AEROLATE SR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).

How it works

AEROLATE SR is a sustained-release formulation of theophylline, a methylxanthine bronchodilator. It acts by inhibiting phosphodiesterase (PDE) isoenzymes, leading to increased intracellular cyclic AMP (cAMP) levels. This results in relaxation of bronchial smooth muscle and suppression of the response of airways to stimuli. Theophylline also has anti-inflammatory effects, including inhibition of late-phase allergen-induced responses and reduction of eosinophil infiltration.

What the body does with it

Metabolism	Primarily hepatic via cytochrome P450 enzymes (CYP1A2, CYP2E1, and CYP3A4). Theophylline is metabolized to 1,3-dimethyluric acid, 1-methyluric acid, and 3-methylxanthine.
Excretion	Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites; 10% as unchanged in feces.
Half-life	Terminal elimination half-life 12 hours (range 10–15 h) in adults; prolonged in hepatic impairment (up to 24 h) and elderly.
Protein binding	55–65% bound to plasma proteins, primarily albumin.
Volume of Distribution	0.4–0.6 L/kg, indicating distribution into total body water.
Bioavailability	Oral: 90–100% for sustained-release formulation; food decreases rate but not extent (AUC unchanged).
Onset of Action	Oral: 30–60 minutes for bronchodilation (peak at 2–4 h).
Duration of Action	Sustained-release formulation: 12–24 hours; clinical bronchodilation maintained for 12 h in most patients.

Classification & Brands

Dosing & administration

400-800 mcg inhaled twice daily. For acute bronchospasm, 200-400 mcg as needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	Use with caution in severe hepatic impairment (Child-Pugh class C); consider dose reduction by 50%.
Pediatric use	Children 6-12 years: 200-400 mcg inhaled twice daily. Children over 12 years: same as adult dose.
Geriatric use	Start at lower end of dosing range (400 mcg twice daily) and titrate to response; monitor for systemic effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).

Breastfeeding	Salbutamol is excreted into breast milk in minimal amounts; estimated infant dose <2% of maternal weight-adjusted dose. No known adverse effects in nursing infants. M/P ratio not established. Use with caution.
Teratogenic Risk	Pregnancy Category C. In first trimester: insufficient human data; animal studies show adverse effects at high doses. Second and third trimesters: may cause fetal tachycardia, hypoglycemia, and reduced uterine contractility; avoid use near term due to potential for neonatal bradycardia and hypoglycemia.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning exists for this drug.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to theophylline or any component of the formulation; active seizure disorder; untreated cardiac arrhythmias; severe hypertension; hyperthyroidism; peptic ulcer disease; caution with concurrent use of ephedrine or other sympathomimetics.

Clinical Precautions

Precautions	Theophylline has a narrow therapeutic index; serum levels must be monitored to avoid toxicity. Toxicity can include seizures, cardiac arrhythmias, and death. Caution in patients with heart failure, hepatic impairment, or those over 55 years. Risk of toxicity increased by concurrent medications such as cimetidine, fluoroquinolones, and macrolides.
Food/Dietary	High-fat meals may delay absorption. Avoid charcoal-grilled foods and large amounts of caffeine. Grapefruit juice may increase theophylline levels; limit intake.

Clinical Tips & Counseling

Drug interactions

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AEROLATE SR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).

How it works

What the body does with it

Metabolism	Primarily hepatic via cytochrome P450 enzymes (CYP1A2, CYP2E1, and CYP3A4). Theophylline is metabolized to 1,3-dimethyluric acid, 1-methyluric acid, and 3-methylxanthine.
Excretion	Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites; 10% as unchanged in feces.
Half-life	Terminal elimination half-life 12 hours (range 10–15 h) in adults; prolonged in hepatic impairment (up to 24 h) and elderly.
Protein binding	55–65% bound to plasma proteins, primarily albumin.
Volume of Distribution	0.4–0.6 L/kg, indicating distribution into total body water.
Bioavailability	Oral: 90–100% for sustained-release formulation; food decreases rate but not extent (AUC unchanged).
Onset of Action	Oral: 30–60 minutes for bronchodilation (peak at 2–4 h).
Duration of Action	Sustained-release formulation: 12–24 hours; clinical bronchodilation maintained for 12 h in most patients.

Classification & Brands

Dosing & administration

400-800 mcg inhaled twice daily. For acute bronchospasm, 200-400 mcg as needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	Use with caution in severe hepatic impairment (Child-Pugh class C); consider dose reduction by 50%.
Pediatric use	Children 6-12 years: 200-400 mcg inhaled twice daily. Children over 12 years: same as adult dose.
Geriatric use	Start at lower end of dosing range (400 mcg twice daily) and titrate to response; monitor for systemic effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).

Breastfeeding	Salbutamol is excreted into breast milk in minimal amounts; estimated infant dose <2% of maternal weight-adjusted dose. No known adverse effects in nursing infants. M/P ratio not established. Use with caution.
Teratogenic Risk	Pregnancy Category C. In first trimester: insufficient human data; animal studies show adverse effects at high doses. Second and third trimesters: may cause fetal tachycardia, hypoglycemia, and reduced uterine contractility; avoid use near term due to potential for neonatal bradycardia and hypoglycemia.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning exists for this drug.

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions	Theophylline has a narrow therapeutic index; serum levels must be monitored to avoid toxicity. Toxicity can include seizures, cardiac arrhythmias, and death. Caution in patients with heart failure, hepatic impairment, or those over 55 years. Risk of toxicity increased by concurrent medications such as cimetidine, fluoroquinolones, and macrolides.
Food/Dietary	High-fat meals may delay absorption. Avoid charcoal-grilled foods and large amounts of caffeine. Grapefruit juice may increase theophylline levels; limit intake.

Clinical Tips & Counseling

Drug interactions

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Clinical Pearls	AEROLATE SR contains theophylline; narrow therapeutic index (10-20 mcg/mL). Monitor serum levels, especially with CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine) or inducers (e.g., carbamazepine, phenytoin). SR formulation avoids peak-trough fluctuations; do not crush or chew. Caution in heart failure, hepatic impairment, and elderly.
Patient Advice	Take exactly as prescribed; do not crush or chew the sustained-release tablet. · Do not stop suddenly; sudden withdrawal may worsen breathing. · Avoid excessive caffeine (coffee, tea, chocolate) as it may increase side effects. · Report nausea, vomiting, insomnia, palpitations, or seizures immediately. · Keep regular appointments for blood level monitoring.