TUSSIGON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TUSSIGON (TUSSIGON).
TUSSIGON (cloperastine fendizoate) is a centrally acting antitussive agent. It suppresses the cough reflex by acting on the cough center in the medulla oblongata, without affecting the respiratory center. Additionally, it exhibits mild antihistaminic and local anesthetic properties.
| Metabolism | Hepatic metabolism via CYP450 enzymes (primarily CYP3A4 and CYP2D6); major metabolite is cloperastine N-oxide. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 60% of elimination, with the remainder undergoing hepatic metabolism followed by renal excretion of metabolites. Fecal excretion is minimal (<5%). |
| Half-life | The terminal elimination half-life is approximately 4–6 hours in adults with normal renal function, allowing for dosing every 6–8 hours. In renal impairment (CrCl <30 mL/min), half-life may extend to 12–18 hours. |
| Protein binding | Approximately 25–30% bound to serum albumin. |
| Volume of Distribution | 3.5–5.0 L/kg, indicating extensive tissue distribution and accumulation in peripheral compartments. |
| Bioavailability | Oral bioavailability is 40–50% due to first-pass hepatic metabolism; intramuscular bioavailability is nearly 100%. |
| Onset of Action | Oral administration: 30–60 minutes; intramuscular injection: 10–20 minutes; intravenous injection: 2–5 minutes. Onset may be delayed with food. |
| Duration of Action | Oral: 4–6 hours; parenteral: 3–5 hours. Clinical antitussive effect lasts 4–6 hours, supporting q6h dosing. |
5-10 mg orally every 6-8 hours as needed for cough, maximum 40 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-50 mL/min: increase dosing interval to every 12 hours; GFR <30 mL/min: increase interval to every 24 hours or avoid use. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: avoid use. |
| Pediatric use | Children 6-12 years: 2.5-5 mg orally every 6-8 hours, maximum 20 mg/day; <6 years: not recommended. |
| Geriatric use | Start at 2.5 mg every 8-12 hours due to increased sensitivity and risk of sedation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TUSSIGON (TUSSIGON).
| Breastfeeding | No human data on excretion into breast milk; M/P ratio unknown. Use caution due to potential for respiratory depression or sedation in infant; benefit of breastfeeding should outweigh minimal risk. |
| Teratogenic Risk | Insufficient human data; animal studies not located. First trimester: avoid unless benefit outweighs risk due to lack of data. Second and third trimesters: no specific malformation signal identified; monitor for maternal respiratory depression and neonatal withdrawal if used near term. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to cloperastine or any component of the formulation","Concurrent MAO inhibitor therapy or within 14 days of discontinuation","Severe respiratory failure or asthma attack","Pregnancy and lactation (relative contraindication; use only if benefit outweighs risk)"]
| Precautions | ["May cause drowsiness or dizziness; caution when driving or operating machinery.","Avoid concurrent use with CNS depressants (e.g., alcohol, sedatives).","Use with caution in patients with liver or renal impairment.","Prolonged use may lead to dependence or abuse potential.","Not recommended in children under 2 years due to risk of respiratory depression."] |
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| Monitor maternal respiratory rate, oxygen saturation, and level of sedation. Fetal heart rate monitoring if used during labor. Assess neonatal respiratory status and Apgar scores at delivery if used near term. |
| Fertility Effects | No human studies on fertility; animal reproductive studies not available. Theoretical risk of hormonal disruption based on opioid class effects; clinical significance unknown. |