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__NOTOC__ | __NOTOC__ | ||
{{ | {{Methyldopa}} | ||
{{CMG}}; {{AE | {{CMG}}; {{AE}} | ||
'''''For patient information about | '''''For patient information about Methyldopa, click [[Methyldopa (patient information)|here]].''''' | ||
{{SB}} | |||
Methylodopa<sup>®</sup> | |||
==Overview== | ==Overview== | ||
''' | '''Methyldopa''' or '''alpha-methyldopa''' (brand names '''Aldomet®''', '''Apo-Methyldopa®''', '''Dopamet®''', '''Novomedopa®''') is a centrally-acting adrenergic [[antihypertensive]] medication. Its use is now deprecated following introduction of alternative safer classes of agents. However it continues to have a role in otherwise difficult to treat hypertension and [[pregnancy-induced hypertension]]. | ||
==Category== | ==Category== | ||
Central adrengeric antihypertensives. | |||
==FDA Package Insert== | ==FDA Package Insert== | ||
==== | ====Methyldopa tablet<sup>®</sup>==== | ||
''' [[ | |||
'''| [[ | |||
'''| [[ | ''' [[Methyldopa tablet indications and usage|Indications and Usage]]''' | ||
'''| [[ | '''| [[Methyldopa tablet dosage and administration|Dosage and Administration]]''' | ||
'''| [[ | '''| [[Methyldopa tablet dosage forms and strengths|Dosage Forms and Strengths]]''' | ||
'''| [[ | '''| [[Methyldopa tablet contraindications|Contraindications]]''' | ||
'''| [[ | '''| [[Methyldopa tablet warnings |Warnings ]]''' | ||
'''| [[ | '''| [[Methyldopa tablet precautions| Precautions]]''' | ||
'''| [[ | '''| [[Methyldopa tablet adverse reactions|Adverse Reactions]]''' | ||
'''| [[ | '''| [[Methyldopa tablet drug interactions|Drug Interactions]]''' | ||
'''| [[ | '''| [[Methyldopa tablet use in specific populations|Use in Specific Populations]]''' | ||
'''| [[ | '''| [[Methyldopa tablet overdosage|Overdosage]]''' | ||
'''| [[ | '''| [[Methyldopa tablet description|Description]]''' | ||
'''| [[ | '''| [[Methyldopa tablet clinical pharmacology|Clinical Pharmacology]]''' | ||
'''| [[ | '''| [[Methyldopa tablet nonclinical toxicology|Nonclinical Toxicology]]''' | ||
'''| [[Methyldopa tablet clinical studies|Clinical Studies]]''' | |||
'''| [[Methyldopa tablet how supplied storage and handling|How Supplied/Storage and Handling]]''' | |||
'''| [[Methyldopa tablet patient counseling information|Patient Counseling Information]]''' | |||
'''| [[Methyldopa tablet labels and packages|Labels and Packages]]''' | |||
====Methyldopa injection<sup>®</sup>==== | |||
''' [[Methyldopa injection indications and usage|Indications and Usage]]''' | |||
'''| [[Methyldopa injection dosage and administration|Dosage and Administration]]''' | |||
'''| [[Methyldopa injection dosage forms and strengths|Dosage Forms and Strengths]]''' | |||
'''| [[Methyldopa injection contraindications|Contraindications]]''' | |||
'''| [[Methyldopa injection warnings| Warnings]]''' | |||
'''| [[Methyldopa injection precautions|Precautions]]''' | |||
'''| [[Methyldopa injection adverse reactions|Adverse Reactions]]''' | |||
'''| [[Methyldopa injection drug interactions|Drug Interactions]]''' | |||
'''| [[Methyldopa injection use in specific populations|Use in Specific Populations]]''' | |||
'''| [[Methyldopa injection overdosage|Overdosage]]''' | |||
'''| [[Methyldopa injection description|Description]]''' | |||
'''| [[Methyldopa injection clinical pharmacology|Clinical Pharmacology]]''' | |||
'''| [[Methyldopa injection nonclinical toxicology|Nonclinical Toxicology]]''' | |||
'''| [[Methyldopa injection clinical studies|Clinical Studies]]''' | |||
'''| [[Methyldopa injection how supplied storage and handling|How Supplied/Storage and Handling]]''' | |||
'''| [[Methyldopa injection patient counseling information|Patient Counseling Information]]''' | |||
'''| [[Methyldopa injection labels and packages|Labels and Packages]]''' | |||
==Mechanism of action== | |||
Methyldopa has variable absorption from the gut of approximately 50%. It is metabolized in the [[intestine]]s and [[liver]]; its metabolite alpha-methylnorepineprine acts in the [[brain]] to stimulate [[alpha-adrenergic receptor]]s decreasing [[total peripheral resistance]]. It is [[excretion|excreted]] in [[urine]]. | |||
