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Brand names,
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Analogs
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Brand Names Mixture
- Zylet (0.5% loteprednol etabonate + 0.3% tobramycin)
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Chemical_Formula
C14H16ClN3O4S2
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RX_link
No information avaliable
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
389.879 g/mol
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Melting Point
227-228oC
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H2O Solubility
No information avaliable
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State
Solid
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LogP
1.048
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Dosage Forms
Tablets (oral, 5mg)
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Indication
Cyclothiazide is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. It is also indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension.
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Pharmacology
Like other thiazides, cyclothiazide promotes water loss from the body (diuretics). It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. Cyclothiazide affects the distal renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic efficacy. Cyclothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate.
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Absorption
No information avaliable
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side effects and Toxicity
Oral LD50 in mouse is > 10000 mg/kg, and > 4000 mg/kg in rat. Signs of overdose include those caused by electrolyte depletion (hypokalemia, hypochloremia, hyponatremia) and dehydration resulting from excessive diuresis. If digitalis has also been administered hypokalemia may accentuate cardiac arrhythmias.
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Patient Information
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Organisms Affected
Humans and other mammals