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- Pharmacology For Theophylline + Ephedrine + Phenobarbitone
Theophylline + Ephedrine + Phenobarbitone Pharmacology
Theophylline + Ephedrine + Phenobarbitone
About Theophylline + Ephedrine + PhenobarbitoneN/AMechanism of Action of Theophylline + Ephedrine + PhenobarbitoneN/APharmacokinets of Theophylline + Ephedrine + PhenobarbitoneN/AOnset of Action for Theophylline + Ephedrine + PhenobarbitoneN/ADuration of Action for Theophylline + Ephedrine + PhenobarbitoneN/AHalf Life of Theophylline + Ephedrine + PhenobarbitoneN/ASide Effects of Theophylline + Ephedrine + PhenobarbitoneN/AContra-indications of Theophylline + Ephedrine + PhenobarbitoneN/ASpecial Precautions while taking Theophylline + Ephedrine + PhenobarbitoneN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Theophylline + Ephedrine + PhenobarbitoneN/AInteractions for Theophylline + Ephedrine + PhenobarbitoneN/ATypical Dosage for Theophylline + Ephedrine + PhenobarbitoneN/ASchedule of Theophylline + Ephedrine + PhenobarbitoneN/AStorage Requirements for Theophylline + Ephedrine + PhenobarbitoneN/AEffects of Missed Dosage of Theophylline + Ephedrine + PhenobarbitoneN/AEffects of Overdose of Theophylline + Ephedrine + PhenobarbitoneN/ATheophylline
About TheophyllineBronchodilator, a methylxanthine derivative, Anti asthma, in COPD.Mechanism of Action of TheophyllineIt inhibit phosphodiesterase enzyme which degrades cyclic nucleotides intracellularly and it results the cyclic AMP accumulation in the cell. This cause bronchodialatation, cardiac stimulation and vasodilatation. This drug release calcium from sarcoplasmic reticulam, especially in cardiac muscles and results increased cardiac muscle contraction. This drug also blocks adenosine receptors (adenosine acts as a local mediator in CNS & CVS and other organs- which contracts smooth muscles, especially in bronchi, blood vessels etc). This results bronchodialatation and vasodialatation.Pharmacokinets of TheophyllineAbsorption- Well absorbed after oral administration. Rapidly and well absorbed after intravenous administration.
Distribution- Widely distributed in the body. 40% bound to the plasma proteins.
Metabolism- Metabolized in the liver by demethylation and oxidation. 1-methyluric acid is its metabolite.
Excretion- Excreted through urine.
Onset of Action for Theophylline15 to 60 min. after oral administration and 15 minutes after intravenous administration.Duration of Action for TheophyllineN/AHalf Life of TheophyllineIts plasma half life is 8 hrsSide Effects of Theophylline1. Upset stomach
2. Stomach pain
3. Diarrhea
4. Headache
5. Restlessness
6. Insomnia
7. Irritability
8. Vomiting
9. Increased or rapid heart rate
10. Irregular heartbeat
11. Seizures
12. Skin rash
Contra-indications of Theophylline1. Hypersensitivity to the drug
2. Peptic ulcer
3. Underlying seizure disorders
Special Precautions while taking Theophylline1. Cardiac disease
2. Hypertension
3. Hyperthyroidism
4. Hepatic impairment
5. Fever
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with cautionIndications for Theophylline1. Asthma
2. Chronic obstructive pulmonary disease
3. Chronic bronchitis
4. Emphysema
5. It can be used in premature infants who stop breathing
Interactions for TheophyllineBenzodiazepines: Sedative effects may be antagonized.
Beta agonists: Additive effect.
Halothane: Catecholamine induced arrhythmias may occur.
Tetracyclines: Theophylline adverse reaction may be enhanced.
Food: Theophylline elimination is increased by a low carbohydrate, high protein diet.
