Gastro-intestinal System Medications PDF

Chapter One: Gastro-intestinal System 1.1-Antacids 1-Antacids are basic compounds that neutralize hydrochloric acid in the gastric secretions. They are used in the symptomatic management of gastrointestinal disorders associated with gastric hyperacidity such as dyspepsia, gastrooe...

Chapter One: Gastro-intestinal System 1.1-Antacids 1-Antacids are basic compounds that neutralize hydrochloric acid in the gastric secretions. They are used in the symptomatic management of gastrointestinal disorders associated with gastric hyperacidity such as dyspepsia, gastrooesophageal reflux disease, and peptic ulcer disease (1). 2-Antacids are best given when symptoms occur (i.e. when required ) or are expected, usually between meals and at bedtime (2). Antacid suspensions are more effective and work more quickly than tablets-3.(of the same type and quantity) Patient should be instructed to chew the tablets thoroughly followed by a full-4.glass of water to ensure maximum therapeutic effect It might be appropriate for the patient to have both; tablet antacid may be-5.taken during a day at the work while suspension is taken at home :Interactions-6 A-Antacids can affect the absorption of a number of drugs (via chelation and adsorption) and the majority of these interactions are easily overcome by.leaving a minimum gap of (1-2) hours between the doses of each drug B-Antacids -------increase the PH of the stomach---------cause a premature release of enteric coated tablets or granules in the stomach rather than the intestine. Side effects of antacids -7 A- AL-containing antacids tend to be constipating, Mg-containing antacids tend to cause osmotic diarrhea and are useful in patients who are slightly constipated. Thus combination products of AL and Mg salts cause.minimum bowel disturbances B- Antacids containing sod. Bicarbonate should be avoided in patients if ,sodium intake should be restricted ( e.g. in patient with CHF.(..…,hypertension Other drugs that may be combined with antacid formulations include-8 simeticone, which acts as a defoaming agent to reduce excess gas in the stomach, and alginates, which form a gel or foam on the surface of the stomach contents thereby impeding reflux and protecting the oesophageal mucosa 1.from acid attack (1) Antacids (including those combined with simethicone, and alginate ) Scientific names Trade names Dosage form 1 Sod. Alginate, potassium Gaviscon (Reckitt Suspension Banckiser) bicarbonate 2 Mg-Hydroxide 400mg Maalox Chewable tablet , Al-Hydroxide 400mg Suspension 3 Ca-carbonate 680mg Rennie Chewable tablet Mg-carbonate 80mg 4 Mg-Hydroxide, simethicone Maalox Plus Chewable tablet , Al-Hydroxide Suspension 5 Mg-trisilicate , Al-Hydroxide Gaviscon Chewable tablet Na-bicarbonate ,Alginic acid 6 Mg-Hydroxide 195mg /5mL Maalox (Sanofi-Aventis) suspension Al-Hydroxide 220mg/5mL Any extra notes: 1.2-Proton pump inhibitors(PPIs) 1- PPIs are the most potent inhibitors of gastric acid secretion and include omeprazole, lansoprazole, rabeprazole, pantoprazole, and esomeprazole (3). 2-PPIs are used for the treatments of gastric and duodenal ulcers; they are also used in combination with antibacterials for the eradication of Helicobacter pylori (a bacteria that is common cause of ulcer ). PPIs can be used for the treatment of dyspepsia and gastro-oesophageal reflux disease. They are also used for the prevention and treatment of NSAID-associated ulcers (2). 3- Regimen for the eradication of Helicobacter pylori usually composed of proton pump inhibitor (PPI), clarithromycin, and either amoxicillin or metronidazole for 10–14 days. This regimen is called (triple therapy) (4). 4-They are most effective when taken 30 to 60 minutes before meals (4).The once daily dose usually given in the morning before meals (2). While twice daily dose given morning and night before meals. 5-Various PPI dosage forms and formulations exist and include the enteric- coated granules contained in gelatin capsules (omeprazole, esomeprazole, and lansoprazole), and delayed release enteric-coated tablets (rabeprazole, 2 pantoprazole). The enteric coating prevents degradation of the drug in stomach acid (4). PPIs Scientific names Trade name Dosage form Omeprazole Prilosec , Gasec Cap. 10 , 20 , 40. Losec (AstraZeneca) Lansoprazole Lancid , Holicol Cap. 15 , 30. Zolon (Pfizer) Rabeprazole Aciphex Tab. 10 , 20. Pariet (Janssen , Eisal ) Pantoprazole Protonix Tab. 20 , 40. Protium (Takeda) Vial 40mg Esomeprazole Nexium (AstraZeneca) Tab. 20 , 40. Any extra notes: 1.3-Histamine-2 Receptor Antagonists (H2RAs) 1-H2RAs include cimetidine, ranitidine, famotidine, and nizatidine (3). 2- H2RAs are used for the treatments of gastric and duodenal ulcers. They can be used for the treatment of dyspepsia and gastro-oesophageal reflux disease (2). 3-Cimetidine inhibits several CYP450 isoenzymes , resulting in numerous drug interactions (e.g., theophylline, warfarin, and clopidogrel) (4). Avoidance of the combination, or a reduction in the dosage of these drugs may be required (1). 4-Ranitidine has less potential for hepatic CYP450 drug interactions , while famotidine and nizatidine do not interact with drugs metabolized by the hepatic CYP450 pathway (4). 5-Cimetidine has a weak anti-androgenic effect and gynaecomastia and impotence have also occasionally occurred in men; these are usually reversible (1). 3  H2RAs Scientific names Trade name Dosage form Cimetidine Tagamet (chemidex) Tab. 200 , 400 , 800. Amp. 20mg/1mL Ranitidine Zantac (GSK) Tab. 150 , 300. Amp.50 mg/2mL Famotidine Pepcid , Famadar , Tab. 20 , 40. Famosam Any extra notes: 1.4-Laxatives 1- Laxatives promote defecation and are used in the treatment of constipation and for bowel evacuation before investigational procedures such as endoscopy (1). Type of laxative -2 Type of laxative Example(s) Approximate onset of action 1-Stimulant laxative Senna, Bisacodyl, Sodium Oral:6-12hours picosulfate, and Glycerin (supp.) Rectal: within 1 hour 2-Bulk-forming laxative Methylcellulose, Bran , Sterculia 1-3 days and Ispaghula (Metamucil®) 3-Lubricant(faecal softeners) Liquid paraffin 6-8 hours 4-Osmotic laxative Lactulose 1-2 days 3- Product selection guidelines Patient Preferred laxative Pregnant women Bulk-forming laxative, or Lactulose may be used. Breast-feeding mother Bulk-forming laxative Children Glycerin(supp.) , Lactulose Advanced age(elderly) Bulk-forming laxative , Also Lactulose and Glycerin (supp.) are safe. A-Stimulant laxatives: 4  1- Prolonged use may result in loss of colonic smooth muscle tone. Stimulant laxatives should therefore be used for only short periods of a few days. 2-Bisacodyl tablet is enteric-coated; therefore, it should be swallowed whole and should not be taken within one hour of antacid or milk as this will lead to dissolution of the coating and release of the drug into the stomach and cause gastric irritation. 3-Usual Doses :Senna tab., Bisacodyl 5 mg tab. Adult dose: usually 2 tablets (usually take at night to produce the effect next morning). While the dose of supp. Is one supp. (usually in the morning ). Glycerin suppositories: The patient should expect to have bowel movement quickly (within one hour). 4-Senna may colour the urine yellowish-brown at acid pH, and red at alkaline pH (1). B-Lactulose ( Osmotic laxative): 1-It can be taken by all age group , and can be safely used in pregnancy. 2-It is intensely sweet in taste (but it is safe for diabetic patients). 3-Adult laxative dose : 15 ml twice daily. 4- It discourages the proliferation of ammonia-producing organisms. It is therefore useful in the treatment of hepatic encephalopathy (in patients with liver cirrhosis) (2). C- Bulk-forming laxative 1-The laxative effect can take several days to develop. 2- Bulk-forming laxative preparations should be not taken immediately before going to bed , because there may be a risk of oesophageal blockage if the patient lies down directly after taking them. 3-When recommending the use of a bulk laxative, the pharmacist should advise that an increase in fluid intake would be necessary. D- Liquid paraffin: its use decline nowadays due to many disadvantages. Laxatives (try to include the different types of laxatives ) Scientific name Trade names Type Dosage form(s) 1 Streculia Normacol Plus Bulk forming Granules (Norgine ) Frangula 2 streculia Normacol Bulk forming Granules (Norgine ) 3 Bicodyl Dulcolax Tab. 5 5  Laxidyl Stimulant Supp. 5 , 10. laxative 4 Glycerine Glycerine Stimulant Supp. 2 , 4 laxative 5 Sennoside Senade Stimulant Tab.7.5 , 13.5 Senokot (Reckitt laxative Syrup7.5mg/5mL Benckiser) 6 Castor oil Castor oil Stimulant Castor oil liquid laxative 7 Lactulose Laxolac Osmotic Syrup.65g/100mL Lactolac Any extra notes: 1.5-Antidiarrhoeals Note :the main aim in the management of acute diarrhoea is the correction of fluid and electrolyte depletion with rehydration therapy; this is especially important in infants and young children and antidiarrhoeals are not generally recommended for this age group. 