Maprotiline (Ludiomil) is a tetracyclic antidepressant drug that may be used to treat patients with depression.

Alternatively, it may be classified as a tricyclic antidepressant drug.

Maprotiline Uses:

• Depression:

  • Helping people with major depressive disorder (MDD) and anxiety connected to depression.

Maprotiline Dose in Adults:

Maprotiline Dose in the treatment of Depression:

• Oral:

  • Start with 25 to 75 mg once a day or split into multiple doses.

  • After two weeks, increase by 25 mg increments based on how well it's working and how well it's tolerated.

  • The typical dose is 150 to 225 mg once a day or divided into multiple doses.

  • The highest dose should not exceed 225 mg per day.

  • If someone is in the hospital with severe depression, they might begin with higher starting doses of 100 to 150 mg per day.

Discontinuation of therapy:

• When you stop taking antidepressants after using them for more than three weeks, it's recommended to gradually reduce the dose over 2 to 4 weeks.

• This helps minimize withdrawal symptoms and allows for the detection of returning symptoms.

• If a medication has a short half-life (like paroxetine or venlafaxine), if there's a history of withdrawal symptoms, or if someone is on high doses, a slower taper may be necessary.

• If withdrawal symptoms become too severe, you may need to go back to the previous dose or decrease the dose more slowly.

• For certain patients, especially those with a history of discontinuation syndrome, tapering over more extended periods (more than three months) might be beneficial.

• It's important to note that there's limited evidence on the ideal tapering rates, and the approach should be individualized based on the patient's specific situation.

• Always consult with a healthcare professional when making decisions about stopping or changing antidepressant medications.

Switching antidepressants:

• There's limited information on the best techniques for switching antidepressants.

• Two common methods are cross-titration, where you gradually reduce the first antidepressant while gradually increasing the new one, and straight changeover, which involves abruptly stopping the first antidepressant and then starting the new one at an equivalent or lower dose and increasing it gradually.

• When transitioning to or from a monoamine oxidase inhibitor (MAOI), cross-titration is generally not recommended.

• The process may take 1 to 4 weeks, depending on sensitivity to withdrawal symptoms and adverse effects.

• If the antidepressant to be stopped has been used for less than a week or if discontinuation is due to side effects, a direct changeover to another agent in the same or a similar class (e.g., switching between two SSRIs) might be the preferred approach.

• When deciding on the switching method, consider factors such as the risk of withdrawal symptoms, potential medication interactions, characteristics of the antidepressants (including half-life, adverse effects, and pharmacodynamics), and the desired level of symptom control.

• Always consult with a healthcare professional to determine the most suitable approach based on individual circumstances.

• Switching to or from an MAOI:

  • It's crucial to wait for a period of 14 days before starting maprotiline after discontinuing a monoamine oxidase inhibitor (MAOI).
  • Similarly, when transitioning from maprotiline to an MAOI, it's recommended to separate the two medications by a 14-day interval.
  • This precaution helps minimize the risk of potential interactions and adverse effects that can occur when combining these medications or switching between them too quickly.
  • Always follow the guidance and recommendations of your healthcare professional when making changes to your medication regimen.

Use in Children:

Not indicated.

Pregnancy Risk Factor B

• The use of maprotiline during pregnancy is not known to have any significant effects, but it's essential to approach the treatment of depression during pregnancy with caution and consideration.

• For pregnant individuals dealing with depression, a personalized treatment plan is recommended.

• This plan should be developed collaboratively by mental healthcare providers, obstetricians, and primary care providers, taking into account the unique needs and circumstances of the individual.

• The American Psychiatric Association emphasizes that medication treatment for depression during pregnancy carries risks, but these risks should be carefully weighed against the potential negative effects of untreated depression.

• If a woman has discontinued antidepressant medication during pregnancy and is at risk of postpartum depression, it's generally considered safe to resume the medication after delivery.

• Both the American College of Obstetricians and Gynecologists (ACOG) and the American Psychiatric Association (APA) have developed treatment algorithms to guide healthcare providers in managing depression in women before conception and during pregnancy.

• These algorithms aim to provide a structured approach to balancing the risks and benefits of various treatment options while considering the well-being of both the mother and the developing fetus.

Use of maprotiline during breastfeeding

• It's important to note that maprotiline, an antidepressant, is present in breast milk at a concentration similar to that found in the mother's bloodstream.

• This suggests that the medication can be transferred to the infant through breastfeeding.

• It's crucial for breastfeeding individuals taking maprotiline to exercise caution.

• Before making any decisions about medication use during breastfeeding, it's advisable to consult with a healthcare professional.

• They can provide personalized advice based on the specific circumstances, weighing the potential benefits of the medication against any potential risks to the infant.

• Healthcare providers may consider alternative medications or closely monitor the infant for any signs of adverse effects if maprotiline is used during breastfeeding.

