Metabolites of Antihypertensive Drugs

Ebihara, Akio; Fujimura, Akio

doi:10.2165/00003088-199121050-00002

Cited by 12 publications

(2 citation statements)

References 93 publications

(44 reference statements)

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“…Amiodarone is examined first as anti-anginal coronary artery vasodilator, this agent comprises of a procainamide-Lidocaine congener part, physiological effect on diethyl amine group. And thyroid function effects on iodine group 23 . Amiodarone inhibits the calcium and sodium channel in SA and AV nodes and purkinje's fibres respectively, it leads to falls of conduction in Phase-0.…”

Section: Therapy Class I (Anti-arrhythmic Agents)mentioning

confidence: 99%

Arrhythmia's: Types, Pathophysiology and Therapy: A Review

Dhinakaran¹,

Tamilanban²,

Chitra³

2019

Int. Res. J. Pharm.

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Arrhythmia is irregular heartbeat, too slow or too fast. Heart function is regulated by electrical impulse which initiate from the sinus node and deputed over heart. Rhythmic change occurs in heart due to abnormal conduction of impulse results in arrhythmia Origin and mechanism of the arrhythmia is different and the electrocardiogram is used to have complete knowledge of arrhythmias, methodology and its construction of electrical impulse. Tele ECG is one among, the recent invention which has reduced the workload of recording heartbeat in the diagnosis of cardiovascular disease. According to the impulse disorder in heart, different arrhythmia were categorised. Mainly two, disorder of impulse occur in atrium is a called atrial arrhythmia and irregular impulse occur in ventricle is a known as ventricular arrhythmia. Anti-arrhythmic agents are classified based on changes in the phases of myocardial cell to treat the various arrhythmia. Herbal medicine has a minimized in side effects.

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Section: Therapy Class I (Anti-arrhythmic Agents)mentioning

confidence: 99%

Arrhythmia's: Types, Pathophysiology and Therapy: A Review

Dhinakaran¹,

Tamilanban²,

Chitra³

2019

Int. Res. J. Pharm.

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“…However, the contribution of the metabolites to the pharmacological effect is low because of their low plasma concentrations at steady state. 4,5 The formation of ␣-hydroxymetoprolol and part of the O-demethylation of metoprolol are dependent on CYP2D6, the isoform responsible for the oxidative polymorphism of debrisoquine and sparteine that divides the Caucasian population into poor metabolizers (approximately 6.3%) and extensive metabolizers. 14,15,22 Metoprolol clearance is approximately 10-fold higher in extensive metabolizers (409 L h −1 ) than in poor metabolizers (49.7 L h −1 ).…”

Section: Introductionmentioning

confidence: 99%

Enantioselectivity in the steady-state pharmacokinetics of metoprolol in hypertensive patients

et al. 1999

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In the present study we investigated the enantioselectivity in the pharmacokinetics of metoprolol administered in a multiple‐dose regimen as the racemate. The study was conducted on 10 patients of both sexes with mild to severe essential hypertension, aged 28 to 76 years, with normal hepatic and renal function and phenotyped as extensive metabolizers of debrisoquine (urine debrisoquine to 4‐hydroxydebrisoquine ratios of 0.28 to 6.56). The patients were treated with racemic metoprolol (two 100 mg tablets every 24 h) for 7 days. Serial blood samples were collected at times zero, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 20, 22, and 24 h and urine at each 6 h period until 24 h after metoprolol administration. The plasma concentrations of the (−)‐(S)‐ and (+)‐(R)‐metoprolol enantiomers were determined by HPLC using a chiral stationary phase (Chiralpak AD, 4.6 × 250 mm) and fluorescence detection. The enantiomeric ratios differing from one were evaluated by the paired t test and the results are reported as means (95% CI). No differences were observed between metoprolol enantiomers in half‐lives and absorption, distribution and elimination rate constants. However, the following differences (p < 0.05) were observed between the (−)‐(S) and (+)‐(R) enantiomers: maximum plasma concentration, Cmax, 179.99 (123.33–236.64) versus 151.30 (95.04–207.57) ng/mL; area under the plasma concentration versus time curve, AUC 0–24SS, 929.85 (458.02–1401.70) versus 782.11 (329.80–1234.40) ng h/mL; apparent total clearance, ClT/f, 1.70 (0.79–2.61) versus 2.21 (1.06–3.36) L/h/kg, apparent distribution volume, Vd/f, 10.51 (6.35–14.68) versus 13.80 (6.93–20.68) L/kg, and renal clearance, ClR, 0.06 (0.05–0.08) versus 0.07 (0.05–0.09) L/kg. The enantiomeric ratios AUC(−)‐(S)/AUC(+)‐(R) ranged from 1.14 to 1.44, with a mean of 1.29. The data obtained demonstrate enantioselectivity in the kinetic disposition of metoprolol, with plasma accumulation of the pharmacologically more active (−)‐(S)‐metoprolol enantiomer in hypertensive patients phenotyped as extensive metabolizers of debrisoquine. Chirality 11:591–597, 1999. © 1999 Wiley‐Liss, Inc.

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Assessment of the Role of ACE Inhibitors in the Elderly

Sica

Clinical Hypertension and Vascular Diseases

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Metabolites of Antihypertensive Drugs

Cited by 12 publications

References 93 publications

Arrhythmia's: Types, Pathophysiology and Therapy: A Review

Arrhythmia's: Types, Pathophysiology and Therapy: A Review

Enantioselectivity in the steady-state pharmacokinetics of metoprolol in hypertensive patients

Assessment of the Role of ACE Inhibitors in the Elderly

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