Methyldopa, in its active metabolite form, leads to increased alpha-2 receptor-mediated inhibition of SNS (centrally and peripherally), allowing PSNS tone to increase. Such activity leads to a decrease in total peripheral resistance (TPR) and [[cardiac output]]. | |||
== | If methyldopa is abruptly withdrawn, rebound hypertension happens. This results because the long term use of methyldopa lowers the sensitivity of presynaptic alpha 2 receptors: the release of [[norepinephrine]] (NE) from sympathetic nerve endings is modulated by NE itself acting on the presynaptic alpha 2 autoreceptors thus inhibiting its own release. The discontinuation of methyldopa removes the inhibition on NE release leading to excessive NE release from the SNS and the rebound hypertension.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = METHYLDOPA TABLET [CARDINAL HEALTH] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=d87d63fd-48f7-4130-af03-5e263c338fe4 | publisher = | date = | accessdate = 10 March 2014 }}</ref> | ||
==References== | ==References== | ||
{{Reflist|2}} | {{Reflist|2}} | ||
[[Category:Cardiovascular Drugs]] | [[Category:Cardiovascular Drugs]] | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
Revision as of 18:45, 15 July 2014
| Methyldopa |
|---|
| Methyldopa tablet® FDA Package Insert |
| Indications and Usage |
| Dosage and Administration |
| Contraindications |
| Warnings |
| Precautions |
| Adverse Reactions |
| Drug Interactions |
| Use in Specific Populations |
| Overdosage |
| Description |
| Clinical Pharmacology |
| Nonclinical Toxicology |
| How Supplied/Storage and Handling |
| Labels and Packages |
| Methyldopa injection® FDA Package Insert |
| Indications and Usage |
| Dosage and Administration |
| Contraindications |
| Warnings |
| Precautions |
| Adverse Reactions |
| Drug Interactions |
| Use in Specific Populations |
| Overdosage |
| Description |
| Clinical Pharmacology |
| Nonclinical Toxicology |
| How Supplied/Storage and Handling |
| Labels and Packages |
| Clinical Trials on Methyldopa |
| ClinicalTrials.gov |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief:
For patient information about Methyldopa, click here.
Synonyms / Brand Names: Methylodopa®
Overview
Methyldopa or alpha-methyldopa (brand names Aldomet®, Apo-Methyldopa®, Dopamet®, Novomedopa®) is a centrally-acting adrenergic antihypertensive medication. Its use is now deprecated following introduction of alternative safer classes of agents. However it continues to have a role in otherwise difficult to treat hypertension and pregnancy-induced hypertension.
Category
Central adrengeric antihypertensives.
FDA Package Insert
Methyldopa tablet®
Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings | Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages
Methyldopa injection®
Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings | Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages
Mechanism of action
Methyldopa has variable absorption from the gut of approximately 50%. It is metabolized in the intestines and liver; its metabolite alpha-methylnorepineprine acts in the brain to stimulate alpha-adrenergic receptors decreasing total peripheral resistance. It is excreted in urine.
Methyldopa, in its active metabolite form, leads to increased alpha-2 receptor-mediated inhibition of SNS (centrally and peripherally), allowing PSNS tone to increase. Such activity leads to a decrease in total peripheral resistance (TPR) and cardiac output.
If methyldopa is abruptly withdrawn, rebound hypertension happens. This results because the long term use of methyldopa lowers the sensitivity of presynaptic alpha 2 receptors: the release of norepinephrine (NE) from sympathetic nerve endings is modulated by NE itself acting on the presynaptic alpha 2 autoreceptors thus inhibiting its own release. The discontinuation of methyldopa removes the inhibition on NE release leading to excessive NE release from the SNS and the rebound hypertension.[1]
References
- ↑ "METHYLDOPA TABLET [CARDINAL HEALTH]". Retrieved 10 March 2014.