Lege Artis Medicinae

[On rivaroxaban’s mechanism of effect]

BODA Zoltán

DECEMBER 20, 2010

Lege Artis Medicinae - 2010;20(12)

[A new era of anticoagulant therapy is approaching. No new oral anticoagulants have been introduced for seventy years. However, two large groups of anticoagulants (molecules with anti-FXa and anti-FIIa acitivity) are currently at advanced stages of clinical trials. This publication summarises the most important information on the mechanism of effect of the anti-FXa drug rivaroxaban. The possible advantages of the “direct” effect and the anti-FXa effect are emphasized. The most significant drug interactions of the new anticoagulant are also presented.]

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[Lecturis Salutem! Greetings to the Reader!]

KAPÓCS Gábor

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[Members of the editorial and advisory board and the redaction of the LAM, 1990-2010]

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[Farewell to rosiglitazone: where to go?]

TAMÁS GYULA, KERÉNYI ZSUZSA

[The European Medicines Agency concluded that the marketing authorisation for all rosiglitazonecontaining medicines (Avandia, Avandamet, Avaglim) should be suspended across the European Union. The National Health Insurance Fund Administration in Hungary in a circular letter called the attention of GP’s to the necessity in getting the medical proposal (of an internist, endocrinologist or diabetologist) for substituting rosiglitazone to arrange a smooth modification of their treatment regimen. The review taking into account updated recommendations of the ADA-EASD and the Hungarian Diabetes Association summarises the potential drugs. The first line therapy of choice has to be starting with insulin. Pioglitazone might also be administered, with all known side effects of the glitazone family, e.g. congestive heart failure and bone fractures. Further alternatives are choosing the newer drugs of the incretin principle: the incretin mimetics (exenatid, liraglutid) and the incretin enhancers (sitagliptin, vildagliptin, saxagliptin). Beside their favourable profile of effect they do not have longterm follow up outcome studies and evidences for cardiovascular safety.]

Lege Artis Medicinae

[Pancreatology in practice: acute pancreatitis]

TAKÁCS Tamás

[Acute pancreatitis requires various diagnostic and treatment procedures. The clinical picture of acute pancreatitis is diverse, ranging from mild abdominal pain or dyspepsia to severe, lifethreatening multiorgan failure or sepsis. Most cases of pancreatitis result in a mild/edematous inflammation of the pancreas, whereas the remaining 15-20 percent results in severe necrotising pancreatitis with a mortality rate as high as 10-30 percent, although imaging diagnostics, operative endoscopy and intensive internal and surgical therapy have improved significantly in the past few years. Quick and accurate diagnosis of the disease is required for early therapeutic intervention. For example, we know that in cases of biliary acute pancreatitis an early (within 24-48 hours following the onset of symptoms) endoscopic sphincterotomy and stone extraction significantly improve the prognosis of the disaese. It is also important to introduce an adequate perfusion/rehydration therapy and a simultaneous enteral feeding introduced as soon as possible to avoid the superinfection of the pancreatic necrosis. Therefore, when reviewing the epidemiological characteristics, pathophysiology, up-to-date diagnostic and therapeutic approaches of the disease, we emphasise early interventions. We also highlight the importance of patient care and follow-up checks after an incident of acute pancreatitis.]

Lege Artis Medicinae

[The up-to-date approach of Parkinson’s disease]

HIDASI Eszter

[Parkinson’s disease is the second most frequent neurodegenerative disease. Its aetiology has not been clarified yet, but genetical as well as environmental factors might have a significant role in its development. The differentiation between Parkinsonian syndromes and Parkinson’s disease (idiopathic Parkinsonian syndrome) could be very difficult even today. The accuracy of the diagnosis is no more than 90% despite the expertise of the best-trained neurologists and the use of the most sophisticated diagnostic procedures. A 100% of confidence can be achieved only by neuropathological examination. The precise recording of the anamnesis, the thorough knowledge of clinical symptoms and diagnostic tests could be helpful in establishing diagnosis as early and as accurately as possible, which might be crucial for choosing the most effective therapy. Nowadays we have a lot of pharmacotherapies and non-pharmacotherapies, the use of which can significantly increase the number of years with a good quality of life of patients with this currently untreatable condition.]

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[Non-valvular AF is the most common cardiac arrhytmia. Its incidence increases with age. AF is an independent risk factor for ischaemic stroke, representing a five times higher risk for it, associated with a high mortality rate. Beside AF, there are several other risk factors which influence the risk of stroke. Stroke risk calculator can be used to assess the risk of patient having a stroke. The most endangered group of patients with AF are those who have already suffered from cerebrovascular event. The only effective medication for prevention of stroke due to AF had been the application of vitamin K antagonists (VKA) which considerably decrease the rate of ischaemic event in a patient with AF providing that the INR is in the therapeutic range. VKA have several limitations of use in clinical practice and the fear of bleeding complications results an underusing of these drugs. Only 50% of all patients treated with VKA reaches the therapeutic range of INR. The breakthrough of prevention of stroke in recent years is undisputedly the coming out of novel oral anticoagulants (NOACs, thrombin and Xa-factor inhibitors). Recent studies suggest that these novel drugs prove the same efficacy as VKA drugs, furthermore dabigatran in a dose of 2×150 mg or apixaban in 2×5mg was statistically superior to warfarin in the prevention of stroke. NOACs have shown a large reduction in intracranial hemorrhage compared with warfarin. They are given as a fixed dose and do not require persistent monitoring making them much more convenient. NOACs at guidelines of European Society of Cardiology act as a preferable drugs in case of ischaemic stroke with AF. Probably the extended use of NOACs in clinical practice will be the mainstream of stroke prevention in the future.]

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[Atrial fibrillation (AF) is well established risk factor for cardioembolic stroke. With thromboprophylatic treatment we can reduce the risk of stroke in patients with AF. Oral vitamin K antagonists (VKA) such as warfarin and acenocoumarol are effective for stroke prevention in patients with atrial fibrillation. VKAs are associated with several limitations including very narrow therapeutic range, several factors (diet, drugs, alcohol consumption) affecting the effect of VKA and excessive bleeding may occur if INR value not controlled successfully. New oral anticoagulant direct Xa factor inhibitor rivaroxaban has a good therapeutic efficacy in prevention (primary and secondary) of stroke in AF patients. Its advantages are including no need for monitoring, fixed oral dose, not affected by meal, age and body weight, all of them can improve patient adherence. In ROCKET AF trial in patients with AF, rivaroxaban was noninferior to warfarin for the prevention of stroke or systemic embolism. There was no significant between-group difference in the risk of major bleeding, although intracranial and fatal bleeding occurred less frequently in the rivaroxaban group.]

LAM Extra for General Practicioners

[ON RIVAROXABANS MECHANISM OF EFFECT]

BODA Zoltán

[A new era of anticoagulant therapy is approaching. No new oral anticoagulants have been introduced for seventy years. However, two large groups of anticoagulants (molecules with anti-FXa and anti-FIIa acitivity) are currently at advanced stages of clinical trials. This publication summarises the most important information on the mechanism of effect of the anti-FXa drug rivaroxaban. The possible advantages of the “direct” effect and the anti-FXa effect are emphasized. The most significant drug interactions of the new anticoagulant are also presented.]

Clinical Neuroscience

[The importance of anticoagulant therapy in patients with artial fibrillation in stroke prevention – summary of international data and novel therapeutic modalities]

MIROLOVICS Ágnes, PAPP Csaba, ZSUGA Judit, BERECZKI Dániel

[The most common cardiogenic cause of ischaemic stroke is atrial fibrillation which increases the probability of stroke five-fold and doubles case fatality. Based on international data the incidence of atrial fibrillation is approx. 2% however this rapidly increases with age. The necessity of using oral anticoagulants in the prevention of non-valvular atrial fibrillation related stroke is decided based on estimated stroke risk. The CHADS2 and the more predictive CHA2DS2-VASc scales are used for this purpose while the bleeding risk of patients treated with anticoagulant may be estimated by the HAS-BLED scoring scale. For decades oral anticoagulation meant using vitamin-K antagonists. Based on international data we can see that rate of anticoagulation is unacceptably low, furthermore most of the anticoagulated patients aren’t within the therapeutic range of INR (INR: 2-3). A lot of disadvantages of vitamin-K antagonists are known (e.g. food-drug interaction, need for regular coagulation monitoring, increased risk of bleeding), therefore compounds with new therapeutic target have been developed. The novel oral anticoagulants (NOAC) can be divided in two major subgroups: direct thrombin inhibitors (dabigatran etexilate) and Xa-factor inhibitors (rivaroxaban, apixaban, edoxaban). These products are administered in fix doses, they less frequently interact with other medications or food, and regular coagulation monitoring is not needed when using these drugs. Moreover several studies have shown that they are at least as effective in the prevention of ischaemic stroke than the vitamin-K antagonists, with no more haemorrhagic complications.]