1.5.1-Antimotility drugs (Loperamide , (Diphenoxylate+Atropine)) 1-Antimotility drugs are not recommended for acute diarrhoea in young children (2). In the UK, diphenoxylate hydrochloride is not licensed for children under 4 years of age (1). In the UK, loperamide is not licensed for children under 4 years of age. In the USA, loperamide is not recommended for children under the age of 2 years (1). 2- Adult doses : Loperamide: Initially 2 tablets followed by 1 tablet after each loose stool. Diphenoxylate+Atropine: 4 tablets initially followed by 2 tablets every 6 hours. 1.5.2- Adsorbents (pectin +kaolin) 1- Adsorbents such as kaolin are not recommended for acute diarrhoeas (2). 2-Kaolin can form insoluble complexes with some drugs in the gastrointestinal tract and reduce their absorption; oral doses should not be taken at the same time (1). 6 1.5.3- Oral rehydration solution (ORS) 1- Only water should be used to make the solution and that boiled and cooled water should be used for children < 1 year. 2-Stability of ORS after reconstitution: After reconstitution, any unused solution should be discarded after 1 hour of preparation unless it stored in refrigerator where it may kept for up to 24 hours. 3-Dose of ORS : See table Antidiarrhoeals Scientific name Trade names Dosage form 1 Diphenoxylate 4mg Lomotil , Entero-stop Tab. Atropine 0.25 mg 2 Loperamide Imodium , diarr-stop Tab.2mg Vancotil. Drop 2mg/mL 3 Loperamide 2mg Imodium Plus (McNeil) Cap. Simeticone 125mg Any extra notes: 1.6-Antispasmodics 1.6.1-Antimuscarinics (e.g Hyoscine butylbromide) 1- Used for symptomatic relief of gastro-intestinal disorders characterized by smooth muscle spasm (1). 2-Antimuscarinics are contra-indicated in patients with prostatic enlargement (2). 1.6.2-Other antispasmodics ( mebeverine) are used to relieve pain in irritable bowel Syndrome (2). Antispasmodics Scientific name Trade names Dosage form 1 Hyoscine N-butyl Antispasmine Tab. 10 , amp.20mg/2mL bromide Buscopan (Boechring Drop.10mg/mL , syrup 5/5mL ingelheim) 7 2 Mebeverine Dusptalin M.R cap.200mg , Colofac (Abbott healthcare) tab.100 , 135. 3 Alverine citrate Spasmanol (Meda) Cap.60mg Note: antichloinergics may be combined with benzodiazepine (librax®) or phenothiazine (stelabid®) and they are used for gastrointestinal disorders associated with anxiety; and for irritable bowel syndrome. Also they may be combined with an analgesics. Compound antichloinergics Trade names Scientific name Dosage form Librax® Chlordiazepoxide 5mg Tab. Clidinium bromide 2.5mg Stelabid® Isopropamide 5mg Tab. Trifluoperazine 1mg Antispasmine- Homotropine methyl bromide Tab. 4+350+60 co® Paracetamol Drop 2+120+30 Papverine Riabal-co® Prifinium bromide 30 mg Tab. Paracetamol 325mg Any extra notes: 1.7-Antiemetics 1-(Prochlorperazine, Metoclopramide and domperidone) are used to treat or prevent nausea and vomiting. 2-Cinnarizine is used to prevent motion sickness where the dose is taken 2 hours before travel (2). 3- Domperidone has the advantage over metoclopramide and the Prochlorperazine of being less likely to cause central effects such as dystonic reactions (a tetanus-like reaction ) because it does not readily cross the blood- brain barrier (2). Important note : in patients under 20 years: the dose of Metoclopramide should be determined on the basis of body-weight (0.1 mg/kg/dose) to avoid 8 dystonic reaction (1, 2). Antiemetics Scientific name Trade names Dosage form(s) 1 Metoclopramide Plasil Tab. 10mg Amp.10mg/2mL 2 domperidone Motillium (Janssen) Tab.10, supp. 30 , 60 , susp.1mg/mL 3 Prochlorperazine Stemetil Tab. 5 mg. Amp. 1.25% 4 Cinnarizine Stugeron (Janssen) Tab.25 , cap. 75 , Any extra notes: 1.8-Drugs for Inflammatory bowel disease ( ulcerative colitis and Crohn’s disease). Note: Ulcerative colitis (UC) is confined to the rectum and colon, while Crohn's disease (CD) can involve any part of the gastrointestinal (GI) tract (4). A-Aminosalicylates (like Mesalamine, and Sulfasalazine) 1-Sulfasalazine is given orally and it contain mesalamine combined with sulfapyridine which is believed to be responsible for many of the adverse reactions to sulfasalazine , mesalamine alone can be used (4). 2-Mesalamine can be used topically as an enema or suppository for the treatment of proctitis or given orally in slow-release formulations that deliver mesalamine to the small intestine and colon (4). 3-Because the oral mesalamine formulations are coated tablets or granules , they should not be crushed or chewed. Unlike sulfasalazine, it safe to use for patients with sulfonamide allergies (4). 4-Enemas or suppositories should be administered in the evening (3). They are given rectally, particularly when disease affects the sigmoid colon and rectum (1). 9 B-Other drugs may be used for Inflammatory bowel disease include corticosteroids, immunosuppressants ,…. Aminosalicylates Scientific name Trade names Dosage form(s) 1 Sulfasalazine Salazopyrin Tab. 500. (Pharmacia) 2 Mesalamine Ipxol (Sandoz) M.R tab. 1.2g , tab. 400mg Mezovante (Shire) Any extra notes: 1.9-Local preparations for anal and rectal disorders 1-These products are used mainly for haemorrhoids and anal fissure. 2-They are usually formulated as ointments and creams or suppositories. 3-Ointments and creams can be used for internal and external hemorrhoids while suppositories are used for internal hemorrhoids. However both are usually given twice daily (morning and evening) and after each bowel movement. 3-When used intrarectally, the ointment may be inserted using an applicator or finger but the applicator is preferred because it can reach an area where the finger cannot reach. The applicator should be lubricated by the ointment before insertion. Local preparations for anal and rectal disorders Scientific name Trade names Dosage form 1 Cinchocaine , Hydrocortisone Proctosedyle Ointment Supp. 2 Flucinolone acetonide , lidocaine , Proctocinolone , Ointment mentol, bismuth subgallate Proctohate 3 Aluminium acetate , Hydrocortisone , Xyloproct Oin tment (AstraZeneca) lidocaine , Zinc oxide Any extra notes: 10 1.10- Administration of Rectal Suppositories and enemas (5) : Suppositories 1-Gently squeeze the suppository to determine if it is firm enough to insert. Chill a soft suppository by placing it in the refrigerator for a few minutes or by running it under cool running water. 2-Remove the suppository from its wrapping. 3-Dip the suppository for a few seconds in lukewarm water to soften the exterior. 4-Lie on your left side with knees bent or in the knee-to-chest position (see drawings A and B). Position A is best for self-administration of a suppository. Small children can be held in a crawling position. 5-Relax the buttock just before inserting the suppository to ease insertion. Gently insert the tapered end of the suppository high into the rectum. If the suppository slips out, it was not inserted past the anal sphincter (the muscle that keeps the rectum closed). 6-Continue to lie down for a few minutes, and hold the buttocks together to allow the suppository to dissolve in the rectum. The parent/caregiver may have to gently hold a child's buttocks closed. 7-Remember that the medication is most effective when the bowel is empty. Try to avoid a bowel movement after insertion of the suppository for up to 1 hour so that the intended action can occur. Enemas 1-If someone else is administering the enema, lie on your left side with knees bent or in the knee-to-chest position (see drawings A and B). Position A is preferred for children older than 2 years. If self-administering the enema, lie on your back with your knees bent and buttocks raised (see drawing C). A pillow may be placed under the buttocks. 2-If using a concentrated enema solution, dilute solution according to the product instructions. Prepare 1 pint (500 mL) for adults and 1/2 pint (250 mL) for children. 3-Lubricate the enema tip with petroleum jelly or other non-medicated ointment/cream. Apply the lubricant to the anal area as well. 4-Gently insert the enema tip 2 (recommended depth for children) to 3 inches into the rectum. 5-Allow the solution to flow into the rectum slowly. If you experience discomfort, the flow is probably too fast. 6-Retain the enema solution until definite lower abdominal cramping is felt. The parent/caregiver may have to gently hold a child's buttocks closed to prevent the solution from being expelled too soon. 11 References 1- Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press 2009. 2-BNF 61. 3- Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 8th Edition. 2011. 4- Mary Anne koda-kimble (ed.), Applied Therapeutics: The clinical use of drugs, 10th ed.2013 5- Rosemary R Berardi. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 16th Edition. 2009. 