Business

Dr.Khan

Fill in the blank:

1. Widely used salicylate is Aspirin.

2. Mefenamic acid and meclofeamate are inhibtors of prostaglandins synthesis.

3. Proxicam advantage: Advantage: long half-life, which permits the administration of a single daily dose. It may be better tolerated and more potent than aspirin and indomethacin.

4. Nalorphine is a morophine Antagonist

5. Etorphine is prepared The prototype of 6, 14-endo- ethenotetrahydrooripavines, is 5000-10,000 times more potent than morphine. Its great lipopilicity in comparison to morphine. Accounts for its greater ease in penetrating BBB resulting in the enormous activity.Is used mainly in veterinary practice to immobilize large animals eg: elephants.

6. Isomer of iburphone is more active (S)-Enantiomers like Flurbiprofen.

7 . Which are similar to morphine but less dependent liability Methadone

SAR:

1. Morophine :

Structure- Activity Relationship in Morphine and Its Derivatives

* The following structure- activity relationship has been observed in morphine and its derivatives.

* The alteration of phenolic OH morphine or related compounds by etherification or esterification increases convulsant action and decreases morphine like effects, e.g., Codeine, a methyl ether, has 1/7th potency of morphine and is used as an antitussive agent, whereas the diacetylmorphine derivative i.e., heroin, has twice the potency of morphine.

* A change of the alcoholic OH group, e.g., by oxidation to a keto group or by substitution with halogen or hydrogen increases toxicity and convulsant action but also increases analgesic action.

* A shift in the position of alcoholic hydroxyl group from position 6 to position 8 results in the decrease of pharmacologic action.

* The opening of the ether bridge and substitution in aromatic ring decreases pharmacological activity.

* The saturation of 7, 8- double bond in morphine and codeine by catalytic reduction gives dihydro compounds that exhibit increased...