dihydroergotamine


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dihydroergotamine

 [di-hi″dro-er-got´ah-mēn]
hydrogenated ergotamine, an alpha-adrenergic blocking agent and vasoconstrictor used as ergotamine mesylate in treatment of migraine; administered intramuscularly, subcutaneously, intravenously, or intranasally.

dihydroergotamine

(dye-hye-droe-er-got-a-meen) ,

D.H.E. 45

(trade name),

Dihydroergotamine-Sandoz

(trade name),

Migranal

(trade name)

Classification

Therapeutic: vascular headache suppressants
Pharmacologic: ergot alkaloids
Pregnancy Category: X

Indications

Vascular headaches including:
  • Migraine,
  • Cluster headaches.

Action

Vasoconstriction of dilated blood vessels by stimulating alpha-adrenergic and serotonergic (5-HT) receptors.
Larger doses may produce alpha-adrenergic blockade and vasodilation.

Therapeutic effects

Constriction of dilated carotid artery bed with resolution of vascular headache.

Pharmacokinetics

Absorption: Rapidly absorbed following IM and subcut administration and 32% absorbed from nasal mucosa.
Distribution: Unknown.
Protein Binding: 90%.
Metabolism and Excretion: Highly metabolized (90%) by the liver. Some metabolites are active.
Half-life: 10 hours.

Time/action profile (relief of headache)

ROUTEONSETPEAKDURATION
Nasal within 30 minunknown unknown
IM, subcut15–30 min15 min–2 hr8 hr
IV <5 min15 min–2 hr8 hr

Contraindications/Precautions

Contraindicated in: Peripheral vascular disease; Ischemic heart disease; Uncontrolled hypertension; Severe renal or liver disease ; Malnutrition; Known alcohol intolerance (injection only); Obstetric: Pregnancy; Lactation: Lactation; Concurrent use of CYP 3A4 enzyme inhibitors (macrolide anti-infectives and protease inhibitors).
Use Cautiously in: Illnesses associated with peripheral vascular pathology such as diabetes mellitus; Concurrent administration of other vasoconstricting agents; Pediatric: Children <6 yr (safety not established).

Adverse Reactions/Side Effects

Central nervous system

  • dizziness

Ear, Eye, Nose, Throat

  • rhinitis (most frequent)

Cardiovascular

  • myocardial infarction (life-threatening)
  • hypertension (most frequent)
  • angina pectoris
  • arterial spasm
  • intermittent claudication

Gastrointestinal

  • abdominal pain (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • altered taste
  • diarrhea
  • polydipsia

Musculoskeletal

  • extremity stiffness
  • muscle pain
  • stiff neck
  • stiff shoulders

Neurologic

  • leg weakness
  • numbness or tingling in fingers or toes

Miscellaneous

  • fatigue

Interactions

Drug-Drug interaction

Concurrent use of CYP 3A4 enzyme inhibitors (macrolide anti-infectives and protease inhibitors ) may produce serious, life-threatening peripheral ischemia and is contraindicated.Concurrent use with beta blockers, oral contraceptives, or nicotine (heavy smoking) may ↑ risk of peripheral vasoconstriction.Dihydroergotamine antagonizes the antianginal effects of nitrates.Concurrent use with vasoconstrictors may have ↑ effects (avoid concurrent use).Concurrent use with sumatriptan may result in prolonged vasoconstriction (allow 24 hr between use).

Route/Dosage

Intramuscular Subcutaneous (Adults) 1 mg; may repeat in 1 hr to a total of 3 mg (not to exceed 3 mg/day or 6 mg/wk).
Intramuscular Subcutaneous (Children ≥6 yr) 0.5 mg; may be repeated in 1 hr.
Intravenous (Adults) 0.5 mg; may repeat in 1 hr (not to exceed 2 mg/day or 6 mg/wk). For chronic intractable headache, 0.5–1 mg q 8 hr may be given until relief (not to exceed 6 mg/wk).
Intravenous (Children ≥6 yr) 0.25 mg; may be repeated in 1 hr.
Intravenous (Children and Adolescents 12–16 yr ) Severe, acute migraine—0.25–0.5 mg; 1–2 more doses may be given q 20 min.
Intravenous (Children 9–12 yr) Severe, acute migraine—0.2 mg; 1–2 more doses may be given q 20 min.
Intravenous (Children 6–9 yr) Severe, acute migraine—0.1–0.15 mg; 1–2 more doses may be given q 20 min.
Intranasal (Adults) 1 spray (0.5 mg) in each nostril, repeat after 15 min (2 mg total dose); not to exceed 3 mg/24 hr or 4 mg/wk.

Availability

Injection: 1 mg/mL (contains alcohol)
Nasal spray: 4 mg/1 mL in 1-mL ampules with nasal spray applicator

Nursing implications

Nursing 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. For adults, metoclopramide 10 mg IV may be administered 3–5 min before administration of dihydroergotamine IV. In children, metoclopramide or a phenothiazine antiemetic may be given orally as prophylaxis 1 hr before administration of dihydroergotamine IV. Oral administration may decrease risk of extrapyramidal and other side effects encountered with IV administration.
  • 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.