12  Chapter Two : Cardiovascular System Angiotensin-converting enzyme inhibitors (ACE inhibitors) -2.1.Examples include ( captopril, enalapril, lisinopril and ramipril)-1 They act as vasodilators. The main uses of ACE inhibitors are in the -2.management of heart failure, hypertension, and myocardial infarction (1) Pronounced hypotension may occur at the start of therapy with ACE -3 :inhibitors (first dose hypotension) (1). Therefore.A- The first dose s hould preferably be given at bedtime (2).B- Starting dose should be low then increased gradually Other adverse effects include persistent dry cough (1)(see angiotensin II-4.(receptor antagonists below ACE inhibitors Scientific name Trade names Dosage form 1 Captopril Capoten (Squibb) Tab. 25 , 50 , 100. 2 Enalapril Vasotec Tab. 10 , 2o. Innovace (MSD) 3 Lisinopril Zestril (AstraZeneca ) Tab. 5 , 10 ,20. Any extra notes: 4 Ramipril Altace Tab. 1.25 , 2.5 , 5 ,10 Tritace (Sanofi Aventis) 2.2-Angiotensin II receptor antagonists(A2RAs) (angiotensin II receptor blockers). 1- Examples include (Candesartan, telmisartan, losartan and valsartan)(sartans). 2- They act as vasodilators. The main uses of A2RAs inhibitors are in the management of heart failure, hypertension, and myocardial infarction (1) 3-Imortant: unlike ACE inhibitors , they are less likely to cause the persistent dry cough which can complicate ACE inhibitor therapy. They are therefore a useful alternative for patients who have to discontinue an ACE inhibitor because of persistent cough (2). 13  Note 2 : There are many combination products in the market that contain a combination of an A2RA and diuretic (mostly hydrochlorothiazide) used for hypertension not adequately controlled with A2RA alone (2). Angiotensin II receptor antagonists (including at least one combination product with diuretic) scientific name Trade names Dosage form 1 Candesartan Atacand Tab. 8 , 16. cilexetil Amias (Takeda) Tab. 2, 4,8,16,32. 2 losartan Cozaar (MSD) Tab. 50 ,100. 3 Valsartan Diovan (Novertis) Tab. 80 , 160. 4 Irbesartan Sabervel or Aprovel Tab. 75, 150 , 300. 5 Telmisortan Micordis (Boehringer ) Tab. 20, 40 ,80. MicordisPlus (Boehringer) Tab.40/12.5, 80/12.5, 80/25 Any extra notes: Valsartan +Hydrochlorothiazide Diovan Plus (Novertis) tab.80/12.5 ,160/12.5, 160/25 Losartan+ hydrochlorothiazide Angezaar – H Tab. 50/12.5, 100/12.5 2.3-Beta-adrenoceptor blocking drugs (beta-blockers) 1-Examples include (Atenolol, bisoprolol, carvedilol, metoprolol, and propranolol). 2-Beta blockers are used in the management of: A-Cardiovascular disorders such as hypertension, angina pectoris, cardiac arrhythmias, myocardial infarction, and some of them are used for heart failure (1). B-They are also given to control symptoms of sympathetic overactivity, anxiety states , hyperthyroidism, and in the prophylaxis of migraine (1). C-Some Beta blockers used as eye drops ( e.g. timolol) to reduce raised intra -ocular pressure in glaucoma (1). 3-Important: A- Bisoprolol , carvedilol , metoprolol and nebivolol are the beta-blockers that are used to treat heart failure (other beta- blokers are contraindicated). B-When used for heart failure, β-blockers should be started in very low doses with slow upward dose titration (start low, go slow) e.g : Carvedilol start with 3.125 mg 6.25 mg 12.5 mg 25 mg) 14 4-Beta-blockers can precipitate bronchospasm and should therefore usually be avoided in patients with a history of asthma (2). 5-Abrupt cessation of β-blocker therapy should be avoided (abrupt discontinuation of β-blockers may be associated with tachycardia, in addition to increased BP). For these reasons, it is always prudent to taper the dose gradually over 1 to 2 weeks before discontinuation (2). Beta-blockers (try to select different scientific names) scientific name Trade name Dosage form 1 Atenolol Tenormin Tab. 25, 50 ,100. 2 Metoprolol Topral Tab. 50, 100. Betaloc (AstraZeneca) 3 Carvedilol Coreg Tab. 3.125, 6.25, 12.5 ,25. 4 Propranolol Inderal Tab. 10, 40. Inderal LA (AstraZeneca) Tab. 80 ,160. 5 Bisoprolol Cardicor (Merck Serona ) Tab. 1.25, 2.5 , 3.75, 5 ,7.5 , 10. 6 labetalol Trandate (phor Safer) Tab. 50 , 100 , 200 Any extra notes: Nadolol Corgard (Sanofi Aventis) tab.80. 2.4- Calcium-channel blockers (CCBs) 1-CCBs include : A-Dihydropyridine CCBs (examples amlodipine, nifedipine): They have a greater selectivity for vascular smooth muscle than for heart and therefore their main effect is vasodilatation (1). B- Non-Dihydropyridine CCBs (examples diltiazem and verapamil): They have a greater selectivity for heart than for vascular smooth muscle. 2-The main use of CCBs is in the management of angina pectoris and hypertension (both types of CCBs ) ; some are also used in cardiac arrhythmias (non-dihydropyridine CCBs) (1). 3-CCBs (especially dihydropyridine CCBs) can cause ankle edema as a side effect (2). 15 4-Nifedipine is a short acting , therefore it is commonly formulated as sustained release formulation (long acting dosage form). CCBs Scientific name Trade names Dosage form 1 Amlodipine Amlostin or Norvasc Tab. 5 , 10. Istin (Pfizer) 2 Diltiazem Cardizem Tab. 60 , 90 , 120. Tildiem (Sanofi Aventis ) 3 Nifedipine Procardia S.R Tab. 5 , 10. Adalat (Bayer) 4 Verapamil Isoptin or zolvera Tab. 40 ,80 ,120, 160. Cardilax (Dexcel) Amp. 2.5mg/mL 5 Nimodipine Nimotop (Bayer) Tab. 30. Amp. 0.2mg /mL 6 Any extra notes: Note : Fixed-dose combination products Several fixed-dose combination products are available , their use can reduce the number of tablets or capsules taken by patients. This has been demonstrated to improve adherence compared with using two separate single-drug products. Improved adherence may increase the likelihood of achieving goal BP values (3). Fixed-dose combination products Scientific name Trade name Dosage form 1 Lisinopril 5mg Hipril-A® Tab. Amlodipine 5mg 2 Candesartan 8 , 16 Atacand Plus Tab. Hydrochlorthiazide 12.5 , 25 3 Lisinopril 10 or 20 mg Zestoetic (AstraZeneca ) Tab. Hydrochlorthiazide 12.5 , 25 16 Diuretics-2.5 Diuretics promote the excretion of water and electrolytes by the kidneys. They-1 are used in the treatment of heart failure, hypertension and other diseases.when salt and water retention has resulted in oedema (1).The principal groups of diuretics are as follows-2 Diuretic type examples Thiazide and related diuretics Hydrochlorothiazide, Chlortalidone Loop Diuretics Furosemide, Bumetanide Potassium (K +)-sparing diuretics Amiloride Aldosterone antagonist Spironolactone Carbonic anhydrase inhibitors Acetazolamide (mainly for glaucoma ( Diuretics ideally should be dosed in the morning if given once daily and in -3 the morning and afternoon if dosed twice daily to minimize the risk of.nighttime diuresis (4) 4- Thiazide and loop diuretics can cause hypokalemia while K-sparing diuretics can cause retention of potassium and therefore, they are given with thiazide or loop diuretics to minimize hypokalemia (2). 5- Spironolactone has an anti-androgenic properties, therefore: A-It may cause side effects like Gynecomastia (breast enlargement ) , and impotence in men. B- It has been used for its anti-androgenic properties in some cases of acne and for women with Hirsutism (hair on the face) (1). Diuretics Scientific name Trade names Dosage form 1 Chlortalidone Hygroton (Alliance) Tab. 50 2 Furosemide Lasix (Sanofi Aventis) Amp. 10mg/mL Tab.20, 40 3 Spironolactone Aldactone (pharmacia) Tab. 25 , 50 ,100. 4 Acetazolamide Cidamax Tab.250. 5 Hydrochlorothiazid Moduretic Tab. e – Amiloride 6 Bumetanide Burinx Tab.1 , 5.amp.0.5mg/mL Syrup 1mg /5mL Any extra notes: 17 Lipid-regulating drugs-2.6 1- Lipid regulating drugs are used to modify blood lipid concentrations in the management of hyperlipidaemias and for the reduction of cardiovascular risk (1). 2-The principal groups of lipid regulating drugs are the A- Statins like (atorvastatin, rosuvastatin, and simvastatin) B- Fibrates like gemfibrozil. 3-Important : The main effect of statins is to reduce cholesterol while the main effect of fibrates is to reduce triglycerides (1). 4- Important : Cholesterol synthesis in the liver peaks during the early morning (midnight to 3 a.m.) and therefore most of statins such as simvastatin should be taken in at night (1). 5- Important : patients taking simvastatin or atorvastatin should be advised to avoid Grapefruit juice (because it inhibit their metabolism increase their conc. increase their side effects). (1) Lipid-regulating drugs Scientific name Trade names Dosage form 1 Atorvastatin Lipitor (Pfizer) Tab. 10 ,20 ,40. 2 Gemfibrozil Lopid (Pfizer) Cap. 300 ,600. 3 Simvastatin Zocor (MSD) Tab. 10 , 20 ,40 , 80. 4 Rosuvastatin Crestor (AstraZeneca) Tab. 5, 10 , 20 , 40. 5 Omega-3 fatty acid Omacor (Abbott healthcare ) Cap. 380. (may be used to reduce triglycerides) Any extra notes: (Novertis) Fluvastatin Lescol cap. 20 ,40. Nitrates-2.7 1-Nitrates are peripheral and coronary vasodilators used in the management of angina pectoris , heart failure, and myocardial infarction (1). 2- Sublingual (or aerosol spray) of glyceryl trinitrate are used to provide rapid symptomatic relief of acute anginal attack while and transdermal patches of glyceryl trinitrate are used the long-term prophylaxis of angina. 