Histamine H1 Antagonists, Non-Sedating
Histamine H1 Antagonists
Rhinitis, Allergic, Perennial
Receptors, Histamine H1
Rhinitis, Allergic, Seasonal
Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs. (1/98)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)
Histamine response and local cooling in the human skin: involvement of H1- and H2-receptors. (2/98)AIMS: Histamine may contribute locally to cutaneous blood flow control under normal and pathologic conditions. The objective of this study was to observe the influence of skin temperature on histamine vasodilation, and the roles of H1-and H2-receptors using novel noninvasive methods. METHODS: Eleven healthy subjects received, double-blind, single doses of the H1-receptor antagonist cetirizine (10 mg), cetirizine (10 mg) plus the H2-receptor antagonist cimetidine (400 mg), or placebo on separate occasions. Histamine was dosed cumulatively by iontophoresis to the forearm skin at 34 degrees C and 14 degrees C. Laser-Doppler flux (LDF) was measured at the same sites using customised probeholder/iontophoretic chambers with Peltier cooling elements. Finger mean arterial pressure (MAP) was measured and cutaneous vascular conductance calculated as LDF/MAP. RESULTS: Histamine vasodilation was reduced in cold skin. Cetirizine shifted the histamine dose-response at both temperatures: statistically significantly at 14 degrees C only. Combined H1- and H2-receptor antagonism shifted the response significantly at both temperatures. CONCLUSIONS: H1- and H2-receptors mediate histamine-induced skin vasodilation. The sensitivity of these receptors, particularly the H1- receptor, is attenuated at low skin temperature. Whether the reduced effect in cold skin represents specific receptor or postreceptor desensitization, or nonspecific attenuation of cutaneous vasodilation remains to be elucidated. (+info)
Mutational analysis of the antagonist-binding site of the histamine H(1) receptor. (3/98)We combined in a previously derived three-dimensional model of the histamine H(1) receptor (Ter Laak, A. M., Timmerman, H., Leurs, H., Nederkoorn, P. H. J., Smit, M. J., and Donne-Op den Kelder, G. M. (1995) J. Comp. Aid. Mol. Design. 9, 319-330) a pharmacophore for the H(1) antagonist binding site (Ter Laak, A. M., Venhorst, J., Timmerman, H., and Donne-Op de Kelder, G. M. (1994) J. Med. Chem. 38, 3351-3360) with the known interacting amino acid residue Asp(116) (in transmembrane domain III) of the H(1) receptor and verified the predicted receptor-ligand interactions by site-directed mutagenesis. This resulted in the identification of the aromatic amino acids Trp(167), Phe(433), and Phe(436) in transmembrane domains IV and VI of the H(1) receptor as probable interaction points for the trans-aromatic ring of the H(1) antagonists. Subsequently, a specific interaction of carboxylate moieties of two therapeutically important, zwitterionic H(1) antagonists with Lys(200) in transmembrane domain V was predicted. A Lys(200) --> Ala mutation results in a 50- (acrivastine) to 8-fold (d-cetirizine) loss of affinity of these zwitterionic antagonists. In contrast, the affinities of structural analogs of acrivastine and cetirizine lacking the carboxylate group, triprolidine and meclozine, respectively, are unaffected by the Lys(200) --> Ala mutation. These data strongly suggest that Lys(200), unique for the H(1) receptor, acts as a specific anchor point for these "second generation" H(1) antagonists. (+info)
Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice. (4/98)OBJECTIVES: To investigate the frequency with which sedation was reported in post-marketing surveillance studies of four second generation antihistamines: loratadine, cetirizine, fexofenadine, and acrivastine. DESIGN: Prescription-event monitoring studies. SETTING: Prescriptions were obtained for each cohort in the immediate post-marketing period. SUBJECTS: Event data were obtained for a total of 43 363 patients. MAIN OUTCOME MEASURES: Reporting of sedation or drowsiness. RESULTS: The odds ratios (adjusted for age and sex) for the incidence of sedation were 0.63 (95% confidence interval 0.36 to 1.11; P=0.1) for fexofenadine; 2.79 (1.69 to 4.58; P<0.0001) for acrivastine, and 3.53 (2.07 to 5.42; P<0.0001) for cetirizine compared with loratadine. No increased risk of accident or injury was evident with any of the four drugs. CONCLUSIONS: Although the risk of sedation was low with all four drugs, fexofenadine and loratadine may be more appropriate for people working in safety critical jobs. (+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. (5/98)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)
