Universal reference book for medicines
Product name: FORSIIGA (FORXIGA )

Active ingredient: dapagliflozin

Type: Oral hypoglycemic drug

Manufacturer: ASTRAZENECA UK (UK) manufactured by ASTRAZENECA PHARMACEUTICALS LP (USA) primary packaging ASTRAZENECA UK (UK) secondary packaging and quality control manufacturer ASTRAZENEKA INDUSTRIES (Russia)

The tablets covered with a film cover of yellow color, round, biconcave, with engraving "5" on one side and "1427" on the other side.

1 tab.

dapagliflozin propanediol monohydrate 6.15 mg,

which corresponds to the content of dapagliflozin 5 mg

Excipients: microcrystalline cellulose - 85.725 mg, anhydrous lactose - 25 mg, crospovidone - 5 mg, silicon dioxide - 1.875 mg, magnesium stearate - 1.25 mg.

The composition of the shell: Opadrai ® II yellow - 5 mg (polyvinyl alcohol partially hydrolysed - 2 mg, titanium dioxide - 1.177 mg, macrogol 3350 - 1.01 mg, talc - 0.74 mg, iron oxide oxide yellow - 0.073 mg).

10 pieces.
- blisters perforated from aluminum foil (3) - packs of cardboard with control of the first opening.
The tablets covered with a film membrane of yellow color, rhomboid, biconcave, with an engraving "10" on one side and "1428" on the other side.

1 tab.

dapagliflozin propanediol monohydrate 12.3 mg,

which corresponds to the content of dapagliflozin 10 mg

Excipients: microcrystalline cellulose - 171.45 mg, anhydrous anhydrous - 50 mg, crospovidone - 10 mg, silicon dioxide - 3.75 mg, magnesium stearate - 2.5 mg.

Sheath composition: Opadrai ® II yellow - 10 mg (polyvinyl alcohol partially hydrolysed - 4 mg, titanium dioxide - 2.35 mg, macrogol 3350 - 2.02 mg, talc - 1.48 mg, iron oxide oxide yellow - 0.15 mg).

10 pieces.
- blisters perforated from aluminum foil (3) - packs of cardboard with control of the first opening.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Oral hypoglycemic drug.

Mechanism of action

Dapagliflozin is a potent (inhibition constant (K i ) 0.55 nM), a selective reversible inhibitor of the sodium-glucose cotransporter of the second type (SGLT2).
SGLT2 is selectively expressed in the kidneys and is not found in more than 70 other body tissues (including liver, skeletal muscle, adipose tissue, mammary glands, bladder and brain). SGLT2 is the primary carrier involved in the process of glucose reabsorption in the renal tubules. Reabsorption of glucose in the renal tubules in patients with type 2 diabetes mellitus (DM 2) continues despite hyperglycemia. By inhibiting the kidney transference of glucose, dapagliflozin reduces its reabsorption in the renal tubules, which leads to the excretion of glucose by the kidneys. The effect of dapagliflozin is to reduce fasting and post-prandial glucose and reduce the concentration of glycosylated hemoglobin in patients with diabetes.
Excretion of glucose (glucosuric effect) is observed after the first dose of the drug, remains for the next 24 hours and continues throughout the therapy.
The amount of glucose released by the kidney due to this mechanism depends on the concentration of glucose in the blood and on the glomerular filtration rate (GFR). Dapagliflozin does not interfere with the normal production of endogenous glucose in response to hypoglycemia. The effect of dapagliflozin is independent of insulin secretion and insulin sensitivity. In clinical studies of the drug Forsig , there was an improvement in the function of? -cells (HOMA test, homeostasis model assessment).
The excretion of glucose by the kidneys, caused by dapagliflozin, is accompanied by a loss of calories and a decrease in body weight.
Inhibition of sodium-glucose cotransport by dapagliflozin is accompanied by weak diuretic and transient natriuretic effects.
Dapagliflozin has no effect on other glucose transporters carrying glucose to peripheral tissues, and exhibits more than 1400 times greater selectivity for SGLT2 than for SGLT1, the main transporter of the intestine responsible for glucose uptake.

