People suffering from excess weight try to find the easiest way to get rid of it. They do not give preference to physical training and the selection of a balanced diet, but choose the pharmacological industry as their assistant, for which they later pay.
The main reason for excess weight is increased appetite, because no one has yet gained weight from the air. Goldline diet pills help to tame this unhealthy feeling. Once the appetite disappears, the person does not eat, which means that he loses his kilograms.
All medications that truly suppress hunger are prescribed by an endocrinologist. In this case, you will first have to undergo tests so that the doctor is convinced that the cause of obesity is overeating. Without a doctor's prescription, they will sell you a dummy or a fake, which can be very harmful.
pharmachologic effect
A drug for the treatment of obesity with central action. Sibutramine is a prodrug and exerts its effect in vivo through metabolites (primary and secondary amines) that inhibit the reuptake of monoamines (mainly serotonin and norepinephrine). An increase in the content of neurotransmitters in synapses increases the activity of central serotonin 5HT receptors and adrenoreceptors, which increases the feeling of satiety and reduces the need for food, as well as an increase in thermal production. By indirectly activating β3-adrenergic receptors, sibutramine acts on brown adipose tissue.
A decrease in body weight is accompanied by an increase in the concentration of HDL in the blood serum and a decrease in the amount of triglycerides, total cholesterol, LDL and uric acid.
Sibutramine and its metabolites do not affect the release of monoamines, do not inhibit MAO, and do not have an affinity for a large number of neurotransmitter receptors, including serotonin (5HT1-, 5HT1A-, 5HT1B-, 5HT2A-, 5HT2C-), adrenergic (β1-, β2-, β3-, α1-, α2-), dopamine (D1-, D2-), muscarinic, histamine (H1-), benzodiazepine and NMDA receptors.
Pharmacokinetics
Suction
After oral administration, it is quickly absorbed from the gastrointestinal tract by at least 77%. During the “first pass” through the liver, it undergoes biotransformation under the influence of the cytochrome P450 3A4 isoenzyme with the formation of two active metabolites (mono- and didesmethylsibutramine). After taking a single dose of 15 mg, the Cmax of monodesmethylsibutramine is 4 ng/ml (3.2-4.8 ng/ml), the Cmax of didesmethylsibutramine is 6.4 ng/ml (5.6-7.2 ng/ml). Tmax of sibutramine - 1.2 hours, Tmax of active metabolites - 3-4 hours. Simultaneous food intake reduces the Cmax of metabolites by 30% and increases the time to reach it by 3 hours, without changing the AUC.
Distribution
Quickly distributed throughout tissues. Protein binding is 97% (sibutramine) and 94% (mono- and didesmethylsibutramine). Css of active metabolites in the blood is achieved within 4 days after the start of treatment and is approximately 2 times higher than the plasma level after taking a single dose.
Metabolism and excretion
T1/2 of sibutramine - 1.1 hours, monodesmethylsibutramine - 14 hours, didesmethylsibutramine -16 hours. Active metabolites undergo hydroxylation and conjugation to form inactive metabolites, which are excreted mainly by the kidneys.
Goldline tablets - instructions
As indicated in the instructions, this remedy should be taken only once a day, in the morning on an empty stomach, with 200 ml of water. The initial dosage should not exceed 5 mg. If after a month the weight loss was less than 2 kg, then the dosage is increased.
Do not delude yourself that once you start taking pills, the weight will begin to melt before your eyes. This remedy must be taken for a year, following an appropriate diet and physical activity. Only a doctor can increase or decrease the dosage, or even stop taking the drug if certain symptoms occur.
When taking this remedy, the temperature rises slightly, due to which fat reserves are burned faster. If after three months the weight has not decreased by more than 5%, then the drug should be completely abandoned. If after completing the course a person begins to gain weight again, then a repeat course is prohibited for him.
Dosage
Goldline is prescribed orally 1 time/day. The dose is set individually, depending on tolerability and clinical effectiveness. An initial dose of 10 mg is recommended; in case of poor tolerance, 5 mg can be taken. Capsules should be taken in the morning, without chewing and with a sufficient amount of liquid (a glass of water). The drug can be taken on an empty stomach or combined with meals. If within 4 weeks from the start of treatment a reduction in body weight of 5% or more is not achieved, then the dose is increased to 15 mg/day.
