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granisetron (Rx)Brand and Other Names:Granisol Oral Solution, Sustol, more...Sancuso

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • Avalailable as generics
  • 0.1mg/mL
  • 1mg/mL

extended relase SC injection

  • 10mg/0.4mL single-dose prefilled syringe (Sustol)

patch

  • 3.1mg/24hr (Sancuso)

tablets

  • 1mg (generic)

oral solution

  • 1mg/5mL (Granisol)
more...

Chemotherapy Induced Nausea & Vomiting

Oral

  • 1 mg PO 1 hr before chemotherapy, then 1 mg 12 hr after 1st dose; OR 2 mg 1 hr before chemotherapy

IV

  • 0.01 mg/kg/dose infused over 5 min or direct injected over 30 sec, 30 min before chemotherapy  

Patch (Sancuso)

  • 1 patch 24-48 hr before chemotherapy; keep at least 24 hr post-chemo treatment
  • May wear same patch for up to 7 days

SC (Sustol)

  • Indicated in combination with other antiemetics in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination chemotherapy regimens
  • 10 mg SC in combination with dexamethasone at least 30 minutes before the initiation of MEC or AC combination chemotherapy
  • Administer on Day 1 of chemotherapy and not more frequently than once q7days because of the extended-release properties of the formulation
  • Also see Administration
  • Dexamethasone with Sustol
    • MEC regimen: Dexamethasone 8 mg IV on Day 1
    • AC combination chemotherapy regimens: Dexamethasone 20 mg IV on Day 1, followed by 8 mg PO BID on Days 2, 3, and 4
    • If administered with an NK1 receptor antagonist, see the prescribing information of the NK1 receptor antagonist for the recommended dexamethasone dosage

Radiation-Induced Nausea & Vomiting

2 mg PO, 1 hr before radiation treatment

Postoperative Nausea & Vomiting

Prevention: 1 mg (undiluted) IV push over 30 seconds; administer before anesthetic induction or immediately before reversal of anesthesia

Treatment: 1 mg (undiluted) IV push over 30 seconds

Dosage Modifications

Renal impairment

  • SC (Sustol)
    • Moderate (CrCl 30-59 mL/min): Administer on Day 1 of chemotherapy and not more frequently than once q14days
    • Severe (CrCl <30 mL/min): Avoid use
  • IV
    • Severe (CrCl <30 mL/min): Total clearance was not affected in patients with severe renal failure who received a single 40 mcg/kg IV dose
  • PO
    • No dosage adjustment required

Hepatic impairment

  • No dosage adjustment required

Dosage Forms & Strengths

injectable solution

  • 0.1mg/mL
  • 1mg/mL
more...

Chemotherapy Induced Nausea & Vomiting

<2 years: Safey and efficacy not established

2-16 years: As adults; 0.01 mg/kg infused over 5 min or direct inj over 30 sec, 30 min before chemotherapy 

Oral administration: Currently FDA-approved for IV administration in children; safety and efficacy of oral administration is not established

Postoperative Nausea & Vomiting

Safety and efficacy not established

Not approved for postoperative N/V in pediatric patients because of lack of efficacy and QT prolongation observed in clinical trials

Chemotherapy Induced Nausea & Vomiting

Oral: 2 mg 1 hr before chemotherapy, then 1 mg 12 hr after 1st dose; OR 2 mg 1 hr before chemo

IV: 0.01 mg/kg/dose infused over 5 min or direct injected over 30 sec, 30 min before chemotherapy 

Patch: 1 patch 24-48 hr before chemotherapy; keep at least 24 hr post-chemo treatment; may wear same patch for up to 7 days

Extended-release SC: 10 mg SC in combination with dexamethasone at least 30 minutes before the initiation of MEC or AC combination chemotherapy

Radiation-Induced Nausea & Vomiting

2 mg PO, 1 hr before radiation treatment

Postoperative Nausea & Vomiting

Prevention: 1 mg (undiluted) IV push over 30 seconds; administer before anesthetic induction or immediately before reversal of anesthesia

Treatment: 1 mg (undiluted) IV push over 30 seconds

Renal impairment

SC (Sustol): Moderate (CrCl 30-59 mL/min): Administer on Day 1 of chemotherapy and not more frequently than once q14days

SC (Sustol): Severe (CrCl <30 mL/min): Avoid use

IV: Severe (CrCl <30 mL/min): Total clearance was not affected in patients with severe renal failure who received a single 40 mcg/kg IV dose

PO: No dosage adjustment required

Hepatic impairment

No dosage adjustment required

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Interactions

Interaction Checker

granisetron and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (10-21%)

            1-10%

            Diarrhea (1-9%)

            Constipation (3-18%)

            Asthenia (5%)

            Somnolence (10%)

            Sedation (10%)

