Dosing & Uses
Dosage Forms & Strengths
tablet, extended release
- 300mg
- 450mg
tablet
- 300mg
capsule
- 150mg
- 300mg
- 600mg
solution
- 8mEq/5mL
Bipolar Disorder
Immediate release: 900-1800 mg/day PO divided q6-8hr
Extended release: 900-1800 mg/day PO divided q12hr
Lower initial dosage may be used to minimize adverse drug reactions
Serum lithium should be monitored 12 hours after dose, twice weekly until serum concentration and clinical condition stabilize, and every other month thereafter
Increase dose as tolerated to target serum lithium concentrations of 0.8-1.2 mEq/L (acute goal) or 0.8-1.0 mEq/L (maintenance goal)
Huntington's Disease (Orphan)
Lithium citrate tetrahydrate (in reverse micelle formulation)
Orphan indication sponsor
- Medesis Pharma; L'Oree des Mas, 34 670 Baillargues, France
Administration
Preferably taken with food
Dosage Forms & Strengths
tablet, extended release
- 300mg
- 450mg
tablet
- 300mg
capsule
- 150mg
- 300mg
- 600mg
solution
- 8mEq/5mL
Bipolar Disorder (Off-label)
<7 years: Safety and efficacy not established
≥7 years (<30 kg): 300 mg PO BID; increase dose by 300 mg/day at weekly intervals based on response and tolerability; titrate dose to maintain serum trough concentration of 0.8-1.2 mEq/L
≥7 years (<30 kg): 300 mg PO TID; first week of therapy; may increase dose by 300 mg/day at weekly intervals; titrate to response to maintain serum trough concentration of 0.8-1.2 mEq/L
Extended release (≥12 years)
Fixed dosing
- <22 kg: 600 mg/day PO divided BID
- 22-41 kg 900 mg/day PO divided BID
- >41 kg: 1200 mg/day PO divided BID
- Increase dose as tolerated to target serum lithium concentrations of 0.8-1.2 mEq/L (acute goal) or 0.8-1.0 mEq/L (maintenance goal)
Weight based dosing
Dosing in elderly patients should be cautious, usually starting at low end of range
Elderly patients often respond to reduced dosage and may exhibit signs of toxicity at serum concentrations ordinarily tolerated by younger patients
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Leukocytosis (most patients)
Polyuria/polydypsia (30-50%)
Dry mouth (20-50%)
Hand tremor (45% initially, 10% after 1 year of treatment)
Confusion (40%)
Decreased memory (40%)
Headache (40%)
Muscle weakness (30% initially, 1% after 1 year of treatment)
Electrocardiographic (ECG) changes (20-30%)
Nausea, vomiting, diarrhea (10-30% initially, 1-10% after 1-2 years of treatment)
Hyperreflexia (15%)
Muscle twitch (15%)
Vertigo (15%)
1-10%
Extrapyramidal symptoms, goiter (5%)
Hypothyroidism (1-4%)
Acne (1%)
Hair thinning (1%)
Frequency Not Defined
Coma
Lethargy
Seizures
Renal toxicity
Acute lithium toxicity
Lithium-induced polyuria
Ataxia/gait disturbance
Postmarketing Reports
Dermatologic: Drying and thinning of hair, alopecia, anesthesia of skin, chronic folliculitis, xerosis cutis, psoriasis onset or exacerbation, generalized pruritus with or without rash, cutaneous ulcers, angioedema, drug reaction with eosinophilia and systemic symptoms (DRESS)
Warnings
Black Box Warnings
Toxicity is closely related to serum lithium concentrations and may occur at dosages close to therapeutic levels; monitor therapy by measuring serum lithium
Equipped facilities should be identified before initiation of therapy to provide prompt and accurate serum lithium concentration data
Contraindications
Documented hypersensitivity
Severe cardiovascular disease
Pregnancy in 1st trimester
Unstable renal function, sodium depletion, severe dehydration
Severe debilitation
Cautions
Cardiovascular disease; reports of possible association between lithium treatment and unmasking of Brugada syndrome (abnormal ECG and risk of sudden death)
Use with caution in patients with thyroid disease
Narrow therapeutic index
Risk of nephrogenic diabetes insipidus; such patients should be carefully managed to avoid dehydration with resulting lithium retention and toxicity; condition is usually reversible when lithium is discontinued
Lithium-sensitive patients may experience toxicity symptoms with serum lithium concentrations of 1-1.5 mEq/L
Lithium toxicity is closely related to serum levels and can occur at therapeutic dosages; if manifestations of toxicity occur, discontinue for 24-48 hours, then resume at lower dosage
Mainitain geriatric patients on dosages that produce serum lithium concentrations at lower end of desired range
May cause central nervous system (CNS) depression and impair ability to operate heavy machinery
Hypercalcemia reported with or without hyperparathyroidism; women and older patients are possibly at greater risk; onset does not appear to be associated with duration of therapy
Monitor changes in renal function; chronic therapy may diminish renal concentrating ability; usually reversible when lithium therapy discontinued
Use caution in debilitated patients; may increase risk of lithium toxicity
Use with caution in patients at risk for suicide
Cases consistent with nephrotic syndrome reported with use of lithium; discontinuation of lithium in patients with nephrotic syndrome has resulted in remission of nephrotic syndrome
