Sustol

What is Sustol?

Sustol (granisetron extended-release injection) is a serotonin-3 (5-HT3) receptor antagonist used in adults help prevent the nausea and vomiting that happens right away or later with certain anti-cancer medicines (chemotherapy).

Granisetron structure

Granisetron3Dan

What are the uses of this medicine?

• Sustol (granisetron extended-release injection) is a prescription medicine called an "antiemetic."
• Sustol is used 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.

How does this medicine work?

• Sustol - an extended-release (er), polymer-based injectable formulation containing the indazole derivative granisetron, a selective serotonin (5-hydroxytryptamine; 5-ht) receptor type 3 (5-ht3) antagonist, with anti-emetic activity.
• Upon subcutaneous administration, granisetron is released from the polymer in a sustained manner, which is based upon the controlled hydrolysis of the polymers, and selectively binds to and inhibits the activity of the 5-ht3 receptors located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone (ctz) of the area postrema.
• By preventing stimulation of 5-ht3 receptors, granisetron is able to suppress chemotherapy-induced nausea and vomiting (cinv).
• Compared to the injection of granisetron alone, injection of the polymer-based formulation allows for therapeutic levels of granisetron over an extended period of time.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to granisetron or any of the ingredients in SUSTO.
• any other 5-HT3 receptor antagonist medicine used to help prevent nausea and vomiting.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.
• Serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular symptoms) has been described following the concomitant use of 5-HT3 receptor antagonists and other serotonergic drugs, including selective serotonin reuptake inhibitors (SSRIs) and serotonin and noradrenaline reuptake inhibitors (SNRIs). Avoid coadministrartion.

Is this medicine FDA approved?

• The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA.

How should this medicine be used?

Recommended dosage:

• The recommended dosage in adults is 10 mg administered as a single subcutaneous injection at least 30 minutes before the start of emetogenic chemotherapy on Day 1.
• Do not administer Sustol more frequently than once every 7 days.
• Use of Sustol with successive emetogenic chemotherapy cycles for more than 6 months is not recommended.

Renal Impairment:

• In patients with moderate renal impairment (Clcr 30-59 mL/min), administer Sustol not more frequently than once every 14 days.
• Avoid Sustol in patients with severe renal impairment (CLcr < 30 mL/min).

Administration:

• Sustol will be given to you by an injection under your skin (subcutaneously) in the back of your upper arm or in your stomach-area (abdomen) on Day 1 of your chemotherapy cycle.
• Sustol will be given to you by a healthcare provider.
• Sustol is usually given about 30 minutes before you receive your anti-cancer medicine (chemotherapy).
• You should not receive Sustol more often than 1 time every 7 days.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-Release Injection: 10 mg/0.4 mL in a single-dose, pre-filled syringe.

This medicine is available in fallowing brand namesː

• Sustol

What side effects can this medication cause?

The most common side effects of this medicine include:

• injection site reactions
• constipation
• fatigue
• headache
• diarrhea
• stomach-area (abdominal) pain
• trouble sleeping or falling asleep
• indigestion
• dizziness
• weakness
• heartburn

Sustol may cause serious side effects, including:

• Injection site reactions
• Stomach and intestinal problems
• Serious allergic reaction
• Serotonin Syndrome

What special precautions should I follow?

• Injection site reactions (ISRs), including infection, bleeding, pain, nodules, swelling and induration may occur. Monitor for ISRs following Sustol injection. Inform patients that some ISRs may occur 2 weeks or more after Sustol administration. In patients receiving antiplatelet agents or anticoagulants, consider the increased risk of bruising or severe hematoma prior to the use of Sustol.
• Sustol may mask a progressive ileus and/or gastric distention. Monitor for decreased bowel activity, particularly in patients with risk factors for gastrointestinal obstruction.
• Hospitalization due to constipation or fecal impaction was reported in 5 Sustol-treated patients. Monitor for constipation and consider optimizing patients’ current bowel regimens used for managing preexisting constipation. Also monitor for decreased bowel activity, particularly in patients with risk factors for gastrointestinal obstruction. Instruct patients to seek immediate medical care if signs and symptoms of ileus occur.
• Hypersensitivity reactions, including anaphylaxis, have been reported in granisetron-treated patients who have exhibited hypersensitivity to other 5-HT3 receptor antagonists. Serious reactions have been reported and may occur up to 7 days or longer following Sustol administration and may have an extended course. If a reaction occurs, administer appropriate treatment and monitor until signs and symptoms resolve.
• The development of serotonin syndrome has been reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs. If such symptoms occur, discontinue Sustol and initiate supportive treatment. If concomitant use of Sustol with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• headache

Management of overdosage:

• There is no specific antidote for granisetron overdosage.
• In the case of overdosage, symptomatic treatment should be given.

Can this medicine be used in pregnancy?

• There are no available data on the use of Sustol in pregnant women.
• Limited published data on granisetron use during pregnancy are not sufficient to inform a drug-associated risk.

Can this medicine be used in children?

• The safety and effectiveness of Sustol in pediatric patients under 18 years of age have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: granisetron
• Inactive ingredients: triethylene glycol poly(orthoester) polymer and polyethylene glycol monomethyl ether

Who manufactures and distributes this medicine?

• Manufactured by: Lifecore Biomedical, Chaska, MN
• Marketed by: Heron Therapeutics, Inc., San Diego, CA
• Sustol® is a registered trademark of Heron Therapeutics, Inc.

What should I know about storage and disposal of this medication?

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

• Dailymed label info on Sustol
• FDA Sustol

Sustol Resources
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