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| <languages />
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| {{Drugbox
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| | Verifiedfields = changed
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| | Watchedfields = changed
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| | verifiedrevid = 445909355
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| | IUPAC_name = (1''R'',3''R'',7''E'',17β)-17-[(1''R'',2''E'',4''S'')-5-hydroxy-1,4,5-trimethylhex-2-en-1-yl]-9,10-secoestra-5,7-diene-1,3-diol
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| | image = Paricalcitol.svg
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| | width = 200px
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| | image2 = Paricalcitol3Dan.gif
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| | width2 = 200px
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| <!--Clinical data-->
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| | tradename = Zemplar
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| | Drugs.com = {{drugs.com|monograph|paricalcitol}}
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| | MedlinePlus = a682335
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| | pregnancy_AU = C
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| | pregnancy_US = C
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| | pregnancy_category =
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| | legal_AU = S4
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| | legal_CA = Rx-only
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| | legal_UK = POM
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| | legal_US = Rx-only
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| | legal_status =
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| | routes_of_administration = Oral, Intravenous
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| <!--Pharmacokinetic data-->
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| | bioavailability = 72%
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| | protein_bound = 99.8%
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| | metabolism = [[Hepatic]]
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| | elimination_half-life = 14-20 hours
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| | excretion = Faeces (74%), urine (16%)
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| <!--Identifiers-->
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| | CAS_number_Ref = {{cascite|correct|??}}
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| | CAS_number = 131918-61-1
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| | ATC_prefix = H05
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| | ATC_suffix = BX02
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| | ATC_supplemental =
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| | ChEBI_Ref = {{ebicite|changed|EBI}}
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| | ChEBI = 7931
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| | PubChem = 5281104
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| | IUPHAR_ligand = 2791
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| | DrugBank_Ref = {{drugbankcite|changed|drugbank}}
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| | DrugBank = DB00910
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| | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
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| | ChemSpiderID = 4444552
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| | UNII_Ref = {{fdacite|correct|FDA}}
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| | UNII = 6702D36OG5
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| | KEGG_Ref = {{keggcite|changed|kegg}}
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| | KEGG = D00930
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| | ChEMBL_Ref = {{ebicite|correct|EBI}}
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| | ChEMBL = 1200622
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| <!--Chemical data-->
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| | chemical_formula =
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| | C=27 | H=44 | O=3
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| | StdInChI_Ref = {{stdinchicite|correct|chemspider}}
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| | StdInChI = 1S/C27H44O3/c1-18(8-9-19(2)26(3,4)30)24-12-13-25-21(7-6-14-27(24,25)5)11-10-20-15-22(28)17-23(29)16-20/h8-11,18-19,22-25,28-30H,6-7,12-17H2,1-5H3/b9-8+,21-11+/t18-,19+,22-,23-,24-,25+,27-/m1/s1
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| | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
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| | StdInChIKey = BPKAHTKRCLCHEA-UBFJEZKGSA-N
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| | synonyms = <small>(1''R'',3''S'')-5-[2-[(1''R'',3a''R'',7a''S'')-1-<nowiki>[</nowiki>(2''R'',5''S'')-6-hydroxy-5,6-dimethyl-3''E''-hepten-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1''H''-inden-4-ylidene]ethylidene]-cyclohexane-1,3-diol</small>
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| }}
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|
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| '''パリカルシトール'''（化学的には'''19-ノル-1,25-(OH)<sub>2</sub>-ビタミンD<sub>2</sub>'''である。[[Abbott Laboratories]]から'''ゼンプラール'''の商品名で販売されている）は、[[chronic kidney failure/ja|慢性腎不全]]に伴う[[secondary hyperparathyroidism/ja|二次性副甲状腺機能亢進症]]（[[parathyroid hormone/ja|副甲状腺ホルモン]]の過剰分泌）の予防と治療に用いられる[[pharmaceutical drug/ja|医薬品]]である。[[Vitamin D2/ja|ビタミンD<sub>2</sub>]]（エルゴカルシフェロール）の活性型である1,25-ジヒドロキシエルゴカルシフェロールの[[analog (chemistry)/ja|類似体]]である。
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|
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| <!-- Society and culture -->
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| 1989年に特許を取得し、1998年に医療用として承認された。
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| ==医薬用途{{Anchor|Medical uses}}==
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| 医療における主な用途は、[[chronic kidney disease/ja|慢性腎臓病]]に伴う二次性[[hyperparathyroidism/ja|副甲状腺機能亢進症]]の治療である。しかし、現在のところ、この適応症に対する非選択的ビタミンD誘導体に対するパリカルシトールの優位性を示す証拠は十分ではない。
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| ==副作用{{Anchor|Adverse effects}}==
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| '''頻度別の副作用：'''<br />
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| '''非常に多い（頻度10％以上）:'''
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| * 吐き気
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|
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| <div class="mw-translate-fuzzy">
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| '''一般的（頻度1～10％）:''' | | '''一般的（頻度1～10％）:''' |
| {{div col|colwidth=18em}} | | {{div col|colwidth=18em}} |
