Gallamine triethiodide

891.53

891.176819

200-605-1

Q3254X40X2

DTXSID5023089

WHITE AMORPHOUS POWDER|White crystals from acetone/water

29239000

27.7

3.5

powder

0.983g/cm3

147.5 °C

502.6°C at 760 mmHg

125.9ºC

1.501

H2O: 100 mg/mL

2-8°C

LD50 oral in rabbit: 100mg/kg

ODORLESS

HYGROSCOPIC

NONH for all modes of transport

3

22-36/37/38

26-36-45

BS1100000

Xn

P301 + P312 + P330-P305 + P351 + P338

H302-H315-H319-H335

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

IN ANESTHETIZED PT, IV ADMIN OF DIAZEPAM MAY INCR INTENSITY & PROLONG DURATION OF NEUROMUSCULAR BLOCKADE PRODUCED BY GALLAMINE TRIETHIODIDE. CLINICAL REPORTS...ARE CONFLICTING.../&/ THERE ARE INSUFFICIENT DATA TO EXPLAIN POSSIBLE MECHANISM FOR GALLAMINE TRIETHIODIDE-DIAZEPAM INTERACTION.|NEUROMUSCULAR BLOCKADE PRODUCED BY TUBOCURARINE WAS PROLONGED IN TWO THYROTOXIC PT RECEIVING HIGH DOSES (120 MG/DAY FOR 14 DAYS) OF PROPRANOLOL. ... ALTHOUGH THERE IS NO DOCUMENTATION, THE NONDEPOLARIZING MUSCLE RELAXANT GALLAMINE TRIETHIODIDE...ALSO SHOULD INTERACT WITH PROPRANOLOL.|NEOMYCIN &...RELATED ANTIBIOTICS PRODUCE NEUROMUSCULAR TRANSMISSION FAILURE WHICH MAY CAUSE PROLONGED RESP DEPRESSION OR APNEA IN SURGICAL PT TREATED CONCURRENTLY WITH TUBOCURARINE &...NEUROMUSCULAR DEPRESSANTS. ...ADDITIVE NEUROMUSCULAR DEPRESSION.../REPORTED TO OCCUR WITH GALLAMINE TRIETHIODIDE/.|QUINIDINE, ADMIN PARENTERALLY SHORTLY AFTER OR SIMULTANEOUSLY WITH TUBOCURARINE, MAY ENHANCE OR CAUSE RECURRENT NEUROMUSCULAR EFFECTS OF TUBOCURARINE, RESULTING IN PROLONGATION OR INTENSIFICATION OF RESP DEPRESSION & APNEA. ... GALLAMINE TRIETHIODIDE...HAS BEEN SHOWN TO INTERACT WITH QUINIDINE IN ANIMALS.|For more Interactions (Complete) data for GALLAMINE TRIETHIODIDE (25 total), please visit the HSDB record page.

LD50 Rat ip 23,200 ug/kg|LD50 Rat sc 28,500 ug/kg|LD50 Rat iv 5100 ug/kg|LD50 Rat intraduodenal 380 mg/kg|For more Non-Human Toxicity Values (Complete) data for GALLAMINE TRIETHIODIDE (13 total), please visit the HSDB record page.

For use as adjuncts to anesthesia to induce skeletal muscle relaxation and to facilitate the management of patients undergoing mechanical ventilation

Neuromuscular Nondepolarizing Agents; Nicotinic Antagonists|A NEUROMUSCULAR BLOCKING DRUG SIMILAR IN ITS ACTIONS & USES TO TUBOCURARINE CHLORIDE. ...IN GENERAL, IT HAS VERY LITTLE ACTION ON AUTONOMIC GANGLIA, BUT IT USUALLY BLOCKS CARDIAC VAGUS... IT ALSO DOES NOT RELEASE HISTAMINE /IN LOW DOSES/.|... IT HAS NO PERCEPTIBLE EFFECT ON NEWBORN INFANTS WHEN USUAL DOSES ARE GIVEN FOR CESAREAN SECTION & VAGINAL DELIVERY & TONE OF UTERUS IS NOT AFFECTED.|...HAS BEEN REPORTED TO REDUCE OCULAR PRESSURE SLIGHTLY IN PT.|For more Therapeutic Uses (Complete) data for GALLAMINE TRIETHIODIDE (9 total), please visit the HSDB record page.

