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PHARMACODYNAMICS:
Cefuroxime axetil undergoes hydrolysis by esterase enzymes to the active antibiotic, cefuroxime. Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
PHARMACOKINETICS:
After oral administration cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation. Optimum absorption occurs when it is administered shortly after a meal.
The rate of absorption of cefuroxime from the suspension is reduced compared with the tablets, leading to later, lower peak serum levels and reduced systemic bioavailability (4 to 17% less). Cefuroxime axetil oral suspension is not bioequivalent to cefuroxime axetil tablets, and therefore is not substitutable on a milligram-per-milligram basis.
Following administration of cefuroxime axetil tablets peak serum levels occur approximately 2.4 hours after dosing when taken with food.
Protein binding has been stated as 33 to 50% depending on the methodology used. Cefuroxime passes the blood-brain barrier when the meninges are inflamed. Cefuroxime is not metabolised. The serum half-life is between 1 and 1.5 hours. Cefuroxime is effectively removed by dialysis.
INDICATIONS:
Cefuroxime is indicated for the treatment of the infections listed below in adults and children from the age of 3 months.
CONTRAINDICATIONS:
Cefuroxime is contraindicated in patients with a known allergy to the cephalosporin group of antibiotics.
It is also contraindicated in patients with a history of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
SIDE EFFECTS:
The most common adverse reactions are Candida overgrowth, eosinophilia, headache, dizziness, gastrointestinal disturbances and transient rise in liver enzymes.
WARNINGS & PRECAUTIONS:
Hypersensitivity reactions: Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactam antibiotics because there is a risk of cross-sensitivity. As with all beta-lactam antibacterial agents, serious and occasionally fatal hypersensitivity reactions have been reported. In case of severe hypersensitivity reactions, treatment with cefuroxime must be discontinued immediately and adequate emergency measures must be initiated.
Overgrowth of non-susceptible microorganisms: As with other antibiotics, use of cefuroxime axetil may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of other non-susceptible microorganisms (e.g. enterococci and Clostridium difficile), which may require interruption of treatment. Antibacterial agent–associated pseudomembranous colitis have been reported with nearly all antibacterial agents, including cefuroxime and may range in severity from mild to life threatening. This diagnosis should be considered in patients with diarrhoea during or subsequent to the administration of cefuroxime. Discontinuation of therapy with cefuroxime and the administration of specific treatment for Clostridium difficile should be considered.
Interference with diagnostic tests: It is recommended that either the glucose oxidase or hexokinase methods are used to determine blood/plasma glucose levels in patients receiving cefuroxime axetil.
Pregnancy:
There are limited data from the use of cefuroxime in pregnant women. Cefuroxime-MP should be prescribed to pregnant women only if the benefit outweighs the risk.
Breastfeeding:
Cefuroxime is excreted in human milk in small quantities. Adverse effects at therapeutic doses are not expected, although a risk of diarrhoea and fungus infection of the mucous membranes cannot be excluded. Breastfeeding might have to be discontinued due to these effects. Cefuroxime should only be used during breastfeeding after benefit/risk assessment by the physician.
Effect on driving and operating machines:
As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
DRUG INTERACTIONS:
Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil compared with that of the fasting state and tend to cancel the effect of enhanced absorption after food.
Cefuroxime axetil may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives.
Concomitant use with oral anticoagulants may give rise to increased INR.
DOSAGE AND METHOD OF ADMINISTRATION:
For optimal absorption cefuroxime axetil suspension should be taken with food.
Administer cefuroxime tablets with or without food.
The usual course of therapy is seven days (may range from five to ten days).
Adults and children (13 years and older) ( ≥ 40 kg )
Indication | Dosage |
Acute tonsillitis and pharyngitis, acute bacterial sinusitis | 250 mg twice daily |
Acute otitis media | 500 mg twice daily |
Acute exacerbations of chronic bronchitis | 500 mg twice daily |
Uncomplicated urinary tract infections( Cystitis) | 250 mg twice daily |
Pyelonephritis | 250 mg twice daily |
Uncomplicated skin and soft tissue infections | 250 or 500 mg twice daily |
Lyme disease | 500 mg twice daily for 14 days (range of 10 to 21 days) |
Uncomplicated gonorrhea | 1,000 mg as a single dose |
Children(3 months to 12 years) (<40 kg)
Indication | Dosage |
Acute tonsillitis and pharyngitis | 10 mg/kg twice daily to a maximum of 500 mg for 10 days |
acute bacterial sinusitis | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Acute bacterial otitis media | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Cystitis | 15 mg/kg twice daily to a maximum of 250 mg twice daily |
Pyelonephritis | 15 mg/kg twice daily to a maximum of 250 mg twice daily for 10 to 14 days |
Uncomplicated skin and soft tissue infections | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Lyme disease | 15 mg/kg twice daily to a maximum of 250 mg twice daily for 14 days (10 to 21 days) |
Impetigo | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
There is no experience of using Cefuroxime in children under the age of 3 months.
In infants (from the age of 3 months) and children with a body mass of less than 40 kg, it may be preferable to adjust dosage according to weight or age. The dose in infants and children 3 months to 18 years is 10 mg/kg twice daily for most infections, to a maximum of 250 mg daily. In otitis media or more severe infections the recommended dose is 15 mg/kg twice daily to a maximum of 500 mg daily.
Renal impairment:
Cefuroxime is primarily excreted by the kidneys. In patients with markedly impaired renal function it is recommended that the dosage of cefuroxime should be reduced to compensate for its slower excretion. Elderly patients are more likely to have decreased renal function; therefore, the dose should be adjusted in accordance with the renal function in the elderly. Cefuroxime is effectively removed by dialysis.
Recommended doses for Cefuroxime Granules for Oral Suspension in renal impairment
Creatinine clearance | T1/2 (hrs) | Recommended dosage |
≥ 30 ml/min/1.73 m2 | 1.4 – 2.4 | no dose adjustment necessary (standard dose of 125 mg to 500 mg given twice daily) |
10 – 29 ml/min/1.73 m2 | 4.6 | standard individual dose given every 24 hours |
<10 ml/min/1.73 m2 | 16.8 | standard individual dose given every 48 hours |
Patients on haemodialysis | 2 – 4 | a further standard individual dose should be given at the end of each dialysis |
Directions for Mixing Cefuroxime Granules for Oral Suspension:
Prepare a suspension at the time of dispensing as follows: Shake the bottle to loosen the powder, add water for reconstitution (37 ml for CEFUROXIME 125 mg, and 19 ml for CEFUROXIME 250 mg) and replace the cap. Invert the bottle and vigorously shake the bottle.
OVERDOSAGE:
Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can occur if the dose is not reduced appropriately in patients with renal impairment. Serum levels of cefuroxime can be reduced by haemodialysis and peritoneal dialysis.
Packing:
Oral Suspension: Each box contains amber glass bottles 60ml or 100 ml.
tablets: Each box contains 20 tablets.
Storage:
oral Suspension: Before reconstitution, store dry powder between 2° and 30°C. Store the reconstituted suspension between 2° and 8°C (in a refrigerator). Discard after 10 days.
tablets: Store the tablets in a room temperature ( 15 – 30 C) °.
PHARMACODYNAMICS:
Cefuroxime axetil undergoes hydrolysis by esterase enzymes to the active antibiotic, cefuroxime. Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
PHARMACOKINETICS:
After oral administration cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation. Optimum absorption occurs when it is administered shortly after a meal.
The rate of absorption of cefuroxime from the suspension is reduced compared with the tablets, leading to later, lower peak serum levels and reduced systemic bioavailability (4 to 17% less). Cefuroxime axetil oral suspension is not bioequivalent to cefuroxime axetil tablets, and therefore is not substitutable on a milligram-per-milligram basis.
