Calcium channel blockers modulate airway constriction in the canine lung periphery

1991 ◽  
Vol 70 (2) ◽  
pp. 624-630 ◽  
Author(s):  
K. S. Lindeman ◽  
C. A. Hirshman ◽  
A. N. Freed

We studied the effect of two voltage-sensitive calcium channel blockers on Na2EDTA-induced bronchoconstriction in the canine lung periphery. A wedged bronchoscope technique was used to measure collateral system resistance before and after challenges with aerosolized Na2EDTA, hypocapnia, aerosolized acetylcholine, and increased flow of dry air in anesthetized mongrel dogs. Nifedipine, a dihydropyridine calcium channel blocker, reduced hypocapnia-induced bronchoconstriction by 88 +/- 6% (SE) but did not alter Na2EDTA-induced constriction. Verapamil, a phenylalkylamine calcium channel blocker, attenuated hypocapnia- and Na2EDTA-induced bronchoconstriction by 69 +/- 6 and 44 +/- 7%, respectively, but did not significantly alter responses to either acetylcholine or dry air challenge. We conclude that calcium influx through voltage-sensitive calcium channels, perhaps of the T subtype, has a limited role in the initiation of Na2EDTA-induced bronchoconstriction in the canine lung periphery.

2018 ◽  
Vol 23 (5) ◽  
pp. 433-445 ◽  
Author(s):  
Sandip Chaugai ◽  
Lhamo Yangchen Sherpa ◽  
Amir Ali Sepehry ◽  
Scott Reza Jafarian Kerman ◽  
Hisatomi Arima

Background: Dihydropyridine calcium channel blockers are a heterogeneous group of antihypertensive drugs. Long-acting dihydropyridine agent amlodipine is widely used for monotherapy and combination therapy for hypertension in clinical practice, while intermediate-acting dihydropyridine agents have shown inconsistent results in randomized clinical trials (RCTs). Methods and Results: A meta-analysis of 18 RCTs enrolling a total of 80,483 patients with hypertension followed for a mean of 51.4 months was performed. Amlodipine therapy was associated with 25% higher risk of heart failure (relative risk [RR]: 1.25, 95% confidence interval [CI], 1.05-1.49, P = .019) but 17% lower risk of stroke (RR: 0.83, [95% CI, 0.72-0.97], P = .009) without statistically significant effect on acute myocardial infarction (AMI) compared to major alternative antihypertensive therapy (MAAT), including β-blocker, diuretic, angiotensin-converting enzyme inhibitor, or angiotensin-receptor blocker. Intermediate-acting dihydropyridine calcium channel blocker therapy was associated with 25% higher risk of heart failure (RR: 1.25, [95% CI, 1.06-1.47], 0.005, P = .005) and 26% higher risk of AMI (RR: 1.26, [95% CI, 1.05-1.51], 0.019, P = .019) compared to MAAT. Results of the subgroup analysis suggested that the intermediate-acting dihydropyridine calcium channel blocker was associated with higher risk of heart failure (RR: 1.30, [95% CI, 1.08-1.56], P = .005) and AMI (RR: 1.50, [95% CI, 1.01-2.22], P = .043) compared to renin–angiotensin system blockers and a trend toward higher risk of AMI (RR: 1.17, [95% CI, 0.99-1.38], P = .064) compared to conventional therapy, including β-blockers and diuretics. Meta-regression analyses suggested that long-acting dihydropyridine calcium channel blocker is associated with lower risk of AMI ( B: −0.327, [95% CI, −0.530 to −0.123], P = .002) with a trend toward lower risk of stroke ( B: −0.203, [95% CI, −0.410 to 0.003] P = .054). Conclusions: This study suggests that Amlodipine offers greater protection against major complications of hypertension compared to intermediate-acting dihydropyridine calcium channel blockers.


2020 ◽  
Vol 4 (2) ◽  
pp. 1
Author(s):  
Gunawan Gunawan ◽  
Suhardjo Sitam ◽  
Lusi Epsilawati

Objectives: The purpose of this research was to describe radiographic density of mandibular bone in calcium channel blocker anti-hypertensive drug users. Bone density in the mandible is assessed from the trabecular. Panoramic radiograph is a routine examination that is often done in dentistry that can be used to assess changes in quality in the form of changes in bone density in users of anti-hypertensive calcium channel blockers Material and Methods: This research is a descriptive study of 21 panoramic radiographs of calcium channel blocker anti-hypertensive drug users aged 40-75 years. Panoramic radiograph archive density checks in the distal region of the foramen mentale and the mandibular angular region using software image j, with the final result was the percentage between bone and marrow. Results: This research showed the average radiographic density in male using calcium channel blocker antihypertensive drugs was 18.81% and the average radiographic density in female was 20.92%. Conclusion: Based on the results of the study found that the average radiographic density of female patients taking antihypertensive drugs calcium channel blockers was higher than male.


