Paramax

Paramax is an antipyretic and analgesic drug.

[1], [2]

Indications of the paramax

It is used to eliminate mild or moderate pain, as well as to reduce high fever, which are noted against a background of various diseases.

Release form

The drug is produced in the form of rectal suppositories, 5 pieces per strip. The box contains 2 strips.

Pharmacodynamics

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

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

[3], [4], [5]

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 application.

Paracetamol is distributed at high speed within all tissues. The indices of the substance inside the 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, non-active compounds with sulfates as well as glucuronic acid are formed.

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

Excretion occurs mainly along with urine. Approximately 90% of the dosage used is excreted through the kidneys over a period of 24 hours (more in the form of glucuronic acid with conjugates (60-80%)), and in addition sulfate-type conjugates (20-30%).

Less than 5% of the drug is excreted unchanged.

The half-life is 4-5 hours.

With a severe renal insufficiency (KC level - less than 10 ml / min), the excretion of paracetamol with its degradation products is slowing.

[6], [7], [8]

Dosing and administration

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

Suppositories are administered rectally. Separate them to get the required portion is prohibited. If you need a single dose, which is smaller than the volume of one candle, you should consult a doctor and use paracetamol in other forms of release (such as oral solution, for example).

In case of treatment in children, the size of the portion is calculated taking into account the weight of the child. With this in mind, the optimal form of drug production is also selected. Below is the approximate age of children, according to their weight.

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

Rectal suppository with a volume of 150 mg is prescribed for children weighing 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 conducted calculations are similar to those mentioned above.

The recommended daily dose of paracetamol is about 60 mg / kg. It is divided into 4 applications - 15 mg / kg at intervals of 6 hours. If the patient has renal insufficiency in severe form (CC level is below 10 ml / minute), the interval between uses should be at least 8 hours.

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

Contraindications

The main contraindications:

• the presence of hypersensitivity to paracetamol or other medicamentous elements;
• infants less than 1 month of age (and children weighing less than 4 kg);
• renal or hepatic functional disorders in severe degree;
• having a congenital hyperbilirubinemia;
• deficiency of the G6PD element in the body;
• alcoholism;
• blood diseases, leukopenia, as well as anemia of a pronounced nature;
• inflammatory process in the intestinal mucosa, as well as problems with the activity of the anus;
• application for diarrhea.

[9]

Side effects of the paramax

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

• signs of allergy: angioedema, anaphylaxis, urticaria and erythema, and in addition to rashes on the epidermis and mucous membranes, pruritus, TEN, and also MEE;
• disorders of the hematopoietic system: thrombocyto-, leuko- and neutropenia, anemia (possibly hemolytic), and also sulfemoglobinemia with methemoglobinemia (the appearance of cyanosis, pain in the heart and dyspnea);
• disorders of the respiratory system: 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 hepatic disorders, as well as an increase in the activity of the action of liver enzymes (usually without jaundice afterwards) and hepatonecrosis (this effect depends on the size of the portion of the drug);
• disorders of the endocrine system: development of hypoglycemia, which can develop into a hypoglycemic coma;
• lesions at the site of administration: irritation developing in the anus and rectum.

[10]

Overdose

To avoid intoxication with medicines, it is forbidden to use other drugs with paracetamol.

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

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

Children with a weight in the range of 38-50 kg, the maximum daily dose of the drug is a maximum of 3 g.

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

One-time use of 150 mg / kg may lead to the development of hepatocellular insufficiency in the child, the metabolic form of acidosis, glucose metabolism disorders, hypoglycemia, hemorrhages, and besides encephalopathy, coma and death. At the same time, liver transaminases, bilirubin and LDH increase, and prothrombin values decrease within 12-48 hours.

The acute form of kidney failure, against which there is acute tubular necrosis, and in addition strong pain sensations in the lumbar region and proteinuria with hematuria, can occur even in the absence of liver damage in severe degree. In addition, there was pancreatitis with cardiac arrhythmia.

Prolonged use of the drug in high amounts can lead to many complications:

• manifestations of the hematopoietic system: agranulocytosis, leuko-, thrombocyto-, neutropenic and pancytopenia, and in addition aplastic form of anemia;
• disorders of the central nervous system: an excitation that has a psychomotor character, dizziness, and in addition, an orientation disorder;
• lesions affecting the urinary tract: development of nephrotoxicity (necrotic papillitis, colic in the kidney and tubulointerstitial nephritis);
• disorders of digestive activity: the appearance of hepatonecrosis.

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

In case of intoxication, the victim should be immediately brought to the hospital, even if there are no early manifestations of poisoning. Signs of disturbance occur during the first 24 hours: it is vomiting with nausea, pallor, loss of appetite, and in addition abdominal pain. It should be borne in mind that the symptoms may not adequately reflect the severity of poisoning or the likelihood of injury. Among the proposed urgent medical measures:

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

[11], [12]

Interactions with other drugs

The use of paracetamol in maximum daily portions (4 g) for a minimum of 4 days can lead to potentiation of the effect of oral anticoagulants, as well as an increase in the likelihood of bleeding. It is required to monitor the values of INRs through the same time intervals. If required, it is possible to correct the portion of the received anticoagulant during therapy with paracetamol.

The rate of absorption of Paramax can increase when combined with domperidone and metoclopramide, and also decrease when combined with cholestyramine.

Barbiturates weaken the antipyretic properties of paracetamol.

Anticonvulsants (including carbamazepine, as well as barbiturates with phenytoin), stimulating the activity of hepatic microsomal enzymes, can increase the toxic effect of drugs against the liver - by increasing the degree of conversion of the drug into hepatotoxic degradation products.

Combination of the drug with hepatotoxic drugs increases the degree of hepatotoxic effects against the liver.

Combination of large portions of the drug with rifampicin or isoniazid increases the likelihood of a hepatotoxic syndrome.

The efficacy of diuretic agents is weakened when combined with paracetamol.

It is forbidden to combine the medicine with alcoholic beverages.

High paracetamol levels can be influenced by laboratory indications when detecting the level of glucose inside the blood (with the help of oxidase-peroxidase method), and in addition the uric acid values (application of the method with phosphotungstic acid).

[13], [14], [15]

Storage conditions

Paramax is required to be kept in a place that is closed from small children. The temperature level is within 25 ° C.

[16]

Shelf life

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

[17]

Application for children

During therapy, children need to calculate dosages, taking into account the weight of the child. In view of this, a suitable form of the medicine 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 to administer to children weighing 8-12 kg (children 0.5-2 years old).

Analogues

Analogues of the drug are such drugs as Paracetamol with Paracetamol-Altpharm, and besides Efferalgan, Panadol with Teraflu and Dolaren with Cefekon D. The list also includes Antigrippin and Caffetin.

[18], [19]