Medicines & You

= Chemical Compound
= Indications
= Dosage
= Contraindication
= Special Precautions
= Adverse Reactions
= Drug-Drug Interaction

Metabolism

a) Insulin

Neutral soln of human monocomponent (HM) insulin. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma. Usage in insulin pump.
Psychic stress, infection or other diseases that may increase insulin requirement. Pregnancy.
Rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemic effect. Corticosteroids, thyroid hormones, OCs & diuretics may increase insulin requirements.

Insulin lispro (recombinant DNA origin).
Treatment of diabetes mellitus for the control of hyperglycemia.
Hypoglycaemia.
Transferring from other insulins. Emotional distress. Infection. Pregnancy. Renal or hepatic failure. Activity or diet changes.
Lipodystrophy. Local & generalized allergic reaction.
Corticosteroids, diuretics, OCs, thyroxine may increase insulin requirement, oral hypoglycemics, salicylates, sulfa antibiotics, ß-blockers, MAOIs, alcohol may intensify hypoglycemic effect of insulin.

Recombinant DNA origin. Humulin R Regular human insulin. Humulin N NPH human insulin. Humulin L Lente human insulin, insulin Zn susp. Humulin 30/70 30% regular human insulin inj & 70% NPH human insulin isophane susp.
Diabetes mellitus.
Hypoglycemia.
Transferring from other insulins. Emotional distress. Infection. Pregnancy.
Lipodystrophy, insulin resistance. Local & generalized allergic reactions.
Corticosteroids, diuretics, OCs, thyroxine may increase insulin requirement. ?-blockers, MAOIs, alcohol may intensity hypoglycemic effect of insulin.

Neutral isophane susp of human monocomponent (HM) insulin. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma.
Psychic stress, infection or other diseases that increase insulin requirement. Pregnancy.
Rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemic effect. Corticosteroids, thyroid hormones, OCs & diuretics may increase insulin requirements.

A neutral pre-mixed product consisting of 30% soluble human monocomponent insulin & 70% isophane human monocomponent insulin. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma.
Psychic stress, infection or other diseases that increase insulin requirement. Pregnancy.
Rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemic effect. Corticosteroids, thyroid hormones, OC s & diuretics may increase insulin requirements.

A neutral pre-mixed product consisting of 30% soluble human monocomponent insulin & 70% isophane human monocomponent insulin. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma.
Psychic stress, infection or other diseases that increase insulin requirement. Pregnancy.
Rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemic effect. Corticosteroids, thyroid hormones, OCs & diuretics may increase insulin requirements.

Neutral human monocomponent (HM) insulin Zn susp, 30% amorphous & 70% crystalline. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma.
Psychic stress, infection or other diseases that increase insulin requirement. Pregnancy.
Rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemia effect. Corticosteroids, thyroid hormones, OCs & diuretics may increase insulin requirements.

Neutral insulin Zn susp crystalline, human monocomponent. Recombinant DNA origin.
Insulin-requiring diabetes mellitus.
Hypoglycaemia, insulinoma.
Psychic stress, infection or other diseases that increase insulin requirement. Pregnancy.
rare incidence of allergy & lipoatrophy.
MAOIs, alcohol & ß-blockers may enhance the hypoglycaemic effect. Corticosteroids, thyroid hormones, OCs & diuretics may increase insulin requirements.