2021 ◽  
Vol 14 (1) ◽  
pp. e238872 ◽  
Author(s):  
Satoru Morikawa ◽  
Mana Nasu ◽  
Yoko Miyashita ◽  
Taneaki Nakagawa

Gingival overgrowth is a common side effect of calcium channel blockers used in the treatment of cardiovascular diseases. While controversial, management includes discontinuing the calcium channel blocker. We report the case of a 66-year-old Japanese man with hypertension and type 2 diabetes mellitus who was diagnosed with severe periodontitis covering almost all the teeth. The patient had been on nifedipine (40 mg/day) and amlodipine (10 mg/day) medication for 5 years. With his physician’s consent, nifedipine was discontinued during his treatment for periodontitis, which consisted of oral hygiene instructions and scaling and root planing on all areas. Gingivectomy was performed on the areas of hard fibrous swelling. Nifedipine was resumed during periodontal treatment when the patient’s hypertension worsened. His periodontal scores improved when he resumed treatment. We report that significant improvement in gingival overgrowth can occur with basic periodontal treatment, surgery and sustained intensive follow-up without adjusting calcium channel blockers.


1996 ◽  
Vol 270 (1) ◽  
pp. E96-E100 ◽  
Author(s):  
S. R. Kelley ◽  
T. J. Kamal ◽  
M. E. Molitch

Verapamil, a phenylalkylamine calcium channel blocker, causes a doubling of serum prolactin (PRL) levels in humans. To determine whether the mechanism involved a decrease in the PRL response to dopamine (DA), we infused low doses of DA, finding that the percent inhibition of PRL was not affected by verapamil (max %decrements for 0.003, 0.01, and 0.03 microgram.kg-1.min-1 doses of DA, respectively, 86.7 +/- 19.1, 73.2 +/- 24.8, and 65.2 +/- 20.0% without verapamil and 93.4 +/- 24.6, 79.7 +/- 14.9, and 58.0 +/- 18.1% with verapamil). To determine whether the PRL elevation was due to a decrease in hypothalamic generation of DA, we measured the inhibition of PRL by L-dopa before and after inhibition of peripheral decarboxylase activity with carbidopa. Without verapamil, L-dopa alone and carbidopa-L-dopa caused similar maximum decreases in PRL levels of 83.2 +/- 2.5 and 80.3 +/- 2.0%, respectively. With verapamil, the PRL maximum decrement with L-dopa was 85.2 +/- 2.7% and with carbidopa-L-dopa was 76.3 +/- 1.9% (P < 0.01). We also found that dihydropyridine and benzothiazepine calcium channel blockers had no effect on PRL. These results suggest that verapamil acts by decreasing central DA generation, possibly through N-type calcium channels.


DICP ◽  
1989 ◽  
Vol 23 (11) ◽  
pp. 855-858 ◽  
Author(s):  
Mark A. Malesker ◽  
Karen S. Rovang ◽  
Syed M. Mohiuddin ◽  
Aryan N. Mooss ◽  
Daniel E. Hilleman ◽  
...  

The effectiveness of nifedipine for the treatment of acute hypertensive episodes in patients already taking chronic calcium-channel blocker therapy is unknown. We report our experience with 43 consecutive patients who received nifedipine for acute hypertensive episodes in the coronary care unit. Of the 43 patients (24 men, 19 women), 23 (53 percent) were taking chronic (>2 mo) calcium-channel blocker therapy. Nifedipine 10 mg capsules were chewed and swallowed with repeat doses given at hourly intervals if necessary. Target BP was 140/90 mm Hg, which was achieved in 31 of 43 patients (72 percent). In patients already taking calcium-channel blockers, target BP was achieved in 18 of 23 patients (78 percent). Response in patients not taking chronic calcium-channel blockers was observed in 13 of 20 patients (65 percent). Overall, adverse effects occurred in 16 of 43 patients (37 percent): 11 of 23 patients (48 percent) taking calcium-channel blockers, and 5 of 20 patients (25 percent) not taking calcium-channel blockers. Nifedipine is equally effective in lowering BP in patients taking calcium-channel blockers as it is in patients not taking them. Although associated with a higher incidence of adverse effects in patients already taking calcium-channel blockers, these effects were not considered serious. Nifedipine is an effective agent in acute hypertensive episodes, even in patients receiving chronic calcium-channel blocker therapy.


2018 ◽  
Vol 28 (12) ◽  
pp. 1468-1470
Author(s):  
Ramzi Hamzeh ◽  
Ziad Bulbul ◽  
Jana Assy

AbstractIn diffuse forms of arteriovenous malformation following Fontan procedure, “classical” medical therapy, inhaled nitric oxide and sildenafil, may play a role, until re-direction of hepatic flow to pulmonary circulation cures it. However, in refractory cases, as reported in our 2-year-old patient, unusual medications such as calcium channel blockers can be tried and continued if patients respond adequately.


