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Drug overview for METHYLDOPATE HCL (methyldopate hcl):
Generic name: METHYLDOPATE HCL
Drug class: Central Adrenolytics
Therapeutic class: Cardiovascular Therapy Agents
Methyldopa is a centrally acting hypotensive agent.
No enhanced Uses information available for this drug.
Generic name: METHYLDOPATE HCL
Drug class: Central Adrenolytics
Therapeutic class: Cardiovascular Therapy Agents
Methyldopa is a centrally acting hypotensive agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
METHYLDOPATE 250 MG/5 ML VIAL
The following indications for METHYLDOPATE HCL (methyldopate hcl) have been approved by the FDA:
Indications:
Hypertension
Professional Synonyms:
Elevated blood pressure
Essential hypertension
Hyperpiesia
Hyperpiesis
Hypertensive disorder
Systemic arterial hypertension
Indications:
Hypertension
Professional Synonyms:
Elevated blood pressure
Essential hypertension
Hyperpiesia
Hyperpiesis
Hypertensive disorder
Systemic arterial hypertension
The following dosing information is available for METHYLDOPATE HCL (methyldopate hcl):
Dosage of methyldopa must be adjusted according to the patient's blood pressure response and tolerance. Adverse effects such as drowsiness may be minimized by starting dosage increases in the evening or by giving a larger dose at bedtime than in the morning. Geriatric patients may respond to smaller doses of methyldopa.
When parenteral drug therapy is indicated, the usual IV dosage of methyldopate hydrochloride in adults is 250-500 mg every 6 hours as required; the maximum dosage is 1 g every 6 hours.
The usual IV dosage of methyldopate hydrochloride in pediatric patients is 20-40 mg/kg per 24 hours, administered in equally divided doses at 6-hour intervals. The maximum IV dosage in children is 65 mg/kg daily or 3 g daily, whichever is less. When blood pressure is controlled, oral therapy should be substituted using the same dosage as the parenteral dosage.
Patients with impaired renal function may respond to smaller doses of methyldopa.
When parenteral drug therapy is indicated, the usual IV dosage of methyldopate hydrochloride in adults is 250-500 mg every 6 hours as required; the maximum dosage is 1 g every 6 hours.
The usual IV dosage of methyldopate hydrochloride in pediatric patients is 20-40 mg/kg per 24 hours, administered in equally divided doses at 6-hour intervals. The maximum IV dosage in children is 65 mg/kg daily or 3 g daily, whichever is less. When blood pressure is controlled, oral therapy should be substituted using the same dosage as the parenteral dosage.
Patients with impaired renal function may respond to smaller doses of methyldopa.
Methyldopa is administered orally; methyldopate hydrochloride is administered by IV infusion. IM or subcutaneous administration of methyldopate hydrochloride is not recommended because of unpredictable absorption. Methyldopate hydrochloride IV infusions are prepared by adding the required dose of the drug to 100 mL of 5% dextrose injection.
