Paramax

Paramax is an antipyretic and analgesic drug.

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Indications Paramaxa

It is used to eliminate mild or moderate pain, as well as to reduce high temperatures that occur against the background of various diseases.

Release form

The medicine is released in the form of rectal suppositories, 5 pieces inside a strip. The box contains 2 strips.

Pharmacodynamics

The medication has antipyretic and analgesic, as well as weak anti-inflammatory properties.

The effect of the drug is due to the suppression of PG binding processes, as well as a preferential effect on the thermoregulatory center within the hypothalamus.

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Pharmacokinetics

Absorption of paracetamol after rectal administration occurs at a lower rate than in the case of oral administration, but it is more complete. Peak plasma values are recorded after 2-3 hours after administration.

Paracetamol is distributed at high speed within all tissues. The substance indices within plasma, blood and saliva have comparable values. The level of synthesis of the component with plasma protein is quite low.

Metabolic processes involving paracetamol occur inside the liver. During these processes, inactive compounds with sulfates and glucuronic acid are formed.

The minimal metabolic pathway, which is catalyzed by hemoprotein P450, causes the formation of an intermediate type reagent (the element N-acetylbenzoquinoneimine). In case of its normal use, it is quickly detoxified by reduced glutathione and then excreted with urine after conjugation processes with mercatopurine acid and cysteine. But in case of severe intoxication, the volume of this metabolic product increases.

Excretion occurs mainly in urine. Approximately 90% of the dose used is excreted via the kidneys within 24 hours (mostly as glucuronic acid conjugates (60-80%)), and in addition as sulfate conjugates (20-30%).

Less than 5% of the drug is excreted unchanged.

Half-life is 4-5 hours.

In case of severe renal failure (creatinine clearance level is less than 10 ml/minute), the excretion of paracetamol and its breakdown products slows down.

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Dosing and administration

The medicine is used only under the supervision of a doctor. Particular caution is required when using Paramax in infants under 1 year of age.

Suppositories are administered rectally. It is prohibited to divide them to obtain the required portion. If it is necessary to use a single portion, the size of which is less than the volume of one suppository, you should consult a doctor and use paracetamol in other forms of release (such as an oral solution, for example).

In case of treatment in children, the portion size is calculated taking into account the child's weight. Taking this into account, the optimal form of release of the drug is selected. Below is the approximate age of children, in accordance with their weight.

Rectal suppositories of 80 mg are used in children weighing 4-6 kg (age approximately 1-4 months). It is necessary to administer 3-4 suppositories per day to the patient, with intervals of 6 hours, taking into account his weight at the rate of 60 mg/kg/day.

Rectal suppositories of 150 mg are prescribed to children weighing between 8-12 kg (the age of such children is about 0.5-2 years). The sizes of daily portions, the scheme of application and the form of calculations are similar to those indicated above.

The recommended daily dose of paracetamol is approximately 60 mg/kg. It is divided into 4 doses of 15 mg/kg at 6-hour intervals. If the patient has severe renal failure (creatinine clearance level is below 10 ml/minute), the interval between doses should be at least 8 hours.

Due to the risk of local toxicity, it is prohibited to use more than 4 suppositories per day. The duration of the course of treatment with the rectal method of administration of the drug should be the minimum necessary.

Contraindications

Main contraindications:

• the presence of hypersensitivity to paracetamol or other medicinal components;
• infants under 1 month of age (and children weighing less than 4 kg);
• severe renal or hepatic functional disorders;
• congenital hyperbilirubinemia;
• deficiency of the element G6PD in the body;
• alcoholism;
• blood diseases, leukopenia, and also severe anemia;
• inflammatory process in the area of the intestinal mucosa, as well as problems with the functioning of the anus;
• use for diarrhea.

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Side effects Paramaxa

The use of suppositories may lead to the appearance of certain side effects:

• signs of allergy: angioedema, anaphylaxis, urticaria and erythema, as well as rashes on the epidermis and mucous membranes, itching, TEN, and also MEE;
• disorders of the hematopoietic system: thrombocyto-, leuko- and neutropenia, anemia (possibly of a hemolytic nature), as well as sulfhemoglobinemia with methemoglobinemia (the appearance of cyanosis, pain in the heart area and dyspnea);
• respiratory system dysfunction: the appearance of spasms in the bronchi in people with hypersensitivity to aspirin, as well as other NSAIDs;
• problems with digestive activity: epigastric pain, nausea, functional liver disorders, as well as increased activity of liver enzymes (usually without the appearance of jaundice later) and hepatonecrosis (this effect depends on the size of the dose of the drug);
• disorders of the endocrine system: development of hypoglycemia, which can develop into a hypoglycemic coma;
• Lesions at the injection site: irritation developing in the area of the anus and rectum.

