HALOPERIDOL (Haloperidolum; synonym: Aloperidin, Haldol, Haloridin, Halophen, Halopidol, Serenace; joint venture. B) — neuroleptic. 4 (Para-chlorophenyl)-1-[3 '-(couple-ftorbenzoil) - propyl] - piperidinol-4; With 21 H 23 ClFNO 2 :
Treats derivatives of phenyl propyl ketone. Drugs of this group have strong antipsychotic activity.
On pharmakol, to properties G. it is close to neuroleptics of a fenotiazinovy row — to aminazine (see), Triphtazinum (see), to an etaperazin (see), etc. G. has antipsychotic properties, exerts the calming impact on c. the N of page, strengthens effect of narcotic and analgesic substances; oppresses conditioned-reflex activity, reduces a physical activity at animals, causes a katalepsy (catalepsy). Unlike aminazine, G. significantly does not influence the arterial pressure and functions of the autonomic nervous system; surpasses aminazine in antiemetic action. The synchronizing influence on EEG is expressed at G. more weakly, than at neuroleptics of a fenotiazinovy row; at increase in a dose animals have a motive excitement which is followed by activation of EEG.
In the mechanism of action of G. plays an important role, apparently, its influence on exchange of dopamine in a brain therefore the speed of synthesis and disintegration of this monoamine increases and increases concentration of its metabolites — gomovanilinovy and dihydroxy-phenyl-acetic acids.
Use drug of hl. obr. in psychiatry at paranoid schizophrenia with dominance of the hallucinatory-dilision phenomena without the expressed systematization of nonsense, periodically proceeding schizophrenia, maniacal and various neurotic states, alcoholic, epileptiform and oligofrenichesky psychoses, and also in anesthesiology for a neyroleptanalgeziya in combination with Promedolum or fentanyl. Positive takes are received at G.'s treatment slow schizophrenia. At catatonic and gebefrenny schizophrenia, and also at paranoiac symptomatology of G. it is ineffective. Along with antipsychotic effect of G. at prolonged use can eliminate nonsense, hallucinations, mental avtomatizm. Unlike the aminazine and levomepromazinum causing drowsiness and psychoaffective indifference in patients, G. has even a nek-swarm a promoting effect.
Drug is appointed inside, intramusculary and intravenously. For stopping of psychomotor excitement in the first days G. enter parenterally on 0,002 — 0,005 z (0,4 — 1 ml of 0,5% of solution) 2 — 3 times a day. On reaching steady sedation pass to administration of drug inside 0,005 — 0,01 g a day. The dose decline is made gradually. The patient with poorly expressed psychomotor excitement appoint 0,005 — 0,01 g a day in 3 — 5 receptions. The average therapeutic dose of G. in most cases makes 0,01 — 0,015 g a day, at slow schizophrenia — 0,02 — 0,04 g. The daily dose of G. at intake usually does not exceed 0,05 — 0,06 g. To children up to 5 years appoint 1/4, from 6 to 15 years — 0,5 doses of adults. Duration of treatment — depending on a form and the course of a disease, efficiency and portability of drug, on average 2 — 3 months. At a maintenance therapy of a dose of G. shall be minimum, but not allowing an exacerbation of a disease. At G.'s replacement with aminazine it is necessary to consider a ratio of their activity (0,001 g of G. correspond to 0,05 — 0,075 g of aminazine) and to make it gradually.
As an antiemetic of G. apply 0,002 g in a dose.
For a neyroleptanalgeziya enter 0,005 and G. and 0,01 — 0,02 g of Promedolum in 30 min. prior to operation (premedication) intramusculary, then 0,01 — 0,015 (at the rate of 0,2 mg on 1 kg of body weight) and 0,06 — 0,08 g of Promedolum (1 — 1,5 mg on 1 kg of body weight) intravenously. On this background carry out an anesthesia by nitrous oxide with oxygen, adding in case of need G. (0,0025 — 0,005 g) and Promedolum (0,01 — 0,02 g) intravenously. In total for operation it is spent 0,015 — 0,025 and a haloperidol and 0,1 — 0,12 g of Promedolum.
, As a rule, does not cause somatic frustration; skin manifestations are very rare, the photosensitization — sensitization by a sunlight is sometimes noted. Complications at G.'s use are characterized by hl. obr. neurologic frustration, among them most sushchestven the extrapyramidal syndrome of parkinsonichesky type with dominance of a muscular hypertension which is combined with an immovability (an akineto-hypertensive syndrome). Signs of vegetative disturbances — greasiness of skin, perspiration and the raised sialosis are sometimes noted. The phenomena of an akathisia (restlessness, internal concern), a tremor of extremities are frequent; oculogyric spasms, a lockjaw of chewing muscles, paroxysms of an open mouth with a pulling of language are sometimes noted. Crises of motor excitement are seldom observed; there can be phenomena of alarm and fear, sleeplessness.
The paroxysmal phenomena are stopped after intramuscular administration of aminazine (0,05 g) or caffeine, parkinsonichesky — by means of antiparkinsonichesky means (Cyclodolum, Tropacinum, Dinezinum, etc.).
It is contraindicated at organic diseases of c. N of page, hysteria; at cardiovascular diseases at a stage of a decompensation, disturbances of conductivity of a cardiac muscle and severe damage of kidneys it is necessary to appoint drug with care.
Forms of release: tablets on 0,0015 and 0,005 g, 0,2% solution in bottles on 10 ml for intake, 0,5% solution in ampoules on 1 ml. Make in the Hungarian People's Republic.
See also Neuroleptics .
Bibliography: Psychotropic drugs in medical practice, under the editorship of G. Ya. Av-rutsky, page 105, M., 1971; O'K e e f f e R., S h and of m a n D. P. a. Vogt M. Effect of drugs used in psychoses on cerebral dopamine metabolism, Brit. J. Pharmacol., y. 38, p. 287, 1970.
K. S. Rayevsky.