| Stereochemistry | ACHIRAL |
| Molecular Formula | C7H7ClN4O2 |
| Molecular Weight | 214.609 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(NC(Cl)=N2)C(=O)N(C)C1=O
InChI
InChIKey=RYIGNEOBDRVTHA-UHFFFAOYSA-N
InChI=1S/C7H7ClN4O2/c1-11-4-3(9-6(8)10-4)5(13)12(2)7(11)14/h1-2H3,(H,9,10)
| Molecular Formula | C7H7ClN4O2 |
| Molecular Weight | 214.609 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Chlorotheophylline (8-Chlorotheophylline) is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. Its main use is in combination with Diphenhydramine as the antiemetic drug Dimenhydrinate (marketed as Draminate, Dramamine, Detensor and Gravol among others). Dimenhydrinate is primarily used to treat nausea, vomiting, and dizziness caused by motion sickness.The stimulant properties of 8-chlorotheophylline are thought to ward off the drowsiness caused by diphenhydramine's anti-histamine activity in the central nervous system. 8-chlorotheophylline produces a number of effects including nervousness, restlessness, insomnia, headache, and nausea, which are primarily attributed to its ability to block the adenosine receptor. Because adenosine causes a decrease in neuronal firing, blockade of the adenosine receptor causes the reverse effect resulting in excitation.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Dimenhydrinate in the injectable form is indicated when the oral form is impractical.
Adults
Nausea or vomiting may be expected to be controlled for approximately 4 hours with 50 mg, and prevented by a similar dose every 4 hours. Its administration may be attended by some degree of drowsiness in some patients, and 100 mg every 4 hours may be given in conditions in which drowsiness is not objectionable or is even desirable.
For intramuscular administration, each milliliter (50 mg) of solution is injected as needed, but for intravenous administration, each milliliter (50 mg) of solution must be diluted in 10 mL of 0.9% Sodium Chloride Injection, USP and injected over a period of 2 minutes.
Pediatric
For intramuscular administration, 1.25 mg/kg of body weight or 37.5 mg/m2 of body surface area is administered four times daily. The maximum dose should not exceed 300 mg daily
Route of Administration:
Oral
The direct influence of sodium-8-chlorotheophyllinate (S8CT) on lymphocytes in vitro was
examined by measuring their transformation rate (3H-thimidine
uptake) and acid phosphatase activity. An enhanced transformation was only seen with B-lymphocytes showing a transformation index of 1.21 at concentrations of 10 and 100 ug S8CT per ml.
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