Pharmacodynamics

After taking dapagliflozin by healthy volunteers and patients with CD2, there was an increase in the number of glucose output by the kidneys.
When receiving dapagliflozin at a dose of 10 mg / day for 12 weeks, in patients with CD2, approximately 70 g of glucose / foot was excreted by the kidneys (which corresponds to 280 kcal / day). In patients with CD2, who took dapagliflozin at a dose of 10 mg / day for a long time (up to 2 years), the excretion of glucose was maintained throughout the course of therapy.
Excretion of glucose by the kidneys with dapagliflozin also leads to osmotic diuresis and an increase in the volume of urine.
The increase in urine volume in patients with DM2, who took dapagliflozin at a dose of 10 mg / day, was maintained for 12 weeks and was approximately 375 ml / day. The increase in the volume of urine was accompanied by a small and transient increase in the excretion of sodium by the kidneys, which did not lead to a change in the concentration of sodium in the blood serum.
A planned analysis of the results of 13 placebo-controlled trials demonstrated a 3.7 mmHg decrease in systolic blood pressure (SBP).
and diastolic blood pressure (DBP) by 1.8 mm Hg. at the 24th week of therapy with dapagliflozin at a dose of 10 mg / day compared with a decrease in SBP and DBP by 0.5 mm Hg. in the placebo group. A similar decrease in blood pressure was observed during 104 weeks of treatment.
When using dapagliflozin at a dose of 10 mg / day in patients with diabetes mellitus with inadequate control of glycemia and arterial hypertension receiving angiotensin II receptor blockers, ACE inhibitors, incl.
in combination with another antihypertensive drug, there was a decrease in glycosylated hemoglobin by 3.1% and a decrease in SBP by 4.3 mm Hg. after 12 weeks of therapy compared with placebo.
PHARMACOKINETICS

Suction

After ingestion, dapagliflozin is rapidly and completely absorbed from the digestive tract and can be taken either during meals or outside it.
C max of dapagliflozin in blood plasma is usually achieved within 2 hours after taking an empty stomach. The C max and AUC values ​​increase in proportion to the dose of dapagliflozin.Absolute bioavailability of dapagliflozin when taken in a dose of 10 mg is 78%. The intake of food had a moderate effect on the pharmacokinetics of dapagliflozin in healthy volunteers. A high-fat meal reduced C max of dapagliflozin by 50%, lengthened T max in plasma by about 1 h, but did not affect AUC as compared to fasting.These changes are not clinically relevant.
Distribution

The binding of dapagliflozin to plasma proteins is approximately 91%.
In patients with various diseases, for example, with impaired renal or hepatic function, this indicator did not change.
Metabolism

Dapaglyflozin is a C-linked glucoside whose aglycone is linked to glucose by a carbon-carbon bond, which ensures its resistance to glucosidases.
Dapagliflozin is metabolized with the formation of a mainly inactive metabolite of dapagliflozin-3-O-glucuronide.
After ingestion of 50 mg of 14 C-dapagliflozin, 61% of the dose is metabolized to dapagliflozin-3-O-glucuronide, which accounts for 42% of the total plasma radioactivity (AUC 0-12 h ).
The unchanged drug accounts for 39% of the total plasma radioactivity. The fractions of the other metabolites separately do not exceed 5% of the total plasma radioactivity. Dapaglyflozin-3-O-glucuronide and other metabolites do not have a pharmacological effect. Dapagliflozin-3-O-glucuronide is formed by the enzyme uridine-diphosphate-glucuronosyltransferase 1A9 (UGT1A9), present in the liver and kidneys, cytochrome CYP isoenzymes are less involved in metabolism.
Excretion

The mean T 1/2 from the plasma in healthy volunteers was 12.9 hours after a single dose of dapagliflozin inside at a dose of 10 mg.
Dapagliflozin and its metabolites are excreted mainly by the kidneys, and only less than 2% is excreted unchanged. After taking 50 mg of 14 C-dapagliflozin, 96% of the radioactivity was detected-75% in urine and 21% in feces. Approximately 15% of the radioactivity found in the feces was due to unchanged dapagliflozin.
Pharmacokinetics in special clinical cases

