Universal reference book for medicines
Product name: NAKLOFEN PROTECT (NAKLOFEN PROTECT)

Active substance: diclofenac, lansoprazole

Type: NSAIDs

Manufacturer: КРКА-РУС (Russia)
Composition, form of production and packaging
Capsules with prolonged release
number 2, capsule body white, cap of blue color;
the contents of the capsules are pellets, coated with an enteric coating, and pellets of prolonged release from white to cream color.
1 caps.

diclofenac sodium 75 mg

Capsules enteric -soluble № 3, capsule body white, cap of red-brown color;
the contents of capsules - pellets from white to white with a slightly yellowish or slightly pink tinge of color.
1 caps.

lansoprazole 15 mg

10 pieces.
(5 + 5) - packings of cellular contour (2) - packs cardboard.
10 pieces.
(5 + 5) - packings of cellular contour (4) - packs cardboard.
10 pieces.
(5 + 5) - packings the cellular contour (6) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Diclofenac is a non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid.
Has anti-inflammatory, analgesic, antipyretic and antiplatelet effect.Inappropriately inhibiting cycloxygenase 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) in the inflammatory focus, suppresses the exudative and proliferative phases of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the joint condition.
Lansoprazole is a drug from the proton pump inhibitor group.
Does not exhibit antiploneergic or antihistaminic properties, binds specifically to H + / K + -ATPase (also called a proton pump) on the secretory surface of parietal cells of the stomach and prevents the final stage of secretion of gastric juice.
Lansoprazole reduces basal, day and night secretion of gastric juice, which prevents food-stimulated gastric juice secretion and increased secretion caused by other factors such as gastrin and pentagastrin, and also prevents insulin-induced increase in gastric acid volume and acidity.
Reduces the acidity of gastric juice and the length of time during which the pH value> 4. The effect is proportional to the dose value.
After discontinuing therapy with lansoprazole.
The pH of the gastric juice decreases gradually and returns to normal within 2-4 days. There were no cases of a significant increase in secretion of gastric juice after discontinuation of treatment.
Lansoprazole increases the activity of pepsinogen in the serum and lowers the activity of pepsin below the basal values ​​after stimulation with food.

During treatment with lansoprazole.
the average activity of gastrin in the blood serum increases 1.5-2 times. The concentration rises during the first 8 weeks of treatment, after which it reaches the plateau and at the end of therapy after 4 weeks to the initial values.
PHARMACOKINETICS

Absorption

Absorption - fast and complete, the poor slows the absorption rate.
The maximum concentration is noted 30-60 minutes after ingestion. The concentration in the blood plasma is linear depending on the amount of oral dose. Changes in the pharmacokinetics of diclofenac against a background of repeated use are not noted.Bioavailability - 50%.
Distribution

Do not cumulate while respecting the recommended interval between doses.
The connection with plasma proteins is more than 99% (most of it is associated with albumins).
Metabolism

50% is metabolized during the "first pass" effect through the liver.
Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The isoenzyme CYP2C9 also participates in the metabolism of diclofenac. The pharmacological activity of metabolites is lower than that of diclofenac.
Elimination

Systemic clearance is 260 ml / min.
T 1/2 from the blood plasma - 2h. Excretion from the synovial fluid is slower than from the plasma. 70% of the administered dose is excreted as metabolites through the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile. In patients with severe renal dysfunction, excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood. In patients with chronic hepatitis or compensated liver cirrhosis, pharmacokinetic parameters are the same as in patients without liver disease. Diclofenac penetrates into breast milk.
Lansoprazole

Absorption

Absorption is high, bioassayability is 80%.
Eating lowers absorption and bioavailability (50%), but the inhibitory effect on gastric secretion remains the same, regardless of food intake. The maximum concentration (0.75-1.15 mg / l) is 1.7 hours. The maximum plasma concentration and the area under the concentration / time curve (AUC) are approximately proportional to the accepted dose of the drug.
Distribution

Cumulation does not occur.
The connection with plasma proteins is 97%. Good penetrates into tissues, incl. in the lining cells of the gastric mucosa. The volume of distribution is 0.5 l / kg.
Metabolism

