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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
CYP2D6 plays an important role in the metabolism of many indolealkylamines agents, which are 5-hydroxytryptamine (5-HT/serotonin) analogs that mainly act on the serotonin system (Yu 2008). Structurally, this group of compounds contains an indole moiety and a basic nitrogen atom, which are connected by an alkyl chain usually of two carbons in length. They mainly act on the 5-HT receptors, and some indolealkylamines such as ergotamine and a series of triptans including sumatriptan, zolmitriptan, naratriptan, almotriptan, frovatriptan, and rizatriptan have been developed for the clinical treatment of migraine (Saper and Silberstein 2006). However, many other indolealkylamine agents are widely abused compounds in developed countries although some have demonstrated therapeutic potential in psychopharmacotherapy. These include the notorious lysergic acid amides such as D-lysergic acid diethylamide and ergine; tryptamine derivatives such as psilocybin (O-phosphoryl-4-hydroxy-N,N-dimethyltryptamine), N,N-dimethyltryptamine (DMT), bufotenine (5-hydroxy-dimethyltryptamine), 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), and 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT, “Foxy,” or “Foxy Methoxy”); and β-carbolines such as harman, harmaline, harmine, and ibogaine (Yu 2008). All these compounds produce hallucinogenic and stimulant activities and high doses of administration will cause mydriasis, nausea, jaw clenching, and overt hallucinations with auditory and visual distortions.
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
Frovatriptan is a 5HT1B/1D receptor agonist with a high affinity for the 5HT1BaD receptors. A randomized, double-blind, placebo–controlled, parallel-group, outpatient study of placebo and 2.5, 5, 10, 20, or 40 mg of frovatriptan allocated in a 1:1:1:2:2:2 ratio was performed in 38 USA centers. At 2 hours there was a two–fold significant difference in response rates between all doses of frovatriptan (40–48%) and placebo (22%) (p≤0.012). More patients in each of the frovatriptan groups had relief of associated migraine symptoms and functional improvement than did those in the placebo group. Low recurrence rates were observed: 9–14% for frovatriptan and 18% for placebo, although in direct comparison with sumatriptan, the rates were comparable.86
Primary Headache Disorders
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Frovatriptan is a relatively new triptan with a long duration of action. It has a 25-hour elimination half-life and a favorable headache recurrence rate (Ryan et al., 2002). Frovatriptan is well tolerated and is available in 2.5 mg oral tablets. Because of its long duration of action, it is frequently used in menstrual migraine and in patients who suffer with prolonged attacks.
Current and emerging pharmacotherapy for menstrual migraine: a narrative review
Published in Expert Opinion on Pharmacotherapy, 2023
Claire E. J. Ceriani, Stephen D. Silberstein
Patients with fairly predictable cycles and a well-established pattern of MM attacks may be able to use a short-term prophylaxis approach. All women with migraine should keep a headache diary to look for such patterns, as even women who do not self-report MM may fulfill ICHD-3 criteria in two thirds of cases and could be candidates for this treatment approach [5]. Research on short-term prophylaxis using triptans has established an effective treatment strategy that should be investigated with other classes of medications. Multiple triptans have been shown to be effective at reducing the frequency, duration, and severity of MM when taken for 5–6 days starting 2–3 days before the anticipated onset of headache. Frovatriptan should be considered first-line based on overall efficacy, low recurrence rate, and good tolerability. NSAIDs appear to be a reasonable second-line option if triptans cannot be used or are ineffective, but more research is needed to determine the optimal dosing schedule. Evidence for DHE is limited but does point to it being an effective option. With newer, more-effective formulations of DHE now available, this is an avenue of research that deserves revisiting. The growing body of evidence linking estrogen fluctuations to changes in oxytocin and CGRP activity also suggests that the use of oxytocin agonists and CGRP antagonists may be fruitful areas of research.
Lasmiditan: an additional therapeutic option for the acute treatment of migraine
Published in Expert Review of Neurotherapeutics, 2021
Daniele Martinelli, Vito Bitetto, Cristina Tassorelli
The drugs most frequently used by migraine patients to treat their attacks include: Paracetamol/acetaminophen (PCM)Nonsteroidal anti-inflammatory drugs (e.g. ibuprofen, naproxen, diclofenac, desketoprofen, celecoxib, etc.)Acetylsalicylic acid (ASA)Triptans: sumatriptan, rizatriptan, eletriptan, almotriptan, zolmitriptan, naratripan and frovatriptanErgot alkaloidsCombination analgesics (e.g. triptan+NSAID or caffeine+NSAID+antiemetic)Miscellaneous: caffeine, metamizole, antiemetics (dopamine receptor antagonists: metoclopramide, chlorpromazine and prochlorperazine), opioids and barbiturates.
Pharmacological strategies to treat attacks of episodic migraine in adults
Published in Expert Opinion on Pharmacotherapy, 2021
In three crossover RCTs, 2.5 mg frovatriptan was compared to 10 mg rizatriptan, 2.5 mg zolmitriptan, and 12.5 mg almotriptan [59]. Patients were instructed to take the study medication as early as possible after the onset of a migraine attack. Preference, on a scale of 0 to 5, was the primary endpoint and similar for frovatriptan (2.9 to 3.1) and the three triptan comparators (3.0 to 3.4). Similarly, pain freedom after 2 h did not differ between frovatriptan and the three other triptans [59]. In contrast, in one unpublished RCT [71] in which moderate to severe headaches were treated, 100 mg sumatriptan was superior to 2.5 mg frovatriptan (+9%, see Table 4).