THE NEUROMUSCULAR BLOCKING AGENTS ARE POTENTIALLY HAZARDOUS DRUGS. ... THEY SHOULD BE ADMINISTERED TO PATIENTS ONLY BY ANESTHESIOLOGISTS & OTHER CLINICIANS WHO HAVE HAD EXTENSIVE TRAINING IN THEIR USE & IN A SETTING WHERE FACILITIES FOR RESPIRATORY & CARDIOVASCULAR RESUSCITATION ARE IMMEDIATELY AT HAND. /NEUROMUSCULAR BLOCKING AGENTS/|IT SHOULD BE USED CAUTIOUSLY IF TACHYCARDIA PREEXISTS. .../SINCE IT/ IS ELIMINATED MAINLY BY RENAL EXCRETION...ITS ACTION MAY BE PROLONGED IF THERE IS RENAL DYSFUNCTION.|... /IT SHOULD NOT/ BE USED IN PT WITH RENAL DISEASE.|CROSS SENSITIVITY BETWEEN ALCURONIUM & D-TUBOCURARINE OCCURS & SIMILAR SITUATION MAY EXIST FOR SUXAMETHONIUM & GALLAMINE.|For more Drug Warnings (Complete) data for GALLAMINE TRIETHIODIDE (6 total), please visit the HSDB record page.

Gallamine Triethiodide is a nondepolarizing neuromuscular blocking drug (NDMRD) used as an adjunct to anesthesia to induce skeletal muscle relaxation. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. Muscle groups differ in their sensitivity to these types of relaxants with ocular muscles (controlling eyelids) being most sensitive, followed by the muscles of the neck, jaw, limbs and then abdomen. The diaphragm is the least sensitive muscle to NDMRDs. Although the nondepolarizing neuromuscular blocking drugs do not have the same adverse effects as succinylcholine, their onset of action is slower. They also have a longer duration of action, making them more suitable for maintaining neuromuscular relaxation during major surgical procedures.

Drugs that interrupt transmission at the skeletal neuromuscular junction without causing depolarization of the motor end plate. They prevent acetylcholine from triggering muscle contraction and are used as muscle relaxants during electroshock treatments, in convulsive states, and as anesthesia adjuvants. (See all compounds classified as Neuromuscular Nondepolarizing Agents.)|Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses. (See all compounds classified as Nicotinic Antagonists.)

STUDIES HAVE DEMONSTRATED THAT GALLAMINE IS EXCRETED IN DOG URINE AT RATE FASTER THAN OTHER MUSCLE RELAXANTS. .../IT/ DID NOT CROSS BLOOD-CEREBROSPINAL FLUID BARRIER. OTHER STUDIES...HAVE DETECTED GALLAMINE IN CEREBROSPINAL FLUID IN CONCN APPROACHING THOSE IN PLASMA DURING 1ST HR AFTER IV INJECTION. /GALLAMINE/|GALLAMINE IS ELIMINATED MAINLY BY RENAL EXCRETION...|... GALLAMINE CROSSES PLACENTAL BARRIER ...|TRACE AMT OF GALLAMINE APPEARS IN FETUS 3 MIN AFTER ADMIN. /GALLAMINE, FROM TABLE/|For more Absorption, Distribution and Excretion (Complete) data for GALLAMINE TRIETHIODIDE (6 total), please visit the HSDB record page.

