Monthly Archives: July 2017

1 Respiratory Stimulants and Pulmonary Surfactants

Respiratory stimulants

Respiratory stimulants (analeptic drugs) have a limited place in the treatment of ventilatory failure in patients with chronic obstructive pulmonary disease. They are effective only when given by intravenous injection or infusion and have a short duration of action. Their use has largely been replaced by ventilatory support including nasal intermittent positive pressure ventilation. However, occasionally when ventilatory support is contra-indicated and in patients with hypercapnic respiratory failure who are becoming drowsy or comatose, respiratory stimulants in the short term may arouse patients sufficiently to co­operate and clear their secretions. Respiratory stimulants can also be harmful in respiratory failure since they stimulate non-respiratory as well as respiratory muscles. They should only be given under expert supervision in hospital and must be combined with active physiotherapy.

DOXAPRAM HYDROCHLORIDE:

Indications: Post-Anesthesia Respiratory Depression, Respiratory Depression, Neonatal Apnea

Contraindications: Acute Asthma Attack, Acutely Decompensated Chronic Heart Failure, Cerebral Edema, Cerebrovascular Accident, Epilepsy, Flail Chest, Head Injury, Neuromuscular Blockade, Paralysis, Pheochromocytoma, Physical Obstruction of Respiratory Tract, Pneumothorax, Pulmonary Fibrosis, Pulmonary

Thromboembolism, Severe Coronary Artery Disease, Severe Uncontrolled Hypertension

Dose and Administration: Postoperative respiratory depression, by intravenous injection over at least 30 seconds, 1–1.5 mg/kg repeated if necessary after intervals of 1 hour or alternatively by intravenous infusion, 2–3 mg/minute adjusted according to response; child not recommended. Acute respiratory failure, by intravenous infusion, 1.5–4 mg/minute adjusted according to response (given concurrently with oxygen and whenever possible monitor with frequent measurement of blood gas tensions); child not recommended.

Pulmonary surfactants

Pulmonary surfactants are used in the management of respiratory distress syndrome (hyaline membrane disease) in neonates and preterm neonates. They may also be given prophylactically to those considered at risk of developing the syndrome. Continuous monitoring is required to avoid hyperoxaemia caused by rapid improvement in arterial oxygen concentration. Pulmonary haemorrhage has been rarely associated with therapy especially in more preterm neonates; obstruction of the endotracheal tube by mucous secretions has also been reported.

BERACTANT:

Indications: treatment of respiratory distress syndrome in preterm neonates over 700 g; prophylaxis of respiratory distress syndrome in preterm neonates less than 32 weeks post-menstrual age.

Contraindications: NO DATA AVAILABLE

Dose and Administration: By endotracheal tube, phospholipid 100 mg/kg equivalent to a volume of 4 mL/kg, preferably within 8 hours of birth; may be repeated within 48 hours at intervals of at least 6 hours for up to 4 doses.

Mucolytics

Mucolytics are prescribed to facilitate expectoration by reducing sputum viscosity. In some patients with chronic obstructive pulmonary disease and a chronic productive cough, mucolytics can reduce exacerbations; mucolytic therapy should be stopped if there is no benefit after a 4-week trial. Steam inhalation with postural drainage is effective in bronchiectasis and in some cases of chronic bronchitis.

Mucolytics should be used with caution in those with a history of peptic ulceration because they may disrupt the gastric mucosal barrier.

CARBOCISTEINE:

Indications: reduction of sputum viscosity

Contraindications: active peptic ulceration

Dose and Administration: Initially 2.25 g daily in divided doses, then 1.5 g daily in divided doses as condition improves; child 2–5 years 62.5–125 mg 4 times daily, 5–12 years 250 mg 3 times daily

AMBROXOL HCL:

Indications: All forms of tracheobronchitis, emphysema with bronchitis pneumoconiosis, chronic inflammatory pulmonary conditions, bronchiectasis, bronchitis with bronchospasm asthma. During acute exacerbations of bronchitis it should be given with the appropriate antibiotic.

Contraindications: There are no absolute contraindications but in patients with gastric ulceration relative caution should be observed.

Dose and Administration:

Adults: daily dose of 30 mg to 120 mg taken in 2 to 3 divided doses.

Children up to 2 years: 7.5MG twice daily.

Children 2 – 5 years: 7.5MG 3 times daily.

Children over 5 years: 15MG 2-3 times daily.

BROMHEXINE HCL:

Indications:

Reduces the viscosity of mucus in the tracheobronchial tree; this is expected to make carriage of mucus up the tracheobronchial tree by the mucociliary clearance mechanism easier, and also to increase ease of expectoration of mucus during coughing.

To assist in control of respiratory disease involving production of excessive tenacious mucus.

Contraindications: There are no absolute contraindications but in patients with gastric ulceration relative caution should be observed.

Dose and Administration:

Adults, 5-10ml 3 times daily.

Children over 8 years 5ml 3 times daily.

Infant’s 1.25ml 3 times daily.