Actively metabolized at the "first pass" through the liver with the participation of isofermite CYP2C19 with the formation of sulfonyl, sulfone and hydroxy derivatives.
Ishibition of the activity of CYP2C19.
Elimination

T 1/2 of lansoprazole for less than 2 hours and does not reflect the duration of suppression of gastric juice secretion.
If there is a violation of liver function T 1/2 , it increases 3-4 times. Lansoprazole is excreted as metabolites; approximately one third of lansoprazole is excreted by the kidneys and two-thirds - with bile through the intestine (renal failure is not significantly affected by the rate of excretion).
INDICATIONS

Symptomatic therapy of inflammatory and degenerative diseases of the musculoskeletal system in patients with the risk of developing gastric ulcers and / or duodenal ulcers associated with the use of PPVP:

- rheumatoid arthritis;

- psoriatic arthritis;

juvenile chronic arthritis;

ankylosing spondylitis (Bekhterev's disease);

- gouty arthritis;

- rheumatic soft tissue damage;

- osteoarthrosis of peripheral joints and spine, including with radicular syndrome;

- Tendovaginitis;

bursitis.

DOSING MODE

The kit is designed for combined intake of two kinds of capsules.
Separate application of diclofenac capsules is possible only in the absence of ulcerative lesions of the stomach and / or duodenum and the risks of its development.
Diclofenac

Inside, squeezed a small amount of liquid, during or immediately after a meal.
The initial dose is 1 capsule (75 mg) once a day. The maximum daily dose is 2 capsules / day (150 mg). At the expressed painful syndrome, it is possible to accept at once a daily dose of a preparation (2 capsules 1 time a day). In case of erosive-ulcerative lesions of the mucous membrane of the stomach or duodenum, one capsule (75 mg) per day should be limited to no more than 8 weeks.
Lansoprazole

Inside, whole, preferably in the morning, before eating.

The initial dose is 15 mg / day (1 capsule).
The maximum dose is 30 mg / day (2 capsules). In case of erosive-ulcerative lesions of the mucous membrane of the stomach or duodenum, 30 mg / day (2 capsules) should be used. Elderly patients, as well as patients with impaired renal and / or liver function, do not need dose adjustment.
If it is impossible to swallow the capsule entirely, it must be opened, the contents mixed with a small amount of apple juice and swallowed without chewing.

The same actions are possible if the substance is injected through a nasogastric tube.
Duration of dose 30 mg / day (2 capsules) not more than 8 weeks. A dose of 15 mg / day (1 capsule) can be used up to 12 months.
SIDE EFFECT

Classification of the incidence of side effects recommended by the World Health Organization (WHO):

Very often (from? 1/10)

Often (from? 1/100 to <1/10)

Infrequently (from? 1/1000 to <1/100)

Rarely (from? 1/10000 to <1/1000)

Very rarely (from <1/10000)

Frequency is unknown (can not be estimated from available data)

Diclofenac

From the digestive system:

often: enigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases;

rarely: gastritis, proctitis, bleeding from the digestive tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function;

very rarely: stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis;

From the nervous system:

often: headache, dizziness;

rarely: drowsiness;

very rarely: a violation of sensitivity (including paresthesia), memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders;

From the sense organs:

often: vertigo;

very rarely: visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disorders;

From the urinary system:

very rarely: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis;

From the hematopoiesis:

very rarely: thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis;

Allergic reactions:

Very rarely: angioedema (including faces), anaphylactic / anaphylactoid reactions, including severe BP depression and shock;

From the cardiovascular system:

very rarely: palpitation, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction;

From the respiratory system:

rarely: exacerbation of bronchial asthma (including dyspnea);

very rarely: pneumonitis;

From the skin:

often: skin rash;

rarely: urticaria;

very rarely: bullous rash, erythema, incl.
multiform and Stevens-Johnson syndrome. Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
Lansoprazole

From the digestive system:

often: constipation;

infrequently: abdominal pain, diarrhea, nausea, dryness of the oral mucosa, dyspepsia, taste disorders, flatulence;

very rarely: colitis, ulcerative colitis, candidiasis of the gastrointestinal tract, increased activity of "liver" enzymes, hyperbilirubinemia;

rarely: jaundice, hepatitis;

