- March 15, 2022
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Brand Name :
Aventyl, pamelor
Synonyms :
nortriptyline
Class :
Typical antidepressants
Dosage Forms & Strengths
Capsule
10mg
20mg
50mg
75mg
Oral solution
10mg/5ml
25
mg
Orally
every 6 -8 hours
Capsule
Do not exceed 150mg/day
75
mg
Orally
everyday
Capsule
attention-deficit/hyperactivity disorder (ADHD)
25
mg
Orally
every 6-8 hours
Capsule
25mg orally every day
Dosage Forms & Strengths
Capsule
10mg
20mg
50mg
75mg
Oral solution
10mg/5ml
<6 years: Safety and efficacy not established
6-12 years:1-3mg/kg/day orally divided every 6-8 hours
>12 hours:30-50mg orally every day
attention-deficit/hyperactivity disorder (ADHD)
0.5mg/kg/day orally, increase to a maximum 2mg/kg/day or 100mg
Indicated for Nocturnal enuresis:
6-7 years:10mg orally whenever necessary
8-11 years: 10-20mg orally whenever necessary
>11 years: 25-30mg orally whenever necessary
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
may increase the toxic effects of agents with seizure threshold, lowering potential
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the toxic effects of CNS depressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the CNS depressants effects of CNS depressants
may increase the CNS depressants effects of CNS depressants
QT-prolonging Strong may enhance the QTc-prolonging effect of delamanid
may enhance the QTc-prolonging effect of Fluorouracil Products
may increase the anticholinergic effect of anticholinergic agents
may decrease the therapeutic effects
may decrease the therapeutic effects
may decrease the therapeutic effects
may decrease the therapeutic effects
may decrease the therapeutic effects
may increase the anticholinergic effect of anticholinergic agents
may increase the arrhythmogenic effect
may increase the CNS depressants effects of CNS depressants
may increase the anticholinergic affect
may increase the serotonergic effect of tricyclic antidepressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the serotonergic effect of tricyclic antidepressants
may increase the serotonergic effect of tricyclic antidepressants
when used together, encorafenib and nortriptyline both increase the QTc interval
may enhance the QTc-prolonging effect of Nilotinib
glycopyrrolate inhaled and formoterol
may increase the QTc interval when combined
it may enhance the QTc-prolonging effect of QT-Prolonging Anesthetics
it may enhance the QTc-prolonging effect of QT-Prolonging Anesthetics
it may enhance the QTc-prolonging effect of QT-Prolonging Anesthetics
it may enhance the QTc-prolonging effect of QT-Prolonging Anesthetics
it may enhance the QTc-prolonging effect of QT-Prolonging Anesthetics
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the arrhythmogenic affect
may increase the arrhythmogenic affect
may increase the arrhythmogenic affect
may increase the arrhythmogenic affect
may enhance the serum concentration
It may enhance the QTc interval when combined with efavirenz
both lapatinib and nortriptyline increase the QTc interval
fedratinib increases the effect of nortriptyline by altering the intestinal/ hepatic CYP2D6 enzyme metabolism
when both drugs are combined, there may be an increase in the serum concentration of nortriptyline
it may enhance the QTc-prolonging effect of levoketoconazole
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
may enhance the QTc-prolonging effect of other QT-prolonging Agents
Mechanism of action
The mechanism of action of TCAs is not fully understood, but it is thought to involve the inhibition of the reuptake of the neurotransmitter’s serotonin and norepinephrine in the brain. This leads to increased levels of these neurotransmitters, which are thought to regulate mood and emotions. It is also a strong antihistamine, and it can block the reuptake of norepinephrine and serotonin.
Spectrum
The spectrum of activity of nortriptyline is primarily used to treat depression. It is also a second-line neuropathic pain, anxiety, and insomnia treatment. Nortriptyline has also been found to be effective in treating symptoms of attention-deficit/hyperactivity disorder (ADHD), and it has been used as an adjunctive treatment for smoking cessation.
