Procyclidine is a muscarinic antagonist that crosses the blood-brain. Procyclidine hydrochloride (brand name Kemadrin) is a synthetic antispasmodic compound of relatively low toxicity. It has been shown to be useful for the symptomatic treatment of parkinsonism (paralysis agitans) and extrapyramidal dysfunction caused by tranquilizer therapy. Procyclidine hydrochloride was developed at The Wellcome Research Laboratories as the most promising of a series of antiparkinsonism compounds produced by chemical modification of antihistamines. Kemadrin is indicated in the treatment of parkinsonism including the postencephalitic, arteriosclerotic, and idiopathic types. Partial control of the parkinsonism symptoms is the usual therapeutic accomplishment. Procyclidine hydrochloride is usually more efficacious in the relief of rigidity than tremor; but tremor, fatigue, weakness, and sluggishness are frequently beneficially influenced. It can be substituted for all the previous medications in mild and moderate cases. For the control of more severe cases, other drugs may be added to procyclidine therapy as indications warrant. The mechanism of action is unknown. It is thought that procyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Pharmacologic tests have shown that procyclidine hydrochloride has an atropine-like action and exerts an antispasmodic effect on smooth muscle. It is a potent mydriatic and inhibits salivation. It has no sympathetic ganglionblocking activity in doses as high as 4 mg/kg, as measured by the lack of inhibition of the response of the nictitating membrane to preganglionic electrical stimulation.

Nylidrin (Buphenine, Arlidin) is a beta-adrenergic agonist. Nylidrin causes peripheral vasodilation, a positive inotropic effect, and increased gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. In peripheral vascular disorders, Arlidin (nylidrin HCl) increases walking ability and promotes healing of trophic ulcers. Nylidrin hydrochloride acts predominantly by beta-receptor stimulation. Beta stimulation with nylidrin has been demonstrated in a variety of isolated tissues from rabbits, guinea pigs and dogs. It has been shown to dilate arterioles in skeletal muscle and to increase cardiac output in the anesthetized dog and cat and in unanesthetized man. An increase in cerebral blood flow and a decrease in vascular resistance has also been reported. The result of this combination of actions is a greater blood supply to ischemic tissues, with usually minimal change in blood pressure. Arlidin may be of benefit in elderly patients with mild to moderate symptoms that are commonly associated with organic mental disorders. Short-term (3 months’ duration) and long-term (12 months’ duration) clinical studies have demonstrated a modest improvement in ability to perform general activities of daily living, self-care and in a capability for social interactions. The mechanism whereby nylidrin may provide relief of selected symptoms in some elderly patients with organic brain disorders is not known.

Azacyclonol (aka gamma-pipradrol) is an ataractive agent; a compound which diminished hallucinations in psychotic individuals. It is sometimes referred to as a tranquilizer or antipsychotic, though it does not actually possess these properties. It was used in Europe during the 1950's for treatment of schizophrenia; likely to reduce the psychedelic effects of LSD and mescaline. However, it had mixed clinical effectiveness and did not gain widespread adoption and was eventually discontinued. Azacyclonol was sold under several trade names: Ataractan, Calmeran, Frenoton, Frenquel and Psychosan.

Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.

Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.

Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.

Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.

Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.

Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs. It’s usually used to kill the cramp-like pain of gastric/duodenal ulcer, gastritis, enteritis, gallstones, cholecystitis and biliary tract dyskinesia and to improve some symptoms in threatened miscarriage/premature delivery. Piperidolate blocked the contraction of ACh, Ba ++ and electrical stimulations on the isolated rat, mouse and guinea-pig ileum and trachea. In guinea-pig teania caeci, piperidolate like papaverine blocked specifically the tonic response, however, piperidolate in high doses completely blocked both spike and tonic responses. These results indicate that spasmolytic action of piperidolate like that of papaverine may depend upon inhibition of the release of store Ca++. Moreover piperidolate, given at high doses, may inhibit the contractile elements in the smooth muscle. In the rat uterus pretreated with sex hormones, piperidolate nonspecifically blocked the contraction of ACh, Ba ++ and oxytocin and sex hormones had no influence on the spasmolytic action of piperidolate.

Buclizine, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. The drug is used mainly for its antiemetic action, particularly in the prevention of motion sickness, and in the treatment of migraine in combination with analgesics. The following side/adverse effects have been selected on the basis of their potential clinical significance: drowsiness; Incidence less frequent; blurred vision; dryness of mouth, nose, and throat; headache; nervousness, restlessness, or trouble in sleeping; upset stomach. The following drug interactions have been selected on the basis of their potential clinical significance: alcohol; anticholinergics or other medications with anticholinergic activity; apomorphine.