drugs

Aripiprazole

Aripiprazole is an atypical antipsychotic drug. It is marketed by the pharmaceutical company Otsuka Pharmaceutical Europe under the name Abilify ®.

Indications

For what it uses

The use of aripiprazole is indicated for the treatment of:

  • Schizophrenia, in adults and adolescents over 15 years;
  • Moderate or severe manic episodes in adults and adolescents over 13 years with bipolar disorder.
    Aripiprazole - Chemical Structure

Warnings

Cases of suicidal thoughts and / or behavior have been reported during treatment with aripiprazole.

Patients most at risk for the development of these symptoms, therefore, must be kept under strict control.

Since aripiprazole can cause disorders in the cardiovascular system, caution should be used when administering the drug in patients suffering from cardiovascular diseases and in patients with a high risk of developing hypertension.

Since aripiprazole may induce venous thromboembolism, attention should be paid to the administration of the drug in affected patients - or those who have been affected - by coagulation disorders.

Aripiprazole in combination with other antipsychotics should be used with caution in patients who have suffered prolongation of the QT interval (the interval of time necessary for the ventricular myocardium to depolarize and repolarize).

Aripiprazole may cause tardive dyskinesia following long-term treatment, if this occurs, a reduction in the dose of medication administered or treatment interruption may be necessary.

Treatment with aripiprazole may cause neuroleptic malignant syndrome, in which case the drug should be stopped immediately.

As aripiprazole may induce seizures, caution should be used in the use of the drug in patients with a history of seizure disorders.

In elderly patients with dementia there may be a greater incidence of side effects, even with fatal outcomes.

Alcohol intake during treatment with aripiprazole should be avoided.

Aripiprazole therapy may affect the ability to drive and / or use machines.

Interactions

Aripiprazole may increase the activity of antihypertensive drugs.

Concomitant intake of aripiprazole and drugs capable of potentiating the serotonin signal increases the risk of occurrence of undesirable effects. Among these drugs, we recall:

  • Triptans, drugs used to treat migraine;
  • Tramadol and pethidine, opioid analgesics;
  • Tryptophan ;
  • SSRIs (selective serotonin reuptake inhibitors), such as - for example - paroxetine and fluoxetine ;
  • TCA (tricyclic antidepressants), such as - for example - clomipramine and amitriptyline ;
  • Venlafaxine, an antidepressant inhibitor of serotonin and noradrenaline reuptake;
  • Products based on St. John's wort (or St. John's wort), a plant with antidepressant properties.

The concomitant administration of aripiprazole and carbamazepine (a drug used for the treatment of epilepsy) may cause a decrease in the plasma concentration of aripiprazole.

Some cases of serotonin syndrome have been reported during concomitant administration of aripiprazole and SSRIs.

Side effects

Treatment with aripiprazole may induce side effects although not all patients experience them. The type of adverse effects and the intensity with which they occur depend on the sensitivity that each individual has towards the drug.

The following are the main side effects that may occur following treatment with aripiprazole.

Nervous system disorders

Aripiprazole therapy may cause:

  • Headache;
  • Fatigue;
  • Drowsiness;
  • Weakness;
  • Uncontrollable movements;
  • Difficulty sleeping;
  • Restlessness;
  • Feeling of anxiety;
  • agitation;
  • Nervousness;
  • Speech disorders;
  • Convulsions.

Psychiatric disorders

Treatment with aripiprazole may cause depression, alteration or increase in libido, excessive gambling, thoughts and / or suicide attempts and suicide.

Cardiovascular disorders

Aripiprazole therapy can cause sudden changes in blood pressure, hypertension, reduced consciousness, fainting, abnormal heart rhythm, heart attack, sudden and unexplained death. Furthermore, aripiprazole can promote thrombus formation and promote the onset of stroke or transient ischemic attack.

Hepatobiliary disorders

Treatment with aripiprazole can cause changes in liver function, inflammation of the liver, liver failure and jaundice.

Gastrointestinal disorders

Following treatment with aripiprazole, nausea, vomiting, diarrhea or constipation, pancreatitis, abdominal and stomach discomfort may occur.

Allergic reactions

Aripiprazole can trigger allergic reactions in sensitive individuals. The symptoms that can occur are swelling of the face, mouth, tongue and throat, itching and skin rash.

