Methyldopa

What is Methyldopa?

• Methyldopa (Aldomet) is an aromatic-amino-acid decarboxylase inhibitor used as an antihypertensive drug.

Methyldopa

What are the uses of this medicine?

• Methyldopa (Aldomet) is used for the treatment of Hypertension.

Methyldopa

How does this medicine work?

• Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man.
• The antihypertensive effect of methyldopa probably is due to its metabolism to alpha-methylnorepinephrine, which then lowers arterial pressure by stimulation of central inhibitory alpha-adrenergic receptors, false neurotransmission, and/or reduction of plasma renin activity.
• Methyldopa has been shown to cause a net reduction in the tissue concentration of serotonin, dopamine, norepinephrine, and epinephrine.

Methyldopa molecule ball

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with active hepatic disease, such as acute hepatitis and active cirrhosis.
• with liver disorders previously associated with methyldopa therapy.
• with hypersensitivity to any component of this product.
• on therapy with monoamine oxidase (MAO) inhibitors.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• monoamine oxidase (MAOs) inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate)
• haloperidol (Haldol), levodopa (in Sinemet, in Stalevo), lithium (Lithobid), other medications for high blood pressure, and tolbutamide
• iron supplements or vitamins containing iron

Is this medicine FDA approved?

• Methyldopa was discovered in 1960.
• It is on the World Health Organization's List of Essential Medicines.

How should this medicine be used?

Recommended dosage: Adults: Initiation of Therapy

• The usual starting dosage of methyldopa tablet is 250 mg two or three times a day in the first 48 hours.
• When methyldopa is given with anti-hypertensives other than thiazides, the initial dosage of methyldopa should be limited to 500 mg daily in divided doses; when methyldopa is added to a thiazide, the dosage of thiazide need not be changed.

Maintenance Therapy:

• The usual daily dosage of methyldopa is 500 mg to 2 g in two to four doses.
• Although occasional patients have responded to higher doses, the maximum recommended daily dosage is 3 g.

Pediatric patients:

• Initial dosage is based on 10 mg/kg of body weight daily in two to four doses.
• The daily dosage then is increased or decreased until an adequate response is achieved.
• The maximum dosage is 65 mg/kg or 3 g daily, whichever is less.

Administration:

• Methyldopa comes as a tablet and a liquid to take by mouth.
• It usually is taken two to four times a day.
• Shake the liquid well before each dose to mix the medication evenly.
• Use a dose-measuring spoon or cup to measure the correct amount of liquid for each dose, not a regular household spoon.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet and a liquid

This medicine is available in fallowing brand namesː

• Aldomet

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• diarrhea
• headache
• dizziness
• sedation
• dry mouth
• rash
• muscle weakness
• swollen ankles or feet
• upset stomach
• gas

Rare but potentially severe adverse effects include hemolytic anemia (Coombs positive), lupus-like syndrome, mycocarditis, pancreatitis and hepatotoxicity.

What special precautions should I follow?

• It is important to recognize that a positive Coombs test, hemolytic anemia, and liver disorders may occur with methyldopa therapy. If Coombs-positive hemolytic anemia occurs, the cause may be methyldopa and the drug should be discontinued.
• Before treatment is started, it is desirable to do a blood count (hematocrit, hemoglobin, or red cell count) for a baseline or to establish whether there is anemia. Periodic blood counts should be done during therapy to detect hemolytic anemia.
• Occasionally, fever has occurred within the first 3 weeks of methyldopa therapy, associated in some cases with eosinophilia or abnormalities in one or more liver function tests, such as serum alkaline phosphatase, serum transaminases (SGOT, SGPT), bilirubin and prothrombin time.
• Rarely, fatal hepatic necrosis has been reported after use of methyldopa. Periodic determinations of hepatic function should be done, particularly during the first 6 to 12 weeks of therapy or whenever an unexplained fever occurs.
• Rarely, a reversible reduction of the white blood cell count with a primary effect on the granulocytes has been seen.
• Methyldopa should be used with caution in patients with a history of previous liver disease or dysfunction.
• Some patients taking methyldopa experience clinical edema or weight gain which may be controlled by use of a diuretic. Methyldopa should not be continued if edema progresses or signs of heart failure appear.
• Blood count, Coombs tests and liver function tests are recommended before initiating therapy and at periodic intervals.
• Methyldopa appears in breast milk. Therefore, caution should be exercised when methyldopa is given to a nursing woman.
• Methyldopa has been clearly linked to instances of acute and chronic liver injury that can be severe and even fatal.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• acute hypotension
• excessive sedation
• weakness
• bradycardia
• dizziness
• light-headedness
• constipation
• distention
• flatus
• diarrhea
• nausea
• vomiting

Management of overdosage:

• In the event of overdosage, symptomatic and supportive measures should be employed.
• When ingestion is recent, gastric lavage or emesis may reduce absorption.
• When ingestion has been earlier, infusions may be helpful to promote urinary excretion.
• Otherwise, management includes special attention to cardiac rate and output, blood volume, electrolyte balance, paralytic ileus, urinary function and cerebral activity.
• Sympathomimetic drugs (e.g., levarterenol, epinephrine, metaraminol bitartrate) may be used.
• Methyldopa is dialyzable.

Can this medicine be used in pregnancy?

• Pregnancy Category B.
• There are, however, no adequate and well-controlled studies in pregnant women in the first trimester of pregnancy.

Can this medicine be used in children?

• There are no well-controlled clinical trials in pediatric patients.
• Information on dosing in pediatric patients is supported by evidence from published literature regarding the treatment of hypertension in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• METHYLDOPA

Inactive ingredients:

• CALCIUM SULFATE
• CITRIC ACID MONOHYDRATE
• SILICON DIOXIDE
• EDETATE DISODIUM
• ETHYLCELLULOSES
• HYPROMELLOSES
• MAGNESIUM STEARATE
• METHYLCELLULOSE
• POLYETHYLENE GLYCOL
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• TITANIUM DIOXIDE
• HYDROXYPROPYL CELLULOSE
• TALC

Who manufactures and distributes this medicine?

Manufactured In India By:

• EMCURE PHARMACEUTICALS LTD.
• Hinjwadi, Pune, India

Manufactured For:

• TEVA PHARMACEUTICALS USA
• Sellersville, PA

What should I know about storage and disposal of this medication?

• Store at 20° to 25° C (68° to 77° F).

• Dailymed label info on Methyldopa
• FDA Methyldopa

Methyldopa Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Antihypertensive agents

• Dailymed label info on Methyldopa
• FDA Methyldopa

Methyldopa Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Methyldopa Resources
Latest articles Most recent articles Ongoing trials	Wikipedia