Antigrippin

Antigrippin is a combination medicine intended for symptomatic treatment of colds and flu. It contains three active components: paracetamol, chlorphenamine maleate and ascorbic acid. Each of these components has its own specific action, which together provides comprehensive treatment.

1. Paracetamol:

   • Action: Has analgesic and antipyretic properties. Helps reduce pain and temperature.
   • Mechanism: Blocks the synthesis of prostaglandins in the central nervous system, which reduces pain and lowers body temperature.

2. Chlorphenamine maleate:

   • Action: An antihistamine that eliminates allergy symptoms such as runny nose, watery eyes, and itching.
   • Mechanism: Blocks histamine H1 receptors, which reduces the manifestation of allergic reactions.

3. Ascorbic acid (vitamin C):

   • Action: Strengthens the immune system, increases the body's resistance to infections, improves tissue regeneration.
   • Mechanism: Participates in oxidation-reduction processes, collagen synthesis, carbohydrate and lipid metabolism.

Indications Antigrippina

Antigrippin is used to relieve cold and flu symptoms such as:

• Headache.
• Elevated temperature.
• Runny nose.
• Pain in muscles and joints.
• Sneezing and watery eyes.

Release form

1. Effervescent tablets:
   • Tablets that dissolve in water to make a drink.
   • Convenient for fast and effective absorption of active ingredients.
2. Powder for solution preparation:
   • A powder that dissolves in water to make a drink.
   • It also provides rapid absorption and symptom relief.

Pharmacodynamics

Paracetamol

• Mechanism of action: Paracetamol has an analgesic (pain-relieving) and antipyretic effect by blocking the synthesis of prostaglandins in the central nervous system (CNS). It inhibits the enzyme cyclooxygenase (COX), which leads to a decrease in the formation of prostaglandins, which are responsible for pain and inflammation.
• Effects: Reduces body temperature and relieves pain during colds and flu.

Chlorphenamine maleate

• Mechanism of action: Chlorphenamine is an antihistamine that blocks histamine H1 receptors. This prevents the action of histamine, which is a mediator of allergic reactions.
• Effects: Reduces allergy symptoms such as runny nose, sneezing, itchy nose and eyes, and watery eyes. Chlorphenamine also has a mild sedative effect, which can help improve sleep during colds.

Ascorbic acid (vitamin C)

• Mechanism of action: Ascorbic acid is involved in numerous metabolic processes. It is an important antioxidant that protects cells from damage by free radicals. It also plays a key role in the synthesis of collagen, increasing the strength and integrity of vascular walls and tissues.
• Effects: Strengthening the immune system, increasing the body's resistance to infections, accelerating the healing and tissue restoration processes.

Synergistic effect

The combination of these three components allows Antigrippin to effectively combat a wide range of cold and flu symptoms. Paracetamol reduces pain and fever, chlorphenamine reduces allergic reactions and improves overall well-being, and ascorbic acid supports immunity and speeds up recovery.

This multi-component approach helps alleviate the patient's condition and promote faster recovery from colds and flu.

Pharmacokinetics

Paracetamol

• Absorption: Paracetamol is rapidly and completely absorbed from the gastrointestinal tract. Maximum plasma concentration is reached 0.5-2 hours after administration.
• Distribution: Distributed evenly throughout tissues, penetrates the placental barrier, and enters breast milk. Plasma protein binding is low — about 10-25%.
• Metabolism: Metabolized in the liver by conjugation with glucuronic and sulfuric acids. Less than 5% of the dose undergoes hydroxylation to form the active metabolite, which is then conjugated with glutathione.
• Excretion: Excreted by the kidneys, mainly as metabolites; about 3% is excreted unchanged. The half-life is 1-4 hours.

Chlorphenamine maleate

• Absorption: Chlorphenamine is rapidly absorbed from the gastrointestinal tract, reaching maximum plasma concentrations within 2-6 hours.
• Distribution: Penetrates well into tissues, including the central nervous system. Plasma protein binding is about 70%.
• Metabolism: Metabolized in the liver by demethylation and oxidation. The main metabolites are desmethylchlorphenamine and dihydroxychlorphenamine.
• Excretion: Excreted by the kidneys as metabolites and unchanged. The half-life is 12-15 hours.