Determination of cetirizine dichloride in tablets by HPLC method. (6/98)A HPLC method for the determination of the cetirizine dichloride in tablets was developed and validated. The determination was performed with a LiChrosorb RP-18 column, mobile phase of KH2PO4 (0.01 mol/l)--acetonitrile 65:35 (v/v), flow rate: 2 ml.min-1, UV detection at 230 nm and methyl paraben as an internal standard. (+info)
Stability of cetirizine dihydrochloride in solid state. (7/98)Influence of temperature and relative humidity on stability of cetirizine dihydrochloride in solid state was followed by HPLC method in this study. (+info)
A descriptive analysis of the use and cost of new-generation antihistamines in the treatment of allergic rhinitis: a retrospective database analysis. (8/98)OBJECTIVE: This retrospective database analysis was conducted to evaluate the use and cost of new-generation antihistamines (i.e., those that are nonsedating) in the treatment of allergic rhinitis in a managed care population. STUDY DESIGN: The study is a retrospective database review of medical and pharmacy-related claims linked by episodes of care. METHODS: Patients who had been diagnosed as having allergic rhinitis and had at least 1 prescription claim were identified from a database containing patient-level medical and pharmacy-related claims. The treatment patterns of patients with allergic rhinitis who met the study criteria were documented for a 12-month period in which the use of nonsedating antihistamines was described and the associated costs of various medications were assessed. Subanalyses of patients categorized by comorbidity status were also performed. RESULTS: A total of 202,426 patients participated in the study. Nonsedating antihistamines were used by 71% of the patients; the most commonly prescribed drugs were loratadine and fexofenadine. The mean annual charges per patient for the treatment of allergic rhinitis in the study population were $465.21 (standard deviation [SD], 548). The greatest departmental cost was that of pharmacy-related charges (mean, $236.02; SD, 233); the next highest cost was that of outpatient charges (mean, $216.31; SD, 396). Comparisons of departmental charges indicated the use of loratadine was associated with significantly higher treatment costs than that of fexofenadine in a number of patient subgroups. CONCLUSION: In this analysis, loratadine was associated with significantly higher treatment charges than was fexofenadine. This result was observed consistently across different stratifications of patients, including the presence of comorbid respiratory infection, concomitant use of nasal steroids, and the presence of asthma and/or sinusitis. These results provided useful insights into the differential costs associated with the use of nonsedating antihistamines in the treatment of rhinitis. (+info)
Perennial allergic rhinitis can be caused by a variety of allergens, including:
1. Dust mites: These tiny organisms live in bedding, carpets, and upholstered furniture and feed on human skin cells. Their waste products are the primary allergen that triggers an allergic reaction.
2. Mold: This type of fungus grows in damp environments and can be found in basements, bathrooms, and outdoors.
3. Pet dander: The dead skin flakes from animals such as cats, dogs, and birds can trigger an allergic reaction in some people.
4. Insect bites: Some people may experience an allergic reaction to the saliva or venom of certain insects such as bees, wasps, or hornets.
5. Food: Certain foods such as milk, eggs, wheat, and nuts can cause an allergic reaction in some people.
The symptoms of perennial allergic rhinitis are similar to those of seasonal allergic rhinitis, but they occur throughout the year rather than just during a specific season. Treatment options for perennial allergic rhinitis include over-the-counter or prescription medications such as antihistamines, decongestants, and corticosteroids, as well as immunotherapy, which involves exposing the body to small amounts of the allergen over time to build up tolerance.
