Amitriptyline - mankhwala oletsa kupsinjika kwakukulu
Kufotokozera kogwirizana ndi 22.09.2014
- Dzina lachi Latin: Ammitriptyline
- Code ya ATX: N06AA09
- Chithandizo: Amitriptyline
- Wopanga: Grindeks (Latvia), Nycomed (Denmark), Synthesis (Russia), Ozone (Russia), ALSI Pharma (Russia)
Mapaipi ndi mapiritsi Amitriptyline ali ndi 10 kapena 25 mg yogwira ntchito mu mawonekedwe a amitriptyline hydrochloride.
Zina zomwe zimapezeka m'mapiritsi ndi microcrystalline cellulose, talc, lactose monohydrate, silicon dioxide, magnesium stearate, pregelatinized starch.
Zowonjezera mu dragees ndi: magnesium stearate, mbatata wowuma, talc, polyvinylpyrrolidone, lactose monohydrate.
1 ml ya yankho lili ndi 10 mg yogwira ntchito. Zowonjezera ndizo: hydrochloric acid (sodium hydroxide), dextrose monohydrate, madzi a kulowetsedwa, sodium chloride, benzetonium chloride.
Pharmacodynamics ndi pharmacokinetics
Mankhwala amachepetsa kudya, amathetsa kugona, ali antiserotonin kanthu. Mankhwala ali ndi chapakati ndi zotumphukira anticholinergic kwenikweni. Mphamvu yothandizira akwaniritsidwa ndi kuchuluka kuchuluka kwa serotonin mu mantha dongosolo ndi norepinephrine mu ma synapses. Kutalika kwakanthawi kwamankhwala kumayambitsa kuchepa kwa ntchito ya serotonin ndi beta-adrenergic receptors mu ubongo. Amitriptyline amachepetsa kuwonongeka kwa mawonetseredwe achisoni, chipwirikitinkhawa nthawi nkhawa komanso kukhumudwa. Mwa kutsekereza H2-histamine receptors khoma la m'mimba (maselo a parietal) zotsatira za antiulcer zimaperekedwa. Mankhwalawa amatha kuchepetsa kutentha kwa thupi, kuthamanga kwa magazi ndi opaleshoni yayikulu. Mankhwala sikuletsa monoamine oxidase. Mphamvu yotsutsana imawonekera patatha milungu itatu ya mankhwala.
Kuchuluka kwazinthu zambiri m'magazi kumachitika pambuyo pa maola ochepa, nthawi zambiri pambuyo 2-12. Likukhalira metabolites ndi mkodzo. Amamangidwa bwino ndi mapuloteni.
Contraindication
Malinga ndi kunena kwa mankhwalawa, mankhwalawa sagwiritsidwa ntchito pophwanya myocardial, tsankho kwa chinthu chachikulu, kutseka-kotsekera glaucomakuledzera pachimake ndi psychoactive, analgesic, hypnotics, ndi mowa pachimake kuledzera. Mankhwalawa ali contraindified mu yoyamwitsa, kuphwanya kwambiri intraventricular conduction, antioventricular conduction. Ndi matenda a mtima dongosolo, ndi chopinga chotupa hematopoiesis, manic-okhumudwitsa psychoses, mphumu ya bronchial, uchidakwa wambiri, kutsika kwa magalimoto ntchito ya m'mimba, kukanika, chiwindi ndi matenda a impso, intraocular matenda oopsa, kusungika kwamkodzo, hyperplasia ya prostatic, ndi hypotension ya chikhodzodzo, chithokomiro, khunyu Amitriptyline amalembedwa mosamala.
Bongo
Mawonekedwe kuchokera dongosolo lamanjenje: chikomokere, stupor, kuchuluka kugona, nkhawa, kuyerekezera zinthu zina, ataxia, matenda a khunyu, choreoathetosisHyperreflexia dysarthria, kukhazikika kwa minofu minofu, chisokonezo, kusokonezeka, kusokonezeka kwa chidwi, kusinthasintha kwa psychomotor.
