Pain and analgesics
Hugh McGavock in How Drugs Work, 2017
The management of acute migraine (a blinding one-sided headache which usually incapacitates the patient for its duration) has been revolutionised by the discovery of the drug family the triptans, of which sumatriptan was the first. They may be taken as tablets, injections (subcutaneous), or nasal spray. They are agonists (stimulants) at the 5-HT1D receptors in the brain. Unfortunately, the pathophysiology of migraine is still unknown - another example of our ignorance of much CNS function (described in Chapter 11). It is known that cerebral blood flow is altered in certain migraine attacks. Triptans have no place in the prophylaxis (prevention) of migraine. Drugs are used for prevention in severe cases only (two or more acute migraines per month). They include a beta-blocker (seeChapter 7), a tricyclic antidepressant (seeChapter 18), or a newer drug, pizotifen, which blocks histamine (an inflammatory amine released during inflammation) and is a serotonin receptor antagonist. See the BNF, 'prophylaxis of migraine', for more details. As in acute migraine drug treatment, the mode of action of these effective prophylactics in preventing the neurophysiological disorder causing migranous headache is unknown.
Primary Headache Disorders
Mark V. Boswell, B. Eliot Cole in Weiner's Pain Management, 2005
The utility of these medications in arresting migraine attacks is due to their ability to counteract the dilation of small cerebral arteries and arterioles, primarily the branches of the external carotid artery. Nausea and lethargy are common side effects of the ergotamine preparations. Ergotamine tartrate use should be limited and not repeated for at least 4 days to avoid the possibility of ergotamine rebound headache, characterized by a self-sustaining cycle of daily or near daily migraine headaches coupled with the urge to take ergotamine to relieve symptonms (Gallagher, 1983). Ergotamine and its derivatives should be avoided in elderly and in pregnant patients. Dihydroergotamine, which was developed as an improvement over ergotamine tartrate, is highly effective and has a better safety profile. It is available in parenteral and nasal formulations. The nasal spray is more convenient and tolerable, has a low recurrence rate, and resolves migraine attacks in up to 70% of patients (Gallagher, 1996).
Pharmacopeial and Regulatory Guidances on Product Quality and Performance
Anthony J. Hickey, Sandro R.P. da Rocha in Pharmaceutical Inhalation Aerosol Technology, 2019
Figure 26.2 indicates the general chapters describing requirements and test of relevance to inhalation products. The important performance measures for these products are the dose, which is influenced by formulation and device design and the aerodynamic particle size distribution, which influences the deposition in the lungs. Nasal sprays and powders are also dependent on dose-delivered and plume characteristics although it is clear that the aerosol delivered from a nasal spray is unlikely to fully develop in the nasal cavity. Consequently, these performance measures for nasal products are mostly indicators of quality rather than bioavailability. GC<601> describes delivered dose uniformity and aerodynamic particle size distribution measurement for inhalation and nasal products (USP41-NF36 2018f). GC<602> and GC<604> describe propellants and leak rate testing (USP41-NF36 2018g, 2018h).
Montelukast nasal spray: formulation development and in vitro evaluation
Published in Pharmaceutical Development and Technology, 2019
Thunyaporn Jullaphant, Titpawan Nakpeng, Teerapol Srichana
The advantages of nasal spray include rapid onset, low dose, low systemic side effects, and avoidance of first-pass metabolism (Illum 2002; Ugwoke et al. 2005; Jadhav et al. 2007). Even though intranasal drug delivery offers many advantages, one of the limitations is the mucociliary clearance mechanism (MCC) (Illum 2002; Ugwoke et al. 2005; Jadhav et al. 2007; Touitou and Illum 2013; Gizurarson 2015). The formulation must prolong the residence time within the nasal cavity to enhance the bioavailability of the drug. To achieve this goal, the use of mucoadhesive polymer-based systems must demonstrate a prolonged contact time with the mucosa. There are some studies that use cellulose derivatives like hydroxypropyl cellulose (HPC) and acrylates copolymer like carbomer 940 (C940) as the mucoadhesive in the formulations. These polymers were used in various dosage forms such as powder, liquid and gel for intranasal drug administration. They are widely used in topical formulation drug delivery systems as a mucoadhesive agent because of nontoxic, nonirritant and safe in humans (Chaturvedi et al. 2011). In this work, HPC and C940 were employed as mucoadhesive polymers.
Papilledema from gain-of-function mutations in the STAT3 gene
Published in Ophthalmic Genetics, 2019
Young-Woo Suh, Jonathan C. Horton
Evaluation revealed anemia, neutropenia, and idiopathic thrombocytopenia. Fundus examination showed marked bilateral optic disc swelling. A lumbar puncture was performed under sedation, yielding an opening pressure of 45 cm of water. There were 14 white cells/ml (97% lymphocytes, 3% monocytes), with a normal protein and glucose. He was thought to have an autoimmune lymphoproliferative syndrome and was treated with acetazolamide, prednisone, and mycophenolate mofetil. Over the subsequent year, the papilledema resolved completely and nerve fiber layer thickness measurements returned to normal. Treatment with acetazolamide and prednisone was halted, but he continued to receive mycophenolate mofetil and monthly infusions of IVIG. Other medications included cetirizine, diphenhydramine, montelukast, fluticasone nasal spray, loratadine, and ondansetron.
The current state of acute treatment for migraine in adults in the United States
Published in Postgraduate Medicine, 2020
Wade Cooper, Erin Gautier Doty, Helen Hochstetler, Ann Hake, Vincent Martin
According to the American Headache Society Evidence Assessment of Migraine Pharmacotherapies, no recent high-quality studies have been published for injected DHE [25]. In clinical trials with DHE nasal spray, 30% to 61% of participants reported a reduction in headache severity to mild or no pain in 2 h, compared to 20% to 33% for placebo. The most common side effects associated with DHE nasal spray were rhinitis, altered sense of taste, application site reactions, dizziness, nausea, and vomiting [36]. Because nausea and vomiting are common side-effects of DHE, coadministration of an antiemetic is recommended [37]. DHE should be used with caution, or avoided entirely, in patients with cardiovascular disease including coronary artery disease, peripheral vascular disease, and uncontrolled hypertension [1].
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