Plenalgin (Tablets, Solution) Instructions for Use

Instructions
Dosage forms

ATC Code

A03DA02 (Pitofenone and analgesics)

Active Substances

Metamizole sodium (Rec.INN registered by WHO)

Fenpiverinium bromide (Rec.INN registered by WHO)

Pitofenone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Spasm analgesic

Pharmacotherapeutic Group

Non-narcotic analgesic agent (non-narcotic analgesic + spasmolytic)

Pharmacological Action

Metamizole sodium, a pyrazolone derivative, possesses analgesic, antipyretic, and weak anti-inflammatory action, the mechanism of which is associated with the inhibition of prostaglandin synthesis due to non-selective inhibition of cyclooxygenase.

Pitofenone – a myotropic spasmolytic has a direct effect on the smooth muscles of internal organs, causing its relaxation.

Fenpiverinium bromide – an m-cholinolytic exerts an additional spasmolytic effect on smooth muscles.

Pharmacokinetics

Metamizole sodium is well and rapidly absorbed from the gastrointestinal tract. It is hydrolyzed in the intestinal wall to form an active metabolite; unchanged Metamizole sodium is absent in the blood (only after intravenous administration a slight concentration is detected in plasma). The binding of the active metabolite to plasma proteins is 50-60%. It is metabolized in the liver and excreted by the kidneys. At therapeutic concentrations, it penetrates into breast milk.

Pitofenone is rapidly absorbed from the gastrointestinal tract; C_max in plasma is reached within 30-60 minutes; it is rapidly distributed in organs and tissues and is excreted in the urine sufficiently quickly. T_1/2 is 1.8 hours.

Fenpiverinium bromide is rapidly absorbed from the gastrointestinal tract and reaches maximum plasma concentration within 1 hour. It is excreted by the kidneys 32.4-40.4% unchanged, and by the intestines 2.5-5.3%.

Indications

Mild or moderately severe pain syndrome associated with spasms of the smooth muscles of internal organs

Biliary colic;
Spasms of the smooth muscles of the gastrointestinal tract organs;
Biliary dyskinesia of the hyperkinetic type;
Algodysmenorrhea.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
K80	Cholelithiasis [cholelithiasis] (including biliary colic)
K82.8	Other specified diseases of gallbladder and cystic duct (including dyskinesia)
N94.4	Primary dysmenorrhea
N94.5	Secondary dysmenorrhea
R10.4	Other and unspecified abdominal pain (colic)
R52.0	Acute pain
R52.2	Other chronic pain

ICD-11 code	Indication
DC11.Z	Cholelithiasis, unspecified
DC1Z	Diseases of gallbladder and biliary tract, unspecified
DD93.1	Infantile colic
DD94	Functional disorder of the gallbladder
GA34.3	Dysmenorrhea
MD81.4	Other and unspecified abdominal pain
MG30.Z	Chronic pain syndrome, unspecified
MG31.Z	Acute pain, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Tablets

Orally, without chewing, with a small amount of liquid.

Adults and adolescents over 15 years— 1-2 tablets 2-3 times a day; the maximum daily dose should not exceed 6 tablets. Children 13-15 years 1 tablet 2-3 times a day. Children 8-12 years 1/2 tablet 2-3 times a day.

The course of treatment should not exceed 5 days.

Solution

A single dose for adults and adolescents over 15 years is 2-5 ml (IV or IM); daily dose – up to 10 ml.

Intravenous administration in a single dose exceeding 2 ml is possible only after careful clarification of indications.

When prescribing the drug to children (including infants) the daily dose is set based on body weight.

Body weight / Age	Daily dose for IV administration	Daily dose for IM administration
5-8 kg/3-5 months	–	0.1-0.2 ml
9-15 kg/1-2 years	0.1-0.2 ml	0.2-0.3 ml
16-23 kg/3-4 years	0.2-0.3 ml	0.3-0.4 ml
24-30 kg/5-7 years	0.3-0.4 ml	0.4-0.5 ml
31-45 kg/8-12 years	0.5-0.6 ml	0.6-0.7 ml
46-53 kg/12-15 years	0.8-1.0 ml	0.8-1.0 ml

The IV drug should be administered slowly (1 ml over at least 1 minute), with the patient in a lying position and under the control of blood pressure, heart rate, and respiratory rate. During administration, the solution should be at body temperature.

Adverse Reactions

Allergic reactions skin rash, itching, urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), angioedema; malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospasm, anaphylactic shock.

