Hydralazine Hydrochloride

2021 ◽  
pp. 829-832
Author(s):  
Himanshu Acharya ◽  
Rakesh Patel

Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 24 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Polymers of hydroxy propyl methyl cellulose (HPMC K100M), HPMC K15M, carbopol 940 and sodium bicarbonate were used as the release retarding agents. This study investigated utility of a 3-factor, 3-level Box-Behnken design and optimization process for floating tablet of Hydralazine with 5 replicates of center points. Amount of HPMC K4 (Hydroxy Propyl Methyl cellulose), amount of sodium bicarbonate were selected as the independent variables whereas total floating time (TFT), T90, % cumulative drug release at 24 hours, and T20, Q1 were selected as dependent variables. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. The produced tablets exhibited good floating time and controlled drug release over a period of 24 h. The resultant data were critically analyzed to locate the composition of optimum formulations. All predicted values of response variables of optimized formulation demonstrated close agreement with the experimental data during optimization procedure.


RSC Advances ◽  
2021 ◽  
Vol 11 (45) ◽  
pp. 27820-27831
Author(s):  
Hemanth Kumar Chanduluru ◽  
Abimanyu Sugumaran

Analysing isosorbide dinitrate and hydralazine by using an eco-friendly method is an initial stepping stone towards environmentally benign method development, and its combination with the AQbD makes it the method to use for ages without revalidation.


1993 ◽  
Vol 50 (4) ◽  
pp. 683-686
Author(s):  
Kennth S. Alexander ◽  
Madhusudhan Pudipeddi ◽  
Gordon A. Parker

2020 ◽  
Vol 51 (10) ◽  
pp. 764-776 ◽  
Author(s):  
Kimberly S. Collins ◽  
Anthony L.J. Raviele ◽  
Amanda L. Elchynski ◽  
Alexander M. Woodcock ◽  
Yang Zhao ◽  
...  

<b><i>Background:</i></b> Despite its approval in 1953, hydralazine hydrochloride continues to be used in the management of resistant hypertension, a condition frequently managed by nephrologists and other clinicians. Hydralazine hydrochloride undergoes metabolism by the N-acetyltransferase 2 (NAT2) enzyme. NAT2 is highly polymorphic as approximately 50% of the general population are slow acetylators. In this review, we first evaluate the link between NAT2 genotype and phenotype. We then assess the evidence available for genotype-guided therapy of hydralazine, specifically addressing associations of NAT2 acetylator status with hydralazine pharmacokinetics, antihypertensive efficacy, and toxicity. <b><i>Summary:</i></b> There is a critical need to use hydralazine in some patients with resistant hypertension. Available evidence supports a significant link between genotype and NAT2 enzyme activity as 29 studies were identified with an overall concordance between genotype and phenotype of 92%. The literature also supports an association between acetylator status and hydralazine concentration, as fourteen of fifteen identified studies revealed significant relationships with a consistent direction of effect. Although fewer studies are available to directly link acetylator status with hydralazine antihypertensive efficacy, the evidence from this smaller set of studies is significant in 7 of 9 studies identified. Finally, 5 studies were identified which support the association of acetylator status with hydralazine-induced lupus. Clinicians should maintain vigilance when prescribing maximum doses of hydralazine. <b><i>Key Messages:</i></b> NAT2 slow acetylator status predicts increased hydralazine levels, which may lead to increased efficacy and adverse effects. Caution should be exercised in slow acetylators with total daily hydralazine doses of 200 mg or more. Fast acetylators are at risk for inefficacy at lower doses of hydralazine. With appropriate guidance on the usage of <i>NAT2</i> genotype, clinicians can adopt a personalized approach to hydralazine dosing and prescription, enabling more efficient and safe treatment of resistant hypertension.


2017 ◽  
Vol 43 (1) ◽  
pp. 65-72 ◽  
Author(s):  
Sunil M. Patil ◽  
Ramesh S. Vadavi ◽  
Suneel Dodamani ◽  
Umashri Kendur ◽  
Geeta Chimmalagi ◽  
...  

1983 ◽  
Vol 17 (10) ◽  
pp. 726-731 ◽  

Knowledge about drug interactions with plastic materials used in medical and surgical practice is at an elementary stage. Information that has appeared so far on the sorption of drugs to intravenous fluid containers, delivery sets, syringes, or other plastic apparatus has highlighted that polyvinyl chloride (PVC) is the major offender in this respect. Fortunately, in only a few cases is this sorption phenomenon and loss of drug from fluid likely to present a clinical hazard; in most instances, methods are available to prevent or overcome the problem, providing it is recognized. Current information suggests that the following drugs may exhibit clinically significant sorption to plastic materials: insulin, glyceryl trinitrate (nitroglycerin), diazepam, chlormethiazole, vitamin A acetate, isosorbide dinitrate, and a miscellaneous group of drugs including some phenothiazines, warfarin sodium, hydralazine hydrochloride, and thiopentone sodium. In addition, chloroquine binds strongly to glass and to cellulose acetate, but seemingly not to plastics. Brief details of these interactions and their management are given, together with some preliminary information and warnings on drug interactions (e.g., epinephrine, rifampicin) with hydrophilic contact lenses. The latter interactions may cause irreversible coloration of the lenses.


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