Diabetes

Aripiprazole therapy can cause an increase in the amount of sugar in the blood, can promote the onset of diabetes or worsen pre-existing diabetes, sometimes resulting in ketoacidosis and coma.

Renal disorders

Treatment with aripiprazole can cause incontinence and urination difficulties.

Skin and subcutaneous tissue disorders

Aripiprazole can cause skin rashes, photosensitivity reactions, unusual hair loss and increased sweating.

Serotonin syndrome

The concomitant administration of aripiprazole and selective serotonin reuptake inhibitors may trigger the serotonin syndrome.

This syndrome can also be defined as serotonin poisoning and is caused by excessive serotonin activity in the central nervous system. Intoxication can occur in live, moderate or severe form.

Some of the symptoms that can occur are euphoria, drowsiness, restlessness, feeling of drunkenness, headache, fever, increased sweating, muscle stiffness, myoclonia (short and involuntary contraction of a muscle or a group of muscles), rhabdomyolysis (rupture of skeletal muscle cells and subsequent release into the bloodstream of substances present in the musculature) and seizures. Some patients may even enter a state of shock, with body temperatures above 40 ° C.

Malignant Neuroleptic Syndrome

Neuroleptic malignant syndrome is a neurological disorder characterized by:

  • Temperature;
  • Dehydration;
  • Muscle stiffness;
  • akinesia;
  • Sweating;
  • Tachycardia;
  • Arrhythmia;
  • Changes in the state of consciousness that can progress to stupor and coma.

If such symptoms occur, treatment with aripiprazole should be stopped immediately and medical attention should be sought immediately.

Other side effects

Other side effects that may arise following treatment with aripiprazole are:

  • Temperature;
  • Increased salivation;
  • Blurred or double vision;
  • Alterations in the concentration of some blood cells;
  • Hyponatremia (low blood sodium levels);
  • Weight gain or loss;
  • Anorexia;
  • Muscle stiffness;
  • Muscle pains;
  • Accelerated breathing;
  • Accidental inhalation of food with the risk of developing pneumonia;
  • Difficulty swallowing;
  • Chest pain;
  • Edema;
  • Long and / or painful erection.

Overdose

If you suspect that you have overdosed, you should contact a doctor immediately or contact your nearest hospital.

Action mechanism

Aripiprazole exerts its antipsychotic action differently than other drugs. Indeed - while many other antipsychotics are dopamine and serotonin receptor antagonists - aripiprazole is a partial agonist of dopamine D2 (DA) receptors and serotonin (5-HT) 5-HT2A and 5-HT2C receptors.

Furthermore, the drug also has a moderate affinity for α 1 adrenergic receptors and for histamine H1 receptors.

Mode of Use - Posology

Aripiprazole is available for oral administration as tablets. The tablets should preferably be taken in the evening with the help of a glass of water. They can be taken either on a full stomach or on an empty stomach.

Aripiprazole is also available for intramuscular administration in a prolonged release pharmaceutical form.

The dose of aripiprazole must be established by the doctor on an individual basis. Below are the doses of drug normally used.

Oral administration

For adults, the recommended dose of aripiprazole is 15 mg a day. Your doctor may decide to prescribe a lower dose or increase the dose up to a maximum of 30 mg of medication per day.

In children and adolescents, the recommended dose of aripiprazole is 10 mg a day. Your doctor can decide whether to prescribe a lower dose or increase it up to a maximum of 30 mg a day.

Intramuscular administration

In this case, aripiprazole should not be used in children and adolescents under 18 years of age.

The drug appears as a powder that must be suspended in a special solvent - by the doctor or nurse - just before being given. The injection is made on the buttock or shoulder.

The dose of aripiprazole usually administered is 400 mg once a month. The interval between two doses must not be less than 26 days.

After the first injection, oral treatment is usually continued for 14 days. Subsequently, the drug is administered only intramuscularly.

Pregnancy and Lactation

The use of aripiprazole by pregnant women should only be done if the doctor considers it indispensable.

Infants whose mothers took the drug in the last trimester of pregnancy developed symptoms such as tremors, stiffness and / or muscle weakness, drowsiness, agitation, respiratory problems and feeding difficulties.

Breastfeeding is not recommended in mothers taking aripiprazole. In any case, it is necessary to discuss this with your doctor.

Contraindications

The use of aripiprazole is contraindicated in case of known hypersensitivity to the drug.