Methyldopa

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Methyldopa , sold under the trademark Aldomet among others, is a drug used for high blood pressure. This is one of the preferred treatments for high blood pressure in pregnancy. For other types of high blood pressure including very high blood pressure resulting in other drug symptoms are usually preferred. Can be given by mouth or injection into blood vessels. The onset of the effect is about 5 hours and lasts about a day.

Common side effects include drowsiness. More severe side effects include damage to red blood cells, liver problems, and allergic reactions. Methyldopa is in the adrenergic alpha-2 drug-receptor agonist group. It works by stimulating the brain to reduce the activity of the sympathetic nervous system.

Methidopa was discovered in 1960. It is a List of Essential Medicines of the World Health Organization, the most effective and safe medicines needed in the health system. Wholesale costs in developing countries are around 4.31 to 9.48 USD per month. In the United States it costs less than 25 USD per month.

Video Methyldopa

Medical use

Methyldopa is used in clinical care of the following disorders:

• Hypertension (or high blood pressure)
• Gestational hypertension (or pregnancy induced hypertension) and pre-eclampsia

Maps Methyldopa

Side effects

Methyldopa is able to induce a number of adverse side effects, ranging from mild to severe. However, they are generally mild when the dose is less than 1 gram per day. Side effects may include:

• Psychological
  • Depression or even suicidal, and nightmare
  • Apathy or anhedonia, as well as dysphoria
  • Anxiety, especially social anxiety variants
  • Decreased alertness, awareness, and awareness
  • Distraction, focus, and concentration
  • Desire, drive, and declining motivation
  • Fatigue or lethargy or malaise or lethargy
  • Sedation or drowsiness or somnolence or sleepiness
  • Agitation or anxiety
  • Cognitive and memory impairments
  • Realized or depersonalized, as well as mild psychosis
  • Sexual dysfunction includes libido, desire, and encouragement disorders
• Physiological
  • Dizziness, dizziness, or vertigo
  • Miosis or pupil constriction
  • Xerostomia or dry mouth
  • Gastrointestinal disorders such as diarrhea or constipation
  • Headaches or migraines
  • Myalgia or muscle pain, arthralgia or joint pain, or paresthesia ("pin and needle")
  • Restless legs syndrome (RLS)
  • Parkinsonian symptoms such as muscle tremor, stiffness, hypokinesia, or postural instability or balance
  • Akathisia, ataxia, dyskinesia and tardive tardive, or dystonia
  • Bell palsy or facial paralysis
  • Sexual dysfunction consists of erectile dysfunction disorder or anorgasmia
  • Hyperprolactinemia or excess prolactin, gynecomastia/breast enlargement in males, or amenorrhea or absence of menstrual cycles in women
  • Bradycardia or decreased heart rate
  • Hypotension or decreased blood pressure (although this can also be considered a therapeutic benefit)
  • Orthostatic hypotension (also known as postural hypotension)
  • Hepatitis, hepatotoxicity, or liver dysfunction or damage
  • Pancreatitis or inflammation of the pancreas
  • A warm autoimmune hemolytic anemia or red blood cell deficiency (red blood cells)
  • Myelotoxicity or bone marrow suppression, potentially leading to thrombocytopenia or blood platelet deficiency or leukopenia or white blood cell deficiency (WBC)
  • Hypersensitivity such as lupus erythematosus, myocarditis, or pericarditis
  • Lichenoid reactions such as skin lesions or rashes
  • Pallor

Rebound/withdraw

Hypertension rebounded through withdrawal because of tolerance at sudden termination of methyldopa has been reported.

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Action mechanism

Methyldopa has a dual mechanism of action:

• This is a competitive inhibitor of the decarboxylase DOPA enzyme, also known as aromatic L -amino acid decarboxylase, which converts L -DOPA into dopamine. Dopamine is a precursor for norepinephrine (noradrenaline) and then epinephrine (adrenaline). This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. This effect can lower blood pressure and cause central nervous system effects such as depression, anxiety, apathy, anhedonia, and parkinsonism. In addition, decreased dopamine may reduce its inhibitory effect on prolactin leading to signs and symptoms of hyperprolactinemia.
• Converted to? -methylnorepinephrine by dopamine beta-hydroxylase (DBH). ? -methylnorepinephrine is a presynaptic central nervous system agonist? ₂ adrenergic receptors. Activation of these receptors in the brainstem seems to inhibit the output of the sympathetic nervous system and lower blood pressure. This is also the mechanism of action of clonidine.

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Pharmacokinetics

Methyldopa shows the absorption of variables from the gastrointestinal tract. It is metabolized in the liver and intestines and excreted in the urine.

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History

When methyldopa was first introduced, it was a mainstay of antihypertensive treatment, but its use has declined due to adverse side effects, with increasing use of other agents that are safer and more tolerable such as alpha blockers, beta blockers, and calcium channel blockers.. In addition, it has not been associated with a reduction in adverse cardiovascular events including myocardial infarction and stroke, or overall causes of mortality reduction in clinical trials. Nevertheless, one indication of methyldopa is currently still in the management of pregnancy induced hypertension (PIH), as it is relatively safe in pregnancy compared to other antihypertensives that can affect the fetus.

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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, Adrenaline, Epiped, Twinject, etc.)

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References

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External links

Source of the article : Wikipedia