PRINIL coated tablets
PRINIL
International non-patented name: Meloxicam + Pridinol
Composition
Active substance: 1 tablet contains 15 mg of meloxicam, 4 mg of pridinol.
Excipients: lactose hydrate, microcrystalline cellulose, sodium citrate dihydrate, croscarmellose sodium, sellactose 80, colloidal silicon dioxide, magnesium stearate, 4R bright red aluminum varnish.
Description
The medicinal product is an oblong, hard gelatin capsule, approximately 21.4 mm x 7.4 mm, with a brown surface and an orange cap, imprinted with C001 in black ink. Each hard capsule contains granules containing tamsulosin hydrochloride and a soft gelatin capsule containing dutasteride.
Pharmacotherapeutic group
Anti-inflammatory, analgesic and muscle relaxant.
ATC : M01AC56.
Pharmacological properties
Pharmacodynamics
Meloxicam
A non-steroidal anti-inflammatory drug (NSAID) belonging to the enolcarboxamide group is characterized by the fact that it inhibits and prevents prostaglandins (inflammatory mediators) by being more selective in inflammatory sites other than the gastroduodenal (gastric-duodenal) mucosa or kidney. This mechanism of action is based on the superior inhibition of the enzyme cyclooxygenase-2 (SOG-2) in the inflammatory zone in relation to cyclooxygenase-1 (SOG-1), which is responsible for adverse effects.
Pridinol
A centrally acting muscle relaxant indicated in the symptomatic treatment of spasms and muscle contractions.
Pharmacokinetics
Meloxicam
This drug is rapidly absorbed orally, with a bioavailability of 89% after single doses of 30 mg and 7.5 mg, reaching concentrations of 2 ug/ml at 15 mg and 1 ug/ml at 7.5 mg. happens. Peak plasma concentrations are reached during fasting or after a light meal and between 5-6 hours after the stomach is full. The onset of action occurs 80-90 minutes after oral administration and 30 minutes after IV (intravenous) administration. Absorption after rectal administration is similar to oral administration, and absorption after IM (intramuscular) injection takes longer than after oral administration, which can be a maximum of 1 to 1½ hours. Absorption is dose-independent, causing a linear increase in plasma concentrations in the range of 7.5-30 mg depending on the dose. 90% of Meloxicam binds to albumin and circulates in a protein bound manner. The volume of distribution is approximately equal to the extracellular space, ranging from 10 to 15 liters. It penetrates tissues and the concentration in synovial fluid is half as high as in plasma. Meloxicam is perfectly digested and less than 1% of the parent drug appears in the urine. By oxidation of the methyl group present in thiazonil molecule, 4 main metabolites are isolated.
Pridinol
Human pharmacokinetic studies are not available. After oral administration of radiolabeled Pridinol (14C-Pridinol) in rats, maximum plasma radioactivity was detected 1 hour after administration. 30-40% of the intended dose was found in the bile and tissues, especially the liver and kidneys, which indicates that Pridinol is rapidly taken up by tissues after administration (after 30 minutes, the concentration was higher in tissues than in plasma). After 12 hours, 94% of the radioactivity was measured outside the digestive tract. 80% of 14C-Pridinol is excreted after 24 hours, 96% after 4 days, and 56% is excreted through urine.
Instructions for use
Lumbargia, cervicalgia, cervicobrachialgia, torticollis and/or vertebral discopathy, inflammatory musculoskeletal processes with pain associated with muscle accumulation such as fibrocytism, tension-type headache, muscle hypertonia with post-stroke pain, trauma (tendon strain, fractures ).
Contraindications
Hypersensitivity to any component. Hypersensitivity reactions may occur with aspirin or other NSAIDs, and the use of this drug is contraindicated in patients with a history of asthma, nasal polyps, angioedema, or urticaria caused by aspirin or other NSAIDs. Active gastrointestinal ulcer. Gastrointestinal, cerebral or other hemorrhagic types. Acute liver and/or kidney failure. Preoperative pain management in revascularization surgery.
Due to the possibility of anticholinergic effects, it is not recommended to take the drug in cases of angle-closure glaucoma, urodynamic disorders with urinary retention, mechanical occlusion of the gastrointestinal tract, tachyarrhythmias, megacolon or acute pulmonary edema. Its use during pregnancy or lactation is not recommended. Children or adolescents should not take.
