Pentalgin is

Pentalgin is a complex drug with antipyretic, anti-inflammatory and analgesic activity. It contains 5 active elements, whose therapeutic effect leads to the development of the medicinal effect of the drug.

Metamizole Na, as well as paracetamol, are non-selective drugs from the NSAID group. [ 1 ]

Codeine is a medicinal substance from the category of opioid analgesics; it reduces the excitability of the cough center and also has an analgesic effect. [ 2 ]

In addition, the drug contains phenobarbital and caffeine.

Indications Pentalgin is

It is used to eliminate acute pains of various localizations. Among them:

• myalgia with arthralgia, toothache or headache of various origins and neuralgia;
• algomenorrhea;
• migraine attacks, as well as migraine-like headaches.

In addition, the medication is prescribed to eliminate the symptoms of acute respiratory viral infections or flu - reducing elevated temperature, as well as eliminating muscle pain and inflammation.

Release form

The medicinal substance is released in tablets - 10 pieces in a cell pack, 1 pack in a box.

Pharmacodynamics

Metamizole Na with paracetamol have an intense analgesic and antipyretic effect; metamizole Na also has a strong anti-inflammatory activity. The principle of the influence of these elements is based on the ability to suppress the binding of PG, slowing down the action of the COX enzyme.

Phenobarbital exhibits intense muscle relaxant, antispasmodic and sedative effects, helping to potentiate the medicinal effect of NSAIDs.

The use of codeine in therapeutic doses does not lead to suppression of the respiratory center and does not affect the excretory activity of the bronchi. Frequent administration of codeine or the use of large doses can provoke drug dependence. The substance causes potentiation of the activity of NSAIDs and sedatives.

Caffeine stimulates the activity of the central nervous system, prevents collapse and potentiates the medicinal effect of metamizole Na and paracetamol.

Pharmacokinetics

When administered orally, the active ingredients of the drug are well absorbed in the gastrointestinal tract.

Metamizole Na is converted inside the intestinal walls; the unchanged element is not registered inside the bloodstream. The synthesis rates of its active metabolic component with plasma protein are 50-60%. Metabolic processes are realized inside the liver, and excretion occurs mainly through the kidneys in the form of metabolic elements, with or without medicinal effect.

Paracetamol has a high rate of synthesis with intraplasmic protein. Paracetamol with caffeine participate in intrahepatic metabolism and are excreted in the form of metabolic components mainly through the kidneys. The half-life of paracetamol is 1-4 hours.

Phenobarbital is also a participant in intrahepatic metabolic processes; it induces liver microsomal enzymes. Excretion is realized mainly by the kidneys in the form of metabolic products. The half-life is approximately 3-4 days.

Codeine easily overcomes the blood-brain barrier and accumulates inside the body. Its accumulation is observed mainly in the lungs, fatty tissue, kidneys and liver. The influence of tissue esterases leads to the hydrolysis of codeine, as a result of which it conjugates with glucuronic acid inside the liver. Codeine breakdown products have an analgesic effect. Excretion of the majority of the substance (in the form of metabolic components) occurs through the kidneys; a small part is excreted with bile.

Dosing and administration

The medicine is taken orally, swallowing the tablet whole (no need to crush or chew it). It must be washed down with plain water. It is necessary to adhere to a minimum 4-hour interval between the use of the medicine.

The duration of the treatment cycle and the dose sizes of the medication are selected by the attending physician, individually for each patient.

In case of short-term acute pain, you need to take 1 tablet of the medicine once. If the pain lasts for a long time (in diseases associated with damage to the nervous system and musculoskeletal system), you need to take 1 tablet 1-3 times a day. The treatment cycle can last no more than 5 days (unless the attending physician has selected a different scheme).

As an antipyretic substance, Pentalgin is often used 1 tablet 1-3 times a day. Therapy can last a maximum of 3 days, unless otherwise indicated by a doctor.

You can take no more than 4 tablets per day.

Long-term use of drugs can lead to drug dependence.

If the medication needs to be taken for more than 1 week in a row, it is necessary to monitor liver function, as well as morphological blood parameters.

• Application for children

Not intended for use in persons under 12 years of age.

Use Pentalgin is during pregnancy

The medication should not be used during pregnancy.

If the drug needs to be taken during lactation, the issue of stopping breastfeeding should be considered first.

