AMELOTEX 5MG AMP № 5(AMPOULES)

Amelotex®




International nonproprietary name

Meloxicam



Dosage form

Solution for intramuscular administration 10 mg/ml, 1.5 ml



Compound

1.5 ml solution for intramuscular administration contains

active substance – meloxicam 15 mg,

excipients: meglumine, glycofurfural, poloxamer 188, sodium chloride, glycerol, 1 M sodium hydroxide solution, water for injection.




Description

Transparent or slightly opalescent yellow liquid with a greenish tint



Pharmacotherapeutic group

Non-steroidal anti-inflammatory drugs. Oxycams.

ATX code M01AC06

Pharmacological properties

Pharmacokinetics

Plasma protein binding: 99%. Passes through histohematic barriers and penetrates into the synovial fluid. Concentrations in synovial fluid reach 50% of maximum plasma concentrations.

It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines; 
the drug is found unchanged in urine only in trace amounts. The half-life (T1/2) of meloxicam is 15-20 hours. 
Plasma clearance averages 8 ml/min. In elderly people, drug clearance is reduced. The volume of distribution is low, averaging 11 L.

Hepatic or renal failure of moderate severity does not have a significant effect on the pharmacokinetics of meloxicam.

Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID), has anti-inflammatory, antipyretic, analgesic effects.

Selectively inhibits the enzymatic activity of cyclooxygenase-2. Suppresses the synthesis of prostaglandins in the area of ​​inflammation to a greater 
extent than in the gastric mucosa or kidneys. Less commonly than non-selective non-steroidal anti-inflammatory drugs,
 it causes erosive and ulcerative lesions of the gastrointestinal tract.

Belongs to the class of oxicams; enolic acid derivative.

Indications for use

– inflammatory and degenerative diseases of the joints, accompanied by pain, including rheumatoid arthritis

– osteoarthritis

– ankylosing spondylitis (ankylosing spondylitis)

Directions for use and doses

Intramuscularly, deeply - 7.5-15 mg 1 time per day. With a slight or moderate decrease in renal function (creatinine clearance more than 25 ml/min), 
as well as with liver cirrhosis in a stable clinical condition, no dose adjustment is required. The starting dose in patients at increased risk of side effects is 7.5 mg/day.

The maximum daily dose is 15 mg, in patients with severe renal failure on hemodialysis - 7.5 mg.

When using different dosage forms of meloxicam in combination, its maximum dose should be no more than 15 mg.

The drug is used for 3-6 days (depending on the severity of the condition), followed by a transition to other dosage forms.

Side effects

Often

headache
abdominal pain, dyspepsia, diarrhea, nausea, vomiting
swelling at the injection site, pain at the injection site

Infrequently

dizziness
increased blood pressure, feeling of a rush of blood to the face
hidden or obvious gastrointestinal bleeding, gastritis
constipation, flatulence, belching, stomatitis
transient changes in liver function tests (eg, increased transaminase or bilirubin levels)
itching, angioedema
changes in kidney function tests (increased serum creatinine and/or urea levels)
anemia
other immediate hypersensitivity reactions
swelling

Contraindications

hypersensitivity to meloxicam or any other component of the drug
history of signs of asthma, nasal polyps, angioedema or urticaria with concomitant use of acetylsalicylic acid or other NSAIDs
perioperative pain in the area of ​​graft placement for coronary artery bypass grafting (CABG)
erosive and ulcerative changes in the mucous membrane of the stomach and duodenum/perforation in the acute phase or recently suffered
acute inflammatory bowel diseases (nonspecific ulcerative colitis in the acute phase, Crohn's disease)

• severe liver failure
  severe renal failure (unless hemodialysis is performed)
  ulcerative gastrointestinal bleeding, recent cerebrovascular hemorrhage or other hemorrhagic diseases
  decompensated heart failure
  pregnancy, breastfeeding period
  children and teenagers up to 18 years of age

• Drug interactions Other prostaglandin synthesis inhibitors (PSIs), including corticosteroids or salicylates (acetylsalicylic acid):
• Coadministration of PSIs is not recommended as the synergistic interaction may increase the risk of ulceration or gastrointestinal bleeding.
• Oral anticoagulants, heparin, thrombolytics: increased risk of bleeding. If it is not possible to avoid co-administration of drugs, it is necessary to carefully monitor the effect of anticoagulants on coagulation.

• Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs): increased risk of bleeding due to decreased platelet function.
  Lithium: NSAIDs have been reported to increase plasma lithium levels. Simultaneous administration is not recommended.
   If concomitant use cannot be avoided, plasma lithium levels should be determined at the beginning and end of treatment, as well as after changing the dose of meloxicam.
  Methotrexate: NSAIDs reduce the tubular secretion of methotrexate, thereby increasing the plasma concentration of methotrexate.
   For this reason, concomitant use of NSAIDs is not recommended for patients taking high doses of methotrexate (more than 15 mg/week).

