A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
A syndrome characterized by HYPERPIGMENTATION, enlarging pituitary mass, visual defects secondary to compression of the OPTIC CHIASM, and elevated serum ACTH. It is caused by the expansion of an underlying ACTH-SECRETING PITUITARY ADENOMA that grows in the absence of feedback inhibition by adrenal CORTICOSTEROIDS, usually after ADRENALECTOMY.
Agents that are used to stimulate appetite. These drugs are frequently used to treat anorexia associated with cancer and AIDS.
Alkaloids, mainly tropanes, elaborated by plants of the family Solanaceae, including Atropa, Hyoscyamus, Mandragora, Nicotiana, Solanum, etc. Some act as cholinergic antagonists; most are very toxic; many are used medicinally.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.
A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.
Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin.
A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.
A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.
The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)

Inhibitory effects of cyproheptadine on pituitary-thyroid axis and pancreatic beta cells in rats. (1/134)

AIM: To study the influences of cyproheptadine (Cyp) on the endocrine functions of pituitary-thyroid axis and pancreatic beta cells in rats. METHODS: The effects of Cyp on functions of pituitary-thyroid axis and pancreatic beta cells were observed by radioimmunoassay, biochemical analysis, and electron microscope. RESULTS: Cyp 2.3 mg.kg-1 ig for 10 d decreased serum thyroid stimulating hormone (TSH) from control groups (5.3 +/- 0.9) to (4.2 +/- 0.9) mU.L-1 and insulin levels from (64 +/- 8) to (50 +/- 9) kIU.L-1 (P < 0.05 and 0.01). Cyp 4.6 mg.kg-1 decreased serum TSH (3.8 +/- 0.5) mU.L-1, T3 (1.2 +/- 0.2) mmol.L-1, T4 (62 +/- 7) mmol.L-1, and insulin levels (42 +/- 8) kIU.L-1 decreased (P < 0.05 or 0.01). The retrograde changes of ultrastructure of pituitary TSH cells and pancreatic beta cells. CONCLUSION: Cyp has an inhibiting action on endocrine functions of pituitary-thyroid axis and pancreatic beta cells in rats.  (+info)

Effects of dexamethasone, cyproheptadine, anisodamine, and dinoprostone on TNF alpha production in endotoxic shock. (2/134)

AIM: To study the effects of dexamethasone (Dex), cyproheptadine (Cyp), anisodamine (Ani), and dinoprostone (Din) on lipopolysaccharides (LPS)-induced tumor necrosis factor alpha (TNF alpha) gene expression and antishock effects of inhibiting TNF alpha production. METHODS: Endotoxic shock in rats was produced by i.v. injection of LPS (E coli O111B4, 5 mg.kg-1). TNF alpha mRNA accumulation was assessed by Northern blot. Plasma TNF alpha contents were determined by radioimmunoassay. RESULTS: The TNF alpha mRNA levels in rat liver at 2 h after LPS challenge was increased obviously (autoradiograms analyzed by scanning were 38 +/- 10 vs saline control 11 +/- 8, P < 0.01). The plasma TNF alpha contents were markedly increased [(22 +/- 3) micrograms.L-1 vs saline control (2.2 +/- 1.0) micrograms.L-1, P < 0.01]. Dex 5, Cyp 5, Ani 10, or Din 2 mg.kg-1 immediately injected after i.v. LPS markedly decreased the TNF alpha mRNA levels in rat liver and plasma TNF alpha contents. The Dex, Cyp, Ani, and Din improved the mouse survival rate 24 h after LPS 20 mg.kg-1 challenge. CONCLUSION: Dex, Cyp, Ani, and Din strongly inhibit LPS-induced TNF alpha gene expression, and have a beneficial antishock effects.  (+info)

Effects of rupatadine, a new dual antagonist of histamine and platelet-activating factor receptors, on human cardiac kv1.5 channels. (3/134)

