drugs

Metoclopramide: What is it? How does it work? Indications, Side Effects and Contraindications of I.Randi

Generality

Metoclopramide is an active ingredient with prokinetic and antiemetic activity .

Metoclopramide - Chemical Structure

Metoclopramide, to carry out the aforementioned activities, can be administered either orally (tablets, granules and effervescent tablets, syrup), or parenterally (solution for injection).

Some metoclopramide-based medicines are classified as over-the -counter (OTC) drugs, therefore, their free sale is allowed; others, on the other hand, need a repeatable medical prescription (RR) to be dispensed. Some of them, however, are classified as band A drugs, therefore, when possible, they can be dispensed to the National Health System.

The aforementioned difference in the classification and mode of dispensing of medicines depends above all on the dose of active principle contained in them and on the route of administration through which the drug must be taken.

Examples of Specialties Medicinal products containing Metoclopramide

  • Clopan®
  • Geffer® (in combination with dimethicone, potassium citrate, citric acid, tartaric acid, sodium bicarbonate)
  • Isaprandil®
  • Migpriv® (in association with D, L lysine acetylsalicylate)
  • Maalox Nausea®
  • Metoclopramide Accord®
  • Plasil®

Therapeutic indications

When is the use of Metoclopramide indicated?

Given its activities, the use of metoclopramide is indicated in cases where it is necessary to prevent and treat nausea and vomiting and in cases where it is necessary to exercise a prokinetic action.

Please note

The indications could vary slightly depending on the medicinal product used, the dose of active ingredient contained in it, the presence of other active ingredients in combination and depending on the route of administration used. In this article we will try to provide a general overview on the uses of metoclopramide; for more detailed information, however, it is advisable to consult your doctor or pharmacist and read the package leaflet of the medicine you are going to use.

However, by going into more detail, metoclopramide is indicated:

  • In the prevention and symptomatic treatment of nausea and / or vomiting;
  • In the treatment and prevention of nausea and vomiting associated with migraine.

Did you know that ...

Metoclopramide can also be used in combination with analgesic drugs used to combat migraine attacks.

  • In the prevention of nausea and vomiting that may occur after surgery;
  • For the prevention of nausea and vomiting caused by anticancer chemotherapy and / or radiotherapy.

Children and adolescents

Depending on the medicinal product used, metoclopramide can be used:

  • In children and adolescents aged 1 to 18 years, metoclopramide to prevent and treat nausea and vomiting is indicated only when other treatments are not effective or cannot be used.

or

  • To treat nausea in adolescents over 16 years old.

Did you know that ...

Metoclopramide is an active ingredient also used in the veterinary field, where it is used in medicines used in the symptomatic treatment of vomiting and reduced intestinal motility associated with various diseases (for example, gastritis, pyloric spasm, chronic nephritis, etc.) .

Warnings

Warnings and Precautions for the use of Metoclopramide

Before taking metoclopramide medicines, you must tell your doctor if:

  • You suffer from heart disease (such as, for example, bradycardia, long QT syndrome, etc.);
  • There are alterations in the levels of mineral salts in the blood;
  • You are suffering from liver and / or kidney disorders;
  • Drugs are being used that can act on the heartbeat and / or nervous system.

As a precautionary measure, before taking metoclopramide-based medicines, it is still advisable to inform your doctor or pharmacist of your health conditions and the possible presence of any type of disorder or illness.

However, during treatment with metoclopramide, the doctor may subject the patient to regular blood tests in order to promptly identify the possible onset of methaemoglobinaemia .

Furthermore, it is important to note that taking metoclopramide could increase blood prolactin levels.

Finally, remember that in the event of neurological symptoms such as involuntary muscle spasms (tardive dyskinesia), treatment with metoclopramide should be stopped immediately and the doctor should be contacted immediately .

Please note

Taking metoclopramide could cause side effects that could affect the ability to drive and / or use machinery, therefore, caution is advised and the aforementioned activities should be avoided if such effects should occur.

