Grippostad C, capsules 10 pcs

Pharmacodynamics

Combined drug for treating symptoms of colds.

Ascorbic acid is involved in the regulation of redox processes, carbohydrate metabolism, blood clotting, tissue regeneration (repair), the synthesis of steroid hormones;

increases resistance to infection, 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 effect (delays its elimination).

Caffeine has antispasmodic (relaxing) effect, expands the bronchi, tones cerebral vessels, stimulates the heart, has a general tonic effect.

Caffeine is a derivative of xanthine, it enhances the analgesic effect of paracetamol.

Paracetamol has analgesic (pain reliever), antipyretic and weak anti-inflammatory effect due to its influence on the thermoregulation center in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues.

Chlorphenamine is an antihistamine drug with antiallergic effect: it reduces nasal discharge and congestion, lacrimation and sneezing.

The combination of components of the drug provides better tolerance of symptoms of malaise and fever in acute respiratory viral infections and other colds.
Pharmacokinetics

Ascorbic acid

Absorbed in the proximal small intestine. Binding with plasma proteins – 25%.

It easily penetrates into leukocytes, platelets and then into all tissues; the highest concentration is achieved in glandular organs, leukocytes, liver and eye lens; penetrates through the placenta.

Metabolized primarily in the liver to deoxyascorbic acid and then to oxalic acid and ascorbate-2-sulfate.

Excreted by kidneys through the intestines, with sweat, breast milk unchanged and as metabolites.

Caffeine

Fully and quickly absorbed. Maximal concentrations are observed during the period from 5 to 90 minutes after the intake on an empty stomach.

In adults it is almost completely eliminated through hepatic metabolism.

There is a pronounced variability of individual elimination values in adults.

The average elimination half-life (T1/2/) from plasma is 4.9 h within the range of 1.9-12.2 h.

Caffeine is distributed in all body fluids. The binding of caffeine to plasma proteins is 35%.

Caffeine is almost completely metabolized by oxidation, demethylation and acetylation and excreted by the kidneys. The main metabolites are 1-methylxanthine, 7-methylxanthine, 1,7-dimethylxanthine.

Paracetamol

Fully and rapidly absorbed in the gastrointestinal tract, the maximum plasma concentrations are found after 30-60 minutes.

Paracetamol is rapidly distributed in most body tissues, penetrates through the placenta and is present in breast milk.

In therapeutic concentrations, binding to plasma proteins is insignificant and increases with increasing concentration.

It is subjected to primary metabolism in the liver, eliminated mainly in the urine as glucuronide and sulfate compounds.

Half-life period is 1-3 hours.

The hydroxylated metabolite, which forms in small amounts in the liver under the influence of mixed oxidases and is usually neutralized by binding to glutathione, can accumulate in paracetamol overdose and cause liver damage.

Chlorphenamine

Maximum plasma concentration is reached 1-2 hours after ingestion.

The duration of action is 3-6 hours.
Metabolism is mainly carried out in the liver via hydroxylation and conjugation as well as demethylation and formation of N- and S-oxides.

Bioavailability when taken orally is 25-50% due to a pronounced first pass effect that decreases in liver function insufficiency.

Binding with blood plasma proteins is 69-72%. Apparent volume of distribution of the drug is relatively high and amounts to 3-7 liters per kilogram of body weight.

The half-life from plasma of chlorphenamine in adult patients is 15-36 hours, and in children – 10-13 hours.
For patients with renal insufficiency a prolongation of the metabolites elimination half-life should be taken into account.

Depending on pH level (acidic or alkaline environment) 0-34% of the administered dose is excreted in the urine as unchanged chlorphenamine.

Accumulation is possible with prolonged use.

Indications

Active ingredient

Composition

Associates:

Lactose monohydrate,

Glyceryl tristearate,

Gelatin.

Capsule contents:

Gelatin,

Water,

Titanium dioxide.

Capsule cap composition:

Gelatin,

Quinoline yellow,

Water,

Sunset Yellow dye,

Titanium dioxide.

How to take, the dosage

Overly with a small amount of liquid, 2 capsules per dose.

If necessary, repeat in the same dose in 4-6 hours 3-4 times a day.

The maximum daily dose should not exceed 12 capsules.

Interaction

Ethanol promotes the development of acute pancreatitis. Microsomal oxidation inhibitors (cimetidine) reduce the risk of hepatotoxic effects.

The drug reduces the effectiveness of uricosuric drugs.

It enhances the effect of drugs that depress the central nervous system, ethanol.

In case of delayed gastric emptying (propantelin) there may be a delayed onset of action of paracetamol.

If gastric emptying is accelerated (metoclopramide), the drug takes effect more quickly. The toxicity of chloramphenicol is increased.

Perhaps caution should be exercised with prolonged use of paracetamol and concomitant therapy with oral blood-clotting inhibitors.

Stimulants of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase production of hydroxylated active metabolites, which causes the possibility of severe intoxication in case of small overdose.

Myelotoxic drugs increase manifestations of hematotoxicity of the drug.

Special Instructions

It is not recommended that Grippostad C be used for more than 3 days as an antipyretic and more than 5 days as an analgesic without medical supervision.

In case of hyperthermia (high body temperature) lasting more than 3 days and pain syndrome for more than 5 days, a physician’s consultation is required.

Ascorbic acid, which is part of Grippostad C, distorts the results of laboratory tests assessing the concentration of glucose and uric acid in the plasma.

Do not use simultaneously other medicinal products containing paracetamol, as well as other non-narcotic analgesics and NSAIDs (metamisole, acetylsalicylic acid, ibuprofen, etc.), as well as barbiturates, antiepileptic drugs, rifampicin, chloramphenicol.

The simultaneous use of other drugs should be coordinated with the doctor. When using for more than 5 days the peripheral blood picture and the functional state of liver should be controlled.

Persons who are prone to drink ethanol should consult their physician before starting treatment with the drug, because paracetamol may have a damaging effect on the liver.

Contraindications

Side effects

In therapeutic doses the drug is usually well tolerated.

Sometimes there may be skin allergic reactions (skin rash, pruritus, urticaria, angioedema); gastrointestinal disorders (nausea, epigastric pain, dry mouth); difficulty in urination.

Rarely – disorders of the blood system (anemia, leukopenia – decreased content of leukocytes in the blood, thrombocytopenia – decreased content of platelets in the blood).

In prolonged use in high doses (more than 12 caps. daily for more than 5 days) – hepatotoxic effect, blood system disorders; erosive-ulcerous lesions of the gastrointestinal tract; nephrotoxicity (papillary necrosis).

Overdose

Symptoms (caused by paracetamol): pallor of the skin, decreased appetite, nausea, vomiting; hepatonecrosis (severity of necrosis, due to intoxication, directly depends on the degree of overdose).

The toxic effect in adults is possible after taking more than 10-15 g of paracetamol: increase of liver transaminases activity, increase of prothrombin time (12-48 hours after taking it); the detailed clinical picture of liver damage is seen after 1-6 days.

Rarely, liver failure develops fulminantly and may be complicated by renal failure (tubular necrosis).

Treatment: administration of SH-group donators and precursors of glutathione synthesis – methionine 8-9 hours after overdose and N-acetylcysteine – after 12 hours.

The need for additional therapeutic measures (further administration of methionine, intravenous N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.