Nitalapram

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

Nitalapram is an orally administered selective serotonin reuptake inhibitor (SSRI) with a chemical structure unrelated to that of other SSRIs, tricyclic, tetracyclic or other available antidepressant agents. The mechanism of action of Nitalapram as an antidepressant is presumed to be linked to potentiation of serotonergic activity in central nervous system resulting from its inhibition of CNS neuronal reuptake of serotonin (5-HT).

Nitalapram belongs to a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It has been found to relieve or manage symptoms of depression, anxiety, eating disorders and obsessive-compulsive disorder among other mood disorders. The antidepressant, anti-anxiety, and other actions of citalopram are linked to its inhibition of CNS central uptake of serotonin . Serotonergic abnormalities have been reported in patients with mood disorders. Behavioral and neuropsychological of effects of serotonin include the regulation of mood, perception, reward, anger, aggression, appetite, memory, sexuality, and attention, as examples. The onset of action for depression is approximately 1 to 4 weeks. The complete response may take 8-12 weeks after initiation of citalopram .

In vitro studies demonstrate that citalopram is a strong and selective inhibitor of neuronal serotonin reuptake and has weak effects on norepinephrine and dopamine central reuptake. The chronic administration of citalopram has been shown to downregulate central norepinephrine receptors, similar to other drugs effective in the treatment of major depressive disorder. Nitalapram does not inhibit monoamine oxidase .

Trade Name Nitalapram
Availability Prescription only
Generic Citalopram
Citalopram Other Names Citalopram, Citalopramum, Nitalapram
Related Drugs Rexulti, sertraline, trazodone, fluoxetine, Lexapro, amitriptyline, venlafaxine, Zoloft, Cymbalta, Prozac
Type
Formula C20H21FN2O
Weight Average: 324.3919
Monoisotopic: 324.163791509
Protein binding

Citalopram, dimethylcitalopram, and didemethylcitalopram are 80% bound to plasma proteins .

Groups Approved
Therapeutic Class SSRIs & related anti-depressant drugs
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Nitalapram
Nitalapram

Uses

Nitalapram is used for depressive illness and panic disorder. It is also used for substance abuse disorders and alcohol dependence. Nitalapram has also been given in variety of anxiety disorders including obsessive-compulsive disorder and social phobia. It is also effective in generalized anxiety disorder, post-traumatic stress disorder, premenstrual syndrome, idiopathic Parkinson's disease and eating disorder.

Nitalapram is also used to associated treatment for these conditions: Anorexia Nervosa (AN), Bulimia Nervosa, Depression, Diabetic Neuropathies, Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD), Panic Disorder, Post Traumatic Stress Disorder (PTSD), Premature Ejaculation, Premenstrual Dysphoric Disorder, Social Anxiety Disorder (SAD)

How Nitalapram works

The mechanism of action of citalopram results from its inhibition of CNS neuronal reuptake of serotonin (5-HT) . The molecular target for citalopram is the serotonin transporter (solute carrier family 6 member 4, SLC6A4), inhibiting its serotonin reuptake in the synaptic cleft .

Nitalapram binds with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs . This drug has no or neglible affinity for 5-HT1A, 5-HT2A, dopamine D1 and D2, α1-, α2-, and_ β­ adrenergic, _histamine H1, gamma-aminobutyric acid (GABA), muscarinic, cholinergic, and benzodiazepine receptors. Antagonism of muscarinic, histaminergic, and adrenergic receptors is thought to be associated with several anticholinergic, sedative, and cardiovascular effects of other psychotropic drugs .

Dosage

Nitalapram dosage

Depressive illness 20 mg daily as a single dose in the morning or evening; increased ifnecessary to maximum 60 mg daily (Elderly maximum 40 mgdaily).Panic disorder Initially 10 mg daily, increased to 20 mg after 7 days; usual dose 20-30 mg daily; maximum 60 mg daily (Elderly maximum 40 mgdaily).

Side Effects

SSRIs are less sedating and have fewer antimuscarinic and cardiotoxic effects than tricyclic antidepressants. However, side-effects may be seen, includes gastro-intestinal effects (nausea, vomiting, dyspepsia, abdominal pain, diarrhoea, constipation), anorexia with weight loss, palpitations, tachycardia, postural hypotension, cough, confusion, impaired concentration, amnesia, urinary retention, sweating, movement disorders, urticaria, anaphylaxis, arthralgia, myalgia and photosensitivity.

