Ozagrel Na I.V. Infusion 40mg MEEK

Ozagrel Na I.V. Infusion 40mg MEEK

Manufacturer:

Kobayashi Kako

Distributor:

Zuellig Pharma

Marketer:

Daiichi-Sankyo
Full Prescribing Info
Contents
Ozagrel Sodium.
Description
See Table 1.

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It occurs as white crystals or crystalline powder.
It is freely soluble in water, soluble in methanol, and practically insoluble in ethanol (99.5).
Chemical name: Monosodium(2E)-3-[4-(1H-imidazol-l-ylmethyl)phenyl] prop-2-enoate.
Molecular formula: C13H11N2NaO2.
Molecular weight: 250.23.
Action
Pharmacology: Ozagrel sodium selectively inhibits synthesis of thromboxane A2 (TXA2), which exists in the arachidonic acid cascade, to decrease production of TXA2, as a result, the function of platelet aggregation by TXA2 is weakened.
It also accelerates the production of prostacyclin and improves the balance between prostacyclin and TXA2. In addition, it has an inhibitory action on cerebrovascular spasm and cerebral blood flow decrease.[The Japanese Pharmacopoeia Seventeenth Edition, Kaisetsusho]
Pharmacokinetics: Blood concentrations[Internal data of KOBAYASHI KAKO CO., LTD. (Blood concentration testing)]: When 8 mL of this drug (80mg of ozagrel sodium in 8 mL) was diluted with 250 mL of Isotonic Sodium Chloride Solution JP and administered continuously by intravenous drip infusion over a period of 2 hours, the mean plasma concentration of ozagrel sodium reached the peak of 1102ng/mL at 1.8 hours after administration. The half-life after the end of administration was 0.74 hour (Table 2). The concentration decreased to the detection limit and below at 6 hours after administration (figure). (See figure and Table 2.)

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Indications/Uses
Improvement of cerebral vasospasm after operation for subarachnoid hemorrhage and its resultant ischemic symptoms.
Improvement of motor dysfunction resulting from cerebral artery thrombosis (acute phase).
Dosage/Direction for Use
Improvement of cerebral vasospasm after operation for subarachnoid hemorrhage and its resultant ischemic symptoms: Usually for adults, dilute a daily dose of 80 mg of ozagrel sodium with a suitable amount of an electrolyte or sugar solution, and administer intravenously continuously over a 24-hour period. It is desired to start administration soon after operation for subarachnoid hemorrhage and to administer continuously for two weeks.
The dosage may be adjusted according to the patient's age and severity of symptoms.
Improvement of motor dysfunction resulting from cerebral artery thrombosis (acute phase): Usually for adults, dilute 80 mg of ozagrel sodium with a suitable amount of an electrolyte or sugar solution, and administer intravenously twice daily (in the morning and evening), over a period of two hours each, for about two weeks.
The dosage may be adjusted according to the patient's age and severity of symptoms.
Contraindications
OZAGREL Na I.V. Infusion 40mg MEEK is contraindicated in the following patients: Patients with hemorrhage: Patients complicated by hemorrhagic cerebral infarction, extradural hemorrhage, intracerebral hemorrhage, or primary intraventricular hemorrhage [There is a possibility of aggravated hemorrhage].
Patients with cerebral embolism [Hemorrhagic cerebral infarction is likely to occur in patients with cerebral embolism].
Patients with a history of hypersensitivity to any of the ingredients of this drug.
RELATIVE CONTRAINDICATIONS: As a general rule, OZAGREL Na I.V. Infusion 40mg MEEK is contraindicated in the following patients. If the use of this drug is considered essential, it should be administered with care: Patients with a risk of cerebral embolism: Patients with atrial fibrillation, myocardial infarction, valvular disease of heart, infectious endocarditis or nervous symptoms of instantaneous completed type [Hemorrhagic cerebral infarction is likely to occur in patients with cerebral embolism].
Patients with major infarction accompanied by severe consciousness disorder [Hemorrhagic cerebral infarction is likely to occur in patients with major infarction].
Special Precautions
Careful Administration (OZAGREL Na I.V. Infusion 40mg MEEK should be administered with care in the following patients): Patients with hemorrhage: Digestive tract hemorrhage, subcutaneous hemorrhage, etc. [There is a possibility of hemorrhage being aggravated.]
Patients with possible hemorrhage: Patients with a history of cerebral hemorrhage, severe hypertension, severe diabetes mellitus, thrombocytopenia, etc. [There is a possibility of hemorrhage being aggravated.]
Patients taking antiplatelets, thrombolytics or anticoagulants (refer to Interactions.)
Important Precautions: There is a possibility that hemorrhagic cerebral infarction, extradural hemorrhage or intracerebral hemorrhage may be aggravated by the administration of this drug. Therefore, administer this drug while preparing emergency treatment. Also, be sure to make adequate observation of clinical symptoms and to carry out computerized tomography. If hemorrhage occurs, administration should be discontinued immediately and appropriate measures must be taken.
Use in Children: The safety of this drug in low-birth-weight infants, neonates, nursing infants, infants and children has not been established.
Use in the Elderly: Since the elderly often have reduced physiological function, this drug should be administered carefully.
Use In Pregnancy & Lactation
This drug should be used in pregnant women or in women who may possibly be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment. [The safety of this drug in pregnant women has not been established.]
Adverse Reactions
This drug has not been investigated (drug use investigation etc.) to determine the incidence of adverse reactions.
Clinically significant adverse reactions (Incidence unknown): Hemorrhage: Since hemorrhagic cerebral infarction, extradural hematoma, intracerebral hemorrhage, digestive tract hemorrhage, subcutaneous hemorrhage, hematuria, etc., may occur, patients should be monitored carefully. If abnormalities are observed, administration should be discontinued. [Because this drug inhibits the function of platelet aggregation.]
Shock, anaphylaxis: Since shock or anaphylaxis may occur, patients should be monitored carefully. If symptoms such as hypotension, dyspnea, laryngeal edema or cold feeling occur, administration should be discontinued and appropriate measures must be taken.
Hepatic function disorder, jaundice: Since severe hepatic function disorder with marked increase in AST (GOT) and/or ALT (GPT) or jaundice may occur, patients should be monitored carefully. If such symptoms are observed, administration should be discontinued and appropriate measures must be taken.
Thrombocytopenia: Thrombocytopenia may occur. If such a symptom is observed, reduction in dose or discontinuation of the administration should be made.
Leucopenia, granulocytopenia: Leucopenia or granulocytopenia may occur. If such symptoms are observed, administration should be discontinued and appropriate measures must be taken. Fever and/or rigors often occur with these symptoms. In these cases, development of leucopenia and granulocytopenia should be suspected and blood test must be done.
Renal function disorder: Since severe renal function disorder such as acute renal failure may occur, patients should be monitored carefully. If abnormalities in renal function are observed, administration should be discontinued and appropriate measures must be taken. Many cases with renal function disorder are accompanied by thrombocytopenia.
Other adverse reactions: See Table 3.

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Drug Interactions
Precautions for coadministration (OZAGREL Na I.V. Infusion 40mg MEEK should be administered with care when coadministered with the following drugs: See Table 4.

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Caution For Usage
Precautions concerning Use: Preparations: White turbidity may be formed if this drug is diluted with transfusions containing calcium. When using calcium-containing transfusions (Ringer's solution etc.) to dilute this drug, use at least 300 mL (per 80 mg of this drug) of the transfusion for dilution.
This drug is supplied as one-point-cut ampoules. But to prevent foreign matter from entering the ampoule, wipe with an alcohol swab prior to cutting.
Precautions for Handling: Stability testing[Internal data of KOBAYASHI KAKO CO., LTD. (Stability testing)]: OZAGREL Na I.V. Infusion 40mg MEEK: The accelerated testing (40℃, 6 months) of this drug with finished products suggested 3 years stability of this drug under usual market circumstances.
Storage
Store below 30 degree Celsius.
(Store under protection from light.)
ATC Classification
B01AC - Platelet aggregation inhibitors excl. heparin ; Used in the treatment of thrombosis.
Presentation/Packing
Inj (amp) 40 mg/4 mL x 10's.
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