PROCALAMINE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PROCALAMINE (PROCALAMINE).

How it works

Procalamine is a combination of antihistamines (chlorpheniramine and pheniramine) and a sympathomimetic (phenylephrine). Chlorpheniramine and pheniramine are histamine H1 receptor antagonists, blocking the effects of histamine, while phenylephrine is an alpha-1 adrenergic receptor agonist causing vasoconstriction.

What the body does with it

Metabolism	Chlorpheniramine undergoes hepatic metabolism via CYP450 enzymes (primarily CYP3A4, CYP2D6). Pheniramine is also metabolized in the liver. Phenylephrine undergoes extensive first-pass metabolism by intestinal and hepatic monoamine oxidase (MAO) and sulfotransferase.
Excretion	Primarily renal; >95% of the dose excreted unchanged in urine within 24 hours. Minimal biliary/fecal elimination (<5%).
Half-life	2.5–3.5 hours in healthy adults; prolonged in renal impairment (up to 20–30 hours in ESRD).
Protein binding	<5%; negligible binding to albumin or other plasma proteins.
Volume of Distribution	0.2–0.4 L/kg; indicates distribution largely confined to extracellular fluid.
Bioavailability	Subcutaneous: 55–80%; no oral bioavailability.
Onset of Action	Subcutaneous: 30–60 minutes; intravenous: immediate. Peak effect at 1–3 hours.
Duration of Action	3–6 hours for subcutaneous route; shorter for IV (2–4 hours). Duration depends on renal function and dose.

Classification & Brands

Dosing & administration

Intravenous: 1.5 g/kg ideal body weight (IBW) over 12-24 hours; maximal rate: 0.625 g/kg/hour.

Dosage form	INJECTABLE
Renal impairment	GFR 10-50 mL/min: no adjustment; GFR <10 mL/min: not recommended.
Liver impairment	Child-Pugh A-C: no dosage adjustment required.
Pediatric use	Safety and efficacy not established for pediatric patients.
Geriatric use	No specific dose adjustment; monitor renal function due to age-related decline.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for PROCALAMINE (PROCALAMINE).

Breastfeeding	Excretion in breast milk unknown; M/P ratio not established. Use with caution, monitor infant for adverse effects (e.g., bradycardia, hypotension).
Teratogenic Risk	PROCALAMINE is not associated with teratogenicity; no fetal harm reported in animal studies. Insufficient human data; avoid in first trimester unless benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to any component, severe hypertension, severe coronary artery disease, narrow-angle glaucoma, concurrent MAO inhibitor therapy, urinary retention, and severe renal impairment.

Clinical Precautions

Precautions

May cause drowsiness; avoid activities requiring mental alertness. Use with caution in patients with hypertension, cardiovascular disease, hyperthyroidism, diabetes, glaucoma, prostatic hypertrophy, or urinary retention. Avoid concurrent use with MAO inhibitors or within 14 days of discontinuation. Use in children may cause paradoxical excitation.

Clinical Tips & Counseling

Drug interactions

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PROCALAMINE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PROCALAMINE (PROCALAMINE).

How it works

What the body does with it

Metabolism	Chlorpheniramine undergoes hepatic metabolism via CYP450 enzymes (primarily CYP3A4, CYP2D6). Pheniramine is also metabolized in the liver. Phenylephrine undergoes extensive first-pass metabolism by intestinal and hepatic monoamine oxidase (MAO) and sulfotransferase.
Excretion	Primarily renal; >95% of the dose excreted unchanged in urine within 24 hours. Minimal biliary/fecal elimination (<5%).
Half-life	2.5–3.5 hours in healthy adults; prolonged in renal impairment (up to 20–30 hours in ESRD).
Protein binding	<5%; negligible binding to albumin or other plasma proteins.
Volume of Distribution	0.2–0.4 L/kg; indicates distribution largely confined to extracellular fluid.
Bioavailability	Subcutaneous: 55–80%; no oral bioavailability.
Onset of Action	Subcutaneous: 30–60 minutes; intravenous: immediate. Peak effect at 1–3 hours.
Duration of Action	3–6 hours for subcutaneous route; shorter for IV (2–4 hours). Duration depends on renal function and dose.

Classification & Brands

Dosing & administration

Intravenous: 1.5 g/kg ideal body weight (IBW) over 12-24 hours; maximal rate: 0.625 g/kg/hour.

Dosage form	INJECTABLE
Renal impairment	GFR 10-50 mL/min: no adjustment; GFR <10 mL/min: not recommended.
Liver impairment	Child-Pugh A-C: no dosage adjustment required.
Pediatric use	Safety and efficacy not established for pediatric patients.
Geriatric use	No specific dose adjustment; monitor renal function due to age-related decline.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for PROCALAMINE (PROCALAMINE).

Breastfeeding	Excretion in breast milk unknown; M/P ratio not established. Use with caution, monitor infant for adverse effects (e.g., bradycardia, hypotension).
Teratogenic Risk	PROCALAMINE is not associated with teratogenicity; no fetal harm reported in animal studies. Insufficient human data; avoid in first trimester unless benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to any component, severe hypertension, severe coronary artery disease, narrow-angle glaucoma, concurrent MAO inhibitor therapy, urinary retention, and severe renal impairment.