TAMGILAN [Tamsulosin] 0.4 mg Capsules
TAMGILAN
instructions
for the medical use of the medicinal product
Tradename
Tamgilan, Тамгилан
International non-proprietary name or generic
name
Tamsulosin, Тамсулозин
Composition
Each capsule
contains: tamsulosin (as tamsulosin hydrochloride) 0.4 mg.
Dosage form
Capsules.
Alpha1-blocker.
Pharmacological properties
Pharmacodynamics
Tamsulosin selectively and competitively blocks
postsynaptic alpha1A-adrenergic receptors located in the smooth muscles of the
prostate gland, bladder neck and prostatic urethra, as well as
alpha1D-adrenergic receptors, mainly located in the body of the bladder. This
leads to a decrease in the tone of the smooth muscles of the prostate gland,
the bladder neck, the prostatic part of the urethra, improves the outflow of
urine, reduces the symptoms of obstruction and irritation of the urinary tract
in benign prostatic hyperplasia. The ability of tamsulosin to act on
alpha1A-adrenergic receptors is 20 times greater than its ability to interact
with alpha1A-adrenergic receptors located in vascular smooth muscle. Due to
this high selectivity, the drug does not cause any clinically significant
systemic decrease in blood pressure (BP) in both hypertensive patients and
patients with normal baseline blood pressure. As a rule, the therapeutic effect
is achieved 2 weeks after the start of taking the drug.
After oral administration, tamsulosin is rapidly and almost completely
absorbed from the gastrointestinal tract. After a single oral intake of 400 μg, the
Cmax of the active substance in plasma is reached after 6 hours.
Plasma protein binding - 99%. Vd is insignificant and amounts to 0.2 l /
kg.
Tamsulosin is slowly metabolized in the liver to form pharmacologically
active metabolites that retain high selectivity for alpha1A-adrenergic
receptors. Most of the active substance is present in the blood unchanged.
T1 / 2 of tamsulosin with a single dose - 10 hours, terminal T1 / 2 is -
22 hours. It is excreted by the kidneys, 9% - unchanged.
Treatment of dysuric disorders in benign prostatic
hyperplasia.
Hypersensitivity to tamsulosin; orthostatic
hypotension (including history), severe liver failure; children and adolescents
up to 18 years old.
Method of administration and dosage
Inside
after eating, without chewing, drinking a small amount of liquid. Take 1 capsule (0.4 mg) 1 time per day.
Special instructions and precautions
At the first signs of orthostatic
hypotension (dizziness, weakness), one should sit or lie down until these
symptoms disappear. Before starting treatment with Tamgilan, it is necessary to
examine the patient to exclude other diseases that can cause the same symptoms
as benign prostatic hyperplasia. Before starting treatment with the drug and
during therapy, you should regularly examine the prostate gland and, if
necessary, determine the prostate specific antigen (PSA).
Due to the possibility of
complications during cataract surgery, it is not recommended to prescribe
Tamgilan treatment to patients with cataracts if surgery is planned.
Prescribe with caution to patients
with severe renal failure (CC less than 10 ml / min) and arterial hypotension.
When taking the drug, drowsiness,
blurred vision, dizziness and fainting are possible, therefore, the drug should
be used with caution during work by drivers of vehicles and people whose
profession requires increased concentration of attention.
Interaction with other medicinal products
With the simultaneous use of tamsulosin with atenolol,
enalapril or theophylline, no interactions were found.
Concomitant use of cimetidine causes an increase in
plasma tamsulosin levels, while furosemide decreases them, but since levels
remain within the normal range, the dosage does not need to be adjusted.
Diazepam, propranolol, trichloromethiazide,
chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and
warfarin do not alter the free fraction of tamsulosin in human plasma in vitro.
In turn, tamsulosin also does not change the free fractions of diazepam,
propranolol, trichloromethiazide and chlormadinone.
However, diclofenac and warfarin may increase the rate
of elimination of tamsulosin.
Concomitant use of tamsulosin with strong inhibitors
of CYP3A4 can lead to increased exposure to tamsulosin. Concomitant
administration with ketoconazole (a known strong inhibitor of CYP3A4) led to an
increase in AUC and Cmax of tamsulosin by 2.8 and 2.2 times, respectively.
Tamsulosin should not be given in combination with
potent CYP3A4 inhibitors in patients with the CYP2D6 phenotype with poor
metabolism.
Tamsulosin should be used with caution in combination
with strong to moderate CYP3A4 inhibitors.
The simultaneous use of tamsulosin with paroxetine, a
strong inhibitor of CYP2D6, led to an increase in Cmax and AUC of tamsulosin by
1.3 and 1.6 times, respectively, but this increase is not considered clinically
significant.
Side effect
From the side of the cardiovascular system: palpitations, atrial
fibrillation, arrhythmia, tachycardia, shortness of breath, orthostatic
hypotension.
From the nervous system: headache, dizziness, fainting.
From the digestive system: constipation, diarrhea,
nausea, vomiting, dry mouth.
Skin and subcutaneous
tissue disorders: skin rash, pruritus, urticaria, angioedema, Stevens-Johnson
syndrome, erythema multiforme, exfoliative dermatitis.
From the reproductive system: ejaculation disorders,
priapism.
Others: rhinitis, asthenia, visual impairment.
If any of the side effects
indicated in the instructions are aggravated, or you notice any other side
effects not listed in the instructions, inform your doctor.
Symptoms: Acute hypotension is possible.
Treatment: transfer the patient to a horizontal position
and take measures aimed at maintaining the function of the cardiovascular
system (restoration of blood pressure and heart rate); gastric lavage, the
introduction of activated charcoal and osmotic laxatives such as sodium
sulfate. In the absence of an effect, substances that increase the volume of
circulating blood, and, if necessary, vasoconstrictors should be administered.
Kidney function should be monitored and measures should be taken to maintain
it. Dialysis is not very effective, since the drug is largely bound to blood plasma
proteins.
Store in a dry and dark place, at a temperature not
exceeding 25°C.
Keep out of the reach
of children!
2 years. Do not use
after the expiration date printed on the package.
Dispensed by prescription.
Release form
10 capsules in aluminum foil blister. 3 blisters together with instructions for use in a cardboard box.