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Lithium Citrate

FDA Drug Information • Also known as: Lithium

Brand Names
Lithium
Route
ORAL
Dosage Form
SOLUTION
Product Type
HUMAN PRESCRIPTION DRUG

⚠ Boxed Warning (Black Box)

WARNING: LITHIUM TOXICITY Lithium toxicity is closely related to serum lithium concentrations, and can occur at doses close to therapeutic concentrations. Facilities for prompt and accurate serum lithium determinations should be available before initiating treatment [see Dosage and Administration (2.3) , Warnings and Precautions (5.1) ] WARNING: LITHIUM TOXICITY See full prescribing information for complete boxed warning. Lithium toxicity is closely related to serum lithium concentrations, and can occur at doses close to therapeutic concentrations. Facilities for prompt and accurate serum lithium determinations should be available before initiating therapy ( 2.3 , 5.1 ).

Description

11 DESCRIPTION Each 5 mL of solution for oral administration contains lithium ion (Li + ), 8 mEq (equivalent to amount of lithium in 300 mg of lithium carbonate), alcohol 0.3% v/v and the following other inactive ingredients: citric acid, purified water, artificial cherry flavor, sodium benzoate and sorbitol solution. May also contain sodium hydroxide for pH adjustment. Lithium Oral Solution, USP is a palatable oral dosage form of lithium ion. It is prepared in solution from trilithium citrate tetrahydrate and citric acid in a ratio approximately di-lithium citrate. Lithium is an element of the alkali-metal group with atomic number 3, atomic weight 6.94, and an emission line at 671 nm on the flame photometer. The empirical formula for Lithium Citrate is C 6 H 5 Li 3 O 7 ; molecular weight 209.93. Lithium acts as an antimanic.

What Is Lithium Citrate Used For?

1 INDICATIONS AND USAGE Lithium is a mood stabilizing agent indicated as monotherapy for the treatment of bipolar I disorder: Treatment of acute manic and mixed episodes in patients 7 years and older [see Clinical Studies (14) ] Maintenance treatment in patients 7 years and older [see Clinical Studies (14) ] Lithium is a mood-stabilizing agent indicated as monotherapy for the treatment of bipolar I disorder: Treatment of acute manic and mixed episodes in patients 7 years and older ( 1 ) Maintenance treatment in patients 7 years and older ( 1 )

Dosage and Administration

2 DOSAGE AND ADMINISTRATION Recommended starting dosage for adults and pediatric patients over 30 kg ( 2.2 ): Oral Solution: 8mEq lithium (5 mL) three times daily Recommended starting dosage for pediatric patients 20 to 30 kg ( 2.2 ): Oral Solution: 8mEq (5 mL), twice daily Obtain serum lithium concentration assay after 3 days, drawn 12 hours after the last oral dose and regularly until patient is stabilized. Acute Manic or Mixed Episodes (patients 7 years and older): Titrate to serum lithium concentrations 0.8 to 1.2 mEq/L ( 2.2 ). Maintenance Treatment for Bipolar I Disorder (patients 7 years and older): Titrate to serum lithium concentrations 0.8 to 1 mEq/L ( 2.2 ). Pre-treatment Screening: Evaluate renal function, vital signs, electrolytes, thyroid function, concurrent medications, and pregnancy status ( 2.1 ). Mild to Moderate Renal Impairment (Cler 30 to 89 mL/min): Start with dosages less than those for patients with normal renal function, titrate slowly with frequent monitoring ( 2.5 ). Severe Renal Impairment (Cler<30mL/min): Avoid use of lithium ( 2.5 ). 2.1 Pre-treatment Screening Before initiating treatment with lithium, renal function, vital signs, serum electrolytes, and thyroid function should be evaluated. Concurrent medications should be assessed, and if the patient is a woman of childbearing potential, pregnancy status and potential should be considered. 2.2 Recommended Dosage See Table 1 for dosage recommendations for acute and maintenance treatment of bipolar I disorder in adult and pediatric patients (7 to 17 years). Obtain serum lithium concentration assay after 3 days, drawn 12 hours after the last oral dose and regularly until patient is stabilized. Fine hand tremor, polyuria, and thirst may occur during initial therapy for the acute manic phase and may persist throughout treatment. Nausea and general discomfort may also appear during the first few days of lithium administration. These adverse reactions may subside with continued treatment, concomitant administration with food, or temporary reduction or cessation of dosage. Table 1. Lithium Dosing for Bipolar I Disorder Patient Group Formulation Starting Dose Dose Titration Acute Goal Maintenance Goal Serum Level Usual Dose Serum Level Usual Dose Adult and Pediatric Patients over 30 kg Liquid 8 mEq(5 mL) three times daily 8 mEq(5 mL) every 3 days 1.8 to 1.2 mEq/L 16 mEq(10 mL) two to three times daily 1.8 to 1.2 mEq/L 8 to16 mEq (5 to 10 mL) two to three times daily Pediatric Patients 20 to 30 kg Liquid 8 mEq(5 mL) twice daily 8 mEq(5 mL) weekly 16 to 40 mEq (10 to 25 mL) in divided doses daily 16 to 32 mEq (10 to 20 mL) in divided doses daily Each 5 mL of Lithium Oral Solution contains 8 mEq lithium ion (Li + ) which is equivalent to the amount of lithium in 300 mg of lithium carbonate. See Table 2 for lithium carbonate and lithium oral solution dose conversion. Table 2. Lithium Carbonate and Lithium Oral Solution Dose Conversion Lithium Carbonate Tablets or Capsules...

