is categorized as an Alpha-/Beta- Agonist.

1. US Boxed Warning

• Supine Hypertension: Monitor supine blood pressure before and during treatment, especially when increasing doses. Elevating the head of the bed can reduce the risk of supine hypertension. If supine hypertension cannot be managed, reduce or discontinue Droxidopa.

2. Indications and Dosage

2.1 Hypotension Neurogenic Orthostatic (Adult)

• Initial: 100 mg 3 times daily (morning, midday, late afternoon, at least 3 hours before bedtime)
• Titrate in increments of 100 mg 3 times daily every 24 to 48 hours to symptomatic response
• Maximum dose: 600 mg 3 times daily

2.2 Kidney Impairment

• GFR >30 mL/minute: No dose adjustments necessary.
• GFR ≤30 mL/minute: No dosage adjustments provided in the manufacturer’s labeling (has not been studied).

2.3 Hepatic Impairment

• No dosage adjustments provided in the manufacturer’s labeling.

3. Adverse Reactions

3.1 >10%

• Headache (6% to 13%)

3.2 1% to 10%

• Hypertension (2% to 7%; including supine hypertension)
• Nausea (9%)
• Dizziness (4% to 10%)

3.3 Postmarketing

• Cardiovascular: Chest pain
• Gastrointestinal: Abdominal pain, diarrhea, pancreatitis, vomiting
• Hypersensitivity: Reactions including anaphylaxis and angioedema
• Nervous system: Behavioral changes, cerebrovascular accident, cognitive dysfunction, fatigue, neurological signs and symptoms
• Ophthalmic: Blurred vision

4. Contraindications

• Hypersensitivity to droxidopa or any component of the formulation.

5. Warnings/Precautions

• Anaphylaxis/Allergic Reactions: Emergency treatment may be necessary. Discontinue use if a reaction occurs.
• Hypertension: Monitor blood pressure in supine and head-elevated positions. Reduce or discontinue if supine hypertension persists.
• Neuroleptic Malignant Syndrome: Symptoms have included hyperpyrexia and confusion.

6. Monitoring Parameters

• Monitor supine blood pressure before and during treatment, especially when increasing the dose.

7. Mechanism of Action

• Droxidopa is metabolized to norepinephrine, which increases blood pressure by inducing peripheral arterial and venous vasoconstriction.

8. Pharmacokinetics

• Absorption: High-fat meals reduce Cmax and AUC by 35% and 20% respectively; delay Cmax by ~2 hours.
• Distribution: Vd ~200 L
• Protein Binding: 26% to 75%
• Metabolism: Converted to norepinephrine by DOPA decarboxylase.
• Half-life Elimination: ~2.5 hours
• Excretion: Urine (~75%)

9. Administration (Adult)

• Administer capsule whole, consistently with or without food, in the morning, midday, and late afternoon (at least 3 hours before bedtime).

10. Use: Labeled Indications

• Treatment of orthostatic dizziness, light-headedness, or “feeling that you are about to black out” in adults with symptomatic neurogenic orthostatic hypotension (NOH) caused by conditions like Parkinson’s disease, multiple system atrophy, pure autonomic failure, dopamine beta-hydroxylase deficiency, and nondiabetic autonomic neuropathy.

11. Brand Names: International

• China: Shan wei
• Japan: Dops, Droxidopa Amel
• Norway: Northera
• Puerto Rico: Northera