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. |
| Molecular Weight | 249.31 |
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 | Generally avoided due to potential teratogenicity; limited human data, but animal studies indicate risk. |
| 2nd trimester | Use only if clearly needed; no well-controlled studies in humans. |
| 3rd trimester | Avoid in late pregnancy due to risk of respiratory depression in neonate. |
Clinical note
Comprehensive clinical and safety monograph for TUSSIGON (TUSSIGON).
| Placental transfer | Crosses placenta; documented in animal studies and assumed in humans due to pharmacokinetics. |
| Breastfeeding | Excreted into breast milk; potential for infant sedation and respiratory depression; use with caution and monitor infant for lethargy and poor feeding. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to TUSSIGON or any componentSignificant respiratory depressionAcute or severe bronchial asthmaCor pulmonaleGI obstructionConcurrent use of MAOIs or within 14 days
| 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. |
| Food/Dietary | Avoid grapefruit juice as it may increase serum levels via CYP3A4 inhibition. Avoid excessive caffeine intake as it may reduce antitussive effects. Maintain adequate fluid and fiber intake to prevent opioid-induced constipation. |
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| L3 |
| 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 | 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. |
| Clinical Pearls | TUSSIGON (dihydrocodeine bitartrate) is a semi-synthetic opioid antitussive. Use with caution in patients with respiratory depression, asthma, COPD, or head injury. Monitor for CNS depression when co-administered with other CNS depressants. Avoid in patients with MAOI use within 14 days. May cause physical dependence; taper to discontinue. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Avoid alcohol and other CNS depressants (e.g., sedatives, tranquilizers) as they may cause severe drowsiness or respiratory depression. · Do not drive or operate machinery until you know how this medication affects you. · Do not share this medication with others; it can cause fatal respiratory depression in children or individuals for whom it is not prescribed. · Store securely out of sight and reach of children; properly dispose of unused medication via a drug take-back program. · Report any symptoms of allergic reaction (rash, itching, swelling of face/tongue, difficulty breathing) or severe constipation. |