Amide Local AnestheticPrescription OnlyPregnancy Cat. Not classifiedFDA Yes
Zynrelef
BUPIVACAINE AND MELOXICAM
1 INDICATIONS AND USAGE ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic surgical procedures – foot and ankle procedures – other orthopedic surgical procedures (e.g., total joint arthroplasty) in which direct exposure to articular cartilage is avoided [see Warnings and Precautions (5.10) ] ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic su...
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Brand names:ZYNRELEF
Quick Reference
Medicine ClassAmide Local Anesthetic
FDA ApprovedYes
PregnancyCategory Not classified
Quick Facts
- Active ingredient
- BUPIVACAINE AND MELOXICAM
- Medicine class
- Amide Local Anesthetic
- Brand names
- ZYNRELEF
- Availability
- Prescription only (Rx)
- Pregnancy category
- Not classified
- Half-life
- half-life (t 1/2 ) for bupivacaine from ZYNRELEF is approximately 10 to 25 hours
- FDA approved
- Yes
What Is Zynrelef?
1 INDICATIONS AND USAGE ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic surgical procedures – foot and ankle procedures – other orthopedic surgical procedures (e.g., total joint arthroplasty) in which direct exposure to articular cartilage is avoided [see Warnings and Precautions (5.10) ] ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic su...
Zynrelef (BUPIVACAINE AND MELOXICAM) belongs to the Amide Local Anesthetic class of medications. It was first approved by the FDA in Yes. This medication requires a prescription from a licensed healthcare provider.
Key Safety Information
- •Always follow the dose recommended by your healthcare professional. Taking more than prescribed increases the risk of side effects including serious complications.
- •Seek emergency care if you experience signs of an allergic reaction — hives, swelling, difficulty breathing, or rash. Stop the medication and call your doctor immediately.
- •Some medications can increase the risk of cardiovascular events. Tell your doctor if you have high blood pressure, a history of heart attack or stroke, or any pre-existing health condition.
- •Avoid or limit alcohol while taking Zynrelef. Do not drink alcohol without first discussing it with your healthcare provider as it may increase adverse effects.
- •Take Zynrelef with food or a full glass of water if stomach upset occurs. Stop use and talk to your doctor if you experience persistent stomach pain or GI symptoms.
- •Tell your doctor about all medications, supplements, and vitamins you take. Some combinations significantly increase the risk of harm.
This is a summary only. Always read the full prescribing information and consult your healthcare provider for personalized medical advice.
Uses & Indications
Zynrelef is prescribed for the following conditions. Some uses are FDA-approved indications; others may be evidence-based off-label uses. Consult your healthcare provider for personalized guidance.
1 INDICATIONS AND USAGE ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic surgical procedures – foot and ankle procedures – other orthopedic surgical procedures (e.g., total joint arthroplasty) in which direct exposure to articular cartilage is avoided [see Warnings and Precautions (5.10) ] ZYNRELEF is indicated in adults for postsurgical analgesia for up to 72 hours after: soft tissue surgical procedures orthopedic surgical procedures – foot and ankle procedures – other orthopedic surgical procedures (e.g., total joint arthroplasty) in which direct exposure to articular cartilage is avoided [see Warnings and Precautions (5.10) ] Limitations of Use Safety and efficacy have not been established in highly vascular surgeries, such as intrathoracic, large 4 or more level spinal, and head and neck procedures ( 1 ).
Limitations of Use Safety and efficacy have not been established in highly vascular surgeries, such as intrathoracic, large 4 or more level spinal, and head and neck procedures.
Dosage Guide
The following are general dosing guidelines only. Your actual dose should be determined by your healthcare provider based on your condition, renal/hepatic function, and other medications.
AD
Adult Dosage
2 DOSAGE AND ADMINISTRATION ZYNRELEF is intended for single-dose administration only ( 2.1 ). Administer ZYNRELEF via instillation only. The toxic effects of local anesthetics are additive. Avoid additional use of local anesthetics within 96 hours following administration of ZYNRELEF ( 2.1 ). ZYNRELEF should only be prepared and administered with the components provided in the ZYNRELEF kit ( 2.1 ). ZYNRELEF is applied without a needle into the surgical site following final irrigation and suction and prior to suturing ( 2.1 ). – The recommended dose of ZYNRELEF is up to a maximum dose of 400 mg/12 mg (14 mL) ( 2.4 ). See Full Prescribing Information for important preparation and administration instructions, dose selection, and compatibility considerations ( 2.2 , 2.3 , 2.4 , 2.5 ). 2.1 Important Dosage and Administration Information ADMINISTER ZYNRELEF VIA INSTILLATION ONLY. ZYNRELEF should not be administered via the following routes. – Epidural – Intrathecal – Intravascular – Intra-ar
Available Forms
Available Strengths
Side Effects
Common
- 6 ADVERSE REACTIONS The following serious adverse reactions have been associated with bupivacaine HCl or meloxicam and are discussed in greater detail in other sections of the labeling: Cardiovascular System Reactions [see Warnings and Precautions (5.1 , 5.4) ] Gastrointestinal Bleeding, Ulceration, and Perforation [see Warnings and Precautions (5.2) ] Dose-Related Toxicity [see Warnings and Precautions (5.3) ] Hepatotoxicity [see Warnings and Precautions (5.5) ] Hypertension [see Warnings and Precautions (5.6) ] Heart Failure and Edema [see Warnings and Precautions (5.7) ] Renal Toxicity and Hyperkalemia [see Warnings and Precautions (5.8) ] Anaphylactic Reactions [see Warnings and Precautions (5.9) ] Chondrolysis [see Warnings and Precautions (5.11) ] Methemoglobinemia [see Warnings and Precautions (5.12) ] Exacerbation of Asthma Related to Aspirin Sensitivity [see Warnings and Precautions (5.13) ] Serious Skin Reactions [see Warnings and Precautions (5.14) ] Drug Reaction with Eosinophilia and Systemic Toxicity (DRESS) [see Warnings and Precautions (5.15) ] Fetal Toxicity [see Warnings and Precautions (5.16) ] Hematologic Toxicity [see Warnings and Precautions (5.17) ] Most common adverse reactions (incidence ≥5%) are: Soft tissue procedures: vomiting ( 6.1 ).
