What is Olanzapine?
Olanzapine (Olanzapina) is a drug used for the treatment of schizophrenia and bipolar disorder. The product ingredients are: Olanzapine hydrochloride, Olanzapine pamoate, Olanzapine tartrate.
The brand names of olanzapine are: Zyprexa, Zyprexa Zydis, Zyprexa Intramuscular, Zyprexa Relprevv.
Mechanism of action of Olanzapine
Antipsychotic, antimaniac and mood stabilizer. Presents affinity for serotonin receptors, dopamine, cholinergic muscarinics, alpha-1-adrenergic and histamine.
Therapeutic Indications, Uses, Benefits and Dosage of Olanzapine
Adults
– Oral: schizophrenia and relapse prevention in bipolar disorder: initial, 10 mg/day; manic episode, initial, 15 mg/day in monotherapy or 10 mg/day in combination treatment.
Subsequent adjustment, 5-20 mg/day depending on clinical status.
Elderly, renal insufficiency and/or hepatic insufficiency: initial, 5 mg/day.
– Intramuscular injection: rapid control of agitation and altered behaviour in schizophrenia or manic episode, when oral treatment is not adequate.
Adults: initial: 5-7.5 or 10 mg, 5-10 mg may be administered 2 h later depending on clinical status; elderly: initial: 2.5-5 mg, may be repeated 2 h later depending on clinical status. Max. 3 inj./24 h, max. 20 mg/day. Max. 3 consecutive days. Renal insufficiency and/or hepatic insufficiency: initial, 5 mg/day. As soon as possible, start oral treatment.
Mode of administration of Olanzapine
Tablets: Administer with or without meals.
Oralispersible tablets: with or without food. Place in the mouth where it is quickly dispersed with saliva, so it is easily swallowed. Take immediately after opening the blister. It can also be dispersed, immediately before administration, in a glass of water or another suitable drink (orange or apple juice, milk, coffee).
Contraindications of Olanzapine
Hypersensitivity to olanzapine, narrow angle glaucoma.
Warnings and Precautions with Olanzapine
Children (no experience), elderly, dyslipemias (basal lipid control 12 weeks after starting treatment and every 5 years thereafter), prostatic hypertrophy or paralytic ileus and enf. related, history of convulsions, patients with ALT and/or elevated AST, signs and symptoms of hepatic dysfunction, with hepatotoxic medications or increase the QTc interval, prolonged congenital QT syndrome, CHF, cardiac hypertrophy, hypokalemia or hypomagnesemia, patients with low leukocyte and/or neutrophil counts, treatment with drugs that cause neutropenia, medullary depression, radiation therapy or chemotherapy, and patients with disorders associated with hypereosinophilia or myeloproliferative disease.
Increased risk of tardive dyskinesia in prolonged exposure, if present, reduce dose, or discontinue.
Caution is recommended when combined with other central-acting medications or alcohol.
Not recommended: for treatment of psychosis induced by dopaminergic agonists in Parkinson’s disease, psychosis and/or behavioural disorders associated with dementia (increased mortality and risk of stroke).
Risk of hyperglycemia and/or onset or exacerbation of diabetes occasionally associated with ketoacidosis or coma. Measure basal blood glucose after 12 weeks of starting treatment and annually thereafter. Control the weight of diabetic patients or patients at risk of diabetes, e.g. basal, at 4, 8 and 12 weeks after starting treatment and then quarterly.
Suspend if signs of MNS, hepatitis are observed. Risk of sudden cardiac death.
Do not administer intramuscular olanzapine to patients with AMI, unstable angina pectoris, severe hypotension and/or bradycardia, sick sinus syndrome or after heart surgery.
Concomitant use with parenteral (intramuscular) benzodiazepines is not recommended.
Monitor the onset of hypotension, bradyarrhythmia and/or hypoventilation in intramuscular treatment.
Not evaluated safety and efficacy of intramuscular olanzapine in ethyl poisoning, by drugs or drugs.
Liver failure
Consider a lower starting dose (5 mg). In moderate liver failure in controlled-release injection: 150 mg/4 week. (established an effective and well-tolerated posological regimen of oral olanzapine).
Kidney failure
Consider a lower starting dose (5 mg). In controlled-release injection 150 mg/4 week. (established an effective and well-tolerated posologic regimen of oral olanzapine).
Interactions with Olanzapine
- Reduced concentration of: tobacco, carbamazepine.
- Concentration increased by: fluvoxamine or other CYP1A2 inhibitor.
- Reduced oral bioavailability (50-60%) by: active carbon.
- Can antagonize the effects of direct and indirect dopamine agonists.
Pregnancy
Newborns exposed to antipsychotics during the 3rd trimester of pregnancy are at risk of extrapyramidal symptoms and/or withdrawal syndromes. Watch newborns.
Breastfeeding
In a study of healthy women, during lactation, olanzapine was excreted in breast milk. The mean exposure of the infant in the stationary state (mg/kg) was estimated at 1.8% of the maternal dose of olanzapine (mg/kg). Breastfeeding should be discouraged for mothers treated with olanzapine.
Effects on driving ability
Olanzapine acts on the central nervous system and can produce: drowsiness, dizziness, visual alterations and decreased ability to react.
These effects as well as the disease itself make it advisable to be cautious when driving vehicles or operating dangerous machinery, especially until each patient’s particular sensitivity to the medication has been established.
Adverse reactions and side effects of Olanzapine
Eosinophilia, leukopenia, neutropenia; increased weight and appetite; elevated glucose, triglycerides and cholesterol levels; glycosuria; drowsiness, dyskinesia, akathisia, parkinsonism; orthostatic hypotension.
Mild transient anticholinergic effects; asymptomatic and transient increases of ALT, AST; exanthema; arthralgia; asthenia, fatigue, edema, fever.
Increased alkaline phosphatase, elevated creatine phosphokinase levels, high gammaglutamyltransferase, elevated uric acid, increased plasma prolactin level.
DRESS (drug reaction with eosinophilia and systemic symptoms). Intramuscular: bradycardia with or without hypotension or syncope, tachycardia; hypotension; malaise instead of injection.
⭐⭐⭐⭐⭐ VIDEO OF OLANZAPINE/ZYPREXA (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: N7U69T4SZR
ChemIDplus
DrugPortal
NCI Thesaurus: C47639