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Product Name
:
HYPOJIT
Chemical Name
:
Methyldopa
Therapeutic Category
:
Cardiovascular drugs
Pharmacologic Category
:
Alpha2-Adrenergic Agonist
Pharmaceutical Form
:
Tablets
Composition
:
Methyldopa 125mg / 250mg
Monitoring Parameters
Dosing
 
Dosing: Adult
Hypertension:
Oral: Initial: 250 mg 2-3 times/day; increase every 2 days as needed (maximum dose: 3 g/day); usual dose range (JNC 7): 250-1000 mg/day in 2 divided doses

Dosing: Pediatric

Hypertension:
Oral: Initial: 10 mg/kg/day in 2-4 divided doses; increase every 2 days as needed to maximum dose of 65 mg/kg/day. Do not exceed 3 g/day.

Dosing: Geriatric

Refer to adult dosing. Initiate at the lower end of the dosage range.

Dosing: Renal Impairment

Clcr >50 mL/minute: Administer every 8 hours.
Clcr 10-50 mL/minute: Administer every 8-12 hours.
Clcr <10 mL/minute: Administer every 12-24 hours.
Slightly dialyzable (5% to 20%)
Use
 
Management of moderate-to-severe hypertension
Adverse Reactions
 
>10%: Cardiovascular: Peripheral edema
1% to 10%:
Central nervous system: Drug fever, mental depression, anxiety, nightmares, drowsiness, headache
Gastrointestinal: Dry mouth
<1% (Limited to important or life-threatening): Bradycardia (sinus), cholestasis or hepatitis and heptocellular injury, cirrhosis, dyspnea, gynecomastia, hemolytic anemia, hyperprolactinemia, increased liver enzymes, jaundice, leukopenia, orthostatic hypotension, positive Coombs' test, sexual dysfunction, SLE-like syndrome, sodium retention, thrombocytopenia, transient leukopenia or granulocytopenia
Contraindications
 
Hypersensitivity to methyldopa or any component of the formulation; active hepatic disease; liver disorders previously associated with use of methyldopa; on MAO inhibitors; bisulfite allergy if using oral suspension or injectable
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• Hemolytic anemia: May rarely produce hemolytic anemia; positive Coombs' test occurs in 10% to 20% of patients (perform periodic CBCs).
• Hepatic effects: May rarely produce liver disorders; use with caution in patients with previous liver disease or dysfunction.
• Sedation: Usually transient, sedation may occur during initial therapy or whenever the dose is increased.
Disease-related concerns:
• Renal impairment: Use with caution in patients with renal impairment; may respond to smaller doses. The active metabolites of methyldopa accumulate in uremia.
Special populations:
• Elderly: May be inappropriate in this age group due to a risk of bradycardia and depression (Beers Criteria). Use with caution in the elderly; may experience syncope (avoid by giving smaller doses). Not considered a drug of choice.
• Pregnancy: Often considered the drug of choice for treatment of hypertension in pregnancy.
Dosage form specific issues:
• Injection: Do not use injectable if bisulfite allergy.
Other warnings/precautions:
• Tolerance: May occur usually between the second and third month of therapy; adding a diuretic or increasing the dosage of methyldopa frequently restores blood pressure control.
Interactions
 
COMT Inhibitors: May decrease the metabolism of COMT Substrates. Risk C: Monitor therapy
Iobenguane I 123: Methyldopa may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
Iron Salts: May decrease the absorption of Methyldopa. Only oral iron salts are of concern. Exceptions: Ferric Gluconate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Risk D: Consider therapy modification
Lithium: Methyldopa may enhance the adverse/toxic effect of Lithium. This may occur without notable changes in serum lithium concentrations. Risk C: Monitor therapy
MAO Inhibitors: May enhance the adverse/toxic effect of Methyldopa. Risk X: Avoid combination
MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy
Pregnancy
 
B
Pregnancy Implications
Adverse events have not been observed in animal reproduction studies. Methyldopa crosses the placenta and appears in cord blood. Methyldopa is considered an appropriate agent for the treatment of hypertension in pregnancy.
Lactation
 
Enters breast milk/use caution (AAP rates “compatible”; AAP 2001 update pending)
Mechanism of Action
 
Stimulation of central alpha-adrenergic receptors by a false transmitter that results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature
Pharmacodynamics / Kinetics
 
Onset of action: Peak effect: Hypotensive: Oral
Duration: 12-24 hours
Protein binding: <15%
Metabolism: Intestinal and hepatic
Half-life elimination: 75-80 minutes; End-stage renal disease: 6-16 hours
Excretion: Urine (85% as metabolites) within 24 hours
 
   
 
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