brands

Class

• Neuroscience-based Nomenclature: glutamate; yet to be determined (Glu)
• Glutamatergic modulator
• Often classified as a tricyclic antidepressant, but pharmacologically distinct

Coaxil commonly prescribed for

(Bold for FDA approved)

How Coaxil works

• Modulates glutamatergic neurotransmission, perhaps through potentiation of AMPA receptor function

• Full agonist at mu opioid receptors; animal studies suggest that this may contribute to its antidepressant effects

How long until Coaxil works

• Onset of therapeutic actions usually not immediate, but often delayed 2–4 weeks

• If it is not working within 6–8 weeks for depression, it may require a dosage increase or it may not work at all

• May continue to work for many years to prevent relapse of symptoms

Notable Side Effects

• Headache, dizziness, insomnia, sedation

• Nausea, constipation, abdominal pain, dry mouth

• Abnormal dreams

• Increased transaminases

• Tachycardia

Life Threatening Side Effects

• Theoretically, rare induction of mania and activation of suicidal ideation or behavior

• Cases of activation of suicidal ideation and behavior (suicidality) (short-term did not show an increase in the risk of suicidality with antidepressants compared to placebo beyond age 24)

• Hepatitis that can, in exceptional cases, be severe

• Dermatitis bulbous in exceptional cases

weight gain

unusual

sedation

not usual

What to do about Coaxil side effects

• Wait

• Wait

• Wait

• Lower the dose

• In a few weeks, switch or add other drugs

• For skin reactions, stop treatment

usual dosage range

• 37.5 mg/day

Dosage Forms

Tablet 12.5 mg

long term use

• Safe

habit forming

• Abuse and dependence may occur, in particular in patients under 50 years of age with a history of drug or alcohol dependence

Renal Impairment

• Dose should be reduced for severe impairment to 25 mg/day

Hepatic Impairment

• In patients with severe cirrhosis (class C, Child–Pugh Scale), the dosage should be restricted to 25 mg/day

Cardiac Impairment

• Baseline ECG is recommended

Elderly

• Baseline ECG is recommended for patients over age 50

• Dose should be reduced to 25 mg/day

• Reduction in the risk of suicidality with antidepressants compared to placebo in adults age 65 and older

Children and Adolescents

• Tianeptine is not recommended for use in children or adolescents under 18

• Carefully weigh the risks and benefits of pharmacological treatment against the risks and benefits of nontreatment with antidepressants and make sure to document this in the patient’s chart

• Monitor patients face-to-face regularly, particularly during the first several weeks of treatment

• Use with caution, observing for activation of known or unknown bipolar disorder and/ or suicidal ideation, and inform parents or guardians of this risk so they can help observe child or adolescent patients

Pregnancy

• Not recommended for use during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• Not recommended for use during pregnancy

• Immediate postpartum period is a high-risk time for depression, especially in women who have had prior depressive episodes, so drug may need to be reinstituted late in the third trimester or shortly after childbirth to prevent a recurrence during the postpartum period

• Must weigh benefits of breast feeding with risks and benefits of antidepressant treatment versus nontreatment to both the infant and the mother

• For many patients, this may mean continuing treatment during breast feeding