The symptoms of urticaria can vary in severity and may include:
* Appearance of hives or wheals on the skin, often in a patterned or widespread distribution
* Itching or burning sensations on the skin
* Redness, swelling, or warmth of the affected area
* In some cases, angioedema (swelling of the deeper layers of skin)
Urticaria can be caused by a variety of factors, including:
* Allergies to foods, drugs, or insect bites
* Exposure to environmental allergens such as pollen, dust mites, or animal dander
* Infections, such as colds or flu
* Physical stimuli, such as pressure, cold, or heat
* Certain medications, such as antibiotics or nonsteroidal anti-inflammatory drugs (NSAIDs)
* Hormonal changes, such as those that occur during pregnancy or menstruation
Urticaria can be diagnosed through a physical examination and medical history, and may require further testing to determine the underlying cause. Treatment for urticaria typically involves avoiding triggers, using antihistamines or corticosteroids to reduce symptoms, and addressing any underlying conditions that may be contributing to the condition. In severe cases, hospitalization may be necessary to manage the symptoms and prevent complications.
Symptoms of seasonal allergic rhinitis typically begin soon after exposure to the allergen and may last for several days or weeks. In addition to nasal congestion and discharge, other common symptoms include:
* Itchy eyes and throat
* Sneezing and coughing
* Headaches and facial pain
* Fatigue and general malaise
* Loss of sense of smell (hyposmia)
Seasonal allergic rhinitis is most commonly caused by exposure to airborne pollens from trees, grasses, and weeds. Treatment typically involves avoiding exposure to the allergen, medications such as antihistamines or decongestants, and immunotherapy (allergy shots) in severe cases.
The symptoms of seasonal allergic rhinitis can be managed with over-the-counter or prescription medications, and home remedies like saline nasal sprays, humidifiers, and steam inhalers. In addition to these treatments, avoiding exposure to the allergen and taking steps to reduce nasal congestion can also help alleviate symptoms.
Previous Post What is the definition of 'Rhinitis' in the medical field? Next Post What are the common symptoms of seasonal allergic rhinitis?
There are several triggers that can cause sneezing, including:
1. Allergens: Allergic reactions to pollen, dust mites, mold and other substances can cause sneezing.
2. Cold and flu viruses: These viruses can cause inflammation in the nasal passages and sinuses, leading to sneezing.
3. Sinus infections: Bacterial or fungal infections of the sinuses can cause sneezing.
4. Irritants: Exposure to irritants such as smoke, dust, and strong odors can cause sneezing.
5. Hormonal changes: Changes in hormone levels during pregnancy or menstruation can lead to increased nasal secretions and sneezing.
Sneezing can be treated with over-the-counter medications such as antihistamines, decongestants, and saline nasal sprays. If the sneezing is persistent or accompanied by other symptoms such as a fever, facial pain or swelling, it is important to see a healthcare professional for proper diagnosis and treatment.
In some cases, sneezing can be a sign of a more serious condition such as a sinus infection, meningitis or encephalitis. If you experience any of the following symptoms along with sneezing, seek medical attention immediately:
1. Severe headache
2. Fever over 101°F (38.3°C)
3. Facial pain or swelling
4. Difficulty breathing or swallowing
5. Nasal discharge that is thick and yellow or greenish in color
6. Seizures or convulsions
7. Change in mental status or confusion
In summary, sneezing during pregnancy can be caused by a variety of factors, including hormonal changes, allergies, and respiratory infections. If you experience persistent or severe sneezing during pregnancy, it is important to see a healthcare professional for proper diagnosis and treatment. Additionally, if you experience any other symptoms along with sneezing, seek medical attention immediately as these could be signs of a more serious condition.
* Nasal polyps: Growths in the nasal passages that can block airflow.
* Deviated septum: A crooked partition between the two sides of the nasal passages that can narrow or block one side.
* Enlarged adenoids or turbinate bones: These structures can grow and obstruct the airway.
* Trauma to the nose: A broken nose or other injury can cause obstruction of the nasal passages.
* Infections such as rhinitis, sinusitis, or allergies: Swelling and congestion in the nasal passages can cause obstruction.
* Nasal tumors: Growths in the nasal passages that can block airflow.
* Anatomical abnormalities: Some people may be born with abnormalities such as a narrow nasal passage or a deviated septum, which can cause nasal obstruction.