Side Effects (Adverse Reactions)

6 ADVERSE REACTIONS The following adverse reactions are described in greater detail in other sections: Acute Lithium Toxicity [see Warnings and Precautions (5.1) ] Lithium-Induced Polyuria [see Warnings and Precautions (5.2) ] Hyponatremia [see Warnings and Precautions (5.3) ] Lithium-Induced Chronic Kidney Disease [see Warnings and Precautions (5.4) ] Encephalopathic Syndrome [see Warnings and Precautions (5.5) ] Serotonin Syndrome [see Warnings and Precautions (5.6) ] Hypothyroidism or Hyperthyroidism [see Warnings and Precautions (5.7) ] Hypercalcemia and Hyperparathyroidism [see Warnings and Precautions (5.8) ] Unmasking of Brugada Syndrome [see Warnings and Precautions (5.9) ] Pseudotumor Cerebri [see Warnings and Precautions (5.10) ] Common Adverse Reactions: Adult Patients: fine hand tremor, polyuria, mild thirst, nausea, general discomfort during initial treatment ( 6 ) Pediatric Patients (7-17 years): nausea/vomiting, polyuria, thyroid abnormalities, tremor, thirst/polydipsia, dizziness, rash/ dermatitis, ataxia/gait disturbance, decreased appetite, and blurry vision ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Precision Dose, Inc. by email at [email protected] or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Pediatric Patients (7 to 17 years): Bipolar I Disorder: The following findings are based on an 8-week, placebo-controlled study for acute manic or mixed episodes of bipolar I disorder in pediatric patients 7 to 17 years (N=81). In this study, lithium was administered at daily doses ranging from 300 to 3600 (mean dose 1483 mg ± 584) with serum levels ranging from 0 to 2.0 (mean level 0.98 mEq/L ± 0.47). Common Adverse Reactions (incidence ≥ 5% and at least twice the rate of placebo): nausea/vomiting, polyuria, thyroid abnormalities, tremor, thirst/polydipsia, dizziness, rash/dermititis, ataxia/gait disturbance, decreased appetite, and blurry vision. Adverse Reactions Occurring at an Incidence of 2% or More in Lithium-Treated Pediatric Patients: Adverse reactions associated with the use of lithium (incidence of 2% or greater, rounded to the nearest percent, and lithium incidence greater than placebo) that occurred during acute therapy (up to 8-weeks in pediatric patients with bipolar disorder) are shown in Table 3. Table 3: Adverse Reactions Reported in 2% or More or Pediatric Patients on Lithium and That Occurred at Greater Incidence Than in the Placebo Group in the 8-Week Acute Bipolar Trial System Organ Class/Preferred Term Placebo N = 28% Lithium N = 53% Gastrointestinal Disorders Nausea/vomiting 29 57 General Disorders Fatigue 4 26 Genitourinary Disorders Polyuria (including Enuresis) 14 38 Investigations Increased TSH 0 25 Metabolism and nutrition disorders Thirst/polydipsia 11 28 Decreased appetite 4 9 Nervous system disorder Ataxia/gait disturbance 0 13 Blurry vision 0 9 Disorientation 0 6 Dizziness 7 23 Tremor 7 32 Skin and subcutaneous tissue disorders Rash/dermatitis 0 13 Adult Patients: The following adverse reactions have been identified following use of lithium. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Central Nervous System: tremor, muscle hyperirritability (fasciculations, twitching, clonic movements of whole limbs), hypertonicity, ataxia, choreoathetotic movements, hyperactive deep tendon reflexes, extrapyramidal symptoms including acute dystonia, cogwheel rigidity, blackout spells, epileptiform seizures, slurred speech, dizziness, vertigo, downbeat nystagmus, incontinence of urine or feces, somnolence, psychomotor retardation,...

