Wikipedia

Teofilin/efedrin

Teofilin/efedrin (INN)[1] adalah formulasi kombinasi dosis tetap dari teofilin, suatu antagonis reseptor adenosin; dengan efedrin, suatu agen pelepas norepinefrin dan agen simpatomimetik yang bekerja secara tidak langsung; yang telah digunakan sebagai bronkodilator dalam pengobatan asma dan sebagai dekongestan hidung.[3][4][5][6][7][8][9][2] Obat ini pertama kali dipelajari dan digunakan untuk mengobati asma pada tahun 1930-an atau 1940-an dan kombinasi kedua obat tersebut kemudian digunakan secara luas.[9][7][10] Rasio teofilin dan efedrin 5:1 biasanya digunakan dalam kombinasi obat-obatan tersebut.[11] Penelitian selanjutnya menemukan bahwa kombinasi tersebut tidak lebih efektif untuk asma daripada teofilin saja tetapi menghasilkan lebih banyak efek samping.[9][1][12][7]

Kombinasi
Teofilin Antagonis reseptor adenosin
Efedrin Agen pelepas norepinefrin
Data klinis
Nama dagang Asmasolon, Bufakris, Franol, Neo Napacin, dll[1][2]
Kat. kehamilan ?
Status hukum ?
Pengenal
Nomor CAS 15766-94-6
Kode ATC ?
PubChem CID 86278139
ChemSpider 34992091
UNII LMS3EG69X8

Kombinasi teofilin, efedrin, dan fenobarbital juga telah banyak digunakan untuk mengobati asma.[12][13][14][15] Banyak kombinasi tersebut telah dipasarkan dengan berbagai nama merek. Teofilin juga telah dipasarkan dalam kombinasi dengan simpatomimetik serupa efedrin lainnya seperti rasefedrin dan pseudoefedrin serta dengan barbiturat lainnya seperti amobarbital dan butabarbital.[15] Kombinasi teofilin, efedrin, dan hidroksizin telah dipasarkan juga.[16][17][18] Kombinasi teofilin, efedrin, dan barbiturat kemudian dihapuskan demi kombinasi teofilin dan efedrin saja.[2][1] Kombinasi dosis tetap teofilin dan efedrin ditinggalkan setelah tahun 1970-an karena tidak memungkinkan titrasi dosis dalam terapi asma akibat toksisitas efedrin.[19]

Efek teofilin/efedrin sebagai obat peningkat performa dalam latihan fisik dan olahraga telah dipelajari.[20][21] Penggunaan kombinasi teofilin/efedrin telah menyebabkan diskualifikasi atlet elit karena efedrin dilarang dalam olahraga kompetitif.[22]