Symptoms of Nasal Obstruction include:
* Difficulty breathing through the nose
* Congestion or stuffiness in the nose
* Noise or snoring while breathing
* Sleep disturbances due to difficulty breathing
* Headaches or facial pain due to straining to breathe
* Postnasal drip (a sensation of mucus running down the back of the throat)
* Coughing or sneezing
Treatment for Nasal Obstruction depends on the underlying cause and can include:
* Medications such as nasal decongestants, antihistamines, and steroids to reduce swelling and congestion.
* Nasal strips or dilators to open up the nasal passages.
* Saline nasal irrigation to flush out mucus and debris.
* Surgery to remove nasal polyps, correct a deviated septum, or other structural abnormalities.
* Allergy treatment to reduce inflammation and congestion.
It is important to seek medical attention if you experience persistent or severe symptoms of nasal obstruction as it can lead to complications such as sinus infections, sleep disorders, and other health problems. A healthcare professional can diagnose the underlying cause and recommend appropriate treatment options.
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Histamine H1 recep3
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Effect of cetirizine3
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- To describe a case of recurrent acute hepatitis related to the use of cetirizine, a selective histamine(1)-receptor antagonist approved for the treatment of common allergic diseases. (nih.gov)
- Cetirizine is an allergy medication that you can buy over the counter (OTC) at a pharmacy. (healthline.com)
- You may receive cetirizine injection in a hospital or you may administer the medication at home. (medlineplus.gov)
- If you will be using cetirizine injection at home, your healthcare provider will show you how to use the medication. (medlineplus.gov)
- Cetirizine was approved for use by prescription in the United States in 1995 and as an over-the-counter medication in 2007. (nih.gov)
- Immunoallergic and autoimmune features were rare, but recurrence of acute liver injury upon reexposure to cetirizine has been described. (nih.gov)
- The cause of acute liver injury from cetirizine is not known. (nih.gov)
- The patient had suffered 2 previous episodes of "acute hepatitis of unknown origin," and both had occurred after cetirizine use. (nih.gov)
- Use of the Naranjo probability scale indicated cetirizine as the probable cause of acute hepatitis, and the positivity for liver-kidney microsome antibodies is suggestive of an autoimmune mechanism for liver damage. (nih.gov)
- As of September 13, 2004, ours is the fourth reported case of acute hepatitis associated with cetirizine and the second in which liver-kidney microsome antibodies have been documented. (nih.gov)
- Cetirizine forms a complex with histamine for H 1 -receptor sites in blood vessels, the gastrointestinal (GI) tract, and the respiratory tract. (medscape.com)
- This is, in Piriteyxl-BR, the "chicken and the egg question" - which came first, the receptor or the cetirizine indikasi ligand. (granodesal.com)
- Generally, cetirizine is a safe and effective drug, but you should be aware of certain warnings and precautions when taking this drug. (healthline.com)
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- On this date, the us food and drug administration received new information regarding this drug and it will be communicated tab cetirizine 10 mg price in a subsequent letter. (dewysparkle.com)
- Cholestatic hepatitis caused by cetirizine. (nih.gov)
- Talk to your doctor or healthcare provider before you take cetirizine if you are pregnant or planning to become pregnant, or if you're breastfeeding. (healthline.com)
- A total of 76 women aged 56 - 79 years with osteoporosis were treated for 18 weeks with cetirizine allerkid drops price daily oral doses of 1.25 mg and 2.5 mg of stendra and. (prioritymedical.us)
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- Buy doxycycline monohydrate, a commonly prescribed antibiotic, is also prescribed when good rx cetirizine your urine test reveals a urinary tract infection, urinary tract infection, or if the infection has spread to a kidney. (prioritymedical.us)
- Cetirizine is a newer, second-generation antihistamine. (healthline.com)
- they may be charged with violating Nevada DUI laws Thanks funny site lsmagazine com my cetirizine cost at cvs childhood 824. (granodesal.com)
- Obat cetirizine salep - similarly, if a person had resulting chronic liver disease they should be assessed using Table 10 - Digestive and Reproductive Function. (geoproblems.eu)
- If you become pregnant while taking cetirizine, call your doctor. (medlineplus.gov)