Approved by at least one major regulator for a defined indication, with published human pharmacokinetics and a prescribing label. Well-characterised does not mean risk-free, read the label warnings.
Mean terminal half-life ~2.7 h (range 1.9-4.0 h) after a single subcutaneous dose. Clearance 6.5 L/hr; volume of distribution 25 L; 21% serum protein bound.
Model a dosing schedule →Label dose is a single 1.75 mg subcutaneous injection as needed, at least 45 minutes before anticipated activity.
Reconstituted: Commercial autoinjector: store at room temperature per label.
Contraindicated in uncontrolled hypertension or known cardiovascular disease, causes transient blood pressure increases and heart rate decreases after each dose. Common: nausea (often severe enough to stop treatment), flushing, injection-site reactions, headache, vomiting. May cause focal hyperpigmentation, more likely with daily dosing, which is why the label caps frequency. Can slow gastric emptying and reduce absorption of oral medications.