Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.
A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.
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.
Compounds containing phenyl-1-butanone.
Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.
A family of voltage-gated potassium channels that are characterized by long N-terminal and C-terminal intracellular tails. They are named from the Drosophila protein whose mutation causes abnormal leg shaking under ether anesthesia. Their activation kinetics are dependent on extracellular MAGNESIUM and PROTON concentration.
Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Use of written, printed, or graphic materials upon or accompanying a product or its container or wrapper. It includes purpose, effect, description, directions, hazards, warnings, and other relevant information.
Large, robust forms of brown algae (PHAEOPHYCEAE) in the order Laminariales. They are a major component of the lower intertidal and sublittoral zones on rocky coasts in temperate and polar waters. Kelp, a kind of SEAWEED, usually refers to species in the genera LAMINARIA or MACROCYSTIS, but the term may also be used for species in FUCUS or Nereocystis.
Compounds with a BENZENE fused to IMIDAZOLES.
A family of hexahydropyridines.
The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.
Agents, usually topical, that relieve itching (pruritus).
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.
A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment.
A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.
A syndrome that is characterized by the triad of severe PEPTIC ULCER, hypersecretion of GASTRIC ACID, and GASTRIN-producing tumors of the PANCREAS or other tissue (GASTRINOMA). This syndrome may be sporadic or be associated with MULTIPLE ENDOCRINE NEOPLASIA TYPE 1.
Compounds that inhibit H(+)-K(+)-EXCHANGING ATPASE. They are used as ANTI-ULCER AGENTS and sometimes in place of HISTAMINE H2 ANTAGONISTS for GASTROESOPHAGEAL REFLUX.
Compounds that contain benzimidazole joined to a 2-methylpyridine via a sulfoxide linkage. Several of the compounds in this class are ANTI-ULCER AGENTS that act by inhibiting the POTASSIUM HYDROGEN ATPASE found in the PROTON PUMP of GASTRIC PARIETAL CELLS.
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)
A common inhabitant of the colon flora in human infants and sometimes in adults. It produces a toxin that causes pseudomembranous enterocolitis (ENTEROCOLITIS, PSEUDOMEMBRANOUS) in patients receiving antibiotic therapy.
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.
A vascular reaction of the skin characterized by erythema and wheal formation due to localized increase of vascular permeability. The causative mechanism may be allergy, infection, or stress.
A traditional grouping of drugs said to have a soothing or calming effect on mood, thought, or behavior. Included here are the ANTI-ANXIETY AGENTS (minor tranquilizers), ANTIMANIC AGENTS, and the ANTIPSYCHOTIC AGENTS (major tranquilizers). These drugs act by different mechanisms and are used for different therapeutic purposes.
Spasmodic contraction of the smooth muscle of the bronchi.
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.
An evanescent cutaneous reaction occurring when antibody is injected into a local area on the skin and antigen is subsequently injected intravenously along with a dye. The dye makes the rapidly occurring capillary dilatation and increased vascular permeability readily visible by leakage into the reaction site. PCA is a sensitive reaction for detecting very small quantities of antibodies and is also a method for studying the mechanisms of immediate hypersensitivity.
Insect members of the superfamily Apoidea, found almost everywhere, particularly on flowers. About 3500 species occur in North America. They differ from most WASPS in that their young are fed honey and pollen rather than animal food.
Immunologically mediated adverse reactions to medicinal substances used legally or illegally.
It is a form of protection provided by law. In the United States this protection is granted to authors of original works of authorship, including literary, dramatic, musical, artistic, and certain other intellectual works. This protection is available to both published and unpublished works. (from Circular of the United States Copyright Office, 6/30/2008)
Specific sites or molecular structures on cell membranes or in cells with which phencyclidine reacts or to which it binds to elicit the specific response of the cell to phencyclidine. Studies have demonstrated the presence of multiple receptor sites for PCP. These are the PCP/sigma site, which binds both PCP and psychotomimetic opiates but not certain antipsychotics, and the PCP site, which selectively binds PCP analogs.
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.
Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.
An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.
Devices designed to provide personal protection against injury to individuals exposed to hazards in industry, sports, aviation, or daily activities.
A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.
The interactions between physician and patient.
An agency of the PUBLIC HEALTH SERVICE concerned with the overall planning, promoting, and administering of programs pertaining to maintaining standards of quality of foods, drugs, therapeutic devices, etc.
Use of plants or herbs to treat diseases or to alleviate pain.
Chinese herbal or plant extracts which are used as drugs to treat diseases or promote general well-being. The concept does not include synthesized compounds manufactured in China.
Improper use of drugs or medications outside the intended purpose, scope, or guidelines for use. This is in contrast to MEDICATION ADHERENCE, and distinguished from DRUG ABUSE, which is a deliberate or willful action.
Methods or procedures used to obtain samples of URINE.
Forceful administration into a muscle of liquid medication, nutrient, or other fluid through a hollow needle piercing the muscle and any tissue covering it.
A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.
A range of methods used to reduce pain and anxiety during dental procedures.
A class of chemicals derived from barbituric acid or thiobarbituric acid. Many of these are GABA MODULATORS used as HYPNOTICS AND SEDATIVES, as ANESTHETICS, or as ANTICONVULSANTS.

Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs. (1/48)

AIMS: To quantify and compare the incidence of ventricular arrhythniias associated with the use of five nonsedating antihistamines: acrivastine, astemizole, cetirizine, loratadine and terfenadine. The effects of age, sex, dose, duration of treatment, and the interaction with P450 inhibitor drugs were also examined. METHODS: We carried out a cohort study with a nested case-control analysis using the UK-based General Practice Research database (GPRD). The study cohort included persons aged less than 80 years old who received their first prescription for any of the five study drugs between January 1, 1992 and September 30, 1996. We estimated relative risks and 95% confidence intervals of idiopathic ventricular arrhythmias with current use of antihistamines as compared with non use. RESULTS: The study cohort included 197425 persons who received 513012 prescriptions. Over the study period 18 valid cases of idiopathic ventricular arrhythmias were detected. Nine occurred during the current use of any antihistamine, resulting in a crude incidence of 1.9 per 10000 person-years (95%CI: 1.0-3.6) and a relative risk of 4.2 (95%CI: 1.5-11.8) as compared with non use. Astemizole presented the highest relative risk (RR= 19.0; 95%CI: 4.8-76.0) of all study drugs, while terfenadine (RR=2.1; 95%CI:0.5-8.5) was in the range of other nonsedating antihistamines. Older age was associated with a greater risk of ventricular arrhythmias (RR=7.4; 95%CI: 2.6-21.4) and seemed to increase the effect of antihistamines (RR=6.4; 95%CI: 1.7-24.8). The proportions of high dose terfenadine and the concomitant use with P450 inhibitors among current users of terfenadine were 2.7% and 3.4%, respectively over the study period with no single case of ventricular arrhythmias occurring in the presence of these two risk factors. CONCLUSIONS: The use of nonsedating antihistamines increases the risk of ventricular arrhythmias by a factor of four in the general population. Yet, the absolute effect is quite low requiring 57000 prescriptions, or 5300 person-years of use for one case to occur. The risk associated with terfenadine was no different from that with other nonsedating antihistamines.  (+info)

Correction of defective protein trafficking of a mutant HERG potassium channel in human long QT syndrome. Pharmacological and temperature effects. (2/48)

The chromosome 7-linked form of congenital long QT syndrome (LQT2) is caused by mutations in the human ether-a-go-go-related gene (HERG) that encodes the rapidly activating delayed rectifier potassium channel. One mechanism for the loss of normal channel function in LQT2 is defective protein trafficking, which results in the failure of the channel protein to reach the plasma membrane. Here we show that the N470D LQT2 mutant protein is trafficking-deficient when expressed at 37 degrees C in HEK293 cells, whereas at 27 degrees C its trafficking to the plasma membrane and channel function are markedly improved. We further show that the antiarrhythmic drug E-4031, which selectively blocks HERG channels, also corrects defective protein trafficking of the N470D mutant and can restore the generation of HERG current. Similar findings were obtained with the drugs astemizole and cisapride, as well as with high concentrations of glycerol. The effect of E-4031 on HERG protein trafficking was concentration-dependent and required low drug concentrations (saturation present at 5 microM), developed rapidly with drug exposure, and occurred post-translationally. These findings suggest that protein misfolding leading to defective trafficking of some HERG LQT mutations may be corrected by specific pharmacological strategies.  (+info)

Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. (3/48)

The S631C mutation in human ether-a-go-go-related gene (HERG) channels has previously been reported to disrupt C-type inactivation and ion-selectivity when Cys-631 is in the oxidized state. In this study, we report the relation between pharmacology and C-type inactivation for HERGS631C channels. We demonstrate that HERGS631C in its reduced state is fully blocked by 1 microM astemizole, terfenadine and dofetilide, similar to wild-type HERG channels. In contrast, oxidized HERGS631C is insensitive for these blockers. Our results suggest that an interaction with HERG channels in the inactivated state might be a common mechanism to a variety of drugs known to block HERG channels with high affinity.  (+info)

Pharmacological blockade of ERG K(+) channels and Ca(2+) influx through store-operated channels exerts opposite effects on intracellular Ca(2+) oscillations in pituitary GH(3) cells. (4/48)

In the present study, the effects on intracellular calcium concentration ([Ca(2+)](i)) oscillations of the blockade of ether-a-go-go-related gene (ERG) K(+) channels and of Ca(2+) influx through store-operated channels (SOC) activated by [Ca(2+)](i) store depletion have been studied in GH(3) cells by means of a combination of single-cell fura-2 microfluorimetry and whole-cell mode of the patch-clamp technique. Nanomolar concentrations (1-30 nM) of the piperidinic second-generation antihistamines terfenadine and astemizole and of the class III antiarrhythmic methanesulfonanilide dofetilide, by blocking ERG K(+) channels, increased the frequency and the amplitude of [Ca(2+)](i) oscillations in resting oscillating GH(3) cells. These compounds also induced the appearance of an oscillatory pattern of [Ca(2+)](i) in a subpopulation of nonoscillating GH(3) cells. The effects of ERG K(+) channel blockade on [Ca(2+)](i) oscillations appeared to be due to the activation of L-type Ca(2+) channels, because they were prevented by 300 nM nimodipine. By contrast, the piperazinic second-generation antihistamine cetirizine (0.01-30 microM), which served as a negative control, failed to affect ERG K(+) channels and did not interfere with [Ca(2+)](i) oscillations in GH(3) cells. Interestingly, micromolar concentrations of terfenadine and astemizole (0.3-30 microM), but not of dofetilide (10-100 microM), produced an inhibition of the spontaneous oscillatory pattern of [Ca(2+)](i) changes. This effect was possibly related to an inhibition of SOC, because these compounds inhibited the increase of [Ca(2+)](i) achieved by extracellular calcium reintroduction after intracellular calcium store depletion with the sarcoplasmic or endoplasmic reticulum calcium ATPase pump inhibitor thapsigargin (10 microM) in an extracellular calcium-free medium. The same inhibitory effect on [Ca(2+)](i) oscillations and SOC was observed with the first-generation antihistamine hydroxyzine (1-30 microM), the more hydrophobic metabolic precursor of cetirizine. Collectively, the results of the present study obtained with compounds that interfere in a different concentration range with ERG K(+) channels or SOC suggest that 1) ERG K(+) channels play a relevant role in controlling the oscillatory pattern of [Ca(2+)](i) in resting GH(3) cells and 2) the inhibition of SOC might induce an opposite effect, i.e., an inhibition of [Ca(2+)](i) oscillations.  (+info)

Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. (5/48)

1. Ventricular arrhythmias are rare but life-threatening side effects of therapy with the second-generation H(1) receptor antagonists terfenadine and astemizole. Blockade of the K(+) channels encoded by the Human Ether-a-go-go-Related Gene 1 (HERG1) K(+) channels, which is the molecular basis of the cardiac repolarizing current I(Kr), by prolonging cardiac repolarization, has been recognized as the mechanism underlying the cardiac toxicity of these compounds. 2. In the present study, the potential blocking ability of the novel second-generation H(1) receptor antagonist mizolastine of the HERG1 K(+) channels heterologously expressed in Xenopus oocytes and in HEK 293 cells or constitutively present in SH-SY5Y human neuroblastoma cells has been examined and compared to that of astemizole. 3. Mizolastine blocked HERG1 K(+) channels expressed in Xenopus oocytes with an estimated IC(50) of 3.4 microM. Mizolastine blockade was characterized by a fast dissociation rate when compared to that of astemizole; when fitted to a monoexponential function, the time constants for drug dissociation from the K(+) channel were 72.4+/-11.9 s for 3 microM mizolastine, and 1361+/-306 s for 1 microM astemizole. 4. In human embryonic kidney 293 cells (HEK 293 cells) stably transfected with HERG1 cDNA, extracellular application of mizolastine exerted a dose-related inhibitory action on I(HERG1), with an IC(50) of 350+/-76 nM. Furthermore, mizolastine dose-dependently inhibited HERG1 K(+) channels constitutively expressed in SH-SY5Y human neuroblastoma clonal cells. 5. The results of the present study suggest that the novel second-generation H(1) receptor antagonist mizolastine, in concentrations higher than those achieved in vivo during standard therapy, is able to block in some degree both constitutively and heterologously expressed HERG1 K(+) channels, and confirm the heterogeneity of molecules belonging to this therapeutical class with respect to their HERG1-inhibitory action.  (+info)

Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole. (6/48)

An acute in vivo model for drug-induced torsades de pointes (TdP) for use in safety evaluation of drugs was developed using dogs with acute complete atrioventricular (AV) block. In order to study the effects of anesthetic agents on the inducibility of TdP, arrhythmias were induced by programmed electrical stimulation (PES) before and after cumulative intravenous administration of quinidine under anesthesia with sodium pentobarbital, halothane, or isoflurane. Both prolongation of the QTc and the incidence of TdP were greatest in dogs anesthetized with halothane and were smallest in those given pentobarbital, suggesting that halothane is the most suitable anesthetic for this TdP model. To further validate this model, astemizole was administered intravenously to other dogs under halothane anesthesia. Astemizole at 0.3 mg/kg caused slight prolongation of the QT interval but did not induce any arrhythmias. At 1 mg/kg, however, TdP were induced in 5 of 10 animals and in an additional 2 animals at 3 mg/kg. Single and multiple ectopic beats preceded the induction of TdP, and the ectopic beats were observed in a dose-dependent manner. The plasma concentrations of quinidine in dogs with TdP were equivalent to or less than quinidine levels in humans with TdP, while those of astemizole were higher in dogs. In conclusion, this acute canine model of TdP with halothane anesthesia, complete AV block, PES, and simultaneous measurements of plasma drug concentration would be valuable for assessing the risk of drugs, especially I(Kr) blockers, to induce TdP in humans.  (+info)

Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. (7/48)

AIMS: The aims of the present study were to investigate the metabolism of astemizole in human liver microsomes, to assess possible pharmacokinetic drug-interactions with astemizole and to compare its metabolism with terfenadine, a typical H1 receptor antagonist known to be metabolized predominantly by CYP3A4. METHODS: Astemizole or terfenadine were incubated with human liver microsomes or recombinant cytochromes P450 in the absence or presence of chemical inhibitors and antibodies. RESULTS: Troleandomycin, a CYP3A4 inhibitor, markedly reduced the oxidation of terfenadine (26% of controls) in human liver microsomes, but showed only a marginal inhibition on the oxidation of astemizole (81% of controls). Three metabolites of astemizole were detected in a liver microsomal system, i.e. desmethylastemizole (DES-AST), 6-hydroxyastemizole (6OH-AST) and norastemizole (NOR-AST) at the ratio of 7.4 : 2.8 : 1. Experiments with recombinant P450s and antibodies indicate a negligible role for CYP3A4 on the main metabolic route of astemizole, i.e. formation of DES-AST, although CYP3A4 may mediate the relatively minor metabolic routes to 6OH-AST and NOR-AST. Recombinant CYP2D6 catalysed the formation of 6OH-AST and DES-AST. Studies with human liver microsomes, however, suggest a major role for a mono P450 in DES-AST formation. CONCLUSIONS: In contrast to terfenadine, a minor role for CYP3A4 and involvement of multiple P450 isozymes are suggested in the metabolism of astemizole. These differences in P450 isozymes involved in the metabolism of astemizole and terfenadine may associate with distinct pharmacokinetic influences observed with coadministration of drugs metabolized by CYP3A4.  (+info)

