Prochlorperazine: medicine to help stop you feeling or being sick (nausea or vomiting).

1. About prochlorperazine

Prochlorperazine is an anti-sickness medicine. It can help stop you feeling or being sick (nausea or vomiting).

You can take prochlorperazine to treat:

• morning sickness
• feelings of dizziness (vertigo)
• travel sickness
• feelings of sickness due to migraines
• sickness caused by general anaesthetics after surgery, cancer treatment or taking other medicines
• problems with balance such as Ménière’s disease

Prochlorperazine may occasionally be used to treat some forms of anxiety.

It’s available as tablets and a liquid that you swallow. It can also be given as an injection, but this is usually done in hospital.

Prochlorperazine tablets and liquid are available on prescription. You can also buy tablets in a pharmacy without a prescription to treat nausea and vomiting, but only if you’ve been previously diagnosed with migraines.

2. Key facts

• Prochlorperazine starts to work in around 30 to 60 minutes.
• Common side effects include feeling sleepy and blurred vision.
• You can usually take prochlorperazine when you need it, up to 3 times a day.
• It’s best not to drink alcohol while taking prochlorperazine. It can increase the chance of side effects, such as feeling sleepy.

3. Who can and cannot take prochlorperazine

Prochlorperazine can be taken by most adults and children aged 1 year and over.

Prochlorperazine is not suitable for some people. Tell your doctor or pharmacist if you:

• have had an allergic reaction to prochlorperazine or any other medicines in the past
• have high blood pressure due to a tumour near the kidney (phaeochromocytoma)
• have glaucoma
• have a history of blood clots or may be at higher risk of developing a clot
• have Crohn’s disease, diverticulitis, hernia or colon cancer, or any other condition that can lead to a blockage in your bowel
• have liver problems
• have epilepsy or any condition that causes fits or seizures
• have high blood pressure or heart failure

4. How and when to take prochlorperazine

If you or your child have been prescribed prochlorperazine, follow your doctor’s instructions about how and when to take it.

Prochlorperazine tablets come as:

• standard tablets that you swallow whole with a drink of water
• tablets that dissolve between your upper lip and gum (buccal tablets)

Standard tablets and liquid can be taken with or without food.

Buccal tablets work best if they’re taken after meals. This gives them more time to dissolve.

Dosage

The dose varies depending on what you are taking prochlorperazine for, but it is usually taken 2 to 3 times a day.

The dose for children aged 1 to 17 years is based on their weight.

What if I forget to take it?

For travel sickness, take it as soon as you remember.

For anything else, skip the missed dose and take your next dose at the usual time.

Never take 2 doses at the same time.

What if I take too much?

Taking too much prochlorperazine can be dangerous.

Urgent advice: Contact 111 for advice now if:

• you take too much prochlorperazine

Go to 111.nhs.uk or call 111

If you need advice for a child under the age of 5 years, call 111.

If you need to go to A&E, do not drive yourself. Get someone else to drive you or call for an ambulance.

Take the prochlorperazine packet, or the leaflet inside it, plus any remaining medicine with you.

5. Side effects

Like all medicines, prochlorperazine can cause side effects, although not everyone gets them.

Common side effects

These common side effects happen in more than 1 in 100 people. They’re usually mild and go away by themselves.

Talk to your doctor or pharmacist if these side effects bother you or do not go away:

• feeling sleepy or drowsy
• blurred vision
• dry mouth
• headaches
• stuffy nose

Serious side effects

Serious side effects are rare and happen in less than 1 in 10,000 people.

Tell your doctor straight away if you get:

• muscle stiffness or shaking, or uncontrollable face or tongue movements
• a sudden high temperature or an infection
• sore breasts in both men and women
• yellowing skin or the whites of your eyes turn yellow – these can be signs of liver problems
• a fast or irregular heartbeat (your heart feels like it’s pounding)

Serious allergic reaction

In rare cases, it’s possible to have a serious allergic reaction (anaphylaxis) to prochlorperazine.

Immediate action required: Call 999 or go to A&E if:

• you get a skin rash that may include itchy, red, swollen, blistered or peeling skin
• you’re wheezing
• you get tightness in the chest or throat
• you have trouble breathing or talking
• your mouth, face, lips, tongue or throat start swelling

You could be having a serious allergic reaction and may need immediate treatment in hospital.

These are not all the side effects of prochlorperazine. For a full list, see the leaflet inside your medicine packet.

Information:

You can report any suspected side effect to the UK safety scheme.

