Northera 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
Pharmacologic Class
Synthetic amino acid analog; prodrug
Pregnancy Category
Category C
FDA Approved
Feb 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Northera (droxidopa) is a medication used to treat very low blood pressure (orthostatic hypotension) that occurs when you stand up, especially in people with certain nerve conditions. It works by helping your body make a chemical called norepinephrine, which can 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.
When taking your medication:
- Swallow the tablet whole.
- Do not chew, open, or crush the tablet.
- You can take your medication with or without food, but it's essential to take it the same way each time. Choose to either always take it with food or always take it on an empty stomach.
- Make sure to take your last dose of the day at least 3 hours before bedtime. This helps reduce the risk of high blood pressure during sleep.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication:
- Store it at room temperature in a dry place.
- Avoid storing your medication in a bathroom.
- Keep all medications in a safe location.
- Ensure that all medications are 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.
- Do not take extra doses to make up for the missed dose.
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.
When taking your medication:
- Swallow the tablet whole.
- Do not chew, open, or crush the tablet.
- You can take your medication with or without food, but it's essential to take it the same way each time. Choose to either always take it with food or always take it on an empty stomach.
- Make sure to take your last dose of the day at least 3 hours before bedtime. This helps reduce the risk of high blood pressure during sleep.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication:
- Store it at room temperature in a dry place.
- Avoid storing your medication in a bathroom.
- Keep all medications in a safe location.
- Ensure that all medications are 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.
- Do not take extra doses to make up for the missed dose.
Lifestyle & Tips
- Take exactly as prescribed by your doctor.
- Do not take the last dose of the day within 3 hours of bedtime to reduce the risk of high blood pressure while lying down (supine hypertension).
- Elevate the head of your bed while sleeping to help prevent supine hypertension.
- Avoid sudden changes in position (e.g., standing up too quickly) even with medication.
- Stay well-hydrated unless otherwise advised by your doctor.
- Avoid alcohol, as it can worsen orthostatic hypotension.
- Inform your doctor about all other medications you are taking, including over-the-counter drugs and supplements.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 100 mg three times daily (TID), titrated up to 600 mg TID. Maximum daily dose is 1800 mg.
Dose Range:
100 - 600 mg
Condition-Specific Dosing:
neurogenic_orthostatic_hypotension:
Initial 100 mg TID, increasing by 100 mg TID increments every 1 to 2 days, based on supine blood pressure and symptom control. 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:
Use with caution; no specific dose adjustment guidelines available. Monitor closely for adverse effects.
Dialysis:
Not available; use with caution.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution; no specific dose adjustment guidelines available. Monitor closely for adverse effects.
Pharmacology
Mechanism of Action
Droxidopa is a synthetic amino acid analog that is converted to norepinephrine (noradrenaline) by the enzyme DOPA decarboxylase. Norepinephrine acts as an agonist at alpha-1 adrenergic receptors on blood vessels, causing vasoconstriction and increasing blood pressure. It also has effects on beta-adrenergic receptors.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly quantified, but well absorbed.
Tmax:
1.7 to 2.5 hours (for droxidopa); 3 to 7 hours (for norepinephrine metabolite)
FoodEffect:
A high-fat meal delays Tmax by approximately 2 hours and reduces Cmax by approximately 30% for droxidopa, but does not significantly affect the Cmax or AUC of norepinephrine.
Distribution:
Vd:
Not readily available
ProteinBinding:
<30%
CnssPenetration:
Limited
Elimination:
HalfLife:
2 to 3 hours (for droxidopa); 3 to 7 hours (for norepinephrine)
Clearance:
Not readily available
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
<1% (droxidopa)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Approximately 2-3 hours (for blood pressure increase)
DurationOfAction:
Approximately 3-5 hours
Safety & Warnings
BLACK BOX WARNING
Droxidopa can cause supine hypertension. Blood pressure should be monitored in the supine position prior to and during treatment and more frequently when increasing dose. Patients should be instructed to elevate the head of the bed and to avoid taking droxidopa within 3 hours of 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 immediate medical attention:
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
Most people experience no side effects or only mild ones. However, if you notice 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 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 immediate medical attention:
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
Most people experience no side effects or only mild ones. However, if you notice 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 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
- Pounding in the ears
- Shortness of breath
- Irregular heartbeat (palpitations)
- Nausea or vomiting
- Dizziness or lightheadedness (if worsening or not improving)
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 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 existing 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 symptoms 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 existing 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 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 benefits and risks associated with using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Excessive increase in blood pressure (hypertensive crisis)
- Headache
- Palpitations
- Bradycardia (reflex)
- Chest pain
- Blurred vision
- Nausea
- Vomiting
- Anxiety
- Tremor
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222. Treatment is supportive and symptomatic, focusing on managing blood pressure and cardiovascular effects.
