Names and pronunciation
(ay-car′bose) Glucobay , Prandase , Precose
PDF page 24
Loading InternPractice…
Drug reference
(ay-car′bose) Glucobay , Prandase , Precose
PDF page 24
Func. class.: Oral antidiabetic Func. class.: Nonopioid analgesic, antipyretic
PDF page 24
USES: Type 2 diabetes mellitus, alone or in combination with a sulfonylurea, metformin, insulin USES: Mild to moderate pain or fever, arthralgia, dental pain, dysmenorrhea, headache, myalgia, osteoarthritis
PDF page 24
Chem. class.: Nonsalicylate, paraami- nophenol derivative
PDF page 24
Do not confuse: Acephen/Anacin/Aspirin 3/Anacin-3
PDF page 24
ACTION: May block pain impulses peripherally that occur in response to inhibition of prostaglandin synthesis; does not possess antiinflammatory prop- erties; antipyretic action results from inhibition of prostaglandins in the CNS (hypothalamic heat-regulating center)
PDF page 24
Unlabeled uses: Migraine
PDF page 24
CONTRAINDICATIONS: Breast- feeding, hypersensitivity, diabetic ketoac- idosis, cirrhosis, inflammatory bowel disease, ileus, colonic ulceration, partial intestinal obstruction, chronic intestinal disease, serum creatinine >2 mg/dL, CCr <25 mL/min CONTRAINDICATIONS: Hyper- sensitivity to this product, phenacetin aspartame, saccharin, tartrazine Precautions: Pregnancy, breastfeeding, geriatric patients, anemia, renal/hepatic disease, chronic alcoholism
PDF pages 24, 25
Black Box Warning: Hepatotoxicity Black Box Warning: Hepatotoxic- ity: occurs with high doses (>4 g/day); dark urine; clay-colored stools; yellow- ing of skin, sclera; itching; abdominal pain; fever; diarrhea if patient is on long-term therapy; may require liver transplant, those malnourished or using alcohol chronically are at higher chance of hepatotoxicity; consult poison control with suspected acute toxicity, draw 4-hr serum level and administration of acetyl- cysteine based on the 4-hr level on the Rumack-Matthew nomogram • Potentially fatal hypersensitivity, allergic reactions: rash, urticaria; if these occur, product may have to be dis- continued • Stevens-Johnson syndrome, toxic epi- dermal necrolysis may occur when beginning treatment or any other dose • Pregnancy/breastfeeding: cautious use in pregnancy, breastfeeding (PO), use only if clearly needed (IV) Black Box Warning: Hepatotoxicity: not to exceed recommended dosage; the elixir, liquid, suspension come in sev- eral concentrations, read label carefully; acute poisoning with liver damage may result; tell parents of children to check products carefully; that acute toxicity in- cludes nausea, vomiting, abdominal pain; prescriber should be notified immedi- ately; that toxicity may occur with other combination products • Not to use with excessive alcohol, herbals, OTC products without approval of prescriber • To recognize signs of chronic over- dose: bleeding, bruising, malaise, fever, sore throat • That those with diabetes may notice blood glucose monitoring changes • To notify prescriber of pain or fever lasting more than 3 days • Not to be used in patients <2 yr unless approved by prescriber • Hypersensitivity: to stop product, call prescriber if rash occurs • Pregnancy/breastfeeding: May be used when breastfeeding, short-term
PDF pages 25, 26, 27
SIDE EFFECTS CNS: Agitation (child) (IV); headache, fatigue, anxiety (IV) RESP: Dyspnea (IV), atelectasis (child) (IV) CV: Hyper- and hypotension (IV) GI: Nausea, vomiting, abdominal pain; hepatotoxicity, hepatic seizure (overdose), GI bleeding GU: Renal failure (high, prolonged doses) HEMA: Leukopenia, neutropenia, hemo- lytic anemia (long-term use), thrombocy- topenia, pancytopenia INTEG: Rash, urticaria, injection site pain SYST: Stevens-Johnson syndrome, toxic epidermal necrolysis TOXICITY: Cyanosis, anemia, neutropenia, jaundice, pancytopenia, CNS stimulation, delirium followed by vascular collapse, sei- zures, coma, death
PDF page 25
INTERACTIONS Increase: renal adverse reactions— NSAIDs, salicylates; consider lower dose Increase: methemoglobinemia—nitric oxide, prilocaine; avoid concurrent use Increase: hypoprothrombinemia—war- farin, long-term use, high doses of acetaminophen Increase: hepatotoxicity—barbiturates, alcohol, carBAMazepine, hydantoins, rifAMPin, rifabutin, isoniazid, diflunisal, zido vudine, lamoTRIgine, imatinib, dasatinib, mipomersen; monitor for hepatotoxicity Decrease: absorption—colestipol, cholestyramine Decrease: zidovudine, lamoTRIgine effect Drug/Herb Increase: hepatotoxicity—St. John’s wort, due to acetaminophen metabolism Drug/Lab Test Increase: LFTs, potassium, bilirubin, LDH, prothrombin time Decrease: HB/Hct, WBC, RBC, platelets; albumin, magnesium, phosphate (pediat- rics)
PDF page 26
TREATMENT OF OVERDOSE: Product level, gastric lavage; administer oral acetylcysteine to prevent hepatic damage (see acetylcysteine mono graph); monitor for bleeding
PDF page 27
DOSAGE AND ROUTES • Adult: PO 25 mg tid initially, with 1st bite of meal; maintenance dose may be increased to 50-100 mg tid; dosage adjust- ment at 4- to 8-wk intervals, individualized (a-seat-a-mee′noe-fen) 222AF , Abenol , Acephen, Acephen Infant Feverall, ACET , Acetab , Apacet, APAP, Apra, Atasol , Children’s FeverAll, Fortolin , Genapap, Infantaire, Mapap, NeoPAP, Novo-Gesic , Pediaphen , Pediatrix , Q-Pap, Q-Pap Children’s, Rapid Action Relief , Redutemp, Ridenol, Robigesic , Rounox , Silapap, Taminol , Tempra , T-Painol, Tylenol, XS pain reliever acetaminophen (IV) (Rx) Ofirmive DOSAGE AND ROUTES • Adult/child >12 yr: PO/RECT 325- 650 mg q4-6hr prn, max 4 g/day; weight ≥50 kg IV 1000 mg q6hr or 650 mg q4hr prn, max single dose 1000 mg, min dosing interval 4 hr; weight <50 kg IV 15 mg/kg/dose q6hr or 12.5 mg/kg/dose q4hr, max single dose 15 mg/kg, min dosing interval 4 hr, max 75 mg/kg/day from all sources; EXTENDED RELEASE 650-1300 mg q8hr as needed, max 4 g/day • Child ≥2 yr and <50 kg: IV 15 mg/kg/ dose q6hr or 12.5 mg/kg/dose q4hr, max single dose 15 mg/kg, min dosing interval 4 hr, max 75 mg/kg/day from all sources Renal dose • Adult: IV CCr <30 mL/min reduce dose and prolong interval, CCr <10 mL/min PO/ RECT/IV minimum interval of q8hr Hepatic dose • Adult: Mild to moderate: max 2000 mg/day; severe liver damage: contraindi- cated Migraine (unlabeled) • Adult and adolescent: PO/RECT 500- 1000 mg, max 1 g/dose or max 4 g/day
PDF pages 24, 25
Available forms: Rectal suppository 120, 325, 650 mg; soft chew tablets 80, 160 mg; capsules 500 mg; elixir 120, 160, 325 mg/5 mL; oral disintegrating tablets 80, 160 mg; oral drops 80 mg/0.8 mL, liquid 500 mg/5 mL, 160/5 mL, 1000/30 mL; extended release 650 mg, 80 mg/mL; tablets 325, 500, 650 mg; solution for injection 1000 mg/100 mL
PDF page 25
