LITHOBID

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LITHOBID (LITHOBID).

How it works

Lithium modulates neurotransmitter receptors and second messenger systems; inhibits inositol monophosphatase, reducing phosphoinositide signaling; alters ion transport; enhances serotonin and norepinephrine reuptake; modulates G-proteins.

What the body does with it

Metabolism	Lithium is not metabolized; excreted renally as free ion; reabsorbed in proximal tubule; influenced by sodium balance.
Excretion	Renal: >95% excreted unchanged in urine. Biliary/fecal: <5%.
Half-life	Terminal elimination half-life: 18-36 hours (mean 24 hours) in young adults, increases with age and renal impairment. Long half-life supports once-daily dosing in sustained-release formulation.
Protein binding	0% (lithium is not protein bound).
Volume of Distribution	0.7-1.0 L/kg (total body water). Large Vd indicates extensive distribution into tissues; reduces efficacy of dialysis in overdose.
Bioavailability	Oral immediate-release: 90-100%. Oral extended-release: 60-90% (lower due to reduced absorption).
Onset of Action	Oral immediate-release: 1-3 hours for initial symptom reduction; full therapeutic effect may require 1-2 weeks. Oral extended-release: onset delayed, clinical effect may take 2-3 weeks.
Duration of Action	24 hours for sustained-release formulation; immediate-release requires multiple daily doses. Steady-state achieved after 5-7 days with regular dosing.

Classification & Brands

Dosing & administration

300-600 mg orally 2-3 times daily; extended-release formulation (LITHOBID) 300-450 mg orally twice daily.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	Contraindicated if CrCl < 30 mL/min. For CrCl 30-59 mL/min: reduce dose by 50% and monitor serum lithium levels. For CrCl 60-89 mL/min: reduce dose by 25%.
Liver impairment	No specific Child-Pugh based dose adjustment recommended; use with caution and monitor serum levels due to potential volume of distribution changes.
Pediatric use	Children ≥12 years: 15-20 mg/kg/day in 2-3 divided doses; titrate based on serum levels (therapeutic range 0.6-1.2 mEq/L).
Geriatric use	Start with 150-300 mg once or twice daily; titrate slowly due to reduced renal function and increased sensitivity; target serum level 0.4-0.8 mEq/L.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LITHOBID (LITHOBID).

Breastfeeding	Lithium (LITHOBID) is excreted into breast milk. Milk-to-plasma ratio ranges from 0.24 to 0.68. Adverse effects in breastfed infants include hypotonia, hypothermia, cyanosis, and ECG changes. Breastfeeding is generally not recommended during lithium therapy. If breastfeeding is undertaken, monitor infant serum lithium levels and renal function.
Teratogenic Risk	First trimester: Increased risk of Ebstein's anomaly and other cardiac defects; odds ratio for Ebstein's anomaly approximately 10-20. Second trimester: Risk of preterm delivery and neonatal complications. Third trimester: Risk of neonatal toxicity including lethargy, hypotonia, cyanosis, and feeding difficulties; risk of neonatal hypothyroidism and nephrogenic diabetes insipidus.

Warnings & precautions

■ FDA Black Box Warning

Lithium toxicity risk: narrow therapeutic index; monitor serum levels closely. Toxicity may be fatal or cause irreversible neurological damage.

Side Effect Profile

Serious Effects

Absolute Contraindications

Severe renal failure; severe cardiovascular disease; severe dehydration; sodium depletion; concomitant use with thiazide diuretics (relative); hypersensitivity to lithium.

Clinical Precautions

Precautions

Renal impairment; dehydration; sodium depletion; thyroid dysfunction; parathyroid dysfunction; electrocardiographic changes; neurotoxicity; concomitant use with NSAIDs, diuretics, ACE inhibitors; pregnancy (risk of Ebstein's anomaly); lactation.

Clinical Tips & Counseling

Drug interactions

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LITHOBID

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LITHOBID (LITHOBID).

How it works

What the body does with it

Metabolism	Lithium is not metabolized; excreted renally as free ion; reabsorbed in proximal tubule; influenced by sodium balance.
Excretion	Renal: >95% excreted unchanged in urine. Biliary/fecal: <5%.
Half-life	Terminal elimination half-life: 18-36 hours (mean 24 hours) in young adults, increases with age and renal impairment. Long half-life supports once-daily dosing in sustained-release formulation.
Protein binding	0% (lithium is not protein bound).
Volume of Distribution	0.7-1.0 L/kg (total body water). Large Vd indicates extensive distribution into tissues; reduces efficacy of dialysis in overdose.
Bioavailability	Oral immediate-release: 90-100%. Oral extended-release: 60-90% (lower due to reduced absorption).
Onset of Action	Oral immediate-release: 1-3 hours for initial symptom reduction; full therapeutic effect may require 1-2 weeks. Oral extended-release: onset delayed, clinical effect may take 2-3 weeks.
Duration of Action	24 hours for sustained-release formulation; immediate-release requires multiple daily doses. Steady-state achieved after 5-7 days with regular dosing.

Classification & Brands

Dosing & administration

300-600 mg orally 2-3 times daily; extended-release formulation (LITHOBID) 300-450 mg orally twice daily.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	Contraindicated if CrCl < 30 mL/min. For CrCl 30-59 mL/min: reduce dose by 50% and monitor serum lithium levels. For CrCl 60-89 mL/min: reduce dose by 25%.
Liver impairment	No specific Child-Pugh based dose adjustment recommended; use with caution and monitor serum levels due to potential volume of distribution changes.
Pediatric use	Children ≥12 years: 15-20 mg/kg/day in 2-3 divided doses; titrate based on serum levels (therapeutic range 0.6-1.2 mEq/L).
Geriatric use	Start with 150-300 mg once or twice daily; titrate slowly due to reduced renal function and increased sensitivity; target serum level 0.4-0.8 mEq/L.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LITHOBID (LITHOBID).

Breastfeeding	Lithium (LITHOBID) is excreted into breast milk. Milk-to-plasma ratio ranges from 0.24 to 0.68. Adverse effects in breastfed infants include hypotonia, hypothermia, cyanosis, and ECG changes. Breastfeeding is generally not recommended during lithium therapy. If breastfeeding is undertaken, monitor infant serum lithium levels and renal function.
Teratogenic Risk	First trimester: Increased risk of Ebstein's anomaly and other cardiac defects; odds ratio for Ebstein's anomaly approximately 10-20. Second trimester: Risk of preterm delivery and neonatal complications. Third trimester: Risk of neonatal toxicity including lethargy, hypotonia, cyanosis, and feeding difficulties; risk of neonatal hypothyroidism and nephrogenic diabetes insipidus.

Warnings & precautions

■ FDA Black Box Warning

Lithium toxicity risk: narrow therapeutic index; monitor serum levels closely. Toxicity may be fatal or cause irreversible neurological damage.

Side Effect Profile

Serious Effects

Absolute Contraindications

Severe renal failure; severe cardiovascular disease; severe dehydration; sodium depletion; concomitant use with thiazide diuretics (relative); hypersensitivity to lithium.