CARBOCISTEINE, PROMETHAZINE:

Indications: it is recommended for the alleviation of unproductive and irritative

coughs in adults and children aged over 1 year.

Contraindications: former or recent agranulocytosis.

Dose and Administration:

Adults 15ml 3-4 times daily.

Infants 5ml 3-4 times daily.

Bronchodilators

Adrenoceptor agonists (Sympathomimetics)

The selective beta2 agonists (selective beta2-adrenoceptor agonists, selective beta2 stimulants) such as salbutamol or terbutaline are the safest and most effective short-acting beta2 agonists for asthma. Less selective beta2 agonists such as orciprenaline should be avoided whenever possible. Adrenaline (epinephrine) (which has both alpha- and beta-adrenoceptor agonist properties) is used in the emergency management of allergic and anaphylactic reactions and in the management of croup.

Salbutamol:

Indications: used to treat asthma, chronic bronchitis, emphysema and to prevent exercise-related asthma.

Contraindications: contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.

Dose and Administration:

By mouth, 4 mg (elderly and sensitive patients initially 2 mg) 3–4 times daily; max. single dose 8 mg; child under 2 years 100 micrograms/kg 4 times daily [unlicensed]; 2–6 years 1–2 mg 3–4 times daily, 6–12 years 2 mg 3–4 times daily By intravenous infusion, initially 5 micrograms/minute, adjusted according to response and heart-rate usually in range 3–20 micrograms/minute, or more if necessary; child 1 month–18 years initially 1–5 micrograms/kg/minute, adjusted according to response and heart rate (doses above 2 micrograms/kg/minute in intensive care setting). By aerosol inhalation, 100–200 micrograms (1–2 puffs); for persistent symptoms up to 4 times daily (but see also Chronic Asthma table); child 100 micrograms (1 puff), increased to 200 micrograms (2 puffs) if necessary; for persistent symptoms up to 4 times daily. Prophylaxis in exercise-induced bronchospasm, 200 micrograms (2 puffs); child 100 micrograms (1 puff), increased to 200 micrograms (2 puffs) if necessary. By inhalation of nebulised solution, chronic bronchospasm unresponsive to conventional therapy and severe acute asthma, adult and child over 18 months 2.5–5 mg, repeated up to 4 times daily; more frequently in severe cases; max. 40 mg daily; child under 18 months, [unlicensed] (transient hypoxaemia may occur—consider supplemental oxygen), 2.5 mg up to 4 times daily or more frequently in severe cases

 

Terbutalin:

Indications: asthma and other conditions associated with reversible airways obstruction.

Contraindications: Chronic Coronary Insufficiency, Conduction Disorder of the Heart, Hypertension.

Dose and Administration: By mouth, initially 2.5 mg 3 times daily for 1–2 weeks, then up to 5 mg 3 times daily; child 1 month–7 years 75 micrograms/kg 3 times daily; 7–15 years 2.5 mg 2–3 times daily.

Formoterol:

Indications: reversible airways obstruction (including nocturnal asthma and prevention of exercise-induced bronchospasm) in patients requiring long-term regular bronchodilator therapy, chronic obstructive pulmonary disease.

Contraindications: Acutely Deteriorating Asthma, Status Asthmaticus, Chronic Coronary Insufficiency, Conduction Disorder of the Heart, Hypokalemia, Seizure Disorder, Thyrotoxicosis.

Dose and Administration: asthma, adult and child over 5 years, 12 micrograms twice daily, increased to 24 micrograms twice daily in more severe airways obstruction. Chronic obstructive pulmonary disease, 12 micrograms twice daily.

 

Antimuscarinic bronchodilators

Ipratropium:

Indications: reversible airways obstruction, particularly in chronic obstructive pulmonary disease; rhinitis.

Contraindications: Benign Prostatic Hypertrophy, Bladder Outflow Obstruction, Narrow Angle Glaucoma, Ocular Hypertension, And Urinary Retention.

Dose and Administration: By inhalation of nebulised solution, reversible airways obstruction in chronic obstructive pulmonary disease, 250– 500 micrograms 3–4 times daily. Acute bronchospasm, 500 micrograms repeated as necessary; child under 5 years 125–250 micrograms, max. 1 mg daily; 6–12 years 250 micrograms, max. 1 mg daily.

Tiotropium:

Indications: maintenance treatment of chronic obstructive pulmonary disease

Contraindications: Acute Asthma Attack, Increased Cardiovascular Event Risk, Narrow Angle Glaucoma. Benign Prostatic Hypertrophy, Bladder Outflow Obstruction, Renal Disease with Moderate to Severe Function Impairment.

Dose and Administration: By inhalation of powder, adult over 18 years, 18 micrograms once daily.

 

Theophyllines

Theophylline:

Indications: Bronchial Asthma, Chronic Obstructive Asthma, Chronic Obstructive Pulmonary Disease with Bronchospasms, and COPD Associated with Chronic Bronchitis, Pulmonary Emphysema.

