Asmapax Depot
Asmapax Depot Uses, Dosage, Side Effects, Food Interaction and all others data.
Pseudoephedrine is both an α-and β-adrenergic receptor agonist. It causes vasoconstriction via direct stimulation of α-adrenergic receptors of the respiratory mucosa. It also directly stimulates β-adrenergic receptors causing bronchial relaxation, increased heart rate and contractility.
Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect. This is its main and direct mechanism of action. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors.
Ephedrine is a sympathomimetic amine that activates adrenergic receptors, increasing heart rate and blood pressure, and causing bronchodilation. The therapeutic window is wide as patients can be given doses of 5mg up to 50mg. Patients should be counselled regarding the pressor effects of sympathomimetic amines and the risk of tachyphylaxis.
Phenobarbital is a long-acting barbiturate. It depresses the sensory cortex, reduces motor activity, changes cerebellar function and produces drowsiness, sedation and hypnosis. Its anticonvulsant property is exhibited at high doses.
Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal).
Theophylline is a bronchodilator, structurally classified as a Methylxanthine. Theophylline has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation and suppression of the response of the airways to stimuli. Theophylline also increases the force of contraction of diaphragmatic muscles. The half-life of Theophylline is influenced by a number of known variables. In adult nonsmokers with uncomplicated asthma the half-life ranges from 3 to 9 hours
Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).
Trade Name | Asmapax Depot |
Generic | Theophylline + Ephedrine + Phenobarbital |
Weight | 65mg |
Type | Tablet |
Therapeutic Class | |
Manufacturer | Abbott Healthcare Pvt Ltd |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pseudoephedrine is a decongestant of the mucous membranes of the upper respiratory tract, especially the nasal mucosa, sinuses and eustachian tube. It is used for the symptomatic relief of allergic rhinitis (hay fever), vasomotor rhinitis, the common cold, influenza (flu) and ear congestion caused by ear inflammation or infection. Pseudoephedrine can also be used as a bronchodilator.
Pseudoephedrine is a stereoisomer of Ephedrine with similar but less potent pharmacological activity. It has nasal and bronchial decongestant activity.
Phenobarbital is used as-
- Sedative and hence it relieves anxiety, tension and fear
- Hypnotic and hence it is used for short term insomnia
- Pre-anaesthetics
- Anti-epileptic in epilepsy with Partial seizure or Generalized Tonic-clonic seizure, status epilepticus
- Certain acute convulsive episodes
This is used for the symptomatic treatment of reversible bronchoconstriction associated with bronchial asthma, chronic obstructive pulmonary emphysema, chronic bronchitis and related bronchospastic disorders.
Asmapax Depot is also used to associated treatment for these conditions: Allergic Disorder, Bronchial Asthma, Common Cold, Cough, Depression, Fever, General Anesthesia Induced Hypotension, Headache, Joint Pain, Myasthenia Gravis, Narcolepsy, Nasal Congestion, Rhinorrhoea, Sore Throat, Dry coughAlcohol Withdrawal Syndrome, Anxiety, Febrile Convulsions, Hyperbilirubinemia, Insomnia, Menopausal Symptoms, Partial-Onset Seizures, Withdrawal Symptoms, Generalized seizure, SedationAsthma, Bronchitis, Bronchoconstriction, Bronchospasm, Chronic Obstructive Pulmonary Disease (COPD), Chronic bronchial inflammation, Airway secretion clearance therapy, Bronchodilation
How Asmapax Depot works
Ephedrine is a direct and indirect sympathomimetic amine. Ephedrine activates adrenergic α and β-receptors as well as inhibiting norepinephrine reuptake, and increasing the release of norepinephrine from vesicles in nerve cells. These actions combined lead to larger quantities of norepinephrine present in the synapse, for longer periods of time, increasing stimulation of the sympathetic nervous system. Ephedrine's stimulation of α-1 receptors causes constriction of veins and a rise in blood pressure, stimulation of β-1 adrenergic receptors increase cardiac chronotropy and inotropy, stimulation of β-2 adrenergic receptors causes bronchodilation.
Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
Dosage
Asmapax Depot dosage
As a decongestant and symptomatic treatment for upper respiratory tract infections the recommended dose is:
Adults: 1 tablet every 4 to 6 hours, up to maximum of 240 mg in 24 hours
Children:
- 6-12 years of age: 1/2 tablet every 4 to 6 hours daily
- 2-5 years of age: 1/4 tablet every 4 to 6 hours daily
- Less than 2 years of age: This drug is not advised unless specifically recommended by a physician.
