PAREDRINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PAREDRINE (PAREDRINE).
Paredrine (hydroxyamphetamine) is a sympathomimetic amine that acts as an indirect-acting adrenergic agonist, displacing norepinephrine from presynaptic nerve terminals and inhibiting its reuptake, leading to activation of alpha- and beta-adrenergic receptors.
| Metabolism | Primarily metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT). |
| Excretion | Renal (approximately 80% as unchanged drug and metabolites); biliary/fecal (minor, <10%). |
| Half-life | Terminal elimination half-life is 12-15 hours; may be prolonged in renal impairment. |
| Protein binding | Approximately 20%; primarily to albumin. |
| Volume of Distribution | Vd approximately 3-5 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 80-90% (first-pass metabolism minimal). |
| Onset of Action | Oral: 30-60 minutes; Intravenous: within 5 minutes. |
| Duration of Action | Oral: 4-6 hours; Intravenous: 2-3 hours. |
5-10 mg intramuscularly (IM) or subcutaneously (SC) every 30-60 minutes as needed; intravenous (IV) dose: 2-5 mg every 5-10 minutes, not to exceed 50 mg total.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No specific dose adjustment guidelines available; use with caution in severe renal impairment (CrCl <30 mL/min) due to risk of accumulation. |
| Liver impairment | No specific dose adjustment guidelines available; caution in severe hepatic impairment (Child-Pugh C) due to potential prolonged effects. |
| Pediatric use | Not recommended for pediatric use; safety and efficacy not established. |
| Geriatric use | Use lower initial doses (2.5-5 mg) due to increased sensitivity; monitor for hypertension, tachycardia, and CNS stimulation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PAREDRINE (PAREDRINE).
| Breastfeeding | It is unknown whether hydroxyamphetamine is excreted in human breast milk. No M/P ratio is available. Due to its sympathomimetic effects, it may potentially cause adverse effects in the nursing infant (e.g., tachycardia, irritability). Breastfeeding is not recommended during therapy. |
| Teratogenic Risk | Paredrine (hydroxyamphetamine) is a sympathomimetic amine. Data on teratogenicity in humans are limited. Animal studies have not been reported. Due to its vasoconstrictive properties, use in the first trimester may theoretically pose a risk of fetal hypoxia; however, no specific malformations are documented. In the second and third trimesters, potential risks include reduced uteroplacental blood flow and fetal tachycardia. Avoid use unless clearly needed. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to hydroxyamphetamine or any component","Concurrent use of MAO inhibitors or within 14 days","Narrow-angle glaucoma (for ophthalmic use)"]
| Precautions | ["May cause severe hypertension in patients with hyperthyroidism","Use with caution in patients with cardiovascular disease or hypertension","Potential for tachyphylaxis with prolonged use"] |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and fetal heart rate (if applicable). Assess for signs of uterine hyperstimulation if used as a mydriatic agent. Long-term use requires monitoring for maternal arrhythmias and hypertensive crisis. |
| Fertility Effects | No studies have evaluated effects on fertility. Sympathomimetics can theoretically alter uterine blood flow, but no direct evidence of impaired fertility exists. Effects on spermatogenesis or ovulation are unknown. |