Peptic Ulcer Disease Meds..

Ulcer, peptic (treatment)Omeprazole is indicated for the short-term treatment of active duodenal ulcer {01} {26} {31} and active benign gastric ulcer {26} {32} {41}. Ulcer, peptic, Helicobacter pylori associated (treatment adjunct)Omeprazole is indicated in combination with clarithromycin [and amoxicillin or metronidazole {42}] for the treatment of duodenal and gastric ulcer associated with H. pylori infection {42} {43}. Eradication of H. pylori has been shown to reduce the risk of ulcer recurrence {43}. [Ulcer, peptic, nonsteroidal anti-inflammatory druginduced (treatment)]Omeprazole is indicated for the treatment of duodenal or gastric ulcers associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs). {42} pKa 4 and 8.8 Mechanism of action/Effect: Omeprazole is a selective and irreversible {47} proton pump inhibitor. {48} Omeprazole suppresses gastric acid secretion by specific inhibition of the hydrogenpotassium adenosinetriphosphatase (H +, K +ATPase) enzyme system found at the secretory surface of parietal cells {46}. It inhibits the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen. {03} {04} Since the H +, K +ATPase enzyme system is regarded as the acid (proton) pump of the gastric mucosa, omeprazole is known as a gastric acid pump inhibitor. {46} {01} The inhibitory effect is dose-related. {46} Omeprazole inhibits both basal and stimulated acid secretion irrespective of the stimulus. {01} {46} Omeprazole does not have anticholinergic or histamine H 2-receptor antagonist properties {46}.

Other actions/effects: Omeprazole has demonstrated antimicrobial activity in vitro against Helicobacter pylori , by selective inhibition of H. pylori urease, which is necessary for gastric colonization. {47} Omeprazole has the ability to inhibit the hepatic cytochrome P450 mixed function oxidase system. {01} Absorption: Rapid. {01} {46} Absolute bioavailability is about 30 to 40% at doses of twenty to forty milligrams, due in large part to presystemic metabolism {46}. Bioavailability in patients with chronic hepatic disease is about 100%, reflecting decreased first-pass effect {46}. Bioavailability in healthy elderly volunteers was 76%, as compared with 58% in young volunteers {46}. Distribution:

Distributed in tissue, particularly gastric parietal cells. {01} {07} Protein binding: Very high (approximately 95% {46}, bound to albumin and alpha 1-acid glycoprotein). {01} {18} {22} Biotransformation: Hepatic, extensive. {01} Omeprazole is subject to saturable, first-pass metabolism {46} {48}, and is completely and rapidly metabolized by the hepatic P450 (CYP) enzyme system. {48} Half-life:

Plasma: Normal hepatic function: 30 minutes to 1 hour. {01} {46} Chronic hepatic disease: 3 hours. {01} {46}

Onset of action: Within one hour. {01} Time to peak concentration: Within 30 minutes to 3.5 hours. {01} {46} Time to peak effect: Within 2 hours. {01} Duration of action: Up to 72 hours or more (96 hours required for full restoration of acid production). {01} {27} Elimination: Renal70 to 77% {46}. No unchanged omeprazole was detected in urine {46}. Fecal18 to 23%. {01} {18} In dialysisNot readily dialyzable, because of extensive protein binding. {01}

Precautions to Consider Carcinogenicity/Tumorigenicity/Mutagenicity In two 2-year studies in rats, omeprazole, given in doses corresponding to 4 to 352 times the human