Patients with impaired renal function.
In the equilibrium state (mean AUC), the systemic exposure of dapagliflozin in patients with diabetes mellitus and renal failure of mild, moderate or severe degree (defined by the clearance of yogexol) was 32%, 60% and 87% higher than in patients with DM2 and normal function kidneys, respectively. The amount of glucose excreted by the kidneys during the day when dapagliflozin was taken in an equilibrium state depended on the state of kidney function. In patients with CD2 and normal renal function, and with mild, moderate or severe renal insufficiency, 85, 52, 18 and 11 g of glucose, respectively, were excreted per day, respectively. There were no differences in the binding of dapagliflozin to proteins in healthy volunteers and in patients with renal insufficiency of varying severity. It is not known whether hemodialysis affects the exposure of dapagliflozin.
Patients with impaired liver function.
In patients with mild to moderate hepatic insufficiency, the average C max and AUC of dapagliflozin were respectively 12% and 36% higher compared to healthy volunteers. These differences are not clinically significant, so adjustments to the dose of dapagliflozin in mild to moderate hepatic insufficiency are not required. In patients with severe hepatic insufficiency (Child-Pugh class C), the mean C max and AUC of dapagliflozin were 40% and 67% higher, respectively, compared to healthy volunteers.
Patients of advanced age (? 65 years).
There was no clinically significant increase in exposure in patients under the age of 70 (unless other factors other than age were taken into account). Nevertheless, we can expect an increase in exposure due to a decrease in kidney function associated with age. Data on exposure in patients over the age of 70 years are insufficient.
Floor.
In women, the average value of AUC in the equilibrium state is 22% higher than in men.
Race affiliation.
Clinically significant differences in systemic exposure among representatives of the Caucasoid, Negroid and Mongoloid races have not been revealed.
Body mass.
Lower values ​​of exposure at increased body weight were noted. Therefore, in patients with low body weight, there may be some increase in exposure, and in patients with increased body weight, a decrease in the exposure of dapagliflozin. However, these differences are not clinically relevant.
INDICATIONS

Diabetes mellitus type 2 in addition to diet and exercise to improve glycemic control as:

- monotherapy;

- additions to the therapy of metformin, sulfonylurea derivatives (including in combination with metformin), thiazolidinediones, inhibitors of dipeptidyl peptidase 4 (DPP-4) (including in combination with metformin), insulin preparations (incl. in combination with one or two hypoglycemic preparations for oral administration) in the absence of adequate glycemic control in this therapy;

- starting combination therapy with metformin, if this therapy is appropriate.

DOSING MODE

The drug is taken orally, regardless of food intake.

Monotherapy: the recommended dose of the drug Forsig is 10 mg 1 time / day.

Combination therapy: The recommended dose of the drug Forsig is 10 mg 1 time / day in combination with metformin, sulfonylurea derivatives (including in combination with metformin), thiazolidinediones, DPP-4 inhibitors (including in combination with metformin ), insulin preparations (including in combination with one or two hypoglycemic drugs for oral administration).

In order to reduce the risk of hypoglycemia when co-prescribing Forsig with insulin preparations or preparations that increase insulin secretion (for example, with the sulfonylurea derivative), it may be necessary to reduce the dose of insulin preparations or preparations that increase insulin secretion.

Initial combination therapy with metformin: the recommended dose of the drug Forsiga is 10 mg 1 time / day, the dose of metformin is 500 mg 1 time / day.
In case of inadequate glycemic control, the dose of metformin should be increased.
If the liver function is mild or moderate, there is no need to adjust the dose of the drug.
Patients with severe liver dysfunction are recommended an initial dose of 5 mg. With good tolerability, the dose can be increased to 10 mg.
The effectiveness of dapagliflozin depends on the function of the kidneys.
In patients with impaired renal function of moderate severity, the effectiveness of treatment is reduced, and in patients with severe disorders - most likely, there is no. The drug Forsig ™ is contraindicated in patients with moderate to severe renal insufficiency (CC <60 mL / min or GFR <60 mL / min / 1.73 m 2 ) or with terminal renal failure . With violations of the function of the kidneys of an easy degree, dose adjustment is not required.
The safety and effectiveness of dapagliflozin in children and adolescents under the age of 18 years has not been studied.

