The post DIMENHYDRINATE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>Diphenhydramine (53-55.5%) + 8-Chlorotheophylline (44-47%)
2-benzhydryloxy-N,N-dimethylethanamine;8-chloro-1,3-dimethyl-7H-purine-2,6-dione
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 470 g/mol |
2 | Physical appearance | Crystalline white powder |
3 | Melting point | 102-107oC |
4 | Solubility | Freely soluble in alcohol, soluble in water; insoluble in ether |
5 | Octanol/water partition coefficient | -0.39 |
6 | Presence of ring | Phenyl, purine |
7 | Number of chiral centers | Not present |
Structure activity of ethanolamine ethers can be summarized as:
i. Reaction of benzhydrylbromide and 2-dimethylaminoethanol produces diphenhydramine.
ii. Theophylline anhydrous is warmed up to 50-60oC and dissolved in water, drip N-chlorosuccimide to get a crude product. The product is then dissolved in 5% NaOH aqueous solution to get Chlorotheophyline. [2]
Dimenhydrinate is used for treatment of:
Side effects of dimenhydrinate are:
Q.1 Dimenhydrinate is the mixture of?
a) Diphenhydramine and Epinephrine
b) Xylometazoline and Bicalutamide
c) Diphenhydramine and 8-chlorotheophylline
d) 8-chlorotheophylline and brompheniramine
Q.2 Which amongst the following statements is/are incorrect related to the SAR of ethanolamine ethers antihistamine drugs?
I. 8-chlorotheophyllinate salt of diphenhydramine is used for treatment of motion sickness
II. Compounds with p-Cl-Ph and 2-pyridyl aryl groups are carboxamine, which is a potent anti-histamine drug.
III. Substitution of the methyl group at the carbon alpha to the ether function gives a related compound known as doxylamine.
IV. An additional carbon atom between oxygen and nitrogen produces clemastine which has higher sedative properties.
a) I, II
b) II, IV
c) I, II, IV
d) IV
Q.3 Type of rings present in the structure of dimenhydrinate?
I. Pyridine
II. Purine
III. Phenyl
IV. Pyrimidine
a) II, III
b) I, IV
c) I, III
d) II, IV
Q.4 Side effects of drug dimenhydrinate is/are?
a) Asthma
b) Heart diseases
c) Enlarged prostate
d) All of the above
Q.5 Match the following drugs with their correct melting point-
i. Dimenhydrinate | A. 211.5oC |
ii. Epinephrine | B. 181.21oC |
iii. Pyridostigmine | C. 282.22oC |
iv. Niflumic acid | D. 102-107oC |
a. i-A, ii-D, iii-C, iv-B
b. i-D, ii-A, iii-B, iv-C
c. i-C, ii-B, iii-A, iv-D
d. i-B, ii-C, iii-A, iv-D
Q.6 An example of drug from class ethanolamine ether antihistamines is?
a) Dimenhydrinate
b) Dobutamine
c) Ethosuximide
d) All of the above
Q.7 Dimenhydrinate is used for the treatment of?
a) Nausea
b) Vomiting
c) Dizziness
d) All of the above
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1-c
2-d
3-a
4-d
5-b
6-a
7-d
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