Ergotamine

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MIMS

Ergotamine
Indications Migraine.
Dosage Adult : Sublingual 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. Inhalation 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.
Dosage Details 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
Contraindicated.
Impairment
Hepatic
Contraindicated.
Impairment
Administration May be taken with or without food.
Contraindications 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).
Special
Patient w/ anaemia. Lactation.
Precautions
Adverse Drug Nausea and vomiting, abdominal pain, tingling of fingers and toes,
Reactions weakness, muscle pains in the extremities and numbness, localised oedema,
itching, bradycardia, transient tachycardia.
Pregnancy
Category (US PO/Rectal/SL: X
FDA)
Patient May cause dizziness and feelings of anxiety, if affected, do not drive or
Counselling operate machinery.
Monitoring
Evaluate CV status prior to initiation and periodically thereafter.
Parameters
Overdosage 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.
Drug Interactions 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.
Mechanism of Description: Ergotamine has marked vasoconstrictor effects and partial
Action 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).
Storage Store between 20-25°C. Protect form heat and light.
MIMS Class Antimigraine Preparations
ATC N02CA02 - ergotamine ; Belongs to the class of ergot alkaloids
Classification preparations. Used to relieve migraine.

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