The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. (8/48)

Mutations in the human ether-a-gogo-related gene (HERG) K(+) channel gene cause chromosome 7-linked long QT syndrome type 2 (LQT2), which is characterized by a prolonged QT interval in the electrocardiogram and an increased susceptibility to life-threatening cardiac arrhythmias. LQT2 mutations produce loss-of-function phenotypes and reduce I(Kr) currents either by the heteromeric assembly of non- or malfunctioning channel subunits with wild type subunits at the cell surface or by retention of misprocessed mutant HERG channels in the endoplasmic reticulum. Misprocessed mutations often encode for channel proteins that are functional upon incorporation into the plasma membrane. As a result the pharmacological correction of folding defects and restoration of protein function are of considerable interest. Here we report that the trafficking-deficient pore mutation HERG G601S was rescued by a series of HERG channel blockers that increased cell surface expression. Rescue by these pharmacological chaperones varied directly with their blocking potency. We used structure-activity relationships and site-directed mutagenesis to define the binding site of the pharmacological chaperones. We found that binding occurred in the inner cavity and correlated with hydrophobicity and cationic charge. Rescue was domain-restricted because the trafficking of two misprocessed mutations in the C terminus, HERG F805C and HERG R823W, was not restored by channel blockers. Our findings represent a first step toward the design of pharmacological chaperones that will rescue HERG K(+) channels without block.  (+info)

Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects. - Mechanism of Action & Protocol.
Learn about Hismanal (Astemizole (WITHDRAWN FROM US MARKET)) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
The IUPHAR/BPS Guide to Pharmacology. astemizole ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Astemizole,1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine,1-(p-fluorobenzyl)-2-[[1-(p-methoxyphenethyl)-4-piperidyl]amino]benzimidazole,R-43512,Astemisan,Hismanal,Histamen,Histaminos,Kelp,Laridal,Metodik,Novo-Nastizol A,Paralergin,Retolen,Waruzol
A prolonged QT interval is an important risk factor for ventricular arrhythmias and sudden cardiac death. QT prolongation can be caused by drugs. There are
Vi har undersøgt antihistaminer og fokuseret på deres potentiale som anti-cancer stoffer i kemoresistente brystkræftceller. To brystkræft cellelinjer MDA-MB-231 og MCF-7 samt deres docetaxel-resistente udgaver blev brugt som modelsystem i dette studie. Det blev fundet, at opregulering af MDR1 udover at medføre docetaxel-resistens også gjorde cellerne krydsresistente overfor kemoterapien doxorubicin. Derudover viste vi, at de tre antihistaminer, astemizole, loratadine og ebastine, var i stand til at genskabe følsomheden overfor docetaxel og doxorubicin i resistente MDA-MB-231 celler og i svagere grad i resistente MCF-7 celler. Astemizole, loratadine og ebastine var i stand til at inhibere MDR1 aktivitet i resistente MDA-MB-231 celler i varierende grad, hvilket muligvis spiller en rolle for deres evne til at genskabe følsomheden overfor kemoterapi.. Konklusion og ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
This report is the first to detail the effects of clobutinol, a commonly used antitussive drug, on the HERG cardiac K+ channel. The rhythmic incident correlated to clobutinol in-take in the proband revealed the potential effects of the drug and instigated the present study, which also resulted in the identification of a novel HERG mutation responsible for LQT2.. Drug-Induced Action Potential Prolongation. We found that clobutinol displays an IC50 of ≈2 μM on HERG. As illustrated by computer modeling, clobutinol would induce only mild modifications in the ventricular action potential duration of unaffected individuals. The effects of clobutinol displayed a positive voltage dependence, suggesting that the molecule interacts with an activated state of the HERG channel. Drugs that block HERG current, are often associated with QT prolongation and development of the ventricular arrhythmia known as torsades de pointes. Among them are terfenadine, astemizole, and cisapride. Published IC50 values ...
This invention relates to a process for the preparation of a controlled release pharmaceutical composition comprising two discrete zones wherein the first discrete zone comprises therapeutically effective amount of pseudoephedrine or its pharmaceutically acceptable salt as active ingredient and the second discrete zone comprises a therapeutically effective amount of a long-acting antihistamine selected from the group consisting of loratadine, azatidine, fexofenadine, terfenadine, cetirizine, astemizole, and levocabastine, or their pharmaceutically acceptable salt as active ingredient.
Do not receive this medicine if you are also using astemizole (Hismanal®) or terfenadine (Seldane®). Using these medicines together may cause serious unwanted effects. Check with your doctor right away if you or your child have pain or tenderness in the upper stomach; pale stools; dark urine; loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem. Erythromycin may cause diarrhea, and in some cases it can be severe. It may occur 2 months or more after you stop using this medicine. Do not take any medicine to treat diarrhea without first checking with your doctor. Diarrhea medicines may make the diarrhea worse or make it last longer. If you have any questions about this or if mild diarrhea continues or gets worse, check with your doctor. This medicine can cause changes in heart rhythms, such as a condition called QT prolongation. It may change the way your heart beats and cause fainting or serious side effects in some ...
Some MEDICINES MAY INTERACT with Tofranil . Tell your health care provider if you are taking any other medicines, especially any of the following:. Azole antifungals (eg, fluconazole), cimetidine, duloxetine, flecainide, methylphenidate, mibefradil, phenothiazines (eg, chlorpromazine), propafenone, quinidine, selective serotonin reuptake inhibitors (SSRIs) (eg, fluoxetine), or terbinafine because they may increase the risk of Tofranil s side effects. Arsenic, astemizole, droperidol, furazolidone, MAOIs (eg, phenelzine), pimozide, streptogramins (eg, dalfopristin), terfenadine, or tramadol because the risk of high blood pressure, serious heart problems (eg, irregular heartbeat), or seizures may be increased. Barbiturates (eg, phenobarbital) or phenytoin because they may decrease Tofranil s effectiveness. Anticholinergics (eg, benztropine), carbamazepine, or sympathomimetics (eg, phenylephrine) because the risk of their side effects may be increased by Tofranil. Clonidine, guanethidine, or ...
Here a primary cardiac cell line was examined for its potential use to screen for cardiac metabolism-related liabilities. These ventricular cells are derived from adult humans, which is important considering the interspecies differences in CYP2J activity previously reported (Ma et al., 2004; Yamasaki et al., 2004; Aiba et al., 2006; Elshenawy et al., 2013). Further, much of the drug-induced cardiotoxicity can be attributed to ventricular tissue. The P450 mRNA expression profile was similar to human cardiac ventricular tissue, with CYP2J2 by far the dominant isoform. The ability of the cells to metabolize CYP2J2 substrates astemizole and terfenadine was also established. Various compounds most notably danazol and ketoconazole readily inhibited CYP2J2 activity. However, CYP2J2 mRNA were mostly unchanged in the presence of potential inducers.. Others have shown the dominant presence of CYP2J2 in cardiac tissue, using immunoblotting or quantitative real-time PCR (Wu et al., 1996; Michaud et al., ...
The hERG potassium channel is essential for repolarization of the cardiac action potential. Due to this vital function, absence of unintended and potentially life-threatening interactions with hERG is required for approval of new drugs. The structure of hERG is therefore one of the most sought-after. To provide purified hERG for structural studies and new hERG biomimetic platforms for detection of undesirable interactions, we have developed a hERG expression platform generating unprecedented amounts of purified and functional hERG channels. Full-length hERG, with or without a C-terminally fused green fluorescent protein (GFP) His 8-tag was produced from a codon-optimized hERG cDNA in Saccharomyces cerevisiae. Both constructs complemented the high potassium requirement of a knock-out Saccharomyces cerevisiae strain, indicating correct tetramer assembly in vivo. Functionality was further demonstrated by Astemizole binding to membrane embedded hERG-GFP-His
CONTROL. Documented HIV-1 seronegative, confirmed by ELISA and Western blot.. Male or female, at least 18 years of age.. Laboratory values within established National Institute of Allergy and Infectious Diseases (NIAID) guidelines for participation in clinical studies.. Unremarkable physical exam. Signed written informed consent.. Must not use (or, depending on the agent, must not have used up to the last 28 days) of medications known to inhibit or induce cytochrome P450 during the initial period of the study period (Arm 1: Screening visit to Day 17; Arm 2: Screening visit to Day 15). After this initial period, use of these agents will be permitted on a case-by-case basis as per Investigators clinical judgement; where necessary, additional PK studies may be performed. The prohibited medications include, but are not limited to: isoniazid, rifampin, rifabutin, astemizole, terfenadine, cisapride, cimetidine, triazolam, midazolam, quinidine, nifedipine, diltiazem, verapamil, amiodarone, or ergot ...
|p style=text-align: justify;|Diflucan is used for:|br /|Treating and preventing certain yeast and fungal infections. It may also be used for other conditions as determined by your doctor. Diflucan is an azole antifungal. It kills sensitive fungi by interfering with the formation of the fungal cell membrane.|br /|Do NOT use Diflucan if:|br /|• you are allergic to any ingredient in Diflucan|br /|• you are taking astemizole, an aldosterone blocker (eg, eplerenone), cisapride, an ergot alkaloid (eg, ergotamine), erythromycin, pimozide, a serotonin (5-HT1) receptor agonist (eg, eletriptan), or terfenadine|br /|Contact your doctor or health care provider right away if any of these apply to you.|br /|Before using Diflucan:|br /|Some medical conditions may interact with Diflucan . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:|br /|• if you are pregnant, planning to become pregnant, or are breast-feeding|br /|• if you
You or your child should not use astemizole (Hismanal®), cisapride (Propulsid®), erythromycin (Ery-Tab®), pimozide (Orap®), quinidine (Cardioquin®), or terfenadine (Seldane®) while receiving this medicine because of the risk of unwanted side effects. Using this medicine for a long time or using it too much while you are pregnant (especially during the first trimester) can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using this medicine, tell your doctor right away. This medicine may rarely cause serious liver problems. Check with your doctor right away if you or your child are having more than one of these symptoms: abdominal or stomach pain or tenderness, clay-colored stools, dark urine, decreased appetite, fever, headache, itching, loss of appetite, nausea and vomiting, skin rash, swelling of the feet or lower legs, unusual tiredness or weakness, or yellow eyes or skin. This medicine may rarely ...
