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Granisetron Hydrochloride 1 mg/mL Injection, 1 vial

by Akorn · 1 VIAL, SINGLE-DOSE in 1 CARTON (17478-546-02) / 1 mL in 1 VIAL, SINGLE-DOSE
NDC 17478-0546-02
🏷️ FDA NDC (as labeled) 17478-546-02 billing pads the product segment with a zero
This package
Contains1 vial Pack sizes2 compare ↓
Also comes in: 4 mL 17478-0546-05
Rx only Generic Discontinued Non-controlled ⚠ Inactivated by FDA
🗂️ Data synced Jul 14, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

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Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

⚠️
Excluded from the active FDA NDC Directory. FDA inactivated this product’s listing record, so it is excluded from the active NDC Directory. The listing was last certified through Dec 2023. A label may still appear on DailyMed, but the NDC is no longer in the current FDA NDC Directory. Search the FDA NDC Directory ↗

🆔 Identity & classification

FDA NDC (as labeled) 17478-546-02
Product NDC 17478-546
11-digit billing NDC 17478054602
NCPDP billing unit ML — per mL (volume)
Application # ANDA079078
SPL Set ID 02f350c9-b7d2-4906-af28-70ed4461ff23
Established class (EPC) Serotonin 3 Receptor Antagonists [MoA], Serotonin-3 Receptor Antagonist
DEA schedule Non-controlled
Marketing category ANDA
Marketing status Discontinued
FDA listing status Inactivated by FDA (certified through Dec 2023)
Route INTRAVENOUS
Dosage form INJECTION
Substance GRANISETRON HYDROCHLORIDE
GCN Seq No 063545
GCN 99267
HICL code 007611
Ingredient (HICL) Granisetron Hcl
HIC1 code H
Therapeutic class — broad (HIC1) Nervous System (Except Autonomic)
HIC2 code H6
Therapeutic class — intermediate (HIC2) Drugs Acting Principally On The Midbrain
HIC3 code H6J
Therapeutic class — specific (HIC3) Antiemetic/Antivertigo Agents
AHFS code 56:22.20.00
AHFS class 5-Ht3 Receptor Antagonists
FDB label name GRANISETRON HCL 1 MG/ML VIAL
FDB brand name Granisetron Hcl
Legend status F — Federal legend — prescription drug or device
TE code (Orange Book) AP · RLD · RS
Why two NDCs? The FDA registers this code as 17478-546-02 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 17478-0546-02. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏭 Manufacturer & labeler

LabelerAkorn
Application holderRISING PHARMA HOLDINGS INC
FDA applicationANDA079078 (ANDA)
Labeler code17478
Product typeHuman Prescription Drug
Portfolio3 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

Label name GRANISETRON HCL 1 MG/ML VIAL Ingredient Granisetron Hcl
📗 Our plain-language guide HelloPharmacist
  • Granisetron is an anti-nausea medicine. It's mainly used to prevent nausea and vomiting that cancer chemotherapy or radiation therapy can cause. Depending on which product you've b...
  • The Sancuso patch delivers granisetron slowly through your skin over up to 7 days — you apply it to your upper outer arm at least 24 hours before chemotherapy starts and leave it o...
  • How does the Sancuso patch work differently from the pill or injection?
  • The most common ones are headache and constipation — these are the side effects most often reported in clinical studies. Some people also notice fever, stomach pain, or a slight ch...
📖 Read our full Granisetron guide →

Supplement & herbal interactions

🌿 Drug–supplement interaction checker →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Try another pack size: 4 mL
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Granisetron Hydrochloride 1 mg/mLthis 17478-0546-02 Akorn 1 vial — AP Discontinued —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

⏳ Availability & generic status

📍
2026
Currently FDA-listed
listed with the FDA
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Granisetron hydrochloride — the ingredient across all brands.

