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ropivacaine hydrochloride injection, USP Nonclinical Toxicology

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Long-term studies in animals to evaluate the carcinogenic potential of ropivacaine have not been conducted.

Mutagenesis

Weak mutagenic activity was seen in the mouse lymphoma test. However, ropivacaine was negative in an in vitro Ames assay and an in vivo mouse micronucleus assay.

Impairment of Fertility

No adverse effects on fertility or early embryonic development were reported in a 2-generational reproduction study in which female rats (F0) were administered subcutaneous doses of 6.3, 12, and 23 mg/kg/day (equivalent to 0.08, 0.15, and 0.29 times the maximum recommended human dose (MRHD) of 770 mg/24 hours for epidural use, respectively, and 0.24, 0.45, and 0.88 times the MRHD of 250 mg for nerve block use, respectively, based on BSA comparisons and a 60 kg human) throughout the mating period and pregnancy, partus, and lactation.

13.2 Animal Toxicology and/or Pharmacology

The mean dosages of ropivacaine producing seizures, after intravenous infusion in dogs, non-pregnant and pregnant sheep were 4.9, 6.1 and 5.9 mg/kg (HED: 5.3, 6.6 and 6.4 mg/kg, based on 75 kg sheep weight and 60 kg human weight) respectively. These doses were associated with peak arterial total plasma concentrations of 11.4, 4.3 and 5 mcg/mL, respectively.

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