Names and pronunciation
(sih-los′tah-zol)
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Drug reference
(sih-los′tah-zol)
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Func. class.: Platelet aggregation inhibitor Func. class.: H2-histamine receptor antagonist
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Chem. class.: Quinolinone derivative Chem. class.: Imidazole derivative
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ACTION: Multifactorial effects (anti- thrombotic, antiplatelet vasodilation) ACTION: Inhibits histamine at H2-receptor site in the gastric parietal cells, which inhibits gastric acid secretion
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USES: Intermittent claudication asso- ciated with PVD USES: Short-term treatment of duode- nal and gastric ulcers and maintenance; management of GERD (PO) and Zollinger-Ellison syndrome; prevention of upper GI bleeding; prevent, relieve heartburn, acid indigestion
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CONTRAINDICATIONS: Hyper- sensitivity, acute MI, active bleeding con- ditions, hemostatic conditions CONTRAINDICATIONS: Hyper- sensitivity to this product, H2 blockers, benzyl alcohol Precautions: Pregnancy, breastfeeding, children <16 yr, geriatric patients, organic brain syndrome, renal/hepatic disease
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Black Box Warning: HF Precautions: Pregnancy, breastfeeding, children, geriatric patients, previous hepatic disease, cardiac/renal disease, increased bleeding risk, low platelet count, platelet dysfunction, smoking Black Box Warning: Decrease: survival rates—when used with phosphodiester- ase III inhibitors (milrinone) in those with heart failure class III, IV Drug/Herb Decrease: action—chamomile, coen- zyme Q10, feverfew, garlic, ginger, ginkgo biloba, flax, goldenseal, St. John’s wort Drug/Food • Do not use with grapefruit juice; toxic- ity may occur Increase: cilostazol action—fatty meal; avoid giving with food Black Box Warning: For underlying CV disease because CV risk is great; for CV lesions with repeated oral administration; do not administer to patients with HF of any severity; for severe headache, signs of toxicity • Blood studies: CBC q2wk, Hct, HB, PT • Beers: avoid in older adults; may pro- mote fluid retention and/or exacerbate heart failure
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SIDE EFFECTS CNS: Dizziness, headache CV: Palpitations, tachycardia, postural hypotension, chest pain GI: Nausea, vomiting, diarrhea, GI dis- comfort, colitis, cholelithiasis, ulcer, esophagitis, gastritis, anorexia, flatu- lence, dyspepsia INTEG: Rash, Stevens-Johnson syndrome RESP: Cough, pharyngitis, rhinitis SIDE EFFECTS CNS: Confusion, headache, depression, dizziness, psychosis CV: Bradycardia, tachycardia, dysrhythmias GI: Diarrhea, abdominal cramps GU: Gynecomastia, galactorrhea, impo- tence, increase in BUN, creatinine INTEG: Urticaria, rash RESP: Pneumonia
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INTERACTIONS Increase: bleeding tendencies—antico- agulants, NSAIDs, thrombolytics, abcix- imab, eptifibatide, tirofiban, ticlopidine Increase: cilostazol levels—CYP3A4, CYP2C19 inhibitors; dilTIAZem, erythro- mycin, clarithromycin, verapamil, pro- tease inhibitors, omeprazole; exercise caution when coadministering with flu- voxaMINE, FLUoxetine, ketoconazole, isoniazid, gemfibrozil, omeprazole, itra- conazole, voriconazole, fluconazole; reduce dose to 50 mg bid Decrease: cilostazol levels—CYP3A4 inducers INTERACTIONS Increase: toxicity due to CYP450 path- way—benzodiazepines, beta-blockers, calcium channel blockers, carBAMazepine, chloroquine, lidocaine, metroNIDAZOLE, moricizine, phenytoin, quiNIDine, quiNINE, sulfonylureas, theophylline, tricyclics, valproic acid, warfarin Increase: bone marrow suppression— carmustine Decrease: absorption of cimetidine— antacids, sucralfate Decrease: absorption—ketoconazole, itraconazole Drug/Lab Test Increase: alkaline phosphatase, AST, cre- atinine, prolactin False positive: gastroccult, hemoccult tests False negative: TB skin tests