Top reported reactions

Nausea1,204
Febrile Neutropenia857
Diarrhoea789
Vomiting762
Pyrexia759
Dyspnoea651
Fatigue563

Age at onset

Neonate6
Infant8
Child76
Adolescent69
Adult807
Elderly786

Reporter sex

10,382 reports
Male · 47%
Female · 53%
Unknown · 0%

Serious outcomes

Hospitalization5,651
Life-threatening1,355
Disabling296
Reports over time (by year) — tap or hover for the count & year
2021 2022 2024 2026 863 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
17478-0546-02 You're viewing this 1 VIAL, SINGLE-DOSE in 1 CARTON (17478-546-02) / 1 mL in 1 VIAL, SINGLE-DOSE 2009-10-01 Inactivated by FDA
17478-0546-05 1 VIAL, MULTI-DOSE in 1 CARTON (17478-546-05) / 4 mL in 1 VIAL, MULTI-DOSE 2009-10-01 Inactivated by FDA

Pack size FAQ

What quantity is in NDC 17478-0546-02?
NDC 17478-0546-02 contains 1 vial — 1 vial, single-dose in 1 carton / 1 ml in 1 vial, single-dose.
What NDC number is used to bill for this package of Granisetron Hydrochloride 1 mg/mL Injection?
Bill NDC 17478-0546-02 — the 11-digit billing format is 17478054602. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

🧭 About this NDC listing & data coverage

Finished prescription product No longer marketed (per FDA listing data)
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
What does the discontinued status mean for this NDC?
The labeler reported a marketing end date (or the listing was delisted), so this specific package is no longer actively marketed. Remaining stock may still be dispensed for a time, and the NDC stays valid for historical records and claims — but data feeds (pricing, labeling) typically stop updating for it. Other package sizes or other manufacturers' versions of the same medication may still be marketed — see the equivalents section where available.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The FDA registers it as 17478-546-02, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 17478-0546-02, written without dashes as 17478054602. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 17478-0546-02, the first segment (17478) is the labeler code FDA assigned to Akorn; the middle segment (0546) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (02) identifies this exact package size and type. Together they name one specific package of one specific product.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 1 vial (17478-0546-05). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Akorn is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients
🎯 Indications and Usage 73 words ▾

1 INDICATIONS AND USAGE Granisetron Hydrochloride Injection, USP is a serotonin-3 (5-HT 3 ) receptor antagonist indicated for: The prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. Granisetron Hydrochloride Injection, USP is a serotonin-3 (5-HT 3 ) receptor antagonist indicated for: The prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. ( 1 )

⏱️ Dosage and Administration 219 words ▾

2 DOSAGE AND ADMINISTRATION Prevention of chemotherapy-induced nausea and vomiting ( 2.1 ): Recommended dosage is 10 mcg/kg intravenously within 30 minutes before initiation of chemotherapy Pediatric patients (2 to 16 years): Recommended dosage is 10 mcg/kg

2.1Prevention of Chemotherapy-Induced Nausea and Vomiting Adult Patients The recommended dosage for granisetron hydrochloride injection is 10 mcg/kg administered intravenously within 30 minutes before initiation of chemotherapy, and only on the day(s) chemotherapy is given. Infusion Preparation Granisetron hydrochloride injection may be administered intravenously either undiluted over 30 seconds, or diluted with 0.9% Sodium Chloride or 5% Dextrose and infused over 5 minutes. Stability Intravenous infusion of granisetron hydrochloride injection should be prepared at the time of administration.

However, granisetron hydrochloride injection has been shown to be stable for at least 24 hours when diluted in 0.9% Sodium Chloride or 5% Dextrose and stored at room temperature under normal lighting conditions. As a general precaution, granisetron hydrochloride injection should not be mixed in solution with other drugs. Parenteral drug products should be inspected visually for particulate matter and discoloration before administration whenever solution and container permit.

Pediatric Patients The recommended dose in pediatric patients 2 to 16 years of age is 10 mcg/kg [see Clinical Studies ( 14 )] . Pediatric patients under 2 years of age have not been studied.

