INN monograph
Ergotamine / Caffeine
Central Nervous System Stimulant [EPC], Methylxanthine [EPC] · POM
Verified · Updated 01 Aug 2026 · Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Component monographs (multi-source pipeline); Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Kenya market
Wholesale / list prices where loaded
Risk first
Contraindications
- CONTRAINDICATIONS Coadministration of ergotamine with potent CYP 3A4 inhibitors (ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, and troleandomycin) has been associated with acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities (see PRECAUTIONS : Drug Interactions), with some cases resulting in amputation.
- There have been rare reports of cerebral ischemia in patients on protease inhibitor therapy when ergotamine tartrate and caffeine was coadministered, at least one resulting in death.
- Because of the increased risk for ergotism and other serious vasospastic adverse events, ergotamine use is contraindicated with these drugs and other potent inhibitors of CYP 3A4 (e.g., ketoconazole, itraconazole) (see WARNINGS : CYP 3A4 Inhibitors).
- Ergotamine tartrate and caffeine may cause fetal harm when administered to pregnant women.
- Ergotamine tartrate and caffeine is contraindicated in women who are or may become pregnant.
- If this drug is used during pregnancy or if the patient becomes pregnant while taking this product, the patient should be apprised of the potential hazard to the fetus.
- Peripheral vascular disease, coronary heart disease, hypertension, impaired hepatic or renal function and sepsis.
- Hypersensitivity to any of the components.
Precautions
- WARNINGS CYP 3A4 Inhibitors (e.g.
- Macrolide Antibiotics and Protease Inhibitors) Coadministration of ergotamine with potent CYP 3A4 inhibitors such as protease inhibitors or macrolide antibiotics has been associated with serious adverse events
- for this reason, these drugs should not be given concomitantly with ergotamine (See CONTRAINDICATIONS ).
- While these reactions have not been reported with less potent CYP 3A4 inhibitors, there is a potential risk for serious toxicity including vasospasm when these drugs are used with ergotamine.
- Examples of less potent CYP 3A4 inhibitors include: saquinavir, nefazodone, fluconazole, fluoxetine, grapefruit juice, fluvoxamine, zileuton, metronidazole, and clotrimazole.
- These lists are not exhaustive, and the prescriber should consider the effects on CYP 3A4 of other agents being considered for concomitant use with ergotamine.
- Fibrotic Complications There have been a few reports of patients on ergotamine tartrate and caffeine therapy developing retroperitoneal and/or pleuropulmonary fibrosis.
- There have also been rare reports of fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with long-term continuous use of ergotamine tartrate and caffeine.
- Ergotamine tartrate suppositories should not be used for chronic daily administration (see DOSAGE AND ADMINISTRATION ).
Point of care
Dosing
Adult
DOSAGE AND ADMINISTRATION Procedure For best results, dosage should start at the first sign of an attack. Rectally Two suppositories is the maximum dose for an individual attack. Total weekly dosage should not exceed 5 suppositories. Ergotamine Tartrate and Caffeine Suppositories 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. Maximum Adult Dosage: One suppository at start of attack; second suppository after 1 hour, if needed for full relief. Early administration gives maximum effectiveness.
Paediatric
See label paediatric section if present; otherwise use paediatric formulary — do not extrapolate adult doses.
Renal
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Hepatic
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Safety
Drug interactions
- Fixed-dose/multi-ingredient product.
- Clinical details partially inherited from component monographs: Ergotamine, Caffeine Citrate.
- Confirm combination SmPC for exact dosing.
Safety
Adverse effects
- ADVERSE REACTIONS Cardiovascular: Vasoconstrictive complications of a serious nature may occur at times.
- These include ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes and muscle pains.
- Although these effects occur most commonly with long-term therapy at relatively high doses, they have also been reported with short-term or normal doses.
- Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension.
- Gastrointestinal: Nausea and vomiting
- rectal or anal ulcer (from overuse of suppositories).
- Neurological: Paresthesias, numbness, weakness, and vertigo.
- Allergic: Localized edema and itching.
- Fibrotic Complications: (See WARNINGS ).
