A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.
Agents, usually topical, that relieve itching (pruritus).
A hypnotic and sedative used in the treatment of INSOMNIA.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies.
A sleep disorder characterized by grinding and clenching of the teeth and forceful lateral or protrusive jaw movements. Sleep bruxism may be associated with TOOTH INJURIES; TEMPOROMANDIBULAR JOINT DISORDERS; sleep disturbances; and other conditions.
A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.
A range of methods used to reduce pain and anxiety during dental procedures.
A drug-induced depression of consciousness during which patients respond purposefully to verbal commands, either alone or accompanied by light tactile stimulation. No interventions are required to maintain a patent airway. (From: American Society of Anesthesiologists Practice Guidelines)
Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
The giving of attention to the special dental needs of children, including the prevention of tooth diseases and instruction in dental hygiene and dental health. The dental care may include the services provided by dental specialists.

Correlates of sleep and waking in Drosophila melanogaster. (1/46)

Drosophila exhibits a circadian rest-activity cycle, but it is not known whether fly rest constitutes sleep or is mere inactivity. It is shown here that, like mammalian sleep, rest in Drosophila is characterized by an increased arousal threshold and is homeostatically regulated independently of the circadian clock. As in mammals, rest is abundant in young flies, is reduced in older flies, and is modulated by stimulants and hypnotics. Several molecular markers modulated by sleep and waking in mammals are modulated by rest and activity in Drosophila, including cytochrome oxidase C, the endoplasmic reticulum chaperone protein BiP, and enzymes implicated in the catabolism of monoamines. Flies lacking one such enzyme, arylalkylamine N-acetyltransferase, show increased rest after rest deprivation. These results implicate the catabolism of monoamines in the regulation of sleep and waking in the fly and suggest that Drosophila may serve as a model system for the genetic dissection of sleep.  (+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. (2/46)

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)

Effects of anti-allergic drugs on intestinal mastocytosis and worm expulsion of rats infected with Neodiplostomum seoulense. (3/46)

The effects of anti-allergic drugs on intestinal mastocytosis and the expulsion of Neodiplostomum seoulense were observed in Sprague-Dawley rats, after oral infection with 500 metacercariae. The drugs used were hydroxyzine (a histamine receptor H1 blocker), cimetidine (a H2 blocker), cyclosporin-A (a helper T-cell suppressant), and prednisolone (a T- and B-cell suppressant). Infected, but untreated controls, and uninfected controls, were prepared. Worm recovery rate and intestinal mastocytosis were measured on weeks 1, 2, 3, 5, and 7 post-infection. Compared with the infected controls, worm expulsion was significantly (P < 0.05) delayed in hydroxyzine- and cimetidine-treated rats, despite mastocytosis being equally marked in the duodenum of all three groups. In the cyclosporin-A- and prednisolone-treated groups, mastocytosis was suppressed, but worm expulsion was only slightly delayed, without statistical significance. Our results suggest that binding of histamine to its receptors on intestinal smooth muscles is more important in terms of the expulsion of N. seoulense from rats than the levels of histamine alone, or mastocytosis.  (+info)

Inhibition of histamine-induced nasal obstruction by cetirizine in allergic rhinitis. (4/46)

This double-blind randomized crossover placebo-controlled study was designed to assess objectively the nasal antihistamine effect of cetirizine in patients with allergic rhinitis and control subjects. Nasal challenge was performed by nebulization of increasing doubling doses of histamine (0; 0.04 to 1.28 mg/nostril) in six patients with allergic rhinitis and six control subjects on cetirizine (2 x 10 mg daily for 3 days) or placebo. Sneezings were counted and nasal obstruction was assessed by subjective scoring and by objective measurement of nasal airway resistance by posterior rhinomanometry. Histamine induced sneezing and a dose-dependent increase in nasal airway resistance and in perceived sensation of obstruction. Responses were greater in patients with allergic rhinitis compared with controls, although of borderline significance for nasal obstruction. Cetirizine totally abolished sneezing and significantly reduced increase in nasal airway resistance and perceived sensation of nasal obstruction both in normal and rhinitic subjects. Our results demonstrate by an objective measurement the nasal antihistamine effect of cetirizine. We propose this simple provocation test to assess the time-course of the effect of antihistamines and to compare the relative potency of related compounds.  (+info)

Interference of cetirizine with the late eosinophil accumulation induced by either PAF or compound 48/80. (5/46)

