Novigan

Pharmacological properties

Novigan - a combined drug, belongs to the group of analgesic and antispasmodic drugs. the composition of the drug includes: ibuprofen - npvp, p-piperidinoethoxy-o-carbomethoxybenzophenone hydrochloride - myotropic antispasmodic and alpha-piperidinoethyl diphenylacetamide metabromide - anticholinergic agent of central and peripheral action.

The main mechanism of pharmacological action of ibuprofen is the inhibition of prostaglandin synthesis. Non-selective NSAIDs, which include ibuprofen, act as systemic inhibitors (peripheral and central) of the synthesis of prostaglandin G / H enzymes, also known as COX-1 and COX-2. These enzymes are responsible for the conversion of arachidonic acid into various tissue-specific prostaglandins and thromboxanes. COX-1 is constitutively expressed in all tissues and is responsible for the production of prostaglandins, which support the functioning of organs, protect the integrity of the gastric mucosa and generate thromboxine, which is responsible for platelet aggregation and vasoconstriction. With inflammation, COX-2 is induced, which produces prostaglandins that mediate pain and inflammatory processes.

P-piperidinoethoxy-O-carbomethoxybenzophenone hydrochloride has a direct myotropic effect on the smooth muscles of internal organs, inhibits PDE, causes the accumulation of cAMP and a decrease in the calcium content in the cell, weakens the smooth muscles of blood vessels and internal organs.

Alpha-piperidinoethyl diphenylacetamide metabromide due to ganglion-blocking and parasympathetic effects reduces the tone and motility of the smooth muscles of the stomach, intestines, bile and urinary tract.

Ibuprofen is well absorbed in the gastrointestinal tract when taken orally. C_max in plasma is observed 1–2 hours after administration. About 99% of ibuprofen binds to plasma proteins. It is excreted mainly with urine in unchanged form or in the form of oxidized inactive metabolites. It is completely eliminated from the body within 24 hours.

The combination of 3 components of the drug causes a mutual strengthening of their pharmacological action, which leads to a decrease in the severity of pain, relaxation of smooth muscles, and a decrease in elevated body temperature.

Indications

Mild or moderate pain syndrome with spasms of smooth muscles of internal organs - renal or hepatic colic, biliary dyskinesia, intestinal cramps, spastic dysmenorrhea and other spastic conditions of smooth muscles of internal organs. headache, including migraine-like. can be used for short-term symptomatic treatment for arthralgia, neuralgia, sciatica, myalgia. to reduce elevated body temperature in infectious and inflammatory diseases.

Application

Usually, 1-2 tablets are prescribed up to 4 times a day. The maximum daily dose is 8 tablets. with dysmenorrhea, 1 tablet is prescribed every 4 hours. It is advisable to take novigan 1 hour before or 3 hours after a meal. in order to avoid irritation of the gastric mucosa, it should be taken immediately after eating or washed down with milk. Novigan is intended for episodic or short-term treatment (up to 5 days). more prolonged use is possible only under medical supervision.

Contraindications

Hypersensitivity to the components of the drug and other NSAIDs, erosive and ulcerative lesions of the gastrointestinal tract, gastrointestinal bleeding or perforation after applying NSAIDs, history of BA, rhinitis or rash when taking acetylsalicylic acid or other NSAIDs, severe heart failure, severe liver and the kidneys.

The use of ibuprofen along with other NSAIDs, including selective COX-2 inhibitors, should be avoided due to the possible occurrence of additive effects.

The drug is also contraindicated in hepatic porphyria, hereditary deficiency of glucose-6-phosphate dehydrogenase, tachyarrhythmia, optic nerve damage, hematopoiesis, blood disease, angle-closure glaucoma, decompensated heart failure, prostatic hypertrophy, gastrointestinal obstruction or megacolon.

Pregnancy and lactation, children under 16 years old.

Side effects

From the digestive tract: infrequently - abdominal pain, dyspepsia, nausea; rarely - diarrhea, flatulence, constipation, vomiting; very rarely - a stomach ulcer and duodenal ulcer, perforation or gastrointestinal bleeding, heartburn, melena, ulcerative stomatitis, exacerbation of ulcerative colitis and Crohn’s disease, gastritis, esophagitis.

On the part of the cardiovascular system: rarely - tachycardia, shortness of breath, cerebrovascular complications, arterial hypotension, palpitations; very rarely - edema, hypertension, heart failure.

With prolonged use and in high doses (2400 mg / day), an increase in the risk of arterial thrombotic events or stroke, a decrease in the effectiveness of antihypertensive drugs is possible.

General disorders: very rarely - non-specific allergic reactions and anaphylactic shock, asthma or worsening of asthma, bronchospasm, rash, itching, urticaria, purpura, angioedema.

From the nervous system: infrequently - headache; very rarely - optic neuritis, paresthesia, nervousness, dizziness, drowsiness, irritability, tinnitus, depression, insomnia, anxiety, psychomotor agitation, emotional instability, convulsions.

From the immune system: in patients with systemic lupus erythematosus and mixed connective tissue diseases, taking ibuprofen in rare cases can lead to symptoms of aseptic meningitis, which is manifested by stiff neck, headache, vomiting, hyperthermia or disorientation.

On the part of the hematopoietic organs and lymphatic system: very rarely - hematopoietic disorders (hemolytic anemia, aplastic anemia, thrombocytopenia, neutropenia, eosinophilia, decreased hematocrit and hemoglobin level, pancytopenia, agranulocytosis). The first signs are hyperthermia, sore throat, ulcers on the oral mucosa, flu symptoms, severe exhaustion, unexplained bleeding and hematomas. Reversible platelet aggregation, alveolitis, pulmonary eosinophilia.

From the side of the organ of vision: very rarely - blurred vision, a change in color perception, toxic amblyopia.

From the hepatobiliary system: very rarely - impaired liver function, hepatitis, jaundice, duodenitis, pancreatitis, hepatorenal syndrome, liver failure, hepatonecrosis.

On the part of the skin: rarely - peeling of the skin, alopecia, photosensitivity; very rarely - bullous lesions, including Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis.

From the urinary system: very rarely - papillonecrosis, cystitis, hematuria, nephrotic syndrome, oliguria, polyuria, tubular necrosis, glomerulonephritis, impaired renal function, toxic nephropathy in various forms, including interstitial nephritis, nephrotic syndrome and renal failure.

Other effects: rarely - dry mucous membranes of the eyes and oral cavity, stomatitis, hyperthermia, poor health, weakness, increased fatigue, hearing impairment, ulcerative stomatitis; very rarely - changes in the endocrine system and metabolism, decreased appetite.

special instructions

With caution and under the supervision of a physician, the drug should be used to treat patients with moderate impaired liver or kidney function, with a tendency to ag, bronchospasm, systemic lupus erythematosus and other systemic diseases of the connective tissue - an increased risk of history of aseptic meningitis with heart failure, which was accompanied by fluid retention and edema when using NSAIDs.

An increase in the dose of NSAIDs, old age, a history of gastric and duodenal ulcers are risk factors regarding the occurrence of adverse reactions from the digestive tract. During treatment in such cases, it is recommended to use the minimum effective dose of the drug.

Caution is advised to use the drug in patients who receive therapy with drugs that can increase the risk of stomach ulcers and duodenal ulcers or bleeding, in particular oral GCS, anticoagulants, warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents, such as acetylsalicylic acid. Patients who have had gastrointestinal upsets, especially the elderly, should stop treatment and consult a doctor if any unwanted symptoms (especially bleeding from the gastrointestinal tract) occur.

With prolonged (more than a week) use of the drug, it is necessary to monitor the parameters of peripheral blood and the functional state of the liver.

The drug can affect the psychophysiological state of patients while taking it with alcohol and drugs that depress the central nervous system.

Prolonged and uncontrolled use of painkillers, especially a combination of various painkillers, can lead to chronic kidney damage with the risk of renal failure (analgesic nephropathy).

Adverse reactions can be minimized by applying the minimum effective dose for the least prolonged period necessary to relieve symptoms.

The drug should not be used in the presence of hereditary intolerance to galactose and dairy products, lactase deficiency.

Like other NSAIDs, ibuprofen can mask signs of infection.

Use during pregnancy and lactation. The drug is not used during pregnancy. Breastfeeding for the period of treatment should be discontinued.

Children. Do not prescribe the drug to children under the age of 16 years.

The ability to influence the reaction rate when driving or working with other mechanisms. Care must be taken when driving and working with other potentially dangerous mechanisms that require an increased concentration of attention and speed of psychomotor reactions.

Interactions

The simultaneous use of novigan with other NSAIDs or non-narcotic analgesics can lead to a double increase in toxic effects.

Antihypertensive drugs, ACE inhibitors - while the use of antihypertensive effect is reduced.

Diuretics - with simultaneous use with ibuprofen, the diuretic effect and diuretic activity are reduced, the nephrotoxicity of NSAIDs is increased.

Cardiac glycosides - with simultaneous use with NSAIDs, exacerbation of heart failure, a decrease in glomerular filtration rate and an increase in the concentration of cardiac glycosides in blood plasma are possible.

Lithium preparations - with simultaneous use, the elimination of lithium preparations decreases, their toxicity and concentration in the blood plasma increase.

Methotrexate - with simultaneous use, the elimination of methotrexate is reduced, its toxicity and plasma concentration increase.

Cyclosporin - with simultaneous use with NSAIDs, nephrotoxicity increases.

Mifepristone - NSAIDs are allowed only 8-12 days after the withdrawal of mifepristone, since NSAIDs reduce the effectiveness of mifepristone.

GCS - with simultaneous use, the risk of bleeding in the digestive tract increases.

Anticoagulants - with simultaneous use, the effect of anticoagulants is enhanced.

Quinolone-type antibiotics - NSAIDs may increase the risk of convulsions associated with quinolone intake.

Zidovudine - there is evidence of an increased risk of hemarthrosis and hematomas in HIV-infected patients receiving concomitant treatment with zidovudine and ibuprofen.

Tacrolimus - increased risk of nephrotoxicity.

Herbal preparations of ginkgo biloba can potentiate the risk of bleeding when using NSAIDs.

Overdose

It manifests itself in the form of gastrointestinal disorders (nausea, vomiting, anorexia, pain in the epigastric region, diarrhea), manifestations of hepatotoxicity, impaired consciousness.

Treatment. Symptomatic therapy is indicated. Within 1 hour after taking a large dose, gastric lavage and activated carbon are indicated. It is necessary to ensure proper diuresis and monitor the state of kidney and liver function. After taking potentially toxic doses, the patient should be monitored for at least 4 hours. In case of convulsions, diazepam can be used.

Storage conditions

In a dry, dark place at temperatures up to 25 ° C.