Contraindications

Among the contraindications:

• strong personal sensitivity to the elements of the drug;
• kidney or liver diseases of a severe nature;
• gastrointestinal tract lesions that have an erosive-ulcerative form;
• problems with hematopoiesis, including leukopenia or thrombocytopenia, as well as anemia;
• pathologies associated with the function of the cardiovascular system, including arrhythmia, myocardial infarction in the active phase and elevated blood pressure;
• use after a recent TBI, and also with increased ICP rates of various origins;
• G6PD deficiency;
• glaucoma;
• tendency to develop bronchial spasms;
• conditions in which respiratory depression is observed.

Caution is required when used by individuals with asthma or kidney/liver dysfunction, the elderly and diabetics.

Side effects Pentalgin is

Main side effects:

• lesions affecting the gastrointestinal tract: loss of appetite, vomiting, indigestion, pain in the epigastric region, xerostomia, nausea and bowel disorders (both diarrhea and constipation may be observed). In addition, an increase in the activity of liver enzymes may be observed, often not accompanied by the development of jaundice;
• disorders associated with the functioning of the PNS and CNS: circadian rhythm disorder, increased fatigue, problems with motor coordination, irritability, anxiety, tremors in the limbs and headaches;
• problems with the function of the cardiovascular system and hematopoiesis: heart rhythm disorders, increased blood pressure, extrasystole, met- or sulfhemoglobinemia, as well as anemia (also hemolytic);
• disturbances in the functioning of the sensory organs: increased intraocular pressure, tinnitus and visual disturbances;
• signs of allergy: urticaria, Quincke's edema, epidermal rashes, bronchial spasm, itching, SJS and TEN;
• Others: acute renal failure, renal colic, renal/hepatic dysfunction, hyperhidrosis, dyspnea, asthenia, tubulointerstitial nephritis and increased blood glucose levels. Long-term use of Pentalgin followed by abrupt discontinuation may result in withdrawal syndrome.

It is important to take into account that the medication may change its indications when athletes undergo doping control.

The use of drugs sometimes complicates diagnosis in individuals with abdominal pain in the active phase.

If negative symptoms appear, you should stop using the medication and consult a doctor.

Overdose

Overdose of the drug causes vomiting, allergy symptoms, weakness, nausea, heart rhythm disorders, decreased blood pressure, pain in the epigastric region, paleness of the epidermis and hepatonecrosis. Subsequent increase in the dose may lead to suppression of the central nervous system and respiratory center.

Poisoning with the drug requires gastric lavage, the use of enterosorbents and symptomatic actions. In case of paracetamol intoxication, N-acetylcysteine can be administered, and methionine can be taken orally.

Interactions with other drugs

The use of the drug together with NSAIDs, as well as aminophenazone, leads to potentiation of the toxic activity of both drugs.

The combination of the drug and coumarin-type anticoagulants causes a potentiation of their medicinal activity.

Paracetamol weakens the effect of drugs that undergo intensive intrahepatic metabolic processes.

Administration in combination with rifampicin causes a decrease in the medicinal effect of paracetamol.

The combination with cimetidine weakens the toxic effects of paracetamol and potentiates its therapeutic properties.

Concomitant use with tricyclics, oral contraception and allopurinol leads to potentiation of the toxicity of metamizole Na.

Administration together with drugs that induce the action of intrahepatic microsomal enzymes weakens the effect of metamizole Na.

When combined with metamizole Na, there is a decrease in blood levels of cyclosporine.

The combination with codeine potentiates the activity of drugs that suppress the central nervous system.

The effects of MAOIs, codeine and tricyclics are mutually potentiated when using such a drug combination.

Caffeine weakens the effect of drugs that depress central nervous system function and also potentiates the medicinal activity of NSAIDs.

Phenobarbital increases the rate of conversion of doxycycline, carbamazepine with quinidine and estrogens.

The combination of Pentalgin with substances that suppress the central nervous system leads to a potentiation of the medicinal activity of phenobarbital.

Sodium valproate together with valproic acid, used in combination with the drug, lead to a weakening of the metabolic processes of phenobarbital.

The medicine should not be used together with ethyl alcohol.

Storage conditions

Pentalgin should be stored in a dark and dry place at a temperature of no more than 25°C.

Shelf life

Pentalgin can be used for a period of 3 years from the date of sale of the medicinal product.

Analogues

The analogue of the drug is the substance Sedal-M.