6. How to cope with side effects of prochlorperazine

What to do about:

• feeling sleepy or drowsy – do not drive, cycle or use tools or machinery. It’s best not to drink alcohol, as it’ll make you feel more tired. This should wear off as your body gets used to the medicine. Talk to your doctor if it continues for longer than a week, they may be able to suggest a different medicine.
• blurred vision – do not drive, cycle or use tools or machinery. If it lasts for more than 2 days, speak to your doctor.
• dry mouth – try chewing sugar-free gum or sucking sugar-free sweets.
• headache – rest and drink plenty of fluids. You can take an everyday painkiller like paracetamol or ibuprofen. Talk to your doctor if the headaches last longer than a week or are severe.
• stuffy nose – try a menthol decongestant or talk to your pharmacist if this bothers you.

7. Pregnancy and breastfeeding

Prochlorperazine and pregnancy

Your doctor may prescribe prochlorperazine for morning sickness.

There’s no evidence that prochlorperazine will harm your baby, but for safety it’s best to take it for the shortest possible time.

Prochlorperazine and breastfeeding

Prochlorperazine passes into breast milk in small amounts. Talk to your doctor, as other medicines might be better while you’re breastfeeding.

If your baby was premature, had a low birthweight or is not feeding as usual, speak to your doctor before taking any anti-sickness medicine.

If you take prochlorperazine while breastfeeding and notice your baby is sleeping more than usual or is behaving differently, talk to your health visitor or doctor as soon as possible.

Non-urgent advice: Tell your doctor if you’re:

• trying to get pregnant
• pregnant
• breastfeeding

For more information about how prochlorperazine can affect you and your baby during pregnancy, read the leaflet about the best use of prochlorperazine in pregnancy (BUMPS).

8. Cautions with other medicines

Some medicines and prochlorperazine do not work well together. This can increase the chance of having side effects.

Tell your pharmacist or doctor if you’re taking any medicine that:

• makes you sleepy or drowsy
• gives you a dry mouth
• can affect your heart – taking prochlorperazine might make these side effects worse

Taking with other anti-sickness medicines

It’s usually best to only take one type of medicine for feeling or being sick.

If prochlorperazine does not work for you, speak to your doctor and they may suggest a different medicine for you.

Mixing prochlorperazine with herbal remedies or supplements

Some herbal remedies can make your side effects worse. Speak to your pharmacist before taking any herbal supplements.

Important

Tell your doctor or pharmacist if you’re taking any other medicines, including herbal remedies, vitamins or supplements.

9. Common questions

How does prochlorperazine work?

Prochlorperazine belongs to a group of medicines called phenothiazines.

Phenothiazines are thought to work by blocking the action of a chemical called dopamine in the brain. This stops nausea messages from being sent to a part of your brain called the “vomiting centre”.

The vomiting centre controls when you feel sick or vomit.

How long does it take to work?

Prochlorperazine starts to work in around 30 to 60 minutes.

If you’re taking it for Ménière’s disease, it will take a few days before it reaches its full effect.

How long will I take it for?

Prochlorperazine should be used for the shortest possible time and at the lowest dose that works for you.

If you take it for a long time and stop suddenly, it can cause withdrawal symptoms such as feeling or being sick and problems sleeping.

Talk to your doctor if you want to stop taking prochlorperazine. They will probably want to reduce your dose gradually to stop you having any of these withdrawal symptoms.

Can I take it for a long time?

Prochlorperazine can be taken long term if you need it, however, this should only be done if your doctor advises it.

Is prochlorperazine addictive?

Prochlorperazine is not usually addictive, however, if you stop taking it suddenly after taking it for a long time, it can cause withdrawal symptoms such as feeling or being sick and problems sleeping.

Talk to your doctor if you want to stop taking prochlorperazine after taking it for a long time. They will probably want to reduce your dose gradually to stop you having any of these withdrawal symptoms.

Are there other anti-sickness medicines?

Prochlorperazine belongs to a group of medicines known as anti-sickness (anti-emetic) medicines.

There’s not enough information available to say whether one is better than another for helping with sickness. You may need to try a few different medicines to find out what works best for you.

There are also other medicines that can help with different types of sickness, such as metoclopramide, ondansetron, domperidone and cyclizine.

Can I drink alcohol with it?

It is best not to drink alcohol when taking prochlorperazine.

Drinking alcohol can make side effects worse, such as feeling sleepy or an irregular heartbeat.

Are there foods and drinks to avoid?

Apart from avoiding alcohol, you can eat and drink normally while taking prochlorperazine.

It’s best to take buccal tablets after food so you do not accidentally swallow them before they dissolve.

Will it affect my contraception?

Prochlorperazine does not affect any type of contraception, including the combined pill and emergency contraception.

But if prochlorperazine is not working for you and you’re being sick, your contraceptive pills may not protect you from pregnancy.

Look at your pill packet to find out what to do.

Find out what to do if you’re on the pill and you’re sick.

Will it affect my fertility?

Prochlorperazine can increase levels of a hormone called prolactin. If levels of prolactin become high enough this can cause periods to stop in women and impotence in men.

However, this is not usually an issue while taking prochlorperazine for a short time to treat sickness.