💊 Dosage Forms and Strengths 36 words ▾

3 DOSAGE FORMS AND STRENGTHS Single-dose Vials for Injection: 1 mg/mL, 0.1 mg/mL Multiple-dose Vials for Injection: 4 mg/4 mL Injection 1 mg/mL (free base). ( 3 ) Injection 0.1 mg/mL (free base). ( 3 )

⛔ Contraindications 42 words ▾

4 CONTRAINDICATIONS Granisetron hydrochloride injection is contraindicated in patients with known hypersensitivity (e.g., anaphylaxis, shortness of breath, hypotension, urticaria) to the drug or to any of its components. Hypersensitivity to granisetron hydrochloride injection or to any of its components. ( 4 )

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Granisetron hydrochloride does not stimulate gastric or intestinal peristalsis and should not be used instead of nasogastric suction. ( 5.1 ) QT prolongation has been reported with granisetron hydrochloride. Use with caution in patients with pre-existing arrhythmias or cardiac conduction disorders.

( 5.2 ) Contains benzyl alcohol ( 5.5 ) Hypersensitivity reactions, such as anaphylaxis, shortness of breath, hypotension, and urticaria, may occur in patients with known hypersensitivity to other selective 5-HT 3 receptor antagonists. ( 5.3 ) Serotonin syndrome has been reported with granisetron, alone but particularly with concomitant use of serotogenic drugs. ( 5.4 )

5.1Gastric or Intestinal Peristalsis Granisetron hydrochloride is not a drug that stimulates gastric or intestinal peristalsis. It should not be used instead of nasogastric suction. The use of granisetron hydrochloride in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distention.

5.2Cardiovascular Events An adequate QT assessment has not been conducted, but QT prolongation has been reported with granisetron hydrochloride. Therefore, granisetron hydrochloride should be used with caution in patients with pre-existing arrhythmias or cardiac conduction disorders, as this might lead to clinical consequences. Patients with cardiac disease, on cardio-toxic chemotherapy, with concomitant electrolyte abnormalities and/or on concomitant medications that prolong the QT interval are particularly at risk.

5.3Hypersensitivity Reactions Hypersensitivity reactions (e.g., anaphylaxis, shortness of breath, hypotension, urticaria) may occur in patients who have exhibited hypersensitivity to other selective 5-HT 3 receptor antagonists.

5.4Serotonin Syndrome The development of serotonin syndrome has been reported with 5-HT 3 receptor antagonists. Most reports have been associated with concomitant use of serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue). Some of the reported cases were fatal.

Serotonin syndrome occurring with overdose of another 5-HT 3 receptor antagonist alone has also been reported. The majority of reports of serotonin syndrome related to 5-HT 3 receptor antagonist use occurred in a post-anesthesia care unit or an infusion center. Symptoms associated with serotonin syndrome may include the following combination of signs and symptoms: mental status changes (e.g., agitation, hallucinations, delirium, and coma), autonomic instability (e.g., tachycardia, labile blood pressure, dizziness, diaphoresis, flushing, hyperthermia), neuromuscular symptoms (e.g., tremor, rigidity, myoclonus, hyperreflexia, incoordination), seizures, with or without gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).

Patients should be monitored for the emergence of serotonin syndrome, especially with concomitant use of granisetron and other serotonergic drugs. If symptoms of serotonin syndrome occur, discontinue granisetron and initiate supportive treatment. Patient should be informed of the increased risk of serotonin syndrome, especially if granisetron is used concomitantly with other serotonergic drugs [see Drug Interaction ( 7 ), Patient Counseling Information (17.4)] .

