![]() ![]() Thioridazine is used to treat schizophrenia and related psychoses. Anticholinergic effects including blurred vision, decreased gastrointestinal motility, delirium, agitation, hallucination, hyperthermia, tachycardia, and seizures have been seen. Clinical signs of toxicity most frequently include sedation, coma, hypotension, extrapyramidal effects, and cardiac arrhythmias. ![]() Phenothiazines may lower the seizure threshold. Phenothiazines also possess peripheral adrenergic receptor blockade and quinidine-like cardiac effects. Phenothiazines primarily block postsynaptic neurotransmission by binding to dopamine (D 1 and D 2), muscarinic, histamine H 1, and serotonergic 5-hydroxytryptamine (HT) 2 receptors. Phenothiazines are used to treat psychosis including schizophrenia violent, agitated, disturbed behavior and mania secondary to bipolar disorder. Chlorpromazine was the first of the phenothiazines used clinically as an antipsychotic. Phenothiazines are neuroleptic agents that affect a variety of receptors including dopaminergic receptor sites. Marraffa, in Encyclopedia of Toxicology (Third Edition), 2014 Abstract Olanzapine therefore may also be used in combination with other agents like dexamethasone or an NK-1 antagonist. These symptoms improved by days 3 to 5 despite continued use of oral olanzapine. Patients who received olanzapine had significantly increased sedation, which was severe in 5% of cases, particularly at day 2 as compared with baseline. A double-blind trial that compared olanzapine, 10 mg, with placebo, both in combination with dexamethasone, oral aprepitant, or IV fosaprepitant and a 5-HT 3 receptor antagonist demonstrated a clinically significant reduction in chemotherapy-induced nausea and vomiting, with benefits extending up to 120 hours after administration. 125,126 Side effects of the use of olanzapine include mild sedation, weight gain, and increased risk of diabetes mellitus. Olanzapine, a second-generation neuroleptic agent, is an attractive alternative because of its strong antinausea and antiemetic action and lack of extrapyramidal side effects. ![]() 124 For this reason, the dose of droperidol should not exceed 1 mg. 122,123 Safety concerns, especially extrapyramidal effects, have limited the use of all these agents to some degree. They are also useful for patients with vomiting from toxic agents, from chemotherapy and after surgery. These drugs tend to induce relaxation and somnolence and are generally used parenterally or as suppositories in patients with acute intense vomiting of central origin, as in vertigo, migraine headaches, and motion sickness. The phenothiazines (chlorpromazine, perphenazine, prochlorperazine, promethazine, and thiethylperazine) and butyrophenones (droperidol and haloperidol) also block D2 dopaminergic receptors in addition to muscarinic M1 receptors phenothiazines also block histamine H 1 receptors. Mark Feldman MD, in Sleisenger and Fordtran's Gastrointestinal and Liver Disease, 2021 Phenothiazines and Butyrophenones ![]()
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