Paracetamol
(Acetaminophen)
1.
Indications:
Paracetamol is primarily used as an analgesic
and antipyretic agent, meaning it is effective for:
- Pain relief
(mild to moderate pain): headaches, toothaches, muscle aches, back pain,
arthritis, and menstrual cramps.
- Fever reduction:
Commonly used in cases of fever associated with cold, flu, or infections.
- It is also used for conditions such as osteoarthritis
and post-surgical pain.
2.
Pharmacology:
- Mechanism of Action:
Paracetamol inhibits the synthesis of prostaglandins in the central
nervous system (CNS) and works primarily in the brain to reduce fever and
alleviate pain. It does not possess significant anti-inflammatory activity
like nonsteroidal anti-inflammatory drugs (NSAIDs).
- Absorption:
Paracetamol is rapidly absorbed from the gastrointestinal tract. Peak
plasma concentration is achieved within 30 to 60 minutes after oral
administration.
- Metabolism:
Primarily metabolized in the liver through conjugation to form glucuronide
and sulfate metabolites. A small portion is metabolized by cytochrome P450
into a reactive metabolite, which is neutralized by glutathione.
- Excretion:
Primarily excreted in the urine. Most of the drug is excreted as
metabolites (glucuronide and sulfate conjugates), with less than 5%
excreted unchanged.
3.
Dosage & Administration:
- Adults:
500 mg to 1,000 mg every 4-6 hours as needed. Do not exceed 4,000 mg (4 g)
per day to avoid the risk of liver damage.
- Children:
Dosage is based on weight. Typically, 10-15 mg/kg every 4-6 hours, not
exceeding 60 mg/kg per day.
- Routes of Administration: Oral (tablets, liquid), intravenous (IV), rectal
suppositories.
4.
Interactions:
- Alcohol:
Increased risk of liver toxicity when taken with alcohol.
- Warfarin:
Prolonged use of high doses of paracetamol may increase the anticoagulant
effect of warfarin, increasing the risk of bleeding.
- Anticonvulsants (e.g., carbamazepine, phenobarbital,
phenytoin): These drugs may induce
hepatic enzymes that increase the metabolism of paracetamol, potentially
enhancing its hepatotoxicity.
- Rifampin:
Can increase the metabolism of paracetamol, also increasing the risk of
liver damage.
5.
Contraindications:
- Hypersensitivity:
Paracetamol is contraindicated in individuals with known hypersensitivity
to it.
- Severe Liver Impairment: Should not be used in individuals with severe liver
disease or active hepatic impairment.
- Severe Renal Impairment: Dose adjustment or avoidance is necessary in cases of
severe renal impairment.
6.
Side Effects:
- Common:
Generally well-tolerated. However, occasional side effects can include
nausea, vomiting, and mild allergic reactions (rash, itching).
- Rare/Serious:
Hepatotoxicity (liver damage), especially in overdose. In very rare cases,
serious skin reactions like Stevens-Johnson syndrome (SJS), toxic
epidermal necrolysis (TEN), and acute generalized exanthematous pustulosis
(AGEP) may occur.
7.
Pregnancy & Lactation:
- Pregnancy:
Paracetamol is generally considered safe for use during pregnancy. It is
often the first-line analgesic and antipyretic recommended for pregnant
women. However, some studies suggest a potential link to behavioral issues
in children with frequent use during pregnancy, so it should be used only
when necessary.
- Lactation:
Paracetamol is excreted in breast milk in small quantities, but it is
considered safe for use by breastfeeding mothers at recommended doses.
8.
Precautions & Warnings:
- Liver Disease:
Use with caution in patients with pre-existing liver conditions or a
history of alcohol abuse. Paracetamol overdose can lead to fatal hepatic
necrosis.
- Kidney Disease:
Prolonged use or high doses may lead to renal impairment, especially in
those with existing kidney disease.
- Alcohol Use:
Caution in those who consume alcohol regularly, as they are at higher risk
of liver damage.
- Geriatric Population:
Monitor liver and kidney function as both decline with age.
- Chronic Use:
Avoid chronic use of high doses due to the risk of liver damage.
9.
Overdose Effects:
- Symptoms of Overdose:
Nausea, vomiting, abdominal pain, jaundice, confusion, liver failure, and
even death in severe cases.
- Treatment:
Overdose should be treated promptly with N-acetylcysteine (NAC), which
replenishes glutathione and detoxifies the harmful metabolite of
paracetamol. NAC is most effective when administered within 8 hours of
overdose.
10.
Therapeutic Class:
- Analgesic and Antipyretic. It is classified as a non-opioid analgesic.
11.
Storage Conditions:
- Store at room temperature (15°C - 30°C or 59°F - 86°F),
away from heat, moisture, and direct sunlight.
- Keep out of reach of children to prevent accidental
overdose.
12.
Chemical Structure:
- IUPAC Name:
N-(4-hydroxyphenyl)acetamide
- Molecular Formula:
C8H9NO2
- Molecular Weight:
151.16 g/mol
- Chemical Structure:
Common
Questions about Paracetamol (FAQ)
https://www.healthcitylife.com/
- What is Paracetamol used for? Paracetamol is used for relieving pain (headaches,
muscle pain, toothaches) and reducing fever. It's commonly found in
over-the-counter cold and flu medications.
- Is Paracetamol safe for children? Yes, Paracetamol is safe for children when given in
the correct dose based on weight. Always follow pediatric dosage
guidelines.
- What happens if I take too much Paracetamol? Overdose of Paracetamol can cause serious liver
damage, and if untreated, it can be fatal. If you suspect an overdose,
seek medical help immediately.
- Can I take Paracetamol with other medications? Paracetamol is generally safe with many medications,
but it can interact with certain drugs like warfarin, anticonvulsants, and
alcohol. Always check with a healthcare provider before combining
medications.
- Is Paracetamol an anti-inflammatory drug? No, unlike NSAIDs (like ibuprofen), Paracetamol does
not have significant anti-inflammatory effects. It primarily works on pain
and fever.
- Can pregnant women take Paracetamol? Yes, Paracetamol is considered safe during pregnancy,
but it should be used only when necessary and as recommended by a
healthcare professional.
- Can Paracetamol cause allergies? Allergic reactions to Paracetamol are rare, but they
can occur. Symptoms may include rash, swelling, and difficulty breathing.
If any of these occur, seek medical attention immediately.
- How long does it take for Paracetamol to work? Paracetamol typically starts working within 30 minutes
to 1 hour after oral administration.
- Is Paracetamol addictive? No, Paracetamol is not addictive. It does not have the
potential for abuse like opioid medications.
- Can Paracetamol cause drowsiness? No, Paracetamol does not typically cause drowsiness. It is a non-sedating pain reliever.
