Northera 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
Vasopressor; Sympathomimetic
Pharmacologic Class
Synthetic amino acid precursor of norepinephrine
Pregnancy Category
C
FDA Approved
Feb 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Northera 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 helping your body make more of a natural chemical called norepinephrine, which helps to raise your blood pressure and reduce 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 closely.
Take your medication as directed, swallowing the tablets whole without chewing, opening, or crushing them.
You can take your medication with or without food, but it's essential to take it the same way each time. Choose to take it either always with food or always on an empty stomach to maintain consistency.
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
To ensure the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms and areas prone to moisture.
* Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion or exposure.
What to Do If You Miss a Dose
If you miss a dose, skip it and resume 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 closely.
Take your medication as directed, swallowing the tablets whole without chewing, opening, or crushing them.
You can take your medication with or without food, but it's essential to take it the same way each time. Choose to take it either always with food or always on an empty stomach to maintain consistency.
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
To ensure the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms and areas prone to moisture.
* Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion or exposure.
What to Do If You Miss a Dose
If you miss a dose, skip it and resume 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 body position (e.g., standing up too quickly).
- Elevate the head of your bed while sleeping to reduce the risk of high blood pressure when lying down (supine hypertension).
- Stay well-hydrated unless otherwise advised by your doctor.
- Avoid overheating, as this can worsen orthostatic hypotension.
- Wear compression stockings if recommended by your doctor.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
100 mg three times daily (morning, midday, late afternoon/evening, at least 3 hours prior to bedtime)
Dose Range:
100 - 600 mg
Condition-Specific Dosing:
initialDose:
100 mg three times daily
titration:
Increase by 100 mg three times daily every 1-2 days, up to a maximum of 600 mg three times daily (1800 mg/day)
supineHypertension:
Reduce dose or discontinue if supine hypertension is unmanageable
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:
No specific dose adjustment recommended; Droxidopa is not dialyzable
Hepatic Impairment:
Mild:
No specific dose adjustment recommended
Moderate:
No specific dose adjustment recommended
Severe:
No specific dose adjustment recommended
Pharmacology
Mechanism of Action
Droxidopa is a synthetic amino acid precursor of norepinephrine. It is converted to norepinephrine by the enzyme DOPA decarboxylase, which is widely distributed throughout the body. Norepinephrine acts on alpha-1 adrenergic receptors to cause vasoconstriction and increase blood pressure, thereby alleviating symptoms of neurogenic orthostatic hypotension (NOH). It also acts on alpha-2, beta-1, and beta-2 adrenergic receptors.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (oral absorption is rapid and extensive)
Tmax:
Approximately 1.7 hours (for droxidopa); 3 hours (for active metabolite norepinephrine)
FoodEffect:
High-fat meal delays Tmax by approximately 2 hours and reduces Cmax by approximately 30% for droxidopa, but has no significant effect on norepinephrine exposure (AUC).
Distribution:
Vd:
Approximately 40 L (for droxidopa)
ProteinBinding:
Approximately 90% (primarily to albumin)
CnssPenetration:
Limited (Droxidopa itself has limited penetration, but its conversion to norepinephrine occurs both peripherally and centrally)
Elimination:
HalfLife:
Approximately 2-3 hours (for droxidopa); 3 hours (for norepinephrine)
Clearance:
Not available
ExcretionRoute:
Primarily renal (as metabolites)
Unchanged:
Less than 1% (of droxidopa)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Approximately 3 hours (for effect on standing blood pressure)
DurationOfAction:
Approximately 3-5 hours
Safety & Warnings
BLACK BOX WARNING
Northera can increase supine blood pressure. Patients should be advised to sleep with the head of the bed elevated. Supine blood pressure should be monitored prior to and during treatment and more frequently when increasing dose. If supine systolic blood pressure increases to 180 mmHg or greater, or supine diastolic blood pressure increases to 110 mmHg or greater, the dose should be reduced or Northera discontinued.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when 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 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 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. Many people experience no side effects or only mild ones. If you notice 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.
While rare, some people may experience severe and potentially life-threatening side effects when 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 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 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. Many people experience no side effects or only mild ones. If you notice 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
- Numbness or tingling
- Any signs of very high blood pressure when 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 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 medications and health conditions.
Remember, do not start, stop, or change the dosage 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 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 medications and health conditions.