In elderly patients, dose adjustment is not required.
However, when choosing a dose, it should be borne in mind that in this category of patients, kidney dysfunction and the risk of a reduction in BCC are more likely. Since the clinical experience of using the drug in patients aged 75 years and older is limited, it is contraindicated to start therapy with dapagliflozin in this age group.
SIDE EFFECT

A pre-planned analysis of the pooled data included the results of 12 placebo-controlled studies in which 1,193 patients took dapagliflozin at a dose of 10 mg and 1,393 patients received a placebo.

The overall incidence of adverse events (short-term therapy) in patients taking dapagliflozin at a dose of 10 mg was similar to that in the placebo group.
The number of adverse events that led to the abolition of therapy was small and balanced between treatment groups. The most frequent adverse events leading to the abolition of 10 mg of dapagliflozin therapy were an increase in creatinine concentration in the blood (0.4%), urinary tract infection (0.3%), nausea (0.2%), dizziness (0.2%) and rash (0.2% ). One patient who took dapagliflozin noted the development of an undesirable phenomenon on the part of the liver with a diagnosis of drug-induced hepatitis and / or autoimmune hepatitis.
The most common adverse reaction was hypoglycemia, the development of which depended on the type of basic therapy used in each study.
The incidence of episodes of mild hypoglycemia was similar in treatment groups, including placebo.
Below are the undesirable reactions observed in placebo-controlled clinical trials.
None of them depended on the dose of the drug. The frequency of unwanted reactions is presented in the following gradation: very often (? 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10 000, <1/1000), very rarely (<1/10 000) and unspecified frequency (can not be estimated from the received data).
Undesirable reactions in placebo-controlled trials a

Very often Often * Uncommon **

Infections and invasions

Vulvovaginitis, balanitis and similar infections of the genitals b, c Urinary tract infection b Vulvovaginal itching

From the side of metabolism

Hypoglycemia (when used in combination with a sulfonylurea derivative or insulin) b Reduction of bcc b, c Thirst

From the digestive system

Constipation

From the skin and subcutaneous tissues

Increased sweating

From the musculoskeletal system

Backache

From the urinary system

Dysuria Polyuria d Nicturia

Laboratory and instrumental data

Dyslipidemia f Increase in hematocrit g Increase in the concentration of creatinine in the blood Increase in the concentration of urea in the blood

a The table shows the application data for the drug up to 24 weeks (short-term therapy), regardless of the use of an additional hypoglycemic drug.

b See the relevant subsection below for more information.

c Vulvovaginitis, balanitis and similar infections of the genitals include, for example, the following predefined preferred terms: vulvovaginal fungal infection, vaginal infection, balanitis, fungal genital infection, vulvovaginal candidiasis, vulvovaginitis, candidal balanitis, genital candidiasis, genital infection, genital infection organs in men, infection of the penis, vulvitis, bacterial vaginitis, abscess of the vulva.

d Polyuria includes the preferred terms: pollakiuria, polyuria, and diuresis.

e Reduction of BCC includes, for example, the following predefined preferred terms: dehydration, hypovolemia, arterial hypotension.

f The mean change in the following values ​​as a percentage of baseline values ​​in the 10 mg dapagliflozin group and placebo group, respectively, was: total cholesterol 1.4% vs. -0.4%;
HDL cholesterol 5.5% compared with 3.8%; Cholesterol-LDL 2.7% compared with -1.9%; triglycerides -5.4% compared to -0.7%.
g Mean changes in hematocrit values ​​from baseline were 2.15% in the 10-mg dapagliflozin group versus -0.40% in the placebo group.

