Antikolinergik

Antikolinergik (agen antikolinergik) adalah zat yang menghalangi kerja neurotransmiter asetilkolin (ACh) pada sinapsis di sistem saraf pusat dan sistem saraf tepi.^[1]^[2]

Agen-agen ini menghambat sistem saraf parasimpatis dengan secara selektif memblokir pengikatan ACh ke reseptornya di sel saraf. Serabut saraf sistem parasimpatis bertanggung jawab atas pergerakan otot polos yang tidak disengaja di saluran pencernaan, saluran kemih, paru-paru, kelenjar keringat, dan banyak bagian tubuh lainnya.^[3]

Secara luas, antikolinergik dibagi menjadi dua kategori sesuai dengan target spesifiknya di sistem saraf pusat dan perifer serta pada sambungan neuromuskular:^[3] agen antimuskarinik dan agen antinikotinik (penghambat ganglionik, penghambat neuromuskular).^[4]

Istilah "antikolinergik" biasanya digunakan untuk merujuk pada antimuskarinik yang secara kompetitif menghambat pengikatan ACh ke reseptor asetilkolin muskarinik; agen tersebut tidak memusuhi pengikatan reseptor asetilkolin nikotinat di sambungan neuromuskular, meskipun istilah ini kadang-kadang digunakan untuk merujuk pada agen yang melakukan hal tersebut.^[3]^[5]

Kegunaan dalam medis

Obat antikolinergik digunakan untuk mengobati berbagai kondisi seperti:

Pusing (termasuk gejala yang berhubungan dengan vertigo dan mabuk gerak)
Gejala ekstrapiramidal, potensi efek samping obat antipsikotik
Gangguan gastrointestinal (misalnya tukak lambung, diare, pilorospasme, divertikulitis, kolitis ulseratif, mual, dan muntah)
Gangguan genitourinari (misalnya sistitis, uretritis, dan prostatitis)
Insomnia, meski biasanya hanya dalam jangka pendek
Gangguan pernapasan (misalnya asma, bronkitis kronis, dan penyakit paru obstruktif kronik [PPOK])
Sinus bradikardia karena saraf vagus yang hipersensitif
Keracunan zat saraf berbasis organofosfat, seperti VX, sarin, tabun, dan soman (atropin lebih disukai jika digabungkan dengan oksim, biasanya pralidoksim)^[6]^[7]

Antikolinergik umumnya memiliki efek antisialagogue (menurunkan produksi air liur), dan sebagian besar menghasilkan efek sedasi pada tingkat tertentu, keduanya bermanfaat dalam prosedur pembedahan.^[8]^[9]

Hingga awal abad ke-20, obat antikolinergik banyak digunakan untuk mengobati gangguan kejiwaan.^[10]

Contoh

Agen Antimuskarinik
- Antidepresan trisiklik
- Antipsikotik (klozapin, kuetiapin)^[11]
- Atropin
- Benztropin
- Biperiden
- Klorfenamin
- Difenhidramin^[11]
- Dimenhidrinat^[11]
- Disiklomin (Disikloverin)
- Doksepin
- Doksilamin
- Flavoksat
- Glikopironium/-late
- Hiosiamin
- Ipratropium bromida
- Oksibutinin^[11]
- Oksitropium
- Orfenadrin
- Prometazin
- Propantelin bromida
- Skopolamin
- Solifenasin
- SSRI tertentu (Paroksetin)^[11]
- Tolterodin
- Tiotropium
- Triheksifenidil
- Tropikamida^[12]
- Umeklidinium
Agen Antinikotinat
- Bupropion – Penghambat ganglion^[13]^[14]^[15]
- Dekstrometorfan - Penekan batuk dan penghambat ganglion^[16]^[17]^[18]
- Doksakurium – Relaksan otot rangka nondepolarisasi
- Heksametonium – Penghambat ganglion
- Mekamilamin – Penghambat ganglion dan bantuan penghentian merokok sesekali^[19]
- Tubokurarin - Relaksan otot rangka nondepolarisasi

Antidot

Fisostigmin adalah salah satu dari sedikit obat yang dapat digunakan sebagai penangkal keracunan antikolinergik. Nikotin juga melawan antikolinergik dengan mengaktifkan reseptor asetilkolin nikotinat. Kafeina (meskipun merupakan antagonis reseptor adenosina) dapat melawan gejala antikolinergik dengan mengurangi sedasi dan meningkatkan aktivitas asetilkolin, sehingga menyebabkan kewaspadaan dan gairah.