5.5Benzyl Alcohol Granisetron hydrochloride injection, USP 1 mg/mL contains benzyl alcohol. Benzyl alcohol, a component of granisetron hydrochloride injection, USP 1 mg/mL, has been associated with serious adverse reactions and death, particularly in neonates. The "gasping syndrome," characterized by central nervous system depression, metabolic acidosis, gasping respirations, and high levels of benzyl alcohol and metabolites in blood and urine, has been associated with benzyl alcohol dosages >99 mg/kg/day in neo…

🤒 Adverse Reactions ~2 min read ▾

6 ADVERSE REACTIONS QT prolongation has been reported with granisetron hydrochloride [see Warnings and Precautions ( 5.2 ) and Drug Interactions ( 7 )] . Most common adverse reactions: Chemotherapy-induced nausea and vomiting (≥3%): Headache, and constipation ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Akorn, Inc. at 1-800-932-5676 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in patients. Chemotherapy-Induced Nausea and Vomiting The following have been reported during controlled clinical trials or in the routine management of patients. The percentage figures are based on clinical trial experience only.

Table 1 gives the comparative frequencies of the two most commonly reported adverse reactions (≥3%) in patients receiving granisetron hydrochloride injection, in single-day chemotherapy trials. These patients received chemotherapy, primarily cisplatin, and intravenous fluids during the 24-hour period following granisetron hydrochloride injection administration. Reactions were generally recorded over seven days post-granisetron hydrochloride injection administration.

Table 1 Principal Adverse Reactions in Clinical Trials – Single-Day Chemotherapy *Metoclopramide/dexamethasone and phenothiazines/dexamethasone. Percent of Patients With Event Granisetron Injection 40 mcg/kg (n=1268) Comparator* (n-422) Headache Constipation 14% 3% 6% 3% Additional adverse events reported in clinical trials were asthenia, somnolence and diarrhea. In over 3,000 patients receiving granisetron hydrochloride injection (2 to 160 mcg/kg) in single-day and multiple-day clinical trials with emetogenic cancer therapies, adverse events, other than those adverse reactions listed in Table 1 , were observed; attribution of many of these events to granisetron hydrochloride is uncertain.

Hepatic: In comparative trials, mainly with cisplatin regimens, elevations of AST and ALT (>2 times the upper limit of normal) following administration of granisetron hydrochloride injection occurred in 2.8% and 3.3% of patients, respectively. These frequencies were not significantly different from those seen with comparators (AST: 2.1%; ALT: 2.4%). Cardiovascular: Hypertension (2%); hypotension, arrhythmias such as sinus bradycardia, atrial fibrillation, varying degrees of A-V block, ventricular ectopy including non-sustained tachycardia, and ECG abnormalities have been observed rarely.

Central Nervous System: Agitation, anxiety, CNS stimulation and insomnia were seen in less than 2% of patients. Extrapyramidal syndrome occurred rarely and only in the presence of other drugs associated with this syndrome. Hypersensitivity: Rare cases of hypersensitivity reactions, sometimes severe (e.g., anaphylaxis, shortness of breath, hypotension, urticaria) have been reported.

Other: Fever (3%), taste disorder (2%), skin rashes (1%). In multiple-day comparative studies, fever occurred more frequently with granisetron hydrochloride injection (8.6%) than with comparative drugs (3.4%, P <0.014), which usually included dexamethasone.

6.2Postmarketing Experience The following adverse reactions have been identified during post approval use of granisetron hydrochloride. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to granisetron hydrochloride exposure. QT prolongation has been reported with granisetron hydrochloride [see Warnings and Precautions ( 5.2 ) and Drug Interactions ( 7 )] .

🔄 Drug Interactions ~2 min read ▾

7 DRUG INTERACTIONS Granisetron does not induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system in vitro . There have been no definitive drug-drug interaction studies to examine pharmacokinetic or pharmacodynamic interaction with other drugs; however, in humans, granisetron hydrochloride injection has been safely administered with drugs representing benzodiazepines, neuroleptics and anti-ulcer medications commonly prescribed with antiemetic treatments. Granisetron hydrochloride injection also does not appear to interact with emetogenic cancer chemotherapies.

Because granisetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes, inducers or inhibitors of these enzymes may change the clearance and, hence, the half-life of granisetron. No specific interaction studies have been conducted in anesthetized patients. In addition, the activity of the cytochrome P-450 subfamily 3A4 (involved in the metabolism of some of the main narcotic analgesic agents) is not modified by granisetron hydrochloride in vitro .

