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OZAC ®
ozacProduct
(Ozagrel Sodium)
Powder for Injection
Generic name: Ozagrel Sodium for Injection
The principal component of this product is Ozagrel Sodium.
Chemical name: (E)—3—(imidazolethyl—1—methyl) sodium acid cinnamon. Structural formula:
Molecular formula: C13H11N2NaO2
Molecular weight: 250.23
Description: The drug is white to almost white loose mass.
Indications: Used for the treatment of acute thrombotic cerebral infarction or disturbance on motor functions.
Usage and dosage:
For Adult: 80mg per time, twice a day, dissolved in 500ml of normal saline or 5% glucose solution, I.V., Intravenous 1~2 weeks for a course.
Adverse reactions:
Gastrointestinal reactions and allergic reactions, such as nausea, vomiting, urticaria, skin rashes and so on, to mitigate with appropriate treatment. GOT GPT, BUN increase sometime. intracranial, gastrointestinal, skin may bleed and thrombocytopenia may happen.
Contraindication:
The patients with following symptoms:
1. Allergic to ozagrel;
2. Cerebral hemorrhage or cerebral infarction with hemorrhage,
deep coma accompanied large area cerebral infarction;
3. Severe impairment on heart, lung, liver, kidney, such as
severe arrhythmia or cardiovascular infarction;
4. Hemopathy or hemorrhagic tendency;
5. Severe hypertension, with a contracting pressure of 200mmHg.
Precautions:
Avoid mixing use of this drug and solution containing calcium (Green's solution) in case there will be white turbidity.
Pregnancy and lactation:
Used with caution in pregnancy. Others are not clear.
Children: There is no experience of using it in children till now.
Senile patient:
Used with caution in senile patient because of the poor physical condition.
Drug interactions:
When used with platelet anti-coagulant, thrombosis dissolutant or other anti-coagulants, hemorrhagic tendency can be increased, therefore it should be used with extreme care. If necessary, the dose can be decreased.
Drug overdose:
Once the over-dosage happens, specific treatment should be granted to different symptoms, but the focus is to monitor the hemorrhage and coagulation and to deal with them promptly.
Pharmacology and toxicology:
Pharmacology
The product is of high effect, choice thromboxane synthetase, by inhibiting production of thromboxane A2 (TXA2) to improve balance, has anti-platelet aggregation and dilate vessels, and inhibit vasospasm, increase blood flow quantity, improve microcirculation disturbance and energy metabolism, so improve brain local ischemia after arachnoid under cavity hemorrhage operation and ataxia of patient with cerebral thrombosis.
Toxicity research:
Repeated dose toxicity: rats and dogs were given the product by intravenous injection. Rats at high dosage are found that electrolyte excretion increase slightly, other abnormal reaction is not found. Maximum tolerance dose of rat is 125mg/kg, for dog is 10～12.5mg/kg. Reproduction toxicity: rat and rabbit are gave the product by intravenous injection, as a result, increasing of animal’ weight has been inhibited, embryo could die at big dose. Growth is inhabited and new-birth animals are died. In sensitive period of teratogenic test , fetal with visceral and skeleton teratogenic increase slightly.
Pharmacokinetics:
As report, after intravenous injection Ozagrel Sodium for Injection, concentration-time of serum drug complies two-compartment open mode, t1/2ß is 1.22±0.44h, Vd is 2.32±0.62L/kg, AUC is 0.47±0.08ｕg.hr/ml, Cl is 3.25± 0.82L/h/kg. When single inject the product, it disappears quickly. The main component in blood is Ozagrel, ß-oxidosome and reducing body. The metabolism of product has no pharmacology action.
The products are injected continually, come up to summit of concentration within 2hours. The large half-life is 1.93. After stopping drug 3hours, drug in serum could be monitored still. Most of the product is excreted in 24 hours. After stopping drug 24hours, all drugs are excreted from urine.
Storage: Preserve in tightly closed containers, protected from light. (10~30OC)
Package: Vials in strength of 20, 40, & 80mg are available.
Period of validity: 24 Months.
Available at all leading pharmacies in Pakistan on prescription only.
For further queries.
Tel: +92 21 34123535, 34123636, 0346-3636201
UAN: +92 21 111-graton (472-866)
Fax: +92 21 34937304
Email: info@gratonpharma.com
Web: www.gratonpharma.com |