Kuwonetsera kwa bongo wa Amitriptyline ndi mtima: kuphwanya intracardiac conduction, arrhythmia, tachycardia, kugwa magazi, mantha, kulephera kwa mtimakawirikawiri - kumangidwa kwa mtima.
Zodziwikanso anuriaoliguria, thukuta likukula, hyperthermia, kusanza, kupuma movutikira, kupsinjika kwa kupuma, cyanosis. Mwina poyizoni wa mankhwala osokoneza bongo.
Kuti mupewe mavuto omwe amabwera chifukwa cha kuchuluka kwa mankhwala osokoneza bongo, chiwopsezo chapamimba cham'mimba ndikuwongolera kwa cholinesterase inhibitors amafunikira chiwonetsero chachikulu cha anticholinergic. Zimafunikanso kusungabe mphamvu yamagetsi yamagetsi, kuchuluka kwa kuthamanga kwa magazi, kuyang'anira kayendedwe kazinthu zamtima, kupatsanso mphamvu ndi kupondereza, ngati kuli kofunikira. Kukakamizidwa diuresis, ndipo hemodialysis sinawonetsedwe kuti siyothandiza pakachitika mankhwala ochulukirapo a amitriptyline.
Kuchita
Zotsatira zoyipa, kupuma, zomwe zimakhumudwitsa dongosolo lamanjenje zimawonedwa ndi kuphatikiza kwa mankhwala omwe amalepheretsa dongosolo lamkati lamanjenje: opaleshoni yayikulu, benzodiazepines, barbiturates, antidepressants ndi ena. Mankhwalawa amathandizira kuuma kwa zotsatira za anticholinergic tikamamwa amantadine, antihistamines, biperiden, atropine, antiparkinsonia mankhwala, phenothiazine. Mankhwala timapitiriza anticoagulant ntchito za indadione, coumarin zotumphukira, yosalunjika anticoagulants. Kuchepa mphamvu alpha blockersphenytoin. Fluvoxamine, fluoxetine onjezani kuchuluka kwa mankhwalawa m'magazi. Chiwopsezo chodwala khunyu imachuluka, ndipo zotsatira zoyipa za anticholinergic komanso sedative zimathandizidwanso ndi chithandizo chophatikizidwa ndi benzodiazepines, phenothiazines, ndi mankhwala a anticholinergic. Kulandila munthawi yomweyomethyldopa, reserpine, betanidine, guanethidine, clonidine amachepetsa kuopsa kwa iwo oopsa. Mukamamwa cocaine, amayamba kupanga. Delirium imayamba mutenga acetaldehydrogenase zoletsa, disulfiram. Amitriptyline imathandizira zotsatira zamitsempha yama mtima phenylephrinenorepinephrine epinephrineisoprenaline. Chiwopsezo cha hyperpyrexia chikuwonjezereka pogwiritsa ntchito ma antipsychotic, m-anticholinergics.
Malangizo apadera
Musanapange chithandizo, ndikofunikira kuti muwongolere kuthamanga kwa magazi. Pareteral makonzedwe a amitriptyline amaperekedwa kokha moyang'aniridwa ndi achipatala pachipatala. M'masiku oyambirira a chithandizo, kupuma pabedi ndikofunikira. Kukana kwathunthu kwa ethanol kumafunika. Kukana kwambiri mankhwala kungayambitse achire syndrome. Mankhwala osokoneza bongo oposa 150 mg patsiku amabweretsa kuchepa kwapakhomo kogwira ntchito, komwe ndikofunikira kuganizira mukamayamba kugwidwa ndi khunyu kwa odwala omwe ali ndi vuto lotha kudziwiratu. Mwina chitukuko cha hypomanic kapena manic limati mwa anthu omwe ali ndi vuto la cyclical, vuto lothandizika pa nthawi yovuta. Ngati ndi kotheka, mankhwalawa amayambiranso ndi Mlingo wocheperako atasiya izi. Muyenera kusamala pochiza odwala omwe amatenga mankhwalawa a chithokomiro pochiza odwala omwe ali ndi chithokomiro chifukwa cha chiwopsezo chokhala ndi zotsatira za mtima. Mankhwalawa angayambitse kukula kwamitsempha yodwala mwa okalamba, komanso kuyamba kudzimbidwa. Ndikofunikira kuti achenjeze ochita opaleshoni kuti asatenge mankhwala osokoneza bongo musanayambe kuchita opaleshoni yam'deralo kapena wamba. Chithandizo cha nthawi yayitali chimayambitsa chitukuko makasitomala. Kufunika kowonjezereka kwa riboflavin. Amitriptyline imadutsa mkaka wa m'mawere; mu makanda, imapangitsa kugona. Mankhwalawa amathandizira kuyendetsa.
