Absorption, Distribution and Excretion
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.

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Metabolism / Metabolites
.../GALLAMINE/ IS UNMETABOLIZED. /GALLAMINE/

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Biological Half-Life
135 minutes /From table/

Interactions
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.

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Non-Human Toxicity Values
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.

J Pharmacol Exp Ther.1986 Jan;236(1):219-23.

A synthetic nondepolarizing blocking drug. 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. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
A synthetic nondepolarizing blocking drug. 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. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)

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

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Mechanism of Action
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.

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Therapeutic Uses
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.

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Drug Warnings
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.

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Pharmacodynamics
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.

C30H60I3N3O3

891.53

891.176

65-29-2

6172

White to yellow solid powder

0.983g/cm3

502.6ºC at 760 mmHg

235ºC (dec.)

125.9ºC

1.501

0

6

21

39

489

0

REEUVFCVXKWOFE-UHFFFAOYSA-K

InChI=1S/C30H60N3O3.3HI/c1-10-31(11-2,12-3)22-25-34-28-20-19-21-29(35-26-23-32(13-4,14-5)15-6)30(28)36-27-24-33(16-7,17-8)18-9;;;/h19-21H,10-18,22-27H2,1-9H3;3*1H/q+3;;;/p-3

2-[2,3-bis[2-(triethylazaniumyl)ethoxy]phenoxy]ethyl-triethylazanium triiodide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: 50 mg/mL (56.08 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)