Nortrilen
Nortrilen Uses, Dosage, Side Effects, Food Interaction and all others data.
Nortrilen, a dibenzocycloheptadiene tricyclic antidepressant, is the primary active metabolite of amitriptyline. It increases synaptic concentration of serotonin and/or norepinephrine in the CNS by blocking the neuronal reuptake of norepinephrine and serotonin.
Nortrilen exerts antidepressant effects likely by inhibiting the reuptake of serotonin and norepinephrine at neuronal cell membranes. It also exerts antimuscarinic effects through its actions on the acetylcholine receptor.
| Trade Name | Nortrilen |
| Availability | Prescription only |
| Generic | Nortriptyline |
| Nortriptyline Other Names | Demethylamitriptyline, Desmethylamitriptyline, Nortriptylina, Nortriptyline, Nortriptylinum |
| Related Drugs | Rexulti, sertraline, trazodone, Lexapro, amitriptyline, venlafaxine, Zoloft, citalopram, Cymbalta, Effexor XR |
| Type | |
| Formula | C19H21N |
| Weight | Average: 263.3767 Monoisotopic: 263.167399677 |
| Protein binding | The plasma protein binding of nortriptyline is approximately 93%. |
| Groups | Approved |
| Therapeutic Class | Tricyclic & related anti-depressant drugs, Tricyclic Anti-depressant |
| Manufacturer | |
| Available Country | Netherlands, Switzerland, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nortrilen is used for the treatment of depression and nocturnal enuresis.
Nortrilen is also used to associated treatment for these conditions: Irritable Bowel Syndrome (IBS), Major Depressive Disorder (MDD), Myofascial Pain Syndrome, Orofacial Pain, Pain, Chronic, Post-Herpetic Neuralgia (PHN)
How Nortrilen works
Though prescribing information does not identify a specific mechanism of action for nortriptyline, is believed that nortriptyline either inhibits the reuptake of the neurotransmitter serotonin at the neuronal membrane or acts at the level of the beta-adrenergic receptors. It displays a more selective reuptake inhibition for noradrenaline, which may explain increased symptom improvement after nortriptyline therapy. Tricyclic antidepressants do not inhibit monoamine oxidase nor do they affect dopamine reuptake. As with other tricyclics, nortriptyline displays affinity for other receptors including mACh receptors, histamine receptors, 5-HT receptors, in addition to other receptors.
Dosage
Nortrilen dosage
Depression:
- Adult: Low dose initially increased as necessary to 75-100 mg daily in divided doses or as a single dose (max. 150 mg daily)
- Adolescent & Elderly: 30-50 mg daily in divided doses; Child not recommended for depression
Nocturnal enuresis:
- Child 7 years: 10 mg
- 8-11 years: 10-20 mg
- Over 11 years: 25-35 mg, 30 minutes before bedtime; max period of treatment (including gradual withdrawal) 3 months- full physical examination and ECG before further course.
Side Effects
The most common side effects include dry mouth, sedation, constipation and increased appetite, mild blurred vision, tinnitus, often euphoria and mania. An occasional side effect is a rapid or irregular heartbeat. Alcohol may exacerbate some of its side effects and should be avoided.
Toxicity
The oral LD50 of nortriptyline in the rat is 405 mg/kg.Symptoms of overdose with nortriptyline include cardiac arrhythmias, severe hypotension, shock, congestive heart failure, pulmonary edema, convulsions, coma, and CNS depression. Changes in the electrocardiogram, particularly in QRS segment, may be indicative of tricyclic antidepressant toxicity.
Precaution
Not intended for treatment of bipolar depression. Avoid abrupt withdrawal. Patient at risk of seizures, with DM, narrow angle glaucoma, urinary retention, prostatic hyperplasia, chronic constipation, history of CV disease. Renal and hepatic impairment. Elderly, childn. Pregnancy and lactation.
Interaction
Nortrilen should not be given with adrenaline, ephedrine, isoprenaline, noradrenaline, phenylephrine, phenylpropanolamine, drugs that are metabolized by CYP4502D6, MAOIs, guanethidine, debrisoquine, bethanidine, clonidine and reserpine etc. Barbiturates may increase the rate of metabolism of nortriptyline.
