Thursday, 17 May 2012

some important drugs and their mechanism of action


some important drugs and their mechanism of action


         Drug                                                             mechanism of action
Allopurinol                                   inhibits the enzyme xanthine oxidase, involved in the                                                                   synthesis of   Uric acid
Antipsychotics:                           acts by blocking dopamine receptors.
Aspirin                                          inhibits enzyme cyclooxygenase and prevents synthesis of                                                               prostaglandins
Acetazolamide                             inhibits carbonic anhydrase used as diuretics
Aminoglycosides                         binds to 30 S ribosome and inhibit protein synthesis.
Acyclovir                                    incorporated in to viral DNA and inhibits viral replication.
Amantadine                                inhibits viral attachment and uncoating
Benzodiazepines                      act on benzodiazepines receptors and facilitate the effect of GABA.
Cimetidine                                  blocks H2 receptors.
Chloramphenicol  
Tetracycline’s, erythromycin        bind to 50 S and inhibit protein synthesis.
Griseofulvin                               acts as anti- fungal interferes with mitotic spindle structure
Isoniazid                                    inhibits the synthesis of mycolic acid, imp. Part of cell wall of                                                             mycobacterium
Nalidixic acid                             prevents DNA synthesis
Warfarin                                    antagonize the action of vitamin K
Primethamine                           block folic acid production by acting on dihydrofolate reductase
Penicillin                                    acts on cell wall
Sulfinpyrazole and probenecid     block uric acid reabsorbtion at PCT
Sodium valproate                        inhibits the enzyme GABA transaminase…thus increase the action                                                     of GABA
Spironolactone                           inhibits the action of aldosterone
Vinca alkaloids                             bind to tubulin fibers and inhibit mitosis
Zidovudine                                  inhibits the enzyme reverse transcriptase and inhibits the                                                                  synthesis of viral DNA
Dapsone                                    inhibition of PABA incorporation into folic acid.
Polyene class;                            acts as anti-fungal and attach to ergosterol n fungal cell wall
Terbinafine                                competitive inhibitor of squalene epoxidase acts as anti-fungal
Metronidazole                           cytotoxic in nature and cause damage to DNA
Mebendazloe                             acts on β- tubulin of parasite, similar mechanisms for class azoles.

HERBAL DRUGS that are used in diff. pathological conditions:


HERBAL DRUGS that are used in diff. pathological conditions:


1.Liquorice - anti-ulcer
2.Ipecac - emetic
3.Hyoscine, Cannabinoids - anti-emetic
4.Senna, Cascara, Castor oil - treatment of constipation
5.Gum guggul - anti-rheumatic
6.Colchicum - Anti-gout
7.Guggul lipids, Garlic, Oats - Anti-atherosclerotic
8.Ephedra, Gingkoside B, Theophylline - Anti -asthmatic
9.Vinca, Taxanes, Podophyllotoxins - Anti-cancer
10.Artemesinin derivatives - Anti-malarial

uses of Magnesium Sulphate in diff. routes of administration:


uses of Magnesium Sulphate in diff. routes of administration:


Oral - Cathertic
IV - Sedative & Hypnotic
Topical - Wound healing

SPECIFIC ANTIDOTES FOR CERTAIN DRUGS:


SPECIFIC ANTIDOTES FOR CERTAIN DRUGS:


    DRUG                               ANTIDOTE
     1. Paracetamol              --   N-acetyl cysteine
     2. Atropine                    --   Physostigmine, Neostigmine
     3. Organophosphates   --   Atropine, Prolidoxime
     4. Barbiturates              --   Sodium bicarbonate
     5. Benzodiazipines         --   Flumagenil
     6. Amphetamine            --   Ammonium chloride
     7. Opioids                      --   Naloxone
     8. Digoxin                      --   Digibind
     9. Heparin                     --   Protamine sulphate
   10. Warfarin                    --   Vit. K
   11. Beta blockers             --   Glucagon
   12. Carbon monoxide      --   100% oxygen

alkylating agents in chemotherapy


alkylating agents in chemotherapy


Alkylating agents in cancer therapy:
Nitrogen mustards          cyclophosphamide, estramustine, melphalan, chlorambucil
Nitrosoureas                     chloroethylnitrosourea, lomustine, carmustine
Busulfan
Others                                 thiotepa, treosulfan
Platinum comp’s               cisplatin, carboplatin, oxaliplatin
Dacarbazine ( prodrug )
Temozolimide   
                     