Referensi

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  1. ^ a b c d Mansfield PR (1991). "Classifying improvements to drug marketing and justifications for claims of efficacy". The International Journal of Risk & Safety in Medicine. 2 (4): 171–184. doi:10.3233/JRS-1991-2401. PMID 23511913. Dr Lathem, Sterling's Vice President for Scientific Affairs replied to MaLAM that "Franol is approved for marketing in the United Kingdom in a formulation containing theophylline and ephedrine. We have initiated a re-formulation worldwide to make all Franol formulations consistent with those of the U.K.". Weinberger and Bronsky (1974) compared theophylline and ephedrine separately and combined. They concluded that "the inclusion of ephedrine resulted in no further benefit but did appear to increase the frequency of adverse effects" [26]. 
  2. ^ a b c Head S (2022). "A breath of fresh air". Prescriber. 33 (2): 41–42. doi:10.1002/psb.1973. ISSN 0959-6682. Amesec contained ephedrine and amylobarbitone with a whiff of aminophylline. Franol contained ephedrine and theophylline, and earlier versions also contained phenobarbital. 
  3. ^ Elks J (2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer US. hlm. 1179. ISBN 978-1-4757-2085-3. Diakses tanggal 29 August 2024. 
  4. ^ "INN Proposed List 14". World Health Organization (WHO). 31 October 1964. Diakses tanggal 29 August 2024. 
  5. ^ National Archives (U.S.) (1978). Federal Register (dalam bahasa Jerman). Office of the Federal Register, National Archives and Records Service, General Services Administration. hlm. 12450–12382. Diakses tanggal 30 August 2024. 
  6. ^ Sims JA, doPico GA, Reed CE (July 1978). "Bronchodilating effect of oral theophylline-ephedrine combination". The Journal of Allergy and Clinical Immunology. 62 (1): 15–21. doi:10.1016/0091-6749(78)90066-0. PMID 350932. 
  7. ^ a b c Weinberger M, Bronsky E, Bensch GW, Bock GN, Yecies JJ (May 1975). "Interaction of ephedrine and theophylline". Clinical Pharmacology and Therapeutics. 17 (5): 585–592. doi:10.1002/cpt1975175585. PMID 1092514. Brown1 reported uncontrolled clinical observations suggesting the apparent effectiveness of a fixed dose combination of ephedrine and theophylline in 1940, Such preparations have become very popular, though a search of the literature since that initial report unearthed only one controlled study (of very limited scope) that suggested additive effect from drug combination.15 
  8. ^ Pinnas JL, Schachtel BP, Chen TM, Roseberry HR, Thoden WR (March 1991). "Inhaled epinephrine and oral theophylline-ephedrine in the treatment of asthma". Journal of Clinical Pharmacology. 31 (3): 243–247. doi:10.1002/j.1552-4604.1991.tb04969.x. PMID 2019665. 
  9. ^ a b c Stargrove M, Treasure J, McKee D (2007). Herb, Nutrient, and Drug Interactions: Clinical Implications and Therapeutic Strategies. Elsevier Health Sciences. hlm. 45. ISBN 978-0-323-02964-3. Diakses tanggal 2024-08-31. Theophylline is generally more potent than caffeine in its effects; it was often combined with ephedrine in nasal decongestant products before more selective adrenergic blockers became available. An early study found the theophylline-ephedrine combination no more effective than theophylline alone in 23 asthmatic children, whereas the ADR rate was higher for the combination than for theophylline.40 Another study of asthmatic children, however, showed no additional adverse effects from the combination. 
  10. ^ Weinberger M, Hendeles L (October 1986). "Therapeutic effect and dosing strategies for theophylline in the treatment of chronic asthma". The Journal of Allergy and Clinical Immunology. 78 (4 Pt 2): 762–768. doi:10.1016/0091-6749(86)90058-8. PMID 3534057. Theophylline has undergone a major transition in clinical use over the past 10 to 15 years. Used primarily for its cardiovascular effects in the early part of this century, theophylline was found in the 1920s to have clinically beneficial effects on acute bronchospasm.1 In the 1930s, theophylline became popular as an oral agent, particularly in fixed-dose combination with ephedrine. Its predominant use continued in this manner into the early 1970s. Since then, definition of the pharmacodynamics and pharmacokinetics of theophylline has led to its present use as a major prophylactic agent for the prevention of chronic asthma. 
  11. ^ O'Loughlin JM (March 1979). "Drug therapy of bronchial asthma". The Medical Clinics of North America. 63 (2): 391–396. PMID 35721. 
  12. ^ a b Hendeles L, Weinberger M (1980). "Avoidance of adverse effects during chronic therapy with theophylline". European Journal of Respiratory Diseases. Supplement. 109: 103–119. PMID 7002576. Until recently, combination products containing theophylline, ephedrine, and a "sedative" were the most frequently prescribed bronchodilators in the United States. Several studies, however, have documented that the combination of ephedrine and theophylline produce synergistic toxicity without significantly enhancing the therapeutic efficacy of theophylline alone (Figure 1). 
  13. ^ Khouzam H, Tan D, Gill T (2007). Handbook of Emergency Psychiatry. Elsevier Health Sciences. hlm. 53. ISBN 978-0-323-07661-6. Diakses tanggal 30 August 2024. 
  14. ^ Heinzelman RV (1972). Annual Reports in Medicinal Chemistry. ISSN. Elsevier Science. hlm. 92. ISBN 978-0-08-058351-8. Diakses tanggal 30 August 2024. 
  15. ^ a b Project Label: Alphabetical Listing by Drug Product. Department of Justice, Drug Enforcement Administration, Office of Compliance and Regulatory Affairs, Regulatory Support Division, Information Systems Section. 1979. Diakses tanggal 2024-08-31. 
  16. ^ Emergency Medical Care: A Manual for the Paramedic in the Field. Emergency Medical Care: A Manual for the Paramedic in the Field. U.S. Department of Transportation, National Highway Traffic Safety Administration. 1983. hlm. 3-PA33. Diakses tanggal 31 August 2024. 
  17. ^ Emergency Department Trends from the Drug Abuse Warning Network: Preliminary Estimates January-June 2001 with Revised Estimates 1994-2000. DHHS publication. Department of Health and Human Services, Substance Abuse and Mental Health Services Administration. 2002. hlm. 210. Diakses tanggal 31 August 2024. 
  18. ^ Mosby's Pocket Dictionary of Medicine, Nursing & Health Professions - E-Book: Mosby's Pocket Dictionary of Medicine, Nursing & Health Professions - E-Book. Elsevier Health Sciences. 2016. hlm. 810. ISBN 978-0-323-41427-2. Diakses tanggal 31 August 2024. 
  19. ^ Akazawa M, Stempel DA (2006). "Single-inhaler combination therapy for asthma: a review of cost effectiveness". PharmacoEconomics. 24 (10): 971–988. doi:10.2165/00019053-200624100-00005. PMID 17002480. The concept of using a single therapy and maximising the dose of ICS might have been driven by the desire to avoid fixed combinations. These were commonly used in the US during the 1970s with products such as Tedral®1 and Marax® that combined theophylline and ephedrine with a sedative. The earlier fixed combinations did not allow for significant dose titration, due to the toxicity of ephedrine, and thus the concept of fixed dosing combinations for asthma was relegated to an ‘unacceptable’ status. 
  20. ^ Kennedy M (January 2021). "Effects of theophylline and theobromine on exercise performance and implications for competition sport: A systematic review". Drug Testing and Analysis. 13 (1): 36–43. doi:10.1002/dta.2970. PMID 33188564 Periksa nilai |pmid= (bantuan). 
  21. ^ Sidney KH, Lefcoe NM (1978). "Effects of anti-asthmatic medication (ephedrine plus theophylline) upon the physical performance and work capacity of healthy track athletes". Can J Appl Sport Sci. 3: 93–97. 
  22. ^ Helenius I, Haahtela T (September 2000). "Allergy and asthma in elite summer sport athletes". The Journal of Allergy and Clinical Immunology. 106 (3): 444–452. doi:10.1067/mai.2000.107749. PMID 10984362. Dokter tim mulai tertarik pada asma pada atlet elit setelah Olimpiade 1972 di Munich. Pemenang lomba renang gaya bebas putra 400 m didiskualifikasi karena sejumlah besar obat terlarang, termasuk efedrin yang ditemukan dalam sampel urinalisisnya setelah lomba. Perenang tersebut telah menggunakan kombinasi teofilin dan efedrin untuk mengobati asmanya. Sejak saat itu, Komite Olimpiade AS dan Australia telah memberikan penekanan khusus pada diagnosis dan pengobatan asma yang akurat pada tim Olimpiade mereka.1,2 
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