Food Interaction
- Avoid alcohol.
- Take with or without food. Food decreases gastrointestinal irritation.
Nortrilen Alcohol interaction
[Moderate] GENERALLY AVOID:
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.
Nortrilen Drug Interaction
Major: duloxetine, cyclobenzaprine, escitalopram, topiramate, ondansetron, sertralineModerate: zolpidem, diphenhydramine, pregabalin, acetaminophen / hydrocodone, levothyroxine, alprazolam, cetirizineUnknown: aspirin, omega-3 polyunsaturated fatty acids, esomeprazole, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
Nortrilen Disease Interaction
Major: anticholinergic effects, cardiovascular disease, pheochromocytoma, acute myocardial infarction recovery, cardiovascular disease, depression, seizure disordersModerate: bone marrow suppression, diabetes, renal/liver disease, schizophrenia/bipolar disorder, tardive dyskinesia, acute alcohol intoxication, bipolar disorder screening, glaucoma, hyper/hypoglycemia, liver/renal disease, neutropenia, schizophrenia, thyroid disorders, urinary retention
Volume of Distribution
The apparent volume of distribution (Vd)β, estimated after intravenous administration is 1633 ± 268 L within the range of 1460 to 2030 (21 ± 4 L/kg). Nortrilen crosses the placenta and is found in the breast milk. It distributes to the heart, lungs, brain, and the liver.
Elimination Route
Nortrilen is readily absorbed in the gastrointestinal tract with extensive variation in plasma levels, depending on the patient. This drug undergoes first-pass metabolism and its plasma concentrations are attained within 7 to 8.5 hours after oral administration. The bioavailability of nortriptyline varies considerably and ranges from 45 to 85%.
Half Life
The average plasma half-life of nortriptyline in healthy volunteers is about 26 hours, but is said to range from 16 to 38 hours. One study mentions a mean half-life of about 39 hours.
Clearance
The average plasma clearance of nortriptyline in a study of healthy volunteers was 54 L/h. The average systemic clearance of nortriptyline is 30.6 ± 6.9 L / h, within the range of 18.6 to 39.6 L/hour.
Elimination Route
Nortrilen and its metabolites are mainly excreted in the urine, where only small amounts (2%) of the total drug is recovered as unchanged parent compound. Approximately one-third of a single orally administered dose is excreted in urine within 24 hours. Small amounts are excreted in feces via biliary elimination.
Pregnancy & Breastfeeding use
The safety of nortriptyline for use in pregnancy has not been established. Nortrilen should only be given during pregnancy when there are no alternatives and benefit outweighs risk.
Contraindication
Nortrilen is contraindicated in patients with hypersensitivity to nortriptyline. Concomitant administration with MAOI is contraindicated. Do not use with or within 2 weeks of stopping an MAOI. Nortrilen is contraindicated during the acute recovery period after myocardial infarction.
Acute Overdose
Symptoms: Severe hypotension, cardiac dysrhythmias, shock, CHF, pulmonary oedema, convulsions, and CNS depression, including coma; changes in ECG.
Management: Symptomatic and supportive treatment. Admin IV Na bicarbonate, benzodiazepines. Admin activated charcoal to reduce absorption. Emesis is contraindicated. Initiate cardiac monitoring and observe for signs of CNS or resp depression, hypotension, cardiac dysrhythmias and/or conduction blocks, and seizures.
Storage Condition
Store at 15-30° C. Protect from light and moisture.
Innovators Monograph
You find simplified version here Nortrilen
Nortrilen contains Nortriptyline see full prescribing information from innovator Nortrilen Monograph, Nortrilen MSDS, Nortrilen FDA label
FAQ
What is Nortrilen used for?
Nortrilen is used to treat depression. Nortrilen is in a group of medications called tricyclic antidepressants. It works by increasing the amounts of certain natural substances in the brain that are needed to maintain mental balance.
Is Nortrilen a sleeping pill?
Your doctor prescribed Nortrilen to help relieve your pain. Although it is often used to treat depression, it is also used for pain and to improve sleep. It has been found to be safe and effective over many years of use.
What are side effects of Nortrilen?
