Diphenoxalate
Brand names,
Diphenoxalate
Analogs
Diphenoxalate
Brand Names Mixture
- Lomotil (Atropine Sulfate + Diphenoxylate Hcl)
Diphenoxalate
Chemical_Formula
C30H32N2O2
Diphenoxalate
RX_link
http://www.rxlist.com/cgi/generic3/diphenoxylate.htm
Diphenoxalate
fda sheet
Diphenoxalate
msds (material safety sheet)
Diphenoxalate
Synthesis Reference
Janssen, U.S. pat. 2,898,340 (1959)
Diphenoxalate
Molecular Weight
452.587 g/mol
Diphenoxalate
Melting Point
221 oC
Diphenoxalate
H2O Solubility
0.8 mg/ml
Diphenoxalate
State
Solid
Diphenoxalate
LogP
7.385
Diphenoxalate
Dosage Forms
Oral solution; Tablet
Diphenoxalate
Indication
For as adjunctive therapy in the management of diarrhea
Diphenoxalate
Pharmacology
Diphenoxylate, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Diphenoxylate is rapidly and extensively metabolized in man by ester hydrolysis to diphenoxylic acid (difenoxine), which is biologically active and the major metabolite in the blood.
Diphenoxalate
Absorption
90%
Diphenoxalate
side effects and Toxicity
Coma, dry skin and mucous membranes, enlarged pupils of the eyes, extremely high body temperature, flushing, involuntary eyeball movement, lower than normal muscle tone, pinpoint pupils, rapid heartbeat, restlessness, sluggishness, suppressed breathing
Diphenoxalate
Patient Information
INFORM THE PATIENT (PARENT OR GUARDIAN) NOT TO EXCEED THE RECOMMENDED DOSAGE AND TO KEEP DIPHEN-OXYLATE HCL AND
ATROPINE SULFATE OUT OF THE REACH OF CHILDREN AND IN A CHILD-RESISTANT CONTAINER, INFORM THE PATIENT OF THE
CONSEQUENCES OF OVERDOSAGE, INCLUDING SEVERE RESPIRATORY DEPRESSION AND COMA, POSSIBLY LEADING TO PERMANENT BRAIN
DAMAGE OR DEATH.
Diphenoxylate HCl and atropine sulfate may produce drowsiness or dizziness. The patient should be cautioned
regarding activities requiring mental alertness, such as driving or operati ng dangerous machinery. Potentiation of
the action of alcohol, barbiturates and tranquilizers with concomitant use of diphenoxylate HCl and atropine sulfate
should be explained to the patient. The physician should also provide the patient with other information in this
labeling, as appropriate.
Diphenoxalate
Organisms Affected
Humans and other mammals