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methyldopa (Rx)Brand and Other Names:Aldomet

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • 50mg/mL

tablet

  • 250mg
  • 500mg
more...

Hypertension

Initial: 250 mg PO q8-12hr for 2 days, increase q2Days PRN

Maintenance: 250-1000 mg/day divided q6-12hr PO, usually no more than 3 g/day

IV (methyldopate): 250-1000 mg infusion over 30-60 minutes q6-8hr PRN; no more than 4 g/day

Hypertensive Crisis

20-40 mg/kg/day divided IV q6hr  

No more than 65 mg/kg/day or 3 g/day (whichever is less)

Renal Impairment

Adjust dosage frequency with renal impairment

CrCl >50 mL/min: q8hr

CrCl 10-50 mL/min: q8-12hr

CrCl <10 mL/min: q12-24hr

Administration

May increase dose/give higher amount HS to avoid adverse events during waking hours

Dosage Forms & Strengths

injectable solution

  • 50mg/mL

tablet

  • 250mg
  • 500mg
more...

Hypertension

Neonate: 2.5-5 mg/kg PO or IV q8hr 

10 mg/kg/day divided q12hr PO, increase q2Days PRN

Hypertensive Crisis

20-40 mg/kg/day IV divided q6hr 

No more than 65 mg/kg/day or 3 g/day (whichever is less)

Administration

May increase dose/give higher amount HS to avoid adverse events during waking hours

Adverse CNS effects; may cause bradycardia and orthostatic hypotension; not recommended as routine treatment for hypertension (Beers criteria)

Not drug of choice in elderly because of CNS effects

Monitor renal function; renally excreted; decreased renal function more likely in elderly

Hypertension

Lower initial doses and more gradual adjustments recommended

125 mg qDay or q12hr; may increase by 125 mg-increments q2-3days PRN

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Interactions

Interaction Checker

methyldopa and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Angina

            Bradycardia

            Orthostatic hypotension

            Depression

            Dizziness

            Lethargy

            Sedation

            Rash

            Gynecomastia

            Impotence

            Dry mouth

            Nausea

            Vomiting

            Hemolytic anemia

            Thrombocytopenia

            Liver toxicity

            Arthralgia

            Autoimmune disease

            Lupus-like syndrome

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            Warnings

            Contraindications

            Active liver disease, liver disorders associated with previous methyldopa treatment

            Hypersensitivity to methyldopa or other ingredients (eg, sulfites)

            Pheochromocytoma

            Concomitant MAOIs

            Cautions

            CHF, dialysis patients (increased risk of hypertension following procedure), edema, hemolytic anemia, hypotension, severe bilateral CVD, history of liver disease

            Avoid abrupt withdrawal

            Risk of decreased libido and impotence in men

            May impair ability to perform hazardous tasks

            Tolerance develops on prolonged treatment, especially if no concurrent diuretic (methyldopa causes Na and water retention)

            Interferes with some lab tests

            IM/SC NOT recommended due to erratic absorption

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: distributed in breast milk but not in clinically significant amounts; compatible w/ breastfeeding

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Methyldopa may lower blood pressure by stimulating central inhibitory alpha-adrenergic receptors, false neurotransmission, and/or reduction of plasma renin activity.

            Pharmacokinetics

            Onset: PO 3-6 hr; IV 4-6 hr

            Duration: PO 12-24 hr; IV 10-16 hr

            Absorption: 50%

            Protein Bound: Minimal

            Vd: 0.6 L/kg

            Metabolism: Liver

            Metabolite: Methyldopa-o-sulfate (may be active), 3-methoxy-methyldopa (inactive)

            Excretion: Urine (70%), feces (30-50%)

            Dialyzable: Yes (HD; removes 60%; PD removes lesser amount)

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            Administration

            IV Incompatibilities

            Additive: ampho B, methohexital

            IV Compatibilities

            Solution: D5W, NS, Ringer's, D5/NS

            Additive: aminophylline, ascorbic acid, chloramphenicol, diphenhydramine, heparin, MgSO4, netilmicin, KCl, promazine, NaHCO3, succinylcholine, verapamil, vitamin B/C

            Y-site: esmolol, heparin, meperidine, morphine SO4, theophylline

            IV Preparation

            Dilute required dose in 100 mL D5W

            IV Administration

            Slow infusion over 30-60 min

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            Images

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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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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