Contraindications: Angina, Myocardial Infarction, Peptic Ulcer, Seizure Disorder, and Tachyarrhythmia.

Dose and Administration:

Adult Min/Max Dose: 6.0mg/kg/24.0mg/kg

Pediatric Min/Max  Dose: 2.0mg/kg/24.0mg/kg.

Plasma-theophylline concentration for optimum response 10–20 mg/litre (55–110 micromol/litre); 4–6 hours after a dose and at least 5 days after starting treatment; narrow margin between therapeutic and toxic dose

Aminophylline:

Indications: Asthma Prevention, Bronchial Asthma, Bronchitis, Bronchospastic Pulmonary Disease, Chronic Obstructive Asthma, Nocturnal Asthma, Pulmonary Disease, Pulmonary Emphysema, and Status Asthmaticus.

Contraindications: Angina, Myocardial Infarction, Peptic Ulcer, Seizure Disorder, and Tachyarrhythmia

Dose and Administration: Acute severe asthma or acute exacerbation of chronic obstructive pulmonary disease not previously treated with theophylline, by slow intravenous injection over at least 20 minutes (with close monitoring), 250–500 mg (5 mg/kg), then see below; child 5 mg/kg. Acute severe asthma or acute exacerbation of chronic obstructive pulmonary disease, by intravenous infusion (with close monitoring), 500 micrograms/kg/hour, adjusted according to plasma-theophylline concentration; child 6 months–9 years 1 mg/kg/hour, 10–16 years 800 micrograms/kg/hour, adjusted according to plasma-theophylline concentration.

Corticosteroids

Corticosteroids are used for the management of reversible and irreversible airways disease. An inhaled corticosteroid used for 3–4 weeks may help to distinguish asthma from chronic obstructive pulmonary disease; clear improvement over 3–4 weeks suggests asthma. Corticosteroids are effective in asthma; they reduce airway inflammation (and hence reduce oedema and secretion of mucus into the airway). An inhaled corticosteroid is used regularly for prophylaxis of asthma when patients require a beta2 agonist more than twice a week, or if symptoms disturb sleep more than once a week, or if the patient has suffered exacerbations in the last 2 years requiring a systemic corticosteroidor a nebulised bronchodilator. Regular use of inhaled corticosteroids reduces the risk of exacerbation of asthma.

Inhaled Corticosteroids 

Budesonide:

Indications: Asthma Prevention, Bronchial Asthma. Severe Chronic Obstructive Pulmonary Disease

Contraindications: Acutely Deteriorating Asthma, Status Asthmaticus. Acute Tuberculosis, Fungal Infection of Lung, Fungal Infections, Ocular Herpes Simplex, Parasitic Infection, Uncontrolled Bacterial Infections.

Dose and Administration: By inhalation of powder, adult and child over 12 years, 100–800 micrograms twice daily, adjusted as necessary; alternatively, in mild to moderate asthma, 200–400 micrograms (max. 800 micrograms if stabilised on equivalent daily dose given in divided doses) as a single dose each evening; child 6–12 years, 100–400 micrograms twice daily; alternatively, in mild to moderate asthma, 200–400 micrograms as a single dose each evening. By inhalation of nebulised suspension, when starting treatment, during periods of severe asthma, and while reducing or discontinuing oral corticosteroids, 1–2 mg twice daily (may be increased further in very severe asthma); child 3 months–12 years, 0.5–1 mg twice daily.

Maintenance, usually half above doses.

Croup , 2 mg as a single dose (or as two 1-mg doses separated by 30 minutes).

Fluticasone:

Indications: Asthma Prevention, Bronchial Asthma, And Severe Chronic Obstructive Pulmonary Disease

Contraindications: Acute Asthma Attack, Status Asthmaticus, Acute Tuberculosis, Fungal Infections, Ocular Herpes Simplex, Parasitic Infection, And Uncontrolled Bacterial Infections

Dose and Administration: By aerosol inhalation, adult and child over 16 years, 100–250 micrograms twice daily, increased according to severity of asthma to 1 mg twice daily; child 4–16 years, 50–100 micrograms twice daily adjusted as necessary; max. 200 micrograms twice daily. By inhalation of nebulised suspension, adult and child over 16 years, 0.5–2 mg twice daily; child 4–16 years, 1 mg twice daily.

Ciclesonide:

Indications: Asthma Prevention, Bronchial Asthma, And Severe Chronic Obstructive Pulmonary Disease.

Contraindications: Acute Asthma Attack, Status Asthmaticus, Acute Tuberculosis, Fungal Infections, Inactive Tuberculosis, Ocular Herpes Simplex, Oropharyngeal Candidiasis, Parasitic Infection, Uncontrolled Bacterial Infections. Dose and Administration: By aerosol inhalation, adult and child over 12 years, 160 micrograms daily as a single dose reduced to 80 micrograms daily if control maintained.