1. The effect of topical or systemic treatment with the histamine H1-receptor antagonist, cetirizine, on the rat pleural eosinophil accumulation induced by PAF or compound 48/80 was investigated. The number of pleural resident eosinophils increased 6 h after the intrathoracic (i.t.) injection of PAF (1 microgram/cavity), peaked within 24 h and persisted significantly augmented for at least 96 h. Compound 48/80 (25 micrograms/cavity) also produced a long lasting pleural eosinophilia but this was first noted only 24 h after stimulation. 2. Intraperitoneal pretreatment with cetirizine inhibited eosinophilia induced by either PAF (ED50 = 19 mg kg-1) or compound 48/80 (ED50 = 14 mg kg-1) whereas meclizine, another histamine H1-receptor antagonist, was inactive. 3. Administered locally, cetirizine (5 and 15 micrograms/cavity) also dose-dependently inhibited both PAF- and compound 48/80-induced eosinophilia, providing evidence that its inhibitory effect is not due to any action upon circulating eosinophils. Consistent with this result, incubation of isolated peritoneal eosinophils with cetirizine failed to modify in vitro eosinophil migration caused by PAF. 4. Since the late eosinophilia induced by PAF may depend on the synthesis of a transferable protein mediator, cetirizine was administered to donor or recipient rats in order to determine whether it interferes with the generation or with the expression of this protein. We showed that only the treatment of recipient rats abolished the transfer of the eosinophilotactic activity, indicating that cetirizine does not modify the generation but inhibits the expression of this activity. 5. Our findings indicate that cetirizine is able to inhibit eosinophil accumulation by acting locally. The mechanism is neither related to its recognized ability to antagonize histamine H,-receptors nor to a direct action upon circulating eosinophils.  (+info)

SOME ACTIONS OF CENTRALLY ACTIVE AND OTHER DRUGS ON THE TRANSMISSION OF SINGLE NERVE IMPULSES THROUGH THE ISOLATED SUPERIOR CERVICAL GANGLION PREPARATION OF THE RABBIT. (6/46)

The effect of some centrally-active and other drugs on the transmission of single nerve impulses through the isolated superior cervical ganglion preparation of the rabbit has been studied by recording both preganglionic and postganglionic action potentials. Block of conduction in the axon could be distinguished from block of the synaptic mechanism. The drugs did not appear to exert any one characteristic form of blocking action. A continuous spectrum of drug action linked an agent such as meprobamate which acted predominantly on the synapse to benactyzine which acted mainly by blocking axonal conduction. The drugs have been divided into three groups. Group I: hexamethonium, meprobamate, paraldehyde, amylobarbitone, methylpentynol and azacyclonal; these acted relatively selectively at the ganglion. Group II: N714C (the cis-isomer of chlorprothixene), prochlorperazine, methylpentynol carbamate, pipradrol, promethazine, perphenazine and procaine; the action of these drugs on the ganglion could be accounted for entirely in terms of their axonal depressant action. Group III: chlorprothixene, promazine, N720 (dihydrochlorprothixene), chlorpromazine, hydroxyzine and benactyzine; these drugs also blocked axonal conduction but in addition they appeared to exert a "facilitating" action at the ganglionic synapse. The actions of adrenaline, adrenochrome, iproniazid, ergotoxine, mescaline and lysergic acid diethylamide on transmission were also studied. The implications of the modifications of ganglionic transmission produced by these drugs is discussed.  (+info)

A randomized, controlled, crossover trial of oral midazolam and hydroxyzine for pediatric dental sedation. (7/46)

The effectiveness of oral midazolam in pediatric dentistry is controversial. This randomized, controlled, crossover, double blind clinical trial was conducted in order to study the effect of midazolam, used either alone or in association with hydroxyzine, during child dental treatment. Thirty seven dental sedation sessions were carried out on 11 ASA I uncooperative children less than five years-old. In each appointment children were randomly assigned to groups: P - placebo, M - midazolam (1.0 mg/kg), or MH - midazolam (0.75 mg/kg) plus hydroxyzine (2.0 mg/kg). Vital signs (blood pressure, breathing rate, pulse and oxygen saturation) and behavior parameters (consciousness, crying, movement, overall behavior) were evaluated every 15 minutes. Friedman and Wilcoxon statistical tests were used to compare groups and different moments in the same group. Normal values of vital signs were usually registered. Heart rate increased in groups P and M as the session went on. Group M presented less crying and movement at the first 15 minutes of treatment. Group MH caused more drowsiness at the beginning of the session. Overall behavior was better in group M than in groups P or MH. Group M produced effective sedation in 77% of the cases, and group MH did so in 30.8%. It was concluded that midazolam was effective and safe, and its association with hydroxyzine did not lead to additional advantages in pediatric dental sedation.  (+info)