Toxicity

Oral (Human) LD: 56 mg/kg Intraperitoneal (Mouse) LD50: 179 mg/kg

Acute toxicity

Symptoms of toxicity include dizziness, sweating, nausea, vomiting, tremor, somnolence, and sinus tachycardia. Rarely, symptoms included amnesia, confusion, coma, convulsions, hyperventilation, cyanosis, rhabdomyolysis, and ECG changes (including QTc prolongation, nodal rhythm, ventricular arrhythmia, and extremely rare cases of cardiac torsade de pointes) may occur. Acute renal failure has been a rare occurrence .

In cases of overdose, establish and maintain the airway to ensure adequate ventilation and oxygen delivery. Due to the large volume of distribution of citalopram, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit. Gastric evacuation by lavage and use of activated charcoal should be considered. Careful observation and cardiac and vital sign monitoring are advised, in addition to supportive care. With the large volume of distribution of citalopram, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit .

Pregnancy

This drug is categorized as pregnancy category C. In animal reproduction studies, citalopram has been shown to have adverse effects on embryo/fetal and postnatal development, which includes teratogenic effects when given at doses higher than human therapeutic doses. There are no sufficient and well-controlled studies in pregnant women; therefore, citalopram should be used during pregnancy only in cases where the potential benefit justifies the possible risk to the fetus .

Pregnancy-Nonteratogenic Effects

Neonates exposed to celexa and other SSRIs or SNRIs, late in the third trimester, have undergone complications requiring prolonged hospitalization, respiratory support, and parenteral feeding. Complications such as these can arise immediately upon delivery .

Nursing Mothers

Nitalapram is excreted in human breast milk. There have been two reports of infants demonstrating high levels of somnolence, reduced feeding, and weight loss associated with breastfeeding from a mother taking citalopram. In one specific case, the infant was reported to recover completely after the discontinuation of citalopram. In the second case, no follow-up information was available for assessment. The decision whether to continue or discontinue either nursing or celexa should consider the risks of citalopram exposure for the infant versus the benefits of celexa treatment for the mother .

Precaution

Caution should be taken in patients with epilepsy, concurrent electroconvulsive therapy, history of mania, cardiac disease, diabetes mellitus, angle-closure glaucoma, history of bleeding disorders, hepatic and renal impairment. Abrupt withdrawal of Nitalapram should be avoided.

Interaction

Ketoconazole, Itraconazole or Macrolide antibiotics and Nitalapram co-administration decreases the metabolism of Nitalapram. Omeprazole and Nitalapram co-administration might decrease the clearance of Nitalapram.

Food Interaction

  • Avoid alcohol.
  • Avoid St. John's Wort.
  • Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

12 L/kg

Nitalapram is highly lipophilic and likely widely distributed throughout the body, including the blood-brain-barrier. However, its metabolite, demethylcitalopram does not penetrate the blood-brain-barrier well .

Elimination Route

Rapidly and well absorbed from the GI tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Bioavailability is 80% following oral administration. Food does not affect absorption .

Half Life

About 35 hours .

Clearance

The systemic clearance of citalopram is 330 mL/min, with approximately 20% renal clearance .

Elimination Route

12-23% of an oral dose of citalopram is found unchanged in the urine, while 10% of the dose is found in the faeces .

Pregnancy & Breastfeeding use

PregnancyThere are no adequate and well-controlled studies in pregnant women; therefore, Nitalapram should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

LactationNitalapram is excreted in human breast milk. So, the decision whether to continue or discontinue either nursing or Nitalapram therapy should take into account the risks of Nitalapram exposure for the infants and the benefits of Nitalapram treatment for the mother.

Contraindication

Nitalapram should not be used if the patient enters a manic phase. Concomitant use in patients taking MAO inhibitor is contraindicated. Nitalapram is contraindicated in patients with a hypersensitivity to this drug or any of its ingredients.

Acute Overdose

It is a very safe drug. There were no reports of fatal Nitalapram overdose in clinical trials involving overdoses of up to 2000 mg.

Symptoms: Dizziness, sweating, nausea, vomiting, tremor, somnolence and sinus tachycardia. Rarely, amnesia, confusion, coma, seizures, hyperventilation, cyanosis, rhabdomyolysis and ECG changes (e.g. QT prolongation, sinus bradycardia, ventricular arrhythmias, nodal rhythm, torsade de pointes and left bundle branch block).

Management: Symptomatic and supportive treatment. Maintain and ensure adequate ventilation and oxygenation. Gastric evacuation by lavage and use of activated charcoal should be considered. Frequently monitor cardiac function and vital signs.

