Action and Spectrum

Actions and Spectrum:

clomipramine is a tricyclic antidepressant medication that acts on the neurotransmitter’s serotonin and norepinephrine. It is primarily used to treat depression and obsessive-compulsive disorder (OCD).

In terms of its mechanism of action, clomipramine works by increasing the levels of serotonin and norepinephrine in the brain, which can help to elevate mood and reduce symptoms of anxiety and depression.

In terms of its spectrum of activity, clomipramine is classified as a tricyclic antidepressant, which means it has a broader range of activity compared to selective serotonin reuptake inhibitors (SSRIs), and is used to treat a range of psychiatric disorders, including depression, OCD, panic disorder, and eating disorders.

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Headache (50-55%)

Xerostomia (84%)

Constipation (47%)

Fatigue (35-40%)

Ejaculation failure (42%)

Nausea (30-35%)

Weight gain (18%)

Impotence (20-25%)

1-10% 

Hepatotoxicity (1-3%)

Weight loss (5%)

Frequency Not Defined 

Blurred vision

Dyspepsia

Dizziness

Black Box Warning

Black Box Warning

The black box warning for clomipramine, an antidepressant medication, states that the drug has been associated with an increased risk of suicidal thoughts and behavior in children, adolescents, and young adults up to the age of 24.

Contraindication / Caution

Contraindication/Caution:

Contraindications: 

• clomipramine is contraindicated in patients with a known hypersensitivity to clomipramine or any of its components.
• clomipramine should not be used in patients with a history of heart attack, heart block, and arrhythmia.
• clomipramine is also contraindicated in patients with liver disease, liver damage, and liver failure.
• clomipramine should not be used in patients with a history of suicidal ideation or attempts.

Cautions: 

• clomipramine may cause drowsiness and dizziness, so patients should avoid driving or operating heavy machinery until they know how the medication affects them.
• clomipramine may increase the risk of seizures, so it should be used with caution in patients with a history of seizures or epilepsy.
• clomipramine may interact with other medications, so patients should inform their healthcare provider about all medications they are taking, including prescription, over the counter, and herbal remedies.
• clomipramine may cause changes in weight, appetite, and sleep patterns.
• clomipramine may increase the risk of suicide in children, adolescents, and young adults, so close monitoring is necessary in this population.
• clomipramine may cause withdrawal symptoms if stopped suddenly, so patients should not stop taking the medication without consulting their healthcare provider.

Pregnancy / Lactation

Pregnancy warnings:   

US FDA pregnancy category: C

Lactation:  

Excreted into human milk is known

Pregnancy Categories:        

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

clomipramine is a tricyclic antidepressant drug used to treat depression, obsessive-compulsive disorder (OCD), and panic disorder.

Pharmacodynamics: 

It works by increasing the levels of certain neurotransmitters, such as serotonin, in the brain. clomipramine acts as a reuptake inhibitor for serotonin, norepinephrine, and to a lesser extent, dopamine, which enhances the activity of these neurotransmitters in the brain. It is absorbed well orally and is metabolized in the liver. Common side effects of clomipramine include dry mouth, blurred vision, constipation, and drowsiness. It may also have anticholinergic effects.

Pharmacokinetics:  

Absorption 

clomipramine is absorbed well from the gastrointestinal tract, with peak plasma concentrations achieved within 2-6 hours after oral administration. The drug has a high bioavailability, which means that it is easily absorbed and utilized by the body.

Distribution 

clomipramine is distributed throughout the body and is highly bound to plasma proteins. It has a large volume of distribution, which means that it spreads out throughout the body after being absorbed into the bloodstream.

Metabolism 

clomipramine is metabolized in the liver, primarily through the cytochrome P450 system. The drug is metabolized into several active and inactive metabolites, which are then eliminated from the body through the kidneys.

Elimination and Excretion 

clomipramine is eliminated from the body primarily through the kidneys, with only a small amount eliminated through the feces. The half-life of the drug is approximately 24 hours, which means that it takes about 24 hours for half of the drug to be eliminated from the body.

Adminstartion

Administration: 

Oral administration

clomipramine is an antidepressant medication typically used to treat depression and obsessive-compulsive disorder (OCD). It is available in oral tablet form and is usually taken once or twice a day, with or without food.

The recommended starting dose is 25mg per day, with gradual increases up to a maximum of 250mg per day. The dosage will be adjusted based on the individual’s response and tolerance to the medication.

Patient Information Leaflet

Patient information leaflet

Generic Name: clomipramine

Why do we use clomipramine?

clomipramine is a tricyclic antidepressant medication used to treat depression and obsessive-compulsive disorder (OCD).

Depression is a mental disorder characterized by persistent feelings of sadness, hopelessness, and lack of interest in activities. clomipramine helps to improve mood and reduces symptoms of depression by increasing levels of neurotransmitters, such as serotonin and norepinephrine, in the brain.