This paper describes case reports and pharmacokinetic information regarding the continuous intravenous administration of naloxone in treatment of narcotic overdose. Continuous naloxone infusion has been used successfully in acutely narcotized patients, and a review of the pharmacodynamic and pharmacokinetic properties of naloxone indicate the reasons for this mode of administration. Summaries of clinical studies in support of the infusion method are given. A naloxone protocol is outlined.
GilbertPEMartinWR.The effects of morphine and nalorphine-like drugs in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog. J Pharmacol Exp Ther1976; 196: 66–82.
2.
MartinWREadesCGThompsonJAThe effects of morphine and nalorphine-like drugs on the non-dependent and morphine-dependent chronic spinal dog. J Pharmacol Exp Ther1976; 197: 517–32.
3.
MartinWR.Naloxone. Ann Intern Med1976; 85: 765.
4.
MartinWRJasinskiDRManskyPA.Naltrexone, an antagonist for the treatment of heroin dependence. Arch Gen Psychiatry1973; 128: 784–91.
5.
McGilliardKLTakemoriAE.Antagonism by naloxone of narcotic-induced respiratory depression and analgesia. J Pharmacol Exp Ther1978; 207: 497–503.
6.
GosselinREHodgeHCSmithRPGleasonMN.Clinical toxicology of commercial products, 4th ed.Baltimore: Williams & Wilkins, 1976: 237–42.
7.
Physicians' desk reference. Oradell, NJ: Medical Economics Co., 1981: 881.
8.
NelsonJ.A comparison of intravenous naloxone infusion to intermittent intravenous dosing (thesis). Austin: University of Texas, August, 1976.
9.
EvansLEJTreatment of drug overdose with naloxone, a specific narcotic antagonist. Lancet1973; 1: 452.
KurklandAAMcCabeL.Rapid detoxification of the narcotic addict with naloxone hydrochloride. J Clin Pharmacol1976; 16: 66–75.
12.
KastrupEDBoydJR.Facts and comparisons. St. Louis: Facts and Comparisons, Inc., 1979: 246,246a.
13.
FishmanJRoffwargHHellmanLDisposition of naloxone 7,8-3H in normal and narcotic-dependent men. J Pharmacol Exp Ther1973; 187: 575–80.
14.
BerkowitzBADisposition of naloxone: use of a new radioimmunoassay. J Pharmacol Exp Ther1975; 195: 499–504.
15.
NgaiSHPharmacokinetics of naloxone in rats and in man: basis for its potency and short duration of action. Anesthesiology1976; 44: 398–401.
16.
MisraALPhysiological disposition and bio-transformation of 14C-naloxone in the rat. Pharmacologist1974; 16: 225.
17.
BerkowitzBAThe disposition of morphine in surgical patients. Clin Pharmacol Ther1975; 17: 629–35.
18.
WeinsteinSHPfefferMSchorJMAbsorption and distribution of naloxone in rats after oral and intravenous administration. J Pharm Sci1973; 62: 1416–9.
19.
FujimotoJM.Isolation of naloxone-3-glucuronide from human urine. Proc Soc Exp Biol Med1970; 133: 317–9.
20.
WeinsteinSHMetabolites of naloxone in human urine. J Pharm Sci1971; 60: 1567–8.
21.
ConeEF.General procedure for the isolation and identification of 6- and 6-β-hydroxy metabolites of narcotic agonists and antagonists with a hydromorphone structure. J Chromatogr1976; 129: 355–61.
22.
RoerigSPreliminary characterization of enzymes for reduction of naloxone and naltrexone in rabbit and chicken liver. Drug Metab Dispos1976; 4: 53–8.
23.
ChatterjieNInturrisiCEDaytonHBBlumbergH.Stereospecific synthesis of the 6-β-hydroxy metabolites of naltrexone and naloxone. J Med Chem1975; 18: 490–2.
24.
FujimatoJMRoerigSWangRHChatterjieNInturrisiCE.Narcotic antagonistic activity of several metabolites of naloxone and naltrexone tested in morphine dependent mice. Proc Soc Exp Biol Med1975; 148: 443–8.
25.
SimonQEricJ. In: EssmanWBValzelliL, eds. Current developments in psychopharmacology, vol. 4. New York: Spectrum Publications, 1977: 33–69.
26.
EvansJMHoggMIJLunnJNDegree and duration of reversal by naloxone of effects of morphine in conscious subjects. Br Med J1974; 2: 589–91.
27.
BerkowitzBA.The relationship of pharmacokinetics to pharmacological activity: morphine, methadone, and naloxone. Clin Pharmacokinet1976; 1: 219–30.
28.
KutterEHerzATeschemacherHJHessR.Structure-activity correlation of morphine-like analgesics based on efficiencies following intravenous and intraventricular application. J Med Chem1970; 13: 801–5.
29.
KaufmanJJSemoNMKoskiWSMicroelec-trometric titration measurement of the pKas and partition and drug distribution coefficients of narcotic antagonists and their pH and temperature dependence. J Med Chem1976; 18: 647–55.
30.
PertCBSnyderSH.Opiate receptor: demonstration in nervous tissue. Science1973; 179: 1011–4.
31.
LeeCYEffects of Na+, K+, Mg++, and Ca++ on the saturable binding of H dihydromorphine and H naloxone in vitro. J Pharmacol Exp Ther1977; 202: 166–73.
32.
LeeCYSaturable binding of dihydromorphine and naloxone to rat brain tissue in vitro. J Pharmacol Exp Ther1975; 194: 583–92.
33.
WaldronVDMethadone overdose treated with naloxone infusion. JAMA1973; 255: 53.
34.
JohnstoneREReversal of morphine anesthesia by naloxone. Anesthesiology1974; 41: 361–7.