• Nausea

Sustol Generic Name & Formulations

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



Generic Availability


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


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


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.


<18yrs: not established.

Sustol Contraindications


Hypersensitivity to other 5-HT3 receptor antagonists.

Sustol Boxed Warnings

Not Applicable

Sustol 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


  • 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).


  • ~65% plasma protein bound.


  • Hepatic (CYP1A1, CYP3A4).


  • Renal (49%), fecal (34%). Half-life: ~24 hours.

Sustol 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