Tekostine
Tekostine Uses, Dosage, Side Effects, Food Interaction and all others data.
Tekostine, a piperidine derivative, is a long-acting, nonsedating, second-generation histamine receptor antagonist that binds preferentially to peripheral H1 receptors. It is metabolised to active metabolite, carebastine. It has antihistaminic, antiallergic activity and prevents histamine-induced bronchoconstriction. It does not have significant sedative or antimuscarinic actions.
| Trade Name | Tekostine |
| Generic | Ebastine |
| Ebastine Other Names | Ebastina, Ebastine |
| Weight | 10mg |
| Type | Tablet |
| Formula | C32H39NO2 |
| Weight | Average: 469.6576 Monoisotopic: 469.298079497 |
| Groups | Approved, Investigational |
| Therapeutic Class | Non-sedating antihistamines |
| Manufacturer | Gray`s Pharmaceuticals |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tekostine is used for the symptomatic treatment of: Seasonal and perennial allergic rhinitis, Idiopathic chronic urticaria.
Tekostine is also used to associated treatment for these conditions: Allergic Rhinitis (AR)
Dosage
Tekostine dosage
Children between 2 and 5 years: 2.5 ml (half teaspoonful) once daily (up to 5 ml in severe cases such as perennial allergic rhinitis)
Children between 6 and 11 years: 5 ml (one teaspoonful) / 5 mg (half tablet) once daily (up to 10 ml in severe cases such as perennial allergic rhinitis)
Adults and older children more than 11 years: 10 mg (1 tablet) or 10 ml (two teaspoonfuls) once daily.
Tekostine may be taken with or without food.
Side Effects
The most common side-effects are headache, dry mouth and drowsiness. Other less commonly reported side-effects include pharyngitis, abdominal pain, dyspepsia, asthenia, epistaxis, rhinitis, sinusitis, nausea and insomnia.
Precaution
It is advisable to exercise caution when using ebastine in patients known to have the following conditions: long QT syndrome, hypokalaemia, treatment with any medicine known to produce an increase in QT interval or inhibit CYP3A4 enzyme systems such as azole antifungals and macrolide antibiotics. Use in Pregnancy and Lactation The safety of ebastine during pregnancy and lactation has not been established. Tekostine should not be used during pregnancy only if clearly needed. It is not known whether ebastine is excreted in milk, therefore, ebastine should not be used during lactation.
Interaction
The interaction of ebastine in combination with either ketoconazole or erythromycin (both known to prolong the QTc interval) has been evaluated. A significant pharmacokinetic and pharmacodynamic interaction has been observed with this combination; an 18-19 msec (4.7% - 5%) increase in QTc has been reported with either combination. Tekostine does not interact with the kinetics of theophylline, warfarin, cimetidine, diazepam or alcohol. The sedation effect of alcohol and diazepam may be enhanced. When ebastine is administered with food, there is a 1.5 to 2.0 fold increase in the plasma levels and the AUC of the main active acid metabolite of ebastine. This increase does not alter the Tmax. The administration of ebastine with food does not cause a modification in its clinical effect.
Food Interaction
- Take with or without food. Taking ebastine with food may increase its bioavailability.
Pregnancy & Breastfeeding use
The safety of Tekostine during pregnancy and lactation has not been established.
Contraindication
Patients with a known hypersensitivity to Tekostine or any of its ingredients.
Acute Overdose
No clinically meaningful signs or symptoms were observed up to 100 mg given once daily. There is no specific antidote for Tekostine. In case of accidental over dosages, gastric lavage, monitoring of vital functions including ECG, and symptomatic treatment should be carried out.
Storage Condition
Store below 25° C.
Innovators Monograph
You find simplified version here Tekostine
Tekostine contains Ebastine see full prescribing information from innovator Tekostine Monograph, Tekostine MSDS, Tekostine FDA label
FAQ
What is Tekostine used for?
Tekostine is a second-generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis.
How safe is Tekostine?
Tekostine appears to be a safe, effective and well-tolerated second-generation antihistamine in the treatment of allergic rhinitis and chronic idiopathic urticaria.
How does Tekostine work?
Tekostine works by inhibiting the H1 receptor that is mainly responsible for allergic responses like hives (skin rash triggered by a reaction).
What are the common side effects of Tekostine?
Common side effects of Tekostine are include:
- Nausea
- Drowsiness
- Dry mouth
- Nose bleed
- Weakness
- Indigestion
- Sleepiness
- Headache
- Drowsiness
- Abdominal pain
- Pharyngitis
- Dyspepsia
- Asthenia
- Sinusitis
Is Tekostine safe during pregnancy?
It is preferable to avoid the use of Tekostine during pregnancy.
Is Tekostine safe during breastfeeding?
Preliminary evidence indicates that the amounts in milk are unlikely to affect a breastfed infant.
Can I drink alcohol with Tekostine?
Do not drink alcohol while taking this medication as it may cause increased sleepiness. Stop taking Tekostine at least three days before taking an allergy test as it can affect the test results.
Can I drive after taking Tekostine?
Do not drive if you experience drowsiness after taking this medicine.
How many time can I take Tekostine daily?
One 10mg tablet is usually taken once a day.
Can I take Tekostine on an epmty?
It should be taken regardless of food or meal.
How long does Tekostine take to work ?
The effect of this medicine can be observed within 1 to 3 hours of administration of the dose. The effect of this medicine lasts for an average duration of 24 hours.
How long does Tekostine stay in my system?
The pharmacokinetics of Tekostine is linear in the therapeutic dose range; maximum plasma concentrations of Tekostine are achieved 4–6 h after dosing; and steady-state is reached after 4 days.
Is Tekostine safe for heart patients?
The overall cardiac tolerability of Tekostine is excellent. In Tekostine dose-ranging studies in adults and children, there were no meaningful dose-related changes in the QTc interval.
Is it safe to stop taking Tekostine ?
Do not stop taking Tekostine without talking to your doctor. Your doctor may start you on a low dose of Tekostine and increase your dose after 4 to 6 weeks. Your doctor may increase your dose again 3 or more months later.
What happen If I missed Tekostine?
If you missed any dose, take it as early as you remember. If it is time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose of medicine to compensate for a missed one.
What happen if I overdose on Tekostine?
The symptoms of barnd overdose include increased heart rate, abnormal behaviour, headache, dizziness, oliguria low urine output), and gastrointestinal disorders. Consult your doctor immediately if you happen to take an overdose of this medicine
Is Tekostine safe for heart patients?
The overall cardiac tolerability of Tekostine is excellent. In Tekostine dose-ranging studies in adults and children, there were no meaningful dose-related changes in the QTc interval.
Can I take Tekostine every day?
The recommended dose of Tekostine tablets is one 5 mg tablet once daily.
Does Tekostine cause drowsiness?
Some of the common and major side effects of Tekostine are: Nausea, Drowsiness.