Mankhwalawa akufotokozedwa pa Wikipedia.
Zotsatira za pharmacological
Njira yothetsera kupsinjika. Amachepetsa nkhawa, kukhumudwa kwambiri, kumangika. Mfundo yochitira pothana ndi kukhumudwa imatheka chifukwa cha kuchuluka kwa norepinephrine mu ma synapses ndi / kapena serotonin mkati wamanjenje (kuchepa kwa mayankho awo obwezeretsanso). Kudzikundikira kwa ma neurotransmitters awa amawonekera chifukwa cha kuponderezedwa kwawo kosinthidwa ndikugwira nembanemba am'mimba a presynaptic neurons.
Kuchita kwa mankhwala oletsa kupanikizika kumachitika mkati mwa masabata awiri kapena atatu kuyambira pomwe madokotala amayambitsidwa.
Amitriptyline ali ndi sedative, M-anticholinergic, antihistamine, antiserotonin, timoleptic, anxiolytic ndi analgesic, antiulcer.
Pa mankhwala opaleshoni, amachepetsa kuthamanga kwa magazi ndi kutentha kwa thupi.
Sizingaletse monoamine oxidase.
Mlingo Wamitundu
Amitriptyline amapangidwa ndi opanga ambiri. Mitundu yayikulu yamankhwala - mapiritsi, yankho la jakisoni:
- jakisoni njira - ampoules 20 mg / 2 ml, Mbale 10 mg / ml,
- mapiritsi a 0.025 g
- shuga mapiritsi 10 mg, 25 mg,
- mapiritsi, Filimu wokutira 10 mg, 25 mg, 50 mg, 75 mg,
- dragee 25 mg
- makapisozi okhazikika otulutsa 50 mg.
Kuchulukitsa kwa mankhwala, komanso mphamvu inayake ya mphamvu yogwira, ikhoza kukhala yosiyana.
Kamangidwe ka yankho la jakisoni:
- yogwira - amitriptyline hydrochloride,
- zotupa - shuga (dextrose), madzi a jakisoni.
Mapangidwe a mapiritsi okhala ndi filimu:
- ntchito yogwira ndi amitriptyline hydrochloride,
- excipients - magnesium stearate, talc, povidone, mbatata wowuma, microcrystalline cellulose, lactose monohydrate.
Mapangidwe a Shell: propylene glycol, hypromellose, titanium dioxide, talc.
Mapale:
- ntchito yogwira - amitriptyline,
- zotupa - lactose, magnesium stearate, microcrystalline cellulose, croscarmellose sodium, polyethylene glycol 6000, talc, polysorbate 80, colloidal silicon dioxide, hypromellose, titanium dioxide (E 171), carmoisine (E 122).
Kuphatikizira kwa makapisozi osasinthika:
- ntchito yogwira ndi amitriptyline hydrochloride,
- zokopa - stearic acid, magawo a shuga, zipolopolo (zosapindika za zipolopolo), talc, povidone.
Kuphatikizika kwa kapisozi kopanda kanthu ndi gelatin, utoto wachitsulo wofiira (E 172), titanium dioxide (E 171).
