Zidine 300mg (Zidovudine)

DESCRIPTION

Zidine    is pharmacologically categorized as nucleoside reverse transcriptase inhibitor. Reverse transcriptase enzyme is essential for viral production.

Zidine    tablets are combination tablets which containing an active constituents known as zidovudine as an anti-retroviral medications and is used with other anti-retroviral drugs for better activity. Patients who are getting Zidine    tablets treatment should have better able to attach to complex drug therapy regimen, thereby improving the compliance.

INDICATION

Zidine    is a most conspicuous nucleoside analogues which express anti-retroviral activity. Zidine    should be combined with other anti-retroviral drugs for better action. The usually indicated for the treatment of HIV-1 infection in adult and pediatric patient

MECHANISM OF ACTION

The mechanism of action of zidovudine is also similar to lamivudine, like inhibition of viral reverse transcriptase by zidovudine triphosphate which is an active moiety of zidovudine. Finally viral DNA chain termination occurs.

PHARMACOKINETIC

ABSORPTION

The absorption of zidovudine is occurs very quickly. The oral bioavailability of Zidine    ;

DISTRIBUTION

The Zidine    is highly distributed in body. The component of Zidine    tablets are binding to human plasma protein with the range of <38% for zidovudine. The binding plasma ratio of Zidine    is low.

METABOLISM

Zidovudine is undergoes metabolism by glucoronide conjugation.

EXCRETION

Zidine    is undergoes hepatic metabolism elimination. Route of elimination of zidovudine is 29% through urine; 45% excreted as zidovudine metabolite. The zidovudine half life period of is 0.5 to 3 hours. The renal creatinine clearance of zidovudine is 0.34 plus or minus 0.05 L/hr/kg.

DOSAGE MANAGEMENT

IN ADULT

The recommended dose is 300mg Zidovudine capsules for twice daily in combination with other antiretroviral.

PEDIATRIC PATIENTS (AGE OF 4 WEEKS TO < 18 YEARS)

The dose is usually calculated based on body weight(kg) and not to be exceed the usual adult dose The patient body weight 4 to <9 = 24mg/kg/day given as 12mg/kg twice daily; 8mg/kg three times daily >9 to >30 = 18mg/kg/day given as 9mg/kg for twice daily ; 6mg/kg three times daily ≥ 30 = 600mg/day given as 300mg for twice daily ; 200mg for three times daily

PREVENTION OF MATERNAL-FETAL HIV-1 TRANSMISSION

Maternal dosing: Before start of labor administrate 100mg orally 5 times /day. During labor and delivery, administered 2mg/kg IV over 1 hour followed by a continuous IV infusion of 1mg/kg/hr until clamping of umbicalcord Neonatal dosing After birth Dosing within 12 hours and continue through 6 weeks of age Oral route = 8mg/kg/day total daily dose but given as 2mg/kg for every 6 hours Intrevenous route = 6mg/kg/day total daily dose but given as 1.5mg/kg infused over 30min, every 6hrs Zidine    tablet should be administered with or without food.

OVER DOSAGE

The over dosage of Zidine    should be treated by undergoing hemodialysis. Hemodialysis helps to remove the content of zidovudine from the body. The acute over dosage condition, causes adverse effects like fatigue, headache, vomiting & hematological disturbance. Provide supportive measures.

WARNING & PRECAUTION

WARNING

Hematological toxicity, lactic acidosis or hepatomegaly with steatosis & aggravation of hepatitis B infection; these are all possible adverse occurred during or after completion of therapy with Zidovir.

HEMATOLOGICAL TOXIC

Periodic blood cells count should be taken. In case of neutropenia or thrombocytopenia, Zidine    treatment should be postponed.

LACTIC ACIDOSIS OR HEPATOMEGALY WITH STEATOSIS

This condition may leads to produce fatal cases, majorly in women. The most common adverse effect is obesity In severe condition treatment should be discontinued.

RIBAVIRIN BASED THERAPY

Zidine    combined with ribavirin causes hematological problems in severe condition. Avoid the concomitant use Check the blood cell count during the therapy if necessary. In Immune reconstitution syndrome, Zidine    tablets should be

HEPATITIS B CO INFECTION

To overcome the post treatment aggravation of hepatitis infection, patient should be monitored with hepatic function frequently after completion of treatment. The incidence of lamivudine resistance caused hepatitis infection; the potency of lamivudine in patient with HIV-1 HCV co infection has not been evaluated. The concurrent use of lamivudine may leads to cause this type of infection. discontinued

SIDE EFFECTS

THE MOST COMMON SIDE EFFECTS
Headache Malaise Fatigue Anorexia Loss of appetite Dyspepsia Abdominal cramps Neuropathy Insomnia Dizziness Depression Nasal signs Cough Rashes Musculoskeletal pain Myalgia Arthralgia

LAB ABNORMALITIES
Neutropenia Anemia Thrombocytopenia Elevated AST, ALT Hyperbilirubinaemia Increased amylase Fat redistribution Cardiomyopathy Gynecomastia Lymphadenopathy Splenomegaly Wheezing Alopecia Erythema multiforme Stevens Johnson’s syndrome

THE MOST SERIOUS ADVERSE EFFECTS ARE
Hematological toxicity Symptomatic myopathy Lactic acidosis or hepatomegaly with steatosis Aggravation of hepatitis B Hepatic decompensated cirrhosis in patient with HCV/HIV co infection. Aggravation of anemia due to patients who are co infected with HIV-1/HCV getting ribavirin & zidovudine. Pancreatitis Immune reconstitution syndrome Lipoatrophy

DRUG INTERACTION

Drugs which are opposing the activity of zidovudine; The combination of zidovudine with some drugs produces antagonist effects, like Stavudine Doxorubicin Nucleoside analogues like ribavirin

Zidine    tablets are concurrent use with ribavirin, Ganciclovir, interferon alfa or other drugs may elevate the hematological toxicity effect of zidovudine. Avoid this concomitant treatment. Avoid this combination therapy. Zidine    should not be combined with Zalcitabine which may alters t or inhibits the intracellular phosphorylation of one another.

CONTRAINDICATIONS

Anaphylactic reaction may occur in the patient are contraindicated to the component present in Zidine    tablets.

PREGNANCY & LACTATION

The pregnancy category of Zidine    is C Animal reproduction studies have shown adverse effect on fetus while in human there are no sufficient and well tolerated studies, but possible use may warrant the in drug in pregnant women produce possible risk. Generally HIV infected patients should not feed the baby. Zidine    metabolites are eliminated via human breast milk.

STORAGE 

Zidine    tablet kept at 20° to 25°C temperature Protect the container away from moisture, heat & light.

MISSED DOSE

If a dose is missed by the patient then have the dose as soon as possible or skip the medicine and follow regular schedule. Please consult with the doctor