Administer: PO route • Do not confuse 2 × 325 (650 mg) with 650-mg extended-release tablets • Crushed or whole, do not crush extended-release product; chewable tablets may be chewed; give with full A glass of water • With food or milk to decrease gastric symptoms if needed • Suspension after shaken well; check elixir, liquid, suspension concentration carefully; suspension and capsules are bioequivalent Rectal route • Store suppositories <80°F (27°C) Intermittent IV INFUSION route • No further dilution needed; do not add other medications to vial or infusion device • For doses equal to single vial, a vented IV set may be used to deliver directly from vial; for doses less than a single vial, withdraw dose and place in an empty sterile syringe, plastic IV container, or glass bottle; infuse over 15 min • Discard unused portion; if seal is bro- ken, vial penetrated, or drug transferred to another container, give within 6 hr Y-site compatibilities: Do not admix
PDF page 25
Assess: • For fever and pain: Type of pain, loca- tion, intensity, duration, aggravating/alle- viating factors; assess for diaphoresis, fever baseline and periodically • Hepatic studies: AST, ALT, bilirubin, creatinine before therapy if long-term therapy is anticipated; may cause hepatic toxicity at doses >4 g/day with chronic use • Renal studies: BUN, urine creatinine, occult blood, albumin, if patient is on long-term therapy; presence of blood or albumin indicates nephritis, I&O ratio; decreasing output may indicate renal fail- ure (long-term therapy) • Blood studies: CBC, PT if patient is on long-term therapy • Chronic poisoning: rapid, weak pulse; dyspnea; cold, clammy extremities; report immediately to prescriber
PDF page 26
Evaluate: • Therapeutic response: absence of pain using pain scoring; absence of fever
PDF page 26
CLINICAL CONSIDERATIONS
PDF page 26
Patient and caregiver information:
PDF page 26
PHARMACOKINETICS 85%-90% metabolized by liver, excreted by kidneys; metabolites may be toxic if overdose occurs; widely distributed; crosses placenta in low concentrations; excreted in breast milk; half-life 1-4 hr PO: Onset 10-30 min, peak ½-2 hr, dura- tion 4-6 hr, well absorbed IV: Onset rapid, peak 30-120 min, dura- tion 3-4 hr RECT: Onset slow, peak 1-2 hr, duration 4-6 hr, absorption varies
PDF pages 25, 26
• Adult: PO 25 mg tid initially, with 1st bite of meal; maintenance dose may be increased to 50-100 mg tid; dosage adjust- ment at 4- to 8-wk intervals, individualized (a-seat-a-mee′noe-fen) 222AF , Abenol , Acephen, Acephen Infant Feverall, ACET , Acetab , Apacet, APAP, Apra, Atasol , Children’s FeverAll, Fortolin , Genapap, Infantaire, Mapap, NeoPAP, Novo-Gesic , Pediaphen , Pediatrix , Q-Pap, Q-Pap Children’s, Rapid Action Relief , Redutemp, Ridenol, Robigesic , Rounox , Silapap, Taminol , Tempra , T-Painol, Tylenol, XS pain reliever acetaminophen (IV) (Rx) Ofirmive DOSAGE AND ROUTES
PDF pages 24, 25
• Adult/child >12 yr: PO/RECT 325- 650 mg q4-6hr prn, max 4 g/day; weight ≥50 kg IV 1000 mg q6hr or 650 mg q4hr prn, max single dose 1000 mg, min dosing interval 4 hr; weight <50 kg IV 15 mg/kg/dose q6hr or 12.5 mg/kg/dose q4hr, max single dose 15 mg/kg, min dosing interval 4 hr, max 75 mg/kg/day from all sources; EXTENDED RELEASE 650-1300 mg q8hr as needed, max 4 g/day
PDF pages 24, 25
• Adult: IV CCr <30 mL/min reduce dose and prolong interval, CCr <10 mL/min PO/ RECT/IV minimum interval of q8hr Hepatic dose
PDF pages 24, 25
• Adult: Mild to moderate: max 2000 mg/day; severe liver damage: contraindi- cated Migraine (unlabeled)
PDF pages 24, 25
• Adult and adolescent: PO/RECT 500- 1000 mg, max 1 g/dose or max 4 g/day
PDF pages 24, 25