Alternatively, the required dose may be administered in 5% dextrose injection in a concentration of 100 mg/10 mL. The IV infusion should be administered slowly over a period of 30-60 minutes. ADD-Vantage(R) vials labeled as containing 50 mg/mL of methyldopate hydrochloride should be diluted and administered according to the manufacturer's directions. Vials containing solutions of methyldopate hydrochloride for injection and reconstituted solutions of the drug should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Alternatively, the required dose may be administered in 5% dextrose injection in a concentration of 100 mg/10 mL. The IV infusion should be administered slowly over a period of 30-60 minutes. ADD-Vantage(R) vials labeled as containing 50 mg/mL of methyldopate hydrochloride should be diluted and administered according to the manufacturer's directions. Vials containing solutions of methyldopate hydrochloride for injection and reconstituted solutions of the drug should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| METHYLDOPATE 250 MG/5 ML VIAL | Maintenance | Adults infuse 5 milliliters (250 mg) by intravenous route every 6 hours as needed |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| METHYLDOPATE 250 MG/5 ML VIAL | Maintenance | Adults infuse 5 milliliters (250 mg) by intravenous route every 6 hours as needed |
The following drug interaction information is available for METHYLDOPATE HCL (methyldopate hcl):
There are 1 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Methyldopa/MAOIs SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Monoamine oxidase inhibitors (MAOI's) may inhibit the antihypertensive effects of methyldopa.(1) CLINICAL EFFECTS: Concurrent use of MAOI's and methyldopa may result in hypertensive crisis(2) and/or hallucinations.(3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The Australian,(4) UK,(1) and US(5,6) manufacturers of methyldopa state that concurrent use of MAOI's is contraindicated. The US manufacturer of phenelzine states that concurrent use of methyldopa is contraindicated.(2) DISCUSSION: In a case report, a patient maintained on pargyline developed hallucinations following the increase of her methyldopa from 250 mg daily to 250 mg twice daily.(2) Methylene blue, when administered intravenously, has been shown to reach sufficient concentrations to be a potent inhibitor of MAO-A.(7,8) Metaxalone is a weak inhibitor of MAO.(9,10) |
AZILECT, EMSAM, FURAZOLIDONE, LINEZOLID, LINEZOLID-0.9% NACL, LINEZOLID-D5W, MARPLAN, MATULANE, METAXALONE, METHYLENE BLUE, NARDIL, PARNATE, PHENELZINE SULFATE, PROCARBAZINE HCL, PROVAYBLUE, RASAGILINE MESYLATE, SELEGILINE HCL, TRANYLCYPROMINE SULFATE, XADAGO, ZELAPAR, ZYVOX |
There are 1 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Methyldopa/Beta-Blockers (Nonselective) SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Unopposed alpha-adrenergic vasoconstriction produced by alpha-methylnorepinephrine in the presence of beta-blockade. CLINICAL EFFECTS: Severe hypertension. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Monitor blood pressure during concomitant administration of methyldopa and a nonselective beta-blocker. If hypertension occurs, treatment with phentolamine should be considered. DISCUSSION: Although methyldopa and propranolol have been used together to treat hypertension, severe increases in blood pressure, including death in one patient, has been reported during administration of these drugs. In addition, methyldopa alone has been reported to cause paradoxical hypertension. Additional studies are needed to define the specific population at risk. |
BETIMOL, BRIMONIDINE TARTRATE-TIMOLOL, CARVEDILOL, CARVEDILOL ER, COMBIGAN, COREG, COREG CR, CORGARD, COSOPT, COSOPT PF, DORZOLAMIDE-TIMOLOL, HEMANGEOL, INDERAL LA, INDERAL XL, INNOPRAN XL, ISTALOL, LABETALOL HCL, LABETALOL HCL-WATER, NADOLOL, PINDOLOL, PROPRANOLOL HCL, PROPRANOLOL HCL ER, PROPRANOLOL-HYDROCHLOROTHIAZID, TIMOLOL, TIMOLOL MALEATE, TIMOLOL-BIMATOPROST, TIMOLOL-BRIMONI-DORZOL-BIMATOP, TIMOLOL-BRIMONIDIN-DORZOLAMIDE, TIMOLOL-DORZOLAMIDE-BIMATOPRST, TIMOPTIC OCUDOSE |
