Imipramine Hydrochloride

Imipramine Hydrochloride Uses, Dosage, Side Effects, Food Interaction and all others data.

Imipramine Hydrochloride 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.

Imipramine Hydrochloride is a tricyclic antidepressant with general pharmacological properties similar to those of structurally related tricyclic antidepressant drugs such as amitriptyline and doxepin. While it acts to block both, imipramine displays a much higher affinity for the serotonin reuptake transporter than for the norepinephrine reuptake transporter . Imipramine Hydrochloride produces effects similar to other monoamine targeting antidepressants, increasing serotonin- and norepinephrine-based neurotransmission.

This modulation of neurotransmission produces a complex range of changes in brain structure and function along with an improvement in depressive symptoms. The changes include increases in hippocampal neurogenesis and reduced downregulation of this neurogenesis in response to stress . These implicate brain derived neurotrophic factor signalling as a necessary contributor to antidepressant effect although the link to the direct increase in monoamine neurotransmission is unclear.

Serotonin reuptake targeting agents may also produce a down-regulation in β-adrenergic receptors in the brain .

Trade Name Imipramine Hydrochloride
Availability Prescription only
Generic Imipramine
Imipramine Other Names Imipramin, Imipramina, Imipramine, Imipraminum, Imizine
Related Drugs Rexulti, Buprenex, aspirin, acetaminophen, sertraline, tramadol, trazodone, Lexapro, naproxen, Tylenol
Formula C19H24N2
Weight Average: 280.4073
Monoisotopic: 280.193948778
Protein binding

Imipramine is 60-96% bound to plasma proteins in circulation . It is known to bind albumin, α1-acid glycoprotein, and lipoproteins.

Groups Approved
Therapeutic Class Tricyclic & related anti-depressant drugs, Tricyclic Anti-depressant
Manufacturer Rosemont Pharmaceuticals Limited
Available Country United Kingdom
Last Updated: September 19, 2023 at 7:00 am
Imipramine Hydrochloride
Imipramine Hydrochloride


Depression: For the relief of symptoms of depression. Endogenous depression is more likely to be alleviated than other depressive states. One to three weeks of treatment may be needed before optimal therapeutic effects are evident.

Childhood Enuresis: May be useful as temporary adjunctive therapy in reducing enuresis in children aged 6 years and older, after possible organic causes have been excluded by appropriate tests. In patients having daytime symptoms of frequency and urgency, examination should include voiding cystourethrography and cystoscopy, as necessary. The effectiveness of treatment may decrease with continued drug administration.

Imipramine Hydrochloride is also used to associated treatment for these conditions: Attention Deficit Hyperactivity Disorder (ADHD), Bulimia Nervosa, Enuresis, Major Depressive Disorder (MDD), Neuropathic Pain, Panic Disorder, Post Traumatic Stress Disorder (PTSD)

How Imipramine Hydrochloride works

Imipramine Hydrochloride works by inhibiting the neuronal reuptake of the neurotransmitters norepinephrine and serotonin . It binds the sodium-dependent serotonin transporter and sodium-dependent norepinephrine transporter reducing the reuptake of norepinephrine and serotonin by neurons. 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, producing knock-on effects in protein kinase signalling which is thought to contribute to changes in neurotransmission and brain physiology which relieves symptoms of depression .


Imipramine Hydrochloride dosage

Depression: Initially up to 75 mg daily in divided doses increased gradually to 150-200 mg (up to 300 mg in hospital); up to 150 mg may be given as a single dose at bed time; elderly, initially 10 mg daily, increased gradually to 30-50 mg daily; child not recommended for depression.

Panic attack: Initially 10-25 mg/day, depending on how the medication is tolerated, raise the dose until the desired response is obtained. The daily doses required vary greatly from patient to patient, between 75-150 mg, if necessary it can be increased to 200 mg.Nocturnal enuresis(Child):

  • 7 years: 25 mg
  • 8 to 11 years: 20-50 mg
  • Over 11 years: 50-75 mg at bedtime; max. period of treatment (Including gradual withdrawal) is 3 months; full physical examination is required before further course.

Side Effects

Dry mouth, less sedation, blurred vision (disturbances of accommodation, increased intraocular pressure), constipation, nausea, difficulty with micturation; cardiovascular side-effects, sweating, tremors, rashes and hypersensitivity reaction (including urticaria & photosensitivity), behavioral disturbances (particularly in children) hypomania or mania (particularly in elderly), interference with sexual function; blood sugar changes, increased appetite, weight gain (occasionally weight loss).