Drug Interactions

7 DRUG INTERACTIONS Diuretics, NSAID, renin-angiotensin system antagonists, or metronidazole may increase lithium serum concentrations. Recommend frequent monitoring of serum lithium concentration and adjust dosage when necessary. ( 2.3 , 7.1 ) Serotonergic Agents: Increased risk of serotonin syndrome when co administered with lithium. ( 5.6 , 7.1 ) Antipsychotics: There have been reports of neurologic adverse reactions in patients treated with lithium and an antipsychotic, ranging from extrapyramidal symptoms to neuroleptic malignant syndrome. ( 5.5 , 7.1 ) 7.1 Drugs Having Clinically Important Interactions with Lithium Table 4: Clinically Important Drug Interactions with Lithium Diuretics Clinical Impact: Diuretic-induced sodium loss may reduce lithium clearance and increase serum lithium concentrations. Intervention: More frequent monitoring of serum electrolyte and lithium concentrations. Reduce lithium dosage based on serum lithium concentration and clinical response [see Dosage and Administration (2.3) , Warning and Precautions (5.3) ] Non-Steroidal Anti-inflammatory Drugs(NSAID) Clinical Impact: NSAID decrease renal blood flow, resulting in decreased renal clearance and increase serum lithium concentrations. Intervention: More frequent serum lithium concentration monitoring. Reduce lithium dosage based on serum lithium concentration and clinical response [see Dosage and Administration (2.3) ]. Renin-Angiotensin System Antagonists Clinical Impact: Concomitant use increase steady-state serum lithium concentrations. Intervention: More frequent monitoring of serum lithium concentrations. Reduce lithium dosage based on serum lithium concentration and clinical response [see Dosage and Administration (2.3) ]. Serotonergic Drugs Clinical Impact: Concomitant use can precipitate serotonin syndrome. Intervention: Monitor patients for signs and symptoms of serotonin syndrome, particularly during lithium initiation. If serotonin syndrome occurs, consider discontinuation of lithium and/or concomitant serotonergic drugs [see Warnings and Precautions (5.6) ]. Nitroimidazole Antibiotics Clinical Impact: Concomitant use may increase serum lithium concentrations due to reduced renal clearance. Intervention: More frequent monitoring of serum lithium concentration. Reduce lithium dosage based on serum lithium concentration and clinical response [see Dosage and Administration (2.3) ]. Acetazolamide, Urea, Xanthine Preparations, Alkalinizing Agents Clinical Impact: Concomitant use can lower serum lithium concentrations by increasing urinary lithium excretion. Intervention: More frequent serum lithium concentration monitoring. Increase lithium dosage based on serum lithium concentration and clinical response [see Dosage and Administration (2.3) ]. Methyldopa, Phenytoin and Carbamazepine Clinical Impact: Concomitant use may increase risk of adverse reactions of these drugs. Intervention: Monitor patients closely for adverse reactions of methyldopa, phenytoin, and...