In in vitro human microsomal studies, ketoconazole inhibited ring oxidation of granisetron hydrochloride. However, the clinical significance of in vivo pharmacokinetic interactions with ketoconazole is not known. In a human pharmacokinetic study, hepatic enzyme induction with phenobarbital resulted in a 25% increase in total plasma clearance of intravenous granisetron hydrochloride.

The clinical significance of this change is not known. QT prolongation has been reported with granisetron hydrochloride. Use of granisetron hydrochloride in patients concurrently treated with drugs known to prolong the QT interval and/or are arrhythmogenic may result in clinical consequences.

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) [see Warnings and Precautions ( 5.4 )]. Granisetron hydrochloride injection has been administered safely with benzodiazepines, neuroleptics, and anti-ulcer medications. ( 7 ) Does not appear to interact with emetogenic cancer chemotherapies.

( 7 ) Inducers or inhibitors of CYP450 enzymes may change the clearance and therefore the half-life of granisetron. ( 7 ) Coadministration of granisetron hydrochloride injection with drugs known to prolong the QT interval and/or are arrhythmogenic may result in clinical consequences. ( 7 )

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Pregnancy: Use only if clearly needed. ( 8.1 ) Nursing mothers: Caution should be exercised when administered to a nursing woman. ( 8.3 ) Pediatric use: Safety and efficacy in pediatric patients have not been established for use in postoperative nausea and vomiting. ( 8.4 ) Geriatric use: No differences in responses between the elderly and younger patients were observed in reported clinical experience. ( 8.5 )

8.1Pregnancy Pregnancy Category B Reproduction studies have been performed in pregnant rats at intravenous doses up to 9 mg/kg/day (54 mg/m 2 /day, 146 times the recommended human dose based on body surface area) and pregnant rabbits at intravenous doses up to 3 mg/kg/day (35.4 mg/m 2 /day, 96 times the recommended human dose based on body surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to granisetron. There are, however, no adequate and well-controlled studies in pregnant women.

Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

8.3Nursing Mothers It is not known whether granisetron is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when granisetron hydrochloride injection is administered to a nursing woman.

8.4Pediatric Use Chemotherapy-Induced Nausea and Vomiting [See Dosage and Administration ( 2 )] for use in chemotherapy-induced nausea and vomiting in pediatric patients 2 to 16 years of age. Safety and effectiveness in pediatric patients under 2 years of age have not been established. Postoperative Nausea and Vomiting Safety and efficacy have not been established in pediatric patients for the prevention of postoperative nausea and vomiting (PONV).

Granisetron has been evaluated in a pediatric patient clinical trial for use in the prevention of PONV. Due to the lack of efficacy and the QT prolongation observed in this trial, use of granisetron for the prevention of PONV in children is not recommended. The trial was a prospective, multicenter, randomized, double-blind, parallel-group trial that evaluated 157 children aged 2 to 16 years who were undergoing elective surgery for tonsillectomy or adenotonsillectomy.

The purpose of the trial was to assess two dose levels (20 mcg/kg and 40 mcg/kg) of intravenous granisetron in the prevention of PONV. There was no active comparator or placebo. The primary endpoint was total control of nausea and vomiting (defined as no nausea, vomiting/retching, or use of rescue medication) in the 24 hours following surgery.

Efficacy was not established due to lack of a dose response. The trial also included standard 12 lead ECGs performed pre-dose and after the induction of anesthesia. ECGs were repeated at the end of surgery after the administration of granisetron and just prior to reversal of anesthesia.

QT prolongation was seen at both dose levels. Five patients in this trial experienced an increase of ≥ 60 msec in QTcF. In addition, there were two patients whose QTcF was ≥ 500 msec.

Interpretation of the QTcF prolongation was confounded by multiple factors, including the use of concomitant medication and the lack of either a placebo or active control. A thorough QT trial in adults has not been performed. Other adverse events that occurred in the study included: vomiting (5 to 8%), post-procedural hemorrhage (3 to 5%), and dehydration (0 to 5%).

