Niselat (Amtolmetin guacil) 600mg 20 tablets

International nonproprietary name 

Amtolmetin guacil

Dosage form

Tablets, film-coated, 600 mg

Composition

One tablet contains

active substance – amtolmetin guacil 600 mg,

excipients: lactose monohydrate, hypromellose 15 CPS, silica colloidal anhydrous, sodium starch glycolate (type A), magnesium stearate,

the composition of the shell: hypromellose 5 CPS, titanium dioxide E 171 and macrogol (PEG 400).

Description

Tablet form, dripping, film-coated from white to almost white, smooth on both sides.

Pharmacotherapeutic group

Nonsteroidal anti-inflammatory drugs. Acetic acid derivatives.

Pharmacological properties

Pharmacokinetics

Suction amtolmetin of gualla after ingestion occurs quickly and completely. Amtolmetin guacil concentrated mainly in the gastro-intestinal wall where it is concentrated the maximum level within 2 hours after taking the drug. Its transformation into active metabolites occurs as soon as it enters the plasma, so amtolmetin guacil as such, barely detected in blood plasma and in tissues.

Amtolmetin guacil hydrolyzed by serum esterases to the following plasma metabolites: MED5, tolmetin and guaiacol. MED5 (tolmetin-glycinamide) is the main metabolite in plasma. Tolmetin–glycinamide tolmetin and metabolized to the active metabolite and achieves high concentrations in tissues. Excretion of the drug is almost complete within 24 hours and is happening mostly in the urine (77% of the administered dose) in the form of glucuronides. A small amount is excreted in the bile and faeces (7, 5%).

Pharmacodynamics

Amtolmetin guacil is a nonsteroidal anti-inflammatory (NSAID) prodrug tolmetin possessing analgesic and anti-inflammatory action. The primary mechanism of action of amtolmetin guacil, like other NSAIDs, is manifested in the inhibition of COX and prostaglandin synthesis. Amtolmetin increases the level of antioxidant enzymes in gastric mucosa, such as super-oxidants (SOD), catalase, glutathione, while reducing the level of super-oxide anion, peroxide or nitrite peroxide chloride and malonic dialdehyde. In addition, when using amtolmetin increases the level of nitric oxide (NO) in the stomach, which is manifested gastroprotective effect of the drug.

Antioxidant effect amtolmetin may have additional value in the treatment of patients with osteoarthritis accompanied by inflammation and pain, which increases oxidative stress, damage to cartilage by free radicals. Reduction in pain when using amtolmetin is also associated with a decrease in the level of nitric oxide, contributing to the overcoming of oxidative stress.

These two actions are selective and specific, when applied amtolmetin. 

Indications for use

osteoarthritis, rheumatoid arthritis, arthralgia, myalgia, pain after injuries

Method of application and doses

The drug is taken orally with sufficient quantity of liquid. Naisulat should appoint on an empty stomach to preserve its gastroprotective effect.

Adults

600 mg twice a day.

The recommended dose for osteoarthritis is 600 mg twice a day for the first 3 days, then once a day. The recommended dose in rheumatoid arthritis 600 mg tablet twice a day.

The children

Children over 12 years is assigned to one tablet a day (600 mg). Naisulat forbidden to take children under 12 years

Use in elderly patients

At patients of elderly age (over 65 years) whose renal function is usually reduced, and tolerability of NSAIDs in the gastrointestinal tract is reduced, is assigned a low dosage (600 mg) amtolmetin of guatil.

The duration of treatment determined by the doctor depending on the characteristics of the disease and the severity of the condition. Not recommended for long-term treatment.