• The safety of medications during breastfeeding is an individualized decision that should be made in consultation with a healthcare professional.

Maprotiline dose in Kidney Disease:

• If there are no dosage adjustments provided in the manufacturer's labeling for maprotiline in the context of kidney disease, it is essential to consult with a healthcare professional for personalized advice.

• While maprotiline may not be extensively metabolized by the kidneys, individual variations and the specific condition of a person's kidneys can still influence the medication's clearance from the body.

• In the absence of specific dosage recommendations in the manufacturer's labeling, a healthcare provider may consider factors such as the severity of kidney disease, other medications being taken, and the overall health of the individual.

• A healthcare professional may opt to monitor the individual closely for any signs of adverse effects and adjust the dosage accordingly.

• It's crucial to work collaboratively with your healthcare provider to ensure that the medication is used safely and effectively, taking into account your specific health profile and medical history.

Maprotiline dose in Liver disease:

• If the manufacturer's labeling for maprotiline does not provide specific dosage adjustments for kidney disease, it's important to follow your healthcare provider's guidance.

• In such cases, healthcare professionals often need to carefully assess the individual's kidney function, overall health, and other medications being taken to determine the appropriate dosage.

• Since the manufacturer's labeling does not offer specific recommendations, your healthcare provider may decide to monitor you more closely for any potential side effects or adverse reactions.

• They may also consider alternative medications or adjust the dosage based on their clinical judgment.

• Always consult with your healthcare provider before making any changes to your medication regimen, especially when dealing with conditions like kidney disease where careful consideration of drug dosages is crucial.

• They can provide personalized advice based on your specific health situation.

Common Side Effects of Maprotiline:

• Central nervous system:

  • Drowsiness

• Gastrointestinal:

  • Xerostomia

Less Common Side Effects of Maprotiline:

• Central Nervous System:

  • Agitation
  • Headache
  • Nervousness
  • Anxiety
  • Fatigue
  • Insomnia
  • Dizziness

• Gastrointestinal:

  • Nausea
  • Constipation

• Neuromuscular & Skeletal:

  • Tremor
  • Weakness

• Ophthalmic:

  • Blurred Vision

Contraindications to Maprotiline:

• If you can't tolerate maprotiline or its ingredients, it's best to avoid it.

• For those with a history of seizures, maprotiline might not be suitable, and alternatives should be discussed with a doctor.

• Using maprotiline with MAO inhibitors or within 14 days of stopping either can be risky and may lead to serotonin syndrome.

• If recovering from a recent heart attack, using maprotiline requires careful consideration due to potential risks; consult a doctor for guidance.

Warnings and precautions

• Anticholinergic effects

  • This antidepressant may cause some side effects related to anticholinergic effects, such as constipation, dry mouth (xerostomia), and blurred vision.

  • People with conditions like reduced gastrointestinal motility, paralysis and ileus, urinary retention, benign prostatic hyperplasia (BPH), dry mouth, and visual impairments should be cautious when using it.

  • It's important to note that this antidepressant has a moderate level of anticholinergic blocking, which means it can affect certain nerve signals in the body.

  • If you experience any discomfort or have concerns about these side effects, it's recommended to discuss them with your healthcare provider.

  • They can provide guidance on managing these effects or explore alternative treatment options if necessary.

• Depression in the CNS:

  • CNS (central nervous system) depression caused by this antidepressant can result in mental or physical impairment.
  • It's crucial to inform patients about activities that demand mental alertness, like driving or operating machinery.
  • In comparison to other antidepressants, the level of sedation from this medication can range from moderate to severe.
  • This information is important for patients to be aware of, ensuring their safety and the safety of others when engaging in activities that require focus and coordination.
  • Always follow the guidance provided by healthcare professionals regarding the use of medications and potential side effects.

• Fractures

  • Antidepressant treatment has been linked to an increased risk of bone fractures.
  • If someone taking antidepressants starts to feel unexplained bone pain or tenderness, notices swelling, or experiences unusual bleeding or bruising, it's important to consider the possibility of a fragility fracture.
  • Seeking medical attention and discussing these symptoms with a healthcare professional is crucial for proper evaluation and management.
  • Monitoring and addressing potential side effects are essential aspects of antidepressant treatment to ensure overall well-being.

• Ocular effects

  • Mild pupillary dilation may happen, and in some cases, it can increase the risk of narrow-angle glaucoma.

  • It's important to assess patients who haven't had an iridectomy (a surgical procedure to reduce the risk of narrow-angle glaucoma) to ensure their eye health and manage any potential risks associated with pupillary dilation.

  • Regular evaluation by an eye care professional is recommended in such cases.

  • If individuals experience changes in vision or other eye-related concerns, they should promptly consult their healthcare provider.

