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Some common Definitions

Absorption Absorption means the process entry of constituents from the lumen of gut to the
body. Food constituents are mainly absorbed from the proximal area (duodenum) of small
intestine.
Absorption site The most important site of the drug absorption is the small intestine. Small
intestine transit time (SITT) ranges from 3 to 4 hours for mostly healthy subjects. If absorption
not occurs by this time, absorption becomes erratic. In contrast the fluids in the color are
reabsorbed, making the drug to difficult to further dissolution. As a result absorption will be
erratic.
Affinity Tendency of a drug to combine with receptor or bind with receptor.
Agonist Drug that binds with receptor and activates them to produce a therapeutic response is
called agonist.
Agonist Have both affinity and efficacy. Drug that has ability to bind with the receptor and
stimulates receptor thus giving physiological activity.
Anaphylactic shock Severe allergic reaction
Antagonist Have only affinity but no efficacy. Drug that bind to the cell receptor and thus
blocks the action of other substance (neurotransmitter, hormone etc.)
Bio-availability How much drug present in plasma level of blood or presence of drug in
plasma level or measurement of active drugs reach to systemic circulation.
Biological half-life Time required to elimination of 50% drug from the body
Biological response The doses are taken at a time or in a fractions amount within particular
time to get Biological response.
C max Maximum plasma concentration
Digestion is the breakdown of food constituents into smaller in preparation for absorption.
Dose Dose is measurement which is required to produce certain measurable biological
response, either at once or sometime after administration.
Drug - (WHO scientific group definition) A drug is any substance or product that is used or
intended to the used to modify or explore physiologic systems or pathological states for the
benefit of the recipient.
Drug Antagonism It may be defined as the abolition or inhibitor of the effect of one drug by
another drug. So that the combined effect of two drugs is less than that of individual drug.
Drug dependence The psychophysical state of a drug user in which the usual or increasing
dose of the drug are required to prevent the onset of withdrawal symptoms.
Drug receptor A molecule on the surface or within a cell that recognizes and binds with other
specific molecules, thats producing a specific effect in the cell. Drug receptor is organized cell,
macromolecular in structure, protein in nature where drug interacts.
Drug resistance Some time body cannot response with the given dose. These occur due to
excess quantity or irregular drug intake.
Drug tolerance How many dose of drug a person can tolerate.
ED50 Effective dose in 50% population within 100 people
Efficacy Ability to produce therapeutic effects by stimulating receptor.
Efficacy Efficacy is the capacity of a drug, after binding with a receptor can produces a
pharmacologic effect.
Fatal dose Dose in which 100% population will die or must die
Food Food is the active ingredient of the body, which provides energy and enhances the
physiological process of the body.
Inverse agonist Some drug binds with receptors and produce effects that are opposite to those
produced by a true agonist. These agents are called inverse agonist.
LD50 50% population must have lethal activity of Drug within 100 People. 50% population may
die.
Medicine- Medicine is any form which has a definite form, dose, level and is the therapeutically
used for the treatment of decreases in living subjects (WHO definition).
Partial agonist Drug that binds receptor and is capable of low degree of activating of receptors
is called partial agonist.
Pharmacodynamics The study of the biochemical and physiological effects / change of drugs
and the mechanism of their actions.
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Pharmacokinetics - It deals with absorption, distribution, metabolism and excretion. The action
of drugs in the body over a period of time, including the process of absorption, distribution,
localization of tissue, biotransformation and excretion.
Pharmacology The science that deals with the origin, nature, chemistry, effects, and use of
drugs.
Pharmacopoeia An authoritative treatise on drugs and their preparations. Use to test for purity,
method of standardization.
Plasma half-life The Time when plasma drug concentration will be half Or The time required
by the body, tissue, or organ to metabolize or inactivate half amount of substance taken in.
Potency Potency is a comparative measure refers to the different doses of two drugs that are
needed to produce the same effect.
Reflux action an involuntary motor response of CNS due to the presence of any stimulants
T max - Maximum time required to reach C max
Teratogenic effects If a drug crosses placenta barrier it shows teratogenicity. It is harmful for
infants and mother
Therapeutic index - LD50/ ED50, it is a measure of the safety margin of a drug. The large value
indicates that there is a wide margin between doses that are effective and doses that are toxic.
Side effects Usually caused when a drugs binds to more than one type of receptor
Dictionary
Alopecia Baldness absence of hair from skin areas where it is normally present
Anorexia Lack or loss of appetite for food.
Antibiotic A chemical substance produced by a microorganism, which has the capacity to
inhibit the growth of or to kill other microorganism without affecting the host cell. It is use in the
treatment of infectious disease.
Antibody An immunoglobulin that reacts with specific antigen that induce its synthesis and
with similar molecules.
Antigen Any substance capable of inducing (persuade or influence) a specific immune
response and of reacting with the products of response.
Anuria Complete suppression of urine formation by the kidney
Catabolism Any destructive process by which complex substances are converted by living
cells into more simple compounds with release of energy
Catheter A tubular, flexible surgical instrument that is inserted into a cavity of the body to
withdraw or introduce fluid.
Erythema Redness of skin due to congestion of the capillaries
Congenital Present at and existing from the time of birth.
Anaplasia Loss of differentiation of cells and of their orientation to one another and their axial
framework and blood vessels, a characteristic of tumor tissue
Anemia Reduction below normal of the number of erythrocyte, quantity of hemoglobin, or the
volume of peaked red cells in the blood; a symptom of various disease and disorder.
Leukemia A progressive, malignant disease of the blood-forming organs, marked by distorted
proliferation and development of leukocyte and their precursors in the blood and bone marrow
Dementia An organic mental syndrome characterized by a general loss of intellectual abilities
involving impairment of memory, judgment, and abstract thinking as well as change in
personality.
Dyspnea Labored or difficult to breathing. Episode of respiratory distress

Calculation of pediatric dose
- Adult dose
12 Age
year in Age
+

- Adult dose
20
year in Age

- Adult dose
150
pound in children of Weight



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Pharmacology

Fast past metabolism
- In this process drug doesnt metabolize in the systemic circulation other than portal
circulation. A drug goes to portal circulation or hepatic circulation.
- When a drug is absorbed across the GI, it enters the portal circulation before entering the
systemic circulation.
GABA - -amino butyric acid

Anti Microbial Drugs

Antimicrobial drugs are effective in the treatment of infections because of there selective toxicity- the
ability to hill an invading microorganism without harming the host cells.
Therapeutic strategy in treating patients with an infection of unknown origin

Empiric therapy
- Coverage by a combination of antibiotics such as Clindamycin + Gentamycin
- Effective against gram (+) and gram (-) & anaerobes.
Or
- A single broad-spectrum antibiotics such as imipenem / cilastatin



- Receive culture report with sensitivities and take the following strategies

1. If gram positive only than only continue gram positive coverage.
2. If gram negative, only continue gram negative coverage.
3. If anaerobic, only continue anaerobic coverage.
4. If mix then continue initial therapy.


Laboratory method of identification the susceptibility to antibiotics is disk diffusion.
Three type of chemotherapic spectra
A. Narrow spectrum Chemotherapeutic agents acting only on a single or limited group of
microorganisms are said to have a narrow spectrum
For example ionized is only against mycobacterium.
B. Extended spectrum Which act against gram positive & also against a sufficient number of gram
negative bacteria. Ampicillin which act against gram positive and some gram negative bacteria.
C. Broad spectrum Drug such as Tetracycline and Chloramphenicol affect a wide variety of
microbial species and referred to as broad spectrum antibiotic.
Classification of antimicrobial Agents
1. Inhibitor of metabolism Sulfonamide, Trimethoprim
2. Inhibitor of cell wall synthesis -lactum, Vancomycin
3. Inhibitor of protein synthesis Tetracycline, Aminoglycoside, Macrolides, Clindamycin,
Chloramphenicol
4. Inhibitor of nucleic acid function or synthesis Fluoroquinolones, Rifampin

1. Folate Antagonist (inhibitor of metabolism)
Folic acid co-enzymes are required for the synthesis of purines and Pyrimidines (precursor of RNA &
DNA).

Inhibitor of Folate synthesis Mafenide / Sulfacetamide / Sulfamethoxazole / Sulfasalazine /
Sulfisoxazole
Mechanism of action All are sulfonamide and synthetic structural analogs of p-amino benzoic acid
(PABA) and formation of its one carbon carrying co-factor. This deprives the cell of essential co-factors
for Purine, Pyrimidine and amino acid synthesis.
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Then compete with the Dihydrofolate sythetase and prevent the synthesis of bacterial folic acid.

Inhibitor of Folate reduction Pyri-methamine / Trimethoprim
Mechanism of action These inhibit the reduction of dihydrofolate reductase leading to decrease in
the folate coenzymes for purine, Pyrimidine and amino acid synthesis.
Inhibitor of folate synthesis and reduction Cotrimoxazole - Trimethoprim / Sulfamethoxazole
Mechanism of action
Trimethoprim Prevent reduction of Dihydrofolate to Tetrahydrofolate
Sulfamethoxazole Inhibit the incorporation of PABA into folic acid

2. Inhibitor of cell wall synthesis

Penicillin (-Lactum antibiotics) Penicillin-G (Benzyl penicillin) / Penicillin-V (Phenoxy
Methyl Penicillin) / Nafcillin / Oxacillin / Cloxacillin / Dicloxacillin / Ampicillin / Amoxicillin /
Carbencillin / Ticascillin
Mechanism of action The penicillin interfere with the best step of bacterial cell synthesis
(Transpeptidation or Cross linkage) thus exposing the less stable membrane. Cell lysis can occur, and
thus it is bactericidal.

Cephalosporin (-Lactum antibiotics)
- 1
st
generation - Cefazolin, Cephalexin, Cephradin
- 2
nd
generation - Cefaclor, Cefoxitin, Cefuroxime
- 3
rd
generation - Cefixime,Cefoxitin, Ceftriaxone, Cefdinir
- 4
th
generation - Cefepime.
Mechanism of action Most cephalosporins are produce semi synthetically by the chemical attachment
of side chain 7-amino cephalosporanic acid. Same mechanisms of action like penicillins but they tend to
be more resistance to -lactamase then penicillin.

Carbapenems (-Lactum antibiotics) Imipenem / Cilastatin
Mechanism of action Broad spectrum -Lactum antibiotics and penicillinase producing gram positive
and gram negative organism, anaerobes and pseudomonas aeruginosa

Monobactum (-Lactum antibiotics) Az-treonam
Mechanism of action Same as Carbapenems (currently available in the market)

-Lactamase inhibitors Clava-lanic acid / Sulbactum / Tazobactum

Other antibiotics (That affecting the cell wall) Vancomycin / Bacitracin
Mechanism of action Inhibits synthesis of bacterial cell wall phospholipid as well as peptidoglycan
polymerization at a side earlier than that inhibited by the -lactum antibiotics.

3. Protein synthesis inhibitor Can not use in Pregnancy
Main target is bacterial ribosome (50S + 30S) = 70S (Subunit)
In case of Mammalian (60S + 30S) = 80S

Tetracycline Demecocycline / Doxycyline /Minocyline /Tetracycline
Mechanism of action Drug bind to 30s subunit of bacterial ribosome and block the access of the amino
acyl-tRNA to the mRNA ribosome complex at acceptor site, thus inhibiting bacterial protein synthesis.
Aminoglycoside Two amino sugars joined into glycoside linkage to a central hexose (amino
cycitol) nucleus. Amikacin / Gentamicin / Neomycin / Streptomycin / Tobramycin
Mechanism of action Inhibit bacterial protein synthesis to binding separately 30s ribosome subunit,
interfering with assembly of functional ribosomal apparatus thus inhibit the protein synthesis.

Macrolides (Macro-cyclic lactone structure) Azithromycin / Clarithromycin / Erythromycin
Mechanism of action The Macrolides irreversibly bind to 50s subunit of bacterial ribosome, this
inhibiting the translocation step of protein synthesis. Generally considered to be bacteriostatic

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Chloramphenicol Wide range of gram (+) & gram () organism. It is use when no alternative
choice is available.
Mechanism of action The drug binds to the bacterial 50s ribosomal subunit and inhibits protein
synthesis at the peptidyl transferase reaction.
@ Produce bone marrow toxicity

Clindamycin
Mechanism of action The same as that of Macrolides. It is well absorbed by the oral route.

4. Inhibitors of nucleic acid function or synthesis
Fluoroquinolones / Rifampin
@ Quinolones and urinary tract antiseptics

Fluoroquinolones Ciprofloxacin / Norfloxacin / Ofloxacin / Trvafloxacin
Mechanism of action The Fluoroquinolones enter the cell by passive diffusion through water-fluid
protein channels (porins) in the outer membrane. They uniquely inhibit the replication of bacterial DNA
by interfering with the action of DNA gyrase during bacterial growth & reproduction.

Quinolones Nalidixic acid
Mechanism of action Nalidixic acid is a non fluorinated quinolones with the same mechanism of
action that of the fluoroquinolones. It is effective against most of the gram negative bacteria that
commonly cause UTI. It is well absorbed (>90%).

Urinary tract antiseptics Methe-namine / Nitro-fura-toin
Mechanism of action
Methe-namine Must decompose at an acidic P
H
5.5 or less in the urine, thus producing formaldehyde,
which is toxic to most bacteria.
Nitro-fura-toin Inhibit various enzymes and damage DNA activity greater in acidic urine.




Anti Hypertensive Drug
Hypertension: Persistently high arterial blood pressure
Environmental factors causes hypertension, such as
- A stressful life style
- High dietary intake of Na
- Obesity
- Smocking
Anti-hypertensive agent Drug which act against hypertension
1. Diuretics
- increase Na and H O excretion
2
- Decrease cardiac out put and renal blood flow
Furosemide / Torsemide (Loop Diuretics)
Hydrochlorothiazide (Thazide Diuretics)
Triamtrene / Amiloride / Spironolactone (K Sparing Diuretics)
Manitol / Urea (Osmotic Diuretics)

2. - Adrenoreceptor Blockers
- Decrease cardiac out put
- Inhibit release of rennin from kidney
Atenolol / Metoprolol / Propanolol / Timolol

3. ACE inhibitor
- Inhibit Angiotensin Converting enzyme
- Inhibit conversion of Angiotensin I Angiotensin II
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Benzapril / Captopril / Elanapril / Moexipril / Quinapril / Ramipril

4. Angiotensin II Antagonist
- Block Aldosteron secretion
- Produce Vasodilatation
Losertan / Valsartan

5. Ca Channel Blockers
+ +
- Block the inward movement of Ca by binding to L type Calcium channel in the heart &
in smooth muscle of the coronary and peripheral vasculator
Amlodipine / Felodipine / Diltiazem / Verapamil

6. - Adrenergic Blockers
- It causes the relaxation of both arterial & venus smooth muscle
- Lower arterial blood pressure
Doxazosin / Prazosin / Terazosin

7. Vasodilator
Hydralazine / Minoxidil

8. Hypertensive emergency
Sodium nitropruside / Diazoxide / Labetelol

Drug Affecting Blood
1. Platelet inhibitors
- Aspirin Block the thromboxane A synthesis from arachidonic acid in platelets by irreversible
acetylation & cycloxygenase, a key enzyme in prostaglandin and thromboxane A Synthesis.
2
2
- Ticlopidine The drug inhibit the pathway ADP which involved in the binding of platelet to
fibrinogen and to each other
2. Anticoagulants
- Heparin Heparin acts indirectly by binding anti-thrombin III to cause a rapid anti-coagulant
effect.
- Warferin Cumarin anti-coagulant
3. Thrombolytic agent
- The thrombolytic agent act either directly or indirectly to convert Plasminogen plasmin,
which turn cleaves fibrin, thus lysing thrombi.
Alteplase / Sterptokinase / Urokinase
4. Treatment of Bleeding
Protamine sulfate / Vitamin K
5. Treatment of anemia
Cyanocobalamin (Vita B
12
) / Folic acid / iron
6. Treatment of sickle cell anemia
Hydroxyurea


Anti Hyperlipidemic Drugs

Metabolic disorder like: Diabetes mellitus / Hyperthyroidism / Primary biliary cirrhosis

1. Statin Group (HMG-CoA reductase inhibitors)
- Hydroxymethylglutaryl coenzyme A reductase produce Mevalonic acid from HMG-CoA which
turns into Cholesterol but Statin groups hyperlipidemic agent inhibit HMG-CoA to restrict the
formation of cholesterol.
Atorvastatin / Simvastatin / Lovastatin / Fluvastatin / Pravastatin

2. Fibrates
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- Decrease plasma triglycerol level by increasing lipoprotein lipase activity.
Clofibrate / Gemfibrozil

3. Bile acid bindings resins
- Anion exchange resin that binds with negatively charged bile acids and bile salt in the small
intestine
Chlestyramine / Colestipol

4. Niacin(Nicotinic acid)
- A water soluble vitamin strongly inhibit lipolysis in adipose tissue thus no free fatty acid is
formed which is major precursors for triglycerol synthesis
- Niacin causes a decrease in liver triglycerol synthesis


Chemotherapeutic Drugs

Antibiotic - A chemical substance produced by a microorganism, which has the capacity to inhibit the
growth of or to kill other microorganism without affecting the host cell. It is use in the treatment of
infectious disease

Name of bacteria with Disease
Gram (+) Cocci
- Staphylococcus aureus Abscesses / Endocarditis / Pneumonia / Osteomyelitis / Cellulitis
- Streptococcus pneumoniae Pneumonia / Arthritis / Sinusitis / Otitis
- Streptococcus pyrogens Pharyngitis / Otitis media / Sinusitis / Cellulitis
- Streptococcus bovis Endocarditis / Bacteremia

Gram (+) Bacilli
- Bacillus anthracis Pneumonia
- Corynebacterium diptheriae Pharyngitis / Pneumonia
- Colostridium tetani Tetanus
- Colostridium difficile Antibiotic associated colitis

Gram () Cocci
- Moraxella catarrhalis Pneumonia / Sinusitis / Otitis
- Neisseria gonorrhoea
- Neisseria meningitides Meningitis

Gram () Bacilli
- Escherichia coli UTI / Bacteremia
- Pseudomonus aeruginosa UTI & other infections
- Salmonella typhi Typhoid fever / Para Typhoid fever
- Haemophilus influenza Pneumonia / Sinusitis / Otitis media
- Vibrio cholerae Cholera

Acid Fast Bacilli
- Mycobacterium tuberculosis Pulmonary tuberculosis
- Mycobacterium leprae Leprosy

Spirochetes
- Treponeme pallidum Syphilis
- Leptospira Meningitis

Actinomycetes
- Actinomyces israeli Abdominal, thoracic lesion
- Nocardia asteroids Pulmonary lesions / Brain abscess

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Drug use to treat peptic ulcer diseases / Anti-ulcerant




1. H Receptor Blockers
tor antagonist act on H -receptors in the stomach, blood vessels, and
Cemeti nitidine / Femotidine / Nizatidine
. Proton pump inhibitors
ATpase enzyme system of the parietal cell, suppressing secretion of
Om r azole / Pentoprazole
. Prostaglandins analogous
I , Produced by the gastric mucosa, inhibit secretion of HCL and
u
Misopr
. Antimuscarinic agents
increase gastrointestinal motility and secretory activity, Antimuscarinic
Hyo y
. Antacid
acid neutralizing agent present in the stomach
Alu n ydroxide / Sodium bicarbonate
. Mucosal protective
s, known as cytoprotective, have actions that enhance mucosal protection
Colloidal bismuth / Sucralfate

reatment for H. pylori induce ulcer
etracycline / Metronidazole / Clarithromycin
oxycillin + Clarithromycin


Drug affecting the Thyroid

2
- Histamine H
2
recep
2
other sites. These agent completely inhibit gastric acid secretion induce by histamine, or
gastrin.
dine / Ra

2
- It binds to the H
+
/K
+
hydrogen ion into he astric lumen
ep azole (1
t g
st
) / Lansoprazole / Esomepr

3
- Prostaglandins E
2
and
2
stimulate secretion of muc s and bicarbonate
ostol (Has cytoprotective action)

4
- Muscarinic receptor
agent prevent these secretory activity
sc amine / Pirezepine

5
- Act as
mi um hydroxide / Calcium hydroxide / Magnesium h

6
- These compound
mechanisms, thereby preventing mucosal injury, reducing inflammation, and healing existing
ulcers.
T
- Only Proton pump inhibitors
- Antibiotics Amoxycillin / T
- Triple therapy for H. pylori
Lansoprazole + Am
Omeprazole + Metronidazole + Clarithromycin
Pentoprazole + Tetracycline + Amoxycillin


Iodide / Levothyronine / Methimazo xine / Triiodothyronine

Drugs use in Diabetics
le / Propylthiouracil / Thyro


Oral Hypoglycemic agent
ration
amide
de

1. Sulphonyl ureas
- First gene
- Tolbut
- Chlorpropami
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- Secon e
e
de
2. Biguanides
f min (1st generation)
3.
d g neration
- Glipi-zid
- Gilme-peri
- Phen or
- Metformin
- Buformin
- Glucosidase inhibitor
4. Other Anti diabetics


nsulin Prep
lin pre
n
luble crystalline Zinc insulin. It is usually given subcutaneously and
s in with zinc ion in acetate buffer)
ine Hagedorn, is a suspension of crystalline zinc insulin combined
in)
insulin such as 70% isophene + 30% regular, or 50% of each of these are
3. Pro sulin prep
n
r ate buffer thats composed of large

Antifungal drugs
- Acarbose
- Repagli-nide
- Guar gum
- Piogli-tazone
- Nategli-nide
I aration
1. Rapid action insu p
Regular insulin is short-acting so
lowers blood sugar within minutes.
2. Intermediate action insulin prep
n

- Semilente insulin suspension (in ul
- Isophene insulin suspension
Some times called neutral protam
at neutral pH with the positively charge polypeptide, protamine.
- Lente insulin (30% Semilente insulin and 70% ultralente insul
- Insulin combination
Combine human
also available
longed action in
Ult alente insulin is a suspension zinc insulin crystals in acet
particles which are slow to dissolve.

Drugs for subcutaneous and systemic mycoses


ru for superficial mycoses
n infections are called dermatophytes. Common dermatomycoses, such as
in

Antiproto al Drugs

- Amphotericin B
- Flu-conazole
- Flu-cytosine
- Itra-conazole
D gs
Fungi that cause superficial ski
tinea infection, are often referred to as ringworm.
- Clotrimazole
- Econazole
- Geriseofulv
- Miconazole
- Nystatin
zo

hemotherapy of Amebiasis
ne
Che t Malaria
C
- Chloroquine
- Dihydroemeti
- Emetine
mo herapy of
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Che t plasmosis
Che t s

Anti Helmintic Drugs
- Chloro-quine
- Meflo-quine
- Prima-quine
mo herapy of Toxo
- Pyri-methamine
mo herapy of Giardiasi
- Quina-crine

Chemotherapy of Nematodes
ABA of parasites
crotubules of parasite.
Che t odes
Che t des

Antiviral Drug

- Ivermectin: Inhibit G
- Mebendazole: Decrease synthesis of mi
- Thiabendazole
mo herapy of Tremat
- Prazi-quentel
mo herapy of Cesto
- Niclos-amide

Amantadine / Rimantadine / Acyclovir / Ganciclovir / Penciclovir / Indinavir / Ritonavir /
Anti cancer drug / chemotherapeutic agent

Saquinavir / Stavudine / Zidovudine


There are three stages involved to from tumor to neoplastic cells
Neoplastic cells
. Ant metabolites
analogs: Methtrexate Inhibit dihydrofolate reductase.
ptopurine / 6-thioguanine Both inhibit
2. Alkylat
mbucil
stin
3. Ant o
nomycin / Doxorubicin (Inhibit RNA synthesis)
air)
4. Natu
lkaloids (Inhibit function of the microtubules)
5. Others /
tinum coordination complex)

Initiation Promotion Progression
1-2 Days >10 years >1 years

1
- Folic Acid
- Pyrimidine analogs: 5 Fluorouracil Inhibit
- Purine analogs & related inhibitors: 6-merca
novo synthesis of Purine ring & inhibit nucleotide interconversion.
ing agent Alter structure and DNA function by cross linking.
- Nitrogen Mustered: Cyclophosphamide / Melphalan / Chlora
- Alkyl Sulphonate: Busulpfan
- Nitrosuria: Carmustin / Lomu
- Triazenes: Dacarbazine
ibi tic
- Dacti
- Belomycin / Pilomycin (Damage DNA and Prevent rep
ral Products
- Vinka A
Vincristine / Vinblastin
Miscellaneous
- Cisplatin (Pla
- Interferon (Biological response modifier)

- Procarbazine Methyl hydrazine derivatives) (
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