Methylergonovine maleate (Methergine®), an ergot derivative with vasoconstrictive properties, has been cited as an effective treatment for vascular headaches. Few studies are available to support its use in headache management. An uncontrolled pilot study of 20 episodic cluster headache patients confirmed its effectiveness and tolerability as an adjunct cluster headache prophylactic. Decreased headache frequency was reported by 19 of 20 patients (95%), and 15 of 20 patients (75%) reported decreased intensity of headaches within 1 week of initiating therapy. A review of methylergonovine's pharmacokinetic, molecular, and tolerability profile clarifies its mechanisms and clinical role in headache management.