1. The effects of rupatadine, a new dual antagonist of both histamine H1 and platelet-activating factor receptors, were studied on human cloned hKv1.5 channels expressed in Ltk- cells using the whole-cell patch-clamp technique. 2. Rupatadine produced a use- and concentration-dependent block of hKv1.5 channels (KD=2.4+/-0.7 micronM) and slowed the deactivation of the tail currents, thus inducing the 'crossover' phenomenon. 3. Rupatadine-induced block was voltage-dependent increasing in the voltage range for channel opening suggesting an open channel interaction. At potentials positive to +10 mV the blockade decreased with a shallow voltage-dependence. Moreover, rupatadine also modified the voltage-dependence of hKv1.5 channel activation, which exhibited two components, the midpoint of the steeper component averaging -25. 2+/-2.7 mV. 4. When the intracellular K+ concentration ([K+]i) was lowered to 25% the voltage-dependent unblock observed at positive potentials was suppressed and the activation curve in the presence of rupatadine did not exhibit two components even when the midpoint of the activation curve was shifted to more negative potentials (-30. 3+/-1.3 mV). 5. On channels mutated on the residue R485 (R485Y) which is located on the external entryway of the pore the rupatadine-induced block did not decrease at potentials positive to +10 mV. In contrast, on V512M channels rupatadine reproduced all the features of the blockade observed on wild type channels. 6. All these results suggest that rupatadine blocks hKv1.5 channels binding to an external and to an internal binding site but only at concentrations much higher than therapeutic plasma levels in man. Efflux of K+ promotes the unbinding from the external site. Furthermore, rupatadine binds to an internal site and dramatically modifies the voltage-dependence of channel opening.  (+info)

5-HT1P receptor-mediated slow depolarization in neurons of guinea pig inferior mesenteric ganglion. (4/134)

AIM: To study the effects of several 5-hydroxytryptamine (5-HT) receptor subtype antagonists on 5-HT-induced depolarization and the effects of 5-HT1P receptor agonist on the membrane potential in the neurons of guinea pig inferior mesenteric ganglion (IMG). METHODS: Intracellular recordings were made from neurons of the isolated guinea pig IMG. RESULTS: Cyproheptadine (5-HT1/2 antagonist 10 mumol.L-1, n = 7) and BRL 24924 (5-HT1P antagonist 10 mumol.L-1, n = 19) reversibly suppressed 5-HT slow response; pressure ejection of MCPP (5-HT1P agonist 10 mmol.L-1) induced a slow depolarization in most of 5-HT sensitive neurons (10/14). CONCLUSION: 5-HT-induced slow depolarization is mediated by 5-HT1P receptor.  (+info)

A double blind controlled study of propranolol and cyproheptadine in migraine prophylaxis. (5/134)

Role of propranolol and cyproheptadine in the prophylaxis of migraine was studied in a controlled double blind trial. Two hundred fifty-nine patients were divided into four groups. Each group was either given a placebo, cyproheptadine, propranolol or a combination of the latter two drugs. The patients were followed for a period of three months. Significant relief in frequency, duration and severity from migranous attacks was seen in all drug treated groups over placebo. Significant correlation in response was seen in frequency, duration and severity in all the groups which received drugs. Statistically more significant relief was seen in cyproheptadine and propranolol treated group as compared to individual drug treated groups. In cyproheptadine and propranolol treated groups, the dropout rate was lower and associated symptoms were better relieved than in other groups. The study shows efficacy of combination of cyproheptadine and propranolol in migraine prophylaxis.  (+info)

Verapamil, cyproheptadine, and anisodamine antagonized [Ca2+]i elevation induced by TNFalpha in a single endothelial cell. (6/134)

AIM: To study the effect of tumor necrosis factor alpha (TNFalpha) on intracellular free Ca2+ concentration ([Ca2+]i) and the effects of verapamil (Ver), cyproheptadine (Cyp), and anisodamine (Ani) on TNFalpha-induced [Ca2+]i changes in single endothelial cell, and to explore the mechanisms of TNFalpha-mediated shock and antishock actions of Cyp and Ani. METHODS: Human umbilical vein endothelial cell strains (ECV304) were seeded in 35-mm tissue culture dish with 2 mL DMEM culture medium. The cultured cells were loaded by Fluo-3/AM. The spatial distribution and the dynamic changes of [Ca2+]i in single endothelial cell were determined by laser scanning confocal microscopy. RESULTS: After stimulation with TNFalpha, [Ca2+]i in single endothelial cell rapidly increased in a concentration-dependent manner and arrived at the peak value within 60 s, afterwards, decreased and kept above the basal level. The confocal scanning image showed that [Ca2+]i elevation was more obvious in nuclear than in cytoplasma and decreased slowly. Ver (1, 2 micromol/L), Cyp (30, 60 micromol/L), and Ani (20, 40 micromol/L) markedly inhibited TNFalpha 1.2 nmol/L-induced [Ca2+]i elevation. CONCLUSION: TNFalpha markedly induces elevation of [Ca2+]i in a single endothelial cell, it may be an important mechanism of TNFalpha-induced shock and tissue injury. That Cyp and Ani obviously suppress TNFalpha-induced [Ca2+]i elevation probably is one of the mechanisms of their antishock effects.  (+info)

