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Histamine
| Question | Answer | ||
|---|---|---|---|
| Contraindications of histamine | Bronchial asthma Active peptic ulcer Pheochromocytoma | ||
| What is used to Tx Meneire’s disease? | Betahistine | ||
| Betahistine | It is analogue of histamine and acts on H1 receptor | ||
| Histamine is synthesized by 2 enzymes | Histidine de-carboxylase that converts histidine to histamine. This enzyme is inhibited by methyl histidine. | - Aromatic amino acid de-carboxylase which is non specific enzyme and inhibited by methyl-dopamine . | |
| Pharmacological actions of H1 blockers | anti-nausea and anti-emetic Anti-cholinergic effect Local anesthetic effect. Anti- parkinsonism effect. Antiserotoninergic effect α- adrenoceptor blocking effects. they inhibit P-glycoprotein | ||
| 1st generation H1-blockers General properties | Great CNS depression Relatively of short duration of action. Relatively of little dangerous drug interaction with macrolides antibiotics and antifungal drugs. Blockage of muscarinic receptor | ||
| Names of 1st generation H1-blockers | Diphenhydramine Dimenhydrinate Promethazine Hydroxyzine | Cyproheptadine Meclizine Pheniramine Cinnarizine Buclizine | Chlorpheniramine Cyclizine Clemastine Triprolidine Demethindene |
| Contraindications of H1 blockers | Hypersensitivity to the drugs. Severe bronchial asthma. Prostatic hyperplasia. Closed angle glaucoma. Bladder neck obstruction. Breast feeding. |