b) Oral Hypoglycaemic Agents

Glimepiride.
As an adjunct to diet & exercise in NIDDM, whenever blood sugar levels cannot be controlled adequately by diet, physical exercise & weight reduction alone.
Insulin-dependent (type 1) diabetes mellitus; diabetic ketoacidosis; diabetic precoma or coma; hypersensitivity to glimepiride or any of its excipients, other sulfonylureas or sulfonamides; serious renal or hepatic dysfunction; dialysis patients. Pregnancy, lactation.
Regular monitoring of glucose levels in blood & urine. Milder or absent symptoms of hypoglycaemia eg in patients w/ autonomic neuropathy or taking ß-blockers, clonidine, reserpine, guanethidine or other sympatholytic drugs. Temporary changeover to insulin in exceptional stress situations (eg trauma, surgery, infections w/ fever).
Hypoglycaemia; adrenergic counter-regulation; temporary visual impairment; Gl symptoms. Rarely thrombopenia, haemolytic anaemia, erythrocytopenia, leucopenia, agranulocytosis.
Potentiation of the blood-sugar-lowering effect by insulin & other (oral) antidiabetics, ACE inhibitors, allopurinol, anabolic steroids & male sex hormones, azapropazone, chloramphenicol, coumarin derivatives, fibrates, fluoxetine, ifosfamide, MAOIs, miconazole, oxyphenbutazone, pentoxyphylline, probenecid, quinolones, salicylates, sulfonamides, tetracyclines. Weakening of the blood-sugar-lowering effect by acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine & other synpathomimetic agents, glucagons, laxatives, (after protracted use), nicotinic acid (in high doses), oestrogens & progestogens, phenothiazines, phenytoin, rifampicin, thyroid hormones.

Glibenclamide.
NIDDM.
Type l diabetes mellitus, diabetic coma, diabetic metabolic decompensation; severe renal impairment & hepatic dysfunction.
Cross-sensitivity to sulfonamides & sulfonamide derivatives. Pregnancy & lactation.
Gl disturbances. Hypersensitivity reactions. Blood dyscrasias.
Potentiation of hypoglycemic effect w/ alcohol, ß-blockers, bezafibrate, biguanides, chloramphenicol, clofibrate, coumarin derivatives, MAOIs, salicylates, tetracyclines. Attenuation & aggravation of metabolic state by laxatives, corticosteroids, nicotinic acid, estrogens, phenothiazine derivatives, saluretics, sympathomimetics, thyroids hormones.

Chlorpropamide.
NIDDM.
Juvenile or growth-onset diabetes mellitus, severe or unstable ‘brittle’ diabetes. Diabetes complicated by ketoacidosis, major surgery, severe infection or severe trauma. Impairment of hepatic, renal or thyroid function. Pregnancy.
Hypoglycaemia; elderly, debilitated or malnourished patients; adrenal or pituitary insufficiency.
Jaundice; disulfiram-like reactions (rare).
Potentiation of hypoglycemia by salicylates, sulfonamides, chloramphenicol, probenecid, MAOIs & ß-blockers. Hypoglycaemia antagonized by thiazide diuretics, corticosteroids.

Gliclazide.
Type II diabetes.
Type 1 diabetes.
Hepatic &/or renal impairment. Hypoglycaemic may occur w/ reduced dietary intake or too high doses.
Nausea, headache, rashes & Gl disturbances.
Potentiated hypoglycemic effect w/ sulfonamides, salicylates, phenylbutazone, ß-blockers, MAOIs, ketoconazole & miconazole. Diminished hypoglycemic effect w/ thiazide diuretics, corticosteroids & estrogens.

Acarbose.
Additional therapy in association w/ diet in patients w/ diabetes mellitus.
Patients < 18 yr, chronic intestinal disorders associated w/ distinct disturbances of digestion & absorption, conditions which may deteriorate as a result of increased intestinal gas formation. Pregnancy, lactation. Severe renal impairment.
Frequently flatulence & bowel sounds, occasionally diarrhea & abdominal pain.
Cholestyramine, intestinal absorbents & digestive enzymes may attenuate its effect.

Metformin HCI.
NIDDM: Monotherapy or in combination w/ other oral antidiabetics. NIDDM & IDDM: in in combination w/ insulin.
Diabetic coma; ketoacidosis; renal impairment; chronic liver disease; cardiac failure & recent MI; alcoholism; hypoxemia; history of lactic acidosis; hypersensitivity; shock.
Pregnancy, lactation, stop therapy 2-3 days before surgery, conditions which may cause dehydration, patients w/ serious infection or trauma. Regular renal monitoring is needed.
Gl disturbances; lactic acidosis (rare).
May cause hypoglycemia w/ sulfonylurea or insulin. May impair absorption of vit B12. Anticoagulant may need adjustment. Reduced renal clearance if given w/ cimetidine.

