DIACARBUM (Diacarbum). 2-Atsetilamino-1, 3, 4-thiadiazol color-5-sulphamide.
Synonyms: Fonuritum, Acetazolamide, Acetazolamidum, Acetamox, Anicar, Dehydratin, Dilamox, Diluran, Diuramid, Ederen, Eumicton, Fonurit, Glaucomide, Glauconox, Glaupax, Lediamox, Natrionex, Nephramid, Renamid, Sulfadiurine, etc.
White crystal powder. We will dissolve in water and alcohol very little, it is easy - in shchelochka.
Diacarbum is the representative of group of medicines which effect is connected with selective ability to oppress activity of a karboangidraza (coal anhydrase) - the enzyme participating in process of hydration and dehydration of carbonic acid. This property was for the first time revealed at streptocide and other sulfanamide connections, however at Diacarbum which molecule also contains sulphonamide group, it is significant much stronger.
Diacarbum can be used with the medical purpose at various states at which it is reasonable to lower activity of a karboangidraza. It has the greatest use as diuretic means and also for treatment of glaucoma.
The diuretic effect is based on oppression of activity of a karboangidraza in kidneys and change of the acid-base state (ABS) in an organism. It affects mainly proximal tubules. Oppression of a karboangidraza leads to reduction of formation of carbonic acid and decrease in a reabsorption of bicarbonate and Na + an epithelium of tubules; discharge with Na urine +, a sales tax 3 - in this connection water discharge considerably increases raises; rn urine raises. Potassium ions under the influence of Diacarbum are also allocated in bigger quantity. Increase in discharge of chlorides does not happen. Due to the strengthened discharge from an organism of bicarbonates the acidosis can develop. After the termination of intake of Diacarbum the alkaline reserve in 1 - 2 day returns to initial.
Diacarbum is effective at intake. It is quickly soaked up from digestive tract and, coming to fabrics and bodies, oppresses the karboangidraza which is contained in them.
As usual diuretic Diacarbum is applied rather seldom as there are more effective drugs, but it is especially shown in hypostases owing to a pulmonary heart when lowering of the increased contents WITH and bicarbonates in blood is reasonable.
Due to lowering of contents WITH in blood, Diacarbum in certain cases improves a condition of lungs sore with emphysema.
The significant diuretic effect is observed at the combined use of Diacarbum and Euphyllinum.
With ammonium chloride and other acid-forming diuretics it is not necessary to combine Diacarbum as the diuretic effect at the same time decreases or even completely disappears.
In hypostases of renal origin Diacarbum is ineffective, and in cirrhosis its use is undesirable because of hypersensitivity of patients to a hypopotassemia and also because of danger of possible increase in content of ammonia in blood.
Diacarbum is applied also at treatment of glaucoma in various phases of its development (at simple, congestive, youthful and other forms of primary and secondary glaucoma). The lowering of intraocular pressure caused by drug is connected with oppression of a karboangidraza of a ciliary body and reduction of secretion of watery moisture and also with improvement of its outflow. Diacarbum does not cause narrowing of a pupil; it can be applied also in a cataract. The hypotensive effect at patients with a bad attack of glaucoma is most significant.
Diacarbum is appointed also in epilepsy; the therapeutic effect, perhaps, is connected with oppression of activity of a karboangidraza of a brain; it should be noted that under the influence of Diacarbum the formation of cerebrospinal fluid decreases. Diacarbum at patients with rare absentias epileptica is especially effective.
Accept Diacarbum inside. A single dose 0, 125 - 0, 25 g (0, 5 g are more rare). Accept as diuretic once a day every day or every other day courses for 2 - 4 days with an interval several days. At frequent use the diuretic effect decreases as the content of bicarbonates in blood strongly falls; for the specified periods the bicarbonate content increases again and intake of Diacarbum causes increase in discharge of ions of sodium and bicarbonate with urine again and also strengthening of a diuresis. Higher doses do not enhance effect.
In glaucoma Diacarbum is appointed on 0, 125 - 0, 25 g to reception from 1 to 3 times a day, sometimes 2 times a day (in the morning and in the evening) every other day. After each 5 days of intake of Diacarbum take a break for 2 days. The good effect is observed in some cases at co-administration of Diacarbum and miotocs. Duration of use of Diacarbum in glaucoma depends on the nature of a disease and efficiency of treatment.
At a preparation for surgery (concerning glaucoma) give 0, 5 g a day on the eve of operation and in the morning in day of operation.
In epilepsy appoint usually 0, 25 - 0, 5 g a day.
The patient with rare absentias epileptica (see Trimethinum) add Diacarbum in 7 - 10 days after the beginning of the main treatment on 0, 125 - 0, 25 g for the night. Drug is given for 3 days in a row with a break for every fourth day.
Diacarbum malotoksichen is also usually well transferred by patients even at prolonged use, however certain patients can have a drowsiness, disturbance of orientation, paresthesia; these phenomena, perhaps, are connected with oppression of a karboangidraza and with a hypopotassemia. At reduction of a dose or drug withdrawal the by-effects quickly pass.
At long intake of Diacarbum for maintaining balance of electrolytes in an organism it is necessary to enter sodium bicarbonate.
Because at people of advanced age potassium discharge with urine under the influence of Diacarbum increases more than at young people, in geriatric practice it is recommended to be limited 1 - 2-day courses with obligatory correction of potassium exchange.
Use of Diacarbum at treatment of newborns
The main indicator to prescribing of Diacarbum the newborn is the increased intracranial pressure as drug is diuretic and is capable to reduce products of cerebrospinal liquid at the newborn. Diacarbum promotes reduction of puffiness of a brain of the child and removal of excess liquid. Side effect at the same time is "washing away" from an organism of the potassium, necessary for heart, therefore Diacarbum the newborn only in combination with the Asparkam is appointed.
Diacarbum contraindications: tendency to acidosis, the raised discharge of ions of sodium and potassium, Addison's disease, acute diseases of a liver and kidneys, diabetes and uraemia. It is not necessary to appoint Diacarbum in the first 3 months of pregnancy.
Packagings: powder; tablets on 0, 25 g in packing on 24 pieces.
Storage: in the dry place.