It is very important that your doctor check you or your child closely while you are receiving this medicine. This will allow your doctor to see if the medicine is working properly and to check for any unwanted effects. If your or your childs symptoms do not improve within a few weeks, or if they become worse, check with your doctor. Do not receive this medicine if you are also using astemizole (Hismanal®) or terfenadine (Seldane®). Using these medicines together may cause serious unwanted effects. Check with your doctor right away if you or your child have pain or tenderness in the upper stomach; pale stools; dark urine; loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem. Erythromycin may cause diarrhea, and in some cases it can be severe. It may occur 2 months or more after you stop using this medicine. Do not take any medicine to treat diarrhea without first checking with your doctor. Diarrhea medicines may ...
Pimozide, astemizole, and terfenadine are medicines that should never be taken with aprepitant. This eMedTV page lists other medicines that may cause serious drug interactions with aprepitant and explains the possible effects of mixing the medicines.
Anticoagulants (eg, warfarin), aldosterone blockers (eg, spironolactone), alfentanil, arsenic, astemizole, benzodiazepines (eg, alprazolam), bromocriptine, buspirone, carbamazepine, cilostazol, cisapride, clozapine, corticosteroids (eg, hydrocortisone), cyclosporine, digitoxin, digoxin, disopyramide, ergot alkaloids (eg, ergotamine), felodipine, H1 antagonists (eg, diphenhydramine), HMG-CoA reductase inhibitors (eg, lovastatin), imatinib, macrolide immunosuppressants (eg, tacrolimus), meglitinide antidiabetics (eg, repaglinide), midazolam, phosphodiesterase type 5 inhibitors (eg, sildenafil), pimozide, QT-prolonging agents (eg, quinidine, sotalol), quinolones (eg, ciprofloxacin), rifampin, serotonin reuptake inhibitors (eg, fluoxetine), sumatriptan, theophyllines, tricyclic antidepressants (eg, amitriptyline), valproic acid, or vinca alkaloids (eg, vincristine) because the risk of their side effects may increased by Erythromycin ...
Anticoagulants (eg, warfarin), aldosterone blockers (eg, spironolactone), alfentanil, arsenic, astemizole, benzodiazepines (eg, alprazolam), bromocriptine, buspirone, carbamazepine, cilostazol, cisapride, clozapine, corticosteroids (eg, hydrocortisone), cyclosporine, digitoxin, digoxin, disopyramide, ergot alkaloids (eg, ergotamine), felodipine, H1 antagonists (eg, diphenhydramine), HMG-CoA reductase inhibitors (eg, lovastatin), imatinib, macrolide immunosuppressants (eg, tacrolimus), meglitinide antidiabetics (eg, repaglinide), midazolam, phosphodiesterase type 5 inhibitors (eg, sildenafil), pimozide, QT-prolonging agents (eg, quinidine, sotalol), quinolones (eg, ciprofloxacin), rifampin, serotonin reuptake inhibitors (eg, fluoxetine), sumatriptan, theophyllines, tricyclic antidepressants (eg, amitriptyline), valproic acid, or vinca alkaloids (eg, vincristine) because the risk of their side effects may increased by Erythromycin ...
Hi everyone, My fresh IVF cycle failed last month. Today, I got a call from the nurse confirming a new cycle in possibly Aug or Sept. Wondering any of you also plan to have IVF/PET done at this time, if yes, lets share experiences, ideas - page 3
The major finding of these experiments is that terfenadine and astemizole significantly inhibited the IK1 in both guinea pig and rat ventricular myocytes. In the rat myocytes, both drugs also blocked a component of the Ito. Terfenadine, but not astemizole, additionally blocked IK to a small extent. The results of our experiments with terfenadine are consistent with previous studies showing the suppressive effect of terfenadine on the IK in cat and human myocytes.27 28 In cat ventricular myocytes, the IK-associated tail currents on deactivation of the channel were prominent and were markedly suppressed by terfenadine.27 In guinea pig ventricular myocytes, we did not find a similarly large suppression of IK tail current. However, the amplitude of the tail current appears to be somewhat species dependent, ie, quite large in cat, shark, and frog ventricular myocytes and relatively small in human and rodent myocytes.27 28 29 30 31 32 In addition, since deactivation of IK at −40 mV may activate a ...
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially other seizure medications, acetaminophen (Tylenol), astemizole (Hismanal), clarithromycin (Biaxin), danazol (Danocrine), diltiazem (Cardiazem), doxycycline (Vibramycin), erythromycin, haloperidol (Haldol), isoniazid (INH), lithium, medications for colds or allergies such as chlorpheniramine (Chlor-Trimeton), medications for depression such as amitriptyline (Elavil) and fluoxetine (Prozac), oral contraceptives, propoxyphene (Darvon), sedatives such as phenobarbital, terfenadine (Seldane), theophylline (Theo-Dur), verapamil (Calan), and vitamins. Carbamazepine affects the action of other medications, and many medications can affect the action of carbamazepine. Tell your doctor and pharmacist everything you are taking ...
Tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially other seizure medications, acetaminophen (Tylenol), astemizole (Hismanal), clarithromycin (Biaxin), danazol (Danocrine), diltiazem (Cardiazem), doxycycline (Vibramycin), erythromycin, haloperidol (Haldol), isoniazid (INH), lithium, medications for colds or allergies such as chlorpheniramine (Chlor-Trimeton), medications for depression such as amitriptyline (Elavil) and fluoxetine (Prozac), oral contraceptives, propoxyphene (Darvon), sedatives such as phenobarbital, terfenadine (Seldane), theophylline (Theo-Dur), verapamil (Calan), and vitamins. Carbamazepine affects the action of other medications, and many medications can affect the action of carbamazepine. Tell your doctor and pharmacist everything you are taking ...
Aldosterone blockers (eg, eplerenone), amiodarone, astemizole, cisapride, pimozide, serotonin receptor agonists (eg, eletriptan), macrolide antibiotics (eg, erythromycin), quinolines (eg, ciprofloxacin), or terfenadine, Rifabutin, Macrolide immunosuppressants (eg, tacrolimus), Rifampin or proton pump inhibitors (eg, omeprazole), Anticoagulants (eg, warfarin), benzodiazepines (eg, alprazolam), buspirone, carbamazepine, cyclophosphamide, cyclosporine, ergot alkaloids (eg, ergotamine ), haloperidol, HMG-CoA reductase inhibitors or statins (eg, simvastatin), hydantoins (eg, phenytoin), methadone, muscarinic antagonists (eg, solifenacin, tolterodine), narcotics (eg, codeine), ramelteon, sulfonylureas (eg, glipizide), theophylline, or tricyclic antidepressants (eg, amitriptyline ...
It is very important that your doctor check the progress of you or your child at regular visits to make sure this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects. Do not use this medicine if you or your child are also using astemizole (Hismanal®), cisapride (Propulsid®), lovastatin (Mevacor®), pimozide (Orap®), simvastatin (Zocor®), terfenadine (Seldane®), or certain ergot medicines (such as dihydroergotamine, ergotamine, D.H.E. 45®, Ergomar®, Ergostat®, or Migranal®). If you have kidney or liver disease, do not take both this medicine and colchicine (Colcrys®). Using these medicines together may increase risk for more serious side effects. If your or your childs symptoms do not improve within a few days, or if they become worse, check with your doctor. Make sure your doctor knows if you are pregnant or planning to become pregnant. If you become pregnant while using this medicine, tell your doctor right away. Stop using this medicine ...
Parenteral or oral corticosteroids 30 days Nasal corticosteroids 30 days Topical use of flurandrenolide 30 days Topical use of clobetasol propionate 30 days Topical use of halobetasol propionate 30 days Astemizole 30 days Ketotifene 21 days Nedocromil or Sodium cromoglycate 14 days Loratadine 10 days Cetirizine 7 days Antileukotrienes 7 days Other H1 antihistamine 3 days Nasal decongestant 3 days Any food supplements including probiotics 3 days. ...
Antiarrhythmics ▪ Flecainide (Tambocor®) Antiarrhythmics ▪ Amiodarone (Cordarone®) Antibiotics ▪ Rifampin (Rifadin®, Rofact®) Antihistamines ▪ Astemizole (Hismanol®) Antibiotics ▪ Clarithromycin (Biaxin®) Ergot Derivatives ▪ Bellergal Spacetabs® Anticonvulsant ▪ Carbamazepine (Tegretol®) Antifungals ▪ Itraconazole (Sporanox®) GI Mortality Agents ▪ Cisapride (Propulsid®)3 Herbal Products ▪ St. Johns Wort (Hypericum perforatum) Calcium Channel Blockers ▪ Felodipine (Plendil/Renedil®) ▪ Nicardipine (Cardene®)▪ Nifedipine (Adalat®) Corticosteroids ▪ Dexamethasone (Decadron®) Immunosuppressants ▪ Cyclosporine (Neoral®, Sandimmune®) Inhaled Steroids ▪ Fluticasone (Flonase®, Advair®) PDE5 Inhibitors ▪ Sildenafil (Viagra®) ▪ Tadalafil (e.g., Cialis®)▪ Vardenafil (Levitra®) Oral/Patch Contraceptive ▪ Norethindrone Statins ▪ Atorvastatin (Lipitor®) or Rosuvastatin 1 History of hepatitis does not rule out HIV PEP. MD and/or HIV Expert ...
Astemizole - increased risk of arrhythmia; • Indomethacin and other does not exceed 50-60 mg per day. Dermatological reactions: possible (Halotestin) Fluoxymesterone (Halotestin) - is a steroid oral form of application, showing a powerful androgenic and relatively low anabolic activity. If this does not happen often the 15th) ovulation should occur. Although it is worth remembering that often produced precisely in the form of tablets), most prefer the injection enanthate, which is more powerful, evenly acting and does not require frequent administration of the drug. No specific methods of treatment headaches, nervousness, agitation, aggressiveness, increased blood pressure and symptoms from the heart. These effects include the growth and maturation of the prostate gland more potent androgen receptor agonist (activator) than DHT. Useful properties and why it is used in bodybuilding Without going into the anastrozole is an antiestrogenic drug designed to treat common breast cancer in women ...
Antihistamine, any of a group of synthetic drugs that selectively counteract the pharmacological effects of histamine, following its release from certain large cells (mast cells) within the body. Antihistamines replace histamine at one or the other of the two receptor sites at which it becomes
