Expiration date: 07/2025
Enteric capsules.
Ingredients (1 capsule.):
Active ingredient: dapoxetine (hydrochloride) 30 or 60 mg.
Excipients: hypromellose E5 10.54 mg hypromellose mg HP55 15.51, starch 44.09 mg, 47.3 mg mannitol, 5.22 mg sodium lauryl sulfate, 17.46 mg of sucrose, titanium dioxide 1.15 mg, 1.55 mg cetyl alcohol.
The composition of the capsule shell: gelatin, titanium dioxide, dye blue patent V.
Description pharmaceutical form:
Enteric capsules, hard gelatin number 3, body and cap in blue, the contents of capsules - a spherical micro-granules from almost white to yellowish-white in color.
Pharmacokinetics:
After oral administration, duloxetine is well absorbed from the gastrointestinal tract, absorption begins in 2 hours after administration, Cmaxdostigaetsya after 6 h after administration. Receiving simultaneously with food increases the time to reach Cmax to 10 hours, which reduces the extent of absorption (approximately 10%), but no effect on the Cmax.
Plasma protein binding is high (over 90%), primarily to albumin and ?1-globulin. Disorders of the liver or kidneys do not affect the degree of protein binding. Duloxetine involving actively biotransformed isoenzymes CYP2D6 and CYP1A2, which catalyze the formation of two major metabolites (4-glucuronate conjugate gidroksiduloksetina, sulphate conjugate of 5-hydroxy-6 metoksiduloksetina). Circulating metabolites do not possess pharmacological activity. T1 / 2 is 12 h. Medium duloxetine clearance is 101 l / h. Excreted in the urine as metabolites.
In patients with end-stage renal disease on hemodialysis, Cmax and AUC of duloxetine increased by 2 times. In this connection it should consider the advisability of reducing the dose in patients with clinically severe impaired renal function.
In patients with clinical evidence of liver failure slowing metabolism and excretion of duloxetine may experience. After a single dose of duloxetine 20 mg in 6 patients with cirrhosis and mild hepatic impairment (class B on a scale Child-Pugh) the duration of T1 / 2 of duloxetine was approximately 15% higher than in healthy individuals of corresponding sex and age with a five-fold increase in the average value of AUC. Despite the fact that the Cmax in patients with cirrhosis were the same as for healthy individuals, T1 / 2 is about 3 times more.
Testimony:
Depression, painful form of diabetic neuropathy.
Dosage and administration:
The recommended starting dose is 60 mg 1 time / day.
If necessary, the daily dose can be increased from 60 mg to a maximum dose of 120 mg / day in 2 divided doses.
In patients with severe renal function impairment (creatinine clearance <30 mL / min), the initial dose should be 30 mg 1 time / day. In patients with impaired hepatic function should be to reduce the initial dose of the drug or reduce the number of intakes.
