Paricalcitol

Source: Wikipedia, the free encyclopedia.
Paricalcitol
Clinical data
Trade namesZemplar
Other names(1R,3S)-5-[2-[(1R,3aR,7aS)-1-[(2R,5S)-6-hydroxy-5,6-dimethyl-3E-hepten-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-cyclohexane-1,3-diol
AHFS/Drugs.comMonograph
MedlinePlusa682335
Pregnancy
category
  • AU: C
Routes of
administration
Oral, Intravenous
ATC code
Legal status
Legal status
Hepatic[1]
Elimination half-life14-20 hours[1]
ExcretionFaeces (74%), urine (16%)[1]
Identifiers
  • (1R,3R,7E,17β)-17-[(1R,2E,4S)-5-hydroxy-1,4,5-trimethylhex-2-en-1-yl]-9,10-secoestra-5,7-diene-1,3-diol
ECHA InfoCard
100.184.862 Edit this at Wikidata
Chemical and physical data
FormulaC27H44O3
Molar mass416.646 g·mol−1
  • InChI=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 checkY
  • Key:BPKAHTKRCLCHEA-UBFJEZKGSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Paricalcitol (chemically it is 19-nor-1,25-(OH)2-vitamin D2. Marketed by

vitamin D2
(ergocalciferol).

It was patented in 1989 and approved for medical use in 1998.[2]

Medical uses

Its primary use in medicine is in the treatment of secondary hyperparathyroidism associated with chronic kidney disease.[3] However current evidence is not sufficient to demonstrate an advantage of paricalcitol over non-selective vitamin D derivatives for this indication.[4]

Adverse effects

Adverse effects by frequency:[1][3][5][6]
Very common (>10% frequency):

  • Nausea

Common (1-10% frequency):

Uncommon (0.1-1% frequency):

These are adverse effects only seen in patients with grade 3 or 4 chronic kidney disease. These are adverse effects only seen in patients with grade 5 chronic kidney disease.

Contraindications

Contraindications include:[6]

  • Vitamin D intoxication
  • Hypercalcaemia
  • Hypersensitivity to paricalcitol or any of its excipients

whereas cautions include:[1]

  • Impaired liver function
  • It is also advised that physicians regularly monitor their patients' calcium and phosphorus levels.

Interactions

Drugs that may interact with paricalcitol include:[1][6]

Overdose

Electrolyte abnormalities (e.g.

haemodialysis is unlikely to be helpful in cases of overdose.[6]

Early symptoms of overdose can include:[6]

  • Weakness
  • Headache
  • Somnolence
  • Nausea
  • Vomiting
  • Dry mouth
  • Constipation
  • Muscle pain
  • Bone pain
  • Metallic taste in the mouth.

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.[6]

Late symptoms of overdose include:

  • Loss of appetite
  • Weight loss
  • Conjunctivitis (calcific)
  • Pancreatitis
  • Photophobia
  • Rhinorrhoea
  • Pruritus
  • Hyperthermia
  • Decreased libido
  • Elevated BUN
  • Hypercholesterolaemia
  • Elevated AST and ALT
  • Ectopic calcification
  • Hypertension
  • Cardiac arrhythmias
  • Somnolence
  • Death
  • Psychosis (rare)

Mechanism of action

3D structure of paricalcitol

Like 1,25-dihydroxyergocalciferol, paricalcitol acts as an agonist at the vitamin D receptor and thereby lowers parathyroid hormone levels in the blood.[1]

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).[7][8]

References

  1. ^ a b c d e f g h i "Zemplar (paricalcitol) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 26 January 2014.
  2. .
  3. ^ .
  4. .
  5. ^ "PARICALCITOL capsule, liquid filled [Teva Pharmaceuticals USA Inc]" (PDF). DailyMed. Teva Pharmaceuticals USA Inc. September 2013. Retrieved 26 January 2014.
  6. ^ a b c d e f g h "Zemplar Soft Capsules 1 mcg - Summary of Product Characteristics". electronic Medicines Compendium. AbbVie Limited. 15 April 2013. Retrieved 26 January 2014.
  7. ^ Rxlist: Zemplar
  8. ^ "Zemplar (paricalcitol) [prescribing information]". North Chicago, IL: AbbVie Inc. October 1, 2015. Retrieved December 12, 2016.