dose, caused end-life gastric carcinoid tumors and enterochromaffin-like (ECL) cell hyperplasia in a doserelated manner in both male and female animals. {01} {46} Incidence was markedly higher in female rats, which had higher blood levels of omeprazole {46}. These ECL cell changes have been shown to be caused by high levels of gastrin (or hypergastrinemia) {27}. Pronounced acid inhibition at extremely high doses of gastric acid pump inhibitors or H 2-receptor antagonists results in the same feedback elevation of gastrin and subsequent ECL cell changes of the stomach. {27} Omeprazole was not mutagenic in the Ames test, in an in vitro mouse lymphoma cell assay, and in an in vivo rat liver DNA damage assay. {46} A mouse micronucleus test at 625 and 6250 times the human dose gave a borderline result, as did an in vivo bone marrow chromosome aberration test. A second mouse micronucleus test at 2000 times the human dose, but with different (suboptimal) sampling times, was negative {46}. Pregnancy/Reproduction Fertility In a rat fertility and general reproductive performance test, omeprazole, in a dose 35 to 345 times the human dose, was not toxic or deleterious to the reproductive performance of parental animals. {01} {46} Pregnancy Adequate and well-controlled studies in humans have not been done {46}. Sporadic instances of congenital abnormalities in infants born to women who received omeprazole during pregnancy have been reported. {46} Studies in pregnant rats did not show omeprazole to have any teratogenic potential at doses 345 times the human dose. Omeprazole produced dose-related increases in embryo-lethality, fetal resorptions, and pregnancy disruptions in rabbits receiving 17 to 172 times the human dose. In rats, dose-related embryo/fetal toxicity and postnatal developmental toxicity were observed in offspring resulting from parents treated with 35 to 345 times the human dose. {01} FDA Pregnancy Category C. {01} Breast-feeding It is not known whether omeprazole is distributed into human milk. However, because omeprazole has been shown to cause tumorigenic and carcinogenic effects in animals, risk-benefit must be considered.
{01} {46}

Pediatrics Appropriate studies on the relationship of age to the effects of omeprazole have not been performed in the pediatric population. {01} Safety and efficacy have not been established {46}.

Geriatrics

No information is available on the relationship of age to the effects of omeprazole in geriatric patients. However, a somewhat decreased rate of elimination and an increased bioavailability are more likely to

occur in geriatric patients taking omeprazole. {01}

Pharmacogenetics Pharmacokinetic studies in Asian subjects receiving single 20-mg doses of omeprazole showed an approximately fourfold increase in the area under the plasma concentration-time curve (AUC) as compared to Caucasian subjects. {38} {39} Dosage adjustments should be considered for Asian patients, especially for prophylaxis of recurrence of erosive esophagitis. {38} {39} Drug interactions and/or related problems The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)not necessarily inclusive ( = major clinical significance): Overdose For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ). Clinical effects of overdose The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)not necessarily inclusive: Blurred vision{41}{46} confusion{41}{44}{46} diaphoresis{41}{46} (increased sweating) drowsiness{41}{44}{46} dryness of mouth{41}{46} flushing headache malaise(general feeling of discomfort or illness) nausea tachycardia(fast or irregular heartbeat)

Treatment of overdose Since there is no specific antidote for overdose with omeprazole, treatment should be symptomatic and supportive. Due to extensive protein binding, omeprazole is not readily dialyzable. Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.

Patient Consultation As an aid to patient consultation, refer to Advice for the Patient, Omeprazole (Systemic). In providing consultation, consider emphasizing the following selected information ( = major clinical significance): Before using this medication Conditions affecting use, especially: Sensitivity to omeprazole PregnancyReports of congenital defects; risk-benefit must be considered

Breast-feedingMay be distributed into breast milk; may cause potentially serious adverse effects in nursing infants Other medications, especially anticoagulants, diazepam, or phenytoin Other medical problems, especially chronic hepatic disease or history of Proper use of this medication Taking the capsule form of this medication immediately before a meal, preferably the morning meal May take antacids for relief of pain, unless otherwise instructed by physician Swallowing capsule form of this medication whole; not crushing, breaking, chewing, or opening the capsule Compliance with full course of therapy Proper dosing Missed dose: Taking as soon as possible; not taking if almost time for next dose; not doubling doses Proper storage Precautions while using this medication Regular visits to physician to check progress

Side/adverse effects Signs of potential side effects, especially generalized skin reactions, hematologic abnormalities, hematuria, proteinuria, and urinary tract infection

General Dosing Information Omeprazole capsules should be swallowed whole, and not chewed or crushed. Omeprazole magnesium

tablets also should be swallowed whole. Symptomatic response to omeprazole therapy does not preclude the presence of gastric malignancy . For therapy of dyspepsia, omeprazole usually is used for 4 weeks. If after 2 weeks of treatment the patient does not respond to therapy, or there is an early clinical indication of a lack of efficacy, the patient should be thoroughly investigated in order to rule out organic disease. If there are indications of a clinical response following the initial 2 weeks of treatment, omeprazole may be continued for an additional 2 weeks. For therapy of gastrointestinal reflux disease, omeprazole usually is used for short-term (4- to 8-week) courses; however, additional 4- to 8-week courses of treatment may be considered if there is recurrence of severe or symptomatic gastroesophageal reflux poorly responsive to customary medical treatment. Controlled studies of omeprazole used as maintenance therapy to prevent erosive esophagitis recurrence have not been conducted beyond 12 months , although a limited number of patients have received continuous maintenance treatment for up to 6 years. Dosage adjustments should be considered for Asian patients, especially for prophylaxis of erosive esophagitis recurrence , since pharmacokinetic studies in Asian subjects receiving single 20-mg doses of omeprazole showed an approximately fourfold increase in the area under the plasma concentration-time curve (AUC) as compared to Caucasian subjects. Omeprazole may be taken with antacids. Initial titration of doses and subsequent dosage adjustment of omeprazole is recommended in the longterm treatment of pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome, systemic mastocytosis, multiple endocrine adenomas). Doses of up to 120 mg three times a day have been administered. Patients may require at least one increase in dose per year. If the daily dose is greater than 80 mg, it should be administered in divided doses.Zollinger-Ellison syndrome has been treated continuously with omeprazole for more than 5 years. Diet/Nutrition Omeprazole capsules should be taken immediately before meals . Omeprazole magnesium tablets may be taken with food or on an empty stomach. Bioequivalence information Omeprazole capsules and omeprazole magnesium tablets are not bioequivalent.

Oral Dosage Forms Note: Dosing recommendations vary between dosage forms; please check the appropriate section for dosage formspecific dosing recommendations.

OMEPRAZOLE DELAYED-RELEASE CAPSULES Usual adult dose Gastroesophageal reflux disease (treatment)

Oral, 20 mg once a day for four to eight weeks. Note: A dosage of 40 mg once a day has been used for esophagitis associated with gastroesophageal reflux disease refractory to other treatment regimens.

2.) Brand Name: Buscopan Generic Name: Hyoscine-N-butylbromide Classification: Antispasmodics Pregnancy Category: C Availability: Tablet 10 mg,Ampule 20mg Action: The mechanism of action of Buscopan is that it blocks the muscarinic receptors found on the smooth muscle walls which means its blocks the action of acetylcholine on the receptors found within the smooth muscle of the gastrointestinal and urinary tract and thus reduces the spasms and contractions. This relaxes the muscle and thus reduced the pain from the cramps and spasms. Indication: 1. 2. 3. 4. Spasm in the genitourinary tract Spasm in the gastrointestinal tract Spasm in the biliary tract Colic

Contraindications: Myasthenia gravies, megacolon, hypersensitivity to drug contents, narrow angle glaucoma, prostate hypertrophy with urinary retention, mechanical stenosis in the GI tract, tachycardia. Cautious Use: Thyrotoxicosis, cardiac insufficiency, pyrexia, fructose intolerance. Route & Dosage Tablet Adult and child >6 y/o 1 to 2 tab TID-QID Ampule Colic Pain Adult and adolescent >12 y/o 1-2 amp IV/IM/SC several times daily. Maximum dose: 100mg/day Infant and young children 0.3-0.6 mg/kg/body weight by slow IV/IM/SC several times daily. Maximum dose: 1.5 mg/kg/body weight. Adverse effects: 1. Constipation

2. Decreased sweating 3. Mouth, skin, eye dryness 4. Blurred feeling 5. Bloating 6. Dysuria 7. Nausea or vomiting 8. Lightheadedness 9. Headache 10. Weakness Drug Interaction: 1. 2. 3. 4. 5. 6. 7. Potassium chloride Metoclopramide MAO inhibitors Beta-agonists Anticholinergics Antacids Droperidol

Patient & Family Education 1. 2. 3. 4. 5.

