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Imipramine

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Imipramine
Systematic (IUPAC) name
 ?
Identifiers
CAS number 50-49-7
ATC code N06AA02
PubChem 3696
DrugBank APRD00672
Chemical data
Formula C19H24N2 
Mol. weight 280.407
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Main active metabolite desipramine
Half life 11-25 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

D(US)
Known risk of damage to fetus.

Legal status

Prescription only

Routes Oral

Imipramine (sold as Antideprin®, Deprenil, Deprimin, Deprinol, Depsonil, Dynaprin, Eupramin, Imipramil, Irmin, Janimine®, Melipramin, Surplix, Tofranil®) is an antidepressant medication, a tricyclic antidepressant of the dibenzazepine group, mainly used in the treatment of clinical depression and enuresis.

Contents

[edit] History

Imipramine was, in the late 1950s, the first tricyclic antidepressant to be developed (by Ciba-Geigy). Initially, it was tried against psychotic disorders (e.g. schizophrenia), but proved insufficient. During the clinical studies its antidepressant qualities, unsurpassed until the advent of SSRIs, became evident. Subsequently it was extensively used as standard antidepressant and later served as a prototypical drug for the development of the later released tricyclics. It is not as commonly used today but sometimes used to treat major depression as a second-line treatment. It has also seen limited use in the treatment of migraines, ADD and post concussive syndrome. Imipramine has additional indications for the treatment of panic attacks and chronic pain. In pediatric patients it is relatively frequently used to treat pavor nocturnus and nocturnal enuresis.

[edit] Mechanism of Action

Imipramine, a tertiary amine, inhibits the reuptake of serotonin more so than most secondary amine tricyclics, meaning that it blocks the reuptake of neurotransmitters serotonin and noradrenaline almost equally.

[edit] Metabolism

Imipramine is converted to desipramine, another TCA, in the body.

[edit] Contraindications and Precautions

See Tricyclic antidepressants

[edit] Side effects

Some common side effects of the drug include: tremors, dry mouth, blurred vision, constipation, insomnia, drowsiness, perspiration, flushing and weight gain. Agitation, irritability, confusion, and delirium are also possible, particular in the elderly.

[edit] Dosage

  • Ambulatory patients : starting with 25 to 75mg daily, increasing up to a maximum of 200mg daily, after remission dose is often reduced to 50-100mg daily.
  • Hospitalized patients : starting with 3 time 25mg, increasing to 200mg. Up to 300mg may be given in resistant cases. After remission dose is often reduced to 50-100mg daily.
  • Pediatric patients : starting with 10mg daily the dose is adjusted according to the severity of the symptoms to be treated, the side-effects encountered and the weight of the patient.

[edit] Overdose

The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants. Cardinal symptoms are cardiac and neurological disturbances. Any ingestion by children should be considered as serious and potentially fatal.

[edit] External links


Antidepressants (ATC N06A) edit
Monoamine oxidase inhibitors (MAOI) Harmaline, Iproclozide, Iproniazid, Isocarboxazid, Nialamide, Phenelzine, Selegiline, Toloxatone, Tranylcypromine
Reversible inhibitor of monoamine oxidase A (RIMA) Brofaromine, Moclobemide
Dopamine reuptake inhibitor (DARI) Amineptine, Phenmetrazine, Vanoxerine, Modafinil
Norepinephrine-dopamine reuptake inhibitors Bupropion
Norepinephrine reuptake inhibitor (NRI) or (NARI) Atomoxetine, Maprotiline, Reboxetine, Viloxazine
Serotonin-norepinephrine reuptake inhibitor (SNRI) Duloxetine, Milnacipran, Venlafaxine
Selective serotonin reuptake inhibitor (SSRI) Alaproclate, Etoperidone, Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Zimelidine
Selective serotonin reuptake enhancer (SSRE) Tianeptine
Tricyclic antidepressants (TCA) Amitriptyline, Amoxapine, Butriptyline, Clomipramine, Desipramine, Dibenzepin, Dothiepin, Doxepin, Imipramine, Iprindole, Lofepramine, Melitracen, Nortriptyline, Opipramol, Protriptyline, Trimipramine
Tetracyclic antidepressants Maprotiline, Mianserin, Nefazodone, Trazodone
Noradrenergic and specific serotonergic antidepressant (NaSSA) Mirtazapine
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