Paracetamol + Loratadine + Phenylpropanolamine Pharmacology

Paracetamol + Loratadine + Phenylpropanolamine

About Paracetamol + Loratadine + Phenylpropanolamine
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Mechanism of Action of Paracetamol + Loratadine + Phenylpropanolamine
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Pharmacokinets of Paracetamol + Loratadine + Phenylpropanolamine
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Onset of Action for Paracetamol + Loratadine + Phenylpropanolamine
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Duration of Action for Paracetamol + Loratadine + Phenylpropanolamine
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Half Life of Paracetamol + Loratadine + Phenylpropanolamine
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Side Effects of Paracetamol + Loratadine + Phenylpropanolamine
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Contra-indications of Paracetamol + Loratadine + Phenylpropanolamine
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Special Precautions while taking Paracetamol + Loratadine + Phenylpropanolamine
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Paracetamol + Loratadine + Phenylpropanolamine
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Interactions for Paracetamol + Loratadine + Phenylpropanolamine
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Typical Dosage for Paracetamol + Loratadine + Phenylpropanolamine
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Schedule of Paracetamol + Loratadine + Phenylpropanolamine
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Storage Requirements for Paracetamol + Loratadine + Phenylpropanolamine
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Effects of Missed Dosage of Paracetamol + Loratadine + Phenylpropanolamine
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Effects of Overdose of Paracetamol + Loratadine + Phenylpropanolamine
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Paracetamol

About Paracetamol
Acetanilide derivative, Non narcotic Analgesic,Antipyretic.
Mechanism of Action of Paracetamol
Paracetamol 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 Paracetamol
Absorption: 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 Paracetamol
30 - 60 minutes
Duration of Action for Paracetamol
6 hours
Half Life of Paracetamol
1-4 hours
Side Effects of Paracetamol
1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol
1. Hypersensitivity to Paracetamol
Special Precautions while taking Paracetamol
1. Hepatic impairment
2. Renal impairment
3. Hypertension
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
NEONATES : Contraindicated
Indications for Paracetamol
1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for Paracetamol
Cholestyramine: 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 Paracetamol
Adult:
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 Paracetamol
H
Storage Requirements for Paracetamol
Store 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 Paracetamol
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 Paracetamol
Give 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.

Loratadine

About Loratadine
Second Generation H1 Antagonist, Antihistamine.
Mechanism of Action of Loratadine
Loratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation (activation releasing other chemicals which produce the symptoms associated with allergy) of cells by histamine. Drug also has mast cell stabilizing property.
Pharmacokinets of Loratadine
Absorption- Rapidly absorbed after oral administration.
Distribution-Widely distributed in the body.97% bound to the plasma proteins.
Metabolism- Metabolized in the liver to its metabolites, Descarboethoxyloratidine is its active metabolite.
Excretion- Excreted through both the urine and feces.
Onset of Action for Loratadine
1 - 3 hrs
Duration of Action for Loratadine
24 hrs
Half Life of Loratadine
N/A
Side Effects of Loratadine
1. Headache
2. Dry mouth, nose, and throat
3. Drowsiness
4. Rapid heartbeat
5. Difficulty urinating
6. Vision problems
7. Dizziness
8. Muscle weakness
9. Anxiety
10. Change in menstruation
11. Clumsiness
12. Depression
13. Feeling faint
14. Flushing of the face
15. Hallucinations
16. Migraines
17. Palpitations
18. Rash
19. Seizures
20. Shortness of breath
21. Sleeping disorders
22. Sore throat
23. Tightness in the chest or back
24. Yellowing of the eyes or skin
Contra-indications of Loratadine
1. Allergy to drug or any other antihistamines
2. Stenosing peptic ulcer
3. Symptomatic prostatic hypertrophy
4. Asthmatic attack
5. Bladder neck obstruction
6. Pyloroduodenal obstruction
7. Narrow-angle glaucoma
Special Precautions while taking Loratadine
Use with caution in patients with severe hepatic damage.
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
NEONATES- Contraindicated
Indications for Loratadine
1. Allergic rhinitis (perennial and seasonal )
2. Vasomotor rhinitis
3. Allergic conjunctivitis
4. Urticaria( mild, uncomplicated )
5. Angioedema
6. Amelioration of allergic reactions to blood or plasma
7. Dermatographism
8. Adjunctive therapy in anaphylactic reactions
9. Decongestant

Interactions for Loratadine
Macrolide antibiotics, ketoconazole, cimetidine, ranitidine and theophylline: Caution should be exerted while co-administration of these drugs which are known to inhibit hepatic metabolism.
Typical Dosage for Loratadine
Oral-
General dose-
Adult-
10mg/day.
Children (>6) - Same as adult.