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|p style=text-align: justify;|Drug Uses|br /|Biaxin is used for treating infections caused by certain bacteria.|br /||br /|Do NOT use Biaxin if:|br /|• you are allergic to any ingredient in Biaxin or any other macrolide (eg, erythromycin)|br /|• you are taking cisapride, cyclosporine, dofetilide, eletriptan, ergot alkaloids (eg, ergotamine, dihydroergotamine), H1 antagonists (eg, terfenadine, astemizole), pimozide, QT-prolonging agents (eg, quinidine, sotalol, thioridazine), quinolones (eg, ciprofloxacin), or sumatriptan|br /||br /|Contact your doctor or health care provider right away if any of these apply to you.|br /|Before using Biaxin:|br /|Some medical conditions may interact with Biaxin.|br /||br /|Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:|br /|• if you are pregnant, planning to become pregnant, or are breast-feeding|br /|• if you are taking any prescription or nonprescription medicine, herbal
|p style=text-align: justify;|Drug Uses|br /|Biaxin is used for treating infections caused by certain bacteria.|br /||br /|Do NOT use Biaxin if:|br /|• you are allergic to any ingredient in Biaxin or any other macrolide (eg, erythromycin)|br /|• you are taking cisapride, cyclosporine, dofetilide, eletriptan, ergot alkaloids (eg, ergotamine, dihydroergotamine), H1 antagonists (eg, terfenadine, astemizole), pimozide, QT-prolonging agents (eg, quinidine, sotalol, thioridazine), quinolones (eg, ciprofloxacin), or sumatriptan|br /||br /|Contact your doctor or health care provider right away if any of these apply to you.|br /|Before using Biaxin:|br /|Some medical conditions may interact with Biaxin.|br /||br /|Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:|br /|• if you are pregnant, planning to become pregnant, or are breast-feeding|br /|• if you are taking any prescription or nonprescription medicine, herbal
Cost of clarithromycin Central nervous system: dizziness, confusion, anxiety, insomnia; nightmares. Allergic reactions: rash, anaphylactic reactions; in some cases - Stevens-Johnson syndrome. Other reactions: temporary changes in taste sensations. Contraindications for receiving clarithromycin Cost of clarithromycin severe liver failure, hepatitis (history) Klaritro Sandoz - klaritomitsin. registered in Ukraine porphyria first trimester of pregnancy co-therapy with terfenadine, cisapride, astemizole, pimozide hypersensitivity to clarithromycin and other macrolides The pharmacokinetics of clarithromycin Cost of clarithromycin Clarithromycin is metabolized by enzymes of the cytochrome CYP3A4. The absolute bioavailability of approximately 50%. With multiple dose clarithromycin metabolism character does not change, there is no accumulation. clarithromycin Interaction with other drugs ...
Some medicines may interfere with the absorption of Generic Rulide. These include: theophylline (Neulin, Austyn, Theo-dur), a medicine used to treat asthma some medicines for migraine headache such as ergotamine (Migral, Ergodryl, Cafergot) or dihydroergotamine (Dihydergot tablets) disopyramide (Rythmodan), a medicine to treat irregular heart rhythms terfenadine (Teldane) and astemizole (Hismanal), over the counter medicines used to treat allergies warfarin (Coumadin, Marevan), a medicine used to prevent blood clots digoxin (Lanoxin, Sigmaxin), a medicine used to treat heart failure midazolam (Hypnovel, Midazolam Sandoz), used to induce sleep before operations cyclosporin (Neoral, Cicoral, Cysporin, Sandimmun), a medicine used to prevent organ transplant rejection or to treat certain problems with the immune system · cisapride (Prepulsid), a medicine used to treat gastrointestinal problems · pimozide (Orap), an antipsychotic medicine These medicines may be affected by roxithromycin, or may ...
Now that the cellular infiltrates in both acute and chronic disease are better characterised, there are significant implications for treatment of allergic eye disease (for review see Abelson and Schaefer73).. Topical therapy is the preferred treatment in mild diseases of SAC and PAC. Since neither are life threatening, or even sight threatening, experimental systemic treatments are not indicated in the way they may be in more serious ocular allergic disease such as AKC. Powerful anti-CD4+ T cell agents, such as cyclosporin, should be kept for severely affected cases with keratopathy. In the T cell driven processes of VKC and AKC27 28 specific anti-TH-2 treatment of VKC, rather than blanket anti-T cell therapy, may be a future option.. In SAC and PAC, where mast cells and histamine release are involved in the disease pathogenesis, both topical and systemic therapies have been tried. Oral histamine H1 receptor antagonists (antihistamines) such as astemizole, terfanidine, and loratidine have been ...
Do not take Generic Sporanox if you are allergic to Generic Sporanox components or to itraconazole or similar medications (such as fluconazole (Diflucan) or ketoconazole (Nizoral)).. Do not take Generic Sporanox if you are pregnant, planning to become pregnant, or are breast-feeding.. Do not use Generic Sporanox together with nisoldipine (Sular), simvastatin (Zocor), midazolam (Versed), dofetilide (Tikosyn), ergonovine (Ergotrate), triazolam (Halcion), dihydroergotamine (D.H.E. 45, Migranal), quinidine (Quinaglute, Quinidex, Quin-Release), cisapride (Propulsid), lovastatin (Altocor, Altoprev, Mevacor), ergotamine (Ergomar), methylergonovine (Methergine), pimozide (Orap), astemizole (Hismanal), levomethadyl (Orlaam), antacids or stomach acid reducers (Tagamet, Pepcid, Axid, Zantac) within 1 hour befor or 2 hours after Generic Sporanox usage.. Do not use Generic Sporanox if you have congestive heart failure.. Be careful if you are taking any prescription or nonprescription medicine, herbal ...
Unfortunately, astemizole wens not appear to be generally healthy as it is only in preventing que hace el captopril en el cuerpo sickness (Kohl et al, ) and because it has Phenothiazines, such as prochlorperazine (Compazine) and promethazine (Phenergan), are preferred antiemetics, probably because of your dopamine blocking activity. 1 Tablet (question resolved) - Messed in: vertigo, prochlorperazine - Courante: Prochlorperazine can be used to treat similar, once the cause has been. Do not take this go if you are allergic to valacyclovir or acyclovir. Zovirax (Acyclovir) Bach Information: How Should I Collaborator. Acyclovir use while Being zyrtec d allegra d Resuming m Acyclovir use while Breastfeeding. Acyclovir fins cross into breast milk. El captopril es un inhibidor de la enzima convertidora de angiotensina (IECA) que actúa bloqueando la proteína peptidasa del centro activo de la misma. El captopril mimetiza la forma de los dos últimos restos peptídicos de la angiotensina I, lo que ...
We investigated the involvement of serine protease and proteinase-activated receptor 2 (PAR2) in dermatophyte-induced itch in mice. An intradermal injection of an extract of the dermatophyte Arthroderma vanbreuseghemii (ADV) induced hind-paw scratching, an itch-related behavior. ADV extract-induced scratching was inhibited by the opioid receptor antagonists naloxone and naltrexone, the serine protease inhibitor nafamostat mesylate, and the PAR2 receptor antagonist FSLLRY-NH2. ADV extract-induced scratching was not inhibited by the H1 histamine receptor antagonist terfenadine or by mast cell deficiency. Heat pretreatment of the ADV extract markedly reduced the scratch-inducing and serine protease activities. Proteolytic cleavage within the extracellular N terminus of the PAR2 receptor exposes a sequence that serves as a tethered ligand for the receptor. The ADV extract as well as tryptase and trypsin cleaved a synthetic N-terminal peptide of the PAR2 receptor. The present results suggest that ...
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Like all medicines, this medicine can cause side effects, although not everybody gets them.. If any of the following happen to you, stop taking Cabren and tell a doctor straight away:. • Hypersensitivity and allergic reactions: The signs may include raised lumps on your skin (weals) or swelling of your face, lips, mouth, tongue or throat.. The following undesirable effects have been identified. Most of these reactions appear at start of treatment or after a dose increase. Should such reactions occur, they are usually brief and diminish in intensity with time. If you experience any of the following symptoms and they persist, please tell your doctor.. Mild enlargement of the gums has been reported in patients with an inflammation in the mouth (gingivitis/periodontitis). The enlargement can be avoided or reversed by careful oral hygiene.. Very common: may affect more than 1 in 10 people. • Ankle swelling. Common: may affect up to 1 in 10 people. • Headache. • Flushing. Uncommon: may affect ...
Chlorcyclizine antihistamine drug molecule. Used in treatment of allergy, urticaria, rhinitis and pruritus and possibly also to treat hepatitis C. Atoms are represented as spheres with conventional colour coding: hydrogen (white), carbon (grey), chlorine (green), nitrogen (blue). - Stock Image F012/9892
Large complex polygons were generated by shortening effect ascribing the differences in APDs with numerous points lying distant from the identity type of the Poincar plot. Moreover, while 0. 01 and 0. 1 mM terfenadine did not somewhat increase STV during 0. 5 Hz, higher levels induced a decrease that became significant at 10 mM. Additionally, throughout the transition towards the steady state reduction in APD in Ivacaftor solubility LVMMs, terfenadine induced a marked upsurge in temporal BVR at 1 Hz. Figure 2A shows that before the shortening effect of 1 mM terfenadine, the progression towards the plateau phase of the AP, although not APD, was affected. Even though between 198 and records 170, the best shift of the development phase became more pronounced, and the plateau phase was depressed, APD wasnt afflicted, and terfenadine caused the loss in AP dome. During the transition to the steady-state decline in APD, large variations in effective APDs were seen. Four out-of 10 myocytes showed this ...
Coformulated lopinavir/ritonavir has the potential to interact with wide variety of drugs via several mechanisms, mostly involving the CYP enzymes. Coadministration of lopinavir/ritonavir is contraindicated with certain drugs (i.e. flecainide, propafenone, astemizole, terfenadine, ergot derivatives, …
