Droxidopa 100mg 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
Pharmacologic Class
Synthetic Amino Acid Precursor of Norepinephrine
Pregnancy 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 occurs when you stand up (called neurogenic orthostatic hypotension). It works by increasing the amount of a natural chemical in your body called norepinephrine, which helps to tighten blood vessels and raise blood pressure.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription and follow the instructions closely.
When taking your medication:
- Swallow the tablet whole.
- Do not chew, open, or crush it.
- You can take it 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
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Ensure that all medications are kept 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 continue with 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, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription and follow the instructions closely.
When taking your medication:
- Swallow the tablet whole.
- Do not chew, open, or crush it.
- You can take it 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
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Ensure that all medications are kept 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 continue with 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
- Take your blood pressure regularly, especially when lying down, sitting, and standing, as directed by your doctor.
- Avoid taking your last dose too close to bedtime (at least 3 hours before) to reduce the risk of high blood pressure while lying down.
- Report any symptoms of high blood pressure (e.g., severe headache, blurred vision) or very low blood pressure (e.g., dizziness, fainting) to your doctor immediately.
- Stay hydrated 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:
Initial 100 mg orally three times daily (TID). May be titrated by 100 mg TID increments every 1 to 2 days.
Dose Range:
100 - 600 mg
Condition-Specific Dosing:
maximumDailyDose:
1800 mg/day (600 mg TID)
administration:
Administer at least 3 hours prior to bedtime to reduce the 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:
No specific dose adjustment recommended, but use with caution due to limited data.
Dialysis:
Not available; use with caution.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended, but use with caution due to limited data.
Confidence:
Medium
Pharmacology
Mechanism of Action
Droxidopa is a synthetic amino acid precursor of norepinephrine. It is converted to norepinephrine by the enzyme aromatic L-amino acid decarboxylase (AAAD) in the central and peripheral nervous systems. Norepinephrine acts on alpha-1 adrenergic receptors on blood vessels, leading to vasoconstriction and increased blood pressure, which helps to alleviate orthostatic hypotension.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly quantified, but well absorbed.
Tmax:
Approximately 3 hours (for droxidopa); 4-5 hours (for active metabolite threo-DOPS).
FoodEffect:
A high-fat meal delays Tmax by approximately 1 hour and reduces Cmax by approximately 20% for droxidopa, but does not significantly affect AUC.
Distribution:
Vd:
Approximately 1.5 L/kg
ProteinBinding:
Low (<10%)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours (droxidopa); approximately 7 hours (threo-DOPS).
Clearance:
Not available
ExcretionRoute:
Primarily renal (urine)
Unchanged:
Less than 1% of droxidopa is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 1-2 hours
PeakEffect:
Approximately 3-5 hours
DurationOfAction:
Approximately 6-8 hours
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. Manage supine hypertension by reducing the dose or discontinuing droxidopa. Administer the last dose at least 3 hours prior to bedtime.
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 when passing urine
+ 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 deadly 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 experience no side effects or only mild ones, others may have more bothersome symptoms. 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
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact 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 when passing urine
+ 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 deadly 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 experience no side effects or only mild ones, others may have more bothersome symptoms. 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
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact 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
- Pounding in the ears
- Nosebleeds
- Chest pain
- Shortness of breath
- Confusion
- Dizziness or lightheadedness (especially when standing)
- Fainting spells
- Palpitations (feeling your heart race or pound)
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 symptoms you experienced.
If you are currently taking or have recently taken any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine (monoamine oxidase inhibitors)
+ Linezolid or methylene blue
* If you are breastfeeding, as 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 existing health conditions and other medications. Never start, stop, or adjust the dosage 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 symptoms you experienced.
If you are currently taking or have recently taken any of the following medications:
+ Isocarboxazid, phenelzine, or tranylcypromine (monoamine oxidase inhibitors)
+ Linezolid or methylene blue
* If you are breastfeeding, as 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 existing health conditions and other medications. Never start, stop, or adjust the dosage 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. Regularly monitor your blood pressure as directed by your healthcare provider. If you have a known allergy to tartrazine (FD&C Yellow No. 5), consult with your doctor, as some formulations of this drug may contain tartrazine.
