Analeptics are the classes of stimulant drugs which are generally used to treat respiratory depression particularly in case of coma and fainting. Most of them are central nervous system stimulants with very censorious therapeutic indexes. They stimulate respiration and can have resuscitative value in breathing failure or apnoea. Since most of them have narrow margin of safety, hence they are meticulously preferred for the purpose of treatment. Doxapram is one of the best known analeptic medicament approved for human use in the treatment of drug induced respiratory depression and apnoea of prematurity. It has tendency to stimulate chemoreceptors in carotid body of carotid artery and respiratory centre in medulla oblongata. It blocks potassium channel also. Unlike other analeptic drugs, doxapram hasn’t drug dependence or addictive property. Although, almitrine is a safe drug, but doxapram has better clinical preference in the treatment of apnoea and respiratory depression. Chronic maladies of obstructive pulmonary ailments are generally treated by almitrine, which is a well tolerated through oral route. It enhances respiration by agonising peripheral chemoreceptors of receptors of carotid body without impairing the quality of sleep.
Cite this article:
Jeetendra Kumar Gupta. Safety and Toxicological profile of Contemporary Analeptics: Prodigious Focus on Doxapram and Almitrine. Research J. Pharm. and Tech. 2021; 14(2):1104-1108. doi: 10.5958/0974-360X.2021.00199.2
1. Dekhuijzen PNR, Machiels HA, Heunks LMA, Van Der Heijden HFM, Van Balkom RHH. Athletes and doping: Effects of drugs on the respiratory system. Thorax. 1999;54(11):1041–1046.
2. Wax PM. Analeptic use in clinical toxicology: A historical appraisal. Journal of Toxicology - Clinical Toxicology. 1997; 35(2): 203–209.
3. Cotton JF. The latest pharmacologic ventilator. Anesthesiology. 2014;121(3):442–444.
4. Gupta JK, Shah K, Mishra P. Environmental pollutants and aggressive climatic conditions: combination scaffolds of brain stroke. Current Science. 2018; 114 (10): 2034-38.
5. Yost CS. A new look at the respiratory stimulant doxapram. CNS Drug Reviews. 2006;12(3–4):236–249.
6. Docherty JR. Pharmacology of stimulants prohibited by the World Anti-Doping Agency (WADA). British Journal of Pharmacology. 2008; 154(3): 606–622.
7. Caldwell JA, Caldwell JL, Smith JK, Brown DL. Modafinil’s effects on simulator performance and mood in pilots during 37 h without sleep. Aviation Space and Environmental Medicine. 2004;75(9):777–784.
8. Leong GB, Shaner AL, Silva JA. Narcolepsy, paranoid psychosis, and analeptic abuse. Psychiatric Journal of the University of Ottawa: Revue de psychiatrie de l’Universite d’Ottawa. 1989;14(3):481–3.
9. Richards JR, Davis MT, Curry MR, Tsushima JH, McKinney HE. Doxapram reversal of suspected gamma-hydroxybutyrate–induced coma. American Journal of Emergency Medicine. 2017;35(3): 517.e1-517.e3.
10. Kruszynski S, Stanaitis K, Brandes J, Poets CF, Koch H. Doxapram stimulates respiratory activity through distinct activation of neurons in the nucleus hypoglossus and the pre-bötzinger complex. Journal of Neurophysiology. 2019; 121(4): 1102–1110.
11. Bales MJ, Timpe EM. Respiratory stimulant use in chronic obstructive pulmonary disease. Annals of Pharmacotherapy. 2004;38(10):1722–1725.
12. Zhao J, Gonzalez F, Mu D. Apnea of prematurity: From cause to treatment. European Journal of Pediatrics. 2011;170(9):1097–1105.
13. Coper H, Herrmann WM. Psycho stimulants, analeptics, nootropics: An attempt to differentiate and assess drugs designed for the treatment of impaired brain functions. Pharmacopsychiatry. 1988; 21(5):211–217.
14. Steinkellner T, Freissmuth M, Sitte HH, Montgomery T. The ugly side of amphetamines: Short-and long-term toxicity of 3,4-methylenedioxymethamphetamine (MDMA, ’Ecstasy’), methamphetamine and d-amphetamine. Biological Chemistry. 2011; 392(1–2):103–115.
15. Tseng W, Sutter ME, Albertson TE. Stimulants and the lung: Review of literature. Clinical Reviews in Allergy and Immunology. 2014;46(1):82–100.
16. Nehlig A. Effects of respiratory stimulants on cerebral metabolism and blood flow. Neonatology. 1994;65(3–4):258–264.
17. Whitsett TL. The cardiovascular effects of caffeine. Primary Cardiology. 1986;12(2):36–44.
18. Taylor R. Chemical stimulants to respiration. Applied therapeutics. 1963;5: 1019–21 PASSIM.
19. Hutas I. Respiratoty analeptics in the treatment of chronic respiratory failure. Therapia Hungarica (English edition). 1964;12: 109–14.
20. Dodson ME, Fryer JM. Postoperative effects of methylphenidate. British Journal of Anaesthesia. 1980;52(12):1265–1270.
21. Zetler G. Drug-induced catalepsy as influenced by convulsant and anticonvulsant drugs. Neuropharmacology. 1973;12(8):741–749.
22. De Waal CG, Hutten GJ, Kraaijenga J V., De Jongh FH, Van Kaam AH. Doxapram treatment and diaphragmatic activity in preterm infants. Neonatology. 2019;115(1):85–88.
23. Chiumello D, Coppola S, Ferrari E. A Simple Effective Pharmacological Treatment of Hypoxemia During One-Lung Ventilation. Journal of Clinical Medicine. 2019;8(8):1139.
24. Gillart T, Bazin JE, Cosserant B, Guelon D, Aigouy L, Mansoor O, Schoeffler P. Combined: nitric oxide inhalation, prone positioning and almitrine infusion improve oxygenation in severe ARDS. Canadian Journal of Anaesthesia. 1998;45(5 I):402–409.