Salmeterol

Long-acting selective β2-agonist (LABA, bronchodilator)

ATC code: R03AC12

Brand names: Serevent Diskus, Serevent

Updated 1 Jun 2026 · Methodology

Indications

Asthma

Adjunct

Salmeterol is a LABA for asthma control only in fixed combination with an inhaled corticosteroid (ICS+LABA: Seretide, Aerivio, Plusvent). 2024 and GEMA 5.4 from step 3 onward permit LABA only on top of ICS. Salmeterol monotherapy is not used in asthma: the SMART trial (Nelson 2006, over 26,000 patients) demonstrated increased asthma-related mortality. The added a black-box warning for all LABAs in 2010; AEMPS issued a parallel safety note. If salmeterol was prescribed without an ICS as a stand-alone long-term bronchodilator or as a reliever for attacks, consider seeking a second opinion.

Sources

ICD-10: J45 · ICD-11: CA23

Chronic obstructive pulmonary disease

First line

LABA for COPD maintenance. 2024 and GesEPOC 2024 list salmeterol as an option in group B (moderate symptoms, few exacerbations) and in LABA+LAMA combinations (Anoro, Ultibro) in group E. In COPD, LABA monotherapy without ICS is acceptable – no excess mortality as seen in asthma.

Sources

ICD-10: J44 · ICD-11: CA22

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Athletic endurance

Not recommended

Salmeterol is used off-label by fitness influencers and athletes without asthma for «endurance gains» via skeletal-muscle β2 stimulation. The hypothesized anabolic effect is not confirmed: systematic reviews find no quality evidence. The drug appears on the WADA 2024 Prohibited List; exemption is possible only with documented asthma under a TUE and within strict dose limits. Real biohacking risks: tachycardia, tremor, hypokalaemia, QT prolongation. If salmeterol is suggested without an asthma diagnosis as a way to «boost cardio», consider seeking a second opinion.

Sources

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

Selective β2-adrenoceptor agonist of bronchial smooth muscle. Long lipophilic side chain anchors the molecule to the receptor and produces a 12-hour action. Activates adenylyl cyclase, raises cAMP, relaxes smooth muscle and suppresses mediator release from mast cells. Onset is slow: 10–20 minutes after inhalation, so it does not relieve an acute attack. Controller, not a reliever.

Safety

Boxed warning

Long-acting beta2-agonists (LABA), including salmeterol, increase the risk of asthma-related death when used as monotherapy without an inhaled corticosteroid. In asthma salmeterol is used only in fixed combination with an ICS. FDA Black Box 2010, AEMPS issued a parallel warning.

Contraindications

Hypersensitivity to salmeterol or excipients
Monotherapy for asthma without inhaled corticosteroid
Relief of acute asthma attack or COPD exacerbation

Serious adverse effects

Paradoxical bronchospasm immediately after inhalation
Severe hypokalaemia at high doses or combined with diuretics
QT prolongation and arrhythmias
Hyperglycaemia
Anaphylactic reactions

Common adverse effects

Hand tremor
Headache
Palpitations and tachycardia
Throat irritation
Muscle cramps

Pregnancy: can you take Salmeterol?

AEMPS summary of product characteristics (section 4.6): data on salmeterol in pregnant women are limited (fewer than 300 pregnancy outcomes), there are no adequate well-controlled studies, and the effect of salmeterol on human pregnancy is unknown. Animal studies showed no direct or indirect harmful effects on reproduction, apart from some effects on the fetus at very high doses. As a precaution, it is preferable to avoid salmeterol during pregnancy.

Breastfeeding: can you take Salmeterol?

Compatible. Hale L2. Inhaled systemic bioavailability is low; only minimal amounts reach milk. GEMA 5.4 allows continued ICS+LABA during lactation.

