Droxidopa 200mg 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
Vasopressor
Pharmacologic Class
Synthetic norepinephrine precursor
Pregnancy Category
Not available
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. It works by increasing a natural chemical in your body called norepinephrine, which helps to raise your blood pressure.
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 with your prescription and follow the instructions closely.
Take your medication as directed, swallowing the tablets or capsules whole. Do not chew, open, or crush them.
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.
To minimize the risk of high blood pressure during sleep, take your last dose of the day at least 3 hours before bedtime.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding storage in a bathroom.
* Keep all medications in a safe location, out of the reach of children and pets, to prevent accidental ingestion.
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 with your prescription and follow the instructions closely.
Take your medication as directed, swallowing the tablets or capsules whole. Do not chew, open, or crush them.
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.
To minimize the risk of high blood pressure during sleep, take your last dose of the day at least 3 hours before bedtime.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding storage in a bathroom.
* Keep all medications in a safe location, out of the reach of children and pets, to prevent accidental ingestion.
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 taking the last dose too close to bedtime (at least 3 hours before) to reduce the risk of high blood pressure while lying down.
- Elevate the head of your bed to help reduce supine hypertension.
- Stay hydrated and maintain adequate salt intake as advised by your doctor.
- Avoid sudden changes in position (e.g., standing up too quickly).
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
100 mg three times daily (TID)
Dose Range:
100 - 600 mg
Condition-Specific Dosing:
neurogenicOrthostaticHypotension:
Initial dose 100 mg TID, titrated up to 600 mg TID (maximum 1800 mg/day) based on supine and standing blood pressure and symptom control. Doses should be separated by at least 3 hours. The last dose should be taken at least 3 hours prior to bedtime.
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:
No specific dose adjustment recommended
Dialysis:
Not studied; use with caution and monitor blood pressure closely.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended
Moderate:
No specific dose adjustment recommended
Severe:
Not studied; use with caution and monitor blood pressure closely.
Pharmacology
Mechanism of Action
Droxidopa is a synthetic amino acid precursor of norepinephrine. It is converted to norepinephrine by the enzyme DOPA decarboxylase (aromatic L-amino acid decarboxylase) in the central and peripheral nervous systems. Norepinephrine acts on alpha-1 adrenergic receptors in the vasculature, leading to vasoconstriction and an increase in blood pressure, thereby alleviating orthostatic hypotension symptoms.
Pharmacokinetics
Absorption:
Bioavailability:
Not available
Tmax:
Approximately 3 hours (for droxidopa), 4 hours (for active metabolite, norepinephrine)
FoodEffect:
High-fat meal delays Tmax by approximately 1 hour and decreases Cmax by approximately 30% for droxidopa, but does not significantly affect AUC or Cmax of norepinephrine.
Distribution:
Vd:
Not available
ProteinBinding:
Not available
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
Approximately 2-3 hours (for droxidopa), 3-7 hours (for norepinephrine)
Clearance:
Not available
ExcretionRoute:
Primarily renal (as metabolites)
Unchanged:
Less than 1% (of droxidopa)
Pharmacodynamics
OnsetOfAction:
Within 1-2 hours
PeakEffect:
Approximately 3-4 hours
DurationOfAction:
Approximately 4-6 hours (based on dosing frequency)
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
Droxidopa can cause supine hypertension. Monitor supine blood pressure prior to and during treatment and more frequently when titrating droxidopa. If supine blood pressure increases excessively, reduce or discontinue droxidopa. The risk of supine hypertension is greatest during the first 2 weeks of treatment and with higher doses.
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
+ Passing out
+ 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 eyesight
Falls
Neuroleptic malignant syndrome (NMS), a rare but potentially life-threatening condition, characterized by:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Fast 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 help:
Dizziness
Headache
* Upset stomach
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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
+ Passing out
+ 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 eyesight
Falls
Neuroleptic malignant syndrome (NMS), a rare but potentially life-threatening condition, characterized by:
+ Fever
+ Muscle cramps or stiffness
+ Dizziness
+ Severe headache
+ Confusion
+ Changes in thinking
+ Fast 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 help:
Dizziness
Headache
* Upset stomach
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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:
- Severe headache
- Blurred vision
- Chest pain
- Shortness of breath
- Pounding in the ears
- Nosebleeds
- Any new or worsening symptoms of high blood pressure while lying down (supine hypertension).
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, including any symptoms that occurred.
If you are currently taking or have recently taken any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine (monoamine oxidase inhibitors, or MAOIs)
+ Linezolid or methylene blue
* If you are breast-feeding, as you should not breast-feed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter (OTC) 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 to ensure your safety.
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, including any symptoms that occurred.
If you are currently taking or have recently taken any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine (monoamine oxidase inhibitors, or MAOIs)
+ Linezolid or methylene blue
* If you are breast-feeding, as you should not breast-feed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter (OTC) 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 to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Regularly monitor your blood pressure as instructed by your healthcare provider.
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.
Patients with pre-existing heart conditions, such as abnormal heartbeat or heart failure, should be aware that this medication may exacerbate these conditions. If you have a history of heart problems, discuss the potential risks with your doctor. Immediately contact your doctor if you experience any new or worsening symptoms, including abnormal heartbeat, shortness of breath, significant weight gain, or swelling in the 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.
