مضادات الكولين

الأدوية المضادة للكولين anticholinergic (مضادات كولينية Cholinergic Antagonist) هي أحد مجموعات الأدوية العلاجية التي تفيد في خفض تأثيرات الأستيل كولين في الجهاز العصبي المركزي و الجهاز العصبي المحيطي .

تكون هذه الأدوية عادة مثبطات تنافسية عكوسة لأحد نمطي المستقبلات الكولينية ، و تصنف حسب نوع المستقبل الذي تؤثر فيه إلى : مضادات مسكارينية antimuscarinic agents يعمل على المستقبل الكوليني الموسكاريني ، و مضادات نيكوتينية تعمل على المستقبلات النيكوتينية .

لكن اغلبية المضادات الكولينية تندرج ضمن مجموعة المضادات الموسكارينية.

. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .

الاستخدامات الطبية

Anticholinergic drugs are used to treat a variety of conditions:

Anticholinergics generally have antisialagogue effects (decreasing saliva production), and most produce some level of sedation, both being advantageous in surgical procedures.[3][4]

Until the beginning of the 20th century anticholinergic drugs were widely used to treat psychiatric disorders.[5]


الآثار الفسيولوجية

Clinically the most significant feature is delirium, particularly in the elderly, who are most likely to be affected by the toxidrome.[9]

الآثار الجانبية

Long-term use may increase the risk of both cognitive and physical decline.[10][11] It is unclear whether they affect the risk of death generally.[10] However, in older adults they do appear to increase the risk of death.[12]

Possible effects of anticholinergics include:

Possible effects in the central nervous system resemble those associated with delirium, and may include:

  • Confusion
  • Disorientation
  • Agitation
  • Euphoria or dysphoria
  • Respiratory depression
  • Memory problems[15]
  • Inability to concentrate
  • Wandering thoughts; inability to sustain a train of thought
  • Incoherent speech
  • Irritability
  • Mental confusion (brain fog)
  • Wakeful myoclonic jerking
  • Unusual sensitivity to sudden sounds
  • Illogical thinking
  • Photophobia
  • Visual disturbances[بحاجة لمصدر]
    • Periodic flashes of light
    • Periodic changes in visual field
    • Visual snow
    • Restricted or "tunnel vision"
  • Visual, auditory, or other sensory hallucinations
    • Warping or waving of surfaces and edges
    • Textured surfaces
    • "Dancing" lines; "spiders", insects; form constants
    • Lifelike objects indistinguishable from reality
    • Phantom smoking
    • Hallucinated presence of people not actually there (i.e., the shadow people and/or the hat man.)
  • Rarely: seizures, coma, and death
  • Orthostatic hypotension (severe drop in systolic blood pressure when standing up suddenly) and significantly increased risk of falls in the elderly population.[16]

Older patients are at a higher risk of experiencing CNS side effects.

السمية

An acute anticholinergic syndrome is reversible and subsides once all of the causative agents have been excreted. Reversible acetylcholinesterase inhibitor agents such as physostigmine can be used as an antidote in life-threatening cases. Wider use is discouraged due to the significant side effects related to cholinergic excess including seizures, muscle weakness, bradycardia, bronchoconstriction, lacrimation, salivation, bronchorrhea, vomiting, and diarrhea. Even in documented cases of anticholinergic toxicity, seizures have been reported after the rapid administration of physostigmine. Asystole has occurred after physostigmine administration for tricyclic antidepressant overdose, so a conduction delay (QRS > 0.10 second) or suggestion of tricyclic antidepressant ingestion is generally considered a contraindication to physostigmine administration.[17]

Pharmacology

Anticholinergics are classified according to the receptors that are affected:

أمثلة

Examples of common anticholinergics:

Antidotes

Physostigmine is one of only a few drugs that can be used as an antidote for anticholinergic poisoning. Nicotine also counteracts anticholinergics by activating nicotinic acetylcholine receptors. Caffeine (although an adenosine receptor antagonist) can counteract the anticholinergic symptoms by reducing sedation and increasing acetylcholine activity, thereby causing alertness and arousal.

Psychoactive uses

When a significant amount of an anticholinergic is taken into the body, a toxic reaction known as acute anticholinergic syndrome may result. This may happen accidentally or intentionally as a consequence of either recreational or entheogenic drug use, though many users find the side effects to be exceedingly unpleasant and not worth the recreational effects they experience. In the context of recreational use, anticholinergics are often called deliriants.[19]

المصادر النباتية

The most common plants containing anticholinergic alkaloids (including atropine, scopolamine, and hyoscyamine among others) are:

الاستخدام كرادع

Several narcotic and opiate-containing drug preparations, such as those containing hydrocodone and codeine are combined with an anticholinergic agent to deter intentional misuse.[27] Examples include Hydromet/Hycodan (hydrocodone/homatropine), Lomotil (diphenoxylate/atropine) and Tussionex (hydrocodone polistirex/chlorpheniramine). However, it is noted that opioid/antihistamine combinations are used clinically for their synergistic effect in the management of pain and maintenance of dissociative anesthesia (sedation) in such preparations as Meprozine (meperidine/promethazine) and Diconal (dipipanone/cyclizine), which act as strong anticholinergic agents.[28]