Glipizide.
NIDDM not manageable by diet alone.
IDDM, keto-acidosis, pre-coma or coma; impaired kidney or liver function; adrenal insufficiency; gangrene; severe trauma, major surgery; infection or febrile states.
Elderly, debilitated subjects, unusual physical exertion. Hypoglycemia. Pregnancy.
Occasionally, Gl disturbances, headache, vertigo, skin reactions & alteration of the hematopoietic system. Rarely, hypoglycemic episodes (especially in debilitated & elderly subjects, after unusual physical exertion, irregular food intake or alcohol consumption, when kidney or liver function is impaired).
Hypoglycemia activity may be enhanced by dicoumarol, MAOIs, sulfonamides, phenylbutazone, chloramphenicol, cyclophosphamide, probenecid, & salicylates. Hy-poglycemic effect may be reduced by adrenaline, corticosteroids, OCs & thiazide diuretics. ?-blockers may mask hypoglycemic response.

c) Thyroid Preparations

Thyroxine Na.
Management of demonstrated thyroid hormone deficiency. Suppression of thyrotropin for the management of TSH-responsive tumours of the thyroid. Management of thyroiditis eg Hashimoto’s disease.
Presence of cardiac disorders. Corticosteroid replacement therapy must precede initiation of Oroxine therapy in cortisone deficiency.
Tachycardia, nervousness, tremor, headache, flushing, sweating & excessive wt loss.
Coumarin anticoagulants, pethidine, pentobarbitone, methadone, morphine, catecholamines, insulin, tricyclic antidepressants & dihydrotachysterol. Corticosteroids, digoxin, ketamine, cholestyramine, colistepol, soya flour.

d) Antithyroids

Carbimazole.
Thyrotoxicosis, prep for thyroidectomy, pre-& post-radioactive iodine treatment.
Pregnancy, lactation; agranulocytosis.
Frequently, Gl distress; agranulocytosis, blood disorders; fever, headache, arthralgia, lupus-like illness, vasculitis, hepatitis & alopecia, skin rashes.

Propylthiouracil.
Treatment of hyperthyroidism of the thyrotoxic patient prior to surgery or radioactive iodine therapy.
Lactation.
Cross-sensitivity between antithyroid agents may occur. Pregnancy. Patients should report sore throat, fever, skin eruptions, chills, headache & malaise. Perform regular full blood counts & monitor liver & thyroid function tests.
Agranulocytosis. Skin rashes, urticaria, pruritus, nausea, vomiting, gastric distress & headache, drowsiness, neuritis, vertigo, loss of taste, arthralgia, myalgia, paraesthesia, alopecias, skin pigmentation, oedema, a lupus-like illness, vasculitis, hepatitis & nephritis.
Anticoagulants, heparin.

Propylthiouracil.
Treatment of hyperthyroidism.
Lactation
Renal impairment.
Gastric distress, headache, nausea, skin rash, vomiting. Alopecia, arthralgia, hepatitis, renal-nephritis, systemic lupus erythematosus, vasculitis, agranulocytosis.

e) Antihyperlipidaemic Agents

Etofylline clofibrate.
Lowering of elevated blood lipid levels in hyperlipoproteinaemias. Lowering of elevated blood uric acid levels, if they occur in combination w/ hyperlipoproteinaemia.
Liver diseases (w/ the exception of fatty liver), gall bladder diseases w/ or w/o cholelithiasis, severe renal insufficiency, pregnancy, lactation. Recent MI, epilepsy.
Childn.
Hot flushes, elevated CPK, muscle pain.
Anticoagulants, sulfonylureas.

Fluvastatin Na.
Treatment of elevated total & LDL-cholesterol levels in patient w/ primary hypercholesterolaemia.
Active liver disease, unexplained persistent elevations in serum transaminases; lactation, pregnancy.
History of liver disease or heavy alcohol ingestion. Perform liver function tests before the initiation of treatment & periodically thereafter. Unexplained diffuse myalgias, muscle tenderness. Severe renal insufficiency.
Dyspepsia, nausea, insomnia, abdominal pain, headache.
Caution when used w/ immunosuppressive drugs, gemfibrozil, nicotinic acid, erythromycin, fifampicin, cimetidine, omeprazole.