 

Compound Preparations

Budesonide & Formeterol:

Indications: Bronchial Asthma, Chronic Obstructive Pulmonary Disease, COPD Associated with Chronic Bronchitis, and Prevention of Bronchospasms with Emphysema

Contraindications: Acutely Deteriorating Asthma, Status Asthmaticus, Acute Tuberculosis, Chronic Coronary Insufficiency, Conduction Disorder of the Heart, Fungal Infection of Lung, Fungal Infections, Hypokalemia, Ocular Herpes Simplex, Parasitic Infection, Seizure Disorder, Thyrotoxicosis, Uncontrolled Bacterial Infections

Dose and Administration: By inhalation of powder, asthma maintenance therapy, 1 puff twice daily increased if necessary to max. 2 puffs twice daily, reduced to 1 puff once daily if control maintained; child 12–17 years 1 puff twice daily reduced to 1 puff once daily if control maintained.

Fluticasone & Salmeterol:

Indications: Bronchial Asthma, Chronic Obstructive Pulmonary Disease.

Contraindications: Acute Asthma Attack, Acutely Deteriorating Asthma, and Status Asthmaticus. Acute Tuberculosis, Chronic Coronary Insufficiency, Conduction Disorder of the Heart, Fungal Infections, Ocular Herpes Simplex, Parasitic Infection, Uncontrolled Bacterial Infections.

Dose and Administration: By aerosol inhalation, asthma, adult and child over 4 years, 2 puffs twice daily, reduced to 2 puffs once daily if control maintained.

Leukotriene Receptor Antagonists

MONTELUKAST:

Indications: prophylaxis of asthma, symptomatic relief of seasonal allergic rhinitis in patients with asthma.

Contraindications: Anxiety, Depression, Dream Disorder, Feeling Agitated, Hallucinations, Mood Changes, Nervousness, Suicidal Ideation, and Tremors

Dose and Administration:

Prophylaxis of asthma, adult and child over 15 years, 10 mg once daily in the evening; child 6 months–6 years 4 mg once daily in the evening, 6–15 years 5 mg once daily in the evening.

Seasonal allergic rhinitis, adult and child over 15 years, 10 mg once daily in the evening.

Lipid Regulating Drugs

Statins:

Simvastatin:

Indications: primary hypercholesterolaemia, homozygous familial hypercholesterolaemia or combined (mixed) hyperlipidaemia in patients who have not responded adequately to diet and other appropriate measures;

prevention of cardiovascular events in patients with atherosclerotic cardiovascular disease or diabetes mellitus.

Contraindications: Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels. Women who are pregnant or may become pregnant. Serum cholesterol and triglycerides increase during normal pregnancy, and cholesterol or cholesterol derivatives are essential for fetal development. Nursing mothers. It is not known whether simvastatin is excreted into human milk; however, a small amount of another drug in this class does pass into breast milk

Dose and Administration: Primary hypercholesterolaemia, combined hyperlipidaemia, 10–20 mg daily at night, adjusted at intervals of at least 4 weeks; usual range 10–80 mg once daily at night. Homozygous familial hypercholesterolaemia, 40 mg daily at night or 80 mg daily in 3 divided doses. Prevention of cardiovascular events, initially 20–40 mg once daily at night, adjusted at intervals of at least 4 weeks; max. 80 mg once daily at night.

Atorvastatin:

Indications: primary hypercholesterolaemia, heterozygous familial hypercholesterolaemia, homozygous familial hypercholesterolaemia or combined (mixed) hyperlipidaemia in patients who have not responded adequately to diet and other appropriate measures; prevention of cardiovascular events in patients with type 2 diabetes and at least one additional risk factor for cardiovascular disease

Contraindications: Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels. Women who are pregnant or may become pregnant. atorvastatin may cause fetal harm when administered to a pregnant woman.

Dose and Administration: Primary hypercholesterolaemia and combined hyperlipidaemia, usually 10 mg once daily; if necessary, may be increased at intervals of at least 4 weeks to max. 80 mg once daily; child 10–17 years usually 10 mg once daily. Familial hypercholesterolaemia, initially 10 mg daily, increased at intervals of at least 4 weeks to 40 mg once daily; if necessary, further increased to max. 80 mg once daily (or 40 mg once daily combined with anion-exchange resin in heterozygous familial hypercholesterolaemia); child 10–17 years initially 10 mg daily, increased if necessary after at least 4 weeks to 20 mg once daily. Prevention of cardiovascular events in type 2 diabetes, 10 mg once daily.

Fluvastatin:

Indications: adjunct to diet in primary hypercholesterolaemia or combined (mixed) hyperlipidaemia (types IIa and IIb); adjunct to diet to slow progression of coronary atherosclerosis in primary hypercholesterolaemia and concomitant coronary heart disease; prevention of coronary events after percutaneous coronary intervention.

Contraindications: in patients with active liver disease or unexplained, persistent elevations in serum transaminases. If the patient becomes pregnant while taking this class of drug, therapy should be discontinued and the patient apprised of the potential hazard to the fetus.

