Ergotamine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Inhalation/Respiratory
Migraine
Adult: As ergotamine tartrate: Inhale single dose (360 mcg) at the onset of attack and repeat at 5-min intervals, if necessary. Max: 6 inhalations/24 hr, 15 inhalations/wk.

Sublingual
Migraine
Adult: As ergotamine tartrate: 2 mg on the onset of attack, then 2 mg every 30 min if necessary. Max: 6 mg/24 hr, 10 mg/wk.
Renal Impairment
Contraindicated.
Hepatic Impairment
Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Patient w/ severe or uncontrolled HTN, severe or persistent sepsis, shock, peripheral vascular disease, temporal arteritis, ischaemic heart disease, hyperthyroidism; basilar or hemiplegic migraine. Renal or hepatic impairment. Pregnancy. Concomitant admin w/ potent CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors, macrolide antibiotics).
Thận trọng
Patient w/ anaemia. Lactation.
Phản ứng phụ
Nausea and vomiting, abdominal pain, tingling of fingers and toes, weakness, muscle pains in the extremities and numbness, localised oedema, itching, bradycardia, transient tachycardia.
PO/Rectal/SL: X
Thông tin tư vấn bệnh nhân
May cause dizziness and feelings of anxiety, if affected, do not drive or operate machinery.
MonitoringParameters
Evaluate CV status prior to initiation and periodically thereafter.
Quá liều
Symptoms: Numbness, vomiting, tingling, pain, cyanosis of the extremities associated w/ diminished or absent peripheral pulses; HTN or hypotension; stupor, drowsiness, convulsions, shock, coma; reversible bilateral papillitis w/ ring scotomata. Management: Maintain adequate pulmonary ventilation, correction of hypotension and control or BP and convulsions. Keep the extremities warm to treat peripheral vasospasm. Vasodilators may be beneficial.
Tương tác
Increased risk of peripheral vasoconstriction w/ β-blockers. Increased vasoconstrictor effect w/ sympathomimetics (e.g. epinephrine).
Potentially Fatal: Increased risk of ergotism w/ potent CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors, macrolide antibiotics).
Food Interaction
May enhance toxicity w/ grapefruit juice.
Tác dụng
Description: Ergotamine has marked vasoconstrictor effects and partial agonistic action at serotonin (5-HT) receptors. It causes constriction of peripheral and cranial blood vessels and produces central vasomotor center depression. It also has a powerful oxytocic action on the uterus.
Pharmacokinetics:
Absorption: Poorly absorbed from the GI tract. Bioavailability: Approx ≤5%. Time to peak plasma concentration: 2 hr (oral).
Distribution: Crosses the blood-brain barrier; enters breast milk. Volume of distribution: 1.85 L/kg. Plasma protein binding: Approx 93-98%.
Metabolism: Undergoes extensive hepatic metabolism, including high first-pass effect.
Excretion: Via faeces (90%, mainly as metabolites); urine (approx 4%). Biphasic elimination half-life: Approx 2 hr (initial phase); 21 hr (terminal phase).
Đặc tính

Chemical Structure Image
Ergotamine

Source: National Center for Biotechnology Information. PubChem Database. Ergotamine, CID=8223, https://pubchem.ncbi.nlm.nih.gov/compound/Ergotamine (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C. Protect form heat and light.
Phân loại MIMS
Phân loại ATC
N02CA02 - ergotamine ; Belongs to the class of ergot alkaloids preparations. Used to relieve migraine.
References
Anon. Ergotamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/01/2016.

Buckingham R (ed). Ergotamine Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/01/2016.

Ergomar Tablet, Orally Disintegrating (Rosedale Therapeutics). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/01/2016.

Joint Formulary Committee. Ergotamine Tartrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/01/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Ergotamine Tartrate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 20/01/2016.

Medihaler Ergotamine Aerosol, Metered (3M Riker). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/01/2016.

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