Phenalzine
Phenalzine - General Information
One of the monoamine oxidase inhibitors used to treat depression; phobic disorders; and panic. [PubChem]
Pharmacology of Phenalzine
Phenalzine belongs to a class of antidepressants called monoamine oxidase inhibitors (MAOIs). Phenalzine works by irreversibly blocking the action of a chemical substance known as monoamine oxidase (MAO) in the nervous system. Within neurons, MAO appears to regulate the levels of monoamines released upon synaptic firing. Since depression is associated with low levels of monoamines, the inhibition of MAO serves to ease depressive symptoms.
Phenalzine for patients
Prescribers or other health professionals should inform patients, their families, and their caregivers about the benefits and risks associated with treatment with NARDIL and should counsel them in its appropriate use. A patient Medication Guide About Using Antidepressants in Children and Teenagers is available for NARDIL. The prescriber or health professional should instruct patients, their families, and their caregivers to read the Medication Guide and should assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have. The complete text of the Medication Guide is reprinted at the end of this document.
Patients should be advised of the following issues and asked to alert their prescriber if these occur while taking NARDIL.
Clinical Worsening and Suicide Risk: Patients, their families, and their caregivers should be encouraged to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation, especially early during antidepressant treatment and when the dose is adjusted up or down. Families and caregivers of patients should be advised to observe for the emergence of such symptoms on a day-to-day basis, since changes may be abrupt. Such symptoms should be reported to the patient's prescriber or health professional, especially if they are severe, abrupt in onset, or were not part of the patient's presenting symptoms. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in medication.
Medication Guide
About Using Antidepressants in Children and Teenagers
What is the most important information I should know if my child is being prescribed an antidepressant?
Parents or guardians need to think about 4 important things when their child is prescribed an antidepressant:
- There is a risk of suicidal thoughts or actions
- How to try to prevent suicidal thoughts or actions in your child
- You should watch for certain signs if your child is taking an antidepressant
- There are benefits and risks when using antidepressants
1. There is a Risk of Suicidal Thoughts or Actions
Children and teenagers sometimes think about suicide, and many report trying to kill themselves.
Antidepressants increase suicidal thoughts and actions in some children and teenagers. But suicidal thoughts and actions can also be caused by depression, a serious medical condition that is commonly treated with antidepressants. Thinking about killing yourself or trying to kill yourself is called suicidality or being suicidal.
A large study combined the results of 24 different studies of children and teenagers with depression or other illnesses. In these studies, patients took either a placebo (sugar pill) or an antidepressant for 1 to 4 months. No one committed suicide in these studies, but some patients became suicidal. On sugar pills, 2 out of every 100 became suicidal. On the antidepressants, 4 out of every 100 patients became suicidal.
For some children and teenagers, the risks of suicidal actions may be especially high.These include patients with
- Bipolar illness (sometimes called manic-depressive illness)
- A family history of bipolar illness
- A personal or family history of attempting suicide
If any of these are present, make sure you tell your health care provider before your child takes an antidepressant.
2. How to Try to Prevent Suicidal Thoughts and Actions
To try to prevent suicidal thoughts and actions in your child, pay close attention to changes in her or his moods or actions, especially if the changes occur suddenly. Other important people in your child's life can help by paying attention as well (e.g., your child, brothers and sisters, teachers, and other important people). The changes to look out for are listed in Section 3, on what to watch for.
Whenever an antidepressant is started or its dose is changed, pay close attention to your child.
After starting an antidepressant, your child should generally see his or her health care provider
- Once a week for the first 4 weeks
- Every 2 weeks for the next 4 weeks
- After taking the antidepressant for 12 weeks
- After 12 weeks, follow your health care provider's advice about how often to come back
- More often if problems or questions arise
You should call your child's health care provider between visits if needed.
3. You Should Watch for Certain Signs If Your Child is Taking an Antidepressant
Contact your child's health care provider right away if your child exhibits any of the following signs for the first time, or if they seem worse, or worry you, your child, or your child's teacher:
- Thoughts about suicide or dying
- Attempts to commit suicide
- New or worse depression
- New or worse anxiety
- Feeling very agitated or restless
- Panic attacks
- Difficulty sleeping (insomnia)
- New or worse irritability
- Acting aggressive, being angry, or violent
- Acting on dangerous impulses
- An extreme increase in activity and talking
- Other unusual changes in behavior or mood
Never let your child stop taking an antidepressant without first talking to his or her health care provider. Stopping an antidepressant suddenly can cause other symptoms.
Prozac™ is a registered trademark of Eli Lilly and Company.
Zoloft™ is a registered trademark of Pfizer Pharmaceuticals.
Anafranil™ is a registered trademark of Mallinckrodt Inc.
This Medication Guide has been approved by the US Food and Drug Administration for all antidepressants.
Phenalzine Interactions
In patients receiving nonselective monoamine oxidase (MOA) inhibitors in combination with serotoninergic agents (e.g., dexfenfluramine, fluoxetine, fluvoxamine, paroxetine, sertraline, venlafexine) there have been reports of serious, sometimes fatal, reactions. Because Nardil is a monoamine oxidase (MAO) inhibitor, Nardil should not be used concomitantly with a serotoninergic agent.
