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Intestinal Pharmacomanometry
Published in Fuad Lechin, Bertha van der Dijs, Neurochemistry and Clinical Disorders: Circuitry of Some Psychiatric and Psychosomatic Syndromes, 2020
Fuad Lechin, Bertha van der Dijs, Francisco Gomez, Marcel Lechin, Luis Arocha, Simon Villa
The following generalizations may be made, overlooking some variants which continue to be recorded in detailed published papers: drugs which activate the NE system, besides lowering IT, tend to raise rectal PA; drugs which activate the DA system, besides reducing IT tend to raise sigmoidal PA; and anti-ACh drugs which cross the hemato-brain barrier tend to lower sigmoidal PA and raise rectal PA. The motility changes induced by NE/DA agonists are reverted by NE/ DA antagonists. Similarly, antagonistic effects are frequently found between NE/DA antagonists and ACh antagonists, as well as between presynaptic NE/DA and postsynaptic NE/DA blocking agents. Domperidone, a DA-blocking agent lacking central effects, does not affect DCM,17 whereas hioscine, a peripheral anti-ACh agent lacking central effects, does influence DCM. Furthermore, this drug induces opposite effects to those induced by biperiden, a central acting anti-ACh agent.
Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
Parkinson’s disease (PD) characterized tremors and rigidity results from cholinergic overactivity in basal ganglia (Sharma and Sharma, 2017). The combination of antimuscarinic drugs with a dopaminergic drug is advantageous than using either drug alone. Most of the centrally acting antimuscarinics used in PD due to their ability to block muscarinic receptors in the striatum. These agents are used either alone in early stage or as an adjunct to levodopa in later stages of the disease. These drugs are also useful in relieving neuroleptic-induced extrapyramidal side effects. These drugs like benzhexol, procyclidine, benzatropine, and biperiden used in PD show adverse effects attributed to their anticholinergics effect that include dryness of mouth, blurred vision, confusion, reduced secretions, decreased motility as in urinary and gastric retention, hallucinations, and so on (Rang et al., 2003; Sharma and Sharma, 2017).
The Epileptic Gerbil. Neuronal Networks and Actions of Antiepileptic Drugs
Published in Carl L. Faingold, Gerhard H. Fromm, Drugs for Control of Epilepsy:, 2019
In general, the role of cholinergic neurons in genetic animal models of epilepsy has received little attention.44 In gerbils the classical anticholinergic drug atropine exerted only weak anticonvulsant effects at doses (20% protection at 10 mg/kg i.p.), clearly above those necessary for selective anticholinergic action.32 Similarly, the central anticholinergic (anti-parkinsonism) drug biperiden proved capable of blocking seizures in gerbils with an ED-50 of 12 mg/kg;32 however, this dosage was considerably higher than the anticholinergic ED-50 determined in the oxotremorine test in gerbils (1.5 mg/kg). This casts doubt on the specificity of the anticonvulsant effects of the anticholinergics in gerbils. Interestingly, the muscarinic agonist oxotremorine induced generalized convulsions in several gerbils at 0.3 mg/kg i.p.32 However, in view of the lack of effect between anticholinergic effect and anticonvulsant effect of anticholinergic drugs found in gerbils, acetylcholine does not seem to be critically involved in the seizure-prone state in gerbils.
Lurasidone in adolescents and adults with schizophrenia: from clinical trials to real-world clinical practice
Published in Expert Opinion on Pharmacotherapy, 2022
Andrea Fiorillo, Alessandro Cuomo, Gaia Sampogna, Umberto Albert, Paola Calò, Giancarlo Cerveri, Sergio De Filippis, Gabriele Masi, Maurizio Pompili, Gianluca Serafini, Antonio Vita, Alessandro Zuddas, Andrea Fagiolini
The duration of the illness was of about 28 years, the patient had been treated with different typical antipsychotics (including haloperidol and chlorpromazine), but he reported several side effects including increase in body weight, prolongation EPS extrapyramidal symptoms including inability to sit still, involuntary muscle contraction, tremors, and involuntary facial movements. Furthermore, he had achieved a remission of positive symptomatology, in terms of reduction of severity of delusions and hallucinations, while anhedonia, cognitive deficits including lack of attention and difficulties in recalling memories, still persisted. Therefore, during the hospital admission due to the persisting and disabling cognitive symptoms and EPS, a treatment with LUR was initiated (with a simultaneous reduction of typical antipsychotics) at a dose of 37.5 mg for three days, and then increased at 74 mg for seven days. The patient reported a reduction in tremors and inability to sit still when haloperidol was completely suspended (after 10 days from hospital admission). A remission of clinical symptomatology - both positive and negative symptoms - was observed with the increased dose at 111 mg/day. At day 17, he started to present akathisia and tremors, therefore it was introduced biperiden 1 mg/twice daily. He reported a subjective reduction of inability to sit and of tremor. After 5 days, biperiden was increased at 2 mg/twice daily with a dosage of 111 mg lurasidone once/daily. Therefore, the EPS were significantly reduced, and the clinical status was in remission.
Where do we go next in antidepressant drug discovery? A new generation of antidepressants: a pivotal role of AMPA receptor potentiation and mGlu2/3 receptor antagonism
Published in Expert Opinion on Drug Discovery, 2022
Andrzej Pilc, Agata Machaczka, Paweł Kawalec, Jodi L. Smith, Jeffrey M. Witkin
The structures of two muscarinic receptor antagonists that have clinical use in patients are shown in Figure 5. Biperiden is used in the clinical management of Parkinson’s disease [80]. Both scopolamine and biperiden have been studied for their antidepressant effects with scopolamine being the most widely investigated in depressed patients. Scopolamine is a naturally derived alkaloid of a species of plant from the Solanaceae family. Scopolamine is a nonselective antagonist of muscarinic acetylcholine receptors and is widely used as a butyl bromide salt in the treatment of abdominal pain, irritable bowel syndrome and bladder spasms (in this form it does not readily penetrate into the CNS). A hydrobromide derivative (which enters the brain) is used as a motion sickness reliever and sometimes as a preoperative medication [81]. Scopolamine induces hyperactivity and dream-like ‘hallucinations,’ and at a dose of 24 ug/kg i.m., produced delirium in humans [82]. Scopolamine belongs to a separate group of drugs that have been termed deliriants [83].
Constipation, ileus and medication use during clozapine treatment in patients with schizophrenia in Iceland
Published in Nordic Journal of Psychiatry, 2018
Oddur Ingimarsson, James H. MacCabe, Engilbert Sigurdsson
There were 28 patients out of 154 (18.2%) participants on clozapine that used other medication which are known to reduce bowel movements (anticholinergics, TCA and opioids). Of them biperiden was the most common medication, 21 patients using it. Four patients were on amitriptyline, two on tramadol, two on morphine and one on a codeine-paracetamol combination. Of the 28 patients on clozapine as well as some other medication associated with constipation only half were receiving laxatives. Of the four patients diagnosed with ileus, three were taking biperiden (an anticholinergic) and two out of four were on laxatives.