المراجع

  1. ^ "NERVE AGENTS". fas.org. Retrieved 2020-07-27.
  2. ^ Nair, V. Priya; Hunter, Jennifer M. (2004-10-01). "Anticholinesterases and anticholinergic drugs". Continuing Education in Anaesthesia, Critical Care & Pain (in الإنجليزية). 4 (5): 164–168. doi:10.1093/bjaceaccp/mkh045. ISSN 1743-1816.
  3. ^ 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.
  4. ^ Barash, Paul G. (2009). Clinical Anesthesia. ISBN 9780781787635. Archived from the original on 20 February 2017. Retrieved 8 December 2014.
  5. ^ Bangen, Hans: Geschichte der medikamentösen Therapie der Schizophrenie. Berlin 1992, ISBN 3-927408-82-4
  6. ^ "ATROPINE- atropine sulfate solution/ drops". DailyMed. 2017-11-20. Retrieved 2020-03-28.
  7. ^ "MYDRIACYL- tropicamide solution/ drops". DailyMed. 2019-12-13. Retrieved 2020-03-28.
  8. ^ "MYDRIACYL- tropicamide solution/ drops". DailyMed. 2019-12-13. Retrieved 2020-03-28.
  9. ^ أ ب خطأ استشهاد: وسم <ref> غير صحيح؛ لا نص تم توفيره للمراجع المسماة Migirov Datta 2020 p.
  10. ^ أ ب Fox, C; Smith, T; Maidment, I; Chan, WY; Bua, N; Myint, PK; Boustani, M; Kwok, CS; Glover, M; Koopmans, I; Campbell, N (September 2014). "Effect of medications with anti-cholinergic properties on cognitive function, delirium, physical function and mortality: a systematic review". Age and Ageing. 43 (5): 604–15. doi:10.1093/ageing/afu096. PMID 25038833.
  11. ^ Andre, L; Gallini, A; Montastruc, F; Montastruc, JL; Piau, A; Lapeyre-Mestre, M; Gardette, V (29 August 2019). "Association between anticholinergic (atropinic) drug exposure and cognitive function in longitudinal studies among individuals over 50 years old: a systematic review". European Journal of Clinical Pharmacology. 75 (12): 1631–1644. doi:10.1007/s00228-019-02744-8. PMID 31468067. S2CID 201675824.
  12. ^ Ruxton, K; Woodman, RJ; Mangoni, AA (2 March 2015). "Drugs with anticholinergic effects and cognitive impairment, falls and all-cause mortality in older adults: A systematic review and meta-analysis". British Journal of Clinical Pharmacology. 80 (2): 209–20. doi:10.1111/bcp.12617. PMC 4541969. PMID 25735839.
  13. ^ Falk, N; Cole, A; Meredith, TJ (15 March 2018). "Evaluation of Suspected Dementia". American Family Physician. 97 (6): 398–405. PMID 29671539.
  14. ^ Gray SL, Anderson ML, Dublin S, Hanlon JT, Hubbard R, Walker R, et al. (March 2015). "Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study". JAMA Internal Medicine. 175 (3): 401–407. doi:10.1001/jamainternmed.2014.7663. PMC 4358759. PMID 25621434.
  15. ^ Talan, Jamie (July–August 2008). "Common Drugs May Cause Cognitive Problems". Neurology Now. 4 (4): 10–11. doi:10.1097/01.NNN.0000333835.93556.d1. Archived from the original on 2019-06-26. Retrieved 26 June 2019.
  16. ^ "Lifeline Learning Center". Lifeline.theonlinelearningcenter.com. Archived from the original on 12 July 2012. Retrieved 8 December 2014.
  17. ^ Rosen, Peter, John A. Marx, Robert S. Hockberger, and Ron M. Walls. Rosen's Emergency Medicine: Concepts and Clinical Practice. 8th ed. Philadelphia, PA: Mosby Elsevier, 2014.
  18. ^ أ ب ت ث ج "[113] How well do you know your anticholinergic (antimuscarinic) drugs? | Therapeutics Initiative". Therapeutics Initiative. 10 September 2018. Retrieved 20 September 2018.
  19. ^ أ ب 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.
  20. ^ 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. Vol. 69. pp. 177–216. doi:10.1016/B978-0-12-420118-7.00005-6. ISBN 9780124201187. PMID 24484978. {{cite book}}: |journal= ignored (help)
  21. ^ Dwoskin, Linda P. (29 January 2014). Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. Elsevier Science. pp. 177–216. ISBN 978-0-12-420177-4. Archived from the original on 20 March 2017.
  22. ^ 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. Archived from the original on 20 March 2017.
  23. ^ 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. S2CID 149958.
  24. ^ 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.
  25. ^ 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.
  26. ^ 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.
  27. ^ "NIH DailyMed – Hydromet Syrup". Dailymed.nlm.nih.gov. Archived from the original on 2011-05-23. Retrieved 2008-08-17.
  28. ^ Zacny, James P. (2003). "Characterizing the subjective, psychomotor, and physiological effects of a hydrocodone combination product (Hycodan) in non-drug-abusing volunteers". Psychopharmacology. 165 (2): 146–156. doi:10.1007/s00213-002-1245-5. PMID 12404072. S2CID 7835794.

قالب:Acetylcholine receptor modulators

تمّ الاسترجاع من "https://www.marefa.org/w/index.php?title=مضادات_الكولين&oldid=2881294"