Pentalgin (Piralgin) (tablets)
Pentalgin
International unlicensed name
Metamizole sodium. Paracetamol. Caffeine. Phenobarbital. Codeine.
Pharmacotherapy group
Analgesics – antipyretics. Pyrazolones. Metamizole sodium in combination with psycholeptics.
Composition
1 tablets contains analgin 300 mg(metamizole sodium), paracetamol 25 mg, caffeine 50 mg, phenobarbital 10 mg, codeine 10 mg.
Pharmacological action
Pharmacodynamics
The medication has an analgesic, antipyretic, anti-inflammatory, spasmolytic and sedative action.Pharmacological effects of the combined medication are provided by characteristics of its agents.
Metamizole sodium and naproxen are non steroid anti—inflammatory agents having an anti-inflammation action and analgesic activity.Besides, naproxen is characterized by marked anti-inflammation action.The action mechanism of metamizole sodium and naproxen is related to inhibiting cyclooxygenase enzyme that depresses the prostaglandin synthesis from arachidonic acid.
Codeine and caffeine intensify analgesic action of analgesics contained in pentalgin Н.
Caffeine stimulates the brain psychomotor centres, Кофеин стимулирует психомоторные центры головного мозга, provides an analeptical action, removes drowsing and fatigue, increases physical and mental efficiency, increases the penetrability of blood-tissue interfaces, increases arterial blood pressure on hypotension.
Codeine has a central antitussive action (due to cough centre excitability depression) and analgesic action caused by excitation of opiate receptors in various parts of the central nervous system that stimulate antinoceptive system and change the emotional pain perception.
Phenobarbital has a sedative, soporific, smasmolytic and muscle relaxing action.
Pharmacokinetics
The medication components are well absorbed in the gastrointestinal tract.
Metamizole sodium hydrolyzes in the intestine wall creating an active metabolite, 4-methyl-amino-antipyrin that in its turn creates 4-formyl-amino-antypirin and other metabolites.The level of active metabolite bounding is 50-60 %.Metabolites are excreted via kidney and in the breast milk.
Naproxen bioavailability is 95 %.In therapeutic concentrations naproxen is bound with blood proteins more than 99 %.It diffuses in the synovial fluid, penetrates through the placenta and in small quantities is excreted in the breast milk.The half-period is 12-15 hours. It is excreted in the urine (mainly as demethylnaproxen metabolites) and in small quantities in the faeces (less than 5 %).
Caffeine is absorbed in the intestine, half-period is 5 hours (sometimes up to 10 hours). It is excreted by the kidney as metabolites and about 10% unaltered.
Codiene is slightly bound with plasma proteins. It is subject to biotransformation in the liver. About 10 % of codeine is transformed into morphine. It is excreted by the kidney (5-15 % unaltered).
Naproxen bioavailability is 80%.Bounding with plasma proteins is from low to moderate. It metabolizes in the liver mainly with participation of microsomal enzymes. The main phenobarbital metabolite does not have a pharmacological activity. It is excreted by the kidney (20-25 % unaltered).
Indication
“Pentalgin” is used for arresting moderate pain syndrome of various genesis:headache, radiculitis, menstrual pains, toothache, myalgia, arthralgia, migraine, primary dysmenorrhea and other conditions, as well as has an antipyretic action on fever of various aetiology, catarrhal diseases and other diseases accompanied by pain syndrome and inflammation.
Route and dosage
The medication is for oral administration, usually 1 tablet 1-3 times a day.Max.daily dose is 4 tablets.The medication shall not be taken more than 5 running days without the doctor’s surneillance.
Special indications
Effect on the capability to drive and work with the machines:
after the administration of the medication one should refrain from driving and carrying out potentially dangerous activities that require a higher concentration and quick psychomotor reactions.
The patient shall be notified of the fact that on prolonged use of the medication without the doctor’s surveillance the risk of addiction to the medication can develop.
It is strongly recommended not to drink alcohol on the administration of the medication.
Side effects
Various dyspeptic disturbances are possible (nausea, vomiting, epigastria pains, constipation), allergic skin reactions (rush, itching, nettle-rush), vertigo, drowse, palpitation).In rare cases hematosis depression may develop (leucopenia, granulocytopenia, agranulocytosis).On prolonged administration in elevated doses kidney and liver function may be compromised.
Contraindications
High sensitivity to the components of the medication, marked compromises kidney and liver functions, glucosa-6-phosphatdehydrogenase deficit; stomach and duodenum peptic ulcer in the acute condition; bronchospasm, blood diseases, conditions accompanied by respiratory depression; high intracranial pressure, craniocelebral injuries; acute myocardial infarction; rhythm disturbances; high blood pressure, glaucoma, alcoholic intoxication, age up to 12 years old, breast-feeding (breast-feeding shall be ceased during the period of treatment with the medication).
Precautions
The medication is prescribed with care to patients with compromises kidney and liver functions, stomach and duodenum peptic ulcer at the remission stage, prolonged alcoholic anamnesis and elderly patients.
In case of administration of the medication for more than 5 days monitoring of peripheral blood pattern and liver function shall be carried out.
The administration of the medication may complicate the diagnosis on acute pain syndrome in the abdominal region.
Interaction with other medications
It increases a toxic action of neopyoid analgesics and decreases the level of cyclosporine concentration in the plasma.Sedative agents and tranquilizers intensify an analgesic action of the preparation.
Tricyclic antidepressants, oral contraceptives, allopurinol increase a toxic action of metamiozole sodium (contained in the medication), and barbiturate and phenilbutazone decrease it.
Overdosing
Symptoms:Nausea, vomiting, pain in the stomach, tachycardia, arrhythmia, dizziness, drowse, delusion, respiratory depression.
Treatment:vomiting induction, stomach lavage, adsorbents administration (charcoal), symptomatic therapy aimed at support of life functions.
Product form
10 tablets in a contour cell pack.One or two contour packs with administration data sheet are placed into the carton package.