Warnings
The use of NSAIDs can increase the risk of serious gastrointestinal conditions, including bleeding, ulceration, or perforation of the stomach or intestines, which can be fatal. These conditions can occur at any time during use and without warning symptoms. Elderly patients are at greater risk of serious gastrointestinal adverse events. Close monitoring is recommended in patients with symptoms suggestive of gastrointestinal disease, a history of gastric or intestinal ulcers, ulcerative colitis or Crohn’s disease, and those receiving anticoagulants. Discontinuation of drug treatment should be considered if skin or mucous membrane reactions occur during treatment. In case of gastrointestinal bleeding or ulceration, the drug should be stopped.
If there is any indication of liver damage (nausea, vomiting, weakness, pruritus, yellowing of the skin and mucous membranes), the drug should be stopped immediately and liver function should be assessed. As with other NSAIDs, Meloxicam may mask the signs and symptoms of an infection.
Close monitoring is recommended in patients with symptoms suggestive of gastrointestinal disease, a history of gastric or intestinal ulcers, ulcerative colitis or Crohn’s disease, and those receiving anticoagulants.
Cardiovascular risk: NSAIDs may increase the risk of serious cardiovascular thrombotic events, potentially fatal myocardial infarction, and stroke. This risk may increase with long-term use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. Meloxicam is contraindicated for the treatment of preoperative pain in patients undergoing coronary bypass surgery.
Precautions
Thrombotic cardiovascular events: Clinical studies conducted up to 3 years with various SOG-2 selective and non-selective NSAIDs have shown an increased risk of serious thrombotic cardiovascular events, myocardial infarction, and potentially fatal stroke. Both SOG-2-selective and non-selective NSAIDs have a similar risk. Patients with known cardiovascular disease or risk factors for it may be at greater risk. To minimize the potential risk of cardiovascular effects treated with NSAIDs, the lowest effective dose should be used for the shortest possible time. Physicians and patients should be vigilant when these conditions occur, even in the absence of previous cardiovascular symptoms. Patients should be informed about the signs and/or symptoms of serious cardiovascular disease and what action to take when they occur. There is no reasonable evidence that concomitant use of aspirin reduces the risk of serious thrombotic cardiovascular events associated with NSAIDs.
Patients with kidney disease, heart or liver dysfunction, and elderly patients should be carefully monitored, as the use of NSAIDs can lead to deterioration of renal function. In these patients, the lowest effective dose should be used and renal function should be monitored. The importance of prostaglandins in maintaining renal blood flow should be taken into account in patients with impaired heart and kidney function, or those treated with diuretics, or after difficult surgery. Effects on kidney function are usually reversible with discontinuation of the drug. As with other NSAIDs, Meloxicam may rarely slightly increase transaminase levels or other parameters of hepatic function. In case of significant and persistent elevations, the use of the drug should be discontinued. Meloxicam may inhibit platelet aggregation. Patients with hemostasis changes, hemorrhaparous diathesis and hematological abnormalities should be carefully monitored. Patients receiving long-term NSAID treatment, especially elderly patients, should have their kidney and liver functions checked regularly and blood tests performed. Like other prostaglandin inhibitors, Meloxicam and other NSAIDs can cause bronchospasm when taken in asthmatic patients. Care should be taken in patients with heart failure or arterial hypertension, as cases of edema have been reported after taking NSAIDs. When these patients receive long-term treatment, blood pressure should be checked regularly. Patients suffering from porphyria should not use this medicine. NSAIDs, including Meloxicam, can cause arterial hypertension or worsen existing hypertension, so such drugs should be used with caution in hypertensive patients. In patients treated with thiazides or diuretics, inappropriate reactions to these treatments may occur when NSAIDs are taken. Blood pressure should be closely monitored and monitored regularly when starting treatment with NSAIDs. Pridinol may increase the effects of other anticholinergic drugs. Concomitant use of pridinol and aspirin reduces the bioavailability of both compounds.
Interaction with other medicines
Meloxicam
As with other NSAIDs, Meloxicam may increase plasma levels of lithium and increase the hematologic toxicity of methotrexate. It has been noted that NSAIDs can reduce the effectiveness of intrauterine substances. Due to their inhibitory effect on the production of vasodilator prostaglandin, NSAIDs can reduce the antihypertensive effect of ACF inhibitors, β-blockers, vasodilators and diuretics. Cholestyramine keeps Meloxicam in the gastrointestinal tract by causing it to be cleared more quickly. Concomitant treatment with NSAIDs and diuretics may increase the risk of acute renal failure in dehydrated patients. The simultaneous use of NSAIDs and anticoagulants (ticlopidine, heparin, thrombolytics) increases the risk of bleeding.
