LITHIUM CATION

First marketed in 1921

Details

Stereochemistry	ACHIRAL
Molecular Formula	Li
Molecular Weight	6.94
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	1

SHOW SMILES / InChI

Structure Search

SMILES

[Li+]

InChI

InChIKey=HBBGRARXTFLTSG-UHFFFAOYSA-N

InChI=1S/Li/q+1

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/017812s028,018421s027lbl.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/12459525 | http://www.isaltis.com/en/module/99999689/28/lithium_gluconate | https://www.ncbi.nlm.nih.gov/pubmed/18330588
Curator's Comment:: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19538681 | https://www.ncbi.nlm.nih.gov/pubmed/23371914 | http://www.rsc.org/periodic-table/element/3/lithium

Lithium gluconate is used in oligotherapy for psychological problems (normothymia, manic depressive psychosis) under special biological surveillance and more specifically when the lithium rate is to be controlled. Lithium gluconate ointment was significantly more effective than placebo, with a complete clinical remission after 4 and 8 weeks respectively in the treatment of seborrhoeic dermatitis. At low concentration (1.6 mM), Li enhanced TNFalpha secretion, whereas, at higher concentration (5 mM), Li significantly enhanced IL10 expression and secretion in skin models. However, there was no significant modulation of Li on IL6 and TGFbeta1 secretion. Moreover, Li at 5 mM significantly decreased TLR2 and TLR4 expressions by differentiated keratinocytes. As Li concentration during topical treatment is probably closer to 5 mM than to 1 mM, the therapeutic effect of Li gluconate in seborrhoeic dermatitis may be explained by two anti-inflammatory actions: an increased expression and secretion of IL10 and a decreased expression of TLR2 and TLR4 by keratinocytes.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Glycogen synthase kinase-3 beta 49 Target ID: CHEMBL262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24094818	Inhibitor 7728	6.53 µM [IC50]
Glycogen synthase kinase-3 beta 49 Target ID: CHEMBL262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8710892	Inhibitor 7728	2.0 mM [Ki]
3'(2'),5'-bisphosphate nucleotidase 1 30 Target ID: O95861 Gene ID: 10380.0 Gene Symbol: BPNT1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10675562	Inhibitor 7728	0.3 mM [IC50]
neurotrophin signaling pathway 31 Target ID: GO:0038179 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19538689	Modulator 780

Conditions

Condition	Modality	Targets	Highest Phase	Product
Bipolar disorder, manic episodes 38 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/017812s028,018421s027lbl.pdf	Primary		Approved 8043	LITHIUM CARBONATE Approved Use Lithium is indicated in the treatment of manic episodes of Bipolar Disorder. Launch Date -1.26316798E11

