Prochlorperazine for Anxiety (An Update)
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Prochlorperazine is phenotiazine, a first generation antipsychotic drug.
This drug was first developed in 1950 and got approval by FDA in 1956.
This drug is used to treat short term psychotic disorders schizophrenia and generalized non-psychotic anxiety.
It cannot treat schizophrenia but can help in management if its symptoms.
This drug should not be the first choice to treat non-psychotic anxiety due to risk factors but it has been proven effective in treating anxiety.
This drug can also be used to treat vomiting and severe nausea.
Many of its antagonists are promoted but it is still widely used for anxiety and other psychotic disorders.
In this article we will discuss Prochlorperazine for Anxiety.
Prescription products:
This drug is prescribed in different forms with different potencies.
It can be taken orally; an oral tablet or capsule can either be 5 mg, 10 mg or 15 mg.
For rectal intake, the suppository’s potency ranges from 2.5 mg to 25 mg.
It can also be administered intramuscularly and intravenously.
For intramuscular or intravenous intake solution is of 5 mg/1mm potency.
The common brand name for this drug is compazine having two ingredients Prochlorperazine edisylate and Proclorperazine maleate.
Pharmacodynamics:
This drug works due to its anti-dopaminergic effects where it blocks D2 dopamine receptors in the brain and have an effect similar to anti-emetic which prevents delayed nausea and vomiting.
It also inhibits histaminergic , cholinergic and alpha-1 adrenergic receptors which results in muscle relaxation, sedation and hypotension.
These inhibitions of particular receptors also display anti-anxiety effect.
When a research compared Prochlorperazine with other phenotiazine derivatives, results indicated that Prochlorperazine is less likely to induce sedation in its consumer and is less likely to potentiate the effect of depressant or anesthesia on CNS.
It also has low propensity to induce hypotension.
Metabolism and absorption:
Prochlorperazine is metabolized in the liver that is known as hepatic metabolism.
Different chemical reactions such as oxidation, hydroxylation, demethylation and sulfoxide formation results in metabolism of this drug.
It may enter into enterohepatic metabolism.
Absorption of this drug in blood takes place through the gastrointestinal tract.
It occurs usually 30-40 minutes after oral administration and 10-20 minutes after intramuscular injection.
The total time period of action for this drug is 3 to 4 hours.
After ingestion plasma reaches the highest concentration of this drug in about 5 hours.
This drug stays in the body for 8 to 9 hours.
Uses of Prochlorperazine:
In adults, doctors usually prescribe Prochlorperazine for following purposes:
- It is prescribed to treat nausea, feeling of sickness or vomiting caused by any condition such as cancer treatment, migraine or these symptoms followed by surgery. However it has not been much effective in treating travelling sickness.
- To reduce the sensation of dizziness or spinning caused by Meniere’s disease or any other inner ear disease.
- To manage the long term symptoms of psychotic disorders such as schizophrenia
- For short term management of acute mania
- For short term treatment of severe anxiety disorder
Mechanism:
Main effects of this medicine are on Dopamine D2 receptors, Histamine H1 receptor, and Alpha-1 adrenergic and Alpha-2 adrenergic receptors.
Well defined course of action for this tablet has not been established completely but it is considered as an anti dopaminergic drug.
D2 dopaminergic receptors, which are somatodendritic autoreceptors, are blocked in the brain by this drug.
Thus this inhibits postsynaptic dopamine receptors in the meso-limbic part of the brain.
This inhibition results in increased dopamine turnover.
Nausea and Vomiting:
Vomiting results from a message from the vomiting center in the brain area.
This message results in feelings of discomfort as nausea and vomiting reflex.
Vomiting center of the brain is activated when it receives a message from the chemoreceptor trigger (CTZ) which in turn is activated when it receives a message from the gut.
Prochlorperazine blocks dopaminergic receptors in CTZ, thus blocking the message to the vomiting center which ultimately lessens the nausea and blocks vomiting reflex.
Anxiety:
Prochlorperazine is often called as tranquilizer or neuroleptic.
It has a calming and soothing effect on people suffering from anxiety or other psychological disorders as it tranquilizes them.
But in psychotic illness it is important to look for the main effect of the drug too in addition to its tranquilizing effect.
Increased dopamine in the brain is associated with increased anxiety.
As this drug works by inhibiting the dopamine receptors in the brain thus reducing the dopaminergic activity in the brain and also reducing the anxiety.
Dosage:
There are different methods to take this medicine.
The method and amount of medicine is prescribed by the doctor depending on the need and weight of the patient.
If a patient losses or gains weight during the treatment, the doctor will change the potency of medicine as per the need of the patient.
- It can be administered orally
- It can be administered intramuscularly. Patient is advised to lay down for at least 30 minutes after the injection as it might cause a little dizziness
- It can be taken in the form of buccal tablet, where a patient needs to put it between the upper and gums. It gets dissolved directly there into the bloodstream as there are plenty of blood vessels present in that area. It usually takes 2 hour to get completely dissolved. Patients are advised not to chew the medicine or eat anything during that time period.
- Rectal administration of this medicine is through suppository. It gets into the bloodstream faster than oral ingestion.
Anxiety:
Doctors usually ask patients to take Prochlorperazine on a daily basis until the symptoms of anxiety relieves.