18 ‫‪3-Other nitrate available in Iraq are Isosorbide Dinitrate (ISDN) and‬‬ ‫‪Isosorbide Mononitrate (ISMN) which are commonly given by oral route.‬‬ ‫‪4-ISMN has longer duration than ISDN : The advantage of ISMN is twice‬‬ ‫‪daily dosing (or once daily with sustained release products) which mean better‬‬ ‫‪compliance (3).‬‬ ‫‪5- Nitrate can cause headache that is usually transient, typically lasting several‬‬ ‫‪days to few weeks. Patients can use simple analgesics (Paracetamol) when‬‬ ‫‪required to control any headaches(3).‬‬ ‫)ﻃﺮ ﮵ ﮴ ﺔ اﺳ ﮴ ﻌﻤﺎل ﺣ ﮳ﻮب اﻻ ﮲ ﮳ﺤﺴ ﮵ﺪ ﮴ﺤﺖ اﻟﻠﺴﺎن(‬ ‫وﺻﻊ اﻟﺤ ﮳ﺔ ﮴ﺤﺖ اﻟﻠﺴﺎن‪.‬‬ ‫اﻟﺤﻠﻮس ﮲ ﻮرا ﻣﻊ ﮲‬ ‫‪-1‬ﻋ ﮲ﺪ ﺣﺪوث ا ٔﻻﻟﻢ ﮲ ﮵ﻰ اﻟﺼﺪر‪ ---‬﮵ ﮳ﺤﺐ ﮳‬ ‫أﺣﺮى‬ ‫ﻮﺻﻊ ﺣ ﺔ ﮶ﺎ ﮲ ﺔ ﮴ﺤﺖ اﻟﻠﺴﺎن ‪.‬و اذا ﻟﻢ ﮲ﺤ ﮴ ﻒ ا ٔﻻﻟﻢ ﻌﺪ ‪ 5‬د ﮴ ﺎ ٔﻖ ﮲‬ ‫﮳‬ ‫﮵‬ ‫ٕ‬ ‫﮵‬ ‫﮳‬ ‫‪-2‬اذا ﻟﻢ ﮵ ﮲ﺤ ﮴ ﻒ ا ٔﻻﻟﻢ ﮳ﻌﺪ ‪ 5‬د ﮴ ﺎ ٔﻖ ﮲ ﮴ ﮲‬ ‫ٕ‬ ‫أﺣﺮى ﮲ ﮵ ﮳ﺤﺐ اﻟﺬﻫﺎب ﮲ ﻮرا ٕاﻟﻰ اﻟﻤﺴ ﮴ ﮶ﺴ ﮲ ﻰ‪.‬‬ ‫ﻮﺻﻊ ﺣ ﮳ﺔ ﮶ﺎﻟ ﮶ ﺔ ﮴ﺤﺖ اﻟﻠﺴﺎن و ٕاذا ﻟﻢ ﮵ ﮲ﺤ ﮴ ﻒ ا ٔﻻﻟﻢ ﮳ﻌﺪ ‪ 5‬د ﮴ ﺎ ٔﻖ ﮲‬ ‫﮲ ﮴ ﮲‬ ‫ﺎﻻﺳﻌﺎف ﻋ ﮲ﺪ ﻋﺪم ذﻫﺎب ا ٔﻻﻟﻢ ﮳ﻌﺪ ﮴ ﮲ﺎول اﻟﺤ ﮳ﺔ ا ٔﻻوﻟﻰ ‪.‬‬ ‫ﻮﺻﻰ ﮳ﺎﻻ ﮴ﺼﺎل ﮳ ٕ‬ ‫﮵‬ ‫ﺔ‬ ‫﮶ ﮴‬ ‫﮵‬ ‫اﻟﺤﺪ‬ ‫اﻟﻤﺼﺎدر‬ ‫ﺖ‬ ‫وان ﮲‬ ‫﮳‬ ‫اﻟﺤ ﮲ ﮴ ﺎن أو اﻟﻄﻌﻢ اﻟﺤﺎد ﻟﻠﺤ ﺔ ﮲ ﮵ﻰ اﻟ ﮲ ﻢ وﻫﺬا‬ ‫ﻣﮟ اﻟﺼﺪاع أو اﻟﺪوار أو ﮲‬ ‫﮳‬ ‫﮳‬ ‫‪ -3‬﮴ ﺪ ﮴ ﮶ﺴﻌﺮ ﻋ ﮲ﺪ اﺳ ﮴ ﮲ﺤﺪاﻣﻚ ﻟﻠﺤ ﻮب ﺴﻰ‬ ‫﮶ ٔ ﮲‬ ‫ﻟﻠﺴﺮا ﮵ ﮵ﮟ‪.‬‬ ‫ﻌﻰ ﮲ ﮴ ﺤﺔ ﻋﻤﻞ اﻟﺪواء اﻟﻤﻮﺳﻊ ﮶‬ ‫ﺳﻰ ﻃ ﮳ ﮵ ﮵ ﮵ ﮳‬ ‫﮲‬ ‫﮶ ٔ‬ ‫‪-4‬ﻣﮟ اﻟﻤﻤﻜﮟ أن ﮵ﺴ ﮴ ﮲ﺤﺪم اﻻ ﮲ ﮳ﺤﺴ ﮵ﺪ ﻛﻮ ﮴ ﺎ ﮵ﺔ وذﻟﻚ ﮳ ٔ ﮲ﺣﺬ ﺣ ﮳ﺔ ﮴ﺤﺖ اﻟﻠﺴﺎن ) ‪ 10 -5‬د ﮴ ﺎ ٔﻖ( ﮴ ﮳ﻞ اﻟ ﮴ ﮵ﺎم ﮳ ٔ ي‬ ‫﮲‬ ‫ﻋﻤﻞ ﮲ ﮳‬ ‫ﻣﺤﻬﺪ ﮵ ﮴ ﻮ ﮴ ﻊ ﻟﻪ أن ﮵ﺴ ﮳ﺐ أﻟﻤﺎ ﮲ ﮵ﻰ اﻟﺼﺪر‪.‬‬ ‫وﺣﺎف )وﻟﻜﮟ ﻟ ﮵ﺲ ﮲ ﮵ﻰ‬ ‫ﺎرﺣﻬﺎ‪.‬و ﮵ﺤ ﮲ ﻆ ﮲ ﮵ﻰ ﻣ ن ﮳ﺎرد ﮳‬ ‫‪ -5‬﮵ ﮳ﺤﺐ أن ﮵ﺤ ﮲ ﻆ اﻟﺪواء ﮲ ﮵ﻰ ﻋﻠ ﮳ ﻪ ا ٔﻻﺻﻠ ﮵ﺔ وﻟ ﮵ﺲ ﮲ﺣ ﮳‬ ‫﮴‬ ‫﮲‬ ‫﮵‬ ‫ٕ‬ ‫اﻟﺼﻮء واﻟﺤﺮارة واﻟﺮﻃﻮ ﮳ﺔ‪.‬ﻛﻤﺎ ﮵ ﮳ﺤﺐ أن ﮴ ﮲ﻌﻠﻖ اﻟﻌﻠ ﺔ ﺎﺣ م ﻌﺪ ﰻ ﻋﻤﻠ ﺔ اﺳ ﮴ ﮲ﺤﺪام‪.‬‬ ‫﮳‬ ‫﮳‬ ‫﮳‬ ‫ﻋﮟ ﮲‬ ‫ﻼﺣﺔ( ﮳ﻌ ﮵ﺪا‬ ‫اﻟ ﮳‬ ‫﮶‬ ‫﮲‬ ‫ﻣﺼ ﮵ﻰ ﮲ ﮴ﺮة ﮶ﺳﻬﺮ ﮵ﮟ ﻣﮟ ﮴ﺎر ﮵ ﮲ﺢ ﮲ ﮴ﺢ اﻟﻌﻠ ﮳ﺔ‪.‬‬ ‫﮲‬ ‫‪ -6‬﮴ﺮﻣﻰ اﻟﺤ ﮳ﻮب وﻻ ﮴ﺴ ﮴ ﻌﻤﻞ أ ﮳ﺪا ﮳ﻌﺪ‬ ‫﮲ ﮲‬ ‫ﻣﺴﳫﺔ ﻣﻬﻤﺔ ﮴ﺴﻤﻰ‬ ‫﮵ ﮵‬ ‫﮵‬ ‫﮵‬ ‫ﺣ ﺚ ﮴ ﮴ ﻞ ﮲ ﻌﺎﻟ ﺔ اﻟﺪواء ﻋ ﮲ﺪ اﻻﺳ ﮴ﻌﻤﺎل اﻟﻤ ﮴ﻮاﺻﻞ وﻟ ﮴ ﮲ ﺎدي ﮲ ﮵ﻰ اﻟ ﮲ﺎ ﮴ﺮ ﺖ ﻫ ﮲ﺎك ﮶‬ ‫‪tolerance‬‬ ‫اﻟﻤﺴﳫﺔ ﮲ﻌﻤﻞ ﮲ ﮴ﺮة اﺳ ﮴ﺮاﺣﺔ ﮵ﻮﻣ ﮵ﺔ ﮴ﺴﻤﻰ )‪ : nitrate-free interval (NFI‬﮳ﺎﻟﻄﺮ ﮵ ﮴ ﺔ ا ٓﻻ ﮴ ﮵ﺔ‬ ‫ﻫﺬه ﮶‬ ‫اﻟﺤﺮﻋﺔ ا ٔﻻوﻟﻰ ﮵ ﮴ ﮲ﺎوﻟﻬﺎ ﻋ ﮲ﺪ اﺳ ﮴ ﮵ ﮴ ﮲ﺎﻃﻪ ﺻ ﮳ﺎﺣﺎ‪1-‬‬ ‫ٕاذا ن اﻟﻤﺮ ﮵ﺾ ﮵ ﺎول ﻼث ﺣ ﮳ﺎت ﮲ ﮵ﻰ اﻟ ﮵ﻮم ﮲ ﺎن ﮳‬ ‫﮶‬ ‫﮴﮲‬ ‫اﻟﻤﺼﺎدات اﻟﺤ ﮵ﻮ ﮵ﺔ‬ ‫﮲‬ ‫ﻣﻊ‬ ‫اﻟﺤﺎل‬ ‫ﻫﻮ‬ ‫ﻛﻤﺎ‬ ‫ﺳﺎﻋﺎت‬ ‫‪8‬‬ ‫ﻌﺪ‬ ‫﮳‬ ‫ﺲ‬ ‫﮵‬ ‫)وﻟ‬ ‫ﺳﺎﻋﺎت‬ ‫‪6-5‬‬ ‫ﻌﺪ‬ ‫﮳‬ ‫ﺎوﻟﻬﺎ‬ ‫﮵ ﮵‬ ‫﮳‬ ‫واﻟﺤﺮﻋﺔ اﻟ ﮶ﺎ ﮲ ﺔ ﮴ ﮲‬ ‫اﻟﺤﺮﻋﺔ اﻟ ﮶ﺎﻟ ﮶ﺔ‬ ‫ﻣ ﻼ( و ﮵ ﺎول ﮳‬ ‫﮴﮲‬ ‫﮶‬ ‫واﻟﻤﻌﺮب‬ ‫ﺎح‬ ‫اﻟﺤﺮﻋﺔ اﻟ ﺎ ﮵ﺔ وﻫﻜﺬا ﮲ ﺴ ﺤﺼﺮ ﮲ ﺮة اﻻﺳ ﮲ﺤﺪام ﮳ ﮵ﮟ اﻟﺼ ﮳‬ ‫أ ﮵ ﮲ﺼﺎ ﮳ﻌﺪ ‪ 6-5‬ﺳﺎﻋﺎت ﻣﮟ ﮳‬ ‫﮲‬ ‫﮲‬ ‫﮴‬ ‫﮴‬ ‫﮴﮲‬ ‫﮶ ﮲‬ ‫‪.‬و ﮳ ﻰ ﺮة اﻟﻠ ﮵ﻞ ﮳ ﮲‬ ‫ﺪون دواء )اﺳ ﮴ﺮاﺣﺔ(‬ ‫﮴ ﮴ ﮲﮴‬ ‫أﻣﺎ ٕاذا ن اﻟﻤﺮ ﺾ ﮴ ﮲ﺎول ﺣ ﮴ ﮟ ﮲ ﮵ﻰ اﻟ ﻮم ﮲ ﺎن اﻟﺤﺮﻋﺔ ا ٔﻻوﻟﻰ ﮴ ﮲ﺎوﻟﻬﺎ ﻋ ﮲ﺪ اﺳ ﮴ ﮴ ﮲ﺎﻃﻪ ﺻ ﺎﺣﺎ‪2-‬‬ ‫﮳‬ ‫﮵‬ ‫﮵‬ ‫﮳‬ ‫﮵‬ ‫﮵‬ ‫﮳‬ ‫﮵‬ ‫﮵‬ ‫‪.‬واﻟﺤﺮﻋﺔ اﻟ ﮶ﺎ ﮲ ﮵ﺔ ﮵ ﮴ ﮲ﺎوﻟﻬﺎ ﮳ﻌﺪ ‪ 8‬﮲ﺳﺎﻋﺎت ﮴ ﮴ ﺮ ﮵ ﮳ﺎ )وﻟ ﮵ﺲ ﮳ﻌﺪ ‪ 12‬ﺳﺎﻋﺎت( وﻟ ﮲ ﮲ ﺲ اﻟﺴ ﮳ﺐ أﻋﻼه‬ ‫﮳‬ ‫‪6- Nitrates should not be used within 24 hours of taking sildenafil or‬‬ ‫‪vardenafil or within 48 hours of taking tadalafil because of the potential for‬‬ ‫‪life-threatening hypotension (3).‬‬ ‫‪Nitrates‬‬ ‫‪Scientific name‬‬ ‫‪Trade names‬‬ ‫‪Dosage form‬‬ ‫‪19‬‬ 1 Glyceryl trinitrate Angised (GSK) Sublingual tablet 100mg 2 Glyceryl trinitrate Transiderm –Nitro (Novertis) Patch 3 ISDN Isordil S.R TAB. 20. Isoket retard (UCB pharma) Tab. 10 ,20. 4 ISMN Ismo (durtin ) Tab. 10 , 20. Any extra notes: Antiplatelet drugs-2.8 1- Antiplatelet drugs reduce platelet aggregation and are used to prevent further thromboembolic events in patients at risk (e.g. patients who have suffered myocardial infarction) (3). 2-The most commonly used Antiplatelet drugs in Iraq are aspirin (at low dose) and clopidogrel. Less commonly is dipyridamole. 3- A-Clopidogril may be given as an alternative to aspirin (in patients who cannot take aspirin ) (2). B- Clopidogril may be given in combination with aspirin in some conditions like myocardial infarction (2). 4-Aspirin tablet commonly formulated as enteric coated tablet to decrease GIT irritation. Antiplatelet drugs Scientific name Trade names Dosage form 1 Aspirin (low dose) Nu-seal Aspirin (Alliance ) Tab. 75 , 300 , 81. 2 Clopidogril Plavix (Sanofi-Aventis) Tab. 75 , 300. 3 Dipyridamole Persantin (Boehring ingelheim) Tab. 100 , Amp. 5mg /mL Any extra notes: Anticoagulants -2.9 Anticoagulants are used in the treatment and prophylaxis of-1.thromboembolic disorders (1) 20  : Anticoagulants available in Iraq now are -2. A-Oral anticoagulants : Warfarin B- Parenteral anticoagulants (mostly given subcutaneously)which :include.Heparin (called unfractionated heparin)-1 Low-molecular-weight heparins (LMWHs) like enoxaparin: which -2 have many advantages over unfractionated heparin like lower risk of.bleeding Anticoagulants can cause bleeding , therefore their anticoagulant effects must-3 : be monitored by laboratory test to avoid excessive bleeding A-Warfarin is monitored by a test called international normalized ratio.(INR ) B- Unfractionated heparin is monitored by a test called activated.partial thromboplastin time (APTT) Anticoagulants Scientific name Trade names Dosage form 1 Warfarin Coumadin or warfarin Tab. 1 ,3 , 5 2 Unfractionated heparin 3 Enoxaparin Celexane (Sanofi-Aventis) Amp. 1000 , 2000 , 3000, 4000, 5000, 6000 4 Dalteparin sodium Fragmin (Pfizer) Amp. 12500 I.U ,25000 I.U Any extra notes: Miscellaneous cardiovascular drugs -2.10 Digoxin-1 A- The most common use of digoxin is for certain type of arrhythmia.called atrial fibrillation (AF).B- Less commonly it is used for heart failure :Methyldopa -2.Methyldopa used mostly for the treatment of hypertension in pregnancy :Tranexamic acid and aminocaproic acid -3 They are used to prevent bleeding or to treat bleeding e.g. bleeding associated.with menorrhagia ( excessive menstrual bleeding ) Miscellaneous cardiovascular drugs Scientific name Trade names Dosage form 21 1 Digoxin Lanoxin (Aspen ) Tab. 0.125 , 0.25. 2 Methyldopa Aldmet (Aspen ) Tab. 250 , 500. 3 Tranexamic acid Cyklokapran (Meda , Tab. 500 Pfizer) Amp. 100mcg/mL 4 Aminocaproic Amicor Tab. 500 acid Amp. 250mg/mL Any extra notes: References 1- Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press 2009. 2-BNF 61. 3- Mary Anne koda-kimble (ed.), Applied Therapeutics: The clinical use of drugs, 10th ed.2013 4- Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 8th Edition. 2011. Chapter Three: Respiratory System 3.1-Bronchodilators and Anti-asthma Drugs Note: 1-Administration of drugs by the inhaled route delivers the drug directly to the Airways with fewer systemic side effects than either the parenteral or oral routes (1,2). 22 2-Commonly inhalation dosage forms available in Iraq are inhaler, nebulizer, and turbohaler (the use of turbohaler is much easier than inhaler). How to use a metered dose inhaler 1. Remove the cap covering the mouthpiece and check that there is no fluff or dirt in the mouthpiece. 2. Shake the inhaler. 3. If the inhaler is new or has not been used for some time it will need to be tested. To test: Hold the inhaler away from body. Press the top of the aerosol canister once. A fine mist should be puffed into the air. The inhaler is now ready to use. 4. Tilt head back slightly. 5. Breathe out gently. 6. Place the mouthpiece in the mouth between the teeth (do not bite). Close lips around the mouthpiece. 7. Start to breathe in slowly through the mouth, at the same time press down on the inhaler to release the medicine in to the lungs. 8. Hold breath for between 5 and 10 seconds, then breathe out slowly. 9. If a second dose is required, wait approximately 30 seconds and repeat the process. 10. Replace the cap and if the inhaler is a corticosteroid inhaler, rinse the mouth out with water. How to use a Turbohaler A Turbohaler is a dry powder inhaler. To load it prior to use: 1. Unscrew the cover and remove it. 23 2. Hold the Turbohaler upright with one hand and with the other twist the grip in one direction as far as it will go. 3. Now twist back as far as it will go – a click should be heard, showing the inhaler is primed and ready for use. 4. Breathe out gently. 5. Place the mouthpiece between the lips and breathe in through the mouth as deeply and as hard as possible. 6. Remove the inhaler from the mouth and breathe out slowly. 7. Replace the cover. 8. Repeat the above steps if more than one puff is required. 3.1.1-Selective beta2 agonists 1-Short-acting beta2 agonists (SABAs) (such as salbutamol or terbutaline). Because of their rapid onset of action , they are considered the first choice for the treatment of acute asthmatic attack (and other conditions associated with airways obstruction) (1-3). 2-Inhaled SABAs are given ‘as required’ and NOT as Regular treatment (2). 3- Long-acting beta2 agonists Formoterol and salmeterol : they are taken regularly as prophylaxis for chronic asthma or chronic obstructive pulmonary disease (COPD). 4-Note: Salbutamol may be used by some gynecologist as a uterine relaxant for pregnant women. 3.1.2-Inhaled corticosteroid (e.g. Beclomethasone Dipropionate) 1-An inhaled corticosteroid is used regularly for prophylaxis of asthma. 