The inhaled route for drug administration in neonates offers several advantages over the systemic routes, since it delivers medications directly to the diseased organ, enabling higher doses locally with less systemic toxicity. Respiratory drugs can be administered in both ventilated and non-ventilated term and preterm infants. This review was carried out using selected literature, with a focus on the most used inhaled pharmacological agents in neonatal care, summarizing, with levels of evidence (LoE), their indications, doses, administration schedules, and main adverse effects. Information is given on several inhaled drugs, namely albuterol, budesonide, ipratropium bromide, sodium cromoglycate, racemic epinephrine, nitric oxide, treprostinil, iloprost, epoprostenol, colistin, rhDNase, hypertonic saline, and calfactant. A summary of the main and most recent published studies on each of these inhaled pharmacological agents is also presented.