Anti-endotoxic shock effects of cyproheptadine in rats. (7/134)

OBJECTIVE: To investigate the antagonistic effect and mechanism of the effect of cyproheptadine (Cyp) on endotoxic shock in rats. METHODS: Endotoxic shock was produced in rats by i.v. injection of lipopolysaccharides (LPS) (5 mg/kg). Tumor necrosis factor (TNF(alpha)) mRNA expression was assessed by Northern blot. Plasma TNF(alpha) content was measured by radioimmunoassay. Plasma superoxide dismutase (SOD) activity and malondialdehyde (MDA) content were measured. The intracellular free calcium concentration ([Ca(2+)](i)) in single endothelial cells was determined by laser scanning confocal microscopy (LSCM). RESULTS: Cyp 5 mg/kg injected immediately after i.v. LPS raised the mean arterial blood pressure (MABP) of shocked rats and improved their 24 h survival rate. Meanwhile, Cyp markedly decreased TNF(alpha) mRNA levels in rat liver (18 +/- 10 vs. LPS + saline 38 +/- 10, P < 0.01) as well as plasma TNF(alpha) content [(7.8 +/- 2.4) microg/L vs. LPS + saline (21.5 +/- 3.2) microg/L, P < 0.01)]. It enhanced plasma SOD activity [(1037.2 +/- 112.8) NU/L vs LPS + saline (615.4 +/- 92.6) NU/L, P < 0.01], reduced the MDA content [(5.2 +/- 1.1) micromol/L vs. LPS + saline (9.8 +/- 1.5) micromol/L, P < 0.01], and inhibited TNF(alpha)-induced [Ca(2+)](i) elevation. CONCLUSION: Cyp exerts an anti-endotoxic shock effect by inhibiting TNF(alpha) gene expression, enhancing SOD activity, reducing lipid peroxidation, and preventing [Ca(2+)](i) overload.  (+info)

Suppressive effect of cyproheptadine on L-DOPA-induced growth hormone release in man. (8/134)

In order to elucidate the relationship between dopaminergic and serotoninergic mechanisms in regulating secretion of human growth hormone (hGH), the effect of cyproheptadine, an antiserotoninergic agent, on l-DOPA-induced hGH secretion was studied in normal subjects. Oral administration of 500 mg of l-DOPA caused a rise in plasma hGH in 6 of 7 subjects studied. This rise in plasma hGH was significantly blunted by the intravenous infusion of 5 mg of cyproheptadine. These results suggest the close relationship between dopamine and serotonin in the control of hGH secretion.  (+info)

