pasireotide

Contraindicated in:

Severe hepatic impairment.

Use Cautiously in:

Poorly controlled diabetes mellitus (blood sugar should be controlled prior to therapy);
Acute illness, infection, pancreatic surgery, pancreatic malignancy, or alcohol abuse (↑ risk of ketoacidosis);
Cardiac disease and/or risk factors for bradycardia, including high-grade heart block or concomitant use of drugs associated with bradycardia (dose adjustments of beta blockers, calcium channel blockers, or correction of electrolyte disturbances may be necessary);
Patients at risk of QT interval prolongation, including congenital long QT prolongation; uncontrolled/significant cardiac disease, including recent MI, HF, unstable angina, or bradycardia; on antiarrhythmic therapy or other substances that are known to cause QT interval prolongation, hypokalemia, and/or hypomagnesemia (correct prior to administration);
Moderate hepatic impairment (dose ↓ required);
OB: Safety not established in pregnancy or lactation;
Pedi: Safety and effectiveness not established in children;
Geri: Initial lower dose recommended in older adults, taking into account ↑ frequency of altered hepatic, renal, or cardiac function; concomitant diseases; or other drug therapy.

Adv. Reactions/Side Effects ⬆ ⬇

CV: , hypertension, peripheral edema, , QT INTERVAL PROLONGATION, BRADYCARDIA, hypotension

Derm: alopecia, injection site reactions, pruritus

Endo: hyperglycemia, adrenal insufficiency, hypocortisolism, hypoglycemia, KETOACIDOSIS, pituitary hormone deficiency

F and E: hypokalemia

GI: abdominal pain, anorexia , cholelithiasis, diarrhea, nausea, ↑amylase, ↑liver enzymes, abdominal bloating, cholecystitis, constipation, fat malabsorption, steatorrhea, stool discoloration, vomiting

Hemat: ↑prothrombin time, anemia

Metab: ↑lipase, hypercholesterolemia, weight loss

MS: arthralgia, back pain, extremity pain, myalgia

Neuro: fatigue, headache, anxiety, dizziness, insomnia, vertigo

Interactions ⬆ ⬇

Drug-drug:

QT interval prolonging drugs↑ risk of serious arrhythmias.
May ↓ absorption and effects of cyclosporine; dose adjustment of cyclosporine may be necessary.
May ↑ blood levels and effect of bromocriptine; dose ↓ of bromocriptine may be necessary.

Availability ⬆ ⬇

Powder for intramuscular injection (Signifor LAR): 10 mg/vial; 20 mg/vial; 30 mg/vial; 40 mg/vial; 60 mg/vial
Solution for SUBQ injection (Signifor): 0.3 mg/mL; 0.6 mg/mL; 0.9 mg/mL

Route/Dosage ⬆ ⬇

Cushing's Disease

SUBQ (Adults ): Signifor: 0.6 mg or 0.9 mg twice daily (range 0.3–0.9 mg twice daily based on response/tolerability).

Hepatic Impairment

SUBQ (Adults ): Moderate hepatic impairment (Signifor): 0.3 mg twice a day initially (max dose: 0.6 mg twice a day).
IM (Adults ): Signifor LAR: 10 mg every 4 wk; after 4 mo, if inadequate response, may ↑ to 40 mg every 4 wk.

Hepatic Impairment

IM (Adults ): Moderate hepatic impairment (Signifor LAR): 10 mg every 4 wk; after 4 mo, if inadequate response, may ↑ to 20 mg every 4 wk.

Acromegaly

IM (Adults ): Signifor LAR: 40 mg every 4 wk; after 3 mo, if inadequate response, may ↑ to 60 mg every 4 wk.

Hepatic Impairment

IM (Adults ): Moderate hepatic impairment: 20 mg every 4 wk; after 3 mo, if inadequate response, may ↑ to 40 mg every 4 wk.

US Brand Names ⬆ ⬇

Signifor, Signifor LAR

Action ⬆ ⬇

Acts as a somatostatin analogue, binding to and activating somatostatin receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.