Dose and Administration: Hypercholesterolaemia or combined hyperlipidaemia, initially 20–40 mg daily in the evening, adjusted at intervals of at least 4 weeks; up to 80 mg daily may be required; child and adolescent under 18 years, not recommended. Prevention of progression of coronary atherosclerosis, 40 mg daily in the evening. Following percutaneous coronary intervention, 80 mg daily.

Rosuvastatin:

Indications: primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (type IIb), or homozygous familial hypercholesterolaemia in patients who have not responded adequately to diet and other appropriate measures.

Contraindications: Patients with active liver disease, which may include unexplained persistent elevations of hepatic transaminase levels. Women who are pregnant or may become pregnant. Nursing mothers.

Dose and Administration: Initially 5–10 mg once daily increased if necessary at intervals of at least 4 weeks to 20 mg once daily, increased after further 4 weeks to 40 mg daily only in severe hypercholesterolaemia with high cardiovascular risk and under specialist supervision; elderly initially 5 mg once daily; patient of asian origin, initially 5 mg once daily increased if necessary to max. 20 mg daily.

Ezetimibe:

Indications: administered alone, is indicated as adjunctive therapy to diet for the reduction of elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), and apolipoprotein B (Apo B) in patients with primary (heterozygous familial and non-familial) hyperlipidemia. administered in combination with fenofibrate, is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, Apo B, and non-high-density lipoprotein cholesterol (non-HDL-C) in adult patients with mixed hyperlipidemia. The combination with simvastatin is indicated for the reduction of elevated total-C and LDL-C levels in patients with HoFH, as an adjunct to other lipid-lowering treatments.

Contraindications: Women who are pregnant or may become pregnant. Nursing mothers.

Dose and Administration: adult and child over 10 years, 10 mg once daily.

Simvastatin-Ezetimibe:

Indications: indicated for the reduction of elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and non-high-density lipoprotein cholesterol (non-HDL-C), and to increase high-density lipoprotein cholesterol (HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia or mixed hyperlipidemia. indicated for the reduction of elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable.

Contraindications: Active liver disease or unexplained persistent elevations in hepatic transaminase levels. Women who are pregnant or may become pregnant.

Dose and Administration: The recommended usual starting dose is 10/20 mg/day as a single daily dose in the evening, with or without food. Patients who require a larger reduction in LDL-C (greater than 55%) may be started at 10/40 mg/day.

Atorvastatin-Amlodipine:

Indications: indicated in patients for whom treatment with both amlodipine and atorvastatin is appropriate.

Contraindications: Pregnancy and Lactation. in patients with active liver disease or unexplained persistent elevations of serum transaminases.

Dose and Administration: Dosage should be adjusted according to each patient’s need. In general, titration should proceed over 7 to 14 days so that the physician can fully assess the patient’s response to each dose level.

Fibrates:

Gemfibrozil:

Indications: hyperlipidaemias of types IIa, IIb, III, IV and V in patients who have not responded adequately to diet and other appropriate measures; primary prevention of cardiovascular disease in men with hyperlipidaemias that have not responded to diet and other appropriate measures.

Contraindications: alcoholism, biliary-tract disease including gallstones; photosensitivity to fibrates; hepatic impairment; pregnancy; breast-feeding.

Dose and Administration: 1.2 g daily, usually in 2 divided doses; range 0.9– 1.2 g daily; child not recommended

Fenofibrate:

Indications: hyperlipidaemias of types IIa, IIb, III, IV, and V in patients who have not responded adequately to diet and other appropriate measures.

Contraindications: gall bladder disease; photosensitivity to ketoprofen; severe hepatic impairment; pregnancy; breast-feeding.

Dose and Administration: 200mg once daily.

Antihistamines

All antihistamines are of potential value in the treatment of nasal allergies, particularly seasonal allergic rhinitis (hay fever), and they may be of some value in vasomotor rhinitis. They reduce rhinorrhoea and sneezing but are usually less effective for nasal congestion. Antihistamines are used topically in the eye, in the nose and on the skin. Oral antihistamines are also of some value in preventing urticaria and are used to treat urticarial rashes, pruritus, and insect bites and stings; they are also used in drug allergies. Injections of chlorphenamine (chlorpheniramine) or promethazine are used as an adjunct to adrenaline (epinephrine) in the emergency treatment of anaphylaxis and angioedema.

 

Sedating Antihistamines

Chlorpheniramine maleate:

Indications: Allergic Conjunctivitis, Allergic Rhinitis, Anaphylaxis Adjunct, Dermatographic Urticaria, Nasal Congestion, Pruritus of Skin, Rhinorrhea, Sneezing, Urticaria, Vasomotor Rhinitis.

