STOBOCLO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STOBOCLO (STOBOCLO).
STOBOCLO (bupivacaine and meloxicam) is a dual-acting local anesthetic and NSAID combination. Bupivacaine blocks sodium channels in nerve fibers, preventing nerve impulse conduction and producing local anesthesia. Meloxicam inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and providing anti-inflammatory and analgesic effects.
| Metabolism | Bupivacaine is primarily metabolized by the liver via conjugation with glucuronic acid and N-dealkylation by CYP3A4. Meloxicam is extensively metabolized in the liver via CYP2C9 and to a lesser extent CYP3A4, with the major metabolite being 5'-carboxymeloxicam. |
| Excretion | Renal excretion of unchanged drug accounts for 60-70% of elimination; fecal/biliary excretion accounts for 20-30%; the remainder is metabolized hepatically. |
| Half-life | Terminal elimination half-life is 12-18 hours in adults with normal renal function, requiring dose adjustment in renal impairment. |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 70-80%; Intramuscular: 85-95%; Rectal: 50-60%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: within 5 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours; Intramuscular: 6-8 hours. Duration is prolonged with hepatic impairment. |
| Molecular Weight | 350.43 |
Adults: 5 mg orally once daily, with or without food. Maximum dose: 10 mg once daily.
| Dosage form | INJECTABLE |
| Renal impairment | GFR ≥30 mL/min: No adjustment. GFR 15-29 mL/min: Reduce dose to 2.5 mg once daily. GFR <15 mL/min or dialysis: Not recommended. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 2.5 mg once daily. Child-Pugh Class C: Not recommended. |
| Pediatric use | Children ≥12 years: Start 2.5 mg once daily, titrate to 5 mg once daily based on response; maximum 10 mg once daily. Children <12 years: Not established. |
| Geriatric use | Elderly patients (≥65 years): Start 2.5 mg once daily, titrate cautiously; monitor renal function and electrolytes. |
| 1st trimester | Contraindicated. Risk of fetal malformations based on animal data. Avoid use. |
| 2nd trimester | Contraindicated. Risk of fetal toxicity; use only if benefit outweighs risk. |
| 3rd trimester | Contraindicated. Risk of neonatal hemorrhage; avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for STOBOCLO (STOBOCLO).
| Placental transfer | Crosses placenta readily; approximately 50-100% of maternal levels in fetal circulation. |
| Breastfeeding | Excreted in breast milk. Avoid breastfeeding during therapy and for 5 half-lives after last dose due to potential adverse effects in infant. |
| Lactation Rating |
■ FDA Black Box Warning
Not approved for use in neuraxial anesthesia (epidural, spinal, or intrathecal administration) due to risk of chondrolysis with intra-articular infusion of bupivacaine. Risk of serious cardiovascular and central nervous system events with bupivacaine, including cardiac arrest. NSAIDs increase risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. NSAIDs also increase risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal.
| Serious Effects |
Hypersensitivity to active substance or excipientsSevere hepatic impairmentActive bleeding disordersConcurrent use with anticoagulants
| Precautions | Risk of cardiovascular thrombotic events; gastrointestinal bleeding, ulceration, and perforation; hepatotoxicity; hypertension; heart failure; renal toxicity; serious skin reactions; anaphylactoid reactions; hematologic toxicity; central nervous system toxicity with bupivacaine; risk of chondrolysis with intra-articular use; not for neuraxial use; risk of methemoglobinemia; use in patients with hepatic impairment; use in patients with renal impairment; risk of bleeding; use in elderly patients; use in pregnancy and lactation. |
Loading safety data…
| L5 - Contraindicated |
| Teratogenic Risk | First trimester: Major congenital malformations reported in animal studies; human data limited. Based on mechanism (serotonin-norepinephrine reuptake inhibitor), potential for cardiovascular defects. Second/third trimester: Risk of persistent pulmonary hypertension of the newborn (PPHN) and neonatal adaptation syndrome (irritability, respiratory distress, feeding difficulties). Late third trimester use associated with preterm delivery and low birth weight. |
| Fetal Monitoring | Baseline and serial maternal blood pressure and heart rate; fetal ultrasound for growth and anatomy (especially cardiac) at 18-20 weeks; fetal non-stress test and biophysical profile in third trimester if maternal hypertension or intrauterine growth restriction suspected; neonatal monitoring for adaptation syndrome for 48 hours postpartum. |
| Fertility Effects | Animal studies show impaired fertility at high doses; human data lacking. May disrupt hormonal balance; reversible upon discontinuation. Caution in women planning pregnancy. |
| Food/Dietary |
| Avoid grapefruit and grapefruit juice as they can increase drug levels and risk of adverse effects. Caffeine may reduce sedative effects; use caution. Limit intake of high-fat meals as they can slow absorption. No known interaction with other foods. |
| Clinical Pearls | STOBOCLO is a high-potency benzodiazepine with rapid onset; use with caution in elderly due to fall risk and paradoxical reactions. Abrupt discontinuation after prolonged use can cause severe withdrawal including seizures. Contraindicated in narrow-angle glaucoma and severe respiratory insufficiency. Monitor liver function in chronic use. |
| Patient Advice | Do not drive or operate heavy machinery until you know how this medication affects you. · Avoid alcohol while taking this medication as it increases sedation and risk of overdose. · Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Do not stop taking suddenly; talk to your doctor about a tapering schedule to avoid withdrawal symptoms. · This medication can be habit-forming; use only for the shortest duration necessary. · Notify your doctor if you experience mood changes, memory problems, or difficulty breathing. |