Remember, do not start, stop, or change the dosage 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 directed 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.
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.
Regularly monitor your blood pressure as directed 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.
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:
- Excessive increase in blood pressure (hypertensive crisis)
- Headache
- Palpitations
- Bradycardia (slow heart rate)
- Reflex tachycardia (fast heart rate)
- Chest pain
- Nausea
- Vomiting
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222.
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/norepinephrine.
- Other Sympathomimetic Agents (e.g., pseudoephedrine, phenylephrine, ephedrine): Concomitant use may result in additive pressor effects and increased risk of supine hypertension.
- Beta-adrenergic Blockers: May antagonize the beta-adrenergic effects of norepinephrine, potentially leading to unopposed alpha-adrenergic effects and severe hypertension.
Moderate Interactions
- Alpha-adrenergic Blockers (e.g., prazosin, tamsulosin): May reduce the pressor effect of droxidopa.
- DOPA Decarboxylase Inhibitors (e.g., carbidopa, benserazide): May reduce the conversion of droxidopa to norepinephrine, potentially decreasing efficacy. (Note: Carbidopa is sometimes used to reduce peripheral conversion and increase central norepinephrine, but this is off-label and complex).
Confidence Interactions
Monitoring
Baseline Monitoring
Supine and Standing Blood Pressure
Rationale: To establish baseline and assess severity of orthostatic hypotension, and to identify risk of supine hypertension.
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
Routine Monitoring
Supine Blood Pressure
Frequency: Regularly, especially before the morning dose and before the last dose of the day (at least 3 hours prior to bedtime)
Target: <180/110 mmHg (general guideline, individualize based on patient risk factors)
Action Threshold: If supine systolic BP >180 mmHg or diastolic BP >110 mmHg, consider dose reduction or discontinuation.
Standing Blood Pressure
Frequency: Regularly, especially during dose titration and periodically thereafter
Target: Individualized to improve orthostatic symptoms without causing excessive supine hypertension
Action Threshold: If orthostatic symptoms persist despite adequate standing BP, consider dose increase (within limits).
Heart Rate
Frequency: Regularly, especially during dose titration
Target: Normal limits for patient
Action Threshold: Significant changes (e.g., sustained tachycardia or bradycardia) warrant investigation.
Symptoms of Orthostatic Hypotension
Frequency: Ongoing
Target: Reduction or resolution of dizziness, lightheadedness, syncope
Action Threshold: Persistent or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fainting/Syncope
- Blurred vision
- Fatigue
- Headache (especially new or worsening)
- Palpitations
- Chest pain
- Nausea
- Sweating
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies show adverse effects at doses higher than human therapeutic doses. There are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for adverse effects based on animal data, but human data is lacking.
Second Trimester:
Potential for adverse effects based on animal data, but human data is lacking.
Third Trimester:
Potential for adverse effects based on animal data, but human data is lacking. Consider 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:
Risk unknown; potential for serious adverse reactions in breastfed infants due to norepinephrine activity.
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. Elderly patients may be more susceptible to supine hypertension; monitor blood pressure closely.
Clinical Information
Clinical Pearls
- Droxidopa is a prodrug that requires conversion to norepinephrine; its efficacy can be affected by DOPA decarboxylase inhibitors (e.g., carbidopa).
- The most significant adverse effect is supine hypertension, which is addressed by a Black Box Warning. Patients must be instructed to elevate the head of their bed while sleeping.
- Dosing should be individualized and titrated slowly to balance symptomatic improvement with the risk of supine hypertension.
- The last dose of the day should be taken at least 3 hours prior to bedtime to minimize the risk of nocturnal supine hypertension.
- Monitor supine and standing blood pressure regularly, especially during dose titration.
Alternative Therapies
- Midodrine (another alpha-1 adrenergic agonist)
- Fludrocortisone (mineralocorticoid, increases blood volume)
- Pyridostigmine (cholinesterase inhibitor, may improve autonomic function)
- Non-pharmacological measures (e.g., increased fluid and salt intake, compression stockings, physical counter-maneuvers, small frequent meals, avoiding large carbohydrate meals, avoiding prolonged standing, avoiding overheating).
Cost & Coverage
Average Cost:
$1500 - $3000+ per 90 capsules (1 month supply)
Insurance Coverage:
Specialty Tier / Tier 4-5 (requires prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this 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 seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.