If you have any concerns about this, speak to your doctor.

Can I drive or ride a bike?

Do not drive a car or ride a bike if prochlorperazine makes you sleepy, or if you have an irregular heartbeat caused by taking prochlorperazine.

This may be more likely when you first start taking prochlorperazine, but could happen at any time (for example, when starting another medicine).

It’s an offence to drive a car if your ability to drive safely is affected.

It’s your responsibility to decide if it’s safe to drive. If you’re in any doubt, do not drive.

GOV.UK has more information on the law on drugs and driving.

Talk to your doctor or pharmacist if you’re unsure whether it’s safe for you to drive while taking prochlorperazine.

Prochlorperazine – StatPearls – NCBI Bookshelf

Continuing Education Activity

Prochlorperazine is a first-generation antipsychotic. FDA indications include schizophrenia, schizoaffective, and other conditions presenting with symptoms of psychosis, as well as nausea and vomiting (post-chemotherapy, post-radiation therapy, pre- and post-operative setting, and other conditions). Non-FDA Indications include migraine headaches. This activity outlines the indications, mechanism of action, methods of administration, significant adverse effects, contraindications, monitoring, and toxicity of prochlorperazine, so providers can direct patient therapy in treating conditions for which it is indicated as part of the interprofessional team.

Objectives:

• Summarize the mechanism of action of prochlorperazine.

• Identify the indications for initiating therapy with prochlorperazine.

• Review the potential adverse event profile of prochlorperazine.

• Explain the importance of improving care coordination among the interprofessional team to enhance the delivery of care for patients who can benefit from therapy with prochlorperazine.

Access free multiple choice questions on this topic.

Indications

FDA Indications

• It is for schizophrenia, schizoaffective, and other conditions presenting with symptoms of psychosis. Prochlorperazine can be used to treat both acute psychotic episodes and chronic mental illnesses. As a first-generation antipsychotic, the drug is better at treating positive symptoms than negative ones, including delusions, hallucinations, agitation, and disorganized speech and behavior.[1]      

• To treat nausea and vomiting (Post-chemotherapy, post-radiation therapy, pre- and post-operative setting, and other conditions). One review concluded that prochlorperazine was equally as effective as metoclopramide, ondansetron, promethazine, and droperidol in the emergency department (ED). Side effects for all the medications studied were generally mild.[2]

Non-FDA Indications

Mechanism of Action

As a first-generation antipsychotic, prochlorperazine mainly blocks D2 dopamine receptors in the brain. It can also block histaminergic, cholinergic, and noradrenergic receptors.[1] One study found that prochlorperazine also inhibits the P2X7 receptor in human macrophages but not in mouse cells, preventing a calcium ion influx.[6] This mechanism was independent of dopamine antagonism.  

Administration

Prochlorperazine administration can be oral, parenteral, intramuscular, and rectal.[1] All four routes can be given to control nausea and vomiting. For nausea and vomiting pre- and post-surgery, the intramuscular and parenteral routes are both viable options. For psychiatric conditions, the administration can be via both intramuscular and oral routes. For headaches, parenteral is the route used.[2]

Adult dosing by condition and formulation is as follows:

Oral Formulation (5 or 10 mg tablets)

• For severe nausea and vomiting (including migraine-associated): 5 to 10 mg orally every 6 to 8 hours; max dose is 40 mg per day. (Note – migraine dosing is off-label.)

• Non-psychotic anxiety: 5 to 10 mg orally every 6 to 8 hours. Max dose is 20 mg daily for 12 weeks.

• Schizophrenia: 5 to 10 mg orally every 6 to 8 hours. The dose may be increased 5 to 10 mg every 2 or 3 days. Max dose 150 mg daily.

Injectable Formulation (5 mg/ml)

• Severe nausea and vomiting: 5 to 10 mg IM every 3 to 4 hours; max dose 40 mg daily.

• Migraine-associated nausea and vomiting (off label): 5 to 10 mg IM or IV once.

• Nausea/vomiting – postoperative prophylaxis: 5 to 10 mg IM or IV once. Give IM dose 1 to 2 hours and IV 15 to 30 minutes before induction.

• Schizophrenia: 5 to 10 mg IM daily every 6 to 8 hours. The dose may be increased 5 to 10 mg every 2 or 3 days. Max dose 150 mg daily.

Rectal (25 mg suppositories)

• Severe nausea and vomiting: 25 mg rectally every 12 hours.

• Migraine-associated nausea and vomiting (off label): 25 mg rectally every 12 hours as needed.

Clinicians should discontinue the drug if ANC < 1000, and consider discontinuing if the patient exhibits an unexplained drop in WBC count.

