○ 이 약의 초기권장 용법/용량은 칼시트리올로서 주 3회, 0.5 ㎍(체중 kg당 약 0.01 ㎍)을 격일 투여한다. 이 약은 IV bolus로, 혈액투석 종료시 카테터를 통해 투여할 수 있다. 생화학적 검사치 및 임상증상에 만족할만한 반응이 나타나지 않을 경우, 2∼4주 간격으로 0.25∼0.50 ㎍을 증량한다. 대부분의 혈액투석 환자는 주 3회, 0.5∼3.0 ㎍(체중 kg당 0.01∼0.05 ㎍)의 용량으로 효과를 나타낸다.
○ 용법관련 주의사항
1) 용량결정을 위한 적정기간 중 혈청 칼슘과 인 수치를 주 2회 이상 측정해야 한다. 단, 혈청 칼슘수치가 기준치 상한을 0.5 mg/dL 초과한 경우에는 별도로 측정빈도를 높이고(주 1회 이상), 감량 등도 고려하여 신중히 투여한다. 또한, 혈청 칼슘수치가 기준치 상한을 1 mg/dL 초과하는 경우에는 즉시 휴약한다. 휴약에 의해 혈청 칼슘수치가 기준치까지 저하되었는지 확인한 후, 휴약전의 투여량을 참고하여 감량 등을 고려해 투여를 재개한다. 저알부민혈증(혈청 알부민수치 ＜ 4.0 g/dL)의 경우에는 보정수치를 지표로 사용할 것을 권한다.
Calcitriol에 대한 Mechanism_Of_Action 정보 The mechanism of action of Calcitriol in the treatment of psoriasis is accounted for by their antiproliferative activity for keratinocytes and their stimulation of epidermal cell differentiation. The anticarcinogenic activity of the active form of Calcitriol appears to be correlated with cellular vitamin D receptor (VDR) levels. Vitamin D receptors belong to the superfamily of steroid-hormone zinc-finger receptors. VDRs selectively bind 1,25(OH)2D and retinoic acid X receptor (RXR) to form a heterodimeric complex that interacts with specific DNA sequences known as vitamin D-responsive elements. VDRs are ligand-activated transcription factors. The receptors activate or repress the transcription of target genes upon binding their respective ligands. It is thought that the anticarcinogenic effect of Calcitriol is mediated via VDRs in cancer cells. The immunomodulatory activity of Calcitriol is thought to be mediated by vitamin D receptors (VDRs) which are expressed constitutively in monocytes but induced upon activation of T and B lymphocytes. 1,25(OH)2D has also been found to enhance the activity of some vitamin D-receptor positive immune cells and to enhance the sensitivity of certain target cells to various cytokines secreted by immune cells.
Pharmacology
Calcitriol에 대한 Pharmacology 정보 Calcitriol, a pharmaceutical form of vitamin D, has anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Calcitriol has been found to be effective in the treatment of psoriasis when applied topically. Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in a number of malignant cell lines including human prostate cancer cells. Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of Calcitriol, 1,25 (OH)2 D, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25(OH)2D has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. It has also been found to induce monocyte differentiation and to inhibit lymphocyte proliferation and production of cytokines, including interleukin IL-1 and IL-2, as well as to suppress immunoglobulin secretion by B lymphocytes. Vitamin D appears to demonstrate both immune-enhancing and immunosuppressive effects.
Metabolism
Calcitriol에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Cytochrome P450 24A1 (CYP24A1)
Protein Binding
Calcitriol에 대한 단백결합 정보 99.9%
Half-life
Calcitriol에 대한 반감기 정보 5-8 hours
Absorption
Calcitriol에 대한 Absorption 정보 Rapidly absorbed from the intestine.
Pharmacokinetics
Calcitriol의 약물동력학자료
작용발현시간 : 약 2-6 시간
작용지속시간 : 3-5일
흡수 :
위장관으로부터 잘 흡수된다. (거의 100%)
Calcitriol의 흡수에는 담즙산염이 필요하지 않다.