2-They are ineffective for acute asthmatic attack. 3- Inhaled corticosteroid may cause oral candidiasis (oral fungal infection) and this side effect can be reduced by rinsing the mouth with water after inhalation of a dose. 24  Note : 1-Inhaler to relieve acute asthmatic attack examples: salbutamol are generally colored blue. While inhaler for prophylaxis of asthma (like corticosteroid) are generally colored brown or orange ). 2- Some products contain a combination of inhaled corticosteroid and long acting beta2 agonist e.g. Symbicort ® turbohaler (budesonide with formoterol) 3.1.3-Antimuscarinic bronchodilators (ipratropium, and Tiotropium) 1- They are used by inhalation as a bronchodilator in the treatment of asthma and chronic obstructive pulmonary disease (COPD). 2- Tiotropium has the advantage of having a longer duration of action than ipratropium. 3.1.4-Theophylline (and aminophylline ) 1- Theophylline is a bronchodilator used in asthma and chronic obstructive pulmonary disease (2). 2- Theophylline is given by injection as aminophylline. Aminophylline injection must be given by very slow intravenous injection (over at least 20 minutes). 3-The use of sustained release formulation of theophylline (phyllocontine®) is preferred over ordinary tablet (immediate release tablet) and it is usually given twice daily and the sustained release tablet should not be splinted or crushed. 3.1.5-Leukotriene receptor antagonists (montelukast and zafirlukast) 1-They are given orally mainly for prophylaxis of asthma. 2-In addition to ordinary tablet , montelukast also formulated as Chewable tablet which contain a lower dose and intended mainly for children. Bronchodilators and Anti-asthma Drugs Scientific name Trade names Dosage forms 1 Salbutamol Ventolin (A&H ) Tablet, syrup, inhaler, and nebulizer 25  2 Beclomethasone Pulvinal , Becodisk (A&H) Dry powder for Dipropionate Asmabec (USBpharma) inhalation 100mcg. 3 Theophylline Nuelin SA (Meda) S.R tab 175mg Slo-phyllin (Merck serona ) S.Rcap. 60mg 4 Montelukast Singulair (MSD) Chewable tab. 4 , 10 5 Bambuterol Bambec (AstraZeneca) Tab.10mg 6 Salmeterol Serevent (A&H) Dry powder for inhalation 7 Aminophylline Phyllocontin continuous Tab. 225 (Napp) 8 Fluticasone Flixotide (A&H) Dry powder 50 mcg. Any extra notes: Budesonide Easyhaler -Budesonide (Meda , AstraZeneca) Dry powder 100mcg Budesonide +formeterol Symbicort (AstraZeneca) Dry powder for inhalation 3.2-Antihistamines 1-Antihistamines are used in the treatment of nasal allergies (they reduce rhinorrhoea and sneezing )( Antihistamines are frequently used in combination preparations for the treatment of coughs and colds ). Antihistamines are also used to treat urticarial rashes, pruritus, and insect bites and stings (1). 2-The antihistamines may be classified into : A- Sedating antihistamines : older antihistamines that are associated with troublesome sedative and antimuscarinic effects. Example are (chlorphenamine(chlorpheniarmine) maleate, clemastine, cyproheptadine, ketotifen, diphenhydramine, and dimethindene maleate ) (1). Drowsiness is a major problem with the sedating antihistamines and those affected should not drive or operate machinery (1). B- Non-sedating antihistamines : are newer antihistamines, they generally cause little or no drowsiness (1). Example are (cetirizine, levocetirizine , loratadine , desloratadine, fexofenadine). 3- Because of their antimuscarinic actions (like urinary retention), the sedating antihistamines should be used with caution in conditions such prostatic hyperplasia. Antimuscarinic adverse effects are not a significant problem with the non-sedating antihistamines (1). 4-Important : Cyproheptadine has been widely used as an appetite stimulant , but in the long-term appears to have little value in producing weight gain and 26 such use is no longer generally recommended (1). 5-Diphenhydramine has pronounced sedative properties and may be used as a hypnotic in the short-term management of insomnia (taken before bedtime) (1). Antihistamines Scientific name Trade names Dosage forms 1 Chlorpheniarmine Histadin Tab. 4 mg Piriten (GSK consumerhealthycar) 2 Diphenhydramine Allermine Tab.25 , syrup. 25/5mL 3 Cyproheptadine Periactin (Auden Mckenzte) Tab.4mg. Syrup 2mg/mL 4 Ketotifen Zaditen (Swedish orphan ) Tab. 1mg Elixir 1mg/mL 5 Dimethindene Fenistil (Novertis) Tab.4mg Oral drop 1mg/1mL 6 Loratadine Loratin Syrup 5mg/5mL Tab. 5, 10 7 Desloratadine Neoclarityn (MSD) Tab. 5 , syrup 2.5mg/5mL 8 Fexofenadine Telfast (Sanofi-Aventis ) Tab. 120 ,180. 9 Hydroxyzine Atarax (Alliance ) Tab. 10 , 25. Any extra notes: 3.3-Cough preparations 1- Cough suppressants (antitussive ): like Codeine, and dextromethorphan are used for dry cough. 2- Expectorants (e.g. Glyceryl guaiacolate (also called Guaifenesin)) and Mucolytics (e.g. Bromohexine ): which are used for wet cough. 3-Commonly, cough preparations contain a combination of antitussive or expectorants, antihistamine, and / or sympathomimetic (for congestion). 4-Lozenges may also be used for cough especially for pregnant women. Cough preparations Scientific name Trade names Dosage form 1 Bromoxine HCl Solvodin® Tab. 8mg , syrup 4mg/5mL 2 Dextromethorphan Sedilar® Tab. 15 , syrup 15mg/5mL 27 3 Chlorphenaramine , Tussiram® Syrup phenylephrine , Ephedrine , codeine 4 Chlorphenaramine , Pulmocodin® Syrup phenylephrine , vit. C , codeine , Glyceryl guaiacolate 5 Diphenhydramine , Al- Samillin® Syrup Chloride, Na-citrate, menthol. 6 Chlorphenaramine , Tussilet ® Syrup Glyceryl guaiacolate , phenylephrine 7 Diphenhydramine , NH4 Cl Pectomex® Syrup , Tulo syrup , phenylephrine Pectomed ® 8 Dextromethorphan , Toxil ® Syrup oxomemazine , Na-benzoate Any extra notes: 3.4-Orally administered nasal decongestants 1-These are usually contain a combination of sympathomimetics like pseudoephedrine and phenylphrine (they reduce nasal congestion) and antihistamine (like triprolidine) (they reduce rhinorrhoea and sneezing). 2- Systemic decongestants (sympathomimetics ) should be used with caution in hypertension, hyperthyroidism, and ischaemic heart diseases (1). Orally administered nasal decongestants Scientific name Trade names Dosage form 1 Paracetamol 450mg , promethazine Coldin® Tablet 5mg , phenylephrine 5mg 2 Paracetamol , vit.C , chlorpheniramine Flu-out® Tablet 3 Triprolidine 2.5mg, Actifed® Tablet and Pseodoephedrine 60mg tablet and syrup Triprolidine 1.25mg, yellow colored Pseodoephedrine 30mg syrup 4 Actifed® syrup green colored syrup 28  5 Actifed® red syrup colored syrup 6 Paracetamol ,caffeine , phenylephrine Panadol cold Tablet and flu® (yellow color) 7 Paracetamol , Pseodoephedrine 30mg Panadol cold Tablet Chlorpheniramine maleate 2mg and flu® (green color) 8 Paracetamol , Pseodoephedrine 30mg Panadol Tablet sinus® 9 10 References 1- Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press 2009. 2- BNF 61. 3- Mary Anne koda-kimble (ed.), Applied Therapeutics: The clinical use of drugs, 10th ed.2013. Chapter Four : Central nervous system Note: most of the CNS drugs (like antipsychotics, antidepressant, antiepileptics, anxiolytics, hypnotics, opioid analgesics can cause drowsiness, thereby affecting the ability to drive and operate hazardous machinery and patients should be warned about this. 4.1-Hypnotics and anxiolytics 1- Hypnotics are used for patients with insomnia, while anxiolytics are used for patients with anxiety (2). 2-Prescribing of these drugs is widespread but dependence and tolerance occur. This may lead to difficulty in withdrawing the drug. 3-Hypnotics and anxiolytics should be reserved for short courses to alleviate acute conditions after causal factors have been established (2). 4-Benzodiazepines are the most commonly used anxiolytics and hypnotics. The most commonly Benzodiazepines available in Iraq now are : (Alprazolam, Chlordiazepoxide, Diazepam, and Lorazepam) 29  Benzodiazepines Scientific name Trade names Dosage form 1 Diazepam Valium Tab.2 , 5 ,10. Amp.1mg/mL, syrup 2mg/5mL 2 Lorazepam Ativan Tab.1 ,2.5 , amp.4mg/mL 3 Chlordiazepoxide Librium Tab. 5 , 10. Cap. 5, 10. 4 Alprazolam Xanax or zolam Tab. 0.25 , 0.5 Any extra notes: 4.2-Antipsychotic drugs (for treatment of schizophrenia) Note: Long-acting depot injections antipsychotic are used for maintenance therapy especially when compliance with oral treatment is unreliable. Depot antipsychotics are administered by deep intramuscular injection at intervals of 1 to 4 weeks (2). 1-Classification of the Antipsychotics Antipsychotics have been broadly classified into two groups. A-The older agents are referred to as typical or conventional antipsychotics. 1- They can also be classed by chemical structure (phenothiazine and nonphenothiazine). 2- common adverse effects (extrapyramidal symptoms (EPS), sedation, anticholinergic, and cardiovascular effects) 3- Examples of typical agents include haloperidol, fluphenazine, chlorpromazine, and thioridazine (6). 