Following administration of cefuroxime axetil tablets peak serum levels occur approximately 2.4 hours after dosing when taken with food.
Protein binding has been stated as 33 to 50% depending on the methodology used. Cefuroxime passes the blood-brain barrier when the meninges are inflamed. Cefuroxime is not metabolised. The serum half-life is between 1 and 1.5 hours. Cefuroxime is effectively removed by dialysis.
INDICATIONS:
Cefuroxime is indicated for the treatment of the infections listed below in adults and children from the age of 3 months.
CONTRAINDICATIONS:
Cefuroxime is contraindicated in patients with a known allergy to the cephalosporin group of antibiotics.
It is also contraindicated in patients with a history of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
SIDE EFFECTS:
The most common adverse reactions are Candida overgrowth, eosinophilia, headache, dizziness, gastrointestinal disturbances and transient rise in liver enzymes.
WARNINGS & PRECAUTIONS:
Hypersensitivity reactions: Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactam antibiotics because there is a risk of cross-sensitivity. As with all beta-lactam antibacterial agents, serious and occasionally fatal hypersensitivity reactions have been reported. In case of severe hypersensitivity reactions, treatment with cefuroxime must be discontinued immediately and adequate emergency measures must be initiated.
Overgrowth of non-susceptible microorganisms: As with other antibiotics, use of cefuroxime axetil may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of other non-susceptible microorganisms (e.g. enterococci and Clostridium difficile), which may require interruption of treatment. Antibacterial agent–associated pseudomembranous colitis have been reported with nearly all antibacterial agents, including cefuroxime and may range in severity from mild to life threatening. This diagnosis should be considered in patients with diarrhoea during or subsequent to the administration of cefuroxime. Discontinuation of therapy with cefuroxime and the administration of specific treatment for Clostridium difficile should be considered.
Interference with diagnostic tests: It is recommended that either the glucose oxidase or hexokinase methods are used to determine blood/plasma glucose levels in patients receiving cefuroxime axetil.
Pregnancy:
There are limited data from the use of cefuroxime in pregnant women. Cefuroxime-MP should be prescribed to pregnant women only if the benefit outweighs the risk.
Breastfeeding:
Cefuroxime is excreted in human milk in small quantities. Adverse effects at therapeutic doses are not expected, although a risk of diarrhoea and fungus infection of the mucous membranes cannot be excluded. Breastfeeding might have to be discontinued due to these effects. Cefuroxime should only be used during breastfeeding after benefit/risk assessment by the physician.
Effect on driving and operating machines:
As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
DRUG INTERACTIONS:
Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil compared with that of the fasting state and tend to cancel the effect of enhanced absorption after food.
Cefuroxime axetil may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives.
Concomitant use with oral anticoagulants may give rise to increased INR.
DOSAGE AND METHOD OF ADMINISTRATION:
For optimal absorption cefuroxime axetil suspension should be taken with food.
Administer cefuroxime tablets with or without food.
The usual course of therapy is seven days (may range from five to ten days).
Adults and children (13 years and older) ( ≥ 40 kg )
Indication | Dosage |
Acute tonsillitis and pharyngitis, acute bacterial sinusitis | 250 mg twice daily |
Acute otitis media | 500 mg twice daily |
Acute exacerbations of chronic bronchitis | 500 mg twice daily |
Uncomplicated urinary tract infections( Cystitis) | 250 mg twice daily |
Pyelonephritis | 250 mg twice daily |
Uncomplicated skin and soft tissue infections | 250 or 500 mg twice daily |
Lyme disease | 500 mg twice daily for 14 days (range of 10 to 21 days) |
Uncomplicated gonorrhea | 1,000 mg as a single dose |
Children(3 months to 12 years) (<40 kg)
Indication | Dosage |
Acute tonsillitis and pharyngitis | 10 mg/kg twice daily to a maximum of 500 mg for 10 days |
acute bacterial sinusitis | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Acute bacterial otitis media | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Cystitis | 15 mg/kg twice daily to a maximum of 250 mg twice daily |
Pyelonephritis | 15 mg/kg twice daily to a maximum of 250 mg twice daily for 10 to 14 days |
Uncomplicated skin and soft tissue infections | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
Lyme disease | 15 mg/kg twice daily to a maximum of 250 mg twice daily for 14 days (10 to 21 days) |
Impetigo | 15 mg/kg twice daily to a maximum of 1000 mg for 10 days |
There is no experience of using Cefuroxime in children under the age of 3 months.
