Anti-psychotic activity

Some neuroleptic agents, like cycloindole (497), which has a modified tryptamine structure, and flucindole (498), a difluoro analog of cycloindole, have found use in therapy because of their anti-depressant and anti-psychotic activity (463,464) (Scheme 4.11). 3-Chlorocarbazole (385) (see Scheme 2.102), isolated from female bovine urine, has Diazepam-like activity (354). 

Exhibit 4 Selected Natural Products Investigated for Anti-Psychotic Activity... 

Some of these interactions may be potentially harmful (for example, the potentiation of opiates by MAO inhibitors) some interactions may help reduce the dose of, or frequency of dosing with, opiates so that there may be useful retardation of the development of tolerance and dependence. Other interactions may be less predictable but nevertheless important thus, both reserpine and chlorpromazine are neuroleptics and exert anti-psychotic activity in man, but whereas chlorpromazine may induce a useful potentiation of morphine analgesia in man (a property only partially explained on the basis of impaired hepatic... 

Chlorpromazine had been shown to produce a tranquil state in animals and since it had a similar effect in humans it became known as a major tranquiliser but the term is rarely used today. Sometimes the drugs used to treat schizophrenia are called anti-psychotics but more commonly neuroleptics. Leptic means to activate (take hold of) and in animals these compounds produce a state of maintained motor tone known as catalepsy. This is an extrapyramidal effect and in schizophrenics the neuroleptics can cause a number of extrapyramidal side-effects (EPSs) including Parkinsonism. The new term neuroleptic is unsatisfactory as a description of clinically useful drugs. It really describes a condition (catalepsy) seen in animals and is more indicative of a compound s ability to produce EPSs than to treat schizophrenia. Antipsychotic is more descriptive but could imply a more general efficacy in psychoses than is the case. It would seem more appropriate to call a drug that is used to treat schizophrenia an antischizophrenic just as we use the terms antidepressant or antiepileptic irrespective of how the drug works. Despite such personal reservations, the term neuroleptic will be used in this text. 

BACLOFEN, TIZANIDINE 1. ANAESTHETICS - general 2. ANTICANCER AND IMMUNOMODULATING DRUGS - IL-2 3. ANTIDEPRESSANTS - MAOIs 4. ANTI HYPERTENSIVES AND HEART FAILURE DRUGS 5. ANTI-PSYCHOTICS 6. ANXIOLYTICS AND HYPNOTICS 7. BETA-BLOCKERS 8. CALCIUM CHANNEL BLOCKERS 9. DIURETICS 10. NITRATES 11. PERIPHERAL VASODILATORS-moxisylyte (thymoxamine) 12. POTASSIUM CHANNEL ACTIVATORS t hypotensive effect Additive hypotensive effect. Tizanidine also has a negative chronotropic effect and may cause additive bradycardia with beta-blockers and calcium channel blockers Monitor BP at least weekly until stable. Warn patients to report symptoms of hypotension (light-headedness, dizziness on standing, etc.)... 

A difference in the in vitro activities may sometimes be desirable where a different level of receptor occupancy for each target is associated with a desired pharmacological effect. The atypical profile of the anti-psychotic drug, clozapine, has been variously associated with its lower activity at the D4 or 5-HT2A receptors compared to the... 

Many anti-psychotic drugs have what are called Parkinsonian or extra-pyramidal side effects. These are abnormalities of movement that resemble Parkinson s disease (see page 211) and are due to the blocking of dopamine D2 receptors in the basal nuclei. Anti-psychotics that also have anti-cholinergic activity (for example pericyazine) cause fewer Parkinsonian side effects. 

Brahmyadiyoga Ayurvedic traditional compound herbal formula used to treat madness. Controlled study showed anti-psychotic efficacy comparable to chlorpromazine. Mechanism of action remains unknown, but in-vitro assays confirmed D-2 activity and GABA agonist activity. 

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