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DOSAGE AND ROUTES • Adult: PO 100 mg bid or 50 mg bid if using products that inhibit CYP3A4 and CYP2C19 DOSAGE AND ROUTES Short-term treatment of active ulcers • Adult/adolescents ≥16 yr: PO 300 mg qid × 8-12 wk or 400 mg bid × 8 wk C • Child: PO 20-40 mg/kg/day, divided q6hr Prophylaxis of duodenal ulcer • Adult and child >16 yr: PO 400 mg at bedtime or 300 mg bid GERD • Adult: PO 800-1600 mg/day in di- vided doses × up to 12 wk Hypersecretory conditions (Zollinger-Ellison syndrome) • Adult: PO 300-600 mg q6hr; max 2400 mg/day Heartburn • Adult/child ≥12 yr: PO 200 mg up to bid, may use before eating, max 400 mg/ day, max daily use up to 2 wk Renal disease • Adult: PO CCr <30 mL/min, 300 mg q12hr
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Available forms: Tablets 50, 100 mg Available forms: Tablets 100, 300, 400, 800 mg; oral liquid 300 mg/5 mL
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Administer: • Give bid 30 min prior to or 2 hr after meals with a full glass of water; do not give with grapefruit juice Administer: PO route • With meals for prolonged product ef- fect; antacids 1 hr prior to or 1 hr after cimetidine
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Assess: Assess: • Ulcer symptoms: epigastric pain, du- ration, intensity; aggravating, amelio- rating factors; blood in stools; emesis • Beers: avoid in older adults with de- lirium or at high risk for delirium, ad- verse CNS reactions
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Evaluate: • Therapeutic response: improved walk- ing distance, duration; decreased pain Evaluate: • Therapeutic response: decreased pain in abdomen; healing of ulcers; absence of gastroesophageal reflux; gastric pH of 5
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CLINICAL CONSIDERATIONS CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To avoid hazardous activities until ef- fect is known; dizziness may occur • To report any unusual bleeding • To report side effects such as diar- rhea, skin rashes, subcutaneous bleeding • That effects may take 2-4 wk; treat- ment of up to 12 wk may be required for necessary effect • That reading the patient package in- sert is necessary • That it is best to discontinue tobacco use, not to use grapefruit juice • That there are many drug and herb in- teractions; to obtain approval from pre- scriber before use (sye-met′i-deen) Tagamet HB Patient and caregiver information: • That gynecomastia, impotence may occur, are reversible • To avoid driving, other hazardous ac- tivities until stabilized on this medication; drowsiness or dizziness may occur • To avoid OTC preparations: aspirin; cough, cold preparations; condition may worsen; OTC therapy is used for short term (2 wk) • Not to smoke because smoking de- creases effectiveness of product • That product must be taken exactly as prescribed and continued for pre- scribed time to be effective; not to dou- ble dose; if taking OTC, not to take maximum dose >2 wk unless directed by prescriber • To report diarrhea, black tarry stools, sore throat, rash, dizziness, confusion, delirium to prescriber • To use increased fluids, bulk in diet to decrease constipation • Pregnancy/breastfeeding: to report if pregnancy is planned or suspected or if breastfeeding, avoid breastfeeding
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PHARMACOKINETICS 95%-98% protein binding; metabolism: hepatic extensively by CYP3A4, 2C19 enzymes (active metabolite); excreted in urine (74%), feces (20%); half-life 11-13 hr PHARMACOKINETICS Half-life 1½-2 hr; 30%-40% metabo- lized by liver, excreted in urine (unchanged), crosses placenta, enters breast milk PO: Onset 30 min, peak 45-90 min; duration 4-5 hr, well absorbed
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• Adult/adolescents ≥16 yr: PO 300 mg qid × 8-12 wk or 400 mg bid × 8 wk C
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