Anti tumour drugs

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*Cyclophosphamide*

#Formulations: 

1. Cyclophosphamide tablet IP

2. Cyclophosphamide injection IP

#Brand_Names: Cycloxan, Endoxan-Asta, Ledoxan

#Pharmacological_Action: It is inactive as such: produces few acute effects and is not locally damaging. Transformation into active metabolites (aldophosphamide, phosphoramide mustard) occurs in the liver, and a wide range of Anti-tumour action is exerted. It has prominent immunosuppressant property. Thus, it is one of the most popular alkylating agents useful in many solid tumours. It is less damaging to platelets, but alopecia and cystitis (due to another metabolite acrolein) are prominent.

#Dose: 2-3 mg/Kg/day oral; 10-15mg/kg i.v. every 7-10 days, i.m. use also possible.

#Therapeutic_Uses: Used as an anticancer drug.

*Busulfan*

#Formulations: Busulfan Tablet BP, IP

#Brand_Names : MYLERAN, BUSUPHAN 2mg tab.

#Pharmacological_Action: This alkylating agent is highly specific for myeloid elements; granulocyte pre-cursors being the most sensitive, followed by those of platelets and RBC.

#Side_Effects: It produces little effect on lymphoid tissue and GIT, Hyperuricemia is common; pulmonary fibrosis and skin pigmentation are the specific adverse effects of it. Sterility also occurs. It is now the 2nd choice drug to imatinib for chronic phase of myelocytic leukaemia.

#Dose: 2-6mg/day (0.06 mg/kg/day) orally

#Therapeutic_Uses : Used as anticancer drug.

*Fluorouracil*

#Formulations: Fluorouracil injection IP.

#Brand_Names: Fluracil, Fivocil, Oncpurcil, Flocil, Florac, Fivoflu.

*Methotrexate*

#Formulations: 

Methotrexate Tablets IP

Methotrexate injection IP

#Brand_Names : Neotrexate, Biotrexate

#Pharmacological_Action : This folic acid analogue is one of the oldest and highly efficacious antineoplastic drugs which acts by inhibiting dihydrofolate reductase, thus blocking the conversion of dihydrofolic acid to tetrahydrofolic acid. Utilizing the folate carrier it enters into cells and is transformed to more active polyglutamate from by the enzyme folypolyglutamate synthase. Tetrahydrofolic acid is an essential coenzyme required for one carbon transfer reactions in de novo purine synthesis and amino acid interconversion. The inhibition is pseudo irreversible because Mtx has 50000 times higher affinity for the enzyme than the normal substrate. It kills cells in S phase. In this process synthesis of RNA, DNA & protein suffers. 

#special_effects: It is absorbed orally, 50% plasma protein bound, little metabolised and largely exerted unchanged in urine. Salicylates, sulfonamides, dicumerol, displace it from protein binding sites. Aspirin and sulfonamides enhance toxicity of Mtx by decreasing it's renal tubular secretion.

#Dose: 15-30 mg/day for 5 days orally or 20-40 mg/m² BSA i.m. or i.v. twice weekly.

#Side_Effects : High dose Mtx can induce remission in childhood acute lymphoblastic leukaemia and is also effective in maintenance of remission so that disease may cured.

#Therapeutic_Uses: antineoplastic drugs, immunosuppressant, rheumatoid arthritis

*Dactinomycin*

#Formulations : Dactinomycin injection

#Pharmacological_Action : It is a very potent peptide antineoplastic drugs, highly effiacious in Wilm's tumour and childhood rhabdomyosarcoma. Dactinomycin has been combined with Mtx for cure of choriocarcinoma, or may be used in Mtx resistant cases. Good results have also been obtained in Ewing's sarcoma and metastatic testicular carcinoma. In addition to blocking RNA transcription it causes single strand breaks in DNA. 

#Side_Effects :  vomiting, stomatitis, diarrhoea, erythema, and desquamation of skin, alopecia and bone marrow depression.

#Dose : 15ug/kg i.v. daily for 5 days

#Therapeutic_Uses : used as antineoplastic drugs

*Doxorubicin Hydrochloride*

#Formulations : Doxorubicin HCl tablet IP

Doxorubicin HCl injection IP

Doxorubicin HCl injection BP

#Pharmacological_Action : It intercalate between DNA strands and block DNA as well as RNA synthesis. They combine with and activate topoisomerase -2 causing breaks in DNA. They also generate quinone type free radicals.  They have mutagenic and carcinogenic potential. Maximum action is exerted at S phase, but toxicity usually exhibited in G2 phase.

#Side_Effects : Cardiotoxicity, arrhythmias, hypotension, congestive heart failure, alopecia, stomatitis, vomiting. Urine may be red coloured.

#Therapeutic_Uses : used as antineoplastic drugs

*Vinblastin Sulphate*

#Formulations : Vinblastin injection

#Pharmacological_Action : It is primarily employed along with other drugs in Hodgkin's disease, Kaposi sarcoma, neuroblastoma, non- Hodgkin's lymphoma etc. 

#Side_Effects : neurotoxicity, alopecia, local tissue necrosis.

#Brand_Names : Uniblastin, Cytoblastin

#Therapeutic_Uses : used as antineoplastic drugs

*Cisplatin*


#Formulations : Cisplatin injection IP

#Brand_Names :  Neoplastin, Plastinex, Platinol, Aquaplat

#Pharmacological_Action : The platinum coordination complexes enter cells and are hydrolyzed intercellularly to produce a highly reactive moiety which causes cross linking of DNA. The favoured site is N⁷ of guanine residue. It can also react with -SH groups of cytoplasmic and nuclear proteins. The effects resemble those of alkylating agents and radiation. It is slowly excreted unchanged in urine with a t½ of about 72hrs. Negligible amount enters brain.

#Side_Effects : Tinnitus, deafness, sensory neuropathy and hyperuricaemia.






#Dose : i.v. infusion 50-100 mg/m² BSA every 3-4 weeks.

#Therapeutic_Uses  : Used as antineoplastic drugs

*Dromostenolone Propionate*

#Formulations : dromostenolone Propionate injection


#Brand_Names : Masteril, Masteron, Drolban, Mastisol, Premastril, Prometholone.

#Therapeutic_Uses : used as antineoplastic drugs