Aminophylline + Ephedrine + Phenobarbitone Pharmacology

Aminophylline + Ephedrine + Phenobarbitone

About Aminophylline + Ephedrine + Phenobarbitone
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Mechanism of Action of Aminophylline + Ephedrine + Phenobarbitone
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Pharmacokinets of Aminophylline + Ephedrine + Phenobarbitone
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Onset of Action for Aminophylline + Ephedrine + Phenobarbitone
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Duration of Action for Aminophylline + Ephedrine + Phenobarbitone
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Half Life of Aminophylline + Ephedrine + Phenobarbitone
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Side Effects of Aminophylline + Ephedrine + Phenobarbitone
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Contra-indications of Aminophylline + Ephedrine + Phenobarbitone
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Special Precautions while taking Aminophylline + Ephedrine + Phenobarbitone
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Pregnancy Related Information
Contraindicated; Ephedrine is contraindicated in pregnancy, so the combination generic cannot be used in pregnant women
Old Age Related Information
N/A
Breast Feeding Related Information
Ephedrine and Phenobarbitone are contraindicated in breast feeding mother so the combination generic cannot be used in lactation.
Children Related Information
N/A
Indications for Aminophylline + Ephedrine + Phenobarbitone
1.Breathing problem associated with asthma, emphysema, bronchitis
Interactions for Aminophylline + Ephedrine + Phenobarbitone
N/A
Typical Dosage for Aminophylline + Ephedrine + Phenobarbitone
Adult: 1 - 2 tablet 3 times daily
Schedule of Aminophylline + Ephedrine + Phenobarbitone
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Storage Requirements for Aminophylline + Ephedrine + Phenobarbitone
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Effects of Missed Dosage of Aminophylline + Ephedrine + Phenobarbitone
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Effects of Overdose of Aminophylline + Ephedrine + Phenobarbitone
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Aminophylline

About Aminophylline
Theophylline Ethylenediamine, Bronchodilator.
Mechanism of Action of Aminophylline
Aminophylline is a complex of Theophylline and Ethylenediamine. Aminophylline is converted to Theophylline in aqueous solution and this Theophylline exerts therapeutic effect by inhibiting phosphodiesterase enzyme and blocking adenosine receptors. Inhibition of phosphodiesterase enzyme will dilate the bronchial smooth muscle. Inhibition of cyclic nucleotide phosphodiesterase will lead to accumulation of cyclic AMP and cyclic GMP and increases signal transduction through these pathways. Aminophylline relaxes muscles in lungs and chest to allow more air in, decreases the sensitivity of lungs to allergens and other substances that cause inflammation, and increases the contractions of diaphragm to draw more air into the lungs.
Aminophylline is used to treat the symptoms of asthma, bronchitis, and emphysema
Theophylline is a competitive antagonist at adenosine receptors and produce bronchodilation in asthma patients.
Pharmacokinets of Aminophylline
Absorption: Aminophylline is absorbed well after oral administration.
Distribution: It is distributed to extracellular fluid and all tissues except fatty tissues.
Metabolism: It is initially converted to active Theophylline and then to inactive compounds.
Excretion: It is excreted mainly in urine.
Onset of Action for Aminophylline
Oral: 15 - 60 minutes, IV: 15 minutes
Duration of Action for Aminophylline
N/A
Half Life of Aminophylline
N/A
Side Effects of Aminophylline
1. Nausea
2. Vomiting
3. Diarrhea
4. Abdominal pain
5. Headache
6. Dizziness
7. Insomnia
8. Tremor
9. Anxiety
10. Decreased appetite
11. Weight loss
12. Restlessness
13. Flushing
14. Irritability
15. Nervousness
16. Increased urination
17. Hypotension
Contra-indications of Aminophylline
1. Hypersensitivity to Aminophylline and other Xanthine compounds
2. Epilepsy
3. Infection of the rectum or lower colon (rectal suppositories)
Special Precautions while taking Aminophylline
1. Hepatic impairment
2. Renal impairment
3. Heart failure
4. Hypertension
5. Chronic obstructive pulmonary diseases (COPD)
6. Hyperthyroidism
7. Diabetes mellitus
8. Peptic ulcer
9. Severe hypoxemia
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 Aminophylline
1. Bronchospasm,
2. Acute asthma,
3. Respiratory stimulant,
Interactions for Aminophylline
Benzodiazepines: Sedative effects may be antagonized.
Beta agonists: Additive effect.
Halothane: Catecholamine induced arrhythmias may occur.
Tetracyclines: Theophylline adverse reaction may be enhanced.

Typical Dosage for Aminophylline
Adult:
Oral: 100 - 300 mg 6-8 hours daily should be taken after meals.
IV infusion: 5 mg/kg body weight as IV infusion over 20 minutes.
Children:
IV infusion: 5 mg/kg body weight as IV infusion over 20 minutes
Schedule of Aminophylline
H
Storage Requirements for Aminophylline
Store at room temperature. Protect from heat and light.
Effects of Missed Dosage of Aminophylline
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 Aminophylline
Give supportive measures and symptomatic treatment. Drug can be removed from the body by inducing emesis and the absorption of the drug can be reduced by administration of activated charcoal. Arrhythmia can be treated with Lidocaine and seizure with IV benzodiazepines.

