HealthCare

Bambuterol is an oral prodrug of terbutaline with a prolonged duration of bronchodilator action that allows once-daily administration. It is an inactive site-specific prodrug that delivers active terbutaline only to the target tissue i.e., lung. It is a very effective long acting beta-adrenoceptor agonist. Clinical studies have shown that bambuterol is as effective as other oral and inhaled i2-agonists including salbutamol, terbutaline and Salmeterol, and theophylline(both conventional and controlled release formulations). Bambuterol is commercially available from the pharmacy major AstraZeneca under the trade names Bambec and Oxeol.

Bambuterol is used in maintenance treatment of bronchial asthma, Nocturnal asthma, and Chronic Obstructive Pulmonary Disease (COPD) . The typical dosage for adults is 10mg tablet once daily in the evening, may be increased to 20mg after 1-2 weeks.

Contraindications: Hypersensitivity to any of the ingredients or terbutaline, Hepatic impairment liver, cirrhosis or severely impaired liver function. Special Precautions: Dose should be reduced in patient with severely impaired renal function; care should be taken while prescribing bambuterol in patients with genetic deficiencies of plasma cholinesterase, caution should be implemented in patients with severe ischaemic heart failure. In case of Pregnancy and lactation: it is not recommended. Side effects include Tremor, headache, muscle cramps, palpitation, fatigue and insomnia. Generally, these effects were mild in nature and their incidence decreased with time.

Drug Interactions: Bambuterol reversibly inhibits plasma cholinesterase which prolongs the neuromuscular blockade induced by succinylcholine by upto four times. Hypertensive crisis and other adverse effects occur frequently with the concur rent use of bambuterol with monoamine oxidase inhibitors, bambuterol may partly or totally inhibit
the effect of p-blockers.

SALMETEROL is a selective long acting beta -2 adrenoceptor agonist. Provides effective protection against histamine induced bronchodilation . Its effect lasts for as much as 12hrs. Salmeterol is marketed  by GlaxoSmithKline under the brand name SEREVENT . The other popular inhaler Advair is a salmeterol fluticasone formulation.

Salmeterol is used in the treatment of chronic obstructive pulmonary disease (copd) and reversible airways obstructions in asthma. It is available as metered dosage inhaler. Dosage: For Adults: 2 inhalations (50 microgram) twice daily. And for Severe airway obstruction: 4 inhalations (100 micrograms) twice daily.

Contra-1ndlcations of Salmeterol include Hypersensitivity. Special precautions to be taken in patients  and their lung function should be monitored while taking Salmeterol  as it is not a replacement for oral or inhaled corticosteroids but use is complimentary to them. Salmeterol is not designed to relieve acute asthma symptoms. Serevent/ Salmeterol inhalers not recommended for children under 4 years and in Pregnant women & those lactating it should be used only when clearly indicated.
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Side effects of Salmeterol include Tremor, tachycardia, subjective palpitations and headache. Salmeterol has Drug Interactions with steroid and Diuretics causing Hypokalemia. Its Effects are antagonized by non-selective betablockers and less so by cardioselective betablockers.  It also has potentiation of vascular effects with MAOIs and tricyclic antidepressants. In November of 2005, the American FDA released a health advisory alerting the public to findings that show the use of Long-acting ß2-agonists like Salmeterol could lead to a worsening of symptoms, and in some cases death.

 Lovastatin belongs to statin class of drugs and is used for lowering cholesterol (hypolipidemic agent). Lovastatin is absorbed from GIT.   It under goes extensive first pass metabolism in liver which is it’s primary site of action.    It is highly bound to plasma protein.    Absorption is reduced by approxi 30% in empty stomach than with food. Lovastatin  is available under brand names like Mevacor, Advicor, Altocor , Altoprev and Statosan.

Lovastatin inhibits 3-hydroxy-3methylglutaryl-coenzyme A reductase (HMG-CoA reductase). It is the enzyme which catalyzes the conversion of HMG-CoA to mevalonate which is a required building block for cholesterol biosynthesis. Lovastatin effectively interferes with its production by acting as a competitive inhibitor for HMG-CoA which binds to the HMG-CoA reductase. Lovastatin, is inactive in the native form, the form in which it is administered. It  is hydrolysed to the β-hydroxy acid form in the body and it becomes active only in this form.

Lovastatin is eliminted primarily through fecal route which is the 83% of orally administered dose, 10% of drug is eliminated by renal route. Indication : As an adjunct to diet for the reduction of elevated total & LDL cholesterol in patients of primary hypercholesterolemia, for reduction of elevated  LDL cholesterol levels in patients with combined  hypercholesterolemia  and hypertriglyceridemia.

 Dosage : 10-80 mg/day in single or divided doses. Contraindications of Lovastatin include Hypersensitivity, Active liver disease or unexplained persistent elevations of serum, transaminases, pregnancy & nursing. Special Precaution has to be taken during : Pregnancy & Lactation.