Referensi

^ "Anticholinergics", Anticholinergic Agents, Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases, 2012, PMID 31643610, diakses tanggal 2020-03-23, Anticholinergics have antisecretory activities and decrease nasal and bronchial secretions, salivation, lacrimation, sweating and gastric acid production, and can be used to decrease secretions in allergic and inflammatory diseases. Anticholinergics relax smooth muscle in the gastrointestinal tract, bladder and lung and can be used for gastrointestinal, urological or respiratory conditions associated with spasm and dysmotility.
^ Clinical Pharmacology [database online]. Tampa, FL: Gold Standard, Inc.; 2009. Drugs with Anticholinergic Activity. Prescriber's Letter 2011; 18 (12):271233.
^ ^a ^b ^c Migirov, A; Datta, AR (2020), "article-17683", Physiology, Anticholinergic Reaction, This book is distributed under the terms of the Creative Commons Attribution 4.0 International License, which permits use, duplication, adaptation, distribution, and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, a link is provided to the Creative Commons license, and any changes made are indicated., Treasure Island (FL): StatPearls Publishing, PMID 31536197, diakses tanggal 2020-03-24
^ Sharee A. Wiggins; Tomas Griebling. "Urinary Incontinence". Landon Center on Aging. Diarsipkan dari versi asli tanggal 2011-09-27. Diakses tanggal 2011-07-09.
^ Su, Mark; Goldman, Matthew. Traub, Stephen J.; Burns, Michele M.; Grayzel, Jonathan, ed. "Anticholinergic poisoning". UpToDate. Diakses tanggal 2020-03-24.
^ "NERVE AGENTS". fas.org. Diakses tanggal 2020-07-27.
^ Nair, V. Priya; Hunter, Jennifer M. (2004-10-01). "Anticholinesterases and anticholinergic drugs". Continuing Education in Anaesthesia, Critical Care & Pain (dalam bahasa Inggris). 4 (5): 164–168. doi:10.1093/bjaceaccp/mkh045  . ISSN 1743-1816.
^ Page 592 in: Cahalan, Michael D.; Barash, Paul G.; Cullen, Bruce F.; Stoelting, Robert K. (2009). Clinical Anesthesia. Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 978-0-7817-8763-5.
^ Barash, Paul G. (2009). Clinical Anesthesia. Lippincott Williams & Wilkins. ISBN 9780781787635. Diarsipkan dari versi asli tanggal 20 February 2017. Diakses tanggal 8 December 2014.
^ Bangen, Hans: Geschichte der medikamentösen Therapie der Schizophrenie. Berlin 1992, ISBN 3-927408-82-4
^ ^a ^b ^c ^d ^e "[113] How well do you know your anticholinergic (antimuscarinic) drugs? | Therapeutics Initiative". Therapeutics Initiative. 10 September 2018. Diakses tanggal 20 September 2018.
^ Bersani, F. S.; Corazza, O.; Simonato, P.; Mylokosta, A.; Levari, E.; Lovaste, R.; Schifano, F. (2013). "Drops of madness? Recreational misuse of tropicamide collyrium; early warning alerts from Russia and Italy". General Hospital Psychiatry. 35 (5): 571–3. doi:10.1016/j.genhosppsych.2013.04.013. PMID 23706777.
^ Carroll FI, Blough BE, Mascarella SW, Navarro HA, Lukas RJ, Damaj MI (2014). "Bupropion and Bupropion Analogs as Treatments for CNS Disorders". Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. Advances in Pharmacology. 69. hlm. 177–216. doi:10.1016/B978-0-12-420118-7.00005-6. ISBN 9780124201187. PMID 24484978.
^ Dwoskin, Linda P. (29 January 2014). Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. Elsevier Science. hlm. 177–216. ISBN 978-0-12-420177-4. Diarsipkan dari versi asli tanggal 20 March 2017.
^ Tasman, Allan; Kay, Jerald; Lieberman, Jeffrey A.; First, Michael B.; Maj, Mario (11 October 2011). Psychiatry. John Wiley & Sons. ISBN 978-1-119-96540-4. Diarsipkan dari versi asli tanggal 20 March 2017.
^ Damaj, M. I.; Flood, P; Ho, K. K.; May, E. L.; Martin, B. R. (2004). "Effect of Dextrometorphan and Dextrorphan on Nicotine and Neuronal Nicotinic Receptors: In Vitro and in Vivo Selectivity". Journal of Pharmacology and Experimental Therapeutics. 312 (2): 780–5. doi:10.1124/jpet.104.075093. PMID 15356218.
^ Lee, Jun-Ho; Shin, Eun-Joo; Jeong, Sang Min; Kim, Jong-Hoon; Lee, Byung-Hwan; Yoon, In-Soo; Lee, Joon-Hee; Choi, Sun-Hye; Lee, Sang-Mok; Lee, Phil Ho; Kim, Hyoung-Chun; Nah, Seung-Yeol (2006). "Effects of dextrorotatory morphinans on α3β4 nicotinic acetylcholine receptors expressed in Xenopus oocytes". European Journal of Pharmacology. 536 (1–2): 85–92. doi:10.1016/j.ejphar.2006.02.034. PMID 16563374.
^ Hernandez, S. C.; Bertolino, M; Xiao, Y; Pringle, K. E.; Caruso, F. S.; Kellar, K. J. (2000). "Dextromethorphan and Its Metabolite Dextrorphan Block α3β4 Neuronal Nicotinic Receptors". The Journal of Pharmacology and Experimental Therapeutics. 293 (3): 962–7. PMID 10869398.
^ Shytle, RD; Penny, E; Silver, AA; Goldman, J; Sanberg, PR (Jul 2002). "Mecamylamine (Inversine): an old antihypertensive with new research directions". Journal of Human Hypertension. 16 (7): 453–7. doi:10.1038/sj.jhh.1001416  . PMID 12080428.

