Dosing and uses of Levate (amitriptyline)
Adult dosage forms and strengths
tablet
- 10mg
- 25mg
- 50mg
- 75mg
- 100mg
- 150mg
Depression
Outpatient: 25-50 mg PO qHS initially; increase by 25 mg every 5-7 days to 100-200 mg/day (may divide doses throughout day or give at bedtime); if needed, may increase to 300 mg/day
Inpatient: 100-300 mg PO qDay
Postherpetic Neuralgia (Off-label)
65-100 mg PO qDay for at least 3 weeks
Migraine Prophylaxis (Off-label)
10-25 mg PO qHS; 10-400 mg PO qHS dose range
Eating Disorder (Off-label)
150 mg PO qHS for 8 weeks
Geriatric Dosing
Depression
10-25 mg PO qHS; may increase by 10-25 mg increments qWeek if needed and as tolerated
Dosage range: 25-150 mg/day
Dosing Considerations
- Avoid; strong anticholinergic and sedative effects; may cause orthostatic hypotension (Beers criteria)
- Consider alternatives; if must use, initiate with lower initial dose
Pediatric dosage forms and strengths
tablet
- 10mg
- 25mg
- 50mg
- 75mg
- 100mg
- 150mg
Depression
Adolescents
- Initial: 25-50 mg/day PO in divided doses
- Increase gradually to 100 mg/day in divided doses
Children (Off-label)
- First 3 days: 1 mg/kg/day divided q8hr PO, THEN
- 1.5 mg/kg/day divided q8hr PO
Analgesia for Chronic Pain (Off-label)
Load: 0.1 mg/kg PO qHS; may increase as tolerated over 2-3 weeks
Maintenance: 0.5-2 mg/kg PO qHs
Migraine Prophylaxis (Off-label)
0.25 mg/kg/day PO qHS; may increase dose by 0.25 mg/kg/day; not to exceed 1 mg/kg/day
Dose range: 0.1-2 mg/kg/day; not to exceed 2 mg/kg/day or 75 mg/day; if dose >1 mg/kg/day, divide dose q12hr
Levate (amitriptyline) adverse (side) effects
Frequency not defined
Agitation
Agranulocytosis
Alopecia
Anxiety
Anorexia
Ataxia
Arrhythmia
Blurred vision
Coma
Confusion
Constipation
Diarrhea
Dizziness
Dry mouth
ECG changes
Eosinophilia
Extrapyramidal symptoms (EPS)
Fatigue
Hallucination
Headache
Hypertension
Increased LFTs
Insomnia
Lethargy
Leukopenia
MI
Nausea
Ocular pressure increased
Orthostatic hypotension
Palpitation
Paresthesia
Photosensitivity
Rash
Restlessness
Sedation
Seizure
Sexual dysfunction
SIADH
Stroke
Stomatitis
Syncope
Sweating
Tachycardia
Thrombocytopenia
Tinnitus
Urinary retention
Urticaria
Vomiting
Xerostomia
Weakness
Weight gain
Warnings
Black box warnings
In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 years) taking antidepressants for major depressive disorders and other psychiatric illnesses; this increase was not seen in patients over age 24 years; a slight decrease in suicidal thinking was seen in adults over age 65 years
In children and young adults, the risks must be weighed against the benefits of taking antidepressants
Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during the initial 1-2 months of therapy and dosage adjustments; the patient’s family should communicate any abrupt changes in behavior to the healthcare provider
Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy
This drug is not approved for use in pediatric patients <12 years
Not FDA approved for treatment of bipolar depression
Contraindications
Hypersensitivity
Acute recovery phase following MI
Concurrent use with cisapride
Contraindicated within 14 days of MAOIs; if linezolid or IV methylene blue (MAOIs) must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose, or after 2 weeks of monitoring, whichever comes first
Cautions
Bone marrow suppression reported
Avoid use in narrow-angle glaucoma
May cause sedation and impair mental and physical abilities
Avoid use with any drugs or conditions that prolong QT intervaL
May cause orthostatic hypotension
Use caution in patients with cardiovascular disease, diabetes, mania, hepatic and renal impairment, thyroid dysfunction, and seizure disorder
May worsen mania symptoms or precipitate mania in patients with bipolar disorder
Clinical worsening and suicidal ideation may occur despite medication in adolescents and young adults (18-24 years)
Risk of anticholinergic side effects; may cause constipation, urinary retention, blurred vision, and xerostomia
Use caution in patients with urinary retention, open-angle glaucoma, BPH, decreased gastrointestinal motility, or paralytic ileus
Possibility of EPS and neuroleptic malignant syndrome
Abrupt discontinuation of therapy not recommended in patients receiving high doses for prolonged periods
Fractures reported with therapy
Pregnancy and lactation
Pregnancy category: C
Lactation: Distributed in breast milk; do not nurse (AAP states effect on nursing infants is unknown but may be of concern)
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 of Levate (amitriptyline)
Mechanism of action
Neurotransmitter (especially norepinephrine and serotonin) reuptake inhibitor; anticholinergic
Absorption
Peak serum time: 4 hr
Metabolism
Metabolized by hepatic CYP2C19, CYP3A4
Metabolites: Nortriptyline
Elimination
Half-life: 9-27 hr
Excretion: Urine (18%), small amounts in feces