In infants (from the age of 3 months) and children with a body mass of less than 40 kg, it may be preferable to adjust dosage according to weight or age. The dose in infants and children 3 months to 18 years is 10 mg/kg twice daily for most infections, to a maximum of 250 mg daily. In otitis media or more severe infections the recommended dose is 15 mg/kg twice daily to a maximum of 500 mg daily.
Renal impairment:
Cefuroxime is primarily excreted by the kidneys. In patients with markedly impaired renal function it is recommended that the dosage of cefuroxime should be reduced to compensate for its slower excretion. Elderly patients are more likely to have decreased renal function; therefore, the dose should be adjusted in accordance with the renal function in the elderly. Cefuroxime is effectively removed by dialysis.
Recommended doses for Cefuroxime Granules for Oral Suspension in renal impairment
Creatinine clearance | T1/2 (hrs) | Recommended dosage |
≥ 30 ml/min/1.73 m2 | 1.4 – 2.4 | no dose adjustment necessary (standard dose of 125 mg to 500 mg given twice daily) |
10 – 29 ml/min/1.73 m2 | 4.6 | standard individual dose given every 24 hours |
<10 ml/min/1.73 m2 | 16.8 | standard individual dose given every 48 hours |
Patients on haemodialysis | 2 – 4 | a further standard individual dose should be given at the end of each dialysis |
Directions for Mixing Cefuroxime Granules for Oral Suspension:
Prepare a suspension at the time of dispensing as follows: Shake the bottle to loosen the powder, add water for reconstitution (37 ml for CEFUROXIME 125 mg, and 19 ml for CEFUROXIME 250 mg) and replace the cap. Invert the bottle and vigorously shake the bottle.
OVERDOSAGE:
Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can occur if the dose is not reduced appropriately in patients with renal impairment. Serum levels of cefuroxime can be reduced by haemodialysis and peritoneal dialysis.
Packing:
Oral Suspension: Each box contains amber glass bottles 60ml or 100 ml.
tablets: Each box contains 20 tablets.
Storage:
oral Suspension: Before reconstitution, store dry powder between 2° and 30°C. Store the reconstituted suspension between 2° and 8°C (in a refrigerator). Discard after 10 days.
tablets: Store the tablets in a room temperature ( 15 – 30 C) °.
Composition:
Each ampoule (1 ml ) contains Adrenaline ……………. 1 mg.
Pharmacological Properties:
Adrenaline ( Epinephrine ) is a direct acting sympathomimetic agent, with marked effect on beta-adrenoreceptors than on alpha-adrenoreceptors, its actions vary considerably according to the dose given, and the consequent reflex compensating responses of the body. In practice, major effects of adrenaline include increased speed and force of cardiac contraction (with lowered doses this causes increased systolic pressure yet reduced diastolic pressure since overall peripheral resistance is lowered, but with higher doses both systolic and diastolic pressure are increased as stimulation of peripheral alpha-receptors increases peripheral resistance); blood flow to skeletal muscle is increased ( reduced with higher doses).
Metabolic effects include increased oxygen consumption, blood flow in the kidneys, mucosa, and skin is reduced; there is a little direct effect on cerebral blood flow.
