Tigreat
Tigreat Uses, Dosage, Side Effects, Food Interaction and all others data.
Tigreat is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular those associated with menstruation. Tigreat causes vasoconstriction of arteries and veins that supply blood to the head.
Tigreat is a second generation triptan 5-HT receptor agonist that binds with high affinity for 5-HT1B and 5-HT1D receptors. It is structurally distinct from, but pharmacologically related to other selective 5-HT1B/1D receptor agonists. Tigreat has no significant effects on GABAA mediated channel activity and has no significant affinity for benzodiazepine binding sites. Tigreat is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Research has shown that migraine can be caused by the swelling of blood vessels around the brain. Tigreat eases the pain associated with migraine by narrowing these blood vessels. Tigreat has one of the highest affinities for the 5-HT1B of the second-generation triptan agonists.
| Trade Name | Tigreat |
| Availability | Prescription only |
| Generic | Frovatriptan |
| Frovatriptan Other Names | Frovatriptan |
| Related Drugs | Ubrelvy, Botox, diclofenac, celecoxib, metoclopramide, sumatriptan, Imitrex, Reglan |
| Type | |
| Formula | C14H17N3O |
| Weight | Average: 243.3043 Monoisotopic: 243.137162181 |
| Protein binding | Binding to serum proteins is low (approximately 15%). Reversible binding to blood cells at equilibrium is approximately 60%. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | France |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tigreat is a 5-HT1B/1D receptor agonist used to treat migraines.
For the acute treatment of migraine attacks with or without aura in adults.
Tigreat is also used to associated treatment for these conditions: Menstrual Migraines, Migraine With Aura, Migraine Without Aura
How Tigreat works
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
Toxicity
There is no direct experience of any patient taking an overdose of Tigreat. The maximum single dose of frovatriptan given to male and female patients with migraine was 40 mg (16 times the clinical dose) and the maximum single dose given to healthy male subjects was 100 mg (40 times the clinical dose) without significant adverse events.
Food Interaction
- Take with or without food. Food does not affect bioavailability, but delays maximum concentrations by one hour.
Tigreat Cholesterol interaction
[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.
Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).
Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.
In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.
As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.
Periodic cardiovascular evaluations should be performed during intermittent, long-term use.
Tigreat Drug Interaction
Major: duloxetine, duloxetine, escitalopram, escitalopramUnknown: onabotulinumtoxinA, onabotulinumtoxinA, galcanezumab, galcanezumab, pregabalin, pregabalin, topiramate, topiramate, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, lisdexamfetamine, lisdexamfetamine, alprazolam, alprazolam
Tigreat Disease Interaction
Major: CAD risk factors, cardiovascular diseaseModerate: liver disease
Volume of Distribution
- 4.2 L/kg [males]
- 3 L/kg [females]
Elimination Route
Tigreat is rapidly absorbed from the duodenum, but has low oral bioavailability.
Half Life
26 hours
Clearance
- 220 mL/min [male receiving IV dose of 0.8 mg]
- 130 mL/min [Female receiving IV dose of 0.8 mg]
Elimination Route
Radiolabeled compounds excreted in urine were unchanged frovatriptan, hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, together with several other minor metabolites. Less than 10% of frovatriptan was excreted in urine after an oral dose.
Innovators Monograph
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