Droxidopa 300mg Capsules
WARNING: This drug may cause high blood pressure, especially when lying down. You will need to watch your blood pressure closely before you start this drug and during treatment. Do this also with any increase in dose. Be sure to rest and sleep with your upper body raised. If high blood pressure is not controlled well, the risk of stroke, heart attack, and death may be raised. @ COMMON USES: It is used to treat dizziness or the feeling that you are about to black out.
Drug Class
Alpha/beta-adrenergic agonist (prodrug), Vasopressor, Agent for Neurogenic Orthostatic Hypotension
Pharmacologic Class
Synthetic amino acid, prodrug of norepinephrine
Pregnancy Category
Category C
FDA Approved
Feb 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Droxidopa is a medication used to treat very low blood pressure that happens when you stand up, a condition called neurogenic orthostatic hypotension (nOH). It works by increasing the amount of a natural chemical in your body called norepinephrine, which helps to tighten blood vessels and raise your blood pressure, reducing symptoms like dizziness and fainting.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions precisely.
Take your medication as a whole tablet. Do not chew, break, or crush it.
You can take your medication with or without food, but be consistent in how you take it each time. Choose to either always take it with food or always take it on an empty stomach.
Be sure to take your last dose of the day at least 3 hours before bedtime. This will help reduce the risk of high blood pressure during sleep.
Storing and Disposing of Your Medication
To keep your medication effective and safe:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions precisely.
Take your medication as a whole tablet. Do not chew, break, or crush it.
You can take your medication with or without food, but be consistent in how you take it each time. Choose to either always take it with food or always take it on an empty stomach.
Be sure to take your last dose of the day at least 3 hours before bedtime. This will help reduce the risk of high blood pressure during sleep.
Storing and Disposing of Your Medication
To keep your medication effective and safe:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Avoid sudden changes in position; stand up slowly.
- Increase fluid and salt intake as advised by your doctor.
- Wear compression stockings.
- Elevate the head of your bed (e.g., by 6-9 inches) to reduce supine hypertension.
- Avoid prolonged standing.
- Avoid large meals, especially high-carbohydrate meals.
- Avoid alcohol.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 100 mg orally 3 times daily (TID). Titrate by 100 mg TID increments every 1-2 days based on supine blood pressure and symptom control. Administer at least 3 hours prior to bedtime.
Dose Range:
300 - 1800 mg
Condition-Specific Dosing:
maximumDailyDose:
1800 mg/day (600 mg TID)
administrationTiming:
Administer at least 3 hours prior to bedtime to reduce potential for supine hypertension.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; monitor for supine hypertension. No specific dose adjustment guidelines.
Dialysis:
Not specifically studied; use with caution and monitor closely.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose adjustment guidelines.
Pharmacology
Mechanism of Action
Droxidopa is a synthetic amino acid analog that serves as a prodrug for norepinephrine (noradrenaline). It is converted to norepinephrine by the enzyme aromatic L-amino acid decarboxylase (AADC) in both the central and peripheral nervous systems. Norepinephrine acts on alpha-1 adrenergic receptors on blood vessels, causing vasoconstriction and increasing blood pressure, which helps to alleviate symptoms of neurogenic orthostatic hypotension (nOH).
Pharmacokinetics
Absorption:
Bioavailability:
Not directly reported, well absorbed.
Tmax:
Approximately 3 hours (for droxidopa and threo-DOPS).
FoodEffect:
A high-fat meal delays Tmax by approximately 1 hour and decreases Cmax by approximately 20-30%. Administer consistently with or without food.
Distribution:
Vd:
Not specifically reported for droxidopa; for active metabolite threo-DOPS, Vd is approximately 1.2 L/kg.
ProteinBinding:
Low (approximately 10-20%).
CnssPenetration:
Yes
Elimination:
HalfLife:
Droxidopa: approximately 2-3 hours; Active metabolite (threo-DOPS): approximately 2-3 hours.
Clearance:
Not specifically reported.
ExcretionRoute:
Primarily renal excretion of metabolites.
Unchanged:
Less than 1% of droxidopa is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 1-2 hours
PeakEffect:
Approximately 3 hours
DurationOfAction:
Approximately 4-6 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in eyesight
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain while urinating
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Blurred vision
Falls
Neuroleptic malignant syndrome (NMS), a rare but potentially deadly condition, characterized by:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Rapid heartbeat
+ Abnormal heartbeat
+ Excessive sweating
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
Dizziness
Headache
* Upset stomach
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in eyesight
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain while urinating
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Blurred vision
Falls
Neuroleptic malignant syndrome (NMS), a rare but potentially deadly condition, characterized by:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Rapid heartbeat
+ Abnormal heartbeat
+ Excessive sweating
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
Dizziness
Headache
* Upset stomach
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of high blood pressure (supine hypertension): severe headache, blurred vision, pounding in the ears, chest pain, shortness of breath.
- Allergic reaction: rash, itching, swelling (especially of face/tongue/throat), severe dizziness, trouble breathing.
