PSEUDOEPHEDRINE HYDROCHLORIDE
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. It also has weak beta-adrenergic activity.
| Metabolism | Hepatic metabolism via N-demethylation (CYP450, primarily CYP2D6) to active metabolite pseudoephedrine; minor metabolism to other metabolites. |
| Excretion | Renal: 70-90% unchanged via glomerular filtration and tubular secretion; fecal: <1%; biliary: minimal |
| Half-life | Terminal elimination half-life: 5-8 hours in adults with normal renal function, prolonged in renal impairment (up to 16-20 hours in severe impairment) |
| Protein binding | Plasma protein binding: 20-30% (primarily to albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | Apparent Vd: 2.5-3.5 L/kg, indicating extensive tissue distribution beyond plasma volume |
| Bioavailability | Oral: 100% (complete absorption, minimal first-pass metabolism) |
| Onset of Action | Oral: 15-30 minutes; intranasal: 5-10 minutes |
| Duration of Action | Oral: 4-6 hours (immediate-release), up to 12 hours (extended-release); intranasal: 2-4 hours |
60 mg orally every 4 to 6 hours as needed; maximum 240 mg per day.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 10-50 mL/min: administer every 12 hours; GFR <10 mL/min: avoid use due to risk of accumulation. |
| Liver impairment | No specific adjustment recommended for Child-Pugh Class A or B; use with caution in severe hepatic impairment (Child-Pugh Class C) due to limited data. |
| Pediatric use | Children 6-11 years: 30 mg orally every 4-6 hours; maximum 120 mg/day. Children ≥12 years: same as adult dosing. |
| Geriatric use | Start at lower end of dosing range (30 mg every 6 hours) due to increased sensitivity and potential for adverse effects; monitor blood pressure and heart rate. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
MAOIs can cause hypertensive crisis Can cause insomnia and tachycardia.
| FDA category | Animal |
| Breastfeeding | Small amounts excreted into breast milk; M/P ratio approximately 3.0. Use with caution due to potential irritability and sleep disturbances in infants. Avoid in hypertensive or preterm infants. |
| Teratogenic Risk | First trimester: Increased risk of gastroschisis (OR 1.8) with first-trimester use; avoid use. Second and third trimesters: Uterine vasoconstriction may reduce placental perfusion; use only if benefit outweighs risk. No known structural teratogenicity beyond first trimester. |
■ FDA Black Box Warning
None.
| Common Effects | Insomnia |
| Serious Effects |
Hypersensitivity to pseudoephedrine, severe hypertension, severe coronary artery disease, concurrent use or within 14 days of MAO inhibitor therapy, narrow-angle glaucoma, urinary retention, or severe renal impairment.
| Precautions | Use with caution in patients with hypertension, cardiovascular disease, hyperthyroidism, diabetes, prostatic hypertrophy, or glaucoma. May cause CNS stimulation, nervousness, dizziness, or insomnia. Avoid in patients with severe coronary artery disease or angina. |
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| Fetal Monitoring | Monitor maternal blood pressure and heart rate due to potential hypertension and tachycardia. Assess fetal heart rate if used near term due to possible uterine vasoconstriction. Observe for signs of maternal CNS stimulation. |
| Fertility Effects | No known direct impact on fertility. May theoretically affect implantation via vasoconstrictive properties, but human data lacking. |