Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Methysergide: 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.Nelson 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.Appetite Stimulants: Agents that are used to stimulate appetite. These drugs are frequently used to treat anorexia associated with cancer and AIDS.Solanaceous Alkaloids: 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.Histamine H1 Antagonists: 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.Serotonin: 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.Diphenhydramine: 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.Ketotifen: 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.Pizotyline: Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.Receptors, Serotonin: 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.Fenclonine: 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.Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.Quipazine: 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.5-Hydroxytryptophan: The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant.Ketanserin: 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.Pimozide: 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)Off-Label Use: The practice of prescribing or using a drug outside the scope of the drug's official approved label as designated by a regulatory agency concerning the treatment of a particular disease or condition.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.Akathisia, Drug-Induced: A condition associated with the use of certain medications and characterized by an internal sense of motor restlessness often described as an inability to resist the urge to move.Prenylamine: A drug formerly used in the treatment of angina pectoris but superseded by less hazardous drugs. Prenylamine depletes myocardial catecholamine stores and has some calcium channel blocking activity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1406)Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Potassium: An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.Appetite: Natural recurring desire for food. Alterations may be induced by APPETITE DEPRESSANTS or APPETITE STIMULANTS.Cross-Over Studies: Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)Pharmaceutical Preparations: Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form.Biological Products: Complex pharmaceutical substances, preparations, or matter derived from organisms usually obtained by biological methods or assay.Citrate (si)-Synthase: Enzyme that catalyzes the first step of the tricarboxylic acid cycle (CITRIC ACID CYCLE). It catalyzes the reaction of oxaloacetate and acetyl CoA to form citrate and coenzyme A. This enzyme was formerly listed as EC Enlargement of the BREAST in the males, caused by an excess of ESTROGENS. Physiological gynecomastia is normally observed in NEWBORNS; ADOLESCENT; and AGING males.Sexism: Prejudice or discrimination based on gender or behavior or attitudes that foster stereotyped social roles based on gender.Internal Medicine: A medical specialty concerned with the diagnosis and treatment of diseases of the internal organ systems of adults.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Publishing: "The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.Bibliometrics: The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)Directories as Topic: Lists of persons or organizations, systematically arranged, usually in alphabetic or classed order, giving address, affiliations, etc., for individuals, and giving address, officers, functions, and similar data for organizations. (ALA Glossary of Library and Information Science, 1983)Cats: The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801)Tryptophan Hydroxylase: An enzyme that catalyzes the hydroxylation of TRYPTOPHAN to 5-HYDROXYTRYPTOPHAN in the presence of NADPH and molecular oxygen. It is important in the biosynthesis of SEROTONIN.Drug Prescriptions: Directions written for the obtaining and use of DRUGS.Injections, Intravenous: Injections made into a vein for therapeutic or experimental purposes.Suspensions: Colloids with liquid continuous phase and solid dispersed phase; the term is used loosely also for solid-in-gas (AEROSOLS) and other colloidal systems; water-insoluble drugs may be given as suspensions.Food-Drug Interactions: The pharmacological result, either desirable or undesirable, of drugs interacting with components of the diet. (From Stedman, 25th ed)Administration, Oral: The giving of drugs, chemicals, or other substances by mouth.Capsules: Hard or soft soluble containers used for the oral administration of medicine.Tablets: Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)Proinsulin: A pancreatic polypeptide of about 110 amino acids, depending on the species, that is the precursor of insulin. Proinsulin, produced by the PANCREATIC BETA CELLS, is comprised sequentially of the N-terminal B-chain, the proteolytically removable connecting C-peptide, and the C-terminal A-chain. It also contains three disulfide bonds, two between A-chain and B-chain. After cleavage at two locations, insulin and C-peptide are the secreted products. Intact proinsulin with low bioactivity also is secreted in small amounts.Insulin: A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).Hyperglycemia: Abnormally high BLOOD GLUCOSE level.Blood Glucose: Glucose in blood.Glucose: A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.

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 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 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 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 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 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)

  • Diseases such as Cushing's lead to an increase in serotonin, so cyproheptadine may be used to reduce serotonin levels. (
  • In Experiment 1, ovariectomized (n = 5) and ovariectomized-thyroidectomized (n = 5) hinds received a vehicle solution followed 4 h later by either serotonin (66 µg/kg, i.v.) every 10 minutes for a further 4 h or the serotonin antagonist, cyproheptadine (3 mg/kg, i.v.) as a single injection. (
  • The response of plasma LH to exogenous GnRH was not altered by serotonin or cyproheptadine in either season. (
  • Drugs with anti-serotonin activity, such as cyproheptadine. (
  • Depending on the dose of cyproheptadine and your overall physical health, combining these medications may increase the irritant effects of potassium on your stomach and upper intestine. (
  • µg/kg i.v. per min for 15 minutes), cyproheptadine (3 mg/kg i.v. as a single dose) or vehicle. (
  • Cyproheptadine is known to be an antagonist or inverse agonist of all of the receptors listed in the table to the right. (
  • Cyproheptadine works by blocking H-1 receptors, which occur on the small blood vessels and smooth muscles. (
  • Cyproheptadine is also sometimes used to treat allergic reactions in people who have received blood products as part of medical treatment and to treat life-threatening allergic reactions after the symptoms have been brought under control with other medications. (
  • Cyproheptadine will help relieve symptoms but will not treat the cause of symptoms or speed recovery. (
  • Below are symptoms of a cyproheptadine overdose in different parts of the body. (
  • Cyproheptadine is used to treat sneezing, runny nose, itching, red or watery eyes, and other symptoms of seasonal allergies (hay fever). (
  • Periactin (cyproheptadine) relieves seasonal and year-round allergy symptoms such as watery/itchy eyes, runny nose, and. (
  • Cyproheptadine is used to treat allergic reactions (specifically hay fever). (
  • Cyproheptadine is also used to treat other conditions such as eczema or skin reactions to insect bites. (
  • Cyproheptadine is used to treat allergies and allergic reactions. (
  • To treat allergies and allergic reactions, cyproheptadine is dosed at 0.15 to 1 mg per poung (0.3 to 2 mg/kg) twice daily in dogs, and 2 mg per cat twice daily. (
  • Age-associated changes in less than 50% of infestation include institutionalized patients (both young cyproheptadine order and pulmonary reactions (eg, most often genomic losses and to better understand its effect on commercial airlines is primarily used to leukemia have been noted in the acronym OARS (open-ended questions, ototoxicity, gender, naloxegol, is 20 to seriously ill patients. (
  • Through friends cyproheptadine hcl 4mg for dogs Roger Federer of.What do you want to do when you've finished? (
  • At the said to be an exact duplicate of apparatus in use in the laboratories during operations upon dogs, and one of the witnesses stated that once a week for the last six months she had crawled through a hole in the fence surrounding the animal house so as to inspect the condition of the dogs there confined (cyproheptadine). (
  • cyproheptadine benefits and side effects, the Disparagement of the Prnfession We your Honours Memo, cyproheptadine hydrochloride for dogs, typhus the liberal use of cold water both internally and, cyproheptadine oral tablet 4mg, at Roxbury the number of sick and wounded I cannot ascertain. (
  • Cyproheptadine, a serotonin antagonist, has been shown to be a potentially effective and safe treatment option in children who meet the clinical criteria for FGIDs. (