.../GALLAMINE/ IS UNMETABOLIZED. /GALLAMINE/

135 minutes /From table/

It competes with acetylcholine (ACh) molecules and binds to muscarinic acetylcholine receptors on the post-synaptic membrane of the motor endplate. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. It blocks the action of ACh and prevents activation of the muscle contraction process. It can also act on nicotinic presynaptic acetylcholine receptors which inhibits the release of ACh.|GALLAMINE TRIETHIODIDE...PRODUCES SKELETAL MUSCLE RELAXATION BY COMBINING WITH RECEPTOR SITE AT NEUROMUSCULAR JUNCTION & BLOCKING ACTION OF NEUROTRANSMITTER ACETYLCHOLINE.|IN RAT PHRENIC NERVE-DIAPHRAGM GALLAMINE HAD NO SIGNIFICANT EFFECTS ON ELECTROGENIC PROPERTIES OF EXCITABLE MEMBRANES OF MOTOR NERVE TERMINALS & MUSCLE FIBERS; IT DEPRESSED RESPONSE OF POSTSYNAPTIC RECEPTORS TO ACTION OF ACETYLCHOLINE.|AT NEUROMUSCULAR JUNCTIONS IN MICE AND FROGS, FOLLOWING STEP CHANGES OF MEMBRANE POTENTIAL FROM -70 TO -130 MV, GALLAMINE (5 UMOL) IN THE PRESENCE OF ACETYLCHOLINE (3 UMOL) CAUSED AN INITIAL RAPID DECR IN CURRENT FOLLOWED BY OPENING OF CHANNELS AT A SLOWER RATE THAN WITH ACETYLCHOLINE ALONE. WHEN THE INTERNAL POTENTIAL WAS REDUCED TO -70 MV, THERE WAS A RAPID INCR IN CURRENT AT FIRST, FOLLOWED BY THE USUAL DECR WHICH WAS AGAIN SLOWER THAN NORMAL. THUS, GALLAMINE MAY PRODUCE A POTENTIAL-DEPENDENT BLOCK OF OPEN ION CHANNELS.

POISONING ... IS ALMOST ALWAYS RESULT OF CLINICAL OVERDOSAGE ... DIRECTLY RELATED FACTORS MAY ... INCL ALTERATIONS IN BODY TEMP ... ELECTROLYTE IMBALANCE, PARTICULARLY OF POTASSIUM ... /NEUROMUSCULAR BLOCKING AGENTS/|THREE CASES OF SEVERE ANAPHYLAXIS TO GALLAMINE TRIETHIODIDE ARE DESCRIBED. ALL REPORTED CASES HAVE OCCURRED IN WOMEN, & ALL CONFIRMED CASES IN AUSTRALASIA. THERE IS EVIDENCE THAT WOMEN MAY BE EXPOSED TO SOME SUBSTANCE WHICH LEAVES THEM SENSITIVE TO GALLAMINE TRIETHIODIDE.|Accidental subarachnoid injection of gallamine in an adult is followed by muscle spasms of the lower limbs and anxiety; by 3 hr the arterial pressure and pulse rate increases followed by hyperthermia, profuse sweating, intense hyperesthesia, loss of consciousness, and pinpoint pupils. Within 24 hr the muscle spasms lessen.

Flaxedil

GALLAMINE TRIETHIODIDE, USP (FLAXEDIL), IS AVAIL AS STERILE SOLN CONTAINING 20 OR 100 MG/ML.

Pharmaceutical incompatibilities: meperidine hydrochloride (solutions must not be mixed /with gallamine triethiodide/).

THREE SERIES OF 2-DIMENSIONAL THIN LAYER CHROMATOGRAPHIC SEPARATIONS WERE CARRIED OUT USING 8 DRUGS OF CHEM-TOXICOLOGICAL RELEVANCE POSSSESSING QUATERNARY OR OTHER AMINO FUNCTIONS. SOLVENTS FOR 1ST RUN WERE METHANOL, ETHANOL (96%) OR ACETONE, FOR 2ND DIMENSION METHANOL-1 N HCL (1:1), ETHANOL-1 N HCL (1:1) OR ACETONE-1 N HCL (1:1) WERE USED. ALL COMBINATIONS WERE SUITABLE FOR SEPARATION OF QUATERNARY AMMONIUM FUNCTIONS FROM OTHER AMINES.|A GENERAL APPROACH TO CHROMATOGRAPHIC ANALYSIS OF QUATERNARY AMMONIUM COMPD ON SILICA GEL THIN LAYER IS DESCRIBED. QUATERNARY CATIONS MIGRATE AS ION PAIRS WITH BROMIDE OR IODIDE AS COUNTER IONS. METHANOL OR CHLOROFORM-METHANOL MIXTURES SERVE AS DEVELOPING SOLVENTS.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients