Cafergot: profile and news

LSD faces an acid test as a pain killer Feb 17, 2006
Medications like Cafergot have proven moderately successful in aborting a single cluster headache attack, and other drugs like verapamil and lithium can ... - Australian,

Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006
R) (astemizole), Propulsid(R) (cisapride), Versed(R)(midazolam), Halcion(R) (triazolam), ergot medicines (for example,Wigraine(R) and Cafergot(R)), or Vfend(R ... - Finanzen.net,

Companies Anticipate Filing New Drug Application in Second Quarter ... Jan 9, 2006
...astemizole), Propulsid® (cisapride), Versed® (midazolam), Halcion® (triazolam), ergot medicines (for example, Wigraine® and Cafergot®), or Vfend ... - Nieuwsbank (persbericht),

Abbott Receives FDA Approval for New Kaletra(R) (Lopinavir ... 31 Oct 2005
Kaletra should not be taken with dihydro.ergotamine, ergonovine, ergotamine, and methylergonovine such as Cafergot(R), Migranal(R), DHE 45(R), Ergotrate Maleate ... - PR Newswire (press release),

Abbott Receives FDA Approval for a Once-Daily Kaletra(R)-Based ... May 2, 2005
Kaletra should not be taken with dihydroergotamine, ergonovine, ergotamine, and methylergonovine such as Cafergot(R), Migranal(R), DHE 45(R), Ergotrate Maleate ... - PR Newswire

Abbott Receives FDA Approval for a Once-Daily Kaletra(R)-Based ... May 2, 2005
Kaletra should not be taken with dihydroergotamine, ergonovine, ergotamine, and methylergonovine such as Cafergot®, Migranal®, DHE 45®, Ergotrate Maleate ... - Yahoo News

Bristol-Myers Squibb Extends Assistance to State AIDS Drug ... Mar 22, 2005
...astemizole), Propulsid® (cisapride), Versed® (midazolam), Halcion® (triazolam), ergot medicines (for example, Wigraine® and Cafergot®), or Vfend ... - Yahoo News (press release)

Bristol-Myers Squibb Extends Assistance to State AIDS Drug ... Mar 22, 2005
R) (astemizole), Propulsid(R) (cisapride), Versed(R) (midazolam), Halcion(R) (triazolam), ergot medicines (for example, Wigraine(R) and Cafergot(R)), or Vfend(R ... - PR Newswire (press release)

Other information

Indication
For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.

Pharmacology
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.

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 agonists 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.

Drug Category
Central Nervous System Stimulants; Anorexigenic Agents; Phosphodiesterase Inhibitors; ATC:N06BC01

Brand Names/Synonyms
Acetaminophen; Alert-Pep; Anoquan; Butal Compound; Butalbital; Butalbital Compound; CFF; Cafamil; Cafcit; Cafecon; Cafeina; Cafergot; Caffedrine; Caffedrine Caplets; Caffein; Caffeine; Caffeine Pure; Caffeine, Anhydrous; Caffeine, Monohydrate; Caffeine, Synthetic; Caffine; Cafipel; Coffein; Coffeine; Compound 65; Darvon Compound; Darvon Compound-65; Dasin; Dexitac; Dexitac Stay Alert Stimulant; Dhc Plus; Diurex; Durvitan; Eldiatric C; Enerjets; Ercatab; Esgic; Esgic-Plus; Femcet; Fioricet; Fiorinal; Guaranine; Hycomine; Invagesic; Invagesic Forte; Keep Alert; Kofein; Koffein; Lanorinal; Mateina; Maximum Strength Snapback Stimulant Powders; Medigesic Plus; Methyltheobromide; Methyltheobromine; Migergot; Miudol; Monomethyl Derivative of Theophylline; NCI-C02733; NSC 5036; Natural Caffeinum; Nix Nap; No-Doz; Nodaca; Nodoz Maximum Strength Caplets; Norgesic; Norgesic Forte; Organex; Orphengesic; Orphengesic Forte; Pep-Back; Phensal; Propoxyphene Compound 65; Propoxyphene Compound-65; Quick Pep; Refresh'n; Sk 65 Compound; Stim; Synalgos-Dc; Thein; Theine; Theobromine Me; Theophylline Me; Triad; Ultra Pep-Back; Vivarin; Wake-Up; Wigraine

Dosage Forms
CAPSULE; DROPS; LIQUID; PILL; TABLET

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.

Interactions
Interactions for Caffeine:

Cytochrome P450 1A₂ (CYP1A₂) is known to be the major enzyme involved in the metabolism of caffeine. Therefore, caffeine has the potential to interact with drugs that are substrates for CYP1A₂, inhibit CYP1A₂, or induce CYP1A₂.

Few data exist on drug interactions with caffeine in preterm neonates. Based on adult data, lower doses of caffeine may be needed following coadministration of drugs which are reported to decrease caffeine elimination (e.g., cimetidine and ketoconazole) and higher caffeine doses may be needed following coadministration of drugs that increase caffeine elimination (e.g., phenobarbital and phenytoin).

Caffeine administered concurrently with ketoprofen reduced the urine volume in 4 healthy volunteers. The clinical significance of this interaction in preterm neonates is not known.

Interconversion between caffeine and theophylline has been reported in preterm neonates. The concurrent use of these drugs is not recommended.

Chemical IUPAC Name
1,3,7-trimethyl-3,7-dihydropurine-2,6-dione

Chemical Formula
C8H10N4O2

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

Drug Type
Approved Drug

# Accession No
APRD00673

CAS Registry Number
58-08-2