- mitundu yayikulu ya kukhumudwa, makamaka ndi chizindikiro cha nkhawa, kudzutsidwa m'maganizo, kusokonezeka kwa kugona: kubwereza (kubwereza), kusinthika (pambuyo pa kuvulala kwamisala), mitsempha, mankhwala osokoneza bongo, kusiya mowa, kuwonongeka kwa ubongo, kuphatikiza ubwana.
- schizophrenic matenda amisala, malo okhumudwa mwa odwala a schizophrenia,
- zosokoneza zosiyanasiyana zamalingaliro,
- chisamaliro, ntchito,
- nocturnal enursis (kupatula kwa odwala omwe amachepetsa mphamvu ya makoma a chikhodzodzo),
- bulimia amanosa
- aakulu ululu syndrome - kupweteka kwa odwala khansa, migraine, matenda amisempha, kupweteka kwa pakhungu, postherpetic neuralgia, neuropathies a magwero osiyanasiyana (matenda ashuga, pambuyo pake, zovuta zina zotumphukira).
- mutu
- migraine prophylaxis,
- zilonda zam'mimba ndi duodenum.
Ma Tricyclic antidepressants amakhala mankhwala oyambira mzere wazovuta kwambiri.
Njira yoyendetsera ndi kumwa
Amitriptyline amatengedwa pakamwa osatafuna nthawi yomweyo atatha kudya kuti achepetse kupweteka kwa m'mimba.
Mlingo woyambirira wa akuluakulu ndi 25-50 mg pogona, ndiye kuti kuchuluka kwa mankhwalawa kupitilira masiku 5-6 kufika pa 150-200 mg tsiku lililonse pamiyeso itatu, gawo lalikulu la mankhwalawo limakhazikitsidwa pogona. Ngati patatha masiku 14 palibe kusintha, mlingo wa tsiku ndi tsiku umachulukitsidwa mpaka 300 mg.
Ngati zizindikiro za kukhumudwa zitha, mlingo umachepetsedwa kukhala 50-100 mg patsiku ndipo chithandizo chimapitilizidwa kwa miyezi itatu.
Mukakalamba, ndimatenda ofooka, mlingo wa 30-100 mg patsiku umayikidwa usiku, atatha kupeza chithandizo chamankhwala, amasinthana ndi Mlingo wothandiza wa 25-50 mg patsiku.
Jakisoni amaperekedwa pang'onopang'ono pa 20-25 mg kanayi patsiku, pang'onopang'ono m'malo mwa kumeza. Kutalika kwa chithandizo sikupitilira miyezi 6-8.
Ndi usiku ma enursis:
- mwa ana a zaka 6 mpaka 10 - 10 mpaka 20 mg patsiku usiku,
- mwa ana a zaka 11-16 - 25-50 mg / tsiku.
Ana ngati mankhwala oletsa kuponderezana:
- kuyambira wazaka 6 mpaka 12 - 10-30 mg kapena 1-5 mg pa kilogalamu ya kulemera patsiku,
- achinyamata - 10 mg katatu patsiku, ngati kuli kotheka - mpaka 100 mg patsiku.
Pofuna kupewa migraine, komanso kupweteka kwa neurogenic, kupweteka kwakutali kwa mutu - kuyambira 12,5 - 25 mpaka 100 mg patsiku. Mlingo wapamwamba umatengedwa usiku.
Zotsatira zoyipa
Kuphatikiza pazomwe zimachitika mu njira za neural, amitriptyline imadziwika ndi zambiri zachiwiri zamitsempha yamagetsi zomwe zimapangitsa zotsatira zake:
- antagonism mogwirizana ndi M1-cholinergic receptors amatsimikiza kukula kwa anticholinergic syndrome - tachycardia, kamwa yowuma, kusokonezeka pogona, kudzimbidwa, kusungika kwamikodzo, chisokonezo (delirium kapena hallucinations), kufooka matumbo,
- blockade of alpha1-adrenergic receptors amachititsa orthostatic circulatory circ (chizungulire, kufooka, kufooka kwa chikumbumtima, kukomoka), Reflex tachycardia,
- blockade of H1-histamine receptors - sedation, kulemera,
- kusintha kwa kagayidwe ka ion mu minyewa yaubongo ndi mtima kumachepetsa gawo lokonzekera kutsimikiza ndikuthandizira kuwonekera kwa zotsatira za mtima - mawonekedwe a contractions ndikupereka kwa zokakamiza ku myocardium ikuphwanyidwa.