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Label mentions25 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

MajorAtazanavir
«Inhibitors of Cytochrome P450 3A4: Salmeterol is a substrate of CYP3A4. The use of strong CYP3A4 inhibitors (e.g., ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone…»
FDA, section 7 · Open on DailyMed
MajorClarithromycin
«Inhibitors of Cytochrome P450 3A4: Salmeterol is a substrate of CYP3A4. The use of strong CYP3A4 inhibitors (e.g., ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone…»
FDA, section 7 · Open on DailyMed
MajorItraconazole
«Inhibidores potentes del CYP3A4: Se debe evitar la administración concomitante de ketoconazol, a menos que los beneficios superen el riesgo potencialmente aumentado de padecer efectos sistémicos del…»
AEMPS, section 4.5 · Open on CIMA
MajorItraconazole
«Inhibitors of Cytochrome P450 3A4: Salmeterol is a substrate of CYP3A4. The use of strong CYP3A4 inhibitors (e.g., ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone…»
FDA, section 7 · Open on DailyMed
MajorKetoconazole
«Inhibidores potentes del CYP3A4: Se debe evitar la administración concomitante de ketoconazol, a menos que los beneficios superen el riesgo potencialmente aumentado de padecer efectos sistémicos del…»
AEMPS, section 4.5 · Open on CIMA
MajorKetoconazole
«DRUG INTERACTIONS: • Strong cytochrome P450 3A4 inhibitors (e.g., ritonavir, ketoconazole): Use not recommended. May increase risk of cardiovascular effects. ( 7.1 )»
FDA, section 7 · Open on DailyMed
MajorRitonavir
«Inhibidores potentes del CYP3A4: Se debe evitar la administración concomitante de ketoconazol, a menos que los beneficios superen el riesgo potencialmente aumentado de padecer efectos sistémicos del…»
AEMPS, section 4.5 · Open on CIMA
MajorRitonavir
«DRUG INTERACTIONS: • Strong cytochrome P450 3A4 inhibitors (e.g., ritonavir, ketoconazole): Use not recommended. May increase risk of cardiovascular effects. ( 7.1 )»
FDA, section 7 · Open on DailyMed
Moderatebeta blockersclass named in the label
«DRUG INTERACTIONS: • Beta-blockers: Use with caution. May block bronchodilatory effects of beta-agonists and produce severe bronchospasm. ( 7.3 )»
FDA, section 7 · Open on DailyMed
ModerateCYP3A4 inhibitorsclass named in the label
«Inhibitors of Cytochrome P450 3A4: Salmeterol is a substrate of CYP3A4. The use of strong CYP3A4 inhibitors (e.g., ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone…»
FDA, section 7 · Open on DailyMed
Moderatediuréticosclass named in the label
«Como consecuencia del tratamiento con agonistas β 2 se puede producir una hipocalemia potencialmente grave. Se recomienda tener especial precaución en el asma aguda grave , ya que este efecto puede…»
AEMPS, section 4.4 · Open on CIMA
Moderatediureticsclass named in the label
«DRUG INTERACTIONS: • Diuretics: Use with caution. Electrocardiographic changes and/or hypokalemia associated with non–potassium-sparing diuretics may worsen with concomitant beta-agonists. ( 7.4 )»
FDA, section 7 · Open on DailyMed
Moderateinhibidores del CYP3A4class named in the label
«Inhibidores potentes del CYP3A4: Se debe evitar la administración concomitante de ketoconazol, a menos que los beneficios superen el riesgo potencialmente aumentado de padecer efectos sistémicos del…»
AEMPS, section 4.5 · Open on CIMA
ModerateMAO inhibitorsclass named in the label
«DRUG INTERACTIONS: • Monoamine oxidase inhibitors and tricyclic antidepressants: Use with extreme caution. May potentiate effect of salmeterol on vascular system. ( 7.2 )»
FDA, section 7 · Open on DailyMed
Moderatethiazide diureticsclass named in the label
«Non–Potassium-Sparing Diuretics: The ECG changes and/or hypokalemia that may result from the administration of non–potassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely…»
FDA, section 7 · Open on DailyMed
Moderatetricyclic antidepressantsclass named in the label
«DRUG INTERACTIONS: • Monoamine oxidase inhibitors and tricyclic antidepressants: Use with extreme caution. May potentiate effect of salmeterol on vascular system. ( 7.2 )»
FDA, section 7 · Open on DailyMed
Erythromycin
«Inhibidores moderados del CYP3A4: La administración conjunta de eritromicina (500 mg tres veces al día por vía oral) y salmeterol (50 microgramos dos veces al día por vía inhalatoria) en 15 sujetos…»
AEMPS, section 4.5 · Open on CIMA
QT-prolonging drugsclass named in the label
«Inhibitors of Cytochrome P450 3A4: In a drug interaction trial in 20 healthy subjects, coadministration of inhaled salmeterol (50 mcg twice daily) and oral ketoconazole (400 mg once daily) for 7 days…»
FDA, section 7 · Open on DailyMed