PubMed

Title	Date	PubMed
Renal failure associated with acetazolamide therapy for glaucoma.	1975 Apr	1124417
Sodium bicarbonate and systemic hemodynamics in volunteers anesthetized with halothane.	1975 May	236705
Obsolete but dangerous antacid preparations.	1978 Jan	625456
Organophosphate poisoning: modifications in acid base equilibrium and use of sodium bicarbonate as an aid in the treatment of toxicity in dogs.	1983 Feb	6298988
Calcification of superficial scalp veins secondary to intravenous infusion of sodium bicarbonate and calcium chloride.	1983 Jul	6309480
Bupivacaine cardiotoxicity in a pregnant patient with mitral valve prolapse.	1983 Jun	6859605
[Effect of antacids on mineral metabolism].	1983 Mar	6858403
Experimental amitriptyline intoxication: electrophysiologic manifestations and management.	1984 Jan-Feb	6199617
Treatment of ventricular tachyarrhythmias resulting from amitriptyline toxicity in dogs.	1984 Nov	6092619
Urothelial injury to the rabbit bladder from various alkaline and acidic solutions used to dissolve kidney stones.	1986 Jul	3712608
Experimental amitriptyline intoxication: treatment of cardiac toxicity with sodium bicarbonate.	1986 Sep	3017159
Incidence of hypotension associated with epidural anesthesia using alkalinized and nonalkalinized lidocaine for cesarean section.	1987 Nov	3662059
Summation effects of uracil and other promoters on epithelial lesion development in the F344 rat urinary bladder initiated by N-butyl-N-(4-hydroxybutyl)nitrosamine.	1991 Nov	1752781
Reversal of desipramine toxicity in rats using drug-specific antibody Fab' fragment: effects on hypotension and interaction with sodium bicarbonate.	1992 Mar	1312169
Sodium bicarbonate alleviates penile pain induced by intracavernous injections for erectile dysfunction.	1993 May	8386779
Alkalinization of local anesthesia with sodium bicarbonate--preferred method of local anesthesia.	1994 Jan	8284866
Effects of magnesium sulfate and lidocaine in the treatment of ventricular arrhythmias in experimental amitriptyline poisoning in the rat.	1994 Mar	8125001
Reversal of flecainide-induced ventricular arrhythmia by hypertonic sodium bicarbonate in dogs.	1995 May	7755819
Neutralizing pH of lidocaine reduces pain during Norplant system insertion procedure.	1995 May	7628204
Reduction of desipramine cardiotoxicity and prolongation of survival in rats with the use of polyclonal drug-specific antibody Fab fragments.	1995 Sep	7661425
Effect of calcium chloride and 4-aminopyridine therapy on desipramine toxicity in rats.	1996	8800187
Pathophysiology and treatment of cocaine toxicity: implications for the heart and cardiovascular system.	1996 Dec	8987970
Metabolic alkalosis and myoclonus from antacid ingestion.	1996 Jun	8835608
Oral sodium bicarbonate reduces proximal renal tubular peptide catabolism, ammoniogenesis, and tubular damage in renal patients.	1998 Mar	9574465
Acebutolol-induced ventricular tachycardia reversed with sodium bicarbonate.	1999	10465245
Comparative effects of sodium bicarbonate and sodium chloride on reversing cocaine-induced changes in the electrocardiogram.	1999 Dec	10598131
pH-dependent cocaine-induced cardiotoxicity.	1999 Jul	10452435
The effects of sodium bicarbonate on thioridazine-induced cardiac dysfunction in the isolated perfused rat heart.	2001 Apr	11308123
Ménière's disease in childhood.	2001 Dec 1	11700197
Renal tubular peptide catabolism in chronic vascular rejection.	2001 May-Jul	11499566
Aborted sudden death, transient Brugada pattern, and wide QRS dysrrhythmias after massive cocaine ingestion.	2001 Oct	11590577
Physostigmine, sodium bicarbonate, or hypertonic saline to treat diphenhydramine toxicity.	2002 Feb	11824763
The prevention of pain from injection of rocuronium by magnesium sulphate, lignocaine, sodium bicarbonate and alfentanil.	2003 Jun	12879672
Fanconi syndrome caused by antiepileptic therapy with valproic Acid.	2004 Jul	15230715
Prevention of contrast-induced nephropathy with sodium bicarbonate: a randomized controlled trial.	2004 May 19	15150204
Alkaline induces metallothionein gene expression and potentiates cell proliferation in Chinese hamster ovary cells.	2005 Dec	15965962
Reversal of citalopram-induced junctional bradycardia with intravenous sodium bicarbonate.	2005 Jan	15767228
Quinidine cardiotoxicity.	2005 May	15837031
Nalidixic acid overdose and metabolic acidosis.	2006 Mar	17175866
Acute renal failure due to phenazopyridine (Pyridium) overdose: case report and review of the literature.	2006 Nov	16897003
Deregulation of the p16-cyclin D1/cyclin-dependent kinase 4-retinoblastoma pathway involved in the rat bladder carcinogenesis induced by terephthalic acid-calculi.	2006 Oct	16896691
Comparison of usefulness of sodium bicarbonate versus sodium chloride to prevent contrast-induced nephropathy in patients undergoing an emergent coronary procedure.	2007 Sep 1	17719320
G418-mediated ribosomal read-through of a nonsense mutation causing autosomal recessive proximal renal tubular acidosis.	2008 Sep	18614622
Iatrogenic Flecainide toxicity.	2010 Dec	20736205
Randomized controlled trial: lisinopril reduces proteinuria, ammonia, and renal polypeptide tubular catabolism in patients with chronic allograft nephropathy.	2010 Jan 15	20061926
Acute propafenone toxicity after two exposures at standard dosing.	2010 Jun-Jul	20548984
Hyper-alkalinization without hyper-hydration for the prevention of high-dose methotrexate acute nephrotoxicity in patients with osteosarcoma.	2010 Nov	20155268
High sensitivity of RBL-2H3 cells to cadmium and manganese: an implication of the role of ZIP8.	2011 Jul	21509381
Evaluation of aggregating brain cell cultures for the detection of acute organ-specific toxicity.	2013 Jun	22954530
Hexavalent chromium affects sperm motility by influencing protein tyrosine phosphorylation in the midpiece of boar spermatozoa.	2016 Jan	26582256

Patents

Sample Use Guides

In Vivo Use Guide

Optimal patient response to Lithium Carbonate usually can be established and maintained with 600 mg t.i.d. Optimal patient response to Lithium Oral Solution usually can be established and maintained with 10 mL (2 full teaspoons) (16 mEq of lithium) t.i.d. Such doses will normally produce an effective serum lithium level ranging between 1.0 and 1.5 mEq/l. Dosage must be individualized according to serum levels and clinical response. Regular monitoring of the patient’s clinical state and of serum lithium levels is necessary. Serum levels should be determined twice per week during the acute phase, and until the serum level and clinical condition of the patient have been stabilized.

Route of Administration: Oral

In Vitro Use Guide

Although lithium at a high concentration (10 mM) activated β-catenin in different types of neurons, β-catenin shifted to the nucleus at a therapeutically relevant concentration (1 mM) only in thalamic neurons, both in vivo and in vitro.

Name

Type

Language

LITHIUM CATION

Common Name

English

LITHIUM, ION (LI1+)

Common Name

English

LITHIUM ION

Common Name

English

Classification Tree Code System Code

WHO-ATC

N05AN01