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Analgesics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Zolmitriptan is another triptan used to treat migraine headaches. No studies of its use in human pregnancy are published. In rats, mice and rabbits given up to several thousand times the usual human dose, the frequency of birth defects was not increased. At the usual human dose, no adverse effects were observed, but at high doses, embryolethality was increased in frequency (Manufacturer’s information).
Commercialized Microneedles
Published in Boris Stoeber, Raja K Sivamani, Howard I. Maibach, Microneedling in Clinical Practice, 2020
KangJu Lee, Seung Hyun Park, Ji Yong Lee, Won Hyoung Ryu
Different types of MN applicators have been developed. Using an applicator, drug and vaccine could be delivered by a simple and one-step administration and the MN insertion pressure on the skin surface could be controlled. Corium International, Inc. has developed proprietary MicroCor® transdermal technology that utilizes dissolving MNs for drug delivery (Figure 9.4c). MicroCor® is fabricated by a combination of a water-insoluble backing layer and a solid-state biodegradable microstructure array containing an active therapeutic agent using the drug-in-tip technology. The MicroCor PTH(1-34) product, being developed for the treatment of osteoporosis, has successfully completed a phase 2a clinical evaluation. The Zosano Pharma Corp.'s patch system developed its unique microprojection array, called adhesive dermally applied microarray (ADAM) (Figure 9.4d). ADAM is mounted on the ZP-applicator and attached on the skin surface like an adhesive bandage. In the phase 1 clinical trial, ADAM showed a three-times-higher drug effect than that of the oral administration of Zolmitriptan for migraine treatment [15] and a phase 3 clinical trial has been conducted. Nemaura Pharma, Ltd. developed an advanced drug loading system, a solid dose delivery device called Micropatch™ (Figure 9.4e). Since the drugs are coated on the surface of the needle with a frustoconical-shaped pellet, Micropatch™ can deliver a solid dose below the skin. The pellet is fabricated by compressing the combination of a freeze-dried vaccine and excipients using a micro-press to the desired size.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
The oral bio-availability of zolmitriptan (40%) is greater than sumatriptan (14%). However, it has been found that a moderate to severe migraine attack can reduce absorption by up to 40% (Hale 2017). It has a metabolite that is significantly more active. There are no studies into the amount passing into breastmilk. The BNF states that zolmitriptan should be used with caution as it is present in milk in animal studies.
Differential pharmacokinetic drug-drug interaction potential of eletriptan between oral and subcutaneous routes
Published in Xenobiotica, 2019
Harilal Patel, Nirmal Desai, Prakash Patel, Nirav Modi, Krunal Soni, Nitin Dobaria, Nuggehally R. Srinivas
Triptans such as sumatriptan, zolmitriptan, eletriptan, rizatriptan etc. are typically prescribed for the treatment of migraine. The physician prescription choice takes into account several features like faster onset of action, severity of the attacks, potential adverse events, tolerance, rate of headache reoccurrence and cost (Mayans & Walling, 2018). While oral product appears to be the preferred option for migraine treatment, slower rate of absorption due to delay in gastric emptying accompanied by episodes of nausea and vomiting may be disadvantageous. Hence, formulation strategies and different routes of drug administration of anti-migraine drugs to improve the pharmacokinetic properties and faster delivery have been explored (Kassem, 2016). In this regard, parenteral route such as subcutaneous may be beneficial in providing rapid onset of action resulting in faster relief of headache without being affected by gastrointestinal disturbance that occurs in migraine.
Pharmacotherapy for acute migraines in children and adolescents
Published in Expert Opinion on Pharmacotherapy, 2019
P. Barbanti, L. Grazzi, G. Egeo
The efficacy of oral zolmitriptan in pediatric migraine was suggested by an open study of 38 adolescents treating 276 attacks with incremental doses (2.5 mg for the first 2 migraines, 2.5 or 5 mg, at patient’s discretion, for subsequent attacks) reporting an overall 2 h headache response of 80% and 2 h pain-free response of 66% [23].These encouraging findings were confirmed by a crossover RCT comparing the efficacy of zolmitriptan 2.5 mg, ibuprofen 200–400 mg, and placebo in the acute treatment of 3 consecutive migraine attacks in 32 migraineurs aged 6–18 years. This study demonstrated that zolmitriptan was as effective as ibuprofen and superior to placebo for 2 h pain relief and 2 h pain-free rates, though with a higher incidence of mild and transient side effects. Notably, the placebo effect in this study was unexpectedly lower than in other trials of acute migraine treatment in pediatric populations [24]. However, a very large RCT, enrolling 850 adolescents aged 12–17 years revealed that oral zolmitriptan was ineffective in acute migraine treatment at all doses (2.5, 5, 10 mg) when considering 2 h headache response or 2 h pain-free rates. The authors ascribed the negative results to the high placebo response rate [25].
In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug
Published in Drug Delivery, 2019
Ebtsam M. Abdou, Soha M. Kandil, Amany Morsi, Maysa W. Sleem
Zolmitriptan (4S-4-({3-[2-(dimethylammino)ethyl]-1H-indol- 5-yl}methyl-1,3-oxazolidin2-one) is second generation triptan which is an effective, well-tolerated treatment of acute migraine associated with menses, migraine with aura. It has a selective action on serotonin (5HT1B/1D) receptors and is very effective in reducing migraine symptoms. It is also effective in treatment of acute cluster headache (Cittadini et al., 2006; Cortelli et al., 2017). Oral administration zolmitriptan has been reported to show slow onset of action, low bioavailability (40%), nausea, and incomplete pain relief with recurrence of headaches (Ahonen et al., 2004; Goadsby & Yates, 2006; Mittal et al., 2014) with considerable ratio of migraine patients suffering from gastric stasis, severe nausea, and vomiting during the migraine attack. The matters which causes erratic absorption of the drug from the gastrointestinal tract with delayed gastric emitting which makes the oral treatment is ineffective (Vyas et al., 2005; Aurora et al., 2007; Egla & Abd Al hammid 2016).