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Obesity is one of the main risk factors of non-communicable diseases (NCDs) worldwide, especially in sub-Saharan Africa. The use of Cyproheptadine increases body weight and the risk of becoming obese. The aim of this study is to determine the prevalence of Cyproheptadine misuse in the Kinshasa population and to describe its characteristics. A cross-sectional study was conducted in two town sectors of Kinshasa, Democratic Republic of Congo (DRC), over a 4 month period (May 2011 to August 2011). Data from 499 participants, aged between 13 and 55 years were collected and analyzed. Mean and standard deviation were used for quantitative variables and frequency and percentage for categorical variables. In order to determine the relationship between socio-demographic status and Cyproheptadine use the Chi-square test was conducted. Students t-test was used to compare means age of Cyproheptadine users and non-users. Logistic regression was used to determine predictors of Cyproheptadine use. A p-value of |0.05
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Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. Cyproheptadine is used to treat allergic reactions (specifically hay fever). The evidence for its use for this purpose in children is weak and ketotifen and loratadine showed equal or better results in the small trials in which they have been compared. It is sometimes used, especially in its liquid formulation, as a preventive measure against migraine in children and adolescents, but as of 2017 the evidence for this was weak. This use is on the label in the UK and some other countries. In Australia this is the only indication for which cyproheptadine is subsidised by the PBS. It is also used off-label in the treatment of cyclical vomiting syndrome in infants; the only evidence for this use comes from retrospective studies. Cyproheptadine is sometimes used off label to improve akathisia in people on antipsychotic ...
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entrations were measured. During the breeding season, serotonin reduced LH pulse amplitude in ovariectomized hinds (P , 0.05) and cyproheptadine reduced LH pulse frequency in both ovariectomized and ovariectomized-thyroidectomized hinds (P , 0.05 and P , 0.01, respectively). In the non-breeding season cyproheptadine reduced LH pulse frequency and amplitude in ovariectomized-thyroidectomized hinds (P , 0.01). Serotonin did not affect plasma prolactin concentration, whereas cyproheptadine caused an increase (P,0.01) in plasma prolactin concentration in both the breeding and non-breeding seasons. To determine whether these compounds acted at the level of the pituitary gland, in Experiment 2 was examined their effects on the responsiveness of the pituitary gland to an exogenous GnRH challenge in ovariectomized hinds (n = 5). During the breeding season and after induction of halothane anaesthesia, hinds received either a serotonin infusion (6.6. µg/kg i.v. per min for 15 minutes), cyproheptadine (3 ...
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Cyproheptadine is an antihistamine that is commonly used in cats and dogs to treat allergies, loss of appetite, and increased serotonin production. Come to petMD for a complete list of pet medications and prescriptions.
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Cyproheptadine is sometmes used in cats to stimulate their appetite. What about the distribution in the body after oral or intravenous application?
The entire time Ive been on cyproheptadine (about seven weeks), Ive alternated between wanting to gush to you about it and feeling an immense need to keep quiet, lest I put its effect in jeopardy.
Easy to read patient leaflet for Cyproheptadine Syrup. Includes indications, proper use, special instructions, precautions, and possible side effects.
You can take cyproheptadine before or after meals. Some people find it helps to swallow the tablets with a drink of water. If you forget to take a dose, dont worry, just take the next dose when it is due and then continue as before. Do not take two doses together to make up for a forgotten dose ...
... has been studied for the treatment of posttraumatic stress disorder. Cyproheptadine is used in cats as an ... Cyproheptadine is a second line treatment for pituitary pars intermedia dysfunction in horses. "Cyproheptadine". Dictionary.com ... Cyproheptadine has been reported to block 85% of 5-HT2 receptors in the human brain at a dose of 4 mg three times per day (12 ... Cyproheptadine was studied in one small trial as an adjunct in people with schizophrenia whose condition was stable and were on ...
Goldberg SC, Halmi KA, Eckert ED, Casper RC, Davis JM (January 1979). "Cyproheptadine in anorexia nervosa". The British Journal ...
Another antagonist is cyproheptadine. Pizotifen is a non-selective antagonist. LY-367,265 - dual 5-HT2A antagonist / SSRI with ...
Cyproheptadine, Hydroxyzine, Latrepirdine, etc.) Antipsychotics Typicals (Chlorpromazine, Fluphenazine, Loxapine, Thioridazine ...
Larrey D, Geneve J, Pessayre D, Machayekhi JP, Degott C, Benhamou JP (1987). "Prolonged cholestasis after cyproheptadine- ...
Cyproheptadine is only available as tablets and therefore can only be administered orally or via a nasogastric tube; it is ... Cyproheptadine can be stopped when the person is no longer experiencing symptoms and the half life of serotonergic medications ... If this is not sufficient, a serotonin antagonist such as cyproheptadine may be used. In those with a high body temperature ... The serotonin antagonist cyproheptadine is the recommended initial therapy, although there have been no controlled trials ...
