‫‪Metabolism of methyldopa‬‬

‫‪Inside human body‬‬

‫‪By:‬‬
‫محمد حميد‬ ‫االء محمد‬
‫محمد باقر‬ ‫احمد ماهر‬
‫محمد مرتضى‬ ‫ايمان ناظم‬
‫محمد عماد‬ ‫اسراء جبار‬
‫محمد حسن‬ ‫مؤمل عبد الكريم‬
‫علي حسين ذياب‬
Methyldopa : sold under the brand name (Aldomet) among others,
is a medication used for high blood pressure.It is one of the preferred
treatments for high blood pressure in pregnancy. It can be given by mouth
or injection into a vein
Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication.It
works by stimulating the brain to decrease the activity of the sympathetic
nervous system
Methyldopa is a white to yellowish white, odorless fine powder and is sparingly
soluble in water

Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication.

It works by stimulating the brain to decrease the activity of the sympathetic
nervous system
Methyldopa is used in the clinical treatment of the following disorders:
• Hypertension (or high blood pressure) Methyldopa lowers blood pressure by
decreasing the levels of certain chemicals in your blood. This allows your blood
vessels to relax (widen). Methyldopa is used to treat high blood pressure
• Gestational hypertension (or pregnancy-induced hypertension) and pre-
eclampsia
1-drowsiness 2-headache 3-lightheadedness
-fainting. -dizziness -lack of energy

Therapeutic dose : Adult: oral dose 250mg for two

or three times daily for first 48 hours/ Children :
suggest 10mg/kg daily in two divided doses
Methyldopa exhibits variable absorption from the gastrointestinal tract. It is
metabolized in the liver and intestines and is excreted in urine.
The maximum decrease in blood pressure occurs four to six hours after oral
dosage. Once an effective dosage level is attained, a smooth blood pressure
response occurs in most patients in 12 to 24 hours. After withdrawal, blood
pressure usually returns to pretreatment levels within 24 to 48 hours.
Methyldopa is extensively metabolized. The known urinary metabolites are:
α-methyldopa mono-O-3-0-methyl-αmethyldopa; 3,4-
dihydroxyphenylacetone; α-methyldopamine; 3-0-methyl-α-
methyldopamine and their conjugates. Metabolism of Methyldopa is partly
conjugated, mainly to the methyldopa-O- sulphate. The major metabolite
probably contributes little to the therapeutic effect except in patients with
renal failure.Metabolized extensively in the liver and intestinal cells

 Methyldopa crosses the placental barrier, appears in cord blood, and

appears in breast milk.
Mechanism of action
The mechanism of action of methyldopa is not fully clear. Although it is a
centrally acting sympathomimetic, it does not block reuptake or
transporters. It may reduce the dopaminergic and serotonergic transmission
in the peripheral nervous system and it indirectly affects norepinephrine
(noradrenaline) synthesis. The S-enantiomer of methyldopa is a competitive
inhibitor of the enzyme aromatic L-amino acid decarboxylase (LAAD),
which converts L-DOPA into dopamine. L-DOPA can cross the blood brain
barrier and thus methyldopa may have similar effects. LAAD converts it
into alpha-methyldopamine, a false prescursor to norepinephrine, which in
turn reduces synthesis of norepinephrine in the vesicles. Dopamine beta
hydroxylase (DBH) converts alpha-methyldopamine into
alphamethylnorepinephrine, which is an agonist of the presynaptic α2-
adrenergic receptor causing inhibition of neurotransmitter release.

Some products that may interact with this drug

include:
1- iron products (such as ferrous sulfate, ferrous
gluconate), lithium.
2- Taking MAO inhibitors with this medication may
cause a serious (possibly fatal) drug interaction. Avoid
taking MAO inhibitors (isocarboxazid, linezolid,
methylene blue, moclobemide, phenelzine,
procarbazine, rasagiline, safinamide, selegiline,
tranylcypromine) during treatment with this
medication