Vascurin Suppository
Caffeine + Ergotamine Tartrate
100mg + 2mg
Beximco Pharmaceuticals Ltd.
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| Retail Price | 4.05 AED |
Indications
Vascurin Suppository is used for:
Acute Migraine, Vascular Headache
Adult Dose
Vascular Headache
Indicated as therapy to abort or prevent vascular headache (eg, migraine, migraine variants, “histaminic cephalalgia”)
Adult:
Oral
Each tablet contains ergotamine tartrate 2 mg and caffeine hydrate 100 mg.
Initially, 1 tablet, additional doses of ½-1 tablet may be taken at half-hourly intervals, if needed.
To be taken as soon as possible at the 1st warning of a migraine attack.
Max: 3 tablets in 24 hr, 4 tablets per attack, 6 tablets per week and 2 courses of treatment per month.
Ensure an interval of at least 4 days between successive treatment courses.
Rectal
Suppository: 1 suppository should be taken at the first sign of a migraine attack.
If not relieved from the first dose, a 2nd dose may be taken no sooner than 1 hour after the first dose.
The use of this suppository should not be used on a daily basis.
Maximum 2 suppositories for any single migraine attack and maximum 5 suppositories during any 7-day period.
Child Dose
Renal Dose
Renal impairment
Contraindicated
Administration
Contra Indications
Not to be used with potent inhibitors of CYP3A4 and protease inhibitors. Hyperthyroidism, renal or hepatic impairment. Pre-existing vascular disease including coronary disease, obliterative vascular disease, angina, claudication, peripheral ischaemia, Raynaud's syndrome and hypertension. Not to be used when there is sepsis. Pregnancy and lactation.
Precautions
Serious and/or life-threatening peripheral ischemia associated with coadministration of ergotamine and caffeine with potent CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics
Because CYP3A4 inhibition elevates ergotamine and caffeine serum levels, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased
Concomitant use of these medications is contraindicated
Ergotism
Although ergotism rarely develop even after long-term intermittent use of orally administered ergotamine, do not exceed dosage recommendations
Ergotism manifested by intense arterial vasoconstriction, producing signs and symptoms of peripheral vascular ischemia
Headache, intermittent claudication, muscle pains, numbness, or coldness and pallor of the digits may occur with chronic intoxication; if the condition is allowed to progress untreated, gangrene can result
While most cases result from frank overdosage, some cases involve hypersensitivity
There are few reports among patients taking doses within recommended limits or for brief periods
Withdrawal symptoms (eg, rebound headache) upon discontinuation are rare; typically reported with long, indiscriminate use
Fibrotic complications
Retroperitoneal and/or pleuropulmonary fibrosis reported
Rare reports of fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with long-term, continuous use of ergotamine tartrate and caffeine
Do not use for chronic daily administration
Pregnancy-Lactation
Pregnancy
Contraindicated; ergotamine elicits oxytocic effects
There are no studies on placental transfer or teratogenicity of the combination of ergotamine and caffeine
Labor and delivery
Contraindicated in labor and delivery owing to ergotamine’s oxytocic effect, which is maximal in the third trimester
Animal studies
Caffeine is known to cross the placenta and has been shown to be teratogenic in animals
Ergotamine crosses the placenta in small amounts, although it does not appear to be embryotoxic in this quantity; however, prolonged vasoconstriction of uterine vessels and/or increased myometrial tone leading to reduced myometrial and placental blood flow may have contributed to fetal growth retardation observed in animals
Lactation
Ergot drugs are known to inhibit prolactin, but there are no reports of decreased lactation with ergotamine/caffeine
Ergotamine is excreted in breast milk and may cause symptoms of vomiting, diarrhea, weak pulse, and unstable blood pressure in nursing infants
Owing to the potential serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, considering the importance of the drug to the mother
Interactions
Increased sedative effect when used with alcohol. Caffeine may increase clearance of lithium.
Clearance of caffeine may be reduced when used with oestrogens, progesterones, mexiletine, fluvoxamine, disulfiram or quinoline antibacterial.
Serum levels of ergotamine-containing drugs may be increased when used with macrolide antibacterial.
Concurrent use with MAOIs or TCAs may increase the sedative and antimuscarinic effects of cyclizine.
Increased clearance of caffeine by phenytoin. Increased risk of arterial occlusion with methysergide and vasospasm with 5-HT1 agonists.
Avoid ergotamine for 6 hr after almotriptan, sumatriptan, rizatriptan and zolmitriptan, and for 24 hr after eletriptan.
Avoid almotriptan, eletriptan, sumatriptan and rizatriptan for 24 hr, and zolmitriptan for 6 hr, after ergotamine.
Increased sedative effects when used with anxiolytics and hypnotics.
Increased risk of vasoconstriction when used with β-blockers or nicotine.
May reduce anti-anginal effects of glyceryl trinitrate. May increase plasma levels of theophylline.
Potentially Fatal: Concurrent use with HIV-proteases which are potent CYP3A4 inhibitors (e.g. amprenavir, indinavir, nelfinavir, ritonavir) is not recommended due to increased risk of ergotism.
Contraindicated (32)
almotriptan
clarithromycin
cobicistat
eletriptan
elvitegravir/cobicistat/emtricitabine/tenofovir DF
fezolinetant
frovatriptan
glyceryl trinitrate pr
isocarboxazid
itraconazole
ketoconazole
letermovir
levoketoconazole
linezolid
mifepristone
naratriptan
nirmatrelvir/ritonavir
nitroglycerin IV
nitroglycerin sublingual
nitroglycerin topical
nitroglycerin transdermal
nitroglycerin translingual
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
phenelzine
procarbazine
pseudoephedrine
rizatriptan
selegiline transdermal
sumatriptan
sumatriptan intranasal
tranylcypromine
voriconazole
Adverse Effects
Side effects of Caffeine + Ergotamine Tartrate :
Frequency Not Defined
Gastrointestinal: Nausea and vomiting; rectal or anal ulcer (from overuse of suppositories)
Neurological: Paresthesia, numbness, weakness, and vertigo
Allergic: Localized edema and itching
Cardiovascular
Serious vasoconstrictive complications may occur including ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes, and muscle pains
Most commonly occurs with long-term therapy at relatively high doses; also reported with short-term or normal doses
Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension
Mechanism of Action
Ergotamine is an alpha-adrenergic blocker with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels, it also depresses central vasomotor centers. Caffeine is also a cranial vasoconstrictor.
Note
Vascurin 100mg + 2mg Suppository manufactured by Beximco Pharmaceuticals Ltd.. Its generic name is Caffeine + Ergotamine Tartrate. Vascurin is availble in Bangladesh.
Farmaco BD drug index information on Vascurin Suppository is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.