Orvis Flu, 10 pcs.

Pharmacotherapeutic group:

Pharmacotherapy for symptoms of acute respiratory diseases (ARI) and “colds” (analgesic non-narcotic + H1-histamine receptor blocker + vitamin).

The ATX code: N02BE51

Pharmacological properties

Pharmacodynamics

A combination drug containing paracetamol, pheniramine and ascorbic acid.

Paracetamol is a non-narcotic analgesic, blocks cyclooxygenase, mainly in the central nervous system, affecting the centers of pain and thermoregulation; it has analgesic and antipyretic effects.

Pheniramine is a blocker of H1-histamine receptors; it reduces rhinorrhea and lacrimation, eliminates spastic phenomena, edema and hyperemia of the nasal cavity mucosa, nasopharynx and sinus cavities.

Ascorbic acid is involved in the regulation of redox processes, carbohydrate metabolism, blood coagulation, tissue regeneration, the synthesis of steroid hormones, reduces vascular permeability, reduces the need for vitamins B1, B2, A, E, folic acid, pantothenic acid.

It improves the tolerance of paracetamol and prolongs its effects (associated with prolongation of the half-life (T1/2)).

Pharmacokinetics

Paracetamol

After oral administration is quickly absorbed from the gastrointestinal tract: maximum plasma concentrations of the drug are reached after 10-60 minutes.

The drug is rapidly distributed throughout the body tissues and penetrates the blood-brain barrier.

The binding to plasma proteins is insignificant and has no therapeutic value, but increases with increasing dose.

Metabolism occurs in the liver, 80% of the dose taken enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form inactive metabolites.

One of the hydroxylated metabolic intermediates has hepatotoxic effects.

This metabolite is neutralized by conjugation with glutathione, but it can cumulate and in case of paracetamol overdose (150 mg paracetamol/kg or 10 g of oral paracetamol) cause necrosis of hepatocytes.

Extracted by the kidneys as metabolites, mainly as conjugates. Less than 5% of the dose taken is excreted unchanged. T1/2 is 1 to 3 hours.

Pheniramine

It is almost completely absorbed in the digestive tract. The T1/2 from blood plasma is 1 to 1.5 hours. It is eliminated from the body mainly through the kidneys.

Ascorbic acid

It is absorbed in the small intestine. Bioavailability is approximately 70%. Time of reaching the maximum therapeutic concentration after oral administration – 4 hours. It is metabolized mainly in the liver. It is excreted by the kidneys, through the intestine, with sweat, unchanged and as metabolites.

Indications

Active ingredient

Composition

Interaction

Ethanol increases the sedative effect of antihistamines (pheniramine), so it should be avoided during treatment.

In addition, ethanol in concomitant use with pheniramine promotes the development of acute pancreatitis.

Pheniramine increases the effect of sedatives:

Morphine derivatives, barbiturates, benzodiazepine derivatives and other tranquilizers, neuroleptics (meprobamate, phenothiazine derivatives), antidepressants (amitriptyline, mirtazapine, mianserine), hypotensive drugs of central action, sedatives belonging to the H1-histamine blockers, baclofen;

In this case, not only the sedative effect increases, but also the risk of side effects of the drug (urinary retention, dry mouth, constipation).

When used in combination with other drugs with anticholinergic properties (other antihistamines, antidepressants of imipramine group, phenothiazine-type neuroleptics, m-cholinoblocking antiparkinsonics, atropine-like antispasmodics, disopyramide) the central atropine-like effects may be increased.

When using the drug together with inducers of microsomal oxidation: barbiturates, tricyclic antidepressants, anticonvulsants (phenytoin), flumecinol, phenylbutazone, rifampicin and ethanol, the risk of hepatotoxic effects increases significantly (due to the paracetamol contained in it).

Glucocorticosteroids when used concomitantly increase the risk of glaucoma.

Concomitant use with salicylates increases the risk of nephrotoxic effects.

Concomitant use with levomycetin (chloramphenicol) increases the toxicity of the latter.

The paracetamol contained in the drug increases the effect of indirect anticoagulants and reduces the effectiveness of uricosuric drugs.

Directions for use

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

Similarities