Adults:
- Hypnosis: 100 to 320 mg
- Sedation: 30 to 120 mg/day in 2 to 3 divided doses
- Epilepsy: 60 to 250 mg/day
- Convulsion: 50 to 100 mg/day in 2 to 3 divided doses
- Status epilepticus: IV 10-20 mg/Kg, repeat if needed
Children:
- Preoperative: 1-3 mg/Kg body weight
- Convulsion: 4-6 mg/Kg/day
- Status epilepticus: IV 15-20 mg/Kg over 10-15 minutes
Dosages are adjusted to maintain serum theophylline concentrations that provide optimal relief of symptoms with minimal side effects. Most of the controlled release preparations may be administered every 12 hours in adults while administration every 8 hours may be necessary in some children with markedly rapid hepatic metabolism of theophylline. The recommended dosages for achieving serum theophylline concentrations within the accepted therapeutic range is as follow:
- 1-6 months: 10mg/Kg/day
- 6 months-1 year: 15mg/Kg/day
- 1-9 years: 24mg/Kg/day
- 10-16 years: 18mg/Kg/day
- Adults: 10-15mg/Kg/day
Dilute with most IV infusion soln (e.g. NaCl 0.45% or 0.9%, lactated Ringer's, dextrose 5%, Ringer's).
Side Effects
Serious adverse effects associated with the use of Pseudoephedrine are rare. Symptoms of central nervous system excitation may occur, including sleep disturbances and, rarely, hallucinations have been reported. Skin rashes, with or without irritation, have occasionally been reported.
Drowsiness is the most common side effect. Less common side effects are CNS depression, nervousness, agitation, psychiatric disturbance, lethargy, mental depression, ataxia, nightmares, bradycardia, apnea, nausea, vomiting, constipation, restlessness and confusion in the elderly and hyperkinesia in children.
The following side effects have been observed:
Gastrointestinal: Nausea, vomiting, epigastric pain and diarrhoea.
Central nervous system: Headache, irritability, restlessness, insomnia, muscles twitching.
Cardiovascular: Palpitation, tachycardia, hypotension. circulatory failure.
Respiratory: Tachypnoea.Renal: Potentiation of diuresis.
Others: Alopecia, hyperglycemia, rash etc.
Toxicity
Patients experiencing an overdose of ephedrine will present with rapidly increasing blood pressure. Manage overdose with blood pressure monitoring, and possibly the administration of parenteral antihypertensives. The LD50 in mice after oral administration is 785mg/kg, after intraperitoneal administration if 248mg/kg, and after subcutaneous administration is 425mg/kg.
CNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur.
Symptoms of overdose include seizures, arrhythmias, and GI effects.
Precaution
Although Pseudoephedrine has virtually no pressor effects in normotensive patients, it should be used with caution in patients suffering mild to moderate hypertension. As with other sympathomimetic agents, Pseudoephedrine should be used with caution in patients with hypertension, heart disease, diabetes, hyperthyroidism, elevated intraocular pressure and prostatic enlargement. Caution should be exercised when using the product in the presence of severe hepatic impairment or moderate to severe renal impairment.
Phenobarbital is potentially habit forming if taken over an extended period of time. When being prescribed to overcome insomnia, the drug should not be used for a period longer than two weeks. Caution should be taken in patients who are mentally depressed, have hepatic damage, suicidal tendencies or a history of drug abuse.
Careful consideration is needed for various interacting drugs and physiologic conditions that can alter Theophylline clearance. Dosage adjustment is required prior to initiation of Theophylline therapy, prior to increases in Theophylline dose, and during follow up. The dose of Theophylline selected for initiation of therapy should be low and, if tolerated, increased slowly over a period of time.
Interaction
Phenobarbital can interact with a number of prescription and nonprescription medications including acetaminophen, anticoagulants such as warfarin, chloramphenicol, monoamine oxidase inhibitors (MAOIs), antidepressants, asthma medicine, cold medicine, anti-allergy medicine, sedatives, steroids, tranquilizers, and vitamins. Interactions with these medications can increase the drowsiness caused by phenobarbital.
Allopurinol, cimetidine, norfloxacin, ciprofloxacin, erythromycin, oral contraceptives and propranolol increase serum theophylline levels. Phenytoin, methotrexate and rifampicin lead to decreased serum theophylline levels
Volume of Distribution
Oral ephedrine has an average volume of distribution of 215.6L.
- 0.3 to 0.7 L/kg
Elimination Route
Oral ephedrine reaches an average Cmax of 79.5ng/mL, with a Tmax of 1.81h, and a bioavailability of 88%.
Absorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach.
Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
Half Life
Oral ephedrine has a plasma elimination half life of approximately 6 hours, but there is a large degree of inter-patient variability.
53 to 118 hours (mean 79 hours)
8 hours
Clearance
Oral ephedrine has a clearance of 23.3L/h but there is a high degree of inter-patient variability.
- 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days]
- 0.64 mL/kg/min [Premature neonates, postnatal age 25-57 days]
- 1.7 mL/kg/min [Children 1-4 years]
- 1.6 mL/kg/min [Children 4-12 years]
- 0.9 mL/kg/min [Children 13-15 years]
- 1.4 mL/kg/min [Children 16-17 years]
- 0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics]
- 0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function]
- 0.33 mL/kg/min [Acute pulmonary edema]
- 0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year]
- 0.48 mL/kg/min [COPD with cor pulmonale]
- 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
- 0.31 mL/kg/min [Liver disease cirrhosis]
- 0.35 mL/kg/min [acute hepatitis]
- 0.65 mL/kg/min [cholestasis]
- 0.47 mL/kg/min [Sepsis with multi-organ failure]
- 0.38 mL/kg/min [hypothyroid]
- 0.8 mL/kg/min [hyperthyroid]
Elimination Route
Ephedrine is mainly eliminated in the urine. Approximately 60% is eliminated as the unmetabolized parent compound, 13% as benzoic acid conjugates, and 1% as 1,2-dihydroxypropylbenzene.
Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults.
Pregnancy & Breastfeeding use
Although Pseudoephedrine has been in widespread use for many years without apparent ill consequence, there are no specific data on its use during pregnancy. Caution should therefore be exercised by balancing the potential benefit of treatment to the mother against any possible hazards to the developing foetus. Pseudoephedrine is excreted in breast milk in small amounts but the effect of this on breast-fed infants is not known.
Pregnancy Category D. Phenobarbital can cause potential fetal damage. Their use in pregnancy alone, or in combination with other anticonvulsants, can cause coagulation defects in the newborn infant which may be preventable by the prophylactic administration of Vitamin K to the mother prior to delivery. Phenobarbital is excreted through human milk; so caution should be taken during lactation period.
Pregnancy: It is not known whether Theophylline can cause foetal harm when administered to pregnant woman.Xanthines should be given to a pregnant woman only if clearly needed.
Nursing mother: Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants. Serious adverse effects in the infant are unlikely unless the mother has toxic serum Theophylline concentrations.
Contraindication
Pseudoephedrine is contraindicated in-
- Hypersensitivity of individuals to this drug
- Severe hypertension and coronary artery disease
- Concurrent use of Mono Amine Oxidase Inhibitor (MAOI) drugs
Phenobarbital is contraindicated in patients with acute intermittent porphyria and who have a natural or idiosyncrasy to barbiturates
Hypersensitivity to xanthine derivatives. It is also contraindicated in patients with active peptic ulcer disease and in individuals with underlying seizure disorders (unless receiving appropriate anti-convulsing medication).
Theophylline should not be administered concurrently with other xanthine. Use with caution in patients with hypoxemia, hypertension, or those with history of peptic ulcer. Do not attempt to maintain any dose that is not tolerated.
Special Warning
Debilitated patient: Reduce dose
Renal Impairment: Reduce dose. Severe: Contraindicated
Hepatic Impairment: Reduce dose. Severe: Contraindicated
Acute Overdose
As with other sympathomimetic agents, symptoms of overdosage include irritability, restlessness, tremor, convulsions, palpitations, hypertension and difficulty in micturition. Necessary measures should be taken to maintain and support respiration and control convulsions. Gastric lavage should be performed if indicated. If desired, the elimination of Pseudoephedrine can be accelerated by acid diuresis or by dialysis.
Phenobarbital should not be used more than the dosage guide line. 1 gm Phenobarbital oral dose may cause serious poisoning and 2 gm may cause even death. Over dosage produces severe, persistent depression. Treatment includes artificial respiration, maintenance of fluid balance and antibiotics to prevent pneumonia. Alkalinisation of the urine and forced diuresis or haemodialysis have been used in cases of severe poisoning.
Symptoms may include nausea, vomiting, gastrointestinal irritation, cramps, convulsions, tachycardia & hypotension. The stomach contents should be emptied & supportive measures employed to maintain circulation, respiration & fluid & electrolyte balance. Electrocardiographic monitoring should be carried out & in severe poisoning charcoal haemoperfusion should be used.
Storage Condition
Protect from light, store in cool and dry place. Keep out of reach of children.
Store in a cool and dry place, protect from light and moisture. Keep out of the reach of children
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