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Paricalcitol: Difference between revisions

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Created page with "{{short description|Chemical compound}} {{Drugbox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 445909355 | 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 | image = Paricalcitol.svg | width = 200px | image2 = Paricalcitol3Dan.gif | width2 = 200px <!--Clinical data--> | tradename = Zemplar | Drugs.com = {{drugs.com|monograph|paricalcitol}} | MedlinePlus..."
 
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{{short description|Chemical compound}}
{{short description|Chemical compound}}
{{Drugbox
{{Drugbox
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| routes_of_administration = Oral, Intravenous
| routes_of_administration = Oral, Intravenous
<!--Pharmacokinetic data-->
<!--Pharmacokinetic data-->
| bioavailability = 72%<ref name = MSR/>
| bioavailability = 72%
| protein_bound = 99.8%<ref name = MSR/>
| protein_bound = 99.8%
| metabolism = [[Hepatic]]<ref name = MSR/>
| metabolism = [[Hepatic]]
| elimination_half-life = 14-20 hours<ref name = MSR/>
| elimination_half-life = 14-20 hours
| excretion = Faeces (74%), urine (16%)<ref name = MSR/>
| excretion = Faeces (74%), urine (16%)
<!--Identifiers-->
<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number_Ref = {{cascite|correct|??}}
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'''Paricalcitol''' (chemically it is '''19-nor-1,25-(OH)<sub>2</sub>-vitamin D<sub>2</sub>'''. Marketed by [[Abbott Laboratories]] under the trade name '''Zemplar''') is a [[pharmaceutical drug|drug]] used for the prevention and treatment of [[secondary hyperparathyroidism]] (excessive secretion of [[parathyroid hormone]]) associated with [[chronic kidney failure]]. It is an [[analog (chemistry)|analog]] of 1,25-dihydroxyergocalciferol, the active form of [[Vitamin D2|vitamin D<sub>2</sub>]] (ergocalciferol).
'''Paricalcitol''' (chemically it is '''19-nor-1,25-(OH)<sub>2</sub>-vitamin D<sub>2</sub>'''. Marketed by [[Abbott Laboratories]] under the trade name '''Zemplar''') is a [[pharmaceutical drug|drug]] used for the prevention and treatment of [[secondary hyperparathyroidism]] (excessive secretion of [[parathyroid hormone]]) associated with [[chronic kidney failure]]. It is an [[analog (chemistry)|analog]] of 1,25-dihydroxyergocalciferol, the active form of [[Vitamin D2|vitamin D<sub>2</sub>]] (ergocalciferol).


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<!-- Society and culture -->
It was patented in 1989 and approved for medical use in 1998.
It was patented in 1989 and approved for medical use in 1998.


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==Medical uses==
==Medical uses==
Its primary use in medicine is in the treatment of secondary [[hyperparathyroidism]] associated with [[chronic kidney disease]]. However current evidence is not sufficient to demonstrate an advantage of paricalcitol over non-selective vitamin D derivatives for this indication.
Its primary use in medicine is in the treatment of secondary [[hyperparathyroidism]] associated with [[chronic kidney disease]]. However current evidence is not sufficient to demonstrate an advantage of paricalcitol over non-selective vitamin D derivatives for this indication.


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==Adverse effects==
==Adverse effects==
'''Adverse effects by frequency:'''<br />
'''Adverse effects by frequency:'''<br />
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* Nausea
* Nausea


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'''Common (1-10% frequency):'''
'''Common (1-10% frequency):'''
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'''Uncommon (0.1-1% frequency):'''
'''Uncommon (0.1-1% frequency):'''
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<sup>‡</sup> These are adverse effects only seen in patients with grade 3 or 4 chronic kidney disease.  
<sup>‡</sup> These are adverse effects only seen in patients with grade 3 or 4 chronic kidney disease.  
<sup>†</sup> These are adverse effects only seen in patients with grade 5 chronic kidney disease.
<sup>†</sup> These are adverse effects only seen in patients with grade 5 chronic kidney disease.


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==Contraindications==
==Contraindications==
Contraindications include:
Contraindications include:
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* Hypersensitivity to paricalcitol or any of its excipients
* Hypersensitivity to paricalcitol or any of its excipients


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whereas cautions include:
whereas cautions include:
* Impaired liver function
* Impaired liver function
* It is also advised that physicians regularly monitor their patients' [[calcium]] and [[phosphorus]] levels.
* It is also advised that physicians regularly monitor their patients' [[calcium]] and [[phosphorus]] levels.


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==Interactions==
==Interactions==
Drugs that may interact with paricalcitol include:
Drugs that may interact with paricalcitol include:
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==Overdose==
==Overdose==
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.<ref name = EMC/> As it is so heavily bound to plasma proteins [[haemodialysis]] is unlikely to be helpful in cases of overdose.
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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Early symptoms of overdose can include:
Early symptoms of overdose can include:
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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.
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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Late symptoms of overdose include:
Late symptoms of overdose include:
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==Mechanism of action==
==Mechanism of action==
[[File:Paricalcitol structure.svg|thumb|left|3D structure of paricalcitol]]{{clear left}}
[[File:Paricalcitol structure.svg|thumb|left|3D structure of paricalcitol]]{{clear left}}
Like 1,25-dihydroxyergocalciferol, paricalcitol acts as an [[agonist]] at the [[vitamin D receptor]] and thereby lowers [[parathyroid hormone]] levels in the blood.
Like 1,25-dihydroxyergocalciferol, paricalcitol acts as an [[agonist]] at the [[vitamin D receptor]] and thereby lowers [[parathyroid hormone]] levels in the blood.


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==Pharmacokinetics==
==Pharmacokinetics==
The plasma concentration of paricalcitol decreases rapidly and log-linearly within two hours after initial intravenous administration. Therefore, it is not expected to accumulate with multiple dosing, since paricalcitol is usually given no more frequently than every other day (3 times per week).
The plasma concentration of paricalcitol decreases rapidly and log-linearly within two hours after initial intravenous administration. Therefore, it is not expected to accumulate with multiple dosing, since paricalcitol is usually given no more frequently than every other day (3 times per week).


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{{Vitamins}}
{{Vitamins}}
{{Calcium homeostasis}}
{{Calcium homeostasis}}
{{Vitamin D receptor modulators}}
{{Vitamin D receptor modulators}}


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{{二次利用|date=20 December 2023}}
{{二次利用|date=20 December 2023}}
[[Category:Secosteroids]]
[[Category:Secosteroids]]
[[Category:Vitamin D]]
[[Category:Vitamin D]]
[[Category:Drugs developed by AbbVie]]
[[Category:Drugs developed by AbbVie]]
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