Ephedrine

About Ephedrine
Alpha/Beta Adrenergic Agonist , Sympathomimetic amine, Stimulant, vasopressor(parenteral), bronchodilator.
Mechanism of Action of Ephedrine
Ephedrine is a mixed acting sympathomimetic drug which mainly acting indirectly but also has some direct action on alpha and beta adrenergic receptors. It causes release of nor-epinephrine from it`s storage sites and stimulates alpha and beta adrenergic receptors. It relaxes bronchial smooth muscle by stimulating beta-2 adrenergic receptors and thus causes increased vital capacity, relief of mild bronchospasm, improved air exchange and decreased residual volume. Ephedrine produces cardiac stimulation with increased systolic and diastolic pressure when nor-epinephrine stores aren`t depleted. It produces positive inotropic effects with low doses through action on beta-1 receptors in heart. It causes vasodilatation through beta-2 receptors and vasoconstriction through alpha adrenergic receptors. Presser effects results from vasoconstriction, cardiac stimulation, and increased cardiac output. It produces nasal decongestant action by stimulating alpha receptors in blood vessels of nasal mucosa and causing vasoconstriction and nasal decongestion.
Pharmacokinets of Ephedrine
Absorption: Well absorbed after Oral, S.C., or I.M. administration.
Distribution: Widely distributed throughout the body
Metabolism: Slowly metabolized in liver by oxidative deamination, demethylation, aromatic hydroxylation and conjugation.
Excretion: Excreted mainly through urine as unchanged drug.
Onset of Action for Ephedrine
Oral: 15 to 60 minutes
I.V.: 5minutes
I.M., S.C.: 10 to 20 minutes
Duration of Action for Ephedrine
Oral: 3 to 5 hours
I.V.: 60 minutes
I.M.: S.C.: 30 to 60 minutes
Half Life of Ephedrine
N/A
Side Effects of Ephedrine
1. Arrhythmias
2. Palpitations
3. Tachycardia
4. Hypertension
5. Precordial pain
6. Insomnia
7. Nervousness
8. Headahe
9. Dizziness
10. Confusion
11. Euphoria
12. Delirium
13. Mucosal irritation
14. Dry nose and throat
15. Nausea
16. Vomiting
17. Anorexia
18. Urine retention
19. Painful urination
20. Muscle weakness
21. Diaphoresis.
Contra-indications of Ephedrine
1. Hypersensitivity to the drug or other sympathomimetics
2. Severe coronary artery disease
3. Porphyria
4. Arrhythmias
5. Angina pectoris
6. Susstatial organic heart disease
7. Cardiovascular diseases
8. Angle closure glaucoma
9. Psychoneurosis
10. In those taking MAO inhibitors
Special Precautions while taking Ephedrine
1. Hypertension
2. Hyperthyroidism
3. Nervous or excitable states
4. Diabetes
5. Prostatic hyperplasia
6. Diabetes

Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Ephedrine
1. As nasal decongestant
2. As bronchodilator
3. Acute severe bronchospasm
4. Hypotension
5. Enuresis
Interactions for Ephedrine
N/A
Typical Dosage for Ephedrine
Oral:
Adults:
As bronchodilator or nasal decongestant:12.5 to 50mg at every 3 to 4 hours; as required. Do not exceed 150mg in 24 hours.
Orthostatic hypotension: 25mg 1 to 4 times daily as required.
Children:
Above 12 years:12.5 to 50mg at every 3 to 4 hours; as required. Do not exceed 150mg in 24 hours.
Age 6 to 12: 6.25 to 12.5mg every four hours. Do not exceed 75mg in 24 hours.
Children over 2 years: 2 to 3mg/kg/day in 4 to 6 divided doses.
Orthostatic hypotension: 3mg/kg/day divided in to 4 to 6 doses.
Enuresis: 25 to 50mg at bed time.
Nasal spray:
As nasal decongestant:
Adults and children over 12 years: 2 to 3 sprays to each nostril; not more than every four hours.
Children (age 6 to 12): 1 to 2 sprays to each nostril; not more than every four hours.
I.M., S.C., or I.V.:
Acute severe bronchospasm: 12.5 to 25mg I.M., S.C., or I.V.
Hypotension:
Adults: 25 to 50mg S.C. or I.M., or 10 to 25mg as slow I.V. bolus. A second I.M. dose of 50mg or I.V. dose of 25mg is administered if required. Repeat I.V. doses in 5 to 10minutes if required.
Maximum dose: 150mg/day.
Children: 3mg/kg/day S.C. or I.V. divided in to 4 to 6 doses

Schedule of Ephedrine
N/A
Storage Requirements for Ephedrine
Store at controlled room temperature at a range of 15 to 30 degree C. in a well closed container. Protect from light.
Effects of Missed Dosage of Ephedrine
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 Ephedrine
Provide supportive treatment and symptomatic measures. If patient is conscious induce emesis and reduce absorption by administration of activated charcoal. Perform gastric lavage if required. Maintain airway and blood pressure and closely monitor vital signs. Do not administer vasopressors. Beta blockers such as propranolol are used to treat arrhythmias. Use cardio selective beta blockers in asthmatic patients. Treat hypertension with Phentolamine, Seizures with paraldehyde or Diazepam, Pyrexia with seizures.

