Desipramine; Uses, Dosage, Side Effects, Drug Interactions

Desipramine, Desipramine; Uses, Dosage, Side Effects, Drug Interactions, Rx Harun
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Desipramine is an active metabolite of imipramine, a tertiary amine and a synthetic tricyclic derivative of the antidepressant. Desipramine enhances monoamine neurotransmission in certain areas of the brain by inhibiting the re-uptake of noradrenaline and serotonin at the noradrenergic and serotoninergic nerve endings, respectively. It also induces sedation through histamine 1 receptor blockage and hypotension through the beta-adrenergic blockage.

Desipramine hydrochloride is a dibenzazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, desipramine does not affect mood or arousal but may cause sedation. In depressed individuals, desipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Secondary amine TCAs, such as desipramine and nortriptyline, are more potent inhibitors of norepinephrine reuptake than tertiary amine TCAs, such as amitriptyline and doxepine.

Mechanism of Action of Desipramine

Desipramine is a tricyclic antidepressant (TCA) that selectively blocks the reuptake of norepinephrine (noradrenaline) from the neuronal synapse. It also inhibits serotonin reuptake, but to a lesser extent compared to tertiary amine TCAs such as imipramine. Inhibition of neurotransmitter reuptake increases the stimulation of the post-synaptic neuron. Chronic use of desipramine also leads to down-regulation of beta-adrenergic receptors in the cerebral cortex and sensitization of serotonergic receptors. An overall increase in serotonergic transmission likely confers desipramine its antidepressant effects. Desipramine also possesses minor anticholinergic activity, through its affinity for muscarinic receptors. TCAs are believed to act by restoring normal levels of neurotransmitters via synaptic reuptake inhibition and by increasing serotonergic neurotransmission via serotonergic receptor sensitization in the central nervous system.

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Desipramine is an active metabolite of imipramine, a tertiary amine and a synthetic tricyclic derivative of the antidepressant. Desipramine enhances monoamine neurotransmission in certain areas of the brain by inhibiting the re-uptake of noradrenaline and serotonin at the noradrenergic and serotoninergic nerve endings, respectively. It also induces sedation through histamine 1 receptor blockage and hypotension through the beta-adrenergic blockage.

Indications of Desipramine

Contra-Indications of Desipramine

  • Overactive thyroid gland
  • Schizophrenia
  • Manic-depression
  • Having thoughts of suicide
  • Alcoholism
  • Serotonin syndrome – adverse drug interaction
  • Lower seizure dhreshold
  • Closed angle glaucoma
  • Heart attack within the last 30 days
  • Very rapid heartbeat – torsades de Pointes
  • Prolonged QT interval on EKG
  • Abnormal heart rhythm
  • Abnormal EKG with QT changes from Birth
  • Stroke
  • Liver problems
  • Kidney disease with reduction in kidney function
  • Enlarged prostate
  • Seizures
  • Cannot empty bladder
  • CYP2D6 poor metabolizer
  • Risk of angle-closure glaucoma due to narrow angle of anterior chamber of eye

Dosage of Desipramine

Strengths: 25 mg; 50 mg; 75 mg; 10 mg; 100 mg; 150 mg

Depression

  • 100 to 200 mg orally per day
  • Maximum dose: 300 mg/day

Geriatric Depression

  • 25 to 100 mg orally per day
  • Maximum dose: 150 mg/day

Side Effects of Desipramine

The most common

More common

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Less common

  • Abnormal dreams
  • change in sense of taste
  • congestion
  • discouragement, feeling sad, or empty
  • Suicide attempts
  • Acting on dangerous impulses
  • Aggressive or violent behavior
  • Thoughts about suicide or dying
  • New or worse depression
  • New or worse anxiety or panic attacks
  • Agitation, restlessness, anger, or irritability
  • Trouble sleeping
  • An increase in activity or talking more than normal

Drug Interactions of Desipramine

Desipramine may interact with following drugs ,suppliments & may decrease the efficacy of drug

Pregnancy & Lactation of Desipramine

FDA Pregnancy Category  C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

Desipramine passes into breast milk. If you are a breast-feeding mother and are taking desipramine, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

 

Desipramine, Desipramine; Uses, Dosage, Side Effects, Drug Interactions, Rx Harun

Desipramine, Desipramine; Uses, Dosage, Side Effects, Drug Interactions, Rx Harun

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