These are products obtained from microorganisms and have prominent antitumour activity. Practically all of them intercalate between DNA strands and interfere with its template function.
ANTIBIOTICS
These are products obtained from microorganisms and have
prominent antitumour activity. Practically all of them intercalate between DNA
strands and interfere with its template function.
It is a very potent antineoplastic drug, highly efficacious
in Wilms’ tumour and rhabdomyosarcoma. It has also produced good results in Mtx
resistant choriocarcinoma and few other malignancies. Prominent adverse effects
are vomiting, stomatitis, diarrhoea, erythema and desquamation of skin,
alopecia and bone marrow depression.
Dose: 15 μg/kg i.v. daily for 5
days.
DACMOZEN 0.5 mg/vial
inj.
These are antitumour
antibiotics with quite similar chemical structures. However, utility of
daunorubicin is limited to acute leukaemia (in which it is highly active) while
doxorubicin, in addition, is effective in many solid tumours. They are capable
of causing breaks in DNA strands by activating topoisomerase II and generating
quinone type free radicals. They have mutagenic and carcinogenic potential.
Maximum action is exerted at S phase, but toxicity is usually exhibited in G2
phase.
Both these antibiotics
produce cardiotoxicity as a unique adverse effect. This can manifest either
acutely with ECG changes, arrhythmias and hypotension which are reversible, or
be delayed—congestive heart failure (related to the total dose administered).
CHF is due to cardiomyopathy and may be fatal. Marrow depression, alopecia,
stomatitis, vomiting and local tissue damage (on extravasation) are other
adverse effects.
Daunorubicin: 30–60
mg/m2 BSA i.v. daily for 3 days, repeat weekly.
DAUNOCIN, DAUNOMYCIN
20 mg/vial inj. Doxorubicin: 60–75 mg/m2 BSA slow i.v. injection every 3 weeks; ADRIAMYCIN,
DOXORUBICIN, ONCODRIA 10 mg, 50 mg per vial inj.
A recently introduced analogue of doxorubicin with lower cardiotoxicity,
probably because it does not produce quinone type free radicals. It has a
narrow range of utility: in acute nonhaemolytic leukaemia, chronic myelogenous
leukaemia, nonHodgkin lymphoma and carcinoma breast. Though cardiomyopathy can
occur, major toxicity is marrow depression and mucosal inflammation.
ONCOTRON 20 mg/10 ml
inj; 14 mg/m2 single i.v. dose, repeat at 3 weeks.
This is a mixture of closely related glycopeptide
antibiotics having potent antitumour activity. It chelates copper or iron,
produces superoxide ions and intercalates between DNA strands—causes chain
scission and inhibits repair. It is highly effective in testicular tumour and
squamous cell carcinoma of skin, oral cavity, head and neck, genitourinary tract
and esophagus; also useful in Hodgkin’s lymphoma.
Mucocutaneous toxicity and pulmonary fibrosis, but little
myelosuppression are the special features.
Dose: 30 mg twice weekly
i.v. or i.m. (total dose 300–400 mg);
BLEOCIN,
ONCOBLEO 15 mg inj.
This highly toxic drug
is used only in resistant
cancers of stomach, cervix, colon, rectum, bladder, etc. It is transformed
intracellularly to a form which acts as an alkylating agent and kills cells in
G1M phases. Bone marrow and g.i.t. are the primary targets of
toxicity.
Dose: 10 mg/m2 BSA, infused i.v. in one day or divided
in 5 and infused over 5 days. MITOMYCINC 2, 10 mg
inj.
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