Adverse Effects

As a first-generation antipsychotic, prochlorperazine can cause a variety of adverse effects.[1] Significant extrapyramidal symptoms, including acute dystonia, tardive dyskinesia, Parkinsonism, akathisia, and neuroleptic malignant syndrome. Anticholinergic side effects include anorexia, blurred vision, constipation, dry mucosa, and urinary retention. Antihistaminic side effects (blockage of h2 receptor) include sedation. Prochlorperazine can also lower the seizure threshold. It can also lead to prolonged QTc interval and cause other cardiac conduction abnormalities. Antiadrenergic effects (blockage of the alpha1-adrenergic receptor) can lead to orthostatic hypotension. Due to dopamine blockade in the tuberoinfundibular tract, hyperprolactinemia, amenorrhea, breast enlargement, and sexual dysfunction may also occur. [1]

Leukopenia, agranulocytosis, cholestatic jaundice, and fatty liver are other possible but rare side effects. A rare but very severe condition that can result from any antipsychotic use is neuroleptic syndrome. Symptoms occur over 24 to 72 hours and present with elevated vitals, agitation, confusion, severe muscle rigidity, increased white blood cell count, increased creatinine phosphokinase concentrations, abnormal liver function tests, myoglobinuria, and acute renal failure.[1]

Prochlorperazine may also exert negative effects on melanocytes. In one in-vitro study, the presence of the drug correlated with decreased cell viability as well as reduced melanin content and tyrosinase activity.[7]     

Prochlorperazine may have significant adverse effects on children. One study from 2009, examining treatment modalities for pediatric nausea and vomiting, noted that side effects of prochlorperazine are high in children; therefore, patients under two years of age should not use it, and patients over two years old should consider alternatives such as ondansetron (5-HT3 receptor antagonist). [8] A review/meta-analysis from 2016 examined 49 previous studies and recorded pediatric side effects from dopamine antagonist use. Sedation and extrapyramidal symptoms were the most common, whereas serious adverse effects such as seizure, tardive dyskinesia, neuroleptic malignant syndrome, and autonomic failure were rare.[9] Therefore, healthcare providers should exercise caution when prescribing prochlorperazine to children.

Contraindications

It is important to note that geriatric patients with dementia have a higher risk of death when treated with an antipsychotic, including prochlorperazine.

The following lists contraindications for prochlorperazine[1][8]

• History of allergy to prochlorperazine or the phenothiazine drug class

• Concomitant use of CNS depressants (opioids, benzodiazepines, and barbiturates) leading to sedation

• Concomitant use of anticholinergic medications (scopolamine, atropine, etc.)

• Pre-existing cardiac conduction abnormalities

• History of seizure/epilepsy (prochlorperazine lowers seizure threshold)

• Narrow-angle glaucoma

• Prostatic hypertrophy

• Past or current history of tardive dyskinesia

• Patients under two years of age

It is not a recommended agent for patients who are pregnant. Antipsychotics are generally not recommended in pregnant patients.[1] Also, there is a lack of evidence to suggest that prochlorperazine is clinically effective in treating nausea and vomiting during pregnancy, nor are the side effects completely understood.[10]     

Monitoring

For patients who take prochlorperazine on a short-term basis, there are no recommendations for monitoring. However, some monitoring parameters are recommended for patients with chronic mental illnesses who take the drug long-term.[11] Every physician visit should record the patient’s weight, height, and BMI. Patients who are overweight or have other diabetes mellitus risk factors should have fasting plasma glucose, or hemoglobin A1C measured four months after starting an antipsychotic and then annually. Lipid plasma concentrations are indicated once every two years and once every six months if LDL-C > 130 mg/dl.[11]     

The concentration of prochlorperazine in the blood is not typically measured. When performed in cases such as suspected overdose, high-performance liquid chromatography/tandem mass spectrometry may be performed. The limit for quantifying the metabolite in the plasma is estimated to be around 0.20 ng/ml.[12] Oral prochlorperazine has high first-pass metabolism and poor absorption, so the exact concentration present in the body can be variable.[13]

The cytochrome P450 system metabolizes oral prochlorperazine, so monitoring a patient’s full list of medications is essential.[14] If the patient takes medications that stimulate or inhibit cytochrome P450, the healthcare provider should consider adjusting the dose of prochlorperazine. One study examined the effects of three cytochrome P450 genotypes (CYP2C19, CYP2D6, and CYP3A5) and their effects on the concentrations of prochlorperazine and its metabolites; the authors found no significant differences amongst the three.[14]

Toxicity

There are varying treatments available for extrapyramidal symptoms. Parkinsonism is treatable with benztropine or amantadine. Benztropine or diphenhydramine can treat acute dystonia. Akathisia is treatable with beta-blockers, benztropine, or benzodiazepines. Tardive dyskinesia is treatable by switching to atypical antipsychotics such as clozapine. Tetrabenazine is another option. For neuroleptic malignant syndrome, the healthcare provider should immediately discontinue prochlorperazine and give dantrolene (0.8 to 2.5 mg/kg given four times per day; up to 10 mg/day may be provided).[1] Also, monitor white blood cell count and vitals, and cool and hydrate the patient as much as possible.