Harmful:
Lomustine                         delayed, cumulative myelotoxicity
Cisplatin                                low myelotoxicity
Carboplatin                           high myelotoxicity
Cyclophosphamide             haemorrhagic cystitis   (ifosfamide)
Acrolein
Beneficial:
Estramustine                       prostate cancer
Busulfan                               chronic granulocytic leukemia
Nitrosoureas                      tumors of brain and meanings
Cisplatin                               germ cell tumor
Temozolimide                    malignant glioma

Some important Drugs and its side effects:


Some important Drugs and its side effects:


Some important Drugs and its side effects:
Grey Baby Syndrome- Chloramphenicol
 Pin Point Pupil-Morphine
Reyes Syndrome- Aspirin
Urine Coloration- Rifampicin
Frontal Headache- Indomethacin
Captopril-Persistent dry cough
Bleomycin-Pulmonary fibrosis
 Vancomycin- Red man syndrome
Nicotinic acid- Flush
Steven Johnsons syndrome- Allopurinol
sulphonamides-kernicterus
 aminoglycosides-ototoxicity
discoloration of teeth-tetracycline
doxorubicin & duanorubucin- cardiomyopathy.
 chloroquine- cardiotixicity
 doxycycline- esophageal ulceration
vincristine & vinblastine- neuropathy
cyclophosphamide- alopecia
cimetidine & spironolactone- gynaecomastia


Effects of drugs during pregnancy on fetus
Antiepileptics- neuraltube defect
 Warfarin- cleft palate
 thalidomide- phocomalia
alcohol- cranial bone formation impairment


ANTIDOTES
benzodiazepine- flumazenil
 paracetamol- N-acetyl cysteine
 Morphine- naloxone
 nitrites- methylene blue
 organophosphorus compd.- DAM, PAM, Atropine
Atropine- Physostigmine
lead- BAL
cyanide- edetate+amyl nitrite

Some important drugs and its mechanism…

1. Nalidixic Acid-Prevent DNA synthesis
 2. Dapsone-Folic acid synthesis inhibitor
3. Vinca alkaloid-Mitotic Spindle formation prevention
4. anthracycline-Intercalation of DNA
5. Methotraxate- Folic acid reductase inhibitor.
 6. Warfarin-Vit k antagonist
 7. Zidovudine- Inhibits the enzyme reverse transcriptase, preventing DNA replication
8. Metronidazole- disruption of helical structure of DNA
9. Tetracycline- Inhibits Protein synthesis by acting on 30 S unit of ribosome
10. Erythromycin- Inhibits Protein synthesis by acting on 50 S unit of ribosome
 11. Chloroquine- Binds and alters properties of microbial and fungal DNA
 12. Diazepam- GABA facilitator
 13. Acetazolamide- Carbonic anhydrase inhibitor
14. Allopurinol- Xanthine oxidase inhibitor, inhibitor of uric acid
15. Fluconalzole- P450 enzyme 14α-demethylase Inhibitor
16. Salbutamol-Beta 2 receptor agonist
17. Tolnaftate- Inhibit squalene epoxidase which is necessary for ergosteral syns of fungal cell wall
18. Griesofulvin-inhibits fungal cell wall activity
 19. Chloramphenicol-Inhibition of Protein syntheses
 20. Levodopa- Replenish Brain deleted dopamine

