The ergot derivatives cause constriction of cranial blood vessels and decrease the pulsation of cranial arteries. As a result, they reduce the hyperperfusion of the basilar artery vascular bed. Available ergot derivatives include dihydroergotamine (Migranal, D.H.E. 45) and ergotamine (Ergomar).
The ergot derivatives block alpha-adrenergic and serotonin receptor sites in the brain to cause a constriction of cranial vessels, a decrease in cranial artery pulsation, and a decrease in the hyperperfusion of the basilar artery bed. These drugs are indicated for the prevention or abortion of migraine or vascular headaches. Ergotamine, the prototype drug in this class, was the mainstay of migraine headache treatment before the development of triptans.
The ergot derivatives are rapidly absorbed from many routes, with an onset of action ranging from 15 to 30 minutes. They are metabolized in the liver and primarily excreted in the bile.
麦角衍化物多途径用药吸收迅速,15 – 30 分钟起效。代谢于肝,主要经胆汁排出。
Dihydroergotamine is available as a nasal spray or for IM or IV administration. This agent is the drug of choice if the oral route of administration is not possible.
双氢麦角胺剂型有鼻喷雾剂、IM、IV等。该为口腔途径不可能时的首选药物。
Ergotamine is administered sublingually for rapid absorption. Cafergot, the very popular oral form, combines ergotamine with caffeine to increase its absorption from the GI tract.
麦角胺为舌下药,吸收快。咖啡角是极受欢欣的口服药,将麦胺与咖啡因结合,从而增强其胃肠道吸收。
Ergot derivatives are contraindicated in the following circumstances: Presence of allergy to ergot preparations to avoid hypersensitivity reactions; CAD, hypertension, or peripheral vascular disease, which could be exacerbated by the CV effects of these drugs; impaired liver function, which could alter the metabolism and excretion of these drugs; and pregnancy or lactation because of the potential for adverse effects on the fetus and neonate. Ergotism (vomiting, diarrhea, and seizures) has been reported in affected infants.
Caution should be used in two instances: With pruritus, which could become worse with drug-induced vascular constriction, and with malnutrition because ergot derivatives stimulate the CTZ and can cause severe GI reactions, possibly worsening malnutrition.
The adverse effects of ergot derivatives can be related to the drug-induced vascular constriction. CNS effects include numbness, tingling of extremities, and muscle pain; CV effects such as pulselessness, weakness, chest pain, arrhythmias, localized edema and itching, and MI may also occur. In addition, the direct stimulation of the CTZ can cause GI upset, nausea, vomiting, and diarrhea. Ergotism, a syndrome associated with the use of these drugs, causes nausea, vomiting, severe thirst, hypoperfusion, chest pain, blood pressure changes, confusion, drug dependency (with prolonged use), and a drug withdrawal syndrome.
ergot – n. 麦角
derivative – n. 衍生物,衍化物
pulsation – n. 搏动,跳动
basilar artery – 基底动脉
vascular bed – 血管床
dihydroergotamine – n. 双氢麦角胺
Migranal – n. 甲磺双氢麦角胺
ergotamine – n. 麦角胺
Ergomar – n. 洒石酸麦角胺制剂的商品名
prototype drug – 原型药
mainstay – n. 骨干,唯一依靠
triptan – n. 曲坦
Cafergot – n. 咖啡角
ergotism – n. 麦角中毒
pruritus – n. 瘙痒(症)
constriction – n. 收缩,压缩
CTZ --化学感受器触发区
1. The male client presents to the outpatient clinic complaining of headaches that occur suddenly with throbbing in the right orbital area and on the right side of the forehead that last for an hour or longer and that have been occurring regularly for the past 2 weeks. Which medications would the nurse anticipate being prescribed?
A. Propranolol (Inderal), a beta blocker, and almotriptan (Axert), a triptan.
B. Prednisone, a glucocorticoid, and lithium (Lithobid), a psychotherapeutic agent.
C. Amitriptyline (Elavil), a tricyclic antidepressant, and the estrogen patch Climara.
D. Ibuprofen (Motrin), an NSAID, and metoclopramide (Reglan), an antiemetic. 2. The nurse is administering 1600 medications. Which medication should the nurse administer first?
A. Humalog insulin for a client with a blood glucose level of 200 mg/dL.
B. Meperidine (Demerol), a narcotic analgesic, for a client with a headache rated an 8.
C. Divalproex (Depakote ER) for a client diagnosed with migraine headaches.
D. Metoclopramide (Reglan), an antiemetic, for a client with gastric stasis.
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答案 Answers
1. B. Prednisone, a glucocorticoid, and lithium (Lithobid), a psychotherapeutic agent. Rationale: The client’s symptoms support the diagnosis of cluster headaches, which are related to migraines but differ in several ways. Cluster headaches are less common than migraines and occur in males 5:1. Cluster headaches do not cause nausea and vomiting; they can be more debilitating than migraines; they do not have an aura; and they are not linked to genetics. The drugs of choice to treat cluster headaches are prednisone and lithium. High-dose prednisone can reduce symptoms within 48 hours, and lithium can prevent the headaches altogether. Lithium takes 1–2 weeks before relief is noted. 2. B. Meperidine (Demerol), a narcotic analgesic, for a client with a headache rated an 8. Rationale: Demerol is used to treat severe migraine headaches when other measures have not been effective. This client needs the medication as soon as possible (pain is rated as 8), and this should be the first medication administered.