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Sustol Generic Name & Formulations
Legal Class
Rx
General Description
Granisetron extended-release 10mg/0.4mL; per pre-filled syringe; viscous liq for SC inj.
Pharmacological Class
Selective 5-HT3 receptor antagonist.
How Supplied
Kits—6
Manufacturer
Generic Availability
NO
Mechanism of Action
Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT1, 5-HT1A, 5-HT1B/C, 5-HT2; for alpha1-, alpha2-, or beta-adrenoreceptors; for dopamine-D2; or for histamine-H1; benzodiazepine; picrotoxin or opioid receptors.
Sustol Indications
Indications
In combination with other antiemetics, to prevent acute and delayed nausea/vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination regimens.
Sustol Dosage and Administration
Adult
Give as a slow, SC inj over 20–30secs with IV dexamethasone ≥30mins before chemotherapy. ≥18yrs: 10mg on Day 1 of chemotherapy; give no sooner than once every 7 days. For MEC: use IV dexamethasone 8mg on Day 1. For AC: use IV dexamethasone 20mg on Day 1, then 8mg orally twice daily on Days 2–4. If concomitant NK1 receptor antagonist: see full labeling. Renal impairment (CrCl 30–59mL/min): give Sustol on Day 1 of chemotherapy and no sooner than once every 14 days; (CrCl <30mL/min): avoid.
Children
<18yrs: not established.
Sustol Contraindications
Contraindications
Hypersensitivity to other 5-HT3 receptor antagonists.
Sustol Boxed Warnings
Not Applicable
Sustol Warnings/Precautions
Warnings/Precautions
Monitor for inj site reactions (including infections, bruising/hematoma, bleeding, others); if ongoing or unresolved reactions, administer in unaffected areas. Abdominal surgery. May mask progressive ileus and/or gastric distention. GI obstruction. Monitor for constipation, decreased bowel activity. Monitor for serotonin syndrome; discontinue if symptoms occur. Renal impairment. Pregnancy. Nursing mothers.
Sustol Pharmacokinetics
Absorption
-
Mean concentration: 3.5 ng/mL (range, 0 to 14 ng/mL) observed at 5 days post-dose.
-
Cmax: 9.8 ± 4.8 ng/mL (abdomen); 10.8 ± 4.6 ng/mL (upper arm).
-
Tmax: 12 hours (range, 1 to 144) (abdomen); 11 hours (range, 1 to 120) (upper arm).
Distribution
-
~65% plasma protein bound.
Elimination
- Renal (49%), fecal (34%). Half-life: ~24 hours.
Sustol Interactions
Interactions
Increased risk of severe bruising and/or hematoma with concomitant antiplatelets or anticoagulants. Increased risk of serotonin syndrome with concomitant other SSRIs, SNRIs, MAOIs, mirtazapine, fentanyl, lithium, tramadol, or IV methylene blue.
Sustol Adverse Reactions
Adverse Reactions
Inj site reactions, constipation, fatigue, headache, diarrhea, abdominal pain, insomnia, dyspepsia, dizziness, asthenia, gastroesophageal reflux; hypersensitivity, serotonin syndrome.
Sustol Clinical Trials
See Literature
Sustol Note
Not Applicable
Sustol Patient Counseling
See Literature
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