Drug General Information (ID: DDIXNMC4LS)
  Drug Name Ergocalciferol Drug Info Cimetidine Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Vitamins Antiulcer Agents
  Structure

 Mechanism of Ergocalciferol-Cimetidine Interaction (Severity Level: Minor)
     Non-CYP450 enzyme inhibition Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Ergocalciferol Cimetidine
      Mechanism Vitamin D 25-hydroxylase substrate Vitamin D 25-hydroxylase inhibitor
      Key Mechanism Factor 1
Factor Name Vitamin D 25-hydroxylase
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Structure Sequence
MWKLWRAEEGAAALGGALFLLLFALGVRQLLKQRRPMGFPPGPPGLPFIGNIYSLAASSELPHVYMRKQSQVYGEIFSLDLGGISTVVLNGYDVVKECLVHQSEIFADRPCLPLFMKMTKMGGLLNSRYGRGWVDHRRLAVNSFRYFGYGQKSFESKILEETKFFNDAIETYKGRPFDFKQLITNAVSNITNLIIFGERFTYEDTDFQHMIELFSENVELAASASVFLYNAFPWIGILPFGKHQQLFRNAAVVYDFLSRLIEKASVNRKPQLPQHFVDAYLDEMDQGKNDPSSTFSKENLIFSVGELIIAGTETTTNVLRWAILFMALYPNIQGQVQKEIDLIMGPNGKPSWDDKCKMPYTEAVLHEVLRFCNIVPLGIFHATSEDAVVRGYSIPKGTTVITNLYSVHFDEKYWRDPEVFHPERFLDSSGYFAKKEALVPFSLGRRHCLGEHLARMEMFLFFTALLQRFHLHFPHELVPDLKPRLGMTLQPQPYLICAERR
Gene Name CYP2R1
Uniprot ID CP2R1_HUMAN
KEGG Pathway hsa:120227
Protein Family Cytochrome P450 family
Protein Function
A cytochrome P450 monooxygenase involved in activation of vitamin D precursors. Catalyzes hydroxylation at C-25 of both forms of vitamin D, vitamin D(2) and D(3) (calciol) (PubMed:12867411, PubMed:15465040, PubMed:18511070). Can metabolize vitamin D analogs/prodrugs 1alpha-hydroxyvitamin D(2) (doxercalciferol) and 1alpha-hydroxyvitamin D(3) (alfacalcidol) forming 25-hydroxy derivatives (PubMed:15465040, PubMed:18511070). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:12867411, PubMed:15465040, PubMed:18511070).
    Click to Show/Hide
      Mechanism Description
  • Decreased metabolism of Ergocalciferol caused by Cimetidine mediated inhibition of non-CYP450 enzyme

References
1 Odes HS, Fraser GM, Krugliak P, et al "Effect of cimetidine on hepatic vitamin D metabolism in humans." Digestion 46 (1990): 61-4. [PMID: 2253823]
2 Product Information. Fosamax Plus D (alendronate-cholecalciferol). Merck & Company Inc, West Point, PA.