Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1410
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| dailymed-drugs:1410 | rdf:type | http://www4.wiwiss.fu-berli... | lld:dailymed |
| dailymed-drugs:1410 | rdf:type | dailymed-instance:drugs | lld:dailymed |
| dailymed-drugs:1410 | rdfs:label | Methyldopa&Hydrochlorothiazide (Tablet) | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:dosage | DOSAGE MUST BE INDIVIDUALIZED, AS DETERMINED BY TITRATION OF THE INDIVIDUAL COMPONENTS . Once the patient has been successfully titrated, methyldopa and hydrochlorothiazide tablets may be substituted if the previously determined titrated doses are the same as in the combination. The usual starting dosage is one 250 mg/15 mg tablet of methyldopa and hydrochlorothiazide two or three times a day or one 250 mg/25 mg tablet of methyldopa and hydrochlorothiazide two times a day. Alternatively, one 500 mg/30 mg tablet of methyldopa and hydrochlorothiazide or a 500 mg/50 mg tablet of methyldopa and hydrochlorothiazide once daily may be used. Hydrochlorothiazide doses greater than 50 mg daily should be avoided. Hydrochlorothiazide can be given at doses of 12.5 mg to 50 mg per day when used alone. The usual daily dosage of methyldopa is 500 mg to 2 g. To minimize the sedation associated with methyldopa, start dosage increases in the evening. The maximum recommended daily dose of methyldopa is 3 g. Occasionally tolerance to methyldopa may occur, usually between the second and third month of therapy. Additional separate doses of methyldopa or replacement of methyldopa and hydrochlorothiazide tablets with single entity agents is necessary until the new effective dose ratio is reestablished by titration. If methyldopa and hydrochlorothiazide does not adequately control blood pressure, additional doses of other agents may be given. When methyldopa and hydrochlorothiazide is given with antihypertensives other than thiazides, the initial dosage of methyldopa should be limited to 500 mg daily in divided doses and the dose of these other agents may need to be adjusted to effect a smooth transition. Since both components, methyldopa and hydrochlorothiazide, have a relatively short duration of action, withdrawal is followed by return of hypertension usually within 48 hours. This is not complicated by an overshoot of blood pressure. Since methyldopa is largely excreted by the kidney, patients with impaired renal function may respond to smaller doses. Syncope in older patients may be related to an increased sensitivity and advanced arteriosclerotic vascular disease. This may be avoided by lower doses. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:descripti... | This fixed combination product combines two antihypertensives: methyldopa and hydrochlorothiazide.<br/>Methyldopa: Methyldopa is an antihypertensive and is the L-isomer of alpha-methyldopa. It is levo-3-(3,4-Dihydroxy-phenyl)-2-methylalanine sesquihydrate. Its molecular formula is CHNO���1��HO with a molecular weight of 238.24, and its structural formula is: Methyldopa is a white to yellowish white, odorless fine powder and is sparingly soluble in water.<br/>Hydrochlorothiazide: Hydrochlorothiazide is a diuretic and antihypertensive. It is the 3,4-dihydro derivative of chlorothiazide. Its chemical name is 6-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide. Its molecular formula is CHCINOSand its structural formula is: Hydrochlorothiazide is a white, or practically white, crystalline powder with a molecular weight of 297.75 which is slightly soluble in water, but freely soluble in sodium hydroxide solution. Each tablet for oral administration contains: 250 mg methyldopa and 15 mghydrochlorothiazide,or250 mg methyldopa and 25 mghydrochlorothiazide. Potency for methyldopa is calculated on anhydrous basis. Each tablet also contains the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, D&C Yellow #10 Aluminum Lake, FD&C Blue #1 Aluminum Lake, FD&C Yellow #6 Aluminum Lake, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, sodium lauryl sulfate, titanium dioxide and triacetin. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:clinicalP... | Methyldopa: Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Although the mechanism of action has yet to be conclusively demonstrated, the antihypertensive effect of methyldopa probably is due to its metabolism to alpha-methylnorepinephrine, which then lowers arterial pressure by stimulation of central inhibitory alpha-adrenergic receptors, false neurotransmission, and/or reduction of plasma renin activity. Methyldopa has been shown to cause a net reduction in the tissue concentration of serotonin, dopamine, norepinephrine, and epinephrine. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. In man, the antihypertensive activity appears to be due solely to the L-isomer. About twice the dose of the racemate (DL-alpha-methyldopa) is required for equal antihypertensive effect. Methyldopa has no direct effect on cardiac function and usually does not reduce glomerular filtration rate, renal blood flow, or filtration fraction. Cardiac output usually is maintained without cardiac acceleration. In some patients the heart rate is slowed. Normal or elevated plasma renin activity may decrease in the course of methyldopa therapy. Methyldopa reduces both supine and standing blood pressure. It usually produces highly effective lowering of the supine pressure with infrequent symptomatic postural hypotension. Exercise hypotension and diurnal blood pressure variations rarely occur.<br/>Hydrochlorothiazide: The mechanism of the antihypertensive effect of thiazides is unknown. Hydrochlorothiazide does not usually affect normal blood pressure. Hydrochlorothiazide affects the distal renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosage all thiazides are approximately equal in their diuretic efficacy. Hydrochlorothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate. After oral use diuresis begins within 2 hours, peaks in about 4 hours and lasts about 6 to 12 hours.<br/>Pharmacokinetics and Metabolism:<br/>Methyldopa: 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:��- methyldopa mono-O-sulfate; 3-O-methyl-��-methyldopa; 3,4-dihydroxyphenyl acetone;��-methyldopamine; 3-O-methyl-�����methyldopamine and their conjugates. Approximately 70 percent of the drug which is absorbed is excreted in the urine as methyldopa and its mono-O-sulfate conjugate. The renal clearance is about 130 mL/min in normal subjects and is diminished in renal insufficiency. The plasma half-life of methyldopa is 105 minutes. After oral doses, excretion is essentially complete in 36 hours. Methyldopa crosses the placental barrier, appears in cord blood, and appears in breast milk.<br/>Hydrochlorothiazide: Hydrochlorothiazide is not metabolized but is eliminated rapidly by the kidney. When plasma levels have been followed for at least 24 hours, the plasma half-life has been observed to vary between 5.6 and 14.8 hours. At least 61 percent of the oral dose is eliminated unchanged within 24 hours. Hydrochlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:activeIng... | dailymed-ingredient:Methyld... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:supply | Methyldopa and Hydrochlorothiazide Tablets, USP are available as follows: The 250 mg/15 mg tablets are green, round, unscored, film-coated tablets debossed with MYLAN on one side and 507 on the other side. They are available as follows: NDC 0378-0507-01bottles of 100 tablets The 250 mg/25 mg tablets are green, capsule-shaped, unscored, film-coated tablets debossed with MYLAN on one side and 711 on the other side. They are available as follows: NDC 0378-0711-01bottles of 100 tablets NDC 0378-0711-10bottles of 1000 tablets Store at 20��to 25��C (68��to 77��F). [See USP for Controlled Room Temperature.] Protect from light. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:boxedWarn... | WARNING: This fixed combination drug is not indicated for initial therapy of hypertension. Hypertension requires therapy titrated to the individual patient. If the fixed combination represents the dosage so determined, its use may be more convenient in patient management. The treatment of hypertension is not static, but must be re-evaluated as conditions in each patient warrant. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:activeMoi... | dailymed-ingredient:Methyld... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:magnesi... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:microcr... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:hyprome... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:titaniu... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:triacet... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:polydex... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:polyeth... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:sodium_... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:colloid... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:croscar... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:FD&C_Ye... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:D&C_Yel... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:inactiveI... | dailymed-ingredient:FD&C_Bl... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:overdosag... | Acute overdosage may produce acute hypotension with other responses attributable to brain and gastrointestinal malfunction (excessive sedation, weakness, bradycardia, dizziness, light-headedness, constipation, distention, flatus, diarrhea, nausea, vomiting). In the event of overdosage, symptomatic and supportive measures should be employed. When ingestion is recent, gastric lavage or emesis may reduce absorption. When ingestion has been earlier, infusions may be helpful to promote urinary excretion. Otherwise, management includes special attention to cardiac rate and output, blood volume, electrolyte balance, paralytic ileus, urinary function and cerebral activity. Sympathomimetic drugs (e.g., norepinephrine, epinephrine, metaraminol bitartrate) may be indicated. Methyldopa is dialyzable. The degree to which hydrochlorothiazide is removed by hemodialysis has not been established. The oral LDof methyldopa is greater than 1.5 g/kg in both the mouse and the rat. The oral LDof hydrochlorothiazide is greater than 10 g/kg in the mouse and rat. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:genericMe... | Methyldopa and hydrochlorothiazide | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:fullName | Methyldopa&Hydrochlorothiazide (Tablet) | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:adverseRe... | The following adverse reactions have been reported and, within each category, are listed in order of decreasing severity.<br/>Methyldopa: Sedation, usually transient, may occur during the initial period of therapy or whenever the dose is increased. Headache, asthenia, or weakness may be noted as early and transient symptoms. However, significant adverse effects due to methyldopa have been infrequent and this agent usually is well tolerated. Cardiovascular: Aggravation of angina pectoris, congestive heart failure, prolonged carotid sinus hypersensitivity, orthostatic hypotension (decrease daily dosage), edema or weight gain, bradycardia. Digestive: Pancreatitis, colitis, vomiting, diarrhea, sialadenitis, sore or "black" tongue, nausea, constipation, distention, flatus, dryness of mouth. Endocrine: Hyperprolactinemia. Hematologic: Bone marrow depression, leukopenia, granulocytopenia, thrombocytopenia, hemolytic anemia; positive tests for antinuclear antibody, LE cells, and rheumatoid factor, positive Coombs test. Hepatic: Liver disorders including hepatitis, jaundice, abnormal liver function tests . Hypersensitivity: Myocarditis, pericarditis, vasculitis, lupus-like syndrome, drug-related fever, eosinophilia. Nervous System/Psychiatric: Parkinsonism, Bell's palsy, decreased mental acuity, involuntary choreoathetotic movements, symptoms of cerebrovascular insufficiency, psychic disturbances including nightmares and reversible mild psychoses or depression, headache, sedation, asthenia or weakness, dizziness, light-headedness, paresthesias. Metabolic: Rise in BUN. Musculoskeletal: Arthralgia, with or without joint swelling; myalgia. Respiratory: Nasal stuffiness. Skin: Toxic epidermal necrolysis, rash. Urogenital: Amenorrhea, breast enlargement, gynecomastia, lactation, impotence, decreased libido.<br/>Hydrochlorothiazide: Body as a Whole: Weakness. Cardiovascular: Hypotension including orthostatic hypotension (may be aggravated by alcohol, barbiturates, narcotics or antihypertensive drugs). Digestive: Pancreatitis, jaundice (intrahepatic cholestatic jaundice), diarrhea, vomiting, sialadenitis, cramping, constipation, gastric irritation, nausea, anorexia. Hematologic: Aplastic anemia, agranulocytosis, leukopenia, hemolytic anemia, thrombocytopenia. Hypersensitivity: Anaphylactic reactions, necrotizing angiitis (vasculitis and cutaneous vasculitis), respiratory distress including pneumonitis and pulmonary edema, photosensitivity, fever, urticaria, rash, purpura. Metabolic: Electrolyte imbalance , hyperglycemia, glycosuria, hyperuricemia. Musculoskeletal: Muscle spasm. Nervous System/Psychiatric: Vertigo, paresthesias, dizziness, headache, restlessness. Renal: Renal failure, renal dysfunction, interstitial nephritis. Skin: Erythema multiforme including Stevens-Johnson syndrome, exfoliative dermatitis including toxic epidermal necrolysis, alopecia. Special Senses: Transient blurred vision, xanthopsia. Urogenital: Impotence. | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:indicatio... | Hypertension - . | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:represent... | http://www4.wiwiss.fu-berli... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:routeOfAd... | http://www4.wiwiss.fu-berli... | lld:dailymed |
| dailymed-drugs:1410 | dailymed-instance:name | Methyldopa&Hydrochlorothiazide | lld:dailymed |
| http://www4.wiwiss.fu-berli... | dailymed-instance:producesD... | dailymed-drugs:1410 | lld:dailymed |