Regularly monitor your blood pressure as instructed by your healthcare provider.
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.
Patients with pre-existing heart conditions, such as abnormal heartbeat or heart failure, should be aware that this medication may exacerbate these conditions. If you have a history of heart problems, discuss the potential risks with your doctor. Immediately contact your doctor if you experience any new or worsening symptoms, including abnormal heartbeat, shortness of breath, significant weight gain, or swelling in the 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:
- Excessive hypertension (high blood pressure)
- Headache
- Palpitations
- Bradycardia (slow heart rate, reflex)
- Chest pain
- Blurred vision
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive, focusing on managing blood pressure (e.g., with alpha-adrenergic blocking agents if severe hypertension occurs).
Drug Interactions
Major Interactions
- Monoamine Oxidase Inhibitors (MAOIs): May increase blood pressure due to inhibition of norepinephrine metabolism.
- Tricyclic Antidepressants (TCAs): May potentiate the pressor effect of droxidopa.
- Linezolid: Has MAOI activity and may increase blood pressure.
Moderate Interactions
- Beta-blockers: May reduce the effectiveness of droxidopa or lead to unopposed alpha-adrenergic effects.
- Alpha-adrenergic agonists (e.g., pseudoephedrine, phenylephrine): Additive pressor effects.
- DOPA decarboxylase inhibitors (e.g., carbidopa, benserazide): May reduce the conversion of droxidopa to norepinephrine, decreasing efficacy. (Note: Carbidopa is sometimes used to reduce peripheral conversion and increase CNS availability, but can also reduce overall norepinephrine levels if not carefully managed).
Confidence Interactions
Monitoring
Baseline Monitoring
Supine and standing blood pressure
Rationale: To establish baseline and guide initial dosing, and to assess for supine hypertension risk.
Timing: Prior to initiation of therapy
Heart rate
Rationale: To establish baseline and monitor for reflex bradycardia or tachycardia.
Timing: Prior to initiation of therapy
Renal function (BUN, creatinine)
Rationale: Although no specific dose adjustment is recommended, baseline assessment is prudent.
Timing: Prior to initiation of therapy
Hepatic function (ALT, AST, bilirubin)
Rationale: Although no specific dose adjustment is recommended, baseline assessment is prudent.
Timing: Prior to initiation of therapy
Routine Monitoring
Supine and standing blood pressure
Frequency: Regularly, especially during dose titration and periodically thereafter (e.g., weekly during titration, then monthly or as clinically indicated)
Target: Individualized, aiming for symptom control without excessive supine hypertension (e.g., supine systolic BP <180 mmHg)
Action Threshold: Supine systolic BP >180 mmHg or diastolic BP >110 mmHg; significant increase in supine BP; symptomatic supine hypertension. Consider dose reduction or discontinuation.
Symptoms of orthostatic hypotension
Frequency: Continuously
Target: Reduction or resolution of dizziness, lightheadedness, falls
Action Threshold: Persistent or worsening symptoms despite adequate dosing; new or worsening supine hypertension.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fainting (syncope)
- Falls
- Fatigue
- Blurred vision
- Supine hypertension symptoms (headache, blurred vision, chest pain, shortness of breath, palpitations)
Special Patient Groups
Pregnancy
There are no adequate and well-controlled studies of droxidopa in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at doses higher than human therapeutic doses.
Trimester-Specific Risks:
First Trimester:
Not specifically studied, but general caution for drug exposure during organogenesis.
Second Trimester:
Not specifically studied.
Third Trimester:
Not specifically studied, but potential for effects on fetal circulation due to vasoconstrictive properties.
Lactation
It is not known whether droxidopa or its metabolites are excreted in human milk. Because many drugs are excreted in human milk and because of 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:
Not available, but theoretical risk of cardiovascular effects due to norepinephrine conversion.
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 subjects and younger subjects, 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, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Droxidopa is specifically indicated for symptomatic neurogenic orthostatic hypotension (nOH) caused by primary autonomic failure (e.g., Parkinson's disease, multiple system atrophy, pure autonomic failure), dopamine beta-hydroxylase deficiency, or non-diabetic autonomic neuropathy.
- The most significant adverse effect is supine hypertension, which requires careful monitoring of blood pressure, especially before and during dose titration.
- Patients should be instructed to take the last dose at least 3 hours before bedtime and to elevate the head of their bed to mitigate supine hypertension.
- Efficacy may wane over time in some patients; periodic re-evaluation of treatment benefit is recommended.
- Patients should be advised to report any symptoms of high blood pressure, such as severe headache, blurred vision, or chest pain.
Alternative Therapies
- Midodrine (another alpha-1 adrenergic agonist)
- Fludrocortisone (mineralocorticoid)
- Pyridostigmine (acetylcholinesterase inhibitor, off-label for nOH)
- Non-pharmacological measures (e.g., increased fluid and salt intake, compression stockings, physical counter-maneuvers, head-of-bed elevation)
Cost & Coverage
Average Cost:
Varies widely, typically high per 30 capsules
Insurance Coverage:
Specialty Tier (requires prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 details about the medication taken, the amount, and the time it occurred.