Fenofibrate (standard)/(micronised).
Hypercholesterolaemia (type lla) & isolated (type IV) or associated (type llb & lll) endogenous hypertriglyceridaemia.
Serious hepatic & renal insufficiency. Childn (for lipanthyl 300mg).
rarely, Gl disturbances, allergic skin reactions, elevation of transaminases, muscular pains.
Potentiate actions of anticoagulant.

Atorvastatin.
Reduction of elevated total & LDL cholesterol, apolipoprotein B & triglycerides in patients w/ primary hypercholesterolaemia, mixed hyperlipidaemia, heterozygous & homozygous familial hypercholesterolaemia.
Active liver disease or elevated serum transaminases > 3 times the upper limit of normal. Pregnancy & lactation.
Monitor for creatine phosphokinase & transaminase elevations. Avoid alcohol consumption.
Gl disturbances, headache, myalgia, asthenia, insomnia, angioneurotic edema, muscle cramps, myositis, myopathy, cholestatic jaundice, peripheral neuropathy, pruritus.
Risk of myopathy increased w/ concurrent administration of ciclosporin, fibric acid derivatives, erythromycin, niacin or azole antifungals. Decreased atorvastatin plasma conc w/ oral antacid suspensions containing Mg & Al hydroxides, & colestipol. Increases steady-state plasma digoxin conc. Increased atorvastatin plasma conc w/ erythromycin. Increases AUC values for norethindrone & ethinylestradiol.

Etofibrate.
Severe primary & secondary hyperlipidemias.
Liver diseases (except fatty liver being a frequent concominant syndrome in hypertriglyceridemia), gallbladder diseases, severe renal insufficiency, decompensated heart failure, acute cardiac infarct, acute bleedings.
Flush syndrome & reactions to flush, Gl disorders.

Gemfibrozil.
Primary prevention of CHD & Ml in patients w/ hypercholesterolaemia, mixed dyslipidaemia & hypertriglyceridaemia (Fredrickson types 11A, 11B & IV). Treatment of other dyslipidaemias such as Fredrickson types III & V and those associated w/ diabetes or xanthomata.
Gallbladder disease. Severe hepatic, renal dysfunction. Primary biliary cirrhosis.
Renal & hepatic dysfunction.
Gl upset; diarrhea, nausea, bloating, acute appendicitis, atrial fibrillation.
Increases plasma conc of warfarin. Severe myositis & myoglobinuria may occur when used w/ lovastatin (rare).

Benfluorex.
Hypertriglyceridemias. NIDDM in overwt patients.
Chronic pancreatitis.
pregnancy & lactation.
Loose stools, nausea, epigastric discomfort, asthenia, drowsiness (may be decreased by decreasing the dose).
Antidiabetics.

Lovastatin.
Reduction of elevated total & LDL-cholesterol levels in patients w/ primary hypercholesterolemia when response to diet & other nonpharmacological measures alone has been inadequate. Reduction of elevated cholesterol levels in patients w/ combined hypercholesterolemia & hypertriglyceridemia, when the hypercholesterolemia is the abnormality of most concern. Treatment to slow the progression of coronary atherosclerosis in CHD patients.
Active liver disease or unexplained persistent elevations of serum transaminase. Pregnancy & lactation. Hypersensitivity.
Elevation of serum transaminases. If transaminase level rises persistently to 3 times the upper limit of normal, discontinue drug. Recommended that liver function tests be performed before treatment & periodically thereafter, especially in patients w/ abnormal liver function tests &/or consume substantial quantities of alcohol & patients receiving dose = 40 mg/day. Caution in patients with history of liver disease. If myopathy diagnosed/ suspected &/or marked elevation of CPK levels occur, discontinue drug. Administer to women of child-bearing age only when highly unlikely to conceive. Lactation. Childn. Therapy w/ Mevacor should be temporarily discontinued if systemic azole derivative antifungal therapy is required, in patients w/ acute, serious condition suggestive of a myopathy/ having a risk factor predisposing to development of renal failure secondary to rhabdomyolysis, including severe acute infection, hypotension, major surgery, trauma, severe metabolic, endocrine/electrolyte disorders, & uncontrolled seizures.
Gl upsets, headache, skin rashes, fatigue, pruritus, dry mouth, sleep disorders & dysgeusia, erythema multiforme, toxic epidermal necrolysis.
Use w/ caution w/ coumarin anticoagulants & w/ immunosuppressive drugs, gemfibrozil or niacin (as a lipid lowering agent) or erythromycin. Itraconazole.

