pasireotide

REMS

Signifor:

Treatment of Cushing’s disease when surgery is not an option or has not resulted in cure

Signifor LAR:

Treatment of the following conditions:
- Acromegaly when surgery is not an option or has not resulted in an adequate response;
- Cushing’s disease when surgery is not an option or has not resulted in cure.

Contraindicated in:

Severe hepatic impairment (Child Pugh C).

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: Lactation: 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.

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 distention, cholecystitis, constipation, vomiting.

Hemat: ↑ prothrombin time, anemia.

Metab: ↑ lipase, hypercholesterolemia.

MS: arthralgia, back pain, extremity pain, myalgia.

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

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).

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;

Cushing's Disease

SC (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

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

Signifor, Signifor LAR

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 concentrations.

Therapeutic Classification: hormones

Pharmacologic Classification: somatostatin analogues

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.

(†decrease in urinary free cortisol; ‡ blood levels)

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

†Decrease in urinary free cortisol.

‡Blood levels.

Instruct patient in correct technique for injection, care and disposal of equipment. Advise patient to read Medication Guide prior to using and with each Rx refill, in case of changes.
Advise patient to notify health care professional if signs and symptoms of hypocortisolism and hyperglycemia (excessive thirst, high urine output, increased appetite with weight loss, tiredness) occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications
Rep: Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Therapy may cause improved fertility; discuss potential for unintended pregnancy with premenopausal women.

NDC Code^*

0078- Novartis Pharmaceuticals Corporation
0078-0633- Signifor 0078-0633-20- 60 PACKAGE in 1 BOX (0078-0633-20) > 6 AMPULE in 1 PACKAGE (0078-0633-06) > 1 mL in 1 AMPULE (0078-0633-61)

0078- Novartis Pharmaceuticals Corporation
0078-0634- Signifor 0078-0634-20- 60 PACKAGE in 1 BOX (0078-0634-20) > 6 AMPULE in 1 PACKAGE (0078-0634-06) > 1 mL in 1 AMPULE (0078-0634-61)

0078- Novartis Pharmaceuticals Corporation
0078-0635- Signifor 0078-0635-20- 60 PACKAGE in 1 BOX (0078-0635-20) > 6 AMPULE in 1 PACKAGE (0078-0635-06) > 1 mL in 1 AMPULE (0078-0635-61)

0078- Novartis Pharmaceuticals Corporation
0078-0641- Signifor LAR 0078-0641-81- 1 KIT in 1 KIT (0078-0641-81) * 6 mL in 1 VIAL, SINGLE-USE (0078-0762-61) * 2 mL in 1 SYRINGE

0078- Novartis Pharmaceuticals Corporation
0078-0642- Signifor LAR 0078-0642-81- 1 KIT in 1 KIT (0078-0642-81) * 6 mL in 1 VIAL, SINGLE-USE (0078-0776-61) * 2 mL in 1 SYRINGE

0078- Novartis Pharmaceuticals Corporation
0078-0643- Signifor LAR 0078-0643-81- 1 KIT in 1 KIT (0078-0643-81) * 6 mL in 1 VIAL, SINGLE-USE (0078-0783-61) * 2 mL in 1 SYRINGE

0078- Novartis Pharmaceuticals Corporation
0078-0741- Signifor LAR 0078-0741-81- 1 KIT in 1 KIT (0078-0741-81) * 6 mL in 1 VIAL, SINGLE-USE (0078-0769-61) * 2 mL in 1 SYRINGE

0078- Novartis Pharmaceuticals Corporation
0078-0748- Signifor LAR 0078-0748-81- 1 KIT in 1 KIT (0078-0748-81) * 6 mL in 1 VIAL, SINGLE-USE (0078-0755-61) * 2 mL in 1 SYRINGE

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