  The risk of interaction between NSAIDs and methotrexate should also be considered in patients taking low doses of methotrexate,
   especially in patients with impaired renal function.
   If combined treatment is necessary, blood counts and kidney function should be monitored. Caution should be exercised when 
  coadministering NSAIDs and methotrexate within 3 days as plasma methotrexate levels may increase and result in increased toxicity.

• Contraception: There are reports that NSAIDs reduce the effectiveness of intrauterine contraceptives.
  Diuretics: When treated with NSAIDs, there is a potential for the development of acute renal failure in patients with dehydration. 
  Patients taking meloxicam in combination with diuretics should receive sufficient fluids and renal function should be checked before initiating meloxicam therapy.

• Antihypertensives (eg, beta blockers, angiotensin-converting enzyme (ACE) inhibitors, vasodilators, diuretics): Decreased effectiveness 
  of antihypertensive medications due to blockade of vasodilator prostaglandins has been reported during treatment with NSAIDs.
  The combined use of NSAIDs and angiotensin II receptor antagonists (as well as ACE inhibitors) enhances the effect of reducing glomerular 
  filtration. In patients with impaired renal function, this may lead to the development of acute renal failure

• Cholestyramine binds meloxicam in the gastrointestinal tract, which leads to accelerated elimination of the drug from the body
  Cyclosporines: NSAIDs may indirectly increase the nephrotoxicity of cyclosporines through renal prostaglandins. During co-administration of these drugs,
   it is necessary to monitor renal function.
  Pemetrexed: For concomitant use of meloxicam with pemetrexed in patients with a creatinine clearance of 45 to 79 mL/min, meloxicam should be withheld 5 days before, 
  on the day of, and 2 days after pemetrexed.

• If the combination of meloxicam with pemetrexed is necessary, patients should be closely monitored, particularly for myelosuppression 
  and gastrointestinal adverse reactions. In patients with creatinine clearance below 45 ml/min, concomitant use of meloxicam with pemetrexed is not recommended.
  
  Meloxicam is almost completely eliminated by hepatic metabolism, which is approximately two-thirds mediated by cytochrome (CYP) P450 enzymes
  (major CYP 2C9 and minor CYP 3A4) and one-third by other pathways, such as peroxidase.

  The possibility of pharmacokinetic interactions should be taken into account when meloxicam is coadministered with drugs known to inhibit or 
  be metabolized by CYP 2C9 and/or CYP 3A4. An interaction mediated by CYP 2C9 can be expected in combination with drugs such as oral antidiabetic
   drugs (sulfonylureas, nateglinide); this interaction may result in increased plasma levels of these drugs and meloxicam.

Patients taking meloxicam and sulfonylureas or nateglinide should be closely monitored for hypoglycemia. No pharmacokinetic drug interactions were 
identified with the simultaneous administration of meloxicam and antacids, cimetidine, digoxin, furosemide.

special instructions

To reduce the risk of adverse events, the minimum effective dose should be used in the shortest possible short course for: coronary heart disease, 
cerebrovascular disease, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking,

creatinine clearance less than 60 ml/min, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, in the presence 
of proven Helicobacter pylori infection, in old age, with long-term use of non-steroidal anti-inflammatory drugs, frequent alcohol consumption, 
severe somatic diseases, concomitant therapy with the following drugs: antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), 
oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

If peptic ulcers or gastrointestinal bleeding occur, or side effects on the skin and mucous membranes develop, the drug should be discontinued. 
In patients with a decrease in circulating blood volume and reduced glomerular filtration (dehydration, chronic heart failure, surgery)

Clinically significant chronic renal failure may occur, which is completely reversible after discontinuation of the drug (in such patients, 
daily diuresis and renal function should be monitored at the beginning of treatment). If there is a persistent and significant increase 
in transaminases and changes in other indicators of liver function, the drug should be discontinued and control tests performed. 
In patients with an increased risk of side effects, treatment begins with a dose of 7.5 mg. In end-stage chronic renal failure in patients on dialysis,
 the dose should not exceed 7.5 mg/day.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

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.

Overdose

Symptoms: increased side effects.

Treatment: symptomatic. There are no specific antidotes or antagonists. In clinical studies, colesteramine has been shown to accelerate the elimination of meloxicam.

Release form and packaging

Solution for intramuscular administration 10 mg/ml.

1.5 ml in ampoules of colorless neutral glass with a colored break ring or with a colored dot and notch. The ampoules are additionally coated with one,
 two or three colored rings and/or a two-dimensional bar code, and/or an alphanumeric coding, or without additional color rings, a two-dimensional bar code, or an alphanumeric coding.

3 or 5 ampoules in a blister pack made of polyvinyl chloride film and aluminum foil or polymer film, or without foil and without film.

1 or 2 blister packs along with instructions for medical use in the state and Russian languages ​​in a cardboard pack.

Storage conditions

Store in a place protected from light at a temperature of 8 to 25 ºС.

Do not store in the refrigerator.

Keep out of the reach of children!



Shelf life

2 years

Do not use after the expiration date.




Procedure for dispensing from pharmacies

On prescription



Manufacturer

CJSC PharmFirma Sotex, Russian Federation