Droxidopa 300 mg Capsule, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Adrenergic and dopaminergic agents class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Droxidopa is used to treat symptoms (dizziness, lightheadedness, or a fainting sensation [feeling that you are about to black out]) of neurogenic orthostatic hypotension (a sudden fall in blood pressure that occurs when a person assumes a standing position caused by certain nervous system conditions). Droxidopa is in a class of medications called alpha and beta-adrenergic agonists. It works by increasing the levels of norepinephrine, a natural substance in the body.
Read the full MedlinePlus article ↗- Droxidopa is designed to help with the dizziness, lightheadedness, and that scary 'about to pass out' feeling you get when you stand up too quickly. In your condition, your nervous...
- What exactly is this medication supposed to do for me?
- You'll take it three times a day — morning, midday, and late afternoon. The important rule is that your last dose must be at least 3 hours before you go to bed. As for food, it doe...
- How do I take it, and does it matter if I take it with food?
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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A synthetic yellow dye used to color medicines. It helps make tablets, capsules, and liquids visually distinct so patients can easily identify their medication.
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FD&C Blue No. 1 is a synthetic blue dye approved for use in foods and medicines. It serves as a colorant to give the medication its distinctive appearance and help with product identification.
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Gelatin is a protein derived from animal collagen, commonly used in medicines as a gelling agent and capsule material. It helps create soft or hard capsule shells that hold and release medication, and can also thicken liquid formulations.
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Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
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A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
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Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
7 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $4.06 | $121.75 / 30 capsules |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Droxidopa 300 mg 00904-7394-89 | MAJOR | 90 capsules | $2.146 | AB | Availability likely | — |
| Droxidopa 300 mg 31722-0010-90 | Camber | 90 capsules | $2.146 | AB | Availability likely | — |
| Droxidopa 300 mg 70710-1391-09 | Zydus | 90 capsules | $2.146 | AB | Availability likely | — |
| Droxidopa 300 mg 82249-0554-90 | CivicaScript | 90 capsules | $2.146 | AB | Availability likely | — |
| droxidopa 300 ug 63304-0112-90 | Sun | 90 capsules | $2.604 | AB | FDA listed | — |
| Droxidopa 300 mg 59651-0377-90 | Aurobindo | 90 capsules | $2.723 | AB | FDA listed | — |
| droxidopa 300 mg 70436-0142-06 | Slate | 90 capsules | $2.723 | AB | FDA listed | — |
| Droxidopa 300 mgthis 50228-0431-30 | ScieGen | 30 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 51407-0767-90 | Golden | 90 capsules | — | AB | FDA listed | — |
| Northera 300 mg 67386-0822-19 | Lundbeck | 90 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 67877-0706-05 | Ascend | 500 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 69452-0258-19 | Bionpharma | 90 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 70771-1611-09 | Zydus | 90 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 72205-0074-05 | Novadoz | 500 capsules | — | AB | FDA listed | — |
| Droxidopa 300 mg 68180-0989-02 | Lupin | 500 capsules | — | — | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
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📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 50228-0431-05 | 500 CAPSULE in 1 BOTTLE (50228-431-05) | — | — | 2021-02-18 | Active |
| 50228-0431-30 You're viewing this | 30 CAPSULE in 1 BOTTLE (50228-431-30) | — | — | 2021-02-18 | Active |
| 50228-0431-90 | 90 CAPSULE in 1 BOTTLE (50228-431-90) | $2.15 / ea | $193.10 | 2021-02-18 | Active |
You're viewing the smallest of 3 pack sizes for this product.
Pack size FAQ
What quantity is in NDC 50228-0431-30?
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What NDC number is used to bill for this package of Droxidopa 300 mg Capsule?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
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| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
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 [ see Warnings and Precautions ( 5.1 ) ].
WARNING: SUPINE HYPERTENSION See full prescribing information for complete boxed warning. 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 capsules [ see Warnings and Precautions ( 5.1 ) ].
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Droxidopa capsules are indicated for the treatment of orthostatic dizziness, lightheadedness, or the “feeling that you are about to black out” in adult patients with symptomatic neurogenic orthostatic hypotension (nOH) caused by primary autonomic failure (Parkinson's disease [PD], multiple system atrophy, and pure autonomic failure), dopamine beta-hydroxylase deficiency, and non-diabetic autonomic neuropathy. Effectiveness beyond 2 weeks of treatment has not been established. The continued effectiveness of Droxidopa should be assessed periodically.