Ciprofibrate.
primary hyperlipidaemia including hypercholesterolaemia, hypertriglyceridaemia & combined hyperlipidaemia.
Severe hepatic or renal impairment; pregnancy, lactation.
Hepatic or renal dysfunction. Periodic hepatic function tests recommended.
Gl disturbances; headache, vertigo; rash; myalgia.
May potentiate effects of warfarin. Higher risk of myopathy w/ HMG-CoA inhibitors 7 other fibrates.

Acipimox.
Type IV hyperlipoproteinaemia, Type II, III, V.
Peptic ulcer.
Renal impairment.
Initially, Gl effects; flushing, itching (usually transient).


Pravastatin Na.
In patients w/ previous MI & average (normal) serum cholesterol levels, indicated to reduce the risk of recurrent MI, need for myocardial revascularization procedures & to reduce risk of stroke or transient ischaemic attacks (TIAs). Reduction of elevated total & LDL-cholesterol levels in primary hypercholesterolaemia. Adjunct to diet in patients w/ atherosclerotic CV disease to slow the progressive course of atherosclerosis & to reduce the incidence of clinical CV events.
Active liver disease or unexplained persistent elevations in liver function tests. Pregnancy, Lactation.
Renal failure secondary to rhabdomyolysis. History of liver disease or heavy alcohol ingestion.
Mild, transient: Rash, myalgia, headache, non-cardiac chest pain, nausea, vomiting, diarrhea fatigue.

Simvastatin.
In coronary heart disease; reduce risk of death, coronary death & non-fatal MI; reduce risk of undergoing myocardial revascularization procedures; slow progression of coronary atherosclerosis, including reducing development of new lesions & new total occlusions. In hyperlipidemia: an adjunct to diet to reduce elevated total-C, LDL-C, Apo B & TG, & to increase HDL-C in patients w/ primary hypercholesterolemia, heterozygous familial hypercholesterolemia or mixed hyperlipidemia when response to diet & other nonpharmacological measure is inadequate.
Active liver disease or unexplained persistent elevations of serum transaminases. Pregnancy & lactation. Hypersensitivity.
Elevations of serum transaminase. If the transaminase level rises persistently to 3 times the upper limit of normal, discontinue drug. Recommend that liver function tests be performed before treatment begins & periodically thereafter eg semi-annually, for first year of treatment/until 1 yr after last elevation in disease. Caution in patients who consume substantial quantities of alcohol &/or have a history of liver disease. If myopathy diagnosed/suspected &/or marked elevation of CPK levels occur, discontinue drug. Administer Zocor to women of childbearing age only when highly unlikely to conceive. Not recommended for pediatric use. If patient becomes pregnant, Zocor should be discontinued. Therapy w/ Zocor should be temporarily discontinued if systemic azole derivative antifungal therapy is required, in patients w/ acute, serious condition suggestive of a myopathy/having a risk factor predisposing to development of renal failure secondary to development of renal failure secondary to rhabdomyolysis.
Abdominal pain, flatulence, constipation, asthenia & headache. Rarely hepatitis, hypersensitivity syndrome, myopathy.
Use w/ caution w/ coumarin anticoagulants & in combination w/ immunosuppressive agents, fibric acid derivatives or lipid-lowering doses of niacin. Inhibitors of CYP3A4.

