IBUPROFEN
Indikasi :
Oral
Pain and inflammation
Adult: 1.2-1.8 g/day in divided doses. Maintenance: 0.6-1.2 g daily. Max: 2.4 g/day.
Child: 5-10mg/Kg
Oral
Juvenile idiopathic arthritis
Child: ≥3 mth and weighing >5 kg: 30-40 mg/kg/day in 3-4 divided doses. Max: 2.4 g/day.
Oral
Fever
Adult: 200-400 mg every 4-6 hr. Max: 1.2 g/day.
Child: 1-6 mth: 5 mg/kg 3-4 times daily, 6-12 mth: 50 mg tid, 1-2 yr: 50 mg 3-4 times daily, 2-7 yr: 100 mg 3-4 times daily, >7 yr: 200 mg 3-4 times daily. Max: 40 mg/kg/day.
Intravenous (inj)
Closure of patent ductus arteriosus
Child: Given as three IV doses infused over 15 min at 24-hr intervals. Initially 10 mg/kg followed by 2 doses of 5 mg/kg. A 2nd course may be given if ductus remains open after 48 hr. Surgery may be required if neonate is unreponsive to two courses of treatment. Dose should be based on birth weight.
Topical/Cutaneous
Pain and inflammation associated with musculoskeletal and joint disorders
Adult: As 5% or 10% gel: Apply onto affected area.
Sediaan:
Oral : tablet 200 mg, 400 mg, 600mg, 800mg. Susp: 100mg/5cc , 200mg/5cc (susp. forte) , oral drop: 40mg/cc
Injeksi (caldolor@) : 400 mg/4 mL (100 mg/mL), 800 mg/8 mL (100 mg/mL)
Caldolor must be diluted prior to intravenous infusion. dilute into concentration of 4mg/cc or less
800 mg dose: Dilute 8 mL of Caldolor in no less than 200 mL of diluent.
400 mg dose: Dilute 4 mL of Caldolor in no less than 100 mL of diluent.
Appropriate diluents include 0.9% Sodium Chloride Injection USP (normal saline), 5% Dextrose Injection USP (D5W), or Lactated Ringers Solution.
infusion rate : minimum given in 30 minutes
KI :Active peptic ulcer; hypersensitivity. Neonates with congenital heart disease, suspected necrotising enterocolitis and active bleeding (parenteral).
Cardiovascular Risk
• NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk
• Ibuprofen tablets are contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery
Farmakodinamik
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that possesses anti-inflammatory, analgesic and antipyretic activity.
Its mode of action, like that of other NSAIDs, is not completely understood,
but may be related to prostaglandin synthetase inhibition. After absorption of the racemic ibuprofen, the [-]R-enantiomer undergoes interconversion to the [+]S-form. The biological activities of ibuprofen are associated with the [+]S-enantiomer.
Farmakokinetik
Absorption - In vivo studies indicate that ibuprofen is well absorbed orally from the suspension formulation, with peak plasma levels usually occurring within 1 to 2 hours
Antacids - A bioavailability study in adults has shown that there was no interference with the absorption of ibuprofen when given in conjunction with an antacid containing both aluminum hydroxide and magnesium hydroxide.
H-2 Antagonists – In studies with human volunteers, coadministration of cimetidine or ranitidine with ibuprofen had no substantive effect on ibuprofen serum concentrations.
Food Effects - Absorption is most rapid when MOTRIN is given under fasting conditions. Administration of MOTRIN Suspension with food affects the rate but not the extent of absorption. When taken with food, Tmax is delayed by approximately 30 to 60 minutes, and peak levels are reduced by approximately 30 to 50%.
Distribution - Ibuprofen, like most drugs of its class, is highly protein bound (>99% bound at 20μ g/mL). Protein binding is saturable and at concentrations >20 μ g/mL binding is non-linear. Based on oral dosing data there is an age- or fever- related change in volume of distribution for ibuprofen. Febrile children <11 years old have a volume of approximately 0.2 L/kg while adults have a volume of approximately 0.12 L/kg. The clinical significance of these findings is unknown.
Metabolism - Following oral administration, the majority of the dose was recovered in the urine within 24 hours as the hydroxy-(25%) and carboxypropyl-(37%) phenylpropionic acid metabolites. The percentages of free and conjugated ibuprofen found in the urine were approximately 1% and 14%, respectively. The remainder of the drug was found in the stool as both metabolites and unabsorbed drug.
Elimination - Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of ibuprofen is virtually complete 24 hours after the last dose. It has a biphasic plasma elimination time curve with a half-life of approximately 2.0 hours. There is no difference in the observed terminal elimination rate or half-life between children and adults, however, there is an age-or fever-related change in total clearance. This suggests that the observed change in clearance is due to changes in the volume of distribution of ibuprofen (see Table 1 for Cl/F values).
Indikasi :
Oral
Pain and inflammation
Adult: 1.2-1.8 g/day in divided doses. Maintenance: 0.6-1.2 g daily. Max: 2.4 g/day.
Child: 5-10mg/Kg
Oral
Juvenile idiopathic arthritis
Child: ≥3 mth and weighing >5 kg: 30-40 mg/kg/day in 3-4 divided doses. Max: 2.4 g/day.
Oral
Fever
Adult: 200-400 mg every 4-6 hr. Max: 1.2 g/day.
Child: 1-6 mth: 5 mg/kg 3-4 times daily, 6-12 mth: 50 mg tid, 1-2 yr: 50 mg 3-4 times daily, 2-7 yr: 100 mg 3-4 times daily, >7 yr: 200 mg 3-4 times daily. Max: 40 mg/kg/day.
Intravenous (inj)
Closure of patent ductus arteriosus
Child: Given as three IV doses infused over 15 min at 24-hr intervals. Initially 10 mg/kg followed by 2 doses of 5 mg/kg. A 2nd course may be given if ductus remains open after 48 hr. Surgery may be required if neonate is unreponsive to two courses of treatment. Dose should be based on birth weight.
Topical/Cutaneous
Pain and inflammation associated with musculoskeletal and joint disorders
Adult: As 5% or 10% gel: Apply onto affected area.
Sediaan:
Oral : tablet 200 mg, 400 mg, 600mg, 800mg. Susp: 100mg/5cc , 200mg/5cc (susp. forte) , oral drop: 40mg/cc
Injeksi (caldolor@) : 400 mg/4 mL (100 mg/mL), 800 mg/8 mL (100 mg/mL)
Caldolor must be diluted prior to intravenous infusion. dilute into concentration of 4mg/cc or less
800 mg dose: Dilute 8 mL of Caldolor in no less than 200 mL of diluent.
400 mg dose: Dilute 4 mL of Caldolor in no less than 100 mL of diluent.
Appropriate diluents include 0.9% Sodium Chloride Injection USP (normal saline), 5% Dextrose Injection USP (D5W), or Lactated Ringers Solution.
infusion rate : minimum given in 30 minutes
KI :Active peptic ulcer; hypersensitivity. Neonates with congenital heart disease, suspected necrotising enterocolitis and active bleeding (parenteral).
Cardiovascular Risk
• NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk
• Ibuprofen tablets are contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery
Farmakodinamik
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that possesses anti-inflammatory, analgesic and antipyretic activity.
Its mode of action, like that of other NSAIDs, is not completely understood,
but may be related to prostaglandin synthetase inhibition. After absorption of the racemic ibuprofen, the [-]R-enantiomer undergoes interconversion to the [+]S-form. The biological activities of ibuprofen are associated with the [+]S-enantiomer.
Farmakokinetik
Absorption - In vivo studies indicate that ibuprofen is well absorbed orally from the suspension formulation, with peak plasma levels usually occurring within 1 to 2 hours
Antacids - A bioavailability study in adults has shown that there was no interference with the absorption of ibuprofen when given in conjunction with an antacid containing both aluminum hydroxide and magnesium hydroxide.
H-2 Antagonists – In studies with human volunteers, coadministration of cimetidine or ranitidine with ibuprofen had no substantive effect on ibuprofen serum concentrations.
Food Effects - Absorption is most rapid when MOTRIN is given under fasting conditions. Administration of MOTRIN Suspension with food affects the rate but not the extent of absorption. When taken with food, Tmax is delayed by approximately 30 to 60 minutes, and peak levels are reduced by approximately 30 to 50%.
Distribution - Ibuprofen, like most drugs of its class, is highly protein bound (>99% bound at 20μ g/mL). Protein binding is saturable and at concentrations >20 μ g/mL binding is non-linear. Based on oral dosing data there is an age- or fever- related change in volume of distribution for ibuprofen. Febrile children <11 years old have a volume of approximately 0.2 L/kg while adults have a volume of approximately 0.12 L/kg. The clinical significance of these findings is unknown.
Metabolism - Following oral administration, the majority of the dose was recovered in the urine within 24 hours as the hydroxy-(25%) and carboxypropyl-(37%) phenylpropionic acid metabolites. The percentages of free and conjugated ibuprofen found in the urine were approximately 1% and 14%, respectively. The remainder of the drug was found in the stool as both metabolites and unabsorbed drug.
Elimination - Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of ibuprofen is virtually complete 24 hours after the last dose. It has a biphasic plasma elimination time curve with a half-life of approximately 2.0 hours. There is no difference in the observed terminal elimination rate or half-life between children and adults, however, there is an age-or fever-related change in total clearance. This suggests that the observed change in clearance is due to changes in the volume of distribution of ibuprofen (see Table 1 for Cl/F values).
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