[Anticholinergic_Agents_2012_p.-1] "Anticholinergics", Anticholinergic Agents, Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases, 2012, PMID 31643610, diakses tanggal 2020-03-23, Anticholinergics have antisecretory activities and decrease nasal and bronchial secretions, salivation, lacrimation, sweating and gastric acid production, and can be used to decrease secretions in allergic and inflammatory diseases. Anticholinergics relax smooth muscle in the gastrointestinal tract, bladder and lung and can be used for gastrointestinal, urological or respiratory conditions associated with spasm and dysmotility.

[2] Clinical Pharmacology [database online]. Tampa, FL: Gold Standard, Inc.; 2009. Drugs with Anticholinergic Activity. Prescriber's Letter 2011; 18 (12):271233.

[Migirov_Datta_2020_p.-3] Migirov, A; Datta, AR (2020), "article-17683", Physiology, Anticholinergic Reaction, This book is distributed under the terms of the Creative Commons Attribution 4.0 International License, which permits use, duplication, adaptation, distribution, and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, a link is provided to the Creative Commons license, and any changes made are indicated., Treasure Island (FL): StatPearls Publishing, PMID 31536197, diakses tanggal 2020-03-24

[4] Sharee A. Wiggins; Tomas Griebling. "Urinary Incontinence". Landon Center on Aging. Diarsipkan dari versi asli tanggal 2011-09-27. Diakses tanggal 2011-07-09.

[UpToDate-5] Su, Mark; Goldman, Matthew. Traub, Stephen J.; Burns, Michele M.; Grayzel, Jonathan, ed. "Anticholinergic poisoning". UpToDate. Diakses tanggal 2020-03-24.

[6] "NERVE AGENTS". fas.org. Diakses tanggal 2020-07-27.

[7] Nair, V. Priya; Hunter, Jennifer M. (2004-10-01). "Anticholinesterases and anticholinergic drugs". Continuing Education in Anaesthesia, Critical Care & Pain (dalam bahasa Inggris). 4 (5): 164–168. doi:10.1093/bjaceaccp/mkh045  . ISSN 1743-1816.