f) Other Agents Affecting Metabolism

Pamidronate diNa.
Bone metastases & Multiple myeloma, tumour induced hypercalcaemia, paget’s disease of bone.
Hypersensitivity to other bisphosphonates.
Do not administer as a bolus inj or w/ other biphosponates or Ca-containing IV infusions. Monitoring of serum electrolytes, Ca, phosphates, renal function. Renal impairment, cardiac disease. Road/machinery users. Pregnancy, lactation. Childn.
Mild, transient fever; hypocaemia & hypophosphataemia. Occasional: lymphocytopenia, reactions at infusion site, transient musculoskeletal pain, Gl symptoms, hypomagnesaemis. Rare: symptomatic hypocalcaemia, allergic reactions. Very rare: anaphylactic shock. Isolated cases: deterioration of pre-existing renal disease, thrombocytopenia, seizures, uveitis.

Alendronate Na.
Treatment of osteoporosis in postmenopausal women.
Abnormalities of the oesophagus which delay oesophageal emptying eg stricture or achalasia. Inability to stand or sit upright for at least 30 mins. Hypocalcaemia.
Patients w/ upper Gl problems eg dysphagia, oesophageal diseases, gastritis, duodenitis or ulcers. Correct hypocalcaemia before initiating therapy. Disturbance of mineral metabolism (vit D deficiency) should also be effectively treated. Alert to any signs/symptoms signaling possible esophageal reaction. Discontinue Fosamax & seek medical attention if dysphagia, odynophagia or retrostemal pain occurs. Causes of osteoporosis other than oestrogen deficiency & ageing should be considered. Pregnancy & lactation. Paediatric use. Do not cjew/suck tablet. Follow strict dosing instruction. Not recommended for CrCL<35 mL/min.
Abdominal pain, dyspepsia, oesphageal ulcer, dysphagia, abdominal distension, musculoskeletal pain, constipation, diarrhea, flatulence, headache. Rarely, rash & erythema. Esophagitis, esophageal erosions, esophageal ulcers.
Ca supplements, antacid & other oral medications interfere w/ its absorption.

Lyophilised glucagons HCI.
Severe hypoglycaemia in diabetics. Motility inhibitor in radiography & endoscopy of the GIT. ?-blocker poisoning.
Glucagonoma, insulinoma, phaeochromocytoma.
When employed as a diagnostic aid in diabetics. Patients w/ marked depletion of liver glycogen stores. Not effective in alcohol-induced hypoglycaemia.
Gl upsets. Hypersensitivity.

Synthetic salmon calcitonin.
Osteoporosis, hypercalcaemia & hypercalcaemia crisis, bone pain associated w/ osteolysis, Paget’s disease.
pregnancy. Lactation. For nasal spray, chronic rhinitis. Use for short periods only in childn.
Nausea, vomiting, dizziness, flushing accompanied by heat sensation; rarely polyuria, chills. Hypersensitivity including local effects on inj site or generalized skin reactions. Very rarely, anaphylactic reactions w/ tachycardia, hypotension & collapse.

Alfacalcidol (1 -8-hydroxyvit D3).
Diseases caused by disturbances in the Ca metabolism in consequence of reduced endogenous production of 1,25-dihydroxyvit D3. Osteoporosis. Renal osteodystrophy. Post-op or idiopathic hypoparathyroidism. Pseudohypoparathyroidism. As an adjunct to the management of tertiary hyperparathyroidism. Vit D-resistant rickets or osteomalacia. Vit D-dependent rickets. Neonatal hypocalcemia or rickets. Malabsorption of Ca. Malabsorptive & nutritional rickets & osteomalacia.
Hypercalcemia.
Infants. Lactation.
Hypercalcemia.
Barbiturates. Anticonvulsants.

Synthetic salmon calcitonin.
Postmenopausal osteoporosis, hypercalcaemia, paget’s disease, bone pain associated w/ osteolysis.
Pregnancy & lactation. Should not be given to childn for > few wk.
Nausea, occasionally vomiting, slight facial flushing accompanied by a sensation of heat. Polyuria, chills.