- Other serious side effects: irregular heartbeat, confusion, hallucinations.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
If you are currently taking any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine
+ Linezolid or methylene blue
* If you are breastfeeding. Please note that you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
If you are currently taking any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine
+ Linezolid or methylene blue
* If you are breastfeeding. Please note that you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
To monitor your condition, follow the instructions provided by your healthcare provider for checking your blood pressure.
If you have a known allergy to tartrazine (also referred to as FD&C Yellow No. 5), consult with your doctor before taking this medication, as some formulations may contain this ingredient.
Pre-existing heart conditions, such as abnormal heartbeat and heart failure, may worsen with the use of this drug. If you have a history of heart problems, discuss the potential risks with your doctor. Immediately contact your doctor if you experience any of the following symptoms: abnormal heartbeat, shortness of breath, significant weight gain, or new or worsening swelling in your arms or legs.
If you are pregnant or planning to become pregnant, consult with your doctor to discuss the potential benefits and risks associated with using this medication during pregnancy.
To monitor your condition, follow the instructions provided by your healthcare provider for checking your blood pressure.
If you have a known allergy to tartrazine (also referred to as FD&C Yellow No. 5), consult with your doctor before taking this medication, as some formulations may contain this ingredient.
Pre-existing heart conditions, such as abnormal heartbeat and heart failure, may worsen with the use of this drug. If you have a history of heart problems, discuss the potential risks with your doctor. Immediately contact your doctor if you experience any of the following symptoms: abnormal heartbeat, shortness of breath, significant weight gain, or new or worsening swelling in your arms or legs.
If you are pregnant or planning to become pregnant, consult with your doctor to discuss the potential benefits and risks associated with using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Severe supine hypertension
- headache
- palpitations
- bradycardia
- reflex tachycardia
What to Do:
Call 911 or Poison Control (1-800-222-1222). Treatment is supportive, including elevating the head of the bed, and potentially administering alpha-adrenergic blocking agents if hypertension is severe and persistent.
Drug Interactions
Contraindicated Interactions
- Non-selective monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, tranylcypromine, isocarboxazid, selegiline, linezolid, methylene blue)
Major Interactions
- Tricyclic antidepressants (TCAs) (e.g., amitriptyline, imipramine)
- Other adrenergic agents (e.g., pseudoephedrine, phenylephrine, midodrine, ephedrine)
- Alpha-adrenergic antagonists (e.g., prazosin, tamsulosin)
Moderate Interactions
- Non-selective beta-blockers
- Drugs that inhibit AADC (e.g., carbidopa, benserazide)
Monitoring
Baseline Monitoring
Supine and standing blood pressure (BP) and heart rate (HR)
Rationale: To establish baseline hemodynamic status, assess the severity of orthostatic hypotension, and identify pre-existing supine hypertension.
Timing: Prior to initiation of therapy.
Routine Monitoring
Supine and standing BP and HR
Frequency: At each dose titration step and regularly during maintenance therapy (e.g., weekly initially, then monthly or as clinically indicated).
Target: Supine BP should be maintained below 180/110 mmHg. Standing BP should show improvement in orthostatic symptoms without excessive supine hypertension.
Action Threshold: If supine systolic BP consistently exceeds 180 mmHg or diastolic BP exceeds 110 mmHg, or if symptomatic supine hypertension occurs, reduce dose or discontinue.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Syncope
- Fatigue (for efficacy)
- Headache
- Palpitations
- Nausea
- Pounding in ears
- Blurred vision
- Chest pain (for supine hypertension)
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Animal studies showed developmental toxicity (reduced fetal weight, skeletal variations) at doses higher than human therapeutic doses.
Second Trimester:
Similar risks as first trimester.
Third Trimester:
No specific data, but theoretical risk of effects on fetal circulation due to adrenergic activity.
Lactation
It is not known if droxidopa or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Potential for adverse adrenergic effects (e.g., increased blood pressure, irritability) in the infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range.
Clinical Information
Clinical Pearls
- Droxidopa is a prodrug that requires conversion to norepinephrine; its efficacy can be affected by drugs that inhibit AADC (e.g., carbidopa).
- The primary dose-limiting side effect is supine hypertension; patients must be instructed to elevate the head of their bed and avoid taking the last dose too close to bedtime (at least 3 hours prior).
- Monitor supine and standing blood pressure closely, especially during dose titration and regularly during maintenance therapy.
- It is specifically indicated for symptomatic neurogenic orthostatic hypotension (nOH), not general orthostatic hypotension from other causes.
- Patients should be advised to take the medication consistently with or without food, but be aware that a high-fat meal can delay absorption.
Alternative Therapies
- Midodrine (another alpha-1 adrenergic agonist)
- Fludrocortisone (mineralocorticoid, increases blood volume)
- Pyridostigmine (cholinesterase inhibitor, may improve nOH in some patients)
- Non-pharmacological measures (e.g., increased fluid and salt intake, compression stockings, head-of-bed elevation, physical counter-maneuvers).
Cost & Coverage
Average Cost:
Very high (e.g., $1000s per month) per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Specialty Tier / Tier 4-5
General Drug Facts
If your symptoms or health condition do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may have additional patient information leaflets, so it is a good idea to consult with your pharmacist for more information. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the type and amount of medication taken, as well as the time it occurred.