[8] Page 592 in: Cahalan, Michael D.; Barash, Paul G.; Cullen, Bruce F.; Stoelting, Robert K. (2009). Clinical Anesthesia. Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 978-0-7817-8763-5.

[9] Barash, Paul G. (2009). Clinical Anesthesia. Lippincott Williams & Wilkins. ISBN 9780781787635. Diarsipkan dari versi asli tanggal 20 February 2017. Diakses tanggal 8 December 2014.

[10] Bangen, Hans: Geschichte der medikamentösen Therapie der Schizophrenie. Berlin 1992, ISBN 3-927408-82-4

[TI113-11] "[113] How well do you know your anticholinergic (antimuscarinic) drugs? | Therapeutics Initiative". Therapeutics Initiative. 10 September 2018. Diakses tanggal 20 September 2018.

[autogenerated1-12] Bersani, F. S.; Corazza, O.; Simonato, P.; Mylokosta, A.; Levari, E.; Lovaste, R.; Schifano, F. (2013). "Drops of madness? Recreational misuse of tropicamide collyrium; early warning alerts from Russia and Italy". General Hospital Psychiatry. 35 (5): 571–3. doi:10.1016/j.genhosppsych.2013.04.013. PMID 23706777.

[pmid24484978-13] Carroll FI, Blough BE, Mascarella SW, Navarro HA, Lukas RJ, Damaj MI (2014). "Bupropion and Bupropion Analogs as Treatments for CNS Disorders". Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. Advances in Pharmacology. 69. hlm. 177–216. doi:10.1016/B978-0-12-420118-7.00005-6. ISBN 9780124201187. PMID 24484978.

[Dwoskin2014-14] Dwoskin, Linda P. (29 January 2014). Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. Elsevier Science. hlm. 177–216. ISBN 978-0-12-420177-4. Diarsipkan dari versi asli tanggal 20 March 2017.

[TasmanKay2011-15] Tasman, Allan; Kay, Jerald; Lieberman, Jeffrey A.; First, Michael B.; Maj, Mario (11 October 2011). Psychiatry. John Wiley & Sons. ISBN 978-1-119-96540-4. Diarsipkan dari versi asli tanggal 20 March 2017.

[pmid15356218-16] Damaj, M. I.; Flood, P; Ho, K. K.; May, E. L.; Martin, B. R. (2004). "Effect of Dextrometorphan and Dextrorphan on Nicotine and Neuronal Nicotinic Receptors: In Vitro and in Vivo Selectivity". Journal of Pharmacology and Experimental Therapeutics. 312 (2): 780–5. doi:10.1124/jpet.104.075093. PMID 15356218.

[pmid16563374-17] Lee, Jun-Ho; Shin, Eun-Joo; Jeong, Sang Min; Kim, Jong-Hoon; Lee, Byung-Hwan; Yoon, In-Soo; Lee, Joon-Hee; Choi, Sun-Hye; Lee, Sang-Mok; Lee, Phil Ho; Kim, Hyoung-Chun; Nah, Seung-Yeol (2006). "Effects of dextrorotatory morphinans on α3β4 nicotinic acetylcholine receptors expressed in Xenopus oocytes". European Journal of Pharmacology. 536 (1–2): 85–92. doi:10.1016/j.ejphar.2006.02.034. PMID 16563374.

[pmid10869398-18] Hernandez, S. C.; Bertolino, M; Xiao, Y; Pringle, K. E.; Caruso, F. S.; Kellar, K. J. (2000). "Dextromethorphan and Its Metabolite Dextrorphan Block α3β4 Neuronal Nicotinic Receptors". The Journal of Pharmacology and Experimental Therapeutics. 293 (3): 962–7. PMID 10869398.

[19] Shytle, RD; Penny, E; Silver, AA; Goldman, J; Sanberg, PR (Jul 2002). "Mecamylamine (Inversine): an old antihypertensive with new research directions". Journal of Human Hypertension. 16 (7): 453–7. doi:10.1038/sj.jhh.1001416  . PMID 12080428.

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