Zoryve
Zoryve
Generic Name
Zoryve
Mechanism
- Lung‑specific β3‑adrenergic receptor stimulation → ↑ intracellular cyclic‑AMP → smooth‑muscle relaxation → bronchodilation.
- Provides an alternative bronchodilator pathway distinct from β2‑agonists, with potential benefit in patients poorly responsive to β2‑agonists.
Pharmacokinetics
- Absorption: Rapid uptake from the respiratory tract; peak plasma concentration (Cmax) reached in 30–60 min.
- Distribution: 60–80 % protein bound; low systemic exposure compared with oral mirabegron.
- Metabolism: Primarily via CYP2D6 and CYP3A4; minor contribution from CYP1A2.
- Elimination: Hepatic conjugation → renal excretion (~70 % as inactive metabolites).
- Half‑life (t½): 13–15 h (suitable for once‑daily dosing).
Indications
- COPD (moderate–severe) in patients who require bronchodilator therapy and have inadequate control with standard β2‑agonists or anticholinergics.
Contraindications
- Contraindications:
- Hypersensitivity to mirabegron or any component of the inhaler.
- Uncontrolled hypertension or severe cardiovascular disease (e.g., recent myocardial infarction).
- Severe renal impairment (CrCl < 15 mL/min) – dosing contraindicated.
- Warnings/Cautions:
- Cardiovascular: Monitor for hypertension, tachycardia, and arrhythmias.
- Renal/hepatic impairment: Reduced clearance; not recommended for CrCl 2× ULN.
- Elderly: Higher risk of systemic side‑effects; dose adjustment may be required.
Dosing
- Adult dose: 50 mg inhaled once daily (morning) using the breath‑actuated inhaler.
- Administration technique:
- Inspect device for correct operation.
- Remove cap → exhale fully → inhale slowly and deeply to capture the dose → hold breath 10 s → repeat if a second dose is prescribed (not indicated for Zoryve).
- Missed dose: take as soon as remembered; do not double‑dose.
Adverse Effects
| Frequency | Adverse Effect | Notes |
| Common | Dry mouth, headache, nausea | Usually mild; dose‑related |
| Common | Increased systolic blood pressure | Monitor if baseline BP >140/90 mmHg |
| Common | Dizziness | Avoid driving until effect known |
| Serious | Severe hypertension, supraventricular tachycardia | Rare; immediate evaluation required |
| Rare | Pulmonary edema, exacerbation of respiratory infection | Consider stopping if symptoms persist |
Monitoring
- Baseline:
- Blood pressure (BP) and heart rate (HR) prior to first dose.
- Renal function (serum creatinine, CrCl).
- Hepatic panel (AST, ALT).
- Follow‑up:
- BP & HR every 2–4 weeks for first 3 months, then every 3 months.
- Annual renal and hepatic assessment.
- Pulmonary: Spirometry to evaluate FEV1 changes if clinically indicated.
Clinical Pearls
- Breath‑actuated advantage: Improves dose consistency in COPD patients with variable inhalation effort.
- Adjunctive therapy: Can be paired with standard β2‑agonists/anticholinergics; may reduce reliance on oral β3‑agonists, thus minimizing systemic side‑effects.
- Renal dosing: Avoid dosing in patients with CrCl 20 mmHg above baseline or HR >110 bpm, discontinue drug and notify prescriber.
Key Takeaway: Zoryve offers a lung‑targeted β3‑agonist option for COPD, characterized by rapid bronchodilation, modest systemic exposure, and a well‑defined safety profile when used in appropriately selected patients.
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• *For any clinical decision, refer to the official prescribing information and local guidelines.*