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Paricalcitol (chemically it is 19-nor-1,25-(OH)2-vitamin D2. Marketed by Abbott Laboratories under the trade name Zemplar) is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic kidney failure. It is an analog of 1,25-dihydroxyergocalciferol, the active form of vitamin D2 (ergocalciferol).

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

(2025). 9783527607495, John Wiley & Sons. .


Medical uses
Its primary use in medicine is in the treatment of secondary hyperparathyroidism associated with chronic kidney disease.
(2025). 9780980579093, The Australian Medicines Handbook Unit Trust.
However a 2016 systematic review did not find evidence sufficient to demonstrate an advantage of paricalcitol over non-selective vitamin D derivatives for this indication.


Adverse effects
Adverse effects by frequency:

Very common (>10% frequency):

  • Nausea

Common (1-10% frequency):

  • Diarrhoea
  • Allergic reaction
  • Dizziness
  • Stomach discomfort
  • Gastroesophageal reflux disease
  • Hyperphosphataemia
  • Decreased appetite
  • Headache
  • Breast tenderness
  • Taste changes
  • Hypoparathyroidism
  • Vertigo
  • Rash

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

whereas cautions include:

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


Interactions
Drugs that may interact with paricalcitol include:

  • , as it may interfere with paricalcitol's metabolism in the liver.
  • , hypercalcaemia due to any cause can exacerbate the toxicity of digitoxin.
  • diuretics or calcium supplements as may be induced by this combination
  • -containing products such as may increase the risk of .
  • -containing products such as antacids may increase the risk of aluminium toxicity.
  • Drugs that interfere with the absorption of fat-soluble vitamins, such as may interfere with the absorption of paricalcitol.


Overdose
Electrolyte abnormalities (e.g. 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 is unlikely to be helpful in cases of overdose.

Early symptoms of overdose can include:

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

However, many of these symptoms are also indicative of kidney failure and hence may be masked by the patient's condition.

Late symptoms of overdose include:

  • Loss of appetite
  • Weight loss
  • (calcific)
  • 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
Like 1,25-dihydroxyergocalciferol, paricalcitol acts as an at the vitamin D receptor and thereby lowers parathyroid hormone levels in the blood.


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).Rxlist: Zemplar

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