From other drugs’ labels

MajorAtazanavir
«Established and Other Potentially Significant Drug Interactions: Inhaled beta agonist: salmeterol ↑ salmeterol Coadministration of salmeterol with atazanavir is not recommended. Concomitant use of…»
FDA, section 7 · Open on DailyMed
MajorCobicistat
«Established and Other Potentially Significant Interactions: Inhaled Beta Agonist: salmeterol ↑ salmeterol Coadministration with salmeterol is not recommended and may result in increased risk of…»
FDA, section 7 · Open on DailyMed
MajorDarunavir
«BETA AGONISTAS INHALADOS: No se recomienda el uso concomitante de salmeterol y darunavir potenciado. La combinación puede dar lugar a un mayor riesgo de efectos adversos cardiovasculares con…»
AEMPS, section 4.5 · Open on CIMA
MajorDarunavir
«Established and Other Potentially Significant Drug Interactions: Inhaled beta agonist : salmeterol  salmeterol Co-administration of salmeterol and darunavir/ritonavir is not recommended. The…»
FDA, section 7 · Open on DailyMed
MajorRitonavir
«ß2-agonistas (de acción prolongada): Ritonavir inhibe el CYP3A4 y por lo tanto se espera un aumento en las concentraciones plasmáticas de salmeterol. Por lo tanto, no se recomienda su uso…»
AEMPS, section 4.5 · Open on CIMA
MajorRitonavir
«Established and Other Potentially Significant Drug Interactions: Long-acting beta- adrenoceptor agonist: salmeterol ↑ salmeterol Concurrent administration of salmeterol and ritonavir is not…»
FDA, section 7 · Open on DailyMed
Itraconazole
«Antivirales para uso sistémico: Aunque no se ha estudiado directamente, es probable que itraconazol aumente las concentraciones de salmeterol y del metabolito activo de la ciclesonida.»
AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Salmeterol used for?

Salmeterol is evaluated for the following indications with varying evidence strength: Asthma (evidence tier A), Chronic obstructive pulmonary disease (evidence tier A), Athletic endurance (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Salmeterol?

Common side effects of Salmeterol (≥ 1 in 100): Hand tremor, Headache, Palpitations and tachycardia, Throat irritation, Muscle cramps. See the Safety section for uncommon and serious reactions.

Is Salmeterol safe during pregnancy?

Is Salmeterol compatible with breastfeeding?

Compatible. Hale L2. Inhaled systemic bioavailability is low; only minimal amounts reach milk. GEMA 5.4 allows continued ICS+LABA during lactation.

Who should not take Salmeterol?

Salmeterol is contraindicated in: Hypersensitivity to salmeterol or excipients; Monotherapy for asthma without inhaled corticosteroid; Relief of acute asthma attack or COPD exacerbation. Full list in the Safety section.

Does Salmeterol carry an FDA boxed warning?

Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMALabel dated 04/26/2022
FDA / DailyMedLabel dated 04/01/2026

Other drugs in this group

Salmeterol + Fluticasone, Theophylline, Tiotropium, Aclidinium, Budesonide, Fluticasone propionate, Mometasone, Beclomethasone dipropionate