I.C.I. 35868 - The effect of a change of formulation on the incidence of pain after intravenous injection. 1977

B Kay, and G Rolly

I.C.I. 35868 is a promising new intravenous induction agent, but intravenous injection of the initial 2% formulation frequently caused pain. The solvent vehicle of the 2% formulation, which contained Cremophor E.L. and ethanol, was therefore investigated to see if this could be the cause of the pain. Twenty volunteers received both 5 ml isotonic saline and 5 ml solvent vehicle intravenously. The injection of saline never caused pain, but the solvent caused mild or moderate pain in 9 patients. I.C.I. 35868 was therefore reformulated in a 1% solution, excluding ethanol from the solvent. When intravenous injection of I.C.I. 35868 1% was compared to methohexitone 1% in 24 patients, both agents caused pain. Four out of 12 patients reveiving I.C.I. 35868 1% felt pain, with a total pain "score" of 6, but 6 out of 12 patients who received methohexitone 1%, felt pain, with a total pain "score" of 12. In no instance was intravenous injection followed by persistant pain, or evidence of thrombosis or phlebitis.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D008723 Methohexital An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. Methohexitone,Brevimytal Natrium,Brevital,Brietal,Brietal-Sodium,Methohexital Sodium,Methohexital, Monosodium Salt,Brietal Sodium,Monosodium Salt Methohexital,Natrium, Brevimytal,Sodium, Methohexital
D010146 Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. Suffering, Physical,Ache,Pain, Burning,Pain, Crushing,Pain, Migratory,Pain, Radiating,Pain, Splitting,Aches,Burning Pain,Burning Pains,Crushing Pain,Crushing Pains,Migratory Pain,Migratory Pains,Pains, Burning,Pains, Crushing,Pains, Migratory,Pains, Radiating,Pains, Splitting,Physical Suffering,Physical Sufferings,Radiating Pain,Radiating Pains,Splitting Pain,Splitting Pains,Sufferings, Physical
D010636 Phenols Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D004341 Drug Evaluation Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals. Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000771 Anesthesia, Intravenous Process of administering an anesthetic through injection directly into the bloodstream. Anesthesias, Intravenous,Intravenous Anesthesia,Intravenous Anesthesias
D000777 Anesthetics Agents capable of inducing a total or partial loss of sensation, especially tactile sensation and pain. They may act to induce general ANESTHESIA, in which an unconscious state is achieved, or may act locally to induce numbness or lack of sensation at a targeted site. Anesthetic,Anesthetic Agents,Anesthetic Drugs,Anesthetic Effect,Anesthetic Effects,Agents, Anesthetic,Drugs, Anesthetic,Effect, Anesthetic,Effects, Anesthetic
D014677 Pharmaceutical Vehicles A carrier or inert medium used as a solvent (or diluent) in which the medicinally active agent is formulated and or administered. (Dictionary of Pharmacy, 1986) Pharmaceutical Vehicle,Vehicle, Pharmaceutical,Vehicles, Pharmaceutical

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