Belladonna alkaloids: esters of tropic acid and tropine Parenteral preparations( quaternary derivatives) are more potent than the parent compounds Therapeutic uses: mydriatic(扩瞳药 antispasmodic(解痉药) Side effects: dryness of mouth; urine retention(k 潴留); blurredⅵ nsIon(视力模糊); constipation(便 秘) Atropine is an antidote(解毒药) to poisoning by organophosphorus pesticides(有机磷农药
• Belladonna Alkaloids: esters of tropic acid and tropine. • Parenteral preparations (quaternary derivatives) are more potent than the parent compounds. • Therapeutic uses: mydriatic ( 扩瞳药 ) ; antispasmodic (解痉药). • Side effects: dryness of mouth; urine retention(尿 潴留); blurred vision (视力模糊); constipation (便 秘). • Atropine is an antidote (解毒药) to poisoning by organophosphorus pesticides (有机磷农药)
Atropine sulfate 8CH3 H OH H2So4·H2O 2 a-(Hydroxymethyl)benzeneacetic acid 3-endo ) -8-methyl 8-azabicyclo 3. 2. 1 ]oct-3-yl ester sulphate monohydrate
Atropine Sulfate - (Hydroxymethyl)benzeneacetic acid (3-endo)-8-methyl- 8- azabicyclo[3.2.1]oct-3-yl ester sulphate monohydrate
Atropine Atropine is(±)- hyoscyamine(莨菪碱), an ester of the tropic acid and tropine Vitali reaction for tropic acid .Natural product is(-)-hyoscyamine Atropine results from the base-catalyzed racemization of the chiral carbon of tropic acid, which occurs during isolation process LCH3 OH Antimuscarinic effect SO-Hyoscyamine Atropine >>R(+)-Hyoscyamine
Atropine •Atropine is (+)-hyoscyamine (莨菪碱), an ester of the tropic acid and tropine. •Vitali reaction for tropic acid •Natural product is (-)-hyoscyamine. •Antimuscarinic effect: S(-)-Hyoscyamine > Atropine >> R(+)-Hyoscyamine Atropine results from the base-catalyzed racemization of the chiral carbon of tropic acid, which occurs during isolation process
Anisodamine hydrobromide (氢溴酸山莨菪碱) Hac HQ HBr CH2OH a(s)-(Hydroxymethyl)benzeneacetic acid 6B- hydroxy-lah, 5ah-8-methy l-8-azabicyclo 3.2.11 oct-3 a-yl ester hydrobromide
Anisodanmine hydrobromide (氢溴酸山莨菪碱) N H3C H O O HO CH2OH * HBr (S)- (Hydroxymethyl)benzeneacetic acid 6β- hydroxy-1αH, 5αH-8-methyl-8- azabicyclo[3.2.1] oct-3 α -yl ester hydrobromide
Synthetic muscarinic antagonists Administered orally or by parenteral routes Therapeutic Use: Treatment of gi disorder(in combination with librium(利眠宁), a tranquilizer) Contraindicated(禁忌) in glaucoma(青光眼)
Synthetic Muscarinic antagonists • Administered orally or by parenteral routes • Therapeutic Use: Treatment of GI disorder (in combination with Librium (利眠宁), a tranquilizer) • Contraindicated (禁忌) in glaucoma (青光眼)