Ascorbic acid

• Absorption: Ascorbic acid is rapidly absorbed from the gastrointestinal tract. Maximum plasma concentration is reached after 2-3 hours.
• Distribution: Distributed throughout all tissues of the body, with high concentrations in endocrine glands, liver, leukocytes and the lens of the eye. Plasma protein binding is approximately 25%.
• Metabolism: Metabolized in the liver to dihydroascorbic acid and other metabolites.
• Excretion: Excreted by the kidneys, both unchanged and as metabolites. The half-life is about 16 days at high doses and 3-4 hours at normal doses.

Combined action

The combination of paracetamol, chlorphenamine and ascorbic acid in Antigrippin provides fast and effective relief of cold and flu symptoms. Each of the substances complements the action of the other, helping to improve the patient's general condition and speed up the recovery process.

Dosing and administration

Pills:

• Adults and children over 15 years: 1 tablet every 4-6 hours as needed. Maximum daily dose is 4 grams (8 tablets).
• Children 10 to 15 years: ½-1 tablet every 6-8 hours as needed. Maximum daily dose is 2 grams (4 tablets).
• Children aged 5 to 10 years: ½ tablet every 6-8 hours as needed. Maximum daily dose is 1 gram (2 tablets).
• Children aged 3 to 5 years: ¼-½ tablet every 6-8 hours as needed. Maximum daily dose is 500 mg (1 tablet).

Powder for solution preparation:

• Adults and children over 15 years of age: 1-2 sachets 2-3 times a day.
• Children from 10 to 15 years old: 1 sachet 2-3 times a day.
• For children aged 5 to 10 years: ½-1 sachet 2-3 times a day.
• For children aged 3 to 5 years: ½ sachet 2-3 times a day.

Liquid form (syrup):

Syrup dosages are usually given in milliliters, not milligrams. Follow the instructions on the package or your doctor's instructions to determine the correct dosage in milliliters, depending on the child's age or the recommendations for adults.

Spray for topical use:

• Adults and children over 12 years: 1-2 sprays in each nostril 3-4 times a day.
• Children 6 to 12 years: 1 spray in each nostril 3-4 times daily.
• Children 3 to 6 years: 1 spray in each nostril 1-2 times daily.

Use Antigrippina during pregnancy

1. Paracetamol (acetaminophen):

   • Paracetamol is widely used to treat pain and fever in pregnant women. Research shows that it is considered relatively safe when taken at recommended doses. However, some studies have linked long-term use of paracetamol during pregnancy to an increased risk of behavioral and neurodevelopmental problems in children, such as ADHD and autism spectrum disorders (Liew et al., 2014), (Thiele et al., 2015).

2. Chlorphenamine maleate:

   • Chlorphenamine is an antihistamine used to reduce allergy and cold symptoms. Although there is limited data on its safety during pregnancy, it is typically used in low doses and is considered relatively safe for short-term use. However, antihistamine use in the first trimester requires caution due to potential risks to the fetus (Sun et al., 2006).

3. Ascorbic acid:

   • Ascorbic acid (vitamin C) is safe to use during pregnancy when taken in recommended doses. It is important for maintaining a healthy immune system and does not pose a threat to the fetus (Garmonov & Salakhov, 2009).

Contraindications

General contraindications for all components

1. Hypersensitivity to any of the components of the drug.
2. Age up to 15 years (for adult forms of release) or up to 12 years (for children's forms), unless otherwise indicated in the instructions.

Contraindications associated with paracetamol

1. Severe liver disease (including acute liver failure).
2. Severe renal failure.
3. Congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson syndrome, etc.).
4. Alcoholism.
5. Glucose-6-phosphate dehydrogenase deficiency.

