Methoprazine 5mg

First Generation (Typical) Antipsychotic; Antimanic; Nonopioid Analgesic

CSA NA – Not FDA Approved – REMS (N) – Cannot Ship

Methotrimeprazine/Levomepromazine, Methoprazine antagonizes the D1 and D2 dopamine receptors.  It also binds alpha1– /alpha2-adrenergic, 5-HT1 /5-HT2 serotonin, and M1/M2 muscarinic receptors.

Methotrimeprazine/Levomepromazine, Methoprazine is not FDA approved and has no official indication in the US.  In Canada and other countries, it is indicated on and off-label for conditions such anxiety, insomnia, nausea/vomiting, pain, and various other psychiatric disorders (schizophrenia/psychosis/manic episodes).                                                       

Before starting Methotrimeprazine/Levomepromazine, Methoprazine make sure your physician is aware of any allergies or medications you currently take, if you have liver disease, if you have myasthenia gravis, prostatic hypertrophy, respiratory disease, Parkinson disease, a seizure disorder, cardiovascular disease, dementia, hypothyroidism, or are pregnant or breastfeeding.

Mild symptoms generally start at around 6-25mg divided in up to three times daily, then titrated up as needed.  Severe symptoms such as with severe schizophrenia may require 100-200mg/day divided into three daily dosages and can be titrated up to over 1000mg daily as needed in rare cases.  If high dosages are required at initiation of therapy the patient should remain in bed for a few days while the body adjusts to the medication

How to Take Methotrimeprazine/Levomepromazine, Methoprazine: Follow instructions provided by physician/pharmacy label, take consistently at same times each day unless otherwise directed, store at room temperature

You Need to Avoid: Operating heavy machinery or driving at least until you know how the medication affects you.  Do not stop this medication suddenly, make sure your physician is aware and can create a tapering schedule so you can come off slowly and prevent any withdrawal symptoms.   This medication has many drug interactions so ask your pharmacist before starting any over the counter medications or supplements.

This medication has an extensive list of side effects with unknown frequencies, some of which are assumed based on known information from other agents in the same pharmacologic class.  It does have risk of serious adverse reactions as it affects so many neurotransmitters such as neuroleptic malignant syndrome, akathisia, tardive dyskinesia, etc.  It also can cause QT prolongation which can result in severe cardiac arrythmia, especially if mixed with other QT prolonging agents. It is important to note that most side effects are dosage dependent and this medication does have an exceptionally large dosage range.  Please refer to an official monograph for this information.  

1. What can I do if this medication sedates me too much?
   It is a common side effect but in most cases the tablet can be split for smaller dosages to alleviate fatigue.  Discuss with your pharmacist or physician a plan to manage this or potential alternative medications.
2. This medication has a lot of scary side effects, is it safe?
   All medications have side effects however this medication works on a lot of different neurotransmitter receptors in the brain which can lead to a variety of intentional and unintentional effects.  These are mostly dosage dependant and in lower doses the risk is minimal.  In all cases regular lab work will allow your physician to see if your blood sugar, cholesterol etc. start to move in the wrong direction so action can be taken before they become a problem.  
3. What are extra-pyramidal reactions?
   Blocking dopamine in the extra-pyramidal system in the central nervous system that regulates posture and skeletal muscle tone may cause a variety of movement disorders.  This can include dystonic reactions (muscular spasms, usually repetitive), akathisia (motor restlessness/uneasiness), pseudoparkinsonism (drug induced Parkinsonism – tremor, rigidity, bradykinesia, etc.), tardive dyskinesia (involuntary complex muscle movements in lower face and extremities).  These side effects are generally dose dependant and generally occur with long term use of medications that block dopamine.  If any of these effects may be occurring, speak to your physician as soon as possible to discuss your options.  
4. Why would my doctor give me an antipsychotic?
   Does this mean I am psychotic? This medication can be used for many conditions outside of its original classification.  It commonly is also used for nonpsychotic mood disorders, but this class of medication was given its name back when we knew a lot less about their capabilities.   
5. What is Neuroleptic Malignant Syndrome?
   NMS is a rare but serious reaction from significant blockade of dopamine which can occur from antipsychotic medications or from being on high dosages of levodopa (dopamine analogue) and stopping suddenly.  Presents initially as muscle cramps, tremors, fever, unstable blood pressure, and sudden changes in mental status.  As it progresses over 8-40 hours it can lead to complications of rhabdomyolysis, hyperkalemia, kidney failure, or seizures.  Seek medical attention immediately if this reaction is suspected.