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Product Name
:
NEW-CETAMOL
Chemical Name
:
Paracetamol+Caffeine
Therapeutic Category
:
Analgesic & Anesthetic
Pharmacologic Category
:
Analgesic, Miscellaneous
Pharmaceutical Form
:
Tablets
Composition
:
Paracetamol 500mg+Caffeine 65mg
Monitoring Parameters
Dosing
 
Dosing: Adult
Route of administration: Oral.
Adults, the elderly and children over 12 years of age:
2 tablets up to 4 times daily as required.
The dose should not be repeated more frequently than every 4 hours and not more than 4 doses should be given in any 24 hour period.
As caffeine is found naturally in tea, coffee and chocolate, and in some carbonated drinks there is the potential for users to take more than the recommended 520 mg/day of caffeine (8 tablets) per day. Therefore users should take account of dietary and other medicinal sources of caffeine and ensure that they do not exceed the stated dose.

Dosing: Pediatric

Not recommended for children under 12 years of age.

Dosing: Geriatric

Refer to adult dosing.
Use
 
For the treatment of mild to moderate pain including headache, migraine, neuralgia, toothache, sore throat, period pains, symptomatic relief of sprains, strains, rheumatic pains, sciatica, lumbago, fibrositis, muscular aches and pains, joint swelling and stiffness, influenza, feverishness and feverish colds
Adverse Reactions
 
Adverse events from historical clinical trial data are both infrequent and from small patient exposure. Accordingly, events reported from extensive post-marketing experience at therapeutic/labelled dose and considered attributable are listed below by system class. Due to limited clinical trial data, the frequency of these adverse events is not known (cannot be estimated from available data), but post-marketing experience indicates that adverse reactions to paracetamol are rare and serious reactions are very rare.

Paracetamol
Body System
Undesirable effect
Blood and lymphatic system disorders
Thrombocytopenia, agranulocytosis
 
Agranulocytosis
Immune system disorders
Anaphylaxis
 

Cutaneous hypersensitivity reactions including skin rashes, angioedema, Stevens Johnson syndrome / toxic epidermal necrolysis

Respiratory, thoracic and mediastinal disorders
Bronchospasm
Hepatobiliary disorders
Hepatic dysfunction

* There have been cases of bronchospasm with paracetamol, but these are more likely in asthmatics sensitive to aspirin or other NSAIDs.

Caffeine

Body System
Undesirable effect
Central nervous system
Nervousness,
 
Dizziness

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 restlessness and palpitations.

Undesirable effects are not normally observed in healthy individuals taking caffeine at doses up to 520 mg per day. However some users who are caffeine naïve, have abstained from caffeine for a period or who are more sensitive to caffeine may experience effects more commonly seen at higher doses. These include tremor, insomnia, nervousness, irritability, anxiety, headache, tinnitus, arrhythmia, and tachycardia, diuresis, gastrointestinal disturbances and elevated respiration. Individuals who experience these effects must stop taking this medicine (and any others containing caffeine) and any other dietary caffeine.

Following regular use of caffeine, cessation of intake may lead to withdrawal symptoms which may last for up to a week and which include headache, tiredness and decreased alertness.


Contraindications
 
Hypersensitivity to paracetamol, caffeine and/or other constituents.
This medicine should not be used by people who have been diagnosed with hypertension or who are receiving antihypertensive medication, or who have a history of cardiac arrhythmia.
This medicine should not be used by patients recovering from chronic alcoholism who are taking disulfiram.
This medicine should not be used if antidepressants (including lithium carbonate), anxiolytics (including clozapine) and sedatives are being used , or by persons with anxiety disorders.
This medicine should not be used by any persons who are also taking ephedrine .
Caffeine shares the same metabolic pathway as theophylline and therefore this medicine should not be used concurrently with theophylline.
Warnings / Precautions Drug
 
Patients should be advised to consult their doctor if their headaches become persistent.
- Do not exceed the stated dose
- Keep all medicines out of the reach and sight of children
- Do not take with any other paracetamol-containing products
- Immediate medical advice should be sought in the event of an overdose, even if you feel well, because of the risk of delayed, serious liver damage.
- Care is advised in the administration of paracetamol to patients with severe renal or severe hepatic impairment. The hazards of overdose are 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.
Interactions
 