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| * [[odema/ja|浮腫]] | | * [[odema/ja|浮腫]] |
| * アレルギー反応 | | * アレルギー反応 |
| * [[Arthritis/ja|関節炎 | | * [[Arthritis/ja|関節炎]] |
| * めまい<sup>†</sup> | | * めまい<sup>†</sup> |
| * 胃の不快感<sup>†</sup> | | * 胃の不快感<sup>†</sup> |
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| * [[Hypocalcaemia/ja|低カルシウム血症]]<sup>†</sup> | | * [[Hypocalcaemia/ja|低カルシウム血症]]<sup>†</sup> |
| * [[Hyperphosphataemia/ja|高リン血症]] | | * [[Hyperphosphataemia/ja|高リン血症]] |
| * 食欲減退<sup>†</sup>。 | | * 食欲減退<sup>†</sup> |
| * 頭痛 | | * 頭痛 |
| * 乳房圧痛<sup>†</sup> | | * 乳房圧痛<sup>†</sup> |
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| * 発疹<sup>‡</sup | | * 発疹<sup>‡</sup |
| {{div col end}} | | {{div col end}} |
| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| '''Uncommon (0.1-1% frequency):'''
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| {{div col|colwidth=18em}}
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| * Abnormal hepatic enzymes<sup>‡</sup>
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| * Constipation<sup>‡</sup>
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| * Dry mouth<sup>‡</sup>
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| * [[Pruritus|Itchiness]]<sup>‡</sup>
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| * [[Urticaria|Hives]]
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| * Hypersensitivity<sup>‡</sup>
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| * Muscle spasms<sup>‡</sup>
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| * Bleeding time prolonged
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| * Aspartate aminotransferase increased
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| * Laboratory test abnormal
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| * Weight loss
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| * Elevated blood creatinine
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| * Cardiac arrest
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| * Arrhythmia
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| * Atrial flutter
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| * [[Anaemia]]
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| * [[Leucopenia]]
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| * Lymphadenopathy
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| * Coma
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| * [[Cerebrovascular accident|Stroke]]
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| * [[Transient ischemic attack]]
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| * [[Vasovagal syncope|Fainting]]
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| * [[Myoclonus]]
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| * [[Hypoaesthesia]]
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| * [[Paraesthesia]]
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| * [[Glaucoma]]
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| * [[Conjunctivitis]]
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| * Ear disorder
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| * Pulmonary oedema
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| * Asthma
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| * [[Dyspnoea|Shortness of breath]]
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| * [[Epistaxis|Nose bleed]]
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| * Cough
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| * Rectal haemhorrhage
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| * [[Colitis]]
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| * [[Gastritis]]
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| * [[Dyspepsia|Indigestion]]
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| * [[Dysphagia|Difficulty swallowing]]
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| * Gastrointestinal disorder
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| * Gastrointestinal haemorrhage
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| * Bullous dermatitis
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| * [[Alopecia|Hair loss]]
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| * [[Hirsutism]]
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| * [[Hyperhidrosis]]
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| * [[Arthralgia|Joint pain]]
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| * Joint stiffness
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| * Back pain
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| * Muscle twitching
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| * [[Myalgia|Muscle aches]]
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| * [[Hyperparathyroidism]]
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| * [[Hyperkalaemia]]
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| * [[Hypocalcemia]]
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| * [[Breast cancer]]
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| * [[Sepsis]]
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| * [[Pneumonia]]
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| * Infection
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| * [[Pharyngitis]]
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| * Vaginal infection
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| * Influenza
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| * [[Hypertension|High blood pressure]]
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| * [[Hypotension]]
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| * Gait disturbance
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| * Injection site pain
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| * [[Pyrexia|Fever]]
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| * Chest pain
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| * Condition aggravated
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| * [[Asthenia|Muscle weakness]]
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| * [[Malaise]]
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| * Thirst
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| * Breast pain
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| * [[Erectile dysfunction|Impotence]]
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| * Confusional state
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| * Delirium
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| * Depersonalization
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| * Agitation
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| * Insomnia
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| * Nervousness
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| {{div col end}}
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| <sup>‡</sup> These are adverse effects only seen in patients with grade 3 or 4 chronic kidney disease.
