Candocuronium iodide

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Candocuronium iodide
Clinical data
Other namesChandonium iodide; HS-310
Pregnancy
category
  • Not applicable
Routes of
administration		IV
ATC code
  • none
Legal status
Legal status
  • Discontinued from clinical development
Pharmacokinetic data
Bioavailability100% (IV)[citation needed]
Identifiers
  • (4aS,4bR,8S,10aR,10bS,12aS)-1,1,10a,12a-tetramethyl-8-(1-methylpyrrolidin-1-ium-1-yl)-3,4,4a,4b,5,7,8,9,10,10b,11,12-dodecahydro-2H-naphtho[2,1-f]quinolin-1-ium diiodide
JSmol)
  • [I-].[I-].C\53=C/C[C@@H]1[C@H](CC[C@]2([C@H]1CCC[N+]2(C)C)C)[C@@]3(C)CC[C@H]([N+]4(C)CCCC4)C/5
  • InChI=1S/C26H46N2.2HI/c1-25-14-12-21(28(5)17-6-7-18-28)19-20(25)10-11-22-23(25)13-15-26(2)24(22)9-8-16-27(26,3)4;;/h10,21-24H,6-9,11-19H2,1-5H3;2*1H/q+2;;/p-2/t21-,22+,23-,24-,25-,26-;;/m0../s1 ☒N
  • Key:GGAGIPMNQXAXNH-XDMKMBKMSA-L ☒N
 ☒NcheckY (what is this?)  (verify)

Candocuronium iodide (

neuromuscular-blocking drug. Its use within anesthesia for endotracheal intubation and for providing skeletal muscle relaxation during surgery or mechanical ventilation was briefly evaluated in clinical studies in India, though further development was discontinued due to attendant cardiovascular effects, primarily tachycardia that was about the same as the clinically established pancuronium bromide.[2][3][4][5] Candocuronium demonstrated a short duration in the body, but a rapid onset of action. It had little to no ganglion blocking activity, with a greater potency than pancuronium.[1]

Background

As with other neuromuscular-blocking agents, candocuronium preferentially antagonizes competitively the

succinylcholine).[citation needed
]

Design of candocuronium

The mono- and bis-quaternary azasteroid series of compounds to which candocuronium belongs are based on the same principle that led to aminosteroids such as

editorializing][10][11][12][13]

Modifications to the candocuronium design

Candocuronium did not provide the desired profile,[

editorializing] HS-692, HS-693, HS-704 and HS-705,[clarification needed][14] whose onset and duration were indinguishable from candocuronium, but all demonstrated profound vagolytic effects and much weaker potencies than candocuronium.[11] To improve on potency, further modifications of the candocuronium nucleus were undertaken,[clarification needed] leading to the identification of yet another potentially useful compound, HS-626.[15] Upon further preclinical evaluation,[16]
HS-626 demonstrated a slightly more desirable neuromuscular-blocking profile than that of candocuronium, but its overall improvement was insufficient to warrant advancement to clinical testing.

Modifications at 3- and 16-positions of androstane nucleus

The discovery of candocuronium led to numerous related neuromuscular-blocking agents with short durations of action but also having attendant undesirable cardiovascular effects. The Marshall group then explored other modifications at the 3- and 16-positions of the androstane nucleus,[17][18] and yielded an agent that can go through expanded evaluation to clinical testing.

References

  1. ^
    S2CID 37704229
    .
  2. PMID 2151453
    .
  3. PMID 3397166
    .
  4. PMID 2148735
    .
  5. ^ Suri YV (1984). Chandonium-iodide. New non-depolarising muscle relaxant. In: "Anaesthesiology. Clinical Pharmacology" Suri YV, Singh D (Eds.) New Delhi: Vani Educational Books; 28-35.
  6. S2CID 7700031
    .
  7. ^
    PMID 4472321
    .
  8. S2CID 46013073
    .
  9. PMID 4715215
    .
  10. S2CID 21840628
    .
  11. ^
    S2CID 37032460
    .
  12. PMID 4077122
    .
  13. PMID 4077123
    .
  14. doi:10.1039/P19790000305
    .
  15. doi:10.1039/p19790002451
    .
  16. S2CID 26115020
    .
  17. PMID 11311750
    .
  18. PMID 12446049
    .

External links
Retrieved from "https://en.wikipedia.org/w/index.php?title=Candocuronium_iodide&oldid=1208443085"