Some of the side effects that can occur with use of Nortrilen include:
- low blood pressure
- high blood pressure
- confusion (mainly in seniors)
- sleep problems
- shakiness
- dry mouth
- blurry vision
- constipation
- skin rash
- hives
- itching
- skin sensitivity to light
- nausea
- vomiting
- diarrhea
- stomach cramps
- decreased sexual desire
- unexpected weight loss or gain
- sweating
- headache
If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.
How does Nortrilen works?
Nortrilen (Nortriptyline) belongs to a class of drugs called tricyclic antidepressants. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions. Nortrilen works on your central nervous system to increase the level of certain chemicals in your brain. This helps relieve your depression.
What is Nortrilen?
Nortrilen is a prescription drug. It comes as an oral capsule and an oral solution. Nortrilen oral capsule is available as the Nortrilen-name drug Pamelor. It’s also available as a generic drug. Generic drugs usually cost less than the Nortrilen-name version. In some cases, they may not be available in all strengths or forms as the Nortrilen-name drug.
What does Nortrilen used for?
Nortrilen is used to treat depression. Nortrilen may used as part of a combination therapy. This means you may need to take it with other medications.
What is Dosage of Nortrilen for depression?
Adult dosage (ages 18–64 years)
- Recommended dosage: 25 mg, three to four times per day or once daily; start at the low level and increase as required.
- Maximum dosage: 150 mg per day.
Child dosage (ages 0–17 years)
- This drug is not recommended for use in children.
Senior dosage (ages 65 years and older)
- Recommended dosage: 30–50 mg, once per day or in divided doses; start at the low level and increase as required.
- Maximum dosage: 150 mg per day.
Does Nortrilen affect memory?
Performance on measures of immediate and delayed recognition memory were comparable on Nortrilen and placebo. Discontinuation of Nortrilen resulted in significant improvement on a subset of nine memory self-assessment items.
How long does Nortrilen take to work?
In depression it may take between two to four weeks before Nortrilen starts to work and you begin to feel better, so it's very important that you keep taking it, even if it doesn't seem to make much difference at first.
What should not take with Nortrilen?
Do not use nortriptyline with a monoamine oxidase (MAO) inhibitor (eg, isocarboxazid [Marplan®], linezolid (Zyvox®), methylene blue, phenelzine [Nardil®], selegiline [Eldepryl®], tranylcypromine [Parnate®]). Do not start using nortriptyline during the 2 weeks after you stop a MAO inhibitor.
Is Nortrilen used for nerve pain?
Nortrilen is a tricyclic antidepressant that is occasionally used for treating neuropathic pain, and is recommended in European, UK, and USA guidelines.
What does Nortrilen do for migraines?
Nortrilen is a tricyclic antidepressant. This class of medications works on the central nervous system by increasing the level of serotonin in your brain. Serotonin drops when a migraine attack strikes.
Can I drink coffee while taking Nortrilen?
Nortrilen may irritate the stomach, and should be taken with food. It is best to avoid coffee, spicy food or alcohol.
Can I drink alcohol with Nortrilen?
Your doctor will recommend that you do not drink alcohol while you are on Nortrilen. This is because it increases the risk of side-effects, such as feeling sleepy.
Is Nortrilen an anti inflammatory?
Except nortriptyline and citalopram, all tested drugs showed anti-inflammatory activity.
What happens when I stop taking Nortrilen?
Nortrilen is a tricyclic anti-depressant. Abrupt discontinuation (withdrawal) of tricyclic anti-depressants can cause symptoms of restlessness, anxiety, chills, muscle pain, headache, dizziness, nausea and vomiting. Symptoms can be reduced by slowly reducing the dose.
Why do I take Nortrilen at night?
The best time to take Nortrilen is in the evening. This has the added advantage of helping you to sleep. The other most noticeable side effect that people find is a dry mouth.
Is Nortrilen well tolerated?
Generally well tolerated and has fewer side effects than other medicines in the same class of drugs.
Is Nortrilen good for sciatica?
Although sciatica is common, there are no good treatments for it. Tricyclic antidepressants, such as Nortrilen (nortriptyline), and opioids, such as morphine, have been effective in treating other kinds of pain from nerve damage.
