Alit

Alit is an NSAID drug and contains 2 active ingredients.

Nimesulide is a component with analgesic, anti-inflammatory and antipyretic activity. This element selectively slows down the activity of COX-2, and at the same time suppresses the processes of PG binding within the areas where inflammation occurs. [ 1 ]

Dicyclomine hydrochloride helps to relieve spasms of smooth muscles in the gastrointestinal tract.

Indications Alita

It is used to relieve pain and spasms of various origins. [ 2 ], [ 3 ], [ 4 ]

Release form

The medicinal element is released in tablets - 4 pieces inside a blister pack. There is 1 such pack in a pack.

Pharmacodynamics

Nimesulide slows down the release of the enzyme myeloperoxidase, and at the same time suppresses the formation of free oxygen radicals, without affecting chemotaxis with phagocytosis. The substance also suppresses the formation of tumor necrosis factors and other inflammatory conductors. [ 5 ]

Dicyclomine hydrochloride is an antagonist of cholinergic muscarinic endings and also acts directly on smooth muscle, probably acting as a histamine-bradykinin antagonist. Dicyclomine has shown inhibitory activity against several pathogenic bacteria.[ 6 ]

[ 7 ]

Pharmacokinetics

When taken orally, nimesulide is absorbed from the gastrointestinal tract at a high rate. Plasma Cmax values are recorded after 2-3 hours. Protein synthesis of nimesulide is 97.5%. Metabolic processes are realized in the liver; the main metabolic component is hydroxynimesulide (has medicinal activity). Approximately 65% of the consumed portion of nimesulide is excreted with urine, and the remainder (35%) - with feces.

After oral administration of dicyclomine, it is absorbed at high speed, reaching Cmax after 90 minutes. The half-life is 4-6 hours. Excretion occurs with urine (79.5%) and feces (8.4%). [ 8 ]

[ 9 ]

Dosing and administration

Alita is prescribed only after careful assessment of the balance between potential benefits and existing risks.

The medication should be taken orally, after meals, with plain water. The daily dosage is 1-2 times a day, taking 1 tablet (0.1 g of nimesulide) (in the morning and in the evening). No more than 0.2 g of nimesulide can be taken per day. Therapy can last no more than 5 days. [ 14 ]

Application for children

Nimesulide is approved for use, like other analgesic-antipyretic agents, for short-term use (up to 10 days) in children. The drug should be avoided in known or suspected liver disease; caution is required when prescribing nimesulide concurrently with other hepatotoxic drugs. [ 15 ]

There are data on the restriction of administration of the drug to children under six months of age. There are published cases where the administration of dicyclomine hydrochloride to infants was accompanied by severe respiratory symptoms (dyspnea, respiratory collapse, apnea and asphyxia), seizures, syncope, muscle hypotonia, coma and death, but a causal relationship has not been established. [ 16 ]

Use Alita during pregnancy

It is prohibited to prescribe Alit during pregnancy. Since nimesulide can negatively affect fertility in women, it should not be used when planning conception. Like other NSAIDs that inhibit PG binding, nimesulide can lead to too early closure of the arterial pathway, the development of oliguria, pulmonary hypertension and oligohydramnios. There is also a risk of uterine atony, bleeding and peripheral edema. [ 10 ]

Due to the lack of data on whether nimesulide is excreted in breast milk, the drug is not used during breastfeeding. One possible case of apnea in a breastfed child whose mother was taking Dicycloverine has been reported [ 11 ]

Contraindications

Main contraindications:

• ulcers affecting the gastrointestinal tract (in the active phase);
• the presence of recurrent ulcers or the presence of bleeding in the gastrointestinal tract (in the anamnesis);
• severe liver dysfunction (liver failure), as well as a history of hepatotoxic manifestations associated with the use of drugs;
• use together with substances that have potential hepatotoxicity;
• those with severe renal dysfunction (creatinine clearance values are less than 30 ml per minute);
• severe disorders of blood clotting processes;
• cerebrovascular or other pathologies in which bleeding occurs;
• having a severe form of heart failure;
• severe intolerance to the active element of the drug or other of its components, as well as hypersensitivity associated with other NSAIDs (in history);
• drug or alcohol addiction;
• increased temperature and flu-like conditions;
• existing suspicion of the development of surgical disease in the active phase.

Side effects Alita

Among the side effects associated with the use of the drug (usually appear during the first 7 days of drug administration): [ 12 ]

Caused by the influence of nimesulide:

• lesions of the epidermis and subcutaneous tissues: itching, erythema, hyperemia, hyperhidrosis, rashes and dermatitis are often observed. Swelling of the face, oral mucosa or tongue, SJS, urticaria, hyperemia of the oral mucosa, TEN, erythema multiforme and Quincke's edema occasionally appear;
• digestive problems: symptoms of dyspepsia, including vomiting, bloating, heartburn, constipation, diarrhea and nausea. In addition, there is pain in the abdominal area or gastritis. Melena, ulcer perforation or bleeding inside the gastrointestinal tract are observed isolated, and in addition, stomatitis and ulcers in the gastrointestinal tract;
• liver dysfunction: cholestasis or jaundice, as well as increased intrahepatic transaminase levels. Sometimes fulminant hepatitis (sometimes fatal) may also develop; [ 13 ]
• disorders of the nervous system: headaches, encephalopathy, drowsiness and dizziness;
• mental health symptoms: nervousness, nightmares and anxiety;
• renal lesions: hematuria, edema, urinary retention and dysuria. Occasionally, renal failure, oliguria and tubulointerstitial nephritis occur;
• disorders in the functioning of the blood system: eosinophilia or anemia. Thrombocytopenia or pancytopenia, as well as purpura, develop occasionally;
• immune disorders: anaphylaxis or intolerance symptoms;
• problems with respiratory function: dyspnea. Asthma or bronchial asthma may occasionally appear (especially in people with intolerance to aspirin and other NSAIDs);
• lesions associated with the activity of the cardiovascular system: increased blood pressure or tachycardia. Hot flashes, collapse, bleeding and changes in blood pressure are occasionally observed;
• Others: asthenia, blurred vision or hypothermia.

Associated with dicyclovir activity:

• disorders in the functioning of the cardiovascular system: palpitations, hot flashes, tachycardia and loss of consciousness;
• dysfunction of the nervous system: sensory disturbances, dyskinesia, dizziness, drowsiness, loss of consciousness, severe fatigue and headaches, as well as nervousness, insomnia, paresthesia, problems with gait stability, systemic weakness and lethargy;
• mental health problems: agitation or confusion, mood lability, hallucinations and speech disorders;
• lesions affecting the subcutaneous layer and epidermis: itching, rashes, epidermal dryness, urticaria and other dermatological symptoms;
• signs associated with digestion: nausea, anorexia, xerostomia, bloating, vomiting, thirst, constipation, taste disturbances and pain in the abdominal area;
• disorders of the musculoskeletal system: muscle weakness;
• disorders of the urogenital system: urinary retention or disorder, as well as impotence;
• problems with visual activity: mydriasis, increased IOP, visual blurring, accommodative paralysis and diplopia;
• respiratory system damage: asphyxia, hyperemia in the throat, apnea or dyspnea, sneezing and nasal congestion;
• immune disorders: severe allergic reactions or drug idiosyncrasies, which also include anaphylaxis;
• endocrine dysfunction: suppression of lactation.

Overdose

A sign of nimesulide poisoning is the potentiation of such disorders as drowsiness, pain in the "pit of the stomach" area, vomiting, lethargy and nausea (such manifestations are often curable if supportive measures are taken). In addition, bleeding in the gastrointestinal tract may be observed. Rarely, acute renal failure, anaphylactoid symptoms, increased blood pressure, respiratory depression and coma, hypoglycemia develop. [ 17 ]

In dicycloverine intoxication occurs in two stages: first, the central nervous system is excited, which causes hallucinations, illusions, anxiety, persistent mydriasis, hypertension, and tachycardia. After this, the central nervous system is suppressed, which can lead to coma.

The drug has no antidote. In case of overdose, symptomatic actions and peritoneal dialysis are performed. During the first 4 hours, the victim needs to undergo gastric lavage through a tube, and in addition, take laxatives and activated carbon.

Hemodialysis will be ineffective. It is necessary to closely monitor the functioning of the liver and kidneys. [ 18 ]

Interactions with other drugs

Combination with warfarin and other similar anticoagulants, as well as with aspirin, increases the risk of bleeding.

The combination of nimesulide and furosemide should be done with caution in people with heart and kidney disorders.

NSAIDs reduce lithium clearance rates, which increases its plasma level and its toxic activity. Therefore, with such a combination (nimesulide + lithium), it is necessary to closely monitor the plasma lithium rates.

The administration of nimesulide together with theophylline, ranitidine, digoxin, as well as glibenclamide and antacids did not lead to the development of clinically significant interactions.

Nimesulide slows down the activity of the enzyme CYP 2C9, which is why, when combined with it, an increase in the plasma values of those substances that this enzyme affects may be observed.

Alit should be used with extreme caution when administered less than a day before/every other day after taking methotrexate, as this increases the serum levels and toxic properties of the latter.

Use together with nimesulide may increase the nephrotoxic activity of cyclosporine.

Dicyclomine can potentiate the effects of other anticholinergic substances (including atropine sulfate), which is why they cannot be combined with Alit.

Storage conditions

Alit must be stored in a place closed to children, moisture and sunlight. Temperature indicators - no more than 25 ° C.

Shelf life

Alit is permitted to be used within a 36-month period from the date of manufacture of the pharmaceutical substance.

Analogues

Analogues of the drug are Nimuspaz, Nanogan with Oxygan, as well as Sigan and Nigan.