Kuopsa kwa zovuta zoyipa nthawi zambiri kumakwiyitsa madokotala kuti agwiritse ntchito moyenera mankhwalawa, komanso kumachepetsa kwambiri kutsatira kwa odwala, zomwe zimachepetsa kwambiri chithandizo.
Chifukwa cha chiwopsezo chakupha chakupha ndi ma tridclic antidepressants, amasankhidwa ndi odwala omwe ali ndi malingaliro ofuna kudzipha kuti akwaniritse zofuna zawo. Chifukwa chake, mankhwalawa amalembedwa kuti wodwalayo sangathe kudziunjikira kuchuluka kokwanira kodzipha.
Amitriptyline analogues
Kukonzekera komwe gawo lake lalikulu ndi amitriptyles ndi Amizol, Elivel, Saroten retard. Momwemo, fanizo la mankhwalawa limaphatikizidwa ndi mankhwala omwe amapezeka m'gulu la antidepressant atatu: imipramine, clomipramine, desipramine, doxepin, pipofesin, tianeptine. Komabe, zochita zawo zamankhwala zimasiyanasiyana.
Mwambiri, zotsatira za mankhwala a antidepressant aliwonse, makamaka pogwiritsa ntchito nthawi yayitali, zimadziwika kudzera mu zovuta zambiri zama neurotransmitter ndi receptor system ya ubongo. Chifukwa chake, chiwonetsero cha munthu payekha cha psychotropic, neurotropic ndi somatotropic zotsatira za mankhwala polimbana ndi kutaya mtima zimatengera chiyezo cha pulayimale ndi kulimba kwa izi. Kuwerengera kwawo kophatikizidwa kumakupatsani mwayi kuti musankhe mankhwala okhawo owona muzochitika zonse, zomwe zimapangitsa kupambana kwachipatala.
Yang'anani! Kufotokozera kwa mankhwalawa ndi mtundu wosavuta komanso wowonjezera wa malangizo ovomerezeka kuti agwiritse ntchito. Zambiri zokhudzana ndi mankhwalawa zimaperekedwa pazidziwitso zokhazokha ndipo siziyenera kugwiritsidwa ntchito ngati chitsogozo chodzidziwitsa nokha.
Mlingo
Mapiritsi Amtambo, 25 mg
Piritsi limodzi lili
ntchito yogwira - amitriptyline hydrochloride malinga ndi amitriptyline 25 mg,
zokopa: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hypromellose, magnesium stearate, colloidal silicon dioxide, polyethylene glycol 6000, titanium dioxide (E 171), talc, polysorbate 80, carmoisin (E 122).
Mapiritsiwo ndi ozungulira, okutira, kuyambira ku pinki kupita ku pinki, okhala ndi mawonekedwe apamwamba komanso otsika. Pa zolakwika pansi pagalasi lokulitsa mutha kuwona chapakati kuzunguliridwa ndi wosanjikiza umodzi wosapitilira.
Mankhwala
Pharmacokinetics
Amitriptyline imatengeka bwino kuchokera m'matumbo am'mimba, kuchuluka kwambiri kwa plasma kumafikiridwa patatha pafupifupi maola 6 mutayamwa pakamwa.
The bioavailability ya amitriptyline ndi 48 ± 11%, 94.8 ± 0.8% imagwirizanitsidwa ndi mapuloteni a plasma. Izi magawo samatengera zaka za odwala.
Hafu ya moyo ndi maola 16 ± 6, voliyumu yogawa ndi 14 ± 2 l / kg. Magawo onsewa amakula kwambiri ndikukula kwa wodwalayo.
