Bioequivalence Study of Cyclizine Hydrochloride 50 Mg Tablets in Healthy volunteers: a randomized, open-label, single-dose Study

Abhyankar, Dhiraj; Shedage, Ashish; Gole, Milind; Raut, Preeti

doi:10.4155/tde-2016-0023

Cited by 2 publications

(3 citation statements)

References 8 publications

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“…3 it is possible to observe that the hydrochloride species of guanfacine (6) and heroin (16) have a total de 6 N+O atoms while 2-CB (4), naloxone (11), both forms of scopolamine (12,15) and cocaine (13) have 5 N+O atoms. Morphine (10) only has 4 N+O atoms while a total of 3 N atoms present clonidine (5). With 2 N+O atoms appear tolazoline (2), gramine (3), diphenhydramine (7), cyclizine (8), promethazine (9) and methadone (14) and with only one N atom tropane (1).…”

Section: Stabilization and Solvation Energies Dipole Moment And Volumentioning

confidence: 99%

“…In pharmacology and medicine, the hydrochloride / hydrobromide species are generally used as drugs in multiple and clinical applications, including in dosage, because these species present higher solubilities than their free bases, this way, they can be easily absorbed and assimilated in the human organism [1][2][3][4][5][6][7][8][9][10]. Veber et al [9] have studied important molecular properties necessary to the oral bioavailability of drugs while Lipinski et al have predicted the absorption or permeation of a drug taking into account the presence of H bonds acceptors (N-H or OH groups) and donors (N and O atoms) and, also, the molecular weights, among other factors [10].…”

Section: Introductionmentioning

confidence: 99%

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Correlations in hydrochloride drugs with diverse pharmacological activities. Role of N-H…Cl bonds

2020

Biointerface Res Appl Chem

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In this work, the structural and vibrational properties of sixteen hydrochloride/hydrobromide drugs with different pharmacological activities have been compared and analysed in order to find some correlations among their properties and, mainly elucidate the role of N-H•••Cl bonds in them. Here, the properties of ten alkaloids: tropane, gramine, morphine, cocaine, methadone, naloxone, heroin and scopolamine as hydrochloride and hydrobromide including, the psychotropic 2-CB agent; three antihistaminic: diphenhydramine, cyclizine and promethazine and; three antihypertensive tolazoline, clonidine and guanfacine agents have been evaluated. All properties were predicted in gas phase and aqueous solution by using the hybrid B3LYP/6-31G* method and the same were evaluated in functions of their molecular weights. Here, stabilization and solvation energies, dipole moments and volumes in both media, atomic MK charges and bond N-H and N+Cl- lengths, N-H stretching modes of N-HCl bonds of hydrochloride and their cationic species and, frontier orbitals together with global electrophilicity and nucleophilicity descriptors were compared for those sixteen drugs. The results have shown that bonds N+Cl- lengths of all hydrochloride species are higher in solution, as compared with the values in gas phase. Hydrochloride species of alkaloids and antihistaminic agents in both media present higher positive MK values on the N atoms of N-HCl bonds while the species related to antihypertensive agents show higher negative MK values on the N atoms or low positive values. The species of guanfacine presents the higher number of donors and acceptors groups, higher dipole moment value in solution, low bond N-H lengths, higher negative charge on the N atom of N-HCl bond and, higher global electrophilicity index. Hydrochloride species of scopolamine and heroin present the more negative solvation energies while tolazoline the lower value. Hydrochloride species of 2-CB and diphendramine show the higher expansions volumes in solution while the species of naloxone, scopolamine and cocaine evidence volumes contractions in this medium. These studies show that the knowledge of hydration degrees, that is, the number of water molecules that hydrate the hydrochloride species are essential to understand the hydration process of these species in relation to the differences observed in solvation energies, volume variations and dipole moment values.

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Section: Stabilization and Solvation Energies Dipole Moment And Volumentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Correlations in hydrochloride drugs with diverse pharmacological activities. Role of N-H…Cl bonds

2020

Biointerface Res Appl Chem

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“…Cyclizine is a piperazine-derived, first-generation histamine-1 receptor antagonist, first produced in 1952 1. The antiemetic mechanism of cyclizine is poorly understood, but is generally accepted to be related to its antihistaminergic and anticholinergic properties 2. It has an oral bioavailability of 50% and is extensively metabolised to inactive metabolites, with a half-life in healthy volunteers of between 13 and 20 hours 3 4.…”

Section: Introductionmentioning

confidence: 99%

Cyclizine pharmacovigilance in hospice/palliative care: net effects for nausea or vomiting

McNeill

Prael

Hunt

et al. 2022

BMJ Support Palliat Care

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ObjectivesTo describe the contemporary real-world use of cyclizine for nausea or vomiting, and the associated benefits and harms.MethodsThis was a prospective, consecutive case series of routine clinical use of cyclizine for nausea or vomiting in palliative care conducted across 19 sites in Australia, Aotearoa/New Zealand and the UK. Clinical outcomes were graded using the National Cancer Institute Common Terminology Criteria for Adverse Events at baseline and 72 hours after initiation of cyclizine. Ad hoc safety reporting continued for 2 weeks.ResultsData were collected from 101 patients between May 2018 and December 2020. Cyclizine was mostly used in combination with another antiemetic. Overall, 79 patients benefited and 32 experienced harm (56 had benefit without harm; 9 had harm without benefit). The most common harms were constipation (13%), somnolence (9%) and confusion (7%), adding to the already high rates of these symptoms at baseline. For the four patients with serious harms (grade ≥3), these were exacerbations of existing symptoms. Nine patients stopped cyclizine at 72 hours and a further 20 patients within 2 weeks. The most common reasons for stopping were lack of benefit and symptom resolution; none stopped because of harms.ConclusionsWhen used as described in a palliative care setting, cyclizine benefits about three-quarters of patients, with about one-third experiencing tolerable harms.

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Bioequivalence Study of Cyclizine Hydrochloride 50 Mg Tablets in Healthy volunteers: a randomized, open-label, single-dose Study

Abstract: Cyclizine 50 mg is bioequivalent to the reference.

Cited by 2 publications

References 8 publications

Correlations in hydrochloride drugs with diverse pharmacological activities. Role of N-H…Cl bonds

Correlations in hydrochloride drugs with diverse pharmacological activities. Role of N-H…Cl bonds

Cyclizine pharmacovigilance in hospice/palliative care: net effects for nausea or vomiting

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