Pediatric patients under 2 years of age have not been studied.

8.5Geriatric Use During chemotherapy clinical trials, 713 patients 65 years of age or older received granisetron hydrochloride injection. The safety and effectiveness were similar in patients of various ages.

🤰 Pregnancy 109 words ▾

8.1Pregnancy Pregnancy Category B Reproduction studies have been performed in pregnant rats at intravenous doses up to 9 mg/kg/day (54 mg/m 2 /day, 146 times the recommended human dose based on body surface area) and pregnant rabbits at intravenous doses up to 3 mg/kg/day (35.4 mg/m 2 /day, 96 times the recommended human dose based on body surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to granisetron. There are, however, no adequate and well-controlled studies in pregnant women.

Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

🧒 Pediatric Use ~2 min read ▾

8.4Pediatric Use Chemotherapy-Induced Nausea and Vomiting [See Dosage and Administration ( 2 )] for use in chemotherapy-induced nausea and vomiting in pediatric patients 2 to 16 years of age. Safety and effectiveness in pediatric patients under 2 years of age have not been established. Postoperative Nausea and Vomiting Safety and efficacy have not been established in pediatric patients for the prevention of postoperative nausea and vomiting (PONV).

Granisetron has been evaluated in a pediatric patient clinical trial for use in the prevention of PONV. Due to the lack of efficacy and the QT prolongation observed in this trial, use of granisetron for the prevention of PONV in children is not recommended. The trial was a prospective, multicenter, randomized, double-blind, parallel-group trial that evaluated 157 children aged 2 to 16 years who were undergoing elective surgery for tonsillectomy or adenotonsillectomy.

The purpose of the trial was to assess two dose levels (20 mcg/kg and 40 mcg/kg) of intravenous granisetron in the prevention of PONV. There was no active comparator or placebo. The primary endpoint was total control of nausea and vomiting (defined as no nausea, vomiting/retching, or use of rescue medication) in the 24 hours following surgery.

Efficacy was not established due to lack of a dose response. The trial also included standard 12 lead ECGs performed pre-dose and after the induction of anesthesia. ECGs were repeated at the end of surgery after the administration of granisetron and just prior to reversal of anesthesia.

QT prolongation was seen at both dose levels. Five patients in this trial experienced an increase of ≥ 60 msec in QTcF. In addition, there were two patients whose QTcF was ≥ 500 msec.

Interpretation of the QTcF prolongation was confounded by multiple factors, including the use of concomitant medication and the lack of either a placebo or active control. A thorough QT trial in adults has not been performed. Other adverse events that occurred in the study included: vomiting (5 to 8%), post-procedural hemorrhage (3 to 5%), and dehydration (0 to 5%).

Pediatric patients under 2 years of age have not been studied.

🧓 Geriatric Use 30 words ▾

8.5Geriatric Use During chemotherapy clinical trials, 713 patients 65 years of age or older received granisetron hydrochloride injection. The safety and effectiveness were similar in patients of various ages.

🆘 Overdosage 44 words ▾

10 OVERDOSAGE There is no specific antidote for granisetron hydrochloride injection overdosage. In case of overdosage, symptomatic treatment should be given. Overdosage of up to 38.5 mg of granisetron hydrochloride injection has been reported without symptoms or only the occurrence of a slight headache.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Granisetron is a selective 5-hydroxytryptamine 3 (5-HT 3 ) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT 1 ; 5-HT 1A ; 5-HT 1B/C ; 5-HT 2 ; for alpha 1 -, alpha 2 - or beta-adrenoreceptors; for dopamine-D 2 ; or for histamine-H 1 ; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy-induced vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT 3 receptors.

This evokes vagal afferent discharge and may induce vomiting. Animal studies demonstrate that, in binding to 5-HT 3 receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds.