Interactions

Interactions between Metoclopramide and Other Drugs

Because of the drug interactions that could occur, before taking metoclopramide, you need to tell your doctor if you are taking other medicines, such as:

  • Levodopa and other drugs for the treatment of Parkinson's disease;
  • Morphine and its derivatives;
  • Sedative-hypnotic drugs;
  • Anticholinergic drugs;
  • Selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine and paroxetine (the concomitant intake of these drugs and metoclopramide increases the risk of the occurrence of serotonin syndrome);
  • Anxiolytic and antidepressant drugs;
  • Barbiturates;
  • Anti-H1 antihistamine drugs;
  • Adrenergic drugs (such as, for example, clonidine);
  • Neuroleptic drugs;
  • Immunosuppressive drugs such as cyclosporine;
  • Muscle relaxants such as mivacurium and succinylcholine;
  • Digoxin (a cardioactive glycoside);
  • Apomorphine (metoclopramide can reduce its effects);
  • Cisplatin (an anticancer medicine, the association between this active ingredient and metoclopramide could lead to an increase in renal toxicity);
  • Insulin (adjustments of the administered dose may be necessary).

In any case, before using any type of medicine based on metoclopramide, it is good to inform your doctor if you are taking - or have recently been taken - drugs or products of any kind, including non-prescription medicines ( SOP), other over-the-counter drugs (OTC), herbal and phytotherapeutic products and homeopathic products.

Metoclopramide and alcohol

During treatment with metoclopramide it is necessary to avoid alcohol consumption, as it increases the sedative effect of the active ingredient in question.

Side effects

Side Effects Caused by the Intake of Metoclopramide

Metoclopramide is able to cause different types of side effects, although not all patients manifest them or manifest them in equal measure. In fact, each individual responds differently to the administration of the active ingredient, manifesting undesirable effects that are different in type and / or intensity, or not at all.

Please note

The following are the main side effects that may occur during treatment with metoclopramide; however, these may vary depending on the dosage of active ingredient contained in the medicine to be used, the presence of any other active ingredients in combination and depending on the route of administration through which the drug should be taken. For more and more in-depth information on the subject, therefore, see the reading of the medicinal product to be used.

Blood disorders

Metoclopramide intake could cause methemoglobinemia - often related to NADH cytochrome-b5 reductase deficiency - and on hemoglobinemia.

Cardiac and vascular disorders

Treatment with metoclopramide may cause:

  • bradycardia;
  • Cardiac arrest;
  • Atrioventricular block;
  • QT interval extension;
  • Twist tip;
  • Hypertension or hypotension;
  • Syncope after parenteral administration.

Psychiatric disorders

With the administration of metoclopramide, hallucinations may occur, or depression, confusion or suicidal ideation may occur.

Nervous system disorders

Metoclopramide therapy may cause the appearance of:

  • Drowsiness;
  • Extrapyramidal disorders;
  • Dyskinesia, including tardive dyskinesia;
  • Dystonia;
  • Reduction of the level of consciousness;
  • Malignant neuroleptic syndrome.

Other side effects

Other side effects that could occur during treatment with metoclopramide consist of:

  • Allergic reactions, even serious, in sensitive individuals;
  • Diarrhea;
  • Asthenia;
  • hyperprolactinemia;
  • Amenorrhea;
  • Galactorrhea;
  • Gynecomastia.

Overdose

In case of overdose with metoclopramide, symptoms may occur, such as:

  • Drowsiness;
  • Extrapyramidal symptoms;
  • Decreased level of consciousness;
  • Confusion;
  • Hallucinations;
  • Cardiorespiratory arrest.

Treatment is symptomatic and supportive. Therefore, in the case of ingestion of excessively high doses of metoclopramide, it is necessary to go to the nearest emergency room, taking care to bring along the packaging of the medicine used.

Action mechanism

How does Metoclopramide work?

Metoclopramide carries out its activity by acting on different mechanisms of action. More in detail, metoclopramide exercises, both at central and peripheral level, an action:

  • Antagonist of dopamine D2 receptors present in the Chemoreceptor Trigger Zone (or CTZ). The CTZ detects the emetogenic substances present in the body and sends the information to the center of the vomit, modulating its activity.
  • Antagonist against serotonin 5-HT3 receptors.
  • Agonist against gastrointestinal type 5-HT4 receptors (mechanism mainly responsible for the prokinetic activity of metoclopramide).

