Acetaminophen + Caffeine
ACETAMIN® EXTRA
Film coated tablet
Category:
Mild analgesic and antipyretic (www.medicines.org.uk)
Chemistry:
Acetaminophen/caffeine (500 mg/65 mg) film coated tablets.
Acetaminophen: N-(4-hydroxyphenyl)acetamide
C8H9NO2 = 151.2
Caffeine: 1,3,7-Trimethylpurine-2,6(3H,1H)-dione
C8H10N4O2 = 194.2 (Martindale)
Pharmacokinetics:
The absorption of paracetamol by oral route is complete and quick. Maximum plasma concentrations are reached 30 to 60 minutes after ingestion. Excretion is almost exclusively renal, in the form of conjugated metabolites. The plasma protein binding is low.
Caffeine is rapidly and completely absorbed. Maximum plasma concentrations are achieved within one hour and the plasma half-life is about 3.5 hours. 65 - 80% of administered caffeine is metabolized by the liver and excreted in the urine as 1-methyluric acid and 1-methylxanthine.
(www.medicines.org.uk & vidal)
Indications
Symptomatic treatment of mild to moderate pain and/or febrile conditions (vidal)
Contraindications:
- This medicine is not suitable for children (under 15) because of its caffeine content.
- Hypersensitivity to paracetamol, caffeine or any of the other constituents.
- Hepatocellular insufficiency. (www.medicines.org.uk & vidal)
Warnings & Precautions:
- To avoid the risk of overdose, check for paracetamol in the composition of other drugs.
- Due to the presence of caffeine, the drug can cause insomnia, it should not be taken late in the day.
- Care is advised in the administration of paracetamol to patients with renal or hepatic impairment. The hazard of overdose is greater in those with non-cirrhotic alcoholic liver disease.
- Excessive intake of caffeine (e.g. coffee, tea and some canned drinks) should be avoided while taking this product.
- Do not exceed the stated dose.
- Patients should be advised to consult their doctor if their headaches become persistent.
- Paracetamol may distort blood glucose by oxidase method peroxidase glucose in case of abnormally high concentrations.
- Paracetamol can alter the dosage of the blood uric acid by the method phosphotungstic acid.
(www.medicines.org.uk & vidal)
Pregnancy and Breast – feeding:
FDA Pregnancy Category: C
Paracetamol-caffeine is not recommended for use during pregnancy due to the possible increased risk of lower birth weight and spontaneous abortion associated with caffeine consumption.
Caffeine in breast milk may potentially have a stimulating effect on breast fed infants.
Due to the caffeine content of this product it should not be used if you are pregnant or breast feeding. (www.medicines.org.uk)
Drug Interactions:
Enoxacin, stiripentol, ciprofloxacin, norfloxacin, oral anticoagulants (warfarin and other coumarins), metoclopramide, domperidone, colestyramine. (www.medicines.org.uk & vidal)
Adverse Reactions:
Hypersensitivity reactions to type of anaphylaxis, angioedema, rash, urticaria, skin rash, Steven Johnson syndrome/toxic epidermal necrolysis, thrombocytopenia, agranulocytosis (leukopenia and neutropenia), hepatic dysfunction, excitement, insomnia, palpitations, nervousness, dizziness, bromchospasm (There have been cases of bronchospasm with paracetamol, but these are more likely in asthmatics sensitive to aspirin or other NSAIDs).
- When the recommended paracetamol-caffeine dosing regimen is combined with dietary caffeine intake, the resulting higher dose of caffeine may increase the potential for caffeine-related adverse effects such as insomnia, restlessness, anxiety, irritability, headaches, gastrointestinal disturbances and palpitations. (www.medicines.org.uk & vidal)
OVERDOSE:
Immediate treatment is essential in the management of paracetamol overdose. Gastric lavage or the administration of activated charcoal may be beneficial when performed within one hour of the overdose but can be considered for up to four hours after the overdose. Antidotes such as N-acetylcysteine (NAC) and methionine protect the liver if administered within 12 hours of overdose. NAC is effective up to and possibly beyond 24 hours. General supportive measures must be available.
Symptoms of paracetamol overdose in the first 24 hours are pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12 to 48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur. In severe poisoning, hepatic failure may progress to encephalopathy, coma and death. Acute renal failure with acute tubular necrosis may develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have been reported. Liver damage is possible in adults who have taken 10g or more of paracetamol. It is considered that excess quantities of a toxic metabolite (usually adequately detoxified by glutathione when normal doses of paracetamol are ingested) become irreversibly bound to liver tissue.
Overdose of caffeine may result in epigastric pain, vomitting, diuresis, tachycardia or cardia arrhythmia, CNS stimulation (insomnia, restlessness, excitement, agitation, jitteriness, tremors and convulsions).
It must be noted that for clinically significant symptoms of caffeine overdose to occur with this product, the amount ingested would be associated with serious paracetamol-related toxicity.
(www.medicines.org.uk)
DOSAGE AND ADMINISTRATION:
Two tablets up to four times daily
It is usually not necessary to exceed 3 grams of acetaminophen per day (6 tablets). However, in case of more severe pain, the maximum dose may be increased up to 4 grams per day or 8 tablets per day. Always respect a 4 hour interval between doses.
The tablets are swallowed whole with a beverage (eg water, milk, fruit juice).
www.medicines.org.uk & vidal))
Storage:
Store below 30°C.
How supplied:
Acetaminophen/caffeine (500 mg/65 mg) film coated tablets are manufactured at Tehran Darou pharmaceuticals and are available, blister of ? in a box of ?׳s.