Contraindications

4 CONTRAINDICATIONS Lithium is contraindicated in patients with known hypersensitivity to any inactive ingredient in the lithium citrate products [see Adverse Reactions (6) ]. Known hypersensitivity to any inactive ingredient in the drug product. ( 4 )

Pregnancy and Breastfeeding

8.1 Pregnancy Risk Summary: Lithium may cause harm when administered to a pregnant woman. Early voluntary reports to international birth registries suggested an increase in cardiovascular malformations, especially for Ebstein's anomaly, with first trimester use of lithium. Subsequent case-control and cohort studies indicate that the increased risk for cardiac malformations is likely to be small; however, the data are insufficient to establish a drug-associated risk. There are concerns for maternal and/or neonatal lithium toxicity during late pregnancy and the postpartum period [see Clinical Considerations ]. Published animal developmental and toxicity studies in mice and rats report an increased incidence of fetal mortality, decreased fetal weight, increased fetal skeletal abnormalities, and cleft palate (mouse fetuses only) with oral doses of lithium that produced serum concentrations similar to the human therapeutic range. Other published animal studies report adverse effects on embryonic implantation in rats after lithium administration. Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population(s) is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations: Dose Adjustments During Pregnancy and the Postpartum Period: If the decision is made to continue lithium treatment during pregnancy, serum lithium concentrations should be monitored and the dosage adjusted during pregnancy. Two to three days prior to delivery, lithium dosage should be decreased or discontinued to reduce the risk of maternal and/or neonatal toxicity. Lithium may be restarted in the post-partum period at preconception doses in medically stable patients as long as serum lithium levels are closely monitored [see Dosage and Administration (2.4) , Warnings and...

Overdosage

10 OVERDOSAGE The toxic concentrations for lithium (≥1.5 mEq/L) are close to the therapeutic concentrations [see Warnings and Precautions (5.1 ) ]. At lithium concentrations greater than 3 mEq/L, patients may progress to seizures, coma, and irreversible brain damage. Treatment: For current information on the management of poisoning or overdosage, contact the National Poison Control Center at 1 -800-222-1222 or www.poison.org No specific antidote for lithium poisoning is known. Mild symptoms of lithium toxicity can usually be treated by reduction in dose or cessation of the drug. In severe cases of lithium poisoning, the goal of treatment is elimination of this ion from the patient. Administration of gastric lavage should be performed, but use of activated charcoal is not recommended as it does not significantly absorb lithium ions. Hemodialysis is the treatment of choice as it is an effective and rapid means of removing lithium in patients with severe toxicity. As an alternative option, urea, mannitol and aminophylline can induce a significant increase in lithium excretion. Appropriate supportive care for the patient should be undertaken. Patients with impaired consciousness should have their airway protected and it is critical to correct any volume depletion or electrolyte imbalance. Patients should be monitored to prevent hypernatremia while receiving normal saline and careful regulation of kidney function is of utmost importance. Serum lithium concentrations should be closely monitored as there may be a rebound in serum lithium concentrations as a result of delayed diffusion from the body tissues. Likewise, during the late recovery phase, lithium should be re-administered with caution taking into account the possible release of significant lithium stores in body tissues.

How Supplied

16 HOW SUPPLIED/STORAGE AND HANDLING Lithium Oral Solution USP, 8 mEq per 5 mL. Lithium Oral Solution USP is supplied as a clear, colorless solution. NDC 68094-077-62 5 mL per unit dose cup Thirty (30) cups per shipper Store and Dispense Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). [See USP Controlled Room Temperature.] Dispense in a tight, child-resistant container as defined in the USP/NF.

About This Information

This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.

What are side effects?

Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.

What are drug interactions?

Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.