pasireotide (Rx)

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Brand and Other Names:Signifor, Signifor LAR

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

SC injection solution (Signifor)

  • 0.3mg/mL
  • 0.6mg/mL
  • 0.9mg/mL

IM injection suspension (Signifor LAR)

  • 20mg/vial
  • 40mg/vial
  • 60mg/vial
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Cushing Disease

Indicated for treatment of adults with Cushing disease in whom pituitary surgery is not an option or has not been curative

Signifor: 0.6-0.9 mg SC BID initially; titrate dose based on response and tolerability

Dosage range: 0.3-0.9 mg SC BID

Dosage Modifications (Cushing Disease)

If started on 0.6 mg BID, a dosage increase to 0.9 mg BID may be considered if treatment tolerated

Temporarily reduce dose for significant adverse effects by decrements of 0.3 mg/injection

Renal impairment: No dosage adjustment required

Hepatic impairment (Cushing Disease)

  • Moderate (Child Pugh B): 0.3 mg SC BID initially; not to exceed 0.6 mg BID
  • Severe (Child Pugh C): Avoid use

Acromegaly

Indicated for the treatment of patients with acromegaly who have had an inadequate response to surgery and/or for whom surgery is not an option

Signifor LAR (initial dose): 40 mg IM q4wk

If tolerated, may increase dose to a maximum of 60 mg for patients who have not normalized growth hormone (GH) and/or age and sex adjusted insulin-like growth factor-1 (IGF-1) levels after 3 months of treatment with 40 mg

Dosage Modifications (Acromegaly)

Renal impairment: No dosage adjustment required

Adverse effect/over-response

  • Adverse reactions or over-response to treatment (age and sex adjusted IGF-1 less than the lower limit of normal) may require dose reduction
  • Decrease the dose, either temporarily or permanently, by 20 mg decrements

Hepatic impairment

  • Mild (Child-Pugh C): No dosage adjustment required
  • Moderate (Child-Pugh B): 20 mg IM q4wk; not to exceed 40 mg q4wk
  • Severe (Child-Pugh C): Avoid use

Dosing Considerations

Evaluation for treatment response is based on reduction in 24-hr urinary free cortisol levels and/or improvement in disease signs and symptoms

Maximum urinary free cortisol reduction typically seen by 2 months of treatment

Continue treatment as long as benefit is derived

Intensively optimize antidiabetic therapy (if blood glucose poorly controlled) before initiating pasireotide

Baseline tests

  • Obtain the following before initiating:
  • -Fasting plasma glucose
  • -Hemoglobin A1c
  • -Liver tests
  • -Electrocardiogram
  • -Gallbladder ultrasound

Administration

SC injection (Signifor)

  • Visually inspect solution for particulate matter and discoloration; do not use if particulates and/or discoloration observed
  • Avoid injection in sites showing signs of inflammation or irritation
  • Gently pinch skin at the injection site and hold the needle/syringe at an angle of approximately 45 degrees
  • Administer SC by self-injection into the top of thigh or abdomen
  • Rotate injection sites; use of the same injection site for 2 consecutive injections is not recommended

IM injection (Signafor LAR)

  • Remove kit from refrigerator and let it sit for at least 30 min (but not longer than 24 hr)
  • Reconstitute with supplied diluent until powder is completely suspended (see package instructions)
  • Insert the needle fully into the left or right gluteus at a 90° angle to the skin
  • Slowly pull back the plunger to check that no blood vessel has been penetrated (reposition if a blood vessel has been penetrated)
  • Slowly depress the plunger until the syringe is empty
  • Withdraw the needle from the injection site and activate the safety guard

Safety and efficacy not established

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Interactions

Interaction Checker

and pasireotide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Diarrhea (58%)

            Nausea (52%)

            Hyperglycemia (40%)

            Cholelithiasis (30%)

            Headache (28%)

            Abdominal pain (24%)

            Fatigue (19%)

            Diabetes mellitus (18%)

            Injection site reactions (17%)

            Nasopharyngitis (13%)

            Alopecia (12%)

            Asthenia (11%)

            Increased A1c (11%)

            1-10%

            Increased ALT (10%)

            Increased GGT (10%)

            Edema, peripheral (10%)

            Upper abdominal pain (10%)

            Decreased appetite (10%)

            Hypercholesterolemia (10%)

            Hypertension (10%)

            Dizziness (9%)

            Hypoglycemia (9%)

            Type 2 diabetes mellitus (9%)

            Anxiety (9%)

            Influenza (9%)

            Insomnia (9%)

            Myalgia (9%)

            Arthralgia (8%)

            Pruritus (8%)

            Increased lipase (7%)

            Constipation (7%)

            Hypotension (7%)

            Vomiting (7%)

            Back pain (6%)

            Dry skin (6%)

            Prolonged QT interval (6%)

            Hypokalemia (6%)

            Pain in extremity (6%)

            Sinus bradycardia (6%)

            Vertigo (6%)

            Abdominal distension (6%)

            Adrenal insufficiency (6%)

            Increased AST (6%)

            Increased blood glucose (6%)

            Anemia (4%)

            Increased amylase (2%)

            Prolonged PTT (2%)

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            Warnings

            Contraindications

            None

            Cautions

            Suppresses ACTH, which may lead to decreased cortisol and potential hypocortisolism; monitor for weakness, fatigue, anorexia, nausea, vomiting, hypotension, hyponatremia, or hypoglycemia

            Nearly all patients develop worsening glycemia in first 2 weeks of treatment; higher risk in poorly controlled diabetics (ie, HBA1c >8%)

            May cause bradycardia and QT prolongation; obtain baseline and periodic ECG, and potassium and magnesium levels; correct/supplement potassium and /or magnesium if clinically warranted

            Increased liver enzymes may require dose interruption and reduction

            Cholelithiasis reported; perform gallbladder ultrasound at baseline and at 6- to 12-months

            Monitor for pituitary hormone deficiency (eg, TSH/free T4, GH/IGF-1)

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown whether distributed in human breast milk; excreted in rat milk at levels 30% of the plasma level; cannot exclude risk to breastfeeding children

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Cyclohexapeptide somatostatin analog; binds to human somatostatin receptors (hsst) 1, 2, 3, 4 and 5

            Absorption

            Peak plasma time: 0.25-.5 hr

            Distribution

            Protein bound: 88%

            Vd: >100 L

            P-gp substrate (low)

            Metabolism

            Since somatropin increases CYP450 enzymes, suppression of growth hormone secretion by somatostatin analogs may decrease clearance of compounds metabolized by CYP450 enzymes

            Elimination

            Total body clearance: 3.8 L/hr

            Excretion: bile (main), renal (small)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
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