* Are they marked?
2% of patients who took dapagliflozin at a dose of 10 mg, and ≥ 1% more often than in the placebo group.
** Are they marked?
0.2% of patients and 0.1% more often and more patients (at least 3) in the 10 mg dapagliflozin group compared to the placebo group, regardless of the use of an additional hypoglycemic drug.
Description of individual adverse reactions

Hypoglycaemia

The frequency of hypoglycaemia depended on the type of base therapy used in each study.
In studies dapagliflozin as monotherapy, combination therapy with metformin up to 102 weeks, incidence of mild hypoglycemia episodes were similar (<5%) in treatment groups including placebo. In all studies, episodes of severe hypoglycemia observed infrequently, and their rates were comparable between the group of dapagliflozin and placebo.
The decrease in the bcc
Adverse reactions associated with a decrease in the bcc (including messages of dehydration, hypovolemia or hypotension) were observed in 0.8% and 0.4% of patients treated with dapagliflozin 10 mg and placebo, respectively; severe reactions were reported in <0.2% of patients, and they were comparable in groups of dapagliflozin 10 mg and placebo.
Vulvovaginitis, balanitis and genital infections such
Vulvovaginitis, balanitis and the like genital infections were observed in 4.8% and 0.9% of patients treated with dapagliflozin 10 mg and placebo, respectively. Most infections were mild to moderate; initial course of standard therapy was effective, and therefore patients rarely stops receiving dapagliflozin. These infections usually develop in women (6.9% and 1.5% with dapagliflozin and placebo, respectively), and in patients with such infections in a history they often recur.
Urinary tract infections
Urinary tract infections are more marked in the application dapagliflozin 10 mg than for placebo (4.3% compared to 3.7% respectively). Most infections were mild to moderate; initial course of standard therapy was effective, and therefore patients rarely discontinued use of dapagliflozin. These infections usually develop in women, and in patients with such infections in a history they often recur.
Parathyroid hormone (PTH)
noted a slight increase PTH concentration in blood serum, and to a greater degree in patients with higher baseline PTH concentrations. Study of bone mineral density in patients with normal renal function or mild violation of renal function showed no bone loss within one year of therapy.
Malignant tumors
In clinical studies, the overall proportion of patients with malignant tumors or unspecified was similar in group dapagliflozin (1.47%) and the placebo group / reference drug (1.35%). According to studies in animal drug showed no mutagenic or carcinogenic properties. When considering the incidence of tumors of various organ systems, the relative risk associated with dapagliflozin, was higher than 1 for some tumors (bladder, prostate, mammary gland), and less than 1 for the other (e.g., blood and lymphatic system, ovaries, urinary system) generally without increasing the cancer risk associated with dapagliflozin. Increase / decrease the risk was not statistically significant for any of the organ systems. Given the lack of preclinical data on the development of tumors,as well as a short latency period between the first drug exposure and tumor diagnosis, causal relationship is assessed as unlikely.
Because numerical imbalance of breast tumors, bladder and prostate cancer needs special attention, the study of this issue will continue in the framework of post-marketing studies.
Elderly patients (? 65 years)
Adverse reactions associated with impaired renal function or renal insufficiency, reported in 2.5% of patients receiving dapagliflozin, and in 1.1% of patients receiving placebo, in patients aged ≥ 65 years. The most common adverse reactions associated with impaired renal function, was to increase the concentration of creatinine in serum. The majority of these reactions were transient and reversible. Among patients aged ≥ 65 years of decline in BCC, the most frequently reported as arterial hypotension was seen in 1.5% and 0.4% of patients taking dapagliflozin and placebo, respectively.
CONTRAINDICATIONS

- type 1 diabetes;
- diabetic ketoacidosis;
- kidney failure secondary to severe (GFR <60 mL / min / 1.73 m 2 ) or end-stage renal failure;
- hereditary lactose intolerance, lactase deficiency and glucose-galactose intolerance;
- Pregnancy;

- the period of breastfeeding;

- Children and teens under 18 years of age (safety and efficacy have not been studied);
- Patients taking "loop" diuretics, bcc or reduced, e.g., due to acute diseases (such as gastrointestinal diseases);
- elderly patients aged 75 years and older (for the start of therapy);
- Individual hypersensitivity to any component of the formulation.
Precautions: hepatic failure, severe, infections of the urinary system, reducing the risk of BCC, patients of advanced age, chronic heart failure, increased hematocrit value.
PREGNANCY AND LACTATION