Frequency undefined:
Lethargy
Weakness
Constipation
Agitation
Headache
Nausea
Sweating
Confusion
Increased LFT
Seizure
Eosinophilia
Thrombocytopenia
Fatigue
Sedation
Dry mouth
Blurred vision
Anxiety
Insomnia
Vomiting
Orthostatic hypotension
Rash
Sexual dysfunction
Agranulocytosis
Leukopenia
Post-marketing reports
Brugada syndrome
Black box warning
Antidepressants have been found to increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 years) taking antidepressants for major depressive disorders or other psychiatric illnesses. This risk does not appear to be present in adults over 24 years, and a slight decrease in suicidal thinking may be seen in adults over 65.
It is essential for patients and their families to closely monitor for changes in behavior, clinical worsening, and suicidal tendencies and to communicate any abrupt changes to the healthcare provider. Worsening behavior and suicidal tendencies that are not part of the original symptoms may require discontinuation of therapy. It is important to note that this drug is not approved for pediatric patients.
Contraindications
It is contraindicated in certain situations, such as in patients with hypersensitivity or those taking drugs or conditions that prolong the QT interval. It should not be used during acute recovery post-MI. It is also contraindicated for coadministration with serotonergic drugs or within 14 days of MAOIs (monoamine oxidase inhibitors) as it may cause serotonin syndrome. Starting nortriptyline in a patient treated with linezolid or IV methylene blue is also contraindicated because of an increased risk of serotonin syndrome. If linezolid or IV methylene blue must be administered, discontinue nortriptyline immediately and monitor for CNS toxicity. Nortriptyline may be resumed 24 hours after the last linezolid or methylene blue dose or after two weeks of monitoring, whichever comes first.
Caution
Pregnancy consideration: D
Lactation: Excretion of the drug in human breast milk is known
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
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
It is a tricyclic antidepressant medication used to treat depression and other mental health conditions. It increases the levels of certain neurotransmitters in the brain, such as norepinephrine and serotonin. These neurotransmitters are thought to play a role in regulating mood and other cognitive functions.
Pharmacodynamics
It selectively blocks the reuptake of norepinephrine and serotonin, which leads to an increase in the levels of these neurotransmitters in the synaptic cleft. This, in turn, leads to an enhancement of neurotransmission and a modulation of various neuronal receptors, ultimately improving mood and other cognitive functions.
It also has antihistaminic solid, anticholinergic, and anti-alpha-adrenergic properties. Its antihistaminic properties contribute to its sedative effects, while its anticholinergic properties contribute to its dry mouth, constipation, and blurred vision side effects. Its anti-alpha-adrenergic properties contribute to its orthostatic hypotension side effect.
Additionally, it has a weak inhibitory effect on the enzyme monoamine oxidase (MAO), which may also contribute to its antidepressant effects.
Pharmacokinetics
Absorption
It is an oral medication rapidly absorbed and reaches peak plasma levels within 7-8.5 hours after administration. The onset of therapeutic action is usually within 1-3 weeks of starting treatment. The steady-state therapeutic plasma concentration is typically between 50-150 ng/mL.
Distribution
It is highly protein-bound, with a protein binding rate of 93-95%. Its volume of distribution is 21 L/kg, which indicates that it distributes well throughout the body.
Metabolism
It is metabolized in the liver by the enzyme CYP2D6.
Elimination/excretion
The metabolites of nortriptyline are eliminated primarily through the urine and feces, with a half-life of 28-31 hours, which means it remains in the body for about 1 to 2 days.
Administration
Patient information leaflet
Generic Name: nortriptyline
Pronounced: [ nor-TRIP-ti-leen ]
Why do we use nortriptyline?
It is a tricyclic antidepressant medication used to treat depression and other mental health conditions. Some of the primary uses of nortriptyline include:
Depression: It is used to treat major depressive disorder in adults. It helps to improve mood and reduce symptoms of depression, such as sadness, hopelessness, and loss of interest in activities.
Anxiety disorders: It may also treat anxiety disorders such as generalized anxiety and panic disorders.
Chronic pain: It is also an adjunctive treatment for chronic pain conditions such as neuropathic pain and chronic headaches.
Attention deficit hyperactivity disorder (ADHD): It is an adjunctive therapy for ADHD in children and adolescents.
Insomnia: It is used as a sleep aid for patients with insomnia
Migraine: It is also used as a prophylactic treatment for migraines
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