EFIDAC 24 PSEUDOEPHEDRINE HYDROCHLORIDE/BROMPHENIRAMINE MALEATE
Clinical safety rating: safe
MAOIs can cause hypertensive crisis Can cause insomnia and tachycardia.
Pseudoephedrine is a sympathomimetic amine that acts as a decongestant by stimulating alpha-adrenergic receptors in the respiratory tract mucosa, causing vasoconstriction and reducing nasal congestion. Brompheniramine is a first-generation antihistamine that competitively antagonizes histamine at H1 receptors, alleviating symptoms of allergic rhinitis.
| Metabolism | Pseudoephedrine is partially metabolized in the liver by N-demethylation via CYP450 enzymes; about 70-90% is excreted unchanged in urine. Brompheniramine is extensively metabolized in the liver via CYP450 enzymes (CYP2D6, CYP3A4) and other pathways, with renal excretion of metabolites. |
| Excretion | Pseudoephedrine: ~70-90% excreted unchanged in urine, with the remainder as inactive metabolites; renal elimination depends on urine pH (acidic urine increases excretion). Brompheniramine: ~75% metabolized in liver; renal excretion of metabolites and <5% unchanged; biliary/fecal elimination is minor. |
| Half-life | Pseudoephedrine: 4-6 hours (range 3-16 hours); prolonged in alkaline urine or renal impairment. Brompheniramine: 11-27 hours (mean ~24 hours); prolonged in elderly or hepatic impairment. |
| Protein binding | Pseudoephedrine: Low, ~20-30% bound to plasma proteins (primarily albumin). Brompheniramine: 70-80% bound to plasma proteins (albumin). |
| Volume of Distribution | Pseudoephedrine: 2.6-3.3 L/kg; distributes widely including CSF. Brompheniramine: 4.5-12 L/kg; extensive tissue distribution. |
| Bioavailability | Pseudoephedrine: Oral, ~100% (well absorbed). Brompheniramine: Oral, 50-70% due to first-pass metabolism. |
| Onset of Action | Pseudoephedrine: Oral, 15-30 minutes. Brompheniramine: Oral, 1-2 hours. |
| Duration of Action | Pseudoephedrine: Immediate release, 4-6 hours; extended release, up to 24 hours (as per EFIDAC 24). Brompheniramine: 4-6 hours for immediate release; extended release up to 12-24 hours (as per EFIDAC 24). |
| Molecular Weight | Pseudoephedrine HCl: 201.69 Da; Brompheniramine maleate: 435.52 Da; Combination drug product contains both. |
| Action Class | Sympathomimetic (pseudoephedrine) and first-generation antihistamine (brompheniramine) |
1 tablet orally every 12 hours. Each tablet contains pseudoephedrine HCl 120 mg and brompheniramine maleate 4 mg.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | For eGFR 15-30 mL/min: avoid or reduce to 1 tablet every 24 hours. For eGFR <15 mL/min: contraindicated. |
| Liver impairment | Child-Pugh class A: no adjustment. Child-Pugh class B: reduce to 1 tablet every 24 hours. Child-Pugh class C: avoid or contraindicated. |
| Pediatric use | Not recommended for children under 12 years. For ages 12 and above, same as adult dosing. |
| Geriatric use | Avoid in patients >65 years due to increased risk of anticholinergic effects; if necessary, use 1 tablet every 24 hours. |
| 1st trimester | Pseudoephedrine is associated with a small risk of gastroschisis and other birth defects if used in first trimester; brompheniramine is generally considered safe but data limited. Avoid use unless benefit outweighs risk. |
| 2nd trimester | Pseudoephedrine may cause uterine artery vasoconstriction; brompheniramine has anticholinergic effects. Use only if clearly needed. |
| 3rd trimester | Pseudoephedrine may cause uterine artery vasoconstriction and reduced placental perfusion; avoid near term due to risk of neonatal irritability and respiratory depression. Brompheniramine may cause neonatal withdrawal symptoms. |
Clinical note
MAOIs can cause hypertensive crisis Can cause insomnia and tachycardia.
| FDA category | Animal |
| Placental transfer | Pseudoephedrine crosses the placenta (fetal-to-maternal ratio ~0.7). Brompheniramine likely crosses placenta; limited data. |
■ FDA Black Box Warning
None
| Common Effects | Insomnia |
| Serious Effects | Hypertension, Tachycardia, Arrhythmias, Myocardial infarction, Stroke, Seizures, Psychosis, Urinary retention, Angle-closure glaucoma |
Hypersensitivity to pseudoephedrine or brompheniramineSevere hypertensionSevere coronary artery diseaseMonoamine oxidase inhibitor (MAOI) use within 14 daysNarrow-angle glaucomaUrinary retentionSevere hepatic or renal impairment
| Precautions | May cause drowsiness; avoid driving or operating machinery, Use with caution in patients with hypertension, cardiovascular disease, diabetes, hyperthyroidism, increased intraocular pressure, prostatic hypertrophy, or urinary retention, Avoid concurrent use with MAO inhibitors or within 14 days of stopping them, Do not exceed recommended dosage due to risk of serious cardiovascular effects, Not recommended for patients with severe hepatic or renal impairment, May cause excitability in children, especially with overdose |
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| Breastfeeding | Pseudoephedrine is excreted into breast milk in small amounts, but may reduce milk supply and cause irritability in infants. Brompheniramine is excreted into breast milk and may cause drowsiness or irritability. Use with caution, especially in neonates or preterm infants. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Pseudoephedrine: First trimester use associated with gastroschisis (OR 1.8, 95% CI 1.0-3.2); avoid in first trimester. Second/third trimester: Risk of fetal tachycardia and reduced uterine blood flow; use only if benefit outweighs risk. Brompheniramine: Generally considered low risk; no consistent teratogenic signals. FDA Category for combination: Not assigned; pseudoephedrine is C, brompheniramine is B. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate due to pseudoephedrine's sympathomimetic effects. In third trimester, assess fetal heart rate and uterine activity if prolonged use. Watch for signs of fetal tachycardia or maternal hypertension. No specific fetal monitoring required for brompheniramine. |
| Fertility Effects | No direct evidence of adverse effects on fertility. Pseudoephedrine may cause transient vasoconstriction of reproductive organs; theoretical concern but no human data. Brompheniramine has no known impact on fertility. Combination not studied for fertility endpoints. |
| Food/Dietary |
| Avoid high-tyramine foods (e.g., aged cheeses, cured meats) as pseudoephedrine may increase blood pressure. Limit caffeine intake as it may exacerbate stimulant effects. Alcohol may increase sedation from brompheniramine. |
| Clinical Pearls | Avoid use in patients with severe hypertension or coronary artery disease due to pseudoephedrine's vasoconstrictive effects. Brompheniramine may cause sedation; caution when driving. Use with caution in patients with narrow-angle glaucoma, prostatic hypertrophy, or urinary retention. Extended-release formulation should not be crushed or chewed. |
| Patient Advice | Do not crush or chew the tablets; swallow whole. · May cause drowsiness; avoid alcohol and do not drive or operate machinery if affected. · Do not use with other medications containing pseudoephedrine or other decongestants. · Stop use and consult a doctor if symptoms persist beyond 7 days or are accompanied by fever. · Inform your doctor if you have high blood pressure, heart disease, diabetes, or thyroid disease. |