Treatment with Goldline should not continue for more than 3 months in patients who do not respond well to therapy, i.e. who fail to achieve a 5% reduction in body weight from the initial level within 3 months of treatment. Treatment should not be continued if, with further therapy, after achieving a reduction in body weight, the patient again gains 3 kg or more in body weight. The duration of treatment should not exceed 2 years, since there are no data on efficacy and safety for a longer period of taking sibutramine.
Treatment with Goldline should be carried out in combination with diet and exercise under the supervision of a physician with practical experience in the treatment of obesity.
Who is prescribed Goldline?
Sometimes doctors do prescribe this drug, but not everyone. They are prescribed only to people who are extremely obese and only under strict supervision, supplemented with a low-calorie diet and appropriate physical activity.
It can be prescribed only if the patient tolerates sibutramine well, which is an appetite suppressant, thanks to which not only weight loss, but also all the troubles occur.
Why is strict control necessary? Yes, because sometimes you have to rinse the stomach or administer beta-blockers. That’s why pharmacies sell this product strictly according to a prescription, and through the Internet you will only encounter scammers who buy something from them that is unclear.
Overdose
There are extremely limited data on sibutramine overdose. Specific signs of overdose are unknown, however, the possibility of more pronounced side effects should be taken into account. You should notify your doctor if an overdose is suspected.
The most common symptoms
: tachycardia, increased blood pressure, headache, dizziness.
Treatment:
There is no special treatment or specific antidotes. It is necessary to ensure free breathing, monitor the state of the cardiovascular system, and, if necessary, provide supportive symptomatic therapy. Timely use of activated charcoal can reduce the absorption of sibutramine in the intestine. Gastric lavage also reduces drug absorption. Patients with high blood pressure and tachycardia can be prescribed beta-blockers. The effectiveness of forced diuresis or hemodialysis has not been established.
Drug interactions
Inhibitors of microsomal oxidation, incl. inhibitors of the CYP3A4 isoenzyme (ketoconazole, erythromycin, cyclosporine) increase plasma concentrations of sibutramine metabolites with an increase in heart rate and a clinically insignificant increase in the QT interval.
Rifampicin, macrolide antibiotics, phenytoin, carbamazepine, phenobarbital and dexamethasone can accelerate the metabolism of sibutramine.
The simultaneous use of several drugs that increase the level of serotonin in the blood can lead to the development of a serious interaction.
Serotonin syndrome may develop in rare cases when Goldline is used concomitantly with selective serotonin reuptake inhibitors (drugs to treat depression), with certain migraine drugs (sumatriptan, dihydroergotamine), with opioid analgesics (pentazocine, pethidine, fentanyl) or antitussives. (dextromethorphan).
Sibutramine does not affect the effect of oral contraceptives.
Medicines that increase blood pressure or heart rate (ephedrine, phenylpropanolamine, pseudoephedrine, and combination cold medications containing these drugs) increase the risk of increased blood pressure and heart rate.
When sibutramine and alcohol were taken simultaneously, there was no increase in the negative effects of ethanol. However, alcohol is absolutely not compatible with the dietary measures recommended when taking sibutramine.
Side effects
Most often, side effects occur at the beginning of treatment (in the first 4 weeks). Their severity and frequency weaken over time.
Side effects are generally mild and reversible and, depending on the effect on organs and organ systems, are presented in the following order: often (>10%), sometimes (1-10%), rarely (<1%).
From the side of the central nervous system:
often - insomnia; sometimes - headache, dizziness, anxiety, paresthesia.
From the cardiovascular system:
sometimes - tachycardia, palpitations, increased blood pressure, symptoms of vasodilation (including skin hyperemia), exacerbation of hemorrhoids. There is a moderate rise in blood pressure at rest by 1-3 mmHg. Art. and a moderate increase in heart rate by 3-7 beats/min. In some cases, a more pronounced increase in blood pressure and heart rate cannot be ruled out. Clinically significant changes in blood pressure and pulse levels are recorded mainly at the beginning of treatment (in the first 4-8 weeks).
From the digestive system:
often - dry mouth, loss of appetite and constipation; sometimes - nausea, change in taste.
Dermatological reactions:
sometimes - increased sweating.
In isolated cases, the following clinically significant adverse events have been described during treatment with sibutramine: dysmenorrhea, edema, flu-like syndrome, skin itching, back pain, abdominal pain, paradoxical increase in appetite, thirst, rhinitis, depression, drowsiness, emotional lability, anxiety, irritability, nervousness, acute interstitial nephritis, bleeding, Henoch-Schönlein purpura (bleeding into the skin), convulsions, thrombocytopenia, transient increase in the activity of liver enzymes in the blood.
