Imipramine is a synthetic tricyclic derivative, antidepressant Imipramine enhances monoamine neurotransmission in certain areas of the brain. It also induces sedation through histamine 1 receptor blockage; hypotension through beta-adrenergic blockage; and diverse parasympatholytic effects. Imipramine has less sedative effect than other members of its therapeutic family. It is used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders.
Imipramine is the prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.
In non-depressed individuals, imipramine does not affect mood or arousal but may cause sedation. In depressed individuals, imipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Imipramine is used to treat symptoms of depression. Imipramine is sometimes used to treat bed-wetting in children ages 6 and older.
Mechanism of Action of Imipramine
Imipramine works by inhibiting the neuronal reuptake of the neurotransmitters norepinephrine and serotonin. It binds the sodium-dependent serotonin transporter and sodium-dependent norepinephrine transporter preventing or reducing the reuptake of norepinephrine and serotonin by nerve cells. Depression has been linked to a lack of stimulation of the post-synaptic neuron by norepinephrine and serotonin. Slowing the reuptake of these neurotransmitters increases their concentration in the synaptic cleft, which is thought to contribute to relieving symptoms of depression. In addition to acutely inhibiting neurotransmitter re-uptake, imipramine causes down-regulation of cerebral cortical beta-adrenergic receptors and sensitization of post-synaptic serotonergic receptors with chronic use. This leads to enhanced serotonergic transmission.
Indications of Imipramine
- Bulimia nervosa
- Enuresis
- Major depressive disorder
- ADHD
- Depression
- Enuresis
- Interstitial cystitis
- Chronic pain
- Irritable Bowel Syndrome
- Night terrors
- Panic disorder
- Primary Nocturnal Enuresis
- Somatoform pain disorder
- PTSD
- Pain, neuropathic
Imipramine is also used to manage some types of chronic, severe, neurogenic pain; to reduce craving and/or prevent depression upon cocaine withdrawal; to relieve symptoms of attention deficit hyperactivity disorder in children over 6 years of age and in adolescents; as a treatment adjunct with amphetamines or methylphenidate in cataplexy associated with narcolepsy; to block the recurrence of panic attacks, with or without phobias; in the treatment of stress and urge incontinence; and to control binge eating and purging in bulimia.
Contra-Indications of Imipramine
- Overactive thyroid gland
- Schizophrenia
- Manic-Depression
- Having thoughts of suicide
- Alcoholism
- Alcohol intoxication
- Serotonin syndrome – adverse drug interaction
- Increased Pressure in the Eye
- Closed-angle glaucoma
- Heart attack within the last 30 days
- Prolonged QT interval on EKG
- Abnormal heart rhythm
- Chronic heart failure
- Abnormal EKG with QT changes from Birth
- Stroke
- Blood Pressure Drop Upon Standing
- Paralysis of the Intestines
- Blocked Bowels with Decreased Peristaltic Movement
- Liver problems
- Kidney disease with a reduction in kidney function
- Enlarged Prostate
- Recent operation
- Seizures
- Cannot Empty Bladder
- Pregnancy
- Chronic idiopathic constipation
- CYP2D6 poor metabolizer
- Risk of angle-closure glaucoma due to narrow-angle of the anterior chamber of the eye
- Allergies to Tricyclic Compounds
Side Effects of Imipramine
The most common
- stomach or abdominal cramps, gas, or pain
- decreased sexual desire or ability
- Failure to discharge semen (in men)
- chest pain
- a headache
- joint painPain
- dizziness
- nausea and vomiting
- Severe stomach ache
- epigastric pain,
- diarrhea,
- anorexia,
- flatulence,
- a headache,
- dizziness,
- fainting, fast or pounding heartbeats.
More common
- Fast or irregular heartbeat
- fever
- Back pain
- dizziness
- headache
- increased cough
- Acid or sour stomach
- decreased appetite
- Agitation
- chest congestion
- chest pain
- cold sweats
- confusion
- decreased sexual ability or desire
- diarrhea or loose stools
- heartburn
- sleepiness or unusual drowsiness
- trouble sleeping
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 Imipramine
Imipramine may interact with following drugs ,suppliments & may decrease the efficacy of drug
- anticholinergic medications (e.g., atropine, diphenhydramine, hydroxyzine)
- barbiturates (e.g., phenobarbital)
- benzodiazepines (e.g., diazepam, lorazepam)
- butyrophenones (e.g., haloperidol)
- carbamazepine
- clarithromycin
- cimetidine
- domperidone
- erythromycin
- MAO inhibitors (e.g., phenelzine, moclobemide)
- methylphenidate
- metoclopramide
- phenothiazines (e.g., chlorpromazine, thioridazine)
- phenylephrine
- sotalol
- SSRI antidepressants (e.g., fluoxetine, fluvoxamine, paroxetine)
- tramadol
- ziprasidone
Pregnancy & Lactation of Imipramine
FDA Pregnancy Category N – Not classified.
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
Imipramine passes into breast milk. If you are a breast-feeding mother and are taking imipramine it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
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