ibuprofen/pseudoephedrine (Advil Cold and Sinus)

Dosing and uses of Advil Cold and Sinus (ibuprofen/pseudoephedrine)

• Adult
• Pediatric

 

Adult dosage forms and strengths

ibuprofen/pseudoephedrine

caplet

• 200mg/30mg

liquid gel capsule

• 200mg/30mg

 

Cold Symptoms

1 caplet/capsule PO q4-6hr PRN; may increase to 2 caplets/capsules q4-6hr if necessary while symptoms persist

Not to exceed 6 doses/24 hr

 

Administration

Take with food or milk if stomach upset occurs

 

Pediatric dosage forms and strengths

ibuprofen/pseudoephedrine

caplet

• 200mg/30mg

liquid gel capsule

• 200mg/30mg

 

Cold Symptoms

<12 years: Safety and efficacy not established

>12 years: 1 caplet/capsule PO q4-6hr PRN; may increase to 2 caplets/capsules q4-6hr if necessary while symptoms persist Not to exceed 6 doses/24 hr

 

Administration

Take with food or milk if stomach upset occurs

 

Advil Cold and Sinus (ibuprofen/pseudoephedrine) adverse (side) effects

Frequency not defined

GI upset

Insomnia

Arrhythmia

Palpitations

Convulsion

Dizziness

Drowsiness

Excitability

Headache

Tremor

Weakness

NauseaVomiting

Hemolytic anemia

Aplastic anemia

Arrhythmia

Bronchospasm

CHF

Efoliative dermatitis

Constipation

Hypertension

Neutropenia

Thromboembolism

Abdominal pain

Anxiety

CNS stimulation

Hepatotoxicity

Dizziness

 

Warnings

Contraindications

Hypersensitivity

Immediately before or after heart surgery

History of induce asthma or urticaria with NSAIDs

Do not use with MAO inhibitors or for 2 weeks after discontinuing MAO inhibitors because of risk for hypertensive crisis

 

Cautions

Caution with hypertension, heart disease, hepatic or renal impairment, asthma, thyroid disease, diabetes, BPH, peptic ulcer disease

NSAID content

• May increase risk for GI ulceration, increased risk if age >60 yr or history of PUD
• Coadministration with antiplatelets/anticoagulants
• May decrease benefit of cardioprotective low-dose aspirin

Pseudoephedrine

• May exacerbate poorly controlled hypertension
• Caution if underlying cardiovascular risks present

 

Pregnancy and lactation

Pregnancy category: C; d

Do not take NSAIDs within 3 months before delivery because of risk for premature closure of the ductus arteriosus

The Quebec Pregnancy Registry identified 4705 women who had spontaneous abortions by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had spontaneous abortions; exposure to nonaspirin NSAIDs during pregnancy was documented in approximately 7.5% of cases of spontaneous abortions and in approximately 2.6% of controls. (CMAJ, September 6, 2011; DOI:10.1503/cmaj.110454)

Lactation: NSAIDs and pseudoephedrine excreted in breast milk, AAP states compatible with breastfeeding

 

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.

 

Pharmacology of Advil Cold and Sinus (ibuprofen/pseudoephedrine)

Mechanism of action

Ibuprofen: Inhibits synthesis of prostaglandins by inhibiting cyclooxygenase (COX-1, COX-2); may inhibit chemotaxis, alter lymphocyte activity, decrease proinflammatory cytoking activity, and inhibit neutrophil aggregation, which in turn may result in anti-inflammatory activity

Pseudoephedrine stimulates the alpha-adrenergic receptors causing bronchodilation and vasoconstriction

 

Pharmacokinetics

Ibuprofen

• Absoroption: Rapid (85%)
• Bioavailability: 80-100%
• Onset: 30-60 min
• Duration: 4-6 hr
• Peak plasma concentration: 20 mcg/mL (tab)
• Protein bound: 90-99%
• Vd: 0.12 L/kg (adults); 0.2 L/kg (children)
• Peak plasma time: 120 min (tab)
• Metabolism: Rapid hepatic oxidation to inactivate metabolites; CYP2C9; CYP2C19 substrate
• Half-life: 2-4hr
• Excretion: Urine (50-60%); feces (50-40%)

Pseudoephedrine

• Half-Life: 3 hr (children); 9-16 hr (adults)
• Onset: 30 min (decongestant)
• Duration: 3-8 hr  
• Peak Plasma Time: 1.97 hr
• Concentration: 422 ng/mL
• Metabolism: Liver, by N-demethylation
• Metabolites: Inactive
• Clearance: 7.3-7.6 mL/min/kg
• Excretion: Urine (43-96%)