Contraindications: Acute Asthma Attack, Narrow Angle Glaucoma, Benign Prostatic Hypertrophy, Bladder Outflow Obstruction, Chronic Idiopathic Constipation, Gastrointestinal Obstruction, Illus, And Urinary Retention

Dose and Administration: By mouth, 4 mg every 4–6 hours max. 24 mg daily; for Children, 1–2 years 1 mg twice daily; 2–6 years 1 mg every 4–6 hours, max. 6 mg daily; 6–12 years 2 mg every 4–6 hours, max. 12 mg daily. By subcutaneous or intramuscular injection or by intravenous injection over 1 minute, 10–20 mg, repeated if required up to 4 times in 24 hours; max. 40 mg in 24 hours; child 1 month–1 year 250 micrograms/kg, repeated if required up to 4 times in 24 hours; 1–12 years 200 micrograms/kg or 1–6 years 2.5–5 mg, repeated if required up to 4 times in 24 hours; 6–12 years 5–10 mg, repeated if required up to 4 times in 24 hours

CYPROHEPTADINE HYDROCHLORIDE:

Indications: Allergic Conjunctivitis, Allergic Rhinitis, Dermatographic Urticaria, Nasal Congestion, and Pruritus of Skin, Rhinorrhea, Sneezing, and Urticaria

Contraindications: Acute Asthma Attack, Lactating Mother, Benign Prostatic Hypertrophy, Bladder Outflow Obstruction, Chronic Idiopathic Constipation, Glaucoma, Stenosing Peptic Ulcer, And Urinary Retention

Dose and Administration: Allergy, usual dose 4 mg 3–4 time’s daily; usual range 4–20 mg daily maxes. 32 mg daily; infant under 2 years not recommended, child 2–6 years 2 mg 2–3 times daily, max. 12 mg daily; 7–14 years 4 mg 2–3 times daily, max. 16 mg daily. Migraine, 4 mg with a further 4 mg after 30 minutes if necessary; maintenance, 4 mg every 4–6 hours

DIMETHINDENE MALEATE:

Indications: indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hey fever and perennial rhinitis, food and drug allergies; pruritus of various origins, also indicated for pruritus in eruptive skin diseases such as chicken pox.

Contraindications: When the patient is hypersensitive to the active substance

Dose and Administration: Average daily dosage (in three doses spread over the day)

KETOTIFEN:

Indications: allergic rhinitis

Contraindications: pregnancy and breast-feeding

Dose and Administration:

1 mg twice daily with food increased if necessary to

2 mg twice daily; initial treatment in readily sedated patients 0.5–1 mg at night;

child 3 years and over, 1 mg twice daily

PROMETHAZINE HYDROCHLORIDE:

Indications: symptomatic relief of allergy such as hay fever, urticaria; premedication; emergency treatment of anaphylactic reactions, sedation and motion sickness.

Contraindications: Coma, Lactating Mother, Agranulocytosis, Bone Marrow Depression, Chronic Idiopathic Constipation, Chronic Obstructive Pulmonary Disease, CNS Depression, Extrapyramidal Disease, Gangrene, Injection Site Sequelae, Leukopenia, Lower Seizure Threshold, Narrow Angle Glaucoma, Neuroleptic Malignant Syndrome, Respiratory Depression, Seizure Disorder, Sleep Apnea, Tissue Necrosis

Dose and Administration: By mouth, 25 mg at night increased to 25 mg twice daily if necessary or 10–20 mg 2–3 times daily; child under 2 years not recommended, 2–5 years 5–15 mg daily in 1–2 divided doses, 5–10 years 10– 25 mg daily in 1–2 divided doses. Premedication, child under 2 years not recommended, 2–5 years 15–20 mg, 5–10 years 20–25 mg. By slow intravenous injection in emergencies, 25–50 mg as a solution containing 2.5 mg/mL in water for injections; max. 100 mg.

Non-Sedating Antihistamines

LORATIDINE:

Indications: Allergic Rhinitis, Chronic Idiopathic Urticaria, Nasal Congestion, and Sneezing.

Contraindications: Disease of Liver, Hepatic Failure, Renal Disease with

Moderate to Severe Function Impairment

Dose and Administration:

adult and child over 6 years 10 mg once daily;

child2–6 years 5 mg once daily

CETIRIZINE HYDROCHLORIDE:

Indications: Allergic Rhinitis, Atopic Rhinitis, Chronic Idiopathic Urticaria, Seasonal Allergic Rhinitis, Atopic Dermatitis, and Urticaria

Contraindications: Renal Disease, Disease of Liver, Glaucoma, And Urinary Retention.

