CAFERGOT TABLET

Caffeine
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.

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 |

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.

Pharmacodynamics

Caffeine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.

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:

In young infants, the elimination of caffeine is much slower than that in adults due to immature hepatic and/or renal function.

Half-life

3 to 7 hours in adults, 65 to 130 hours in neonates

Clearance

Not Available

Toxicity

LD50=127 mg/kg (orally in mice)

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.

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 |

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.

Pharmacodynamics

Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.

Pharmacokinetics

Absorption:

The bioavailability of sublingually administered ergotamine has not been determined.

Distribution:

Not Available

Metabolism:

Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.

Elimination:

Not Available

Half-life

2 hours

Clearance

Not Available

Toxicity

Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

CAFERGOT TABLET was registered with Health Science Authority of Singapore by A. MENARINI SINGAPORE PTE LTD. It is marketed with the registration number of SIN01077P with effective from 1988-12-05.

This product contains 100mg of Caffeine, and 1mg of Ergotamine in the form of TABLET.

The medicine was manufactured by NOVARTIS PHARMACEUTICALS UK LTD CENEXI in FRANCE, and in UNITED KINGDOM

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N02CA52

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