Drug Interactions
Major Interactions
- Monoamine Oxidase Inhibitors (MAOIs) (e.g., phenelzine, selegiline, linezolid): May lead to hypertensive crisis due to inhibition of norepinephrine metabolism.
- Tricyclic Antidepressants (TCAs) (e.g., amitriptyline, imipramine): May potentiate the pressor effect of droxidopa by inhibiting norepinephrine reuptake.
- Other sympathomimetic agents (e.g., pseudoephedrine, phenylephrine, other alpha/beta agonists): Increased risk of supine hypertension and other cardiovascular adverse effects.
Moderate Interactions
- Beta-blockers (e.g., propranolol, metoprolol): May reduce the efficacy of droxidopa or lead to unopposed alpha-adrenergic effects.
- Antihypertensive agents: May have additive effects, requiring dose adjustment of antihypertensives.
- DOPA decarboxylase inhibitors (e.g., carbidopa, benserazide): May inhibit the conversion of droxidopa to norepinephrine, reducing its efficacy. Co-administration is generally not recommended unless specifically indicated for other conditions and monitored closely.
Minor Interactions
- Not typically listed in detail for minor interactions.
Monitoring
Baseline Monitoring
Supine and Standing Blood Pressure (BP)
Rationale: To establish baseline orthostatic hypotension severity and identify pre-existing supine hypertension.
Timing: Prior to initiation of therapy.
Heart Rate
Rationale: To assess baseline cardiovascular status.
Timing: Prior to initiation of therapy.
Symptoms of nOH
Rationale: To quantify baseline symptom severity and guide treatment goals.
Timing: Prior to initiation of therapy.
Routine Monitoring
Supine and Standing Blood Pressure (BP)
Frequency: Regularly, especially during dose titration (e.g., daily or every other day) and periodically thereafter (e.g., weekly to monthly).
Target: Standing SBP increase without excessive supine hypertension (e.g., supine SBP <180-200 mmHg).
Action Threshold: If supine SBP consistently >180-200 mmHg, consider dose reduction or discontinuation. If standing BP remains low, consider further titration.
Heart Rate
Frequency: During dose titration and periodically thereafter.
Target: Within normal limits or patient's baseline.
Action Threshold: Significant tachycardia or bradycardia may warrant investigation.
Symptoms of nOH (e.g., dizziness, lightheadedness, falls, syncope)
Frequency: Regularly during treatment.
Target: Improvement or resolution of symptoms.
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Symptoms of Supine Hypertension (e.g., headache, blurred vision, chest pain, palpitations)
Frequency: Regularly, especially after dose increases.
Target: Absence of symptoms.
Action Threshold: Presence of symptoms warrants immediate assessment of supine BP and potential dose reduction.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fainting (syncope)
- Falls
- Fatigue
- Headache (especially when lying down)
- Blurred vision (especially when lying down)
- Chest pain (especially when lying down)
- Palpitations
- Nausea
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies of droxidopa in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Risk unknown. Animal studies showed adverse effects at high doses.
Second Trimester:
Risk unknown. Animal studies showed adverse effects at high doses.
Third Trimester:
Risk unknown. Animal studies showed adverse effects at high doses. Potential for effects on fetal circulation due to adrenergic activity.
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 nursing 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 adverse effects on the infant due to adrenergic activity.
Pediatric Use
The safety and effectiveness of droxidopa 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. Elderly patients may be at increased risk for supine hypertension and should be monitored closely.
Clinical Information
Clinical Pearls
- Droxidopa is a prodrug that requires DOPA decarboxylase for activation; therefore, co-administration with DOPA decarboxylase inhibitors (e.g., carbidopa) may reduce its efficacy.
- The most significant adverse effect is supine hypertension. Emphasize the importance of taking the last dose at least 3 hours before bedtime and elevating the head of the bed.
- Blood pressure monitoring (both supine and standing) is crucial, especially during dose titration.
- Patients should be advised to report symptoms of supine hypertension (e.g., severe headache, blurred vision, chest pain) immediately.
- Titrate the dose slowly and individually based on patient response and tolerability, balancing symptomatic improvement with the risk of supine hypertension.
Alternative Therapies
- Midodrine (another alpha-1 adrenergic agonist)
- Fludrocortisone (mineralocorticoid)
- Pyridostigmine (cholinesterase inhibitor, off-label for nOH)
- Non-pharmacological interventions (e.g., increased fluid and salt intake, compression stockings, physical counter-maneuvers, small frequent meals, avoiding large carbohydrate meals, avoiding prolonged standing)
Cost & Coverage
Average Cost:
$1,500 - $3,000+ per 30 capsules (300mg)
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or deductibles)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about your medication, don't 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 reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.