Side effects

• lack of appetite, increased appetite, dry mouth, glossitis, stomatitis, ulceration of the mouth, ulcerative stomatitis, gingival bleeding, dysphagia, belching, nausea, vomiting, esophagitis, gastritis, gastroenteritis, enteritis, flatulence, dyspepsia, abdominal pain, colitis, rectal bleeding, pain in region of gall-bladder, gastric ulcer and duodenal ulcer, diarrhea, tarry stools, constipation, tenesmus, hepatitis, abnormal liver function, pancreatitis, cholestatic jaundice
• nasopharyngitis, rhinitis, epistaxis, bronchitis, pneumonia, shortness of breath, asthma
• insomnia, drowsiness, disturbing dreams, headache, dizziness, paresthesia, hypoesthesia, amnesia, emotional instability, poor coordination, peripheral neuropathy, torticollis, facial paralysis, hyperkinesis, depression, hypotension
• arthralgia, arthritis, convulsions in the lower extremities, bursitis, tenosynovitis, tendon rupture, myasthenia, myalgia, contracture of muscles, muscle cramps, myositis, myopathy, rhabdomyolysis
• itching, contact dermatitis, alopecia, dry skin, increased sweating, urticaria, eczema, seborrhea, skin ulceration
• urinary tract infections, frequent urination, cystitis, hematuria, dysuria, kidney calculus, nocturia, albuminuria, nephritis, urinary incontinence, urinary retention, urge to urinate
• epididymitis, impotence, decreased libido, premature ejaculation, fibrocystic breast, vaginal bleeding, acyclic uterine bleeding
• hypertrophy chest
• amblyopia, dry eye, disturbance of refraction, hemorrhaging in the eyes, glaucoma, tinnitus, deafness, parosmia, loss of taste, taste perversion
• palpitation, vasodilatation, syncope, migraine, orthostatic hypotension, phlebitis, arrhythmia, angina, hypertension
• peripheral edema, hyperglycemia, hypoglycemia, increased levels of kreatininfosfokinaza, gout, increase in body weight
• ecchymosis, anemia, lymphadenopathy, thrombocytopenia, petechial hemorrhage
• chest pain, back pain, swelling of the face, fever, muscle stiffness of neck, disorientation, hypersensitivity reaction photosensitivity, generalized edema, anaphylaxis, angioedema, bubble rash (including erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis, Lyell’s syndrome), acute necrosis of skeletal muscles

Contraindications

• hypersensitivity to any component of the drug
• intolerance to other NSAIDs patients with complete or incomplete combination of asthma, rhinitis, urticaria
• erosivno-azwenne defeat of the gastrointestinal tract (stomach ulcer and duodenal ulcer, ulcerative colitis)
• chronic heart failure, swelling, arterial hypertension, hemophilia, hypocoagulation
• impairment of liver function
• chronic renal failure
• hearing loss, pathology of the vestibular apparatus
• pregnancy and lactation
• children up to age 12 years

Caution: hyperbilirubinemia.

Drug interactions

H1-histamine antagonists, known, prevent the capsaicin receptor. Avoid the simultaneous application of amtolmetin guacil with the H1 – histamine antagonists

NSAIDs may enhance the effects of anticoagulants, such as warfarin, the risk for gastrointestinal bleeding or ulcers when used together with corticosteroids and antiplatelet agents. NSAIDs can reduce the antihypertensive effect of diuretics, ACE inhibitors and other antihypertensive agents. Some patients with renal impairment, the combined use of NSAIDs and ACE inhibitors may result in further deterioration of renal function. These interactions should be taken into account when using amtolmetin of gwazela in combination with ACE inhibitors.

Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites. Reduces the effectiveness of uricosuric drugs, enhances hypoglycemic effect of sulfonylureas. Antacids and cholestyramine reduce the absorption amtolmetin. Increase the blood concentration of lithium, methotrexate. Myelotoxic drugs increase the manifestation gematotoksichnosti drug.

Special instructions

Patients with hepatic or renal insufficiency, treatment amtolmetin guillom should be done under clinical monitoring, with periodic monitoring of renal function and liver. In case of deterioration of renal function and liver, the treatment must be suspended. Patients in history where there was a therapy of coagulopathy, treatment with anticoagulants should be under careful medical supervision. During treatment needed to be monitored picture peripheral blood. As in patients receiving other NSAIDs, has been registered changes in the eyes, in the case of visual disturbances during treatment with amtolmetin guillom, treatment should be discontinued and conducted eye examinations. If you experience any allergic reactions, treatment should be stopped immediately. Treatment should be discontinued 48 hours prior to determination of 17-ketosteroids.

In the preparation includes lactose monohydrate, in this regard, Naisulat not recommended to patients with hereditary galactose intolerance, Lapp lactase deficiency, malabsorption of glucose/galactose.

The use of pregnant or breastfeeding women

Safety and efficacy during pregnancy and lactation is not established.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous machinery

Drug may cause dizziness and drowsiness, so the period of treatment patients should not drive a vehicle or potentially dangerous machinery.

Overdose

Symptoms: blurred vision, tachycardia, dry mouth, nausea, vomiting, sweating.

Treatment: gastric lavage, reception activated carbon, symptomatic therapy.

Shape of release and packing

10 tablets are placed in a contour cell package made of polyvinylchloride film and aluminum foil.

1 contour packaging along with instructions for medical use in the state and Russian languages is placed in a cardboard pack of the box.

Storage conditions

Store in a dry, protected from light place at temperature not exceeding 25 °C

Keep out of reach of children!

Shelf life

2 years

Do not use after expiration date.