Side effects of Lovastatin are  : Flatulence, diarrhoea, constipation, nausea, abdominal pain, cramps, dyspepsia, heart burn,  dysgeusia,  myopathy,        myalgia, rhabdbmyolysis, blurred vision, headache, dizziness, rashes, impotence, insomnia.

Lovastatin  has Drug interactions  with Anticoagulants, coumarin-or indandione derivative, HMG-COA reductase inhibitors,   cyclosporine   erythromycin,   Gemfibrozil, immunosuppresants or niacin.

Fenofibrate is a lipid lowering drug possessing a prominent lowering action on serum triglycerides. It also reduces serum uric acid levels in hyperuicemic and normal individuals by increasing the urinary excretion of uric acid. Fenofibrate was discovered by France based Groupe Fournier SA which is presently owned by Solvay Pharmaceutical. It is available under brand name Lipanthyl.

Fenofibrate is used in the treatment of in the treatment of type lla, Mb, III, IV and V hyperlipidemia resistant to diet therapy. Fenofibrate is helpful in reducing serum triglyceride levels.  Dosage: One capsule of 200mg per day should be administered with food.

Contraindications:     Hepatic dysfunction, Preexisting gall bladder disease and Hypersensitivity.

Side effects of Fenofibrate include Digestive problems, hepatitis, cholelithiasis, cholecystitis,   hepatomegaly;   Musculoskeletal myalgia, myasthenia, rhabdomylosis; Skin and appendages : photosensitivity, eczema; Respiratory: allergic pulmonary alveolitis.

Bezafibrate  suppresses endogenous cholesterol synthesis, causing the expression of an increased number of specific LDL (low density lipoproteins) receptors and thus an increased catabolism of LDL which  leads to lower plasma cholesterol.  It also suppresses the endogenous synthesis of triglycerides while simultaneously stimulating their catabolism through systemic lipoprotein lipase and hepatic lipase. Bezafibrate effectively brings about lower triglyceride levels. Bezafibrate  is commercially available under brand name Bezalip. 

Bezafibrate is used in the treatment of    Type    Ma,    lib,    III,    IV   &   V hyperlipidemias resistant to diet alone.  Dosage : Bezafibrate 200 mg is given three times daily with food.

Contraindications of Bezafibrate include: Gall bladder disease, Pregnancy, lactation, kidney or liver dysfunction, Nephrotic syndrome. Side effects of Bezafibrate are  Myalgia, diarrhoea, skin rashes, Reversible alopecia, decreased libido, G.I. upset.  Drug  Interaction:    Action  of sulphonylureas potentiated .

GEMFIBROZIL - brand name Lopid  is a hypolipidemic drug & has action resembling nicotinic acid; decreases very low density lipoprotein and blood lipids (VLDL). It is very effective in lowering triglycerides levels primarily. Though the decrease in total cholesterol may be modest, a more favorable distribution is indicated. Primary action of GEMFIBROZIL appears to be reduction of VLDL secretion by liver. Additional decrease in adipose tissue lipolysis and   uptake of fatty acids by liver has been demonstrated.

GEMFIBROZIL is used to treat Hyperlipidemia and lipoprotein abnormalities resistant to diet alone.

Dosage: 900-1500 mg daily (usual dose : 1200 mg) in 2 divided doses 1/2 hr before meals. Contra-indications  : Children,  severe impairment of renal & hepatic functions, Alcoholism, gall bladder disease and hypersensitivity.

Special Precautions: Conduct   blood count, liver function BEFORE TREATMENT & lipid profile tests before initiating therapy and repeat   them periodically. Discontinue if abnormal liver function persists. Regular Ophthalamic checkup required.

Paediatrics: Should not be used in children as well as in pregnant women and those lactating.

GEMFIBROZIL (lopid) Side effects include Epigastric distress, loose motions. Skin rashes, eosinophilia, bodyache, Raised blood sugar, blurred vision and impotence. GEMFIBROZIL (lpoid) has drug interactions with anticoagulants – aggravating effects.

Metolazone is a diuretic with actions and uses similar to those of the thiazide diuretics even though it does not contain a thiazide ring system. Metalazone is available under brand names  Zaroxolyn and Mykrox. It is mainly  used to treat congestive heart failure and high blood pressure.

Metolazone is used in the treatment edema,  including that associated with heart failure and for hypertension. For edema usual dose is 5 to 10mg, in some cases doses of 20mg or more but nor more than 80mg to be given in 24 hrs.For  Hypertension:- 2.5 to 5 mg daily either alone or with other anti hypertensives.

Metolazone aggravates  hypersensitivity to other thiazides and sulfonamide derivatives. It is contraindicated in  anuria, hepatic coma, severe renal and hepatic dysfunction, refractory hypokalaemia, hyponatraemia, hypercalcaemia, symptomatic hyperuricaemia and Addison's disease.