3.)

Take this drug 30 minutes to 1 hour before meals Buscopan will potentiate the effect of alcohol and other CNS depressants. Do not take antacids and antidiarrheal 2 to 3 hours prior to raking this drug. It is not necessary to take the medication if you are not in pain. Avoid driving or operating machinery after parenteral dose.

Indication & Dosage Oral Nausea and vomiting Adult: 10-20 mg every 4-8 hr. Max: 80 mg/day. Child: >2 yr and >35 kg: 10-20 mg 3-4 times daily. Max: 80 mg daily. Oral Non-ulcer dyspepsia Adult: 10-20 mg tid and at night. Oral Migraine Adult: 20 mg every 4 hr, in combination with paracetamol, as required. Max: 4 doses in 24 hr. Rectal Nausea and vomiting Adult: 60 mg bid. Child: 60 mg bid. Max Dosage: Administration Should be taken on an empty stomach. Take 15-30 min before meals. Contraindications Hypersensitivity. GI haemorrhage, obstruction and perforation, patients with

prolactin releasing pituitary hormone, chronic admin or routine prophylaxis of postoperative nausea and vomiting. Special Precautions Phaeochromocytoma; children<2 yr, elderly; renal or hepatic impairment. Risk of cardiac arrhythmias and hypokalaemia if administered IV. Pregnancy and lactation. Adverse Drug Reactions Drowsiness, extrapyramidal reactions, galactorrhoea, gynaecomastia; constipation or diarrhoea, lassitude, decreased libido, skin rash, itch. Potentially Fatal: Convulsions, arrhythmias and cardiac arrest, dysrrhythmias in patients with CV disease or hypokalaemia, patients on cancer chemotherapy. Seizures; hypertensive crisis in patients with phaeochromocytoma. Drug Interactions Reduces absorption of digoxin. Increases absorption of aspirin, paracetamol and oral diazepam. Enhances CNS depression by phenothiazine. Antimuscarinic agents and opioids antagonise GI effects. May antagonise hypoprolactinaemic effect of drugs such as bromocriptine. Increased effects when used with CYP3A4 inhibitors such as erythromycin or ritonavir. Potentially Fatal: Reduces absorption of digoxin. Increases absorption of aspirin, paracetamol and oral diazepam. Enhances CNS depression by phenothiazine. Antimuscarinic agents and opioids antagonise GI effects. May antagonise hypoprolactinaemic effect of drugs such as bromocriptine. Increased effects when used with CYP3A4 inhibitors such as erythromycin or ritonavir. Click to view more domperidone Drug Interactions Food Interaction Delayed absorption but higher bioavailability due to reduced first-pass metabolism in gut wall. Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Oral: Store at 15-30C. Rectal: Store at 15-30C. Mechanism of Action Domperidone is a peripheral dopamine-receptor blocker. It increases oesophageal peristalsis, lower oesophageal sphincter pressure, gastric motility and peristalsis, thus facilitating gastric emptying and decreasing small bowel transit time. Onset: Oral: 30 min-1hr. Duration: Oral: 6-8 hr. Absorption: Peak plasma concentrations after 1 hr (rectal), 30 min (oral). Distribution: Enters breast milk (small amounts). Protein-binding: >90%. Metabolism: Extensively hepatic. Excretion: Urine (as metabolites), faeces (as unchanged drug); 7.5 hr (elimination half-life).