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- Pharmacology For Paracetamol + Phenylephrine + Pseudoephedrine
Paracetamol + Phenylephrine + Pseudoephedrine Pharmacology
Paracetamol + Phenylephrine + Pseudoephedrine
About Paracetamol + Phenylephrine + PseudoephedrineN/AMechanism of Action of Paracetamol + Phenylephrine + PseudoephedrineN/APharmacokinets of Paracetamol + Phenylephrine + PseudoephedrineN/AOnset of Action for Paracetamol + Phenylephrine + PseudoephedrineN/ADuration of Action for Paracetamol + Phenylephrine + PseudoephedrineN/AHalf Life of Paracetamol + Phenylephrine + PseudoephedrineN/ASide Effects of Paracetamol + Phenylephrine + PseudoephedrineN/AContra-indications of Paracetamol + Phenylephrine + PseudoephedrineN/ASpecial Precautions while taking Paracetamol + Phenylephrine + PseudoephedrineN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Paracetamol + Phenylephrine + PseudoephedrineN/AInteractions for Paracetamol + Phenylephrine + PseudoephedrineN/ATypical Dosage for Paracetamol + Phenylephrine + PseudoephedrineN/ASchedule of Paracetamol + Phenylephrine + PseudoephedrineN/AStorage Requirements for Paracetamol + Phenylephrine + PseudoephedrineN/AEffects of Missed Dosage of Paracetamol + Phenylephrine + PseudoephedrineN/AEffects of Overdose of Paracetamol + Phenylephrine + PseudoephedrineN/AParacetamol
About ParacetamolAcetanilide derivative, Non narcotic Analgesic,Antipyretic.Mechanism of Action of ParacetamolParacetamol has analgesic and antipyretic action.
It is more active on cyclo-oxygenase enzyme in brain. Peripherally it is a poor inhibitor of prostaglandin synthesis.
Analgesic action: Paracetamol raises the pain threshold and produces analgesic effect.
Antipyretic action: Paracetamol lowers fever by direct action on the thermoregulatory centre in the Hypothalamus and block the effects of endogenous pyrogen.
Pharmacokinets of ParacetamolAbsorption: Paracetamol is rapidly and completely absorbed after oral administration.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
Onset of Action for Paracetamol30 - 60 minutesDuration of Action for Paracetamol6 hoursHalf Life of Paracetamol1-4 hoursSide Effects of Paracetamol1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol1. Hypersensitivity to ParacetamolSpecial Precautions while taking Paracetamol1. Hepatic impairment
2. Renal impairment
3. Hypertension
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
NEONATES : Contraindicated
Indications for Paracetamol1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for ParacetamolCholestyramine: Reduces absorption of paracetamol.
Charcoal: Activated, administered immediately reduces absorption of paracetamol.
Domperidone and metochlopramide: Enhance absorption of paracetamol.
Alcohol: Chronic excessive ingestion of alcohol potentiates hepatotoxicity of paracetamol.
Zidovudine: Effects zidovudine may be decreased.Typical Dosage for ParacetamolAdult:
500 - 1000 mg in 3 times daily
Maximum dose: 4 g / day
For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.
Children:
60 mg / kg body weight /day in 4 divided doses.
Schedule of ParacetamolHStorage Requirements for ParacetamolStore at 15-30 degree C in a tightly closed container. Protect from heat and moisture. Keep out of the reach of children.Effects of Missed Dosage of ParacetamolTake 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 ParacetamolGive supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. N-acetylcysteine is the specific antidote for Paracetamol poisoning. Dose: 150 mg /kg body weight as IV infusion over 15 minutes followed by same dose over 20 hours.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.
Phenylephrine
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.
Pseudoephedrine
About PseudoephedrineAlpha/Beta Adrenergic Agonist, a phenethylamine derivative, A nasal decongestant.Mechanism of Action of PseudoephedrineIt is a nasal decongestant with alpha-2 agonistic action. It produces local vasoconstriction, reduces blood flow, and causes shrinkage of mucosa which provides relief of nasal congestion. It reduces oedema of the nasal mucosa, thus improving ventilation, drainage and nasal stuffiness.Pharmacokinets of PseudoephedrineAbsorption: Well absorbed orally, Distribution: Widely distributed throughout the body, Metabolism: Partially metabolized in liver by N-demethylation, Excretion: Excreted through urine mainly as unchanged drug and also as metabolites.Onset of Action for Pseudoephedrine30 minutesDuration of Action for Pseudoephedrine4 to 8 hoursHalf Life of PseudoephedrineN/ASide Effects of Pseudoephedrine1. Rise in blood pressure
2. Tachycardia
3. Arrhythmias
4. CNS stimulation
5. Restlessness
6. Insomnia
7. Anxiety
8. Tremors
9. Skin rashes
10. Urinary retention
11. Respiratory difficulties
Contra-indications of Pseudoephedrine1. Hypersensitivity to the drug
2. Severe hypertension
3. Coronary artery disease
4. Patients taking monoamine oxidase inhibitors (MAOIs) or who have taken MAOIs within the previous 14 days
5. Extended release preparations are contraindicated in children below 12 yearsSpecial Precautions while taking Pseudoephedrine1. Hypertension
2. Cardiac diseases
3. Diabetes
4. Glaucoma
5. Prostatic hyperplasia
6. Hyperthyroidism
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Pseudoephedrine1. Nasal and Eustachian tube congestion
2.Upper respiratory tract congestion
3.Adjunctive therapy in symptomatic relief of common cold, allergic rhinitis, blocked Eustachian tube, and upper respiratory tract infectionsInteractions for PseudoephedrineN/ATypical Dosage for PseudoephedrineOral:
Adults and children over 12 years: 60mg 3 to 4 times daily
Maximum dose: 240mg/day
Children (age 6 to 12): 30mg 3 to 4 times daily
Maximum dose: 120mg/day
Children (age 2 to 6): 15mg 3 to 4 times daily
Maximum dose: 60mg/day or 4mg/kg.
Schedule of PseudoephedrineN/AStorage Requirements for PseudoephedrineStore at controlled room temperature at a range of 15 to 30 degree C. Keep out of reach of childrenEffects of Missed Dosage of PseudoephedrineTake the missed dose as soon as noticed and if it is the time for next dose
Effects of Overdose of PseudoephedrineContinue the regular schedule. Do not double the dose.
Over dosage and poisoning: Provide symptomatic treatment and supportive measures. Perform emesis and gastric lavage within 4 hours of ingestion. If renal function is adequate forced diuresis will increase elimination of the drug. (Do not force diuresis in severe poisoning). Monitor and assist vital signs, cardiac state and electrolyte balance. Treat cardiac toxicity with Propranolol or other effective drugs. Treat seizures with Diazepam (I.V.) and give dilute Potassium chloride solution for hypokalaemia.
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