2010/09/20

Amelotex

Composition, structure and packing

Solution for i / m administration in the form of transparent or light yellow opalescence liquid with a greenish tint.

1 ml of 1 amp. Meloxicam 10 mg 15 mg.

Excipients: meglumine, glikofurfurol, poloksamer 188, sodium chloride, glycerol, sodium hydroxide (1M solution), water d / and.

Clinico-pharmacological group: NSAID.

Pharmacological action

NSAIDs (nonsteroidal anti-inflammatory drug). It belongs to the class oksikamov, derivative enolievoy acid. Has anti-inflammatory, antipyretic and analgesic effects. Selectively inhibits the enzymatic activity of COX-2. Inhibits synthesis of prostaglandins in the area of inflammation to a greater extent than in the mucosa of the stomach or kidneys. Rarely cause erosive-ulcerative lesions GIT.

Pharmacokinetics

Distribution

Plasma protein binding is 99%. Passes through histohematogenous barriers, penetrate into synovial fluid. Concentration in the synovial fluid is 50% of the Cmax in the plasma.

Withdrawal

We derive equally from the feces and urine, mostly as metabolites. Through the intestine unchanged displayed <5% of the daily dose in the urine as unchanged drug is found only in trace amounts.

T1 / 2 of meloxicam is 15-20 h. The plasma clearance is approximately 8 ml / min. In elderly patients the drug clearance decreases. Vd is low and amounts to an average of 11 liters.

Hepatic or renal insufficiency moderately significant effect on the pharmacokinetics of meloxicam does not have.

Statement
rheumatoid arthritis;
osteoarthritis;
ankylosing spondylitis (Bechterew's disease);
inflammatory and degenerative diseases of the joints, accompanied by pain syndrome.

Dosage regimen

The drug should be injected deep into the / m of 7.5-15 mg 1 time / day. The maximum dose - 15 mg / day. The initial dose in patients with increased risk of side effects is 7.5 mg / day. With low or moderate decline of renal function (CC> 25 ml / min) dose adjustment is required. In patients with severe renal insufficiency who are on hemodialysis, the maximum dose - 7.5 mg / day. The cirrhotic liver in clinically stable correction dose is not required.

Side effect

On the part of the digestive system: nausea, vomiting, flatulence, abdominal pain, constipation or diarrhea, bloating, increase in liver transaminases, hyperbilirubinemia, stomatitis, erosive and ulcerative lesions gastrointestinal tract, esophagitis, gastritis, colitis, perforation of the gastrointestinal tract, latent or obvious gastrointestinal -intestinal bleeding, hepatitis.

From the side of the central nervous system: dizziness, vertigo, headache, tinnitus, confusion, drowsiness, disorientation, emotional lability.

On the part of the hemopoietic system: anemia, leukopenia, thrombocytopenia.

Since the cardiovascular system: peripheral edema, increased blood pressure, flushing of the face and upper chest, feeling the heartbeat.

From the urinary system: edema, hypercreatininemia, increasing the concentration of urea in the blood serum; rarely - acute renal failure, interstitial nephritis, albuminuria, hematuria. From the side of the organ of vision: conjunctivitis, visual disturbances (including blurred vision).

Allergic reactions: itching, skin rash, urticaria, photosensitivity, bullous eruption, erythema multiforme, toxic epidermal necrolysis, bronchospasm, angioedema, anaphylactoid, anaphylactic reactions.

Local reactions: possible burning and pain at the injection site.

Contraindications
period after coronary artery bypass grafting;
uncompensated heart failure;
complete or incomplete combination of asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and other NSAIDs (including history);
erosive and ulcerative changes in gastric or duodenal ulcer;
active gastrointestinal bleeding;
inflammatory bowel disease (including ulcerative colitis, Crohn's disease);
cerebrovascular (or other) bleeding;
marked hepatic impairment;
active liver disease;
expressed in renal failure patients not undergoing dialysis (CC <30 ml / min);
progressive renal disease (including those with confirmed hyperkalaemia);
Pregnancy
breastfeeding;
childhood and adolescence to 15 years;
Hypersensitivity to the drug's components.

C care use in patients with coronary heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, smoking, CC <60 ml / min, anamnestic data on the development of ulcerative lesions gastrointestinal infection in the presence of Helicobacter pylori, long-term NSAID use, frequent alcohol use, severe somatic diseases, elderly patients, with concomitant therapy of the following medications: anticoagulants (warfarin), antiplatelet agents (aspirin, clopidogrel), oral GCS (prednisone), selective serotonin reuptake inhibitors (citalopram, fluoxetine , paroxetine, sertraline).

In the above-mentioned diseases and conditions to reduce the risk of adverse events should use the lowest effective dose of the lowest possible short course.

Pregnancy and lactation

Do not use this drug during pregnancy and lactation.

Application for violations of liver function

Do not use this drug in marked hepatic insufficiency, active liver disease.

Application for violations of renal function

Do not use this drug in marked renal failure in patients not undergoing dialysis (CC <30 ml / min) and progressive kidney disease (including confirmation hyperkalaemia).

Cautions

If you have peptic ulcers or gastrointestinal bleeding, development of side effects from the skin and mucous membranes of the drug should be abolished.

Patients with lower BCC and reduced glomerular filtration (dehydration, chronic heart failure, surgery) may cause clinically manifested with chronic renal failure, which is completely reversible after discontinuation of the drug.

In these patients early in treatment should be monitored daily urine output and renal function.

In the terminal stage of chronic renal failure patients on dialysis, the dose of the drug should not exceed 7.5 mg / day. With a persistent and significant increase of transaminases and changes in other indicators of liver function medication should be repealed and to control tests.

Effects on ability to drive vehicles and management mechanisms

During the period of treatment must be careful when driving and busy with other potentially hazardous activities that require high concentration and speed of psychomotor reactions (with the appearance of dizziness and drowsiness).

Overdose

Symptoms: increased side effects.

Treatment: symptomatic. Specific antidotes and antagonists, no.

Drug Interactions
With simultaneous application Ameloteksa with other NSAIDs increases the risk of gastrointestinal ulcers and gastrointestinal bleeding. At simultaneous application with Ameloteksom increases the concentration of lithium in blood plasma.
At simultaneous application with Ameloteksom reduced effectiveness of intrauterine contraceptive devices, antihypertensive drugs.
With simultaneous application Ameloteksa with indirect anticoagulants, tiklopidiom, heparin, thrombolytics increases the risk of bleeding.
With simultaneous application Ameloteksa with methotrexate increases mielodepressivnoe action.
With simultaneous application Ameloteksa with diuretics increases the risk of renal dysfunction.
With simultaneous application Ameloteksa with cyclosporine increases nephrotoxicity meloxicam.

When applied simultaneously with Ameloteksa kolestiraminom accelerated excretion meloxicam. Myelotoxic drugs increase the expression gematotoksichnosti Ameloteksa.

Terms and Conditions of storage

List B. The drug should be stored out of reach of children, protected from light at a temperature of 8 ° to 25 ° C Do not freeze.

Shelf life - 2 years.