Amtolmetin: A Reappraisal of NSAID with Gastroprotection

Garg, Amit; Shoeb, Ahsan; Moodahadu, Latha Subramanya; Gandhi, Arul; Akku, Shyam

doi:10.1155/2016/7103705

Cited by 9 publications

(6 citation statements)

References 23 publications

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“…В более позднем метаанализе трех РКИ (n=349), в которых АМГ сравнивался с диклофенаком, пироксикамом и целекоксибом, также было показано преимущество первого препарата в отношении меньшего риска развития серьезных НР. Так, общее число серьезных осложнений, потребовавших прерывания терапии, на фоне АМГ составило 5 случаев (3,0%), других НПВП -15 случаев (8,5%; p<0,05) [34].…”

Section: Discussionunclassified

Evaluation of efficacy and safety of long-term use of amtolmetin guacil in rheumatic diseases: results of a 9-month observational AURORA study (Amtolmetin guacil: allRussian Register for Osteoarthritis, Rheumatoid arthritis and Ankylosing spondylitis)

Каратеев¹,

Nasonov

Глухова³

et al. 2019

Naučno-praktičeskaâ revmatologiâ

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Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for the treatment of rheumatic diseases (RD). In some cases, their long-term use is advisable: NSAIDs slow the progression of spondylarthritis, are an important element in the control of chronic pain in osteoarthritis (OA) and rheumatoid arthritis (RA). However, the risk of serious adverse events (AE) should be considered. A good choice for long-term therapy may be amtolmetin guacil (AMG), which rarely induce gastrointestinal AE.The aimof the study was to assess the effect and safety of long-term use of AMG in RD.Material and methods.An open observational study was conducted in which AMG (Nayzilat) was assigned to 442 patients with OA (mean age 60.6±10.2 years, women 88.7%), 126 patients with RA (55.0±14.0 years, women 84.2%) and 73 with ankylosing spondylitis (AS, 47.0±12.0 years, women 30.0%). The dose of AMG depended on the clinical situation and was determined by the attending physician: from 1800 to 600 mg/day. The main criterion of the effect was the changes of pain by numeric rating scale (NRS), additional measures of efficacy were pain on the WOMAC and HAQ for OA, DAS28 for RA, BASDAI, BASFI and ASDAS-CRP for AS. The result of treatment was evaluated during three consecutive visits every 3 months (9 months of follow-up).Results and discussion.At the end of follow-up 65.2% of patients with OA, 75.3% of patients with RA and 82.2% of patients with AS continued treatment with AMG. The reasons for discontinuation of treatment were significant reduction or absence of pain (70.3%), the patient's decision (26.6%) or AE (3.1%). At the end of follow-up, there was a significant decrease in pain intensity compared to the baseline: in OA, the median pain decreased from 5.6 [4.1; 6.9] to 3.4 [1.7; 5.1], in RA from 5.8 [4.0; 7.5] to 3.4 [2.0; 4.8], in AS from 5.8 [4.2; 7.5] to 3.1 [1.5; 5.0] according to NRS, the difference was significant in all groups (p<0.001). In OA, the median WOMAC pain decreased from 127 [24; 159] to 13.7 [14; 40] (p<0.001), the average HAQ value – from 0.54±0.44 to 0.34±0.26 (p<0.001). In RA, the average value of DAS28 decreased from 4.81±1.18 to 4.30±1.24 (p<0.05). The number of painful and swollen joints, ESR and C-reactive protein also significantly decreased. In AS, the median BASDAI index decreased from 4.5 [1.0; 8.0] to 3.0 [0; 8.0] (p<0.001). The number of patients with high activity according to ASDAS-CRP (>3.5) decreased from 76.9 to 25.8% (p<0.001). The BASFI index did not changed. 77.9% of patients with OA, 77.0% with RA and 74.5% with AS were satisfied with the results of AMG treatment. AMG tolerance was good. Mild dyspepsia was observed in 15–25% of patients. AE, which caused the discontinuation of therapy, were observed only in 6 (0.93%) patients. There was no development or deterioration of hypertension, as well as other cardiovascular complications.Conclusion.AMG is an effective NSAID with good tolerability, which is advisable to use for long-term treatment of RD. Limitations are the open nature of the study and the absence of a control group.

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Section: Discussionunclassified

Evaluation of efficacy and safety of long-term use of amtolmetin guacil in rheumatic diseases: results of a 9-month observational AURORA study (Amtolmetin guacil: allRussian Register for Osteoarthritis, Rheumatoid arthritis and Ankylosing spondylitis)

Каратеев¹,

Nasonov

Глухова³

et al. 2019

Naučno-praktičeskaâ revmatologiâ

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“…Однако частота язвенно-некротических поражений (язвы желудка и двенадцатиперстной кишки, высокий эндоскопический счет) при использовании АМГ была не ниже, чем в случае терапии другими НПВП (р<0,05). Примечательно, О р и г и н а л ь н ы е и с с л е д о в а н и я что тяжелые НР, приводившие к отмене препарата, на фоне лечения АМГ развивались достоверно реже (р<0,05) [20]. Более того, наши данные свидетельствуют о хорошей субъективной (опросник SODA) переносимости терапии у пациентов с ОА и диспепсией после замены стандартных НПВП на АМГ.…”

Section: Discussionunclassified

“…АМГ относится к числу неселективных НПВП с соотношением селективности к ЦОГ2/ ЦОГ1, равным 4,4 [16]. Имеются данные о том, что АМГ обладает сходной эффективностью с неселективными в отношении ЦОГ НПВП и селективным ингибитором ЦОГ2 целекоксибом, но лучшей переносимостью со стороны органов ЖКТ [16][17][18][19][20]. Полагают, что этот благоприятный эффект АМГ связан с наличием в структуре молекулы остатков ванилина, которые стимулируют рецепторы капсаицина и образование пептида, связанного с геном кальцитонина, что в свою очередь способствует образованию оксида азота, обладающего «гастропротективной» активностью [21,22].…”