Enhancing Healthcare Team Outcomes

Prochlorperazine is a medication that can produce numerous side effects and drug-drug interactions. Therefore, close interprofessional coordination amongst clinicians (Mds, DOs, NPs, PAs), nurses, pharmacists, and other healthcare providers is necessary to monitor for signs and symptoms related to the above. Working together with team members and the patient is also essential to determine if prochlorperazine is the optimal therapeutic choice and increase medication adherence. As referenced above, prescribers should investigate cytochrome P450 enzyme status. Nurses can provide patient counsel on dosing, potential adverse events to watch for and answer patient questions. Pharmacists can perform medication reconciliation, paying particular attention to CYP450 inducers and inhibitors. This interprofessional team approach will drive better patient outcomes and preclude more serious adverse events. [Level 5]

Review Questions

• Access free multiple choice questions on this topic.

• Comment on this article.

References

1.

Chokhawala K, Stevens L. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Feb 26, 2023. Antipsychotic Medications. [PubMed: 30137788]

2.

Furyk JS, Meek RA, Egerton-Warburton D. Drugs for the treatment of nausea and vomiting in adults in the emergency department setting. Cochrane Database Syst Rev. 2015 Sep 28;2015(9):CD010106. [PMC free article: PMC6517141] [PubMed: 26411330]

3.

Orr SL, Friedman BW, Christie S, Minen MT, Bamford C, Kelley NE, Tepper D. Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies. Headache. 2016 Jun;56(6):911-40. [PubMed: 27300483]

4.

Bachur RG, Monuteaux MC, Neuman MI. A comparison of acute treatment regimens for migraine in the emergency department. Pediatrics. 2015 Feb;135(2):232-8. [PubMed: 25624377]

5.

Sheridan DC, Laurie A, Pacheco S, Fu R, Hansen ML, Ma OJ, Meckler GD. Relative Effectiveness of Dopamine Antagonists for Pediatric Migraine in the Emergency Department. Pediatr Emerg Care. 2018 Mar;34(3):165-168. [PubMed: 27176905]

6.

Hempel C, Nörenberg W, Sobottka H, Urban N, Nicke A, Fischer W, Schaefer M. The phenothiazine-class antipsychotic drugs prochlorperazine and trifluoperazine are potent allosteric modulators of the human P2X7 receptor. Neuropharmacology. 2013 Dec;75:365-79. [PubMed: 23954492]

7.

Otręba M, Beberok A, Wrześniok D, Buszman E. In vitro melanogenesis inhibition by fluphenazine and prochlorperazine in normal human melanocytes lightly pigmented. Daru. 2018 Sep;26(1):85-89. [PMC free article: PMC6154481] [PubMed: 30159761]

8.

Manteuffel J. Use of antiemetics in children with acute gastroenteritis: Are they safe and effective? J Emerg Trauma Shock. 2009 Jan;2(1):3-5. [PMC free article: PMC2700583] [PubMed: 19561947]

9.

Lau Moon Lin M, Robinson PD, Flank J, Sung L, Dupuis LL. The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis. Drug Saf. 2016 Jun;39(6):509-16. [PubMed: 26884326]

10.

Festin M. Nausea and vomiting in early pregnancy. BMJ Clin Evid. 2009 Jun 03;2009 [PMC free article: PMC2907767] [PubMed: 21726485]

11.

Marder SR, Essock SM, Miller AL, Buchanan RW, Casey DE, Davis JM, Kane JM, Lieberman JA, Schooler NR, Covell N, Stroup S, Weissman EM, Wirshing DA, Hall CS, Pogach L, Pi-Sunyer X, Bigger JT, Friedman A, Kleinberg D, Yevich SJ, Davis B, Shon S. Physical health monitoring of patients with schizophrenia. Am J Psychiatry. 2004 Aug;161(8):1334-49. [PubMed: 15285957]

12.

Yan M, Zhu YG, Li HD, Chen BM, Ma N, Lei YQ, Liu YP. Quantification of prochlorperazine maleate in human plasma by liquid chromatography-mass spectrometry: Application to a bioequivalence study. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Oct 01;877(27):3243-7. [PubMed: 19682959]

13.

Finn A, Collins J, Voyksner R, Lindley C. Bioavailability and metabolism of prochlorperazine administered via the buccal and oral delivery route. J Clin Pharmacol. 2005 Dec;45(12):1383-90. [PubMed: 16291713]

14.

Tashiro M, Naito T, Kagawa Y, Kawakami J. Influence of cytochrome P450 genotype on the plasma disposition of prochlorperazine metabolites and their relationships with clinical responses in cancer patients. Ann Clin Biochem. 2018 May;55(3):385-393. [PubMed: 28853295]

Disclosure: Lennox Din declares no relevant financial relationships with ineligible companies.