            Drowsiness (10%)

            Frequency Not Defined

            Anxiety

            Fatigue

            Malaise

            Increased LFTs

            Postmarketing reports

            Administration site reactions: Pain, pruritus, erythema, rash, irritation, vesicles, burn, discoloration, urticaria

            Cardiac Disorders: bradycardia, chest pain, palpitations, sick sinus syndrome

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            Warnings

            Contraindications

            Hypersensitivity

            Coadministration with apomorphine; combination reported to cause profound hypotension and loss of consciousness

            Cautions

            Liver disease

            May mask paralytic ileus/gastric distension

            Cross-sensitivity among selective 5-HT antagonists may occur

            Serotonin syndrome reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs including SSRIs, SNRIs, MAO inhibitors, lithium, tramadol, methylene blue IV, and mirtazapine

            Protect patch from sunlight

            May prolong QT interval; coadministration with drugs known to prolong QT interval may result in serious arrhythmias

            Mild application site reactions have occurred; remove patch if severe reactions or generalized skin reaction occur

            Avoid exposing granisetron patch and surrounding area to direct external heat sources, such as heating pads; plasma concentration continues to increase during period of heat exposure

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: excretion in milk unknown; use with caution

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Selective 5-HT3 receptor antagonist; granisetron binds to 5-HT3 receptors both in the peripheral and central nervous system with primary effects in GI tract

            Pharmacokinetics

            Half-life: 3-14 hr

            Onset: 4-10 min (IV)

            Duration: 24 hr (IV)

            Bioavailability: 60% (PO)

            Release rate (patch): 3.1 mg/24 hr

            Protein bound: 65%

            Vd: 2-4 L/kg

            Metabolism: Extensively metabolized in liver via N-demethylation, oxidation, conjugation, and CYP3A subfamily

            Metabolites: Inactive

            Total body clearance: 0.2-0.79 L/hr/kg

            Excretion

            • Feces: 38%
            • Urine: 60%
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            Administration

            IV Incompatibilities

            Y-site: amphotericin B

            IV Compatibilities

            Solution: BWI, D5/½NS, D5/NS, D5W, NS

            Additive: dexamethasone sodium phosphate, methylprednisolone sodium succinate

            Syringe: dexamethasone sodium phosphate, methylprednisolone sodium succinate

            Y-site (partial list): allopurinol, amphotericin B cholSO4, ampicillin, butorphanol, carboplatin, cisplatin, ctarabine, dactinomycin, docetaxel, diphenhydramine, etoposide, famotidine, fluorouracil, furosemide, fluconazole, heparin, hydromorphone, linezolid, lorazepam, MgSO4, meoperidine, morphine, metoclopramide, metronidazole, paclitaxel, KCl, prochlorperazine, promethazine, Na-bicarb, thiotepa, vincristine, vancomycin

            IV Preparation

            IV infusion: dilute to 20-50 mL with D5W or NS

            IV Administration

            IVP undiluted over 30 sec, or

            IV infusion over 5 min after dilution to 20-50 mL with D5W or NS

            SC Preparation (Sustol)

            At least 60 minutes before administration, remove kit from refrigerator

            Unpack the kit to allow the Sustol syringe and all other contents to warm to room temperature

            Activate 1 of the syringe warming pouches, and wrap the syringe in the warming pouch for 5-6 minutes to warm Sustol to body temperature

            Prior to administration, inspect the Sustol syringe visually for particulate matter and discoloration

            Note that the syringe is amber colored glass

            Do not administered if particulate matter or discoloration observed, the tip cap is missing or has been tampered with, or if the Luer fitting is missing or dislodged

            SC Administration (Sustol)

            For SC injection only

            Intended for administration by a health care provider

            Use standard aseptic technique when performing the SC injection

            Administer as a single SC injection in the back of the upper arm or in the skin of the abdomen at least 1-inch away from the umbilicus

            Avoid injecting anywhere the skin is burned, hardened, inflamed, swollen, or otherwise compromised

            Topical anesthetic may be used at the injection site prior to administration

            Due to the viscosity of the liquid, the time required for injection is greater than most medications administered SC; requires a slow, sustained injection which may take up to 20-30 seconds

            Pressing the plunger harder will NOT expel the viscous liquid faster

            Storage

            IV

            • Store at controlled room temperature 20-25°C (68-77°F)
            • Protect from light and freezing
            • Stable for 24 hr after dilution

            Extended-release SC (Sustol)

            • Refrigerate at 2-8°C (36-46°F)
            • Can be placed back in the refrigerator after being kept at room temperature
            • Can remain at room temperature for up to a maximum of 7 days
            • Protect from light
            • Do not freeze
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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            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
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Add or Remove Plans
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            Select a box to add or remove a plan.

            Select a class to view formulary status for similar drugs

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