Metolazone  Drug Interactions: In drugs like Furosemide, ACE inhibitors and  glibendamide. Preacaustiosn should be taken while using Metolazone in cases of  Diabetes mellitus; gout; electrolyte,disturbances; lupus erythematosus; hepatic and renal impairment;

Side effects on using Metolazone (zaroxolyn ) include dizziness, headache, or heart arrhythmias (palpitations).The  Serious, though rare, side effects include aplastic anemia, pancreatitis, agranulocytosis, and angioedema. Metolazone, like other thiazide diuretics, may unmask latent diabetes mellitus or exacerbate gout, especially by interacting with medicines used to treat gout.

Nebivolol available from Mylan Laboratories under brand name Nebilet is a lipophilic beta 1 blocker drug . It exerts its actions by exhibiting a high selectivity for p-adrenergic receptors and also by reducing the peripheral vascular resistance by modulating NO release. It is devoid of intrinsic sympathomimetic or membrane stabilizing activity but appears to have nitric oxide-mediated vasodilator effects.

Nebivolol is used mainly for hypertension and high blood pressure. Dosage is typically 5mg once daily taken with or without food, preferably at a fixed time in a day. A reduced starting dose of 2.5mg (with upward titration where necessary) is recommended in the elderly and in patients with renal insufficiency.

Contraindications of Nebivolol: Use of the drug in children and patients with hepatic insufficiency is not recommended. Side-effects of Nebivolol include Headache, fatigue, paraesthesias and dizziness.

Carvedilol –brand name Coreg and Coreg CR is an arylethanolamine nonspecific fl-adrenoreceptor antagonist with beta blocking activity. It is a beta blocker group of drugs having anti hypertension effect partly by reducing total peripheral resistance and vasodilatation. It blocks adreno receptors and inhibits J-adreno receptor-mediated compensatory mechanisms.

Carvedilol is widely used for the treatment of hypertension and congestive heart failure.
Dosage for hypertension is initially 6.25 mg twice daily. If tolerated well after 7-14 days, increase to 12.5mg twice daily if needed. If needed again increase the dose up to 25 mg twice daily, after 7-14 days. Maximum total daily dose is 50mg.

In case of congestive heart failure start the dosage with 3.125 mg twice daily for 2 weeks. If tolerated raise to 6.25mg twice daily and then double the dose every 2 weeks to the level tolerated by patients. Maximum dose is 25mg and 50mg for patients weighing less than 85 kgs and more than 85 kgs respectively.

Contraindications of Carvedilol include hypersensitivity; Patients with NYHA class IV decompensated cardiac failure requiring IV inotropic therapy, bronchial asthma, second or third-degree AV block, Sick Sinus syndrome, cardiogenic shock or severe bradycardia, severe hepatic impairment and lactation.

Special Precautions: Before starting the Carvedilol treatment, laboratory confirmation of liver injury is very much essential. Abrupt withdrawal of 3-blockers may result in exacerbation of the symptoms of hyperthyroidism. During the initiation of therapy, avoid driving or operating machinery. Safety of Carvedilol is not established during pregnancy. as well as in Children. Side effects of Carvedilol include increased sweating, fatigue, oedema, bradycardia, hypotension (including postural), hyperglycaemia, hypercholesterolemia, bronchitis, insomnia, impotency, skin reactions, tinnitus, anaemia and even sudden death.

Drug interactions of Carvedilol: Rifampicin decrease while cimetidine increase the AUC & Cmax of carvedilol. Increase in Steady-state AUC and trough concentration of digoxin. Catecholamine-depleting agents & beta-receptors blockers results in hypotension or severe bradycardia.

Esmolol drip is a cardiovascular system medicine used in the treatment of Supraventricular, tachycardia, perioperative tachycardia and hypertension. It is rapid Acting Blood Pressure Medicine

Esmolol hcl is a beta 1-selective (cardioselective) adrenergic receptor blocking agent available under brand name of Brevibloc. It can rapidly control ventricular rate.

The normal dosage is 500 mcg/kg/min for 1 min, in case of Perioptachy-1000 meg/kg within 30 sees. Maintenance - for SVT & perioptachycardia: Initiate with 50 mcg/kg/min for 4 mins increasing maximum up to 300 mcg/kg/min. Every increment of 50 meg/ kg/min in maintenance should be preceded by the same loading dose.

Contra indication of Esmolol includes sinus bradycardia, heart block, cardiogenic shock or overt heart failure. Special precaution has to be taken for use in pregnancy, nursing mothers, and in children. Side effects of esmolol include hypotension, dizziness, headache, confusion, fatigue, paresthesia, asthenia, depression, anxiety, anorexia and bronchospasm. No significant drug interaction is seen with with digoxin, warfarin and morphine.