Disclosure: Charles Preuss declares no relevant financial relationships with ineligible companies.

Prochlorperazine – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English title

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Prochlorperazine

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• Application of the substance Prochlorperazine

• Contraindications

• Application restrictions

• Side effects of Prochlorperazine

• Interaction

• Dosage and administration

• Precautionary measures

Structural formula

Russian name

Prochlorperazine

English name

Prochlorperazine

Latin name

Prochlorperazini)

Chemical name

2-Chloro-10-[3-(4- methyl-1-piperazinyl)propyl]-10H-phenothiazine (and as maleate, dimethanesulfonate or 1,2-ethanedisulfonate)

Gross formula

C ₂₀ H ₂₄ ClN ₃ S

Pharmacological group of the substance Prochlorperazine

Antiemetics

Antipsychotics

Nosological classification

ICD-10 code list

• F20 Schizophrenia

• F28 Other nonorganic psychotic disorders

• R11 Nausea and vomiting

CAS code

58-38-8

Pharmacological action

Pharmacological action –

antipsychotic , antiemetic .

Characterization

Piperazine derivative of phenothiazine. White with a slightly yellowish tint or light cream crystalline powder. Practically insoluble in water, very slightly soluble in alcohol. Reddens in the world.

Pharmacology

Reduces psychotic symptoms (delusions, hallucinations), has an activating (stimulating, energizing) effect. Sedative effect is moderate. It has a strong antiemetic effect. Causes severe extrapyramidal disorders. Anticholinergic effects and hypotensive effect are mild.

Application of the substance Prochlorperazine

Schizophrenia, involutional psychosis (with a predominance of lethargy, apathy, asthenic phenomena, substuporous and stuporous states in the clinical picture), nausea and vomiting.

Contraindications

Hypersensitivity, severe CNS depression or coma, severe cardiovascular disease, progressive systemic diseases of the brain and spinal cord, acute period of traumatic brain injury, impaired hematopoiesis, liver failure, pregnancy, breast-feeding, childhood.

Restrictions for use

Alcoholism (may increase CNS depression, hepatotoxic effect), breast cancer (due to the induction of prolactin secretion, progression of the disease and the development of resistance to treatment with endocrine and cytotoxic drugs are possible), angle-closure glaucoma, benign prostatic hyperplasia with clinical manifestations (the risk of urinary retention increases), acute infectious diseases, nephritis, myxedema, pheochromocytoma, peptic ulcer of the stomach and duodenum (in the acute phase), Parkinson’s disease (extrapyramidal effects increase), elderly and debilitated patients.

Side effects of the substance Prochlorperazine

From the nervous system and sensory organs: tardive dyskinesia, extrapyramidal disorders, drowsiness / insomnia, dizziness, increased fatigue, paradoxical reactions (hallucinations, psychomotor agitation).

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): thrombocytopenia, leukopenia, anemia, pancytopenia, eosinophilia.

From the digestive tract: dry mouth, anorexia or increased appetite, nausea, vomiting, cholestatic jaundice.

Allergic reactions: skin rash, urticaria, angioedema.

Other: amenorrhea, hyperprolactinemia, decreased libido, ejaculation disorder, dysmenorrhea, galactorrhea, gynecomastia, weight gain, false positive pregnancy tests.

Interactions

Incompatible with ethanol and drugs that depress the central nervous system.

Method of administration and doses

Orally (after meals), for psychosis initial daily dose – 12.5-25 mg with a gradual increase by 12.5-25 mg / day to a daily dose of 150-300 mg. The maximum daily dose is 400 mg. The duration of the course of treatment is 2-3 months, after which the dose is reduced to maintenance. For nausea and vomiting: 5-10 mg 3-4 times a day.

Precautions

Elderly patients are more likely to develop extrapyramidal disorders such as tardive dyskinesia and parkinsonism. Perhaps the development of irreversible dyskinesia. May mask vomiting associated with toxic overdose of other drugs and make it difficult to diagnose acute conditions.

Should not be used during work by drivers of vehicles and people whose profession is associated with increased concentration of attention.

Prochlorperazine Maleate – instructions for use, dosages, composition, analogs, side effects / Pillintrip

WARNINGS
may be confused with central nervous system features of an undiagnosed primary
The disease responsible for vomiting, for example. Reye’s syndrome or other encephalopathy.
The use of prochlorperazine and other potential hepatotoxins should be avoided.
in children and adolescents whose signs and symptoms suggest Reye’s syndrome.