1989 ◽  
Vol 66 (6) ◽  
pp. 2527-2532 ◽  
Author(s):  
K. S. Lindeman ◽  
C. A. Hirshman ◽  
A. N. Freed

Magnesium sulfate has been shown to be effective clinically as a bronchodilator, but its mechanism of action is unknown. We used a wedged bronchoscope technique to study the ability of MgSO4 at clinically relevant concentrations to attenuate hypocapnia-, acetylcholine- (ACh), and dry air-induced bronchoconstriction in the canine lung periphery. Control experiments demonstrated that consecutive challenges of either hypocapnia or ACh resulted in greater collateral system resistance (Rcs) after the second challenge compared with the first. Intravenous infusion of MgSO4 diminished the maximum response to a second hypocapnic challenge (Rcs = 1.59 +/- 0.29 cmH2O.ml-1.s prechallenge vs. 1.12 +/- 0.20 postchallenge) but had no effect on either ACh- or dry air-induced bronchoconstriction. Serum magnesium levels before MgSO4 administration were 1.59 +/- 0.04 meq/l and rose to 6.20 +/- 0.13 during the infusion. Previous studies demonstrated that nifedipine, like MgSO4 in this study, attenuates hypocapnia-induced bronchoconstriction in the canine lung periphery but has no effect on ACh- or dry air-induced bronchoconstriction. We conclude that these results are consistent with the idea that, like nifedipine, magnesium acts in the airway as a voltage-sensitive calcium channel blocker.


2005 ◽  
Vol 18 (3) ◽  
pp. 169-174 ◽  
Author(s):  
Matthew Hedge

Calcium channel blockers are commonly prescribed antihypertensive medications in the United States and as such are a common presenting ingestion. The pharmacology and mechanism of action of this class of drugs will be discussed. The clinical presentation and therapeutic options will be reviewed.


2020 ◽  
Vol 7 (1) ◽  
pp. 1-13
Author(s):  
Kulvinder Kochar Kaur ◽  
◽  
Gautam Allahbadia ◽  
Mandeep Singh ◽  
◽  
...  

Aim Obesity is increasing globally by leaps and bounds and thus the incidence of type 2 diabetes mellitus (T2DM) along with it so much so that the term diabesity had to be coined. Earlier we had reviewed how to treat the both together and the role of empagliflozin to improve cardiovascular outcome trials (CVOT). Similarly T2DM and hypertension are pathophysiologically-related diseases which co-exist with a broader complex of metabolic diseases which co-exist possessing similar set of risk factors. Hence it is important to consider which antihypertensives are suitable that possess a positive effect on metabolic factors in cases of T2DM who require an antihypertensive. Method A systematic review was carried out using the PubMed search engine with the MeSH terms: “T2DM”; “essential hypertension; “cardiovascular (CV)”; “Complications of diabetes mellitus (DM) and antihypertensive”; “Antihypertensive preferred in T2DM subjects”; “Renin-angiotensin–aldosterone system inhibitors”; “Angiotensin converting enzyme inhibitors (ACEi)”; “Angiotensin receptor blockers (ARBs)”; “Dihydropyridine calcium channel blocker”; “β2 blockers”; “Diuretics”. Discussion Most diabetes mellitus (DM) subjects need a minimum of two antihypertensive drugs, combining a renin-angiotensinaldosterone system (RAS) inhibitor with a dihydropyridine calcium channel blocker seems to be the most indicated approach. But not all dihydropyridine calcium channel blockers have equivalent effects on metabolic parameters. Hence manidipine that causes positive effect on insulin resistance (IR) seems to be an effective option. We have reviewed how manidipine is superior to amlodipine with regards to improving IR, not seen with amlodipine, along with not causing excessive sympathetic nervous system (SNS) activation, pulse pressure and ankle edema or to much lesser extent than amlodipine. Therefore, manidipine needs to be the first addition to RAS inhibitors in case of DM’s having hypertension of the dihydropyridines calcium channel blockers. Further good blood pressure (BP) control been correlated with good CVs outcomes. Conclusion A RAS inhibitor is the first line of choice of drugs in a subject with T2DM who needs to be treated with empagliflozin for better CVOT outcome, and when a 2nd drug has to be added it is manidipine that is preferred over amlodipine. Plant products are proving to be having a lot of beneficial effects in DM, obesity and hypertension. Thus need for developing agents from plants will prove to be more cost effective in these chronic diseases where compliance is difficult to achieve with the use of common antiDM drugs and antihypertensives with the cost factor along with their side effects.


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