Droxidopa Capsules are indicated for the treatment of orthostatic dizziness, lightheadedness, or the “feeling that you are about to black out” in adult patients with symptomatic neurogenic orthostatic hypotension (nOH) caused by primary autonomic failure (Parkinson's disease [PD], multiple system atrophy, and pure autonomic failure), dopamine beta-hydroxylase deficiency, and non-diabetic autonomic neuropathy. Effectiveness beyond 2 weeks of treatment has not been established. The continued effectiveness of Droxidopa capsules should be assessed periodically ( 1 ).
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Starting dose is 100 mg three times during the day ( 2.1 ) Titrate by 100 mg three times daily, up to a maximum dose of 600 mg three times daily ( 2.1 ) Take consistently with or without food ( 2.1 ) To reduce the potential for supine hypertension, elevate the head of the bed and give the last dose at least 3 hours prior to bedtime ( 2.1 ) Take Droxidopa capsule whole ( 2.1 )
2.1Dosing Information The recommended starting dose of Droxidopa capsules is 100 mg, taken orally three times daily: 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). Administer Droxidopa capsules consistently, either with food or without food. Take Droxidopa capsule whole.
Titrate to symptomatic response, in increments of 100 mg three times daily every 24 to 48 hours up to a maximum dose of 600 mg three times daily (i.e., a maximum total daily dose of 1,800 mg). Monitor supine blood pressure prior to initiating Droxidopa capsules and after increasing the dose. Patients who miss a dose of Droxidopa should take their next scheduled dose.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Droxidopa capsules are available in 100 mg, 200 mg, and 300 mg strengths as specified below. 100 mg: Off white to light brownish powder filled in size “3” hard gelatin capsules with opaque light blue colored cap and opaque white colored body imprinted ‘SG’on cap and ‘429’on body with black ink. 200 mg: Off white to light brownish powder filled in size “2” hard gelatin capsules with opaque light yellow colored cap and opaque white colored body imprinted ‘SG’on cap and ‘430’on body with black ink.
300 mg: Off white to light brownish powder filled in size “1” hard gelatin capsules with opaque light green colored cap and opaque white colored body imprinted ‘SG’on cap and ‘431’on body with black ink. 100 mg, 200 mg, and 300 mg capsules ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Droxidopa capsules are contraindicated in patients who have a history of hypersensitivity to the drug or its ingredients [see Warnings and Precautions ( 5.4 )]. History of hypersensitivity to the drug or its ingredients ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Droxidopa may cause supine hypertension and may increase cardiovascular risk if supine hypertension is not well-managed ( 5.1 ) Hyperpyrexia and confusion ( 5.2 ) May exacerbate symptoms in patients with existing ischemic heart disease, arrhythmias, and congestive heart failure ( 5.3 ) Allergic reactions ( 5.4 )
5.1Supine Hypertension Droxidopa therapy may cause or exacerbate supine hypertension in patients with nOH. Patients should be advised to elevate the head of the bed when resting or sleeping. Monitor blood pressure, both in the supine position and in the recommended head-elevated sleeping position.
Reduce or discontinue Droxidopa if supine hypertension persists. If supine hypertension is not well-managed, Droxidopa may increase the risk of cardiovascular events, particularly stroke.
5.2Hyperpyrexia and Confusion Postmarketing cases of a symptom complex resembling neuroleptic malignant syndrome (NMS) have been reported with Droxidopa use during postmarketing surveillance. Observe patients carefully when the dosage of Droxidopa is changed or when concomitant levodopa is reduced abruptly or discontinued, especially if the patient is receiving neuroleptics. NMS is an uncommon but life-threatening syndrome characterized by fever or hyperthermia, muscle rigidity, involuntary movements, altered consciousness, and mental status changes.
The early diagnosis of this condition is important for the appropriate management of these patients.
5.3Ischemic Heart Disease, Arrhythmias, and Congestive Heart Failure Droxidopa may exacerbate existing ischemic heart disease, arrhythmias, and congestive heart failure. Careful consideration should be given to this potential risk prior to initiating therapy in patients with these conditions.