Therapeutic effects:

Improvement in clinical manifestations of Cushing's disease.
Reduction in growth hormone concentrations and normalization of insulin-like growth factor 1 (IGF-1) concentrations.

Classifications ⬆ ⬇

Therapeutic Classification: hormones

Pharmacologic Classification: somatostatin analogues

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Widely distributed, existing primarily in plasma.

Metabolism/Excretion: Eliminated mainly via hepatic clearance (biliary excretion) with small amounts renally excreted.

Half-Life: 12 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
SUBQ‡	within 1 mo	2 mo	unknown
IM‡	unknown	3 mo	unknown

‡↓in urinary free cortisol.

‡Plasma concentrations.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Advise patient to notify health care professional of excessive thirst, high urine output, ↑ appetite with weight loss, or tiredness, or if they experience new or worsening symptoms of fat in their stool, stool discoloration, loose stools, or abdominal bloating.
Rep: Advise females of reproductive potential that therapy with pasireotide may result in improved fertility. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

55292- Recordati Rare Diseases, Inc.
- 55292-131- Signifor
  - 55292-131-60- 60 PACKAGE in 1 BOX (55292-131-60) / 6 AMPULE in 1 PACKAGE (55292-131-06) / 1 mL in 1 AMPULE (55292-131-01)

55292- Recordati Rare Diseases, Inc.
- 55292-132- Signifor
  - 55292-132-60- 60 PACKAGE in 1 BOX (55292-132-60) / 6 AMPULE in 1 PACKAGE (55292-132-06) / 1 mL in 1 AMPULE (55292-132-01)

55292- Recordati Rare Diseases, Inc.
- 55292-133- Signifor
  - 55292-133-60- 60 PACKAGE in 1 BOX (55292-133-60) / 6 AMPULE in 1 PACKAGE (55292-133-06) / 1 mL in 1 AMPULE (55292-133-01)

55292- Recordati Rare Diseases, Inc.
- 55292-139- Signifor LAR
  - 55292-139-01- 1 KIT in 1 KIT (55292-139-01) * 6 mL in 1 VIAL, SINGLE-USE (55292-134-01) * 2 mL in 1 SYRINGE

55292- Recordati Rare Diseases, Inc.
- 55292-140- Signifor LAR
  - 55292-140-01- 1 KIT in 1 KIT (55292-140-01) * 6 mL in 1 VIAL, SINGLE-USE (55292-135-01) * 2 mL in 1 SYRINGE

55292- Recordati Rare Diseases, Inc.
- 55292-141- Signifor LAR
  - 55292-141-01- 1 KIT in 1 KIT (55292-141-01) * 6 mL in 1 VIAL, SINGLE-USE (55292-136-01) * 2 mL in 1 SYRINGE

55292- Recordati Rare Diseases, Inc.
- 55292-142- Signifor LAR
  - 55292-142-01- 1 KIT in 1 KIT (55292-142-01) * 6 mL in 1 VIAL, SINGLE-USE (55292-137-01) * 2 mL in 1 SYRINGE

55292- Recordati Rare Diseases, Inc.
- 55292-143- Signifor LAR
  - 55292-143-01- 1 KIT in 1 KIT (55292-143-01) * 6 mL in 1 VIAL, SINGLE-USE (55292-138-01) * 2 mL in 1 SYRINGE

71161- Synergy Health AST, LLC
- 71161-126-
  - 71161-126-01- 6 mL in 1 VIAL, SINGLE-USE (71161-126-01)

71161- Synergy Health AST, LLC
- 71161-127-
  - 71161-127-01- 6 mL in 1 VIAL, SINGLE-USE (71161-127-01)

71161- Synergy Health AST, LLC
- 71161-128-
  - 71161-128-01- 6 mL in 1 VIAL, SINGLE-USE (71161-128-01)

71161- Synergy Health AST, LLC
- 71161-129-
  71161-129-01- 6 mL in 1 VIAL, SINGLE-USE (71161-129-01)

71161- Synergy Health AST, LLC
- 71161-130-
  71161-130-01- 6 mL in 1 VIAL, SINGLE-USE (71161-130-01)

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Classifications ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

Code ⬆