Named reactions –to be studied for gpat and niper


Named reactions –to be studied for gpat and niper


Acetoacetic Ester Synthesis
Acyloin Condensation
Aldol Addition + Aldol Condensation
Appel Reaction
Arbuzov Reaction = Michaelis-Arbuzov Reaction
Arndt-Eistert Synthesis
Azo Coupling
Baeyer-Villiger Oxidation
Balz-Schiemann Reaction = Schiemann Reaction
Bamford-Stevens Reaction
Barton Decarboxylation
Barton-McCombie Reaction (Barton Desoxygenation)
Baylis-Hillman Reaction
Beckmann Rearrangement
Benzilic Acid Rearrangement
Benzoin Condensation
Bergman Cyclization
Birch Reduction
Bouveault-Blanc Reduction
Buchwald-Hartwig Cross Coupling Reaction
Cadiot-Chodkiewicz Coupling
Cannizzaro Reaction
Chugaev Reaction
Claisen Condensation
Claisen Rearrangement
Clemmensen Reduction
Cope Elimination
Cope Rearrangement
Corey-Seebach Reaction
Criegee Reaction
Curtius Rearrangement
Delépine Reaction
De Mayo Reaction
Dess-Martin Oxidation
Diazotisation and Azo Coupling
Dieckmann Condensation
Diels-Alder Reaction
Di-ð-Methane Rearrangement
Dötz Reaction
Eglinton Reaction
Ene Reaction = Alder-Ene Reaction
Jacobsen Epoxidation
Ester Pyrolysis
Favorskii Reaction
Finkelstein Reaction
Friedel-Crafts Acylation
Friedel-Crafts Alkylation
Gabriel Synthesis
Gattermann-Koch Reaction
Glaser Coupling and Hay Coupling
Grignard Reaction
Grob Fragmentation
Grubbs Olefin Metathesis
Haloform Reaction
Heck Reaction
Hell-Volhard-Zelinsky Reaction
Henry Reaktion
Hofmann Elimination
Hofmann's Rule
Horner-Wadsworth-Emmons Reaction
Hunsdiecker Reaction
Hydroboration
Ireland-Claisen Rearrangement
Knoevenagel Condensation
Kolbe Reaction
Kolbe-Schmitt Reaction
Kumada–Negishi Coupling
Leuckart–Wallach (Leuckart) Reaction
Malonic Ester Synthesis
Mannich Reaction
Markovnikov's Rule
McMurry Reaction
Meerwein-Ponndorf-Verley Reduction
Michael Addition
Mitsunobu Reaction
Mukaiyama Aldol Addition
Negishi Coupling
Norrish-Type I and II
Nozaki-Hiyama Coupling
Nucleophilic Substitution (SN1 / SN2)
Oppenauer Oxidation
Oxy-Cope Rearrangement
Paterno-Büchi Reaction
Pauson-Khand Reaction
Perkin Reaction
Peterson Olefination
Pinacol Coupling Reaction
Pinacol Rearrangement
Prilezhaev Epoxidation
Reformatsky Reaction
Ritter Reaction
Robinson Annulation
Rosenmund Reduction
Sakurai Reaction (Hosomi Sakurai)
Sandmeyer Reaction
Sanger’s Reagent
Saytzeff's Rule
Schiemann Reaction
Schmidt Reaction
Schotten-Baumann Reaction
Sharpless Epoxidation and Dihydroxylation
Simmons-Smith Reaction
Sonogashira Coupling
Staudinger Reaction
Stille Coupling
Strecker Synthesis
Suzuki Coupling
Swern Oxidation
Tebbe Olefination
Thorpe Reaction
Tishhenko Reaction
Ullmann Reaction
Vilsmeier Reaction
Wacker-Tsuji Oxidation
Willgerodt-Kindler Reaction
Williamson Synthesis
Wittig Olefination
Wittig Rearrangement
Wittig-Horner Reaction
Wohl-Ziegler Reaction
Wolff Rearrangement
Wolff-Kishner Reduction
Wurtz Reaction
Wurtz-Fittig Reaction