The strong vasoconstrictor actions of adrenaline acts quickly to counter vasodilatation and resulting increased capillary permeability. By its effect on smooth muscle, adrenaline relaxes the bronchioles, thereby relieving wheezing and dyspnoea. Its action also relieves angioedema or hives (urticaria).
Indications:
– In general, the most common uses of Adrenaline are to relieve respiratory distress due to bronchospasm, to provide rapid relief of hypersensitivity reactions to drugs and other allergens, and to prolong the action of infiltration anaesthetics.
– Adrenaline is used in cardiopulmonary resuscitation, and its cardiac effects may be of use in restoring cardiac rhythm in cardiac arrest due to various causes and it is similarly indicated for cardiovascular resuscitation procedures, specially in cardiac failure, or in hemorrhagic, or cardiogenic shock, although very hazardous.
– Adrenaline is used as a hemostatic agent. To relieve bronchial asthmatic paroxysms; or symptomatic relief of serum sickness, urticaria, angioneurotic edema; for resuscitation in cardiac arrest following anaesthetic accidents.
– Adrenalin can be utilized to prolong the action of intraspinal and local anaesthetics.
– Major clinical application of Adrenaline include the emergency management of severe allergic reactions (type 1)( anaphylaxis) to hymenoptera stings, foods, and anaphylatic shock to drugs and other allergens.
– In ventricular fibrillation, Adrenaline is the first pharmacological agent to be used if three attempts of electro defibrillation failed.
Contra Indications:
– Narrow angle glaucoma. – Brain damage.
– Pheochromocytoma – Prostatomegaly.
– Severe renal failure. – Coronary insufficiency.
– Adrenaline should not be used in cardiac failure or in haemorrhagic, traumatic, or cardiogenic shock.
Precautions:
– Adrenaline should be administered with extreme caution to patients who have developed ischaemic heart disease.
-Use of Adrenaline with drugs that sensitize the heart to arrhythmias is not recommended.
– Anginal pain may be induced by Adrenaline in patients with coronary insufficiency.
– Administer with caution to hyperthyroid individuals, psychoneurotic individuals, subjects with cardiovascular disease, hypertension, or diabetes, elderly individuals, pregnant women, and children under 30 kg (66 Lbs ) body weight.
– Great care is also needed in patients with arrhythmia or tachycardia, occlusive vascular disorders including arteriosclerosis, or aneurysms.
– Sympathomimetics should be avoided or used with cation in patients undergoing anaesthesia with cyclopropane, halothane, or other halogenated anasthetics, as they may induce ventricular fibrillation.
Pregnancy (Category C) : There are no adequate and well-controlled studies in pregnant women. However, Adrenaline should be used during pregnancy only if potential benefits justifies the potential risks to the fetus.
Pediatric Use : Safety and effectiveness in children has not been established.
Drug Interactions:
Many sympathomimetic drugs interact with monoamine oxidase inhibitors, and should not be given to patients receiving such treatment, or within 14 days of its termination.
– An increased risk of arrhythmias may also occur if sympathomimetic agents are given to patients receiving cardiac glycosides, quinidine, or tricyclic antidepressants.
– Use of Adrenaline with excessive doses of digitalis, diuretics, or other drugs that sensitize the heart to arrhythmias is not recommended.
– The effect of Adrenaline may be potentiated by tricyclic antidepressants, certain antihistamines e.g. Diphenhydramine, tripelennamine, and sodium L-thyroxine.
Side Effects:
– Use of Adrenaline ( Epinephrine) injection may cause transient and minor side effects include anxiety, headache, respiratory difficulty, pallor, dizziness, weakness, tremor, throbbing, restlessness, tenseness, fear and palpitation often occur with therapeutic doses, especially in hyperthyroid individuals.
– Repeated local injection can result in necrosis at sites of injection from vascular constriction.
Dosage And Administration:
Subcutaneously or Intramuscularly : 0.2 to 1 ml ( mg) start with small dose and increase if required.