- Orthopedic procedures: constipation and headache ( 6.1 ).
- To report SUSPECTED ADVERSE REACTIONS, contact Heron Therapeutics, Inc.
- at 1-844-437-6611 and www.ZYNRELEF.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
- 6.1 Clinical Trials Experience Because clinical studies 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 studies of another drug and may not reflect the rates observed in practice.
- The safety of ZYNRELEF has been evaluated in a total of 1627 patients undergoing various surgical procedures across 14 clinical studies including 7 randomized, double-blind, bupivacaine- and placebo-controlled and saline placebo-controlled studies designed to investigate ZYNRELEF to reduce postoperative pain for 72 hours and the need for opioid analgesics, of whom 1183 received ZYNRELEF by instillation.
- Patients treated with ZYNRELEF ranged in age from 18 to 85 years (median age 51 years), with 53.0% female, 82.1% White, 13.7% African-American, and 4.3% all other races.
Serious
- 5 WARNINGS AND PRECAUTIONS Dose-Related Toxicity : Monitor cardiovascular and respiratory vital signs and patient's state of consciousness after application of ZYNRELEF ( 5.3 ).
- When using ZYNRELEF with other local anesthetics, overall local anesthetic exposure must be considered through 72 hours ( 5.3 ).
- Hepatotoxicity : If abnormal liver tests persist or worsen, perform a clinical evaluation of the patient ( 5.5 ).
- Hypertension : Patients taking some antihypertensive medications may have impaired response to these therapies when taking NSAIDs.
- Monitor blood pressure ( 5.6 , 7 ).
Rare
Medicine Interactions
Always inform your healthcare provider and pharmacist about ALL medications you take, including prescriptions, OTC medicines, vitamins, and supplements.
MajorModerateMinor
Warnings & Contraindications
5 WARNINGS AND PRECAUTIONS Dose-Related Toxicity : Monitor cardiovascular and respiratory vital signs and patient's state of consciousness after application of ZYNRELEF ( 5.3 ). When using ZYNRELEF with other local anesthetics, overall local anesthetic exposure must be considered through 72 hours ( 5.3 ). Hepatotoxicity : If abnormal liver tests persist or worsen, perform a clinical evaluation of
How Zynrelef Works
12.1 Mechanism of Action ZYNRELEF is a fixed-dose combination of bupivacaine and meloxicam. Bupivacaine Local anesthetics block the generation and the conduction of nerve impulses presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone. Meloxicam The mechanism of action of meloxicam, like that of other NSAIDs, is not completely understood but involves inhibition of cyclooxygenase (COX
Pharmacokinetics
Absorption
Absorption The rate of systemic absorption of bupivacaine or meloxicam from ZYNRELEF is dependent upon the total dose of drug administered and the vascularity of the administration site
Half-Life
half-life (t 1/2 ) for bupivacaine from ZYNRELEF is approximately 10 to 25 hours
Metabolism
Metabolism Bupivacaine Amide-type local anesthetics such as bupivacaine are metabolized primarily in the liver via conjugation with glucuronic acid
Excretion
Excretion After bupivacaine and meloxicam have been released from ZYNRELEF and are absorbed systemically, their excretion is expected to be the same as for other bupivacaine HCl solution formulations
Pregnancy & Breastfeeding Safety
Not classified
Breastfeeding
Many medications pass into breast milk in varying amounts. Before using Zynrelefwhile breastfeeding, discuss the benefits and risks with your healthcare provider or pharmacist — they can weigh your dose, your infant's age, and available lactation safety data to find the safest option for you and your baby.
Storage & Handling
Storage Store ZYNRELEF kits at 20°C to 25°C (68°F to 77°F) with excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Protect from moisture and light. If ZYNRELEF vials are removed from the kit, store them at controlled room temperature. Protect from light d
Frequently Asked Questions
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Zynrelef side effects
Complete adverse effect profile including common, serious, and rare reactions
Sources & References
- • FDA Prescribing Information — Official labeling and package insert for Zynrelef
- • U.S. National Library of Medicine — MedlinePlus drug information
- • American Hospital Formulary Service (AHFS) — Clinical pharmacology monograph
- • PubMed / MEDLINE — View clinical studies
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Medical Disclaimer
The information on this page is for educational purposes only and is not intended as medical advice, diagnosis, or treatment. Always consult your doctor, pharmacist, or qualified healthcare provider before starting, stopping, or changing any medication.