There are 4 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Sympathomimetics (Direct, Mixed-Acting)/Methyldopa SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Unknown. CLINICAL EFFECTS: The pressor response to sympathomimetics may be increased. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Start with low doses of sympathomimetics and monitor blood pressure of patients during concurrent administration of sympathomimetics and methyldopa. DISCUSSION: The pressor response to sympathomimetics has been reported to be increased during methyldopa administration. In addition to increased duration of pressor response, severe hypertension has been reported. |
ADRENALIN, AKOVAZ, ARTICADENT DENTAL, ARTICAINE-EPINEPHRINE, ARTICAINE-EPINEPHRINE BIT, BIORPHEN, BROMFED DM, BROMPHENIRAMINE-PSEUDOEPHED-DM, BUFFERED LIDOCAINE-EPINEPHRINE, BUPIVACAINE HCL-EPINEPHRINE, BUPIVACAINE-DEXAMETH-EPINEPHRN, CITANEST FORTE DENTAL, CLARINEX-D 12 HOUR, DOBUTAMINE HCL, DOBUTAMINE HCL-D5W, DOPAMINE HCL, DOPAMINE HCL IN 5% DEXTROSE, DROXIDOPA, EMERPHED, EPHEDRINE HCL, EPHEDRINE SULFATE, EPHEDRINE SULFATE-0.9% NACL, EPHEDRINE SULFATE-NACL, EPINEPHRINE, EPINEPHRINE BITARTR-0.9% NACL, EPINEPHRINE BITARTRATE, EPINEPHRINE BITARTRATE-NACL, EPINEPHRINE CONVENIENCE KIT, EPINEPHRINE HCL-0.9% NACL, EPINEPHRINE HCL-D5W, EPINEPHRINE-0.9% NACL, EPINEPHRINE-D5W, EPINEPHRINE-NACL, IMMPHENTIV, ISOPROTERENOL HCL, ISOPROTERENOL HCL-0.9% NACL, ISUPREL, LEVOPHED, LIDOCAINE HCL-EPINEPHRINE, LIDOCAINE HCL-EPINEPHRINE-NACL, LIDOCAINE-EPINEPHRINE, LIGNOSPAN STANDARD, MARCAINE-EPINEPHRINE, MIDODRINE HCL, NOREPINEPHRINE BITAR-0.9% NACL, NOREPINEPHRINE BITARTRAT-WATER, NOREPINEPHRINE BITARTRATE, NOREPINEPHRINE BITARTRATE-D5W, NORTHERA, ORABLOC, PHENYLEPHRINE HCL, PHENYLEPHRINE HCL-0.9% NACL, PHENYLEPHRINE HCL-NACL, PHENYLEPHRINE HCL-WATER, PROMETHAZINE VC, PROMETHAZINE-PHENYLEPHRINE HCL, PSEUDOEPHEDRINE HCL, R.E.C.K.(ROPIV-EPI-CLON-KETOR), RACEPINEPHRINE HCL, RESPA A.R., REZIPRES, SENSORCAINE-EPINEPHRINE, SENSORCAINE-MPF EPINEPHRINE, SEPTOCAINE, VAZCULEP, VIVACAINE, XYLOCAINE DENTAL-EPINEPHRINE, XYLOCAINE WITH EPINEPHRINE, XYLOCAINE-MPF WITH EPINEPHRINE |
| Entacapone; Opicapone/COMT-Metabolized Agents SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Entacapone and opicapone are selective and reversible inhibitors of catechol-O-methyltransferase (COMT) and drugs that are metabolized by COMT can not be fully metabolized when given with entacapone or opicapone.(1) CLINICAL EFFECTS: COMT-metabolized agents can interact with entacapone or opicapone and may result in an increased heart rates, arrhythmias, or an excessive change in blood pressure.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturers of entacapone and opicapone recommend using caution when administering entacapone or opicapone and a COMT-metabolized agent regardless of the route of administration (including inhalation).(1-3) DISCUSSION: In an interaction study, ventricular tachycardia was observed after epinephrine and entacapone administration.(1) Another study on the effect of entacapone given with isoproterenol and epinephrine concluded that entacapone may potentiate the chronotropic and arrhythmogenic effects of isoproterenol and epinephrine.(4) |
CARBIDOPA-LEVODOPA-ENTACAPONE, ENTACAPONE, ONGENTYS |
| Tizanidine/Guanfacine; Methyldopa SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Tizanidine is an alpha-2 agonist. Concurrent use with antihypertensive agents may result in additive effects on blood pressure.(1) CLINICAL EFFECTS: Concurrent use of antihypertensives and tizanidine may result in hypotension.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients receiving concurrent therapy should be monitored for hypotension. The risk of hypotension may be decreased by careful titration of tizanidine dosages and monitoring for hypotension prior to dose advancement. Counsel patients about the risk of orthostatic hypotension.(1) DISCUSSION: Severe hypotension has been reported following the addition of tizanidine to existing lisinopril therapy.(2-4) |
TIZANIDINE HCL, ZANAFLEX |