One patient with schizoaffective disorder, which was presumed to exist before treatment, developed acute psychosis after treatment.
Withdrawal reactions such as headache or increased appetite are rare.
There is no evidence that withdrawal symptoms, withdrawal symptoms or mood disturbances occur after treatment.
Goldline Plus capsules 10+158.5 mg 30 pcs. In Volgograd
Drugs containing this combination should be used only in cases where all non-drug measures for weight loss are ineffective - if the weight loss over 3 months is less than 5 kg.
Treatment with this combination should be carried out as part of complex therapy for weight loss under the supervision of a physician with practical experience in the treatment of obesity. Complex therapy includes both changing diet and lifestyle, as well as increasing physical activity. An important component of therapy is to create the prerequisites for persistent changes in eating behavior and lifestyle, which are necessary to maintain the achieved weight loss even after drug therapy is discontinued. As part of therapy, patients need to change their lifestyle and habits in such a way as to ensure that the achieved weight loss is maintained after completion of treatment. Patients should be clear that failure to comply with these requirements will lead to repeated weight gain and repeated visits to their doctor.
Clinically significant changes in blood pressure and pulse are recorded mainly at the beginning of treatment (in the first 4-8 weeks).
During the treatment period, regular monitoring of blood pressure and heart rate is required. During the first 3 months of treatment, these parameters should be monitored every 2 weeks and then monthly. If during two consecutive visits an increase in resting heart rate >10 beats/min or systolic/diastolic blood pressure >10 mmHg is detected, treatment should be discontinued. In patients with arterial hypertension whose blood pressure is higher than 145/90 mm Hg during antihypertensive therapy. Art., this control should be carried out especially carefully and, if necessary, at shorter intervals.
Alcohol does not combine with the dietary measures recommended when taking sibutramine.
In patients whose blood pressure exceeded 145/90 mmHg twice during repeated measurements, treatment with this combination should be discontinued.
In patients with sleep apnea syndrome, blood pressure must be monitored especially carefully.
If you are prone to constipation in the first days, monitoring the evacuation function of the intestines is necessary. If constipation occurs, stop taking it and take a laxative.
If mental disorders occur, the drug must be discontinued.
The simultaneous administration of drugs that increase the QT interval requires special attention. These drugs include histamine H1 receptor blockers (astemizole, terfenadine); antiarrhythmic drugs that increase the QT interval (amiodarone, quinidine, flecainide, mexiletine, propafenone, sotalol); gastrointestinal motility stimulator cisapride; pimozide, sertindole and tricyclic antidepressants. This also applies to conditions that can lead to an increase in the QT interval, such as hypokalemia and hypomagnesemia.
Although no connection has been established between taking sibutramine and the development of primary pulmonary hypertension, however, given the well-known risk of drugs in this group, with regular medical monitoring it is necessary to pay special attention to symptoms such as progressive dyspnea (shortness of breath), chest pain and swelling in the legs.
When taking sibutramine and other serotonin reuptake inhibitors together, there is an increased risk of bleeding. In patients predisposed to bleeding or taking drugs that affect hemostasis or platelet function, sibutramine should be used with caution.
Impact on the ability to drive vehicles and machinery
The use of this combination may limit the ability to drive vehicles and machinery. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Contraindications
- presence of organic causes of obesity (for example, hypothyroidism);
- serious eating disorders (anorexia nervosa or bulimia nervosa);
- mental illness;
— Gilles de la Tourette syndrome (generalized tics);
- simultaneous use of MAO inhibitors or their use within 2 weeks before prescribing Goldline;
- use of other drugs acting on the central nervous system (for example, antidepressants, antipsychotics);
- the use of drugs prescribed for sleep disorders containing tryptophan, as well as other centrally acting drugs for weight loss;
— IHD, decompensated chronic heart failure, congenital heart defects, occlusive diseases of peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient cerebrovascular accidents);
— uncontrolled arterial hypertension (BP above 145/90 mm Hg);
- thyrotoxicosis;
- severe dysfunction of the liver and/or kidneys;
- benign prostatic hyperplasia;
- pheochromocytoma;
- angle-closure glaucoma;
— established pharmacological, drug or alcohol dependence;
- pregnancy;
- lactation period (breastfeeding);
— age under 18 years and over 65 years;
- established hypersensitivity to sibutramine or other components of the drug.