Hydroxyzine Cyproheptadine Mercier-Guyon C, Chabannes JP, Saviuc P (2004). "The role of captodiamine in the withdrawal from ...
One particular antihistamine, cyproheptadine (Periactin), has been found to be useful. The tricyclic antidepressant doxepin has ...
Benzocycloheptene Cyproheptadine Ketotifen Stark RJ, Valenti L, Miller GC (August 2007). "Management of migraine in Australian ... cyproheptadine and amitriptyline. While pizotifen is effective in adults, evidence of efficacy in children is limited, and its ... syndrome or MDMA overdose in a similar manner to the closely related antihistamine/antiserotonin medication cyproheptadine. ...
Veterinary overdose in dogs is very well treated by Cyproheptadine HCl.: 1371 Venlafaxine is highly toxic to Bacillariophyta ...
The antihistamine cyproheptadine is also effective, probably due to its antiserotonergic effects. A systematic review on non- ...
Homnick, Douglas N. (2005). "Long-term trial of cyproheptadine as an appetite stimulant in cystic fibrosis". Pediatric ... promethazine or cyproheptadine). Essential nutrient List of phytochemicals in food Body image Emaciation Malnutrition Stunted ...
Schwartz, S (1999). "Use of cyproheptadine to control urine spraying and masturbation in a cat". Journal of the American ...
Cyproheptadine US 2546652, Plati JT , Wenner W, "Pyridindenes and process for their manufacture", assigned to F Hoffmann La ... Phenindamine (Nolahist, Thephorin) is an antihistamine and anticholinergic closely related to cyproheptadine. It was developed ... exhibit optical isomerism as do other chemicals of its general type ranging from pethidine and alphaprodine to cyproheptadine ...
It is a syrup containing cyproheptadine, the amino acid lysine, and some vitamins. Cyproheptadine, the active ingredient, is an ...
Medications such as pizotifen, propanolol, and cyproheptadine may be used in rare circumstances. Abdominal migraine can have a ...
Dohmoto H, Takahara A, Uneyama H, Yoshimoto R (February 2003). "Cardiac Ca(2+) channel-blocking effects of the cyproheptadine ... It is derived from cyproheptadine, a compound with known antiserotonic, antihistaminic and calcium channel blocking properties ... "On the ionic mechanism of cyproheptadine-induced bradycardia in a rabbit sinoatrial node preparation". European Journal of ...
The antidepressant mirtazapine has demonstrated benefit, as well as diphenhydramine, trazodone, benzatropine, cyproheptadine, ... "Cyproheptadine versus propranolol for the treatment of acute neuroleptic-induced akathisia: a comparative double-blind study". ... and serotonin antagonists such as cyproheptadine may also be of help in treating acute akathisia but are much less effective ...
They include, but are not limited to: Chlorpromazine Cyproheptadine Metergoline Methysergide Mianserin Mirtazapine Oxetorone ... Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 ... Pizotifen Propranolol Ritanserin Spiperone Carbinoxamine Cyproheptadine Hydroxyzine Methdilazine Pizotifen Promethazine ...
Cyproheptadine is an antihistamine and serotonin antagonist which has been effective in significantly reducing headshaking ...
Cyproheptadine, buspirone, stimulants such as amphetamines (including the antidepressant bupropion), nefazodone has been used ...
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Many therapies have been used including hyperbaric oxygen, dapsone, antihistamines (e.g., cyproheptadine), antibiotics, dextran ...
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5-HT2C receptor antagonists/inverse agonists - mirtazapine, olanzapine, quetiapine, amitriptyline, cyproheptadine, lurasidone ... H1 receptor antagonists/inverse agonists - mirtazapine, olanzapine, quetiapine, amitriptyline, cyproheptadine, pizotifen ...
Cyproheptadine: learn about side effects, dosage, special precautions, and more on MedlinePlus ... Cyproheptadine will help relieve symptoms but will not treat the cause of symptoms or speed recovery. Cyproheptadine is in a ... Before taking cyproheptadine,. *tell your doctor and pharmacist if you are allergic to cyproheptadine, other antihistamines, or ... Cyproheptadine comes as a tablet and a solution (liquid) to take by mouth. It is usually taken two or three times a day. Take ...
Cyproheptadine hydrochloride, USP is an antihistaminic and antiserotonergic agent.. Cyproheptadine hydrochloride, USP is a ... Long -term carcinogenic studies have not been done with cyproheptadine.. Cyproheptadine had no effect on fertility in a two - ... CYPROHEPTADINE HYDROCHLORIDE tablet. To receive this label RSS feed. Copy the URL below and paste it into your RSS Reader ... Cyproheptadine has an atropine-like action and, therefore, should be used with caution in patients with: History of bronchial ...
Ross CA Antiserotonin-antihistaminic properties of cyproheptadine J. Pharmacol. exp. Ther. 1961 131:73-87 ... "Antiserotonin-antihistaminic properties of cyproheptadine" J. Pharmacol. exp. Ther.. 1961;131:73-87. ...
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Cyproheptadine is a first-generation agent. It is used for the symptomatic relief of allergic symptoms caused by histamine ... Cyproheptadine prevents histamine release in blood vessels and is more effective in preventing histamine response than in ... The first-generation H1 antagonists (eg, diphenhydramine, hydroxyzine, doxepin, chlorpheniramine, and cyproheptadine) are ...
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