Drug therapy in the cardiac catheterisation laboratory: A guide to commonly used drugs
John Edward Boland, David W. M. Muller in Interventional Cardiology and Cardiac Catheterisation, 2019
Calcium channel blockers: Calcium channel blockers have been in use for treating hypertension for several decades. These drugs work by blocking the effects of calcium in initiating myocardial activation and reducing vascular tone. Verapamil is a calcium channel blocker that reduces heart rate by slowing atrio-ventricular node conduction and reduces blood pressure by arterial dilatation. It is thus used for hypertension and to treat fast rhythms such as supraventricular tachycardia or atrial fibrillation, or to relieve spasm of the brachial or radial artery (nitrates are not as effective at dilating peripheral arteries). It is also used as an infusion in combination with heparin and nitrates to prevent spasm during coronary rotational atherectomy.
Primary Headache Disorders
Mark V. Boswell, B. Eliot Cole in Weiner's Pain Management, 2005
Calcium channel blocking drugs have been helpful to many patients, especially those with the chronic form of cluster. It is believed that they alter smooth muscle tone of cerebral arteries by interfering with calcium ion function (Gallagher & Freitag, 1987a). Verapamil generally is well tolerated and more frequently used. It has been suggested as a first-line pharmacologic treatment for the prevention of cluster headache, although weeks of therapy may be required before control of the condition is established (Saper, 2000). It is given in divided doses with an average daily dosage of 360 to 480 mg per day. The most frequent side effects with verapamil are constipation and fluid retention. Verapamil is contraindicated in hypotension, cardiac conduction disease, and significant renal or hepatic disease. Other calcium channel blockers sometimes used are nifedipine (40 to 280 mg per day) and nimodipine (30 to 60 mg per day).
Cluster Headache
Gary W. Jay in Clinician’s Guide to Chronic Headache and Facial Pain, 2016
The advent of the calcium channel blockers in the early 80s found them to be effective in migraine and cluster headache. As is the case with lithium, the mechanism of action of the calcium channel blockers is unknown. Possible mechanisms include the direct effect on calcium channels in vascular smooth muscle as well-mediating effects on serotonin. A variety of calcium channel blockers have been shown to be effective in management (71). Verapamil (72,73) has remained the one most consistently used. Onset of activity occurs in less than a week in patients at dose of 240 mg/day. Some patients, especially those with chronic cluster headache where up to 720 mg/day has been used, may require higher doses. Perform vital sign monitoring along with monitoring of the electrocardiogram if doses of greater than 360 mg day are prescribed. Hypotension, bradycardia, and development of heart block may occur at higher doses. Calcium channel blockers may interact with beta-blockers to produce cardiovascular complications. Verapamil also interacts with digitalis, albeit a rare concern in the typical cluster headaches patient. More important may be the interactions with lithium, which can be both advantageous and problematic. A controlled trial (74) demonstrated that verapamil was as effective as lithium but had better tolerability and quicker onset of action. The only common side effect seen with verapamil at normal therapeutic doses is constipation.
Peyronie’s disease – outcomes of collagenase clostridium histolyticum injection: A systematic review
Published in Arab Journal of Urology, 2021
Austin T. Mefford, Omer Raheem, Faysal A. Yafi, Laith M. Alzweri
Verapamil is an L-type calcium channel blocker used in the treatment of hypertension, angina, and heart failure. IL verapamil injection was brought into the spotlight after Levine et al. [21] demonstrated verapamil injection could decrease ‘plaque-associated penile narrowing’ and penile curvature. In a subsequent, and more reputable study, he showed verapamil injection reduced pain in 97% of patients, improved sexual function in 72%, and lessened the degree of curvature and deformity in 54% and 86%, respectively [22]. But other studies have shown IL verapamil to improve sexual function while not having much effect on the size of fibrous plaque [23]. It is for these mixed results and a lack of large-scale placebo-controlled studies that the United States Food and Drug Administration (FDA) has not formally approved verapamil for the treatment of PD.
Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism
Published in Pharmaceutical Biology, 2021
Haihua Shang, Ze Wang, Hong Ma, Yinghui Sun, Xiaoyan Ci, Yuan Gu, Changxiao Liu, Duanyun Si
Rotundic acid, a plant-derived pentacyclic triterpene, is widely present in medicinal and edible plants (Saimaru et al. 2007; Yang, Li, Ruan, Tong, et al. 2018). RA has been reported to possess anti-inflammatory and cardio-protective abilities. However, due to its poor bioavailability just like PTAs, the further development and potential therapeutic application of RA was limited. To our best knowledge, the reasons for the low bioavailability of PTAs are mainly due to the P-gp mediated drug effluxes and/or CYP3A4 mediated metabolisms (Zhao et al. 2012; Yang et al. 2017). We speculated that the poor bioavailability of RA is related to the same reason. Verapamil, commonly used to treat high blood pressure, could improve their absorption of the drugs with poor bioavailability, via inhibiting the activity of CYP3A4 and P-gp (Zhu et al. 2017; Zhou et al. 2019; Xing et al. 2020). Whether verapamil has the same effect on RA is still unclear. Therefore, the effect of verapamil on the pharmacokinetics of RA in rats was investigated and the main mechanism was clarified. Furthermore, we investigated the transporter-enzyme interaction of RA in vivo that could contribute to its low oral bioavailability.
Comparative pharmacokinetics of verapamil and norverapamil in normal and ulcerative colitis rats after oral administration of low and high dose verapamil by UPLC-MS/MS
Published in Xenobiotica, 2020
Hongping Yao, Changhe Wang, Wen Lu, Wen Li, Wanghui Jing, Jiye Zhang, Guangde Yang, Aiguo Zeng
Verapamil [2,8-bis-(3,4-dimethoxyphenyl)-6-methyl-2-isopropyl-6-azaoctanitrile] is a calcium channel blocker used widely in the treatment of hypertension, coronary heart disease and cardiac arrhythmias. Verapamil is rapidly absorbed following oral administration, and subject to extensive metabolism mediated by cytochrome P450 enzymes, with less than 5% of a dose being excreted unchanged in urine (Mikus et al., 1990; Schomerus et al., 1976). Its major route of metabolism is N-demethylation leading to the formation of norverapamil [2,8-bis-(3,4-dimethoxyphenyl)-2-isopropyl-6-azaoctanitrile] (Eichelbaum et al., 1979; Hanada et al., 2008). Verapamil and norverapamil are known substrates of P-gp (Pauli-Magnus et al., 2000), which should exhibit better absorption for UC patients and animals as a result of down-regulation of P-gp and disruption of intestinal tight junction barrier. But, it is contradictory that modulation of P-gp has no significant effect on its absorption due to its high permeability (Varma & Panchagnula, 2005). In this work, the pharmacokinetics of verapamil and norverapamil in normal and UC rats after oral administration of low and high dose verapamil were determined to clarify alteration of absorption in UC rats.
Related Knowledge Centers
- Angina
- Calcium Channel Blocker
- Cluster Headache
- Constipation
- Hypotension
- Supraventricular Tachycardia
- Nausea
- Hypertension
- Migraine
- Intravenous Therapy