United States - English - NLM (National Library of Medicine)
PHYSOSTIGMINE SALICYLATE- physostigmine salicylate injection
A-S Medication Solutions
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Physostigmine Salicylate Injection
Physostigmine Salicylate Injection is a derivative of the Calabar bean, and its active moiety,
physostigmine, is also known as eserine. Its chemical structure is:
It is soluble in water and a 0.5% aqueous solution has a pH of 5.8.
Physostigmine Salicylate Injection is available in 2 mL ampules, each mL containing 1 mg of
Physostigmine Salicylate in a vehicle composed of sodium metabisulfite 0.1%, benzyl alcohol 2.0% as
a preservative in Water for Injection.
Physostigmine Salicylate Injection is a reversible anticholinesterase which effectively increases the
concentration of acetylcholine at the sites of cholinergic transmission. The action of acetylcholine is
normally very transient because of its hydrolysis by the enzyme, acetylcholinesterase. Physostigmine
Salicylate Injection inhibits the destructive action of acetylcholinesterase and thereby prolongs and
exaggerates the effect of the acetylcholine.
Physostigmine Salicylate Injection contains a tertiary amine and easily penetrates the blood brain barrier,
while an anticholinesterase, such as neostigmine, which has a quaternary ammonium ion is not capable
of crossing the barrier. Physostigmine Salicylate Injection can reverse both central and peripheral
anticholinergia. The anticholinergic syndrome has both central and peripheral signs and symptoms.
Central toxic effects include anxiety, delirium, disorientation, hallucinations, hyperactivity and seizures.
Severe poisoning may produce coma, medullary paralysis and death. Peripheral toxicity is characterized
by tachycardia, hyperpyrexia, mydriasis, vasodilation, urinary retention, diminution of gastrointestinal
motility, decrease of secretion in salivary and sweat glands, and loss of secretions in the pharynx,
bronchi, and nasal passages.
Dramatic reversal of the effects of anticholinergic symptoms can be expected in minutes after the
intravenous administration of Physostigmine Salicylate Injection, if the diagnosis is correct and the
patient has not suffered anoxia or other insult. The duration of action of Physostigmine Salicylate
Injection is relatively short, approximately 45 to 60 minutes.
Numerous drugs and some plants produce the anticholinergic syndrome either directly or as a side
effect; this undesirable or potentially dangerous phenomenon may be brought about by either
therapeutic doses or overdoses of the drugs. Such drugs include among others, atropine, other
derivatives of the belladonna alkaloids, tricyclic antidepressants, phenothiazines, and antihistamines.
INDICATIONS AND USAGE:
To reverse the effect upon the central nervous system, caused by clinical or toxic dosages of drugs
capable of producing the anticholinergic syndrome.
Physostigmine Salicylate Injection should not be used in the presence of asthma, gangrene, diabetes,
cardiovascular disease, mechanical obstruction of the intestine or urogenital tract or any vagotonic
state, and in patients receiving choline esters and depolarizing neuromuscular blocking agents
For post-anesthesia, the concomitant use of atropine with physostigmine salicylate is not recommended,
since the atropine antagonizes the action of physostigmine.
Contains sodium bisulfite, a sulfite that may cause allergic-type reactions including anaphylactic
symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The
overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite
sensitivity is seen more frequently in asthmatic than in non-asthmatic people.
If excessive symptoms of salivation, emesis, urination and defecation occur, the use of Physostigmine
Salicylate Injection should be terminated. If excessive sweating or nausea occur, the dosage should be
Intravenous administration should be at a slow, controlled rate, no more than 1 mg per minute (see
dosage). Rapid administration can cause bradycardia, hypersalivation leading to a respiratory
difficulties and possible convulsions.
An overdosage of Physostigmine Salicylate Injection can cause a cholinergic crisis.
Because of the possibility of hypersensitivity in an occasional patient, atropine sulfate injection should
always be at hand since it is an antagonist and antidote for physostigmine.
USAGE IN PREGNANCY:
Safe use in pregnancy and lactation has not been established; therefore, use in pregnant women, nursing
mothers or women who may become pregnant requires that possible benefits be weighed against
possible hazards to mother and child.
Nausea, vomiting and salivation; can be offset by reducing dosage. Bradycardia and convulsions, if
intravenous administration is too rapid. See DOSAGE AND ADMINISTRATION.
Can cause a cholinergic crisis. Appropriate antidote is atropine sulfate.
DOSAGE AND ADMINISTRATION:
Past Anesthesia Care: 0.5 to 1.0 mg intramuscularly or intravenously. INTRAVENOUS
ADMINISTRATION SHOULD BE AT A SLOW CONTROLLED RATE OF NO MORE THAN 1
MG PER MINUTE. Dosage may be repeated at intervals of 10 to 30 minutes if desired patient response
is not obtained.
OVERDOSAGE OF DRUGS THAT CAUSE ANTICHOLINERGIC:
2.0 mg intramuscularly or INTRAVENOUSLY AT SLOW CONTROLLED RATE (SEE ABOVE).
Dosage may be repeated if life threatening signs, such as arrhythmia, convulsions or coma occurs.
Recommended dosage is 0.02 mg/kg; intramuscularly or by slow intravenous injection, no more than 0.5
mg per minute. If the toxic effects persist, and there is no sign of cholinergic effects, the dosage may
be repeated at 5 to 10 minute intervals until a therapeutic effect is obtained or a maximum of 2 mg
dosage is attained.
IN ALL CASES OF POISONING, THE USUAL SUPPORTIVE MEASURES SHOULD BE
NDC: 50090-4406-0 2 mL in a AMPULE / 1 in a BAG
Manufactured by: Akorn, Inc. Lake Forest, IL 60045 Store at 20° to 25°C (68° to 77°F) [see USP
Controlled Room Temperature].
physostigmine salicylate injection
Product T ype
HUMAN PRESCRIPTION DRUG
Ite m Code (Source )
NDC:50 0 9 0 -440 6 (NDC:17478 -510 )
A-S Medication Solutions
Route of Administration
Active Ingredient/Active Moiety
Basis of Strength
Stre ng th
PHYSO STIGMINE SALICYLATE (UNII: 20 46 ZRO9 VU) (PHYSOSTIGMINE -
UNII:9 U1VM8 40 SP)
in 1 mL
Stre ng th
so dium meta bisulfite (UNII: 4VON5FNS3C)
benzyl a lco ho l (UNII: LKG8 49 4WBH)
wa ter (UNII: 0 59 QF0 KO0 R)
Marketing Start Date
Marketing End Date
NDC:50 0 9 0 -440 6 -0
1 in 1 BAG
0 7/0 1/20 19
2 mL in 1 AMPULE; Type 0 : No t a Co mbinatio n Pro duct
Marke ting Cate gory
Application Numbe r or Monograph Citation
Marke ting Start Date
Marke ting End Date
unappro ved drug o ther
0 8 /10 /20 10
A-S Medication Solutions (830016429)
Ad d re s s
Busine ss Ope rations
A-S Medicatio n So lutio ns
8 30 0 16 429
RELABEL(50 0 9 0 -440 6 ) , REPACK(50 0 9 0 -440 6 )