4-Notes concerning chlorpromazine: - It is used in the alleviation of intractable hiccup (‫)ﺳﻬ ﮵ ﮴ ﺔ‬ ‫﮶‬ (1). - Important; Warning: Owing to the risk of contact sensitization, pharmacists, nurses, and other health workers should avoid direct contact with chlorpromazine; tablets should not be crushed and solutions should be handled with care (2). 5- Notes concerning prochlorperazine: 30  - Prochlorperazine is widely used in the prevention and treatment of nausea and vomiting (1). - Prochlorperazine also used for the symptomatic relief of vertigo (1). B-Atypical antipsychotics 1-Newer antipsychotics such as clozapine , risperidone, olanzapine and quetiapine are often referred to as atypical antipsychotics because of their reduced tendency to cause the extrapyramidal effects (1) (better tolerated than other antipsychotic drugs) (2). Antipsychotics(Both typical and Atypical antipsychotics) Scientific name Trade names Dosage form 1 Prochloperazine Stemtil Tab. 5. Amp. 2 Haloperidol Haldo (Janssen) , (Teva- Tab. 5 , 10. cap. 0.5mcg UK) 3 Chlorpromazine Largactil (Sanofi- Tab.25, 50 , 100 , Aventis ) amp.25mg/mL, syrup 25mg/mL 4 Clozapine Clozaril (Novertis) Tab. 25 , 100. 5 Olanzapine Zyprexa (Lilly) Tab. 2.5 , 5, 7.5 , 10, 15, 20. 6 Quetiapine Seroquel (AstraZeneca) Tab. 25 , 100 , 150 , 200, Seroquel XL (AstraZeneca) 300. Any extra notes: (Janssen) 7 Risperidone Risperidal tab. 0.5 , 1, 3 , 6. 4.3-Antidepressant drugs The major classes of antidepressant drugs availablr in Iraq include the tricyclic and related antidepressants (TCAs), the selective serotonin re-uptake inhibitors (SSRIs). 4.3.1- SSRIs 1-SSRIs include : Citalopram, escitalopram, fluoxetine, paroxetine, and sertraline. 2-SSRIs are generally chosen as first-line antidepressants because of their safety in overdose and improved tolerability compared with earlier agents (4). The SSRIs produce fewer sedative, anticholinergic, and cardiovascular adverse effects than the TCAs and are less likely to cause weight gain than the TCAs (4). 31  3-Important : In the treatment of depression the usual initial dose of fluoxetine is 20 mg once daily; US product information recommends giving this dose in the morning (1). 4- Some SSRIs are also used as part of the management of generalised anxiety disorder, obsessive-compulsive disorder, panic disorders. Fluoxetine is also used in the treatment of premenstrual syndrome (1). 5-The most common adverse effects associated with this class of agents include GI complaints, insomnia, restlessness, headache, and sexual dysfunction (5). SSRIs Scientific name Trade names Dosage form 1 Citalopram Celax Tab. 10, 20 ,40 , oral drop Cipramil (lundbeck) 40mg /mL 2 Fluoxetine Prozac (Lilly) Cap. 20 ,40, Liquid 20mg /5mL 3 Sertraline Zoloft Tab. 50 , 100. Lustal (Pfizer) Any extra notes: 4.3.2-TCAs and related antidepressants 1-Examples are Amitriptyline, Clomipramine, and Imipramine. 2-TCAs are antidepressants, but their use has diminished because of the availability of equally effective therapies that are safer on overdose and better tolerated (4). 3-TCAs have α-adrenergic blockade, antihistaminic effects, and anticholinergic effects, which lead to orthostasis, sedation, and anticholinergic symptoms, respectively. They also lead to cardiotoxic effects (5). 4-Some TCAs are used in the management treatment for Neuropathic pain, migraine prophylaxis, anxiety disorders and in nocturnal enuresis in children (2. 5). 32  TCAs and related antidepressants Scientific name Trade names Dosage form 1 Imipramine Tofranil Tab. 10 , 25. Syrup 25mg/5mL 2 Amitriptylline Elavil Tab.10 ,25, 50. Triptafen (Mercury) syrup. 25mg/5mL 3 Trazodone Desyrel Cap. 50, 100, tab. 150. Molipaxin (Sanofi Aventis) Any extra notes: 4.3.3-Serotonin Norepinephrine Reuptake Inhibitors (Duloxetine) 1-Duloxetine is used in the treatment of depression (1). 2-Duloxetine is also used in the treatment of generalized anxiety disorder, treatment of diabetic peripheral neuropathic, and the treatment of moderate to severe stress urinary incontinence in women (1). Scientific name Trade names(if available) Dosage form Venlafaxine Effexor Cap. 75, 150. Epexor XL (Pfizer) Any extra notes: Duloxetine Cymbalta (Lilly) cap. 30, 60. 4.4-Anti-obesity drugs acting on the GIT (Orlistat) Orlistat is a gastric and pancreatic lipase inhibitor that limits the absorption of-1.dietary fat (1) 2-It is used together with dietary modification in the management of obesity , i.e. in patients with a BMI of 30 kg/m 2 or greater. It may also be used in overweight patients with a BMI of 27 kg/m2 or more if there are associated risk factors (such as type 2 diabetes, hypertension) (1). ,Orlistat is given in a usual dose of 120 mg orally three times daily-3 immediately before, during, or up to 1 hour after meals. If a meal is missed 33.or contains no fat, the dose should be omitted Orlistat therapy should be stopped if the patient does not lose at least 5% of-4.their body-weight during the first 12 weeks of therapy (1) Scientific name Trade names Dosage form Orlistat Xenical Cap. 60 , 120. Any extra notes: 4.5-Drugs used in nausea and vertigo.See also antiemetics in chapter one -1 5HT3-receptor antagonists (like ondansetron) are of value in the -2 management of nausea and vomiting in patients receiving cytotoxics and in.postoperative nausea and vomiting (2) Dexamethasone has antiemetic effects and it is used in vomiting associated -3 ,with cancer chemotherapy. It can be used alone or with metoclopramide.prochlorperazine, lorazepam, or a 5HT3 antagonist (2) ,Betahistine is an analogue of histamine and is licensed for vertigo tinnitus -4.and hearing loss associated with Me´nie`re’s disease (2) Me´nie`re’s disease is a disorder of the inner ear that can affect hearing and) -balance to a varying degree. It is characterized by episodes of vertigo, low.(pitched tinnitus, and hearing loss Scientific name Trade names Dosage form Betahistine Betaserc Tab. 8, 16 Serc (Abbot healthcare) Ondansetron Zofran (GSK) Tab.4 , 8 , Syrup 4mg/5mL Amp.2mg/mL Any extra notes: 4.6-Analgesics 4.6.1-non-steroidal anti-inflammatory drugs (NSAIDs). 34 See chapter Nine. 4.6.2-Paracetamol 1- Paracetamol has analgesic and antipyretic effects but no anti- inflammatory effect. Paracetamol is a suitable analgesic for children (2). 2-Over-dosage with paracetamol is particularly dangerous as it may cause hepatic damage (2). 3-Patient should be advised not to take more than 1g ( usually 2 tablet of 500 mg) at any one time. And not take more than 8 tablets (4 gm) in 24 hours (2). 4-Compound analgesic preparations containing paracetamol with a low dose of an opioid analgesic (e.g. 8 mg of codeine phosphate per compound tablet) are commonly used, but the advantages have not been substantiated. The low dose of the opioid may be enough to cause opioid side-effects (in particular, constipation) and can complicate the treatment of overdosage yet may not provide significant additional relief of pain (2). Paracetamol(Compound analgesic preparations) Scientific name Trade names Dosage form 1 Paracetamol (alone) Panadol , Tab. 500 , 650 ,1000. Dilopran, Syrup 120mg/5mL , drop100/20drop. Amp.100 ,375 ,300. Antipyrol 2 Paracetamol 350 , Algesic® Tab. Caffeine 50 , Codeine 10. 3 Paracetamol , No pain Cap. 350+200+40. Ibuprofen , caffeine Novafen 4 Paracetamol , caffeine Saridon (Bayer Cap. 250 +50+150. healthcare) Propyphenozon Any extra notes: 5 Aceclofenac ,paracetamol Actinac tab. 100+ 500. 6 Acetaminophen ,caffeine , A.S.A Excedrin tab. 250+65+250. 4.6.3-Opioid analgesics 1-Opioid analgesics are usually used to relieve moderate. Repeated administration may cause dependence and tolerance (2). 35 Opioids such as codeine or dextropropoxyphene are used in the treatment of-2 less severe pain, and are often combined with non-opioid analgesics such as.aspirin, other NSAIDs, or paracetamol (1) More potent opioids such as morphine are used in severe acute and chronic-3.pain, including cancer pain (1) ,Tramadol produces has fewer of the typical opioid side-effects (notably-4.less respiratory depression, less constipation and less addiction potential (2).(Note: However, tramodaol is abused by some Iraqi addicts) The most common side-effects include nausea and vomiting (particularly in-5.initial stages), and constipation (2) Opioids should be used with caution in patients with impaired respiratory -6 function (avoid in chronic obstructive pulmonary disease) and asthma (avoid.during an acute attack) (2) Scientific name Trade names Dosage form Tramal Cap. 50 Tramadol Zamadol (Meda) Tramquel (Meda) Any extra notes: 4.6.4-Neuropathic pain.Neuropathic pain, occurs as a result of damage to neural tissue (2)-1.Neuropathic pain is generally managed with a tricyclic antidepressant (e.g -2 ,Amitriptyline ) or with certain antiepileptic drugs ( carbamazepine.Gabapentin, and pregabalin) (2).Neuropathic pain may respond to opioid analgesics (2)-3 4.6.5-Antimigraine drugs Treatment of acute migraine Treatment of a migraine attack should be guided by response to previous-1 ,treatment and the severity of the attacks. A simple analgesic such as aspirin paracetamol.or a NSAID is often effective (2) (preferably in a soluble or dispersible form) 36 Peristalsis is often reduced during migraine attacks the medication may ) not be sufficiently well absorbed to be effective; dispersible or effervescent.preparations are therefore preferred ) (2) Concomitant antiemetic treatment may be required (2) (e.g. cyclizine in-2.migril®). (migraine attack is usually associated with nausea) If treatment with an analgesic is inadequate, an attack may be treated with a-3 specific antimigraine compound such as a 5HT1-receptor agonist (‘triptan’) (like.sumatriptan) (2) 4-The value of ergotamine for migraine is limited by its side-effects , it is best avoided (2). 