Close monitoring is necessary to determine the need for anticoagulant adjustment. No significant interactions were observed with digoxin, cimetidine, furosemide, warfarin, or antacids at the same time. Co-administration with other NSAIDs, including aspirin, increases the risk of gastrointestinal ulcers and bleeding. A possible interaction with oral hypoglycemic agents cannot be excluded. Most of the hepatic metabolism of meloxicam is mediated by cytochrome P450, therefore, interactions with drugs that are inhibited or metabolized by this system should be considered.
Pridinol
Simultaneous administration with amantadine, quinidine, tricyclic antidepressants or neuroleptics can increase the anticholinergic effects of Pridinol.
Use during pregnancy and lactation
Pregnancy: PRINIL should not be taken during pregnancy. The use of prostaglandin inhibitors in the last trimester of pregnancy can cause early closure of the ductus arteriosus or inertia of the uterus.
Lactation: PRINIL should not be taken during lactation. A decision should be made whether to discontinue the drug or to discontinue lactation, taking into account the relevance of the drug to the mother.
Use in pediatrics
Not to be taken by children or adolescents.
Method of use and dosage
Adults: ½ or 1 tablet per day. Tablets should be taken after meals.
Side effects
Meloxicam
During the use of meloxicam, the following adverse events were recorded, which were evaluated as regular (more than 10% of patients), occasional (1-10%), rare (0.001-1%) or isolated (less than 0.001%):
Gastrointestinal tract
Occasional: abdominal pain, nausea, vomiting, constipation, diarrhea and foam. Rare cases: temporary changes in liver function, esophagitis, gastrointestinal ulcer, belching, micro or macroscopic gastrointestinal bleeding. Isolated cases: Colitis, gastrointestinal perforation, hepatitis and gastritis.
the central nervous system
Occasional: Headache, malaise. Rare cases: Drowsiness, ringing in the ears, dizziness. Isolated cases: Mood changes, disorientation and confusion.
Respiratory system
Isolated cases: The onset of an asthmatic crisis.
Hematopoietic system
Occasional: Anemia. Rarely: changes in blood test results, including white blood cell count, leukopenia and thrombocytopenia. Concomitant use of myelotoxic drugs, such as methotrexate, is a predisposing factor for the onset of cytopenia.
Leather and derivatives
Uncommon: Erythema and pruritus. Rare cases: Urticaria and stomatitis, isolated cases: photosensitivity reactions. The following may occur more rarely: erythema multiforme, flushing/chilling reactions, toxic epidermal necrolysis or Stevens-Johnson syndrome.
Genitourinary system
Rarely: Changes in kidney function parameters (increased levels of creatinine and ureaplasma). Isolated cases: Acute renal failure
Cardiovascular system
Occasional: Edema. Rarely: palpitations, heatstroke and increased blood pressure
Eyes
Isolated cases: Conjunctivitis and visual disturbances
Hypersensitivity reactions
Isolated cases: Angioedema
Pridinol
Although uncommon at recommended doses, mild anticholinergic effects such as decreased sweating, flushing, balance disturbances, increased intraocular pressure, mucosal dryness, tachycardia, difficulty urinating, psychomotor agitation and/or hallucinations (usually at overdose) may occur. knows
Overdose
No untreated overdoses related to the Meloxicam/Pridinol combination have been reported. There are no specific clinical manifestations due to overdose. Management of NSAID overdoses consists mainly of symptomatic and supportive treatment, due to complications such as hypotension, renal failure, seizures, gastrointestinal irritation, and respiratory depression; specific therapies such as forced diuresis, dialysis, or hemoperfusion are unlikely to contribute to NSAID clearance due to their high protein binding and extensive metabolism.
Packing form
10 tablets, in a blister. 2 blisters are packed in a cardboard box with an insert.
Store condition
It should be stored at a temperature not higher than 30ºС, protected from light and out of the reach of children
Shelf life
3 years
By prescription.
Manufacturer
“Laboratories Temis Lostalo S.A.”/ “Laboratories Temis Lostalo S.A. Argetina.