Dose and Administration: adult and child over 6 years, 10 mg once daily or 5 mg twice daily; child 2–6 years, hay fever, 5 mg once daily or 2.5 mg twice daily

DESLORATADINE:

Indications: Allergic Rhinitis, Atopic Rhinitis, Chronic Idiopathic Urticaria, And

Seasonal Allergic Rhinitis

Contraindications: Disease of Liver, Renal Disease

Dose and Administration:

Adults 5 mg once daily;

child 1–6 years 1.25 mg once daily,

6–12 years 2.5 mg once daily

LEVOCETIRIZINE HYDROCHLORIDE:

Indications: Allergic Rhinitis, Atopic Rhinitis, Chronic Idiopathic Urticaria, Seasonal Allergic Rhinitis, Atopic Dermatitis, and Urticaria

Contraindications: Chronic Renal Failure Syndrome, Hemodialysis with High-Flux Membrane

Dose and Administration: adult and child over 6 years, 5 mg once daily

FEXOFENADINE HYDROCHLORIDE:

Indications: Allergic Rhinitis, Chronic Idiopathic Urticaria, And Seasonal Allergic Rhinitis

Contraindications: Renal Disease

Dose and Administration: Seasonal allergic rhinitis, 120 mg once daily; child 6–12 years, 30 mg twice daily. Chronic idiopathic urticaria, adult and child over 12 years, 180 mg once daily

Local Sclerosants

Local Sclerosants

Ethanolamine Oleate:

Indications: indicated for the treatment of patients with esophageal varices that have recently bled, to prevent rebleeding. sclerotherapy of varicose veins.

Contraindications: inability to walk, acute phlebitis, oral contraceptive use, obese legs.

Dose and Administration: The usual intravenous dose is 1.5 to 5.0 mL per varix. The maximum dose per treatment session should not exceed 20 mL. Patients with significant liver dysfunction (Child Class C) or concomitant cardiopulmonary disease should usually receive less than the recommended maximum dose.

Submucosal injections are not recommended as they are reportedly more likely to result in ulceration at the site of injection.

Fibrinolytic Drugs

Fibrinolytic drugs act as thrombolytics by activating plasminogen to form plasmin, which degrades fibrin and so breaks up thrombi.

Alteplase:

Indications: acute myocardial infarction; pulmonary embolism; acute ischaemic stroke.

Contraindications: in acute stroke, convulsion accompanying stroke, severe stroke, history of stroke in patients with diabetes, stroke in last 3 months, hypoglycaemia, hyperglycaemia.

Dose and Administration: Myocardial infarction, accelerated regimen (initiated within 6 hours of symptom onset), 15 mg by intravenous injection, followed by intravenous infusion of 50 mg over 30 minutes, then 35 mg over 60 minutes (total dose 100 mg over 90 minutes); in patients less than 65 kg, 15 mg by intravenous injection, followed by intravenous infusion of 0.75 mg/kg over 30 minutes, then 0.5 mg/kg over 60 minutes (max. total dose 100 mg over 90 minutes). Myocardial infarction, initiated within 6–12 hours of symptom onset, 10 mg by intravenous injection, followed by intravenous infusion of 50 mg over 60 minutes, then 4 infusions each of 10 mg over 30 minutes (total dose 100 mg over 3 hours; max. 1.5 mg/kg in patients less than 65 kg).Pulmonary embolism, 10 mg by intravenous injection over 1–2 minutes, followed by intravenous infusion of 90 mg over 2 hours; max. 1.5 mg/kg in patients less than 65 kg.Acute stroke (treatment must begin within 3 hours of symptom onset), by intravenous administration over 60 minutes, 900 micrograms/kg (max. 90 mg); initial 10% of dose by intravenous injection, remainder by intravenous infusion; elderly over 80 years not recommended.

Streptokinase:

Indications: acute myocardial infarction; deep-vein thrombosis, pulmonary embolism, acute arterial thromboembolism, and central retinal venous or arterial thrombosis.

Contraindications: Because thrombolytic therapy increases the risk of bleeding, Streptase, Streptokinase, is contraindicated in the following situations: active internal bleeding, recent (within 2 months) cerebrovascular accident, intracranial or intraspinal surgery, intracranial neoplasm and severe uncontrolled hypertension.

Dose and Administration: Myocardial infarction (initiated within 12 hours of symptom onset), by intravenous infusion, 1.5 million units over 60 minutes. Deep-vein thrombosis, pulmonary embolism, acute arterial thromboembolism, central retinal venous or arterial thrombosis, by intravenous infusion, 250 000 units over 30 minutes, then 100 000 units every hour for up to 12–72 hours according to condition with monitoring of clotting parameters.

Anticoagulants

Parenteral Anticoagulants:

The main use of anticoagulants is to prevent thrombus formation or extension of an existing thrombus in the slower-moving venous side of the circulation, where the thrombus consists of a fibrin web enmeshed with platelets and red cells.

They are therefore widely used in the prevention and treatment of deep-vein thrombosis in the legs. Anticoagulants are of less use in preventing thrombus formation in arteries, for in faster-flowing vessels thrombi are composed mainly of platelets with little fibrin. They are used to prevent thrombi forming on prosthetic heart valves.

Heparin:

Indications: Heparin Sodium Injection is indicated for Anticoagulant therapy in prophylaxis and treatment of venous thrombosis and its extension; Low-dose regimen for prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdominothoracic surgery or who, for other reasons, are at risk of developing thromboembolic disease.

Contraindications: haemophilia and other haemorrhagic disorders, thrombocytopenia (including history of heparin-induced thrombocytopenia), recent cerebral haemorrhage, severe hypertension; severe liver disease (including oesophageal varices), peptic ulcer; after major trauma or recent surgery to eye or nervous system; acute bacterial endocarditis; spinal or epidural anaesthesia with treatment doses of heparin; hypersensitivity to heparin or to low molecular weight heparins.

Dose and Administration:

Treatment of deep-vein thrombosis, pulmonary embolism, unstable angina, and acute peripheral arterial occlusion, by intravenous injection, loading dose of 5000 units or 75 units/kg (10 000 units in severe pulmonary embolism), followed by continuous intravenous infusion of 18 units/kg/hour or treatment of deep-vein thrombosis, by subcutaneous injection of 15 000 units every 12 hours.

Prophylaxis in general and gynaecological surgery (see notes above), by subcutaneous injection, 5000 units 2 hours before surgery, then every 8–12 hours for 7–10 days or until patient is ambulant (monitoring not needed); during pregnancy (with monitoring), 5000– 10 000 units every 12 hours.

Haemodialysis by intravenous injection initially 1000–5000 units, followed by continuous intravenous infusion of 250– 1000 units/hour

Low Molecular Weight Heparins:

Low molecular weight heparins are usually preferred over unfractionated heparin in the prevention of venous thromboembolism because they are as effective and they have a lower risk of heparin-induced thrombocytopenia. Also, the standard prophylactic regimen does not require monitoring. In orthopaedic practice Low molecular weight heparins are probably more effective than unfractionated heparin; fondaparinux can also be used. The duration of action of Low molecular weight heparins is longer than that of unfractionated heparin; once-daily subcutaneous dosage means that they are convenient to use.

Enoxaparin:

Indications: indicated for the prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE). Treatment of Acute Deep Vein Thrombosis. Prophylaxis of Ischemic Complications of Unstable Angina and Non­Q-Wave Myocardial Infarction. Treatment of Acute ST-Segment Elevation Myocardial Infarction.

Contraindications: see under heparin.

Dose and Administration:

Prophylaxis of deep-vein thrombosis especially in surgical patients, by subcutaneous injection, moderate risk, 20 mg (2000 units) approx. 2 hours before surgery then 20 mg (2000 units) every 24 hours for 7–10 days; high risk (e.g. orthopaedic surgery), 40 mg (4000 units) 12 hours before surgery then 40 mg (4000 units) every 24 hours for 7–10 days.

Prophylaxis of deep-vein thrombosis in medical patients, by subcutaneous injection, 40 mg (4000 units) every 24 hours for at least 6 days and continued until patient ambulant (max. 14 days).Treatment of deep-vein thrombosis or pulmonary embolism, by subcutaneous injection, 1.5 mg/kg (150 units/kg) every 24 hours, usually for at least 5 days.Unstable angina and non-ST-segment­elevation myocardial infarction, by subcutaneous injection, 1 mg/kg (100 units/kg) every 12 hours usually for 2–8 days (minimum 2 days).

Tinzaparin:

Indications: indicated for the treatment of acute symptomatic deep vein thrombosis with or without pulmonary embolism when administered in conjunction with warfarin sodium.

Contraindications: contraindicated in patients with active major bleeding, in patients with (or history of) heparin-induced thrombocytopenia, or in patients with hypersensitivity to tinzaparin sodium.

Dose and Administration: Prophylaxis of deep-vein thrombosis, by subcutaneous injection, general surgery, 3500 units 2 hours before surgery, then 3500 units every 24 hours for 7–10 days; orthopaedic surgery (high risk), 50 units/kg 2 hours before surgery, then 50 units/kg every 24 hours for 7–10 days or 4500 units 12 hours before surgery, then 4500 units every 24 hours for 7–10 days. Treatment of deep-vein thrombosis and of pulmonary embolism, by subcutaneous injection, 175 units/kg once daily for at least 6 days (and until adequate oral anticoagulation established)

Treatment of thromboembolic disease in pregnancy [unlicensed indication], by subcutaneous injection, 175 units/kg once daily

Oral Anticoagulants: 

Warfarin:

Indications: indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, and pulmonary embolism. indicated for the prophylaxis and/or treatment of the thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement. indicated to reduce the risk of death, recurrent myocardial infarction, and thromboembolic events such as stroke or systemic embolization after myocardial infarction.

Contraindications:  peptic ulcer, severe hypertension; renal impairment (avoid if creatinine clearance less than 10 mL/minute); pregnancy

Dose and Administration: Whenever possible, the base-line prothrombin time should be determined but the initial dose should not be delayed whilst awaiting the result. For patients who require rapid anticoagulation the usual adult induction dose of warfarin is 10 mg on the first day; subsequent doses depend upon the prothrombin time, reported as INR (international normalised ratio). For patients who do not require rapid anticoagulation, a lower loading dose can be used over 3–4 weeks. The daily maintenance dose of warfarin is usually 3–9 mg (taken at the same time each day). The following indications and target INRs

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