Tardive dyskinesia : Tardive dyskinesia, a syndrome consisting of:
irreversible, involuntary, dyskinetic movements may develop in treated patients
with antipsychotics. Although the prevalence of the syndrome appears
be highest in the elderly, especially the elderly, it is impossible
rely on prevalence estimates to predict antipsychotic onset
drug treatment in which patients may develop the syndrome. Be antipsychotic
Drugs differ in their ability to cause tardive dyskinesia is unknown.

Both the risk of developing the syndrome and the likelihood that it will occur
irreversible increase with duration of treatment and total
the cumulative dose of antipsychotics administered to the patient is increased.
However, the syndrome can, although much less frequently, be relative.
short treatment time at low doses.

However, no treatment is known for established cases of tardiver dyskinesia
the syndrome may be partly or wholly related to antipsychotic treatment
withdrawn. However, antipsychotic drug treatment alone can suppress (or
partially suppress) the signs and symptoms of the syndrome and therefore may
mask the underlying disease process.

Effect, symptomatic suppression on a long-term course
The syndrome is unknown.

Given these considerations, antipsychotics must be prescribed in some way
this most likely minimizes the occurrence of tardiver dyskinesia, especially
in old age. Chronic antipsychotic treatment should usually be reserved
for patients suffering from a chronic disease known to be 1)
antipsychotics and 2) for which the alternative is equally effective but
Potentially less harmful treatments are not available or are not suitable. Patients
who needs chronic therapy, the smallest dose and the shortest duration
a treatment that produces a satisfactory clinical response should be sought.
The need for further treatment should be regularly reassessed.

If a patient on antipsychotics develops signs and symptoms of tardive dyskinesia, discontinuation of the drug should be considered. However, some patients may need treatment despite the presence of the syndrome.

More information about the description of tardive dyskinesia and your
clinical detection, please refer to sections PRECAUTIONS and .
REACTION.

neuroleptic malignant syndrome (NMS): potentially fatal complex syndrome
sometimes referred to as neuroleptic malignant syndrome (NMS)
associated with antipsychotic drugs. Clinical manifestations of NMS
hyperpyrexia, muscle stiffness, changes in psychological status, and signs of autonomists
Instability (irregular pulse or blood pressure, tachycardia, diaphoresis, etc.)
cardiac arrhythmias).

Diagnostic evaluation of patients with this syndrome is difficult. When diagnosing, it is important to identify cases in which the clinical picture includes both serious medical conditions (eg. pneumonia, systemic infection, etc.) and untreated or insufficiently treated extrapyramidal signs and symptoms (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug fever, and primary pathology of the central nervous system (CNS).

Management of NMS should include 1) immediate discontinuation of antipsychotics and other medications not necessary for concomitant therapy, 2) intensive symptomatic treatment and medical supervision, and 3) treatment of associated serious medical problems for which specific treatments are available. There is no general agreement on specific pharmacological treatment regimens for uncomplicated NMS.

If a patient requires antipsychotic drug treatment after recovery from NMS, re-introduction of drug therapy should be carefully considered. The patient should be carefully monitored as NMS reports 9 recurrences0049

Encephalopathic syndrome (characterized by weakness, lethargy, fever, tremor
and confusion, extrapyramidal symptoms, leukocytosis, elevated serum enzymes
BUN and FBS) occurred in some patients treated with the antipsychotic lithium plus.
In some cases, the syndrome was followed by irreversible brain damage. There
possible causal relationship between these events and concurrent control
lithium and antipsychotics should be patients receiving such combination therapy
carefully monitored for early signs of neurological toxicity and treatment
Discontinue immediately if such signs occur. This encephalopathic syndrome
be similar or the same as neuroleptic malignant syndrome (NMS).

Patients with bone marrow depression or who have previously had a hypersensitivity reaction (eg, blood dyscrasia, jaundice) with phenothiazine should not receive phenothiazine, including prochlorperazine, unless the clinician considers that the potential benefits of treatment outweigh the potential risks.

Prochlorperazine may affect mental and/or physical abilities, especially during the first days of therapy. Therefore, care must be taken when performing activities requiring vigilance (for example, operating vehicles or machines).

Phenothiazines may increase or prolong the effect of central nervous system depressants (eg alcohol, anesthetics, narcotics).

Use during pregnancy: Safety in using prochlorperazine during pregnancy
was not found. Therefore, prochlorperazine is not recommended for
Use in pregnant women, except for severe nausea and vomiting
so serious and persistent that, in the opinion of the doctor, the drug
intervention is necessary and the potential benefits outweigh the potential hazards.

Cases of prolonged jaundice, extrapyramidal signs have been reported
Hyperreflexia or hyporeflexia in newborns whose mothers received phenothiazines.

Nursing mothers: there are signs that phenothiazines are excreted from the body
in breast milk from nursing mothers. Caution to be taken with prochlorperazine
given to a nursing woman.