5.4Allergic Reactions Hypersensitivity reactions including anaphylaxis, angioedema, bronchospasm, urticaria and rash have been reported in postmarketing experience. Some of these reactions resulted in emergency treatment. If a hypersensitivity reaction occurs, discontinue the drug and initiate appropriate therapy.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions with Droxidopa are included in more detail in the Warnings and Precautions section of the label: Supine Hypertension [see Warnings and Precautions ( 5.1 )] Hyperpyrexia and Confusion [see Warnings and Precautions ( 5.2 )] May exacerbate existing ischemic heart disease, arrhythmias, and congestive heart failure [see Warnings and Precautions ( 5.3 )] The most common adverse reactions (>5% and ≥3% compared to placebo) are headache, dizziness, nausea, and hypertension ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ScieGen Pharmaceuticals, Inc. at 1-855-724-3436 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The safety evaluation of Droxidopa is based on two placebo-controlled studies 1 to 2 weeks in duration (Studies 301 and 302), one 8-week placebo-controlled study (Study 306), and two long-term, open-label extension studies (Studies 303 and 304).
In the placebo-controlled studies, a total of 485 patients with Parkinson's disease, multiple system atrophy, pure autonomic failure, dopamine beta-hydroxylase deficiency, or non-diabetic autonomic neuropathy were randomized and treated, 245 with Droxidopa and 240 with placebo [see Clinical Studies ( 14 )] . Placebo-Controlled Experience The most commonly observed adverse reactions (those occurring at an incidence of greater than 5% in the Droxidopa group and with at least a 3% greater incidence in the Droxidopa group than in the placebo group) in Droxidopa-treated patients during the three placebo-controlled trials were headache, dizziness, nausea, and hypertension.
The most common adverse reactions leading to discontinuation from Droxidopa were hypertension or increased blood pressure and nausea. Table1. Most Common Adverse Reactions Occurring More Frequently in the Droxidopa Group Study 301 and Study 302 (1 to 2 Weeks Randomized Treatment) Study 306 (8 to 10 Weeks Randomized Treatment) Placebo (N=132) n (%) Droxidopa (N=131) n (%) Placebo (N=108) n (%) Droxidopa (N=114) n (%) Headache 4 (3.0) 8 (6.1) 8 (7.4) 15 (13.2) Dizziness 2 (1.5) 5 (3.8) 5 (4.6) 11 (9.6) Nausea 2 (1.5) 2 (1.5) 5 (4.6) 10 (8.8) Hypertension 0 2 (1.5) 1 (0.9) 8 (7.0) Note: n=number of patients.
Adverse reactions that were reported in greater than 5% of patients in the Droxidopa group and with at least a 3% greater incidence in the Droxidopa group than in the placebo group were from Study 306. Long-Term, Open-Label Trials with Droxidopa In the long-term, open-label extension studies, a total of 422 patients, mean age 65 years, were treated with Droxidopa for a mean total exposure of approximately one year. The commonly reported adverse events were falls (24%), urinary tract infections (15%), headache (13%), syncope (13%), and dizziness (10%).
6.2Postmarketing Experience The following adverse reactions have been identified during post-approval use of Droxidopa. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Cardiac Disorders: Chest pain Eye Disorders: Blurred vision Gastrointestinal Disorders: Pancreatitis, abdominal pain, vomiting, diarrhea General Disorders and Administration Site Conditions: Fatigue Nervous System Disorders: Cerebrovascular accident Psychiatric Disorders: Psychosis, hallucination, delirium, agitation, memory disorder
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Use of DOPA decarboxylase inhibitors may require dose adjustments for Droxidopa ( 7.2 )
7.1Drugs that Increase Blood Pressure Administering Droxidopa capsules in combination with other agents that increase blood pressure (e.g., norepinephrine, ephedrine, midodrine, and triptans) would be expected to increase the risk for supine hypertension.
7.2Parkinson's Medications Dopa-decarboxylase inhibitors may require dose adjustments for Droxidopa.