분포 : 지용성이 높으므로 체내에 신속하게 분포한다.
단백결합 : 주로 vitamin D-binding α-globulin에 결합하며 albumin과도 결합한다.
대사 : 주로 1,24,25-[OH]3 D3 및 1,24,25-[OH]2 D3로 대사된다.
반감기 : 3-8 시간
혈중최고농도 도달시간 : 경구 : 약 6시간
소실 : 주로 담즙 및 대변을 통해 배설되며 4-6%는 뇨를 통해 배설된다.
Biotransformation
Calcitriol에 대한 Biotransformation 정보 The first pathway involves 24-hydroxylase activity in the kidney; this enzyme is also present in many target tissues which possess the vitamin D receptor such as the intestine. The end product of this pathway is a side chain shortened metabolite, calcitroic acid. The second pathway involves the conversion of calcitriol via the stepwise hydroxylation of carbon-26 and carbon-23, and cyclization to yield ultimately 1a,25R(OH)2-26,23S-lactone D3. The lactone appears to be the major metabolite circulating in humans.
Toxicity
Calcitriol에 대한 Toxicity 정보 LD50 (oral, rat) = 620 μg/kg; LD50 (intraperitoneal, rat) > 5 mg/kg; Overdose evident in elevated blood calcium levels causing symptoms of anorexia, nausea and vomiting, polyuria, polydipsia, weakness, pruritus, and nervousness, potentially with irreversible calcification of soft tissue in the kidney and liver.
Calcitriol에 대한 Description 정보 Calcitriol or 1,25-dihydroxycholecalciferol (abbreviated 1,25-(OH)2D3) is the active form of vitamin D found in the body (vitamin D3). Calcitriol is marketed under various trade names including Rocaltrol (Roche), Calcijex (Abbott) and Decostriol (Mibe, Jesalis). It is produced in the kidneys via 25-Hydroxyvitamin D3 1-alpha-Hydroxylase by conversion from 25-hydroxycholecalciferol (calcidiol). This is stimulated by a decrease in serum calcium, phosphate (PO43?? and parathyroid hormone (PTH) levels. It regulates calcium levels by increasing the absorption of calcium and phosphate from the gastrointestinal tract, increasing calcium and phosphate reabsorption in the kidneys and inhibiting the release of PTH. Calcitriol is also commonly used as a medication in the treatment of hypocalcemia and osteoporosis.
Dosage Form
Calcitriol에 대한 Dosage_Form 정보 Capsule OralLiquid IntravenousSolution IntravenousSolution Oral
Drug Category
Calcitriol에 대한 Drug_Category 정보 Antihypocalcemic AgentsAntihypoparathyroid AgentsBone Density Conservation AgentsCalcium Channel AgonistsEssential VitaminVitaminsVitamins (Vitamin D)
Smiles String Canonical
Calcitriol에 대한 Smiles_String_canonical 정보 CC(CCCC(C)(C)O)C1CCC2C(CCCC12C)=CC=C1CC(O)CC(O)C1=C
Smiles String Isomeric
Calcitriol에 대한 Smiles_String_isomeric 정보 C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]2[C@]1(C)CCC\C2=C/C=C1\C[C@@H](O)C[C@H](O)C1=C
InChI Identifier
Calcitriol에 대한 InChI_Identifier 정보 InChI=1/C27H44O3/c1-18(8-6-14-26(3,4)30)23-12-13-24-20(9-7-15-27(23,24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11,18,22-25,28-30H,2,6-9,12-17H2,1,3-5H3/t18-,22-,23-,24+,25+,27-/m1/s1
Chemical IUPAC Name
Calcitriol에 대한 Chemical_IUPAC_Name 정보 (1R,3S)-5-[2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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알림
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경고
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ≥4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. CALCITRIOL [GGT Increase] [Composite Activity] (Score)I (Marginal) 0 (Active) 0
전문/일반