Hydroxyzine-induced supraventricular tachycardia in a nine-year-old child. (8/46)

Hydroxyzine is a first generation antihistamine widely used in the paediatric population for a variety of conditions. A nine-year-old girl presented with supraventricular tachycardia while on clinical doses of hydroxyzine for pruritus. On arrival at the hospital, she was diaphoretic, with cool peripheries, poor peripheral pulses and a heart rate of 250/minute. There was a history of three palpitation episodes with chest tightness during the five months she was taking hydroxyzine. The supraventricular tachycardia eventually reverted to sinus rhythm with intravenous verapamil. Relevant cardiac examination and investigations had not shown any cardiac abnormalities. After discontinuing hydroxyzine, she had no further episodes of supraventricular tachycardia. To our knowledge, this is the first report of hydroxyzine induced-supraventricular tachycardia in the medical literature.  (+info)

Hydroxyzine is an antihistamine medication that is primarily used to treat symptoms of allergies such as itching, hives, and swelling. It works by blocking the effects of histamine, a substance in the body that causes allergic reactions. In addition to its antihistaminic properties, hydroxyzine also has sedative and anxiety-reducing effects, which make it useful in treating anxiety disorders, symptoms of alcohol withdrawal, and as a sleep aid. It is available in both oral and injectable forms and is usually taken orally in the form of tablets, capsules, or syrup. As with any medication, hydroxyzine should be used under the supervision of a healthcare provider, and its use may be subject to certain precautions and contraindications depending on the individual's medical history and current health status.

Antipruritics are a class of medications or substances that are used to relieve or prevent itching (pruritus). They work by reducing the sensation of itchiness and can be applied topically to the skin, taken orally, or administered intravenously. Some common antipruritics include diphenhydramine, hydroxyzine, and corticosteroids.

Chloral hydrate is a sedative and hypnotic medication, which means it can help to promote sleep and reduce anxiety. It is a type of compound called a chloral derivative and works by increasing the activity of a neurotransmitter in the brain called gamma-aminobutyric acid (GABA), which has a calming effect on the nervous system.

Chloral hydrate is available in various forms, including tablets, capsules, and liquid solutions. It is typically used for short-term treatment of insomnia or anxiety, but it may also be used for other purposes as determined by a healthcare provider.

Like all medications, chloral hydrate can have side effects, which can include dizziness, headache, stomach upset, and changes in behavior or mood. It is important to use this medication only as directed by a healthcare provider and to report any unusual symptoms or concerns promptly.

Histamine H1 antagonists, also known as H1 blockers or antihistamines, are a class of medications that work by blocking the action of histamine at the H1 receptor. Histamine is a chemical mediator released by mast cells and basophils in response to an allergic reaction or injury. It causes various symptoms such as itching, sneezing, runny nose, and wheal and flare reactions (hives).

H1 antagonists prevent the binding of histamine to its receptor, thereby alleviating these symptoms. They are commonly used to treat allergic conditions such as hay fever, hives, and eczema, as well as motion sickness and insomnia. Examples of H1 antagonists include diphenhydramine (Benadryl), loratadine (Claritin), cetirizine (Zyrtec), and doxylamine (Unisom).

Dimenhydrinate is an antihistamine medication that is primarily used to treat symptoms of motion sickness, such as nausea, vomiting, and dizziness. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms.

The chemical name for dimenhydrinate is 8-chlorotheophylline 1-((2-(diphenylmethoxy)ethyl)dimethylamino) derivative. It is available in various forms, including tablets, capsules, and liquid solutions, and is typically taken orally.

In addition to its use as an anti-motion sickness medication, dimenhydrinate may also be used to treat symptoms of vertigo, Meniere's disease, and other inner ear disorders. However, it should be used with caution, as it can cause drowsiness, dry mouth, and other side effects.

It is important to follow the dosage instructions carefully when taking dimenhydrinate, and to talk to a healthcare provider before using it if you have any medical conditions or are taking other medications.

Sleep bruxism is a sleep-related movement disorder characterized by the involuntary clenching or grinding of teeth and jaw muscle activity during sleep, which can lead to tooth wear, jaw pain, headaches, and other oral health issues. It is typically considered a parasomnia, which is a type of abnormal behavior that occurs during sleep. The exact causes of sleep bruxism are not fully understood, but it may be associated with stress, certain medications, alcohol and drug use, and other factors. Treatment options can include stress management techniques, dental guards to protect the teeth, and in some cases, medication.

Secobarbital is a barbiturate medication that is primarily used for the treatment of short-term insomnia and as a preoperative sedative. It works by depressing the central nervous system, producing a calming effect and helping to induce sleep. Secobarbital has a rapid onset of action and a relatively short duration of effect.

