Cafergot (ergotamine tartrate/caffeine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ergotamine is a naturally occurring ergot alkaloid.
Caffeine is a xanthine-derivative CNS stimulant that occurs naturally in tea and coffee, but is prepared synthetically for commercial drug use.
USES: This combination medication is used to treat or prevent certain types of headaches (vascular headaches including migraine and cluster headaches). Headache pain can sometimes be caused by widened blood vessels in the head. Ergotamine works by narrowing these widened blood vessels.
Caffeine increases the absorption of ergotamine and also narrows widened blood vessels.
Generic name: ergotamine tartrate/caffeine
Pronunciation: (er-GOT-a-meen/KAF-een)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Cafergot
Indications
The following indications are listed for Cafergot:
- Cluster Headache
- Cluster Headache Prevention
- Migraine
Also known as: Cluster Headache Prophylaxis.
Dosing
Some clinicians suggest that when used as a mild CNS stimulant to overcome fatigue, oral doses of 100-200 mg of anhydrous caffeine are required. The manufacturers state that adults and children 12 years of age or older may receive a dosage of 100-200 mg no more frequently than every 3-4 hours.
For the treatment of apnea of prematurity, commercially available caffeine citrate injection in a loading dose of 20 mg/kg (10 mg/kg when expressed in terms of anhydrous caffeine) is administered by slow IV infusion (i.e., over 30 minutes) using a syringe infusion pump. Beginning 24 hours after the loading dose, maintenance doses of caffeine citrate of 5 mg/kg (2.5 mg/kg when expressed as anhydrous caffeine) may be administered every 24 hours, either orally or via slow IV infusion (i.e., over 10 minutes) using a syringe infusion pump. The manufacturer states that the safety and efficacy of dosing periods exceeding 10-12 days have not been established. Other dosing regimens+ for the treatment of apnea of prematurity have used caffeine doses (in terms of anhydrous caffeine) of 5-10 mg/kg, given IV, IM, or orally as a loading dose, and followed by 2.5-5 mg/kg, given IV, IM, or orally once daily. Maintenance dosage has been adjusted according to the patient's response and tolerance and plasma caffeine concentrations.
When caffeine citrate is used for the treatment of apnea of prematurity in infants with hepatic or renal impairment, serum concentrations of caffeine should be monitored and dosage adjusted to avoid toxicity.
Analeptic use of caffeine is strongly discouraged by most clinicians. However, the manufacturers of caffeine and sodium benzoate injection recommend IM, or in emergency respiratory failure, IV injection of 500 mg of the drug (about 250 mg of anhydrous caffeine) or a maximum single dose of 1 g (about 500 mg of anhydrous caffeine) for the treatment of respiratory depression associated with overdosage of CNS depressants, including opiate analgesics and alcohol, and with electric shock.
Some clinicians recommend that when caffeine and sodium benzoate injection is used in children for CNS stimulation+, an IM, IV, or subcutaneous dose of 8 mg/kg (about 4 mg of anhydrous caffeine per kg) (not to exceed 500 mg) or 250 mg/m2 (about 125 mg of anhydrous caffeine per m2) be given up to every 4 hours if necessary.
Ergotamine tartrate is given sublingually. A combination of ergotamine tartrate and caffeine may be administered orally, or rectally as a suppository. If the suppositories become softened, they should be chilled in ice-cold water to solidify before removing the foil wrapper.
To be most effective, ergotamine tartrate should be administered as soon as possible after the first symptoms of a vascular headache (i.e., during the prodromal phase if there is one or at the beginning of an attack). The amount of drug required and the speed and degree of relief are thought to be directly related to the promptness with which the drug is started. After the initial dose is administered, the patient should lie down and relax in a quiet, darkened room. Ergotamine should not be administered within 24 hours of a selective serotonin agonist (e.g., sumatriptan). (See Drug Interactions: Selective Serotonin Agonists.)
Caffeine may be administered orally. Caffeine citrate is administered orally or by slow IV infusion using a syringe infusion pump. Caffeine and sodium benzoate injection may be administered by IM or slow IV injection; the drug has also been administered subcutaneously.
The preservative-free commercially available injection is for single use only, and any unused portion should be discarded. It is important that such oral solution be measured accurately (e.g., using a 1-mL or other appropriate syringe).
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No dosing information is available for this tab.
Drug interactions
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There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
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There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
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There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Retarded fetal growth and increases in intrauterine death and resorption were reported in animals receiving ergotamine. It has been postulated that such fetotoxicity is associated with drug-induced increases in uterine motility and vasoconstriction in the placental vasculature. Ergotamine is contraindicated in women who are or may become pregnant.
There are no adequate and well-controlled studies in pregnant women. In studies performed in adult animals, caffeine (as caffeine base) administered to pregnant mice as sustained-release pellets at 50 mg/kg (less than the maximum IV loading dose for neonates on a mg/m2 basis) during the period of organogenesis caused a low incidence of cleft palate and exencephaly in fetuses. Based on data from a large retrospective epidemiologic study and from a large retrospective case-control study in humans, it appears that use of caffeine during pregnancy has little, if any, effect on the outcome of pregnancy. Although caffeine use during pregnancy does not appear to be associated with substantial risk, most clinicians recommend that pregnant women avoid or limit their consumption of foods, beverages, and drugs containing caffeine, since caffeine crosses the placenta.
Ergotamine is distributed into milk and may cause vomiting, diarrhea, weak pulse, unstable blood pressure, and seizures in nursing infants. Although ergot alkaloids have been reported to inhibit maternal pituitary prolactin secretion, decreased lactation has not been reported to date with ergotamine. Because of the potential for serious adverse reactions to ergotamine in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Caffeine is distributed into the milk of nursing women. Milk-to-plasma ratios of 0.5-0.76 have been reported. The amount of caffeine ingested from usual quantities of caffeinated beverages is considered compatible with breast-feeding; however, caffeine may accumulate in nursing infants following moderate to heavy maternal consumption of caffeine, resulting in irritability and poor sleeping patterns.
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ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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