Drug information of Pimozide

Mechanism of effect

The ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be primarily a function of its dopaminergic blocking activity. Pimozide binds and inhibits the dopamine D2 receptor in the CNS.

Pharmacodynamic

Pimozide is an orally active antipsychotic drug product which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system.
However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide's therapeutic and untoward effects.
In addition, pimozide , in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized. Pimozide also has less potential for inducing sedation and hypotension as it has more specific dopamine receptor blocking activity than other neuroleptic agents (and is therefore a suitable alternative to haloperidol).

Pharmacokinetics

Absorption : Greater than 50% absorption after oral administration.
Serum peak appears : 6-8 hours post ingestion.
Half life : 29 ± 10 hours (single-dose study of healthy volunteers).

Dosage

Usual Adult Dose for Tourette's Syndrome
Initial dose: 1 to 2 mg orally per day in divided doses
Maintenance dose: Typically less than 0.2 mg/kg or 10 mg/day, whichever is less
Maximum dose: 10 mg/day
Usual Pediatric Dose for Tourette's Syndrome
12 years and older:
-Initial dose: 0.05 mg/kg orally at bedtime
-Maximum dose: 0.2 mg/kg, not to exceed 10 mg/day
Renal Dose Adjustments
Use with caution.
Liver Dose Adjustments
Use with caution.

Drug contraindications

breast cancer

Side effects

Headache , dry mouth , constipation , Blurred vision , vertigo , asthenia , fever , extrapyramidal effects , difficulty urinating , tiredness , Restlessness

Interactions

Amitriptyline , Acetylcholine , Amphotericin B , Amiodarone , Epirubicin , Erythromycin , Ofloxacin , Paroxetine , Quetiapine , Clarithromycin , Chloramphenicol , Chlorpromazine , Clozapine , Clomipramine , Solifenacin , Furosemide , Granisetron , Metoclopramide , Hydrochlorothiazide , Venlafaxine , Voriconazole , Ciprofloxacin , Cinacalcet , Cyclosporine , Fluvoxamine , Fluoxetine , Fluconazole , Diltiazem , Zafirlukast , Zonisamide , Cimetidine , Celexib , Sotalol , Daunorubicin , Danazol , Desipramine , Duloxetine , Doxepin , Doxorubicin , Tetrabenazine , Triptorelin , Trimipramine , Topiramate , Gemifloxacin , Terbinafine , Citalopram , Fluphenazine , Methyl phenidate , Ketoconazole , Bicalutamide , fentanyl , Ranolazine , Darunavir , potassium citrate , Methazolamide , Sodium Oxybate , Toremifene , Mirabegron , Tapentadol , safinamide , methylene blue , Histrelin , teriflunomide , codeine , iohexol (Omnipaque) , Nefazodone , ISOPROTERENOL , ritonavir , saquinavir , nelfinavir , Zileuton , Amprenavir , Mifepristone , Dolasetron , Palonosetron , vandetanib , Telithromycin , Droperidol , Quinine , sparfloxacin , Indinavir , Procainamide , Mefloquine , Indapamide , Dofetilide , Inotuzumab‎ , Goserelin , Promazine , Torsemide , brigatinib , Vasopressin , Chlorthalidone , Arsenic trioxide , Tipranavir , Telaprevir , lumacaftor and Ivacaftor , Panitumumab , Halofantrine , Grepafloxacin , Darifenacin , Mibefradil , cobicistat , Delavirdine , Oxiconazole , Terfenadine , Asenapine , Alfuzosin , Amisulpride , Paliperidone , Bendroflumethiazide , Acetaminophen and benzhydrocodone , Perflutren , Pimavanserin , lenvatinib , Crizotinib , Pitolisant , Entrectinib , edetate disodium , Lopinavir and Ritonavir , Oxymorphone , Dacomitinib , Troleandomycin , gilteritinib , Glycerol Phenylbutyrate , glycopyrrolate topical , Gadofosveset , glasdegib , Nitrendipine , Eliglustat , Roxithromycin , Naltrexone and Bupropion , Bepridil , bedaquiline , Dasatinib , Gemtuzumab , Cannabidiol , rolapitant , voxelotor , cyclopenthiazide , Venetoclax , Sodium Stibogluconate , tucatinib , Ombitasvir, Paritaprevir, and Ritonavir

Alerts

Do not take this drug more often or increase the dose. Your symptoms will not improve any faster, and the risk for heart rhythm problems will be increased. Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of this medication in your bloodstream.
Do not stop taking this medication without consulting your doctor. Your condition may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.

Points of recommendation

Take this medication by mouth with or without food, usually once a day at bedtime or as directed by your doctor. Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Pregnancy level

C

Related drugs

Haloperidol , Lumefantrine / artemether , Propiomazine , Molindone