Usage
- This combination medication is primarily prescribed for the symptomatic relief of the common cold, flu, and upper respiratory allergies. It addresses symptoms such as fever, headache, body aches, nasal congestion, runny nose, sneezing, sore throat, and watery eyes.
- Pharmacological Classification: This is a combination product containing:
- Analgesic (Paracetamol)
- Antipyretic (Paracetamol)
- Decongestant (Phenylephrine)
- Antihistamine (Chlorpheniramine)
- Stimulant (Caffeine)
- Mechanism of Action: Paracetamol reduces fever and pain. Phenylephrine shrinks nasal blood vessels to relieve congestion. Chlorpheniramine blocks histamine, reducing allergic symptoms. Caffeine acts as a mild stimulant, counteracting the drowsiness of chlorpheniramine and enhancing the analgesic effect of paracetamol.
Alternate Names
- While no specific international non-proprietary name (INN) exists for this exact combination, it’s commonly referred to by its components.
- Brand Names: Brand names vary depending on the manufacturer and region. Some examples include “Sinarest,” “Col-Col,” “Fevagrip,” and “Restocin.” Many other brand names are available.
How It Works
- Pharmacodynamics: Paracetamol inhibits prostaglandin synthesis, reducing fever and pain. Phenylephrine is an alpha-1 adrenergic agonist, causing vasoconstriction and reducing nasal congestion. Chlorpheniramine is an H1-receptor antagonist, blocking the effects of histamine. Caffeine stimulates the central nervous system, reducing fatigue and drowsiness.
- Pharmacokinetics:
- Absorption: All components are absorbed well orally.
- Metabolism: Primarily hepatic metabolism, mainly via CYP450 enzymes (especially CYP2E1 for paracetamol).
- Elimination: Mostly renal excretion for all components, with some biliary excretion for paracetamol metabolites.
- Mode of Action:
- Paracetamol: Inhibits cyclooxygenase (COX) enzymes in the central nervous system, reducing prostaglandin synthesis. The exact mechanism of its central analgesic action is not fully understood.
- Phenylephrine: Stimulates alpha-1 adrenergic receptors on vascular smooth muscle, leading to vasoconstriction.
- Chlorpheniramine: Competitively binds to H1 receptors, preventing histamine from binding and triggering allergic responses.
- Caffeine: Antagonizes adenosine receptors, leading to increased neuronal activity. It also increases intracellular calcium levels and inhibits phosphodiesterase.
- Elimination Pathways: Primarily renal excretion for all components, with paracetamol undergoing hepatic metabolism to glucuronide and sulfate conjugates. A minor pathway for paracetamol involves CYP2E1 metabolism to a reactive metabolite (NAPQI), which is detoxified by glutathione.
Dosage
Standard Dosage
Adults:
- One tablet every 4-6 hours as needed. Do not exceed the recommended daily dose (which varies with the specific formulation). A maximum of 4 g of paracetamol per day from all sources should generally not be exceeded.
Children:
- Dosage varies according to age and weight and should be determined and closely monitored by a physician. This combination may not be suitable for children under 6 years of age.
Special Cases:
- Elderly Patients: Start with a lower dose and monitor for side effects.
- Patients with Renal Impairment: Dosage adjustment may be necessary.
- Patients with Hepatic Dysfunction: Reduce dosage or avoid use, particularly with severe impairment.
- Patients with Comorbid Conditions: Caution in patients with hypertension, diabetes, cardiovascular disease, hyperthyroidism, glaucoma, and prostatic hypertrophy.
Clinical Use Cases
- This combination is not typically indicated for specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use is primarily for symptomatic relief of common cold and flu symptoms.
Dosage Adjustments
- Dosage adjustments are essential for patients with renal or hepatic impairment, and in elderly patients. Consider patient-specific factors, including other medications and comorbidities.
Side Effects
Common Side Effects
- Drowsiness
- Dizziness
- Dry mouth
- Nausea
- Constipation
- Restlessness or excitability (especially in children)
Rare but Serious Side Effects
- Allergic reactions (rash, itching, swelling, difficulty breathing)
- Hepatotoxicity (with paracetamol overdose)
- Hypertension
- Tachycardia
- Hallucinations
- Seizures
Long-Term Effects
- Potential for hepatotoxicity with chronic paracetamol overuse.
- Potential for medication overuse headache.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (anaphylaxis)
- Liver failure (with paracetamol overdose)
- Hypertensive crisis
Contraindications
- Hypersensitivity to any component.
- Severe liver disease.
- Severe hypertension or coronary artery disease.
- Recent use of MAO inhibitors (within 14 days).
- Narrow-angle glaucoma.
- Pyloroduodenal or bladder neck obstruction.
- Prostatic hypertrophy.
Drug Interactions
- Alcohol: Increased drowsiness and risk of hepatotoxicity.
- MAO inhibitors: Risk of hypertensive crisis.
- Tricyclic antidepressants: Increased anticholinergic effects.
- Beta-blockers: Reduced effectiveness of phenylephrine.
- Other medications that cause drowsiness (e.g., sedatives, opioids): Additive effects.
- CYP2E1 inducers (e.g., alcohol, isoniazid): Increased risk of paracetamol toxicity.
- Warfarin: Possible altered anticoagulant effect.
Pregnancy and Breastfeeding
- Not recommended during pregnancy, especially the third trimester, due to potential risks to the fetus (low birth weight, premature birth).
- Use with caution during breastfeeding. The components are excreted in breast milk and could cause adverse effects in the infant.
Drug Profile Summary
- Mechanism of Action: See above.
- Side Effects: See above.
- Contraindications: See above.
- Drug Interactions: See above.
- Pregnancy & Breastfeeding: Not recommended in pregnancy. Use with caution in breastfeeding.
- Dosage: See above.
- Monitoring Parameters: Blood pressure, liver function tests (especially with long-term use or high doses of paracetamol).
Popular Combinations
This combination is itself a commonly used multi-drug formulation. It is not generally combined with other medications.
Precautions
- Pre-existing medical conditions: See Contraindications and Special Cases under Dosage.
- Lifestyle: Avoid alcohol. Caution when driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Caffeine + Chlorpheniramine Maleate + Paracetamol + Phenylephrine?
A: See Standard Dosage section.
Q2: Can this combination be used in children?
A: Dosage should be carefully determined and monitored by a physician based on the child’s age and weight. Not generally recommended for children under 6.
Q3: What are the common side effects?
A: See Common Side Effects section.
Q4: Can I take this medication if I have high blood pressure?
A: Use with caution in patients with hypertension. Phenylephrine can raise blood pressure. Close monitoring is necessary.
Q5: Can I take this while pregnant or breastfeeding?
A: Not recommended during pregnancy, especially the third trimester. Use with caution during breastfeeding.
Q6: Can I drink alcohol while taking this medication?
A: No. Alcohol can increase drowsiness and the risk of liver damage from paracetamol.
Q7: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is close to the time for your next dose. Do not double the dose to catch up.
Q8: What are the signs of paracetamol overdose?
A: Nausea, vomiting, abdominal pain, loss of appetite, sweating, confusion, and jaundice. Immediate medical attention is required.
Q9: Can I take this combination with other cold and flu medications?
A: Avoid taking this medication with other products containing paracetamol or decongestants, as this can lead to exceeding the maximum recommended daily dose. Consult a physician or pharmacist before combining with other medications.
Q10: How long should I take this medication?
A: Consult your doctor. Generally, this medication should not be used for more than 7 days without medical advice.