Interaction with other Medicine

Ketoconazole, Itraconazole or Macrolide antibiotics and Nitalapram co-administration decreases the metabolism of Nitalapram. Omeprazole and Nitalapram co-administration might decrease the clearance of Nitalapram.

Storage Condition

Store at 25° C.

Innovators Monograph

You find simplified version here Nitalapram

Nitalapram contains Citalopram see full prescribing information from innovator Nitalapram Monograph, Nitalapram MSDS, Nitalapram FDA label

FAQ

What is Nitalapram used for?

It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia. Nitalapram helps many people recover from depression, and has fewer unwanted side effects than older antidepressants. 

How safe is Nitalapram?

Nitalapram is safe to take for a long time. A few people may get sexual side effects, such as problems getting an erection or a lower sex drive. In some cases these can continue even after stopping the medicine. Speak to your doctor if you are worried.

How does Nitalapram work?

Nitalapram work by increasing the amount of serotonin, a natural substance in the brain that helps maintain mental balance.

What are the common side effects of Nitalapram?

Common side effects of Nitalapram are include;

  • nausea
  • diarrhea
  • constipation
  • vomiting
  • stomach pain
  • heartburn
  • decreased appetite
  • weight loss
  • frequent urination
  • excessive tiredness
  • yawning
  • weakness
  • uncontrollable shaking of a part of the body
  • muscle or joint pain
  • dry mouth
  • changes in sex drive or ability
  • heavy menstrual periods

Is Nitalapram safe during pregnancy?

Generally, these Nitalapram are an option during pregnancy: Certain selective serotonin reuptake inhibitors (SSRIs). SSRIs are generally considered an option during pregnancy, including Nitalapram and sertraline. Potential complications include maternal weight changes and premature birth.

Is Nitalapram safe during breastfeeding?

Several studies have shown that small amounts of Nitalapram are found in breast milk. There have been a few cases of sleepiness and weight loss, but in most studies no harmful effects were seen in breastfed babies.

Can I drink alcohol with Nitalapram?

You can drink alcohol while taking Nitalapram, but it may make you feel sleepy. It might be best to stop drinking alcohol until you see how the medicine makes you feel.

Can I drive after taking Nitalapram?

Do not drive or operate machinery until the full effects of Nitalapram are known as it may impair your judgment and affect your ability to drive or operate machinery.

How quickly does Nitalapram enter my system?

It usually takes 4 to 6 weeks for citalopram to work. Side effects such as tiredness, dry mouth and sweating are common.

When should be taken of Nitalapram?

You can take it with or without food. You can take Nitalapram at any time of day, as long as you stick to the same time every day. If you have trouble sleeping, it's best to take it in the morning.

How often can I take Nitalapram?

Take Nitalapram once a day.

How long does Nitalapram take to work?

It usually takes 4 to 6 weeks for Nitalapram to work.

How long can I take Nitalapram ?

Most people take Nitalapram for 6 months. But in some instances, a doctor may prescribe this substance for 9 months. Long-term use of antidepressants may put people at risk for type 2 diabetes, and SSRIs may cause heart rhythm abnormalities at higher doses.

Who should not take Nitalapram?

You should not use Nitalapram if you also take pimozide, as the combination can cause problems with your heart rhythm. Nitalapram can cause a serious heart problem. Call your doctor right away if you have chest pain, fast or pounding heartbeats, shortness of breath, and sudden dizziness. Do not use Nitalapram if you have used a MAO inhibitor in the past 14 days (such as isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, or tranylcypromine) or have received a methylene blue injection. A fatal reaction may occur.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What will happen If I stop taking Nitalapram ?

Stopping Nitalapram abruptly may result in one or more of the following withdrawal symptoms: irritability, nausea, feeling dizzy, vomiting, nightmares, headache, and/or paresthesias (prickling, tingling sensation on the skin).

What happens if I overdose?

Nitalapram overdoses often have only mild to moderate symptoms, particularly with ingestions under 600 mg in adults. However, with higher doses, severe manifestations have been described, including QTc prolongation, TdP, and seizures.

Will Nitalapram affect my fertility?

For women, there's no firm evidence to suggest that taking Nitalapram will reduce your fertility. But speak to a pharmacist or your doctor if you're trying to get pregnant.

Can Nitalapram affects my heart ?

Taking Nitalapram may put you at higher risk of a serious heart rhythm change called QT prolongation, which can cause sudden death. People with slow heart rate, recent heart attack, or severe heart failure should also not take Nitalapram.

Can Nitalapram affect my kidneys?

Nitalapram may build up and cause more side effects in people with severe kidney disease.

*** Taking medicines without doctor's advice can cause long-term problems.
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