| Apomorphine/Selected Antihypertensives and Vasodilators SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Apomorphine causes dose-dependent decreases in blood pressure. Concurrent use with antihypertensive agents may result in additive effects on blood pressure.(1) CLINICAL EFFECTS: Concurrent use of antihypertensives and apomorphine may result in orthostatic hypotension with or without dizziness, nausea, or syncope.(1) PREDISPOSING FACTORS: The risk of orthostatic hypotension may be increased during dose escalation of apomorphine and in patients with renal or hepatic impairment.(1) PATIENT MANAGEMENT: Patients receiving concurrent therapy should be monitored for hypotension. Counsel patients about the risk of orthostatic hypotension.(1) DISCUSSION: Healthy volunteers who took sublingual nitroglycerin (0.4 mg) concomitantly with apomorphine experienced a mean largest decrease in supine systolic blood pressure (SBP) of 9.7 mm Hg and in supine diastolic blood pressure (DBP) of 9.3 mm Hg, and a mean largest decrease in standing SBP and DBP of 14.3 mm Hg and 13.5 mm Hg, respectively. The maximum decrease in SBP and DBP was 65 mm Hg and 43 mm Hg, respectively. When apomorphine was taken alone, the mean largest decrease in supine SBP and DBP was 6.1 mm Hg and 7.3 mm Hg, respectively, and in standing SBP and DBP was 6.7 mm Hg and 8.4 mm Hg, respectively.(1) |
APOKYN, APOMORPHINE HCL, ONAPGO |
The following contraindication information is available for METHYLDOPATE HCL (methyldopate hcl):
Drug contraindication overview.
No enhanced Contraindications information available for this drug.
No enhanced Contraindications information available for this drug.
There are 3 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Hepatic cirrhosis |
| Pheochromocytoma |
| Severe hepatic disease |
There are 4 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Autoimmune hemolytic anemia |
| Depression |
| Hypotension |
| Porphyria |
There are 8 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Anemia |
| Angina |
| Chronic heart failure |
| Disease of liver |
| Edema |
| Kidney disease with reduction in glomerular filtration rate (GFr) |
| Parkinsonism |
| Severe cerebrovascular disease |
The following adverse reaction information is available for METHYLDOPATE HCL (methyldopate hcl):
Adverse reaction overview.
No enhanced Common Adverse Effects information available for this drug.
No enhanced Common Adverse Effects information available for this drug.
There are 14 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Peripheral edema |
Altered mental status Drug fever |
| Rare/Very Rare |
|---|
|
Acute pancreatitis Autoimmune hemolytic anemia Cholestasis Colitis Drug-induced hepatitis Granulocytopenic disorder Hepatocellular damage Leukopenia Myocarditis Systemic lupus erythematosus Thrombocytopenic disorder |
There are 14 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Drowsy Headache disorder Xerostomia |
Abnormal sexual function Diarrhea Erectile dysfunction Libido changes Nasal congestion Nausea Orthostatic hypotension |
| Rare/Very Rare |
|---|
|
Hyperprolactinemia Paresthesia Sinus bradycardia Vomiting |
The following precautions are available for METHYLDOPATE HCL (methyldopate hcl):
No enhanced Pediatric Use information available for this drug.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Reproduction studies in mice, rabbits, and rats using oral methyldopa in dosages of 1000, 200, and 100 mg/kg, respectively, have not revealed evidence of harm to the fetus. These dosages are 16.6, 3.3,
and 1.7 times, respectively, the maximum daily human dosage when compared on the basis of body weight and 1.4, 1.1,
and 0.2 times, respectively, the maximum daily human dosage when compared on the basis of body surface area. Methyldopa has been used for many years in the management of hypertension in pregnant women, and the drug is generally considered safe for mother and fetus when used in association with careful prenatal management.
Uteroplacental blood flow and fetal hemodynamics have been reported to be stable during therapy with the drug. Although no teratogenic effects have been reported, the possibility that methyldopa may cause fetal injury (e.g., secondary to reduced placental blood flow or fetotoxicity) cannot be excluded. In neonates born to women treated with methyldopa, systolic blood pressure may be decreased during the first 2-3 days after delivery; in some neonates, tremors have also been reported.