Schedule of Loratadine
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Storage Requirements for Loratadine
Store it at room temperature and away from excess heat and moisture.
Effects of Missed Dosage of Loratadine
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 Loratadine
Give symptomatic and supportive treatment. Induce emesis except in patients with impaired consciousness. Then administer activated charcoal to adsorb any remaining drug. Provide gastric lavage if emesis is contraindicated.

Phenylpropanolamine

About Phenylpropanolamine
Alfa-and Beta-adrenergic agonist, Phenethylamine derivative, a stimulant, decongestant,anorectic.
Mechanism of Action of Phenylpropanolamine
It is a mixed acting sympathomimetic amine with predominant alpha adrenergic agonistic action. It exerts nasal decongestant action by acting through alpha adrenergic receptors in the respiratory tract mucosa; and produces vasoconstriction. It temporarily reduces the swelling associated with inflammation of nasal mucosa.
Phenylpropanolamine also suppresses the appetite control center in the hypothalamus

Pharmacokinets of Phenylpropanolamine
Absorption: Well absorbed orally, Metabolism: Metabolized in to an active metabolite in liver, Excretion: Excreted mainly through urine.
Onset of Action for Phenylpropanolamine
15 to 30 minutes
Duration of Action for Phenylpropanolamine
3 hours
Half Life of Phenylpropanolamine
N/A
Side Effects of Phenylpropanolamine
1. Hypertension
2. Stroke
3. Arrhythmias
4. Renal failure
5. Rhabdomyolysis
6. Psychotic disturbances
7. Hallucinations
8. Seizures
Contra-indications of Phenylpropanolamine
1. Hypersensitivity to Phenylpropanolamine or other sympathomimetics
2. Coronary artery disease
3. Hypertension
4. Arteriosclerosis
5. Depression
6. Angle-closure glaucoma
7. Diabetes
8. Renal impairment
9. Hyperthyroidism
10. During or within 14 days of use of MAO inhibitors
11. Use as an anorexiant for children less than 12 years of age
12. Sustained-release forms during lactation and in children less than 12 years of age
Special Precautions while taking Phenylpropanolamine
1. Cardiovascular disorders
2. Mild Hypertension
3. Prostatic hypertrophy
4. Psychosis or other psychiatric disorders (Phenylpropanolamine may precipitate psychiatric disorders)
5. Not drinking large amounts of caffeine-containing beverages, such as coffee, tea, or colas
6. Do not engage in driving, using machines, or doing anything else that requires mental alertness while taking medication
7. Inform the physician if cold symptoms do not improve within 7 days or if fever is present
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Indications for Phenylpropanolamine
1. Nasal congestion

Interactions for Phenylpropanolamine
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Typical Dosage for Phenylpropanolamine
Oral:
Adults:
As decongestant: 25mg every four hours or 50mg every 8 hours daily. Not to exceed 150mg/day
Anorexiant: 25mg thrice daily; 30minutes before meals.
Extended release tablets or capsules:As decongestant: 75mg twice daily
Anorexiant: 75mg once daily in the morning.
As decongestant:
Children (6 to 12 years): 12.5mg up to every four hours. Not to exceed 75mg/day
Children (2 to 6years): 6.25mg up to every four hours. Not to exceed 37.5mg/day

Schedule of Phenylpropanolamine
H
Storage Requirements for Phenylpropanolamine
Store 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 Phenylpropanolamine
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 Phenylpropanolamine
Provide symptomatic treatment and supportive measures.Remove drug from the body by induced emesis or gastric lavage. Barbiturate sedatives are sometimes used to control excessive CNS stimulation. Monitor Cardiovascular and respiratory functions. Administer intravenous fluids to control hypotension. Correct hypertension with Intravenous phentolamine or nitrates. Perform forced diuresis by acidification of urine.

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