In most human studies, granisetron has had little effect on blood pressure, heart rate or ECG. No evidence of an effect on plasma prolactin or aldosterone concentrations has been found in other studies. Granisetron hydrochloride injection exhibited no effect on oro-cecal transit time in normal volunteers given a single intravenous infusion of 50 mcg/kg or 200 mcg/kg.

Single and multiple oral doses slowed colonic transit in normal volunteers.

12.3Pharmacokinetics Chemotherapy-Induced Nausea and Vomiting In adult cancer patients undergoing chemotherapy and in volunteers, mean pharmacokinetic data obtained from an infusion of a single 40 mcg/kg dose of granisetron hydrochloride injection are shown in Table 3 . Table 3 Pharmacokinetic Parameters in Adult Cancer Patients Undergoing Chemotherapy and in Volunteers, Following a Single Intravenous 40 mcg/kg Dose of Granisetron Hydrochloride Injection *5-minute infusion † 3-minute infusion Peak Plasma Concentration (ng/mL) Terminal Phase Plasma Half-Life (h) Total Clearance (L/h/kg) Volume of Distribution (L/kg) Cancer Patients Mean Range 63.8* 18.0 to 176 8.95* 0.90 to 31.1 0.38* 0.14 to 1.54 3.07* 0.85 to

10.4Volunteers 21 to 42 years Mean Range 65 to 81 years Mean Range 64.3 † 11.2 to 182 57.0 † 14.6 to 153 4.91 † 0.88 to 15.2 7.69 † 2.65 to 17.7 0.79 † 0.20 to 2.56 0.44 † 0.17 to 1.06 3.04 † 1.68 to 6.13 3.97 † 1.75 to

7.01Distribution Plasma protein binding is approximately 65% and granisetron distributes freely between plasma and red blood cells. Metabolism Granisetron metabolism involves N-demethylation and aromatic ring oxidation followed by conjugation. In vitro liver microsomal studies show that granisetron's major route of metabolism is inhibited by ketoconazole, suggestive of metabolism mediated by the cytochrome P-450 3A subfamily.

Animal studies suggest that some of the metabolites may also have 5-HT 3 receptor antagonist activity. Elimination Clearance is predominantly by hepatic metabolism. In normal volunteers, approximately 12% of the administered dose is eliminated unchanged in the urine in 48 hours.

The remainder of the dose is excreted as metabolites, 49% in the urine, and 34% in the feces. Subpopulations Gender There was high inter- and intra-subject variability noted in these studies. No difference in mean AUC was found between males and females, although males had a higher C generally.

Elderly The ranges of the pharmacokinetic parameters in elderly volunteers (mean age 71 years), given a single 40 mcg/kg intravenous dose of granisetron hydrochloride injection, were generally similar to those in younger healthy volunteers; mean values were lower for clearance and longer for half-life in the elderly patients (see Table 3 ). Pediatric Patients A pharmacokinetic study in pediatric cancer patients (2 to 16 years of age), given a single 40 mcg/kg intravenous dose of granisetron hydrochloride injection, showed that volume of distribution and…

🧬 Mechanism of Action ~1 min read ▾

12.1Mechanism of Action Granisetron is a selective 5-hydroxytryptamine 3 (5-HT 3 ) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT 1 ; 5-HT 1A ; 5-HT 1B/C ; 5-HT 2 ; for alpha 1 -, alpha 2 - or beta-adrenoreceptors; for dopamine-D 2 ; or for histamine-H 1 ; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy-induced vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT 3 receptors.

This evokes vagal afferent discharge and may induce vomiting. Animal studies demonstrate that, in binding to 5-HT 3 receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds.

In most human studies, granisetron has had little effect on blood pressure, heart rate or ECG. No evidence of an effect on plasma prolactin or aldosterone concentrations has been found in other studies. Granisetron hydrochloride injection exhibited no effect on oro-cecal transit time in normal volunteers given a single intravenous infusion of 50 mcg/kg or 200 mcg/kg.

Single and multiple oral doses slowed colonic transit in normal volunteers.