From the nervous system:

often: headache;

infrequently: dizziness, anxiety, fear, confusion, depression, confusion;

From the respiratory system:

rarely: cough, pharyngitis, rhinitis, upper respiratory tract infection, flu-like syndrome;

On the part of the hematopoiesis system:

very rarely: leukopenia, thrombocytopenia, eosinophilia, pancytopenia or agranulocytosis;

Allergic reactions:

rarely: urticaria, angioedema, photosensitization;
very rare: anaphylactic reactions;
Metabolic and nutritional disorders:

rarely: anorexia, increased appetite;

From the sense organs:

very rarely: visual impairment (blurred vision), tinnitus;

From the skin:

often: skin rash;

rarely: purpura, petechiae, hair loss;

very rarely: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme;

From the musculoskeletal system:

rarely: pain in the joints, muscles and bones;

From the genitourinary system:

infrequently: increased concentration of creatinine;

very rarely: interstitial nephritis, renal failure, urogenital disorders, impotence, gynecomastia;

Other:

infrequently: feeling tired;

very rarely: peripheral edema;

CONTRAINDICATIONS

- hypersensitivity to the components of the drug (including other NSAIDs);

- complete or incomplete combination of bronchial asthma, recurrent polyposis of the mucous membrane of the nasal cavity.
paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);
- Inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation;

- condition after aortocoronary shunting;

- active gastrointestinal hemorrhage;

- pregnancy, the period of breastfeeding;

- heart failure in the stage of decompensation;

- violation of hematopoiesis, violation of hemostasis (including hemophilia);

- severe hepatic impairment or active liver disease;

- renal failure (QC less than 30 ml / min), progressive kidney disease, hyperkalemia;

- deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption;

- Children under 18 years.

With caution: erosive and ulcerative lesions of the mucous membrane of the stomach or duodenum (diclofenac applied only in the case of a careful evaluation of the need for use, at a dose of not more than 75 mg / day), malignant neoplasms of the gastrointestinal tract.

Anamnestic data on the development of gastrointestinal ulcer, the presence of Helicobacter pylori infection, advanced age, long-term use of NSAIDs, alcoholism, severe physical illness.

Anemia, bronchial asthma, cerebrovascular disease, coronary artery disease, hypertension, peripheral arterial disease, edematous syndrome, hepatic and / or renal insufficiency (CK 30-60 ml / min), history of liver disease, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, a significant decrease in BCC (including after extensive surgery), induced porphyria, diverticulitis, systemic connective tissue diseases.

Simultaneous administration of glucocorticosteroids (for example, prednisolone), anticoagulants (eg, warfarin), antiplatelet agents (eg, acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

PREGNANCY AND LACTATION

Application of the drug Naklofen Protect (kit) is contraindicated during pregnancy and during breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe hepatic insufficiency or active liver disease.

APPLICATION FOR CHILDREN

Contraindicated for children under 18 years.

SPECIAL INSTRUCTIONS

Long-term use of diclofenac can very rarely cause serious undesirable effects on the part of the liver, which requires periodic monitoring of "hepatic" enzymes.

In infectious diseases, the anti-inflammatory and antiniretic effects of diclofenac should be taken into account, as they can lubricate the clinical picture of the diseases.

When performing long-term therapy, it is necessary to monitor the picture of peripheral blood, the analysis of feces for latent blood.

In connection with the negative effect on fertility, women planning pregnancy, the drug is not recommended.

Like all medicines, diclofenac should be used in elderly patients in a minimally effective dose.

Symptomatic improvement during therapy with lansoprazole does not exclude the possible development of neoplasms in the digestive tract.
Care should be taken in the sudden occurrence or worsening of dyspeptic symptoms, especially in patients older than 45 years.
Cardiovascular and cerebrovascular effects

The use of diclofenac, especially at high doses (150 mg / day), may cause a slight increase in the risk of developing arterial thrombosis (eg, myocardial infarction or stroke).

