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Coronary Artery Disease
Published in Jahangir Moini, Matthew Adams, Anthony LoGalbo, Complications of Diabetes Mellitus, 2022
Jahangir Moini, Matthew Adams, Anthony LoGalbo
Calcium channel blockers are used for persistent symptoms after nitrates are used, or if they cannot be tolerated. These blockers are best used if there is concurrent coronary spasm or hypertension. The dihydropyridines, including amlodipine, felodipine, and nifedipine do not have chronotropic effects, but have widely different negative inotropic effects. The shorter-acting dihydropyridines can cause reflex tachycardia. They are linked to more deaths of patients with CAD, and are not used alone to treat stable angina.
General Medical Emergencies
Published in Anthony FT Brown, Michael D Cadogan, Emergency Medicine, 2020
Anthony FT Brown, Michael D Cadogan
Get senior ED doctor help and take expert advice. Aim to reduce mean arterial pressure (MAP) initially by no more than 25%, or aim for a diastolic BP of 100–110 mmHg within the first 24 h.Use oral treatment with labetalol 100 mg, atenolol 100 mg, or amlodipine 5–10 mg or felodipine sustained-release 5–10 mg.Avoid more potent i.v. agents such as sodium nitroprusside 0.25–10 μg/kg per min i.v., unless intra-arterial blood pressure monitoring is in place. ICU admission is indicated.
Cardiovascular Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown the risk of teratogenicity associated with the use of Felodipine.
Smoking and overweight associated with masked uncontrolled hypertension: a Hypertension Optimal Treatment (HOT) Sub-Study
Published in Blood Pressure, 2021
Magnus Holanger, Sverre E. Kjeldsen, Kenneth Jamerson, Stevo Julius
The ethics committees in all participating countries approved the study. Patients gave informed consent. Blood pressure was measured at enrolment and then at two qualifying visits at least 7 days apart. The diastolic BP had to be in the range of ≥100 to ≤115 mm Hg at both qualifying visits. The number of exclusion criteria were specified [1]. All patients started active antihypertensive treatment with the calcium antagonist felodipine 5 mg once daily. Additional antihypertensive therapy was given with either an angiotensin-converting enzyme inhibitor or a β-adrenoceptor blocker if the target BP was not reached. Dosage adjustments were, if needed, made in accordance with a set protocol. As a final step, a diuretic was added if it was needed. After 6 months [3], the percentages of patients who had achieved their randomised target clinic diastolic BP were 57, 71 and 83% for the target groups at ≤80, ≤85, or ≤90 mmHg, respectively, and after 12 months they were 57, 72 and 84%, respectively. The distributions of the drug dose steps in the three target groups were rather similar.
Physicochemical, pharmacokinetic, and pharmacodynamic characterization of isradipine tablets for controlled release
Published in Pharmaceutical Development and Technology, 2021
D. Nagasamy Venkatesh, S. N. Meyyanathan, R. Shanmugam, S. S. Kamatham, J. R. Campos, J. Dias-Ferreira, E. Sanchez-Lopez, J. C. Cardoso, P. Severino, E. B. Souto
For the assay of drug recovery (DR), five tablets (10% of each batch) produced from different formulations were weighted individually and then placed in a mortar for powdering with a pestle. The validation was carried out following the ICH guidelines and the European Pharmacopoeia. An amount equivalent to 0.7 mg of isradipine was extracted with 100.0 mL of phosphate buffer (pH = 6.8) and sonicated for 15 min. The solution was filtered through a 0.22 µm pore size filter paper (Whatman, Pittsburgh, PA), diluted with the same PBS buffer and the drug content measured at 325 nm using the HPLC (Waters Ltd, Mumbai, India). A column C18 (250.0 mm × 4.6 mm, i.d. 5 µm) was used with a flow rate of 1.0 mL/min and detection wavelength set at 210 nm. The mobile phase consisted of a mixture of acetonitrile:methanol:water (37.5:37.5:25 (v/v)). Felodipine was used as the internal standard. The retention times of isradipine and felodipine were 4.1 min and 6.5 min, respectively. The linearity for isradipine was found between 5.0 μg/mL and 100 μg/mL and the percentage of DR was determined using the following equation:
The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system
Published in Pharmaceutical Development and Technology, 2020
Hongwei Zhang, Xu Liu, Xiangyu Ma
The HPLC method was set up as follows with modification (Migliorança et al. 2005). The isocratic mode was used with the mobile phase of 0.1% PA solution: Acetonitrile (ACN) as 20%: 80% at a flow rate of 1.0 mL/min. A Luna C18 column (250 mm × 4.60 mm, 5 μm) was used with temperature controlled at 25 °C, and the wavelength of the UV detector was 238 nm. The standard solution of felodipine was accurately prepared at the concentration of 200.0 μg/mL, which was termed as standard 100%. Calibration curves were established over the range of 2.0–200.0 μg/mL, with a regression coefficient greater than 0.9999. The nominal retention time of felodipine was around 5.8 min. The limit of detection (LOD, signal/noise ≥ 3) and limit of quantification (LOQ, signal/noise ≥ 10) were determined as 0.2 μg/mL and 0.5 μg/mL, respectively. The method was validated on precision and recovery. The RSD of intra-day precision (n = 6) based on six replicated injections using 100% and 10% standards solution were 0.04% and 0.13%, respectively. The mean recovery ± RSD (n = 9) of felodipine was 100.0% ± 0.1%. All measurements of samples were carried out in triplicate.