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- Pharmacology For Ebastine + Phenylephrine
Ebastine + Phenylephrine Pharmacology
Ebastine + Phenylephrine
About Ebastine + PhenylephrineN/AMechanism of Action of Ebastine + PhenylephrineN/APharmacokinets of Ebastine + PhenylephrineN/AOnset of Action for Ebastine + PhenylephrineN/ADuration of Action for Ebastine + PhenylephrineN/AHalf Life of Ebastine + PhenylephrineN/ASide Effects of Ebastine + PhenylephrineN/AContra-indications of Ebastine + PhenylephrineN/ASpecial Precautions while taking Ebastine + PhenylephrineN/APregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationNot recommended below 2 yearsIndications for Ebastine + PhenylephrineAllergic rhinitisInteractions for Ebastine + PhenylephrineN/ATypical Dosage for Ebastine + PhenylephrineN/ASchedule of Ebastine + PhenylephrineN/AStorage Requirements for Ebastine + PhenylephrineN/AEffects of Missed Dosage of Ebastine + PhenylephrineN/AEffects of Overdose of Ebastine + PhenylephrineN/AEbastine
About EbastineSecond generation, long-acting and selective H1 antagonist, Non-sedative Antihistamine.Mechanism of Action of EbastineDrug and its active metabolite is selective peripheral histamine H1 receptor antagonist. Thus it prevents the attachment of histamine on receptors and its activation (Activation of receptors of histamine on various tissues produce various allergic symptoms e.g. Runny nose).Ebastine also has a specific inhibitory effect on Th2-type cytokine production and inhibit T cell migration and pro-inflammatory cytokine production by T cells and macrophagesPharmacokinets of EbastineAbsorption - Rapidly absorbed after oral administration
Distribution- Widely distributed in the body. >95% bound to the plasma proteins.
Metabolism- Metabolized in the liver to its metabolites by N-dealkylation and hydroxylation.Carebastine is its active metabolite.
Excretion- Excreted through urine
Onset of Action for EbastineN/ADuration of Action for EbastineN/AHalf Life of EbastineIts plasma half life is 15-19 hrsSide Effects of Ebastine1. Headache
2. Dry mouth
3. Drowsiness
4. Pharyngitis
5. Abdominal pain
6. Dyspepsia
7. Asthenia
8. Epistaxis
9. Rhinitis
10. Sinusitis
11. Nausea
12. InsomniaContra-indications of Ebastine1. Hypersensitivity to Ebastine or any of its ingredients
2. Cardiac arrhythmia
Special Precautions while taking Ebastine1. Long QT syndrome
2. Hypokalemia
3. Hepatic impairment
4. Renal impairment
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Ebastine1. Seasonal and perennial allergic rhinitis
2. Idiopathic chronic urticaria
3. T cell-mediated allergic inflammatory disorders (asthma, atopic dermatitis)
4. Th2 -type autoimmune diseases
Interactions for EbastineKetoconazole / Erythromycin: When ebastine is given concomitantly a pharmacokinetic and pharmacodynamic interaction has been observed; an 18-19 msec (4.7%-5%) increase in QT has been reported with either combination.
Typical Dosage for EbastineOral-
Adult-10 mg once a day
Schedule of EbastineN/AStorage Requirements for EbastineStore below 25?C.Protect from light. Keep out of reach of childrenEffects of Missed Dosage of EbastineTake 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 doseEffects of Overdose of EbastineGive symptomatic and supportive treatmentPhenylephrine
About PhenylephrineAn a1-adrenergic receptor agonist, Phenethylamine derivative, Decongestant, Antiglaucoma, Mydriatic.Mechanism of Action of PhenylephrineThe drug exerts it`s pharmacological action by acting as a selective alpha-1 adrenergic agonist. It causes vasoconstriction and increases total peripheral resistance and raises blood pressure. It reduces intraocular tension by constricting ciliary body blood vessels and produce mydriasis (without cycloplegia). It exerts nasal decongestant action; by vasoconstrictory action on arterioles of nasal mucosa. It prolongs and localizes the action of anaesthetics due to it`s vasoconstrictory action on skin, mucous membrane, and viscera and thus slows the rate of absorption of local anaesthetics.Pharmacokinets of PhenylephrineAbsorption: Variable depending up on the route of administration. Metabolism: Metabolized in the liver and intestine.Onset of Action for PhenylephrineNasal: Rapid
Ophthalmic: Rapid
I.V.: Rapid
I.M.: Within 15 minutes
Duration of Action for PhenylephrineNasal: ? to 4 hours
Ophthalmic: 3 to 7 hours
I.V.: 15 to 20 minutes
I.M.: ? to 2 hours.
Half Life of PhenylephrineN/ASide Effects of Phenylephrine1.Bradycardia
2.Arrhythmias
3.Hypertension
4.Tachycardia
5.Palpitations
6.Premature ventricular contractions
7.Pallor
8.Headache
9.Dizziness
10.Nervousness
11.Brow ache(with ophthalmic form)
12.Burning or stinging in eye
13.Blurred vision
14.Elevated intraocular pressure
15.Nausea
16.Episodes of asthma
17.Tachyphylaxis
18.Anaphylaxis
Contra-indications of Phenylephrine1.Hypersensitivity to the drug
2.Hyperthyroidism
3.Ventricular tachycardia and severe hypertension (Injected form)
4.Angle closure glaucoma and in those who wear soft contact lenses(ophthalmic form)
Special Precautions while taking Phenylephrine1.Coronary diseases
2.Advanced arteriosclerosis
3.Bradycardia
4.Partial heart block
5.Myocardial diseases
6.Atherosclerosis
7.Hypertension
8.Nasal and ophthalmic form use cautiously in type-1 diabetes mellitus
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
Below age 6:contraindicatedIndications for Phenylephrine1.Hypotension
2.Paroxysmal supra ventricular tachycardia
3.Maintain blood pressure during spinal and inhalation anaesthesia
4.Prolongation of spinal anaesthesia
5.Shock
6.Mydriasis(without cycloplegia)
7.Nasal congestion.
8.Cataract
Interactions for PhenylephrineMay interact with systemically administered MAOIs.Typical Dosage for PhenylephrineI.M. or S.C.: 2 to 5mg. Then if required; give doses up to 10mg.
Slow I.V. injection: 0.1 to 0.5mg. Then if required; repeat after 15 minutes.
I.V. infusion: Starts with 0.18mg/minute. Then adjust the dosage up to 0.03 to 0.06mg/minute based on patient`s response.
Nasal congestion: Apply 2 to 3 drops or 1 to 2 sprays of 0.25% to 1% solution instilled in each nostril.
Mydriasis (without cycloplegia): Instill 1 to 2drops 2.5% or 10% solution in eye. Repeated if required.
Prolongation of spinal anaesthesia: 2 to 5mg added to anaesthetic solution.
Schedule of PhenylephrineN/AStorage Requirements for PhenylephrineStore at controlled room temperature at range of 15 to 30 degree C. in a well closed container. Protect from light.Effects of Missed Dosage of PhenylephrineTake 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 PhenylephrineDiscontinue the drug and give supportive and symptomatic treatment. Closely monitor vital signs. Use atropine sulfate to block reflex Bradycardia. Treat excessive hypertension with phentolamine. Treat cardiac arrhythmia with propranolol. Treat excessive mydriatic effect with levodopa.
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