The anticholinergic actvity of imipramine can produce dry mucous membranes, blurred vision, increased intraocular pressure, hyperthermia, constipation, adynamic ileus, urinary retention, delayed micturition, and dilation of the urinary tract .

Central nervous system and neuromuscular effects include drowsiness, lethargy, fatigue, agitation, excitement, nightmares, restlessness, insomnia, confusion, disturbed concentration, disorientation, delusions, and hallucinations.

Effects on the GI tract include anorexia, nausea and vomiting, diarrhea, abdominal cramps, increases in pancreatic enzymes, epigastric distress, stomatitis, peculiar taste, and black tongue.

Rarely agranulocytosis, thrombocytopenia, eosinophilia, leukopenia, and purpura have occured.

Infants whose mothers were receiving tricyclic antidepressants prior to delivery have experienced cardiac problems, irritability, respiratory distress, muscle spasms, seizures, and urinary retention.

Serotonin syndrome can occur when used in conjunction with other pro-serotonergic drugs.

LD50/> Values

Rat - Oral 250 mg/kg - Intraperitoneal 79mg/kg - Subcutaneous 250 mg/kg - Intravenous 15.9 mg/kg

Mouse - Oral 188 mg/kg - Intraperitoneal 51.6 mg/kg - Subcutaneous 195 μg/kg - Intravenous 21 mg/kg

Human range of toxicity is considered to include single dosages greater than 5 mg/kg.


Cardiac diseases (particularly with arrhythmias), history with epilepsy, pregnancy and breast feeding, elderly, hepatic impairment (avoid if severe), thyroid disease, psychoses, angle-closure glaucoma, history of urinary retention, concurrent electro-convulsive therapy. Drowsiness may affect performances of skilled tasks (e.g. driving), alcohol induced Imipramine Hydrochloride effect.


Imipramine Hydrochloride should not be used in combination with Monoamine oxidase inhibitors (MAO), anticholinergic agents, antihypertensive agents, methylphenidate, levodopa, antipsychotic drug, cimetidine, barbiturates, and oral contraceptives.

Food Interaction

  • Avoid alcohol.
  • Avoid St. John's Wort.
  • Do not take with bran and high fiber foods.
  • Limit caffeine intake.
  • Take with food.

Imipramine Hydrochloride Alcohol interaction


Concomitant use of ethanol and a tricyclic antidepressant (TCA) may result altered TCA plasma levels and efficacy, and additive impairment of motor skills, especially driving skills.

Acute ethanol ingestion may inhibit TCA metabolism, while chronic ingestion of large amounts of ethanol may induce hepatic TCA metabolism.

Patients should be advised to avoid alcohol during TCA therapy.

Alcoholics who have undergone detoxification should be monitored for decreased TCA efficacy.

Dosage adjustments may be required.

Volume of Distribution

Imipramine Hydrochloride has a high apparent volume of distribution of 10-20 L/kg . The drug is known to accumulate in the brain at concentrations 30-40 times that in systemic circulation.

Elimination Route

Rapidly and well absorbed (>95%) after oral administration . The primary site of absorption is the small intestine as the basic amine groups are ionized in the acidic environment of the stomach, preventing movement across tissues. Bioavailability ranges from 29-77% due to high inter-individual variability. Peak plasma concentration is usually attained 2-6 hours following oral administration. Absorption is unaffected by food.

Half Life

Imipramine Hydrochloride has a mean half life of 12 h. Its active metabolite, desipramine has a mean half life of 22.5 h .


Imipramine Hydrochloride has a mean clearance of 1 L/h/kg. Its active metabolite, desipramine has a mean clearance of 1.8 L/h/kg .

Elimination Route

Imipramine Hydrochloride is primarily excreted in the urine with less than 5% present as the parent compound

Pregnancy & Breastfeeding use

Pregnancy category D. Limited data suggest that imipramine is likely to be excreted in human breast milk. Known risk of damage to fetus.


Recent myocardial infarction, arrhythmias (particularly heart block), not indicated in manic phase, severe liver disease.

Acute Overdose

Children have been reported to be more sensitive than adults to an acute overdosage of imipramine. An acute overdose in infants or young children must be considered serious and potentially fatal.

Storage Condition

Store in a cool & dry place, protected from light and moisture. Keep all medicines out of the reach of children.

Innovators Monograph

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Imipramine Hydrochloride contains Imipramine see full prescribing information from innovator Imipramine Hydrochloride Monograph, Imipramine Hydrochloride MSDS, Imipramine Hydrochloride FDA label
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