It is available in various forms, including capsules and injectable solutions, and is typically prescribed for use on an as-needed basis rather than as a regular medication. Secobarbital can be habit-forming and carries a risk of dependence and withdrawal, so it should only be used under the close supervision of a healthcare provider.

It's important to note that Secobarbital is not commonly prescribed in modern medical practice due to its high potential for abuse and the availability of safer and more effective sleep aids.

Dental anesthesia is a type of local or regional anesthesia that is specifically used in dental procedures to block the transmission of pain impulses from the teeth and surrounding tissues to the brain. The most common types of dental anesthesia include:

1. Local anesthesia: This involves the injection of a local anesthetic drug, such as lidocaine or prilocaine, into the gum tissue near the tooth that is being treated. This numbs the area and prevents the patient from feeling pain during the procedure.
2. Conscious sedation: This is a type of minimal sedation that is used to help patients relax during dental procedures. The patient remains conscious and can communicate with the dentist, but may not remember the details of the procedure. Common methods of conscious sedation include nitrous oxide (laughing gas) or oral sedatives.
3. Deep sedation or general anesthesia: This is rarely used in dental procedures, but may be necessary for patients who are extremely anxious or have special needs. It involves the administration of drugs that cause a state of unconsciousness and prevent the patient from feeling pain during the procedure.

Dental anesthesia is generally safe when administered by a qualified dentist or oral surgeon. However, as with any medical procedure, there are risks involved, including allergic reactions to the anesthetic drugs, nerve damage, and infection. Patients should discuss any concerns they have with their dentist before undergoing dental anesthesia.

Conscious sedation, also known as procedural sedation and analgesia, is a minimally depressed level of consciousness that retains the patient's ability to maintain airway spontaneously and respond appropriately to physical stimulation and verbal commands. It is typically achieved through the administration of sedative and/or analgesic medications and is commonly used in medical procedures that do not require general anesthesia. The goal of conscious sedation is to provide a comfortable and anxiety-free experience for the patient while ensuring their safety throughout the procedure.

Hypnotics and sedatives are classes of medications that have depressant effects on the central nervous system, leading to sedation (calming or inducing sleep), reduction in anxiety, and in some cases, decreased awareness or memory. These agents work by affecting the neurotransmitter GABA (gamma-aminobutyric acid) in the brain, which results in inhibitory effects on neuronal activity.

Hypnotics are primarily used for the treatment of insomnia and other sleep disorders, while sedatives are often prescribed to manage anxiety or to produce a calming effect before medical procedures. Some medications can function as both hypnotics and sedatives, depending on the dosage and specific formulation. Common examples of these medications include benzodiazepines (such as diazepam and lorazepam), non-benzodiazepine hypnotics (such as zolpidem and eszopiclone), barbiturates, and certain antihistamines.

It is essential to use these medications under the guidance of a healthcare professional, as they can have potential side effects, such as drowsiness, dizziness, confusion, and impaired coordination. Additionally, long-term use or high doses may lead to tolerance, dependence, and withdrawal symptoms upon discontinuation.

Dental care for children, also known as pediatric dentistry, is a branch of dentistry that focuses on the oral health of children from infancy through adolescence. The medical definition of dental care for children includes:

1. Preventive Dentistry: This involves regular dental check-ups, professional cleaning, fluoride treatments, and sealants to prevent tooth decay and other dental diseases. Parents are also educated on proper oral hygiene practices for their children, including brushing, flossing, and dietary habits.
2. Restorative Dentistry: If a child develops cavities or other dental problems, restorative treatments such as fillings, crowns, or pulpotomies (baby root canals) may be necessary to restore the health and function of their teeth.
3. Orthodontic Treatment: Many children require orthodontic treatment to correct misaligned teeth or jaws. Early intervention can help guide proper jaw development and prevent more severe issues from developing later on.
4. Habit Counseling: Dental care for children may also involve habit counseling, such as helping a child stop thumb sucking or pacifier use, which can negatively impact their oral health.
5. Sedation and Anesthesia: For children who are anxious about dental procedures or have special needs, sedation or anesthesia may be used to ensure their comfort and safety during treatment.
6. Emergency Care: Dental care for children also includes emergency care for injuries such as knocked-out teeth, broken teeth, or severe toothaches. Prompt attention is necessary to prevent further damage and alleviate pain.
7. Education and Prevention: Finally, dental care for children involves educating parents and children about the importance of good oral hygiene practices and regular dental check-ups to maintain optimal oral health throughout their lives.

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