ergotamine

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: ergot alkaloids

Indications ⬆ ⬇

REMS

Treatment of vascular headaches, including:
- Migraine with or without aura,
- Cluster headaches.

Action ⬆ ⬇

Vasoconstriction of dilated blood vessels by stimulating alpha-adrenergic and serotonergic receptors.
Larger doses may produce alpha-adrenergic blockade and vasodilation.

Therapeutic effects:

Resolution of vascular headache.

Pharmacokinetics ⬆ ⬇

Absorption: Unpredictably absorbed (60%) from the GI tract. Sublingual absorption is very poor.

Distribution: Crosses the blood-brain barrier.

Protein Binding: 93–98%.

Metabolism/Excretion: Highly metabolized (90%) by the liver. Some metabolites are active.

Half-Life: 1.5–2.5 hr.

Time/Action Profile ⬆ ⬇

(relief of headache)

ROUTE	ONSET	PEAK	DURATION
SL	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Peripheral vascular disease;
Ischemic heart disease;
Uncontrolled hypertension;
Severe renal impairment;
Severe hepatic impairment;
Malnutrition;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Illnesses associated with peripheral vascular pathology, such as diabetes mellitus;
Concurrent administration of other vasoconstricting agents;
Pedi: Children 6 yr (safety not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, angina pectoris, arterial spasm, intermittent claudication, MI

F and E: polydipsia

GI: abdominal pain, nausea, vomiting, diarrhea

MS: extremity stiffness, muscle pain, stiff neck, stiff shoulders

Neuro: dizziness, fatigue, leg weakness, numbness or tingling in fingers or toes

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with beta blockers, oral contraceptives, macrolide anti-infectives (erythromycin ), ornicotine (heavy smoking) may ↑ risk of peripheral vasoconstriction.
Antagonizes the antianginal effects of nitrates.
Concurrent use with vasoconstrictors may have additive effects; avoid concurrent use.
Concurrent use with almotriptan, naratriptan, rizatriptan, sumatriptan, or zolmitriptan may result in prolonged vasoconstriction; allow 24 hr between use.

Route/Dosage ⬆ ⬇

(Adults ): 1–2 mg initially; then 1–2 mg every 30 min until attack subsides or a total of 6 mg has been given. Should not be used more than twice weekly, with at least 5 days between courses.

Availability ⬆ ⬇

Sublingual tablets: 2 mg
In combination with: caffeine (Migergot). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess frequency, location, duration, and characteristics (pain, nausea, vomiting, visual disturbances) of chronic headaches. During acute attack, assess type, location, and intensity of pain before and 60 min after administration.
Monitor BP and peripheral pulses periodically during therapy. Report any increases in BP.
Assess for signs of ergotism (cold, numb fingers and toes; nausea; vomiting; headache; muscle pain; weakness).
Assess for nausea and vomiting. Ergotamine stimulates the chemoreceptor trigger zone.

Toxicity and Overdose:

Toxicity is manifested by severe ergotism (chest pain, abdominal pain, persistent paresthesia in the extremities) and gangrene. Vasodilators, dextran, or heparin may be ordered to improve circulation.

Implementation ⬆ ⬇

Administer as soon as patient reports prodromal symptoms or headache.
Allow tablet to dissolve under tongue. Do not allow patient to eat, drink, or smoke while tablet is dissolving. DNC: Do not crush sublingual tablets.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take ergotamine at the first sign of an impending headache and not to exceed the maximum dose prescribed.
- Encourage patient to rest in a quiet, dark room after taking ergotamine.
- Review symptoms of toxicity. Instruct patient to report these promptly.
- Caution patient not to smoke and to avoid exposure to cold; these vasoconstrictors may further impair peripheral circulation.
- May cause dizziness. Caution patient to avoid driving and other activities requiring alertness until response to the drug is known.
- Advise patient to avoid alcohol, which may precipitate vascular headaches.
- May cause fetal harm. Instruct females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding. Ergotamine should not be used during pregnancy.

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Pronunciation ⬇

Classifications ⬆ ⬇