Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone Pharmacology

Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone

About Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Mechanism of Action of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Pharmacokinets of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Onset of Action for Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Duration of Action for Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Half Life of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Side Effects of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Contra-indications of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Special Precautions while taking Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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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 Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Interactions for Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Typical Dosage for Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Schedule of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Storage Requirements for Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Effects of Missed Dosage of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Effects of Overdose of Theophylline + Ephedrine + Guaiphenesin + Chlorpheniramine Maleate + Phenobarbitone
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Theophylline

About Theophylline
Bronchodilator, a methylxanthine derivative, Anti asthma, in COPD.
Mechanism of Action of Theophylline
It 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 Theophylline
Absorption- 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 Theophylline
15 to 60 min. after oral administration and 15 minutes after intravenous administration.
Duration of Action for Theophylline
N/A
Half Life of Theophylline
Its plasma half life is 8 hrs
Side Effects of Theophylline
1. 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 Theophylline
1. Hypersensitivity to the drug
2. Peptic ulcer
3. Underlying seizure disorders

Special Precautions while taking Theophylline
1. Cardiac disease
2. Hypertension
3. Hyperthyroidism
4. Hepatic impairment
5. Fever
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
Indications for Theophylline
1. Asthma
2. Chronic obstructive pulmonary disease
3. Chronic bronchitis
4. Emphysema
5. It can be used in premature infants who stop breathing

Interactions for Theophylline
Benzodiazepines: 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 Theophylline
Adults:
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 Theophylline
N/A
Storage Requirements for Theophylline
Store it at room temperature and away from excess heat and moisture.
Effects of Missed Dosage of Theophylline
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 Theophylline
Give symptomatic and supportive treatment. Induce emesis except in convulsive patient. Administer activated charcoal or cathartics to prevent further absorption of the drug.

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.

Guaiphenesin

About Guaiphenesin
Propanediol derivative, Expectorant.
Mechanism of Action of Guaiphenesin
Guaiphenesin is an expectorant which after absorption from the gastrointestinal tract secreted by tracheobronchial glands and directly increase bronchial secretion and mucosal ciliary action. It increases respiratory tract fluid by reducing adhesiveness and surface tension, reducing viscosity of the secretions and there by facilitating their removal and clears chest congestion.
Action in local vaginal preparations: Guaiphenesin helps to thin the thick or sticky cervical mucus.

Pharmacokinets of Guaiphenesin
Absorption: Well absorbed orally.Distribution: It is secreted by the tracheobronchial glands.
Metabolism: It is metabolized primarily to Beta-2-methoxyphenoxy-lactic acid. Excretion: It is excreted in the urine.
Onset of Action for Guaiphenesin
N/A
Duration of Action for Guaiphenesin
N/A
Half Life of Guaiphenesin
60 minutes
Side Effects of Guaiphenesin
1. Headache
2. Dizziness
3. Nausea
4. Vomiting
5. Rash
6. Diarrhoea
7. Drowsiness
8. Stomach pain
Contra-indications of Guaiphenesin
1. Hypersensitivity to the drug
2. Chronic or persistent cough associated with chronic lower respiratory tract diseases
3. Asthma
4. Bronchitis
5. Chronic obstructive pulmonary disease (COPD)
6. Emphysema
Special Precautions while taking Guaiphenesin
1. Porphyria
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
May be used
Indications for Guaiphenesin
1. Expectorant
2. Thick or sticky cervical mucus
Interactions for Guaiphenesin
N/A
Typical Dosage for Guaiphenesin
Oral :
Adults and children over 12 years: 100 to 400mg up to 6 times daily as required.Maximum dose: 2.4g/day
Children (age 6 to 11): 100 to 200mg up to 6 times daily as required.Maximum dose: 1.2g/day
Children (age 2 to 5): 50 to 100mg up to 6 times daily as required.Maximum dose: 600mg/day
Extended release:
Adults and children over 12 years: 600 to 1200mg twice daily. Not to exceed 2.4g in 24 hours
Children (age 6 to 12): 600mg twice daily. Not to exceed 1.2g in 24 hours
Children (age 2 to 6): 300mg twice daily. Not to exceed 600mg in 24 hours
Thick or sticky cervical mucus: 200mg 2 to 3 times daily from 4 days prior to ovulation and continue through ovulation day.
Schedule of Guaiphenesin
N/A
Storage Requirements for Guaiphenesin
Store at a temperature below 30 degree C. Keep out of reach of children.
Effects of Missed Dosage of Guaiphenesin
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 Guaiphenesin
Provide symptomatic treatment and supportive measures.

Chlorpheniramine Maleate

About Chlorpheniramine Maleate
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Mechanism of Action of Chlorpheniramine Maleate
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Pharmacokinets of Chlorpheniramine Maleate
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Onset of Action for Chlorpheniramine Maleate
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Duration of Action for Chlorpheniramine Maleate
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Half Life of Chlorpheniramine Maleate
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Side Effects of Chlorpheniramine Maleate
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Contra-indications of Chlorpheniramine Maleate
First Generation alkylamine H1 Antagonist, Antihistamine.
Special Precautions while taking Chlorpheniramine Maleate
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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 Chlorpheniramine Maleate
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Interactions for Chlorpheniramine Maleate
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Typical Dosage for Chlorpheniramine Maleate
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Schedule of Chlorpheniramine Maleate
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Storage Requirements for Chlorpheniramine Maleate
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Effects of Missed Dosage of Chlorpheniramine Maleate
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Effects of Overdose of Chlorpheniramine Maleate
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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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