Studies to date, including a long-term follow-up study, of children born to women who received methyldopa during pregnancy have not revealed evidence of substantial adverse effects of the drug on the offspring; however, in the longest follow-up study, treatment with methyldopa was associated with a smaller head circumference (without an apparent effect on intelligence quotient) in male offspring of those women whose therapy was initiated between 16 and 20 weeks' gestation. At 4 years of age, the developmental delay commonly seen in children born to hypertensive mothers was less evident in those whose mothers received methyldopa during pregnancy than in those whose mothers were untreated. Children born to mothers receiving methyldopa scored consistently higher on indices of intellectual and motor development than children born to untreated hypertensive mothers; however, these differences were not apparent by 7.5
years of age. Methyldopa should be used during pregnancy only when clearly needed. In addition, excessive reduction in blood pressure should be avoided, and a conservative approach to treatment generally should be followed. (See Hypertension during Pregnancy under Uses: Hypertension.)
and 1.7 times, respectively, the maximum daily human dosage when compared on the basis of body weight and 1.4, 1.1,
and 0.2 times, respectively, the maximum daily human dosage when compared on the basis of body surface area. Methyldopa has been used for many years in the management of hypertension in pregnant women, and the drug is generally considered safe for mother and fetus when used in association with careful prenatal management.
Uteroplacental blood flow and fetal hemodynamics have been reported to be stable during therapy with the drug. Although no teratogenic effects have been reported, the possibility that methyldopa may cause fetal injury (e.g., secondary to reduced placental blood flow or fetotoxicity) cannot be excluded. In neonates born to women treated with methyldopa, systolic blood pressure may be decreased during the first 2-3 days after delivery; in some neonates, tremors have also been reported.
Studies to date, including a long-term follow-up study, of children born to women who received methyldopa during pregnancy have not revealed evidence of substantial adverse effects of the drug on the offspring; however, in the longest follow-up study, treatment with methyldopa was associated with a smaller head circumference (without an apparent effect on intelligence quotient) in male offspring of those women whose therapy was initiated between 16 and 20 weeks' gestation. At 4 years of age, the developmental delay commonly seen in children born to hypertensive mothers was less evident in those whose mothers received methyldopa during pregnancy than in those whose mothers were untreated. Children born to mothers receiving methyldopa scored consistently higher on indices of intellectual and motor development than children born to untreated hypertensive mothers; however, these differences were not apparent by 7.5
years of age. Methyldopa should be used during pregnancy only when clearly needed. In addition, excessive reduction in blood pressure should be avoided, and a conservative approach to treatment generally should be followed. (See Hypertension during Pregnancy under Uses: Hypertension.)
Since methyldopa is distributed into milk, the drug should be used with caution in nursing women; the possibility of adverse effects on a nursing infant cannot be excluded. The extent to which methyldopa distributes into milk has not been clearly established, but the amount of drug a nursing infant would ingest is believed to be too small to be clinically important; however, if a woman receiving methyldopa breastfeeds, the infant (particularly if preterm) should be monitored for potential systemic effects of the drug (e.g., decreased respiration, blood pressure, or alertness).
No enhanced Geriatric Use information available for this drug.
The following prioritized warning is available for METHYLDOPATE HCL (methyldopate hcl):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for METHYLDOPATE HCL (methyldopate hcl)'s list of indications:
| Hypertension | |
| I10 | Essential (primary) hypertension |
| I11 | Hypertensive heart disease |
| I11.0 | Hypertensive heart disease with heart failure |
| I11.9 | Hypertensive heart disease without heart failure |
| I12 | Hypertensive chronic kidney disease |
| I12.0 | Hypertensive chronic kidney disease with stage 5 chronic kidney disease or end stage renal disease |
| I12.9 | Hypertensive chronic kidney disease with stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13 | Hypertensive heart and chronic kidney disease |
| I13.0 | Hypertensive heart and chronic kidney disease with heart failure and stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13.1 | Hypertensive heart and chronic kidney disease without heart failure |
| I13.10 | Hypertensive heart and chronic kidney disease without heart failure, with stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13.11 | Hypertensive heart and chronic kidney disease without heart failure, with stage 5 chronic kidney disease, or end stage renal disease |
| I13.2 | Hypertensive heart and chronic kidney disease with heart failure and with stage 5 chronic kidney disease, or end stage renal disease |
| I15.1 | Hypertension secondary to other renal disorders |
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