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Droxidopa: Drug information

Droxidopa: Drug information
(For additional information see "Droxidopa: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
ALERT: US Boxed Warning
Supine hypertension:

Monitor supine blood pressure prior to and during treatment and more frequently when increasing doses. Elevating the head of the bed lessens the risk of supine hypertension, and blood pressure should be measured in this position. If supine hypertension cannot be managed by elevation of the head of the bed, reduce or discontinue droxidopa.

Brand Names: US
  • Northera
Pharmacologic Category
  • Alpha-/Beta- Agonist
Dosing: Adult

Hypotension, neurogenic orthostatic: Oral: Initial: 100 mg 3 times daily (in the morning, at midday, and in the 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 up to a maximum dose of 600 mg 3 times daily.

Dosing: Kidney Impairment: Adult

GFR >30 mL/minute: No dose adjustments necessary.

GFR ≤30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Northera: 100 mg, 200 mg [contains fd&c blue #2 (indigotine)]

Northera: 300 mg [contains brilliant blue fcf (fd&c blue #1), corn starch, fd&c red #40, tartrazine (fd&c yellow #5)]

Generic: 100 mg, 200 mg, 300 mg

Generic Equivalent Available: US

Yes

Administration: Adult

Administer capsule whole, consistently with or without food, upon arising in the morning, at midday, and in the late afternoon at least 3 hours prior to bedtime (to reduce the potential for supine hypertension during sleep).

Use: Labeled Indications

Hypotension, neurogenic orthostatic: Treatment of orthostatic dizziness, light-headedness, or the “feeling that you are about to black out” in adults with symptomatic neurogenic orthostatic hypotension (NOH) caused by primary autonomic failure (Parkinson disease [PD], multiple system atrophy [MSA], and pure autonomic failure [PAF]), dopamine beta-hydroxylase deficiency, and nondiabetic autonomic neuropathy.

Medication Safety Issues
Sound-alike/look-alike issues:

Droxidopa may be confused with levodopa, carbidopa, Droxia.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Central nervous system: Headache (6% to 13%)

1% to 10%:

Cardiovascular: Hypertension (2% to 7%)

Central nervous system: Dizziness (4% to 10%)

Gastrointestinal: Nausea (9%)

Postmarketing and/or case reports: Abdominal pain, agitation, blurred vision, cerebrovascular accident, chest pain, confusion, delirium, diarrhea, fatigue, hallucination, hyperpyrexia, hypersensitivity reaction (including anaphylaxis, angioedema, bronchospasm, skin rash, urticaria), memory impairment, pancreatitis, psychosis, vomiting

Contraindications

Hypersensitivity to droxidopa or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylaxis/allergic reactions: Hypersensitivity reactions have been reported. Reactions may include anaphylaxis, angioedema, bronchospasm, rash, and urticaria; emergency treatment may be necessary. Discontinue use and initiate immediate medical support if a hypersensitivity reaction occurs.

• Hypertension: [US Boxed Warning]: Droxidopa may cause or exacerbate supine hypertension. Advise patients to elevate the head of bed when resting or sleeping. Monitor blood pressure in supine position and in recommended head-elevated sleeping position. Reduce or discontinue droxidopa if supine hypertension persists. Risk of cardiovascular events may be increased if supine hypertension is not well managed.

• Neuroleptic malignant syndrome: A symptom complex resembling neuroleptic malignant syndrome has been reported; symptoms have included hyperpyrexia and confusion. Observe patients carefully with dose changes or when concomitant levodopa is reduced abruptly or discontinued, especially if patient is receiving neuroleptics.

Disease-related concerns:

• Cardiovascular disease: Droxidopa may exacerbate existing ischemic heart disease, arrhythmias, and congestive heart failure; consider potential risk prior to initiating therapy.

Dosage form specific issues:

• Tartrazine: May contain FD+C Yellow No. 5 (tartrazine), which may cause allergic reactions, including bronchial asthma in susceptible individuals, especially in patients with aspirin hypersensitivity.

Metabolism/Transport Effects

None known.

Drug Interactions

Amezinium: May enhance the adverse/toxic effect of Droxidopa. Risk C: Monitor therapy

Carbidopa: May diminish the therapeutic effect of Droxidopa. Carbidopa may decrease serum concentrations of the active metabolite(s) of Droxidopa. Carbidopa may increase the serum concentration of Droxidopa. Risk C: Monitor therapy

Ephedra: May enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy

EPHEDrine (Systemic): May enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy

Ifenprodil: May diminish the therapeutic effect of Droxidopa. Risk C: Monitor therapy

Midodrine: May enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Droxidopa. Risk X: Avoid combination

Norepinephrine: May enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy

Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy

Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies.

Breastfeeding Considerations

It is not known if droxidopa is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended by the manufacturer.

Monitoring Parameters

Monitor supine blood pressure prior to and during treatment and more frequently when increasing the dose.

Mechanism of Action

A synthetic amino acid analog that is directly metabolized to norepinephrine by dopadecarboxylase. Droxidopa is believed to exert its pharmacological effects through norepinephrine. Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction.

Pharmacokinetics

Absorption: High-fat meals reduce the Cmax and area under the plasma concentration-time curve (AUC) by 35% and 20%, respectively, and delay the Cmax by approximately 2 hours.

Distribution: Vd: ~200 L

Protein binding: 26% to 75%

Metabolism: The metabolism of droxidopa is mediated by catecholamine pathway. Droxidopa is initially converted to methoxylated dihydroxyphenylserine (3-OM-DOPS), a major metabolite, by catechol-O-methyltransferase (COMT), to norepinephrine by DOPA decarboxylase (DDC), or to protocatechualdehyde by DOPS aldolase.

Half-life elimination: ~2.5 hours

Time to peak, plasma: 1 to 4 hours

Excretion: Urine (~75%)

Pricing: US

Capsules (Droxidopa Oral)

100 mg (per each): $23.33 - $38.83

200 mg (per each): $46.65 - $77.65

300 mg (per each): $69.98 - $116.48

Capsules (Northera Oral)

100 mg (per each): $42.91

200 mg (per each): $85.82

300 mg (per each): $128.74

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Dops (JP)


For country abbreviations used in Lexicomp (show table)

REFERENCES

  1. Northera (droxidopa) [prescribing information]. Deerfield, IL: Lundbeck; December 2021.
Topic 93840 Version 104.0