2 tablets are prescribed on a daily basis usually.
Nausea and Vomiting:
For feelings of sickness or vomiting, doctors prescribe Prochlorperazine to be taken either on daily until it relieves the symptoms or at the specific time when symptoms appear.
If an individual misses a dose of Prochlorperazine, he can take it anytime if it is not near the time of second dose otherwise he can simply miss it.
It does not create much of a difference and patients can go with a normal course of medicine.
However, individuals should not stop taking medicine all of the sudden without informing the doctor as it can cause certain withdrawal symptoms.
Precautions:
Prochlorperazine is suitable for adults and children above 1 year.
Different age groups and different purposes require different potencies of medicine.
As only children above 12 years can take this drug for sickness associated with migraine.
It is prescribed for adults only for non-psychotic generalized anxiety.
Older aged people should be careful while taking this medicine.
It should not be administered on older adults for behavioral problems associated with dementia.
This drug can increase the risk of stroke in older adults.
It is also not recommended to individual’s suffering from adrenal tumor.
Patients should consult his doctor before having Prochlorperazine, if he has following conditions:
- A person is a smoker
- He has kidney or liver impairment
- He has risk factors for stroke such as hypertension, history of stroke or irregular heart beat.
- He has family history of deep vein thrombosis or pulmonary embolism
- He has a heart disease or a family history of heart disease.
- He has low level of required minerals for anxiety, such as potassium,
- He is malnourished or follow poor diet routine
- He is severely dehydrated due to other condition such as vomiting or diarrhoea
- He is diabetic
- He is suffering from hypothyroidism
- His prostate gland is enlarged
- He has history of seizure or suffers from epilepsy
- He suffers from Parkinson’s disease
- He is condition of myasthenia gravis, a condition in which muscle weakens
- He has eye condition, known as angle glaucoma
- He is allergic to phenothiazine
Pregnancy:
It is important to be cognizant of the effects of Prochlorperazine as doctors often prescribe the medicine to treat vomiting and nausea during pregnancy or to treat pregnant women with non-psychotic generalized anxiety symptoms.
In such situations often cost benefit analysis is done by a doctor and medicine is prescribed if the disease is more harmful for a baby than medicine itself.
It should be noted here that if Prochlorperazine is ingested during the third trimester, it might cause some withdrawal symptoms in the baby after birth.
Such babies might need more critical observation than others.
If a lady becomes pregnant during the course of medicine, she should not quit the medicine immediately rather consult her doctor for better suggestions.
Breastfeeding:
Prochlorperazine is often prescribed to breastfeeding mothers to treat anxiety and severe nausea.
It should be noted here that Prochlorperazine passes through breast milk to babies and has an effect on an infant such as drowsiness and poor feeding.
It is recommended that mothers who are taking this drug for a longer period of time should not breastfeed but again cost benefit analysis is done by a doctor.
Side-effect of Prochlorperazine:
As with other medicine this has certain side-effects along with its potential benefits.
Side-effects listed below are associated with the use of Prochlorperazine but it is not necessary that every individual taking this medicine might have these side-effects.
- Lowered blood pressure results in feelings of dizziness while getting up or walking usually when the patient takes medicine for the first time. It is recommended that he should lay down until symptoms pass.
- Stuffy nose
- Dry mouth
- Drowsiness. It is recommended that a person should not operate a machine or drive if he feels drowsy after taking medicine.
- Abnormal muscle movement such as shakiness, rigidity or twitching
- Anxiousness
- Restlessness or agitation
- It increases the skin sensitivity to UV lights. It is recommended that a person should take precaution according to his skin reaction in sunlight after taking this medicine.
- In elderly people, this medicine can interfere with normal temperature regulation of the body for example, it can cause heat stroke in very hot weather and can lead to hypothermia in very cold one. Patient is advised to have detailed consultation with his doctor.
- This can enhance the level of prolactin in blood. This can result in different symptoms such as breast enlargement, difficulty having an erection and production of milk.
It is recommended that a person should immediately concern doctor if he has following symptoms after consumption of Prochlorperazine:
- Sore throat, mouth sores or high temperature
- Yellowing of eyes and skin
- Irregular or increased heart rate
- Stiffening of muscle
- Falling level of consciousness
- Stabbing pain
- Unusual swelling or rash
Prochlorperazine has been proven in short term management of non-psychotic generalized anxiety as it reduces the activity of dopamine in the brain that is associated with increased anxiety.
Major precautionary measures should be taken while taking this medicine.
FAQs about Prochlorperazine for anxiety
Can Prochlorperazine be used for anxiety?
It can be used to treat non-psychotic generalized anxiety but professionals recommend that it should be used as first treatment for anxiety because of the risk factors associated with it.
How quickly does Prochlorperazine work?
If taken orally it usually takes 30-60 minutes for it to be fully functional.
If it is taken intramuscularly it can be effective in 10-20 minutes.
Is Prochlorperazine sedative?
Prochlorperazine causes mild sedation but tolerance is developed over the course of time.
References:
everydayhealth.com/drugs/prochlorperazine
netdoctor.co.uk/medicines/brain-nervous-system/a7566/stemetil-prochlorperazine/
nhs.uk/conditions/generalised-anxiety-disorder/treatment/
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