Pre-existing heart conditions, such as abnormal heartbeat and heart failure, may worsen with the use of this medication. 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.
Pre-existing heart conditions, such as abnormal heartbeat and heart failure, may worsen with the use of this medication. 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:
- Excessive supine hypertension
- Headache
- Palpitations
- Bradycardia (reflex)
- Cardiac arrhythmias
- Chest pain
- Nervousness
- Tremor
- Insomnia
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Monitor blood pressure closely. Alpha-adrenergic blocking agents may be considered for severe hypertension.
Drug Interactions
Major Interactions
- Monoamine Oxidase Inhibitors (MAOIs): May cause hypertensive crisis due to inhibition of norepinephrine metabolism.
- Tricyclic Antidepressants (TCAs): May potentiate the pressor effect of droxidopa due to inhibition of norepinephrine reuptake.
Moderate Interactions
- Beta-adrenergic blocking agents: May antagonize the effects of droxidopa on blood pressure.
- Alpha-adrenergic agonists (e.g., phenylephrine, midodrine): May have additive pressor effects, increasing the risk of supine hypertension.
- Dopamine antagonists (e.g., metoclopramide, antipsychotics): May reduce the effectiveness of droxidopa by inhibiting its conversion to norepinephrine.
Monitoring
Baseline Monitoring
Supine, sitting, and standing blood pressure (BP)
Rationale: To establish baseline BP and assess the degree of orthostatic hypotension.
Timing: Prior to initiation of therapy.
Heart rate (HR)
Rationale: To establish baseline HR.
Timing: Prior to initiation of therapy.
Routine Monitoring
Supine, sitting, and standing blood pressure (BP)
Frequency: Regularly, especially during dose titration and periodically thereafter.
Target: Maintain standing BP within a safe range while avoiding excessive supine hypertension.
Action Threshold: If supine systolic BP consistently exceeds 180 mmHg, consider dose reduction or discontinuation. If supine diastolic BP consistently exceeds 110 mmHg, consider dose reduction or discontinuation.
Heart rate (HR)
Frequency: Regularly, especially during dose titration and periodically thereafter.
Target: Not specified, but monitor for significant changes.
Action Threshold: Significant bradycardia or tachycardia.
Symptom Monitoring
- Symptoms of orthostatic hypotension (dizziness, lightheadedness, fainting upon standing)
- Symptoms of supine hypertension (headache, blurred vision, palpitations, chest pain, shortness of breath, epistaxis, confusion)
- Symptoms of adrenergic excess (nervousness, anxiety, tremor, insomnia)
Special Patient Groups
Pregnancy
Use during pregnancy 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:
Risk not well-established in humans; animal data suggest potential for developmental toxicity.
Second Trimester:
Risk not well-established in humans; animal data suggest potential for developmental toxicity.
Third Trimester:
Risk not well-established in humans; animal data suggest potential for developmental toxicity. Consider potential for effects on uterine contractility and fetal circulation due to adrenergic activity.
Lactation
It is not known whether droxidopa or its metabolites are excreted in human milk. 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:
Risk unknown; potential for adrenergic effects in 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, 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; careful monitoring of blood pressure in all positions is crucial, especially during titration.
- Patients should be instructed to take the last dose at least 3 hours before bedtime to minimize the risk of supine hypertension during sleep.
- Titration should be slow and gradual (every 1-2 days) to find the lowest effective dose that manages orthostatic symptoms without causing excessive supine hypertension.
- Patients should be advised to avoid sudden position changes and to elevate the head of their bed if supine hypertension is a concern.
Alternative Therapies
- Midodrine (another alpha-1 adrenergic agonist for orthostatic hypotension)
- Fludrocortisone (mineralocorticoid for orthostatic hypotension)
- Pyridostigmine (cholinesterase inhibitor, off-label for nOH)
- Non-pharmacological interventions (e.g., increased fluid and salt intake, compression stockings, physical counter-maneuvers, head-of-bed elevation)
Cost & Coverage
Average Cost:
Highly variable, typically several thousand USD per 90 capsules (100mg)
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, step therapy, or is subject to high co-pays/coinsurance)
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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.