Amitriptyline amachepetsa kwambiri chiwindi mpaka metabolite yayikulu - nortriptyline. Njira za metabolism zimaphatikizapo hydroxylation, N-oxidation, ndi kuphatikizika ndi glucuronic acid. Mankhwalawa amamuchotsa mkodzo, makamaka mu mawonekedwe a metabolites, mwaulere kapena mawonekedwe. Chilolezocho ndi 12.5 ± 2.8 ml / mphindi / kg (sizimatengera zaka za wodwalayo), zosakwana 2% zimatulutsidwa mkodzo.
Mankhwala
Amitriptyline ndi mankhwala antidepressant atatu. Adanenanso antimuscarinic komanso katundu wosinthika. The achire zotsatira zochokera kuchepa kwa presynaptic reuptake (ndipo, monga chotsatira, inactivation) wa norepinephrine ndi serotonin (5HT) ndi presynaptic nerve endings.
Ngakhale kuti mawu akuti antidepressant zotsatira, monga lamulo, amadziwonekera patatha masiku 10 mpaka 14 chiyambireni chithandizo, kuletsa ntchito kungawoneke molingana ndi ola limodzi pambuyo pothandizidwa. Izi zikusonyeza kuti momwe amagwirira ntchito amatha kutsendera mankhwala ena amtundu wa mankhwala.
Mlingo ndi makonzedwe
Kuchiza kuyenera kuyamba ndi yaying'ono Mlingo, pang'onopang'ono kuwachulukitsa, kuwunika mosamala mayendedwe azachipatala komanso kuwonetsa kulikonse kwa tsankho.
AkuluakuluMankhwala oyambira ndi 75 mg tsiku lililonse, kumwa mankhwala osiyanitsidwa kapena usiku wonse. Kutengera ndi mankhwalawa, mankhwalawa akhoza kuwonjezeka mpaka 150 mg / tsiku. Ndikofunika kuwonjezera kuchuluka kumapeto kwa tsiku kapena pogona.
Zochita zolimbitsa thupi nthawi zambiri zimadziwonekera mofulumira. Mphamvu yoletsa kukonzekera ya mankhwalawa imatha kuchitika patatha masiku 3-4, kuti chitukuko chikhale chotheka, zingatenge mpaka masiku 30.
Pofuna kuchepetsa mwayi obwereranso, muyenera kumwa mankhwalawa 50-100 mg wamadzulo kapena asanagone.
Ana: Mankhwala osavomerezeka kwa ana ochepera zaka 16.
Okalamba okalamba (woposa zaka 65): Mlingo woyenera woyambira ndi 10-25 mg katatu patsiku ndi kuwonjezeka pang'onopang'ono ngati kuli kofunikira. Kwa odwala amsinkhu uwu omwe sangathe kulekerera waukulu, tsiku lililonse 50 mg akhoza kukhala yokwanira. Kufunika kwa tsiku lililonse kwa mankhwalawa kungafotokozeredwe mwanjira zingapo, kapena kamodzi, makamaka madzulo kapena asanagone.
Mapiritsi amayenera kumezedwa kwathunthu osafuna kutafuna ndi kumwa ndi madzi.
Mankhwalawa amayenera kumwedwa molingana ndi mawu omwe adokotala adapereka, popeza kuti kudzipatsa chithandizo chamankhwala kungakhale koopsa thanzi. Kulephera kusintha kwa mkhalidwe wa wodwalayo kumawonedwa mpaka milungu inayi atayamba chithandizo.
Zotsatira zoyipa
Monga mankhwala ena, amitriptyline, mapiritsi okhala ndi vuto, nthawi zina amatha kuyambitsa mavuto ena mwa odwala, makamaka ngati atchulidwa koyamba. Osati zotsatirapo zonse zoyipa zomwe zimawonedwa pamankhwala amitriptyline, ena a iwo adachitika akamagwiritsa ntchito mankhwala ena a gulu la amitriptyline.
Zotsatira zoyipa zimafotokozedwa pafupipafupi: Nthawi zambiri (> 1/10), nthawi zambiri (kuyambira> 1/100 mpaka 1/1000 mpaka 1/10000 kupita