Pasireotide
Pasireotide Uses, Dosage, Side Effects, Food Interaction and all others data.
Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, which is used in the treatment of Cushing's disease.
Signifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.
| Trade Name | Pasireotide |
| Availability | Prescription only |
| Generic | Pasireotide |
| Pasireotide Other Names | Pasireotida, Pasiréotide, Pasireotide, Pasireotidum |
| Related Drugs | dexamethasone, Decadron, cyproheptadine, octreotide, bromocriptine, mifepristone, Sandostatin, lanreotide, Somatuline Depot |
| Weight | 10mg, 20mg, 30mg, 40mg, 60mg, 0.3mg/ml, 0.6mg/ml, 0.9mg/ml, |
| Type | Intramuscular Powder For Injection, Extended Release, Subcutaneous Solution, Subcutaneous |
| Formula | C58H66N10O9 |
| Weight | Average: 1047.2062 Monoisotopic: 1046.50142376 |
| Protein binding | Plasma protein binding is 88%. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pasireotide is a somatostatin analog used in the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery is not appropriate.
For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
Pasireotide is also used to associated treatment for these conditions: Acromegaly, Cushing's Disease
How Pasireotide works
Pasireotide activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.
Toxicity
The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.
Food Interaction
No interactions found.Pasireotide Drug Interaction
Major: lithium, sotalolModerate: diltiazem, glycerin, metoprolol, metoprololMinor: sulfamethoxazole / trimethoprimUnknown: charcoal, ubiquinone, copper gluconate, glucose, heparin, sodium iodide, arginine, levocarnitine, cysteine, acetaminophen, bioflavonoids, vitamin a topical, bioflavonoids
Pasireotide Disease Interaction
Major: hepatic impairmentModerate: QT prolongation, adrenal insufficiency, bradycardia, cholelithiasis, diabetes
Volume of Distribution
Pasireotide is widely distributed and has a volume of distribution of >100L.
Elimination Route
The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.
Half Life
The half-life is 12 hours.
Clearance
The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.
Elimination Route
Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).
Innovators Monograph
You find simplified version here Pasireotide