7.3Non-selective MAO Inhibitors The concomitant use of selective MAO-B inhibitors, such as rasagiline or selegiline, was permitted in the Droxidopa clinical trials. However, based on mechanism of action, the use of non-selective MAO inhibitors and linezolid should be avoided as there is a potential for increased blood pressure when taken with Droxidopa.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation : Breastfeeding not recommended ( 8.2 ) Patients with Renal Impairment : Dosing recommendations cannot be provided for patients with GFR less than 30 mL/min ( 8.6 )
8.1Pregnancy Risk Summary There are no available data on use of Droxidopa in pregnant women and risk of major birth defects or miscarriage. Droxidopa did not produce significant reproductive toxicity in pregnant female rats or rabbits or in their fetuses. However, when pregnant female rats were dosed during days 7-17 of gestation (the period of fetal organogenesis) with doses of Droxidopa corresponding to 0.3, 1 and 3 times the maximum recommended daily dose of 1,800 mg in a 60 kg patient, based on body surface area, and when their male and female offspring (who were exposed only during fetal life) were subsequently bred, the female offspring exhibited a dose-dependent reduction in the number of live fetuses across all three doses and an increased number of embryonic/fetal deaths at the two higher doses ( see Data ).
The estimated background risk of major birth defects and miscarriage in the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data During a multigenerational reproductive toxicity study in rats, pregnant females were dosed during days 7-17 of gestation (the period of fetal organogenesis) with doses of Droxidopa corresponding to 0.3, 1 and 3 times the maximum recommended daily dose of 1,800 mg in a 60 kg patient.
Reduced weight gain, renal lesions, and a small number of deaths were observed in females treated with the two higher doses. When their male and female offspring (who were exposed to Droxidopa only during fetal life) were subsequently bred, the female offspring exhibited a dose-dependent reduction in the number of live fetuses across all three doses and an increased number of embryonic/fetal deaths at the two higher doses.
8.2Lactation Risk Summary There is no information regarding the presence of Droxidopa or its active metabolite(s) in human milk, the effects of Droxidopa on the breastfed child, nor the effects of Droxidopa on milk production/excretion. Droxidopa is present in rat milk with peak concentrations seen 4 hours after oral drug administration and drug excretion into milk still occurring 48 hours after administration ( see Data ). However, due to species-specific differences in lactation physiology, animal lactation data typically do not reliably predict levels in humans.
Because of the potential for serious adverse reactions, including reduced weight gain in breastfed infants, advise a woman not to breastfeed during treatment with Droxidopa. Data Animal Data In rats, oral administration of droxidopa resulted in excretion into breast milk with peak concentrations seen 4 hours after administration, and excretion still occurring 48 hours after administration. When the drug was administered to nursing dams during the period of lactation at a dose corresponding to 3 times the maximum recommended daily dose of 1,800 mg in a 60 kg patient when based on body surface area, reduced weight gain and reduced survival were observed in the offspring.
Despite the observed decreased weight gain, physical development was normal (with respect to timing and organ morphology).
8.4Pediatric Use The safety and effectiveness of Droxidopa in pediatric patients have not been established.
8.5Geriatric Use A total of 197 patients with symptomatic nOH aged 75 years or above were included in the Droxidopa clinical program. No overall differences in safety or effectiveness were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
8.6 Renal Impairment Droxi…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary There are no available data on use of Droxidopa in pregnant women and risk of major birth defects or miscarriage. Droxidopa did not produce significant reproductive toxicity in pregnant female rats or rabbits or in their fetuses. However, when pregnant female rats were dosed during days 7-17 of gestation (the period of fetal organogenesis) with doses of Droxidopa corresponding to 0.3, 1 and 3 times the maximum recommended daily dose of 1,800 mg in a 60 kg patient, based on body surface area, and when their male and female offspring (who were exposed only during fetal life) were subsequently bred, the female offspring exhibited a dose-dependent reduction in the number of live fetuses across all three doses and an increased number of embryonic/fetal deaths at the two higher doses ( see Data ).
The estimated background risk of major birth defects and miscarriage in the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data During a multigenerational reproductive toxicity study in rats, pregnant females were dosed during days 7-17 of gestation (the period of fetal organogenesis) with doses of Droxidopa corresponding to 0.3, 1 and 3 times the maximum recommended daily dose of 1,800 mg in a 60 kg patient.
