Doxapram

Doxapram
Clinical data
Routes of; administration	Intravenous
ATC code	R07AB01 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 1-ethyl-4- (2-morpholin-4-ylethyl)- 3,3-diphenyl-pyrrolidin-2-one;
CAS Number	309-29-5 ;
PubChem CID	3156;
DrugBank	DB00561 ;
ChemSpider	3044 ;
UNII	94F3830Q73;
KEGG	D07873 ;
ChEBI	CHEBI:681848 ;
ChEMBL	ChEMBL1754 ;
CompTox Dashboard (EPA)	DTXSID2022963 ;
ECHA InfoCard	100.005.653
Chemical and physical data
Formula	C24H30N2O2
Molar mass	378.516 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C4N(CC)CC(CCN1CCOCC1)C4(c2ccccc2)c3ccccc3;
	InChI InChI=1S/C24H30N2O2/c1-2-26-19-22(13-14-25-15-17-28-18-16-25)24(23(26)27,20-9-5-3-6-10-20)21-11-7-4-8-12-21/h3-12,22H,2,13-19H2,1H3 ; Key:XFDJYSQDBULQSI-UHFFFAOYSA-N ;
	(verify)

Doxapram hydrochloride (marketed as Dopram, Stimulex or Respiram) is a respiratory stimulant, or analeptic. Administered intravenously, doxapram stimulates an increase in tidal volume, and respiratory rate.

Mechanism of action

A vial of doxapram

Doxapram stimulates chemoreceptors in the carotid bodies of the carotid arteries, which in turn, stimulates the respiratory center in the brainstem.

Appearance

Doxapram is a white to off-white, odorless, crystalline powder that is stable in light and air. It is soluble in water, sparingly soluble in alcohol and practically insoluble in ether. Injectable products have a pH from 3.5–5. Benzyl alcohol or chlorobutanol is added as a preservative agent in commercially available preparations.

Uses

Doxapram is used in intensive care settings to stimulate the respiratory rate in patients with respiratory failure. It may be useful for treating respiratory depression in patients who have taken excessive doses of drugs such as opioids which may fail to respond adequately to treatment with naloxone.^[1]

It is equally as effective as pethidine in suppressing shivering after surgery.^[2]

Doxapram has been used as a reversal agent after general anesthesia in captive sharks and rays, but it must be used with caution, as the animals can become excitatory as a side effect.^[3]

Side effects

Side effects include high blood pressure, anxiety, rapid heart rate, tremor, sweating, and vomiting. Convulsions have been reported. Its use is relatively contraindicated in people with coronary artery disease, epilepsy, and high blood pressure. It is also contraindicated in newborns and small children, mainly due to the presence of benzyl alcohol, which is included as a preservative.

References

^ "Buprenorphine Drug Data Sheet" (PDF). Reckitt Benckiser Pharmaceuticals, Inc.
^ Singh P, Dimitriou V, Mahajan RP, Crossley AW (November 1993). "Double-blind comparison between doxapram and pethidine in the treatment of postanaesthetic shivering". British Journal of Anaesthesia. 71 (5): 685–688. doi:10.1093/bja/71.5.685. PMID 8251281.
^ Smith MF (2017). The Elasmobranch Husbandry Manual II: Recent Advances in the Care of Sharks, Rays and Their Relatives. Ohio Biological Survey. p. 292. Retrieved 2022-03-30.

[1] "Buprenorphine Drug Data Sheet" (PDF). Reckitt Benckiser Pharmaceuticals, Inc.

[2] Singh P, Dimitriou V, Mahajan RP, Crossley AW (November 1993). "Double-blind comparison between doxapram and pethidine in the treatment of postanaesthetic shivering". British Journal of Anaesthesia. 71 (5): 685–688. doi:10.1093/bja/71.5.685. PMID 8251281.

[3] Smith MF (2017). The Elasmobranch Husbandry Manual II: Recent Advances in the Care of Sharks, Rays and Their Relatives. Ohio Biological Survey. p. 292. Retrieved 2022-03-30.

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