SUDAFED 12 HOUR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUDAFED 12 HOUR (SUDAFED 12 HOUR).
Pseudoephedrine is a sympathomimetic amine that acts as an agonist at alpha-1 and alpha-2 adrenergic receptors, causing vasoconstriction of nasal mucosa and reducing nasal congestion.
| Metabolism | Hepatic metabolism via N-demethylation to active metabolite; primarily excreted unchanged in urine |
| Excretion | Renal: 74-95% as unchanged drug; 1-4% as active metabolite (norpsuedoephedrine); biliary/fecal: minimal (<1%) |
| Half-life | 8-10 hours in adults with normal renal function; prolonged to 19-24 hours in renal impairment (CrCl <30 mL/min); shorter in children (3-4 hours) |
| Protein binding | 50-60% bound (primarily to albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | 2.6-3.5 L/kg in adults; indicates extensive tissue distribution (higher than total body water) |
| Bioavailability | Oral: 90-100% (immediate-release); sustained-release: approximately 95% |
| Onset of Action | Oral: 15-30 minutes; peak effect: 1-2 hours |
| Duration of Action | Sustained-release formulation: 12 hours; immediate-release: 4-6 hours; clinical decongestant effect lasts up to 12 hours with SUDAFED 12 HOUR |
120 mg orally every 12 hours, extended-release tablets. Maximum 240 mg per day.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 30-50 mL/min: reduce dose to 60 mg every 12 hours. GFR <30 mL/min: use is contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: consider reducing dose or extending interval due to reduced clearance; specific guidelines not established. |
| Pediatric use | Children 6-12 years: 60 mg orally every 12 hours; maximum 120 mg/day. Children <6 years: not recommended. |
| Geriatric use | Start at lower end of dosing range (60 mg every 12 hours); monitor for CNS stimulation, hypertension, and urinary retention. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUDAFED 12 HOUR (SUDAFED 12 HOUR).
| Breastfeeding | Pseudoephedrine is excreted into breast milk (M/P ratio approximately 2.0-3.5). Use with caution: may reduce milk production and cause irritability in infants. Highest risk in preterm infants or those with impaired renal function. Avoid if possible; use lowest effective dose if necessary. |
| Teratogenic Risk | Category C. First trimester: Possible risk of gastroschisis (limited data). Second and third trimesters: Uterine vasoconstriction, reduced placental perfusion; avoid due to risk of fetal hypoxia, tachycardia, and intrauterine growth restriction. No adequate well-controlled human studies. |
■ FDA Black Box Warning
None
| Serious Effects |
["Severe hypertension","Coronary artery disease","Concurrent or recent (within 14 days) MAOI therapy","Narrow-angle glaucoma","Urinary retention"]
| Precautions | ["Cardiovascular effects: hypertension, palpitations, tachycardia","CNS stimulation: insomnia, nervousness, dizziness","Exacerbation of narrow-angle glaucoma","Exacerbation of prostatic hypertrophy/urinary retention","Diabetes mellitus: may increase blood glucose"] |
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| Fetal Monitoring | Maternal: Blood pressure, heart rate, signs of hypertension or tachycardia. Fetal: Ultrasound for growth (if chronic use), fetal heart rate monitoring if used near term. Avoid use in preeclampsia or hypertension. |
| Fertility Effects | No specific human data. Animal studies show no effect on fertility at clinically relevant doses. Potential indirect effects due to vasoconstriction on uterine blood flow, but no evidence of impaired fertility. |