1. 2 Side effect: -dependence -Photosensitivity -Electrolyte imbalance( hypertension and hypokalemia) -Colonic atony. -Colonic melanoma. *Contraindication:

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Presentation transcript:

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2 ****Side effect: -dependence -Photosensitivity -Electrolyte imbalance( hypertension and hypokalemia) -Colonic atony. -Colonic melanoma. *****Contraindication: Pregnancy Breast feeding women. Children under the age of 12 years old. *****Drug interaction: Other laxative. Cardiac glycoside. Diuretic steroid. Antibiotics.

3 ***Pharmacodynamics and pharmacokinetics. Stomach: partial hydrolysis for O-glycoside. (so large bulk dose is used) Small intestine: Absorption for non-polar; smaller Mwt. Aglycon. Colon: Activation by normal flora for both O- and C- glycoside

4 *** Physicochemical properties, -Combined form are soluble in aqueous alcohol and chlorinated solvent. -Free aglycone is soluble in chlorinated solvent and alcohols. -Detection for free anthraquinone is done using borntrager’s test. -Detection for combined anthraquinone and dimmer is done using modified borntrager’s test which uses: -acid and heat to free O-glycoside. -Acid, heat and oxidizing agent to oxidatively cleave C- glycosides. -Heat and oxidizing agent to oxidatively cleave C- glycosides -Quantitation: done on the principle of borntragers test, usually using Mg acetate.

5 *******Natural source for anthraquinone glycosides: ***Senna: -Botanical source: Leaveas and legumes of: Cassia acutifolia fam. Fabaceae Cassia angustifolia -Chemical structure -Pharmacological activity:

6 Sennoside A and B: -Dianthrone; Bidesmoside, O-glycosides at C-8 and C-8’, -glucose is the sugar part in β- position. -C-3 and C-3’ : COOH group. -C-10 and C-10’ chiral centre where C- linkage -between anthraquinone dimmer. - Both are diastereomer for each other.

7

8 ***Cascara: -Botanical source: Rhamnus purshiana Rhamnaceae -Chemical structure: -Pharmacological activity:

9 R:-CH 2 OH Cascaroside A& B: -A in β-configuration. -B in α-configuration R:-CH 3 : Cascaroside C &D: -C in β-configuration. -D in α-configuration : R

10 Cascaroside A and B: -monoanthrone; Bidesmoside, O-glycosides at C-8 and C- glycoside at C-10. -glucose is the sugar part in β- position at C-8. -C-3 : CH 2 OH group. -C-10 chiral centre where C- linkage of another Glucose unit. - Both are enantiomer (mirror image isomer).