Methyldopa
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| Clinical data | |
|---|---|
| Trade names | Aldomet, Aldoril, Dopamet, others |
| Other names | L-α-Methyl-3,4-dihydroxyphenylalanine |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682242 |
| License data |
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| Pregnancy category |
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racemic) | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | approximately 50% |
| Metabolism | Liver |
| Onset of action | 4 to 6 hrs[1] |
| Elimination half-life | 105 minutes |
| Duration of action | 10 to 48 hrs[1] |
| Excretion | Kidney for metabolites |
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Methyldopa, sold under the brand name Aldomet among others, is a medication used for
Common side effects include sleepiness.
Methyldopa was discovered in 1960.[2] It is on the World Health Organization's List of Essential Medicines.[3]
Medical uses
Methyldopa is used in the
- Hypertension (or high blood pressure)
- Gestational hypertension (or pregnancy-induced hypertension) and pre-eclampsia.[4]
Side effects
Methyldopa is capable of inducing a number of adverse side effects, which range from mild to severe. Nevertheless, they are generally mild when the dose is less than 1 gram per day.[5] Side effects may include:
- Psychological
- Depression or even suicidal ideation, as well as nightmares
- Apathy or anhedonia, as well as dysphoria
- Anxiety, especially of the social anxiety variant
- Decreased alertness, awareness, and wakefulness
- Impaired attention, focus, and concentration
- Decreased desire, drive, and motivation
- lassitude
- sleepiness
- Agitation or restlessness
- Cognitive and memory impairment
- Derealization or depersonalization, as well as mild psychosis
- drive
- Physiological
- vertigo
- pupil constriction
- dry mouth
- Gastrointestinal disturbances such as diarrhea or constipation
- Headache or migraine
- joint pain, or paresthesia("pins and needles")
- Restless legs syndrome (RLS)
- rigidity, hypokinesia, or balance or postural instability
- Akathisia, ataxia, dyskinesia as well as even tardive dyskinesia, or dystonia
- Bell's palsy or facial paralysis
- Sexual dysfunction consisting of impaired erectile dysfunction or anorgasmia
- amenorrhoea or absence of menstrual cycles in females
- Bradycardia or decreased heart rate
- therapeutic benefit)
- postural hypotension)
- dysfunction or damage
- Pancreatitis or inflammation of the pancreas
- Warm autoimmune hemolytic anemia or deficiency in red blood cells(RBCs)
- Hypersensitivity such as lupus erythematosus, myocarditis, or pericarditis
- skin lesions or rashes
- Pallor
Rebound/withdrawal
Rebound hypertension via withdrawal on account of tolerance upon the abrupt discontinuation of methyldopa has been reported.[6]
Mechanism of action
The mechanism of action of methyldopa is not fully clear. Although it is a
The S-enantiomer of methyldopa is a competitive inhibitor of the
Pharmacokinetics
Maximum decrease in blood pressure occurs 4-6 hours after oral dosage. The half-life of methyldopa is 105 minutes..
History
When methyldopa was first introduced, it was the mainstay of antihypertensive
See also
- Difluoromethyldopa
- D-DOPA (dextrodopa)
- L-DOPA (levodopa; trade names Sinemet, Pharmacopa, Atamet, Stalevo, Madopar, Prolopa, etc.)
- L-DOPS (droxidopa)
- Dopamine (Intropan, Inovan, Revivan, Rivimine, Dopastat, Dynatra, etc.)
- Norepinephrine (noradrenaline; Levophed, etc.)
- Epinephrine(adrenaline; Adrenalin, EpiPed, Twinject, etc.)
References
- ^ a b c d e f g h i j k "Methyldopa". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
- ISBN 9789400926592. Archivedfrom the original on 2016-09-14.
- hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ISBN 978-0-323-42973-3.
- ISBN 978-0-85369-778-7.
- ^ Methyldopa (PIM 342) Archived 2008-03-13 at the Wayback Machine
- ^ "DailyMed - METHYLDOPA tablet, film coated". dailymed.nlm.nih.gov. Retrieved 2022-07-25.
- PMID 19821316.
External links