PRECAUTIONS

Antiemetic effects of prochlorperazine may affect signs and symptoms
overdose of other drugs and can diagnose and treat others
Diseases such as bowel obstruction, brain tumor, and Reye’s syndrome (see
WARNINGS ).

If prochlorperazine is used with anticancer chemotherapy drugs, vomiting may be covered by the antiemetic effect of prochlorperazine as a sign of toxicity of these agents.

Since hypotension may occur, large doses and parenteral administration should be used with caution in patients with a limited cardiovascular system. To minimize the occurrence of hypotension after injection, keep the patient lying there for at least half an hour and observe him. If hypotension occurs after parenteral or oral administration, place the patient with the legs up in the lower head position. If a vasoconstrictor is required, Levophed®* and Neo-Synephrin®** are suitable. Other pressures, including epinephrine, should not be used as they may cause a paradoxical further drop in blood pressure.

Aspiration from vomiting has occurred in some postoperative patients treated with prochlorperazine as an antiemetic. Although a causal relationship has not been established, this option should be considered during surgical follow-up.

Deep sleep, from which patients may be agitated, and coma have been reported, usually with overdose.

Antipsychotics increase prolactin levels; the increase remains during
chronic administration. Tissue culture experiments show that approx.
1/3 of human breast cancer depends on prolactin in vitro factor
potentially important when considering prescribing these drugs
patient with previously recognized breast cancer. Although disorders love
Amenorrhea, gynecomastia and impotence have been reported as galactorrhea
the clinical significance of elevated serum prolactin levels is not known
most patients. An increase in mammary neoplasms has been found in rodents
chronic administration of antipsychotics. Neither clinically nor epidemiologically
Research done so far has an association between chronic
The introduction of these drugs and oncogenesis of the mammary gland; available evidence
considered too limited at present to be convincing.

Chromosomal aberrations in spermatocytes and abnormal sperm detected
in rodents treated with certain antipsychotics.

As with all drugs that have an anticholinergic effect and cause/or mydriasis
prochlorperazine should be used with caution in patients with glaucoma.

Since phenothiazines may interfere with thermoregulatory mechanisms, use
with caution in people exposed to intense heat.

Phenothiazines may reduce the effect of oral anticoagulants. Phenothiazines can cause alpha-adrenergic blockade.

Thiazide diuretics may exacerbate orthostatic hypotension, which may occur with the use of phenothiazines.

The antihypertensive effects of guanethidine and related compounds may be counteracted if phenothiazines are used simultaneously.

Simultaneous administration of propranolol with phenothiazines results in an increase in plasma levels of both drugs.

Phenothiazines may lower seizure threshold; dose adjustment of anticonvulsants may be required. No potentiation of anticonvulsant effects. However, phenothiazines have been reported to interfere with the metabolism of Dilantin® *** and therefore the toxicity of Dilantin.

The presence of phenothiazines can lead to false positive phenylketonuria (PKU))
Test results.

Long-term therapy: Given the likelihood that some patients will be chronically exposed
for the development of antipsychotics, tardive dyskinesia is recommended for all patients
if chronic use is being considered, complete information should be provided where possible
about this risk. The decision to inform patients and/or their legal guardians should be
of course, take into account the clinical circumstances and competence
patient to understand the information provided.

To reduce the likelihood of side effects associated with a cumulative drug effect, patients with a history of long-term therapy with prochlorperazine and/or other antipsychotic drugs should be regularly evaluated to decide whether the maintenance dose can be reduced or therapy with the drug can be stopped.

Children with acute illness (e.g. chickenpox, CNS infections, measles
gastroenteritis) or dehydration appear to be much more susceptible to neuromuscular
Reactions, especially dystonia, as in adults. These patients have the drug
should only be used under strict supervision.

Medicines that lower the seizure threshold, including phenothiazine derivatives
should not be used with Amipaque® _§ As with other phenothiazines. therefore, prochlorperazine should be discontinued at least 48 hours in advance
Myelography should not be restarted for at least 24 hours after the procedure, and
also should not be used to control nausea and vomiting.
for myelography with amipacket or postreku.

Geriatric use: Clinical studies with prochlorperazine did not include
a sufficient number of subjects aged 65 years and over to determine whether the elderly are
Subjects react differently than younger subjects. Geriatric patients more
susceptible to the side effects of antipsychotics, including prochlorperazine.
These side effects include hypotension, anticholinergic effects (such as urinary tract
delay, constipation, and confusion) and neuromuscular reactions (such as
Parkinsonism and tardive dyskinesia) (see PRECAUTIONS and NEGATIVE
REACTIONS ), also post-market security experience points to this
the incidence of agranulocytosis may be higher in geriatric patients than in
young people who received prochlorperazine. Usually dose selection
for an elderly patient, care should be taken, usually starting from the bottom
dose range, which is the greater frequency of liver, kidney decline
or heart function and comorbidities or other drug therapy (i.