4-Triptans and ergotamine are contra-indicated in ischemic heart disease (2). Note : Very important: The maximum recommended doses of ergotamine preparations should not be exceeded ( should not exceed the maximum dose per attack, the maximum dose per day as well as the maximum dose per week). Triptans and ergotamine Scientific Trade names Dosage form Dose during migraine name attack 1 Sumatriptan Imigran (GSK) Tab.50 , 100. 1-2 tab. At attack, 2nd dose after 2hrs. max. dose 6 tab. In 24 hrs. Imigran Radi (GSK) 2 Ergotamine Migril (Warkhardt) Tab. 2mg 1 tab. At attack, 2nd dose after 30 min. max. dose 3tab. In 24 hrs , tartarate Caffeine 100mg max. dose 6 tab. In week Cyclizine 50mg Any extra notes: Prophylaxis of migraine Where migraine attacks are frequent, preventive treatment for migraine should-1.be considered (2) :drugs that are used for Prophylaxis of migraine include -2.A-The beta-blockers (e.g. Propranolol is the most commonly used ) (2) 37 ,B-Tricyclic antidepressants, and antiepileptics (topiramate, sodium valproate.valproic acid, and gabapentin ) are also effective for preventing migraine (2).C-Pizotifen is of limited value and may cause weight gain (2) Scientific name Trade names Dosage form Sanomigran (Novertis) Tab. 0.5 , 1.5 Pizotifen Elixir 0.25mg/5mL Syrup 0.25mg/5mL Any extra notes: 4.7-Antiepileptic drugs (AEDs) :Example of some antiepileptic drugs available in Iraq are-1 , Carbamazepine , Gabapentin , Lamotrigine , Levetiracetam , Phenytoin. Pregabalin , Topiramate , and Valproate The choice of an AED depends on the seizure type, potential for drug -2.interactions and side effects, cost and physician familiarity with the drug (7) Usually therapy is initiated at low dose and gradually increased over 3 or -3.weeks to an effective dose (4) 4 ,One chronic adverse effect that is of concern is osteoporosis. Carbamazepine -4 phenytoin, Phenobarbital , and valproate have all been shown to decrease bone mineral density, even after only 6 months of treatment. Patients taking these drugs for longer than 6 months should take supplemental calcium and.vitamin D (8) :AEDs are associated with many different drug interactions -5 A-Phenobarbital, phenytoin, and carbamazepine are potent inducers of various CYP-450 isoenzymes, increasing the clearance of other drugs.metabolized through these pathways.B-Valproic acid inhibits many hepatic enzyme systems (4, 8) Antiepileptic drugs Scientific name Trade names Dosage form 1 Carbamazepine Tegretol (Novertis) 38  Tab.100, 200, 400, syrup 100mg/5mL, supp125mg 2 Gabapentin Neurontin (Pfizer ) Cap.100, 300,400 3 Pregabalin Lyrica (Pfizer) Cap.25,50,75. Syrup 20mg/mL 4 Lamotrigine Lamictal (GSK) Tab.25,50,75,100,200 5 Phenobarbital Luminal Tab.15,30,60. Amp.200/mL Elixir 15mg/5mL 6 Sodium Valproate Depakine Tab.100,200 Epilim (Sanofi-Aventis) Syrup 200mg/5mL Any extra notes: 4.8-Drugs used in parkinsonism The primary objective of drug therapy is to enhance dopaminergic activity -1 within the damaged areas of the basal ganglia , and this is achieved in various.ways (see table below) (3) 39  Antiparkinsonian drugs Scientific name Trade names Dosage form 1 Bromocriptine Parlodel (Meda , Novertis) Tab. 2.5 , 1.25 2 Levodopa/ Sinemet (MSD) Tab.50/12.5 , 100/10, carbidopa 100/25 3 Procyclidine Kemadrin (Aspen) Tab.5 4 Orphenadrine Biorphen (Alliance) Syrup 25mg/mL, Disipal (Astellas) S.R tab.50mg Any extra notes: 4.9-Drugs for smoking cessation Nicotine replacement therapy (NRT), bupropion, and varenicline are effective aids to smoking cessation (2). 40 4.9.1- Bupropion 1- Bupropion is an antidepressant drug (1). 2-For smoking cessation, treatment should be started about 1 to 2 weeks before the patient attempts to stop smoking , to allow steady-state blood levels of bupropion to be reached, and normally continues for 7 to 12 weeks; if there is no significant progress towards smoking abstinence by the seventh week, then therapy should be stopped (1). 4.9.2- Varenicline 1- Varenicline is a selective nicotinic receptor partial agonist that is used as an aid for smoking cessation (1). 2- Patients are advised to set a date to stop smoking and start varenicline 1 to 2 weeks before. Treatment is normally given for 12 weeks; in patients who successfully stop smoking, a further 12 weeks of treatment has been recommended to reduce the risk of relapse (1). 4.9.3-NRT 1-The first-line pharmacological intervention is NRT (1). 2-NRT is available in numerous formulations: chewing gum, transdermal patches, inhalators, nasal sprays, sublingual tablets, and lozenges (1). 3-Choice of formulation is based on patient preference, tolerance, and previous treatments, if any. A-The transdermal patch is easiest to use and compliance is greatest with this route but local effects may be troublesome. B-The gum has an unpleasant taste initially and some find the chewing action difficult. C-The sublingual tablet may be useful for those who have difficulty chewing the gum. D-The nasal spray has a fast onset of action but may cause local irritation. E-The inhalator has the advantage of simulating cigarette smoking but may cause local irritation of the mouth and throat. The lozenge has the advantage that it can be sucked discreetly (1). 4-NRT for smoking cessation is usually continued for about 3 months before being withdrawn (1). Drugs for nicotine dependence (if available) Scientific name Trade names Dosage form 41 1 Bupropion Zyban (GSK) S.R tab. 150 2 Nicotine Nicotinell (Novertis) Chewing gum 2mg, 4mg. Niquitin (GSK) Mint lozenge 1mg ,2mg. 3 Varenicline Champix (Pfizer) Tab. 0.5 , 1. Any extra notes: 4.10-Drugs for dementia 1-In dementia, there is a is a deterioration memory, judgement, language and communication. Alzheimer’s disease is the most common cause of dementia and accounts for over half of all patients; about one-third of dementia cases are due to vascular disease (1). 2-Donepezil, galantamine, and rivastigmine are the main cholinesterase inhibitors. All have produced modest improvement in patients with mild to moderately severe disease (1). Acetylcholinesterase inhibitors can cause unwanted cholinergic side-effects (2). 3-Memantine is a glutamate receptor antagonist; it is licensed for treating moderate to severe Alzheimer’s disease (2). Drugs for dementia Scientific name Trade names Dosage form 1 Domepezil Aricept (Eisal) Tab.5, 10. 2 Galantamine Reminyl (shire) Tab. 8, 12. Syrup 4mg/ mL 3 Rivastigmine Exelon (Novertis ) Cap. 1.5 ,3 , 4.5 , 6. Syrup 2mg/mL Any extra notes: References 1- Sean C. Sweetman. Martindale: The Complete Drug Reference, 36th Edition. Pharmaceutical Press 2009. 2- BNF 61. 42 3- Russell J Greene, Norman D Harris. Pathology and Therapeutics for Pharmacists : A basis for clinical pharmacy practice third edition. 2008 by pharmaceutical press. 4- Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach, 8th Edition. 2011. 5- ACCP Updates in Therapeutics 2012. 6- Mary Anne koda-kimble (ed.), Applied Therapeutics: The clinical use of drugs, 10th ed.2013. 7- Canadian pharmacists association. Therapeutic choices. 2011. 8- Marie A. Chisholm-Burns.Pharmacotherapy Principles & Practice Copyright © 2008 by The McGraw-Hill Companies. Chapter Five : Infections This chapter include : 1-Antibacterial drugs 2-Antifungal drugs 3-Antiviral drugs 4-Antiprotozoal drugs 5-Anthelmintics 43 Antibacterial drugs-5.1 Penicillins-5.1.1 Classification of penicillins -1 Penicillin groups Examples 1 Natural penicillins Benzylpenicillin and phenoxymethylpenicillin 2 Penicillinase-resistant Flucloxacillin, cloxacillin penicillins 3 Broad-spectrum penicillins Amoxixillin, ampicillin 4 Antipseudomonal Piperacillin, Ticarcillin penicillins 2-The most important side-effect of the penicillins is hypersensitivity which causes rashes and anaphylaxis and can be fatal (1). 3-Ampicillin , flucloxacillin and cloxaciliin must be given on an empty stomach (This means an hour before food or 2 hours after food) while amoxicillin maybe taken without regard to meal (1). 4-Co-amoxiclav consists of amoxicillin with the beta-lactamase inhibitor clavulanic acid. Clavulanic acid inactivates beta-lactamases, making the combination active against beta-lactamase-producing bacteria that are resistant to amoxicillin (1). 