Paracetamol + Ascorbic acid - instructions for use, dose, side effects, contraindications

Has antipyretic, analgesic and anti-inflammatory effect. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and mucous membranes of the gastrointestinal tract, and therefore has little effect on the synthesis of prostaglandins in peripheral tissues.

Ascorbic acid

Regulates the transport of hydrogen ions in oxidation-reduction reactions, including in the process at any stage of the Krebs cycle. Participates in the regulation of carbohydrate metabolism. Provides absorption of iron in the intestine, transferring it from trivalent into a divalent form, facilitating its incorporation into heme. Participates in the formation of tetrahydrofolic acid, the synthesis of steroid hormones, norepinephrine and adrenaline, collagen, prothrombin, glycogen. Inactivates hyaluronidase, activating the regeneration of tissues and normalizing the permeability of capillaries. Disinfects toxins and has an antioxidant effect, catching free radicals. He takes an active part in the regulation of immune processes: enhances the formation of antibodies, phagocytic activity and the synthesis of interferon. It inhibits the release of histamine and strengthens its degeneration, suppresses the release of mediators of inflammation and allergic reactions.

Lengthens the action of paracetamol by slowing its excretion and improves its tolerability.

Pharmacokinetics:

Paracetamol

After oral administration, it is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 20-30 minutes.The connection with plasma proteins is 15%. Penetrates through the blood-brain barrier, enters the breast milk.

Metabolism in the liver by glucuronation and sulfation (80%) with formation of inactive metabolites, about 17% is hydroxylated to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block the enzyme systems of the liver, causing necrosis of hepatocytes.

Half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.

Ascorbic acid

Completely absorbed from the gastrointestinal tract after ingestion. The connection with plasma proteins is 25%. Normally, the concentration of ascorbic acid in the blood is 15-20 μg / ml. The concentration of ascorbic acid in erythrocytes and plasma is lower than in platelets and leukocytes.

Ascorbic acid is oxidized to dehydroascorbic acid, metabolized to inactive ascorbate-2-sulfate and oxalic acid, then excreted in the urine. In cases of exceeding the dose (more than 200 mg.) ascorbic acid is eliminated by the kidneys in an unchanged form.

Indications:

It is used to treat febrile conditions for colds, it is used to relieve pain syndrome of mild or moderate severity in arthralgia, myalgia, migraine. Neuralgia, headache and toothache, as well as with algodismenorrhea.

ICD-10

VI.G40-G47.G43 Migraine

X.J00-J06.J06.9 Acute upper respiratory tract infection, unspecified

X.J10-J18.J10 Influenza caused by an identified influenza virus

XI.K00-K14.K08.8 Other specified changes in teeth and their supporting apparatus

XIII.M20-M25.M25.5 Pain in the joint

XIII.M70-M79.M79.1 Myalgia

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

XIV.N80-N98.N94.4 Primary dysmenorrhea

XIV.N80-N98.N94.5 Secondary dysmenorrhea

XVIII.R50-R69.R50 Fever of unknown origin

XVIII.R50-R69.R51 Headache

Contraindications:

Bleeding in the gastrointestinal tract, phenylketonuria, deficiency of glucose-6-phosphate dehydrogenase, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance.

Carefully:

Gilbert's syndrome, viral hepatitis, old age, alcoholism.

Pregnancy and lactation:

Recommendations for FDA - category is not defined. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Children

Inside, up to 6 years: 10-15 mg / kg at one time;

6-10 years: for ½ bags or ½ tablets, not more than 2 tablets or 2 bags per day;

10-12 years: 1 sachet or ½ tablets - daily dose 3 sachets or 2 tablets;

12-18 years: 1 packet, not more than 4 bags per day.

Adults

Inside, between meals 1-2 tablets (2-4 bags) 1-3 times a day.

The highest daily dose: 4 g (12 tablets).

The highest single dose: 15 mg / kg.

Side effects:

Allergic reactions.

Overdose:

Symtomas: diarrhea, anorexia - with acute overdose (develops 6-14 hours after exceeding the dose), with chronic (develops 2-4 days after exceeding the dose) - hypocoagulation, DIC syndrome, cerebral edema, rarely - fulminant renal failure due to tubular necrosis .

Necrosis of liver cells, due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinonimine.

Treatment: application of donators SH-groups, precursors of the synthesis of glutathione-methionine and N-acetylcysteine within 12 hours after an overdose.

Interaction:

Strengthens the effect of indirect coagulants and toxicity of chloramphenicol.

The intake of ethanol in the treatment of the drug leads to the development of acute pancreatitis.

Simultaneous use with stimulators of microsomal oxidation in the liver - barbiturates, rifampicin, ethanol, phenylbutazone, phenothionine, increases the toxicity of paracetamol.

Reduces the risk of hepatotoxic effects of microsomal oxidation inhibitors (cimetidine).

Special instructions:

Monitoring of glucose and uric acid in the plasma, the composition of peripheral blood, the functional state of the liver.

Instructions

Paracetamol + Ascorbic acid (Paracetamolum + Acidum ascorbinicum)