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Cardiovascular Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Nifedipine has been used as an antihypertensive medication and has been given as an ‘off-label’ tocolytic agent. Nifedipine was teratogenic in rats given 30 times the usual human dose (data from the manufacturer’s insert). There are no studies of nifedipine use during the first trimester of pregnancy. No adverse maternal or fetal effects were reported for the use of nifedipine to treat pre-eclampsia or hypertension, respectively (Sibai et al., 1992). The frequency of congenital anomalies was not increased among 64 infants born to women treated with nifedipine (or a related calcium channel blocker) (Magee et al., 1996). It is regarded as the “second-line” antihypertensive therapy in pregnant women. Of 102 infants born to women who took nifedipine during the first trimester of pregnancy, the frequency of congenital anomalies was not increased in the Swedish Birth Defects Registry (Kallen, 2019). Nifedipine use during pregnancy is probably safe with “little teratogenic or fetotoxic potential” (Childress and Katz, 1994).
Sparking and Sustaining the Essential Functions of Research
Published in Thomas S. Inui, Richard M. Frankel, Enhancing the Professional Culture of Academic Health Science Centers, 2022
Eric B. Larson, Christine Tachibana, Edward H. Wagner
A 1995 population-based, case-control study and resulting intervention at Group Health illustrates the translational efficiency that is possible in a learning health system in collaboration with an academic health science center. Bruce Psaty and UW colleagues found that use of short-acting calcium channel blockers such as nifedipine in hypertensive patients is associated with an increased risk of heart attack.27 This led to a 1996 US FDA recommendation to discourage use of nifedipine for treating high blood pressure. A few months later, Group Health began providing physicians with a summary of evidence about nifedipine, current guidelines about hypertension medication, and patient letters to distribute, advising either a new medication or a physician visit. In a follow-up study of the intervention, Psaty and colleagues found that almost 80% of patients taking short-acting nifedipine had discontinued use within 6 months.28 Within a year of publication, evidence from a Group Health-UW study influenced national recommendations and led to safer drug use in its member population.
Hypertensive Disorders
Published in Vincenzo Berghella, Maternal-Fetal Evidence Based Guidelines, 2022
Most antihypertensive drugs are effective at reducing blood pressure, with little evidence that one is any better or worse than another [2, 30, 99]. Types of medications for acute management of hypertension include the following (Table 1.4).Labetalol: 20 mg IV bolus, then 40, 80, 80 mg as needed, every 10 minutes (maximum 220 mg total dose).Hydralazine: 5 to 10 mg IV (or IM) every 20 minutes. Change to another drug if no success by 30 mg (maximum dose). Hydralazine may be associated with more maternal side effects and NRFHT than IV labetalol or oral nifedipine [100].Nifedipine: 10 to 20 mg orally, may repeat in 30 minutes. This drug is associated with diuresis when used postpartum. Nifedipine and magnesium sulfate can probably be used simultaneously.Sodium nitroprusside (rarely needed): Start at 0.25 μ/kg/min to a maximum of 5 μ/kg/min.
Cationic nanocapsule suspension as an alternative to the sublingual delivery of nifedipine
Published in Pharmaceutical Development and Technology, 2023
Bárbara Felin Osmari, Giovana Aime Medeiros, Jéssica Brandão Reolon, Vinícius Costa Prado, Natália Brucker, Letícia Cruz
Nifedipine (NIFE) is classified as a calcium-channel blocker and is frequently used in clinical practice to treat cardiovascular diseases, angina, and hypertension (Odani et al. 2019; Yao et al. 2020). The drug is available commercially in capsules and tablets for oral administration. However, its high lipophilicity and first-pass metabolism in the liver cause limited oral bioavailability at approximately 45%. Furthermore, NIFE presents a short biological half-life, resulting in frequent daily administrations. Another NIFE limitation is its sensitivity to light, leading to drug degradation as well as treatment ineffectiveness (Granada et al. 2013; Filgueira et al. 2017). Several studies have reported on the development of different formulations for oral and transdermal NIFE administration, aiming to improve its bioavailability (Yasam et al. 2016; Bi et al. 2020). An efficient strategy to increase the bioavailability of drugs is the administration via the sublingual route.
Alternatives to titanium dioxide in tablet coating
Published in Pharmaceutical Development and Technology, 2021
Juliana Radtke, Raphael Wiedey, Peter Kleinebudde
The coated and non-coated nifedipine tablets were weighed after removal from the light cabinet and each was dissolved in 20 ml methanol and diluted with the mobile phase to 50.0 ml. The mobile phase consisted of nine parts acetonitrile, 36 parts methanol, and 55 parts distilled water. To ensure a complete dissolution of the API, the samples were treated in an ultrasonic bath for 20 min and shaken regularly. The samples were handled under exclusion of light and the dissolved sample was transferred into light-protected amber glass vials. Three tablets per coating preparation were examined, whereby the content was determined three times by HPLC. The analysis was carried out according to Ph. Eur. 2.2.29 (European Pharmacopoeia 9.0 2017), which describes the test for related substances of nifedipine. The HPLC (VWR Hitachi HPLC, VWR International GmbH, Darmstadt, Germany) was equipped with a LiChrospher® RP-18 5 µm column (Merck KGaA, Gernsheim, Germany). Nifedipine was identified by the retention time given by the Pharm. Eur. and by comparison with chromatograms of pure nifedipine. The impurities were identified by relative retention times from literature: 0.72 for the nitrophenylpyridine analog and 0.86 for the nitrosophenylpyridine analog (Florey 1990). In absence of pure degradation products for reference, impurities A and B were quantified by comparing the peak areas of the nifedipine peaks and the peak areas of the degradation products. The absolute values for concentration might therefore by to a certain extent flawed, relative comparisons are valid.
Co-amorphous systems for the delivery of poorly water-soluble drugs: recent advances and an update
Published in Expert Opinion on Drug Delivery, 2020
Jiawei Han, Yuanfeng Wei, Yan Lu, Runze Wang, Jianjun Zhang, Yuan Gao, Shuai Qian
For drug-drug CAMs, a drug could be designed by co-amorphization with another drug (with same or different pharmacological effects) for combination therapy. At the same time, the drug-drug CAMs could also exhibit significantly improved in vitro solubility/dissolution behaviors for each drug. For instance, indomethacin with low solubility is a nonsteroidal anti-inflammatory drug. Löbmann et al. selected another nonsteroidal anti-inflammatory drug naproxen as the co-former to develop indomethacin-naproxen CAM in order to obtain pharmacological complementarity in pain relief [84]. The CAM exhibited a synchronized release with 7.6-fold and 1.4-fold increase in IDR for indomethacin and naproxen, respectively. Simvastatin, as a cholesterol-lowering agent belonging to statins, is widely used to treat hypercholesterolemia [105]. Nifedipine acts as a calcium channel antagonist to treat high blood pressure [106]. Cecilia et al. developed these two BCS II drugs into simvastatin-nifedipine CAM as a promising formulation with enhanced solubility for simultaneously targeting hypertension and hypercholesterolemia [91]. The CAM showed 3.7 and 1.7 times increase in solubility for simvastatin and nifedipine, respectively. In addition, it exhibited excellent stability for at least 1 year.