best methods of treatment of allergic rhinitis, that is the most usual, is the usage of classic antihistaminic drugs [such asChlorpheniramine], but their side effects, specially somnolence and malaise, made a few patients to discontinue such treatment. More than a decade has showed that the Non Sedating Anti Histaminic Drugs [Terfenadin, Astemizole andLoratadine] are free from these side effects and do not show the CNS and anticholinergic disorders. The evaluation of their efficacy in the epidemiology of IRAN, beside the comparison of generic products with the registrated ones, is the main goal of this research. In this clinical study, the efficacy and adverse reactions of the Loratadine and its registratedproduct called Claritin are compared with Chlorpheniramine on 90 patients. It has been performed in northeast IRANand the study is a kind of double blind, prospective studies.30 patients have received Chlorpheniramine, as the same for Loratadine and Claritin. Then the results are compared with ...
In the United States, Seldane was brought to market in 1985 as the first nonsedating antihistamine for the treatment of allergic rhinitis.[1][4] In June 1990, evidence of serious ventricular arrhythmias among those taking Seldane prompted the FDA to issue a report on the risk factors associated with concomitant use of the drug with macrolide antibiotics and ketoconazole.[1] Two months later, the FDA required the manufacturer to send a letter to all physicians, alerting them to the problem; in July 1992, the existing precautions were elevated to a black box warning[1] and the issue attracted mass media attention in reports that people with liver disease or who took ketoconazole, an antifungal agent, or the antibiotic erythromycin, could suffer cardiac arrhythmia if they also took Seldane.[4] In January 1997, the same month when the U.S. Food and Drug Administration (FDA) had earlier approved a generic version of Seldane made by IVAX Corporation of Miami, the FDA recommended terfenadine-containing ...
Compositions containing both a sedative compound and a non-sedative antihistamine are provided. More particularly, compositions for administration at bedtime containing a sedating antihistamine or oth
Clarinex is new - but is it really better at battling allergy symptoms than its popular predecessor drug, Claritin? Some experts contend their makers real aim in introducing Clarinex with a flood of ads and discounts is to capture customers before Claritins patent expires - and cheaper knockoffs muscle in.. Its a strategy that makers of other drugs, faced with looming competition from generic and over-the-counter versions, have used effectively.. And in a time of rising drug expenses, some doctors and pharmacists say its a strategy we cant afford.. You may have seen those strange new television ads for Clarinex, Schering-Ploughs chip-off-the-old-blockbuster replacement for its nonsedating antihistamine pill, Claritin:. An enormous Clarinex pill hurtles toward Earth, a meteor of relief. Cut to Clarinex particles capping histamine receptors in a digitized blood vessel. A voice tells us the drug is the only allergy pill that delivers 24-hour relief from any allergy, anywhere, at any ...
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Benadryl is a popular allergy medicine that is also often used as a sleep aid. This eMedTV Web page outlines the benefits of Benadryl and explains what side effects may occur with this antihistamine drug. Benidril is a common misspelling of Benadryl.
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Cardiology Today | In recent years, reports of increased risk for cardiac events associated with use of some antibiotics have been under the spotlight. Widely used antibiotics such as azithromycin have been linked to risk for mortality and others have been linked to pronounced effects on QT interval prolongation. Growing attention on the link led the FDA to issue public health advisories cautioning physicians and
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Wood SF (January 1986). "Astemizole and terfenadine compared in hay fever". The Practitioner. 230 (1411): 41-4. doi:10.1161/ ...
"Treatment of aquagenic urticaria with PUVA and astemizole". Journal of the American Academy of Dermatology. 36 (1): 118-9. doi: ...
Small P, Barrett D, Biskin N (February 1990). "Effects of azatadine, terfenadine, and astemizole on allergen-induced nasal ...
Other reported treatments include PUVA, UVA/UVB phototherapy, astemizole, acitretin, and etretinate. When appears with sun/ ...
... astemizole". Drug Metabolism and Disposition. 30 (11): 1240-5. doi:10.1124/dmd.30.11.1240. PMID 12386130. Marden NY, Fiala-Beer ...
Astemizole, a medication approved for human use, has been found to have anti-prion activity and may lead to a treatment for ... "Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents". Proceedings of the ...
"Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ...
In some cases, this can lead to a fatal interaction with drugs like astemizole or terfenadine. The effect of grapefruit juice ... "Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with ...
Rojo LE, Alzate-Morales J, Saavedra IN, Davies P, Maccioni RB (2010). "Selective interaction of lansoprazole and astemizole ... Astemizole (AST) and Lansoprazole (LNS) interact with anomalous aggregates of tau protein (neurofibrillary tangles). Current ...
astemizole. Chemistry[edit]. It is a racemic 1:1 mixture of the enantiomers dexlansoprazole and levolansoprazole.[17] ...
Other examples include terfenadine (Seldane, Seldane-D), astemizole (Hismanal), cisapride (Propulsid, withdrawn in many ...
The United States government removed two second generation antihistamines, terfenadine and astemizole, from the market based on ...
The Ezh1/2 inhibitors GSK126, GSK343, and UNC1999 as well as astemizole, which interferes with Ezh1/2 association in PRC, were ...
... the antihistamines astemizole and terfenadine, and some antipsychotics may increase the chance of ventricular dysrhythmias. ...
... with an affinity comparable to that of astemizole and diphenhydramine, and superior than that of cetirizine by three-fold and ...
... astemizole, terfenadine, ergotamine, ticagrelor, ranolazine or dihydroergotamine is not recommended. It should not be used with ...
Monoclonal antibody Nonsteroidal anti-inflammatory drug List of antiviral drugs Virucide Antiprion drugs and Astemizole ...
... astemizole MeSH D03.438.103.140 - benomyl MeSH D03.438.103.145 - bisbenzimide MeSH D03.438.103.190 - cambendazole MeSH D03.438. ...
... astemizole, midazolam, triazolam, ergot medications, and several medications for acid reflux. The most common adverse event is ...
... such as astemizole, have this effect. The mechanism of action of certain antiarrhythmic drugs, like amiodarone or sotalol, ...
... astemizole, bepridil, IV erythromycin, halofantrine, pentamidine, sultopride, terfenadine, and vincamine). Symptoms of over ...
Alverine Amiodarone Amitriptyline Amlodipine Aprindine Astemizole AY-9944 Benzatropine Bepridil Biperiden Camylofin Carvedilol ...
Astelin astemizole (INN) Astramorph PF astromicin (INN) astuprotimut-R (USAN) asunaprevir (USAN, INN) Atabrine (Abbott) Atacand ...
R06AX04 Phenindamine R06AX05 Antazoline R06AX07 Triprolidine R06AX08 Pyrrobutamine R06AX09 Azatadine R06AX11 Astemizole R06AX12 ...
Examples - Systemic: Astemizole (Hismanal) Ketotifen (Zaditor) Cetirizine (Zyrtec) Loratadine (Claritin) Rupatadine (Rupafin) ...
astemizole (en) , Azitromizina, bepridil (en) , klorokina, chlorpromazine (en) , cisapride (en) , (RS)-citalopram (en) , ...
... may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed] Astemizole does also act ... Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly ... Astemizole was discovered by Janssen Pharmaceutica in 1977. It was withdrawn from the market globally in 1999 because of rare ... Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that ...
... is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
... (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.[1] A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment.[1] In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus.[2] This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus.[2] ...
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed] Astemizole does also act ... Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly ... Astemizole was discovered by Janssen Pharmaceutica in 1977. It was withdrawn from the market globally in 1999 because of rare ... Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that ...
A Moderate Drug Interaction exists between astemizole and Pepto Diarrhea Control. View detailed information regarding this drug ... Astemizole is no longer on the market in the US. Do not take astemizole with any other medication, food, or beverage. ... Drug Interactions between astemizole and Pepto Diarrhea Control. This report displays the potential drug interactions for the ... and the risk may be increased when combined with other medications that can also cause cardiac problems such as astemizole. You ...
Astemizole (WITHDRAWN FROM US MARKET)) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, ... TABLE 1 - Astemizole, Adverse Reactions Percent of Patients Reporting Controlled Studies*. Adverse Event. Astemizole. Placebo. ... DATA SUGGEST THAT THESE EVENTS ARE ASSOCIATED WITH ELEVATION OF ASTEMIZOLE AND/ OR ASTEMIZOLE METABOLITE LEVELS, RESULTING IN ... Astemizole does not appear to be dialyzable.. Oral LD50 values for Astemizole were 2052 mg/kg in mice and 3154 mg/kg in rats. ...
BioAssay record AID 625171 submitted by ChEMBL: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole).
Astemizole Synergizes Calcitriol Antiproliferative Activity by Inhibiting CYP24A1 and Upregulating VDR: A Novel Approach for ... Astemizole Synergizes Calcitriol Antiproliferative Activity by Inhibiting CYP24A1 and Upregulating VDR: A Novel Approach for ... Astemizole Synergizes Calcitriol Antiproliferative Activity by Inhibiting CYP24A1 and Upregulating VDR: A Novel Approach for ... Astemizole Synergizes Calcitriol Antiproliferative Activity by Inhibiting CYP24A1 and Upregulating VDR: A Novel Approach for ...
astemizole ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ...
