Mechanism of effect
The mechanism of action of the pitolisant is unclear, but it may be through its activity as an inverse antagonist / agonist at histamine-3 receptors.
Pharmacodynamic
The mechanism of action of the pitolisant is unclear, but it may be through its activity as an inverse antagonist / agonist at histamine-3 receptors.
Start the operation
In drug treatment, it may take up to 8 weeks for patients to reach a clinical response.
Time to reach the peak of the work:
3.5 hours (2 to 5 hours)
half life:
20 hours (7.5-24.2)
Pharmacokinetics
It is metabolized by CYP2D6 and to a lesser extent by CYP3A4 to inactive metabolites.
Dosage
The usual dose in adults for narcolepsy
Initial titration: 8.8 mg orally once daily for 1 week, then 17.8 mg orally once daily for 1 week, then may be increased to 36 mg orally once daily
Adjustable dose based on the patient's response and tolerance
Maintenance dose: 17.8 to 35.6 mg per day
Maximum dose: 35.6 mg per day
-Doses should be consumed throughout breakfast.
It may take up to 8 weeks to reach a clinical response.
Side effects
Anxiety , Headache , weight decrease , nausea , dry mouth , Seizures , Cough , fever , RhinorrheaMore common
- Headache
- nausea
- trouble sleeping
Less common
- Anxiety
- body aches or pain
- chills
- cough
- decreased appetite
- difficulty with breathing
- dry mouth
- ear congestion
- fever
- headache
- itching skin or rash
- loss of voice
- muscle or joint pain
- runny or stuffy nose
- seeing, hearing, or feeling things that are not there
- sneezing
- sore throat
- stomach pain or discomfort
- unusual tiredness or weakness
Incidence not known
- Changes in behavior
- discouragement
- feeling sad or empty
- irritability
- lack of appetite
- loss of interest or pleasure
- seizures
- thoughts of killing oneself
- trouble concentrating
- weight gain
Interactions
Doxepin , Medroxyprogesterone , Hydroxyzine , Chlorpheniramine , Paliperidone , Amiodarone , Bupropion , Papaverine , Paroxetine , Pimozide , Terbinafine , Amisulpride , Apalutamide , Cabozantinib , Dacomitinib , Bepridil , bedaquiline , Panobinostat , Ribociclib , Dofetilide , Anagrelide , Arsenic trioxide , Efavirenz , dronedarone , Ivabradine , Dolasetron , Droperidol , Chloroquine , sparfloxacin , Carbamazepine , Clozapine , Enzalutamide , escitalopram , Rifabutin , Rifapentine , Phenobarbital , Fingolimod , Methadone , Nilotinib , Haloperidol , Hydroxychloroquine , Disopyramide , Rifampin , Sotalol , Citalopram , Cinacalcet , Fluoxetine , Entrectinib , Naltrexone and Bupropion , Gemtuzumab , vemurafenibAlerts
Cardiovascular: QT interval may be longer. Do not use in patients with known QT prolongation or concomitant use with other known agents to prolong QT interval. The risk may be higher in patients with liver or kidney failure. Do not use in patients with a known history of cardiac arrhythmias or conditions that may increase the risk of torsades de pointes or sudden death (eg, symptomatic bradycardia, hypokalemia, hypomagnesemia, prolonged Congenital QT interval).
• Hepatic impairment: Use with caution in patients with hepatic impairment. Dose adjustment may be required. Use in cases of severe hepatic impairment (C-Child-Pugh class) is contraindicated.
Kidney defects: Use with caution in patients with renal impairment. Dose adjustment is required. Consumption is not recommended in patients with end-stage renal disease (EGFR <15 ml / min / 1.73 m2)
Points of recommendation
Store at a temperature of 20 to 25 degrees Celsius.
Liver and kidney monitoring should be performed at the beginning and during consumption.
Pitoliant may reduce the effects of hormonal contraceptives. Women of reproductive potential should be advised to use non-hormonal contraceptives during treatment and 21 days after the last dose of Pitoliant.
It is best to take this medicine for narcolepsy in the morning.
Fear of therapeutic effect may take up to 8 weeks
Pregnancy level
HAVE NOT BEEN ESTABLISHEDThere is insufficient data to inform a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes in humans; animal data has shown maternal and embryofetal toxicity in rats at doses 13 times the maximum recommended human dose (MRHD) and in rabbits at greater than 4 times MRHD when administered during organogenesis.
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