Method of use and Posology

How to take Metoclopramide

Metoclopramide is available in pharmaceutical forms suitable for oral administration (granules and effervescent tablets, syrup, tablets), and for parenteral administration, intramuscularly or intravenously (solution for injection).

While formulations that can be taken orally can be used directly by patients at home (while still following the doctor's instructions), metoclopramide in solution for injection should be administered by a healthcare professional.

Regardless of the route of administration used, the single recommended dose of metoclopramide is 10 mg which can be repeated, at the doctor's discretion, up to 3 times a day.

The maximum recommended dose is 30 mg or 0.5 mg / kg body weight.

When it is possible to administer it in children and adolescents (see "Contraindications" chapter), the dose of metoclopramide usually used is 0.1-0.15 mg / kg of body weight, repeated up to three times a day.

The maximum dose in 24 hours is 0.5 mg / kg body weight.

However, it is important to point out that the exact dosage (dose, frequency of administration and duration of treatment) of metoclopramide must be established by the doctor on an individual basis for each patient.

Please note

  • In order to avoid the risk of overdose, the different doses of metoclopramide must be taken at intervals of at least 6 hours from each other.
  • In order to avoid the onset of neurological side effects (such as tardive dyskinesia), treatment with metoclopramide should have a short duration . Usually, a maximum of 5 days treatment is recommended.

For more information, it is a good idea to ask your doctor for advice and read the package insert for the medicine he prescribes.

Pregnancy and breastfeeding

Can Metoclopramide be taken during pregnancy and during breastfeeding?

The possibility of using metoclopramide during pregnancy depends on the type of medicine being considered. In fact, the use of some metoclopramide-based medicines is contraindicated during the whole gestation period; other medicines are contraindicated only during the first trimester of pregnancy; while others only in the last quarter of gestation. However, when permitted, medicines containing metoclopramide can only be used if absolutely necessary and under the strict control of the doctor.

Given this variability in the possibility of using different metoclopramide medicines during gestation, future mothers must necessarily contact their doctor before taking them.

As for breastfeeding, instead, since metoclopramide is excreted in breast milk, its use is always contraindicated in nursing mothers . If treatment with the active ingredient is absolutely necessary, it will therefore be necessary to stop breastfeeding.

Contraindications

When Metoclopramide Should Not Be Used

The use of metoclopramide is contraindicated in the following cases:

  • Known hypersensitivity to metoclopramide itself and / or to one or more of the excipients and any active ingredients present in the combination of the medicinal product to be used;
  • In the presence of bleeding, perforation and / or gastrointestinal blockage;
  • In patients with confirmed or suspected pheochromocytoma;
  • In epileptic patients;
  • In patients with Parkinson's disease;
  • In individuals who have suffered from tardive dyskinesia;
  • In patients suffering, or suffering from, methaemoglobinaemia or NADH cytochrome-b5 deficiency;
  • In patients with porphyria;
  • In patients suffering from glaucoma;
  • In patients taking levodopa (used to treat Parkinson's disease) or dopamine agonists;
  • In patients taking drugs to treat nervous system disorders;
  • During breastfeeding.

Furthermore, depending on the medicine used, the use of metoclopramide may be contraindicated in children under the age of 1 year, or in children and adolescents under the age of 16 years.

Similarly, again depending on the medicinal product used, the use of metoclopramide could be contraindicated during the entire pregnancy, during the first trimester, or only during the last trimester of gestation.

Please note

Also in this case, the contraindications could vary depending on the dosage of active ingredient contained in the medicinal product to be used, depending on the presence of other active ingredients in combination and depending on the route of administration through which the drug should be taken.

Therefore, for more in-depth information on contraindications, but also on indications, warnings and precautions, interactions, side effects, use during pregnancy and during the feeding of different metoclopramide-based medicines, the importance of consult your doctor and carefully read the package insert for the medicinal product to be used.