Product Information
Registration Status: ActiveCAFFOX TABLET is approved to be sold in Singapore with effective from 2001-12-26. It is marketed by JOYSON PTE LTD, with the registration number of SIN11746P.
This product contains Caffeine 100mg, and Ergotamine 1mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by T O PHARMA CO LTD in THAILAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes smooth muscle, stimulates cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide phosphodiesterases, antagonism of adenosine receptors, and modulation of intracellular calcium handling.
Indication
For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
Mechanism of Action
Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3′,5′-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as antagonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.
Pharmacokinetics
- Absorption
- Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.
- Distribution
- * 0.8 to 0.9 L/kg [infants] * 0.6 L/kg [adults]
- Metabolism
- Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).
- Elimination
Toxicity
LD50=127 mg/kg (orally in mice)
Active Ingredient/Synonyms
1-methyltheobromine | 1,3,7-trimethyl-2,6-dioxopurine | 1,3,7-trimethylpurine-2,6-dione | 1,3,7-trimethylxanthine | 3,7-Dihydro-1,3,7-trimethyl-1H-purin-2,6-dion | 7-methyltheophylline | Anhydrous caffeine | Cafeína | Caféine | Caffeinum | Coffein | Coffeinum | Guaranine | Koffein | Mateína | Methyltheobromine | teína | Thein | Theine | Caffeine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders.
Indication
For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".
Mechanism of Action
Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
Pharmacokinetics
- Absorption
- The bioavailability of sublingually administered ergotamine has not been determined.
- Distribution
- Metabolism
- Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.
- Elimination
Toxicity
Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.
Active Ingredient/Synonyms
(5'α)-12'-hydroxy-2'-methyl-5'-(phenylmethyl)ergotoman-3',6',18-trione | 12'-Hydroxy-2'-methyl-5'alpha-(phenylmethyl)ergotaman-3',6',18-trione | 12'-hydroxy-2'-methyl-5'α-(phenylmethyl)ergotaman-3',6',18-trione | Ergotamin | Ergotamina | Ergotamine | Ergotaminum | Ergotamine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.