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Analgesics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Sumatriptan (Imitrex) is a selective 5-hydroxytryptamine receptor agonist. It is used primarily as acute therapy for migraine headaches. The frequency of birth defects was not increased among 658 infants born to women who used sumatriptan during the first trimester (Kallen and Lynger, 2001). Among 479 first-trimester exposures to sumatriptan, the frequency of major birth defects was not increased (Cunnington et al., 2009). According to the manufacturer’s registry, 52 infants born after first trimester exposure did not have an increased frequency of birth defects (Sumatriptan Registry, 2009). Sumatriptan has been shown to cause birth defects in rabbits, but it was not teratogenic in rats. Sumatriptan was shown to cross the placenta by passive transport in the ex vivo isolated perfused cotyledon technique (Schenker et al., 1995). Under the old FDA classification system, it is a category C agent. However, available data suggest the drug is safe for use during pregnancy (Table 8.2). Other triptans include naratriptan, almotriptan, rizatriptan, zolmitriptan. None of these migraine drugs has been adequately studied during pregnancy.
Headache
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
Adverse effects of sumatriptan are common but are usually mild and short-lived. The most frequent are tingling, paresthesias, and warm sensations in the head, neck, chest, and limbs; less frequent are dizziness, flushing, and neck pain or stiffness. The risk and intensity is greater with the fixed subcutaneous formulation. “Chest-related symptoms” include short-lived heaviness or pressure in the arms and chest, shortness of breath, chest discomfort, anxiety, palpitations, and, very rarely, chest pain. The mechanism is unknown. The risk of sumatriptan-induced myocardial ischemia in the absence of coronary artery disease appears to be acceptable (e.g. no greater than the risk of exercise-induced myocardial ischemia in athletes).27
Pharmacological Characterization of 5-Hydroxytryptamine Receptors in the Gastrointestinal Tract
Published in T.S. Gaginella, J.J. Galligan, SEROTONIN and GASTROINTESTINAL FUNCTION, 2020
Jeremy D. Gale, Keith T. Bunce
The only well-defined agonist at the 5-HT1D receptor is sumatriptan, where it is approximately 10 times less potent than 5-HT.9 Sumatriptan has approximately 10-fold selectivity for the 5-HT1D over the rat 5-HT1B receptor and demonstrates approximately 10- to 50-fold selectivity for 5-HT1D receptors over 5-HT1A receptors.53 This situation may be further complicated by recent reports that sumatriptan shows some binding affinity for the newest members of the 5-HT receptor family, which have been identified through molecular biological techniques.54,55 Whether this translates to functional activity has still to be demonstrated. When used in vivo it should be noted that sumatriptan only poorly penetrates the blood-brain barrier.
Current understanding of the etiology of cyclic vomiting syndrome and therapeutic strategies in its management
Published in Expert Review of Clinical Pharmacology, 2022
Rosita Frazier, Thangam Venkatesan
The recommended dose for sumatriptan is 20 mg intranasally, with a head-forward to avoid dripping down the throat and a bitter taste [80]. It can also be administered as a 6 mg subcutaneous injection. In children, a personal and/or family history of migraine predicted a response to treatment. Li et al. found that 69% of children had >50% reduction in vomiting episodes with subcutaneous sumatriptan [79]. Hikita et al. found that 54% of CVS attacks were responsive to sumatriptan therapy (response was defined as at least a 50% reduction in vomiting frequency) [81]. A more recent retrospective study of 101 adults with CVS showed an improvement in nausea (55%), vomiting (59%), and abdominal pain (43%) within 2 h and at 24 h (67%, 73%, and 67%), respectively. Forty-six percent reported that sumatriptan helped them avoid ED visits and 51% avoided being hospitalized. Non-response to sumatriptan was associated with depression, current cannabis use, and use of benzodiazepines or opioids during an episode. No serious side effects were noted [82].
Pharmacological strategies to treat attacks of episodic migraine in adults
Published in Expert Opinion on Pharmacotherapy, 2021
Recurrence cannot be prevented with a second dose of 100 mg oral sumatriptan after 2 to 4 h [82–84], but can usually be treated successfully with a second dose of 100 mg sumatriptan [82,83] and 10 mg rizatriptan [85]. In two RCTs, the initial 100 mg of oral sumatriptan was followed by either 100 mg sumatriptan or placebo after 2 h [82] or 4 h [83]. Headache relief rates after 4 h [82] and 8 h [83] for 100 mg sumatriptan plus 100 mg sumatriptan and 100 mg sumatriptan plus placebo were 80% vs. 77% [82] and 85% vs. 84% [83], respectively. Similar results were observed in two RCTs with subcutaneous sumatriptan plus subcutaneous sumatriptan vs. subcutaneous sumatriptan plus placebo [16]. These RCTs demonstrate that sumatriptan is not as effective as a rescue medication in patients who do not respond to the first dose. Despite this, the prescribing information concerning a second dose of a triptan is often unclear [86].
Treating status migrainosus in the emergency setting: what is the best strategy?
Published in Expert Opinion on Pharmacotherapy, 2018
László Vécsei, Délia Szok, Aliz Nyári, János Tajti
The possible routes of administration of triptans is numerous, including oral, SC, nasal spray, patch, transdermal iontophoresis, and rectal routes. In the ED setting, among parenteral formulations, the SC route is recommended as first choice regarding the way of application of triptans. Before administration of triptans, ECG should be performed to look for ischemic signs [20]. In a severe and long-lasting or recurrent migraine headache, SC sumatriptan (6 mg) should be offered (level B) (Figure 2(b)) [35]. Common adverse events of SC sumatriptan application are chest tightness, rash at injection site, generalized weakness, and dizziness [35]. Contraindications of triptans are cardiovascular diseases, uncontrolled hypertension, and pregnancy [12].