Due to the fact that the use of dapagliflozin in pregnancy has not been studied, the drug is contraindicated in these patients. In the case of diagnosing pregnancy dapagliflozin therapy should be discontinued.
It is unknown whether dapagliflozin and / or its inactive metabolites in breast milk. It is impossible to eliminate the risk to newborns / infants. Dapagliflozin is contraindicated during breast-feeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

When violations of mild renal function is not necessary to adjust the dose of the drug.
Preparation Forsiga is contraindicated in patients with renal failure secondary to severe (creatinine clearance <60 mL / min or a GFR <60 mL / min / 1.73 m 2 ) or end-stage renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

When liver function disorders mild or moderate severity no need to adjust the dose.
Be wary of patients with severe liver failure, it recommended initial dose of 5 mg. With good tolerance dose can be increased to 10 mg.
APPLICATION FOR CHILDREN

Contraindicated use of the drug for children and adolescents under the age of 18 years.

APPLICATION IN ELDERLY PATIENTS

In elderly patients there is no need to adjust the dose of the drug. However, when choosing the dose should be borne in mind that these patients are more likely to impaired renal function and reduce the risk of BCC.
Since clinical experience with the drug in patients 75 years and older is limited, start dapagliflozin therapy is contraindicated in this age group.
SPECIAL INSTRUCTIONS

The use in patients with impaired renal function
Efficiency dapagliflozin depends on renal function, and this efficiency is reduced in patients with renal insufficiency moderate and probably absent in patients with impaired renal function, severe. Among patients with renal moderate impairment (creatinine clearance <60 mL / min or estimated GFR <60 mL / min / 1.73 m 2 ), have a greater proportion of patients treated with dapagliflozin, marked increase of the concentration of creatinine, phosphorus, PTH, and hypotension than in patients treated with placebo. Preparation Forsiga is contraindicated in patients with renal failure secondary to severe (creatinine clearance <60 mL / min or estimated GFR <60 mL / min / 1.73 m 2 ). The drug Forsiga not studied in renal failure severe (creatinine clearance <30 mL / min or estimated GFR <30 mL / min / 1.73 m 2 ) or end-stage renal failure.
It is recommended to monitor renal function as follows:
- prior to initiating therapy dapagliflozin and at least 1 time a year later;
- before the beginning of reception of concomitant medications that may decrease renal function, and periodically thereafter;
- with impaired renal function, close to moderate severity, at least 2-4 times per year. By reducing kidney function values below CC <60 ml / min or estimated GFR <60 mL / min / 1.73 m 2 , it is necessary to stop taking dapagliflozin.
The use in patients with impaired liver function
in clinical trials limited data obtained of the drug in patients with impaired liver function. Exposure increased dapagliflozin in patients with impaired liver function severe.
Use in patients with BCC risk reduction of arterial hypotension and / or electrolyte imbalance
in accordance with dapagliflozin mechanism of action enhances diuresis, accompanied by a slight decrease in blood pressure. The diuretic effect may be more pronounced in patients with a very high concentration of blood glucose.
Dapagliflozin contraindicated in patients receiving "loop" diuretics, or patients with reduced BCC, for example because of acute diseases (such as gastrointestinal diseases).
Caution must be exercised in patients for whom reduction of blood pressure caused dapagliflozin may present a risk, such as patients with cardiovascular diseases in history, in patients with a history of arterial hypertension receiving antihypertensive therapy, or in elderly patients.
When receiving dapagliflozin recommended careful monitoring of BCC and electrolyte concentration (e.g., physical examination, blood pressure measurement, laboratory tests, including hematocrit) against comorbid conditions that may lead to a decrease in the BCC. When reducing the BCC recommended temporary discontinuation of dapagliflozin to correct this condition.
ketoacidosis
When applying the drug post-marketing reports of ketoacidosis, including diabetic ketoacidosis, patients with diabetes mellitus type 1 and 2 taking the drug Forsiga and other SGLT2 inhibitors, although a causal relationship has not been established. Preparation Forsiga is not indicated for patients with type 1 diabetes.
Taking the drug Forsiga patients with signs and symptoms suggestive of ketoacidosis, including nausea, vomiting, abdominal pain, malaise and dyspnea, check for the presence of ketoacidosis, even when blood glucose concentration below 14 mmol / l. For suspected ketoacidosis should consider repealing or suspending the use of the drug Forsiga and to conduct examination of the patient immediately.
Factors that predispose to the development of ketoacidosis include low functional activity of? -cells due to dysfunction of the pancreas (e.g., type 1 diabetes, pancreatitis or pancreatic surgery history), a reduced dose of insulin, reducing caloric intake or increased need for insulin due to infections, diseases or surgery, as well as alcohol abuse. The drug Forsiga ® should be used with caution in these patients.
Urinary tract infection
In the analysis of the combined application of these dapagliflozin to 24 weeks Urinary tract infections are more marked in the application dapagliflozin 10 mg compared with placebo. Development of pyelonephritis rarely observed with similar frequency in the control group. Excretion of glucose by the kidneys may be accompanied by an increased risk of urinary tract infections, so the treatment of pyelonephritis or urosepsis should consider temporary discontinuation dapagliflozin.
Urosepsis and pyelonephritis. When applying the drug post-marketing reports of severe infections of the urinary tract, including urosepsis and pyelonephritis requiring hospitalization of patients taking the drug Forsiga and other SGLT2 inhibitors. SGLT2 inhibitors therapy increases the risk of urinary tract infections. Patients should be observed for signs and symptoms of urinary tract infections and, when indicated, to seek treatment.
Elderly patients