– For bronchial asthma and certain allergic manifestations: Including angioedema, urticaria, serum sickness, anaphylactic shock, use Adrenaline subctuaneously. The adult dose (100-500mg) (0.1 to 0.5 ml) of a 1 in 1000 aqueous solution. Children have received 0.01 mg/kg body weight (10 mg per kg) to a maximum total dose of 0.5 ml (500 mg) administered subcutaneously, repeated every four hours if required.
– For cardiac resuscitation:
* A dose of 0.5 ml (0.5 mg) diluted to 10 ml with sodium chloride injection can be administered intravenously or intracardially to restore myocardial contractility.
* External cardiac massage should follow intracardial administration to permit the drug to enter coronary circulation. The drug should be used secondarily to unsuccessful attempt with physical or electromechanical methods.
– In ventricular fibrillation: 1 mg administerd intravenously, if an intravenous line can not be established a dose of 2 mg via an endotrachial tube can be considered.
In ophthalmic use: ( for producing conjuctival decongestions, to control hemorrhage, produce mydriasis and reduce intraocular pressure). Use a concentration of 1 : 10.000 (0.1 mg/ml) to 1 : 1.000 ( 1 mg/ml ).
Note:
– Adrenaline injection should be protected from exposure to light.
– Do not remove ampoules or vials from carton until ready to use.
Packing: Box containing ( 5-100) ampoules x 1 ml.
Storage: store between (15-30)° C , protect from light and freezing.
Composition:
Each ampoule (1 ml ) contains Adrenaline ……………. 1 mg.
Pharmacological Properties:
Adrenaline ( Epinephrine ) is a direct acting sympathomimetic agent, with marked effect on beta-adrenoreceptors than on alpha-adrenoreceptors, its actions vary considerably according to the dose given, and the consequent reflex compensating responses of the body. In practice, major effects of adrenaline include increased speed and force of cardiac contraction (with lowered doses this causes increased systolic pressure yet reduced diastolic pressure since overall peripheral resistance is lowered, but with higher doses both systolic and diastolic pressure are increased as stimulation of peripheral alpha-receptors increases peripheral resistance); blood flow to skeletal muscle is increased ( reduced with higher doses).
Metabolic effects include increased oxygen consumption, blood flow in the kidneys, mucosa, and skin is reduced; there is a little direct effect on cerebral blood flow.
The strong vasoconstrictor actions of adrenaline acts quickly to counter vasodilatation and resulting increased capillary permeability. By its effect on smooth muscle, adrenaline relaxes the bronchioles, thereby relieving wheezing and dyspnoea. Its action also relieves angioedema or hives (urticaria).
Indications:
– In general, the most common uses of Adrenaline are to relieve respiratory distress due to bronchospasm, to provide rapid relief of hypersensitivity reactions to drugs and other allergens, and to prolong the action of infiltration anaesthetics.
– Adrenaline is used in cardiopulmonary resuscitation, and its cardiac effects may be of use in restoring cardiac rhythm in cardiac arrest due to various causes and it is similarly indicated for cardiovascular resuscitation procedures, specially in cardiac failure, or in hemorrhagic, or cardiogenic shock, although very hazardous.
– Adrenaline is used as a hemostatic agent. To relieve bronchial asthmatic paroxysms; or symptomatic relief of serum sickness, urticaria, angioneurotic edema; for resuscitation in cardiac arrest following anaesthetic accidents.
– Adrenalin can be utilized to prolong the action of intraspinal and local anaesthetics.
– Major clinical application of Adrenaline include the emergency management of severe allergic reactions (type 1)( anaphylaxis) to hymenoptera stings, foods, and anaphylatic shock to drugs and other allergens.
– In ventricular fibrillation, Adrenaline is the first pharmacological agent to be used if three attempts of electro defibrillation failed.
Contra Indications:
– Narrow angle glaucoma. – Brain damage.