Carefully _
the drug should be prescribed for the following conditions: history of arrhythmia, chronic circulatory failure, coronary artery disease (including history), cholelithiasis, arterial hypertension (controlled and history), neurological disorders, including mental retardation and seizures (including including a history), impaired liver and/or kidney function of mild to moderate severity, a history of motor and verbal tics.
Goldline
Use during pregnancy and breastfeeding
Since to date there is not a sufficiently convincing amount of research regarding the safety of the effects of sibutramine on the fetus, this drug should not be used during pregnancy.
Goldline should not be taken while breastfeeding.
Women of childbearing age should use contraception while taking Goldline.
Use for liver dysfunction
The drug should be prescribed with caution for mild to moderate liver dysfunction.
Use for renal impairment
The drug should be prescribed with caution in cases of mild to moderate renal dysfunction.
Use in children
Contraindication: age under 18 years.
Use in elderly patients
Contraindication: age over 65 years.
special instructions
Goldline should be used only in cases where all non-drug measures for weight loss are ineffective, if the weight loss over 3 months is less than 5 kg.
Treatment with Goldline should be carried out as part of complex weight loss therapy under the supervision of a physician with practical experience in the treatment of obesity. Complex therapy includes both changing diet and lifestyle, as well as increasing physical activity. An important component of therapy is the creation of prerequisites for permanent changes in eating habits and lifestyle, which are necessary to maintain the achieved weight loss even after drug therapy is discontinued. As part of Goldline therapy, patients need to change their lifestyle and habits in such a way as to ensure that the achieved weight loss is maintained after completion of treatment. Patients should be clear that failure to comply with these requirements will lead to repeated weight gain and repeated visits to their doctor.
In patients taking Goldline, it is necessary to measure blood pressure and heart rate. During the first 2 months of treatment, these parameters should be monitored every 2 weeks and then monthly. In patients with arterial hypertension whose blood pressure level is above 145/90 mm Hg during antihypertensive therapy. Art., this control should be carried out especially carefully and, if necessary, at shorter intervals. In patients whose blood pressure exceeded 145/90 mm Hg twice during repeated measurements. Art., treatment with Goldline should be suspended.
The simultaneous administration of drugs that increase the QT interval requires special attention. These drugs include histamine H1 receptor blockers (astemizole, terfenadine), antiarrhythmic drugs that increase the QT interval (amiodarone, quinidine, flecainide, mexiletine, propafenone, sotalol), cisapride, pimozide, sertindole and tricyclic antidepressants. This also applies to conditions that can lead to an increase in the QT interval, such as hypokalemia and hypomagnesemia.
The interval between taking MAO inhibitors and Goldline should be at least 2 weeks.
Although no connection has been established between taking Goldline and the development of primary pulmonary hypertension, however, given the well-known risk of drugs in this group, with regular medical monitoring it is necessary to pay special attention to symptoms such as progressive dyspnea, chest pain and swelling in the legs.
If you miss a dose of Goldline, you should not take a double dose of the drug at the next dose; it is recommended to continue taking the drug according to the prescribed regimen.
The duration of taking Goldline should not exceed 2 years.
Impact on the ability to drive vehicles and operate machinery
Taking Goldline may limit the ability to drive vehicles and operate machinery.
special instructions
Goldline should be used only in cases where all non-drug measures for weight loss are ineffective, if the weight loss over 3 months is less than 5 kg.
Treatment with Goldline should be carried out as part of complex weight loss therapy under the supervision of a physician with practical experience in the treatment of obesity. Complex therapy includes both changing diet and lifestyle, as well as increasing physical activity. An important component of therapy is the creation of prerequisites for permanent changes in eating habits and lifestyle, which are necessary to maintain the achieved weight loss even after drug therapy is discontinued. As part of Goldline therapy, patients need to change their lifestyle and habits in such a way as to ensure that the achieved weight loss is maintained after completion of treatment. Patients should be clear that failure to comply with these requirements will lead to repeated weight gain and repeated visits to their doctor.
In patients taking Goldline, it is necessary to measure blood pressure and heart rate. During the first 2 months of treatment, these parameters should be monitored every 2 weeks and then monthly. In patients with arterial hypertension whose blood pressure level is above 145/90 mm Hg during antihypertensive therapy. Art., this control should be carried out especially carefully and, if necessary, at shorter intervals. In patients whose blood pressure exceeded 145/90 mm Hg twice during repeated measurements. Art., treatment with Goldline should be suspended.