- To report SUSPECTED ADVERSE REACTIONS, contact Cosette Pharmaceuticals, Inc. at 1-800-922-1038 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Use
Indications
- INDICATIONS AND USAGE Ergotamine Tartrate and Caffeine Indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants or so-called “histaminic cephalalgia”.
- Clinical selection for Ergotamine / Caffeine should follow culture results where relevant, Kenya STG/EML recommendations, and the current product SmPC.
- Class context: Central Nervous System Stimulant [EPC], Methylxanthine [EPC].
- Confirm site-specific dose, duration and monitoring before prescribing.
Pharmacology
Mode of action
Ergotamine interacts with sever- al neurotransmitter receptors, including alpha- adrenergic, serotonergic and dopaminergic receptors.
Full mechanism text
Ergotamine interacts with sever- al neurotransmitter receptors, including alpha- adrenergic, serotonergic and dopaminergic receptors. It directly stimulates vascular smooth mus- cle causing constriction of both arteries and veins and depresses vasomotor centers in the brain. More specifically, it is thought that agonist activity at the 5-HT1D receptor subtype provides relief of acute headache, whereas antagonist activity at the 5-HT receptor subtype provides headache 2 prophylaxis. Caffeine is thought to act by increasing both the rate and extent of absorption of ergotamine.
ADME
Pharmacokinetics & PD
| Onset | Product-specific |
|---|---|
| Duration | Product-specific |
| Route | See product SmPC |
| Metabolism | of ergotamine (See CONTRAINDICATIONS ). Ergotamine has also been shown to be an inhibitor of cytochrome P450 3A catalyzed reactions. No pharmacokinetic interactions involving other cytochrome P450 isoenzymes are known. |
Full PK/PD text
CLINICAL PHARMACOLOGY Ergotamine is an alpha adrenergic blocking agent with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The compound also has the properties of serotonin antagonism. In comparison to hydrogenated ergotamine, the adrenergic blocking actions are less pronounced and vasoconstrictive actions are greater. Caffeine, also a cranial vasoconstrictor, is added to further enhance the vasoconstrictive effect without the necessity of increasing ergotamine dosage. Many migraine patients experience excessive nausea and vomiting during attacks, making it impossible for them to retain any oral medication. In such cases, therefore, the only practical means of medication is through the rectal route where medication may reach the cranial vessels directly, evading the splanchnic vasculature and the liver. Pharmacokinetics: Interactions Pharmacokinetic interactions (increased blood levels of ergotamine) have been reported in patients treated orally with ergotamine and macrolide antibiotics (e.g., troleandomycin, clarithromycin, erythromycin), and in patients treated orally with ergotamine and protease inhibitors (e.g. ritonavir) presumably due to inhibition of cytochrome P450 3A metabolism of ergotamine (See CONTRAINDICATIONS ). Ergotamine has also been shown to be an inhibitor of cytochrome P450 3A catalyzed reactions. No pharmacokinetic interactions involving other cytochrome P450 isoenzymes are known.
Kenya
Brands & prices
| Brand | Company | Pack | KES |
|---|---|---|---|
| Cafergot | Novartis Pharma | Standard Commercial Pack | — |
| Ergocaf | Prism Life Sciences | Standard Commercial Pack | — |
Special populations
Pregnancy & lactation
Pregnancy
[Ergotamine] Use only if potential benefit justifies potential risk; prefer agents with better reproductive data when alternatives exist. [Caffeine] Use only if potential benefit justifies potential risk; prefer agents with better reproductive data when alternatives exist.
Lactation
[Ergotamine] Assess infant risk vs benefit of maternal therapy; prefer agents with lactation data. [Caffeine] Assess infant risk vs benefit of maternal therapy; prefer agents with lactation data.
Diet
Food & alcohol
- Food
- Food
Trust
Sources & disclaimer
Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Component monographs (multi-source pipeline); Professional class pharmacology (Therapeutic agent (verify pharmacological class))
Last reviewed: 01 Aug 2026
Decision support only — not a substitute for clinical judgment, product SmPC, or Kenya STG/EML.