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| <sup>†</sup> These are adverse effects only seen in patients with grade 5 chronic kidney disease.
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| ==Contraindications==
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| Contraindications include:
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| * [[Hypervitaminosis D|Vitamin D intoxication]]
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| * [[Hypercalcaemia]]
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| * Hypersensitivity to paricalcitol or any of its excipients
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| whereas cautions include:
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| * Impaired liver function
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| * It is also advised that physicians regularly monitor their patients' [[calcium]] and [[phosphorus]] levels.
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| ==Interactions==
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| Drugs that may interact with paricalcitol include:
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| {{div col|colwidth=30em}}
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| * [[Ketoconazole]], as it may interfere with paricalcitol's metabolism in the liver.
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| * [[Digitoxin]], hypercalcaemia due to any cause can exacerbate the toxicity of digitoxin.
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| * [[Thiazide]] diuretics or calcium supplements as [[hypercalcaemia]] may be induced by this combination
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| * [[Magnesium]]-containing products such as [[antacids]] may increase the risk of [[hypermagnesemia]].
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| * [[Aluminium]]-containing products such as antacids may increase the risk of [[aluminium toxicity]].
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| * Drugs that interfere with the absorption of fat-soluble vitamins, such as [[cholestyramine]] may interfere with the absorption of paricalcitol.
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| {{div col end}}
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| ==Overdose==
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| Electrolyte abnormalities (e.g. [[hypercalcaemia]] and [[hyperphosphataemia]]) are common overdose symptoms. Treatment is mostly supportive, with particular attention being paid to correcting electrolyte anomalies and reducing intake of calcium in both the form of supplementation and diet. As it is so heavily bound to plasma proteins [[haemodialysis]] is unlikely to be helpful in cases of overdose.
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| Early symptoms of overdose can include:
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| {{div col|colwidth=18em}}
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| * Weakness
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| * Headache
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| * Somnolence
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| * Nausea
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| * Vomiting
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| * Dry mouth
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| * Constipation
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| * Muscle pain
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| * Bone pain
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| * Metallic taste in the mouth.
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| {{div col end}}
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| It is worth noting, however, that may of these symptoms are also indicative of kidney failure and hence may be masked by the patient's condition.
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| </div>
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|
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| <div lang="en" dir="ltr" class="mw-content-ltr">
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| Late symptoms of overdose include:
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| {{div col|colwidth=18em}}
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| * [[Anorexia (symptom)|Loss of appetite]]
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| * Weight loss
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| * [[Conjunctivitis]] (calcific)
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| * [[Pancreatitis]]
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| * Photophobia
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| * Rhinorrhoea
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| * Pruritus
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| * Hyperthermia
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| * Decreased libido
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| * Elevated BUN
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| * Hypercholesterolaemia
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| * Elevated AST and ALT
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| * Ectopic calcification
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| * Hypertension
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| * Cardiac arrhythmias
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| * Somnolence
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| * Death
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| * Psychosis (rare)
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| {{div col end}}
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| </div>
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|
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| ==作用機序{{Anchor|Mechanism of action}}==
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| [[File:Paricalcitol structure.svg|thumb|left|パリカルシトールの3次元構造]]{{clear left}}
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| 1,25-ジヒドロキシエルゴカルシフェロールと同様に、パリカルシトールは[[vitamin D receptor/ja|ビタミンD受容体]]で[[agonist/ja|アゴニスト]]として作用し、それによって血中の[[parathyroid hormone/ja|副甲状腺ホルモン]]濃度を低下させる。
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| ==薬物動態{{Anchor|Pharmacokinetics}}==
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| パリカルシトールの血漿中濃度は、初回静脈内投与後2時間以内に急速に対数直線的に減少する。したがって、パリカルシトールの投与頻度は通常1日おき（週3回）以下であるため、複数回の投与による蓄積は期待できない。
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| {{Vitamins/ja}}
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| {{Calcium homeostasis/ja}}
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| {{Vitamin D receptor modulators/ja}}
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|
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| [[Category:Secosteroids]]
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| [[Category:Vitamin D]]
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| [[Category:Drugs developed by AbbVie]]
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