brompheniramine/pseudoephedrine (Rx)

Frequency Not Defined

Brompheniramine (Common)

• Anticholinergic effects (blurred vision, dry mouth/nose, throat,
• Drowsiness, dizziness, decreased coordination, headache
• Constipation, stomach upset

Pseudoephedrine (Common)

• CNS (tremor, restlessness, etc)
• Insomnia
• Nausea
• Vomiting

Contraindications

• Hypersensitivity to drugs or excipients
• Within 14 days of MAO inhibitor therapy

Cautions

• Use with caution in mild-mod HTN, asthma, thyroid dysfunction, hyperglycemia, BPH, DM, glaucoma, cardiovascular disease, including hypertension and ischemic heart disease
• Many combo formulations are switching to phenylephrine due to restrictions arising from easy conversion to methamphetamine (The Combat Methamphetamine Epidemic Act of 2005 bans OTC sales of cold medicines that contain ingredients commonly used to make methamphetamine such as pseudoephedrine)

• May cause CNS depression, which may impair physical or mental abilities; caution patients about performing tasks requiring mental alertness, including operating heavy machinery

  Medication may potentiate the effects of sedative drugs or ethanol

Pregnancy category: C; not recommended in first tri-mester or last 2 weeks of pregnancy

Lactation: Contraindicated

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Brompheniramine: Histamine H1-receptor antagonist

Pseudoephedrine: Sympathomimetic; exerts decongestant action on nasal mucosa; stimulates the alpha-adrenergic receptors causing bronchodilation and vasoconstriction

Brompheniramne

Half-Life: 11.8-34.7 hr

Onset: 30 min

Protein binding: 39-49%

Duration: 3-9 hr, may last 48 hr

Peak Plasma Time: 2-4 hr (adults): 3-3.5 hr (children)

Vd: 11.7 L/kg (adults); 20 L/kg (children)

Metabolism: Mainly liver

Metabolites: Propionic acid derivative conjugated with glycine

Excretion: Urine

Antihistamine activity: Jigh

Sedative effect: Low

Anticholinergic effects: Moderate

Pseudoephedrine

Half-Life: 3 hr (children); 3-16hr (adults)

Onset: 30 min

Absorption: Rapid

Duration: 3-8 hr

Peak Plasma Time: 1-3 hr (adults); 2hr (children)

Peak Plasma Concentration: 422 ng/mL

Clearance: 7.3-7.6 mL/min/kg

Excretion: Urine

Vd: 2.5 L/kg (children); 2.64-3.51 L/kg (adults)