Haliparidol

Haloperidol is a typical butyrophenone type antipsychotic that exhibits high affinity dopamine D 2 receptor antagonism and slow receptor dissociation kinetics. [41] It has effects similar to the phenothiazines . [17] The drug binds preferentially to D 2 and α 1 receptors at low dose (ED 50 = and  mg/kg, respectively), and 5-HT 2 receptors at a higher dose (ED 50 =  mg/kg). Given that antagonism of D 2 receptors is more beneficial on the positive symptoms of schizophrenia and antagonism of 5-HT 2 receptors on the negative symptoms, this characteristic underlies haloperidol's greater effect on delusions, hallucinations and other manifestations of psychosis. [42] Haloperidol's negligible affinity for histamine H 1 receptors and muscarinic M 1 acetylcholine receptors yields an antipsychotic with a lower incidence of sedation, weight gain, and orthostatic hypotension though having higher rates of treatment emergent extrapyramidal symptoms .

Haloperidol may be used during pregnancy when treatment of acute psychosis or chronic psychotic illness is necessary. If needed to treat extrapyramidal side effects, biperiden can be added to the medication. Treatment with other butyrophenones is not an indication for termination of pregnancy. Detailed fetal ultrasonography may be offered, with special emphasis on the limbs, after maternal use of a butyrophenone in the first trimester. Regular psychiatric and obstetric care is recommended to diagnose in time a relapse or pregnancy complications (intrauterine growth retardaton, premature contractions). Observation of the neonate for adaptation problems for at least 2 days is recommended when butyrophenones have been used up to delivery. To prevent neonatal adaptation disorders dose reduction or even treatment interruption in the days immediately preceding delivery can be discussed with the patient if the clinical course allows. However, to prevent a relapse at this vulnerable stage, pre-pregnancy dosage should be started immediately after delivery.

That friend and fellow chemist Paul Janssen talked shop with - Arnold Beckett - supposedly provided key synthetic information received from Janssen to SmithKline & French, a competitor of Janssen Laboratories. This competitor seems to have tried whipping-up haloperidol-like molecules and going for a patent. A Johnson & Johnson subsidiary called NcNeil also joined the fray, attempting their own haloperidol patent run. The US Patent Office put a stop to NcNeil. Janssen sued SmithKline & French and won. Janssen got a US patent in 1969 and since then, haloperidol has been extensively used to manage a number of psychotic illnesses.

Haloperidol use may lead to the development of symptoms that resemble Parkinson's disease, but that are not caused by Parkinson's. These symptoms may include a taut or mask-like expression on the face, drooling, tremors, pill-rolling motions in the hands, cogwheel rigidity (abnormal rigidity in muscles, characterized by jerky movements when the muscle is passively stretched), and a shuffling gait. Taking the anti-Parkinson drugs benztropine mesylate or trihexyphenidyl hydrochloride along with haloperidol help to control these symptoms. Medication to control Parkinsonian-like symptoms may have to be continued after haloperidol is stopped. This is due to different rates of elimination of these drugs from the body.

The intravenous route is not FDA approved and is generally not recommended except when no other alternatives are available. Intravenous administration appears to be associated with a higher risk of QT prolongation and torsade de pointes (TdP) than other forms of administration. The manufacturer recommends ECG monitoring for QT prolongation and arrhythmias if IV administration is required. A dose in the range of 1 to 5 mg IV has been suggested, with the dose being repeated at 30 to 60 minute intervals, if needed. A maximum IV dose has not been established. The lowest effective dose should be used in conjunction with conversion to oral therapy as soon as possible.

Haliparidol

haliparidol

Haloperidol use may lead to the development of symptoms that resemble Parkinson's disease, but that are not caused by Parkinson's. These symptoms may include a taut or mask-like expression on the face, drooling, tremors, pill-rolling motions in the hands, cogwheel rigidity (abnormal rigidity in muscles, characterized by jerky movements when the muscle is passively stretched), and a shuffling gait. Taking the anti-Parkinson drugs benztropine mesylate or trihexyphenidyl hydrochloride along with haloperidol help to control these symptoms. Medication to control Parkinsonian-like symptoms may have to be continued after haloperidol is stopped. This is due to different rates of elimination of these drugs from the body.

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