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Overdose

To avoid intoxication with the medication, it is prohibited to take it with other medications that contain paracetamol.

There is a risk of poisoning in young children (there have been cases of both drug overdose and accidental intoxication), which can be fatal.

Children weighing less than 37 kg can be administered a maximum of 80 mg/kg of the drug per day.

For children weighing between 38-50 kg, the maximum daily dose of the medicine is 3 g.

Children weighing more than 50 kg are allowed to receive no more than 4 g of the therapeutic agent per day.

A single dose of 150 mg/kg may cause hepatocellular insufficiency, metabolic acidosis, glucose metabolism disorders, hypoglycemia, hemorrhages, and also encephalopathy, coma, and death. At the same time, liver transaminase, bilirubin, and LDH levels increase, and prothrombin values decrease over 12-48 hours.

Acute renal failure, which is accompanied by acute tubular necrosis, as well as severe pain in the lumbar region and proteinuria with hematuria, may occur even in the absence of severe liver damage. In addition, pancreatitis with cardiac arrhythmia has been observed.

Long-term use of the drug in high doses can lead to many complications:

• manifestations from the hematopoietic system: agranulocytosis, leukopenia, thrombocyto-, neutro- and pancytopenia, as well as aplastic anemia;
• CNS dysfunction: agitation of a psychomotor nature, dizziness, and in addition, disorientation;
• lesions affecting the urinary organs: development of nephrotoxicity (necrotic papillitis, renal colic and tubulointerstitial nephritis);
• digestive disorders: the appearance of hepatonecrosis.

In people with risk factors (such as long-term use of phenytoin, carbamazepine, as well as St. John's wort and primidone with phenobarbital and rifampicin or other drugs that induce liver enzymes; frequent alcohol abuse; deficiency in the glutathione system (improper diet); as well as starvation, AIDS, cachexia and cystic fibrosis) the use of paracetamol in a dosage of 5+ g can cause liver damage, which manifests itself 12-48 hours after poisoning.

In case of intoxication, the victim should be taken to the hospital immediately, even in the absence of early signs of poisoning. Signs of the disorder appear during the first 24 hours: vomiting with nausea, pallor, loss of appetite, and abdominal pain. It is necessary to take into account that the symptoms may not quite adequately reflect the severity of poisoning or the likelihood of damage. Among the proposed emergency treatment measures:

• emergency hospitalization;
• detection of paracetamol levels in blood plasma;
• gastric lavage;
• use of an antidote – oral administration of N-acetylcysteine or methionine (during the first 10 hours after intoxication);
• symptomatic measures.

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Interactions with other drugs

The use of paracetamol in maximum daily doses (4 g) for at least 4 days may potentiate the effect of oral anticoagulants and increase the risk of bleeding. It is necessary to monitor INR values at regular intervals. If necessary, the dose of the anticoagulant taken during paracetamol therapy can be adjusted.

The absorption rate of Paramax may be increased when combined with domperidone and metoclopramide, and decreased when combined with cholestyramine.

Barbiturates weaken the antipyretic properties of paracetamol.

Anticonvulsants (including carbamazepine, as well as barbiturates with phenytoin), which stimulate the activity of liver microsomal enzymes, are capable of increasing the toxic effect of drugs on the liver by increasing the degree of conversion of the drug into hepatotoxic decay products.

The combination of the drug with hepatotoxic drugs increases the degree of hepatotoxic effect on the liver.

Combining large doses of the drug with rifampicin or isoniazid increases the likelihood of hepatotoxic syndrome.

The effectiveness of diuretics is reduced when combined with paracetamol.

It is prohibited to combine the medicine with alcoholic beverages.

High levels of paracetamol can affect laboratory readings for blood glucose levels (using the oxidase-peroxidase method) and uric acid levels (using the phosphotungstic acid method).

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Storage conditions

Paramax should be kept in a place closed to small children. Temperature level – within 25°C.

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Shelf life

Paramax can be used for 2 years from the date of manufacture of the drug.

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Application for children

During therapy in children, it is necessary to calculate dosages taking into account the child's weight. Taking this into account, the appropriate form of the medication is selected.

Suppositories with a volume of 80 mg are administered to children weighing 4-6 kg (infants aged 1-4 months).

Suppositories with a volume of 150 mg are used for administration to children weighing 8-12 kg (children aged 0.5-2 years).

Analogues

The drug's analogues are such medications as Paracetamol with Paracetamol-Altpharm, and also Efferalgan, Panadol with Teraflu and Dolaren with Cefekon D. The list also includes Antigrippin and Caffetin.

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