Section: Methodsunclassified

An Open-Label Multicenter Observational Study of the Efficacy, Tolerability, and Safety of the Nonsteroidal Anti-Inflammatory Drug Amtolmetin Guacil in Patients With Knee Osteoarthritis and Dyspepsia

Цветкова¹,

Denisov²,

Оттева³

et al. 2017

Naučno-praktičeskaâ revmatologiâ

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Objective: to investigate the efficacy and tolerability of amtolmetin guacil (AMG; Niselat®, Dr. Reddy's Laboratories Ltd, India) versus previous therapy with nonsteroidal anti-inflammatory drugs (NSAIDs) in patients with knee osteoarthritis (OA) and signs of dyspepsia.Subjects and methods. The open-label observational study included 220 patients aged 30–65 years who suffered from knee OA and intense pain during NSAID intake and had symptoms of dyspepsia in the absence of contraindications to the use of AMG. Among the comorbidities that generally occurred in 68% of the patients, there was a preponderance of hypertension (42%), lower extremity varicose veins (6.4%), and diabetes mellitus (6%). Treatment efficacy was evaluated using three domains of the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC), by also taking into account pain intensity and general health assessment on the visual analogue scale. A Severity of Dyspepsia Assessment (SODA) scale was used to rate dyspepsia.Results and discussion. AMG had a marked analgesic effect confirmed by 40% or more pain reduction that occurred in 72.5% of the patients. The high analgesic effect of AMG was confirmed by a statistically significant (p <0.001) reduction in the WOMAC index (pain and stiffness) and by an increase in functional activity. There was a significant decrease in painless and painful signs of dyspepsia, as well as positive changes in the measures “overall assessment of dyspepsia severity” (p < 0.001) and “satisfaction with treatment”. Overall assessment of AMG tolerability was only positive: excellent (33%), good (56%), and satisfactory (11%). There were no serious adverse events (AE). AE were graded as moderate and mild in 8 and 82% of cases, respectively. AE were recorded in 7.7% of the patients. Conclusion. The findings suggest that AMG offers good prospects for knee OA treatment.

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“…Взаимодей-ствие амтолметила гуацила с TRPV 1 СОЖ (до по-падания в системный кровоток) сопровождается индукцией каскада биохимических превращений, которые активируют NO-синтазы, снижают стиму-лированную продукцию HCl, подавляют перекисное окисление липидов и др. [29].…”

Section: модуляция «эффекторной функции» афферентных терминалей N Vagusunclassified

Preventive and therapeutic strategies of pharmaco-correction gastropathy induced by nonsteroidal anti-inflammatory drugs

Hladkykh

2017

Rev Clin Pharm Drug Ther

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Today the problem of prevention and treatment of gastropathy associated with nonsteroidal anti-inflammatory drugs has not lost its relevance. In order to reduce the ulcerogenicity of non-steroidal anti-inflammatory drugs, it is classically accepted to supplement the therapy scheme with preparations of other pharmacological groups - antacids, alginates, M-cholinoblockers, gastrin receptor antagonists, H2-histamine blockers, proton pump inhibitors, synthetic analogues of prostaglandins or stimulators of their synthesis, reparants, gastroprotectors. Nowadays, it was suggested I was suggested the use of drugs which have pharmacological properties polyvector (vinboron, thiotriazoline et al.). Also, the scientists started of combined preparations “NSAIDs + drugs other pharmacological groups” - indotril (indomethacin + thiotriazoline) diklokor (diclofenac + quercetin) Artrotek (diclofenac sodium + misoprostol) dueksis (ibuprofen + famotidine) vimovo (naproxen + esomeprazole) aksorid (ketoprofen + omeprazole) tioaspekard (thiotriazoline + ACK) aspifat (ACK + sucralfate), Alka-Zelttser® (ACK + sodium bicarbonate), and others. The second direction is preventing and improving NSAID gastrotoxicity protrudes improving existing non-steroidal drugs - modification of gaseous molecules (NO, H2S, CO), amino acid derivatives, modulators “effector function” of afferent terminals n. vagus (amtolmetina guatsil) то pairing with nanoparticles biometals (Zn-ibuprofen, Zn-naproxen, Zn-indomethacin). (For citation: Hladkykh FV. Preventive and therapeutic strategies of pharmaco-correction gastropathy induced by nonsteroidal anti-inflammatory drugs. Reviews on Clinical Pharmacology and Drug Therapy. 2017;15(4):14-23. doi: 10.17816/RCF15414-23).

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Amtolmetin: A Reappraisal of NSAID with Gastroprotection

Cited by 9 publications

References 23 publications

Evaluation of efficacy and safety of long-term use of amtolmetin guacil in rheumatic diseases: results of a 9-month observational AURORA study (Amtolmetin guacil: allRussian Register for Osteoarthritis, Rheumatoid arthritis and Ankylosing spondylitis)

Evaluation of efficacy and safety of long-term use of amtolmetin guacil in rheumatic diseases: results of a 9-month observational AURORA study (Amtolmetin guacil: allRussian Register for Osteoarthritis, Rheumatoid arthritis and Ankylosing spondylitis)

An Open-Label Multicenter Observational Study of the Efficacy, Tolerability, and Safety of the Nonsteroidal Anti-Inflammatory Drug Amtolmetin Guacil in Patients With Knee Osteoarthritis and Dyspepsia

Preventive and therapeutic strategies of pharmaco-correction gastropathy induced by nonsteroidal anti-inflammatory drugs

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