As caffeine is found naturally in tea, coffee and chocolate, and in some carbonated drinks there is the potential for users to take more than the recommended 520 mg/day of caffeine (8 tablets) per day. Therefore users should take account of dietary and other medicinal sources of caffeine and ensure that they do not exceed the stated dose .
Xanthine derivatives such as caffeine can weaken the vasodilating effect of substances used for myocardial imaging such as adenosine and dipyridamole. Therefore, caffeine should be avoided for 24 hours before myocardial imaging.
Caffeine, a CNS stimulant, has an antagonistic effect towards the action of sedatives and tranquilizers.
Caffeine may enhance the tachycardic effect of phenylpropanolamine.
Caffeine exerts a competitive inhibition of the metabolism of clozapine. Therefore clozapine and caffeine must not be used concurrently (see contraindications).
Caffeine can increase blood pressure and counters the hypotensive action of beta blockers such as atenolol, metoprolol, oxprenolol and propranolol. This medicine should not be used at the same time as beta blockers.
Disulfiram increases caffeine clearance by up to 50%. Concomitant use of disulfiram and caffeine should be avoided (see contraindications).
Use of lithium carbonate and caffeine may cause a small to moderate rise in serum lithium levels. Concomitant use should be avoided (see contraindications).
Monoamine oxidase inhibitors may increase the stimulant effects of caffeine.
Methoxsalen reduces clearance of caffeine and may increase the effects of caffeine.
Phenytoin doubles caffeine clearance, although caffeine does not affect the metabolism of phenytoin.
Pipemidic acid reduces caffeine clearance, enhancing the effects of caffeine.
Theophylline and caffeine share the same metabolic pathway, leading to increased clearance times for theophylline when used concurrently with caffeine. Concomitant use should be avoided (see contraindications).
Levothyroxine, like caffeine can increase blood pressure, and therefore these two active ingredients should not be used concurrently.
Ephedrine and caffeine interact to produce significant cardiovascular effects. Therefore caffeine should be avoided when ephedrine is being taken.
The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by colestyramine.
The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.
Pregnancy
 
Pregnancy Implications

Epidemiological studies in human pregnancy have shown no ill effects due to paracetamol used in the recommended dosage, but patients should follow the advice of their doctor regarding its use.
However, 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.
Lactation
 
Paracetamol is excreted in breast milk but not in a clinically significant amount. Available published data do not contraindicate breast feeding.
Caffeine appears in breast milk. Irritability and poor sleeping pattern in the infant have been reported. Caffeine in breast milk may potentially have a stimulating effect on breast fed infants.
Therefore, due to caffeine content of this product it should not be used if you are pregnant or breast feeding.
Mechanism of Action
 
Paracetamol

ANALGESIC
:
The mechanism of analgesic action has not been fully determined. Paracetamol may act predominantly by inhibiting a prostaglandin synthesis in the central nervous system (CNS) and to a lesser extent through a peripheral action by blocking pain-impulse generation. The peripheral action may also be due to inhibition of prostaglandin synthesis or to inhibition of the synthesis or actions of other substances that sensitise pain receptors to mechanical or chemical stimulation.

ANTIPYRETIC:

Paracetamol probably produces antipyresis by acting centrally on the hypothalamic heat-regulating centre to produce peripheral vasodilation resulting in increased blood flow through the skin, sweating, and heat loss. The central action probably involves inhibition of prostaglandin synthesis in the hypothalamus.

Caffeine

Central nervous system stimulant – Caffeine stimulates all levels of the CNS, although its cortical effects are milder and of shorter duration than those of amfetamines.

ANALGESIA ADJUNCT:

Caffeine constricts cerebral vasculature with an accompanying decrease in cerebral blood flow and in the oxygen tension of the brain. It is believed that caffeine helps to relieve headache by providing a more rapid onset of action and/or enhanced pain relief with lower doses of analgesic. Recent studies with ergotamine indicate that the enhancement of effect by the addition of caffeine may also be due to improved gastrointestinal absorption of ergotamine when administered with caffeine.
Pharmacodynamics / Kinetics
 
PARACETAMOL

Absorption and Fate

Paracetamol is readily absorbed from the gastro-intestinal tract with peak plasma concentrations occurring about 30 minutes to 2 hours after ingestion. It is metabolised in the liver and excreted in the urine mainly as the glucuronide and sulphate conjugates. Less than 5% is excreted as unchanged paracetamol. The elimination half-life varies from about 1 to 4 hours. Plasma-protein binding is negligible at usual therapeutic concentrations but increases with increasing concentrations.
A minor hydroxylated metabolite which is usually produced in very small amounts by mixed-function oxidases in the liver and which is usually detoxified by conjugation with liver glutathione may accumulate following paracetamol overdosage and cause liver damage.

CAFFEINE


Absorption and Fate

Caffeine is absorbed readily after oral administration and is widely distributed throughout the body. Caffeine is metabolised almost completely via oxidation, demethylation, and acetylation, and is excreted in the urine as 1-methyluric acid, 1-methylxanthine, 7-methylxanthine, 1,7-dimethylxanthine (paraxanthine), 5-acetylamino-6-formylamino-3-methyluracil (AFMU), and other metabolites with only about 1% unchanged.
 
   
 
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