GEBEDOL XTRA

 

COMPOSITION
Each uncoated tablet contains:

Paracetamol BP 500 mg,

Ibuprofen BP 400,

Caffeine (Anhydrous) BP 30mg,

Color: Erythrosine.

MECHANISM OF ACTION

Ibuprofen which possesses analgesic and antipyretic activities. Its mode of action, like that of other non- steroidal anti-inflammatory agents, is not completely understood, but may be related to prostaglandin synthetase inhibition. Paracetamol mechanism of action is related to depression of the prostaglandin synthesis by inhibition of the specific cell cyclooxygenase, and depression of the thermoregulatory center in the medulla oblongata Caffeine is structurally related to other methylxanthines, theophylline and theobromine. These include: (1) stimulation of the respiratory center, (2) increased minute ventilation, (3) decreased threshold to hypercapnia, (4) increased response to hypercapnia, (5) increased skeletal muscle tone, (6) decreased diaphragmatic fatigue, (7) increased metabolic rate, and (8) increased oxygen consumption.

PHARMACOKINETICS, ABSORPTION

After oral administration of 10 mg caffeine base/kg to preterm neonates, the peak plasma level (Cmax) for caffeine ranged from 6-10 mg/L and the mean time to reach peak concentration (Tmax) ranged from 30 minutes to 2 hours. The Tmax was not affected by formula feeding. The absolute bioavailability, however, was not fully examined in preterm neonates.

DISTRIBUTION

Caffeine is rapidly distributed into the brain. Caffeine levels in the cerebrospinal fluid of preterm neonates approximate their plasma levels. The mean volume of distribution of caffeine in infants (0.8-0.9 L/kg) is slightly higher than that in adults (0.6 LVkg). Plasma protein binding data are not available for neonates or infants. In adults, the mean plasma protein binding in vitro is reported to be approximately 36%.

METABOLISM 

Hepatic cytochrome P450 1A2. (CYP 1A2) is involved in caffeine biotransformation. Caffeine metabolism in preterm neonates is limited due to their immature hepatic enzyme systems. Interconversion between caffeine and theophylline has been reported in preterm neonates; caffeine levels are approximately 25% of theophylline levels after theophylline administration and approximately 3-8% of caffeine administered would be expected to convert to theophylline.

ELIMINATION 

In young infants, the elimination of caffeine is much slower than that in adults due to immature hepatic and/or renal function. Mean half-life (T1/2) and fraction excreted unchanged in urine (Ae) of caffeine in infants have been shown to be inversely related to gestational/post conceptual age. In neonates, the T1/2 is approximately 3-4 days, and the Ae is approximately 86% (within 6 days). By 9 months of age. the metabolism of caffeine approximates that seen in adults (T1/2 = 5 hours and Ae = 1%).

INDICATION

Paracetamol for the relief of mild to moderate pain and fever. Ibuprofen are indicated for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis. It is indicated for relief of mild to moderate pain. It is also indicated for the treatment of primary dysmenorrhea. Since there have been no controlled clinical trials to demonstrate whether or not there is any beneficial effect or harmful interaction with the use of ibuprofen in conjunction with aspirin, the combination cannot be recommended Controlled clinical trials to establish the safety and effectiveness of ibuprofen in children have not been conducted. Caffeine is indicated for the short-term treatment of apnea of prematurity in infants between 28- and 33-weeks gestational age.

DOSAGE AND ADMINISTRATION

2 to 3 Tablets total daily dose, if gastrointestinal complaints occur, administer Gebedol Xtra Tablets with meats.

SIDE-EFFECTS

Skin rashes and other allergic reactions may occur occasionally.

SPECIAL PRECAUTIONS

The dose should be reduced in renal functional impairment. Paracetamol should also be given with care to patients taking other drugs that affect the liver such as the barbiturates. Fluid retention and oedema have been reported in association with ibuprofen; therefore, the drug should be used with caution in patients with a history of cardiac decompensation or hypertension.

Storage: Store at a temperature not exceeding 30°C. Protect from light.

GB PHARMA LIMITED
65 Chatsworth Road, London NW2 4BG, United Kingdom
Tel.: +44 (0) 20 8830 1057, Fax: +44 (0) 20 8830 4807, E-mail: info@gbpharma.co.uk