Ergotamine and Caffeine

Each tablet for oral administration contains 1 mg ergotamine tartrate, USP, and 100 mg caffeine, USP.

ERGOTAMINE TARTRATE:

(C 33H 35N 5O 5) 2• C 4H 6O 6

M.W. 1313.41

Ergotaman-3’,6’,18-trione, 12’-hydroxy-2’-methyl-5’-(phenyl-methyl)-, (5’α), [R-(R*, R*)]-2,3-dihydroxy-butanedioate (2:1) (salt)

CAFFEINE:

C 8H 10N 4O 2 (anhydrous)

M.W. 194.19

1 H-Purine-2,6-dione, 3,7-dihydro-1,3,7-trimethyl-

Inactive ingredients include colloidal silicon dioxide, crospovidone, magnesium stearate, and microcrystalline cellulose. Film coating includes the following ingredients: macrogol/PEG 3350, polyvinyl alcohol, purified water, talc, titanium dioxide, FD&C blue #2 aluminum lake, FD&C red #40 aluminum lake, and FD&C yellow #5 tartrazine aluminum lake.

Ergotamine tartrate and caffeine tablets are indicated as therapy to abort or prevent vascular headache; e.g., migraine, migraine variants or so-called “histaminic cephalalgia.”

Procedure: For the best results, dosage should start at the first sign of an attack. Adults: Take 2 tablets at the start of attack; 1 additional tablet every ½ hour, if needed for full relief (maximum 6 tablets per attack, 10 per week).

Maximum Adult Dosage:

Total daily dose for any one attack should not exceed 6 tablets. Total weekly dosage should not exceed 10 tablets. Ergotamine tartrate and caffeine tablets should not be used for chronic daily administration. In carefully selected patients, with due consideration of maximum dosage recommendations, administration of the drug at bedtime may be an appropriate short-term preventive measure.

(er GOT a meen & KAF een)

• Caffeine and Ergotamine
• Ergotamine Tartrate and Caffeine
• Ergotamine Tartrate/Caffeine

• Antimigraine Agent
• Central Nervous System Stimulant
• Ergot Derivative

Has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha-adrenergic receptors depending upon their site; is a highly active uterine stimulant; it causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers

Absorption

Ergotamine: Oral, rectal: Erratic (Perrin, 1985)

Metabolism

Ergotamine: Extensively hepatic, including high first-pass metabolism (Perrin, 1985)

Excretion

Ergotamine: Feces (90%, primarily as metabolites) (Perrin, 1985)

Time to Peak

Serum: Ergotamine: 2 hours (Perrin, 1985)

Half-Life Elimination

2 to 2.5 hours (Perrin, 1985)

Vascular headache:

Oral: Note: Each tablet contains ergotamine 1 mg and caffeine 100 mg: Ergotamine 2 mg and caffeine 200 mg (2 tablets) at onset of attack; then ergotamine 1 mg and caffeine 100 mg (1 tablet) every 30 minutes as needed

Maximum dose: Ergotamine 6 mg and caffeine 600 mg (6 tablets) per attack; do not exceed ergotamine 10 mg and caffeine 1,000 mg (10 tablets) per week

Rectal: Ergotamine 2 mg and caffeine 100 mg (1 suppository) at first sign of an attack; follow with second dose after 1 hour, if needed

Maximum dose: Ergotamine 4 mg and caffeine 200 mg (2 suppositories) per attack; do not exceed ergotamine 10 mg and caffeine 500 mg (5 suppositories) per week

Frequency not defined.

Cardiovascular: Bradycardia, cold extremities, ECG changes, edema, hypertension, ischemia, tachycardia, valvular sclerosis, vasospasm

Central nervous system: Numbness, paresthesia, precordial pain, vertigo

Dermatologic: Gangrene of skin or other tissue, pruritus

Gastrointestinal: Anal fissure (with overuse of suppository), nausea, rectal ulcer (with overuse of suppository), vomiting

Genitourinary: Retroperitoneal fibrosis

Neuromuscular & skeletal: Myalgia, weakness

Respiratory: Cyanosis, pleuropulmonary fibrosis

Animal reproduction studies have not been conducted with this combination. Ergotamine and caffeine both cross the placenta and may cause prolonged constriction of the uterine vessels and/or increased myometrial tone leading to reduced placental blood flow. Use is contraindicated in pregnant women.