Astemizole eliminated or decreased total IK when measured at Vt≤0 mV (C). At Vt≥0 mV, astemizole had no consistent effect on ... Astemizole also blocked IKtail almost completely at Vt≤0 mV, but there was no further appreciable block of IKtail at Vt,0 mV (D ... Fig 4⇓ shows the effects of astemizole (0.1 μmol/L) on the I-V relations for the time-dependent IK (C) and repolarizing tail ... Both astemizole and terfenadine inhibited IKr potently (IC50, 1.5 and 50 nmol/L; Hill coefficient, 0.99 and 0.93, respectively ...
... astemizole rather than astemizole alone, and at the same time this preference was confirmed by physician (p = 0.011) and ... astemizole (n = 146) or placebo nasal spray + astemizole (n = 148) or double-dummy (nasal spray + capsules) placebo (n = 71). ... The specific question was, Will the addition of nedocromil sodium 1% nasal spray to astemizole tablets improve control of ... in the astemizole group. Clinical assessments of rhinitis made during the peak pollen visit, after the first week of test ...
The assays and kits are based on the finding that the interaction of astemizole with the HERG (Human Ether-a-go-go-Related Gene ... Figure 1 A shows the saturation binding of [3H]-astemizole to cell membrane preparations of HEK293 cells stably transfected ... astemizole. herg. interaction. related gene. Prior art date. 2001-07-13. Application number. NZ52949602A. Inventor. Godelieve ... The assays and kits are based on the finding that the interaction of astemizole with the HERG (Human Ether-a-go-go-Related Gene ...
... ,1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine,1-(p-fluorobenzyl ...
Astemizole may also act on H3-receptors, producing adverse effects. 10597866. 19110341. 10422790. 12190308. 15272206. 11752352 ... Astemizole competes with histamine for binding at H,sub,1,/sub,-receptor sites in the GI tract, uterus, large blood vessels, ... Astemizole competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial ... Uses/Sources: Astemizole tablets are indicated for the relief of symptoms associated with seasonal allergic rhinitis and ...
Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects. - ... Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a ... Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2 ... Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects. ...
Astemizole. Concomitant administration of fluconazole with astemizole may decrease the clearance of astemizole. Resulting ... To avoid a possible serious reaction, do NOT take DIFLUCAN if you are taking erythromycin, astemizole, pimozide, quinidine, and ... Astemizole. Rifabutin. Voriconazole. Tacrolimus. Short-acting benzodiazepines. Tofacitinib. Triazolam. Oral Contraceptives. ... astemizole, erythromycin, pimozide, and quinidine are contraindicated in patients receiving fluconazole. (See CLINICAL ...
Astemizole Astemizole is an antihistamine, prescribed for allergic rhinitis and chronic idiopathic urticaria. ...
astemizole. Chemistry[edit]. It is a racemic 1:1 mixture of the enantiomers dexlansoprazole and levolansoprazole.[17] ...
Astemizole, BP A3456 , 68844-77-9 , C28H31FN4O , Spectrum Chemical Astemizole, BP was withdrawn from the U.S. market in 1999. ... Astemizole is an antihistamine used to preventsneezing, runny nose, itching and watering of the eyes, and otherallergicsymptoms ...
HISMANAL (Astemizole) --LIBRAX --DIFLUCAN (Fluconazole) --POTABA (Aminobenzoate Potassium) --GUAIFENESIN --QUOTANE --IMITREX( ...
Astemizole at 30 mg/kg (p.o.) and at 1 to 3 mg/kg (i.v.), prolonged QT interval and induced ventricular extrasystole. Torsades ... Effects of terfenadine, astemizole and epinastine on electrocardiogram in conscious cynomolgus monkeys. (opens in new tab) ... Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine. The Journal of ... Torsades de pointes ventricular tachycardia associated with overdose of astemizole. (opens in new tab) ...
Hismanal (Astemizole). HISMANAL® Johnson & Johnson Merck Astemizole Histamine H1-Antagonist Action And Clinical Pharmacology: ... Astemizole is a potent, long-acting, and selective histamine H1-antagonist. It produces a dose-related… ...
De tekst is beschikbaar onder de licentie Creative Commons Naamsvermelding-Gelijk delen. Er kunnen aanvullende voorwaarden van toepassing zijn. Zie de Gebruiksvoorwaarden voor meer informatie ...
Detailed drug Information for Clozaril. Includes common brand names, drug descriptions, warnings, side effects and dosing information.
Astemizole. *Concurrent topical antifungal agents for superficial fungal infections allowed. Sex/Gender ICMJE Sexes Eligible ...
Astemizole. Cisapride. Triazolam. Midazolam. Ergotamine/Dihydroergotamine-containing regimens. Antiretroviral drugs. Vitamin E ...
Astemizole.. Patients with the following prior conditions are excluded:. *History of hypersensitivity to imidazole or azole ...
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.. Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.. ...
This medicine may affect blood sugar levels. If you are diabetic and notice a change in the results of your blood or urine sugar tests, check with your doctor. This medicine may add to the effects of alcohol and other medicines that make you drowsy or less alert. Some examples of these medicines are antihistamines or medicines for hay fever, allergies, or colds, sedatives, tranquilizers, or sleeping medicines, prescription pain medicines or narcotics, medicines for seizures or barbiturates, muscle relaxants, or anesthetics (medicines that numb), including some dental anesthetics. If you are taking any of these medicines, make sure you tell your doctor before you receive aripiprazole injection. Aripiprazole may cause drowsiness, trouble with thinking, or trouble with controlling movements. Make sure you know how you react to this medicine before you drive, use machines, or do other jobs that require you to be alert, well-coordinated, or able to think well. Check with your doctor right away if you ...
... astemizole, levocetirizine, rupatadine, mizolastin, noberastine and mequitazine. Cetirizine, in spite of being a second ... astemizole, norastemizole, desmethylastemizole, cetirizine, acrivastine, and temelastine, or a pharmaceutically acceptable salt ...
astemizole. *bepridil. *bosentan. *cisapride. *colchicine (in people with kidney or liver problems) ...
Oxis turbohaler contains the bronchodilator formoterol, it is used on a regular basis in asthma and COPD to keep your airways open, information about using this formoterol inhaler
  • EMEND should not be used concurrently with pimozide, terfenadine, astemizole, or cisapride since inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions. (nih.gov)
  • Concomitant administration of clarithromycin and any of the following drugs is contraindicated: astemizole, cisapride, domperidone, pimozide and terfenadine as this may result in QT prolongation and cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation, and torsades de pointes (see section 4.4 and 4.5). (medicines.org.uk)
  • Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action. (wikipedia.org)
  • Terfenadine (Seldane) and astemizole (Hismanal), a second generation of H 1 receptor antagonists, are two widely used nonsedating antihistamines that differ pharmacologically from first-generation antihistamines by having preferential affinity for the peripheral H 1 receptors versus the brain H 1 and cholinergic receptors. (ahajournals.org)
  • Concomitant terfenadine (Seldane or Seldane-D) or astemizole (Hismanal). (nih.gov)
  • wherein the second discrete zone comprises an effective amount of a long-acting antihistamine selected from the group consisting of loratadine, azatadine, fexofenadine, terfenadine, cetirizine, astemizole, and levocabastine or their pharmaceutically acceptable salt with at least one pharmaceutically acceptable excipient. (google.com)
  • With allergy drugs such as astemizole, how about claritin (loratadine)? (healthtap.com)
  • With allergy drugs such as astemizole can I take claritin (loratadine)? (healthtap.com)
  • Background Terfenadine and astemizole are widely prescribed nonsedating antihistamines that have been associated with QT-interval prolongation and ventricular arrhythmias. (ahajournals.org)
  • To determine the cellular electrophysiological basis for the proarrhythmic effects of these drugs, this study was designed to investigate the actions of two H 1 receptor antagonists, terfenadine and astemizole, on various potassium (K + ) channels of cardiac myocytes. (ahajournals.org)
  • Astemizole also shows potent hERG K + channel blocking activity with an IC 50 of 0.9 nM. (medchemexpress.com)
  • Astemizole is a histamine H1-receptor antagonist. (wikipedia.org)
  • Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. (wikipedia.org)
  • Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC 50 of 4 nM. (medchemexpress.com)
  • Using excessive doses of loperamide can cause serious and potentially fatal complications such as irregular heart rhythm and cardiac arrest, and the risk may be increased when combined with other medications that can also cause cardiac problems such as astemizole. (drugs.com)
  • Cardiac arrhythmias were initially reported in patients who intentionally or accidentally ingested overdoses of either astemizole 4 5 6 7 8 9 10 11 or terfenadine. (ahajournals.org)
  • Arrhythmias after astemizole overdose. (biomedsearch.com)
  • Astemizole may also act on histamine H3 receptors, thereby producing adverse effects. (wikipedia.org)
  • We studied the effects of astemizole (antihistamine) and nicardipine (Ca2+ channel blocker) on cardiovascular parameters. (meta.org)
  • Both astemizole and terfenadine suppressed the I K1 channel by 17% to 50% in a voltage-dependent manner in rat and guinea pig myocytes. (ahajournals.org)
  • Terfenadine but not astemizole slightly inhibited I K , by 9%, and only at higher drug concentrations. (ahajournals.org)
  • Astemizole is no longer on the market in the US. (drugs.com)
  • Astemizole is off the market as it caused arrythmias (irregular heart beats). (healthtap.com)
  • Terfenadine, astemizole or mizolastine (drugs found in hayfever or anti-his-tamine products). (chemist2customer.com)
  • Nevertheless, the manufacturers of both astemizole and terfenadine contraindicate the concurrent use of SSRIs . (medpill.info)
  • Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. (pharmacycode.com)