• Orthostatic hypotension

  • Orthostatic hypotension, a drop in blood pressure when standing up, may occur with this antidepressant, and the risk is moderate compared to some other antidepressants.
  • Patients at high risk for this effect or those who cannot tolerate temporary drops in blood pressure (due to conditions like cerebrovascular disease, cardiovascular disease, or hypovolemia) should use caution.
  • It's important for individuals taking this medication to be aware of the possibility of orthostatic hypotension and to report any symptoms or concerns to their healthcare provider.
  • Adjustments to the treatment plan may be necessary in some cases.

• Cardiovascular disease

  • Patients with a history of cardiovascular disease, such as a stroke, heart attack (MI), or tachycardia (rapid heart rate), should exercise caution when using this antidepressant.

  • This medication carries a moderate risk of causing conduction abnormalities in the heart, compared to some other antidepressants.

  • Monitoring and discussing any cardiovascular concerns with a healthcare provider is important to ensure the medication's safety and effectiveness for individuals with a history of heart-related conditions.

  • Adjustments to the treatment plan may be considered based on the individual's specific health situation.

• Diabetes:

  • Patients with diabetes mellitus should exercise caution when using this antidepressant, as it has the potential to alter glucose regulation.
  • Individuals with diabetes may need close monitoring of their blood sugar levels, and adjustments to their diabetes management plan may be necessary.
  • It's important for patients to communicate any changes in blood sugar control or other concerns to their healthcare provider.
  • This allows for proper management and coordination of care, ensuring the overall well-being of individuals with diabetes who are taking this medication.

• Hypomania/mania:

  • In individuals with bipolar disorder, there is a risk of experiencing episodes of mania or hypomania when using this antidepressant.

  • It is not recommended as a sole treatment for those with bipolar disorder.

  • Testing for bipolar disorder should be conducted on individuals who exhibit symptoms of depression.

  • When prescribed, it's important to provide comprehensive information, including details about past family relationships, thoughts of suicide, and feelings of despair.

  • Notably, the FDA has not approved maprotiline for treating bipolar depression.

  • Management of bipolar disorder often involves a more comprehensive treatment plan, including mood stabilizers or other medications specifically designed for bipolar disorder, under the guidance of a healthcare professional.

• Seizure disorder

  • Be careful when giving this medicine to people who are likely to have seizures, especially those who have had seizures before, brain damage, or head injuries.

  • If someone has a history of seizures, they shouldn't use this medication.

  • Start with a small amount of the medicine and increase it slowly until it works well to reduce the chance of having seizures.

Maprotiline: Drug Interaction

Monitoring parameters:

• Check the following things regularly, especially for patients with existing heart issues or those at a higher risk of prolonged QT effects:

• Blood pressure, heart rate, and ECG: Keep an eye on these for patients with preexisting heart problems or a higher risk of QT prolongation.

• Electrolytes: Measure potassium and magnesium levels at the beginning and as needed based on clinical indicators.

• Suicidal thoughts: Monitor for any signs of suicidal thoughts, both initially and whenever there's a change in dosage.

• Blood glucose: Check blood sugar levels at the start and as needed based on clinical signs.

• Weight and BMI: Measure weight and Body Mass Index (BMI) at the beginning and at regular intervals.

How to administer Maprotiline?

• Take this medication by mouth either once a day or as directed, spreading the doses if needed.

Mechanism of action of Maprotiline:

• It works by preventing the reabsorption of norepinephrine in the nerve cells, which leads to higher levels of norepinephrine in the central nervous system.

The beginning of action:

• People may react differently to the treatment.
• To assess whether a patient is showing improvement or not, it usually requires 4 to 8 weeks.

Absorption:

• It is absorbed gradually and thoroughly.

Protein binding:

• About 88% of the substance attaches or binds to proteins.

Metabolism:

• In the liver, active and inactive molecules are formed through processes such as aliphatic and aromatic hydroxylation, oxidative deamination, and N-demethylation.

Bioavailability:

• Approximately 65% to 72% of the substance is available and able to enter the bloodstream when taken.

Half-life elimination, serum:

• The time it takes for the concentration of the substance in the blood serum to reduce by half is approximately 28 to 105 hours.

Time to peak, serum:

• It takes about 8 to 24 hours for the substance to reach its highest concentration in the blood serum after administration.

Excretion:

• Approximately 70% of the substance is eliminated from the body through urine, while the remaining 30% is excreted through feces.

International Brands of Maprotiline:

• PMS-Maprotiline
• TEVA-Maprotiline
• Colese
• Epalon
• Keproline
• Ladiomil
• Ludiomil
• Ludiomil[inj.]
• Ludios
• Lunaline
• Maprolu
• Matilina
• Melodil
• Retinyl
• Sandepril

Maprotiline Brand Names in Pakistan: