GI Medications in Pharmacy Classification & Examples PDF

Introduction to GI medications in pharmacy: classification, mechanisms and dosage forms of available products + prescriptions examples o Provided by: Amir Hossein Hosseini, Pharm. D, Clinical pharmacy resident  Medications listed by Pharmacological classification 2  Drugs for peptic...

Introduction to GI medications in pharmacy: classification, mechanisms and dosage forms of available products + prescriptions examples o Provided by: Amir Hossein Hosseini, Pharm. D, Clinical pharmacy resident  Medications listed by Pharmacological classification 2  Drugs for peptic ulcer disease and prophylaxis ▸ Histamine type 2 receptor antagonists (regulating agents), usually administered OD or BD. ▸ Blocking the mentioned receptor can decrease gastric acid secretion. ▸ Indications: GERD (gastroesophageal reflux disease), PUD, H. pylori infection, Zolinger Ellison syndrome (higher doses may be needed), dyspepsia. ▸ CIMETIDINE, 200 mg, 400 mg, 800 mg tabs, 200 mg/2 ml inj (Tagamet®). ▸ Famotidine:20, 40 mg tabs, 20 mg/2 ml inj. ▸ Others: nizatidine, roxatidine,…. 3  PPIs (proton pomp inhibitors) ▸ Omeprazole: 20–60 mg/day, ZE syndrome 60–120 mg/day in two divided doses; 10mg, 20mg, 40mg capsules. Capsules must not be opened or chewed; to be taken in the morning 30 min before meals. (with empty stomach 30 min before breakfast.) ▸ Esomeprazole (s-omeprazole): 20–40 mg OD; Nexium® , Ezonium® , 20, 40 mg tab. ▸ Lansoprazole: 15mg caps, 30mg caps. ▸ Pantoprazole: Pantozol®, Pantosec®, Nolpaza® 20, 40 mg enteric coated tab; PANTIUM,PANTOSEC, PANTIN 40 mg tab, 40 mg inj for i.v. use. ▸ Rabeprazole: RABLET, RAZO, RABLOC, RABICIP, 10, 20 mg tab, 20 mg/ml vial for inj. There is no need to memorize all the brand names for PPIs. (unless the popular ones, which are highlighted) Students should know how to search the net for the brand names on their phone! 4 5  “ ▸ Esomeprazole 20 mg ▸ = Omeprazole 20 mg PPI equivalency ▸ = Pantoprazole 40 mg doses.(important) =Rabeprazole 20 mg ▸ = Lansoprazole 30 mg 6  Misoprostol: CYTOLOG 200 mg Misoprostol cause abortion in can tab; MISOPROST 100 mg, 200 pregnant patients! mg tabs. So the use of this drug is highly limited and controlled. Misoprostol is a synthetic prostaglandin E1 analog that inhibits basal and nocturnal gastric acid secretion by direct stimulation of PGE1 receptors on parietal cells in the stomach.  Antacids: a good choice for Dyspepsia, heart burn, …. Can be used as OTC drugs. Aluminum can cause constipation and magnesium can cause diarrhea. Al and Mg bind to the gastric acid that is secreted, simethicone reduces the surface tension and inhibits the bubble production in the GI system. Aluminum Hydroxide : susp 320 mg/5ml, Chewable Tab 300 mg Aluminum-Mg : susp 225+200 mg/5ml, Tab 200+200 mg Aluminum-Mg-S : susp 225+200+25 mg/5ml, Tab chewable 200+200+25 mg (S stands for simethicone). Magnesium Hydroxide : susp 8%( 400 mg/5ml) = Milk of magnesia= MOM How to use: 13 to 23 cc of suspension or 2 to 4 tablets between 30 minutes and 2 hours after eating the meal. No need for memorizing the doses for antacids. Just know the indication, the role of each compound in the formulation and what is the prescription note. 8 9  Ulcer protectives: Sucralfate: Ulcer healing dose: 1 g taken 1 hour before 3 major meals and at bed time; To prevent recurrences 1 g BD; SUCRACE, ULCERFATE, RECULFATE 500mg and 1 g tab. This drug is sulfated aluminum salt of sucrose. Sucralfate acts as an absorbent and creates a protective coating and has a high tendency to The wounded points in the stomach and duodenum stick (its positive charge sticks to the negative charge of the proteins in the area). Colloidal bismuth subcitrate (CBS, Tripotassium dicitrato-bismuthate): 120 mg (as Bi2O3) taken 30 min before 3 major meals and at bed time; Tab 120 mg. 10 11  Anti-bloating medications ▸ Simethicone ( in the Antacid formulations). ▸ Dimethicone: Infacol®,Colic EZ®,Chewable Tab 40 mg, pearl EC 125 mg ,oral drop 40 mg/ml. This medicine is prescribed in adults between 40 mg and 250 mg three to four times a day. ▸ To solve the problem of flatulence, other products such as activated charcoal (250 mg tab), drops of mint and cumin extract, colpermin and sodium bicarbonate are used. 12 13  Digestive enzymes Pancreatin: Amylase 6500 fipu + Lipase 8000 fipu + Protease 450 fipu Pancreatin Forte (Creon®) : Amylase 18000 fipu + Lipase 25000 fipu + Protease 1000 fipu Digestive: Tab EC (Onoton®, Onanzim®) it consists of Amylase, lipase, Pancrase. Lactase (Lacteeze®): Sachet, This medicine contains the enzyme that breaks down lactose. In people suffering from the problem of lactose intolerance You can use this medicine. In this way, one to two tablets are consumed before consuming dairy products. NO need to memorize the doses of enzymes in the formulations. Know the ingredients and classification. Due to the fact that digestive enzymes are enteric-coated drugs, they should not be crushed or chewed. 14 15  Anti-emetic drugs 16  Anticholinergic anti-emetics: Hyoscine: 0.2–0.4 mg oral/i.m./transdermal patch. Dicyclomine: 10–20 mg oral. Antihistamine anti-emetics: Dimenhydrinate : Tab 25mg, 50 mg Diphenhydramine : syr 12.5 mg/5ml Hydroxyzine : Tab 10,25 mg ,syr 10 mg/5ml Cinnarizine : Tab 25,75 mg Promethazine : Syrup 5mg/5ml ,Amp 25 mg/ml Chlorpromazine: 10–25 mg oral/i.m. (H1 and D2 blocker) Doxylamine: 10mg tab For nausea during pregnancy, vitamin B6 and ginger can Meclozine be used first. hydramine (alexir should not be) and dimenhydrinate are used, again in case of ineffectiveness, respectively promethazine, metoclopramide and Ondansetron should be prescribed. (All except promethazine are category B in pregnancy!) 17 18  5HT3 antagonists as anti-emetics: Ondansetron : (Demitron®) Tab 4mg ,Amp 4mg/2ml or 8mg/4ml Granisetron: Tab 1mg (not available),Amp 1mg/1ml, 3mg/3ml (Kytril®) Palonosetron, tropisetron Neurokinin-1 Antagonists as anti-emetics: Aprepitant : Tab 125,80 mg(Emend®, Emesis®) 5HT4 agonists as anti-emetics: Dexamethasone, Dronabinol and Cisapride : Tab 5,10 mg (it is also a prokinetic agent) Diazepam can also have Tegaserod : Tab 6 mg(Zelmac®) Anti-emetic activity. Anti dopaminergic anti-emetics: Metoclopramide : Tab 10 mg ,drop 4mg/ml ,Amp 10mg/2ml (Plazil®) , it is also a prokinetic agent. Promethazine : syr 5mg/5ml ,Amp 25 mg/ml,Tab:25mg Domperidone : Tab 10 mg (it is also a prokinetic agent.) Thiethylperazine : Tab 6.5 mg, Amp 6.5 mg/1ml 19Haloperidol : Tab 0.5,5 mg ,drop 2mg/ml ,Amp 5,50 mg/ml 20 21  Laxatives 22 Laxatives: Bulk forming agents: (no need to memorize the doses) Psyllium hydrophilic mucilloid: Psyllium hydrophilic mucilloid: 6–12 g to be taken just after mixing with water; ISOVAC 65 g/100 g granules. Musyllium (powder) Ispaghula (refined husk): 3–12 g freshly mixed with water or milk 2–3 times a day. Methyl cellulose: 4–6 g/day mixed with water (granules). Can both administered in diarrhea and constipation (depend on the amount of water, that is consumed!) Stool softeners: Docusates: enema and capsule formulations. Liquid paraffin: 15–30 ml/day as such or in emulsified form. Glycerin supp: 1g for kids (under 6 years old) 2g for adults. 23 24 Laxatives: Others: Prucalopride, caster oil formulations (A stimulant) : Bulk for emulsion 40 g (Laxaricin), Pearl 700, 1000 mg(Gelax), Supp 3g (Lubri-TD), ( no need for memorizing the doses), Polyethylene- Glycol (PEG): Sachet,powder bulk 70gr (Pidrolax®) Higher doses of PEG are used for WBI (whole bowel irrigation) before colonoscopy. 25 Laxatives: Stimulants: (Not a good choice in pregnant patients!) Bisacodyl: 5–15 mg; 5 mg tab; 10 mg (adult) 5 mg (child) suppository; CONLAX 5 mg, 10 mg suppository. Sodium picosulfate: Sodium picosulfate: 5-10 mg at bed time; 10 mg tab,5 mg/5 ml syr. Senna (as Sennosides Cal. salt): 10–40 mg at bed time: usually it will take about 6-7 hours to show the laxative effect. C-Lax: Tablet 750 mg, Herbilax: Capsul 290 mg, Senalin: Powder 40 g, Senalin 7.5:Dragee 500 mg, Sennamed: Tablet 650 mg (no need for dose memorization.) Osmotic purgative: (no need for memorizing the doses.) Mag. sulfate (Epsom salt): 5–15 g dissolved in 150–200 ml water, taken in the morning. Mag. hydroxide (as 8% W/W suspension—milk of magnesia) 30 ml. Sod. sulfate (Glauber’s salt): 10–15 g dissolved in 150–200 ml water, taken in the morning. Sod. phosphate: 6–12 g dissolved in 150–200 ml water, taken in the morning. Sod. pot. tartrate (Rochelle salt): 8–15 g dissolved in 150–200 ml water, taken in the morning. Lactulose: 10 g BD taken with water, 10 g/ 15 ml liquid syrup. 10g sachet. (do you know another indication?). other: Sorbitol sachet 5g. 26 27 28  “ Important slide! You should know if a drug can be prescribed for diarrhea and which class is it. 29  ▸ Rifaximin: For traveller's diarrhoea 200 mg TDS for 3 days. For suppressing ammonia As you saw in the previous forming gut bacteria 550 mg slide, other antibiotics can TDS. be prescribed in some ▸ RIFAGUT, Xigut 200 mg, 550 mg forms of diarrhea. tabs; Examples of probiotics: Lactoare, ▸ Probiotics: Anti-diarrhea by Kidilact, Gerilact, BioGaia, Protexin, Normalizing the gut floor. in cap Yomogi, Mutaflor, Lactofem, drops, and sachet formulations. Gynophilus,Provage, Should be kept at refrigerator Prokid,Prodigest,Lactovage,Vitalact (Alive micro-organisms.). Please study the name of some probiotics for diarrhea. 30 31  Anti-inflammatory agents as anti-diarrhea drug in IBD: The main indication of these drugs are IBD (Inflammatory bowel disease). IBD is associated with Diarrhea. 5-ASA compounds: 1. Sulfasalazine (5-ASA+ Sulfa pyridine) : For inflammatory bowel disease—Remission inducing dose 3–4 g/day, maintenance dose 1.5–2 g/day oral; dosage form: 0.5 g tab. 2. Mesalamine: (5ASA) Tab EC 250,500 mg, Tab 400,800mg (Asacol®, Biosacol) ,Tab 500mg (Pentasa), Supp 500 mg (Asacol®), Supp 1g (Pentasa). In three forms- ASACOL: pH-sensitive tablet with a resin coating that releases the drug in the terminal ileum and colon. PENTASA: capsules coated with ethyl cellulose and containing acid-resistant microgranules that release 5-ASA in the duodenum, jejunum, ileum, and colon. ROWASA: as an enema or suppository that directly releases 5-ASA in the rectum and terminal colon. 3. Balsalazide:750 mg cap and per 5 ml syr. (not available) 4. Olsalazine: prodrug of two 5-ASA. 250mg and 500mg cap. (not available) 32 33  Anti-inflammatory agents as anti-diarrhea drug in IBD: Corticosteroids: For inducing the treatment of moderate to severe IBD and the first drug for the treatment of UC (Ulcerative Colitis): 40-60 mg prednisolone (high-dose Oral Tab) Oral corticosteroids should be taken with meal and preferred to be taken in the morning with milk or breakfast. In case of no response to oral treatment: injectable hydrocortisone 300 mg daily or injectable methylprednisolone 40-60mg. HYDROCORTISONE-EMAD ENEMA RECTAL 100 mg/60mL Budsenide 2mg/100ml enema. 34  Anti-inflammatory agents as anti-diarrhea drug in IBD: Immunosuppressants: They are used in people who do not respond to systemic steroids and also as maintenance therapy in Crohn's and ulcerative colitis. Azathioprine 25mg, 50mg, 100mg tabs. (Azaram) Mercaptopurine 50mg tab. Methotrexate and cyclosporin can also prescribed as immunosuppressant agents in IBD. Infliximab: (Remicade, Remsima) INFLIXIMAB(100mg/20ml) vial or pen. Should be kept in refrigerator. 35  Anti-inflammatory agents as anti-diarrhea drug in IBD: other biologic Immunosuppressants that can be prescribed in severe conditions: ( no need for dose memorization, just know these drugs are biologic immunosuppressants and should be kept in refrigerator.) Etanercept (Enbrel, Altebrel), vial 25mg, vial 50mg, Prefilled syringe 50mg, Sub- cutaneous administration. Adalimumab (Humira, cinnora, kidimab) , 40mg/ 0.8ml amp, 20mg/0.4 ml amp.It is a human IgG1 antibody to TNF-α that is less antigenic than infliximab. It has response rates similar to other TNF inhibitors. Sub-cutaneous administration. Golimumab (Simponi), 50mg/ 0.5ml vial. It is a human antibody to TNF-α with activity and precautions similar to other TNF-α inhibitors. Certolizumab (Cimzia) is a humanized antibody specific for TNF-α with precautions and side effects similar to other TNF-α inhibitors. 36 37  Anti- Motility drugs as anti-diarrhea: Diphenoxylate-atropine: LOMOTIL 2.5 mg diphenoxylate + 0.025 mg atropine per tab and 5 ml liquid; 2–4 tab followed by 1–2 tab 6 hourly. Loperamide: 4 mg followed by 2 mg after each motion (max. 16 mg in a day); IMODIUM, LOPESTAL, DIARLOP: 2 mg tab, cap. Oral Rehydration Salt (ORS): Sachet 28g (dextrose+ bicarbonate+ Cl+ Na+ K). For oral rehydration caused by diarrhea. It can be life- saving in adults and kids. For adults: To use the medicine, dissolve the contents of one sachet in one liter of water and keep it in the refrigerator. The product should be prepared during It should be used for 24 hours and whatever is left after 24 hours should be thrown away. 38 39  Antispasmodic GI drugs: Usually prescribed in stomachache and IBS (irritable bowel syndrome) Usually they are anti-cholinergic drugs, so they can decrease the frequency and the strengths of bowel movements. Belladona PB Syrup: Atropine 19.4 mcg + Scopolamine(Hyoscine) 6.5 mcg + Hyosciamine 103.7 mcg+Phenobarbital 16.2 mg/5ml Belladona PB: Tab: Atropine 19.5 mcg + Scopolamine(Hyoscine) 6.5 mcg + Hyosciamine 104.0 mcg+Phenobarbital 16.2 mg (doses should not be memorized) Clidinium-C : (libro-c) Tab Clidinium Bromide 2.5 mg + Chlordiazepoxide 5 mg Dicyclomine : Tab 10 mg, Syr 10 mg/5ml , Amp 20 mg/2ml Hyoscine N-Buthyl bromide : Tab 10 mg , Amp 20 mg/ml Mebeverine : Tab 135,Cap XR 200 mg (Colofac Retard®) Propantheline : Tab 15 mg, propantheline is also indicated for hypersalivation ( because of anticholinergic activity). Colpermine: Soft gel Cap EC 187 mg peppermint Oil Remember that anticholinergic drugs can also have anti-nausea and anti-vomiting effect. 40 41  Anti-hemorrhoid and Anti-fissure drugs ▸ Anti-hemorrohiod: Supp, rectal ointment (ingredient: Hydrocortisone,Lidocaine,Aluminium subacetate, zinc oxide) ▸ Hydrocortisone as an anti-inflammatory, lidocaine as an anesthetic, and aluminum and zinc as an astringent and gatherer of the skin are present in the composition of the drug. Zinc oxide also can improve the healing time. 42  Anti-hemorrhoid and Anti-fissure drugs ▸ Other Anti-hemorrhoid plant based drugs: ( for topical use) ▸ Myrthus Communis, which has anti-inflammatory, anti-bacterial and anti-oxidant activity: MG ointment, rectol ointment. 43  Other medications , associated with gastrointestinal disorders: Urso deoxy cholic acid: (UDCA) Cap 250,300mg ( Ursodiol, Ursobil®, Ursoflor®, Delursan®) This drug itself is a bile acid and is used to dissolve gallstones. In addition, it has been seen that with the mechanism Uncertainty reduces the secretion of cholesterol in the bile. Octreotide: Amp 50,100,500 mcg (0.05, 0.1 mg) IV, SC (Sandostatin®, Octostatin) , Vial 20,30mg only IM (Sandostatin LAR®, no need for memorizing dose It is an analogue of somatostatin. As we remember, somatostatin is an inhibitory hormone that gastrin, cholecystokinin, hormone It inhibits growth, insulin, glucagon, serotonin, etc. INDICATION OF OCTREOTIDE IN THIS SESSION: Carcinoid diarrhea, diarrhea in HIV+ patients, control of diarrhea in ICU patients. (a good non-oral option) 44 45  Other compounds related to this session ▸ Artificial salvia (gel and spray formulation: kin Hidrat): This composition is for removing the dryness of mouth, due to the decrease in saliva secretion. 46  Other compounds related to this session ▸ BENZYDAMINE HCl. MOUTHWASH 0.15% : This medicine is for relieving conditions It is used for painful inflammation of the mouth and throat. ▸ Chlorhexidine is a medication that comes as an oral rinse (mouthwash). It treats gingivitis. ▸ L – CARNITINE (indicated in metabolic disorders): Chewable :Tablet: 1g, Tablet: 250mg, oral vial 1000mg Solution: 500mg/5ml, Syrup: 500mg/5ml,Injection: 1g/5ml ▸ IPECAC: Syrup: 0.14% Total Alkaloids, Epica as an emetic agent in treatment Emergency use of excessive amounts of drugs and treatment Poisons are prescribed 47 48  Other compounds related to this session ▸ Naloxegol is used to treat constipation caused by opiate (narcotic) pain medications in adults with chronic (ongoing) pain that is not caused by cancer. Naloxegol is in a class of medications called peripherally acting mu-opioid receptor antagonists. (methylnaltrexone and naldemedine is also from this class of anti-diarrhea drugs.) ▸ Lubiprostone (laxative) is used to relieve stomach pain, bloating, and straining and produce softer and more frequent bowel movements in people who have chronic idiopathic constipation. (usually it is not a choice drug.) 49 50  Other compounds related to this session ▸ Nitroglycerin 0.4% ointment. (Rectoderm®) For Anal fissure and fistula ▸ Diltiazem 2% ointment. A CALCIUM CHANNEL BLOCKER THAT CAUSES VASODILATION For anal fissure and fistula. Should be kept in refrigerator. ▸ There are also other plant based compounds (with topical anti-inflammatory, anti-oxidant and anti- bacterial effects), that can be formulated as topical gel, cream or ointment for Anal problems such as hemorrhoids, anal fissures and fistula. 51  Prokinetic agents: Prokinetic agents are drugs that stimulate contractions along your gastrointestinal (GI) tract. They help move food along. What conditions do prokinetic agents treat? Gastroparesis (paralysis of the stomach) GERD (chronic acid reflux) Functional dyspepsia (chronic indigestion) Nausea and vomiting Chronic intestinal pseudo-obstruction Examples of prokinetic agents, which we discussed earlier: Metoclopramide, cisapride, Domperidone. Physostigmine (ACH esterase inhibitor) and bethanecol (Muscarinic ACh agonist) are also prokinetic agents. Macrolide antibiotics, specially Erythromycin can be prescribed as prokinetic agent ( last choice of therapy), by the mechanism of being motilin receptor agonist in GI. Erythromycin: 200mg,250mg ,400mg,500mg tabs ( succinate salt), 500mg and 1g vials and also 135mg/5ml and 200mg/5ml susp. (no need for dose memorizing) 52 Lets review the classification of drugs with some prescriptions. 54 55 56 57 58 59  Thanks for your attention ! Any questions? 60  ‫دانشجو ها در قالب گروه هاي ‪ ٧-٦‬نفره در همون ابتداي جلسه كنار هم‬ ‫“‬ ‫بشينن‪(.‬با اختيار خودتون ولي از قبل اوكي باشيد) ‪ ١٠‬دقيقه حضور‬ ‫غياب و يه سري توضيحات كلي ‪ ١٠ +‬دقيقه پره تست‪.‬در ادامه ‪4٠‬‬ ‫دقيقه مرور اساليد ها( لطفا اساليد هارو خودتون قبل و بعد جلسه‬ ‫بخونين چون اصال وقت نخواهد شد كه دقيق بررسي بكنيم‪.‬صرفا با‬ ‫فرض اينكه شما خوندنين اساليدهارو يه مرور كلي ميكنيم و برا موارد‬ ‫لطفا نوت روبرويي را‬ ‫مهم تاكيد ميكنيم‪ 4٠-).‬الي ‪ ٥٠‬دقيقه اخر نوشتن الگ بوك ها من به‬ ‫قبل از حضور در كارگاه‬ ‫هر گروه چند تا نسخه ميدم بنويسن‪.‬گروه ها در حالي كه در حال‬ ‫بخونين!‬ ‫نوشتن الگ بوك هستن( باهم هم ميتونن مشورت بكنن فقط حالت‬ ‫كپي پيست عين هم نباشه ولي كليات يكي باشه اوكي هست‪ ).‬من‬ ‫دونه دونه گروه هارو ميبرم سر قفسه و با هر گروه يه دور قفسه دارو‬ ‫هاي گوارشي رو چك ميكنيم كه حدودا ‪ ١٠‬دقيقه طول ميكشه برا هر‬ ‫گروه‪ ٥ +.‬دقيقه ثبت نسخه برا هر گروه‪ (.‬اگر وقت باشه) در ارتباط‬ ‫با ‪ ٦‬نمره اون جلسه‪ :‬الگ بوك ‪ ٢‬نمره ‪ ،‬سر وقت حاضر بودن ‪ +‬روپوش‬ ‫و نظم ‪ ١‬نمره‪ ،‬يه نمره پرسش كالسي حين تدريس يا حين ديدن‬ ‫قفسه ها يا ثبت نسخه‪ ٢ ،‬نمره پره تست‪.‬كل طول جلسه ‪١٣٠-١٢٠‬‬ ‫دقيقه خواهد بود ‪ ،‬دوستان اگه كاري دارن نسبت به اين تايم تنظيم‬ ‫بكنن ممنون ميشم‪.‬يا اگه كار خيلي واجبه از قبل به من بگن‪.‬‬ ‫‪61‬‬