| Astemizole Pharmacology |
| Astemizole |
| About Astemizole |
| Non-sedating selective H1-receptor antagonist, anticholinergic, antihistamine,antipruritic. |
| Mechanism of Action of Astemizole |
| Thisa histamine H1-receptor antagonist competitively binds to receptors on the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the activation of receptors by histamine which produces allergic symptoms like itching, edema and pruritis etc |
| Pharmacokinets of Astemizole |
| Absorption- Rapidly absorbed after oral administration Distribution- Widely distributed in the body.96% bound to the plasma proteins Metabolism- Metabolized in the liver to its metabolites Excretion- Excreted via feces |
| Onset of Action for Astemizole |
| N/A |
| Duration of Action for Astemizole |
| 24 hrs |
| Half Life of Astemizole |
| Its plasma half life is 1 day |
| Side Effects of Astemizole |
| 1. Difficulty breathing 2. Closing of throat 3. Swelling of lips, tongue, or face 4. Hives 5. Irregular heartbeat 6. Fainting 7. Seizures. 8. Drowsiness 9. Dizziness 10. Headache 11. Nervousness 12. Nausea 13. Diarrhea 14. Abdominal discomfort 15. Dry mouth 16. Dry skin 17. Itchiness. |
| Contra-indications of Astemizole |
| Contraindicated in patients with 1. Hypersensitivity to the drug 2. Porphyria |
| Special Precautions while taking Astemizole |
| Use with caution in patients with 1. Prostatic neuropathy 2. Urinary retention 3. Glaucoma 4. Pyloroduodenal obstruction 5. Epilepsy 6. Cardiac disease 7. Prolonged QT interval 8. Hypokalemia 9. Any work which require mental alertness |
| Pregnancy Related Information |
| Contraindicated |
| Old Age Related Information |
| Use with caution |
| Breast Feeding Related Information |
| Contraindicated |
| Children Related Information |
| Use with caution |
| Indications for Astemizole |
| 1. Rash 2. Hives 3. Watery eyes 4. Runny nose 5. Itching eyes 6. Sneezing 7. Conjunctivitis 8. Pruritis |
| Interactions for Astemizole |
| Alcohol, MAOIs, CNS Depressants: Effects potentiated. Food: Astemizole absorption reduced by 60 % Should be taken empty stomach or 2 hours after a meal. |
| Typical Dosage for Astemizole |
| Oral- General dose Adult- 10mg once daily Children (6-12 yrs) – 5mg once daily Take astemizole on an empty stomach, 1 hour before or 2 hours after eating food. |
| Schedule of Astemizole |
| H |
| Storage Requirements for Astemizole |
| Store at room temperature away from moisture and heat. |
| Effects of Missed Dosage of Astemizole |
| Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose. |
| Effects of Overdose of Astemizole |
| Give symptomatic and supportive treatment. |