Patients with uncontrolled hypertension, chronic heart failure, ischemic heart disease, peripheral vascular injury, and / or cerebrovascular disorders should take diclofenac only after a thorough examination.
A thorough examination should be performed before the initiation of prolonged therapy in patients at risk of cardiovascular disease (hypertension, hyperlipidemia, diabetes, smoking). It is not recommended simultaneous use of lansoprazole and atazanavir. Before and after treatment, endoscopic control is necessary to exclude malignant neoplasm, because treatment can mask symptoms and delay correct diagnosis. Patients taking lansoprazole may develop ulcerative colitis.
Influence or ability to drive vehicles and other technical devices: care must be taken when driving vehicles and other technical devices that require a high concentration of attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: vomiting, bleeding from the gastrointestinal tract, pain in the epigastric region, diarrhea, dizziness, tinnitus, lethargy, convulsions;
rarely - increased blood pressure, acute renal failure, hepatotoxic effect, respiratory depression, coma, melena, convulsions, irritability.
Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, respiratory depression.

Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
There is no specific antidote.
Lansoprazole

At present, no cases of an overdose of lansoprazole have been reported.
In case of taking high doses of the drug, medical supervision is shown, if necessary, asymptomatic therapy. Hemodialysis is ineffective.
DRUG INTERACTION

Diclofenac

The simultaneous use of diclofenac with:

- Lithium or digoxin can increase their concentration in blood plasma;

- with some diuretics can reduce their diuretic effect;

- potassium-sparing diuretics can cause hyperkalemia;

- Acetylsalicylic acid, glucocorticosteroids and other non-steroidal anti-inflammatory drugs - increases the risk of side effects (bleeding in the gastrointestinal tract);

- cyclosporine increases the nephrotoxicity of cyclosporine;

- Methotrexate increases the toxicity of methotrexate;

- hypotensive drugs - reduces their effectiveness.

Reduces the effect of hypoglycemic agents.

Against the background of the simultaneous application of anticoagulants, antiplatelet and thrombolytic drugs (atgeplaza, streptokinase, urokinase) increases the risk of bleeding (usually gastrointestinal). Reduces the hypnotic drugs. Atsetilsatitsilovaya acid reduces the concentration of diclofenac in the blood.
Paracetamol increases the risk of nephrotoxic effects of diclofenac.
Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.
gold drugs increase the effect of diclofenac on the synthesis of prostaglandins in the kidney, which is manifested by increased nephrotoxicity.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.

The simultaneous use of ethanol, colchicine, corticotropin and drugs St. John's wort increases the risk of bleeding in the gastrointestinal tract. Drugs that cause photosensitivity, increase the sensitizing effect of diclofenac to UV irradiation.
Drugs that block tubular secretion, increase the concentration of diclofenac in plasma, thereby enhancing its efficacy and toxicity. Antibacterial drug of group hiiolona increase the risk of seizures.
lansoprazole
Lansoprazole reduces gastric acidity, which can lead to a change in absorption of certain substances, such as ketoconazole bioavailability ampicillin esters and iron salts reduced. Bioavailability digoxin increased by approximately 10%. clinically insignificant for most patients. There may be interactions with drugs that are metabolized in the liver via CYP3A isozymes and CYP2C19. Thus, while the use of lansoprazole and theophylline (isozyme is involved in the metabolism of CYP3A) indicated a moderate increase in the clearance of theophylline (10%). It is unlikely that this interaction is of clinical significance. However, in some patients, to achieve clinically effective concentrations in the blood of lansoprazole require additional titration of the dose of theophylline at the beginning and at the end of therapy laisoprazolom.
Lansoprazole has no clinically significant interaction with phenazone, diazepam, ibuirofenom. fenigoinom, ipdometatsinom, clarithromycin, prednisolone, propranolo.tom, terfenadine or warfarin.
Lansoprazole can stimulate the secretion of theophylline (10%), but this effect is not clinically significant.
Since the interaction with fenigoinom, teofil.tinom or warfarin can be significant in some patients, at risk, should be taken with caution.
Sucralfate and antacids can reduce the absorption of lansoprazole. Since the reaction is not clinically significant, patients may receive sucralfate or antacids for at least 30 minutes before receiving lansoprazole or after 1 hour.
TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

At a temperature of no higher than 25 ° C.
in its original packaging. Keep out of the reach of children. Shelf life - 2 years.
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