The simultaneous administration of drugs that increase the QT interval requires special attention. These drugs include histamine H1 receptor blockers (astemizole, terfenadine), antiarrhythmic drugs that increase the QT interval (amiodarone, quinidine, flecainide, mexiletine, propafenone, sotalol), cisapride, pimozide, sertindole and tricyclic antidepressants. This also applies to conditions that can lead to an increase in the QT interval, such as hypokalemia and hypomagnesemia.
The interval between taking MAO inhibitors and Goldline should be at least 2 weeks.
Although no connection has been established between taking Goldline and the development of primary pulmonary hypertension, however, given the well-known risk of drugs in this group, with regular medical monitoring it is necessary to pay special attention to symptoms such as progressive dyspnea, chest pain and swelling in the legs.
If you miss a dose of Goldline, you should not take a double dose of the drug at the next dose; it is recommended to continue taking the drug according to the prescribed regimen.
The duration of taking Goldline should not exceed 2 years.
Impact on the ability to drive vehicles and operate machinery
Taking Goldline may limit the ability to drive vehicles and operate machinery.
Goldline plus caps 10mg+158.5mg N90 (Izvarino)
Goldline® PLUS should be used only in cases where all non-drug measures for weight loss are ineffective - if the weight loss over 3 months is less than 5 kg. Treatment with Goldline® PLUS should be carried out as part of complex weight loss therapy under the supervision of a physician with practical experience in the treatment of obesity. Complex therapy includes both changing diet and lifestyle, as well as increasing physical activity. An important component of therapy is to create the prerequisites for persistent changes in eating behavior and lifestyle, which are necessary to maintain the achieved weight loss even after drug therapy is discontinued. As part of treatment with Goldline® PLUS, patients need to change their lifestyle and habits in such a way as to ensure that the achieved weight loss is maintained after completion of treatment. Patients should be clear that failure to comply with these requirements will lead to repeated weight gain and repeated visits to their doctor. Patients taking Goldline® PLUS should have their blood pressure and heart rate measured regularly. During the first 3 months of treatment, these parameters should be monitored every 2 weeks and then monthly. If during two consecutive visits an increase in resting heart rate >\000910 beats per minute or systolic/diastolic pressure > 10 mm Hg is detected. Art., it is necessary to stop treatment. In patients with arterial hypertension whose blood pressure is above 145/90 mm Hg during antihypertensive therapy. Art., this control should be carried out especially carefully and, if necessary, at shorter intervals. In patients whose blood pressure exceeded 145/90 mmHg twice during repeated measurements. Art., treatment with Goldline® PLUS should be discontinued (see section “Side Effects”). In patients with sleep apnea, blood pressure must be monitored especially carefully. The simultaneous administration of drugs that increase the QT interval requires special attention. These drugs include Hi-histamine blockers (astemizole, terfenadine); antiarrhythmic drugs that increase the QT interval (amiodarone, quinidine, flecainide, mexiletine, propafenone, sotalol); gastrointestinal motility stimulator cisapride; pimozide, sertindole and tricyclic antidepressants. This also applies to conditions that can lead to an increase in the QT interval, such as hypokalemia and hypomagnesemia (see also section “Interaction with other drugs”). The interval between taking MAO inhibitors (including furazolidone, procarbazine, selegiline) and Goldline® PLUS should be at least 2 weeks. Although a connection has not been established between taking sibutramine and the development of primary pulmonary hypertension, however, given the well-known risk of drugs in this group, with regular medical monitoring it is necessary to pay special attention to symptoms such as progressive dyspnea (breathing difficulty), chest pain and swelling in the legs . If you miss a dose of Goldline® PLUS, you should not take a double dose of the drug at the next dose; it is recommended to continue taking the drug according to the prescribed regimen. The duration of taking Goldline® PLUS should not exceed 1 year. When taking sibutramine and other serotonin reuptake inhibitors together, there is an increased risk of bleeding. In patients predisposed to bleeding or taking drugs that affect hemostasis or platelet function, sibutramine should be used with caution. Although there is no clinical evidence of addiction to sibutramine, the patient's history of drug dependence should be assessed and attention should be paid to possible signs of drug abuse. Effect on the ability to drive vehicles and machinery Taking Goldline® PLUS may limit the ability to drive vehicles and machinery. During the period of use of the drug Goldline® PLUS, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
