TESSALON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TESSALON (TESSALON).
Benzonatate is a local anesthetic structurally related to tetracaine that inhibits pulmonary stretch receptors and reduces the cough reflex by decreasing the sensitivity of vagal afferent fibers in the respiratory tract.
| Metabolism | Preferentially metabolized by cholinesterase and other plasma esterases to inactive metabolites. |
| Excretion | Renal: <5% unchanged; primary route is hepatic metabolism with metabolites excreted renally and fecally; exact biliary/fecal % not established in humans. |
| Half-life | Terminal elimination half-life is approximately 12-15 hours in adults; significant interindividual variability. No accumulation with q6h dosing. |
| Protein binding | Approximately 60-70%, primarily to albumin. |
| Volume of Distribution | ~2.5 L/kg; suggests extensive tissue distribution. |
| Bioavailability | Oral: ~30-40% due to extensive first-pass metabolism (hepatic and possibly pulmonary). |
| Onset of Action | Oral: 15-30 minutes for antitussive effect. |
| Duration of Action | Oral: 3-6 hours; clinical effect may persist up to 8 hours at higher doses (100 mg). |
100 mg orally three times daily as needed for cough. Maximum 600 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | No specific GFR-based dose adjustments established. Use with caution in severe renal impairment (CrCl <30 mL/min) due to uncertain excretion. |
| Liver impairment | No specific Child-Pugh-based adjustments established. Limited data in hepatic impairment; use with caution. |
| Pediatric use | Not recommended for use in children under 10 years due to risk of serious adverse effects. |
| Geriatric use | No specific dose adjustment required, but monitor for dizziness, sedation, and gastrointestinal effects due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TESSALON (TESSALON).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions (e.g., apnea, bronchospasm) in nursing infants, decision should be made to discontinue nursing or discontinue drug. |
| Teratogenic Risk | Pregnancy Category C. First trimester: Limited human data; animal studies not conducted. Potential risk based on mechanism (sodium channel blockade) cannot be excluded. Use only if benefit outweighs risk. Second/third trimester: No adequate studies; fetal bradycardia and hypoxia possible with maternal toxicity. |
■ FDA Black Box Warning
None
| Common Effects | Application site irritation Increased risk of infection Headache Joint pain Injection site reactions pain swelling redness |
| Serious Effects |
["Hypersensitivity to benzonatate or any component of the formulation","Hypersensitivity to tetracaine or other ester-type anesthetics","Children less than 10 years of age (due to risk of toxicity)"]
| Precautions | ["Accidental ingestion of capsules can lead to severe toxicity including cardiac arrest and death in children, especially those under 10 years of age.","Hypersensitivity reactions including bronchospasm, laryngospasm, and anaphylaxis.","Caution in patients with a history of drug allergy or allergic reactions to anesthetics of the ester type (e.g., tetracaine).","Avoid administering with food or water due to risk of oral mucosal anesthesia and choking."] |
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| Fetal Monitoring |
| Monitor maternal respiratory rate, oxygen saturation, and CNS status. Fetal monitoring (heart rate) recommended in third trimester if used near term due to risk of fetal bradycardia. |
| Fertility Effects | No human data on fertility impairment. In animal studies, no effects on fertility observed; however, relevance to humans unknown. |