, and Steven M. Willi.

No external funding was secured for this study.

Disclosure Summary: The authors have no conflicts to disclose.

Abbreviations

  • DBP

    vitamin D binding protein

  • FGF-23

    fibroblast growth factor 23

  • IIH

    idiopathic infantile hypercalcemia

  • 1,25(OH)2D

  • 25OHD

  • VDR

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Copyright © 2014 by The Endocrine Society

Gave Baby Too Much Vitamin D

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