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Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
Some new drugs were at a relatively early phase tested in animal models. Thus pyri- dazinone derivative C 85-3143 was tested in stenotic and freeze-injured carotids in rats, as well as in stenotic jugular veins of rabbits,731 peptide derivative of factor X in the Wessler- type model of vein thrombosis in rabbits,732 molsidomine and its metabolite SIN-1 in the rat mesenteric microcirculation,733 as well as in silver nitrate-induced venous and arterial thrombosis in rabbits.734 Diferuloyl methan (curcumin), isolated from the indian plant curcuma longa, was effective in a mouse DIC induced by intravenous collagen and epinephrine.41 Born and Kovacs97 successfully tested N-acetyl neuraminic acid in the microcirculation of rats and hamsters injured by laser shots. Herrmann et al.735 observed a marked antithrombotic activity in hamster cheek pouch microthrombosis induced by the fluorescein-isothiocyanate method after the vasodilating agent naftidrofuryl (probably blocking 5-HT2 receptors). Using the Homstra method with the polyethylene loop in the carotid artery Lecker and Kumar736 tested a new pyridazinone derivative. Ott and Smith737 investigated a naphthyridine derivative in rats with a polyethylene tubing inserted into the carotid artery (Chan’s method). The glycosaminoglycan sulodexide was successfully tested in electrically induced carotid artery thrombosis in rats.738
Therapeutic Implications
Published in Thomas F. Lüscher, Paul M. Vanhoutte, The Endothelium: Modulator of Cardiovascular Function, 2020
Thomas F. Lüscher, Paul M. Vanhoutte
The relaxation of nitrovasodilators such as nitroglycerin, sodium nitroprusside, and SIN-1 (the active metabolite of molsidomine) (Figure 16) is associated with increases in the content of cyclic GMP in vascular smooth muscle.96,606,684,1002,1003,1106 The formation of the second messenger usually precedes the relaxation. In a given tissue, the degree of accumulation of the nucleotides correlates with the decreases in tension obtained.638,683,684,1003,1110 In addition, pharmacological inhibition or augmentation of the formation of the cyclic GMP is associated with a reduced or augmented relaxation, respectively.960,1003 The pharmacological activity of the various nitrovasodilators in isolated vascular tissues correlates with the amount of nitric oxide that they release.295,296,919 Hence, nitrates use the same pathway to exert their vascular effects as the EDRF that activates guanylate cyclase513,547,549,550,805,1003 (see Chapter 3).
Advantages and disadvantages in radial and femoral arterial access
Published in Ever D. Grech, Practical Interventional Cardiology, 2017
Rubén Rodríguez, Alessandra Giavarini, Isabelle Vandormael, Giovannni Longo, Carlo Di Mario
The RA is a muscular vessel with high reactivity and propensity for spasms. In addition to unfavourable vascular anatomy, RA spasms have been described as the main cause of procedural failure.19 Vasodilators can be used in this instance. However, the optimal pharmacological agent to minimise the incidence of radial spasms still remains unclear. In the SPASM trial, a combination of 2.5 mg of verapamil and 1 mg of molsidomine was associated with an incidence of radial spasms of 4.9% compared to 13.3% with verapamil only and 22.2% with placebo.20 Shorter and hydrophilic sheaths can also reduce the incidence of radial spasms21 (Figure 24.4 – panel a). It has also been described that RA wall protection from trauma using a long hydrophilic-coated sheath can reduce radial spasms.22
AMI in (bi)ventricular pacing – do not discard the ECG
Published in Acta Clinica Belgica, 2023
T. Versyck, D. Devriese, S. Smith, P. Calle, C. Borin
An 89-year-old man complaining of chest pain was evaluated pre-hospital. He had a history of ischemic heart disease with PCI of the left anterior descending (LAD) coronary artery and atrial fibrillation, for which he took apixaban and bisoprolol. His vital signs were: pulse, 68 bpm; blood pressure, 134/79 mmHg; oxygen saturation, 99%. The patient received aspirin 250 mg IV, ticagrelor 180 mg PO and 5000 IU of heparin IV and was transported to our hospital. His in-hospital ECG showed predominantly right ventricular pacing with a couple of QRS complexes with distressing ST-segment elevation and depression (Figure 2). There was no previous ECG available for comparative analysis. In-hospital the pain almost completely resolved and after consulting with the cardiology department, catheterisation was postponed. The intrinsic QRS complexes with ST segment changes were considered T-wave memory, as the patient’s ECG showed predominantly ventricular pacing. The patient was hospitalised in the coronary care unit with a molsidomine drip. His hs-troponin T level on arrival was 68 ng/l, but a second blood analysis 6 h later showed a rise up to 1463 ng/l (ref: ≤14 ng/l). The patient underwent an urgent coronarography, which showed a new 99% stenosis proximal to his previous LAD stent. He received a drug eluting stent (DES) and was discharged home after 7 days.
Pharmacotherapy for erectile dysfunction in diabetic males
Published in Expert Opinion on Pharmacotherapy, 2018
A recent study evaluated the efficacy of the nitric oxide donor, molsidomine, in a rat model of diabetic ED. Molsidomine significantly and dose-dependently increased sexual behavior, sperm count, and serum T level in diabetic rats. Furthermore, the protective effect of molsidomine was also substantiated by pathological changes in the architect of the penile tissue. Molsidomine showed good membrane stability accounting for its significant anti-inflammatory action. Molsidomine was found to settle well in the active site of the PDE5 enzyme with less binding affinity than the standard drug sildenafil. These results highlighted the rationale behind the repositioning of molsidomine therapy for the management of diabetic ED [71].
What are the considerations for anti-hypertensive treatment in patients with Parkinson’s disease?
Published in Expert Opinion on Pharmacotherapy, 2020
In the treatment of AH in PD antihypertensives containing moxonidine, alpha-methyldopa or reserpine [2,18,23] are contraindicated. Verapamil, diltiazem, amlodipine and nifedipine should not be combined with levodopa. Amlodipine was reported to induce Parkinson symptoms [24], not confirmed in several studies [25,26]. On the other hand some molecules used as antihypertensives are discussed as disease-modifying drugs [25,26] Negative influence on the PD results from preparations containing reserpine [2,18]. Combinations of guanethidine with dopaminergic agents often results in arrhythmias [18]. The effect of molsidomine is reinforced in combination with levodopa [18,23].