Elderly patients are more likely impaired renal function and / or the use of antihypertensive drugs that may affect kidney function such as ACE inhibitors and angiotensin II receptor antagonists, type 1 (ARA). For elderly patients apply the same recommendations with impaired renal function, as well as for all patient populations.
In the group of patients aged ≥65 years of age have a greater proportion of patients treated with dapagliflozin, developed adverse reactions associated with impaired renal function or renal failure as compared to placebo. The most common adverse reactions associated with impaired renal function, was to increase the concentration of creatinine in the blood serum, the majority of cases were transient and reversible.
Elderly patients reduce the risk of BCC can be higher and more likely diuretics. In greater proportion of patients aged ≥65 years of age treated with dapagliflozin, observed adverse reactions associated with a decrease in BCC.
Experience with the drug in patients aged 75 years and older is limited. Contraindicated start dapagliflozin therapy in this population.
Chronic heart failure
experience of the drug in patients with chronic heart failure NYHA III FC on the labeling is limited and in clinical trials dapagliflozin not been used in patients with chronic heart failure FC III-IV of NYHA.
Increasing hematocrit values
In the application of dapagliflozin was an increase in hematocrit, and therefore caution should be exercised in patients with elevated hematocrit value.
Assessment urinalysis results
Due to the mechanism of action of the drug results of urine tests for glucose in patients taking the drug Forsiga , will be positive.
Effect on the determination of 1,5-angidroglyutsitola
Qualification glycemic control by determining 1,5-angidroglyutsitola not recommended as 1,5-angidroglyutsitola measurement is an unreliable method for patients taking SGLT2 inhibitors. Alternative methods should be used to assess glycemic control.
Impact on the ability to drive vehicles and manage mechanisms

Studies on the effect of dapagliflozin on the ability to drive vehicles and mechanisms conducted.
OVERDOSE

Dapagliflozin safe and well tolerated by healthy volunteers in single doses up to admission to 500 mg (50 times the recommended dose). Glucose was determined in urine after dosing (at least for 5 days after a dose of 500 mg), with no cases of dehydration identified, hypotension, electrolyte imbalance, clinically significant effect on the interval QT c . The frequency of hypoglycaemia was similar to the rate for placebo. In clinical studies in healthy volunteers and patients with type 2 diabetes treated with a preparation singly in doses up to 100 mg

The information is provided for your information, do not self-medicate, it is dangerous for your health.

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