Phenalzine Contraindications
Nardil should not be used in patients who are hypersensitive to the drug or its ingredients, with pheochromocytoma, congestive heart failure, a history of liver disease, or abnormal liver function tests.
The potentiation of sympathomimetic substances and related compounds by MAO inhibitors may result in hypertensive crises or related compounds (including methyldopa, L-dopa, L-tryptophan, L-tyrosine, and phenylalanine). Hypertensive crises during Nardil therapy may also be caused by the ingestion of foods with a high concentration of tyramine or dopamine. Therefore, patients being treated with Nardil should avoid high protein food that has undergone protein breakdown by aging, fermentation, pickling, smoking, or bacterial contamination. Patients should also avoid cheeses (especially aged varieties), pickled herring, beer, wine, liver, yeast extract (including brewer's yeast in large quantities), dry sausage (including Genoa salami, hard salami, pepperoni, and Lebanon bologna), pods of broad beans (fava beans), and yogurt. Excessive amounts of caffeine and chocolate may also cause hypertensive reactions.
Nardil should not be used in combination with dextromethorphan or with CNS depressants such as alcohol and certain narcotics. Excitation, seizures, delirium, hyperpyrexia, circulatory collapse, coma, and death have been reported in patients receiving MAOI therapy who have been given a single dose of meperidine. Nardil should not be administered together with or in rapid succession to other MAO inhibitors because HYPERTENSIVE CRISES and convulsive seizures, fever, marked sweating, excitation, delirium, tremor, coma, and circulatory collapse may occur.
A List of MAO Inhibitors by generic name follows:
pargyline hydrochloride
pargyline hydrochloride
and methylclothiazide
furazolidone
isocarboxazid
procarbazine
tranylcypromine
Nardil should also not be used in combination with buspirone HCl, since several cases of elevated blood pressure have been reported in patients taking MAO inhibitors who were then given buspirone HCl. At least 10 days should elapse between the discontinuation of Nardil and the institution of another antidepressant or buspirone HCl, or the discontinuation of another MAO inhibitor and the institution of Nardil.
There have been reports of serious reactions (including hyperthermia, rigidity, myoclonic movements and death) when serotoninergic drugs (e.g., dexfenfluramine, fluoxetine, fluvoxamine, paroxetine, sertraline, venlafaxine) have been combined with an MAO inhibitor. Therefore the concomitant use of Nardil with serotoninergic agents is contraindicated. Allow at least five weeks between discontinuation of fluoxetine and initiation of Nardil and at least 10 days between discontinuation of Nardil and initiation of fluoxetine, or other serotoninergic agents. Before initiating Nardil after using other serotoninergic agents, a sufficient amount of time must be allowed for clearance of the serotoninergic agent and its active metabolites.
The combination of MAO inhibitors and tryptophan has been reported to cause behavioral and neurologic syndromes including disorientation, confusion, amnesia, delirium, agitation, hypomanic signs, ataxia, myoclonus, hyperreflexia, shivering, ocular oscillations, and Babinski signs.
The concurrent administration of an MAO inhibitor and bupropion hydrochloride (Wellbutrin®) is contraindicated. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of treatment with bupropion hydrochloride.
Patients taking Nardil should not undergo elective surgery requiring general anesthesia. Also, they should not be given cocaine or local anesthesia containing sympathomimetic vasoconstrictors. The possible combined hypotensive effects of Nardil and spinal anesthesia should be kept in mind. Nardil should be discontinued at least 10 days prior to elective surgery.
MAO inhibitors, including Nardil, are contraindicated in patients receiving guanethidine.
Additional information about Phenalzine
Phenalzine Indication: For the treatment of depression.
Mechanism Of Action: The irreversible inhibition of MAO by phenelzine causes an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron, relieving depressive symptoms.
Drug Interactions: Not Available
Food Interactions: Avoid alcohol.
Avoid aged foods (cheese, red wine), pickled foods, cured foods (bacon/ham), chocolate, fava beans, beer, unless approved by your physician.
Avoid excessive quantities of coffee or tea (Caffeine).
Avoid St.John's Wort.
Generic Name: Phenelzine
Synonyms: Not Available
Drug Category: Antidepressants
Drug Type: Small Molecule; Approved
Other Brand Names containing Phenelzine: Beta-phenylethylhydrazine; Fenelzina [Inn-Spanish]; Fenelzyna; Fenelzyne; Nardil; Phenalzine; Phenelezine; Phenelzinum [Inn-Latin]; Phenethylhydrazine; Phenylethyl hydrazine-HCl; Phenylethylhydrazine; Stinerval;
Absorption: Readily absorbed after oral administration.
Toxicity (Overdose): Symptoms of overdose include drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions and coma, rapid and irregular pulse, hypertension, hypotension and vascular collapse, precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.
Protein Binding: Not Available
Biotransformation: Hepatic. Acetylation of phenelzine appears to be a minor metabolic pathway. Beta-phenylethylamine is a metabolite of phenelzine, and there is indirect evidence that phenelzine may also be ring-hydroxylated and N-methylated.
Half Life: Not Available
Dosage Forms of Phenalzine: Tablet Oral
Chemical IUPAC Name: 2-phenylethylhydrazine
Chemical Formula: C8H12N2
Phenelzine on Wikipedia: https://en.wikipedia.org/wiki/Phenelzine
Organisms Affected: Humans and other mammals