Routine urinalysis and other tests may be used to evaluate tubular function (e.g., urine specific gravity or osmolality following a period of water deprivation, or 24-hour urine volume) and glomerular function (e.g., serum creatinine ,creatinine clearance, or proteinuria); during lithium therapy, progressive or sudden changes in renal function, even within normal range, indicate the need for re-evaluation of treatment
An encephalopathic syndrome (characterized by weakness, lethargy, fever, tremulousness and confusion, extrapyramidal symptoms, leukocytosis, elevated serum enzymes, BUN, and FBS) has reported in a few patients treated with lithium plus a neuroleptic, most notably haloperidol; in some instances, the syndrome was followed by irreversible brain damage; because of possible causal relationship patients receiving such combined therapy or patients with organic brain syndrome or other CNS impairment should be monitored closely for early evidence of neurologic toxicity and treatment discontinued promptly if such signs appear; encephalopathic syndrome may be similar to or the same as Neuroleptic Malignant Syndrome (NMS)
Lithium may prolong effects of neuromuscular blocking agents; neuromuscular blocking agents should be given with caution to patients receiving lithium
Lithium toxicity
- The risk of lithium toxicity is increased in patients with significant renal or cardiovascular disease, severe debilitation or dehydration, or sodium depletion, and for patients receiving prescribed medications that may affect kidney function, such as angiotensin converting enzyme inhibitors (ACE inhibitors), angiotensin receptor blockers (ARBs), diuretics (loops and thiazides) and NSAIDs; for these patients, consider starting with lower doses and titrating slowly while frequently monitoring serum lithium concentrations and signs of lithium toxicity
- Neurological signs of lithium toxicity range from mild neurological adverse reactions such as fine tremor, lightheadedness, lack of coordination, and weakness; to moderate manifestations like giddiness, apathy, drowsiness, hyperreflexia, muscle twitching, ataxia, blurred vision, tinnitus, and slurred speech; severe manifestations such as clonus, confusion, seizure, coma, and death may occur; in rare cases, neurological sequelae may persist despite discontinuing lithium treatment and may be associated with cerebellar atrophy
- Cardiac manifestations involve electrocardiographic changes, such as prolonged QT interval, ST and T-wave changes and myocarditis; renal manifestations include urine concentrating defect, nephrogenic diabetes insipidus, and renal failure; respiratory manifestations include dyspnea, aspiration pneumonia, and respiratory failure; gastrointestinal manifestations include nausea, vomiting, diarrhea, and bloating; no specific antidote for lithium poisoning known
- Monitor for signs and symptoms of toxicity; if symptoms occur, decrease dosage or discontinue lithium treatment
Serotonin syndrome
- Lithium can precipitate serotonin syndrome, a potentially life-threatening condition; risk is increased with concomitant use of other serotonergic drugs (including selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors, triptans, tricyclic antidepressants, fentanyl, tramadol, tryptophan, buspirone, and St. John’s Wort) and with drugs that impair metabolism of serotonin, eg, MAOIs
- Monitor all patients taking lithium for emergence of serotonin syndrome; discontinue treatment with lithium and any concomitant serotonergic agents immediately if above symptoms occur and initiate supportive symptomatic treatment; if concomitant use of lithium with other serotonergic drugs is clinically warranted, inform patients of increased risk for serotonin syndrome and monitor for symptoms
Pregnancy & Lactation
Pregnancy category: D
Lactation: Drug is excreted in breast milk; use not recommended
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits postsynaptic D2 receptor supersensitivity
Alters cation transport in nerve and muscle cells and influences reuptake of serotonin or norepinephrine
Inhibits phosphatidylinositol cycle second messenger systems
Absorption
Bioavailability: Immediate release, 95-100%; extended release, 60-90%
Onset: Initial antimanic effect, 5-7 days; full effect, 10-21 days
Peak serum time: Immediate release, 0.5-2 hr; extended release, 4-12 hr
Peak plasma concentration: 0.4-0.9 mEq/L
Steady-state therapeutic plasma concentration: 0.5-1.3 mEq/L
Distribution
Vd: Approximates total body water (0.7-1 L/kg)
Metabolism
Not metabolized
Elimination
Half-life: 18-24 hr; up to 36 hr with advanced age or renal impairment
Dialyzable: Yes (hemodialysis, 50-90 mL/min; peritoneal dialysis, 13-15 mL/min)
Renal clearance: 20-40 mL/min
Excretion: Urine (95-99%)
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Formulary
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