Contraindications associated with chlorphenamine maleate

1. Closed-angle glaucoma.
2. Prostatic hypertrophy with urinary retention.
3. Severe cardiovascular diseases.
4. Peptic ulcer of the stomach and duodenum in the acute stage.

Contraindications associated with ascorbic acid

1. Hyperoxaluria (increased excretion of oxalates in urine).
2. Severe kidney disease.
3. Thrombophlebitis and tendency to thrombosis.
4. Glucose-6-phosphate dehydrogenase deficiency (may lead to hemolytic anemia).

Additional contraindications

1. Pregnancy and lactation: The drug is not recommended for use without consulting a doctor, since the safety of use during these periods has not been established.
2. Diabetes mellitus: Since the drug may contain sugar or other sweeteners, this factor must be taken into account when used in patients with diabetes mellitus.

Side effects Antigrippina

Common side effects:

1. Drowsiness or dizziness: Particularly common with formulas containing chlorphenamine maleate.
2. Dry mouth: Due to the anticholinergic properties of chlorphenamine.
3. Stomach disorders: May include nausea, vomiting, diarrhea, or indigestion.
4. Allergic reactions: Include skin rash, itching, hives, or swelling of the face, lips, tongue, and throat.

Related to paracetamol:

1. Liver damage: If the recommended dose of paracetamol is exceeded, hepatotoxicity, including acute liver failure, may develop.
2. Allergic reactions: May include hives, itching, skin rash, or angioedema.

Related to chlorphenamine maleate:

1. Drowsiness and decreased alertness: These effects may result in impaired motor coordination and impaired reaction times.
2. Urethral stenosis: Possible worsening of the course of dysuric conditions in men with prostatic hypertrophy.

Related to ascorbic acid:

1. Stomach disorders: Include nausea, vomiting, heartburn, or diarrhea, especially with high doses.
2. Kidney Stones: Long-term and/or excessive use of vitamin C may increase the risk of kidney stones in some people.

Overdose

1. Symptoms of paracetamol:

   • Nausea.
   • Vomiting.
   • Stomach ache.
   • Loss of appetite.
   • Drowsiness or weakness.
   • Increased activity of liver enzymes in the blood (according to test results).
   • Liver damage, including acute liver failure (in severe cases).

2. Symptoms of Chlorphenamine Maleate:

   • Drowsiness.
   • Blurred vision.
   • Dry mouth.
   • Lowering blood pressure.
   • Tachycardia (increased heart rate).

3. Symptoms of ascorbic acid:

   • Increased acidity of gastric juice.
   • Diarrhea.
   • Risk of kidney stones (with prolonged and/or excessive use).

Interactions with other drugs

1. Medicines containing paracetamol:

   • Taking several medications containing paracetamol at the same time can lead to overdose and liver damage.
   • This is especially important to consider when taking pain medications, headache medications, or antipyretics at the same time.

2. Drugs that have a hepatotoxic effect:

   • The combined use of Antigrippin with other drugs that can damage the liver may increase the risk of developing hepatotoxic effects.
   • These medications may include certain antibiotics, antiviral drugs, and drugs used to treat seizures.

3. Drugs that have a sedative effect:

   • Antigrippin contains chlorphenamine, which has a sedative effect. Combined use with other drugs that also have a sedative effect (e.g., sleeping pills, tranquilizers, antidepressants) can enhance this effect and lead to increased drowsiness and inhibition.

4. Drugs that have anticholinergic action:

   • Chlorphenamine maleate, contained in Antigrippin, has anticholinergic properties. Combined use with other drugs with anticholinergic effects (e.g. pain medications, antihistamines) may lead to an increase in these effects, such as dry mouth, constipation and urinary retention.

5. Drugs that affect the circulatory system:

   • Chlorphenamine maleate may enhance the hypotensive effect of antihypertensive drugs and may also enhance tachycardia caused by sympathomimetic amines.

6. Preparations containing vitamin C:

   • Long-term and/or excessive use of vitamin C-containing drugs together with Antigrippin may increase the risk of kidney stones.