Antiparkinson activity

Introduction of branching in the side chain is apparently consistent with retention of the antiparkinson activity. Bro-mination of propiophenone gives the brominated ketone, 33. Dis-... 

Mechanism of Action Aweakanticholinergicthat exhibits competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which restores balance. Therapeutic Effect Antiparkinson activity... 

The antiparkinsonism activity of a series of N- (n-propyl)norapomorphine diesters has been tabulated.43 The stability of apomorphine in solutions contain-... 

Ravina, E., Montands, J. M., Seco, M. C.. Callcja, J. M., and Zar/osa, M.. Synthesis and potential antiparkinsonism activity of some tcrliaiy substituted P-aminoalcohols containing a bcnzofiiran nucleus, Chim. Ther, 8. 182, 197.3. 

The first group of phenothiazine derivatives to be introduced into clinical practice were also found to have some antiParkinson activity, and like atropine they possess significant anticholinergic, antihistaminic, sedative, and local anaesthetic properties [400]. Four of these fenethazine (14), promethazine (Phenergan, 15), diethazine (Diparcol, 16), and ethopropazine (Parsidol, 17), still find clinical use but the occurrence of agranulocytic reactions tends to preclude them from long-term application. Ethopropazine... 

As a class, these agents tend to be devoid of antihistaminic activity, while they retain some of the sedative and antiparkinson... 

Discuss important preadministration and ongoing assessment activities the nurse should perform on the patient taking antiparkinsonism drugs. 

Amantadine is less effective than levodopa in the treatment of Fhrkinson s disease but more effective than die anticholinergics. Amantadine may be given alone or in combination witii an antiparkinsonism drug witii anticholinergic activity. Amantadine is also used as an antiviral drug (see Chap. 14). 

Frequently seen adverse reactions to dragp with anticholinergic activity include dry mouth, blurred vision, dizziness, mild nausea, and nervousness. These may become less pronounced as therapy progresses. Other adverse reactions may include skin rash, urticaria (hives), urinary retention, dysuria, tachycardia, muscle weakness, disorientation, and confusion. If any of these reactions are severe, the drug may be discontinued for several days and restarted at a lower dosage, or a different antiparkinsonism drag may be prescribed. 

Mechanism of Action An antiparkinson agent that inhibits the enzyme, catechobO-methyltransferase (COMT), potentiating dopamine activity and increasing the duration of action of levodopa. Therapeutic Effect Decreases signs and symptoms of Parkinson s disease. 

Secondly ergot derivatives which reveal a clearcut agonistic activity on prolactin secretion and as antiparkinson agents (20) were inactive on the cyclase. Surprisingly, lisuride and lergotrile were found to be weak antagonists of dopamine stimulated cAMP accumulation, but they could also antagonize the cAMP production stimulated by isoproterenol as... 

Several of the compound types in this chapter have useful biological activities. This is not unexpected since many of those compounds which are effective in the modification of responses to bioamines are themselves organic bases. Quinelorane (114) which is a potent dopamine (D2) agonist has been patented as an antihypertensive and antiparkinsonism agent <85USP4501890>. 

AMANTADINE is used to treat Parkinson s disease as well as having antiviral activity. It has been included in the antiparkinson s drugs section ... 

Benzimidazoles possess important pharmacological activities such as antimicrobial, antifungal, antiparkinson, anticancer, and antibiotic. The one-pot regioselec-tive synthesis of these compounds has been performed by taking a heteroaromatic amine and/or 1,2-phenylenediamine with 2-mercaptoacetic acid and an aromatic aldehyde in ionic liquids, namely, l-butyl-3-methylimidazolium trifluoroborate ([bmim][BF ]) and l-methoxyethyl-3-methylimidazolium trifluoroacetate ([MOEMIM][TFA]). The reaction has been carried out under nitrogen atmosphere (Figs. 12.7, 12.8) [6]. Consideration of the yields of compounds revealed that [MOEMIM][TFA] is a better reaction media in comparison to [bmim][BF ]. 

Parkinsonism is due to an imbalance between DA and ACh activity in the nigrostriatal trad. Drugs attempt to restore this balance either by Increasing DA or decreasing ACh levels. Figure IV-1-8 illustrates the CNS sites targeted in antiParkinsonism therapy. 

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