droxidopa (Rx)

Brand and Other Names:Northera
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg
  • 200mg
  • 300mg
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Neurogenic Orthostatic Hypotension

Indicated for symptomatic neurogenic orthostatic hypotension (NOH) in patients with primary autonomic failure (Parkinson’s disease, multiple system atrophy, and pure autonomic failure), dopamine beta-hydroxylase deficiency, and nondiabetic autonomic neuropathy

100 mg PO TID initially

Titrate to symptomatic response, in increments of 100 mg TID every 24-48 hr; not to exceed 600 mg TID (ie, 1800 mg/day)

Dosage Modifications

Renal impairment

  • Mild-to-moderate (GFR >30 mL/min): No dosage adjustment required
  • Severe (GFR <30 mL/min): Limited data; caution advised

Dosing Considerations

Effectiveness beyond 2 weeks of treatment has not been demonstrated

Continued effectiveness of droxidopa should be assessed periodically

Safety and efficacy not established

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Interactions

Interaction Checker

and droxidopa

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            8-10 week administration

            • Headache (13.2%)

            1-10%

            1-2 week administration

            • Headache (6.1%)
            • Dizziness (3.8%)
            • Nausea (1.5%)
            • Hypertension (1.5%)

            8-10 week administration

            • Dizziness (9.6%)
            • Nausea (8.8%)
            • Hypertension (7%)

            Postmarketing Reports

            Hypersensitivity

            Gastrointestinal Disorders: Pancreatitis, abdominal pain, vomiting, diarrhea

            General Disorders and Administration Site Conditions: Fatigue

            Psychiatric Disorders: Psychosis, hallucination, delirium, agitation, memory disorder

            Eye disorders: Blurred vision

            Nervous system disorders: Cerebrovascular accident

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            Warnings

            Black Box Warnings

            Supine hypertension

            • Monitor supine blood pressure prior to and during treatment and more frequently when increasing doses
            • Elevating the head of the bed lessens the risk of supine hypertension, and blood pressure should be measured in this position
            • If supine hypertension cannot be managed by elevation of the head of the bed, reduce dose or discontinue droxidopa

            Contraindications

            Known hypersensitivity to the drug or ingredients

            Cautions

            May cause or exacerbate supine hypertension in patients with NOH; advise patients to elevate the head of the bed when resting or sleeping (see Black Box Warnings); if supine hypertension is not well-managed, therapy may increase risk of cardiovascular events, particularly stroke

            Hypersensitivity reactions including anaphylaxis, angioedema, bronchospasm, urticaria, and rash (see Contraindications); if hypersensitivity reaction occurs, discontinue drug and initiate appropriate therapy

            Sympathomimetic effect may exacerbate existing ischemic heart disease, arrhythmias, and congestive heart failure

            Coadministration with other drugs that increase blood pressure are expected to increase risk of hypertension

            Coadministration with dopa-decarboxylase inhibitors may decrease the conversion of droxidopa to norepinephrine

            Contains FD+C Yellow No. 5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible persons; although overall incidence of this sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity

            Hyperpyrexia and confusion

            • Symptom complex resembling neuroleptic malignant syndrome (NMS) reported; monitor closely when dosage is changed or when concomitant levodopa is reduced abruptly or discontinued, especially if the patient is receiving neuroleptics
            • NMS is an uncommon, but life-threatening syndrome characterized by fever or hyperthermia, muscle rigidity, involuntary movements, altered consciousness, and mental status changes
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            Pregnancy & Lactation

            Pregnancy: There are no available data on use of dorxidopa in pregnant women and risk of major birth defects or miscarriage

            Lactation: There is no information regarding presence of drug or its active metabolite(s) in human milk, effects on breastfed child, nor effects on milk production/excretion; because of potential for serious adverse reactions, including reduced weight gain in breastfed infants, advise a woman not to breastfeed during treatment

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Norepinephrine precursor; directly metabolized to norepinephrine by dopa-decarboxylase which is extensively distributed throughout the body

            Peak droxidopa plasma concentrations are associated with increases in systolic and diastolic blood pressures

            Droxidopa has no clinically significant effect on standing or supine heart rates in patients with autonomic failure

            Absorption

            Peak plasma concentration: 1-4 hr

            High-fat meals have a moderate impact on droxidopa exposure (decreased Cmax and AUC by ~35% and 20% respectively); Cmax delayed by ~2 hr

            Distribution

            Can cross the BBB

            Protein bound: 75% (100 ng/mL); 26% (10,000 ng/mL)

            Vd: 200 L

            Metabolism

            The metabolism of droxidopa is mediated by catecholamine pathway and not through the cytochrome P450 system

            Initially converted to methoxylated dihydroxyphenylserine (3-OM-DOPS), a major metabolite, by catechol-O-methyltransferase (COMT), to norepinephrine by DOPA decarboxylase (DDC), or to protocatechualdehyde by DOPS aldolase

            After oral dosing in humans, plasma norepinephrine levels peak within 3-4 hr but are generally very low (<1 ng/mL) and variable with no consistent relationship with dose

            The contribution of droxidopa metabolites (other than norepinephrine) to its pharmacological effects is not well understood

            Elimination

            Half-life: 2.5 hr

            Excretion: 75% urine

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            Administration

            Oral Administration

            Administer upon arising in the morning, at midday, and in the late afternoon at least 3 hr prior to bedtime (to reduce the potential for supine hypertension during sleep)

            Administer consistently, either with food or without food

            Swallow capsule whole; do not chew, open, or dissolve contents

            Monitor supine blood pressure prior to initiating and after increasing the dose

            Patients who miss a dose should take their next scheduled dose; do not double the dose to make up for a missed dose

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.