Potential Nursing Diagnoses

Acute pain (Indications)
Risk for injury (Side Effects)

Implementation

  • Administer as soon as patient reports prodromal symptoms or headache.
  • Intravenous Administration
  • pH: 3.4–4.9.
  • Dihydroergotamine may be administered undiluted.
  • Rate: Administer each dose over 1 min.
  • Syringe Compatibility:
    • promethazine.

Patient/Family Teaching

  • Instruct patient to use dihydroergotamine 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.
    • Instruct female patients to inform health care professional if they plan or suspect pregnancy. Dihydroergotamine should not be taken during pregnancy.
  • Intramuscular: Subcutaneous: Inject at the first sign of a headache and repeat at 1-hr intervals up to 3 doses. Once minimal effective dose is determined, adjust dose for subsequent attacks.
  • Intranasal: Instruct patient in proper use of nasal spray. Prime nasal sprayer 4 times before dose. Administer 1 spray to each nostril followed in 15 min by an additional spray in each nostril for a total of 4 sprays. Do not tilt head or sniff following spray. Do not use more than amount instructed. Discard ampule within 8 hr of opening. Do not refrigerate. Assembly may be used for 4 treatments; then discard.
    • Advise patient not to use Migranal to prevent a headache if there are no symptoms or if headache is different from typical migraine.
    • Instruct patient to notify health care professional if numbness or tingling in fingers or toes; pain, tightness, or discomfort in chest; muscle pain or cramps in arms or legs; weakness in legs; temporary speeding or slowing of heart rate; or swelling or itching occurs.

Evaluation/Desired Outcomes

  • Relief of pain from vascular headaches.

dihydroergotamine

/di·hy·dro·er·got·amine/ (-er-got´ah-mēn) an antiadrenergic derived from ergotamine; used as d. mesylate as a vasoconstrictor in the treatment of migraine.

dihydroergotamine

hydrogenated ergotamine, an alpha-adrenergic blocking agent and vasoconstrictor.
References in periodicals archive ?
Co-administration of cisapride, dofetilide, ergot alkaloids such as dihydroergotamine, ergotamine, ergometrine (ergonovine), and methylergometrine (methylergonovine); felodipine, levacetylmethadol (levomethadyl), lovastatin, methadone, oral midazolam, nisoldipine, pimozide, quinidine, simvastatin, and triazolam with ONMEL[TM] is contraindicated.
When used in combination with an antiemetic such as metoclopramide, dihydroergotamine (DHE) has been found to be as effective as opiates, valproate, and ketorolac in relieving migraine headache and preventing relapses, Dr.
Norvir should not be taken with the following medicines: astemizole, terfenadine, amiodarone, bepridil, encainide, flecainide, propafenone, quinidine, dihydroergotamine, ergotamine, ergonovine, methylergonovine, clorazepate, diazepam, estazolam, flurazepam, triazolam or oral (taken by mouth) midazolam, clozapine, pimozide, pethidine, piroxicam, propoxyphene, cisapride rifabutin, voriconazole, simvastatin, lovastatin, alfuzosin, fusidic acid, sildenafil used to treat a lung disease called pulmonary arterial hypertension, and products containing St John's wort (Hypericum perforatum).
Dihydroergotamine has traditionally been used in both an oral form and as an infusion for migraine.
The loss of sales due to the generic entry of blockbuster pain therapies over the next several years will be offset by the uptake of branded and emerging agents in current drug classes such as tapentadol extended release (Johnson & Johnson/Grunenthal's Nucynta ER/Palexia SR), orally inhaled dihydroergotamine (MAP Pharmaceuticals/Allergan's Levadex) and opioid reformulations.
LOS ANGELES -- An experimental inhaled form of dihydroergotamine appears to be effective in reducing migraine pain even if taken as late as 8 hours or more after the start of the headache, a post hoc analysis of a phase III clinical trial suggests.
ergotamine, dihydroergotamine, ergonovine and methylergonovine), products containing St.
The following drugs are contraindicated with nelfinavir: simvastatin (Zocor), lovastatin (Mevacor), rifampin (Rifadin, Rimactane), cisapride (Propulsid), midazolam (Versed), triazolam (Halcion), dihydroergotamine (DHE 45) and ergotamine (Cafergot).
Baron and his colleagues found that triptans or dihydroergotamine (DHE) safely treated both pre- and postcoiling headaches in a small group of migraineurs.
Kaletra should not be taken with amiodarone, astemizole, cisapride, dihydroergotamine, ergonovine, ergotamine, methylergonovine, midazolam, pimozide, terfenadine or triazolam.
If headaches recur, treat attacks earlier, increase the dose, switch triptans, particularly to naratriptan or frovatriptan, add an NSAID, or switch to dihydroergotamine mesylate, Dr.
Lay cautioned that the use of aspirin, ergotamine, dihydroergotamine, and the triptans should be avoided in pregnancy.