Typical Dosage for TheophyllineAdults:
Long term management of chronic bronchospasm: 300 to 1000 mg daily in divided doses in every 6 to 8 hrs or 175 to 500 mg every 12 hrs for modified release preparations.
Bronchospasm-
Adults-
5mg/kg body weight every 6 to 8 hrs.
Children- 5 mg/kg every 4 to 6 hrs.
Neonatal apnoea of prematurity-
Child-
More than 24days - 5mg/kg as maintenance dose and 1.5mg/kg every 12 hrs as loading dose.
Less than 24 days- 1mg/kg every 12 hrs.
Intravenous- Management of severe bronchospasm-
Adult- 4 to 5 mg/kg as loading dose over 20 to 30 minutes.
0.4 mg/kg/hr as maintenance dose.
Children- 4 to 5 mg/kg as loading dose over 20 to 30 minutes.
0.8mg/kg/hr as maintenance dose.
Schedule of TheophyllineN/AStorage Requirements for TheophyllineStore it at room temperature and away from excess heat and moisture.Effects of Missed Dosage of TheophyllineTake 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 TheophyllineGive symptomatic and supportive treatment. Induce emesis except in convulsive patient. Administer activated charcoal or cathartics to prevent further absorption of the drug.Ephedrine
About EphedrineAlpha/Beta Adrenergic Agonist , Sympathomimetic amine, Stimulant, vasopressor(parenteral), bronchodilator.Mechanism of Action of EphedrineEphedrine 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 EphedrineAbsorption: 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 EphedrineOral: 15 to 60 minutes
I.V.: 5minutes
I.M., S.C.: 10 to 20 minutes
Duration of Action for EphedrineOral: 3 to 5 hours
I.V.: 60 minutes
I.M.: S.C.: 30 to 60 minutes
Half Life of EphedrineN/ASide Effects of Ephedrine1. 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 Ephedrine1. 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 Ephedrine1. Hypertension
2. Hyperthyroidism
3. Nervous or excitable states
4. Diabetes
5. Prostatic hyperplasia
6. Diabetes
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Ephedrine1. As nasal decongestant
2. As bronchodilator
3. Acute severe bronchospasm
4. Hypotension
5. Enuresis
Interactions for EphedrineN/ATypical Dosage for EphedrineOral:
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 EphedrineN/AStorage Requirements for EphedrineStore 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 EphedrineTake 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 EphedrineProvide 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 PhenobarbitoneBarbiturate derivative, Sedative-Hypnotic,Anticonvulsant.Mechanism of Action of PhenobarbitoneSedative 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 PhenobarbitoneAbsorption: 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 Phenobarbitone1 hourDuration of Action for Phenobarbitone10 - 12 hourHalf Life of Phenobarbitone5 - 7 daysSide Effects of Phenobarbitone1.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.DependnceContra-indications of Phenobarbitone1.Hypersensitivity to Phenobarbitone and other barbiturates
2.Porphyria
3.Hepatic impairment
3.Renal impairment
4.Emphysema
5.Obstructive sleeps apnoeaSpecial Precautions while taking Phenobarbitone1.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 InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Phenobarbitone1.Anticonvulsant
2.Sedative.Interactions for PhenobarbitoneAlcohol & 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 PhenobarbitoneAdult
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 PhenobarbitoneX DRUGStorage Requirements for PhenobarbitoneStore at 15 - 25 degree C in a tightly closed container. Keep out of the reach of children.Effects of Missed Dosage of PhenobarbitoneTake 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 PhenobarbitoneGive 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.Home Delivery for Theophylline + Ephedrine + Phenobarbitone in Your City
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Theophylline + Ephedrine + Phenobarbitone is a generic medicine name and there are several brands available for it. Some of the brands for theophylline + ephedrine + phenobarbitone might be better known than theophylline + ephedrine + phenobarbitone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have theophylline + ephedrine + phenobarbitone in stock, you can ask for one of the branded alternatives for theophylline + ephedrine + phenobarbitone.