Phenobarbitone

About Phenobarbitone
Barbiturate derivative, Sedative-Hypnotic,Anticonvulsant.
Mechanism of Action of Phenobarbitone
Sedative and antiepileptic actions: Phenobarbitone mainly acts on Picrotoxin site of GABA -BZD receptor Cl- (chloride ion) channel complex. It prolongs the duration of GABA induced chloride channel opening and produces hyperpolarisation and decreases firing rate of neurons. This will alters the normal body functions. Phenobarbitone also has GABA mimetic action. At high concentrations Phenobarbitone directly increases chloride ion conductance and decreases transmission of calcium ion (Ca2+ ) dependent neurotransmitters. Phenobarbitone also inhibits excitatory glutamate neurotransmitters. At high concentration it also inhibits sodium ion channel and potassium ion channel. Phenobarbitone is used as an antiepileptic to control partial and generalised tonic-clonic seizures.
Barbiturates activate inhibitory GABA-A receptors and inhibit excitatory AMPA receptors and produces CNS depression.


Pharmacokinets of Phenobarbitone
Absorption: It is well absorbed after oral administration. Distribution: It is widely distributed in the body. Metabolism: It is metabolised in the liver. Excretion: It is excreted mainly through urine.
Onset of Action for Phenobarbitone
1 hour
Duration of Action for Phenobarbitone
10 - 12 hour
Half Life of Phenobarbitone
5 - 7 days
Side Effects of Phenobarbitone
1.Hang over
2.Drowsiness
3.Lethargy
4.Somnolence
5.Paradoxical excitement
6.Nausea
7.Vomiting
8.Depression
9.Confusion
10.Headache
11.Nystagmus
12.Ataxia
13.Hypothermia
14.Urticaria
15.Rash
16 Hypotension
17.Exacerbation of Porphyria
18.Dependnce
Contra-indications of Phenobarbitone
1.Hypersensitivity to Phenobarbitone and other barbiturates
2.Porphyria
3.Hepatic impairment
3.Renal impairment
4.Emphysema
5.Obstructive sleeps apnoea
Special Precautions while taking Phenobarbitone
1.Cardiovascular diseases
2.Patient with acute or chronic pain
3.Depression
4. Alcoholics
5. Drug abuse
6. Shock
7. Debilitated patients
8. Driving vehicles, operating machines and people involving any other dangerous activities
9. Slowly withdraw the drug with caution
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Phenobarbitone
1.Anticonvulsant
2.Sedative.
Interactions for Phenobarbitone
Alcohol & other CNS Depressants (other sedatives, hypnotics, anesthetics, antihistamines, tranquilizers, phenothiazines): Additive CNS depression.
Valproic acid: Increases efficacy of barbiturates. Half life of valproic acid may be decreased.
Chloramphenicol: Efficacy of barbiturates increased. Barbiturates may decrease efficacy of chloramphenicol.
MAOIs: Effects of barbiturates prolonged.
Efficacy of the following drugs decreased by barbiturates: Oral anticoagulants, digitoxin, TCAs, corticosteroids, doxycycline, oral contraceptives and estrogens, acetaminophen, beta-blockers, quinidine, rifampicin, theophylline and metronidazole.
Phenytoin: Effect on phenytoin metabolism is unpredictable.
Frusemide: May produce or aggravate orthostatic hypotension.
Griseofulvin: Interferes with absorption of oral griseofulvin leading to decreased blood levels.
Typical Dosage for Phenobarbitone
Adult
Anticonvulsant (Not used for absence and febrile seizure): 60 - 180 mg / day at bed time or 3 divided doses
Sedation: 30 - 120 mg / day in 2 or 3 divided doses
Insomnia: 100 - 200 mg/ day
Maximum dose: 400 mg / day
Children
Anticonvulsant: 1 - 8 mg / kg body weight / day in single dose or 2 divided dose.
Sedation: 8 - 32 mg/ day
Schedule of Phenobarbitone
X DRUG
Storage Requirements for Phenobarbitone
Store at 15 - 25 degree C in a tightly closed container. Keep out of the reach of children.
Effects of Missed Dosage of Phenobarbitone
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.
Effects of Overdose of Phenobarbitone
Give supportive measures and symptomatic treatment. Induce emesis or gastric lavage has to be done. Charcoal can be given to reduce the absorption of the drug. Urine alkalinization also helps to reduce the absorption of the drug. Haemodialysis can be done in severe cases.

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