– Pheochromocytoma – Prostatomegaly.
– Severe renal failure. – Coronary insufficiency.
– Adrenaline should not be used in cardiac failure or in haemorrhagic, traumatic, or cardiogenic shock.
Precautions:
– Adrenaline should be administered with extreme caution to patients who have developed ischaemic heart disease.
-Use of Adrenaline with drugs that sensitize the heart to arrhythmias is not recommended.
– Anginal pain may be induced by Adrenaline in patients with coronary insufficiency.
– Administer with caution to hyperthyroid individuals, psychoneurotic individuals, subjects with cardiovascular disease, hypertension, or diabetes, elderly individuals, pregnant women, and children under 30 kg (66 Lbs ) body weight.
– Great care is also needed in patients with arrhythmia or tachycardia, occlusive vascular disorders including arteriosclerosis, or aneurysms.
– Sympathomimetics should be avoided or used with cation in patients undergoing anaesthesia with cyclopropane, halothane, or other halogenated anasthetics, as they may induce ventricular fibrillation.
Pregnancy (Category C) : There are no adequate and well-controlled studies in pregnant women. However, Adrenaline should be used during pregnancy only if potential benefits justifies the potential risks to the fetus.
Pediatric Use : Safety and effectiveness in children has not been established.
Drug Interactions:
Many sympathomimetic drugs interact with monoamine oxidase inhibitors, and should not be given to patients receiving such treatment, or within 14 days of its termination.
– An increased risk of arrhythmias may also occur if sympathomimetic agents are given to patients receiving cardiac glycosides, quinidine, or tricyclic antidepressants.
– Use of Adrenaline with excessive doses of digitalis, diuretics, or other drugs that sensitize the heart to arrhythmias is not recommended.
– The effect of Adrenaline may be potentiated by tricyclic antidepressants, certain antihistamines e.g. Diphenhydramine, tripelennamine, and sodium L-thyroxine.
Side Effects:
– Use of Adrenaline ( Epinephrine) injection may cause transient and minor side effects include anxiety, headache, respiratory difficulty, pallor, dizziness, weakness, tremor, throbbing, restlessness, tenseness, fear and palpitation often occur with therapeutic doses, especially in hyperthyroid individuals.
– Repeated local injection can result in necrosis at sites of injection from vascular constriction.
Dosage And Administration:
Subcutaneously or Intramuscularly : 0.2 to 1 ml ( mg) start with small dose and increase if required.
– For bronchial asthma and certain allergic manifestations: Including angioedema, urticaria, serum sickness, anaphylactic shock, use Adrenaline subctuaneously. The adult dose (100-500mg) (0.1 to 0.5 ml) of a 1 in 1000 aqueous solution. Children have received 0.01 mg/kg body weight (10 mg per kg) to a maximum total dose of 0.5 ml (500 mg) administered subcutaneously, repeated every four hours if required.
– For cardiac resuscitation:
* A dose of 0.5 ml (0.5 mg) diluted to 10 ml with sodium chloride injection can be administered intravenously or intracardially to restore myocardial contractility.
* External cardiac massage should follow intracardial administration to permit the drug to enter coronary circulation. The drug should be used secondarily to unsuccessful attempt with physical or electromechanical methods.
– In ventricular fibrillation: 1 mg administerd intravenously, if an intravenous line can not be established a dose of 2 mg via an endotrachial tube can be considered.
In ophthalmic use: ( for producing conjuctival decongestions, to control hemorrhage, produce mydriasis and reduce intraocular pressure). Use a concentration of 1 : 10.000 (0.1 mg/ml) to 1 : 1.000 ( 1 mg/ml ).
Note:
– Adrenaline injection should be protected from exposure to light.
– Do not remove ampoules or vials from carton until ready to use.
Packing: Box containing ( 5-100) ampoules x 1 ml.
Storage: store between (15-30)° C , protect from light and freezing.