From the central nervous system headache, dizziness.

From the organ of vision blurred vision, accommodation paresis.

From the digestive system dry mouth, heartburn, constipation.

From the urinary system impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red coloration of urine (due to metabolites of sodium metamizole), difficulty urinating.

From the cardiovascular system decreased blood pressure, tachycardia, cyanosis.

From the hematopoietic organs thrombocytopenia, leukopenia, agranulocytosis (may manifest with the following symptoms: unmotivated rise in body temperature, chills, sore throat, painful swallowing, stomatitis, as well as the development of vaginitis or proctitis).

Contraindications

Severe impairment of liver and/or kidney function;
Decompensation of chronic heart failure;
Severe angina pectoris;
Tachyarrhythmia;
Glucose-6-phosphate dehydrogenase deficiency;
Closed-angle glaucoma;
Prostatic hyperplasia (with clinical manifestations);
Inhibition of bone marrow hematopoiesis (including granulocytopenia);
Intestinal obstruction;
Megacolon;
Collapse;
Hypersensitivity to the components of the drug (as well as to other pyrazolone derivatives).

With caution

Mild and moderate renal and/or hepatic insufficiency;
Tendency to arterial hypotension, bronchospasm;
Increased sensitivity to NSAIDs or non-narcotic analgesics (including a history of a complete or incomplete combination of bronchial asthma, nasal polyposis and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.).

Use in Pregnancy and Lactation

The use of the drug during pregnancy and breastfeeding is contraindicated.

Use in Hepatic Impairment

With caution in mild and moderate hepatic insufficiency.

Use in Renal Impairment

With caution in mild and moderate renal insufficiency.

Pediatric Use

Prescribed for children from 8 years of age.

Special Precautions

It is not recommended to take ethanol during treatment with the drug.

While taking Plenalgin (due to the sodium metamizole it contains), the development of agranulocytosis is possible, therefore, if an unmotivated rise in temperature, chills, sore throat, difficulty swallowing, stomatitis, symptoms of vaginitis or proctitis are detected, as well as if thrombocytopenia is detected, immediate withdrawal of the drug is necessary.

Taking the drug in patients with atopic bronchial asthma and hay fever increases the risk of developing allergic reactions.

It is unacceptable (until the causes of the pain syndrome are clarified) to use the drug to relieve acute abdominal pain.

During the drug intake, caution should be exercised by drivers of vehicles and persons engaged in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Overdose cases are possible if the dosing regimen is not followed.

Symptoms dry mouth, nausea, vomiting, abdominal pain, decreased blood pressure, impaired sweating, drowsiness, accommodation paresis, confusion, impaired liver and kidney function, convulsions.

Treatment gastric lavage, intake of activated charcoal, symptomatic therapy.

Drug Interactions

Radiocontrast agents, colloidal blood substitutes and penicillin should not be used during treatment with drugs containing Metamizole sodium. With simultaneous use of sodium metamizole with cyclosporine, the concentration of the latter in the blood decreases.

Metamizole sodium, displacing oral hypoglycemic drugs, indirect anticoagulants, glucocorticosteroids and indomethacin from binding to plasma proteins, increases their effect.

Phenylbutazone, barbiturates and other inducers of liver microsomal enzymes with simultaneous use reduce the effectiveness of sodium metamizole.
Simultaneous use with non-narcotic analgesics, tricyclic antidepressants, hormonal contraceptives and allopurinol can lead to increased toxicity of sodium metamizole.

Sedative and anxiolytic drugs (tranquilizers) enhance the analgesic effect of sodium metamizole.

Thiamazole and cytostatics increase the risk of developing leukopenia against the background of the use of drugs containing Metamizole sodium.

The effect of sodium metamizole is enhanced by codeine, H₂-histamine receptor blockers and propranolol (slows down metabolism).

Myelotoxic drugs enhance the manifestations of hematotoxicity of sodium metamizole.

Butyrophenone derivatives, phenothiazine, tricyclic antidepressants, H₁-histamine receptor blockers, amantadine and quinidine enhance the m-cholinolytic effect of fenpiverinium bromide.

With simultaneous use of fenpiverinium bromide and phenothiazine derivatives (for example, chlorpromazine), the development of severe hyperthermia may be observed.

Metamizole sodium enhances the effect of ethanol.

Storage Conditions

In a dry place protected from light at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 5 years.

Dispensing Status

Over-the-counter.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer