CHEMOTHERAPY DRUGS AND MECANISM

ANTI BACTERIAL DRUGS

S.NO

Drug

Isolate From

Acting On

Type of Activity

Site Of Action

Mechanism

Unwanted Effect

1.

Penicillins (ẞ-lactam antibiotics)

Penicillum

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell wall

Block transpeptidase which is responsible for cross linking of cellwall&activates autolysis(degradative enzymes),binds penicllin binding proteins and inhibit cell wall synthesis

Hypersensitivity (due to degradation Products of Penicillin),skin rashes,fever,Git disturbances)

2

Cephalosporins/ Cephamycins

Cephalosporium fungus/Streptomyces

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell wall

Similarly as Penicillins By inhibiting cell wall synthesis

Hypersensitivity Cefradine-Nephrotoxicity Cefoperazone-Diarrhoea

3

Tetracyclins

-

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell Wall

Inhibit Protein Synthesis by binding to 30s ribosomes-preventing the binding of aminoacyl t-RNA to m-Rna

Git Disturbances, Vit-B complex Deficiency,staining of teeth and hypoplasia and bone deformities due to chelate Ca,hepatotoxic in Pregnant,Vestibular disturbances.

4

Aminoglycosides

-

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell Wall

Binds to 30s &50s subunits and cause misreading the codon message of m-RNA

Idiosyncratic bone marrow depression,pancytopenia Grey baby syndrome in new borns ,hypersensitivity,nausea, Vomiting.

5.

Chloramphenicol

Streptomyces cultures

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell Wall

Binds to 50s subunit and interferes with peptide bond formation& transfer of Peptidechain from  p-site(inhibition of trans peptidation)

Idiosyncratic bone marrow depression,pancytopenia Grey baby syndrome in new borns ,hypersensitivity,nausea, Vomiting.

6.

Macrolides Erythromycin

-

Bacteria

Bacteriostatic & lytic) (Broad Spectrum) Act on gram +ve and  -ve

Cell Wall

Binds to 50 s subunit and inhibit protein synthesis (inhibit translocation)

GIT disturbances, Hypersensitivity.rashes, Fever,transient hearing Disturbances

7.

Sulfonamides

-

Bacteria

Narrow Spectrum and  Bacterio static

Cell wall

Paba antimetabolite inhbit dihydropteroate synthetase also inhibits union of paba and pteridine which conjugate with glutamic acid to form dhf

Nausea,vomiting Mental disturbances, Hepatits,hypersensitivity, Bone marrow depression,crystalluria.

8.

Trimethoprim

-

Bacteria

Narrow Spectrum and  Bacterio static

Cell wall

Inhibits DHF reductase theree by inhibiting the formation of THF which is useful in synthesis of purines

Nausea,vomiting,blood disorders,skin rashes.Megaloblastic anaemia.

9.

Cotrimoxazole

-

Bacteria

(sulphamethoxazole+ Trimethoprim)5:1 Ratio

Cell Wal

-

-

10

Polymixine

-

-

Have high affinity for phospolipids, Components of cell Membranes of bacteria& disrupts their osmotic properties

ANTI- TUBERCULAR DRUGS

1

Isoniazide

-

Inhibit synthesis of Mycolic acid also suppress the formation of DNA&RNA

Fever,haemotological changes,arthritic, vasculitis, Deficiency of pyridoxine, Haemolytic anaemia,decrease the metabolism of antiepileptics phenytoin,ethosuximide, carbamazapine

2.

Rifampicin

-

Inhibit DNa dependent Rna Polymerase

Skin eruptions,fever,git disturb,inducing of metabolizing enzymes and increase the degradation of warfarin,glucocorticoids, Antidiabetics,narcotic analgesics,dapsone and estrogens failure of oral contraceptives.

ANTI LEPROTIC DRUGS

13

Dapsone

Similar to sulphonamide due to chemical similarity inhibition of paba into folic acid

Inflammatory side effects,heamolysis,metha Moglobinaemia,allergic dermatitis,neuropathy.

14.

Clofazamine

-

Act by interfering with template function of DNA

Skin and urine can developreddish colour,lesions of blue black discolouration,nausea, Giddiness,git disturbs,headache

ANTI VIRAL DRUGS

1

Idoxurudine

virus

Structural analogue of thymidine.Compete with it and gets incorporated into DNA so forms faulty DNA-directs synthesis of wrong viral proteins

2

Ayclovir

Preferentially inhibits viral DNA polymerase when phosporylated by viral thymidine kinases

Local inflammation with iv injection

3

Zidovudine

Preferentially inhibits reverse transcriptase of HIV after conversion into triphosphate by series of kinases.

-

4

Nevirapin& Efavirenz

Directly inhibits HIV Reverse transcriptase without the need of  Phosporylation.

5

Ritonavir

Aspartic protease inhibitor.(protease involved in production of structural protein and enzymes of HIV virus)

6

Amantidine

Blocks viral penetration/uncoating

ANTI MALARIAL DRUGS

1

Chloroquine

Being a weak base gets accumulated in lysosome &raises vesicular PH and interferes with degradation of HB.Also prevents formation of hemozoin by forming chloroquine-heme complex

2

Primaquine

It suppresses the mitochondrial functions of plasmodia in exoerythrocytic stages

ANTI FUNGAL DRUGS

1

Metronidazole

In anaerobic environment its nitro group get reduced into nitro radical which exerts cytotoxicity by damaging DNA & other critical biomolecule

2

Emetin

Inhibit protein synthesis of tropozoites by arresting intrabosmal,translocation and t-RNA  AA complex

3

Amphotericin-B

Binds ergosterol,forms membrane pores that disruptes homeostasis.

4

Ketoconazole

Inhibits funal steroid synthesis

5

Gresiofulvin

Interfers with microtubule function disrupts mitosis

6

Flouroquinalones

Inhibit DNA gyrase (Topoisomerase2)

ANTI CANCER/NEOPLASTIC DRUGS

1.

Alkylating Agents

In neutral /alkaline solutions they form quarternary derivative ethylenium cation-reacts with NH2,SH,OH groups and make them unavailable for metabolic reactions. -since they are nucleophiles reacts with DNA bases and inhibit DNA synthesis

2.

Antimetabolites

1)Folic acid analogues-(Methotrexate)--- S-phase specific antimetabolite folic acid analoguethat inhibits DHF reductase. 2)Pyrimidine AnalogueL: 5-Flouro Uracil

GPAT Official Website

http://www.aicte-gpat.in/


IMP DATES :

Registration Start date

Date : 08-03-2013

Registration End date

Date :  08-04-2013

Admit Card download date

Date : 29-04-2013

GPAT 2013 Exam Window

Date : 16-05-2013 to 18-05-2013

GPAT Result declaration

Date : 31-05-2013

Print out of Score Cards

From : 31-05-2013 - 30-06-2013

GPAT & NIPER PREPARATION PLAN

GPAT- PREPARATION:

1.When you start preparation of gpat and niper. First of all give importance to the Gpat, because the preparation strategy is different for gpat and niper. Where as Gpat concentrate on subject knowledge deeply and it is some what time taking to answer the questions when compare to the Niper in which concentrate only on basics of subject especially in organic and stereo chemistry and analytical chemistry.

2.And also when you qualified in gpat then only you will be eligible for Niper.

3.First divide all subjects from simple to difficulty and according to their weight age in entrance. 4.According to my opinion I will give an idea

First start with  order 1.Pharmacognosy

                                    2.Pharmacology

                                    3.Analysis

                                    4.Pharmaceutical calculations

                                    5.Pharmaceutical Jurisprudence

                                    6.Bio chemistry, Microbilogy,Bio technology

                                    7.Pharmaceutics- physical pharmacy

                                                                 Unit operations

                                                                  Bio pharmaceutics

                                                                 Dispensing and clinical pharmacy

                                    8.Medicinal Chemistry (if u can study comparatively with pharmacology otherwise give last preference.

Follow this order I think it is easy for you.

5. a)When you start preparation with pharmacognosy. First you should be concentrate on lecturing of     lecturer. It helps to remember easy and can’t easily forget.

    b) Prepare class running notes by simultaneous listening and note the important points and differences and note down the your doubts separately and ask later class finishing to your lecturer.

  

    c) After class college time it is better to revise on class notes and note the bits which are asked in    previous exams.

    d) Before class starting once you check and observe the notes of yesterday.

For every subject these steps are must be do then there is no tough feel in your preparation .otherwise somewhat difficult you feel.

GPAT Question

1. A patient hypersensitive to metronidazole is suffering from pseudomembranous colitis; what would be you suggest for P colitis?
A) Doxycycline
B) Vancomycin
C) Clindamycin
D) Chloramphenicol

2. Determine the correctness or otherwise of the following Assertion [a] and the Reason [r] -

Assertion (a) : Metronidazole is selectively active against aerobic organism
Reason (r) : Only aerobes reduce it to generate the reactive nitro radicals
(A) Both (a) and (r) are true, and (r) is a correct reason for (a)
(B) Both (a) and (r) are true, and (r) is NOT the correct reason for (a)
(C) (a) is true but (r) is false
(D) Both (a) and (r) are false

3.‎___________________ is a lactam antibiotic having an oxepenam ring

A) SALBACTUM
B) PENICILLIN
C) CLAVULANIC ACID
D) CEPHALOSPORIN

4.What kind of substances can’t permeate membranes by passive diffusion?

a) Lipid-soluble
b) Non-ionized substances
c) Hydrophobic substances
d) Hydrophilic substances

5. Class 100 area is referred to

A-Manufacturing area
B-Aseptic area
C-Clean room
D-Ware house

6.Which one of the following therapeutic classes has been proved clinically as a first

line therapy for heart failure and has shown decreased hospitalization, improved
symptoms and delayed disease progression?
(A) Cardiac glycosides (B) ACE Inhibitors (ACEIs)
(C) Renin Antagonists (D) Nitrites

7.Which is true for volhard s method of end point determination?

A) Argentometric determination of chlorides
B) Requires acidic solutionto prevent precipitation of metal hydroxides
C) Form ppt of AgSCN
D) All of the above

8.in the preparation of small pox vaccine,the drying process used is

a) freez drying
b) drum drying
c) spray drying
d)vaccum drying

9. -In nail polish, following polymer is used as a film-former

A-Nitrocellulose
B-Polylactic acid
C-Hydroxypropyl methylcellulose
D-Cellulose acetate phthalate

10.Standards for patent and proprietary medicines is covered under _______ schedule.

(a) U (b) V (c) W (d) X

11.Recent amendments in Patent Act 1970 were done in

A) 2002
B) 1999
C) 2005
D) 2009

12.Class 100 area is referred to

A-Manufacturing area
B-Aseptic area
C-Clean room
D-Ware house

13.An o/w emulsion is stabilized with sodium stearate; upon addition of calcium chloride lead to formation of w/o emulsion; the phenomenon is known as

A) Breaking of emulsion
B) Creaming of emulsion
C) Phase inversion
D) Coalescence

14.Select the true statement for partition coefficient

A) Ratio of unionized lipophilic and hydrophilic drug concentration
B) Ratio of ionized lipophilic and hydrophilic drug concentration
C) Ratio of unionized hydrophilic and lipophilic drug concentration
D) Ratio of ionized hydrophilic and lipohilic drug concentration

15.Indicate the HPLC detector that is most sensitive to change in temperature

A-PDA detector
B-Refractive Index detector
C-Electrochemical detector
D-Fluorescence detector

16.A metabolite obtained from Aspergillus terreus that can bind very tightly to HMG CoA reductase enzyme is

A-Fluvastatin
B-Cerivastatin
C-Lovastatin
D-Somatostatin

17.Select the formula to calculate steady state concentration follow I/V infusion model....

A) Css= Infusion rate/Clearance
B) Css= Clearance/ Infusion rate
C) Css= Infusion rate x Clearance
D) Css= Infusion rate + Clearance

18.Fourth generation fluoroquinolone is

A) Ciprofloxacin
B) Sparfloxacin
C) Moxifloxacin
D) Ofloxacin

19.Mohr s method of end point detrmination involves

A) Determination of chlorides with the formation of AgCl
B) Determination of flourides with the formation of AgF
C) Determination of chlorides with the formation of NaCl
D) Determination of halides with the formation of AgCl

20.Which is true for volhard s method of end point determination?

A) Argentometric determination of chlorides
B) Requires acidic solutionto prevent precipitation of metal hydroxides
C) Form ppt of AgSCN
D) All of the above

21.Pharmacokinetics is:

a) The study of biological and therapeutic effects of drugs
b) The study of absorption, distribution, metabolism and excretion of drugs
c) The study of mechanisms of drug action
d) The study of methods of new drug development

22.A test solution used to check completeness of extraction process is

(a) hydrogen sulphide (b) mercuric potassium iodide
(c) silver nitrate (d) mercuric oxide

23.All of the following anticancer drugs are correctly matched with their mechanism of action EXCEPT :

a. Lomustine :Alkylating agent
b. Bleomycin : Antimetabolite
c. Paclitaxel : Antimitotic agent
d. Aminoglutethemide : Steroidogenic inhibitors
e. Melphalan : Alkylating agent

24.Which effect may lead to toxic reactions when a drug is taken continuously or repeatedly?

a) Refractoriness
b) Cumulative effect
c) Tolerance
d) Tachyphylaxis

25.An example of N-glycoside is

A-Adenosine
B-Sinigrin
C-Rhein-8-glucoside
D-Aloin

E- mail me ans at : pharmaexperts01@gmail.com

10 Weirdest Diseases

10 Weirdest Diseases

Blue-skinned people? Vampire Syndrome? When we were kids, we couldn't hear enough about illnesses, horrid medical conditions or weird diseases. Not much has changed since then. When we hear about an outbreak of a flesh-eating bacteria or some other rare sickness, we're fascinated. But now we're also terrified. Some rare diseases are very real and if you catch them, you're a goner. Here's a list with 10 of the most rare diseases out there.

Elephantiasis: grossly enlarged members

Lymphatic filariasis, also known as elephantiasis, is best known from dramatic photos of people with grossly enlarged or swollen arms and legs. 

The disease is caused by parasitic worms, including Wuchereria bancrofti, Brugia malayi, and B. timori, all transmitted by mosquitoes. Lymphatic filariasis currently affects 120 million people worldwide, and 40 million of these people are seriously diseased. When an infected female mosquito bites a person, she may inject the worm larvae, called microfilariae, into the blood. The microfilariae reproduce and spread throughout the bloodstream, where they can live for many years. Often disease symptoms do not appear until years after infection. As the parasites accumulate in the blood vessels, they can restrict circulation and cause fluid to build up in surrounding tissues. The most common, visible signs of infection are excessively enlarged arms, legs, genitalia, and breasts.

Progeria: the 80-Year-Old Children

Progeria is caused by a single tiny defect in a child's genetic code, but it has devastating and life-changing consequences. 

On average, a child born with this disease will be dead by the age of 13. As they see their bodies fast forward through the normal process of ageing they develop striking physical symptoms, often including premature baldness, heart disease, thinning bones and arthritis. Progeria is extremely rare, there are only around 48 people living with it in the whole world. However, there is a family that has five children with the disease.

Werewolf Syndrome: the wolf people

When two year-old Abys DeJesus grew dark, hairy patches on her face, doctors said she has a condition known as Human Werewolf Syndrome. The disease is called werewolf syndrome because people with it look like werewolves - except without the sharp teeth and claws. 

In Mexico, a large family of men had hair that covered their faces and upper bodies. Two brothers were even offered a part in the X-Files but they turned down the offer.

Blue Skin Disorder: the blue people

A large family simply known as the "blue people" lived in the hills around Troublesome Creek in Kentucky until the 1960s. They were the blue Fugates. Most of them lived past the age of 80, with no serious illness - just blue skin. The trait was passed on from generation to generation. People with this condition have blue, plum, indigo or almost purple skin. (Source)

Pica: the urge to eat non-food substances

People diagnosed with Pica have an insatiable urge to eat non-food substances like dirt, paper, glue and clay. Though it is believed to be linked with mineral deficiency, health experts have found no real cause and no cure for this disorder.

Vampire Disease: pain from the sun

There are people out there who go to great lengths to avoid the sun. If they are caught in the sun, their skin will blister. Some of them have pain and blistering as soon as the sun touches their skin. Ok, so they're not actually vampires. They don't drink blood and sleep in coffins, but they do suffer from a rare disease that has vampire-like symptoms.

Alice in Wonderland syndrome: time, space and body image are distorted

Alice in Wonderland syndrome (AIWS), or micropsia, is a disorienting neurological condition which affects human visual perception. Subjects perceive humans, parts of humans, animals, and inanimate objects as substantially smaller than in reality. Generally, the object perceived appears far away or extremely close at the same time. For example, a family pet, such as a dog, may appear the size of a mouse, or a normal car may look shrunk to scale. This leads to another name for the condition, Lilliput sight or Lilliputian hallucinations, named after the small people in Jonathan Swift's Gulliver's Travels. The condition is in terms of perception only; the mechanics of the eye are not affected, only the brain's interpretation of information passed from the eyes.

Blaschko's lines: strange stripes all over the body

Blaschko's lines are an extremely rare and unexplained phenomenon of human anatomy first presented in 1901 by German dermatologist Alfred Blaschko. Neither a specific disease nor a predictable symptom of a disease, Blaschko's lines are an invisible pattern built into human DNA. Many inherited and acquired diseases of the skin or mucosa manifest themselves according to these patterns, creating the visual appearance of stripes. The cause of the stripes is thought to result from mosaicism; they do not correspond to nervous, muscular, or lymphatic systems. What makes them more remarkable is that they correspond quite closely from patient to patient, usually forming a "V" shape over the spine and "S" shapes over the chest, stomach, and sides.

Walking Corpse Syndrome: they believe to have died

It is a syndrome of mental depression and suicidal tendencies, in which the patient complains of having lost everything: possessions, part of or entire body, often believing that he or she has died and is a walking corpse. This delusion is usually expanded to the degree that the patient might claim that he can smell his own rotting flesh and feel worms crawling through his skin. The latter phenomenon is a recurring experience of people chronically deprived of sleep or suffering amphetamine/cocaine psychosis. Paradoxically, being "dead" often gives the patient the nation of being immortal.

Jumping frenchman disorder: weird reflexes

The main characteristic is that patients are extremely startled by an unexpected noise or sight. It's not just twitching when someone sneaks up behind you. Patients with this disorder flail their arms, cry out and repeat words. First identified in some of Maine's lumberjacks of French-Canadian origin, the odd reflex has been identified in other parts of the world, too.

IF U THINK UR LIFES GETTING NECROSED,UR DREAMS INFLAMED,UR THOUTHTS THROMBOSED,THEN TRY THIS OUT.SPREAD D NEOPLASIA OF LOVE AROUND U.