5-Various combinations between amoxicillin and Clavulanic acid are presents: Combinations Dosage form Notes 156 ( 125 +31) suspension 312 ( 250 + 62) suspension 457(57 + 400 ) suspension Given twice daily(every 12 hours) (125 + 250 ) 375 Tablet (125 + 500 )625 Tablet (125+ 875 ) 1000 Tablet Given twice daily(every 12 hours) (100 + 500) 600 Injection For intravenous injection only (200 + 1000) 1200 Injection For intravenous injection only 6-For the eradication of H. pylori (a bacteria that cause ulcer), amoxicillin is given with clarithromycin and a proton pump inhibito r; usual doses of amoxicillin for the eradication of H. pylori is 1 g twice daily (or less commonly 500 mg three times daily) (1, 2). Penicillins 44  Scientific name Trade names Dosage form 1 Amoxicillin Amoxil (GSK) Cap.250, 500, tab.1000 , susp.125/5mL , 250/5mL 2 Co-amoxiclave Augmentin (GSK) Tab.625 , 375, 800,1000 , susp. 312.5/5mL ,457/5mL 3 Ampicillin- Ampiclox Cap.(250+250) , vial 500 , cloxacillin susp. 250/5mL 4 Ampicillin Penbritin (Chemidex) Cap.250 , 500, susp. Ampicillin 250/5mL 5 Benzathine Penicillin Troge Vial 1.2 mega/2mL Any extra notes: 5.1.2-Cephalosporins 1-Classification Groups Examples 1 First-generation Cefalexin and cefadroxil 2 Second -generation Cefuroxime 3 Third-generation Cefotaxime, ceftazidime ceftriaxone, cefixime, cefpodoxime 4 Fourth-generation Cefepime 2-In general the activity against gram negative bacteria is increase and the activity against gram positive bacteria is decrease when we move from first to third generations cephalosporins. 3-Some important properties for specific agents (1): Drug Properties Ceftriaxone Has a longer half-life ( may be given once daily ). Ceftazidime Has good activity against pseudomonas. Cefixime Oral third-generation cephalosporin. Cefpodoxime Oral third-generation cephalosporin (must be given after food ). 4-The principal side-effect of the cephalosporins is hypersensitivity and about 0.5–6.5% of penicillin-sensitive patients will also be allergic to the cephalosporins. Patients with a history of immediate hypersensitivity to penicillin should not receive a cephalosporin (contraindicated) (1). 5-Note : important: when given by an intravenous injection, most of these drugs should be given over at least 2–4 minutes ( arrhythmias following rapid injection reported) (1). 45  ٕ ‫ﺳﺤﻠﺖ اﻟﻌﺪ ﮵ﺪ ﻣﮟ ﺣﺎﻻت اﻟﻮ ﮲ ﮵ﺎت ﮲ ﮵ﻰ اﻟﻌﺮاق ﮲ ﮵ ﮳ﺤﺔ‬ ‫اﻻﻋﻄﺎء اﻟﻮر ﮵ﺪي اﻟﺴﺮ ﮵ﻊ ﻟﺪوا ٔ ﮵ﻰ‬ ‫ و﮴ﺪ ﮳‬: ‫﮴‬ ‫﮲‬ Cefotaxime, and ceftriaxone Cephalosporins Scientific name Trade names Dosage form 1 Cefalexin Keflex (Flynn) Cap. 250 , 500, Susp. 125/5mL , 250/5mL 2 Cefotaxime Claforan Vial. 0.5g , 1g 3 Ceftriaxone Ceftriaxone , Vial. 0.25g , 0.5g ,1g. Rocephin (Roche) 4 Cefixime Suprax (Sanofi-Aventis) Cap. 100 , 200 , 400. Susp. 100/ 5mL 5 Cefpodoxime Orebx (Sanofi-Aventis) Tab. 100 , 200 , susp. 50/5mL Cefodox Susp.100/5mL 6 Cefdinir Omnicef , Susp. 125/5mL Sefarin (pharma international) Tab. 300mg. Any extra notes: 5.1.3-Carbapenems (imipenem, meropenem) 1- The carbapenems are beta-lactam antibacterials with a broad-spectrum of activity which includes many Gram positive and Gram-negative bacteria, and anaerobes (1). 2-Imipenem is partially inactivated in the kidney by enzymatic activity and is therefore administered in combination with cilastatin, a specific enzyme inhibitor, which blocks its renal metabolism. Carbapenems Scientific name Trade names Dosage form 1 Imipenem Primaxin (MSD) I.V infusion vial 500mg 2 Meropenem Meronem® (AstraZeneca) 500-mg and 1-g vial Any extra notes: 46 5.1.4-Tetracyclines (like Tetracycline, and Doxycycline) 1-Doxycycline has longer duration than tetracycline and may be given once or twice daily. 2-Important : Oral administration : A-Tetracycline must be given on an empty stomach (This means an hour before food or 2 hours after food) while Doxycycline is given during meals (1). B- Capsules (of both drugs) should be swallowed whole with plenty of fluid while sitting or standing (1) (because it may cause oesophageal irritation). 3-Deposition of tetracycline s in growing bone and teeth (by binding to calcium) causes staining, and they should not be given to children under 12 years, or to pregnant or breast-feeding women (1). 4- Common indications for doxycycline include: genital Chlamydia, acne, and brucellosis (in combination with rifampicin) (1). Tetracyclines Scientific name Trade names Dosage form 1 Doxycycline Vibramycin-D (Pfizer) Cap.100 , 500. 2 Tetracycline Sumycin Cap.250 , 500 , Skin oint.3% ,eye 1% Any extra notes: 5.1.5-Aminoglycosides 1- These include amikacin, gentamicin, neomycin, streptomycin, and tobramycin (1). 2- The aminoglycosides are not absorbed from the gut and must therefore be given by injection for systemic infections (1). 3-The important side-effects are ototoxicity, and nephrotoxicity (1). 4-Streptomycin is used mainly for tuberculosis (2nd line drug) and for brucellosis (1). 47  Aminoglycosides Scientific name Trade names Dosage form 1 Amikacin Amikin (Bristol-Myer-Squibb) Vial 100 , 500. 2 Gentamycin Garamycin , Amp.80/2mL ,40/2mL Genticin (Amdipharm) Eye drop 0.3% Cidomycin (SAnofi-Aventis) 3 Tobramycin Tobrex Eye ointment 0.3% Tobi (Novertis ) Nebulizer sol. 60/mL 4 Streptomycin Streptomycin Vial 1g Any extra notes: 5.1.6- Macrolides 1- These include Erythromycin, Azithromycin and Clarithromycin (1). 2- Azithromycin has a long half-life and once daily dosage is recommended (1). 3-Important : Azithromycin capsules must be given on an empty stomach (an hour before food or 2 hours after food) while Azithromycin tablet and suspension are given without regard to meal (1). 4-Clarithromycin is usually given twice daily. And it is one of the component of triple therapy for eradication of H. pylori (a bacteria that cause ulcer) (1). Macrolides Scientific name Trade names Dosage form 1 Azithromycin Zithromax (Pfizer) Tab. Or cap. 250 , 500, Susp.40/mL 2 Clarithromycin Biaxin Tab.250 ,500 Kloricid (Abbott healthcare) Susp.125/5mL 3 Erythromycin Erythrocin (Amdipharm) Tab.500, cap.250 , Erymax (Cepholon ) susp.200/5mL Any extra notes: 5.1.7-Quinolones 48 1- These include Nalidixic acid, Norfloxacin, Ciprofloxacin, Gatifloxacin, Ofloxacin, Levofloxacin, Moxifloxacin (1, 2). 2- Ciprofloxacin is the drug of choice for typhoid fever (1). 3- Nalidixic acid is used mainly in the treatment of lower urinary-tract infections (1). (It should be avoided in infants less than 3 months old ) (1, 2). 4- Administration A- Norfloxacin should be taken on an empty stomach (1). B- Important: Ciprofloxacin and Norfloxacin should not be taken with Dairy products (interfere with the absorption) (1, 2). 5- Quinolones cause acute haemolytic anaemia when taken by individuals with Glucose 6-phosphate dehydrogenase (G6PD) deficiency (1). 6-One disadvantage of the quinolone antibacterials is that they are generally not recommended for use in children, adolescents, and pregnant or breast- feeding women because of their propensity to cause joint erosions in immature animals (2). Quinolones Scientific name Trade names Dosage form 1 ciprofloxacin Cipro , Ciproxin (Bayer) Tab.250 , 500 , 750 Susp.250/5mL 2 Nalidixic acid Neggram Tab.500 , Nalidxic acid (Rosemont) susp.300/5mL 3 Norfloxacin Noroxin Tab. 400 ,eye&ear drop Utinor (MSD) 0.3% 4 Ofloxacin Floxin Tab.200 , 400 Tarivid (Sanofi-Aventis) Eye drop 0.3% 5 Levofloxacin Levaquin Tab. 250 ,500 Tavonic Any extra notes: 6 Moxifloxacin Avelox (Bayer) tab.400 Lincosamides (lincomycin and clindamycin) -5.1.8 1- Active against Gram-positive cocci, and also against many anaerobes (1). The main indication for the use of lincosamides is now in the treatment of severe anaerobic infections (2)..Clindamycin is much better absorbed from the GIT than lincomycin -2 They both penetrate well into bone and have been used successfully in 49.osteomyelitis (2).The capsules should be taken with a glass of water (2)-3 4-They have also been used topically in the treatment of acne vulgaris (2). 5-Important : Patients should discontinue immediately and contact doctor if diarrhoea develops (1) (Lincosamides are reported to produce diarrhoea. In some patients severe antibiotic-associated or pseudomembranous colitis may develop during therapy or up to several weeks after it, and has proved fatal) (2). Lincosamides Scientific name Trade names Dosage form 1 Clindamycin Cleocin Cap.150 , gel or sol. 1% Dalacin C (pharmacia) 2 Lincomycin Lincocin (Pfizer) Cap.500,Vial 300/2mL , 600/2mL syrup 250/5mL Any extra notes: 5.1.9-Sulfonamides and trimethoprim 1- Sulfamethoxazole and trimethoprim are used in combination (as co- trimoxazole) because of their synergistic activity (2). Trimethoprim is also used alone particularly in the treatment of infections of the urinary and respiratory tracts (2). 2-Co-trimoxazole should not generally be given to infants below 6 weeks of age because of the risk of kernicterus (2). Co-trimoxazole should be avoided by people with G6PD deficiency (2). Scientific name Trade names Dosage form 1 Co-trimoxazole Bactrim or Methoprim T