📦 How Supplied / Storage and Handling 113 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Granisetron Hydrochloride Injection, USP, 1 mg/mL (free base), is supplied in 1 mL Single-dose vials and 4 mL Multi-dose vials. CONTAINS BENZYL ALCOHOL. NDC 17478-546-02 (package of 1 Single-dose Vial) NDC 17478-546-05 (package of 1 Multi-dose Vial) Granisetron Hydrochloride Injection, USP 0.1 mg/mL (free base), is supplied in 1 mL Single-dose Vials.

CONTAINS NO PRESERVATIVE. NDC 17478-547-01 (package of 10 Single-dose Vial) Storage: Store single-dose vials and multiple-dose vials at 20º to 25°C (68º to 77°F) [see USP Controlled Room Temperature]. Protect from light.

Do not freeze. Retain in carton until time of use. Once the multiple-dose vial is penetrated, its contents should be used within 30 days.

📦 Storage and Handling 46 words ▾

Storage: Store single-dose vials and multiple-dose vials at 20º to 25°C (68º to 77°F) [see USP Controlled Room Temperature]. Protect from light. Do not freeze. Retain in carton until time of use. Once the multiple-dose vial is penetrated, its contents should be used within 30 days.

📋 Description 214 words ▾

11 DESCRIPTION Granisetron Hydrochloride Injection, USP is a serotonin-3 (5-HT 3 ) receptor antagonist. Chemically it is endo -N-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride. Its chemical structure is: Granisetron hydrochloride C 18 H 24 N 4 O•HCl M.W.

348.9 (312.4 free base) Granisetron hydrochloride is a white to off-white solid that is readily soluble in water and normal saline at 20°C. Granisetron hydrochloride injection, USP is a clear, colorless, sterile, nonpyrogenic, aqueous solution for intravenous administration. Granisetron hydrochloride injection, USP 1 mg/mL is available in 1 mL Single-dose and 4 mL Multiple-dose vials.

Granisetron hydrochloride injection, USP 0.1 mg/mL is available in a 1 mL single-dose vial. 1 mg/mL: Each 1 mL contains: Active: Granisetron hydrochloride 1.12 mg, equivalent to granisetron, 1 mg; Inactives: Sodium Chloride, 9 mg; Citric Acid, 2 mg; Sodium Citrate, Dihydrate, Sodium Hydroxide and/or Hydrochloric Acid may be added to adjust pH (approximately 4.0 to 6.0), and Water for Injection q.s. to 1 mL; Preservative: Benzyl Alcohol, 10 mg. 0.1 mg/mL (preservative-free): Each mL contains: Active: Granisetron hydrochloride 0.112 mg, equivalent to granisetron, 0.1 mg; Inactives: Sodium Chloride, 9 mg; Citric Acid, 2 mg: Sodium Citrate, Dihydrate, Sodium Hydroxide and/or Hydrochloric Acid may be added to adjust pH (approximately 4.0 to 6.0), and Water for Injection q.s. to 1 mL.

Chemical Structure

💬 Information for Patients 155 words ▾

17 PATIENT COUNSELING INFORMATION Patients should be informed that the most common adverse reactions for the indication of chemotherapy induced nausea and vomiting are headache and constipation (see Table 1 ). Patients should be advised of the risk of allergic reactions if they have a prior allergic reaction to a class of antiemetics known as 5-HT 3 receptor antagonists. Electrocardiogram changes (QT prolongation) have been reported with the use of granisetron hydrochloride.

Patients should be cautioned about the use of this drug if they have heart problems or take medications for heart problems. Advise patients of the possibility of serotonin syndrome with concomitant use of granisetron and another serotonergic agent such as medications to treat depression and migraines. Advise patients to seek immediate medical attention if the following symptoms occur: changes in mental status autonomic instability neuromuscular symptoms with or without gastrointestinal symptoms.

AKORN Manufactured by: Akorn, Inc. Lake Forest, IL 60045 GR00N Rev. 05/18

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
← 17445-6034-00 · Sigma-Aldrich 17504-0007-02 · Lonza →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.