Palikalex
Palikalex Uses, Dosage, Side Effects, Food Interaction and all others data.
Palikalex is a synthetic, biologically active vitamin D analog of calcitriol with modifications to the side chain (D2) and the A (19-nor) ring. Preclinical andin vitro studies have demonstrated that paricalcitol's biological actions are mediated through binding of the VDR, which results in the selective activation of vitamin D responsive pathways. Vitamin D and paricalcitol have been shown to reduce parathyroid hormone levels by inhibiting PTH synthesis and secretion.
Secondary hyperparathyroidism is characterized by an elevation in parathyroid hormone (PTH) associated with inadequate levels of active vitamin D hormone. The source of vitamin D in the body is from synthesis in the skin and from dietary intake. Vitamin D requires two sequential hydroxylations in the liver and the kidney to bind to and to activate the vitamin D receptor (VDR). The endogenous VDR activator, calcitriol [1,25(OH)2 D3], is a hormone that binds to VDRs that are present in the parathyroid gland, intestine, kidney, and bone to maintain parathyroid function and calcium and phosphorus homeostasis, and to VDRs found in many other tissues, including prostate, endothelium and immune cells. VDR activation is essential for the proper formation and maintenance of normal bone. In the diseased kidney, the activation of vitamin D is diminished, resulting in a rise of PTH, subsequently leading to secondary hyperparathyroidism and disturbances in the calcium and phosphorus homeostasis.1 Decreased levels of 1,25(OH)2 D3 have been observed in early stages of chronic kidney disease. The decreased levels of 1,25(OH)2 D3 and resultant elevated PTH levels, both of which often precede abnormalities in serum calcium and phosphorus, affect bone turnover rate and may result in renal osteodystrophy. An in vitro study indicates that paricalcitol is not an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 or CYP3A at concentrations up to 50 nM (21 ng/mL).
Trade Name | Palikalex |
Availability | Prescription only |
Generic | Paricalcitol |
Paricalcitol Other Names | Paricalcitol |
Related Drugs | cinacalcet, Sensipar, Zemplar, Hectorol, doxercalciferol |
Type | |
Formula | C27H44O3 |
Weight | Average: 416.6365 Monoisotopic: 416.329045274 |
Protein binding | 99.8% (bound to plasma proteins) |
Groups | Approved, Investigational |
Therapeutic Class | Vitamin in bone formation, Vitamin-B preparations |
Manufacturer | |
Available Country | Argentina |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Chronic Kidney Disease Stages 3 And 4: Palikalex capsules are used for adults and pediatric patients 10 years of age and older for the prevention and treatment of secondary hyperparathyroidism associated with Chronic Kidney Disease (CKD) Stages 3 and 4.
Chronic Kidney Disease Stage 5: Palikalex capsules are used for adults and pediatric patients 10 years of age and older for the prevention and treatment of secondary hyperparathyroidism associated with CKD Stage 5 in patients on hemodialysis (HD) or peritoneal dialysis (PD).
Palikalex is also used to associated treatment for these conditions: Secondary Hyperparathyroidism (SHPT)
How Palikalex works
Palikalex is a synthetic, biologically active vitamin D analog of calcitriol with modifications to the side chain (D2) and the A (19-nor) ring. Preclinical andin vitro studies have demonstrated that paricalcitol's biological actions are mediated through binding of the VDR, which results in the selective activation of vitamin D responsive pathways. Vitamin D and paricalcitol have been shown to reduce parathyroid hormone levels by inhibiting PTH synthesis and secretion.
Dosage
Palikalex dosage
Usual Adult Dose for Secondary Hyperparathyroidism:
Initial dose:
Stage 3 or 4 Chronic Kidney Disease (CKD): Initial dosing is based on baseline intact parathyroid hormone (iPTH):
- 500 pg/mL or less: 1 mcg orally daily OR 2 mcg orally 3 times a week
- Over 500 pg/mL: 2 mcg orally daily OR 4 mcg orally 3 times a week
Stage 5 Chronic Kidney Disease (CKD):
- Starting dose (micrograms) = baseline iPTH level (pg/mL)/80
- Starting dose is given orally 3 times a week; only start if baseline serum calcium has been adjusted to 9.5 mg/dL or lower.
Usual Pediatric Dose for Secondary Hyperparathyroidism:
Safety and efficacy have not been established in pediatric patients. The following is dosing used in a very small pediatric trial. No data are available on children under 5 years old.
Initial dose, children 5 to 18 years: 0.04 mcg/kg three times per week if baseline intact parathyroid hormone (iPTH) is less than 500 pg/mL 0.08 mcg/kg three times per week if baseline iPTH is 500 pg/mL or higher. Injected as a bolus dose through a hemodialysis vascular access port at any time during dialysis
Maximum frequency: Every other day
Side Effects
Nausea, Vomiting, Edema, Palpitation, Chills, Pneumonia, Lightheadedness, GI bleeding, Flu, Sepsis, Hypokalemia, Hypercalcemia, Increase in blood creatinine
Precaution
Excessive administration of vitamin D compounds, including Palikalex Capsules, can cause over suppression of PTH, hypercalcemia, hypercalciuria, hyperphosphatemia, and adynamic bone disease.
Interaction
Digitalis; ketoconazole & other strong P450 3A inhibitors including atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole. May interfere absorption with cholestyramine (cap only). Increased risk of hypercalcemia with prescription-based phosphate or vit D-related medicinal products & Ca-containing prep or thiazide diuretics. Mg- & Al-containing prep (eg, antacids, phosphate-binders).
Food Interaction
- Avoid antacids. Avoid taking aluminum-containing antacids chronically with paricalcitol as there is an increased risk of aluminum toxicity.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4, and paricalcitol metabolism is mediated partially through CYP3A4; therefore, grapefruit may increase paricalcitol serum levels.
- Take with or without food.
Palikalex Drug Interaction
Major: calcium / vitamin d, ergocalciferol, cholecalciferolUnknown: fluticasone / salmeterol, aspirin, aspirin, nebivolol, docusate, rosuvastatin, apixaban, omega-3 polyunsaturated fatty acids, insulin glargine, furosemide, omega-3 polyunsaturated fatty acids, metoprolol, metoprolol, acetaminophen, clopidogrel, albuterol, acetaminophen
Palikalex Disease Interaction
Major: arrhythmia, electrolyte imbalance, hypercalcemiaModerate: hepatobiliary dysfunction
Volume of Distribution
- 30.8 ± 7.5 L [CKD Stage 5-HD]
- 34.9 ± 9.5 L [CKD Stage 5-PD]
- 23.8 L [healthy subjects]
Elimination Route
Well absorbed
Half Life
4 to 6 hours
Clearance
- 1.49 +/- 0.60 L/h [chronic kidney disease Stage 5 with hemodialysis]
- 1.54 +/- 0.95 L/h [chronic kidney disease Stage 5with peritoneal dialysis]
Elimination Route
Palikalex is excreted primarily by hepatobiliary excretion.
Pregnancy & Breastfeeding use
This drug should not be used during pregnancy unless the benefit outweighs the risk to the fetus.
- AU TGA pregnancy category: C
- US FDA pregnancy category: C
Lactation: Not known if distributed into breast milk, use caution
Contraindication
Hypersensitivity, Hypercalcemia, hypervitaminosis D
Innovators Monograph
You find simplified version here Palikalex
Palikalex contains Paricalcitol see full prescribing information from innovator Palikalex Monograph, Palikalex MSDS, Palikalex FDA label