Reduced weight gain, renal lesions, and a small number of deaths were observed in females treated with the two higher doses. When their male and female offspring (who were exposed to Droxidopa only during fetal life) were subsequently bred, the female offspring exhibited a dose-dependent reduction in the number of live fetuses across all three doses and an increased number of embryonic/fetal deaths at the two higher doses.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of Droxidopa in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use A total of 197 patients with symptomatic nOH aged 75 years or above were included in the Droxidopa clinical program. No overall differences in safety or effectiveness were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE
10.1Symptoms There have been cases of overdose reported during postmarketing surveillance. A patient ingested 7,700 mg of droxidopa and experienced a hypertensive crisis that resolved promptly with treatment. Another patient treated with a total daily dose of 2,700 mg of Droxidopa experienced hypertension and an intracranial hemorrhage.
10.2Treatment There is no known antidote for Droxidopa overdosage. In case of an overdose that may result in an excessively high blood pressure, discontinue Droxidopa and treat with appropriate symptomatic and supportive therapy. Counsel patients to remain in a standing or seated position until their blood pressure drops below an acceptable limit.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The exact mechanism of action of Droxidopa in the treatment of neurogenic orthostatic hypotension is unknown. Droxidopa is a synthetic amino acid analog that is directly metabolized to norepinephrine by dopa-decarboxylase, which is extensively distributed throughout the body. Droxidopa is believed to exert its pharmacological effects through norepinephrine and not through the parent molecule or other metabolites.
Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction. Droxidopa in humans induces small and transient rises in plasma norepinephrine.
12.2Pharmacodynamics Peak droxidopa plasma concentrations are associated with increases in systolic and diastolic blood pressures. Droxidopa has no clinically significant effect on standing or supine heart rates in patients with autonomic failure. Cardiac Electrophysiology No prolongation of the QTc interval was observed with Droxidopa at single oral doses up to 2,000 mg, as shown in a dedicated thorough QT study.
12.3Pharmacokinetics Absorption Peak plasma concentrations (C max ) of droxidopa were reached by 1 to 4 hours post-dose (mean of approximately 2 hours) in healthy volunteers. High-fat meals have a moderate impact on droxidopa exposure with C max and area under the plasma concentration-time curve (AUC) decreasing by 35% and 20%, respectively. The C max was delayed by approximately 2 hours with a high-fat meal.
Distribution Pre-clinical studies suggest that droxidopa can cross the blood-brain barrier. Droxidopa exhibits plasma protein binding of 75% at 100 ng/mL and 26% at 10,000 ng/mL. The estimated apparent volume of distribution of droxidopa is about 200 L in humans.
Elimination The total clearance of droxidopa after oral administration (CL/F) was approximately 400 mL/hr following administration of a single 300 mg dose. Metabolism The metabolism of droxidopa is mediated by catecholamine pathway and not through the cytochrome P450 system. 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.
After oral dosing in humans, plasma norepinephrine levels peak within 3 to 4 hours but are generally very low (less than 1 ng/mL) and variable with no consistent relationship with dose. The contribution of the metabolites of droxidopa other than norepinephrine to its pharmacological effects is not well understood. Excretion The mean elimination half-life of droxidopa is approximately 2.5 hours in humans.
The major route of elimination of droxidopa and its metabolites is via the kidneys in both animals and in humans. Studies in animals with radiolabeled drug showed that ~75% of the administered radioactivity was excreted in urine within 24 hours of oral dosing. Specific Populations There are no clinically relevant effects of age, body mass index, or sex on the pharmacokinetics of droxidopa.
A population pharmacokinetic analysis suggests that hepatic function, assessed by aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase, and total bilirubin, did not influence the exposure to droxidopa. The controlled clinical trials included patients with mild to moderate renal impairment. No dose adjustments are required in patients with mild to moderate renal impairment.
Drug Interaction Studies No dedicated drug-drug interaction studies were performed for droxidopa. Patients in the Phase 3 trials with Droxidopa received concomitant levodopa/carbidopa, dopamine agonists, MAO-B inhibitors, COMT inhibitors and other medications used to treat Parkinson’s disease. Carbidopa, a peripheral dopa-decarboxylase inhibitor, could prevent the conversion of Droxidopa to norepinephrine outside of the central nervous system (CNS).
Patients taking Droxidopa with L-DOPA/dopa-decarboxylase inhibitor combination…
🧬 Mechanism of Action ▾
12.1Mechanism of Action The exact mechanism of action of Droxidopa in the treatment of neurogenic orthostatic hypotension is unknown. Droxidopa is a synthetic amino acid analog that is directly metabolized to norepinephrine by dopa-decarboxylase, which is extensively distributed throughout the body. Droxidopa is believed to exert its pharmacological effects through norepinephrine and not through the parent molecule or other metabolites.
Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction. Droxidopa in humans induces small and transient rises in plasma norepinephrine.
📦 How Supplied / Storage and Handling ▾
16.1How Supplied Droxidopa capsules are supplied in the following dosage strengths: 100 mg: Off white to light brownish powder filled in size “3” hard gelatin capsules with opaque light blue colored cap and opaque white colored body imprinted ‘SG’ on cap and ‘429’ on body with black ink. Bottles of 30 NDC 50228-429-30 Bottles of 90 NDC 50228-429-90 Bottles of 1,000 NDC 50228-429-10 200 mg: Off white to light brownish powder filled in size “2” hard gelatin capsules with opaque light yellow colored cap and opaque white colored body imprinted ‘SG’ on cap and ‘430’ on body with black ink.
Bottles of 30 NDC 50228-430-30 Bottles of 90 NDC 50228-430-90 Bottles of 1,000 NDC 50228-430-10 300 mg: Off white to light brownish powder filled in size “1” hard gelatin capsules with opaque light green colored cap and opaque white colored body imprinted ‘SG’ on cap and ‘431’ on body with black ink. Bottles of 30 NDC 50228-431-30 Bottles of 90 NDC 50228-431-90 Bottles of 500 NDC 50228-431-05
📦 Storage and Handling ▾
16.2Storage and Handling Droxidopa capsules should be stored at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [ see USP Controlled Room Temperature ].
📋 Description ▾
11 DESCRIPTION Droxidopa capsules contain droxidopa, which is a synthetic amino acid precursor of norepinephrine, for oral administration. Chemically, droxidopa is (–)-threo-3-(3,4- Dihydroxyphenyl)-L-serine. It has the following structural formula: Droxidopa is a white to light brown crystalline powder.
It is soluble in dilute hydrochloric acid, and practically insoluble in methanol, glacial acetic acid, ethanol, acetone, ether and chloroform. It has a molecular weight of 213.19 and a molecular formula of C 9 H 11 NO 5 . Droxidopa capsules also contain the following inactive ingredients: mannitol, corn starch, pregelatinized starch, and magnesium stearate.
The capsule shell is printed with black ink. The black inks contain shellac, ethanol, isopropyl alcohol, n-butyl alcohol, propylene glycol, ammonia solution, iron oxide black and potassium hydroxide. The capsule shell contains the following inactive ingredients: 100 mg – gelatin, titanium dioxide, FD&C Blue No.
2, black and red iron oxide; 200 mg – gelatin, titanium dioxide, black and yellow iron oxide; 300 mg – gelatin, titanium dioxide, FD&C Blue No. 1and D&C Yellow No. 10.
Droxidopa capsules differ in size and color by strength [see Dosage Forms and Strengths ( 3 )] . Droxidopa-01
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Elevations in Blood Pressure Counsel patients that Droxidopa causes elevations in blood pressure and increases the risk of supine hypertension, which could lead to strokes, heart attacks, and death. Instruct patients to rest and sleep in an upper-body elevated position and monitor blood pressure. Instruct patients how to manage observed blood pressure elevations.
To reduce the risk of supine hypertension, in addition to raising the upper body, the late afternoon dose of Droxidopa should be taken at least three hours before bedtime [see Warnings and Precautions ( 5.1 )] . Concomitant Treatments Counsel patients about the concomitant use of drugs to treat other conditions that may have an additive effect with Droxidopa [see Drug Interactions ( 7 )]. Allergic Reactions Counsel patients to discontinue Droxidopa and seek immediate medical attention if any signs or symptoms of a hypersensitivity reaction such as anaphylaxis, angioedema, bronchospasm, urticaria or rash occur [see Warnings and Precautions ( 5.4 )].
Lactation Advise women not to breastfeed during treatment with Droxidopa [see Use in Specific Populations ( 8.2 )] . Food Patients should take Droxidopa the same way each time, either with food or without food [see Dosage and Administration ( 2.1 )] . Missed Dose If a dose is missed, patients should take the next dose at the regularly scheduled time and should not double the dose.
Manufactured by: ScieGen Pharmaceuticals Inc Hauppauge, NY 11788 USA Rev. 1/2021